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

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Created May 3, 2010ReportNominate
Tags:description, drug