CNS Pharmacology Flashcards
Typical antipsychotics
- 1st generation dopamine antagonists
- Phenothiazones, Haloperidol, thiothixene
Phenothiazones derivatives
Chlorpromazine- aliphatic derivative of phenothiazone
Atypical Antipsychotics
1ex
Newer 2nd gen dopamine antagonists
Clozapine
Antipsychotic drugs mechanism of action
- Dopamine antagonists
- Block dopamine D2 receptors in dopaminergic pathways
- Some also block 5HT 2 receptors
Types of antidepressant drugs for unipolar
Monoamine uptake inhibitors (NE and 5HT) Monoamine oxidase inhibitors (MAOIs)
Monoamine uptake inhibitors
Tricyclic antidepressants (TCAs): Amitriptyline Selective serotonin reuptake inhibitors (SSRIs): Prozac (Fluoxetine) Newer Mixed 5-HT & NE reuptake inhibitors (SNRIs): Effexor (Venlafaxine) Cymbalta (Duloxetiene) Norepinephrine reuptake inhibitors: Wellbutrin (Bupropion)
Monoamine Oxidase Inhibitors MAOI
Phenelzine Should NOT be used with other antidepressants or autonomic drugs that cause the release of serotonin and catecholamines
Monoamine receptor antagonists ie Unipolar
alpha 2 adrenergic receptor blockers Mirtazapine
Trazodone AoM Unipolar
Thought to potentiate 5HT activity. Get mixed agonist on receptor subtype Also blocks alpha1 adrenergic receptors
St Johns wort AoM Unipolar
Contains hyperforin A weak monoamine uptake inhibitor, activates P450 enzymes and can alter effects of other drugs
Lithium
Bipolar Used prophylactically to avoid manic depressive episodes
Valproate
Bipolar, antiepileptic drugs
Olanzapine for which depression
bipolar, an atypical antipsychotic drug blocks dopamine receptors in hypothalamus and leads to expression of prolactin
Sedative Hypnotics 9
Benzodiazepines Barbiturates Chloral hydrate Zolpidem Buspirone Baclofen Diphenyhydramine Ethanol Flumazenil
Benzodiazepines and Barbiturates moa
Enhance effect of native GABA on GABA-A receptors (modulators not direct agonists) Barbiturates at higher doses also inhibit AMPA (glutamate) receptors
Subclasses of barbiturates 3 how long acting and used for
Long acting- Phenobarbital (antiepileptic) Intermediate acting- Pentobarbital (sleep induction) Short acting- Thiopental, induction anesthetic
Benzodiazipines examples and their half lives
Most have active metabolites–> extends functional half-lives Triazolam 1.5 hrs Midazolam 4 hrs Oxazepam 8 hrs Lorazepam 14 hrs *Diazepam 48-100 hrs Flurazepam 100 hrs most eventually get glucuroniated–> secreted by kidneys
Chloral Hydrate MoA Used for
Similar action to benzodiazepines Short acting sleep inducer Used for conscious sedation in dentistry, no repetitive doses
Zolpidem MOA Used for
Act on GABA receptors (BZ1 receptor site) Not anticonvulsant Tx insomnia
Buspirone MOA Used for
Partial agonist at 5HT1A receptors not GABA Tx anxiety
Baclofen MOA Used
Agonist of GABA-B Muscle relaxant
Diphenyhydramine MOA Used
Block H1 receptors in CNS Sedation
Ethanol MOA Used
Multiple targets including GABA-A Sedation
Flumazenil MOA Used
GABA-A Bensodiazepine receptor antagonist Reverse sedation