neuro pharm 12
Terms
undefined, object
copy deck
- Imipramine
- 3o TCA more potent in inhibiting S uptake
- Amitriptyline
- 3o TCA more potent in inhibiting S uptake
- Desipramine
-
- desmethyl imipramine
- 2o TCA more selective inhibitors of NE uptake - Nortriptyline
-
- desmethyl amitriptyline
- 2o TCA more selective inhibitors of NE uptake - TCA SE's
-
- narrow theraputic range
– CV (arrhythmias, long QRS)
- small quantities prescribed to minimize use in suicide
- muscarinic blockade
– a-blocaide (orthostatic hypotension)
– 5) H blockade (Sedation, Weight gain) - MAOI mechanism
-
- both A and B vital to inactivation of S, EPI, NE, D, and phenethylamine
- classic MAOIs inhibit both - MAOI SE's
-
– potentiate symp amines
– potentiates Tyramine, in wine and cheeses, which means hypertensive crisis
- Strong CNS stimulation, convulsions, and coma ( serotonin syndrome) w/ MAOIs + TCAs, SSRIs
– wait 2 wks to switch (4 w/ fluoxetine b/c long ½ life)
– dont use w/ meperidine (Demerol) - Phenelzine
- MAOI
- SSRI action
-
- Selectively inhibit serotonin (5-HT) reuptake
- most do not manifest noradrenergic or D effects
– little affinity for muscarinic receptors - SSRI SE's
-
- altered GI motility, nausea, agitation, anxiety, sleep disturbance, tremor, and HA
- sexual dysfunction - Fluoxetine
- SSRI
- Sertraline
- SSRI
- Paroxetine
- SSRI
- Citalopram
- SSRI
- Venlafaxine
-
- SNRI devoid of antiH, antiCh, and antiadrendergic effects
– effective in depressed inpatients and outpatients, and relatively rapid therapeutic response
– SE’s like SSRI’s, but Idiopathic HTN may occur at higher doses - Bupropion
-
- noradrenergic uptake inhibitor
– doesn’t affect sexual function
– Zyban for smoking
– small risk of seizures
– not ok if hx seizures, head injury, or eating disorder - Mirtazapine
-
- enhances central noradrenergic and S neurotransmission
– Block presynaptic a2 R’s ïƒ increased 5-HT and NE release
– 5H2 and 5HT3 antagonist
– net effect is selective increase in 5HT1A fcn
– H1 blocker at lower doses
– Side effects wt gain, sedation, none sexual - Trazodone
-
– mixed 5-HT agonist/antagonist
– Weak 5-HT reuptake
– significant a1 blocker and H1 blocker -> orthostatic hypotension and sedation
– small doses as a hypnotic
- Priapism - Valproate
-
– anticonvulsant for acute manic episodes in BPD
– less effective in acute bipolar depression
– may decrease catabolism and turnover to increase GABA and increases GABAB-R density
– few SE’s compared to lithium, but include GI distress, benign elevations in hepatic transaminases, sedation, tremor, wt gain
– rare but serious are hepatic failure, pancreatitis, and thrombocytopenia - Lamotrigine
-
– anticonvulsant for bipolar depression and BPD maintenance
– no evidence of “switchingâ€
– if used w/ carbamazepine, double dosage b/c of enzyme induction
– if used w/ valproic acid, it must be halved b/c of enzyme inhibition - Carbamazepine
- – Extended-release anticonvulsant for BPAD manic and mixed episodes
- Atypicals for acute mania
- Olanzapine, Quetiapine