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

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Created May 3, 2010ReportNominate
Tags:description, drug