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antipsychotic
4th exam
20
Pharmacology
Professional
12/10/2012

Additional Pharmacology Flashcards

 


 

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Term
Antipsychotic  drugs 
Definition

All of the AP drugs have some effect on D2 receptor.Many atypical AP's are 5-HT2A inverse agonsts. No evidence indicaing that antagonism of any DA receptor other than D2 plays a role in anipsychotic action.Most atypical and some of the typicals have a higher affinity for the 5-HT2A receptor than the D2 receptor. Some can also antagonize α2 adrenoceptors

Term
Chlorpromazine
Definition
  • Aliphatic derivative (less potent, but more sedation and weight gain).
  • It has very strong anticholinergic (M1) effect and should be avoided in elderly.
  • causes deposits in the anterior portion of the eye, accentuate normal aging of the lens
  • α1-blockade →orthostatic hypotension
  • H1 - antagonism→ sedation (some tolerance can develop; rebound insomnia/sleep disturbance)
  • H1augmented by 5-HT2C blockade - weight gain
  • seizure risk
  • can cause cholestatic jaundice (rare) and skin rxns/photosensitivity
  • treatment for uncontrolled hiccups
  • inhibits CYP2D6

α1=5-­HT2A>D2>D1

Term
Thioridazine
Definition
  • Piperidine Derivative (less potent)
  • can cause retinal deposits that are associated with "browning" of vision (max doses are limited to reduce this ADR)
  • H1/5-HT2Cantagonism -but more sedation and weight gain
  • black box warning regarding torsade/fatal arrhythmias
  • inhibits Na+channels and at higher doses Ca2+channels
  • has no antiemetc effect
  • inhibits CYP 2D6


Term
Perphenazine, trifluperazine, fluphenazine
Definition
  • Piperazine derivatives (more potent and selective in their Pharmacological effects)
  • Fluphenazine is availabel in long acting injectable formulation
  • Perphenazine inhibits CYP2D6
Term
Thiothixene
Definition

Thioxanthene derivatives (potent)

Typical

Term
Haloperidol
Definition
  • Most widely used typical  drug
  • Diphenylbutylpiperidines (pimozide) are closely relatedcompounds.
  • Compared to phenothiazines, butyrophenones and congeners: Tend to be more potent; Tend to have fewer autonomic effects;  Tend to have greater EPS.
  • black box warning regarding torsade/fatal arrhythmias
  • available in a long acting injectable form

D21>D4>5-HT2A>D1>H1

 

Term
Pimozide
Definition
  • "Newish" typical, used for Tourette Syndrome
  • black box warning regarding torsade/fatal arrhythmias


 

Term
Clozapine
Definition
  • 1st Atypical. It is considered a 2nd -line. Clozapine has unique effectiveness in refractory disease.
  • used in the patients with suicide attempt history
  • Lower risk of hyperprolactinemia. It has a very strong antimuscarinic effect (M1) and should be avoided in elderly
  • It is also M4 agonist - causes Sialorrhea
  • α1- blockade → orthostatic hypotension
  • H1; H1/5-HT2c antagonism - sedation; weight gain (some tolerance; rebound insomnia/sleep disturbance)
  • 3-5% seizure risk
  • associated with myocarditis
  • 1% develop agranulocytosis (reversible, can't be rechallenged)
  • not approved for acute mania
  • levels drop by 50% in smokers
  • should never be discontinued abruptly unless it's  an emergency

D4=α1>5-­HT2A>D2=D1

Term
Loxapine
Definition

Atypical, but classified as typical sometimes. It is closely related to Clozapine, however it's active metabolite causes EPS like typical drugs

Term
Asenapine
Definition
  • Atypical (FDA 2009)
  • not extensively metabolized
Term
Iloperidone
Definition
  • New Atypical
  • Not approved for acute mania
Term
Olazapine
Definition
  • Atypical, 2nd line drug
  • high doses have effectiveness in refractory disease
  • H1/5-HT2c antagonism →weight gain
  • H1antagonism alone - sedation
  • dyslipidemia -reversible upon discontinuation
  • hyperglycemia, impaired glycemic control  - Usually reversible
  • approved as monotherapy for maintenance of mania
  • available in a long acting injectable form
  • w/fluoxitine approved for bipolar depression
Term
Quetiapine
Definition
  • Atypical.
  • Its metabolite has antimuscarinic effect (M1), but not as storng as Clozapine and Chlorpomazine.
  • dyslipidemia, but not as much as with clozapine/olanzapine
  • hyperglycemia - much lower than with clozapine/olanzapine
  • H1antagonism - sedation
  • effective as monotherapy for bipolar depression (NE reuptake inhibition), also effective in trials for unipolar depression
Term
Paliperidone and Risperidone
Definition
  • Atypical.
  • Risperidone is an active metabolite of Paliperidone  (except 10%people who are poor metabolizers).
  • Unlike other atypicals, they have higher risk of hyperprolactinemia.
  • hyperglycemia and dyslipidemia -some risk, but not as much as with clozapine/olanzapine (both usually reversible)
  • Resperidone (inject) is approved as  maintenance monotherapy for mania
  • Resperidone approved for irritability in autism
Term
Sertindole
Definition
Atypical. Not yet approved due to issues with sudden cardiac death
Term
Ziprasidone
Definition
  • Atypical
  • not extensively metabolized
Term
Aripiprazole
Definition

Atypical. Partial D2 agonist. 90%  D2 occupancy; It gains its efficacy thorough 5-HT2Aantagonism and maybe 5-HT1Apartial agonism. Has a low risk of hyperprolactinemia.

Term
Promethazine
Definition
  • Phenothiazine
  • Storng H1 antagonism - used for insomnia and preoperative sedation
Term
Butyrophenone droperidol
Definition
  • used in neuroleptanesthesia (with fentanyl)
  • used in postoperative to decrease N&V
Term
Prochlorperazine
Definition
  • primarily prompted as antiemetic
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