Antipsychotic

Maryam Umar
ROLL NO 4313
 INTRODUCTION

– Also known as neuroleptics/ major tranquilizers

– • Used to treat schizophrenia and to reduce the symptoms
associated with psychotic conditions such as bipolar, psychotic
depression
– • To eliminate psychotic features (positive/ negative) like in
schizophrenia and psychotic symptoms associated with other
psychiatric disorders and physical illness
Typical Antipsychotics

– • Old antipsychotics (1950)

– • Haldol (haloperidol) and Thorazine (chlorpromazine)
– • Cheap drugs
– • 1st generation
– • DRA’s (Dopamine Receptor Antagonists)
– • Target positive symptoms (delusions & hallucination)
– • Higher risk of side effects
Atypical Antipsychotics

– • New antipsychotics (1990)

– • Expensive • 2nd generation
– • SDA’s (Serotonin Dopamine Antagonists)
– • Target both positive and negative symptoms
MECHANISM OF ACTION

– Act on dopamine’s five pathways

– • Mesolimbic-mesocortical pathway
– • Nigrostriatal pathway
– • Medullary-periventricular pathway
– • Incertohypothalamic pathway
– • Tuberoinfundibular pathway
– These pathways affect thinking, cognitive behavior,
learning, sexual and pleasure feelings, and the
coordination of voluntary movement.
– • Extra firing (production of this neurotransmitter) of
dopamine in these pathways produces many of the
symptoms of schizophrenia.
Anti-psychotic Groups
– Phenathiazine antipsyhotic:
– •Classified as typical antipsychotic
– •Dopamine – 2 receptors antagonist = decrease the effects of dopamine in the
brain a. Chorpromazine b. Thioridazine c. Fluphenazine
2. Thioxanthene:

– Act by blocking postsynaptic receptors for dopamine in brain

– a.Clopenthixol
– b. Flupenthixol
– 3. Butyrophenone: Also act as antiemetic (a drug that is effective against
vomiting and nausea)
– a. Haloperidole = triperidol + denperidol
– 4. Dibezodiazepine:
– a. Clozapine
– b. Olanzapine
– 5. Dibenzothiazepine:
– a. Quetiapine
– 6. Substituted Benzamides:
– •Sulpride
– •Amisulpride (more popular)
– 7. Benzisoxazole:
– a. resperidole
Side effects of Typical
Antipsychotics
– • EPS (Extrapyramidal Symptoms)
– • Akathisia (movement disorder characterized by feelings of inner restlessness,
compelling and fidgeting)
– • Torticollis (abnormal head/ neck position)
– • Neuroleptic Malignant Syndrome (NMS)= muscle rigidity, fever, autonomic
instability and cognitive changes (delirium)
– • Tardive Dyskinesia (TD) involuntary movement mostly effect lower face • Tic
Disorder (rapid, sudden, non- rhythmic movements)
– Side
Side effects of Atypical
Antipsychotics
– • Metabolic syndrome
– • 4 up’s (blood pressure, sugar level, weight and cholesterol)
– • Inturn increase the risk of heart attack, stroke and diabetes
 Extrapyramidal symptoms These
symptoms include

❑dystonia (continuous spasms and muscle contractions)

❑akathisia (motor restlessness)
❑parkinsonism (characteristic symptoms such as rigidity),
❑bradykinesia (slowness of movement),
❑tremor
❑tardive dyskinesia (irregular, jerky movements).
1. Phenothiazine

– A. Chlopromazine: Antipsychotic action:

– Reduce delusions and hallucinations
– Develop an insight in psychotic patient
– Dose vary for sleep and vomiting As antipsychotic dose= 400-800 mg (per day)
indications:

• Psychotic disorder, psychosis, schizophrenia

• Manic phase of the bipolar disorder
• Several behaviors and conduct disorders
• anxiety
• Vomiting
• insomnia
• Hiccups
Contraindication:

– Hepatitis
– Hypersomnia
– Glaucoma
– Prostatic hypertrophy
– Renal/ kidney problems
– Delirium
– Other serious physical illnesses
Mechanism of action:

– Block D2 receptors
– Reduce delusions and hallucinations
Side effects:

– Over sedation
– ➢Jaundice
– ➢Constipation
– ➢Urinal problems
– ➢Drowsiness
– ➢Vertigo
– ➢Postural hypotension
– ➢Dryness of mouth
– ➢EPS
– ➢Non- hypersentivity to drugs
– Precautions: Avoid driving Avoid alchol Avoid during pregnancy Lactio mother
should also avoid
 Precautions:

– Avoid driving Avoid alchol

– Avoid during pregnancy
– Lactio mother should also avoid
B. Thioridazine

– Not as much sedative as chlorpromazine

– Indication: Psychosis Anxiety Used as ad joint therapy in depression
– Dose: 5-20 mg daily in divided dose
Side effects:

– ➢Same as Chlorpromazine except postural hypotension which is not included in

its side effects
– ➢Blindness
– ➢Non- hypersentivity to drugs
C. Fluphenazine

– an injection Dose:
– ➢25-50 mg weekly to monthly
– ➢In one week one injection administered.
– 2nd can not be administered before one week
Side effects:

– Side effects:
– ➢EPS
– ➢Neuroleptic malignant syndrome (NMS)
– ➢Same side effects as of chlorpromazine
– ➢Non- hyper-senstivity to drugs
Indication:

– ➢Usually for non- compliance patient

– ➢used as: Depo injection
– Decanote intramuscular
2. Thioxanthene

– Clopenthixol Indication:
– ➢Psychosis Dose: 200 mg weekly to monthly Side effects:
– NMS ➢All previously discussed side effects
– ➢Non-hypersentivity to drugs
– ➢But have relatively better side effects profile
– Mechanism of action:
– ➢Target D1 and D2 receptors
B. Flupenthixd

➢It is stimulant drug which excite body functions e.g. increase speech and decease
appetite Indication:
➢Stupor condition
➢Wonderful for anxiety
➢patient having poor compliance with medication
➢People having schizophrenia and suffer from frequent relapse in illness
– Dose:
– ➢2.5 mg tablet daily
– ➢100 mg injection
– ➢It is antipsychotic in higher dose
– ➢It is anxiolytic in lower dose Mechanism of action:
– ➢Antagonist of D1 and D2 dopamine receptors
– ➢Its antipsychotic activity is related with blocking postsynaptic dopamine in
CNS
Butyrophenone

– A. Haloperidol
– ➢Tablet, liquids, injections
– ➢Excellent safety profile
– ➢Safe in conditions like hepatitis, pregnancy, lactating mother
– ➢A cheap drug
Indication:

– • Psychotic condition specially with delusions and hallucination

– • Chronic schizophrenia (alogia, anhedonia and associality)
– • Negative symptoms of schizophrenia
– • Haloperidol target positive symptoms
– • It is anxiolytic in low dose
– • Ad joint therapy in depression
– • Ad joint therapy in OCD
– • Use for sedation
Dosage:

– • No more than 10 mg per day

– • In western countries only 7.5 mg is recommended
– • For non- aggressive patient 15 mg per day is recommended
– • Rage of dose = 2-60 mg
– Mechanism of Action: D2 receptor blocker Block dopamine and increase its
turnover rate
– Side Effects:
– ➢Akathesia (extreme restlessness)
– ➢Torticollis (dystonic condition/ asymmetrical head and neck position)
➢Neuroleptic Malignant Syndrome (NMS)
– ➢EPS
– ➢Blurring of vision
– ➢Tardive dyskinesia (Stiff jerky movements of face and body)
– ➢Dryness of mouth
– ➢Retention of urine
– ➢Constipation
– ➢Sedation
– ➢Non- hypersensitivity to drugs
– Contraindications:
– Not in case when patient is alcoholic
– Glaucoma
– Driving
– Epileptic
4.Benzodiazapine

– A. Olanzapine:
– Wonderful atypical antipsychotic medicine
– Indications:
– ➢Same as of haloperidol
– ➢But it target both positive and negative symptoms
– ➢Used with specifically with the psychotic patients having sleep problem as
main issue
– ➢Manic patient= Haloperidol+ Olanzapine
– ➢Sleep disturbance ➢Restlessness ➢Low diet (Olanzapine stimulate appetite)
– Side Effects:
– ➢Weight gain
– ➢It specifically increase urge to take carbohydrates
– ➢Metabolic syndrome
– ➢Increase lipid rate
– ➢Increase glucose levels
– ➢Increase sleep
– ➢Increase appetite
– ➢Minimum chance of NMS and EPS
– ➢Non- hyper sensitivity to drugs
Precautions

➢Should not recommended to drivers

– ➢Diabetic patients
– ➢Patient of hypertension
– ➢Obesity
– ➢Ischemic heart disease: Condition effecting supply of blood due to
cholesterol/ restrict blood vesscles