Pharmacology Unit 4 drug list.pdf

Pharmacology CNS drug list L-dopa - 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 effect...

Pharmacology CNS drug list L-dopa - 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 Clozapine, sulpride, ser ndole, que apine – C - D2 receptor antagonist (second genera on an psycho c – less side effects) – 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) 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 - Beta-adrenoceptor antagonist (beta-blocker) – anxiety – panic disorders that trigger SNS 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 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, Ethosuxamide, Phenytoin, Valproate – 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 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 Tigabine – 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)