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While psychiatrists proceed to prescribe diazepam for the short-time period reduction of anxiety, neurology has taken the lead in prescribing diazepam for the palliative treatment of sure kinds of epilepsy and spastic exercise, for example, types of paresis. It is also the primary line of protection for a uncommon disorder referred to as stiff-person syndrome. Diazepam undergoes oxidative metabolism by demethylation , hydroxylation and glucuronidation in the liver as part of the cytochrome P450 enzyme system. Its different energetic metabolites embrace the minor energetic metabolites temazepam and oxazepam.
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Diazepam, as with other benzodiazepine medicine, can cause tolerance, bodily dependence, substance use disorder, and benzodiazepine withdrawal syndrome. Withdrawal from diazepam or different benzodiazepines usually leads to withdrawal symptoms just like these seen during barbiturate or alcohol withdrawal. The greater the dose and the longer the drug is taken, the higher the risk of experiencing unpleasant withdrawal signs. Adverse results of benzodiazepines similar to diazepam embrace anterograde amnesia, confusion and sedation.
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Diazepam is highly lipid-soluble, and is widely distributed throughout the body after administration. It simply crosses both the blood–mind barrier and the placenta, and is excreted into breast milk. After absorption, diazepam is redistributed into muscle and adipose tissue. Continual day by day doses of diazepam quickly construct to a high concentration in the physique , far in excess of the particular dose for any given day. Benzodiazepines are positive allosteric modulators of the GABA sort A receptors .
Rebound anxiousness, more extreme than baseline anxiousness, can be a common withdrawal symptom when discontinuing diazepam or different benzodiazepines. Diazepam is therefore only recommended for brief-term remedy at the lowest potential dose owing to dangers of extreme withdrawal issues from low doses even after gradual reduction. The threat of pharmacological dependence on diazepam is critical, and sufferers experience signs of benzodiazepine withdrawal syndrome if it is taken for six weeks or longer. In people, tolerance to the anticonvulsant results of diazepam happens incessantly.