ABACAVIR (Antiretroviral (Nucleoside Analogue))
Abacavir is a nucleoside reverse transcriptase inhibitor (NRTI) and is used to treat HIV infection in combination with other antiretroviral drugs. Side effects include hypersensitivity reactions, gastrointestinal disturbances, fever and headache.
Metabolised by alcohol dehydrogenase and glucuronyl transferase.
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ACICLOVIR (Antiviral)
Aciclovir can be used to treat herpes simplex and varicella-zoster (chickenpox-shingles). Also used for prophylaxis and for treatment in the immunocompromised. Side effects include gastrointestinal disturbances, rashes, dizziness, headache, increase in liver enzymes, hallucinations and tremors.
Metabolised by non-CYP enzymes but mainly excreted unchanged in the urine.
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ADEFOVIR (Antiviral)
Adefovir is part of a drug class called nucleotide analogues. It inhibits reverse transcriptase. It is an experimental anti-HIV drug and can be used to treat Hepatitis B. Side effects include kidney abnormalities, tinnitus, nausea and vomiting.
Given as a prodrug adefovir dipivoxil. Excreted mainly unchanged.
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ADHERANCE
Taking the medication exactly as prescribed.
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AGRANULOCYTOSIS
A type of blood disorder. Loss or low number of white blood cells.
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AIDS
Acquired Immune Deficiency Syndrome.
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ALCOHOL (Illicit/Recreational)
Alcohol (ethyl alcohol, ethanol) is a sedative hypnotic consumed as a social drug. Judged on a molar basis, the consumption of alcohol far exceeds that of any other drug. Alcohol acts as a general CNS depressant, but also affects the cardiovascular, hepatic and endocrine systems.
Metabolised by alcohol dehydrogenase, CYP2E1 and CYP1A2. An inducer of CYP2E1.
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ALLERGIC RHINITIS
Allergic reaction/inflammation of the nose giving hay fever-like symptoms. Seasonal rhinitis is known as hay fever.
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ALPHA-LIPOIC (THIOCTIC) ACID (Herbal remedy)
Used to treat non-insulin dependent diabetes and usually given with glibenclamide and acarbose, they do not interact with each other. It is also an antioxidant and therefore enhances glutathione levels. It can be used in the treatment of HIV as an antioxidant and may also interfere with the process of viral activation and CD4 cell death.
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ALPRAZOLAM (Anxiolytics/Hypnotics/Sedative)
Alprazolam a is long–acting benzodiazepine and is used, in the short term to treat anxiety. Side effects include drowsiness and light-headedness, headache, rashes, increase in aggression, blood disorders and CNS effects and dependence.
Metabolised by CYP3A.
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AMENORRHOEA
Irregular menstrual cycle/bleeding.
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AMIODARONE (Antiarrhythmic)
A class III antiarrhythmic used to treat paroxysmal and supraventricular, nodal and ventricular tachycardias, atrial fibrillation and ventricular fibrillation. Use if other drugs are ineffective or contraindicated. Wide range of side effects include reversible corneal microdeposits, peripheral neuropathy, bradycardia and conduction disturbances, phototoxicity, hypothyroidism and hyperthyroidism have been reported. Liver disorders and hypersensitivity reactions may occur in susceptible individuals.
Metabolised by CYP3A.
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AMITRIPTYLINE (Antidepressant)
Amitriptyline is a tricyclic antidepressant drug, the complete mechanism of action is not fully understood but it blocks the re-uptake of noradrenaline and serotonin, therefore prolonging their effects. Used to treat depression, particularly when sedation is required and nocturnal enuresis in children. There are a wide range of side effects including sedation, dry mouth, blurred vision, constipation, nausea, cardiovascular side effects such as arrhythmias, hypersensitivity reactions, endocrine and behavioural side effects and blood disorders.
Metabolised by CYP3A, CYP2D6 and CYP2C19 and glucuronyl transferase.
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AMLODIPINE (Calcium Channel Antagonists)
Used to treat hypertension and for the prophylaxis of angina. It is long-acting and can be given once daily. Side effects include headache and flushing, rashes, palpitations, drowsiness.
Metabolised by CYP3A.
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AMPHOTERICIN B (Antifungal)
Used to treat many fungal infections, as it is active against most fungi and yeast, including intestinal candidiasis, oral and perioral infections, systemic fungal infections, severe or deep mycoses. Side effects include nausea and vomiting, anorexia, diarrhoea, renal and cardiovascular toxicity, liver dysfunction, rash, blood disorders and anaphylaxis.
Enzymes for metabolism are not known but about 40% excreted unchanged in urine.
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AMPRENAVIR (Antiretroviral (Protease Inhibitor))
Amprenavir is a protease inhibitor (PI) and is used in the treatment of HIV infection in combination with other antiretroviral drugs. Side effects may include nausea and vomiting, diarrhoea, headache, insomnia and blood disorders and elevated liver enzymes and abnormal fat accumulation (lipodystrophy).
Metabolised by CYP3A4 and glucuronyl transferase as a minor route. A weak inhibitor of CYP3A4.
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ANAEMIA
A type of blood disorder. Loss or low number of red blood cells.
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ANALGESIC
'Pain-killer'; substance taken to relieve pain.
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ANAPHYLAXIS
Type of hypersensitivity reaction, which occurs the second time the patient is exposed to the substance they are sensitive to.
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ANGIOEDEMA
Swelling of blood vessels.
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ANTIRETROVIRAL
A drug used to treat a retrovirus such as HIV.
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ARRHYTHMIA
Abnormal heart rhythm.
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ART
Antiretroviral therapy.
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ASPIRIN (Acetylsalicylic acid) (Analgesic)
A non-steroidal anti-inflammatory drug (NSAID), antiplatelet, antipyretic. Used to treat headaches, musculoskeletal pain, dysmenorrhoea and pyrexia (fever). Side effects can include gastrointestinal irritation and in hypersensitive patients can cause rash and bronchospasm.
Metabolised by glycine conjugase, glucuronyl transferase, CYP2C9.
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ASTEMIZOLE (Antihistamine)
Astermizole is an antagonist at H1 receptors and is used to treat symptoms of allergies such as hay fever and conjunctivitis and allergic skin reactions such as urticaria. Side effects may include antimuscarinic effects such as dry mouth, blurred vision, gastrointestinal disturbances, and it has low CNS effects therefore it produces only slight sedation.
Metabolised by CYP3A4.
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ASTHENIA
Weakness or loss of strength.
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ATAXIA
Incoordination of movement.
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ATENOLOL (Beta-blocker)
Atenolol is a β1 selective antagonist and is used for the treatment of hypertension, angina and arrhythmias. Side effects include heart failure, bradycardia, hypotension, bronchospasm, peripheral vasoconstriction and gastrointestinal disturbances. Reduce the dose in renal impairment.
Excreted mainly unchanged in the urine.
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ATORVASTATIN (Lipid Lowering)
Atorvastatin is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitor, which is involved in cholesterol synthesis. It is used to treat primary hypercholesterolaemia, heterozygous and homozygous familial hypercholesterolaemia or combined hypercholesterolaemia. Side effects include nausea and vomiting, abdominal pain, headache, angioedema, anorexia and alopecia.
Metabolised by CYP3A4.
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ATOVAQUONE (Antiprotozoal)
Atovaquone can be used to treat acute, uncomplicated Plasmodium falciparum malaria where there is resistance to other antimalarials. Also used for the treatment of Pneumocystis carinii pneumonia in those patients intolerant to co-trimoxazole. Side effects include nausea and vomiting, rash, fever, diarrhoea, elevated liver enzymes.
Metabolised by glucuronyl transferase but about 94% excreted unchanged in faeces and less than 1% in urine.
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AUC
Area under the curve. Gives an indication of total concentration of drug in the body.
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AZITHROMYCIN (Antibacterial)
A macrolide antibiotic used to treat upper and lower infections of the respiratory tract; otitis media, skin and soft tissue infections and uncomplicated genital infections caused by Clamydia trachomatis. Side effects include dizziness, headache, nausea and vomiting, anorexia, dyspepsia, photosensitivity, hepatitis, convulsions, mild neutropenia. Rarely it causes tinnitus, hepatic failure, hepatic necrosis, Stevens-Johnson syndrome, toxic epidermal necrolysis, taste disturbances.
Metabolised by CYP3A but excreted mainly unchanged in bile.
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BEE PROPOLIS (Herbal remedy)
This is used by bees to make their hive and is used as a dietary supplement. It has been shown to have antibacterial, antifungal, antiviral and antitumour properties. It may also help difficult wounds to heal. Few side effects reported but can cause allergic effects.
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BEPRIDIL (Antiarrhythmic)
Used to treat supraventricular arrhythmias and atrial fibrillation and can be used to treat angina. Side effects include nausea and dizziness. Also this drug has the ability to prolong the action potential and the QT interval, therefore there is the risk of torsade de pointes.
Metabolised by CYP3A.
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BISOPROLOL (Beta-blocker)
Bisoprolol is a potent, highly beta-1 selective blocker and is used in the management of hypertension and angina pectoris.
Bisoprolol is eliminated equally by renal and non-renal pathways, with ~50% of the dose appearing unchanged in the urine and the remainder as inactive metabolites. Bisoprolol is not metabolised by CYP2D6.
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BRADYCARDIA
Abnormally slow heart rhythm.
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BRONCHOSPASM
Airways go into spasm and constrict therefore narrowing and making it difficult to breathe.
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BUPRENORPHINE (Analgesics)
Buprenorphine is an opioid partial agonist/antagonist which attaches itself to the mu and kappa receptors of the brain. It is used as substitution treatment for opioid drug dependence. Its activity in opioid maintenance treatment is attributed to its slowly reversible link with the mu receptors which, over a prolonged period, minimises the need of the addicted patient for drugs.
Buprenorphine is oxidatively metabolised by 14-N-dealkylation to N-desalkyl-buprenorphine (also known as norbuprenorphine) via CYP3A4 and by glucuroconjugation of the parent molecule and the dealkylated metabolite. Norbuprenorphine is a mu agonist with weak intrinsic activity.
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BUPROPION (Antidepressant)
Bupropion is a heterocyclic, second-generation antidepressant. It is a noradrenaline and dopamine re-uptake inhibitor. It is used to treat depression. It is also used to help give up smoking as the drug ZybanÒ. Side effects include gastrointestinal disturbances, dry mouth, insomnia, hypersensitivity reactions, headache and dizziness, depression and cardiac effects.
Metabolised by CYP2B6 and other CYPs. An inhibitor of CYP2D6.
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Cmax
Maximum drug concentration in the plasma.
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CALENDULA (Herbal remedy)
Calendula (Calendula officinalis) contains saporins and can be useful for buccal membrane irritation, for example mouth ulcers and for other dermatological purposes. Side effects may include slight haemolysis, but it does not appear to cause any local irritation where applied.
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CANDIDIASIS
A fungal infection caused by Candida albicans that infects the linings of the body such as the mouth and vagina. It is also commonly known as thrush.
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CARBAMAZEPINE (Anticonvulsant)
Used to treat simple and complex partial seizures and tonic-clonic seizures. Also used for prophylaxis of manic-depressive psychosis that is unresponsive to lithium and for trigeminal neuralgia. Side effects include nausea and vomiting, headache, drowsiness, dizziness, visual disturbances, constipation or diarrhoea, blood disorders, Stevens-Johnson syndrome and toxic epidermal necrolysis.
Metabolised by CYP 3A and CYP2C8/9 as a minor route. An inducer of CYP3A and glucuronyl transferase and induces its own metabolism.
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CARDIOTOXICITY
Toxic damage to or poisoning of the heart due to a drug.
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CARVEDILOL (Beta-blocker)
Carvedilol is a vasodilating non-selective beta blocker with antioxidant properties. It is used in the management of symptomatic chronic heart failure, hypertension and angina.
Carvedilol undergoes extensive metabolism with glucuronidation and P450-mediated metabolism as the major steps. Cytochromes CYP2D6 and CYP2C9 are the major enzymes responsible for metabolism, with CYP3A4, CYP2C19, CYP1A2 and CYP2E1 having a lesser role.
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CASPOFUNGIN (Antifungals)
Caspofungin is the first of a new class of antifungal drugs (glucan synthesis inhibitors) that act by inhibiting the synthesis of beta (1,3)-D-glucan, a integral component of the fungal cell wall. It is indicated for treatment of invasive candidiasis in non-neutropaenic patients and the treatment of invasive aspergilliosis in adult patients who are refractory to or intolerant of amphotericin B and/or itraconzole.
In vitro studies have shown that caspofungin is not an inhibitor of CYP1A2, 2A6, 2C9, 2D6 or 3A4. In clinical studies it did not induce or inhibit CYP3A4 metabolism of other compounds. It is not a substrate for P-glycoprotein and is a poor substrate for CYP450 enzymes.
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CAT'S CLAW (Herbal remedy)
Cat's Claw (Uncaria tomntosa) or una de gato' is used in Peruvian medicine for stomach complaints and arthritis. It contains pentacyclic oxindole alkaloids, which appear to stimulate endothelial cells in vitro to produce a lymphocyte-proliferation-regulating-factor increasing the number of white blood cells. It also prevents NFκB activation therefore it has anti-inflammatory action. It also causes the induction of apoptosis and so may have a use as an antitumour treatment.
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CD4
A type of molecule on cells of the immune system known as CD4 cells that the HIV virus can bind to. The CD4 cell count can give an idea of the state of the immune system.
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CERIVASTATIN (Lipid Lowering)
Cerivastatin is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitor, which is involved in cholesterol synthesis. It is used to treat primary hypercholesterolaemia (types IIa and IIb) in those patients not responding to dietary control. Side effects include nausea and vomiting, abdominal pain, headache, flu-like symptoms, back pain and insomnia.
Metabolised by CYP3A4 and CYP2C8.
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CETIRIZINE (Antihistamine)
Used to treat symptoms of allergies such as hay fever and urticaria. Side effects include antimuscarinic effects such as dry mouth, blurred vision, gastrointestinal disturbances, however these effects are low, as is any sedation effect. Other side effects may include hypersensitivity and photosensitivity reactions, sweating, convulsions and blood disorders and liver dysfunction.
Metabolised by CYP enzymes but excreted mainly unchanged in the urine.
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CHLOROQUINE (Antiprotozoal)
Used for prophylaxis and treatment of malaria, although not recommended for the treatment of falciparum malaria due to a high degree of resistance. Also used to treat rheumatoid arthritis and lupus erythematosus. Side effects include gastrointestinal disturbances, headache.
Metabolised by CYP3A4 but mostly excreted unchanged in the urine. An inhibitor of CYP2D6.
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CHLORPROMAZINE (Antipsychotic/Neuroleptic)
Chlorpromazine is a phenothiazine, used to treat CNS disorders in particular when sedation is required, schizophrenia, mania, hypomania and hiccups and also for the induction of hypothermia. There are a vast number of side effects and these include extrapyramidal effects, drowsiness, nightmares, insomnia, cardiovascular effects and antimuscarinic effects.
Metabolised by CYP2D6 and possibly CYP1A2 and glucuronyl transferase.
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CICLOSPORIN (Immunosuppressants)
Used as an immunosuppressant, in particular after organ transplants or for the prevention of graft rejection after bone marrow, liver, kidney, pancreas, heart and lung transplants. Also it is used to treat atopic dermatitis and psoriasis and rheumatoid arthritis. Side effects include muscle weakness, cramps, headache, rash, liver dysfunction. It is also nephrotoxic.
Metabolised by CYP3A. A weak inhibitor of P-glycoprotein.
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CIDOFOVIR (Antiviral)
Cidofovir is a DNA polymerase chain inhibitor. It is used in combination with probenecid to treat cytomegalovirus retinitis in AIDS patients where other drugs are contraindicated. Side effects include nephrotoxicity, which is dose-related, neutropenia, nausea and alopecia.
Mostly excreted unchanged.
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CIMETIDINE (Gastrointestinal Agents)
Cimetidine is an antagonist at H2 receptors and is used in the treatment of gastric and duodenal ulcers and stomal ulcers, reflux oesophagitis and Zollinger-Ellison syndrome. Side effects include gastrointestinal disturbances, dizziness and headache, tiredness, rash, cardiac effects and blood disorders and hypersensitivity reactions.
Metabolised by CYP enzymes. An inhibitor of several CYP enzymes.
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CINCHONISM
A toxic state that usually occurs when plasma levels of quinine exceed 7–10 µg/ml. Symptoms include headache, dizziness, nausea, visual disturbances and tinnitus.
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CIPROFLOXACIN (Antibacterial)
A quinolone antibiotic and is a DNA gyrase inhibitor effective against both Gram positive and Gram negative bacteria but in particular Gram negative bacteria. Used to treat respiratory tract and urinary tract infections and infections of the gastrointestinal tract, gonorrhoea. It is not the first line of treatment for pneumococcal pneumonia. Side effects include nausea and vomiting, abdominal pain and diarrhoea, blood disorders, hypersensitivity reactions, tremor, jaundice and hepatitis with necrolysis, renal failure, tinnitus, drowsiness, confusion, convulsions.
Metabolised by CYP and sulphatase. An inhibitor of CYP1A2.
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CISAPRIDE (Gastrointestinal Agents)
Cisapride is a motility stimulant and it thought to work by promoting the release of acetylcholine (ACh) in the gut wall. It is used to treat gastro-oesophageal reflux disease, impaired gastric motility and the symptoms of dyspepsia. Side effects include abdominal cramps and diarrhoea, headache, extrapyramidal effects and hypersensitivity reactions.
Metabolised by CYP3A.
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CITALOPRAM (Antidepressants)
Citalopram is indicated in the treatment of depressive illness in the initial phase and as maintenance against potential relapse/recurrence. It is also indicated in the treatment of panic disorder with or without agoraphobia.
Metabolism of citalopram is mediated by CYP 2C19, CYP3A and CYP2D6. It is a weak inhibitor of CYP1A2 and CYP 2D6 and had minimal or no inhibitory effect on CYP2C9, CYP2C19, CYP2E1 and CYP3A4.
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CLARITHROMYCIN (Antibacterial)
A macrolide antibiotic used to treat upper and lower respiratory tract infections, skin and soft tissue infections, acute otitis media. Side effects include gastrointestinal disturbances, headache, and nausea and vomiting, CNS effects, taste disturbances, hypersensitivity reactions, renal dysfunction, prolonged QT interval.
Metabolised by CYP3A. An inhibitor of CYP3A and possibly CYP1A2.
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CLINDAMYCIN (Antibacterial)
Used to treat staphylococcal bone and joint infections, peritonitis, and prophylaxis of endocarditis. Side effects include diarrhoea (if this occurs discontinue use), abdominal discomfort, antibiotic-associated colitis, nausea and vomiting, rash, thrombocytopenia, neutropenia, eosinophilia, agranulocytosis.
Metabolised by CYP enzymes.
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CLOFIBRATE (Lipid Lowering)
Clofibrate is part of a class of drugs known as fibrates, they lower serum triglycerides and also decrease LDL-cholesterol and increase HDL-cholesterol. It is used to treat hyperlipidaemia types IIa, IIb, III, VI and V where patients have not responded to other measures such as dietary control. Side effects include nausea, anorexia, impotence, headache, dizziness and vertigo.
Metabolised by esterase to the active metabolite CPIB.
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CLONAZEPAM (Anticonvulsant)
Can be used to treat all forms of epilepsy especially myoclonus seizures. Also used to treat status epilepticus. Side effects include drowsiness, dizziness, co-ordination disturbances, fatigue, irritability and mental changes.
Metabolised by nitroreductase and possibly CYP3A.
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CLOPIDOGREL (Anti-platelet and Anticoagulant)
Clopidogrel is a platelet aggregation inhibitor and is indicated for the prevention of atherothrombotic events.
Clopidogrel is a prodrug and is active through a thiol derivative which is formed by the metabolism by CYP2B6 and 3A4 (and to a lesser extent CYP1A1, CYP1A2 and CYP2C19).
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CLORAZEPATE (Anxiolytics/Hypnotics/Sedative)
Clorazepate is a long-acting benzodiazepine and is used, in the short term to treat anxiety. Side effects are as alprazolam and so include drowsiness and light-headedness, headache, rashes, increase in aggression, blood disorders and CNS effects and dependence.
Metabolised by acid hydrolysis to nordiazepam in the gastrointestinal tract.
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CLOZAPINE (Antipsychotic/Neuroleptic)
Clozapine is an atypical antipsychotic and has less extrapyramidal effects than typical antipsychotics. Used to treat schizophrenia in patients that are resistant to or unresponsive to conventional antipsychotic drugs. Side effects include neutropenia and agranulocytosis, fever, drowsiness, confusion, antimuscarinic effects, nausea and vomiting.
Metabolised by CYP1A2 and CYP2D6 and CYP3A to a minor extent and glucuronyl transferase.
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CNS
Central nervous system.
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COLITIS
Inflammation of the colon.
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CONTRAINDICATED
Drugs that should not be taken together, either to treat the same illness or two separate illnesses.
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CROSS-RESISTANCE
The development of resistance to more than one drug in a drug class. For example, if a patient is resistant to one NNRTI they are likely to become resistant to other NNRTIs.
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CYCLOPHOSPHAMIDE (Antineoplastic)
Cyclophosphamide is a cytotoxic drug. It is an alkylating agent, which acts by damaging DNA and thus interfering with DNA replication. Used to treat chronic lymphatic leukaemia, lymphomas and solid tumours. It is activated by metabolism in the liver to the active alkylating agent. Side effects are common and may include nausea and vomiting, myelosuppression, alopecia, risk of cystitis and interference with gametogenesis.
Metabolised by CYP3A, CYP2C19 and CYP2B. Induces its own metabolism.
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CYCLOSPORINE (Immunosuppressant)
See ciclosporin
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CYP
Cytochrome P450. A family of enzymes mainly in the liver and responsible for steroid synthesis and also the metabolism of many drugs. Examples include CYP3A4, CYP2D6 and CYP2C9.
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CYTOCHROME P450
A family of enzymes mainly in the liver and responsible for steroid synthesis and also the metabolism of many drugs. Examples include CYP3A4, CYP2D6 and CYP2C9.
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CYTOMEGALOVIRUS (CMV)
A form of herpes virus, that causes damage to the retina (back of the eye) and other parts of the body in those people with a poor immune system.
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CYTOTOXIC
Toxic or poisonous to cells.
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DANSHEN (Herbal remedy)
Danshen (Salvia miltiorrhiza) is used in Mainland China to treat atherosclerosis-related diseases and used to treat menstrual disorders, angina pectoris, and circulatory system disorders. It is thought to cause vasodilation, promote blood flow and relieve pain and inflammation. Use should be avoided in patients taking warfarin because it inhibits platelet aggregation and increases the bioavailability of warfarin and may cause an exaggerated effect leading to over anticoagulation.
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DAPSONE (Antibacterial)
A sulphone used to treat leprosy, dermatitis herpetiformis and malaria. Side effects include nausea and vomiting, headache, insomnia, blood disorders, hypersensitivity reactions. Side effects are dose related.
Metabolised by N-acetyl transferase, CYP3A, CYP2E1 and glucuronyl transferase.
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DELAVIRDINE (Antiretroviral (NNRTI))
Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used to treat HIV infection. It is not licensed in Europe but is in the USA. Side effects include mainly a rash, but also may cause nausea, diarrhoea, headache and fatigue and reversible liver abnormalities.
Metabolised by CYP3A and possibly CYP2D6. An inhibitor of CYP3A and its own metabolism and inhibits CYP2C9 and CYP2C19.
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DESIPRAMINE (Antidepressant)
Desipramine is a tricyclic antidepressant drug and is the active metabolite of imipramine. It is used to treat depression and nocturnal enuresis in children. There are a wide range of side effects including sedation (this is less than amitriptyline), dry mouth, blurred vision, constipation, nausea, cardiovascular side effects such as arrhythmias, hypersensitivity reactions, endocrine and behavioural side effects and blood disorders.
Metabolised by CYP2D6 and glucuronyl transferase and sulphotransferase.
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DEXAMETHASONE (Steroids)
Used for suppression of inflammatory and allergic reactions, to treat congenital and adrenal hyperplasia, cerebral oedema and rheumatic disease. Used to diagnose Cushing's disease and to prevent nausea and vomiting from chemotherapy. Side effects include gastrointestinal disturbances, musculoskeletal and endocrine effects and also neuropsychiatric and ophthalmic effects.
Metabolised by CYP3A. An inducer of CYP3A.
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DEXTROPROPOXYPHENE (Propoxyphene) (Analgesic)
An opioid analgesic used to treat moderate to severe pain. Alone it is a very mild analgesic but if given with aspirin or paracetamol the analgesic effect is greater than with aspirin or paracetamol alone.
Extensively metabolised by CYP1A2. An inhibitor of CYP2D6.
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DIAMORPHINE (Analgesic)
An opioid analgesic, also known as heroin, and a very powerful analgesic. Side effects can include nausea and vomiting, drowsiness, constipation, headache, sweating, dry mouth, postural hypotension, dependence and in higher doses, respiratory depression. It causes less nausea and hypotension than morphine.
Metabolised by deacetylase.
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DIAZEPAM (Anxiolytics/Hypnotics/Sedative)
Diazepam is a long-acting benzodiazepine and is used, in the short term to treat anxiety or insomnia and also used as an adjunct in alcohol withdrawal. Side effects include drowsiness and light-headedness, headache, rashes, increase in aggression, blood disorders and CNS effects and dependence.
Metabolised by CYP2C19 and CYP3A.
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DIDANOSINE (DDI) (Antiretroviral (Nucleoside Analogue))
Didanosine is a nucleoside reverse transcriptase inhibitor (NRTI) and is used to treat HIV infection in combination with other antiretroviral drugs. Side effects include hypersensitivity reactions, nausea, vomiting, diarrhoea, and pancreatitis and peripheral neuropathy.
Metabolised by xanthine oxidase but a significant proportion is excreted unchanged in urine.
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DIHYDROERGOTAMINE (Antimigraine)
Used to treat acute migraine with or without aura. Side effects may include nausea and vomiting, vertigo, abdominal pain and occasionally increased headache can occur. Reported incidences of myocardial ischaemia but rarely myocardial infarction. With excessive use ergotism, pleural and peritoneal fibrosis may occur.
Metabolised by CYP3A.
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DILTIAZEM (Calcium Channel Agonist)
Diltiazem is a calcium antagonist and is indicated for the prophylaxis and treatment of angina pectoris.
Diltiazem is extensively metabolised in the liver by CYP3A4 and CYP2D6.
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DISOPYRAMIDE (Antiarrhythmic)
A class I antiarrhythmic used to treat ventricular arrhythmias, especially after myocardial infarction and supraventricular arrhythmias. Side effects include ventricular tachycardia, ventricular fibrillation, torsade de pointes, hypotension, AV block. This drug has antimuscarinic effects therefore other side effects include dry mouth, blurred vision, gastrointestinal disturbances, urinary retention.
Metabolised by CYP3A.
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DOMPERIDONE (Gastrointestinal Agents)
Domperidone is a dopamine antagonist and is also a motility stimulant and stimulates gastric emptying. It is used to treat nausea and vomiting and functional dyspepsia. Side effects include allergic reactions, rashes and reduced libido and increased prolactin levels.
Metabolised by CYP3A4, CYP1A2 and CYP2E1.
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DOXEPIN (Antidepressant)
Doxepin is indicated in depressive illness, especially where sedation is required.
Doxepin is metabolised by CYP2D6.
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DOXORUBICIN (Antineoplastic)
Doxorubicin is a cytotoxic anthracycline antibiotic used to treat acute leukaemias, lymphomas and solid tumours. Side effects may include nausea and vomiting, alopecia, myelosuppression and cardiotoxicity.
Metabolised by aldoketoreductase and CYP reductase.
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DRONABINOL (Gastrointestinal Agents)
Used as an antiemetic to prevent nausea and vomiting. Also used in the USA as an appetite stimulant in patients with AIDS-related wasting.
Metabolised by CYP2C9 and CYP3A.
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DYSMENORRHOEA
Painful periods/menses.
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DYSPEPSIA
Indigestion.
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ECHINACEA (Herbal remedy)
Echinacea (Echinacea purpurea and angustifolia) is used for the treatment of cold and flu and may have anti-infective and immunostimulation properties. Side effects are minimal but may include unpleasant taste and anaphylaxis. It is contraindicated in those with autoimmune disorders such as HIV and should not be taken by those with tuberculosis or collagenosis. Also it should not be taken with drugs that are likely to cause hepatotoxicity such as amiodarone, methotrexate and ketoconazole.
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EFAVIRENZ (Antiretroviral (NNRTI))
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used to treat HIV infection in combination with other antiretroviral drugs. Side effects include rash such as Stevens-Johnson syndrome, nausea, dizziness, strange dreams, CNS effects and raised liver enzymes.
Metabolised by CYP3A4 and CYP2B6. An inducer of CYP3A4.
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EMETOGENIC
Induce or cause nausea or vomiting.
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EMTRICITABINE (Antiretroviral (Nucleoside Analogue))
Emtricitabine is a synthetic nucleoside analogue of cytosine with activity that is specific to human immunodeficiency virus (HIV-1 and HIV-2) and hepatitis B virus (HBV). Emtricitabine is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate, which competitively inhibits HIV-1 reverse transcriptase, resulting in DNA chain termination. Emtricitabine is a weak inhibitor of mammalian DNA polymerase alpha, beta and epsilon and mitochondrial DNA polymerase gamma.
There is limited metabolism of emtricitabine. The biotransformation of emtricitabine includes oxidation of the thiol moiety to form the 3'-sulphoxide diastereomers (approximately 9% of dose) and conjugation with glucuronic acid to form 2'-O-glucuronide (approximately 4% of dose). In vitro, emtricitabine did not inhibit metabolism mediated by any of the following human CYP450 isoforms: 1A2, 2A6, 2B6, 2C9, 2C19, 2D6 and 3A4. Emtricitabine did not inhibit uridine-5'-diphosphoglucuronyl transferase, the enzyme responsible for glucuronidation.
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ENDOCARDITIS
Inflammation of the inner membrane of the heart.
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ENFLURANE (General Anaesthetic)
Enflurane is a volatile anaesthetic and can be used for both induction and maintenance of anaesthesia. Side effects include cardiorespiratory depression; it may cause hepatotoxicity in those patients sensitised to halothane. Care must be taken in patients with epilepsy.
Metabolised by CYP2E1.
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ENFUVIRTIDE (T20, Fuzeon) (Antiretrovirals (Fusion Inhibitors))
Enfuvirtide inhibits the binding of HIV to the cell and is used with other antiretroviral medicines in salvage therapy. It is administered by sub-cutaneous injection.
As a peptide, enfuvirtide is expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool. In vitro and in vivo studies have indicated that enfuvirtide is not an inhibitor of CYP450 enzymes.
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ENURESIS
Involuntary urination.
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ENZYME
A protein found in the body that can metabolise drugs.
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EOSINOPHILIA
A type of blood disorder. Loss or low number of white blood cells known as eosinophils.
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ERGOTAMINE (Antimigraine)
Used to treat acute migraine and migraine variants that are unresponsive to simple analgesics. Side effects are as for dihydroergotamine and so include nausea and vomiting, vertigo, abdominal pain and occasionally increased headache can occur. Reported incidences of myocardial ischaemia but rarely myocardial infarction. With excessive use ergotism, pleural and peritoneal fibrosis may occur.
Metabolised by CYP3A.
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ERYTHROMYCIN (Antibacterial)
A macrolide antibiotic used as an alternative to penicillin when hypersensitivity reactions occur. Used to treat infections such as respiratory infections, whooping cough, pneumonia, legionnaires' disease, syphilis, acne vulgaris and diphtheria prophylaxis. Side effects include nausea, vomiting, diarrhoea, rashes, allergic reactions, reversible hearing loss after high doses, cardiac effects.
Metabolised by CYP3A. An inhibitor of CY3A and P-glycoprotein and possibly CYP1A2.
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ESTAZOLAM (Anxiolytics/Hypnotics/Sedative)
Estazolam is a benzodiazepine and is used for sedation. Side effects may include drowsiness and light-headedness, headache, rashes, increase in aggression, blood disorders and CNS effects and dependence.
Metabolised by CYP, probably CYP3A.
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ETHAMBUTOL (Antibacterial)
Used to treat tuberculosis in combination with other drugs. Side effects include optic neuritis, peripheral neuritis, red/green colour blindness, rash, and thrombocytopenia.
Metabolised by alcohol and aldehyde dehyrogenases and CYP.
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ETHINYLESTRADIOL (Steroids)
Ethinylestradiol is a synthetic form of oestrogen. It is used in hormone replacement therapy (HRT) and in oral contraceptives in the form of the combined pill. It is also used in the treatment of acne and breast cancer. Side effects include nausea and vomiting, changes in weight, headache and dizziness.
Metabolised by glucuronyl transferase and sulphatase and CYP3A. An inhibitor of CYP1A2 and CYP3A.
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ETHOSUXIMIDE (Anticonvulsant)
Used to treat simple absence seizures. Side effects include gastrointestinal disturbances, blood disorders, rash, headache, dizziness and drowsiness and CNS effects such as sleep disturbances.
Metabolised by CYP3A.
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EUPHORIA
State of excitement; feeling of well-being.
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FAMCICLOVIR (Antiviral)
A pro-drug of penciclovir and is used to treat herpes zoster, genital herpes simplex and to prevent recurrence of genital herpes. Side effects include nausea and vomiting, dizziness, headache, hallucinations and rash.
Metabolised by deacetylase, aldehyde oxidase.
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FENOFIBRATE (Lipid Lowering)
Fenofibrate is part of a class of drugs known as fibrates, they lower serum triglycerides and also decrease LDL-cholesterol and increase HDL-cholesterol. It is used to treat hyperlipidaemia types IIa, IIb, III, VI and V where patients have not responded to other measures such as dietary control. Side effects include nausea, anorexia, impotence, headache, dizziness and vertigo.
Metabolised by hydrolysis.
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FENTANYL (Analgesic)
An opioid analgesic used to treat chronic pain and used during surgical procedures. Can be given by injection or self-adhesive patch. Side effects as with other opioid analgesics such as, nausea and vomiting, constipation, headache, dependence. Also rashes and itching have been reported.
Metabolised by CYP3A.
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FEVERFEW (Herbal remedy)
Feverfew (Tenacetum parthenium) is mainly used for the treatment and prophylaxis of migraine and the treatment of rheumatoid arthritis. It contains a substance called parthenolide which acts as a serotonin antagonist; it also inhibits serotonin and leukotriene release. It interacts with anticoagulants and has the potential to cause an additive effect with warfarin. It also should not be taken with other antimigraine drugs or aspirin and it may cause allergic reactions.
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FLECAINIDE (Antiarrhythmic)
A class I antiarrhythmic. The tablet form is used to treat symptomatic sustained ventricular tachycardia, non-sustained ventricular tachycardia and premature ventricular contractions. Injection form used to treat ventricular tachyarrhythmias where other treatment is ineffective. Side effects can include visual disturbances and dizziness, proarrhythmic effect (i.e. causes arrhythmias). Can cause nausea and vomiting, skin rash, depression, hallucinations, convulsions, and dyskinesia.
Metabolised by CYP2D6.
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FLUCONAZOLE (Antifungal)
Used to treat many fungal infections including invasive candidal infections, to prevent relapse of cryptococcal meningitis in AIDS patients and for prophylaxis in immunocompromised patients after cytotoxic chemotherapy or radiotherapy. Side effects include nausea, diarrhoea and flatulence, headache, rash, anaphylaxis, toxic epidermal necrolysis and Steven-Johnson syndrome, severe cutaneous reactions in AIDS patients.
Metabolised by CYP3A4 but about 80% excreted unchanged in urine. An inhibitor of CYP2C9 and CYP2C19 and a weak inhibitor of CYP3A.
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FLUCYTOSINE (Antifungal)
Used to treat systemic fungal and yeast infections and as an adjunct to amphotericin. Side effects include nausea and vomiting, diarrhoea, rashes, convulsions, hallucinations, confusion, blood disorders.
Metabolised by cytosine deaminase but about 99% excreted unchanged in the urine.
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FLUOXETINE (Antidepressant)
Fluoxetine (ProzacÒ) is a selective serotonin re-uptake inhibitor (SSRI), and selectively inhibits the re-uptake of serotonin (5-HT) into nerve terminals. Used to treat depression, bulimia nervosa and obsessive compulsive disorder. Side effects include gastrointestinal disturbances, insomnia, dizziness and drowsiness, rash, allergic reactions, hypomania, mania and convulsions.
Metabolised by CYP2D6, 2C9 and other CYP. An inhibitor of CYP2D6, CYP3A and CYP2C19.
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FLURAZEPAM (Anxiolytics/Hypnotics/Sedative)
Flurazepam is a long-acting benzodiazepine and is used as a hypnotic for short-term treatment of insomnia. Side effects include drowsiness and light-headedness, confusion and ataxia and dependence.
Metabolised by CYP, probably CYP3A and CYP2C19.
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FLUVASTATIN (Lipid Lowering)
Fluvastatin is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitor, which is used in the treatment of hypercholesterolaemia type IIa in patients whose cholesterol concentration is 6.5 mmol/litre or more and have not responded to dietary control. It is also used as an adjunct to diet to slow the progression of coronary atherosclerosis in primary hypercholesterolaemia and concomitant coronary heart disease. Side effects include nausea and vomiting, abdominal pain, headache and insomnia.
Metabolised mainly by CYP2C9, but also CYP3A4 and CYP2D6. A weak inhibitor of CYP2C9.
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FOMIVIRSEN (Antiviral)
Used to treat cytomegalovirus retinitis in AIDS patients when other treatment is ineffective or contraindicated. Side effects include local irritation and inflammation, visual disturbances, conjunctival haemorrhage and other eye disorders.
This drug is an antisense oligonucleotide. Some metabolised by exonuclease activity and removal of single terminal nucleotides.
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FOSCARNET (Antiviral)
Used to treat cytomegalovirus retinitis in AIDS patients and mucocutaneous herpes simplex in immunocompromised patients when aciclovir is ineffective. Side effects include nausea and vomiting, diarrhoea, headache, neurological disorders, changes in ECG and blood pressure and blood disorders and renal impairment.
Excreted mainly unchanged in urine.
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GABAPENTIN (Anticonvulsants)
Gabapentin is an anti-epileptic drug indicated as add-on therapy for partial seizures and partial seizures with secondary generalisation in patients who have not achieved satisfactory control with or who are intolerant to standard anticonvulsants used alone or in combination. It is also indicated in the treatment of neuropathic pain.
Gabapentin is not metabolised in humans and does not induce hepatic mixed function oxidase enzymes. In vitro studies showed that gabapentin did not inhibit CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 or CYP3A4. At high concentrations (~15x Cmax), 14-30% inhibition of CYP2A6 was observed.
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GAMMA-HYDROXYBUTYRATE (Illicit/Recreational)
GHB is a chemical compound structurally similar to the inhibitory brain neurotransmitter GABA. Precursors of GHB, gamma butyrolactone and 1,4-butanediol, are converted to GHB following ingestion. Some medical uses of GHB include nacrolepsy, depression, alcohol withdrawal, epilepsy and anaethesia. However, GHB has become a popular drug of abuse when used alone or in combination with other substances.
Metabolised by GHB dehydrogenase.
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GANCICLOVIR (Antiviral)
Used only to treat life-threatening or sight-threatening cytomegalovirus in immunocompromised patients and also for prophylaxis against cytomegalovirus infection in immunosuppressive therapy after organ transplants. There are a vast number of side effects, these include nausea and vomiting, blood disorders, infections, diarrhoea, mood disturbances, retinal detachment in AIDS patients, rash, acne and sweating.
Excreted mainly unchanged in urine.
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GARLIC (Herbal remedy)
Garlic (Allium sativum) is mainly used as an antihypertensive or antihypercholesterolaemic. Side effects include gastrointestinal disorders, allergic reactions such as dermatitis, rhinitis and asthma. May cause a decrease in platelet aggregation and elevated international normalised ratios (INRs) and prothrombin time in patients on warfarin.
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GINKGO (Herbal remedy)
Ginkgo (Ginkgo biloba) improves circulation and so can be used in the treatment of intermittent claudication, vertigo, tinnitus and mood changes. It has also been used in Germany for the treatment of dementia. It should not be used along with NSAIDs or anticoagulants; it may cause bleeding and may reduce the effectiveness of anticonvulsants. It may compete with MAO inhibitors and interact with thiazide diuretics causing hypertension. Side effects include headache and gastrointestinal upset.
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GLIPIZIDE (Oral Anti-diabetic)
Glipizide is a sulphonylurea used to treat diabetes mellitus. Side effects tend to be rare and infrequent, they include weight gain, gastrointestinal disturbances, headache, dizziness and hypersensitivity reactions.
Metabolised by CYP2C9.
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GLOSSITIS
Inflammation of the tongue.
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GOLDENSEAL (Herbal remedy)
Goldenseal (Hydrastis canadensis) can be used to treat digestive disorders, malaria and ventricular tachyarrhythmias. This should not be used in babies as it can cause acute haemolysis in babies that are glucose-6-phosphate dehydrogenase deficient. It should not be used during pregnancy. It may antagonise heparin.
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HAART
Highly active antiretroviral therapy. Usually comprised of a regimen of three or more antiretroviral drugs.
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HAEMATOCRIT
A ratio of the volume of red blood cells to the volume of blood in the sample.
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HAEMATOPOIESIS
Production of blood cells.
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HALF-LIFE (t1/2)
Half-life of a drug. The time taken for the drug concentration to fall to half its original value.
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HALOFANTRINE (Antiprotozoal)
Halofantrine is used in the treatment of chloroquine resistant falciparum malaria. Halofantrine has been shown to prolong QTc interval at the recommended therapeutic dose. There have been rare reports of serious ventricular dysrhythmias sometimes associated with death, which may be sudden. Halofantrine is therefore not recommended in combination with drugs, or clinical conditions, known to prolong QTc interval, or in patients with known or suspected ventricular dysrhythmias, Caution should be used with concomitant intake of drugs which are known to significantly inhibit CYP3A4.
Results indicate that both CYP 3A4 and CYP 3A5 metabolize halofantrine, with major involvement of CYP 3A4. In-vivo, the other CYPs have a minor role only. Moreover, strong inhibition, and consequently increased halofantrine cardiotoxicity, might occur with the coadministration of ketoconazole or other CYP 3A4 substrates.
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HALOPERIDOL (Neuroleptics/Neuroleptic)
Used to treat schizophrenia, mania, hypomania, psychomotor agitation, dangerously impulsive behaviour, excitement and intractable hiccup. There are a vast number of side effects and these include extrapyramidal effects, drowsiness, nightmares, insomnia, cardiovascular effects but less antimuscarinic effects and less sedation.
Metabolised by ketone reductase, CYP2D6, CYP3A and glucuronyl transferase.
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HALOTHANE (General Anaesthetic)
Halothane is a volatile liquid anaesthetic. It is potent and a non-irritant. It also produces some muscle relaxation. It can cause severe hepatotoxicity. It is also a cardiorespiratory depressant and may cause bradycardia.
Metabolised by CYP2E1.
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HEPATOTOXICITY
Toxic damage to or poisoning of the liver due to a drug.
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HIRSUTISM
Excessive hair growth.
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HIV
Human Immunodeficiency Virus.
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HYDROXYCARBAMIDE (HYDROXYUREA) (Immune Modulators)
Used mainly to treat myeloid leukaemia. It can be used to treat polycythaemia and in combination with NRTIs in the treatment of HIV. Side effects include nausea, skin reactions and myelosuppression
Excreted mainly unchanged in urine.
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HYPERCHOLESTEROLAEMIA
Abnormal production of high levels of cholesterol.
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HYPERLIPIDAEMIA
Abnormal production of high levels of lipid/fat.
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HYPERSENSITIVITY
Highly sensitive to a particular stimulus or an abnormal or overactive response to a stimulus.
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HYPERTENSION
A disease involving abnormally high blood pressure.
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HYPERTHYROIDISM
Overactive thyroid.
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HYPOGLYCAEMIA
Low blood sugar levels.
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HYPOKALAEMIA
The loss of, or low levels of potassium in the body.
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HYPOTHYROIDISM
Under-active thyroid.
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IBUPROFEN (Analgesic)
A NSAID and antipyretic. Can be used to treat rheumatoid arthritis, dysmenorrhoea, post-operative pain, pain and fever in children. Side effects as with other NSAID, such as gastrointestinal disturbances (less with ibuprofen), hypersensitivity reactions in susceptible individuals, headache, dizziness, tinnitus.
Metabolised by CYP2C9 and glucuronyl transferase as a minor route.
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IMMUNE SYSTEM
The body's defence mechanism against disease and illness.
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INDINAVIR (Antiretroviral (Protease Inhibitor))
Indinavir is a protease inhibitor (PI) and is used to treat HIV infection in combination with NRTIs. Side effects include nausea and vomiting, diarrhoea, headache, insomnia and blood disorders and elevated liver enzymes and abnormal fat accumulation (lipodystrophy).
Metabolised by CYP3A, CYP2D6 as a minor route and glucuronyl transferase. A weak inhibitor of CYP3A
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INHIBITORY QUOTIENT
IQ = Cmin/IC50 A high IQ value means that the drug exceeds the concentration required to inhibit the virus whereas a low IQ value indicates inadequate drug levels or a resistant virus.
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INTERFERON ALPHA (Immune Modulators)
Interferons are naturally occurring proteins and interferon alpha is used to treat many forms of cancer and hepatitis A and B. Side effects are dose-related and include nausea, flu-like symptoms, depression and cardiovascular effects, hepatoxicity and nephrotoxicity and hypersensitivity reactions.
A non glycosylated protein. Metabolism mainly in the kidney and in the liver by a minor route.
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INTERLEUKIN 2 (Immune Modulators)
The drug aldesleukin, which is an interleukin 2 recombinant, is used to treat metastatic renal cell carcinoma. It is a very toxic drug and can cause bone marrow, hepatic, renal and CNS toxicity and also pulmonary oedema and hypotension due to capillary leak syndrome.
Substantially excreted unchanged.
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IQ (Inhibitory Quotient)
An index of how far the concentration of the drug is in excess of the viral IC50 (inhibitory concentration).
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IQ
Inhibitory Quotient (IQ) = Cmin/IC50 A high IQ value means that the drug exceeds the concentration required to inhibit the virus whereas a low IQ value indicates inadequate drug levels or a resistant virus.
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ISONIAZID (Antibacterial)
Used to treat tuberculosis in combination with other drugs and used for prophylaxis. Side effects include nausea and vomiting, peripheral and optical neuritis, convulsions, psychosis, hypersensitivity reactions.
Metabolised by N-acetyltransferase and CYP. An inhibitor of CYP2E1, CYP1A2, CYP2C9 and CYP3A but can also act as an enzyme inducer.
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ITRACONAZOLE (Antifungal)
Used to treat various fungal infections including candidal infections and systemic infections. Also used for maintenance in AIDS patients to prevent reoccurrence of underlying fungal infections. Not recommended in children or the elderly. Side effects include nausea, constipation, vomiting, diarrhoea, dyspepsia, headache, dizziness, raised liver enzymes, allergic reactions, liver disorders and peripheral neuropathy. With prolonged use, oedema, hypokalaemia and hair loss.
Metabolised by CYP3A. An inhibitor of CYP3A, CYP2C9 and P-glycoprotein.
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KAVA-KAVA (Herbal remedy)
Kava-kava (Piper methysticum) is used as a treatment for anxiety. It should not be used with barbiturates, antipsychotic drugs or alcohol. It may also cause skin discolouration with long-term use; it is therefore recommended that it not be used for longer than six months.
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KETAMINE (General Anaesthetic)
Used for the induction and maintenance of anaesthesia mainly in children. Side effects include hallucinations and slow recovery from anaesthesia.
Undergoes CYP-mediated metabolism followied by conjugation. Individual CYPs need to be identified.
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KETOCONAZOLE (Antifungal)
Used to treat skin and fingernail infections, but not toe nails, mycoses, candidal infections and for prophylaxis of mycoses in immunosuppressed patients. Side effects include nausea and vomiting, abdominal pain, headache, rashes, dizziness, alopecia and fatal liver damage therefore care must be taken as there is a greater risk of developing hepatitis if taken for longer than 14 days.
Metabolised by CYP3A. A potent inhibitor of CYP3A and an inhibitor of CYP2C9 and P-glycoprotein.
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LAMIVUDINE (3TC) (Antiretroviral (Nucleoside Analogue))
Lamivudine is a nucleoside reverse transcriptase inhibitor (NRTI) and is used to treat HIV infection in combination with other antiretroviral drugs. Side effects include nausea, vomiting and diarrhoea, headache, cough, peripheral neuropathy and pancreatitis and raised liver enzymes.
Metabolised by non-CYP enzymes but excreted mainly unchanged in urine.
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LAMOTRIGINE (Anticonvulsant)
Used to treat partial seizures, primary and secondary generalised tonic-clonic seizures and seizures associated with Lennox-Gaustaut syndrome. Side effects include skin rashes, blood disorders, gastrointestinal disturbances, headache, dizziness, CNS effects, blurred vision, conjunctivitis.
Metabolised by glucuronyl transferase and methyltranferase. An inducer of glucuronyl transferase and will induce its own metabolism.
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LANSOPRAZOLE (Gastrointestinal Agents)
Lansoprazole is a proton pump inhibitor which inhibits the release of gastric acid by blocking the hydrogen-potassium ATPase system. Used to treat gastric and duodenal ulcer and ulcers associated with NSAIDs and Helicobacter pylori. Also used to treat acid-related dyspepsia, gastro-oesophageal disease and Zollinger-Ellison syndrome. Side effects include nausea and vomiting, headache and dizziness and constipation.
Metabolised by CYP2C19 and CYP3A.
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LIDOCAINE (LIGNOCAINE) (Antiarrhythmic)
A class I antiarrhythmic used to treat ventricular arrhythmias, especially after myocardial infarction. Side effects include dizziness, drowsiness, parathesia, confusion, respiratory depression, hypotension, bradycardia, convulsions and hypersensitivity in susceptible individuals.
Metabolised by CYP3A4.
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LIPODYSTROPHY
A disease thought to be caused by certain antiretroviral drugs that results in the loss of fat from some areas such as the upper arms and legs and the accumulation of fat in other areas such as the stomach, back of the neck and breasts.
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LIQUORICE (Herbal remedy)
Liquorice (Glycyrrhiza glabra) is potentially harmful if used in high doses or for a long period of time, it is recommended that it only be used under medical supervision. It is contraindicated in those with liver cirrhosis, and other liver disorders, kidney and cardiovascular disease, hypokalaemia and pregnancy. It can potentiate cardiac glycosides and can cause pseudoaldosteronism; symptoms include headache, sodium and water retention, hypertension heart failure and cardiac arrest.
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LOPINAVIR (Antiretrovirals (Protease Inhibitor))
Lopinavir is protease inhibitor and is used to treat HIV. It is co-formulated with ritonavir (as Kaletra); ritonavir is required to increase plasma levels of lopinavir.
Lopinavir is extensively metabolised by the hepatic cytochrome P450 system, almost exclusively by isozyme CYP3A. Ritonavir is a potent CYP3A inhibitor which inhibits the metabolism of lopinavir and therefore, increases plasma levels of lopinavir. Kaletra contains lopinavir and ritonavir, both of which are inhibitors of the P450 isoform CYP3A in vitro. Kaletra does not inhibit CYP2D6, CYP2C9, CYP2C19, CYP2E1, CYP2B6 or CYP1A2 at clinically relevant concentrations. Kaletra has been shown in vivo to induce its own metabolism and to increase the biotransformation of some medicinal products metabolised by cytochrome P450 enzymes and by glucuronidation.
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LORATADINE (Antihistamine)
Used to treat symptoms of allergies such as hay fever and urticaria. Side effects are rare but similar to cetririzine therefore may include; antimuscarinic effects such as dry mouth, blurred vision, gastrointestinal disturbances, however these effects are low, as is any sedation effect. Other side effects may include hypersensitivity and photosensitivity reactions, sweating, convulsions and blood disorders and liver dysfunction.
Metabolised by CYP3A4 and CYP2D6 as a minor route.
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LORAZEPAM (Anxiolytics/Hypnotics/Sedative)
Lorazepam is one of the shorter-acting benzodiazepines and is used for the short-term treatment of anxiety and insomnia. Side effects include drowsiness and light-headedness, headache, rashes, increase in aggression, blood disorders and CNS effects and dependence.
Metabolised by glucuronyl transferase.
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LOVASTATIN (Lipid Lowering)
Lovastatin is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitor. It is used to treat primary and secondary hypercholesterolaemia and in combined hypercholesterolaemia and hypertrglyceridaemia and to treat type III hyperlipidaemia. Side effects include nausea and vomiting, abdominal pain, headache, insomnia, fatigue and dry mouth.
Metabolised by hydrolysis and CYP3A to active metabolites.
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LUMEFANTRINE (Antiprotozoal)
Lumefantrine is given with artemether for the treatment of acute uncomplicated Plasmodium falciparum malaria.
Lumefantrine is metabolised by the cytochrome enzyme CYP3A4 but does not inhibit this enzyme at therapeutic concentrations. Lumefantrine was found to inhibit CYP2D6 in vitro. This may be of particular clinical relevance for compounds with a low therapeutic index.
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MAO
Monoamine oxidase. An enzyme inside the body that breaks down certain endogenous substances and some drugs.
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MDMA ("ECSTASY") (Illicit/Recreational)
MDMA (3,4-methylenedioxymethamphetamine), is an amphetamine with some hallucinogenic properties at high doses. It is directly neurotoxic to the human brain and has been linked to a number of deaths worldwide. Deaths result from hyperthermia, hyponatraemia, or cerebral oedema.
Metabolised by CYP2D6.
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MEC
Minimum effective concentration.
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MEGESTROL ACETATE (Steroids)
Megestrol is a progestogen and is used as a second or third line of treatment in breast cancer. Also used to treat endometrial cancer and renal cell carcinoma. Side effects include gastrointestinal disturbances, changes in weight, acne, fluid retention and irregular menstrual cycles.
Metabolised by CYP and glucuronyl transferase.
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MENINGITIS
Inflammation of the lining of the brain (the meninges).
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METFORMIN (Oral Anti-diabetic)
Meformin is a biguanide with antihyperglycaemic effects and is used in the treatment of type 2 diabetes mellitus in adults.
Metformin is excreted unchanged in the urine. No metabolites have been identified in humans.
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METHADONE (Analgesic)
An opioid analgesic used to treat severe pain and as an adjunct in treating opioid dependence. Side effects as with other opioid analgesics are nausea and vomiting, constipation, headache, dependence. Methadone is not as sedating as morphine.
Metabolised by CYP3A and glucuronyl transferase. Weakly inhibits CYP2D6.
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METHAMPHETAMINE (Illicit/Recreational)
Methamphetamine is a powerfully addictive stimulant that dramatically affects the central nervous system. Methamphetamine's chemical structure is similar to that of amphetamine, but it has more pronounced effects on the central nervous system. Like amphetamine, it causes increased activity, decreased appetite, and a general sense of well-being. Acute intoxication often results in agitation, violence, and death. Chronic use may lead to infection, heart failure, malnutrition, and permanent psychiatric illness.
Metabolised by CYP2D6 and others and MAO (monoamine oxidase).
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METOCLOPRAMIDE (Gastrointestinal Agents)
Metoclopramide is a dopamine antagonist and is also a motility stimulant and stimulates gastric emptying. It is used to treat nausea and vomiting in adults especially in the treatment of gastrointestinal disorders and treatment with cytotoxic drugs. Also used to treat migraine. Side effects include diarrhoea, drowsiness, restlessness, and extrapyramidal effects.
Metabolised by sulphatase and glucuronyl transferase and possibly CYP enzymes.
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METOPROLOL (Beta-blocker)
Metoprolol is a β1 selective antagonist and is used in the treatment of hypertension, angina, arrhythmias, migraine prophylaxis, thyrotoxicosis and to control arrhythmias during anaesthesia. Side effects include heart failure, bradycardia, hypotension, bronchospasm, peripheral vasoconstriction and gastrointestinal disturbances. Reduce the dose in hepatic impairment.
Metabolised by CYP2D6.
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METRONIDAZOLE (Antibacterial)
Used to treat infections caused by anaerobic bacteria and by protozoa and is effective in treating antibiotic-associated colitis. Side effects include nausea and vomiting, furred tongue, gastrointestinal disturbances, headache, dizziness.
Metabolised by CYP enzymes. An inhibitor of aldehyde oxidase.
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MEXILETINE (Antiarrhythmic)
A class I antiarrhythmic used to treat ventricular arrhythmias, especially after myocardial infarction, good if lignocaine ineffective. Side effects include nausea and vomiting, hypotension, palpitations, torsarde de pointes, gastrointestinal disturbances such as constipation and CNS effects such as drowsiness, confusion, convulsions, tremor, blood disorders.
Metabolised by CYP2D6 and methylation.
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MICONAZOLE (Antifungal)
Used to treat oral and intestinal fungal infections and used for prophylaxis. Also can be used to treat skin and nail infections and used for the treatment of acne vulgaris. Side effects include nausea, vomiting and diarrhoea, rarely hypersensitivity reactions and reports of hepatitis.
Metabolised by CYP3A. An inhibitor of CYP3A.
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MICTURITION
Frequently wanting to urinate.
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MIDAZOLAM (Anxiolytics/Hypnotics/Sedative)
Midazolam is a benzodiazepine and is used for sedation before or during surgery and also with anaesthetics to induce anaesthesia. Side effects include drowsiness and light-headedness, headache, rashes, increase in aggression, blood disorders and CNS effects and dependence. Also respiratory depression and arrest with high doses.
Metabolised by CYP3A.
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MILK THISTLE (Herbal remedy)
Milk thistle (Silymarin) has hepatoprotective properties, and the silymarin is thought to be the liver protective agent. It acts through a number of pharmacological actions, such as altering the cell membrane of the hepatocyte to prevent toxins entering and promotes hepatocyte regeneration. It is used by HIV patients to treat liver disease caused by hepatitis, and is also used to treat drug-induced liver damage from drugs such as acetaminophen and halothane. Side effects are few; they include mild allergic reactions and diarrhoea at high doses.
It may alter P450 enzymes and the metabolism of NNRTIs, but there is no clear evidence to support this.
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MIRTAZAPINE (Antidepressants)
Mirtazapine is an antidepressant that can be given as treatment for episodes of major depression and begins to exert its effect in general after 1-2 weeks of treatment.
Extensively metabolised by CYP2D6 and CYP3A4 and to a lesser extent by CYP1A2. In vitro data suggest that it is a very weak competitive inhibitor of CYP1A2, CYP2D6 and CYP3A.
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MORPHINE (Analgesic)
An opioid analgesic used to treat severe pain. It also causes euphoria. Side effects as with other opioid analgesics including nausea and vomiting.
Metabolised by glucuronyl tranferase.
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MYCOPHENOLATE MOFETIL
(See Mycophenolate)
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MYCOPHENOLATE (Immunosuppressants)
Mycophenolate is indicated in combination with ciclosporin and corticosteroids for the prophylaxis of acute transplant rejection in patients receiving allogeneic renal, cardiac or hepatic transplants. Mycophenolate mofetil is the 2-morpholinoethyl ester of mycophenolic acid. Mycophenolic acid is a potent, selective, uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase, and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation into DNA.
Following oral administration, mycophenolate mofetil undergoes rapid and extensive absorption and complete presystemic metabolism to the active metabolite, mycophenolic acid. Mycophenolic acid is metabolised principally by glucuronyl transferase to form the phenolic glucuronide of mycophenolic acid, which is not pharmacologically active.
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MYCOPHENOLIC ACID
(See Mycophenolate)
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MYELOSUPPRESSION
Suppression of the bone marrow (where white blood cells are produced).
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NANDROLONE (Steroids)
Nandrolone is an anabolic steroid. It has been used to treat osteoporosis in post-menopausal women but is no longer recommended. It can be used to treat aplastic anaemia and to reduce the itching of chronic biliary obstruction. Side effects include acne, amenorrhoea, inhibition of spermatogenesis, sodium retention and oedema and in high doses, virilisation.
Similar to testosterone therefore substantially metabolised by reduction and conjugation. Some CYP metabolism.
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NEFAZODONE (Antidepressant)
Nefazodone inhibits the re-uptake of 5-HT (serotonin) and is also a 5-HT2 antagonist. Used to treat depressive illness and depressive illnesses accompanied by anxiety or sleep disturbances. Side effects include dry mouth, constipation, asthenia, ataxia, dizziness, fever, chills, postural hypotension and somnolence.
Metabolised by CYP3A and other CYPs. An inhibitor of CYP3A.
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NELFINAVIR (Antiretroviral (Protease Inhibitor))
Nelfinavir is a protease inhibitor (PI) and is used to treat HIV infection in combination with NRTIs. Side effects include nausea, diarrhoea, flatulence, rash and abnormal fat accumulation (lipodystrophy).
Metabolised by CYP3A and CYP2C19 to an active metabolite M8. An inhibitor of CYP3A.
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NEPHROTOXICITY
Toxic damage to or poisoning of the kidney due to a drug.
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NEURITIS
Inflammation of the nerve.
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NEUROPATHY
Damage to nerves.
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NEUTROPENIA
A type of blood disorder. Loss or low number of white blood cells known as neutrophils.
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NEVIRAPINE (Antiretroviral (NNRTI))
Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used to treat HIV infection in combination with other antiretroviral drugs. Side effects include rash and Stevens-Johnson syndrome, toxic epidermal necrolysis, hepatitis, nausea, dizziness and fever.
Metabolised by CYP3A. An inducer of CYP3A
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NIFEDIPINE (Calcium Channel Antagonists)
Nifedipine relaxes vascular smooth muscle and dilates coronary and peripheral arteries. It is used in the treatment of hypertension and Raynaud's disease and the prophylaxis of angina. Side effects include headache and flushing, dizziness, palpitations, rash, gastrointestinal and visual disturbances.
Metabolised by CYP3A. An inhibitor of P-glycoprotein and a weak inhibitor of CYP3A.
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NNRTI
Non-nucleoside reverse transcriptase inhibitor. A class of antiretroviral drug used to treat HIV.
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NOCTURNAL ENURESIS
In children this is involuntary urination at night i.e. bed-wetting.
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NORTRIPYLINE (Antidepressant)
Nortripyline is a tricyclic antidepressant drug but is less sedating than amitriptyline. Used to treat depression and nocturnal enuresis in children. Side effects as with amitriptyline, including antimuscarinic effects such as dry mouth, blurred vision and constipation, cardiovascular side effects such as arrhythmias, hypersensitivity reactions, endocrine and behavioural side effects and blood disorders.
Metabolised by CYP2D6.
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NRTI
Nucleoside reverse transcriptase inhibitor. A class of antiretroviral drug used to treat HIV.
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NSAID
Non-steroidal anti-inflammatory drug examples include aspirin and ibuprofen.
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OEDEMA
Swelling.
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OFLOXACIN (Antibacterial)
A quinolone antibiotic used to treat urinary tract infections and lower respiratory tract infections, uncomplicated gonorrhoea, non-gonococcal urethritis and cervicitis. Side effects as with other quinolones, and also include cardiac effects, anxiety, tremor, extrapyramidal symptoms and psychotic effects.
Excreted mainly unchanged in the urine.
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OLANZAPINE (Antipsychotics/Neuroleptic)
Olanzapine is indicated for the treatment of schizophrenia and is effective in maintaining the clinical improvement during continuation therapy in patients who have shown an initial treatment response. It is indicated for the treatment of moderate to severe manic episode, but has not been demonstrated to prevent recurrence of manic or depressive episodes.
Olanzapine is metabolised in the liver by CYP1A2 with CYP2D6 having a minor role. Olanzapine does not inhibit the main CYP450 isoenzymes in vitro (e.g., 1A2, 2D6, 2C9, 2C19, 3A4).
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OLIVE LEAF EXTRACT (Herbal remedy)
Taken by people for diabetes.
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OMEPRAZOLE (Gastrointestinal Agents)
Omeprazole is a proton pump inhibitor which inhibits the release of gastric acid by blocking the hydrogen-potassium ATPase system. Used to treat gastric and duodenal ulcer and ulcers associated with NSAIDs and Helicobacter pylori. Also used to treat acid-related dyspepsia, gastro-oesophageal disease and Zollinger-Ellison syndrome and to reduce gastric acid secretion during anaesthesia. Side effects include nausea and vomiting, headache and dizziness and constipation and blood disorders and hypersensitivity reactions such as anaphylaxis.
Metabolised by CYP2C19 and CYP3A. An inhibitor of CYP2C19. An inducer of CYP1A2 at high concentrations.
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ONDANSETRON (Gastrointestinal Agents)
Ondansetron is a 5-HT3 antagonist and used to prevent nausea and vomiting when taking emetogenic chemotherapy and also to prevent nausea and vomiting before surgery. Side effects include headache and flushing, hiccups, constipation, hypersensitivity reactions.
Metabolised by CYP2D6, CYP1A2, and CYP3A.
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OTITIS MEDIA
Inflammation of the middle ear.
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OTOTOXICITY
Toxic damage to or poisoning of the ear due to a drug.
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OXANDROLONE (Steroids)
Oxandrolone is an anabolic steroid and can be used to treat involuntary weight loss due to circumstances such as surgery or severe infections or due to unknown causes. Side effects are rare but may include acne, amenorrhoea and virilisation.
Metabolised by reduction and some CYP metabolism and conjugation.
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OXAZEPAM (Anxiolytics/Hypnotics/Sedative)
Oxazepam is one of the shorter-acting benzodiazepines used for short-term treatment of anxiety. Side effects include drowsiness and light-headedness, headache, rashes, increase in aggression, blood disorders and CNS effects and dependence.
Metabolised by glucuronyl transferase.
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P450
Cytochrome P450. A family of enzymes mainly in the liver and responsible for steroid synthesis and also the metabolism of many drugs. Examples include CYP3A4, CYP2D6 and CYP2C9.
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PACLITAXEL (Antineoplastic)
Paclitaxel is part of a class of drugs know as the taxanes and is used to treat primary ovarian cancer in combination with cisplatin, metastatic ovarian cancer, metastatic breast carcinoma and non-small cell lung cancer. Side effects may include hypersensitivity reactions, nausea and vomiting, peripheral neuropathy, myelosuppression, alopecia, arrhythmias and muscle pain.
Metabolised by CYP2C8 and CYP3A.
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PAEONIAE RADIX (Herbal remedy)
Paeoniae radix (the dried root of Paeonia lactiflora) is used as an anticonvulsant and for the treatment of menstrual disorders.
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PANCREATITIS
Inflammation of the pancreas.
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PARACETAMOL (Analgesic)
Used to treat musculoskeletal pain, has similar actions to aspirin but no anti-inflammatory or antiplatelet activity. Causes less irritation than aspirin. Side effects are rare but can cause rashes and blood disorders. Liver damage, and to a lesser extent kidney damage in overdose.
Metabolised by glucuronyl transferase, sulphation, CYP1A2, CYP2E1 and CYP3A as a minor route.
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PAROXETINE (Antidepressant)
Paroxetine is a selective serotonin re-uptake inhibitor (SSRI). Used to treat depression, obsessive-complusive disorder, panic disorder and social phobia. Side effects include asthenia, insomnia, nausea, tremor, sweating, somnolence, and postural hypotension and hypersensitivity reactions.
Metabolised by CYP2D6 and COMT as a minor route. An inhibitor of CYP2D6 and CYP2C19.
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PEGINTERFERON ALPHA-2a (Immune Modulators)
Peginterferon alfa-2a is a covalent conjugate of recombinant alfa-2a interferon with a single branched bis-monomethoxy polyethylene glycol (PEG) chain. It is indicated for the treatment of adults with histologically proven chronic hepatitis C infection who have compensated liver disease and have not previously been treated with interferon alpha. The optimal way of use is in combination with ribavirin; monotherapy is indicated mainly in cases of intolerance or contraindication to ribavirin.
Metabolism is not fully characterised, however studies in rats indicate that the kidney is the major organ for excretion. In humans, systemic clearance of peginterferon alfa-2a is about 100-fold lower than that of the native interferon alfa-2a.
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PENTAMIDINE (Antiprotozoal)
Used in the treatment of Pneumocystis carinii pneumonia, visceral and cutaneous leishmaniasis and trypanosomiasis. Side effects can be severe and sometimes fatal, they include arrhythmias, hypotension and hypoglycaemia. Also blood disorders, nausea and vomiting and dizziness.
Metabolised by CYP.
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PERIPHERAL NEUROPATHY
Damage to the nerves of usually the hands and feet causing symptoms such as pins and needles and pain.
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PERITONITIS
Inflammation of the peritoneum (the lining of the abdomen).
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PERPHENAZINE (Antipsychotic/Neuroleptics)
Used to treat schizophrenia and other psychoses, psychomotor agitation, dangerously impulsive behaviour, excitement and as an antiemetic to prevent nausea and vomiting. There are a vast number of side effects and these include extrapyramidal effects, drowsiness, nightmares, insomnia, cardiovascular effects but less sedation.
Metabolised by CYP2D6. An inhibitor of CYP2D6.
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PETHIDINE (Analgesic)
An opioid analgesic used to treat moderate to severe pain, but is not suitable for relieving severe continuing pain as it has a short duration of action. Used to treat pain in women during labour. Side effects similar to other opioid analgesics. Avoid use in renal impairment. It may cause convulsions in overdose. Causes less respiratory depression than other opioids and less constipation than with morphine.
Metabolised by CYP and glucuronyl transferase.
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PHARMACOENHANCEMENT
Increasing the plasma concentrations of drug greater than that of the IC95 of wild type and mutant virus. This includes for example, inhibition of metabolism of the drug to increase its concentrations.
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PHENOBARBITAL (PHENOBARBITONE) (Anticonvulsant)
A barbiturate used to treat tonic-clonic and partial seizures. Side effects include mental depression, drowsiness, lethargy, allergic skin reactions, paradoxical excitement, dependence and tolerance.
Metabolised by CYP2C19 and possibly other CYPs and glucuronyl transferase. An inducer of CYP2A6, CYP2C9, CYP3A and glucuronyl transferase.
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PHENYTOIN (Anticonvulsant)
Used to treat most types of seizures, including tonic-clonic seizures, partial seizures and seizures following head injury or neurosurgery and trigeminal neuralgia. It can also be used to treat cardiac arrhythmias. Side effects include nausea and vomiting, CNS effects such as tremor, slurred speech, insomnia, acne, blurred vision, blood disorders and rashes.
Metabolised by CYP2C9 and CYP2C19. An inducer of CYP2C9, CYP3A and glucuronyl transferase.
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PHOTOSENSITIVITY
Sensitivity to light.
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PI
Protease inhibitor. A class of antiretroviral drug used to treat HIV.
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PIMOZIDE (Antipsychotic/Neuroleptic)
Pimozide is a diphenylbutylpiperidine and a D2 receptor antagonist. It is used to treat schizophrenia, hypochondriacal psychosis, paranoid psychosis and Gilles de la Tourette syndrome. Side effects are similar to chlorpromazine but with less sedation. Serious arrhythmias have been reported.
Metabolised by CYP3A.
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PIROXICAM (Analgesic)
A NSAID used to treat pain and inflammation. Used in rheumatic disease, musculoskeletal disorders and acute gout. Side effects as with other NSAIDs. Also suppository form may cause irritation and occasional bleeding and in the injection form there may be pain at the injection site.
Metabolised by CYP2C9 and glucuronyl tranferase.
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PNEUMOCYSTIS CARINII PNEUMONIA (PCP)
A type of pneumonia caused by Pneumocystis carinii. Symptoms include fever, cough and breathlessness.
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POSTURAL HYOPTENSION
Ongoing from a sitting to standing position there is a large fall in blood pressure also resulting in light-headedness and dizziness.
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PRAVASTATIN (Lipid Lowering)
Pravastatin is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitor, which is used in the treatment of hypercholesterolaemia in patients not responding to other measures such dietary control. It is also used as an adjunct to diet to slow the progression of coronary atherosclerosis and to prevent cardiac events in these patients and those without coronary heart disease. It is used to prevent stroke and myocardial infarction or need for revascularisation procedures. Side effects include nausea and vomiting, abdominal pain, headache, chest pain, rash and fatigue.
Not extensively metabolised by CYP enzymes therefore less drug interactions than other statins.
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PREDNISOLONE (Steroids)
Prednisolone is a corticosteroid used to suppress inflammatory and allergic reactions. It used to treat inflammatory bowel disease and Crohn's disease. It is also used to treat asthma and rheumatic disease. Side effects include gastrointestinal disturbances, musculoskeletal and endocrine effects and also neuropsychiatric and ophthalmic effects.
Metabolised by CYP3A. An inhibitor of CYP3A.
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PRO-ARRHYTHMIC
A substance or drug that causes arrhythmias.
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PROCHLORPERAZINE (Gastrointestinal Agents)
Prochlorperazine is a phenothiazine and is a centrally acting dopamine antagonist. It is used to treat severe nausea, vomiting and vertigo and labyrinthine disorders and also can be used to treat schizophrenia and other psychoses. Side effects are as chlorpromazine and include extrapyramidal effects, drowsiness, nightmares, insomnia, cardiovascular effects and antimuscarinic effects.
Metabolised by CYP and glucuronyl transferase. An inhibitor of P-glycoprotein.
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PROGESTERONE/PROGESTOGEN (Steroids)
Progesterone is used to treat menopausal symptoms, pre-menstrual syndrome and post-natal depression. It is also used in the treatment of endometrial cancer and renal cell carcinoma. Progestogens are used in HRT and oral contraceptives either as a combined pill or as a progestogen-only pill. Side effects include gastrointestinal disturbances, changes in weight, acne, fluid retention and irregular menstrual cycles.
Metabolised by CYP 3A and 2C19.
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PROGUANIL (Antiprotozoal)
Proguanil alone is not suitable for the treatment of malaria, but is used for prophylaxis. Side effects include gastrointestinal disturbances such as diarrhoea and sometimes mouth ulcers and skin reactions and hair loss.
Metabolised by CYP2C19 and CYP3A but about 60% is excreted unchanged in urine. Proguanil itself is inactive (a pro-drug) and has to be activated by CYP enzymes to cycloguanil.
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PROPAFENONE (Antiarrhythmic)
A class I antiarrhythmic used to treat ventricular arrhythmias, supraventricular arrhythmias and for their prophylaxis. Side effects include dry mouth, blurred vision due to antimuscarinic effects, nausea and vomiting, dizziness, diarrhoea, headache, allergic skin reactions, pro-arrhythmic effect, can cause hypersensitivity reactions in susceptible individuals.
Metabolised by CYP2D6, CYP3A and CYP1A2. An inhibitor of CYP2D6.
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PROPHYLAXIS
Taking a substance or drug to prevent an illness or disease.
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PROPRANOLOL (Beta-blocker)
Propranolol is a non-selective ß antagonist and can be use in the treatment of hypertension, angina, arrhythmias, anxiety where there are symptoms of palpitations and in migraine prophylaxis and for prophylaxis after myocardial infarction. Side effects include heart failure, bradycardia, hypotension, bronchospasm, peripheral vasoconstriction and gastrointestinal disturbances.
Metabolised by CYP2D6, CYP1A2, CYP2C19 and glucuronyl transferase.
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PROTEASE
An enzyme of the HIV virus that hydrolyses proteins and peptides and is the target for the PIs (protease inhibitors).
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PYRAZINAMIDE (Antibacterial)
Used to treat tuberculosis in combination with other drugs. Side effects include nausea and vomiting, hepatotoxicity, anorexia, jaundice, liver failure, skin rash.
Metabolised by deaminase and xanthine oxidase and aldehyde oxidase.
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PYREXIA
Fever.
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PYRIMETHAMINE (Antiprotozoal)
Pyrimethamine is not used alone to treat malaria. It is used in combination with sulphadoxine in FansidarÒ to treat Plasmodium falciparum malaria and also used in combination with dapsone in MaloprimÒ for the prophylaxis of malaria. Side effects include depression of haematopoiesis and with high doses there is the possibility of rashes and insomnia.
Metabolised by CYP.
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QT INTERVAL
A particular point on the ECG (electrocardiogram) representing a particular part in the contraction of the heart.
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QUERCETIN (Herbals/Nutraceuticals)
Quercetin (3,3',4',5,7-pentahydroxyflavone) is an ubiquitous flavonoid distributed in plant foods, beverages, herbs and dietary supplements, e.g. onions, grapes, berries, apples, red wine, tea, St. John's wort and ginkgo. Numerous experiments have reported biological, pharmacological, and medicinal properties, the beneficial effects thought to be due to the inhibition of enzymes involved in cell cycling and its antioxidant properties. In addition to its various activities, quercetin has |