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46 Cards in this Set
- Front
- Back
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low - potency FGA
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chlorpromazine
thioridazine mORE LIKELY TO cause: sedation, orthostatic hypotension, anticholingergic side effects, weight gain. |
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thioridazine
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dose-related QTc interval
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Intermediate-potency FGA
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- Loxapine (Loxitane)
- Perphenazine (Trilafon) Moderate anticholingergic activity, sedation, EPS. |
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High Potency FGAs
- Require higher dose of antiparkinsian agents. |
Haloperidol (Haldol)
Fluphenazine (Prolixin) Thiothixene (Navane) Trifluoperazine (Stelazine) |
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Haloperidol (Haldol)
Fluphenazine (Prolixin) |
- depot DECANOTE injections.
- Haldol q4w (po x 10) - Prolixin q2w (po x 1.2) - More likely to cause EPS .... |
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Candidates for Depot Injections
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1. History of non-compliance
2. Need for long-term tx. 3. Good response to oral formulation 4. Decreased drug absorption 5. patient refused oral medication but is willing to take I.M. |
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FGA moa:
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D2 Antagonists in ALL four pathways, varying degrees of toerh receptor antagonism at muscarnic, alpha, histamic)
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SGA: "ATYPICALS"
Moa |
First line (except clozapine)
1. D2 and 5HT2A receptor antagonist effects A. 5HT2A reverses blockade at NIGROSTRIATAL pathway --> reducing EPS. B. 5HT2A antagonizes DA activity in the MESOCORTICAL pathway -> improve cognitive and negative symptoms. |
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Atypicals less than:
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1. less EPS
2. less TD 3. less hyperprolactinmia 4. improvement in negative sx and cog. 5. metabolic complications |
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Metabolic complications:
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1. weight gain
2. hyperlipidemia 3. hyperglycemia 4. lipid abnormalities 5. high b.p. |
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Aripiprazole (Abilify)
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Partial D2 Agonist:
- Hypodopaminergic -> agonist at mesocorticol, nigrostriatal, tuberoinfundibular. - Hyperdopaminergic -> antagonist (mesolimbic) |
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Aripiprazole A.E.:
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LESS METABOLIC COMPLICATIONS compared to other SGA.
1. Akathisia 2. Asthenia 3. n/v 4. constipation 5. anxiety 6. insomnia 7. dose related sedation |
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Should you adjust the dose?
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No need to adjust dose for renal or hepatic impairment --> but requied with CYP2D6 inhibitors
-> required with CYP3A4 inducers. |
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Clozapine:
MOA |
- low D2 blockade
- high 5HT2A blockade. - MAX DOSE : 900MG/DAY |
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BLACK BOX WARNING FOR clozapine
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1. Agranulocytosis (1%)
2. Seizures (5%) 3. Myocarditis 4. Other adverse respiratory and cardiovascular effects. 5. Increased MORTALITY in elderly pts w/ dementia-related psychosis. |
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What are the monitoring parameters for CLOZAPINE and frequency?
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WBC at least 3500 / mm3
ANC at least 2000/ mm3 Frequency? QW for 6 mo Q2w for 6 mo Q4W forever |
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What are the adverse effects of Clozapine?
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- syncope, dizziness, n/v, hypotension, drowziness, seizures, profuse salivation, agranulocytosis.
- metabolic sx. |
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What is clozapine used for?
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- treatment-refractory cases.
HIGHLY effective low incidence of EPS/TD. |
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What are the A.E. of Olanzapine (Zyprexa)?
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A.E.:
- DOSE-DEPENDENT SOMNOLENCE AND EPS. - Agitation, dizziness, orthostasis. - Weight gain, hyperglycemia, lipid abnormalities TRY TO AVOID IN OBESE PATIENTS. |
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Are there any dosage requirement for Zyprexa?
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- No dosage adjustments for zyprexa
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Are there any other uses for zyprexa?
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- bipolar depression with fluoxetine.
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Quetiapine:
(Seroquel and Seroquel XR) A.E. |
1. SEDATION
2. HA 3. Xerostomia 4. Constipation 5. Hypotension 6. Dizziness 7. LOW RISK OF EPS -> |
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Dose adjustments for quetiapine:
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- need adjustments done for HEPATIC INSUFFICIENCY.
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Quetiapine is aslo approved for:
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1. Parkinson's Disease
- Lowest D2 binding and rapid disassociation from D2 receptor 2. Bipolar depression |
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Black box warning for quetiapine
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Adults and children with MDD for worsening of their condition and/or emerging suicidal ideation and behavior. (suicidal)
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What was risperdone also approved for?
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- Adolescent 13 to 17 with schizophrenia.
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What are the A.E. of Risperodone?
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1. Dose dependent EPS (> 6mg/day or elderly > 2 mg/day)
2. Hyperprolactinemia 3. Hypotension, dizziness, somnolence 4. Less...but have weight gain. |
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What dosage adjustment do you need for Risperidone?
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1. Dose should be REDUCED for renal, hepatic, and geriatric.
2. LONG ACTING INJECTABLE ONLY:(Consta) -> overlap oral and I.M. for 3 weeks after 1st injection. |
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What is the active metabolite of Risperidone and what should you watch out for?
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Paliperidone ER (INVEGA)
- OROS oral delivery - CrCl 50 - 79 = 6 mg/day - CrCl 10 - 49 = 3 mg/day |
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What a.e. of paliperidone should you watch out for?
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QTc interval prolongation.
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Ziprasidone (Geodon) What other MOA should be added?
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- Inhibits serotonin and NE reuptake...should not be used depression.
- TAKE WITH FOOD. |
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What are some adverse effects of Geodon?
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LESS METABOLIC COMPLICATIONS.
1. Rare QTc interval 2. Rash, 3. Somnolence 4. Constipation 5. Dizziness 6. Nausea |
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What should patients watch out for with Geodon?
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Avoid in pt with QTc interval >450msec.
No dosage adjustment with P.O. but yes with I.M. (Cyclodextrin can accumulate renally. |
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What drugs available in oral solution?
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Abilify
Risperdal |
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in IM inj.
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- Geodon
- Abilify - Zyprexa - Risperdal (long acting) |
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ODT
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- Fazaclo
- abilify DISCMELT - Risperdal - zyprexa |
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What are the other major sideeffects with SGA antipsychotics?
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1. Increased Mortality in Elderly Patents with Dementia related psychosis.
-- NO ATYPICAL IS APPROVED FOR THis. 2. Hyperglycemia and DM. - monitor regularly 3. CV A.E. in elderly patients with Dementia - Related Psychosis: --> Use antipsychotics ONLY for psychotic sx. |
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What other labs values should be monitored for SGA?
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1. Personal/Family History (1st)
2. Weight (BMI)= Baseline, 12wks, quarterly. 3. Waist Circumference = bas,12wks,1yr. 4. B.P.= Baseline, 12 wks,1yr. 5. Fastin plasma glucose = base, 12wks, 1yr. 6. Fasting lipid profile = base, 12wks, 5yrs. |
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Psychosis.
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Presense of delusion or hallicinations with the ABSENCE of insight into their pathological nature.
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Delusions
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Fixed falso befiefs not based in reality or consistent with the pts religion or culture.
Ex. Bizarre, Grandiose, Jealousy, Persecutory, Somatic. |
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Hallucinations: Feeling something is not there.
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False sensory impressions or perception that occur in the absence of external simuli:
auditory, visual, olfactory, gustatory, tactile...continous or intermittent. |
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Schizophrenia
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a devastating, chronic though disoder in which pts are unable to develop interpersonal relationships or function in society on a daily basis.
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Nigrostriatal Pathway causes many EPS and TD? What are the different EPS, SX, and how do you treat each?
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1. Dystonia:
Types; A. Trimus: clenched jaw B. Tongue protusion C. Oculogyric Crisis: fixed upward gaze D. Torticollis: twisting movement of the neck. Treatment: I.V. and I.M. Anticholingerics or Benzo |
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Pseudoparkinsonism
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2. Pseudoparkison:
Rigidity, akinesia, bradykinesia, stooped posture, shuffling gait, tremr. tx: Anticholingers: Amantadine |
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Akathisia
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sense of subjective restlessness:
--> pacing, shuffling, or tapping feet. Tx of akathisia: 1. beta-blockers and benzo, or switch to SGA. |
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Tardive Dyskinesia
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Hyperkinetic movement Disorder:
- Facial and tongue movements (constant chewing, tongue protrusions, facial grimacing) - Limb movement: quick, jerky or choreiform test with AIM tx: prevention - which to CLOZAPINE (SEVERE) - SGA for mild to mod. |
