Azepam Injection, Tablet
Azepam, like other members of the benzodiazepine family, binds to receptors in various regions of the brain, such as the spinal cord, brain stem, cerebellum, limbic system and cerebral cortex. Binding of diazepam to the benzodiazepine receptor potentiates the inhibitory actions of gamma-aminobutyric acid (GABA) mediated through chloride channel, thereby enhancing GABA-facilitated, inhibitory synaptic transmission.
Azepam is used for the management of anxiety disorders or for the shortterm relief of the symptoms of anxiety. Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic. In acute alcohol withdrawal, Azepam may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis.
Azepam is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma), spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia), athetosis, and stiff-man syndrome.
Oral Azepam may be used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy.
The effectiveness of Azepam in long-term use, that is, more than 4 months, has not been assessed by systematic clinical studies. The physician should periodically reassess the usefulness of the drug for the individual patient.
Azepam is also used to associated treatment for these conditions: Alcohol Withdrawal Syndrome, Anxiety, Anxiety Disorders, Refractory Epilepsy, Intermittent distinct from a patient’s usual seizure pattern, stereotypic episode Epileptic seizure, Refractory seizure disorders, Skeletal muscle spasm, Sedation, Perioperative management therapy
|Other Names||Diazepam, Methyl diazepinone|
Despite high binding to plasma proteins (98-99%) - mainly albumin and to a lesser extent α1-acid glycoprotein - diazepam is widely distributed into tissues and crosses the blood-brain barrier and is highly lipid soluble, which causes the initial effects to decrease rapidly as it is redistributed into fat deposits and tissues .
|Therapeutic Class||Benzodiazepine sedatives, Centrally acting Skeletal Muscle Relaxants, Primary anti-epileptic drugs|
|Manufacturer||Acme Laboratories Limited|
|Last Updated:||June 23, 2021 at 11:19 am|
Table Of contents
Dosage should be individualized for maximum beneficial effect. While the usual daily dosages given below will meet the needs of most patients, there will be some who may require higher doses. In such cases dosage should be increased cautiously to avoid adverse effects.
Management of Anxiety Disorders and Relief of Symptoms of Anxiety: Depending upon severity of symptoms 2 mg to 10 mg, 2 to 4 times daily
Symptomatic Relief in Acute Alcohol Withdrawal: 10 mg, 3 or 4 times during the first 24 hours, reducing to 5 mg, 3 or 4 times daily as needed
Adjunctively for Relief of Skeletal Muscle Spasm: 2 mg to 10 mg, 3 or 4 times daily
Adjunctively in Convulsive Disorders: 2 mg to 10 mg, 2 to 4 times daily
Geriatric Patients, or in the presence of debilitating disease: 2 mg to 2.5 mg, 1 or 2 times daily initially; increase gradually as needed and tolerated
Because of varied responses to CNS-acting drugs, initiate therapy with lowest dose and increase as required. Not for use in pediatric patients under 6 months: 1 mg to 2.5 mg, 3 or 4 times daily initially; increase gradually as needed and tolerated
Drowsiness and light headedness the next day; confusion and ataxia (specially in the elderly); amnesia may occur; dependence; paradoxical increase in aggression; occasionally headache, vertigo, hypotension, gastrointestinal disturbances, visual disturbances, dysarthria, tremor, changes in libido, incontinence, urinary retention, blood disorders and jaundice reported.
Azepam is not recommended for use in patients with depressive disorders or psychosis. Patients should be advised against the concurrent use of alcohol and other CNS depressant drugs. Patients with known or presumed dependence from alcohol or drugs should not take benzodiazepines.
Since Azepam has a CNS depressant effect, patients should be warned against driving, operating dangerous machinery, or engaging in other hazardous activities requiring mental alertness and physical coordination.
Azepam may potentiate or interact with the effects of other CNS acting drugs such as alcohol, narcotics, hypnotics, sedative antihistamines, antipsychotics, anxiolytics/ sedatives, anesthetics, antidepressants and anticonvulsants. Besides these diazepam may interact with phenytoin, cimetidine, levodopa, lithium.
- Avoid alcohol.
- Take on an empty stomach. Food may decrease absorption and time to therapeutic effect.
Volume of Distribution
In young healthy males, the volume of distribution at steady-state is 0.8 to 1.0 L/kg .
Azepam has a biphasic half-life with an initial rapid distribution phase followed by a prolonged terminal elimination phase of 1 or 2 days; its action is further prolonged by the even longer half-life of 2-5 days of its principal active metabolite, desmethyldiazepam (nordiazepam), the relative proportion of which increases in the body on long-term administration . The plasma half-life of diazepam is prolonged in neonates, in the elderly, and in patients with kidney or liver disease .
The clearance of diazepam is 20 to 30 mL/min in young adults .
Pregnancy & Breastfeeding use
Category D: The use of Azepam during the first trimester of pregnancy should almost always be avoided as it bears a risk of congenital malformation.
Azepam has been detected in breast milk. If possible the use of diazepam should be avoided during lactation.
Patients with known hypersensitivity to benzodiazepines, & myasthenia gravis are contraindicated to diazepam.
Symptoms: Somnolence, ataxia, confusion, dysarthria, little or no resp depression, hypotension, muscular weakness, deep coma, severe depression, diminished reflexes.
Management: Symptomatic and supportive treatment. Empty stomach by vomiting or gastric lavage. Activated charcoal may help reduce absorption. Flumazenil may be used for the complete or partial reversal of the sedative effects but there is a risk of seizure esp in long-term benzodiazepine users and in cyclic antidepressant overdose.
Store between 15-30°C. Protect from light. Inj: Avoid freezing.