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Otago Pharmacology
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189
Medical
Undergraduate 4
08/17/2008

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Term
Prophylaxis of gout
Definition
ALLOPURINOL
Term
Dose of ALLOPURINOL
Definition
100-800mg OD, high fluid intake.
Term
Important interactions of ALLOPURINOL
Definition
CYP inhibitor. Inhib AZOTHIAPRINE met (decr dose). Renal toxicity w Thiazide
Term
Adverse effects of ALLOPURINOL
Definition
Goutogenic. Rash (>10%). Hepatitis, GI (1-10%)
Term
Mechanism of action of ALLOPURINOL
Definition
Competetive and non-competitive xanthine oxidase inhibitor. Inhibits production of uric acid from xanthine.
Term
Kinetics of ALLOPURINOL
Definition
F>0.8, t1/2=0.5-2hrs (metabolyte 10-40hrs)
Term
Precautions, contraindications of ALLOPURINOL
Definition
Acute gout. Reduce dose in renal impairment.
Term
Class/mechanism of AMITRYPTILINE
Definition
Tricyclic antidepressant. Inhibit uptake of NA and 5-HT.
Term
Dose of AMITRYPTILINE
Definition
Start 25mg nocte. Incr to 75-150mg as nec.
Term
Kinetics of AMITRYPTILINE
Definition
F=0.5, Hepatic metab 2D6.
Term
Important interactions of AMITRYPTILINE
Definition
SSRIs-->serotin syndrome. MOAIs-->HTN, pyrexia.
Term
Adverse reactions of AMITRYPTILINE
Definition
5-HT sydrome. Dose dependent anticholinergic. Rare heam and endo.
Term
Precautions/contra AMITRYPTILINE
Definition
narrow angle glaucoma, prostatism, conduction irreg.
Term
AMITRYPTILINE overdose (Sx and Rx)
Definition
Anticholinergic. Dilated pupils, arrythmias, CV depression, seizure->coma->death.
NaHCO3. Benzo. Defrib.
Term
Classes/Mechanisms of ASPIRIN
Definition
NSAID.
Analgesic (antiprostaglandin), Antiplatelet (irreversible inhibitor of Thromboxane A2)
Term
Doses of ASPIRIN (different uses)
Definition
MI, TIA prophylaxis: 75-300mg EC, OD.
Pain relief: up to 300-900mg q3-4h.
Term
Kinetics of ASPIRIN
Definition
F=0.6. t1/2=15-30min (but antiplatelet effects up to 7/7). Hepatic metab.
Protein bound. Saturable kinetics.
Term
First line antihypertensive (ceteris paribus)
Definition
BENDROFLUMATHIAZIDE
Term
Adverse effects of ASPIRIN
Definition
Gastritis. GI bleeding. Impaired heamostasis. Hypersensitivity (asthma, assoc nasal polyps).
Term
Precautions/Contraindications of ASPIRIN
Definition
Active bleeding. Hypersensitity. Asthma. G6PD. Children.
Term
Class/mechanism of BENDROFLUMATHIAZIDE
Definition
Diuretic/Antihypertensive. Inhibits Na, Cl, and H20 absorb in distal loop.
Antihypertensive mech poorly understood (MedSafe)
Term
Dose of BENDROFLUMETHIAZIDE
Definition
2.5-10mg OD.
Term
Kinetics of BENDROFLUMETHIAZIDE
Definition
F=1. t1/2=3-4hrs (effect longer). ru=0.3. 94% Plasma bound.
Term
Interactions of BENDROFLUMETHIAZIDE
Definition
Incr. Lithium-->don't combine.
Vasculitis c ALLOPURINOL-->careful.
Reduces effect of oral anti-glycaemics.
Term
Adverse effects of BENDROFLUMETHIAZIDE
Definition
Diabetogenic, goutogenic, hypokalaemia.
Term
Precautions/Contraindications of BENDROFLUMETHIAZIDE.
Definition
Contra-Lithium, hypokalaemia.
Prec-diabetes, gout, renal imp, hepatic imp.
Term
Mechanism/Class of codeine
Definition
Opioid analgesic. Hepatically metabolised to morphine. Also weak opioid receptor agonist in unchanged form.
Term
Indication/Dose of CODEINE
Definition
Relief of mild-moderate pain, antidiarrhoeal, antitussive-->16-60mg up to q4h up to max of 240mg/day (120mg/day antitussive).
Available in combined preparations with PARACETAMOL and IBUPROFEN.
Term
Kinetics of CODEINE
Definition
F=0.5, t1/2=3hr, Metabolism-hepatic to morphine plus others.
Term
Interactions of CODEINE
Definition
Additive with other CNS depressants.
Loss of efficacy with CYP2D6 inhibitors (lower conversion to morphine) FLOUXETINE, AMIODARONE, IMIDAZOLES, CIMETIDINE.
Term
Adverse effects of CODEINE
Definition
CNS depression (or paradox. stimulation), constipation, nausea,
tachy- or bradycardia, malaise or euphoria, unrinary retention.
Term
Contraindications/Precautions of CODEINE
Definition
Resp depression, some diarrhoea, head injury, high ICP, acute asthma, B Obst, myasthenia gravis.
Term
Class/Mechanism of DIAZEPAM
Definition
Benzodiazapine.
Indirect enhancer of GABA.
Anxiolytic, muscle relaxant, sedative, anticonvulsant.
Term
Kinetics of DIAZEPAM
Definition
F=1,t1/2=43hrs(long-acting benzo), hepatic metabolism with some active metabolytes
Term
Dose of DIAZEPAM.
Definition
Variable, keep low as possible (tolerance).
1-5mg for anxiety. 10-20mg ETOH withdrawal. 10-30mg/day for muscle spasm. 5-10mg iv/dose for status epilepticus.
Term
Adverse effects of DIAZEPAM.
Definition
CNS depression-->death w incr. dose.
Dependence.
Term
Interactions of DIAZEPAM
Definition
Additive with CNS depressants.
Up of down conc. with inhibitors (CIMETIDINE, SSRIs) and (resp) inducers (CARBEMAZAPINE)
Term
Contraindications/Precautions of DIAZEPAM
Definition
myasthenia gravis, chronic use, COPD
Term
Class/Mechanism of DICLOFENAC
Definition
NSAID. COX 1 and 2 inhibitor, thus inhibitor of prostaglandin systhesis.
Term
Dose/Indications of DICLOFENAC
Definition
Mild-moderate pain. Musculoskeletal including inflammatory arthritis.
25-50mg up to tds, to max 150mg/day. Also SR 75mg formulation.
Term
Kinetics of DICLOFENAC
Definition
F=0.55, t1/2=1hr, hep met (CYP2D6) 99%PB.
Term
Interactions of DICLOFENAC
Definition
Incr concentration with CYP2D6 inhibitors (eg SSRIs).
Reduces diuretic/antiHTN effects.
Increases GI bleed with WARFARIN.
Increases Li and DIGOXIN conc.
Term
Adverse effects of DICLOFENAC
Definition
Na and water retention-->HTN.
Gastritis/GI ulceration.
Term
Contraindications/Precautions of DICLOFENAC
Definition
GI bleeding. CV disease. Renal disease. Hypersentivity (including to aspirin). Pregnancy.
Term
Mechanism/class of DIGOXIN
Definition
Inhibitor of Na+/K+ ATPase. This leads to increased cardiac contractility through increased intracellular Ca2+ (Ca2+ is driven out of the cell by Na+ countertransport). Digoxin also slow heart rate by increasing vagal tone, and altering phases 0 and 4 of cardiac action potential.
Term
Indications/Dose of DIGOXIN
Definition
Atrial fibrillation. Heart failure with arrythmia. (Improves QOL but not mortality in other CHF).
Dose: Maintenance usually 62.5-250mcg OD, calculated wrt CrCl and target concentration.
Term
Kinetics of DIGOXIN
Definition
F=0.7, t1/2=30-40hrs, BIG Vd (500L), renally excreted.
Term
Interactions of DIGOXIN
Definition
Brady arrythmias with B-blockers.
Increased effect with hypokalemia.
Many drugs increase or decrease effect if taken concommitantly.
Term
Adverse effects of DIGOXIN
Definition
Mostly dose dependent.
Confusion, yellow/green visual auras, nausea, vomiting, diarrhoea, urticarial rash.
Term
Treatment of DIGOXIN toxicity
Definition
Supportive therapy. Atropine for bradyarrythmias. Temporary pacing. DIGBIND (anti digoxin antibody).
Term
Class/mechanism of DILTIAZEM
Definition
Ca2+ channel blocker. Major effect on vascular smooth muscle-->vasodilatation. Minor effect on SA node--> decr. HR.
Term
Indications for DILTIAZEM
Definition
Rx of hypertension, or angina. Usually not first line antihypertensive. Use especially if HTN and angina are both present but there is contraindication to B-blocker. (or additive with b-blocker).
Term
Dose of DILTIAZEM
Definition
90mg-360mg/day
Term
Kinetics of DILTIAZEM
Definition
F=0.34-0.54, t1/2 around 5hrs. Hepatically metabolised (CYP3A4)
Term
Prec/ contraindications for DILTIAZEM
Definition
Heart block, sick sinus syndrome, severe heart failure.
Term
Common or serious side effects of DILTIAZEM.
Definition
Common: headache, gum hyperplasia, bradycardia, postural hypotension.
Serious (rare): blood dyscrasias, blindness, CNS problems.
Term
Interactions of DILTIAZEM
Definition
Inhibits CYP3A4, but is metabolised by the same. (Interaction with Grapefruit, fluoxetine, cimetidine, carbemazepine, rifampicin, phenytoin etc.)
Additive effect with B-blockers.
Term
Class/mechanism/effects of ENALAPRIL
Definition
ACE inhibitor. Inhibits conversion of angiotensin I to angiotensin II. Multiple effects including vasodilitatation, K+sparing diuresis, and reducing proteinuria, and improving prognosis in heart failure.
Term
Kinetics of ENALIPRIL
Definition
F=0.4, converted to active metabolite (enalaprilat) by the liver. t1/2 around 24hrs. ENALAPRILAT renally cleared.
Term
Indications of ENALAPRIL
Definition
HTN (usually secondline). Heart Failure. Proteinuria.
Term
Dose of ENALAPRIL.
Definition
Start low--2.5-5mg OD, but usually aiming for 10-20mg OD.
Term
Precautions/contraindications for ENALAPRIL
Definition
Pregnancy-hypocalvaria. Adverse reactions (angiooedema, cough). renal artery stenosis.
Term
Adverse effects of ENALAPRIL
Definition
Cough (common--bradykinin effect), postural hypotension (esp first dose), angiooedema (rare)
Term
Interactions of ENALAPRIL
Definition
Via additive or competetive effects (K+Sparing diuretics, NSAIDS).
Increases LITHIUM conc.
Term
Interactions of ENALAPRIL
Definition
Via additive or competetive effects (K+Sparing diuretics, NSAIDS).
Increases LITHIUM conc.
Term
Class/mechanism of ERYTHROMYCIN
Definition
Macrolide antibiotic. Binds to 50s ribosome subunit. Blocks RNA dependent protein synthesis. Also gastric prokinetic.
Term
Inidications of ERYTHROMYCIN
Definition
Infection by susceptible organisms including: St Pyogenes, St aureus, listeria, legionella pn, chlamydia tr, bordetella per, and mycoplasma pn. Main uses are as penicillin alternative, when EBV is suspected (don't uses AMOXYCILLIN), and in atypical pneumonia.
Term
Kinetics of ERYTHROMYCIN
Definition
F=0.35, t1/2=1.6hours, 90% hepatic metabolism (CYP3A4)
Term
Contra/prec ERYTHROMYCIN
Definition
hepatic dysfunction, prolonged QT segment.
Term
Adverse effects of ERYTHROMYCIN
Definition
GI upset, candidias, hypertrophic pyloric stenosis, arrythmias.
Term
Interactions of ERYTHROMYCIN
Definition
via CYP3A4
Term
Dosing of ERYTHROMYCIN
Definition
PO 250-500mg 2-4times daily. IV up to 4g daily.
Term
Recommended maximum ETHANOL intake.
Definition
Men: Not more than 6 units per day, not more than 21 units per week, with alcohol free days.
Women: not more than 4 units per day, not more than 14 per week, with alcohol free days.
Term
Medical indication for ETHANOL
Definition
Treatment of poisoning with METHANOL or ETHYLENE GLYCOL.
Term
Class/mechanism of FLUOXETINE
Definition
Antidepressant, SSRI.
Term
Indications/dosage of FLUOXETINE
Definition
Depression, obsessive-compulsive disorder, bulimia nervosa, premenstrual dysphoric disorder. 20-80mg OD. OCD and BN often higher doses than depression and PMDD. (?continuos or cyclic/intermittent dosage for PMDD)
Term
Kinetics of FLUOXETINE
Definition
F>0.6, t1/2=53hrs, hepatically metabolised (CYP2D6,3A4)
Term
Precautions/contra for FLUOXETINE
Definition
Other antidepressants (serotonin syndrome), limited evidence for use in children and adolescents.
Term
Adverse effects of FLUOXETINE
Definition
Serotonin syndrome (tachycardia, sweating, anxiety)
Headache, sleep disturbance, decreased libido, suicidal ideation.
Term
Interactions of FLUOXETINE
Definition
Many via CYP. e.g. markedly decreases effectiveness of codeine.
Term
Class/mechanism of FRUSEMIDE
Definition
High ceiling/loop diuretic. Blocks Na+/K+/2Cl- cotransporter in ascending loop of henle.
Term
Indications for FRUSEMIDE
Definition
Oedema associared with heart failure, hypertension,
Term
Kinetics of FRUSEMIDE
Definition
F=0.6, t1/2=1.5hrs, two-thirds renally cleared, rest glucuronidated.
Term
Dose of FRUSEMIDE
Definition
Start with 20mg OD, but doses of up to 1000mg daily by IV infusion are sometimes required (e.g. renal failure)
Term
Contra/precautions of FRUSEMIDE
Definition
Hypokalaemia, Na+ of H20 depletion, sulphonamide allergy, anuria, renal failure.
Term
Adverse effects of FRUSEMIDE
Definition
Postural hypotension, electrolyte imbalance, dehydration.
Term
Adverse effects of FRUSEMIDE
Definition
Postural hypotension, electrolyte imbalance, dehydration.
Term
Interactions of FRUSEMIDE
Definition
Additive or competitive (e.g. NSAIDs) effects.
Increases Li+ conc.
Increased toxicity of DIGOXIN, GENTAMICIN, and CEPHALOSPORINs.
Term
Class/mechanism of GENTAMICIN
Definition
Aminoglycaside antibiotic. Binds to 30s ribosome subunit-->impaired protein synthesis-->cell wall failure.
Term
Indications of GENTAMICIN
Definition
Infection with susceptible organisms. May include pseudomonas, E coli, proteus, gram -ve sepsis, and staphylococcus.
Synergist effect with penicillins e.g. in SBE.
Also transtympanic injection to obliterate vestibular sensation in intractable meniere's disease.
Term
Dose of Gentamicin
Definition
Only parenteral. Effect proportional to max conc. Effect reduced by frequent repeated dosing.
Usually 3-7mg/kg/day, once daily dosing.
Term
Kinetics of GENTAMICIN
Definition
F=0, t1/2=2.5hrs, mostly renal excretion.
Term
Contra/prec GENTAMICIN
Definition
Hypersensitivity, renal disease, vestibulo/cochlear problems, neuromuscular problems.
Term
Adverse effects of GENTAMICIN
Definition
Neuro-/Oto-/Nephrotoxicity. Plus others...
Term
Interactions of GENTAMICIN
Definition
Increases effect of neuromuscular blockers. Increased nephro-/ototoxicity eg by FRUSEMIDE, CEPHALOSPORINs.
Term
Class/mechanism of GLICLAZIDE
Definition
Oral antihyperglycaemic. Sulphonylurea. Stimulates insulin release by enhancing tranmembrane Ca+ transfer.
Term
Indications/dose for GLICLAZIDE
Definition
Treatment of non-insulin dependent diabetes mellitus (usually not obese people who would more commonly have METFORMIN)
Start 40-80mg/day. Increase to up to 320mg/day.
Term
Kinetics of GLICLAZIDE
Definition
F=extensive, t1/2=11hrs, clearance 80-90% CYP3A4.
Term
Prec/contra GLICLAZIDE
Definition
Hepatic impairment, hypersensitivy, type I diabetes, ketosis, acidosis, surgery.
Term
Class/mechanism of GYCERYL TRINITRATE (GTN)
Definition
Antianginal. Organic nitrate vasodilator.
Term
Indications for GLYCERYL TRINITRATE
Definition
Registered for treatment of angina pectoris and congestive heart failure.
Also noted: oesophageal spasm, raynaud's, anal fissures.
Term
Dosage/administration of GLYCERYL TRINITRATE in angina episode
Definition
2 puffs sublingually (0.4-0.8mg), if pain remains after 5minutes repeat, if remains after 10 minutes, repeat and call ambulance. Also available in sublingual tablets, as transdermal patches, and as infusion.
Important to have daily nitrate free period to prevent tolerance.
Term
Precautions/contra for GLYCERYL TRINITRATE (GTN)
Definition
Raised ICP, HOCM, hypovolaemia, inferior MI, glaucoma, SILDENAFIL...
Term
Interactions fo GLYCERYL TRINITRATE
Definition
Additive antihypotensive effects (including with SILDENAFIL).
GTN may reduce effectiveness of HEPARIN.
Term
Adverse effects of GTN
Definition
Postural drop, headache, weakness, 'dizzyness', reflex tachycardia-->arrythmia.
Term
Class/mechanism of HALOPERIDOL
Definition
Typical antipsychotic. Dopaminergic blockage through the CNS.
Term
Indications/dosage to HALOPERIDOL
Definition
Rx of chronic psychiatric disorders including schizophrenia, other psychoses and tourette's.
Acute management of delusional, confused, hallucinating states, and associated agitation and aggression.
Rarely as antiemetic or neurolepticanalgesia.
Acute dose 2-10mg, not more than 100mg/day.
Maintanence usually 1-15mg.
Available, oral, IM, IV, or IM depot.
Watch for arrythmias (long QT, TdPoint).
Term
Kinetics of HALOPERIDOL
Definition
Plasma t1/2 around 24hrs. Highly fat soluble. Both hepatic and renal clearance.
Term
Contra/prec for HALOPERIDOL
Definition
CNS or psych depression, parkinsonism, prolactin dependent tumours, long QT, syndrome, hypersensitivity incl neuroleptic-malignant syndrome, plus others.
Term
Adverse effects of HALOPERIDOL
Definition
Extra pyramidal (akathisia, parkinsonism, dystonia), hallucinations, tiredness, tardive dyskinesis. Rarely neuroleptic malignant syndrome.
Plus many other systems (CVS, haem, GI, resp, endo, derm, autonomic, ocular)
Term
Interactions of HALOPERIDOL
Definition
Kinetic via CYP3A4, 2D6.
Dynamic: many--see www.medsafe.govt.nz.
Term
Class/mechanism of HEPARIN
Definition
Anticoagulant; potentiates effect of antithrombin, plus neutralises other clotting factors.
Term
Indications/dose for HEPARIN
Definition
Treatment of arterial and venous thrombosis. Prophylaxis of VTE. Topically applied to blood-exposed tubing to maintain patency.
Unfractionated--monitored and titrated to appropriate APTT.
LMWH (ENOXAPARIN) more predictable. 20-40mg/day SC for prophylaxis. 1.5-2mg/kg/day for treatment.
Term
Kinetics of HEPARIN
Definition
Nil oral availability, saturable hepatic clearance.
Term
Contra/prec for HEPARIN
Definition
Uncontrolled bleeding. Thrombcytopenia. History of HEPARIN induced thrombocytopenia.
Term
Adverse effects of HEPARIN
Definition
Bleeding, easy bruising, HEPARIN induced thrombocytopenia.
Term
Class/mechanism of LIGNOCAINE
Definition
Local anaesthetic. Blockade of neuronal Na+ channels. (Also sometimes used for antiarrythmic effects--previously more common)
Term
Dose of LIGNOCAINE
Definition
By local injection, avoid intravascular injection, usually 20-100mg, side effects after 4-7mg/kg total dose.
Term
Kinetics/duration of effect for LIGNOCAINE
Definition
Highly lipophilic, plasma t1/2=1.6hrs.
Onset 2-5mins, peak around 20mins, effect lasts up to 1-2 hours.
Term
Symptoms/sign of LIGNOCAINE toxicity
Definition
Periocular tingling-->generalised parasthesia/twitching, hypotension, bradycardia, euphoria, drowsiness-->siezure-->coma-->death.
Term
Class/mechanism of METFORMIN
Definition
Oral antihyperglycaemic. Biguanide. Sensitises to insulin, rather than increases concentration. Exact mechanism not fully understood.
Term
Indications for METFORMIN
Definition
NIDDM when diet control has failed, or adjunct to insulin therapy. Especially in overweight people. (Also to enhance fertility in PCOS).
Term
Dosage of METFORMIN
Definition
Start 500mg BID, increase 500mg/week up to 2500mg. (Careful of renal function)
Term
Kinetics of METFORMIN
Definition
F=0.5, t1/2=2-6hrs, renal excretion.
Term
Prec/contra METFORMIN
Definition
Renal failure, and any other acute of chronic condition where lactic acidosis is likely.
Term
Adverse effects of METFORMIN
Definition
Nausea/GI upset ('METFORMIN BELLY'), lactic acidosis, (No reported hypoglycaemia)
Term
Class/Mechanism of METOPROLOL
Definition
B-adrenergic antagonist (B-blocker). Antihypertensive. Antianginal.
Term
Indications for METOPROLOL
Definition
Angina, hypertension, thyrotoxicosis, some tachyarrythmias, migraine.
Term
Dose of METOPROLOL
Definition
BETALOC (controlled release) available in 23.75,45.5,95,190mg. (use up to 190mg OD)
LOPRESSOR available in 50mg, 100mg and 200mg (daily dose up to 400mg).
Up to 20mg BETALOC as 20mL IV at 1-2mL/min for tachyarrythmias.
Term
Contra/Prec METOPROLOL
Definition
Asthma, peripheral vascular disease, bradyarrythmias, unstable heart failure.
Term
Adverse effects of METOPROLOL
Definition
Postural hypotension, bradycardia, cold peripheries, erectile dysfunction, lethargy, impaired concentration
Term
Interactions of METOPROLOL
Definition
Metabolism via CYP2D6, additive effects with Ca2+-blockers, digoxin.
Term
Class/mechanism of METRONIDAZOLE
Definition
Antimicrobial (esp some bacteria, and protazoa). Nitroimidazole. Causes breakdown of DNA helices.
Term
Indications/dose for METRONIDAZOLE
Definition
Infection with susceptible organisms. Especially anaerobes (e.g. infection from GI flora) and protazoa (giardia, trichomonas). Adult doses of 600mg-2000mg per day, often divided.
Term
Kinetics of METRONIDAZOLE
Definition
F=almost 1, t1/2=8.5hrs, hepatic metabolism via active metabolytes.
Term
Prec/contra for METRONIDAZOLE
Definition
Use of alcohol (disulphram reaction), CNS, hepatic, haem disease.
Term
Adverse effects of METRONIDAZOLE
Definition
Nausea, diarrhoea, vomiting, headache, rarely seizures (+other CNS),
Term
Interactions of METRONIDAZOLE
Definition
Ethanol (disulphram reaction), others via enzyme effects, e.g. WARFARIN, anticonvulsants...
Term
Class/mechanism of MORPHINE
Definition
Opiate analgesic. Agonist especially of mu-opioid receptors.
Term
Indications/dose for MORPHINE
Definition
Analgesia (when pain not controlled by lower level analgesics), surgery, off-licence use for relieving dyspnoea in terminal patients.
Available SC, PO, IV, IM and in rapid or slow acting formulations.
10-200mg divided through the day. Start low, titrate to pain, monitor for respiratory depression.
Term
Kinetics of MORPHINE
Definition
F=0.24, t1/2=2hrs, hepatic metabolism (with some active metabolytes).
Term
Precautions/contra for MORPHINE
Definition
Respiratory disease, head injury with chance of raised ICP, biliary colic.
Term
Adverse effects of MORPHINE
Definition
Respiratory depression, confusion, nausea, vomiting, constipation, bradycardia, hypotension.
Term
Treatment of MORPHINE overdose
Definition
NALOXONE and supportive cares.
Term
Class/mechanism of OMEPRAZOLE
Definition
Proton pump inhibitor (PPI). Reduces gastric acidity by inhibiting H+/K+ATPase in gastric parietal cells.
Term
Indications/dose for OMEPRAZOLE
Definition
Peptic ulcer disease, acid-related dyspepsia, reflux oesophagitis: 10-40mg OD.
Zollinger-Ellison syndrome 60-120mg TDS.
Term
Adverse effects of OMEPRAZOLE
Definition
angina, tachy-/bradycardia, rash, GI upset, renal disturbance.
Term
Class/mechanism of PARACETAMOL
Definition
Analgesic/antipyretic. Central COX inhibitor.
Term
Indications/dose for PARACETAMOL
Definition
First line analgesia for many forms of mild-moderate pain.
Also febrile illness.
PRN or regular up to 1g QID. (Children 15mg/kg QID)
Term
Kinetics of PARACETAMOL
Definition
F=almost 1, t1/2=2hrs, hepatic metabolism (with toxic intermediate metabolyte)
Term
Precautions/contra for PARACETAMOL
Definition
Glucose6Phosphate deficiency (causes haemolysis), and liver disease.
Term
Adverse effects of PARACETAMOL
Definition
All less than 1%.
Hypersensitivy, rash, hepatic and renal damage in OD.
(Recent NZ study linking heavy PARACETAMOL use to childhood asthma but no clear causal link)
Term
Class/mechanism of PENICILLIN
Definition
B-lactam antibiotic. Attaches to penicillin binding proteins (PBPs) in cell wall leading to degredation of wall and cell death.
Term
Indications/doses of PENICILLIN
Definition
Infection with susceptible organism. Most non-B-lactam producing Gram+, plus menigococcus, gonococcus, and spirochetes (eg syphillis).
PENICILLIN G (injectable) anything from 1.2g-24g daily, IV or IM (small doses only).
PENICLLIN V (oral) 1-3g daily (in 4-6 doses). Prophylaxis of RhFever, recurrent tonsillitis, or post splenectomy 250mg BD.
Term
Kinetics of PENICILLIN
Definition
F=0.6, t1/2=30min, mixed hepatic/renal excretion.
Term
Precautions/contr PENICILLIN
Definition
Allergy
Term
Adverse effects of PENICILLIN
Definition
Urticarial rash not uncommon, anaphalaxis rare, seizures at very high doses, can promote infection by non-susceptible organisms (candida, pseudomonas)
Term
Class/mechanism of PHENYTOIN
Definition
Anticonvulsant (and antiarrythmic). Blocks Na+ channels-->membrane stabilisation.
Term
Indications/dose of PHENYTOIN
Definition
Epilepsy, other seizure disorders, arrythmias.
200-400mg day orally for prophylaxis--saturable kinetics so slow increase!
Up to 1500mg/24hr to control active siezures.
Term
Kinetics of PHENYTOIN
Definition
F=0.9, t1/2=average 22hrs but saturable, hepatic metabolism.
Term
Interactions of PHENYTOIN
Definition
Power CYP inducer.
Increased conc with CYP inhibitors (AMIODARONE, FLUOXETINE, ANTIFUNGALs etc.)
Decreased conc with cyp inducers (CARBEMAZIPINE, RIFAMPACIN etc.)
Term
Prec/contra for PHENYTOIN
Definition
Pregnancy (but all antiepileptics are teratogenic, and seizures can harm foetus).
Bradycardia, heart block.
Sensitivity.
Term
Adverse effects of PHENYTOIN
Definition
CNS-tired,drowsy
GI-constipation, nausea, vomiting
Rarely hypotension, arrythmias, ataxia.
Term
Class/mechanism of PREDNISONE
Definition
Synthetic corticosteroid. Anti-inflammatory and immunosuppressive.
Term
Indications/doses of PREDNISONE
Definition
Replacement therapy in andrenal insufficiency. Inflammatory and autoimmune conditions including asthma, RA, temporal arteritis, PMR, ...
Lowest dose for shortest time to acheive result.
Adult doses of 5-80mg/day.
Term
Kinetics of PREDNISONE
Definition
F=0.8, t1/2=3.6hrs, metabolism via active metabolyte (PREDNISOLONE) by liver.
Term
Contra/precautions for PREDNISONE
Definition
Uncontrolled infection, osteoporosis, diabetes, peptic ulcer
Term
Adverse effects of PREDNISONE
Definition
Short term: immunosuppression-->infection, psychosis, glucose intolerance, electrolyte problems, physiological dependence.
Long term: Osteoporosis, cushings syndrome (diabetes, truncal obesity, buffalo hump, fluid retention etc.), cataracts, glaucoma, ...
Term
Class/mechanism for SALBUTAMOL
Definition
B2-adrenergic agonists. Bronchodilator.
Term
Indications/dose for SALBUTAMOL (not just the obvious)
Definition
Asthma, COPD, prevention of premature labour.
Metered dose inhaler, 100-400mcg doses, 1-2 PRN.
Also available as nebulisers and SR oral.
Term
Prec/contra for SALBUTAMOL
Definition
Hypersensitivity, hyperthyroidism, tachyarrythmias, diabetes.
Term
Adverse effects of SALBUTAMOL
Definition
Tachycardia, palpitations, tremor, anxiety, GI upset, CNS (stim or depr)...
Term
Interactions of SALBUTAMOL
Definition
B-blockers, increased effect with IPRATROPRIUM, increased toxicity with TCAs, MAOIs.
Term
Class/mechanism of SIMVASTATIN
Definition
Lipid lowering agent. Lowers LDL, icreases HDL. Inhibits HMG-CoA reductase, a rate limiting enzyme in the production of cholesterol.
Term
Indications/dose for SIMVASTATIN
Definition
Hypercholesterolaemia, prevention of CHD. Daily doses of 5-80mg in the evening with or without food.
Term
Kinetics of SIMVASTATIN
Definition
Metabolised via active metabolyte in Liver (CYP3A4)
Term
Prec/contra for SIMVASTATIN
Definition
Hypersensitivity, liver disease, pregnancy (teratogen).
Term
Interactions of SIMVASTATIN
Definition
Increased toxicity (-->rhabdomyolysis) with CYP3A4 inhibitors, e.g. GRAPEFUIT juice, macrolides, antifungals, protease inhibitors
Term
Adverse effects of SIMVASTATIN
Definition
myalgia-->myocytis-->rhabdomyolysis. Liver damage, Foetal abnormalities.
Term
Class/mechanism of VALPROATE
Definition
Antiepileptic, mood stabiliser. Increases GABA signalling, decreases glutamet signalling via complex mechanisms.
Term
Indications/Dose of VALPROATE
Definition
Epilepsy, bipolar affective disorder, (migraine prophylaxis--unregistered use)
1000-2000mg daily (divided doses), start lower.
Term
Kinetics of VALPROATE
Definition
F=0.95, t1/2=14hrs, hepatic metabolism (glucuronidation)
Term
Precautions/contra for VALPROATE
Definition
Liver disease, pregnancy (Neural tube defects--but seizures almost bad for mother and foetus)
Term
Adverse effects of VALPROATE
Definition
GI upset, disordered menstruation, other <1% eg drowsiness, liver damage, ataxia, rash
Term
Class/mechanism of WARFARIN
Definition
Coumarin anticoagulant. Prolongs prothrombin time (PT, INR) by preventing the reduction vit K, and thus the production of vit K dependent clotting factors 2,7,9,10.
Term
Indications/dose of WARFARIN
Definition
Treatment or long term prophylaxis of DVT/VTE. Prophylaxis of aterial thromboembolus in AF, or with artificial heart valves.
Maintanence dose usually 2-10mg/day, titrated to INR, usually 2-3 (3-4 with mechanical heart valves)
Term
Kinetics of WARFARIN
Definition
F=0.93, t1/2=40hrs, hepatic metabolism.
Term
Precautions/contra for WARFARIN
Definition
Pregnancy, haemorrhage, protein C deficiency (necrosis)
Term
Adverse effects of WARFARIN
Definition
Bleeding, foetal abnormalities, GI upset, alopecia, rarely agranulocytosis, skin necrosis.
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