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RUSMpsychopharm6
Neuroleptics!
| Question | Answer |
|---|---|
| Positive symptoms are schizophrenia are most responsive to what class of neuroleptics? | typical neuroleptics (chlorpromazine, fluphenazine, trifluorperazine, haloperidol |
| What are positive symptoms of schizophrenia? | excess or distortion of normal function. Ie; hallucination |
| What are negative symptoms of schizophrenia? | Deficit in normal function - apathy, ambivalence, affect (flat, unchanged facial expression), association (loose thoughts, etc) |
| Negative symptoms of schizophrenia are most responsive to what class of neuroleptics | atypical (clozapine, risperadone, olanzadine) These drugs increase DA levels in the prefrontal cortex by blocking serotonin at 5-HT2--> relieving the negative symptoms of SCZ |
| typical neuroleptics act at what receptor? | D2 antagonist |
| atypical neuroleptics act at what receptor? | D2 and 5-HT2 receptor antagonist |
| The positive symptoms of SCZ are thought to be due to | excess DA in the limbic system |
| The negative symptoms of schizophrenia are thought to be due to: | Reduced DA in the prefrontal cortex due to excess serotonin (serotonin has inhibitory control over DA levels in the prefrontal cortex) |
| Mesocortical effects of D2-blocking neuroleptics? | relief of bizarre thinking in some pts. |
| Mesolimbic effects of D2-blocking neuroleptics? | Relief of personality and emotion dysfunction in some pts |
| tuberinfundibular effects of D2-blocking neuroleptics? | (tuberoinfundibular = ant. pituitary). DA has inhibitory control over secretions from the ant. pituitary. D2 blockers can cause gynecomasia and galactorrhea. |
| What evidence is there that GLU may play a role in psychosis? | PCP model: PCP binds to NMDA receptors and induces psychosis |
| What are the 3 main groups of typical neuroleptics? | Phenothiazines (the -zine drugs), thioxanthenes (thiothixene), and butyrophenones (haloperidol) |
| What group of neuroleptics are used unless otherwise c/i | atypicals |
| Other uses for neuroleptics | intractable pain, intractable hiccup, antiemetic, tourette syndrome |
| reason for orthostatic hypotension seen as a a/a of classical neuroleptics? | blockade of the alpha-1 receptor |
| What are the major a/a of classical neuroleptics | orthostatic htn, impaired ejaculation, extrapyramidal symptoms (tremor, TD, acute dystonias (twisting and repetitive movement due to sustained muscle contraction) bradykinesia, |
| What are EPS symptoms of classical neuroleptics | drug induced PD:( tremors, rigidity, bradykinesia), akathisia (sensation of inner restlessness / inability to keep still), acute dystonia, tardive diskinesia. |
| Describe the evolution of the EPS side effects of neuroleptics | 4 hours: acute dystonia, 4 days: akinesia, 4 weeks akathisia, 4 mo: tardive dyskinesia |
| What neuroleptic is often used as an antiemetic? | trifluoperazine |
| What drug is known to cause hyperglycemia in pre-diabetics? | chlorpromazine |
| An example of a low potency phenothiazine is? | chlorpromazine |
| and example of a high potency phenothiazine is | trifluoperazine and thioridazine |
| What neuroleptic drug has an active metabolite that is more active than the parent drug. | Thioridazine ----> mesoridazine (active metabolite) |
| Tourette syndrome rx (neuroleptic) | haloperidol |
| What is the mode of action of cloazapine | High affinity for D4 receptors (antagonist) and moderate affinity for D2 (antagonist). Also 5-HT. MINIMAL EPS |
| Side effects of clozapine? | **fatal agranulocytosis** blood test required weekly. |
| indications of clozapine? | Use only in pts not responsive to classicals. must blood test weekly |
| What enzymes metabolize clozapine | CYP1A2 and CYP2D5 (lots of drug-drug interactions). |
| What drug is metab'd by both CYP1A2 and CYP2D5 | Clozapine |
| Risperidone: indications | Used for + and - symptoms of SCZ. Useful in maintenance therapy as it can be taken once / day |
| Rispeidone is metab'd by: | CYP2D6 |
| Risperidone acts on what receptors | Preferentially blocks mesolimbic D2 receptors and 5-HT2a. |
| Wt gain in pt taking neuroleptics is in due to action on what receptor | 5-HT2c |
| What drug is useful for pts who responded to classical neuroleptics but could not tolerate side effects. This drug is also used to treat bipolar I | olanzapine |
| Weight gain is a common problem with what neuroleptic? | olanzapine (acts on 5-HT2C) |
| Common adverse effects of olanzapine | wt gain (5-HT2c action), somnolence (H1 blockade). Rare, but fatal NMS syndrome (fever, delerium but no muscle rigidity) in some pts. |
| NMS (neuroleptic management syndrome) features what symptoms? | Severe muscle rigidity (except olanzapine), altered consciousness (stupor, catatonia), and autonomic instability, (also elevated serum creatine phosphokinase and myoglobinemia). Discontinue drug immediately and give IV dentrolene to relieve muscle symptom |
| What drug, along with block D2 and 5-HT2a receptors, also inhibits NE and 5-HT reuptake? | Ziprasidone. Useful for mood disorder elements of schizoaffective disorder, as well as +/- symptoms of SCZ. Prolongs QT interval |
| What drug is Useful for mood disorder elements of schizoaffective disorder, as well as +/- symptoms of SCZ. and has the side effect of Prolonged QT interval. | ziprasidone |
| Preferred drug for pt who is both psychotic and suffering from PD. | quetiapine |
Created by:
rkirchoff
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