Antipsychotics Flashcards
Neuroleptic dug MOA?
Blockade of dopamine receptors in the brain.
Atypical neuroleptics also act as antagonists or partial antagonists to serotonin receptors.
The chief antipsychotic effects of neuroleptic drugs appear related to the dopamine blockade at which receptor site?
D2 receptors
Psychotic experiences have been linked to excess release of __________ in the ___________ pathway?
Psychotic experiences have been linked to excess release of dopamine in the mesolimbic pathway?
Common SE of neuroleptic drugs
Tremors/Parkinsonian effects Tardive dyskinesia Blurred vision, dry mouth, constipation Urinary retention Increased prolactin release
What is tardive dyskinesia?
Facial grimacing and inappropriate posturing of the tongue, neck, trunk and limbs
Tardive = continues on or first appears after drugs are no longer being taken.
What is neuroleptic malignant syndrome?
Additional SE that rarely occurs. Characterized by catatonia, fluctuating BP, dysarthria and fever.
What is the protocol when a case of neuroleptic malignant syndrome comes on?
Immediately discontinue drug and tx with dopamine agonist like BROMOCRIPTINE.
Neuroleptic drugs can also be helpful in tx this condition due to the fact that they block D2 receptors in the chemoreceptor trigger zone of the medulla?
Severe nausea
Neuroleptics are anti-emetic
Chlorpromazine/Thorazine
Class:
Ind:
MOA:
Chlorpromazine/Thorazine
Class: Neuroleptic
Ind: Psychosis, mania, schizophrenia, N/V, intractable hiccoughs
MOA: D2 dopaminergic receptor site blockade.
Add’l MOA: alpha-adrenergic blockade and H1 blockade
What hormone commonly has an increased release as a result of the dopamine blockade?
Prolactin
SE: galactorrhea and amenorrhea in women and infertility in both sexes
Prochlorperazine/Compazine
Class:
Ind:
MOA:
Prochlorperazine/Compazine
Class: Typical neuroleptic
Ind: Psychosis, vertigo, N/V associated with migraine HA
MOA: Primarily H1-histamine receptor antagonist as well as alpha-adrenergic receptor antagonist and D2 dopaminergic receptor antagonist
Prochlorperazine/Compazine
Char:
SE:
Prochlorperazine/Compazine
Char: Less orthostatic hypotension, fewer extrapyramidal signs, better anti-emetic than other neuroleptics
SE: Lowers seizure threshold
Haloperidol/Haldol
Class:
Ind:
MOA:
Haloperidol/Haldol
Class: Typical neuroleptic
Ind: Psychosis, tourette’s, Huntington’s dz, ACUTE AGITATED BEHAVIOR
MOA: D2 dopaminergic receptor site blockade
Haloperidol/Haldol
Char:
SE:
Haloperidol/Haldol
Char: Careful administration to reduce excessive sedation and tardive dyskinesia
SE: Parkinsonian-like sx, extrapyramidal effects, tremor, NEUROLEPTIC MALIGNANT SYNDROME
Clozapine/Clozaril Class: Ind: MOA: Char:
Clozapine/Clozaril
Class: Atypical neuroleptic
Ind: Schizophrenia
MOA: Receptor site blockade at D2 and 5-HT2 (serotonin) receptors
Char: PO, rapid absorption and extensive metabolism