Pharmacology ALL drug list.pdf

Penicillin - Bera lactam an bio c, first an bio c derived from penicillin mould (Benzyl) - Benzylpenicillin undergoes first pass metabolism in the gut Digitalis (digoxin) - From foxglove plant - therapy of conges ve heart failure Morphine, Buprenorphine, Codeine, heroin, fentanyl, methadone - Opioid a...

Penicillin - Bera lactam an bio c, first an bio c derived from penicillin mould (Benzyl) - Benzylpenicillin undergoes first pass metabolism in the gut Digitalis (digoxin) - From foxglove plant - therapy of conges ve heart failure Morphine, Buprenorphine, Codeine, heroin, fentanyl, methadone - Opioid agonists – therapeu c affect of analgesia but also produces euphoria - Morphine - From opium Poppy – ac ve agent ten mes as potent as opium - Buprenorphine - Par al agonist of μ opioid receptor – produces a submaximal relief of analgesia when compared to morphine – ought to have less addic ve liability than morphine Insulin - From pancrea c extracts – diabeteso - An dote is glucagon – increases plasma glucose levels Recombinant Insulin - Inser ng human insulin gene into E. Coli pioid– didn’t have side effects like blindness that came from bovine and porcine sources of Insulin Sulphanilamide’s and sulphonamides - Dye prontosil – antagonis c proper es against bacteria – sulphanilamide por on of prontosil molecule Ima nib - Highly selec ve inhibitor of BCR-Ab1 tyrosine kinase fusion protein Omeprazole - Proton pump inhibitor that blocks ac on of histamine s mula ng acid secre on of gastric parietal cells Cime dine - H2 receptor antagonist – inverse agonist – diminish basal cAMP levels associated with gastric acid secre on Verapamil - Target for an -dysthymics - voltage gated calcium channels in the heart. Inhibits P-gp (ac ve ABC ac ve transporter) Amlodipine - Target for an -hypertensives - voltage gated calcium channels in the heart Naloxone - Opioid receptor antagonist – compe ve antagonist – opioids cant exert their effects – an dote for opioid overdose – rapidly reverses opioid-induced analgesia and respiratory depression Aspirin, Ibuprofen, Paracetamol - Non-steroidal an -inflammatory drugs (paracetamol has limited an -inflammatory effects so not necessarily an NSAID but is an analgesic and an pyre c) - Paracetomol an dote – N-acetylcysteine (NAC) – precursor to L-Glutathione - neutralises the NAPQI metabolite - Aspirin demonstrates satura on kine cs Theralizumab - Poten al treatment of B cell lymphoma – Phase 1 trial showed serious adverse effects BIA 10-2472 - Treatment of anxiety and mood disorders associated with Parkinson’s disease – par cipant died during phase 1 trial Thalidomide - FDA category X – withdrawn during phase IV – produced phocomelia Flumazenil - Compe vely inhibits ac vity of benzodiazepines that interact with benzodiazepine receptors site on GABA/benzodiazepine receptor complex. An dote for benzodiazepine poisoning Protamine - An dote for heparin poisoning – forms a neutralising inac ve complex Pralidoxime - An dote for an cholinesterases – prevents “ageing” of cholinesterase Propofol - GABA agonist (?) Posi ve modulator of GABA through GABA-A receptor (?). Anaesthe c for surgery – not given orally – intravenous injec ons – have 100% bioavailability Warfarin - An coagulant – concentrates in plasma and inhibits clo ng factor. Metabolised by CYP450 (CYP1A2 / CYP3A4). When given with + Carbamazepine (Enzyme Inducer) – broken down faster – less effec ve. Diphenhydramine - C - Histamine antagonist Rimonabant - Cannabinoid (CB1) receptor antagonist developed for the treatment of obesity – removed from market – phase IV(?) CYP450 enzyme inducers - Sulphonylureas - Carbamazepine - Rifampicin - Alcohol - Phenytoin - Griseofulvin – Phenobarbital CYP450 enzyme inhibitors - Sodium Valproate - Isoniazid - Cime dine - Ketoconazole - Fluconazole - Alcohol: Binge Drinking - Chloramphenicol - Erythromycin - Sulphonamides - Ciprofloxacin - Omeprazole Metronidaxole Cholinergic drugs Vesamicol - B - Blockade of ACh Vesicular storage – NMJ block – presynap cally ac ng. Isn’t used clinically. Bethanacol - C - Muscarinic agonist via M3 receptors – not cleaved by cholinesterase – treats urinary reten on and gut hypotonia Pilocarpine – C - Muscarinic agonist via M3 receptors – not cleaved by cholinesterase – used to treat glaucoma Carbachol - C - Nico nic/muscarinic agonist Suxamethonium – C - Nico nic agonist – used as a muscle relaxant during surgery – depolarising NMJ block Atropine - C - Compe ve muscarinic receptor antagonist – derived from Atropa belladonna. treatment for organophosphates (irreversible acetylcholinesterase), reduces secre ons in anaesthesia, treats GI hypermo lity (binds to M3 receptors), for bradycardia (binds to M2 receptors). - Classic triad of muscarinic antagonist side effects – dry mouth, urinary reten on, blurred vision Hyoscine (Scopolamine) – C - Muscarinic antagonist – extract from thorn apple, reduces secre ons in anaesthesia, GI hypermo lity, bradycardia, an cholinesterase poisoning, mo on sickness – hyoscine crosses blood brain barrier – classic triad of muscarinic side effects as well as seda on Ipratropium - C - Muscarinic antagonist via M3 receptors, bronchodilator for asthma and bronchi s Pirenzepine - C - Muscarinic antagonist – selec vely blocks M1 receptors on gastric parietal cells – used to treat pep c ulcers Revefencain – C - M3 antagonist – first once daily treatment for COPD Pancuronium, Atacurium, Vecuronium – C - Nico nic antagonist – synthe c deriva ve of tubocurarine, used as a muscle relaxant during anaesthesia – Nondepolarizing NMJ blocks. Trimethaphan - C - Nico nic antagonist, ganglion blocker, used (rarely)gf to lower BP in surgery Physos - gmin, pyridos gmine - D Medium dura on an cholinesterase physos gmine used to treat glaucoma pyridos gmine used to treat myasthenia gravis Parathion, Dyflos, ecothiopate - D - Irreversible acetylcholinesterase inhibitor – organophosphate – used in nerve gases and insec cides - Ecothiopate and parathion used to treat glaucoma, dyflos formerly used Edrophonium – D - Short dura on acetylcholinesterase inhibitor – no therapeu c purpose – used clinically to diagnose myasthenia gravis Neos gmine – D - Medium dura on – an cholinesterase – used to treat myasthenia gravis Hemicholinium – E - Blockade of choline reuptake transporter – competes with choline – not taken up itself – not used clinically Triethylcholine – E - Compe ve choline uptake inhibitor – taken up and released as a false transmi er – not used clinically Adrenergic/monoamine drugs α-methyl para-tyrosine - A - Tyrosine hydroxylase inhibitor – inhibits NA synthesis – used to treat phaeochromocytoma Amphetamine - B - S mulates NA release – indirectly-ac ng adrenergic agonist, aka indirectly ac ng sympathomime c amines - psychoac ve s mulant – releases dopamine/noradrenaline from the nerve terminals resul ng in marked tachyphylaxis – used for ADHD and as a drug of abuse - ‘speed’. Side effects – increased heart rate, blood pressure (α1, α2, β2), cons pa on (β2). Can cause schizophrenia like symptoms. Ephedrine/Pseudoephedrine – B - S mulates NA release – treat nasal deconges on (Sudafed) – indirectly ac ng sympathomime c amine Reserpine – B - Deple on of NA vesicles – block NA vesicular storage – sympathe cally-mediated contrac on and vasoconstric on are reduced – formerly used to treat hypertension – side effect of depression Isoprenaline - C - β agonist (non-selec ve) Clenbuterol - C - β2 agonist – used illicitly by athletes to improve performance – causes tremor in skeletal muscle thereby increasing muscle strength Salbutamol – C - β2 agonist – treat premature labour, asthma Salmeterol, terbutaline - C - β2 agonist – treat asthma Dobutamine – C - Selec ve β1-adrenoceptor agonist that is used to treat cardiogenic shock Prazosin, Doxazosin, Terazosin - C - α1 antagonist – used to treat hypertension, side effects – postural hypotension Atenolol, Propranolol, Oxprenolol, Alprenolol - C - Non-selec ve β-adrenoceptor antagonist – treat hypertension, cardiac dysrhythmias, angina pectoris (and some anxiety disorders that cause peripheral consequences – panic a acks) – Beta blockers – side effects include bronchoconstric on, bradycardia, cold extremi es, cardiac failure. Contraindicated in asthma cs (would cause airway constric on). (Atenolol β1 selec ve antagonist) Clonidine - C - α-adrenoceptor agonist – used to treat menopausal flushing Moclobemide, Selegiline - D - Inhibit NA metabolism – inhibit monoamine oxidase Cocaine - E - Dopamine/noradrenaline reuptake blocker – NA can’t be terminated Methyldopa - E - Taken up by noradrenergic neurons and converted to a false transmi er - αmethylnoradrenaline therefore reduces NA availability – used to treat hypertension in pregnancy Guanethidine - B - Blockade of NA release - Inhibits the release of NA from sympathe c nerve terminals – used to be used to treat hypertension – severe side effects: postural hypotension, diarrhoea, nasal conges on CNS drugs L-dopa* (levodopa) - Dopamine precursor – Parkinson’s disease – loca on at synapse: A (synthesis) - Carbidopa, benserazide - DOPA decarboxylase inhibitors given alongside L-DOPA that are unable to cross BBB so conversion to dopamine only occurs in brain – reduces peripheral side effects - Main side effects of levodopa are dyskinesias and on-off effects Pramipexole*, ropinirole – C - D2 receptor agonist – Parkinson’s treatment Apomorphine – C - Non-selec ve dopamine receptor agonists – Parkinson’s treatment Bromocrip ne*, pergolide, cabergoline – C - Slightly selec ve D2 receptor agonists – Parkinson’s treatment Chlorpromazine*, haloperidol*, thioridazine, flupenthixol – C - D2 receptor antagonist (first genera on an psycho c – more side effects (acute dystonia, tardive dyskinesia, hormonal imbalances – tuberhypophyseal pathway – breast swelling, lacta on)) – schizophrenia - Thioridazine withdrawn from market in 2005 Clozapine*, sulpiride*, ser ndole, que apine – C - D2 receptor antagonist (second genera on an psycho c – less side effects) – schizophrenia - (Clozapine for treatment resistant schizophrenia) Risperidone* – C - D2 receptor antagonist (second genera on an psycho c) – schizophrenia and anxiety Olanzapine – C - 5-HT2A and D2 antagonist - schizophrenia and anxiety Diazepam*, clonazepam, lorazepam – C - GABA allosteric modulator, benzodiazepine – long dura on – anxiety (benzodiazepine’s bind to GABA-A receptor and enhance ac ons of GABA (inhibitory). Bind at a different site to GABA – not agonists) - Lorazepam – short dura on Flunitrazepam* (Rohypnol) - Benzodiazepine – “date-rape drug” – causes anterograde amnesia - prevent forma on of memories of events experienced while under their influence. Midazolam – C (?) - GABA allosteric modulator, benzodiazepine - ultrashort dura on – sleeping pills Buspirone – C - Par al 5-HT1A agonist (5-HT1A is an inhibitory autoreceptor – reduces 5-HT – may lead to desensi sa on) – anxiety treatment Propranolol – C - Non-selec ve beta-adrenoceptor antagonist (beta-blocker) – anxiety – panic disorders that trigger SNS (also an example of an inverse agonist – further inac vated receptor ac vity beyond baseline value) Benzatropine*, Trihexyphenidyl – C - Muscarinic cholinergic antagonist – Parkinson’s treatment (cholinergic interneurons in the striatum oppose the effects of dopamine) Amantadine – C - Non-compe ve antagonist of NMDA receptor – Parkison’s treatment Meman ne – C - NMDA receptor antagonist – Alzheimer’s disease Mirtazapine – C - α2, 5-HT2A, 5-HT2C, 5-HT3 antagonist (monoamine receptor antagonist) – an depressant (α2 reduces 5-HT release – antagonising it will increase 5-HT) Trazodone – C - 5-HT2A, 5-HT2c antagonist (monoamine receptor antagonist) Mianserin – C - α1, α2, 5-HT2A, H1 antagonist (monoamine receptor antagonist) Selegeline* – D - MAO-B inhibitor (inhibits dopamine metabolism) – Parkinson’s disease (MAO-B metabolises NA, dopamine and phenylethylamine) Moclobemide*, Clorgyline – D - MAO-A inhibitor – Depression (MAO-A metabolises 5-HT, NA and dopamine) Phenelzine*, Tranylcypromine, Isocarboxazid – D - Non-selec ve MAO inhibitor - depression (MAO’s interact with – SSRI’s – serotonin syndrome, Pethidine (an opiate analgesic), Cheese reac on) Donepezil*, Rivas gmine (CNS selec ve), Galantamine (also a posi ve allosteric modulator of nico nic receptors), tacrine* – D - Acetylcholinesterase inhibitor – Alzheimer’s treatment Fluoxe ne* (also 5-HT2C antagonist), Escitalopram, Sertraline, fluvoxamine, paroxe ne, citalopram*, vor oxe ne (also 5-HT agonist/antagonist) – E - Selec ve Serotonin Reuptake Inhibitor (SSRI) – an depressant - Fluoxe ne also used for anxiety, OCD Amitriptyline*, Clomipramine, Desipramine*, Imipramine, Nortriptyline – E - Serotonin/noradrenaline reuptake inhibitor (TCA’s – more side effects than SSRIs) – an depressant (and neuropathic pain). TCA’s affect muscarinic acetylcholine receptors (an cholinergic effects – dry mouth, cons pa on, blurred vision, urinary reten on), (postural hypotension due to alpha 1 block) Histamine receptors (seda on – day me drowsiness, difficulty concentra ng), 5-HT receptors. Venlafaxine*, desvenlafaxine, duloxe ne – E - Serotonin/noradrenaline reuptake inhibitor (SNRIs) – an depressant (anxiety, menopause symptoms, neuropathic pain, fibromyalgia, urinary incon nence) Bupropion*, Reboxe ne, Atomoxe ne – E - Noradrenaline reuptake inhibitors – (nico ne dependence, ADHD) St. John’s Wort/Hyperforin – E - Monoamine reuptake inhibitor – Depression - serious risk of drug-drug interac ons due to effects on CypP450 enzymes Vilazodone – C - SSRI and par al 5-HT1A agonist - an depressant Carbamazepine, Ethosuximide, Phenytoin*, Valproate*, lamotrigine* – C (?) - an -epilep c drug – inhibits voltage-dependent sodium channel – reduces neuronal membrane excitability (poor safety profile, use dependence occurs – preferen ally bind to inac vated state of the Na+ channel) - Ethosuxamide and Valproate* – inhibit T-type voltage-gated calcium channels – absence seizures - Phenytoin demonstrates satura on kine cs Entacapone* – D - catechol-O-methyltransferase (COMT) inhibitor – inhibits dopamine metabolism – treatment of Parkinson’s disease Agomelatine – antidepressant - melatonin agonist (?), serotonin antagonist (?) – C (?) Gabapen n*, Pregabalin*, – C (?) - Reduces calcium dependent exocytosis of synap c vesicles by binding to a subunit of P/Qtype voltage-gated calcium channels – an -epilep c and anxiety Vigabatrin* – D - An -epilep c drug – inhibits GABA transaminase Tiagabine* – E - An -epilep c drug – inhibi on of GABA reuptake Perampanel – C - An -epilep c drug – antagonises glutamate receptors (glutamate = excitatory), specifically AMPA subtype Phenobarbital (anaesthe c) – C - An -epilep c drug – barbiturates – bind to GABA-A receptor – enhance ac ons of GABA (GABA = inhibitory)