Trifluoperazine + Chlordiazepoxide Pharmacology

Trifluoperazine + Chlordiazepoxide

About Trifluoperazine + Chlordiazepoxide
Mechanism of Action of Trifluoperazine + Chlordiazepoxide
Pharmacokinets of Trifluoperazine + Chlordiazepoxide
Onset of Action for Trifluoperazine + Chlordiazepoxide
Duration of Action for Trifluoperazine + Chlordiazepoxide
Half Life of Trifluoperazine + Chlordiazepoxide
Side Effects of Trifluoperazine + Chlordiazepoxide
Contra-indications of Trifluoperazine + Chlordiazepoxide
Special Precautions while taking Trifluoperazine + Chlordiazepoxide
Pregnancy Related Information
Old Age Related Information
Breast Feeding Related Information
Children Related Information
Indications for Trifluoperazine + Chlordiazepoxide
Interactions for Trifluoperazine + Chlordiazepoxide
Typical Dosage for Trifluoperazine + Chlordiazepoxide
Schedule of Trifluoperazine + Chlordiazepoxide
Storage Requirements for Trifluoperazine + Chlordiazepoxide
Effects of Missed Dosage of Trifluoperazine + Chlordiazepoxide
Effects of Overdose of Trifluoperazine + Chlordiazepoxide


About Trifluoperazine
First-Generation Antipsychotic, piperazine-phenothiazine derivative, Typical Antipsychotic, antiemetic,antimanic.
Mechanism of Action of Trifluoperazine
Antipsychotic action: Trifluoperazine binds to the dopamine receptor (D1, D2, D3 &D4).It exerts its antipsychotic activity by blocking the dopamine projections in the limbic system and in mesocortical area. Peripherally and centrally it acts as a competitive Dopamine antagonist. Trifluoperazine also produces alpha adrenergic blocking activity and anticholinergic activity. It also produces weak H1 antihistaminic activity and anti serotonin activity.
Antiemetic activity: Antiemetic activity is by blocking dopamine receptor (D2 receptor) in the Chemoreceptor trigger zone (CTZ)
Pharmacokinets of Trifluoperazine
Absorption: It is absorbed after oral administration.
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.
Onset of Action for Trifluoperazine
30 - 60 minutes
Duration of Action for Trifluoperazine
4- 6 hours
Half Life of Trifluoperazine
3 - 22 hours
Side Effects of Trifluoperazine
1. Tardive dyskinesia
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
Contra-indications of Trifluoperazine
1. Hypersensitivity to Trifluoperazine and other Phenothiazines
2. Comatose
3. Blood dyscrasias
4. Patient taking antidepressants
5. Liver damage
Special Precautions while taking Trifluoperazine
1. Renal impairment
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
Pregnancy Related Information
Old Age Related Information
Use with caution
Breast Feeding Related Information
Children Related Information
Below 6years : Contraindicated
Indications for Trifluoperazine
1. Psychoses
2. Schizophrenia
3. Antiemetic
4. Anxiety
5. Behavioural disturbances
6. Mania
Interactions for Trifluoperazine
Alcohol: CNS depression, extra-pyramidal reactions.
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.
Typical Dosage for Trifluoperazine
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.

Psychoses, Schizophrenia: 1 - 2 mg / day. Dose can be gradually increased up to 15 mg / day.
Schedule of Trifluoperazine
Storage Requirements for Trifluoperazine
The drug should be kept at 25 degree C in a tightly closed container. Protect from heat and light. Keep out of the reach of children.
Effects of Missed Dosage of Trifluoperazine
Take the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose.
Effects of Overdose of Trifluoperazine
Give supportive measures and treatment. Gastric lavage has to be done. Activated charcoal can be given to reduce the absorption of the drug. Hypotension can be treated with IV fluids, seizure with Diazepam or Barbiturates, arrhythmia with Phenytoin and extra pyramidal reactions with Benztropine.


About Chlordiazepoxide
Benzodiazepine derivative, Sedative /hypnotic, Antianxiety and skeletal muscle relaxant.
Mechanism of Action of Chlordiazepoxide
Chlordiazepoxide mainly acts on Limbic system and ascending reticular formation in the CNS. It binds to the BZD receptor. The binding will facilitates GABA mediated chloride channel opening and produce hyperpolarisation. This will increase the concentration of inhibitory neurotransmitter GABA and chloride ions in the CNS and decreases firing rate of neurons. This in turn alters normal excitatory functions of the body.
Pharmacokinets of Chlordiazepoxide
Absorption: It is absorbed after oral administration. Distribution: It is distributed widely in the body. Metabolism: It is metabolised to active metabolite in the liver. Excretion: Most metabolites are excreted through urine
Onset of Action for Chlordiazepoxide
1 - 2 hour
Duration of Action for Chlordiazepoxide
12 - 24 hour
Half Life of Chlordiazepoxide
5 - 30 hour
Side Effects of Chlordiazepoxide
9.Pain at the site of injection
12.Mood changes
Contra-indications of Chlordiazepoxide
Hypersensitivity to Benzodiazepines
Special Precautions while taking Chlordiazepoxide
1.Renal impairment
2.Hepatic impairment
3.Myasthenia gravis
4.Respiratory disease
6.Use caution while driving vehicles, operating machines or other dangerous activities
Pregnancy Related Information
Old Age Related Information
Use with caution
Breast Feeding Related Information
Children Related Information
Use with caution
children < 6 years: contraindicated
NEONATES- contraindicated
Indications for Chlordiazepoxide
1. Anxiety
2.Treatment of alcohol withdrawal symptom
3. Insomnia
4. Pre and post operative apprehension
Interactions for Chlordiazepoxide
Alcohol & Other CNS Depressants: Enhanced CNS effects.
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.
Typical Dosage for Chlordiazepoxide
Adults: 5 - 10 mg 3 - 4 times daily
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.
Schedule of Chlordiazepoxide
Storage Requirements for Chlordiazepoxide
Store at temperature 15 - 30 degree C.Protect from light and moisture. Keep out of the reach of children.
Effects of Missed Dosage of Chlordiazepoxide
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose.
Effects of Overdose of Chlordiazepoxide
Give support and symptomatic treatment. Induce emesis or gastric lavage has to be done followed by charcoal administration. Flumazenil can be given as antagonist.

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