Miscellaneous Quiz / Anti-psychotics

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Can you name the Anti-psychotics?

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P-kinetics: Systemic availability from 25-35%. Major metabolite is mesoridazine, which is more potent than the parent compound. Fatal if OD --> ventricular arrythmias.
P-kinetics: D4 = α1 > 5-HT2 > D2 = D1 ** also potent at H1 -> sedation. Agranulocytosis in 2% of pts -- mand. weekly blood cts. Be careful & slow withdrawing -- cholinergic reboun
Haloperidol class
SE: Teratogenic -- contraindicated during pregnancy
P-kinetics: α1 = 5-HT2 >D2 >D1. Inexpensive, lots of side effects. Be careful and slow withdrawing -- cholinergic rebound.
MOA: Block a variety of CNS, ANS, & endocrine effects via blockade of a variety of receptors: dopamine, α1 adrenergic, muscarinic ACh, H-1, & 5-HT2 receptors
P-kinetics: Notable SE include cardiotoxicity & retinal pigmentation. Be careful & slow withdrawing -- cholinergic rebound.
Use to prevent recurrence in bipolar disorder
Molindone class
SE: Few EPS but notable weight gain
Use: bipolar if Li+ is ineffective. Can also be used in combo with Li+
Trifluoperazine class
Clozapine class
P-kinetics: D2 > D1 = D4 > α1 > 5-HT2. 65% bioavailability. Severe EPS.
SE: CNS: Parkinson's syndrome, akathisia, dystonia (from dopamine receptor blockade); tardive dyskinesia (supersensitivity of dopamine receptors), toxic-confusional state (from mus
Thiothixene class
P-kinetics: Monovalent cation, well absorbed (complete in 6-8 hrs, peak levels in 30 min - 2 hrs). Distributed in TBW, some sequestered in bone, no PRO binding.
Thioridazine class
Aripiprazole class
SE: Rare toxicities: neuroleptic malignant syndrome (life threatening!!) --- caused by excessive rapid blockade of dopamine receptors (extremely sensitive extrapyramidal effects);
Olanzapine class
Pimozide class
SE: Skin discoloration (blue-gray), rash
Perphenazine class
SE: ANS: Loss of accom, dry mouth, diff urinating, constipation (from muscarinic cholinoceptor block); orthostatic hypotension, impotence, failure to ejaculate, (from α adrenocept
SE: Muscle rigidity, impaired sweating, fever, autonomic instability (BP & HR) - tx w/ muscle relaxants (diazepam, dantrolene), dopamine agonist (bromocriptine), cooling (if fever)
SE: Uncertain toxicities
Fluphenzine class
Loxapine class
P-kinetics: Less efficacious mood stabilizer
Use: 'Schizophrenia'
SE: enters breastmilk at 30-50% of plasma levels (poor suck reflex, cyanosis, hepatomegaly); dysmorphogenesis unclear -- may cause cardiac malformations. Other: edema, leukocytosis
Valproic acid class
SE: Other: weight gain (from possibly combined H1 and 5-HT2 blockade). Dysmorphogenesis: relatively safe during pregnancy, however, there is a small increase in teratogenic risk.
P-kinetics: Most are readily but incompletely absorbed. Most are highly lipid soluble & PRO bound (92-99%), large vol of distrib, much longer DOA than predicted by t1/2.
P-kinetics: Efficacy = lithium during early weeks of therapy
Use: bipolar depression
SE: Broad efficacy, few EPS at low dose, EPS and hypotension at high dose. Dosing daily or Q 2 weeks
SE: Endocrine system: amenorrhea-galactorrhea, infertility, impotence (from dopamine receptor blockade resulting in hyperprolactinemia).
Ziprasidone class
Lithium carbonate class
Carbamazepine class
Use: May help tx-resistant patients. Avoid for first episodes (compliance!!)
Quetiapine class
SE: Renal: polydipsia, polyuria. Cardiac: 'sick sinus' brady-tachy. Pregnancy: renal clearance increases during pregnancy and decreases postpartum (watch for toxicity);
Risperidone class
MOA: Note: 5-HT2A receptor activation on dopaminergic cell bodies and axon terminals inhibits the release of dopamine… thus 5-HT2A antagonists --> more release of dopamine
Anti-manic and mood stablizer
P-kinetics: Not metabolized, 90% excreted in urine. T1/2 = 20 hours
Use: Good for negative & positive symptoms (schizophrenia, acute mania, and bipolar). Avoid for first episodes (compliance!!)
Lamotrigine class
Use: Schizophrenia and manic phase of bipolar disorder
MOA: Na+/Li+ exchanger in AP. Enhances actions of serotonin, decreases NE & DA turnover, may block DA receptor sensitivity, may augment synthesis of ACh
P-kinetics: Extensive first pass metabolism (except thioridazine). Very little is excreted unchanged. Elimination half-lives vary from 10-24 hours.
SE: Tardive dyskinesia: late-occuring, choreoathetoid-like mvmts, caused mainly by older antipsychotics, continue even when drug is d/c'd, may be irreversible.
Chlorpromazine class
SE: GI: n/v, diarrhea. Neuro: motor movement disorders (tremor - reduced by propanolol and atenolol), mental confusion (toxic doses). Thyroid: hypothyroid like symptoms.
MOA: 5-HT2A & D2 agonists. Lower D2 potency -> fewer EPS.
Use: acute mania or prophylactic. Can be used as monotherapy or in combo for refractory pts

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