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- Pharmacology For Amitriptyline + Chlordiazepoxide
Amitriptyline + Chlordiazepoxide Pharmacology
Amitriptyline + ChlordiazepoxideAbout Amitriptyline + ChlordiazepoxideN/AMechanism of Action of Amitriptyline + ChlordiazepoxideN/APharmacokinets of Amitriptyline + ChlordiazepoxideN/AOnset of Action for Amitriptyline + ChlordiazepoxideN/ADuration of Action for Amitriptyline + ChlordiazepoxideN/AHalf Life of Amitriptyline + ChlordiazepoxideN/ASide Effects of Amitriptyline + ChlordiazepoxideN/AContra-indications of Amitriptyline + ChlordiazepoxideN/ASpecial Precautions while taking Amitriptyline + ChlordiazepoxideN/APregnancy Related InformationContraindicated since Chlordiazepoxide is contraindicated in pregnancy.Old Age Related InformationN/ABreast Feeding Related InformationContraindicated since Chlordiazepoxide is contraindicated in lactationChildren Related InformationN/AIndications for Amitriptyline + Chlordiazepoxide1.Anxiety
Interactions for Amitriptyline + ChlordiazepoxideN/ATypical Dosage for Amitriptyline + ChlordiazepoxideAdult: 1 - 3 tablets / day and if needed dose can be gradually increased.Schedule of Amitriptyline + ChlordiazepoxideN/AStorage Requirements for Amitriptyline + ChlordiazepoxideN/AEffects of Missed Dosage of Amitriptyline + ChlordiazepoxideN/AEffects of Overdose of Amitriptyline + ChlordiazepoxideN/A
AmitriptylineAbout AmitriptylineTricyclic Antidepressant (Tertiary Amine), anticholinergic.Mechanism of Action of AmitriptylineAmitriptyline 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 AmitriptylineAbsorption: 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 urineOnset of Action for Amitriptyline2 - 6 weeksDuration of Action for AmitriptylineUp to 6 weeksHalf Life of Amitriptyline20 - 30 hoursSide Effects of Amitriptyline1.Drowsiness
6.Difficulty in micturition
10.Dryness of mouth
21.Loss of libido
Contra-indications of Amitriptyline1.Hypersensitivity to Amitriptyline
4.Severe liver diseaseSpecial Precautions while taking Amitriptyline1.Renal impairment
8. Angle closure glaucoma
9.History of urine retention
10. Increased intraocular pressure
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 InformationUse with caution.Old Age Related InformationUse with caution.Breast Feeding Related InformationUse with caution.Children Related InformationUse with caution
CHILDREN< 12 years: contraindicated
Indications for Amitriptyline1.Depression,
2.Prophylaxis of migraine,
4.Nocturnal enuresis.Interactions for AmitriptylineAnticholinergics : 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 AmitriptylineAdult: 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 12 - 16 years: 25 - 50mg to be taken 1 hour before bed time
Schedule of AmitriptylineHStorage Requirements for AmitriptylineStore at room temperature in a tightly closed container. Protect from light. Keep out of the reach of children.Effects of Missed Dosage of AmitriptylineTake 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 AmitriptylineGive 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.
ChlordiazepoxideAbout ChlordiazepoxideBenzodiazepine derivative, Sedative /hypnotic, Antianxiety and skeletal muscle relaxant.Mechanism of Action of ChlordiazepoxideChlordiazepoxide 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 ChlordiazepoxideAbsorption: 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 urineOnset of Action for Chlordiazepoxide1 - 2 hourDuration of Action for Chlordiazepoxide12 - 24 hourHalf Life of Chlordiazepoxide5 - 30 hourSide Effects of Chlordiazepoxide1.Ataxia
9.Pain at the site of injection
12.Mood changesContra-indications of ChlordiazepoxideHypersensitivity to BenzodiazepinesSpecial Precautions while taking Chlordiazepoxide1.Renal impairment
6.Use caution while driving vehicles, operating machines or other dangerous activitiesPregnancy Related InformationContraindicated.Old Age Related InformationUse with cautionBreast Feeding Related InformationContraindicated.Children Related InformationUse with caution
children < 6 years: contraindicated
NEONATES- contraindicatedIndications for Chlordiazepoxide1. Anxiety
2.Treatment of alcohol withdrawal symptom
4. Pre and post operative apprehensionInteractions for ChlordiazepoxideAlcohol & 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 ChlordiazepoxideAdults: 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 ChlordiazepoxideHStorage Requirements for ChlordiazepoxideStore at temperature 15 - 30 degree C.Protect from light and moisture. Keep out of the reach of children.Effects of Missed Dosage of ChlordiazepoxideTake 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 ChlordiazepoxideGive 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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