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

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