potential Cocaine (LA) Not used clinically Procaine (LA) Infiltration, peripheral nerve block, central nerve block Lignocaine/Lidocaine (LA) Topical, infiltration, peripheral nerve block, central nerve block Prilocaine (LA) Topical, infiltration, peripheral nerve block, central nerve block Amethocaine/tetrocaine (LA) Topical Bupivacane (LA) Peripheral/central nerve block Endrophonium Inhibit acetylcholine esterase Neostigmine Inhibit acetylcholine esterase Physostigmine Inhibit acetylcholine esterase Hemicholinium Binds to choline uptake carrier and blocks it so reducing acetylcholine levels Triethylcholine (TEC) Partly up taken by choline carrier Acetyltriethylcholine False substrate Divalent cations e.g. cadmium Blocks calcium influx so inhibits transmitter release Botulinum toxin Muscle spasticity and destroys nerve terminals so inhibits transmitter release Beta bungarotoxin Reduces acetylcholine release Alpha bungarotoxin Blocks acetylcholine receptor Aminoglycoside antibiotics e.g. Kanamycin blocks influx of calcium by streptomycin, neomycin, kanamycin blocking calcium channels so inhibits transmitter release 4-aminopyridine and tetraethylammonium Blocks potassium channels so prolongs action potentials Tubocurarine Non-depolarising competitive blocker of acetylcholine receptor Pancuronium Non-depolarising competitive blocker of acetylcholine receptor Gallamine Non-depolarising competitive blocker of acetylcholine receptor Alcuronium Non-depolarising competitive blocker of acetylcholine receptor Atracurium Non-depolarising competitive blocker of acetylcholine receptor Vecuronium Non-depolarising competitive blocker of acetylcholine receptor Suxamethonium Depolarising non-competitive blockers of acetylcholine receptors Decamethonium Depolarising non-competitive blockers of acetylcholine receptors Suxethonium Depolarising non-competitive blockers of acetylcholine receptors Salbutamol Used in treatment of asthma (adrenoreceptor agonist) targets GPCRs Sumatriptan Used for headaches targets GPCRs Cetirizine Antihistamine targets GPCRs Erlotinib Inhibits epidermal growth factor receptors acts on receptor tyrosine kinases in cancer treatment Prenalterol Partial agonist acting at beta adrenoreceptors Adrenaline and isoprenaline Full agonists acting at beta adrenoreceptors Dichloroisoprenaline Partial agonist acting on beta adrenoreceptors Propanolol Antagonist acting on beta adrenoreceptors Impromidine Partial agonist acting at histamine H2 receptors Histamine Full agonist acting at histamine H2 receptors Sulphonamides and sulphones Anti-malarial drugs target dihydropteroate synthetase enzyme found in folate pathway of malaria Proguanil and pyrimethamine Anti-malarial drugs antagonist of dihydrofolate reductase enzyme found in malaria and host but malaria more sensitive Chloroquine, quinine, melfoquine Target haem polymerase which catalyses the conversion of free haem to hemozoin in malaria Artemisinin Anti-malarial drug believed to work via a redox mechanism AZT, DdC, Ddl, 3TC Nucleoside reverse transcriptase inhibitors used in treatment of HIV Nevirapine, C1-TIBO, L697-661, efavirenz, Non-nucleoside reverse transcriptase delavirdine inhibitors used in the treatment of HIV Indavir, ritonavir, saquinavir Protease inhibitors used in the treatment of HIV Salvarsan Antibiotic used in the treatment of syphilis Cycloserine, bacitracin, beta lactams, Antibacterials targeting cell wall synthesis glycopeptides Trimethoprim, sulphonamides, sulphones Antibacterials targeting folate metabolism Polymxins Antibacterials targeting cell membrane Quinolones, nitroimidazoles Antibacterials targeting DNA replication Rifamycins Antibacterials targeting DNA-dependent RNA polymerase Aminoglycosides, macrolides, linocosamides, Antibacterials targeting protein synthesis streptogramins, amphenicols, tetracyclines, rhupirocin Chloramphenicol Bactericidal antibiotic that inhibits transpeptidation Tetracycline Bacteriostatic antibiotic that inhibits mRNA- tRNA interaction and competes for the A site Erythromycin (macrolide) Bacteriostatic antibiotic that prevents translocation Streptomycin Aminoglycoside antibiotic that causes misreading of mRNA Ciprofloxacin Fluoroquinolone, bactericidal antibiotic that inhibits DNA gyrase Isoniazid Bactericidal antibiotic used in the treatment of TB as it inhibits the synthesis of mycolic acid Rifampicin Antibiotic used in the treatment of TB as it inhibits prokaryotic DNA-dependent RNA polymerase Bupropion Used as an antidepressant but also used as a smoking cessation therapy with an unknown mechanism of action but believed to involve effects on dopamine and noradrenaline transmission Varenicline Partial agonist of the alpha-4 beta-2 nAChR causes a moderate and sustained increase in mesolimbic dopamine levels. Also competitive binding with nicotine during relapses may reduce rewarding properties Disulfiram Used in alcohol aversion therapy as it inhibits aldehyde dehydrogenase Phenobarbital Barbiturate used in treatment of epilepsy as it acts on GABA receptors chloride channels are held opn Diazepam Benzodiazepine used in treatment of epilepsy and anxiety enhances GABA-A function Carbamazepine, Phenytoin Sodium channel blockers used in treatment of epilepsy Gabapentin Calcium channel blockers used in the treatment of epilepsy Buspirone Enhances 5HT inhibitory function used in treatment of anxiety Chlorpromazine, clozapine Dopamine 2 receptor blockers used in the treatment of schizophrenia L-DOPA Dopamine precursor used in treatment of Parkinsons as dopamine cannot cross blood- brain barrier Carbidopa Blocks L-DOPA breakdown outside CNS given with L-DOPA in treatment of Parkinsons Selegiline Blocks dopamine breakdown in CNS used in treatment of Parkinsons Tacrine Blocks acetylcholine esterase used in treatment of Alzheimers Fluoxetine Increases 5HT activity used in treatment of depression Amytriptiline Increases NA and 5HT function used in treatment of depression Monoamine oxidase inhibitors Block of breakdown of monoamine oxidase used in treatment of depression (but rarely) Selective serotonin reuptake inhibitor (SSRI) Blocks uptake of serotonin at 5HT receptor used in treatment of depression Selective noradrenaline reuptake inhibitor Blocks uptake of noradrenaline at 5HT and (SNRI) noradrenergic receptors used in treatment of depression Aspirin, Ibuprofen Analgesics block the production of pain chemicals (prostanoids) in damaged tissues Morphine Analgesic- Opioid acts on inhibitory mu receptor in spinal cord and midbrain to block transmitter release and reduce sensory neurone activity Naloxone Blocks the effect of opioids, used in substitution therapy Cannabis Analgesia, sedation, elevated mood, amnesia, muscle relaxation Amphetamines Awake, alert, confident MDMA ecstasy Acts on 5HT receptors to increase dopamine levels Ivacaftor CFTR potentiator used in the treatment of cystic fibrosis Zolpidem Alpha 1 subtype selective benzodiazepine agonist sedative/hypnotic effects