PHARM FINAL DRUGS Flashcards
Chlorpromazine (Throrazine)
Phenothiazine, 1st generation antipsychotic (neuroleptic)
low potency, increased cardiovascular/sedation due to alpha, anticholinergic and histamine blocking
Fluphenazine (Prolixin, Prolixin Decanoate [IM])
Phenothiazine, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS
*Available in long-acting depo forms (decanoate and enanthate)
Prochlorperazine (Compazine)
Phenothiazine, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS
**Used as antiemetic
Trifluoperazine (Stelazine, Suprazine)
Phenothiazine, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS
Haloperidol (Haldol, Haldol Decanoate [IM])
Butyrophenone, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS
Clozapine (Clozaril)
Atypical antipsychotic
Blocks mesolimbic dopamine receptors (D4), also blocks 5HT receptors, strong anticholinergic
Little EPS.
**Agranulocytopenia, and agranulocytosis,
Seizures, weight gain, hyperglycemia, T2D, myocarditis
TX: suicidal behavior
Olanzapine (Zyprexa)
Atypical antipsychotic Similar to clozapine, less bone marrow tox. **Weight gain, hyperglycemia >EPS than clozapine TX: schizo and mania
Risperidone (Risperdal)
Atypical antipsychotic Block D2/4 and 5TH receptors >EPS than clozapine and olanzapine **Weight gain and hyperglycemia *Most widely used, available in depo
Aripiprazole (Abilify)
Atypical antipsychotic
*MOA: partial agonist/antagonist at D2 and 5HT-1a receptors
less ESP, less metabolic issues, but less efficacious that clozapine/olanzapine/respiradone
Quetiapine (Seroquel)
Atypical antipsychotic
MOA similar to clozapine BUT less efficacious
Low tendency of EPS
**NO agranulocytosis, high cost
Ziprasidone (Geodon)
Atypical antipsychotic
Same as quetiapine:
MOA similar to clozapine BUT less efficacious
Low tendency of EPS
**NO agranulocytosis, high cost
**fewer metabolic complications (weight gain/hyperglycemia)
Antipsychotic 1st generation (neuroleptics) drug effects
only for positive symptoms
Sedation early in therapy. Lowers seizure threshold. Antiemetic - especially prochlorperazine. Poikilothermia. Anticholinergic** (dry mouth, loss of visual accommodation), constipation, urine retention). Antihistiminic action - sedation. Cardiovascular effects** (Orthostatic HypoTN, tachycardia, EKG changes, sudden cardiac death - Torsades). Sexual dysfunction (alpha blocking). Increased prolactin secretion (due to decreased dopamine) gynecomastia, lactation, menstrual problems. Weight gain, increased appetite, edema, and effect on insulin/glucose metabolism. Teratogenic
Antipsychotic 1st gen neuroleptics Toxicities
idiosyncratic/allergic - blood dyscrasias, obstructive jaundice, rash, phototoxicity, cardiotoxicity, increased mortality with comorbid dementia.
EPS - acute dystonia (days) TX: benztropine, Trihexiphenydyl
akathisia (days-weeks) TX: anticholinergic, propranolol, benzos
parkinsonism (days-months) TX: Anticholinergics
Tardive dyskinesia (Months-years) TX: none, may need to resume antipsychotic
NMS (days-weeks) TX: Dantrolene or bromocryptine (inhibit release of Ca from sarcoplasmic reticulum)
Imipramine (Tofranil, Janimine)
TCA - Prototype
See TCA effects/tox
Amitriptyline (Elavil)
TCA
**More sedation and anticholinergic activity than imipramine
Fluoxetine (Prozac)
SSRI
MOA: inhibitor of 5HT reuptake
Use: antidepressant, OCD, generalized anxiety, and premenstrual dyphoric disorder, bulimia, anorexia, other eating disorders.
**Less sedation, anticholinergic, and cardiovascular effects than typical TCAs
SEs: headache, anxiety, tremor, agitation, nausea, sexual dysfunction. Potential for drug interaction with liver metabolism +active metabolites