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61 Cards in this Set

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  • Back
What are the major chemical subgroups of the older antipsychotics?
phenothiazines (chlorpromazine, thioridazine, fluphenazine)
thiozanthenes (thiothizene)
butyrophenones (haloperidol)
What are newer "second-generation" antipsychotic drugs?
Heterocyclic structure including clozapine, loxapine, olanzapine, risperidone, quetiapine, ziprasidone, and aripiprazole
Which antipsychotic drugs have parenteral forms that are used for rapid initiation and depot therapy?
fluphenazine and haloperidol
What are the 3 main reasons excess dopamine is thought to cause schizophrenia?
1. Many antipsy drugs block D2
2. dopamine agonist drug exacerbate schizophrenia
3. increased dopamine receptors in schizophrenia patient
Which receptor do the older antipsychotic drugs work on? What is the negative side effect?
1. D2 repector
2. blocking can cause extrapyramidal dysfunction due to D2 found at caudate putamen, nucleus accumbens, cerebral cortex, and hypothalamus
Which receptors does Clozapine act on?
D4 and 5-HT2 receptor-blocking action
Which receptors does atypical drugs (Olanzapine, quetiapine, and risperidone) act on?
5-HT2A mainly and some D2
Which receptors does Ziprasidone act on?
ANTAGONIST at D2, 5-HT2A and 5-HT1D,
AGONIST 5-HT1A
Which receptors does Aripiprazole act on?
partial agonist at D2 and 5-HT1A receptor,
strong ANTAGONIST 5-HT2A
With the exception of _____, all antipsychotic drugs block H1 receptor to some degree.
HALOPERIDOL
Which dopaminergic tract regulates mentation and mood?
mesocortical-mesolimbic
Which dopaminergic tract regulates extrapyramidal function?
nigrostriatal pathway
Which dopaminergic tract regulates control of prolactin release?
tuberoinfundibular pathways
Which dopaminergic tract regulates emesis?
chemoreceptor trigger zone
______ dopamine receptor blockade presumably underlies antipsychotic effects
mesocortical-mesolimbic
What are the positive symptoms of schizophrenia?
hyperactivity, bizarre ideation, hallucinations, and delusions
____ is effective in some schizophrenic patients resistant to treatment with other anytipsychotics drugs?
Clozapine
Newer atypical drugs are reported to improve some of the negative symptoms of schizophrenia, including ___, ___, and ___
emotional blunting, social withdrawal and lack of motivation
Which two antipsychotic drugs are used for maintence of bipolar disorder?
olanzapine and aripiprazole
____ is used mainly for Tourette's syndrome and rarely used in schizophrenia
Molindone
With the exception of ___, most phenothizines have antiemetic actions
thioridazine
Which phenothiazine is solely used for antiemetic actions?
prochlorperazine
____ blockade, most often present in short side-chain phenothiazines, provide the basis for their use as antipruritics and sedatives and contribute to antiemetic effects?
H1 receptor blockade
Extrapyramidal side effects most common with which antipsychotics?
haloperidol and piperazine side-chain phenothiazines (fluphenazine and trifluoperazine)
Neurologic dysfunctions akathisia and dystonias from antipsychotics can be treated with what 2 agents?
diphenhydamine or muscarinic blocking agents
What antipsychotic toxicity could be IRREVERSIBLE?
Tardive dyskinesias - choreaoathetoid movements of the muscles of the lips and buccal cavity
Treating extrapyramidal effects with antimuscarinic drugs may cause what side effect?
INCREASE tardive dyskinesia
How does increasing the neuroleptic dosage affect tardive dyskinesias?
TEMPORARILY decrease suggesting tardive dyskinesia may be caused by dopamine receptor sensitization
Which antipsychotic drug has the STRONGEST autonomic effect? WEAKEST?
Strongest- Thioridazine
Weakest- Haloperidol
___ and most the atypical drugs have intermediate autonomic effects?
Clozapine
Which two antipsychotics drugs do NOT have atropine side effects?
ziprasidone and aripiprazole
Which antipsychotics have the most atropine (dry mouth, constipation, urinary retention, and visual problems) side effects?
Thiordiazine and phenothiazines with aliphatic side chains (chlorpromazine)
Which antipsychotics are known to cause postural hypotension caused by A-blockade
older antipsychotics such especially phenothiazines
Which antipsychotics can cause orthostatic hypotension?
atypical drugs
Failure to ejaculate is common in men treated with ___
phenothiazines
What are the main endrocrine and metabolic side effects of antipsychotics?
hyperprolactinemia, gynecomastia, the amenorrhea-galactorrhea syndrome and infertility
Which antipsychotic has prominent elevated prolactin side effect?
Resperidone
Significant weight gain and hyperglycemia due to a diabetogenic action occur with several of the atypical agents, especially ___ and _____
clozapine and olanzapine
Which two antipsychotic drugs has little or no tendency to cause hyperglycemia, hyperprolactinemia, or weight gain?
Aripiprazole and ziprasidone
Drugs used to treat malignant hyperthermic syndrome of antipsychotic drugs?
dantrolene, diazepam, and dopamine agonist
What is the most sedating antipsychotic drug?
phenothiazines especially CHLORPROMAZINE
Which two of the older antipsychotics are least sedating?
fluphenazine and haloperidol
Which newer antipsychotic is least sedating?
aripiprazole
Visual impairment caused by retinal deposits has occurred with ___, at high does, this drug may also cause severe conduction defects in the heart resulting in fatal ventricular arrhythmias
thioridazine
Most atypicals, especially ___, prolong QT interval of the ECG; the underlying myocardial effect may lead to cardiac arrhythias (torsades)
Ziprasidone
____ causes small but important (1-2%) incidence of agranulocytosis and at high doses has caused seizures
Clozapine
Most neuroleptics lower the convulsive threshold and may cause seizures which are treated with ___ and ___
diazepan or phenytoin
Target therapeutic plasma concentration for Lithium is ___
0.8-1.2 mEq/L and for maintenance 0.4-0.7 mEq/L
What drugs can cause a increase of Lithium in the blood to toxic levels?
Thiazides, NSAIDS, ACEIs, loop diuretics and also Dehydration
___ and ___ increase the renal clearance of lithium
Caffeine and theophylline
MoA of Lithium
inhibits inositol monophosphatase, rate limiting enzyme for generation of IP3 and DAG in 2nd messenger amine neurotransmission
____ continues to be the standard treatment of bipolar disorder
Lithium carbonate
Acute mania can be treated with what 3 drugs?
Lithium, valproic acid and olanzapine
What drugs are required for the initiation of bipolar treatment?
Antipsychotics and/or benzodiazepines due to slow onset of lithium and valproic acid
Other then lithium, what drugs can be used in the maintenance of bipolar disorder?
Aripiprazole and olanzapine, as well as anticonvulsants carbamazepine and lamotrigine
Adverse neurologic effects of lithium include ___, ___, __ and ____. ___ enlargement may also occur
tremor, sedation, ataxia and aphasia. Thyroid
____ kidney problem occurs commonly at therapeutic lithium levels
Reversible nephrogenic diabetes insipidus
What skin problems can occur with lithium therapy?
Edema and acneiform skin eruptions
What side effect is ALWAYS present with lithium therapy?
Leukocytosis
The use of Lithium during pregnancy is thought to increase the incidence of ____
congenital cardiac anomalies (Ebstein's anomaly)
Can nursing mothers use Lithium?
NO, should even stop 24-48 hours before delivery