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

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Created May 3, 2010ReportNominate
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