Trade name Librium
Schedule IV drug.
Routes of administration oral and intramuscular.
Metabolism is hepatic.
Half-life 5–30 hours.
Active metabolite is desmethyldiazepam 36–200 hours.
Excretion is renal.
A sedative/hypnotic drug and a benzodiazepine.
Has a medium to long half-life but its active metabolite has a very long half-life.
Has amnestic, anticonvulsant, anxiolytic, hypnotic and skeletal muscle relaxant properties.
Indicated for the short-term treatment of anxiety and acute alcohol withdrawal syndrome.
When combined with amitriptyline can be used to treat new daily persistent headache disorder.
Caution if used in the elderly, pregnant, children, alcohol- or drug-dependent individuals and individuals with comorbid psychiatric disorders.
Should generally be avoided during the first trimester of pregnancy as possible adverse effects include, abortion, malformation, intrauterine growth retardation, functional deficits, carcinogenesis and mutagenesis.
Caution is also advised during breast feeding as the drug passes into breast milk.
Common side-effects of chlordiazepoxide include:
Confusion
Constipation
Drowsiness
Fainting
Altered sex drive
Liver problems
Lack of muscle coordination
Minor menstrual irregularities
Nausea
Skin rash or eruptions
Swelling due to fluid retention
Jaundice
Chronic use leads to the development of tolerance, with a decrease in number of benzodiazepine binding sites.
Tends to lose sleep-promoting properties within 3–14 days of continuous use, and in the treatment of anxiety there is little evidence that benzodiazepines retain efficacy in the treatment of anxiety after 4 months’ continuous use.
Can cause physical dependence, addiction and benzodiazepine withdrawal syndrome.
Withdrawal often leads to withdrawal symptoms that are similar to those seen with alcohol and barbiturates.
The higher the dose and the longer the drug is taken, the risk of withdrawal symptoms is greater.
Treatment with this drug should be discontinued as soon as possible through a slow and gradual dose-reduction regime.
Excess drug may cause:
Somnolence
Mental confusion
Hypotension
Hypoventilation
Impaired motor functions
Impaired reflexes
Impaired coordination
Impaired balance
Dizziness
Muscle weakness
Coma
The antidote for an overdose is flumazenil.
An agent frequently involved in drug intoxication, including overdose.
Has many major drug interactions involving;
ACE inhibitors, Adrenergic neurone blockers, Angiotensin II receptor antagonists, Beta blockers, Calcium channel blockers, Clonidine, Diazoxide, Diuretics, Hydralazine, Methyldopa, Minoxidil, Nitrates, and Sodium Nitroprusside.
Alcohol, barbiturates, opiates, antihistamines, antipsychotics have increased sedative effect in combination with benzodiazapines.
The metabolism of benzodiazepines inhibited by cimetidine, and disulfiram.
There is an increased risk of hypotension, bradycardia and respiratory depression when parenteral benzodiazepines given with intramuscular olanzapine
May increase or decrease plasma concentration of phenytoin.
Rifampicin increases metabolism of benzodiazepines and may reduce plasma concentration.
Acts on benzodiazepine allosteric sites that are part of the GABAA receptor/ion-channel complex and increases binding of the inhibitory neurotransmitter GABA to the GABAA receptor thereby producing inhibitory effects on the central nervous system and body.
Is an anticonvulsant.
Stored in some organs including the heart of the neonate.
Risk of accumulation is significantly increased in the neonate.
Use should be discontinued during pregnancy and breast feeding as it rapidly crosses the placenta and also is excreted in breast milk.
The half-life of chlordiazepoxide increases significantly in the elderly.
A drug of potential misuse.