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Antipsycho/alzheimer
UVa med pharmacology block 2
| Question | Answer |
|---|---|
| Chlorpromazine | 1st gen antipsychotic, Potent D2 receptor antag. Tx acute psychotic sx's of schizo/schizo affect, mania, tourette's, huntingington's, emesis early=sedation, delayed=alleviates psychotic affects, others=alpha1 antag, H1 antag T1/2 30hrs |
| Thioridiazine | 1st gen antipsychotic, Potent D2 receptor antag. Tx acute psychotic sx's of schizo/schizo affect, mania, tourette's, huntingington's, emesis fx similar to chlorpromazine w/decr potency |
| Trifluoperazine, Perphenazine, Thiothixene | 1st gen antipsychotic, Potent D2 receptor antag. Tx acute psychotic sx's of schizo/schizo affect, mania, tourette's, huntingington's, emesis fx similar to chlorpromazine w/intermediate potency |
| Haloperidol | First gen antipsychotic, sim to chlorpromazine w/incr potency added side fx = incr extrapyrimidal fx, decr anticholinergic, no sedation/postural hypotension |
| Fluphenazine | First gen antipsychotic, sim to chlorpromazine w/incr potency added side fx = incr extrapyrimidal fx, decr anticholinergic, no sedation/postural hypotension |
| Fluphenazine decanoate | First gen antipsychotic, sim to chlorpromazine w/incr potency added side fx = incr extrapyrimidal fx, decr anticholinergic, no sedation/postural hypotension delivery by injection |
| Clozapine | 2nd gen (atypical) antipsychotic, psychotic px's resistent to classic tx - incr effec against neg symptoms improved tx profile w/5-HT2a antag & D2 blockade fewer sidefx than first gen, can have agranulocytosis (1-2%) |
| Olanzapine | 2nd gen (atypical) antipsychotic, psychotic px's resistent to classic tx - incr effec against neg symptoms improved tx profile w/5-HT2a antag & D2 blockade, not as good as clozapine fewer sidefx than first gen, no agranulocytosis, no weight gain |
| Risperidone | 2nd gen (atypical) antipsychotic, psychotic px's resistent to classic tx - incr effec against neg symptoms improved tx profile w/5-HT2a antag & D2 blockade, not as good as clozapine fewer sidefx than first gen, no agranulocytosis, no weight gain |
| 1st gen anti-psychotic side effects | CV:a1-blockade = vasodil, orthostat hypoten, neg inotrop Autonom: anticholin-dry mouth, blur vis, constip, urine reten alpha antag-inhib ejac, miosis Endo-galac/amenorrhea, decr libido other = neurolep malig syn, decr seizure thresh, parkinson sx's, T |
| Tacrine | AChE inhib - alzheimer's tx some cognitive benefits in early stage of disease - does not slow course of disease |
| Donezepil | AChE inhib - alzheimer's tx some cognitive benefits in early stage of disease - does not slow course of disease |
| Memantine | non-competitive NMDA-receptor antag - alzheimer's dis (moderate/severe) - blocks pathological & mild activation of NMDA well tolerated, doesn't interfere w/acquisition/processing of cognitive info |
| What are some Classic Antipsychotics other than Chlorpromazine? How do their side effects compare? | Low Potency - Thioridazine: |
| What is the defining property of Chlorpromazine? | Potent D2 receptor Antagonist |
| What are the differences between 1st generation and 2nd generation (Atypical) Anti-psychotics? | 2nd Generation: - More effective in treating negative symptoms/cognitive deficits of Schizophrenia. - Less Extrapyramidal side effects. - When 1st generation not effective, sometimes 2nd generations are. |
| How do other classic Antipsychotics compare to Chlorpromazine in effectiveness? | All of the classic antipsychotics, in proper regimen, give Qual/Quan the same antipsychotic effects. |
| Besides a Dopamine blocker, what other receptors does Chlorpromazine affect? | - Alpha1 Antagonist (Hypotension, Sexual Dysfunction) - Weak Muscarinic Antagonist (Autonomic side effects) - Weak H1 Antagonist (Sedation) - Noncompetitive Channel Blocker (Calcium, Sodium --> Cardiac side-effects) |
| How long does it take for the effect of Anti-Schizophrenic treatment with First generation Antipsychotics? | Several weeks, and by that time, peripheral/sedative effects have decreased. |
| What are the Late onset "Neuroleptic" side effects of Chlropromazine? | Extrapyramidal Symptoms: - Tardive Dyskinesia (Irreversible, Untreatable). *Usually occurs after years of chronic administration and involves up to 20% of chronic Schizophrenic in-patients. |
| How do you manage the Extrapyramidal side effects of Chlropromazine? | - Reduction in Dose - Can administer Anticholinergic Antiparkinson drugs (Diphenhydramine, Trihexiphenidyl, Benztropine). *Tardive Dyskinesia is usually untreatable. |
| What is the clinical use of Chlorpromazine? | Treats acute psychotic symptoms (Schizo, mania, severe agitation) |
| What are side effects of Chlorpromazine other than the Extrapyramidal ("Neuroleptic") side effects? | - Oversedation - Seizures* (in patients with Hx or epilepsy) - Vasodilation*/Orthostatic Hypotension* (from Alpha1 block) - Tachycardia, Long QT interval Dry mouth, blur vision, constipation, urine retention. Weight gain Galactor/Amenorrhea |
| How does Chlorpromazine cause Galactorrhea and Amenorrhea? | Antagonize the tonic inhibitory effect of Dopamine on release of Prolactin. |
| What is the side effect profile of Clozapine? | Very anticholinergic, almost NO Extrapyramidal symptoms. Lowers seizure threshold. *1-2% Agranulocytosis, fatal if unchecked. |
| Which Antipsychotics have the highest risk for Obesity as a side effect? | Clozapine and Olanzapine. |
| What are the Early onset "Neuroleptic" side effects of Chlropromazine? | Extrapyramidal symptoms: - Parkinson-like (Muscle rigidity, "pill rolling" tremor, akinesia, shuffling gate, immobile facies) - Akathisia (Constant pacing/restlessness) - Acute Dystonia (Torticollis*, Oculogyric Crisis) - Occur more commonly in childr |
| What are some uses of First-Generation Antipsychotics? | Schizophrenia Tourette Syndrome Huntington's Chorea (Hyperkinesia treatment) Acute Manic episodes (Until Lithium builds up) Schizo-affective disorders Emesis |
| Olanzapine, Respiredone are also 2nd generation Antipsychotics. What is their side effect profile? | - Unlike Clozapine: No Agranulocytosis - Hypotension - Lower seizure threshold - Weight Gain (Olanzapine) - Neuroleptic Malignant Syndrome - Some EPS symptoms (Tardive Dyskinesia is possible), but still much less than 1st generation drugs. |
| When is Clozapine used clinically? | When other antipsychotic agents have failed. It must be accompanied by weekly WBC due to chance of Agranulocytosis. |
| What causes the Extrapyramidal side effects of Chlorpromazine? | The blockade of D2 receptors in the Sriatum. This leads to an increase of ACh and striatal output. This can explain the "Early" effects, but not the "Late" effects (Tardive Dyskinesia). |
| What are the Rapidly Developing effects of Chlorpromazine (CPZ)? | - Sedation - Disinterest for environment - Psychomotor slowing - Emotional quieting *Sometimes referred to as "Chemical Straightjacket". |
| What is Neuroleptic Malignant Syndrome? | Rare reaction to Antipsychotics: - Hyperthermia - Muscle Rigidity - Autonomic Symptoms (Hypertension, Incontinence) - Stupor Requires IMMEDIATE Treatment! |
| What is a possible drug interaction to be aware of with Chlropromazine? | Combination with CNS Depressants can lead to over-sedation. |
| What are the delayed effects of Chlropromazine (CPZ)? | Alleviates tension, hyperactivity, combatitiveness, hostility, hallucinations, delusions, insomnia, anorexia. |
| Why are Dopamine antagonists used for Schizophrenia? | Schizophrenia is a disease of the Frontal cortex / Limbic structures, which contain Dopamine receptors. No evidence shows that there is an abnormality in activity of Dopaminergic neurons or DA receptors per se. |
| How does Risperidone and Olanzapine's effectiveness compare to Clozapine? | When used on patients with refractory Schizophrenia, Clozapine is more effective. |
| What receptor do 2nd generation (Atypical) Antipsychotics exert their effect at? | D1/D2 antagonists, and also 5-HT2A antagonists (This could give anti-hallucinogenic effects). |
Created by:
sam.mrosenfeld
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