OSCE Drugs Flashcards
Aluminium Hydroxide? (Maalox) Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Antacid
Mechanism of action - Neutralises HCl in gastric secretions to form AlCl and water. Also inhibits action of pepsin by increasing pH.
Indication - Dyspepsia
Pharmacokinetics - 17-30% if absorbed. Rapidly eliminated by the kidneys.
ADR’s: Constipation, hyperalbuminaemia, avoid in hepatic and renal impairment.
Contraindications - hypophosphatemia, infants, neonates
DDI’s - ACE Inhibitors, Aspirin, Certain antibiotics, Bisphosphonates, Digoxin, Folate acid, etc…Can be avoided by not taking at same time as other drugs.
Gaviscon (Compound Alginate) Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Antacids - alginate
Mechanism of action - Raft antacid
Indication - Dyspepsia
Pharmacokinetics
ADR’s - Nausea, constipation, diarrhoea, headache
Contraindications - Intestinal Obstruction, Preterm neonates, or where excessive fluid loss is likely.
DDI’s - Most drugs - don’t take them at the same time. Some risk of hyperkalaemia which certain drugs e.g. ACE inhibitors, Cyclosporine. May damage enteric coating designed to prevent dissolution in the stomach. Not to be used with thickening agents.
Hyoscine Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Ach antagonist - anti-spasmodic, Anti-emetic
Mechanism of action - Direct antagonist of muscarinic cholinergic receptors
Indication - Motion Sickness
Pharmacokinetics - Oral or patch - effects usually last 12 hours, bioavailability 10-50%. Half Life 4.5 hours. Excreted poorly by kidney.
ADR’s - dry mouth, urine retention, constipation, loss of accommodation - photophobia, skin dryness/flushing, transient bradycardia, urinary urgency.
Contraindications - GI obstruction, Intestinal atony, Myasthenia gravis, paralytic ileus, severe UC, pyloric stenosis, bladder outflow obstruction, urinary retention. Acute MI, tachycardia, diarrhoea, elderly, GORD
DDI’s -other anti-muscarinic agents - increased side effects
Mebeverine Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Anti-spasmodic
Mechanism of action - synthetic anti-cholinergic - direct action on smooth muscle of GI tract.
Indication - Releive colicky like pain associated with IBS
Pharmacokinetics - rapidly and completely absorbed. Metabolised completely.
ADR’s - allergic reaction - angioedema, rash, urticaria
Contraindications - paralytic ileus
DDI’s- ???
Ranitidine Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - H2 Antagonist
Mechanism of action - Antagonist of H2 receptor on parietal cells - prevents release of protons.
Indication - Dyspepsia, H. Pylori infection, GORD, Peptic ulcer disease
Pharmacokinetics - 50% bioavailability, hepatic metabolism, excretion in urine.
ADR’s -Diarrhoea, dizziness, headache, (rare - cholestatic jaundice, bradycardia, psychiatric symptoms, thrombocytopenia)
Contraindications -
DDI’s - Histamine, absorption of a select number of drugs
Omeprazole, Lansoprazole, esomeprazole Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Proton Pump Inhibitors
Mechanism of action - Antagonise PPI on parietal cells to reduce acid secretion.
Indication - Dyspepsia, H. Pylori Infection, GORD, Peptic ulcer disease
Pharmacokinetics - prodrug which is converted to active form in acid environment of the stomach. Has no effect elsewhere in the body
ADR’s - risk of SLE, abdo pain, constipation, diarrhoeas, flatulence, GI disturbances, headache, nausea and vomiting
Contraindications
DDI’s - Lots affects plasma concentrations.
Monitoring - measurement of serum Mg before and during prolonged PPI treatment.
Loperamide Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Anti-motility
Mechanism of action - opioid receptor agonist acting on Mu receptor in the mesenteric plexus, does not affect CNS. Prolongs transit time of intestinal contents, reduces daily faecal volume, increases viscosity and bulk density.
Indication - Acute and chronic diarrhoea, Faecal incontinence,
Pharmacokinetics - No significantly absorbed from the gut. Hepatic metabolism and excretion of unchanged loperamide and metabolites is via faeces.
ADR’s - dizziness, flatulence, headache, nausea. Rare - paralytic ileus, Steven-Johnson syndrome.
Contraindications - Acute UC, antibiotic associated colitis, abdominal distension
DDI’s - Desmopressin
Ispaghula (Husk) Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Bulk Laxative
Mechanism of action - Increases the insoluble fibre in the gut, this helps to form solid faeces which distends the gut which activates the stretch receptors and increase gut motility.
Indication - Constipation
Pharmacokinetics - Not absorbed by body, excreted via faeces.
ADR’s - Flatulence, abdominal distension, GI impaction, GI obstruction, hypersensitivity
Contraindications - GI adhesions/ulcerations - May cause intestinal obstruction, Difficulty swallowing.
DDI’s - may delay GI absorption of certain drugs/vitamins and minerals
Senna Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Stimulant Laxative
Mechanism of action - converted by bacteria in the intestine to active form. Stimulated motility, inhibition of water and electrolyte absorption.
Indication - Constipation
Pharmacokinetics - Onset 8-12 hours, excreted in faeces.
ADR’s - Abdominal cramp
Contraindications - Intestinal Obstruction
DDI’s - Can get hypokalaemia with long term abuse or with other drugs that induce hypokalaemia e.g. diuretics.
Lactulose Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Osmotic Laxative
Mechanism of action - Lactulose is broken down into lactic acid in gut. This increases osmotic pressure and slightly acidifies colonic contents. This increases stool water content and softens stool. (Draws out ammonia in hepatic encephalopathy)
Indication - Constipation (hepatic encephalopathy)
Pharmacokinetics - can take up to 48 hours to act. No absorbed from GI tract. Faecal elimination.
ADR’s - Abdominal discomfort, cramps, flatulence, nausea, vomiting.
Contraindications - Galactosamia, intestinal obstruction, lactose intolerance
DDI’s - Coumarins (anticoagulant) - enhanced effect
Movicol Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Macrogols - osmotic laxative
Mechanism of action - Increased stool volume which triggers colon motility via neuromuscular pathwyas.
Indication - Constipation, faecal impaction
Pharmacokinetics - 2-4 days to get full relief. Eliminated in faeces not absorbed.
ADR’s - Abdominal distension, abdominal pain, flatulence, nausea
Contraindications - Intestinal obstruction, crohns disease, intestinal perforation, paralytic ileus, toxic megacolon, UC.
DDI’s
Glycerol Suppositories Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Irritant Laxative
Mechanism of action - promotes peristalsis and evacuation of the lower bowl
Indication - Constipation
Pharmacokinetics - Suppository
ADR’s - Can cause irritation and abdominal cramps
Contraindications - hypersensitivity to glycerol
DDI’s - none known
Phosphate enemas Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Bulk Laxative
Mechanism of action - Increased fluid accumulation in the lower bowel produces distension and promotes peristalsis and bowel movement by activating stretch receptors.
Indication - Constipation, Bowel evacuation before abdominal radiological, endoscopy, surgical procedures.
Pharmacokinetics - absorption minimal - can get hyperphosphataemia though.
ADR’s - Abdominal distensions, abdominal pain, nausea, vomiting, dehydration, dizziness, headache (can cause electrolyte disturbances, arrhythmias, renal failure)
Contraindications - with Oral use - acute severe colitis, ascites, congestive heart failure, GI obstruction, GI perforation, toxic mega colon. By rectal route: conditions association with increased colonic absorption, GI obstruction, inflammatory bowel disease.
DDI’s - Other oral drugs should be taken one hour before or after administration of phosphate enema.
Monitoring - Assess renal function in patients at risk of fluid and electrolyte disturbances.
Mesalazine Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - DMARD - sulphasalazine
Mechanism of action - Inhibits proliferation of T cells by causing T cell apoptosis. This inhibits interleukin 2 production and reduced chemotaxis and degranulation of neutrophils.
Indication - Irritable Bowel Disease - acute attacks and remission
Pharmacokinetics - Metabolised in the gut. Poorly absorbed as main action is within the intestine.
ADR’s - Myelosupression, hepatitis, rash, blood disorders, lupus, Stevens-Johnson syndrome, exacerbation of symptoms of colitis.
Contraindications - Hepatic impairment, monitoring required in renal disease
DDI’s - Preparations that lower stool pH e.g. Lactulose - may prevent release of mesalazine
Infliximab Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - DMARD - anti-TNF agent
Mechanism of action - An anti-human tumour necrosis factor monoclonal antibody. Binds to TNF-alpha and its receptors. This which reduces inflammation by decreasing the cytokine cascade and therefore recruitment of leukocytes to the area.
Indication - IBD, RA (with methotrexate), Ankylosing spondylitis, Psoriatic arthritis (with methotrexate) Plaque psoriasis.
Pharmacokinetics - Onset of action occurs in about 2 weeks in crohn’s. Removed by opsonisation via the reticulo-endothelial system.Half life 9.5 days.
ADR’s - Increased risk of malignancy in those who have has previous malignancy, risk of serious infections, skin/soft tissue infections. TB reactivation
Contraindications - Moderate or severe heart failure, severe infections.
DDI’s - Vaccines Clozapine, Abatacept, Anakinra
Should screen for TB before starting treatment.
Digoxin Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Cardiac Glycoside
Mechanism of action - Blocks the Na+/K+ ATPase exchanger in the myocardium. This causes Na+ to accumulate within the cell and reverses the Na+/Ca2+ exchanger. Ca2+ accumulates in the cell which may promote the activation of contractile proteins.
Indication - Heart Failure, AF,
Pharmacokinetics - Needs a loading dose - 3-5 day half life. Hepatic metabolism but doesn’t depend on CYP. Excreted mainly unchanged in urine.
ADR’s - Arrhythmias, blurred vision, conduction disturbances, diarrhoea, dizziness, oosinophilia, nausea, rash, vomiting, yellow vision.
Contraindications - Constrictive pericarditis, hypertrophic cardiomyopathy, intermittent heart block, second degree AV block,
DDI’s - Acetazolamide, Amphotericin, Beta blockers, calcium salts, Colestipol, Colestryamine, Corticosteroids, Diuretics - loop and thiazide, NSAIDS, Sucralfate, Suxamethonium, Tizanidine
Bendroflumethiazide Indapamide Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Diuretic
Mechanism of action - Acts on the Na+/Cl- Co transporter in the distal tubule to prevent Na+ reabsorption which in turn prevents water reabsorption.
Indication - Hypertension, Oedema
Pharmacokinetics
ADR’s - Altered plasma lipid concentrations, gout, hypercalcamia, glycaemia, uricaemia. Hypokalameia, -magnesaemia, -natraemia. Postural hypotension.
Contraindications - Addison’s, hypercalcaemia, hyponatraemia, refractory hypokalaemia, symptomatic hyperuricaemia. Avoid in sever live disease.
DDI’s - amiodarone, Amphotericin, Antidiabetics, Calcitriol, Ciclosporin, Colecalciferol, Colestryamine, Corticosteroids, Loop Diuretics, Flecainide, Lidocaine, Lithium, Beta 2 sympathomimetics, Vit D.
Furosemide Bumetanide Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Loop Diuretic
Mechanism of action - Inhibit reabsorption from the ascending limb of loop of Henle by blocking the sodium-potassium-chloride cotransporter.
Indication - Oedema (Heart Failure/Liver disease/Renal Disease), Resistant Hypertension.
Pharmacokinetics - 60% absorbed, excreted in the urine, half life of 2 hours.
ADR’s - Ototoxic, Hyponatremia, postural hypertension, electrolyte disturbances, gout, Hypokalaemia. Myelosupression.
Contraindications -Anuria, Comatose and Pre-comatose states related with liver cirrhosis, renal failure due to nephrotoxic/hepatotoxic drugs. Sever Hypokalaemia, severe hyponatremia.
DDI’s - Phenytoin, Aminoglycosides, Amiodarone, Amphotericin, Anti-diabetics, Aspirin, cardiac glycosides, Corticosteroids, Flecanide, lidocaine, lithium, polymixins, sympathomimetics beta 2. Vancomycin.
Amiloride Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Diuretic
Mechanism of action - Inhibits ENaC channels in DCT/CD - K+ sparing. Block Na+ transport channels.
Indication - oedema, potassium conservation when used with thiazide/loop diuretics
Pharmacokinetics - Not metabolised by the liver but excreted unchanged by the kidneys. Half life 6-9 hours.
ADR’s - Abdo. pain, agitation, arrhythmias, encephalopathy, GI bleeding, Jaundice, Postural hypotension, raised intra ocular pressure,
Contraindications - Addison’s, anuria, hyperkalaemia.
DDI’s - ACE inhibitors, ARB Antagonists, Cyclosporine, Lithium, NSAIDS, Potassium salts, Tacrolimus
Spironolactone Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Potassium Sparing Diuretics - Aldosterone antagonist.
Mechanism of action - Acts on aldosterone receptors and blocks the action of aldosterone. Prevents expression of ENac, K+ and Na+/K+ ATPase channels. This prevents the reabsorption of Na+ in the distal tubule and collecting trunks.
Indication - Oedema, Nephrotic Syndrome, Resistant hypertension, Conn’s syndrome. Can be used in combination with thiazide or loop diuretic to reduce K+ excretion.
Pharmacokinetics - completely absorbed orally and strongly bound to proteins. Induces hepatic CYP450.
ADR’s - gastric upsets, peptic ulcers, gynaecomastia in male patients and menstrual abnormalities in females. Hyperkalaemia, nausea, lethargy and mental confusion.
Contraindications - Addison’s anuria, hyperkalaemia
DDI’s - Potassium supplements, ACE Inhibitor, ARB antagonist, Aspirin, Digoxin, Trimethoprim
Adenosine Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Anti-Arrhythmic
Mechanism of action - slows AV conduction and can interrupt re-entry pathways through AV node. It is an endogenous nucleoside and activates cell surface A1 and A2 adenosine receptors. Vasodilation of smooth muscle.
Indication - Rapid reversal of Supraventricular tachycardia, stress test radionuclide myocardial imaging.
Pharmacokinetics - rapidly metabolised by phosphorylation or deamination. Half life is less than 10 seconds.
ADR’s - angina, apprehension, arrhythmia, AV block, dizziness, dyspnoea, flushing, headache, nausea, sinus pause.
Contraindications - Asthma, COPD, decompensated heart failure, long QT, 2nd/3rd degree heart block, sick sinus syndrome, severe hypotension.
DDI’s - Aminophylline (Diuretic) caffeine citrate, Dipyridamole (anti-platelet) Nicotine, Theophylline
Amiodarone Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Class III antiarrhythmic
Mechanism of action - K+ channel blockers - prolongation of phase 3 of the action potential. Increases refractory period and slows down intra-cardiac conduction. Relaxation of vascular smooth muscle - reduction of afterload.
Indication - Ventricular and supraventricular arrhythmias. VF
Pharmacokinetics - Long half life
ADR’s - Bradycardia, jaundice, Pulmonary fibrosis, Hepatic Injury, Increased LDL Cholesterol, Hypo and hyperthyroidism, Photosensitivity
Contraindications - Severe conduction disturbances, SA heart block, sinus bradycardia, thyroid dysfunction
DDI’s - EVERYTHING - Tricyclic antidepressants, Beta blockers, Cimetidine, Coumarins, Citalopram, Digoxin, Loop and thiazide diuretics etc.
Flecanide Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - IC antiarrhythmic
Mechanism of action - Blocks Na+ channels when they are in the active position which prevents after-depolarisations.
Indication - SVT, paroxysmal AF, Ventricular arrhythmias
Pharmacokinetics - Nearly complete oral absorption, Hepatic metabolisms, urinary excretion
ADR’s - Asthenia, dizziness, dyspnoea, fatigue, fever, oedema, pro-arrhythmic effects, visual disturbances
Contraindications - Abnormal left ventricular function, atrial conduction defect, bundle branch block, Valvular disease, heart disease, MI,
DDI’s - Amiodarone, Tricyclic antidepressants, Beta blockers, Cimetidine, Thiazide and Loop Diuretics, Fluoxetine, Verapamil
Lidocaine Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class- IB Antiarrhythmic
Mechanism of action - Na+ channel blocker -stimulation threshold during diastole raised. Fast Na+ channels inactivated so more difficult to initiate AP.
Indication - Antiarrhythmic, local anaesthetic/regional block, CPR (if no Amiodarone available)
Pharmacokinetics - Completely absorbed following parental administration. Hepatic metabolism. Excreted by the kidney.
ADR’s - Bradycardia, confusion, dizziness, drowsiness, paraesthesia, resp. depression. confusion, hypotension, anaphylaxis. Can be avoided with topical administration.
Contraindications - AV block, Myocardial depression, SA disorders, No preparations with preservative for caudal, epidural or spinal block.
DDI’s - cimetidine, HIV drugs, Loop and thiazide diuretics, propranolol,
Atenolol
Bisoprolol
Propanolol
Sotalol
Class - Beta Blockers
Mechanism of action - Antagonist of the Beta 1 Receptors in the SA and AV node. Prevention of Activation of Gs GPCR protein results in less Ca2+ entry so decreased force of contraction. Reduced HR.
Indication - Hypertension, Angina, Heart Failure, prevention of MI, arrhythmias
Pharmacokinetics - Vary depend on drug. Hepatic metabolism. Propranolol complete absorption and urinary secretion. half life 4 hours. Atenolol and bisoprolol 50% faeces 50% renal excretion. Bisoprolol longest half life at 9-12 hours.
ADR’s - Bradycardia, dizziness, bronchoconstriction. dyspnoea, exacerbation of Raynauds, fatigue, GI disturbances, peripheral vasoconstriction, sexual dysfunction, hyper/hypo glycaemia.
Contraindications - Verapamil injection, bradycardia, asthma, hypotension, pheochromocytoma, Prinzmetals angina, 2nd/3rd degree heart block.
DDI’s - adrenaline, Adrenergic Neurone blockers, Alpha blockers, Amiodarone, Anti-arrhythmic, Diltazem, dobutamine, Flecainide, ??? Be careful of hypotension!
Doxazosin Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - alpha adrenoceptor antagonist
Mechanism of action - Antagonises the alpha-1 adrenoceptor on vascular smooth muscle to prevent vasoconstriction.
Indication - hypertension, benign prostatic hyperplasia
Pharmacokinetics - 65% absorbed. Hepatic metabolism, urinary elimination. Half like of 22 hours.
ADR’s - Anxiety, back pain, dyspnoea, fatigue, influenza like symptoms, paraesthesia, sleep disturbance, vertigo.
Contraindications - History of micturition syncope or postural hypotension.
DDI’s -Boceprevir (antiviral)
Tadalafil (antihypertensive)
Lisinopril Ramipril Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - ACE Inhibitors
Mechanism of action - competitive inhibitors of angiotensin converting enzyme to prevent the conversion of angiotensin I to angiotensin II - prevent RAAS activation
Indication - Hypertension, Hypertension, prophylaxis after MI, prevention in CHD,
Pharmacokinetics - Ramipril 50-60% absorption, Hepatic metabolism, also renal metabolism to active metabolite. Lisinopril - 25% absorption excreted unchanged by kidneys.
ADR’s - hypotension, dry cough, angioedema, renal failure, hyperkalaemia.
Contraindications- Pregnancy, Reno-vascular hypertension.
DDI’s - Alskiren (renin inhibitor), ARB, Been venom extracts, diuretics, Everolimus, Lithium, Potassium salts, sodium aurothiomalate (gold for RA), wasp venom extracts
Losartan Candesartan Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Angiotensin II Receptor Antagonists
Mechanism of action - Antagonise angiotensin II receptors to prevent the action of angiotensin II (and activation of RAAS)
Indication - Hypertension, LV Hypertrophy, heart failure, MI, prevention of CHD, Diabetic Nephropathy in type II diabetes.
Pharmacokinetics - Lorsatan - bioavailability of 33%, hepatic metabolism, 35% eliminated in urine, 60% faeces.
Candesartan - bioavailability 15%, eliminated unchanged in urine and faeces.
ADR’s - Hyperkalaemia, angioedema, hypotension
Contraindications - ?
DDI’s - rifampicin, ACE inhibitors, Alskiren, Ciclosporin, Diuretics, Lithium, potassium salts,
Glyceryl Trinitrate Isosorbide Mononitrate Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Nitrates
Mechanism of action - Converted to NO - activates guanylate cyclase pathway with produces cGMP which activates a series of protein kinase dependent reactions (dephosphorylate myosin light chain kinase) resulting in the relaxation of smooth muscle cells and vasodilation. Venodilation reduces preload on the heart and therefore myocardial oxygen demand.
Indication - angina pectoralis - prophylaxis and treatment, medical procedures, anal fissure.
Pharmacokinetics - isosorbide Mononitrate - 100% absorption, hepatic metabolism, excretion via urine. Half life 5 hours. GTN - as above half life is only 3 minutes.
ADR’s - Headache, nausea and vomiting, Dizziness, postural hypotension, tachycardia. Paradoxical bradycardia.
Contraindications - Aortic stenosis, Cardiac tamponade, cardiomyopathy, hypovolaemia, anaemia, Increased ICP.
DDI’s - Heparins, antihypertensive’s
Amlodipine Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - DHP calcium channel blockers.
Mechanism of action - Target L Type Calcium channels. Inhibits initial influx of calcium in smooth muscle so calcium induce calcium release is prevented and the muscle does not contract. Also work on myocardium and reduce contractility.
Indication - Hypertension, Angina
Pharmacokinetics -Almost completely absorbed. Hepatic metabolism, renal excretion. Half life 30-50 hours.
ADR’s - Postural hypotension, dizziness, confusion, SNS activation , tachycardia palpitations, flushing, sweating, headache, oedema, gingival hyperplasia.
Contraindications - cardiogenic shock, significant aortic stenosis, unstable angina
DDI’s - Grapefruit Juice, Lomitapide, Sildenafil, Simvastatin, St Johns Wort, Telaprevir
Diltiazem Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Benzothiazepines Calcium channel blockers
Mechanism of action - Prevent calcium transport across the myocardial and smooth muscle. Prolongs action potential and effective refractory period. Peripheral vasodilation and a reduction in cardiac preload and myocardial contractility.
Indication- Angina
Pharmacokinetics
ADR’s -Bradycardia, Can worsen heart failure, dizziness, GI disturbances, hypotension, oedema
Contraindications - acute porphyria’s, LV failure, 2nd/3rd degree heart block, sever bradycardia, sick sinus syndrome
DDI’s - Amiodarone, Tacrolimus, Sirolimus, Simvastatin, Rifampacin, Oheyntoin, Lurasidone, Lomatapide, Ivabradine, Ibrtinab, Fosphenyoin, Dronedarone, Digoxin, Colchicine, Ciclsporine, Carbamazepine, Bosutinin, Beta blockers, Avanfil, Atazanir.
Verapamil Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Phenylakylamines - Calcium channel blocker(Class IV antiarrhythmic agent)
Mechanism of action - depresses SA node and slows down AV node conduction. Impedes calcium transport across the membrane. Peripheral vasodilation reduction in cardiac preload.
Indication - hypertension, angina, cluster headache prophylaxis, SVT
Pharmacokinetics - 90% absorption, Hepatic metabolism, Urine and faeces elimination. Half life 3-7.5 hours.
ADR’s - Constipation, Bradycardia, reduction in cardiac contractility can worse heart failure. dizziness, flushing, headache, nausea, vomiting.
Contraindications - Acute porphyria’s, AF with accessory conducting pathways, bradycardia, cardiogenic shock, history of heart failure. 2nd/3rd degree heart block
DDI’s - Amiodarone, Theophylline, Sirolimus, Simvastatin, St. Johns Wort, Rifampacin, Oheyntoin, Lurasidone, Lomatapide, Lenalidomide, Ivabradine, Ibrtinab, Flecainide, Fingolimod, Everolimus Dronedarone, Disopyramide, Dabigatran, Digoxin, Colchicine, Ciclsporine, Carbamazepine, Bosutinin, Beta blockers, Avanfil, Atovastatin, GA, aminophylline.
Warfarin Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class -Anticoagulant (Coumarin)
Mechanism of action - Vitamin K antagonist. (Competitive inhibition) Vitamin K needed for addition of Gla domains on clotting factors. Gla domains required for localisation of clotting factors.
Indication - prevention of ischaemic stroke in AF, venous embolism, thromboembolism, prevention of clot formation in patients with prosthetic heart valve, TIA
Pharmacokinetics - Good GI absorption, slow onset, half life 48 hours, Heavily protein bound to albumin, Hepatic metabolism. Metabolites excreted in urine.
ADR’s - Bleeding, Intracranial haemorrhage, epistaxis, Gi loss, Teratogenic. Hepatic dysfunction, jaundice.
Contraindications - if
Fondaparinux, apixiban, Edoxaban Bivalirudin, Dabigatran, desirudin. Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Anticoagulant
Mechanism of action - activates anti-thrombin III. Prevents the formation of a clot. Deactivates factor Xa, IIa, IXa.
Indication - When quick acting anticoagulation is required. DVT/PE. Cover. Thrombophylaxis.
Pharmacokinetics - Poor GI absorption given by injection. Removed by reticulo-endothelial system.Half life 1.5 hours. LMWH - given subcut.
ADR’s - Bruising/Bleeding, at injection sites, GI loss, epistaxis. Thrombocytopenia. Hyperkalaemia (inhibition of aldosterone secretion).
Contraindications -Bacterial endocarditis, after major trauma, haemophilia, peptic ulcer, recent cerebral haemorrhage, thrombocytopenia.
DDI’s - Aspirin, GTN spray,
Monitoring - aPPTq
Protamine Sulphate Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Reversal of Heparin Therapy
Mechanism of action - Dissociates heparin from anti-thrombin III
Indication - Active bleeding from heparin.
Pharmacokinetics
ADR’s - allergy/Anaphylaxis, bradycardia, hyper/hypotension, pulmonary oedema.
Contraindications - allergy to fish
DDI’s - ?
Aspirin Class Mechanism of action Indication Pharmacokinetics ADR's Contraindications DDI's
Class - Anti-platelet and analgesic, anti-inflammatory, antipyretic.
Mechanism of action - Cyclooxygenase 1 and 2 inhibitor (irreversible) - prevents the production of prostaglandin - activate nociceptors in neurones at site of injury. Prevents production prostaglandin and thromboxane A2 in platelets - prevents aggregation.
Indication - Prevention in CHD, Acute injury, Inflammatory conditions, TIA, CVA, AF,
Pharmacokinetics - Good rapid absoption, highly bound to albumin, Metbaolised in liver excreted in urine.
ADR’s - Blood disorders, GI haemorrhage, Gi irritation, Skin reactions, tinnitus, bronchospasm.
Contraindications - Peptic ulcer disease, bleeding disorders, Reye’s syndrome, haemophilia, sever cardiac failure.
DDI’s - SSRI’s, Acetazoloamide, Coumarins, Methotrexate, NSAIDS, Phenindione, Venlafaxine
