antipsychotics Flashcards
(PH-1) List the prototype antipsychotic drugs for the following classes of drugs: phenothiazines, thioxanthenes, and butyrophenones. (PH-2) Describe the mechanism of action of the prototype phenothiazine, thioxanthene, and butyrophenone drugs, categorize them according to potency, and describe their clinical uses and side effects. (PH-3) Describe the motor fluctuations seen both early and late during treatment with the first generation (Typical) antipsychotics. (PH-4) List the prototype atypi
typical antipsychotics
chlorpromazine, thioridazine, fluphenazine, thiothixene, haloperidol
use of typical antipsychotics
schizophrenia and manic bipolar
most potent typical antipsychotics
thoridazine,fluphenazine,
least potent typical antipsychotics
chloropramazine
most sedating typical antipsychotics
chloropramazine and thoridazine
least sedating chloropramazine
thiothixene, fluphenazine, halperidol
typical antipsychotics with most antipyrimidal effects
fluphenazine, halperidol
typical antipsychotics good for hiccups
chlorpromazine
MOA of typical antipsychotics
block dopamine receptors in mesolimbic-mesocortical system
type of dopamine receptor blockage giving anti-psychotic use
D2
typical antipsychotics with active metabolites
cholorpromazine, thioridazine, fluphenazine
SE of typical antipsychotics
motor sx(acute dystonia, akathisia, parkinsonian syndrome, motor fluctations, periobital tremor), endocrine disturbances, edema and weight gain, sedation, covulsions, autonomic SE, skin effects
treatment for motor SE of typical antipsychotics
anticholergenics
drug class to avoid in epileptics
typical antipsychotics
typical antipsychotics that can be used in epileptcis
fluphenzine
rare, but severe SE of typical antipsychotics
neuroleptic malignant syndomre
sx of neuroleptic malignant syndomre
severe parkinsonism with autonomic instability, stupor
drug for neuroleptic malignant syndomre
dantrolene
causes blue-grey skin
typical antipsychotics
typical antipsychotics + CNS depressents/opioids/antihistamines
potentates effects of 2nd drug
typical antipsychotics + L-dopa
less effect of L dopa
typical antipsychotics + TCA
additive anticholergenic effects
classic Atypical
clozapine
use of clozapine
refreactory schizophrenia
major, serious SE of clozapine
agranulocytosis
most potent antipsychotic of any class
clozapine
advantages of clozapine
less extrapyrimidal disfunction and hyperprolactinemia
receptor used by clozapine
D4
higher plasma levels of clozapine in users of
cigarettes
SE of clozapine
sedation, weight gain, diabetes, orthostatic hypotension, n/v, tachycardia,
contraindications of clozapine
bone marrow disorder, leukpenia, carbamazapine
atypical antipsychotics
risperidonw, olanzapine, quetiapine, ziprasidone
MOA of atypical antipsychotics
possibly acts at D2/serotinin receptors
SE of risperidone
high extrapyrimidal effects, weakness, sleep problems, sexual dysfunction
olanzipine SE
postural hypotension, somnolence, weightgain, akathisia
quietiapine SE
increased QT interval, possible cataracts
ziprasidone SE
possible weight loss, monot QT prolongment
prototype partial agonist antipsychotics
aripiprazole
use of aripiprazole
schizophrenia, actute mania
MOA of aripiprazole
partial D2 and 5-HT agonist
extensivly metabolized by CYP3A4 and CYP2D6
aripiprazole
SE of aripiprazole
anxiety, headache, sleep problems, GI problems
drug interactions with aripiprazole
CYP2D6 inhibitors (fluoxetine, paroxetine, quinadine)
advantages of aripiprazole
no extrapyrimidal sx, no weigh gain or male milk,
ways doc determine effective drug regimen
trial and error, prior history, premedical conditions, previoulis doc experience
time frame to see if drug(s) will work
2-3 weeks
new 2nd generation antipstchotics
asenapine,iloperidone, lurasidone
first line bipolar drugs
lithium, valproic acid
most commonly effective bipolar drug
lithium
first drug used to treat acute manic attack
antispychotic
drug used prophalacitly in bipolar
Li
most likely MOA of Li
dereases IP3 and DAG
SE of Li (therputic dose)
nausea, diarreha, drowiness, hypothyroidism, polydipsea/polyuria, bluntng of cognition,
bipolar drug not to be used in nursing moms
lithium
contraindicated drug with Li
NSAID, thiazides
clinical uses of valproic acid
anti-convulsant, manic phase of bipolar
black box warning of valprosic acid
possible hepatic failure (esp in kids)
tetragenic effects of valproic acid
neural tube defects
SE of valproic acid
possible liver failure, thrombocytopenia,
carbamazepine use
anti-convulsant also used in bipolar, aggressive behavior, anxiety
first line drug in mixed bipolar
carbamazepine
black box warnings of carbazepine
asian ancenstry, aplastic anemia/agranulocytosis, dermatigical tox
non black box SE of carbazepine
diplopia, ataxia