Drugs MVST IB - part 1

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Can you name the drugs from MVST IB - part 1?

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DescriptionDrug nameUse
Cholinergic agonist - not selective between nicotinic/muscarinic receptors
Calcium sensitiser - increases cardiac Ca2+ binding efficiency to troponin - inhibits phosphodiesterase III
ACE inhibitor - prodrug, must be metabolised in liver
Double chain recombinant human tissue plasminogen activator
Single chain recombinant human tissue plasminogen activator
Selective alpha-1 agonist (some action on beta-1)
Non-selective phosphodiesterase inhibitor
Selective antagonist for M1 muscarinic receptors
Glucocorticoid receptor antagonist
Reverse inhibition of AChE by organophosphorus agents
Selective beta-2 agonist (slight effect on beta-1)
Depolarising blocker at NMJ
Selective non-depolarising neuromuscular blocking agent at NMJ - long action, not hydrolysed
Progestagen receptor agonist
Inhibits HMG-CoA reductase - also many pleiotropic effects
Blocks transporter carrying ACh into storage vesicles
ADP-ribosylates alpha-s - inhibits GTPase activity - sustained activation of adenylyl cyclase
Blocks release of neurotransmitter via phospholipase A2 - localises to membrane by K channel binding moiety
K channel opener - also NO donor
Binds to SNAREs involved in membrane fusion, preventing ACh release
Inhibits intestinal absorption of cholesterol - circulates enterohepatically
COMT inhibitor
Non-selective phosphodiesterase inhibitor
Competitive inhibitor of tyrosine hydroxylase
Illegal drug - blocks NET
Non-specific endothelin receptor antagonist
Causes development of new blood vessels
Non-selective alpha-adrenoceptor antagonist
Irreversible antagonist at nicotinic NMJ receptors (no effect on ganglionic receptors)
Selective alpha-2 agonist
Selective antagonist for M3 muscarinic receptor
Reversible anticholinesterase - ionic interaction
Calcium channel antagonist - dihydropyridine - affects L-type but not T-type channels
Beta-adrenoceptor agonist
Angiotensin II partial agonist
Acts on imidazoline receptors
Arteriolar vasodilator - unknown mechanism
Local anaesthetic - uncharged
Inhibits platelet activation by inhibiting binding of ADP to its receptor on platelets
Selective MAO-B inhibitor
Cholinergic agonist - +-isomer hydrolysed by AChE
Mineralocorticoid receptor antagonist - potassium-sparing diuretic
Competitive antagonist for ganglionic nicotinic receptor - inactive at NMJ
Estrogen receptor agonist
NSAID used to prevent thrombosis
Converted to alpha-methylNA - released as false transmitter - more potent at alpha-2, less potent at alpha-1
Blocks Na channels from exterior - no use-dependence
Carbonic anhydrase inhibitor
alpha-1 antagonist most commonly used
Irreversible anticholinesterase - organophosphorus agent
Competitively inhibits plasminogen activation - inhibits severe bleeding from excessive clot lysis
Selective inhibitor of phosphodiesterase type V (selectively breaks down cGMP)
DescriptionDrug nameUse
Irreversible anticholinesterase - activated by replacement of sulphur atom with oxygen, deoxified by plasma carboxylesterases
Inhibits liver triglyceride production and VLDL secretion - increases levels of tissue plasminogen activator
Estrogen receptor antagonist
Blocks transport of adenosine into cells - phosphodiesterase type V inhibitor
Binds to neurexins, causing massive ACh release from nerve terminals
Blocks If current in SA node
Intracellular tetravalent polyamine - helps produce inward rectification of K+ channels
Osmotic diuretic - filtered at glomerulus, not reabsorbed
PPAR-gamma agonist
K channel opener
Irreversibly alkylates muscarinic receptor
Indirectly-acting sympathomimetic amine - weak inhibitor of MAO
Local anaesthetic - weak base - use-dependence and voltage-dependence
Interferes with normal function of microtubule growth
Binds to synaptobrevin to prevent vesicle release from inhibitory interneuron synapses with motor neurons
Glucocorticoid receptor agonist
Cardiac glycoside - inhibits Na/K-ATPase
Calcium channel blocker - phenylalkylamine - class IV antidysrhythmic
Nitrovasodilator - produces NO - metabolised in liver to active drug
Potassium-sparing diuretic - blocks apical Na+ channels in late distal tubule
Blocks uptake of choline into neurons
Tricyclic antidepressant - blocks NET
Cyclic heptapeptide inhibitor of glycoprotein IIb/IIIa receptor
Co-released with NA or ACh - acts on purinoceptors (P2 > P1)
Non-selective, reversible MAO inhibitor
Use-dependent block of ganglionic transmission
Combined alpha- and beta-adrenoceptor antagonist
Beta-1 antagonist used in heart failure
ACE inhibitor
Selective beta-2 antagonist (slight effect on beta-1)
Mineralocorticoid receptor agonist
Orally-acting hypoglycaemic agent - sulphonylurea
Selective inhibitor of NOS in neurons
Local anaesthetic (ester, weak base) - broken down by BuChE
Selective alpha-1 antagonist (slight effect on alpha-2)
Slightly selective alpha-2 agonist (also alpha-1 actions) - omitting dose can lead to rebound hypertension
Muscarinic receptor agonist
Immunosuppressant drug with antiproliferative effects
Selective alpha-2 antagonist (slight effect on alpha-1)
Competitively inhibits plasminogen activation - inhibits severe bleeding from excessive clot lysis
Non-peptide inhibitor of glycoprotein IIb/IIIa receptor
Loop diuretic - blocks Na/K/2Cl transport in thick ascending limb
Inhibits clotting by inhibiting synthesis of factors II, VII, IX, IX and regulatory proteins C, S, Z
Selective MAO-A inhibitor
Beta-1 antagonist used in heart failure
Tyrosine kinase inhibitor
Nitrovasodilator - produces NO - taken sublingually
Partial agonist at alpha-adrenoceptors - 5-HT agonist
Anion exchange resin - prevents reuptake of bile acids from intestine
SSRI - blocks 5-HT transporter in Uptake 1
Depolarising blocker selective for ganglion nicotinic receptor
Inodilator used to treat canine dilated cardiomyopathy - calcium sensitiser
DescriptionDrug nameUse
Non-selective agonist for muscarinic receptors
Blocks release of NA evoked by APs (repeated low doses/aftermath of large dose) - indirect sympathomimetic actions (large doses)
Monoclonal antibody against glycoprotein IIb/IIIa receptor - prevents platelet aggregation - also binds to vitronectin receptor
Calcium channel blocker - benzothiazepine
Phosphodiesterase III inhibitor - inodilator
Involved with providing new blood flow to ischaemic tissues
Indirectly acting sympathomimetic amine - converted to octopamine by DBH - found in various foodstuffs
Depolarising blocker selective for NMJ nicotinic receptor - very short duration of action, broken down by BuChe - deficiency in enzyme activity can lead to prolonged action
Plasminogen + anisoylated streptokinase
Uncompetitive inhibitor of phosphatase acting on IP1 --> inositol
Thiazide diuretic - blocks Na/Cl transport in early distal tubule
Potent, irreversible inhibitor of iNOS in activated macrophages
Inhibits DOPA decarboxylase in periphery
Binds very tightly to VMAT-2, preventing loading of catecholamines into vesicles
Class IC antidysrhythmic
Mild partial beta-1 agonist
NOS inhibitor - not very selective for different forms
Acts on imidazoline receptors
Non-peptide angiotensin II antagonist - acts on AT1 receptors
Binds to plasminogen activator, increasing generation of plasmin
Direct acting vasodilator - metabolised to NO or cyanide
Selective beta-1 antagonist (slight effect on beta-2)
Naturally occurring anticoagulant produced by basophils/mast cells - exposes active site of antithrombin III
Nicotinic receptor antagonist - relatively non-selective between NMJ and ganglion at clinical doses
K channel opener
Regulates expression of multiple angiogenic genes
Competitive antagonist for ganglionic nicotinic receptors - inactive at NMJ
Orally-acting hypoglycaemic agent - sulphonylurea
A1 receptor antagonist - non-selective phosphodiesterase inhibitor
Local anaesthetic - slow onset/offset - use dependence at low rates of stimulation - class IA antidysrhythmic
Potassium-sparing diuretic - blocks apical Na+ channels in late distal tubule
Experimental cardiac glycoside
Very potent alpha-2 agonist
Phosphodiesterase III inhibitor - inodilator
Calcium channel agonist - dihydropyridine
Muscarinic receptor antagonist - very long duration of action
K channel opener - also hirsutism effects
Selective non-depolarising neuromuscular blocker at NMJ - ester, broken down by spontaneous hydrolysis and plasma esterases
Non-selective agonist for muscarnic receptors
Lowers VLDL (and LDL) by stimulating lipoprotein lipase - may activate PPARs
Quaternary local anaesthetic analogue - only effective if perfused inside cells
Used experimentally to inhibit dopamine beta-hydroxylase - also inhibits aldehyde dehyddrogenase
Class III antidysrhythmic - prolongs AP and refractory period
Irreversible alpha-adrenoceptor antagonist - blocks Uptake 2 (and Uptake 1 at 10x higher concs)
ADP-ribosylates alpha-i - prevents activation of Gi in response to stimulation
Progestagen receptor antagonist
Beta-1 agonist - weak beta-2 agonist
Non-selective beta-adrenoceptor antagonist
Tricyclic antidepressant - blocks NET
Medium 'reversible' anticholinesterase - binds to esteratic site and carbamoylates ACh
Alpha-2 antagonist (some effect on alpha-1)
Nitrovasodilator - produces NO

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