Vesamicol
Non-competative and reversible blocker of VAChT
Varenicline
High affinity partial agonist for the α4β2nAChRs<div>High affinity full agonst for the α7nAChRs</div>
Trimetaphan
Competative antagonist of the (α3)2(β2)3isoform of the nAChR
Hexamethonium
Competative antagonist of the (α3)2(β2)3isoform of the nAChR
Tetramethylammonium (TMA)
Neuronal (Nn) nAChR agonist
Dimethylphenylpiperazinium (DMPP)
Neuronal (Nn) nAChR agonist
Suxamethonium
Depolarising nAChR antagonist that initially activates the receptor but isnt hydrolysed by AChE so causes a secondary antagonism
Curare (d-tubocurarine)
Non-depolarising nAChR antagonist
Pancuronium
Synthetic non-depolarising aminosteriod nAChR antagonist
Rocuronium
Synthetic non-depolarising aminosteriod nAChR antagonist
Atracurium
Synthetic non-depolarising nAChR antagonist (benzylisoquinolinium)
Mivacurium
Synthetic non-depolarising nAChR antagonist (benzylisoquinolinium)
Botulinum toxin (BTx)
Peptidase that cleaves SNARE proteins to prevent release of ACh, hence blocking cholinergic neurotransmission
α-bungarotoxin
Irreversibly binds to the ACh binding site on the adult nAChR hence blocking cholinergic neurotransmission
β-bungarotoxin
Inhibits ACh release through a mechanism thought to involve phospholipase A2, which leads to blockage of cholinergic neurotransmission
α-lacrotoxin
Causes massive release and subsequent depletion of ACh at the NMJ thought to be due to its ability to form a Ca2+channel
Tetanus neurotoxin
Cleaves synaptobrevin to prevent glycine release by inhibitory interneurones upsteam of those innervating skeletal muscle
Bethanechol
Choline ester that acts as a non-selective agonist of mAChRs
Pilocarpine
mAChR agonist that is stable to hydrolysis by AChE
Atropine
Non-selective mAChR antagonist
Scopoloamine
Non-selective mAChR antagonist
Homatropine
Non-selective mAChR antagonist
Methscopolamine
Non-selective mAChR antagonist
Ipratropium
Short-acting non-selective mAChR antagonist (SAMA) with some selectivity for M3receptors in the airways
Tiotropium
Long-acting non-selective mAChR antagonist (LAMA) with some selectivity for M3receptors in the airways
Glycopyrronium
Long-acting non-selective mAChR antagonist (LAMA) with some selectivity for M3receptors in the airways
Tropicamide
Non-selective mAChR antagonist
Cyclopentolate
Non-selective mAChR antagonist
Pirenzepine
M1selective mAChR antagonist
Darifenacin
M3selective mAChR antagonist
Solifenacin
M3selective mAChR antagonist
Endrophonium
Non-covalent, reversible, short-acting AChE inhibitor
Neostigmine
Covalent, reversible, medium-acting AChE inhibitor
Physostigmine
Covalent, reversible, medium-acting AChE inhibitor
Ecothiophate
Long-acting, irreversible AChE inhibitor
Nerve gases (tabun, sarin, novichok etc.)
Long-acting, irreversible AChE inhibitors
Isoprenaline
β-selective AR agonist
Noradrenaline
αAR-selective agonist
Adrenaline
Non-selective AR agonist
α-Methyldopa
Competative inhibitor of tyrosine hydroxylase
L-DOPA
Product of tyrosine hydroxylase that can boos dopamine synthesis
Carbidopa
Inhibitor of peripheral DOPA decarboxylase
Disulfiram
Inhibitor of dopamine β hydroxylase
α-Μethyldopa
False transmitter released with DA and NA that acts as an α2-selective AR agonist
Reserpine
Irreversible blocker of VMAT2-mediated monoamine uptake into vesicles
Guanethidine
Low doses block impulse conduction at adrenergic synapses<div>High doses leads to a depletion of NA</div>
Dexamfetamine
Indirectly-acting sympatheticomimetic that causes adrenergic neurotransmitter release via a Ca2+-independant mechansim
Ephedrine
Mixed acting sympatheticomimetic that causes both release of NA and acts directly as an agonist at adrenoceptors
Imipramine
TCA that inhibits NET/Uptake 1
6-Hydropamine
Synthetic neurotoxin used to destroy dopaminergic neurones and induce PD in animal models
Phenoxybenzamine
Irreversible αAR antagonist that also blocks ENT/Uptake 2 at high concentrations
Normetanephrine
Metabolite of NA that blocks ENT/Uptake 2
Entacapone
COMT inhibitor
Xylometazoline
αAR-selective agonist
Phenylephrine
α1AR-selective agonist
Clonidine
α2AR-selective agonist
Dobutamine
β1AR-selective agonist
Salbutamol
Short-acting β2AR-selective agonist
Terbutaline
Short-acting β2AR-selective agonist
Salmeterol
Long-acting β2AR-selective agonist
Formerol
Long-acting β2AR-selective agonist
Indacaterol
Long-acting β2AR-selective agonist
Mirabegron
β3AR-selective agonist
Phentolamine
αAR-selective antagonist
Phenoxybenzamine
αAR-selective antagonist
Prazosin
α1AR-selective and competative antagonist
Idazoxan
α2AR-selective antagonist
Tamsulosin
α1AAR-selective antagonist
Yohimbine
α2AR-selective antagonist
Propranolol
Non-selective βAR antagonist
Atenolol
β1AR-selective antagonist
Bisoprolol
β1AR-selective antagonist
Carvedilol
Mixed α1/βAR-selective antagonist that exhibits G-protein signalling bias
Nebivolol
3rd generation β1AR-selective antagonist that also stimulates NO(g) release
Caffeine
Competative antagonist of the A1 adenosine receptors
Regadenoson
A2A-selective adenosine receptor agonist
Tetracaine
Use-dependant neuronal-selective Na+channel blocker
Benzocaine
Use-dependant neuronal-selective Na+channel blocker
RAC-421
Synthetic neuronal-selective Na+channel blocker
QX-314
Synthetic use-dependant Na+channel blocker
Nifedapine
Dihydropyridine smooth muscle-selective Ca2+channel blocker
Amlodipine
Dihydropyridine smooth muscle-selective Ca2+channel blocker
Felodipine
Dihydropyridine smooth muscle-selective Ca2+channel blocker
Verapamil
Phenylalkylamine cardiac muscle-selective Ca2+channel blocker
Diltiazem
Benzothiazepine type Ca2+channel blocker
Tetrodotoxin
Highly-selective, reversible blocker to neuronal Na+ channels
Saxitoxin
Highly-selective, reversible blocker to neuronal Na+channels
Batrachotoxin
Neurotoxin that lowers the threshold for opening and inhibits inactivation of Na+channels
α-scorpiotoxin
Neurotoxin that binds with voltage-dependance and inhibits activation of Na+channels
Quinidine
Class IA antidysrhythmic that acts as a<b> </b>use-dependant sodium channel blocker
Procainamide
Class IA antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker
Disopyramide
Class IA antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker
Lidocaine
Class IB antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker
Mexilitine
Class IB antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker
Flecainide
Class IC antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker
Propafenone
Class IC antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker
Amiodarone
Class III antidysrhythmic that acts as an action potential prolonging agent
Sotalol
Class III antidysrhythmic that acts as an action potential prolonging agent
Digoxin
- Cardiac glycoside that inhibits the Na+/K+ATPase<div>- Also increases vagal activity through actions in the CNS</div>
Ouabain
Cardiac glycoside that inhibits the Na+/K+ATPase
Phenothiazine
PDE1 inhibitor
Milrinone
PDE3 inhibitor
Rolipram
PDE4 inhibitor
Sildenafil
PDE5 inhibitor
Dipyridamole
PDE5 inhibitor
Caffiene
<div>Methylxanthine drug that acts as a non-selective PDE inhibitor and an A1/A2 adenosine receptor antagonist</div>
Theophylline
Methylxanthine drug that acts as a non-selective PDE inhibitor and an A1/A2adenosine receptor antagonist
Prednisolone
Glucocorticoid receptor agonist
Mifepristone
Glucocorticoid receptor antagonist
Spironolactone
Mineralocorticoid receptor antagonist
Fludrocortisone
Mineralocorticoid receptor agonist
Ethinylestradiol
Oestrogen receptor agonist
Tamoxifen
Oestrogen receptor antagonist
Norethisterone
Progestagen receptor agonist
Danazol
Progestagen receptor antagonist
Streptokinase
Tissue plasminogen activator that promotes the generation of plasmin
Alteplase
Recombinant human tissue plasminogen activator that leads to activation of plasmin
Aspirin
COX1 inhibitor that prevents the formation of thromboxane A2and hence inhibits platelet aggregation
Clopidogrel
Irreversible, competative P2Y12receptor antagonist (pro-drug)
Prasugrel
Irreversible, competative P2Y12receptor antagonist (pro-drug)
Ticagrelor
Irreversible, competative P2Y12receptor antagonist
Eptifibatide
Cyclic heptapeptide antagonist of gpIIb/IIIa
Tirofiban
Non-peptide antagonist of gpIIb/IIIa receptor
Abciximab
Monoclonal antibody against gpIIb/IIIa that also binds to the vitronectin receptor to prevent platelet aggregation
Heparin
Indirect thrombin inhibitor that binds to and activates anti-thrombin
Dalteparin
Low molecular weight heparin that acts as an indirect thrombin inhibitor by binding to and activating anti-thrombin
Tinzaparin
Low molecular weight heparin that acts as an indirect thrombin inhibitor by binding to and activating anti-thrombin
Warafin
Vitamin K antagonist that inhibits VKORC1 and the formation of factors II, VII, IX and X
Dabigatran
Direct thrombin inhibitor
Rivaroxaban
Direct oral anticoagulant that acts as a factor Xa inhibitor
Apixaban
Direct oral anticoagulant that acts as a factor Xa inhibitor
Edoxaban
Direct oral anticoagulant that acts as a factor Xa inhibitor
Fondaparinux
Indirect inhibitor of factor Xa
Argatroban
Synthetic direct thrombin inhibitor
Bivalirudin
Hirudin analogue that acts as a thrombin inhibitor
Danaparoid
Indirect inactivator of factor Xa<div>Direct inhibitor of factor IX activation</div>
Tranexamic acid
Competative inhibitor of tissue plasminogen activator
Furosemide
Loop diuretic that blocks NKCC2 in the apical membrane of cells in the TAL
Bumetanide
Loop diuretic that blocks NKCC2 in the apical membrane of cells in the TAL
Probenecid
Competative ligand for the uric acid transporter that inhibits its reabsorption
Hydrochlorothiazide
Thiazide diuretic that blocks NCC on the apical membrane of the cells of the TAL/DCT
Bendroflumethiazide
Thiazide diuretic that blocks NCC on the apical membrane of the cells of the TAL/DCT
Amiloride
K+sparring diuretic that blocks the ENaC channel on the apical membrane of cells in the late DCT
Triamterene
K+sparring diuretic that blocks the ENaC channel on the apical membrane of cells in the late DCT
Spironolactone
K+sparring diuretic that acts as an antagonists of the mineralocorticoid receptor in the cells of the late DCT
Acetozolamide
Carbonic anhydrase inhibitor that acts as a weak diuretic
Mannitol
Osmotic diuretic
Ramipril
ACE-Inhibitor
Captopril
ACE-Inhibitor
Enalapril
ACE-Inhibitor
Lisinopril
ACE-Inhibitor
Perindopril
ACE-Inhibitor
Saralasin
Partial agonist of the angiotensin receptor
Losartan
Angiotensin receptor blocker
Valsartan
Angiotensin receptor blocker
Candesartan
Angiotensin receptor blocker
Desmopressin
AVP/ADH analogue and agonst of the AVPR2 receptor
Aliskiren
Direct renin inhibitor
Doxazocin
α1AR antagonist
Labetalol
<div>α1, β1 and β2 antagonist that is β-selective</div>
Minoxidil
KATP channel activator that causes relaxation of vascular smooth muscle
Nicorandil
KATPchannel activator that also acts as an NO(g)donor to trigger relaxation of vascular smooth muscle
Diazoxide
KATPchannel activator
Simvastatin
Short-acting HMG-CoA Inhibitor
Lovastatin
Short-acting HMG-CoA Inhibitor
Pravastatin
Short-acting HMG-CoA Inhibitor
Atorvostatin
Long-acting HMG-CoA Inhibitor
Rosuvastatin
Long-acting HMG-CoA Inhibitor
Alirocumab
PCSK9 Inhibitor
Evolocumab
PCSK9 Inhibitor
Bezafibrate
PPARα activator that increases transcription of genes involved in lipid metabolism
Ezetimibe
<div>NPC1L1 transport proteinblocker that inhibitsintestinal absorptionofcholesterolinbrush border of enterocytes</div>
Colestyramine
Anion exchange resin that inhibits bile acid uptake by the liver that leads to an upregulation of LDL-R surface expression
Niacin/nicotinic acid
Pro-drug that is converted to nicotinamide which inhibits hepatic VLDL secretion causing a secrease in LDL
Glyceryl Trinitrate/Nitroglycerine/GTN
Short-acting nitrate derivative that activates guanylyl cyclase
Isosorbide mononitrate
Long-acting nitrate derivative that activates guanylyl cyclase
Ivabradine
HCN (If current) blocker
Ranolazine
Inhibitor of the late phase Na+currents
Adenosine
Agonist of the A1receptors which trigger hyperpolarisation of pacemaker and conductive cells
Benserazide
Peripheral DOPA-decarboxylase inhibitor
Ether
- Inhalational general anaesthetic<div>- Prevents cellular depolarisation<br></br></div>
Etomidate
- Intravenous general anaesthetic<div>- Acts on β3 (or β2) subunit of the GABAA receptor resulting in Cl-influx andhyperpolarisation ofthe postsynaptic membrane</div>
Halothane
- Inhalational general anaesthetic<div>- Activates the TASK3 member of the two-pore domain potassium channel (K2P) family leading to hyperpolarisation and reduced neuronal activity<br></br></div><div>-Also acts on theα and β subunits of the GABAAreceptor to cause Cl-influx and hyperpolarisation</div>
Nitrous Oxide, NO(g)
- Inhalational general anaesthetic that activates the TASK3 member of the two-pore domain potassium channel (K2P) family leading to hyperpolarisation and reduced neuronal activity<div>- May also inhibit the excitatory NMDA receptors</div>
Propofol
- Intravenous general anaesthetic<br></br>- Acts on β3(or β2) subunit of the GABAAreceptor resulting in Cl-influx andhyperpolarisation ofthe postsynaptic membrane<br></br>
Thiopental (thiopentone)
- Intravenous general anaesthetic<div>- Short acting barbiturate (positive allosteric modulator)</div><div>- Acts on β3(or β2) subunit of the GABAAreceptor resulting in Cl-influx andhyperpolarisation ofthe postsynaptic membrane<br></br></div>
Isoflurane
- Inhalational general anaesthetic<div>- Activates the TASK3 member of the two-pore domain potassium channel (K2P) family leading to hyperpolarisation and reduced neuronal activity<br></br></div><div>-Also acts on theα and β subunits of the GABAAreceptor to cause Cl-influx and hyperpolarisation</div>
Xenon
- Inhalational anaesthetic<div>- Mayinhibit the excitatory NMDA receptors, which are activated by glutamate</div>
Fosfomycin
- Bacterial cell wall synthesis inhibitor<div>- StructuralanalogueofPEPthat competitivelyinhibits pyruvyl transferasetoprevent synthesisofNAM</div>
Cycloserine
<div>- Bacterial cell wall synthesis inhibitor</div>
<div>- Structural analogue of D-Alanine that competitively inhibits the enzymes responsible for D-Alanine biosynthesis and addition to the peptide crossbridge</div>
Bacitracin
<div>- Bacterial cell wall synthesis inhibitor</div>
<div>- Binds to bactoprenol-pyrophosphate in the extracellular leaflet and prevents its hydrolysis and return to the cytosolic leaflet</div>
Penicillin
- Bacterial cell wall synthesis inhibitor<div>- β-lactam mimicsthe peptide bond in the D-Ala-D-Ala terminus</div><div>- Binds to transpeptidase and prevents it from acting on its target in peptidoglycan synthesis</div>
Vancomycin
<div>- Bacterial cells wall synthesis inhibitor</div>
<div>- Forms hydrogen bonds with the D-Ala-D-Ala terminus<br></br></div>
<div>-This causes steric hindrance of transglycosylation <b></b></div>
<div>- Inhibits bacterial protein synthesis<br></br></div>
Tetracycline
- Broad spectrum tetracycline-class of bacteriostatic antibiotic<div><div>- Reversibly binds to the 30S ribosomal subunit<br></br></div> <div>-Inhibits the entry of aminoacyl-tRNA into the acceptor site (A-site) on the 70S ribosome</div></div><div>- Inhibits bacterial protein synthesis<br></br></div>
Doxycycline
- Broad spectrum tetracycline-class of bacteriostatic antibiotic<div><div>- Reversibly bindsto the30S ribosomalsubunit<br></br></div><div>-Inhibitstheentryofaminoacyl-tRNAinto theacceptor site(A-site) on the 70S ribosome</div></div><div>- Inhibits bacterial protein synthesis</div>
Streptomycin
<div>- Narrow spectrum aminoglycoside bactericidal antibiotic</div>
<div>-Binds to the 30S ribosomal subunit and freeze the 30S pre-initiation complex so that no further initiation can occur</div>
<div>-Also slows down protein synthesis that has already been initiated and induce misreading of the mRNA</div>
<div>- Inhibits bacterial protein synthesis<br></br></div>
Gentamycin
<div>- Narrow spectrum aminoglycosidebactericidalantibiotic</div>
<div>-Binds to the30S ribosomalsubunit andfreezethe 30Spre-initiation complexso that no further initiation can occur.</div>
<div>-Also slows down protein synthesisthat hasalready been initiatedandinduce misreadingof themRNA</div>
<div>- Inhibits bacterial protein synthesis<br></br></div>
Neomycin
<div>- Narrow spectrum aminoglycosidebactericidalantibiotic</div>
<div>-Binds to the30S ribosomalsubunit andfreezethe 30Spre-initiation complexso that no further initiation can occur</div>
<div>-Also slows down protein synthesisthat hasalready been initiatedandinduce misreadingof themRNA</div>
<div>- Inhibits bacterial protein synthesis<br></br></div>
Erythromycin
<div>- Narrow spectrum bacteriostatic macrolide antibiotic</div>
<div>-Binds to the entrance of the polypeptide exit tunnelin 50S subunit</div>
<div>-Specifically,binds to the 23S rRNA component via hydrogen bonds with nitrogenous bases</div>
<div>- Inhibits bacterial protein synthesis</div>
Clarithromycin
<div>- Extended spectrum bacteriostatic macrolide antibiotic</div>
<div>-Binds to the entrance of thepolypeptide exit tunnelin 50S subunit</div>
<div>-Specifically,bindsto the23S rRNAcomponent via hydrogen bonds with nitrogenous bases</div>
<div>- Inhibits bacterial protein synthesis</div>
Azithromycin
<div>- Extended spectrum bacteriostatic macrolideantibiotic</div>
<div>-Binds to the entrance of thepolypeptide exit tunnelin 50S subunit</div>
<div>-Specifically,bindsto the23S rRNAcomponent via hydrogen bonds with nitrogenous bases</div>
<div>- Inhibits bacterial protein synthesis</div>
Chloramphenicol
<div>- Broad-spectrumbacteriostaticantibiotic</div>
<div>- Binds to the 50S ribosomal subunit and binds near aminoacyl-tRNA binding site (A site)</div>
<div>-Prevents peptidyl transferase activity</div>
<div>- Inhibits bacterial protein synthesis</div>
Fusidic Acid
<div>- Narrow spectrum bacteriostatic antibiotic</div>
<div>-Binds to elongation factor G (EF-G) and inhibits its GTPase activity,preventing peptide translocation </div>
<div>- Inhibits bacterial protein synthesis</div>