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Action(s) and notes Inhibits breakdown of IP (Inositol Phosphate) to I --> prevents Inositol recycling --> no IP3 for PLC to act upon; can produce side effect of diabetes insipidus (see Thiazides) Inhibit receptor tyrosine kinases --> inhibit effects of epidermal growth factor (EGF) Agonist for cortisol (steroid) receptor Agonist for oestradiol (steroid) receptor Agonist for aldosterone (steroid) receptor Agonist for progesterone (steroid) receptor Causes Na channel to require more hyperpolarization to reactivate it (by stabilizing inactivated form) - thus increased inactivation; weak base; pH-dependent, use-dependent (only at high rates of stimulation) and voltage dependent; 'fast-in, fast-out' Dihydropyridine; acts as agonist for L-type VGCCs (- isomer), but blocker for T-type VGCCs (+ isomer) Group of compounds with actions on L-type VGCCs - both agonists and antagonists; "highly lipid-soluble, gain access to channel through lipid phase of membrane"
Uses
Covered In
and also
Manic Depression Neoplastic Growth Control (?) Asthma Treatment Contraception Aldosterone deficiencies Contraception
Hiley 12
Lignocaine
Edwardson 18 Hiley 37
Edwardson 20 Hiley 22
Edwardson 20
Drug
Uses
Covered In
and also
Nifedipine
Dihydropyridine; acts as antagonist for L-type VGCCs; binds preferentially to inactivated channels and so selective for smooth muscle
Glibenclamide
See Sulphonylureas
Verapamil Diltiazem
Antagonist for L-type VGCCs in cardiac muscle Antagonist for L-type VGCCs in cardiac muscle; Class: benzothiazepine; (Tolbutamide, Glibenclamide): Group of compounds that antagonise K(ATP) channel in beta cells of pancreas; induce entry of calcium via depolarisation, causing insulin release See Sulphonylureas Inhibits ACh release pre-synaptically Inhibits uptake of Choline into pre-synaptic nerve terminals, so limiting ACh synthesis Blocks ACh transport into vesicles presynaptically
Angina prevention by peripheral and coronary vasodilation; antihypertensive (see Peripheral Vasodilator Agents) Edwardson 20 Hiley 7, 22 Non-Insulin Dependent Diabetes Mellitus Edwardson 22 Class IV Antidysrhythmic (although has some Class I actions also); used also in treatment of chemotherapy resistance Edwardson 21 Hiley 22, 38; Barrand 40 Antidysrhythmic Edwardson 22 Hiley 22
Non InsulinDependent Diabetes Mellitus Edwardson 22 No longer used Edwardson 22 MurrellLagnado 10 MurrellLagnado 10 MurrellLagnado 10
Action(s) and notes Inhibits ACh release pre-synaptically Blocks CNS nAChRs
Uses
and also
Post-synaptic channel-pore blocker for nAChR, acts on autonomic ganglia; use-dependent Agonist for nAChR; When applied in large quantities, will act as a "depolarising block" Competitive antagonist for nAChR, acting on autonomic ganglia Agonist specific to muscarinic AChRs, resistant to hydrolysis in GI tract --> well absorbed Strong agonist for nAChRs, medium-strength for mAChRs Strong agonist for mAChRs, weak agonist for nAChRs
First effective antihypertensive agent, but no longer Murrellused Lagnado 11 MurrellLagnado 11 MurrellLagnado 11 MurrellLagnado 14 MurrellLagnado 14 MurrellLagnado 14 Can cross conjunctival membrane easily and therefore used in treatment of glaucoma Can be used to produce pupillary dilatation (mydriasis)
Pilocarpine
MurrellLagnado 14
Naturally occurring alkaloid, ANTagonist for muscarinic receptors Naturally occurring alkaloid, ANTagonist for muscarinic receptors Naturally occurring alkaloid, agonist for muscarinic receptors
Drug
Action(s) and notes Short-acting anticholinesterase (+ve charge --> binds to anionic site); main site of action: NMJ
Uses Diagnosis of Myasthenia Gravis Reversal of competitive neuromuscular block; Myasthenia Gravis treatment Glaucoma treatment (eye drops) Myasthenia Gravis treatment (longer lasting than Neostigmine)
Covered In MurrellLagnado 16
and also
Edrophonium
Thorn 5
Neostigmine
Physostigmine
Medium-duration anticholinesterase (binds to both active sites in AChE); acts on NMJ Medium-duration anticholinesterase (binds to both active sites in AChE); acts on parasympathetic N.S.
MurrellLagnado 16 MurrellLagnado 16
Thorn 5
Pyridostigmine Dyflos
Medium-duration anticholinesterase (binds to both active sites in AChE); acts on NMJ Long-duration anticholinesterase, actions can be reversed with pralidoxime; highly toxic
Long-duration anticholinesterase Long-duration anticholinesterase Dissociates dyflos (or any organophosphorus anticholinesterase) from cholinesterases
Gibson 10
Carbidopa
Inhibits dopa decarboxylase Metabolised to form -methylnoradrenaline, a "false transmitter" which is less active than noradrenaline on post-synaptic receptors, but more effective on pre-synaptics, inhibiting NT Methyldopa release. inhibits tyrosine hydoxylase, blocking NA -methyltyrosine synthesis
MurrellLagnado 20
MurrellLagnado 20 MurrellLagnado 20
Hiley 7
Drug Disulfiram
Uses
Covered In MurrellLagnado 21
and also
Binds to catecholamine recognition proteins on surface of vesicles, and thereby blocks accumulation of catecholamines in vesicles; acts Reserpine both centrally and peripherally Inhibit uptake 1 (neuronal uptake) of Tricyclic catecholamines --> accumulation of NA and 5Antidepressants HT at receptors, increased sympathetic nerve (e.g. imipramine) activity but main effect is on CNS Strong agonist for nicotinic and muscarinic Acetylcholine receptors; rapidly broken down by Acetylcholine cholinesterases throughout body Amitryptiline Imipramine See tricyclic antiderpressants See tricyclic antidepressants Inhibit uptake 1 (neuronal uptake) of catecholamines --> accumulation of NA and 5HT at receptors, increased sympathetic nerve activity but main effect is on CNS (same actions as tricyclic antidepressants)
MurrellLagnado 21
CNS
CNS
CNS CNS
Cocaine
MurrellLagnado 23 Peripheral vascular disease, treatment Murrellof Lagnado 23, phaeochromocytoma 28 MurrellLagnado 23 Treatment of Parkinson's Disease MurrellLagnado 23
CNS
Phenoxybenzami ne Corticosteroids
Entacapone
Inhibits uptake 2 (non-neuronal uptake) of catecholamines (as do corticosteroids); ANTagonist for adrenoceptors Inhibit uptake 2 (non-neuronal uptake) of catecholamines (as does phenoxylbenzamine) Inhibits COMT (which normally breaks down catechomaines (esp. adrenaline) in non-neuronal tissue)
Drug Sympathomimeti c Amines (e.g. amphetamine, tyramine, ephedrine and MDMA ('ecstasy'))
Uses
Covered In
and also
Structurally related to NA, taken up into presynaptic nerve terminals by Uptake 1; competes with NA for uptake into vesicles, and NA is thereby transported into synapse (as well as being broken down by MAO). Some also have Various (see direct effects on adr.receptors ephedrine)
MurrellLagnado 23
CNS
Ephedrine
Guanethidine Bretylium
Competes with NA for Uptake 1 ('neuronal'), so potentiating exogenously applied catecholamines; displaces NA from vesicle uptake and NA is thereby transported into synapse Related to guanethidine See sympathomimetic amines; found in cheese and red wine, and needs to be eliminated from diet when taking an MAO inhibitor to avoid fatal rises in blood pressure More active on adrenoceptors than receptors: has very low rates of stimulation on 2 receptors
Nasal decongestant (relaxes bronchial Murrellsmooth muscle) Lagnado 23 Chronic, low-dose usage--> released instead of NA, blocks neurons; large doses-> inhibits exocytosis by inhibiting vesicle Murrellfusion) Lagnado 23 Former Murrellantihypertensive Lagnado 23
Tyramine
MurrellLagnado 23 MurrellLagnado 28
Noradrenaline
Adrenaline
Anaphylactic reactions (very powerful vasopressor), acute More active on adrenoceptors than receptors cardiac failure
MurrellLagnado 28
Thorn 2
Drug
Uses Formerly used in asthma treatment but has tachycardia side effect
Covered In
and also
Isoprenaline
Phenylephrine Agonist specific to 1 receptors Methylnoradrenali ne Agonist specific to 2 receptors Topical (local) treatment of hypertension (centrally acting antihypertensive (?)); treatment of narcotic withdrawal syndromes Aerosolic, acute treatment of asthma Acute heart failure treatment
Clonidine
Agonist specific to 2 receptors, acts both by inhibiting pre-synaptic NA release and centrally also; sudden withdrawal of drug (e.g. missing single dose) can cause severe "rebound hypertension" Agonist specific to 2 receptors, produces bronchorelaxation when inhaled Agonist specific to 1 receptors; positive inotropic effect during cardiogenic shock
Hiley 7
Salbutamol Dobutamine
Thorn 5 Hiley 49
Phentolamine Yohimbine
Formerly used as antihypertensive but has tachycardia side Murrelleffect Lagnado 28 MurrellLagnado 28
Hiley 7
Drug
Uses
Covered In
and also
Prazosin
Propanolol
Atenolol Butoxamine
ANTagoinst for 1 receptors ("-blocker"); does not readily enter brain (used as counterargument for 'NA theory' of -blocker action) ANTagonist for 2 receptors
Causes relaxation of bladder neck smooth muscle, useful in urinary retention; antihypertensive (see Peripheral Vasodilator Agents) Hypertension (formerly), but bronchoconstriction side effects; Class I and Class II antidysrhythmic Reduces effects of exercise/excitement on heart; antihypertensive; Class II antidysrhythmic
MurrellLagnado 28
Hiley 7
MurrellLagnado 28
Hiley 4
MurrellLagnado 28 MurrellLagnado 28
Hiley 5
Labetolol
Ergotamine
Generalised ANTagonist for all adrenoceptors; 4 stereoisomers: 2 inactive (RS and SS), SR = blocker, RR = -blocker Partial adrenoceptor agonist; "ergot alkaloid", partial 5HT-1D receptor agonist, produces vasoconstriction
NOT used as antihypertensive: inactive isomers are not approved (potential for immune reaction), and postural hypotension is Murrellproblematic Lagnado 28 Acute treatment of migraines MurrellLagnado 28
Hiley 5
Thorn 4
Uses
and also
Complex range of actions on 5-HT adrenoceptors in CNS Attenuates the response of purinergic nerves to Suramin ATP ANTagonist for A1 (adenosine) receptors, Caffeine reducing presynaptic inhibition of NT release Nitrovasodilators Produce vasodilation via activation of Guanylate (Glyceryl Cyclase in smooth muscle cells; dilate large Trinitrate, conducting vessels in the heart, as well as Isorbide decreasing preload by venous dilation, and Dinitrate, Amyl decreasing BP by arteriodilation. Tolerance may Nitrate) develop Angina treatment Glyceryl Trinitrate See Nitrovasodilators Angina treatment
Isorbide Dinitrate See Nitrovasodilators Angina treatment Amylnitrate Release NO, promoting erection and relaxation of ('Poppers') the anal sphincter Prevents breakdown of cGMP by inhibiting PDE5, causing relaxation of smooth muscle and increasing bloodflow -> corpus cavernosum Erectile dysfunction
37 37 37 38
Hiley 43 Hiley 43
Sildenafil ('Viagra') L-arginine analogues (LNMMA, L-NAME, L-Inhibit NOS, but not very selective for different NOARG) forms of NOS Inhibits nNOS, but not eNOS and iNOS: affects 7-nitroindazole binding of arginine to NOS N-iminoethyl-LPotent and irreversible inhibitor of iNOS in ornithine activated macrophages
MurrellLagnado 38
Hiley 50
Drug
Action(s) and notes -blocker (partial agonist) with "intrinisic sympathetic activity"; antihypertensive but has no direct effect on renin-angiotensin system; however, can reduce renin release via 'orthostatic response') ANTagoinst for 1 receptors ("-blocker"); does not readily enter brain (used as counterargument for 'NA theory' of -blocker action)
Uses Antihypertensive; Class II antidysrhythmic; angina treatment Antihypertensive; Class II and Class III antidysrhythmic Antihypertensive; Class II antidysrhythmic; symptomatic heart failure treatment ('myocardial salvage') Antihypertensive Antihypertensive; treatment of congestive heart failure Antihypertensive; treatment of congestive heart failure Centrally acting antihypertensive Centrally acting antihypertensive
Covered In
and also
Pindolol
Hiley 4
Hiley 44
Sotalol
Hiley 5
Carvedilol Losartan
ANTagonist for receptors ("-blocker") but also for 1 receptors, with 1: potency ratio of 1:10 ANTagonist for A1 angiotensin receptors ACE inhibitor: decreases BP in 85% of primary hypertensives, but has little effect on patients with normal BP Precursor (prodrug) of enalaprilat, an ACE inhibitor (more potent than captopril); undergoes de-esterification to become enalaprilat More active on Imidazoline 1 (I1) receptors than 2 receptors; few side effects More active on Imidazoline 1 (I1) receptors than 2 receptors; few side effects Antihypertensives, but only used in conjunction with other antihypertensives: need -blockers as they tend to cause reflex increase in heart rate, and also not hugely effective alone as they lead to increase in sodium retention
Captopril
Hiley 6
Hiley 47
Hiley 47
Hiley 7
Drug
Action(s) and notes Dihydropyridine; L-type calcium channel ANTagonist; bind preferentially to inactivated channels and so selective for smooth muscle
Covered In
and also
Nicardipine
Hiley 7, 22
Inhibit binding of ATP to K(ATP) channel in vascular smooth muscle, causing it to open (ATP Antihypertensive normally causes it to close), leading to increased (see Peripheral potassium efflux, relaxing smooth muscle Vasodilator Agents) See K+ Channel Openers: active isomer is levcromakalim See K+ Channel Openers See K+ Channel Openers; thiazide See K+ Channel Openers Antihypertensive (see Peripheral Vasodilator Agents)
Hydralazine
Dilates arterioles: mechanism unknown Block Na/K/Cl channel in thick ascending Loop of Henle. Side effects: potassium loss may lead to arhythmia/dysrhythmia; competition for organic acid uptake in prox. con. tubule causes decreased uric acid secretion, may be problematic for gout sufferers Antihypertensive Loop diuretic; derivative of sulphonamides; Secreted into lumen of kidney by organic acid transport process of PCT, blocks Na/K/Cl cotranspoter in Thick ALH, increasing natriuresis and therefore urine flow. Also causes venodilatation See Loop diuretics
Hiley 8
Hiley 10
Antihypertensive; venodilatation means beneficial effects in congestive heart failure. See also Loop Diuretics Hiley 10 Antihypertensive Hiley 10
Action(s) and notes Diuretics; block Na/Cl cotransporter in distal convoluted tubule; inhibit dilute urine formation, but not concentrated; also has KCO actions vasodilator (see Diazoxide); side-effects same as loop diurs. + decreased insulin production See Thiazides
Uses Antihypertensive; can also be used to reduce urine production in diabetes insipidus
Covered In
and also
Probenecid
Allopurinol
Alloxanthine
Spironolactone
Canrenone
See Thiazides Uricosuric agent (enhances uric acid secretion); high dose GOOD as block uric acid reabsorption, low dose BAD as block uric acid secretion; Salicylates (e.g. asparin) reduce effectiveness of uricosuric agents Treatment of Gout Reduces uric acid production: competitive inhibitor of xanthine oxidase, and metabolised by xanthine oxidase to give Alloxanthine, a noncompetitive xanthine oxidase inhibtor Treatment of Gout Product of metabolism of allopurinol by xanthine oxidase; non-competitive inhibitor of xanthine oxidase Treatment of Gout Potassium-sparing Aldosterone ANTagonist; metabolised to diuretic (treatment Canrenone in the liver; slow-onset, limited by of side effects of turnover of sodium channels (as it loop downregulates their transcription) diuretics/thiazides) Potassium-sparing diuretic (treatment of side effects of Metabolite of Spironolactone; aldosterone loop ANTagonist (see also Spironolactone) diuretics/thiazides)
Hiley 13
Hiley 13
Hiley 13
Hiley 14
Hiley 14
Drug
Uses
Covered In
and also
Triamterene
Amiloride
Potassium-sparing diuretic (treatment of side effects of Epithelial Na Channel (ENaC) blocker, acts on loop cells of late distal tubule diuretics/thiazides) Potassium-sparing diuretic (treatment Epithelial Na Channel (ENaC) blocker, acts on of side effects of cells of late distal tubule; at higher concentration loop blocks Na/H exchanger diuretics/thiazides) Carbonic anhydrase inhibitor; prevents reabsorption of H2CO3 in proximal tubule but effects are short-lived; inhibition of HCO3 secretion in eye limits build-up of aqueous humour
Hiley 14
Hiley 14
Acetazolamide
First effective diuretic, but now rarely used; instead used in treatment of glaucoma Hiley 15
Used when GFR is reduced, to reduce Freely filtered by glomerulus, but not cerebral oedema reabsorbed: lower tubular Na concentration, and (and thus Osmotic Diuretics so decrease reabsorption. Do not enter brain or intracranial (Mannitol, the eye. Intravenous administration to promote pressure) and Isosorbide) rapid diuresis intraocular pressure Hiley 15 Non-selective A1/A2 adrenoceptor ANTagonist; as A1 receptor mediates afferent arteriole responses to increased GFR, has weak diuretic action; also phosphodiesterase inhibitor so useful in long-term asthma treatment
Theophylline
Thorn 5
Drug
Uses
Covered In
and also
Mibefradil Nickel (Ni++) Quinidine Procainamide Phenytoin Mexilitine Flecainide Encainide Amiodarone
Streptokinase
Anistreplase
Previously used as antihypertensive and antidysrhythmic, but withdrawn due to interfering with drug metabolism -> Blocks T-type and L-type VGCCs adverse interactions Hiley Blocks T-type and L-type VGCCs Hiley Protects against premature re-excitation and Class IA repolarisation of VGNaCs antidysrhythmic Hiley Protects against premature re-excitation and Class IA repolarisation of VGNaCs antidysrhythmic Hiley Protects against premature re-excitation and Class IB repolarisation of VGNaCs; rapid kinetics antidysrhythmic Hiley Protects against premature re-excitation and Class IB repolarisation of VGNaCs; rapid kinetics antidysrhythmic Hiley Protects against premature re-excitation and Class IC repolarisation of VGNaCs; slow-onset/offset antidysrhythmic Hiley Protects against premature re-excitation and Class IC repolarisation of VGNaCs; slow-onset/offset antidysrhythmic Hiley Inhibits repolarising potassium currents, Class III lengthening APD (action potential duration) antidysrhythmic Hiley Clot lysis for Binds to plasminogen, promoting its conversion emergency to the fibrinolytic protease plasmin, but with side treatment of effect of systemic thrombolysis myocardial infarct Hiley Clot lysis for Streptokinase given in combination with emergency anisoylated plasminogen to restrict systemic treatment of thrombolysis myocardial infarct Hiley
22 22 37 37 37 37 37 37 38 Barrand 40
40
40
Drug
Uses
Covered In
and also
Produced by the kidney and is converted into a two-chain plasminogen activator: synthetic forms include tcu-PA (cultured kidney cells) and scu-PA (recominant form), but no selectivity of fibrin over fibrinogen, so t-PA is normally used Urokinase (u-PA) instead Recombinant human tissue plasminogen activator; greater activity to plasminogen specific to fibrin, localising action to circulation, and not allergenic as they are derived from Alteplase human protein
Hiley 40
Clot lysis for emergency treatment of myocardial infarct Clot lysis for Recombinant human tissue plasminogen emergency activator with mutations in which three domains treatment of including Kringle domain have been deleted myocardial infarct Lys analogue; reverses fibrinolytic actions of clotbusting drugs in cases of overuse Lys analogue; reverses fibrinolytic actions of clotbusting drugs in cases of overuse; less toxic and longer lasting than aminocaprioc acid Group of mucopolysccharides which activate antithrombin III, which inactivates all serine Clot lysis, used in proteases involved in the blood coagulation addition to cascade fibrinolytic drugs Inhibits the actions of vitamin K, which is required for the production of factors in the Clot lysis: oral clotting cascade anticoagulant Nicotinamide nitrate, which may produce same therapeutic effects as nitrovasodilators, but without producing tolerance - combined nitrovasodilator and potassium channel opener
Hiley 41
Hiley 41 Hiley 41
Tranexamic acid
Hiley 41
Heparin
Hiley 41
Warfarin
Hiley 41
Nicorandil
Angina treatment
Hiley 43
Drug
Uses
Covered In
and also
Alprenolol
Attempted use of treating angina without causing side effects of heart failure, but not overly successful... Hiley 44 Attempted use of treating angina without causing side effects of heart failure, but not overly successful Hiley 44 Hypolipidaemic agent, INCREASES SURVIVAL Hiley 45 Hypolipidaemic agent, INCREASES SURVIVAL Hiley 46 Hypolipidaemic agent Hypolipidaemic agent
Xamoterol
Cholestyramine Clofibrate
Partial 1 adrenoceptor agonist Inhibits HMG-CoA reductase, which is the rate limiting enzyme for cholesterol synthesis; upregulates hepatic LDL receptors Inhibits triglyceride synthesis/VLDL secretion by liver; increases levels of t-PA, which lowers levels of lipoprotein A Ion exchange resin that remains in gut and prevents reuptake of bile acids, thereby limiting cholesterol absorption Fibric acid derivative: lowers VLDL and LDL, by stimulating lipoprotein lipase Stimulates production of PGI3 instead of PGI2 (little change), and TXA3 instead of TXA2 (far less pro-thrombotic), as eicopentanoic acid substitutes for arachidonic acid: reduced risk of thrombosis Block Na/K countertransporter, causing a shift in the starling curve of the heart (higher CO for given LVEDP); high toxicity, especially when hypokalaemic
Hiley 46 Hiley 46
Hiley 48
Drug
Action(s) and notes Inodilator: inhibits PDE3, inhibiting cGMP breakdown which --> positive inotropic/chronotropic effects Inodilator: inhibits PDE3, inhibiting cGMP breakdown which --> positive inotropic/chronotropic effects Inhibits PDE4 Inhibits PDE5 Endothelin Anatagonist IV Anaesthetic - see notes IV Anaesthetic - see notes
Uses Congestive Heart Failure (doesn't increase survival) Congestive Heart Failure (doesn't increase survival)
Covered In
and also
Amrinone
Hiley 50
Propofol Nitrous Oxide Cyclopropane Halothane Ether Methoxyfluorane Benzimidazoles (Fenbendazole, Thiabendazole, Triclabendazole) Fenbendazole Thiabendazole Triclabendazol
IV Anaesthetic - see notes; very rapidly metabolised so can be given as constant infusion General Anaesthesia GA 33 Inhalation anaesthetic with low solubility (so fast on/fast off) General Anaesthesia GA 35 Inhalation anaesthetic with low solubility (so fast on/fast off) General Anaesthesia GA 35 Inhalation anaesthetic with middling solubility Inhalation anaesthetic with high solubility (so slow on/slow off) Inhalation anaesthetic with high solubility (so slow on/slow off) Inhibit formation of helminth microtubules, by binding to -tubulin with high affinity; 250/400x affinity for helminth tubulin compared to mammalian See benzimidazoles See benzimidazoles See benzimidazoles; selective against flukes but ineffective against roundworms General Anaesthesia GA 35 General Anaesthesia GA 35 General Anaesthesia GA 35
Drug Proton Ionophores (Salicylanides, Substituted Phenols) Salyclanides (Closantrel) Substituted Phenols (Nitroxynil)
Action(s) and notes Uncouple oxidative phosphorylation (nonselectively cf. mammalian hence low t. index); bind avidly to plasma proteins -> especially blood-sucking helminth-effective; have further action at tegument membrane to lower pH See Proton Ionophores
Uses
Covered In
and also
Anthelmintic, selective to flukes Anthelmintic, selective to flukes Anthelmintic, selective to flukes Anthelmintic, selective to flukes Anthelmintic Anthelmintic, esp. effective against flukes; main drug used against schistosomiasis
Gibson 8 Gibson 8
See Proton Ionophores Inhibit glucose metabolism in helminths by Diamphenithide increasing malate concentration Inhibit phospoglycerate kinase/mutase; binds to Clorsulon plasma proteins Several possible MODAs: increase Ca influx causing paralysis, loss of suction, by acting on subunit of Ca channel; may act on CICR; may cause tegument damage leading to immunePraziquantrel mediated response Anticholinesterase; cause spastic paralysis of helminths allowing for expulsion from host; quite Organophosphoru dangerous (low therapeutic index) --> strict s compounds attention to dose; Pralidoxime = antidote for (Dichlorvos) recent toxicity Anticholinesterase; cause spastic paralysis of Carbamates helminths allowing for expulsion from host; (Aldicarb) Atropine can be used as antidote Agonise nAChRs, causing depolarisation, causing spastic paralysis allowing for rapid expulsion; Bell-shaped response due to open-channel Helminth blockade; especially potent against GI Nicotinic Agonists helmints/lungworms
Gibson 8
Anthelmintic
Gibson 10
Anthelmintic
Gibson 10
Anthelmintic
Gibson 11
Drug
Action(s) and notes See Helminth Nicotinic Agonists; water-soluble so easy to use; l-isomer of Tetramisole; most potent nic.agonist anthelmintic
Uses
Covered In
and also
Imidazothiazoles (Levamisole)
Anthelmintic
Gibson 11
See Helminth Nicotinic Agonists; water-insoluble so minimises side-effects on host (as not readily Tetrahydropyridin absorbed by GI tract), needs to be kept away es (Pyrantel) from water/sunlight to avoid isomerisation Anthelmintic Quaternary Ammonium Salts (Bephenium) See Helminth Nicotinic Agonists Anthelmintic Pyrimidines (Methyridine) See Helminth Nicotinic Agonists Anthelmintic Treatment of excess stomach acid Cimetidine H2 (Histamine) receptor antagonist secretion H1 (Histamine) receptor antagonist; CAN cross blood-brain barrier H1 (Histamine) receptor antagonist; DOES NOT cross blood-brain barrier Treatment of motion sickness/allergy Treatment of mild atopic asthma/allergy Treatment of allegry, used to cause drowsiness as side effect. Now used as SLEEPING TABLET Treatment of excess stomach acid secretion
Gibson 11
Gibson 11 Gibson 11
Thorn 2
Dimenhydrinate
Thorn 2
Loratidine
Thorn 2
Mepyramine
Thorn 2
Omeprazole
Terfanidine
Inhibits H+ pump in stomach parietal cells Thorn 2 H1 (Histamine) receptor antagonist; Blocks K+ Channels in heart (side effect); DOES NOT cross blood-brain barrier Treatment of allergy Thorn 2
Drug
Action(s) and notes NSAID - COX-inhibitor: acts by irreversible acetylation of serine-530; preferentially targets COX-1 over COX-2, so inhbits platelet aggregation (COX-2 endothelial but not found in platelets --> PGI2 sythesis can continue but not TXA2) Stable analogue of PGE1, increases mucus secretion etc. of GI tract NSAID - COX-2 inhibitor; side effect of causing heart attacks so now withdrawn
Uses
Covered In
and also
Aspirin
Misoprostol
Celecoxib
NSAID - COX inhibitor, slightly preferential for COX-1 NSAID - Mechanism of action still unclear, as antipyretic and analgesic effects but NOT antiParacetemol inflammatory (may be COX-3 inhibitor) Dihydroergotamin Ergot alkaloid - 5-HT1d agonist, produces e vasoconstriction Ibuprofen Sumatriptan Valproic Acid Ondansetron Granisetron 5-HT1D agonist, produces vasoconstricion Prevents GABA breakdown, increasing [GABA] 5-HT3 antagonist 5-HT3 antagonist 5-HT3 antagonist, side effect of reducing gut motility 5-HT4 agonist Corticosteroid - agonises glucocorticoid receptor to supress inflammation Mast cell stabiliser - inhibits degranulation (histamine release)
Antipyretic, analgesic, antiinflammatory, anticlotting Protects stomach from ulceration when using NSAIDs Antipyretic, analgesic, antiinflammatory Antipyretic, analgesic, mildly anti-inflammatory Antipyretic, analgesic Acute treatment of migraines Acute treatment of migraines Prevention of migraines Anti-emetic Anti-emetic Treatment of irritable bowel syndrome Increases gut motility Long-term asthma treatment Long-term asthma treatment
Thorn 3
Hiley 41
Thorn 3
Thorn 3
Thorn 3
Drug
Uses
Covered In
and also
Cortisone
Dexamethasone Etanercept
Methotrexate Monteleukast
Organ transplant, Corticosteroid - agonises glucocorticoid receptor treatment of to supress inflammation myasthenia gravis Organ transplant, Corticosteroid - agonises glucocorticoid receptor treatment of to supress inflammation myasthenia gravis Resembles TNF- receptor, so 'mops up' excess Treatment of TNF- rheumatoid arthritis Immunosuppression (myasthenia gravis treatment, organ Calcineurin Inhibitor transplant) Treatment of Interferes with neutrophil migration rheumatoid arthritis Muscarinic AChR antagonist, used to produce Acute treatment of bronchorelaxation asthma Treatment of Inhibits dihydrofolate reductase, inhibiting rheumatoid arthritis production of tetrahydrofolate which is required (low dose); cancer for nucleic acid synthesis; resistance derves from treatment (high low levels of dihydrofolate reductase dose) Leukotriene inhibitor (antagonist for CysLT1 and Long-term asthma CysLT2 receptors) treatment Organ transplant, treatment of myasthenia gravis; anticancer agent Corticosteroid - agonises glucocorticoid receptor (used against acute to supress inflammation, inhibits lymphocyte childhood proliferation leukaemia) Long-lasting 2 adrenoceptor agonist, produces Long-term asthma bronchorelaxation when inhaled treatment Treatment of Modifies lymphocyte behaviour rheumatoid arthritis
Thorn 5
Thorn 5 Thorn 5
Thorn 5 Thorn 5
Barrand 27
Barrand 25
Drug Zileuton
Uses
Covered In
and also
Binds to cytosolic protein, cytophilin, to create calcineurin inhibitory compound Inhibitor of cell proliferation Inhibitor of cell proliferation Inhibits viral attachment to cell surface receptor Prevents acidification of endosome after influenza endocytosis, so blocking entry of influenza A Binds to the 'prehairpin' complex which HIV uses to enter cell in gp120-CD4 interaction, so prevents HIV fusion with cell Nucleoside analogue, specific to DNA replication: inhibits nucleic acid synthesis Nucleoside analogue, specific to reverse transcriptase: inhibits nucleic acid synthesis; some toxicity to host cells Acyclic nucleoside phosphonate: inhibits nucleic acid synthesis Non-nucleoside reverse transcriptase inhibitor: inhibits nucleic acid synthesis
Long-term asthma treatment Thorn 5 Immunosuppression (myasthenia gravis treatment, organ transplant) Thorn 5 Organ transplant Thorn 5 Organ transplant Antiviral agent Antiviral agent (Influenza A) Thorn 5 Barrand 2
Amantidine
Barrand 3
Enfurvitide Acyclovir
Saquinavir
Polymyxins
Protease inhibitor: inhibits cleavage of viral proteins (required by virus to produce functional proteins) in final processing of new virions Antiviral agent Group of cyclic peptides - interfere with the cytoplasmic membrane of bacteria; bactericidal; limited use as interfere with mammalian cytoplasmic membrane also Antibacterial agent
Barrand 4
Barrand 7
Drug
Action(s) and notes Ionophore antibiotic - interferes with cytoplasmic membrane of bacteria; bactericidal; limited use as interfere with mammalian cytoplasmic membrane also Lipopeptide, disrupts bacterial membrane function; bactericidal; used in treatment of skin infections by gram positive bacteria Binds to ergosterol, causing pore formation in the fungal membrane (but poor selectivity against mammalian host; poor solubility) Binds to ergosterol, causing pore formation in the fungal membrane (but poor selectivity against mammalian host, so too toxic -> only used topically) Inhibits enzymes involved in ergosterol synthesis, altering the fluidity of the membrane, ultimately preventing fungal replication Inhibit conversion of L-Alanine to D-Alanine; DAlanine is essential component of bacterial cell wall (peptide side chain) -> inhibits bacterial cell wall synthesis Inhibits transglycosylation of peptidoglycan cell wall - inhibits bacterial cell wall synthesis; used if allergic to penicillin -lactam; binds PBPs that are important in transpeptidation of bacterial cell wall -> inhibits bacterial cell wall synthesis; resistant to lactamase activity, poor access across gram-ve outer membrane; mecA -> low resistance, femA/B/D -> high resistance
Uses
Covered In
and also
Nigericin
Antibacterial agent
Barrand 7
Daptomycin
Antibacterial agent
Barrand 7
Amphotericin B
Antifungal agent
Barrand 8
Nystatin
Antifungal agent
Barrand 8
Fluconazole
Antifungal agent
Barrand 8
Cycloserine
Vancomycin
Antibacterial agent
Barrand 10
Methicillin
Antibacterial agent
Barrand 10
Drug
Action(s) and notes -lactam; binds "penicillin binding proteins" that are important in transpeptidation of bacterial cell wall -> inhibits bacterial cell wall synthesis; resistant to -lactamase activity, "broad spectrum" Binds the 50S ribosomal subunit and prevents complex formation, thereby inhibiting bacterial protein synthesis Bind the 30S ribosomal subunit and prevents tRNA interaction during bactrial protein synthesis; only protein synthesis inhibitor that is bacteriocidal rather than bacteiostatic Binds the 30S ribosomal subunit and inhibits peptide bond formation Binds the 30S ribosomal subunit and inhibits peptide bond formation Binds the 50S ribosomal subunit and inhibits peptide bond formation; resistance involves transformation via acetyltransferase Interacts with the 50S subunit to prevent translocation -> inhibits bacterial protein synthesis Structural analogues of PABA, and therefore act as 'alternative substrates' for DHPS (DiHydroPteroate Synthase), thereby inhibiting tetrahydrofolic acid synthesis and thereby inhibiting nucleic acid synthesis Competitively inhibits DHFR (DiHydroFolate Reductase), thereby inhibiting tetrahydrofolic acid synthesis and thereby inhibiting nucleic acid synthesis Trimethoprim and sulphamethoxazole given in conjunction; inhibits nucleic acid synthesis Inhibit bacterial RNA polymerase
Uses
Covered In
and also
Ampicillin
Antibacterial agent
Barrand 10
Linezolid
Antibacterial agent
Barrand 13
Chloramphenicol
Antibacterial agent
Barrand 13
Ertythromycin
Antibacterial agent
Barrand 13
Sulphonamides
Barrand 14
Drug
Uses
Covered In
and also
Ciprofloxacin
Example of a QUINOLONE -> group of compounds that bind and inactivate DNA gyrase Antibacterial agent Prodrug, which during activation affects mycolic acid synthesis -> production of free radicals, to which Mycobacterium tuberculosis is very sensitive (but resistance develops rapidly)
Barrand 14
Isoniazid Pyrazinamide
Pyrimethamine
Chloroquine
Antitubercular agent Barrand 15 Interfere with nucleic acid synthesis in Plasmodia (malaria) by blocking plasmodial DHFR (DiHydroFolate Reductase) Antimalarial agent Barrand 16 Inhibits heme polymerase (produced by malaria), thereby interfering with Plasmodium life cycle (but leads to increase in heme concentration which can be toxic, and now has widespread resistance) Antimalarial agent Barrand 16 Inhibits heme polymerase, thereby interfering with Plasmodium life cycle (but leads to increase in heme concentration which can be toxic, and now has widespread resistance) (?) Antimalarial agent Anti-estrogen, used in treatment of breast cancer (has a range of agonist and antagonist effects) Anticancer agent Inhibit synthesis of estrogens from androgens, so used in treatment of breast cancer Salvages normal tissues from folate depletion when being treated with high doses of methotrexate Antimetabolite - Metabolised to produce 'fraudulent' nucleotide, fDUMP, which inhibits DNA synthesis
Mefloquine
Barrand 16
Barrand 26
Anticancer agent
Barrand 26
Leucovorin
Anticancer agent
Barrand 27
5-fluorouracil
Anticancer agent
Barrand 28
Drug
Uses
Covered In
and also
Antimetabolite - incorporated (in its phosphorylated form) into DNA/RNA -> main action of inhibiting DNA synthesis; side effects: Cytarabine nausea/vomiting Etopocide Topoisomerase II inhibitor Camptothecins Topoisomerase I inhibitor Nitrogen mustard -> DNA intercalator; but can have side effect of producing secondary mutatiions due to alkylated guanine erroneously Melphalan pairing with thymine Prodrug that upon heptaic conversion is used to produce cytotoxic nitrogen mustard -> has exposed Cl- that is released in neutral/alkaline Cyclophosphamid pH, and reacts with guanines in DNA, so e inhibiting DNA replication Cross-link DNA, inhibiting DNA replication; Mitomycin preferential action in hypoxic conditions Nitrosourea - bind guanines at the O6 position, inhibiting DNA replication; can cross blood-brain Carmustine barrier
Anticancer agent
Barrand 32
Barrand 31 Barrand 32
Anticancer agent
Barrand 32
Cisplatin
Platinum complex, exchanges Cl- for nucleophilic groups to give intercalating agent -> inhibits DNA synthesis; resistance derives from elevated cellular levels of DNA repair enzymes Anticancer agent Non-covalently intercalates with DNA, no selectivity of tumour over normal except cells are more rapidly dividing; severe side effect of carditoxicity due to generation of free radicals in cardiac tissue (limited by encapsulation) Anticancer agent Non-covalently intercalates with DNA, no selectivity of tumour over normal except cells are more rapidly dividing; modified version of doxorubicin without cardiotoxic side-effects Anticancer agent
Barrand 32
Doxorubicin
Barrand 34
Mitoxantone
Barrand 34
Drug
Action(s) and notes Anti-mitotic agent (vinca alkaloid): prevents formation of the mitotic spindle and arrests cell in metaphase; disrupts the balance between microtubule assembly and dissembly Anti-mitotic agent: prevents formation of the mitotic spindle and arrests cell in metaphase; disrupts the balance between microtubule assembly and dissembly Small molecule kinase inhibitor Humanised monoclonal antibody against the EGF receptor Blocks growth receptor autophosphorylation Matrix metalloproteases inhibitor, limiting metastasis Endogenous inhibitor of angiogenesis Blcoks angiogenic proteins secreted by tumour cells -> inhibits angiogenesis
Uses
Covered In
and also
Vincristine
Anticancer agent
Barrand 36
Anticancer agent Anticancer agent Anticancer agent Anticancer agent Anticancer agent Anticancer agent Anticancer agent