Drug Function

Tetrodatoxin Blocks sodium channels so no action

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