antipsychotic

Question 1

neuroleptic drugs

Answer 1

do not cure underlying dz- help pt funx more effectively
classified as typical(1st gen) or atypical(2 gen)
main MOA- blockade of dopamine receptors in brain- both classifications affect various receptor subtypes of NE, acetylcholine, & histamine
atypical also serve as antagonists or partial antagonists to serotonin receptors

Question 2

neuroleptic drug receptors blockade

Answer 2

• 5 dopamine receptors identified, blockade of D2 receptors
• psychotic experiences have been related to excessive dopamine in the mesolimbic pathway
• non-specific blockade of dopamine in other pathways is what is thought to cause unfavorable SE in the drugs

Question 3

adverse effects of neuroleptic drugs

Answer 3

• tremors/parkinsonian effects- dystonia, extrapyramidal signs
• tardive dyskinesia- facial grimacing, involuntary movements that may appear & continue after drug is ceased
• blurred vision, dry mouth, constipation, urinary retention
• inc prolactin release
• postural hypotension
• sexual dysfunction
• drowsiness
• anti emetic effects are common- tx for nausea of chemotherapy

Question 4

neuroleptic malignant syndrome

Answer 4

rare SE from neuroleptic drugs
catatonia, fluctuating blood pressure, dysarthria, fever
may be fatal if drug is not discontinued immediately & pt receives tx with a DOPAMINE AGONIST(BROMOCRIPTINE)

Question 5

chlorpromazine/ thorazine

Answer 5

typical neuroleptic
for psychosis, mania, schizophrenia, N/V & **intractable hiccoughs
MOA- chiefly D2 dopaminergic receptor site blockade. also alpha-adrenergic blockade & H1 blockade(anti-histamine effects)
SE- INC release of PROLACTIN- glalctorrhea & amenorrhea in women, infertility in both sexes. same SE as previously mentioned(parkinsonian sxs)

Question 6

prochlorperazine/ compazine

Answer 6

typical neuroleptic
for psychosis, vertigo, N/V- particularly assoc. w/migraine
MOA- H1-histamine receptor antagonist, alpha-adrenergic receptor antagonist, D2 dopaminergic receptor antagonist
-better anitemetic effect than other neuroleptics
-less orthostatic hypotension & extrapyramidal signs than chlorpromazine
SE- drowsiness, dry mouth, constipation, urinary retention. lowers seizure threshold. extrapyramidal signs usu only w/high doses for long periods

Question 7

haloperidol/ haldol

Answer 7

typical neuroleptic
for psychosis, tourette’s, huntington’s dz, ACUTE AGITATED BEHAVIOR
MOA- chiefly D2 doapminergic receptor site blockade. less muscarinic & alpha-adrenegric receptor blockade as compared to other neuroleptics
-careful admin to prevent excessive sedation & tarditive dyskinesia
SE- parkinsonian-like sxs, EXTRAPYRAMIDAL effects(m/b dramatic), NEUROLEPTIC MALIGNANT SYNDROME is a sig. possibility

Question 8

clozapine/ clozaril

Answer 8

atypical neuroleptic(1st developed)
for schizophrania- esp when other anti-psychotics have failed or produced undesirable effects
MOA- multiple receptor site blockade- mostly on D2 & 5-HT2(serotonin) receptor sites
PO- rapid absorption & extensive metabolism
SE- less extrapyramidal than other drugs. AGRANULOCYTOSIS in 1-2% of pts, MYOCARDITIS, s/t severe weight gain

Question 9

respiradone/ risperdal

Answer 9

atypical neuroleptic
for psychosis
MOA- presumed dopamine & serotonin receptor blockade
SE- extrapyramidal sx, tarditive dyskinesia, constipation, sedation.WEIGHT GAIN< HYPERGLYCEMIA & DM. inc risk of STROKE in older pts.
slow withdrawl recomended to red. risk of acute psychosis

Question 10

olanzaprine/ zyprexa

Answer 10

atypical neuroleptic
for schizophrenia when other drugs have failed
MOA- multiple receptor site blockade, esp. D2 & 5-HT2 receptor sites
PO, rapid absorption & extensive metabolism
SE- relativly diminished extrapyramidal SE compared to other neuroleptics. WT GAIN, HYPERGLYCEMIA< DM. inc risk for STROKE in elderly

Question 11

lithium salts

Answer 11

prophylactic tx of bipolar DO, and tx of manic episodes
MOA- exact MOA unknown- widely distributed in CNS, interacts with many neurotransmitters & receptors- dec NE release & inc serotonin synthesis. diminishes CNS response to glutamate

Question 12

lithium carbonate/ eskalith

Answer 12

lithium salt
for bipolar DO & manic episodes, schizophrenia
MOA- previous slide
char- cleared by kidneys, narrow TI- must check blood levels frequently!! sxs of high blood lvls- lethargy, confusion, diarrhea, abd pn, N/V, ataxia, severe tremors. seizures can develop as well cardiotoxicity
SE- wt gain, cognitive impairment, short term memory deficits- lack of compliance
reduced renal response to ADH= impaired urine concentration capacity
**nephrogenic diabetes insipidus= polyuria in 20% of pts on chronic tx
**hypothyroidism 5-35% of pts on long term therapy