Final Pharm Flashcards
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Dobutamine
Directly acting adrenoceptor agonist - beta 1 selective. Stimulates cardiac contraction without major effect on HR (+ve inotrope). Treats heart block, half-life 2mins (rapid metabolism by COMT), lacks isoprenaline’s reflex tachycardia.
Digoxin
Cardiac glycoside used to slow HR in atrial fibrillation (-ve chronotrope, +ve inotrope) and for heart failure in patients still symptomatic following diuretics and ACE-Is. Narrow therapeutic index.
Atenolol
Beta-1 selective beta-blocker used to treat angina, post MI, dysrhythmias, CHF, hypertension. Not safe for asthmatic patients.
Diltiazem + verapamil
Rate limiting/slowing Ca channel blockers (cardiac and smooth muscle actions). -ve inotropic effect Verapamil > Diltiazem. Ca be used to control/correct dysrhythmias. Verapamil is a Phenylalkaylamine, Diltiazem is a Benzothiazepine. Can double Carbamezepine levels (anti-convulsant/mood stabiliser).
Enalapril + captopril
ACEI - reduces preload and afterload. Used for hypertension, HF, post-MI, diabetic nephropathy, progressive renal insufficiency, high CVD risk.
Losartan
Angiotensin receptor blocker (ARB/AIIA). Antagonist of AT1 receptors. Hypertension as alternative to ACEIs with less side effects, CHF in patients who cannot tolerate ACEIs.
Nicorandil
K channel opener and Organic nitrate that stimulates guanylate cyclase to cause vasodilation. Used for angina, acute and chronic HF, BP control during anaesthesia. Adverse effects - hypotension and headache.
Bendrofluazide
aka bendroflumethiazide. Thiazide diuretic. Inhibit Na and Cl reabsorption in early distal tubule. Increases Na/Cl, K and Mg loss, Ca reabsorption. Moderate increase in urine volume. Used for HF, hypertension, severe resistant oedema, idiopathic hypercalciuria, nephrogenic diabetes insipidus. Side effect - inhibits insulin secretion (DM)
Spironolactone
Potassium sparing diuretic/aldosterone receptor antagonist. Acts in the distal convoluted tubule. Small increase in urine volume and Na loss. Used for primary and secondary hyperaldosteronism. Side effects - gynaecomastia, menstrual disorders, hyperkalaemia.
Amiodarone
Wide spectrum anti-arrhythmic used for supraventricular and ventricular tachyarrhythmias. Prolongs cardiac action potentials. Adverse effects - accumulation in body (long half life) causes photosensitive skin rashes, hypo-/hyper-thyroidism, pulmonary fibrosis, corneal deposits, Neuro and gastro disturbances. Potent inhibitor of Phenytoin (antiepileptic) metabolism.
Glyceryl trinitrate
Organic nitrate that releases NO into smooth muscle causing vasodilation. Often given sublingually for rapid relief of angina - short half life ~5mins. Via transdermal patch gives longer action. Prolonged use associated with tolerance.
Minoxidil
Anti hypertensive vasodilator that also slows/prevents hair loss. Potassium channel opener causing hyperpolarisation.
Doxazosin
Competitive Alpha-1 adrenoceptor blocker -> antihypertensive and coronary vasodilator but associated with increased rates of CHF by ALLHAT study. Can induce postural hypotension.
Sumitriptan
5HT-1D receptor agonist. Constricts large arteries and inhibits trigeminal nerve transmission. Used to treat migraines - contraindicated if have coronary disease.
Streptokinase
Thrombolytic - converts plasminogen to plasmin (natural fibrin protease). Bacterial product hence tolerance develops after first admin. Used in the treatment of MI.
Alteplase
Thrombolytic - converts plasminogen to plasmin (natural fibrin protease). Recombinant plasmin activator. Used in the treatment of acute MI and ischaemic stroke. Must be given within 12 hrs symptom onset.
Warfarin
Anticoagulant - Vitamin K antagonist. Long delay of onset (~5days) narrow therapeutic window, unpredictable pharmacokinetics and numerous drug interactions. Protein binding interactions most clinically significant with warfarin. Phenytoin (antiepileptic) increases clearance.
Heparin
Anticoagulant - activates Antithrombin-III (LMWHs also inhibit factor Xa). Short half life ~1hr, LMWHs longer.
Aspirin
Antiplatelet activator - irreversible non-specific cyclo-oxygenase inhibitor (but binds COX-1 more avidly) - prevents platelet production of thromboxane A2. At higher doses also inhibits endothelial COX preventing production of protective prostacyclin PGI2 (COX-2). Major side effects - gastric irritation + ulceration, bronchospasm in asthmatic (pseudoallergy), prolonged bleeding times, nephrotoxicity. Can displace other drugs from albumin increasing their free conc. Preferentially absorbed in stomach (acid pH) but majority in gut.
Analgaesic - inhibiting prostanoid (PG) synthesis prevents sensitisation of nociceptors thus increases threshold for pain.
Clopidogrel
Antiplatelet activator - ADP/P2Y receptor antagonist.
Abciximab
Antiplatelet activator - Glycoprotein IIb/IIIa receptor antagonist. GPIIb/IIIa receptor plays important role in platelet aggregation. Used for treatment of thrombotic disorders.
Simvastatin
HMG-CoA reductase inhibitor. Lipid lowering drug. Used to treat dyslipidemia and to prevent CVD. Grapefruit juice inhibits cytochrome P450 thus inhibits metabolism. Side effects - rhabdomyolysis.
Ibuprofen
Typical non-selective NSAID. Inhibits COX reversibly. Has anti-inflammatory, analgesic and anti-pyretic actions.
Celecoxib
Selective COX-2 inhibitor. Get fewer ulcers than with non-selective NSAIDs. Increased risk to CVS however - MIs
Mannitol
Osmotic diuretic - inert, filtered but not reabsorbed, decreases water reabsorption. Clinically used to prevent acute renal failure, decrease intra-cranial and ocular pressures. Side effects - increases ECF volume, hyponatraemia.
Acetazolamide
Carbonic anhydrase inhibitor - acts on the proximal tubule to prevent reabsorption of HCO3 and Na. Weak diuretic. Clinical used for renal stones, metabolic alkalosis and to decrease intra-ocular pressure. Unwanted - K loss and met. acidosis
Frusemide
Aka furosemide - Loop diuretic. Blocks the Na/Cl/K transport in the ascending limb of loop of Henle. Decreases the osmolarity of the medullary interstitium hence reduced concentrating power of collecting duct. Leads to a large increase in urine volume, Na, Cl, K, Ca and Mg loss. Clinical uses - oedema, moderate hypertension, hypercalcaemia, hyperkalaemia. Unwanted effects - hypovolaemia, hypotension, metabolic alkalosis (K loss)
Amiloride
Potassium sparing diuretic - aldosterone-sensitive Na channel inhibitor. Prevents Na reabsorption from the early distal tubule - increases Na and uric acid loss but H retention. Small increase in urine volume. Clinical uses - combine with K losing diuretics. Unwanted effects, hyperkalaemia, metabolic acidosis.
Promethazine
Anti-emetic. Competitive antagonist at histaminergic (H1), cholinergic (M), and dopaminergic receptors (D2). Acts centrally (labyrinth, NTS, VC) to block activation of vomiting centre. Used to treat/prevent - motion sickness, labyrinth disorders (Meniere’s), hyperemesis gravidarium, pre- and post-operatively. Unwanted effects - dizziness, tinnitus, fatigue, sedation, excitation in excess, convulsions, anti-muscarinic effects.
Metoclopramide
Anti-emetic, dopamine receptor antagonist (D2). Acts centrally CTZ and in GIT (increases gastric motility and emptying). Care must be taken with bioavailability of co-admin oral drugs. Uses - uraemia, radiation sickness, GIT disorders, chemotherapy. Side-effects - drowsiness, dizziness, anxiety, extrapyramidal reactions (children), hyperprolactinaemia, galactorrhoea, menstrual disorders. Note - no anti-psychotic actions.
Hyoscine
Anti-emetic, muscarinic receptor antagonist. Acts centrally esp in vestibular nuclei, NTS, VC to block VC activation. Uses - prevent motion sickness (little effect once nausea established), pre-op medication (sedation). Side-effects - drowsiness, dry mouth, cycloplegia, mydriasis, constipation (at higher doses)
Ondansetron
Anti-emetic, 5HT3 receptor antagonist. Blocks visceral afferent transmission and CTZ. Uses - preventing chemotherapy induced vomiting, radiation sickness, post-op nausea. Side effects - headache, flushing sensation, increased large bowel transit time (constipation).
Metronidazole
Antibiotic active against anaerobic bacteria and Protozoa. Used against H. pylori as part of triple therapy with clarithromycin and a PPI. Interferes with alcohol metabolism.
Amoxycillin
Broad spectrum beta-lactam antibiotic useful against sensitive bacteria. Used against H. pylori as part of triple therapy along with clarithromycin and a PPI, depending on pattern of local resistance.
Clarithromycin
Macrolide antibiotic - inhibits translocation of bacterial tRNA. Used against H. pylori as part of triple therapy along with a PPI and either metronidazole or amoxycillin. Can also be used with a H2 receptor antagonist and bismuth.
Omeprazole
Proton pump inhibitor. Irreversible inhibitor of H/K ATPase. Inhibits basal and stimulated gastric acid secretion from parietal cells by >90% Uses - component of triple therapy against H. pylori, peptic ulcers resistant to H2 antagonists, reflux Oesophagitis, with NSAIDs to limit gastric side effects.
Cimetidine + ranitidine
Histamine type 2 receptor antagonists - inhibit gastric acid secretion by ~60%. Relapses likely after withdrawing treatment. Cimetidine inhibits CYP 450 and hence can decrease metabolism of other substances.
Sucralfate
Cytoprotective drug - polymer containing aluminium hydroxide and sucrose octasulphate. Forms gel-like complex in stomach that coats and protects gastric ulcer. May cause constipation and reduce absorbance of other drugs.
Bismuth chelate
Cytoprotective drug sometime used in triple therapy.
Misoprostol
Cytoprotective drug - stable prostaglandin analogue that mimics the action of locally produced prostaglandins to maintain the gastroduodenal mucosal barrier. May be co-prescribed with chronic NSAIDs use. Side effects - diarrhoea, abdominal cramps, uterine contraction (do not use in pregnancy!)
Prednisolone + Fluticasone
Glucocorticoid. Powerful anti-inflammatory and immunosuppressive. Used for symptomatic treatment of active IBD and to prevent relapse. Drug of choice to induce remission of Crohn’s but declining use for Ulcertive colitis. Chronic systemic use associated with Cushing Syndrome.
Budesonide
Glucocorticoid that is degraded locally, limiting its systemic effects. Powerful anti-inflammatory and immunosuppressive. Given topically for Crohn’s disease and associated with less side effects that prednisolone.
Sulfasalazine + mesalazine (5-ASA)
Aminosalicylates - anti-inflammatory but not immunosuppressive. Used to treat active ulcerative colitis and maintain remission. Ineffective in treating active Crohn’s disease but may help maintain surgically-induced remission. Topical delivery, pH-dependent capsules or slow release microspheres used to control site of absorption. Superior to topical steroids for inducing Ulcerative colitis remission.
Azathioprine
Immunosuppressant used to maintain remission for both UC and CD. Can be used to induce CD remission. Prodrug activated by gut flora to 6-mercaptopurine which interferes with purine biosynthesis, DNA synthesis and cell replication. Side effects - bone marrow suppression. Metabolised by xanthine oxidase - allopurinol inhibits this hence leads to accumulation -> blood disorders.
Ipratropium Bromide
Muscarinic receptor antagonist (anticholinergic) used in asthma/obstructive airway disease to dilate the airways.
Salbutamol
Aka ventolin. Directly acting sympathomimetic / beta-2-adrenergic receptor agonist. Synthetic catecholamine derivative with relative resistance to MAO and COMT. Used to treat asthma (relax bronchial smooth muscle and inhibit release of bronco constrictor substances from mast cells) and to prevent premature labour (i.v.) Side effects - reflex tachycardia, tremor, hyperthyroidism and diabetes.
Morphine
Opiate (alkaloid derived from poppy). Tertiary nitrogen = analgesia. Poor lipid solubility. Metabolised by liver to morphine-6 glucuronide (more potent analgesic) and excreted in urine. Pharmaco effects - analgesia, euphoria, sedation, respiratory depression, cough suppression, nausea and vomiting, pupillary constriction, constipation, histamine release -> bronchoconstriction and hypotension.
Heroin
Aka diamorphine is essentially a prodrug rapid converted to morphine and 6-monoacetylmorphine. Has greater lipid solubility than morphine thus crosses the blood brain barrier more rapidly when injected i.v. More likely to cause dependence than i.v. Morphine.
Codeine
More readily absorbed by oral route than morphine, but has ~20% analgesic properties. 5-10% converted by demethylation to morphine (analgesic effects). Causes little or no euphoria and rarely addictive, however same degree of resp depression (seldom problem however). Causes constipation and has marked anti-tussive effect.