Peripheral benzodiazepine receptor in cholesterol transport and steroidogenesis

Diazepam and other benzodiazepines should be administered cautiously in patients with CNS depression. Ambulatory patients receiving diazepam should be warned of the hazards of driving or operating machinery, and should avoid engaging in these activities until the full effect of the drug has dissipated. There is a potential for synergistic CNS-depressant effects if benzodiazepines are administered concomitantly with alcohol, barbiturates, or other CNS depressants. If opiate agonists are used concomitantly, the dose of the opiate should be reduced by at least one-third. Except as indicated for acute alcohol withdrawal, diazepam should not be administered parenterally to patients with acute ethanol intoxication, shock, or coma because the drug can worsen CNS depression.

After oral administration of loprazolam on an empty stomach, it takes 2 hours for serum concentration levels to peak, significantly longer than other benzodiazepine hypnotics. This delay brings into question the benefit of loprazolam for the treatment of insomnia when compared to other hypnotics (particularly when the major complaint is difficulty falling asleep instead of difficulty maintaining sleep for the entire night), although some studies show that loprazolam may induce sleep within half an hour, indicating rapid penetration into the brain. The peak plasma delay of loprazolam, therefore, may not be relevant to loprazolam's efficacy as a hypnotic. If taken after a meal it can take even longer for loprazolam plasma levels to peak and peak levels may be lower than normal. Loprazolam significantly alters electrical activity in the brain as measured by EEG , with these changes becoming more pronounced as the dose increases. Roughly half of each dose is metabolized in humans to produce an active metabolite with similar potency to loprazolam, the other half is excreted unchanged. The half-life of the active metabolite is about the same as the parent compound loprazolam. [20]

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Peripheral benzodiazepine receptor in cholesterol transport and steroidogenesis

peripheral benzodiazepine receptor in cholesterol transport and steroidogenesis

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