Amitriptyline + Chlordiazepoxide Pharmacology

Amitriptyline + Chlordiazepoxide

About Amitriptyline + Chlordiazepoxide
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Mechanism of Action of Amitriptyline + Chlordiazepoxide
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Pharmacokinets of Amitriptyline + Chlordiazepoxide
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Onset of Action for Amitriptyline + Chlordiazepoxide
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Duration of Action for Amitriptyline + Chlordiazepoxide
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Half Life of Amitriptyline + Chlordiazepoxide
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Side Effects of Amitriptyline + Chlordiazepoxide
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Contra-indications of Amitriptyline + Chlordiazepoxide
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Special Precautions while taking Amitriptyline + Chlordiazepoxide
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Pregnancy Related Information
Contraindicated since Chlordiazepoxide is contraindicated in pregnancy.
Old Age Related Information
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Breast Feeding Related Information
Contraindicated since Chlordiazepoxide is contraindicated in lactation
Children Related Information
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Indications for Amitriptyline + Chlordiazepoxide
1.Anxiety
2.Depression
Interactions for Amitriptyline + Chlordiazepoxide
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Typical Dosage for Amitriptyline + Chlordiazepoxide
Adult: 1 - 3 tablets / day and if needed dose can be gradually increased.
Schedule of Amitriptyline + Chlordiazepoxide
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Storage Requirements for Amitriptyline + Chlordiazepoxide
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Effects of Missed Dosage of Amitriptyline + Chlordiazepoxide
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Effects of Overdose of Amitriptyline + Chlordiazepoxide
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Amitriptyline

About Amitriptyline
Tricyclic Antidepressant (Tertiary Amine), anticholinergic.
Mechanism of Action of Amitriptyline
Amitriptyline acts by inhibiting the re-uptake of Noradrenaline and Serotonin (5 HT) in the CNS nerve terminals .This will result in an increased concentration of neurotransmitters in the synaptic cleft and produces antidepressant effect. Amitriptyline more selectively inhibit reuptake of Serotonin than Noradrenaline. Amitriptyline also has anticholinergic activity.
It is also useful in migraine prophylaxis. The monoamine uptake blocking property is related to migraine prophylactic activity. These are suited for patient with depression.
Pharmacokinets of Amitriptyline
Absorption: Amitriptyline is rapidly absorbed after oral administration. Distribution: It is widely distributed in the body in protein bound form Metabolism: Imipramine is metabolised in the liver to the active metabolite Nortriptyline. Excretion: Drug is excreted mainly through urine
Onset of Action for Amitriptyline
2 - 6 weeks
Duration of Action for Amitriptyline
Up to 6 weeks
Half Life of Amitriptyline
20 - 30 hours
Side Effects of Amitriptyline
1.Drowsiness
2 Dizziness
3.Nausea
4.Vomiting
5.Blurred vision
6.Difficulty in micturition
7.Tachycardia
8.Hypotension
9.Arrhythmia
10.Dryness of mouth
11.Constipation
12.Confusion
13.Headache
14.Sedation
15.Agranulocytosis
16.Urticaria
17.Rash
18.Jaundice
19.Anorexia
20.Impotence
21.Loss of libido
22.Galactorrhea
23.Gynecomastia
Contra-indications of Amitriptyline
1.Hypersensitivity to Amitriptyline
2.Myocardial infarction
3.CHF
4.Severe liver disease
Special Precautions while taking Amitriptyline
1.Renal impairment
2.Hepatic impairment
3.Cardiac arrhythmia
4.Myocardial infarction
5.Tachycardia,
6.Heart failure
7.Strokes
8. Angle closure glaucoma
9.History of urine retention
10. Increased intraocular pressure
11.Hyperthyroidism,
12.Alcoholics
13.Patient at risk for suicide
14. Slowly withdraw the drug with caution
15.Patient should be cautioned against driving vehicle, operating machine and activities requiring mental alertness or judgment
Pregnancy Related Information
Use with caution.
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Use with caution.
Children Related Information
Use with caution
CHILDREN< 12 years: contraindicated
NEONATES: contraindicated
Indications for Amitriptyline
1.Depression,
2.Prophylaxis of migraine,
3.Bulimia nervosa,
4.Nocturnal enuresis.
Interactions for Amitriptyline
Anticholinergics : Enhanced effect of anticholinergics may occur.
Barbiturates : Serum level of amitriptyline decreased; additive respiratory depressant effect.
Clonidine : Hypertensive crisis.
Dicoumarol : Increase in anticoagulation effects.
Disulfiram : Acute organic brain syndrome.
Fluoxetine & Haloperidol : Potentiate action of amitriptyline.
Levodopa : Its bioavailability is reduced, hypertensive episodes.
MAOIs, Furazolidone : Seizures, sweating, coma, hyperexcitabilty, hyperthermia, tachycardia, mydriasis, confusion, DIC. (Disseminated Intravascular Coagulation) and death.
Oral Contraceptives and Phenothiazines : Increase plasma levels of imipramine.
Smoking : Increases metabolic bio-transformation.
Alcohol : Sedative effect of alcohol potentiated.
Typical Dosage for Amitriptyline
Adult: 25 mg 3 times a day dose can be gradually increased up to 150 mg / day.
Maintenance dose: 50 - 100 mg / day
Maximum daily dose: 300 mg
Prophylaxis of migraine: 10 mg at bed time. Dose can be gradually increased up to 100 mg.
Children:
Nocturnal enuresis
Children 12 - 16 years: 25 - 50mg to be taken 1 hour before bed time
Schedule of Amitriptyline
H
Storage Requirements for Amitriptyline
Store at room temperature in a tightly closed container. Protect from light. Keep out of the reach of children.
Effects of Missed Dosage of Amitriptyline
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 Amitriptyline
Give supportive measures and treatment. Remove the drug from the body by inducing emesis and gastric lavage. Activated charcoal can be given to reduce the absorption of the drug. Seizure can be treated with Diazepam or Phenytoin, arrhythmia with Lidocaine, and acidosis with Sodium bicarbonate.

Chlordiazepoxide

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
1.Ataxia
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
Contra-indications of Chlordiazepoxide
Hypersensitivity to Benzodiazepines
Special Precautions while taking Chlordiazepoxide
1.Renal impairment
2.Hepatic impairment
3.Myasthenia gravis
4.Respiratory disease
5.Jaundice
6.Use caution while driving vehicles, operating machines or other dangerous activities
Pregnancy Related Information
Contraindicated.
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated.
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
H
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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