Trihexyphenidyl + Trifluoperazine Pharmacology

Trihexyphenidyl + Trifluoperazine

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

About Trihexyphenidyl
Anticholinergic(antimuscarinic), Anti-Parkinson`s Agent ,synthetic antispasmodic.
Mechanism of Action of Trihexyphenidyl
Trihexyphenidyl is a synthetic Atropine substitute. It produces antiparkinsonian action by blocking the central cholinergic receptors. It inhibits cerebral cortex centers and blocks efferent impulses.
Trihexyphenidyl produces Mydriasis, increase the heart rate and spasmolytic action on smooth muscles. It decreases sweating and salivation.
Pharmacokinets of Trihexyphenidyl
Absorption: It is rapidly absorbed after oral administration.
Distribution: It crosses the blood brain barrier.
Excretion: It is excreted in urine.
Onset of Action for Trihexyphenidyl
1 hour
Duration of Action for Trihexyphenidyl
6 - 12 hours
Half Life of Trihexyphenidyl
3.7 hours
Side Effects of Trihexyphenidyl
1. Dry mouth
2. Nausea
3. Vomiting
4. Constipation
5. Abdominal cramps
6. Dizziness
7. Headache
8. Nervousness
9. Drowsiness
10. Blurred vision
11. Irritability
12. Tachycardia
13. Urinary retention
14. Mydriasis
15. Increased intraocular pressure
Contra-indications of Trihexyphenidyl
1. Hypersensitivity to Trihexyphenidyl
Special Precautions while taking Trihexyphenidyl
1. Renal impairment
2. Hepatic impairment
3. Cardiac impairment
4. Gastrointestinal obstructive disease
5. Genitourinary obstructive disease
6. Glaucoma
7. Prostatic hyperplasia
8. Slowly withdraw the drug with caution
9. Patient should be cautioned about driving a vehicle operating a machine or involving in any hazardous activities
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Contraindicated
NEONATES : Contraindicated
Indications for Trihexyphenidyl
1. Parkinsonism (idiopathic and drug induced Parkinsonism)
Interactions for Trihexyphenidyl
Amantadine: Increased incidence of anticholinergic side effects which disappear on reducing the dose of trihexiphenidyl.
Digoxin: Serum levels of digoxin increased when given orally as a slow dissolution tablet.
Haloperidol: Decreased Haloperidol serum concentration may result in worsening of schizophrenic symptoms; also development of tardive dyskinesia.
Levodopa: Efficacy of levodopa may be reduced.
Typical Dosage for Trihexyphenidyl
Adult:
Idiopathic Parkinsonism: initial dose: 1mg / day gradually increase the dose every 3 - 5 days up to 10 - 15 mg /day in 3 - 4 divided doses.
Post encephalitic Parkinsonism: 12 - 15 mg / day in divided doses.
Drug induced Parkinsonism: 5- 15 mg / day in divided doses
Schedule of Trihexyphenidyl
N/A
Storage Requirements for Trihexyphenidyl
Store at 15 - 30 degree C
Effects of Missed Dosage of Trihexyphenidyl
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Trihexyphenidyl
Give supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage or inducing emesis. Absorption of the drug can be reduced by administration of activated charcoal. Control excitement with Diazepam (IV). Physostigmine is given to counteract the antimuscarinic effect of Trihexyphenidyl.

Trifluoperazine

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
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
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
Adult:
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.
Schedule of Trifluoperazine
H
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.

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