Brands, Medical Use, Clinical Data
Drug Category
- Anti-anxiety Agents
- Hypnotics and Sedatives
- Adjuvants, Anesthesia
- Benzodiazepines
- GABA Modulators
Dosage Forms
- Capsule (5 mg, 10 mg or 25 mg)
Brands / Synonyms
A-Poxide; Abboxide; Apo-Chlordiazepoxide; Balance; CD 2; CDO; CDP; Chloradiazepoxide; Chlordiazachel; Chlordiazepoxid; Chlordiazepoxide; Chlordiazepoxide and Amitriptyline; Chlordiazepoxide and Clidinium; Chlordiazepoxide Base; Chlordiazepoxide Hcl; Chlordiazepoxidum; Chloridazepoxide; Chloridiazepide; Chloridiazepoxide; Chlorodiazepoxide; Chlozepid; Clopoxide; Clordiazepossido; Contol; Control; Decacil; Eden; Elenium; Helogaphen; Ifibrium; Kalmocaps; Librax; Librelease; Librinin; Libritabs; Librium; Limbitrol; Limbitrol Ds; Lygen; Menrium; Mesural; Methaminodiazepoxide; Mildmen; Multum; Napoton; Napton; Novo-Poxide; Psicosan; Radepur; Risolid; Silibrin; Tropium; Viopsicol
Indications
For the management of anxiety disorders or for the short-term relief of symptoms of anxiety, withdrawal symptoms of acute alcoholism, and preoperative apprehension and anxiety.
Pharmacology
Chlordiazepoxide has antianxiety, sedative, appetite-stimulating and weak analgesic actions. The precise mechanism of action is not known. The drug blocks EEG arousal from stimulation of the brain stem reticular formation. The drug has been studied extensively in many species of animals and these studies are suggestive of action on the limbic system of the brain, which recent evidence indicates is involved in emotional responses. Hostile monkeys were made tame by oral drug doses which did not cause sedation. Chlordiazepoxide revealed a "taming" action with the elimination of fear and aggression. The taming effect of chlordiazepoxide was further demonstrated in rats made vicious by lesions in the septal area of the brain. The drug dosage which effectively blocked the vicious reaction was well below the dose which caused sedation in these animals.
Mechanism of Action
Chlordiazepoxide binds to stereospecific benzodiazepine (BZD) binding sites on GABA (A) receptor complexes at several sites within the central nervous system, including the limbic system and reticular formation. BZDs enhance GABA-mediated chloride influx through GABA receptor channels, causing membrane hyperpolarization. The net neuro-inhibitory effects result in the observed sedative, hypnotic, anxiolytic, and muscle relaxant properties.
Absorption
Not Available
Toxicity
LD50=537 mg/kg (Orally in rats). Signs of overdose include respiratory depression, muscle weakness, somnolence (general depressed activity).
Biotrnasformation / Drug Metabolism
Hepatic.
Contraindications
Chlordiazepoxide HCl Capsules are contraindicated in patients with known hypersensitivity to the drug.
Drug Interactions
Although clinical studies have not established a cause and effect relationship, physicians should be aware that variable effects an blood coagulation have been reported very rarely in patients receiving oral anticoagulants and chlordiazepoxide.
The concomitant use of alcohol or other central nervous system depressants may have an additive effect.
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