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Indications

Diazepam is an anxiolytic benzodiazepine, first patented and marketed in the United States in 1963. It is a fast-acting, long-lasting benzodiazepine commonly used to treat anxiety disorders and alcohol detoxification, acute recurrent seizures, severe muscle spasms, and spasticity associated with neurologic disorders. In the setting of acute alcohol withdrawal, diazepam is useful for symptomatic relief of agitation, tremor, alcoholic hallucinosis, and acute delirium tremens.[1] Benzodiazepines have largely replaced barbiturates in treating anxiety and sleep disorders because of their improved safety profile, fewer side effects, and flumazenil(antagonist) availability that can reverse oversedation in cases of benzodiazepine intoxication. Buy Valium Diazepam 10mg online Australia

Diazepam is FDA approved for the management of anxiety disorders, short-term relief of anxiety symptoms, spasticity associated with upper motor neuron disorders, adjunct therapy for muscle spasms, preoperative anxiety relief, management of certain refractory epilepsy patients and adjunct in severe recurrent convulsive seizures, and an adjunct in status epilepticus. Off-label (non-FDA approved) use for diazepam includes sedation in the ICU and short-term treatment of spasticity in children with cerebral palsy.[4] Buy Valium Diazepam 10mg online Australia

Mechanism of Action

Benzodiazepines exert their effects by facilitating the activity of gamma-aminobutyric acid(GABA) at various sites. Specifically, benzodiazepines bind at an allosteric site at the interface between the alpha and gamma subunits on GABA-A receptor chloride ion channels. The allosteric binding of diazepam at the GABA-A receptor leads to an increase in the frequency at which the chloride channel opens, leading to an increased conductance of chloride ions. This shift in charge leads to a hyperpolarization of the neuronal membrane and reduced excitability of the neuron.[5] Buy Valium Diazepam 10mg online Australia

Specifically, the allosteric binding within the limbic system leads to the anxiolytic effects seen with diazepam. Allosteric binding within the spinal cord and motor neurons is the primary mediator of the myorelaxant effects seen with diazepam. Mediation of the sedative, amnestic, and anticonvulsant effects of diazepam is through receptor binding within the cortex, thalamus, and cerebellum.[6] Buy Valium Diazepam 10mg online Australia

Diazepam is highly lipophilic. While there is a moderately quick onset of action, the drug quickly redistributes. Diazepam is mostly broken down by the microsomal enzymes CYP2C19 and CYP3A4 enzymes to several active metabolites, mainly desmethyldiazepam. Other minor active metabolites include oxazepam and temazepam. The average half-lives of oral diazepam and desmethyldiazepam are about 46 hours and 100 hours, respectively.[6] Buy Valium Diazepam 10mg online Australia

Potent inhibition of the CYP2C19 enzyme by certain drugs (fluoxetine and chloramphenicol) and CYP3A4 enzymes by certain medications (ketoconazole, protease inhibitors, erythromycin) may cause increased levels of diazepam. In contrast, inducers of CYP2C19 (rifampicin and prednisone) and CYP3A4 (carbamazepine, topiramate, phenytoin, St. John’s wort, rifampin, or barbiturates) may cause lower levels. Metabolites of diazepam are conjugated with glucuronide and excreted almost entirely in the urine.[7][8] Buy Valium Diazepam 10mg online Australia