Antipsychotic Drugs

Question 0

General Side Effects of Neuroleptics

Answer 0

Tremors, tarditive dyskinesia, blurred vision, dry mouth, constipation, urinary retention, prolactinemia.

Question 1

General Neuroleptic MOA

Answer 1

General blockade of dopamine receptors in the brain. Especially D2 receptors. May also affect NE, ACh and histamine R as well. Affects mesolimbic pathway. Most neuroleptic drugs have an antiemetic effects.

Question 2

Neuroleptic Malignant Syndrome

Answer 2

A slow-onset syndrome which displays progressive catatonia, fluctuating HTN, dysarthria and fever. MAY BE FATAL. Antidote: bromocriptine.

Question 3

Chlorpromazine (Thorazine)

Answer 3

Typical neuroleptic. Used for psychosis, mania, schizophrenia, N/V, intractable hiccoughs.
MOA - dopamine D2 R blockade, alpha-andrenergic blockade and H1 histamine blockade.
SFx - tarditive dyskinesia, extrapyramidal signs, increased prolactin(!) leading to galactorrhea and ammenorrhea in women, and infertility in both sexes.

Question 4

Prochlorperazine (Compazine)

Answer 4

Typical neuroleptic. Used for psychosis, vertigo, N/V, especially when associated with migraine HA.
MOA - primarily H1 blockade, but also D2 and a-andrenergic blockade.
SFx - dry mouth, constipation, urinary retention, lowers seizure threshold.

Question 5

Haloperidol (Haldol)

Answer 5

Typical neuroleptic. Used for psychosis, tourette’s, Huntington’s, and especially for acute agitation. Must be administered carefully to avoid TD. PO, IV.
MAO - D2 receptor antagonist.
SFx - Parkinson’s-like sxs, neuroleptic malignant syndrome.

Question 6

Clozapine (Clozaril)

Answer 6

Atypical (second generation) neuroleptic. Used for schizophrenia, especially when other agents have failed or had severe sfx. Rapidly absorbed orally.
MOA - D2 and 5-HT receptor blockade.
SFx - fewer extrapyramidal effects compared to other neuroleptics. Agranulocytosis can occur (monitor CBC and discontinue if WBC fall below 1500. Myocarditis can also occur.

Question 7

Respiradone (Risperdal)

Answer 7

Atypical neuroleptic. Used for psychosis. Reduce dose in liver dz pts.
MAO - unknown, but presumed to be dopamine and 5-HT R blockade.
SFx - WEIGHT GAIN and hyperglycemia in DM pts. Extrapyramidal effects, sedation, constipation, Stroke risk in elderly pts.

Question 8

Olanzapine (Zyprexa)

Answer 8

Atypical neuroleptic. Used for schizophrenia, especially when other agents have failed.
MOA - D2 and 5-HT R blockade.
SFx - fewer extrapyramidal effects than other neuroleptics. May cause wt gain, hyperglycemia in DM pts, and increased stroke risk in elderly population.

Question 9

Lithium Carbonate (Eskalith)

Answer 9

Lithium salt. Used for BPD and mania, schizophrenia. Cleared by kidney and has very low TI. Check blood levels frequently.
MOA - unknown but may dampen NE and glutamate response.
SFx - Wt gain, memory deficits, impaired concentration (due to reduction in ADH from kidneys), NEPHROGENIC DI in 20% of pts! Hypothyroidism(!) in 5-35% of pts. High blood levels can be CARDIOTOXIC.