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

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