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Chlordiazepoxide (HCl)

Drug #159

Chlordiazepoxide is a 1,4-benzodiazipine. A substituent in the 7th position such as halogen or a nitro group is required for its sedative, and hypnotic activity. Benzdiazipines are the most widely used anxiolytic drugs. The benzodiazipines are more effective and safer. They have largely replaced barbiturates and meprobamates in the treatment of anxiety.

Primary Characteristics

It is of Synthetic origin and belongs to Benzodiazepines.

It belongs to Chloride Channel Potentiater (GABA operated) pharmacological group on the basis of mechanism of action and also classified in Benzodiazepine pharmacological group. It is also classified under Psychotherapeutic Drugs .

Molecular Weight: 336.2 · pKa: 4.6 · Solubility in Water: 1 in 10 · Solubility in Alcohol: 1 in 40 · Non-proprietary name: Chlordiazepoxide (HCl) · pH: 2.7 · Isotonic value: 5.5.

Molecular structure of Chlordiazepoxide (HCl)

Pharmacokinetics

Absorption: Chlordiazepoxide (HCl) has an oral bioavailability is 97% (±2%), pre-systemic (first-pass) metabolism accounts for 2.5% (±2.5%).

Distribution: Chlordiazepoxide (HCl) has a volume of distribution is 0.22-0.75 l/kg. plasma protein binding is 92-96%.

Elimination: it is metabolised via extensive by liver, plasma half-life is 15 hr, renal excretion is partial.

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Indications

Chlordiazepoxide (HCl) is primarily indicated in conditions like Acute alcohol withdrawal, Adjunct in acute alcohol withdrawal, Adjunt in acute alcohol withdrawal, Anxiety, Insomnia, Muscular spasm, Premedication in anaesthesia, Psychosomatic disorders, Suppression of transplant rejection.

Chlordiazepoxide (HCl) is also indicated for secondary conditions like Alcohol withdrawal.

Contraindications

Chlordiazepoxide (HCl) is contraindicated in conditions like Depression, Pulmonary insufficiency, Respiratory depression.

Dosage

Chlordiazepoxide (HCl)'s dosage details are as follows:

DoseSingle DoseFrequencyRouteInstructions
Adult Dosage
20 mg20 mgFor Muscle spasms.The dose is given daily in divided doses
62.5 mg62.5 mgFor acute symptoms of alcohol withdrawl.Maximum dose is 300 mg daily
75 mg75 mgFor premedication before anaesthesia given 1 hr before surgery
75 mg75 mgIV or IMFor severe symptoms of alcohol withdrawl. this dose is given initially ,if necessary repeat dose after 2-4 hr
20 mg20 mgPOFor insomnia given before bedtime
52.5 mg52.5 mgEvery 8hPOFrequency may be increased upto 4 times/day if needed.
Paediatric Dosage (20kg)
5 mg5 mgEvery 12h
Neonatal Dosage (3kg)
0 – 0Not recommended in this age group

Drug Interactions

Unknown9 interactions
2 interactions
Moderate1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Chlordiazepoxide (HCl) in overdosage may give rise to further complications which include Psychological impairment , Cerebral atrophy , Psychomotor performance impairment.

Chlordiazepoxide (HCl) produces potentially life-threatening effects which include Hemolytic anemia, Hypoplastic Anemia . Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Chlordiazepoxide (HCl) are Confusion , Sedation , Ataxia, Drowsiness, Coma.

Chlordiazepoxide (HCl) is known to cause more or less tolerable side effects which are usually transient. These include Aggression, Dependence , Skin reactions.

Warnings / Precautions

Perform periodic blood counts and liver function tests during long term therapy of chlordiazepoxide. It should be used with caution in patients if increased salivation cause respiratory difficulty, because it may produce an increase in salivation. Give least amount of drug to patients in whom depression accompanies anxiety and suicidal tendencies may be present. It should be used with caution (if it contains tartrazine) in patients with aspirin hypersensitivity because it may cause allergic reaction (including bronchial asthma).

Available Brands

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Single Ingredient

Multi-Ingredient Combinations

Tabs

Storage Conditions

Chlordiazepoxide (HCl) should be stored Caps .

Drug Classification

  1. 1.24.3Drugs used in anxiety and sleep disorders

Manufacturers

Manufacturers of Chlordiazepoxide (HCl) in Pakistan: