Trifluoperazine + Chlordiazepoxide Pharmacology
Trifluoperazine + Chlordiazepoxide
Trifluoperazine
Antiemetic activity: Antiemetic activity is by blocking dopamine receptor (D2 receptor) in the Chemoreceptor trigger zone (CTZ)
Distribution: It is distributed widely in the body in protein bound form.
Metabolism: It is metabolised in the liver.
Excretion: It is excreted mainly through urine. Small amount of drug is excreted through faeces and breast milk.
2. Extrapyramidal reactions
3. Drowsiness
4. Sedation
5. Dizziness
6. Hypotension
7. Dry mouth
8. Constipation
9. Blurred vision
10. Agranulocytosis
11. Photosensitivity
12. Insomnia
13. Weight gain
14. Cholestatic jaundice
2. Comatose
3. Blood dyscrasias
4. Patient taking antidepressants
5. Liver damage
2. Hepatic impairment
3. Cardiovascular disease
4. Pheochromocytoma
5. Hypocalcaemia
6. Epilepsy
7. Cholestatic jaundice
8. Patient exposed to extreme heat or cold or phosphorus insecticides
9. Ceribrovascular disorder
10. Patient on ECT
11. Reaction to Insulin
12. Prostatic hyperplasia
13. Glaucoma
14. Peptic ulcer, slowly withdraw the drug with caution
2. Schizophrenia
3. Antiemetic
4. Anxiety
5. Behavioural disturbances
6. Mania
Almunium Salts: Decrease efficacy. Antacids should be given 1 hour before or 2 hours after chlorpromazine.
Anticholinergics: Decrease efficacy and increase the anticholinergic side effects of chlorpromazine.
Barbiturates: Decreases efficacy.
Barbiturate anaesthetics: Increase frequency and severity of neuromuscular excitation and hypotension.
Bromocriptine: Efficacy decreased by chlorpromazine.
Charcoal: Prevents absorption of chlorpromazine.
Epinephrine, Norepinephrine: Pressor effect decreased, peripheral vasoconstrictive effect antagonised.
Lithium: Disorientation, unconsciousness and extra-pyramidal symptoms.
Meperidine: Excessive sedation and hypotension.
TCAs: Serum concentration increased by chlorpromazine.
Valproic acid: Efficacy potentiated.
Propranolol: Increased plasma levels of both drugs.
MAOIs: Additive orthostatic hypotensive effect.
Lab. Tests: Pregnancy tests: False positive results.
Plasma bound iodine (PBI): Increase in PBI occurs.
Psychoses, Schizophrenia
Out patients: 2 - 4 mg / day in 2 divided doses. Dose can be increased depending on the severity of the disease.
Inpatients: 4 - 10 mg / day in 2 divided doses. Dose can be gradually increased up to 40 mg / day.
Antiemetic, Anxiety: 1 - 2 mg twice daily. Dose can be increased up to 6 mg / day in some case.
Children:
Psychoses, Schizophrenia: 1 - 2 mg / day. Dose can be gradually increased up to 15 mg / day.
Chlordiazepoxide
2.Drowsiness
3.Lethargy
4.Hallucination
5.Nausea
6.Constipation
7.Amnesia
8.Dependence
9.Pain at the site of injection
10.Confusion
11.Depression
12.Mood changes
2.Hepatic impairment
3.Myasthenia gravis
4.Respiratory disease
5.Jaundice
6.Use caution while driving vehicles, operating machines or other dangerous activities
children < 6 years: contraindicated
NEONATES- contraindicated
2.Treatment of alcohol withdrawal symptom
3. Insomnia
4. Pre and post operative apprehension
Aminophylline: Antagonizes the sedative effect.
Cimetidine, Oral contraceptives, Disulfiram, Fluoxetine, Isoniazid, Ketoconazole, Metoprolol, Propoxyphene, Propranolol.
Valproic acid: Elimination of chlordiazepoxide decreased due to inhibition of hepatic metabolism leading to enhanced activity.
Digoxin: Increase in serum concentration of Digoxin.
Imipramine & Desipramine: Enhanced activity of these drugs.
Levodopa : Decrease in antiparkinsonism efficacy.
Morphine, Pethidine, Atropine and Magnesium trisilicate: Absorption of chlordiazepoxide is impaired.
Probenecid: May cause rapid onset or prolonged effect.
Rifampicin: Decreases efficacy.
Severe anxiety: 20 - 25 mg 3 - 4 times daily
Treatment of alcohol withdrawal symptom: 25 - 100 mg daily; Depending on the patient`s condition dose can be reduced after 2 - 3 weeks
Pre and post operative apprehension: 5 - 10 mg 3 - 4 times daily; the drug should be given one day before surgery in pre operative apprehension
Children: 5mg 3 - 4 times daily.
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