Antipsychotic Drugs

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Antipsychotic Drugs

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• ??????? ?????? ??? ? ???? ???? ?????

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Terminology

• ???? (Psychosis) ???? ????????? ?? ???????? ????
  ???.
• ???????? (Schizophrenia) ??? ???? ?? ???? ??
  ????? ???? ??? ??????? ???? ??? ?? ???????? ?????
  ???? ?????? ?? ??? ?????????
• ?? ??? ???? ?? ???? ??? ?????
• ??????? ??? Major tranquilizer
• ????????Neuroleptic
• ?? ???? Antipsychotic

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Schizophrenia Clinical Features???????? ?????
??????

• ????? ???? (?????? ?? ?????? ????? ?????)
• ???? (Hallucination) ?????? ?? ???
• ????? (Delusions) ?????? ?? ????
• ????????? ?? ????? ???? ???? ? ?????
• ????? ???? (???? ?? ????? ????? ?????)
• ???? ?? ??????? ??????
• ?? ?? ??? ???? ????
• ???? ???????? ? ??????
• ???? ????? ??????? ? ?????? ????

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Antipsychotics

• Typical antipsychotics which are mainly
  dopamine (D2) blockers
• Atypical antipsychotics which block dopamine as
  well as serotonin (5HT) receptors causing their
  therapeutic efficacy

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??????? ?? ???? ??????

• ????????
• ?????????
• ?????????
• 1- Clozapine
• 2- Resperidone
• 3- Olanzapine
• 4- Aripiprazole

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??????? ?? ???? ????

• ??????? ?? ???? ?? ??????????? ? ??????????
• ??????? ?? ???? ???? ?????????? ?????????
  ??????????? ???????? ??? ???????????

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High Potency Typicals

• ????? ????? ????? ???? ???? ? ?????? ????
  ????????? ????????.
• Fluphenazine (Moditen)
• Haloperidal (Haldol, Sernase)
• Loxapine (Loxitane)
• Molindone (Moban)
• Perphenazine (Fentazin)
• Thiothixene (Navane)
• Trifluoperazine (Eskazina)

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Atypicals

• Clozapine (Leponex,Clozaril)
• Olanzapine (Zyprexa)
• Quetiapine (Seroquel)
• Risperidone (Risperdal)
• Ziprasidone (Geodon)
• Aripiprazole
• Pimozide (Orap)

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Indications

• ????? ???? ???
• ????? ??????
• ????? ???
• ????? ??? ??????? ?? ?????? ?? ????? ???????
• ????? ??? ????
• ?? ???? ? ???????
• ?? ?????

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HALOPERIDOL Indications

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• ?????? ??????? ?? ???? ? ???????? ??
• ???? ????
• ???????? ?????? ?? ?????? ????? ??? ?????
• ?????
• ?????

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Antipsychotic side effects

• ????
• ????? ???? ???? ????? ???????? ??????? ? ?????
  ??? ?????????
• ????? ???? ????????? ????? ????? ? ???? ????
• ????? ???????
• ???? ???? ??? ??????

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Parkinsonian-like effects????? ??? ??????????

• ???? ????? (??????? ????? ?????? ???? ????? ???)
  ????? ???? ?? ????
• ???? ?? ?????? ?????
• ???? ?? ???? ?????????? ????? ?? ??????
  ?????????? ? ??? ???? ?????? ? ???? ???????? ??
  ????? ???? ????????

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Acute dystonia ??????? ???

• ?????? ?????? ????? ?? ???? ?? ???? (????? ????)
  ? ????? ????? ???? ?????????
• ???? ?? ??? ??? ??? ?????
• ????? ????? ????? ???? ???????????? ????
  ???????? ? ?? ????? ??? ?????? ????? ???????

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Akathisia????????? ????? ?????

• ?? ???? ? ???? ???
• ???? ?? ?????? ?????
• ????? ???????? (???????????) ?? ??????????????

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Tardive Dyskinesia (TD)??????? ??????

• ????? ?????? ?????? ??????? ?? ????? ????? ???? ?
  ??? ? ???? ???? ???
• ???? ????? ?? ????? ??? ?? ????? ?? ???? 5 ?????
• ??????? ????? ?? 40-20 ?????
• ?????? ??? ?? ????????
• ??? ????? ?????? ???? ?? ??? ????? ?????? ????
  ??????.

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Contraindication

• Hypersensitivity
• Parkinsons disease
• Bone marrow depression

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Warning

• Neuroleptic Malignant Syndrome
• Antiemtic effect
• Agranulocytosis
• Pregnancy C (Clozapine B)
• Lactation not established

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Drug Interaction

• ???????????? ????? ????? ????? ? ????? ??????
  ???????? ?????
• ???? ??? CNS ? ???? ???????? ?? ????? ?????
  ??????? ? ???? ?????????
• ?? ????????? ???? ??? ??? ??????
• ?????? ????? ????? ?????? ??? ????? ????? ?????
  ? ?????? ???? ???? ?? ????? ??? ???? ??? ????
  ???? ? ..

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Typical anipsychotics
Trade name Dosage form Generic name
Largactil,Normazine Tab25-100mg,Amp50mg/2ml Chlorpromazine
Fluanxol Amp20mg/ml , IM Flupentixol
Modecate, Moditen Amp25mg/ml IM,Tab1-2.5mg Fluphenazine
Haldol, serenace, HALODIC Tab0.5,2,5mg,Drop2mg/ml, Amp5mg/ml(lactate)IM,IV 50mg/ml (decanoate) IM Haloperidol
Fentazin Tab2,4,8 mg,Amp5 mg/ml IM,IV (slow, dilute) Perphenazine
Mellaril Tab10,25,100 mg Thioridazine
Cap5 mg Thiothixene
Eskazina Tab1,2,5 mg, Amp1 mg/ml IM Trifluoperazine
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Dosage
Maximum Daily Dose Increments (mg/d) Initial Daily Dose Initial Daily Dose Agent
150 mg 10-25 mg 10-50 mg Thioridazine Thioridazine
5 mg 0.25-0.5 mg 0.25-0.5 mg Haloperidol Haloperidol
5 mg 0.5 mg 0.5 mg Fluphenazine Fluphenazine
15 mg 1 mg 1 mg Trifluoperazine Trifluoperazine

10 mg 2 mg 2 mg Perphenazine Perphenazine
Divided doses may be necessary to decrease adverse effects Divided doses may be necessary to decrease adverse effects Divided doses may be necessary to decrease adverse effects Divided doses may be necessary to decrease adverse effects Divided doses may be necessary to decrease adverse effects
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Pediatric

• ?????????? 3 ??? ? ?? ????
• ?????? ??? ????
• 0.05-0.075 mg/kg/day ORALLY
• MAX 6 mg/day
• ????????
• 12 ??? ? ?? ????
• ??????????
• 2 ??? ? ?? ????

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Advice to Patient Phenothiazine

• ????? ????? ???? ?????????? ???????? ???? ????
  ??? ??????? ????? ???? ????
• ????? ?? ???? ??? ?? ??

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?? ???? ????

• ????????
• ????????
• ?????????
• ???????????

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LozapineLeponex Clozapex

• ???? ?? ???????????
• ?? ???? ??????
• ?????? ???? ?? ???????? ?????
• ??? 25? 100 ???? ????
• ?????? ??? ?????? mg 900
• ????? ?????
• ?????? ???? ????? ?????????????? ?? ???? 1
• Clozaril Patient Monitoring Services(CPMS)
• ???? ? ??????? ? ?????
• ?????? ???? ???? 40-12
• ?????? ???????? ???? 10
• ?????? ??? ???15-5
• ????????????? ? ??????? ?????????

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Agranulocytosis

• ??? ????????????? 1????
• ????? ?? 6 ?? ??? ??? ?? ?? ???? ???? ??? ?? ???
• ?????? WBC?? 6 ??? ??? ?? 2 ????
• ?? ??? ???? ????? ???? ????? ???

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Clozapine Advantages

• ?? ????? ????? ?? ??????? ?? ???? ???? 50-30 ????
  ????? ?? ???????? ????? ?? ????
• ????? ?? ????? ????? ???? ???? ?? ??????? ????
• ????? ????? ???? ???? ???? ? ????? ???? ?? ??????
  ?????????

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Clozapine Disadvantages

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• ??? ???? ?????? ?? ???
• ?????? ???
• ??? ??? ?????? ? ???? ?? ??? ??? ??????

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???? ???? ?????

• ?????? ??? ???? (???? ????????) ?? ?????? ?? ???.
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• ????? ?????? ??? ???? ????? ? ????
• ???????? ???? ?? ????? ??????? ????
• ??????? ? ??? ???? ?????????

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isperidone (Risperdal, Risbiodal)

• Benzisoxazole
• ???? ?? ???? ????? ????
• ???1 ? 2 ? 3 ? 4 ???? ???? ?????? ??? ??????
  mg/kg 6
• ?????? ???? ?????????????
• - ???? ?????? ??? 5-HT2 ? D2
• - ???? ?????????
• ??? ?? ??? ????? ???? ????? ?????? ?? ?????
  ?????? ? ?????? ?????? ???? ????? ? ???????
  ?????? ? ???????
• ??? ?? ??? ?? ??? ???? ??? ???.
• ??????????? ??????

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Advice

• Food does not affect the rate or extent of
  absorption of oral risperidone. Therefore,
  risperidone can be administered without regard to
  meals
• Photosensitivity
• Orthostatic hypotension

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OlanzapineZyprobiox, Zyprexa

• Tab 2.5,5, 10 ,15 mg
• can be taken with or without meals.
• No routine blood monitoring is required
• Pregnancy risk C

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QuetiapineSeroquelBioquetinTranqopine

• Tab 25 , 100 , 150 and 200mg
• ?? ???????? ?? ??? ???? ????? ???? ????
• ????? ??????? ?? ????
• ?????? ??? ????
• ?????? ????
• ?? ?????
• ??????? ?? ????
• ????? (?????? ??? ?? 10 ????)
• ?????????? ???? ? ???? ??????

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Aripiprazole (Abilify? Abilizol Biopiprazole)

• Tab 5, 10 and 15 mg 30 mg
• ????????
• ??????? ?? ????
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• ?????? ??? ????
• ??????? ?? ???????
• ????? ?? ????? ??

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???? ???? ?????

• ??? ??? ??????? ????
• ??? ?? ??? ??? ???? ?????? ????? (???? ???? ??
  ??? ?? ????? ??????????? ???? ??? ???? ?? ??????
  ?? ??? ??? ?? ????? ????? ??? ?? ????? ???).

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Pimozide (Orap)Tab 4 mg

• ?????? ??? ???? ???? ? ?????
• ???????? ????
• ??? ??????????
• ????? 12 ???
• ?? ???
• FDA Pregnancy Category C