How does diazepam metabolize?

Diazepam is primarily metabolized via CYP2C19 and CYP3A4 to the major active metabolite (desmethyldiazepam), which is found in the plasma at concentrations equivalent to diazepam. Two minor active metabolites include temazepam and oxazaepam, which are usually not detectable.

How is diazepam metabolized and excreted?

Diazepam and its metabolites are excreted mainly in the urine, predominantly as their glucuronide conjugates. The clearance of diazepam is 20 to 30 mL/min in young adults. Diazepam accumulates upon multiple dosing and there is some evidence that the terminal elimination half-life is slightly prolonged.

What is the major metabolite of diazepam?

The three metabolites of diazepam—nordiazepam, temazepam, and oxazepam—are quickly recognized as individual benzodiazepines, which can be prescribed for a variety of medical conditions.

What is the half-life of diazepam in dogs?

Diazepam is a class II drug and is thus available by prescription only. Because of the short half-life of diazepam in dogs (2-4 hours) and the development of tolerance, diazepam should only be used for emergency management of seizures.

Does diazepam undergo first pass metabolism?

Notable drugs that experience a significant first-pass effect are imipramine, morphine, propranolol, buprenorphine, diazepam, midazolam, pethidine, tetrahydrocannabinol (THC), ethanol (drinking alcohol), cimetidine, lidocaine, and chlorpromazine.

What enzyme metabolizes diazepam?

Diazepam is primarily metabolized via CYP2C19 and CYP3A4 to the major active metabolite (desmethyldiazepam), which is found in the plasma at concentrations equivalent to diazepam.

Is diazepam metabolized by the liver?

Diazepam is metabolized in the liver to its active metabolite which is excreted in the urine.

Is dog and human diazepam the same?

Can I give my dog diazepam for humans? Diazepam comes in different dosages for humans and dogs, which could cause your dog to overdose. You should never give your dog any medication that isn’t prescribed by your veterinarian.

What is the duration of diazepam?

Diazepam is long-lasting with a duration of action of more than 12 hours. Treatment of seizures: 2 to 10 mg orally dosed 2 to 4 times daily as adjunctive maintenance therapy. For intermittent management of seizures, rectal gel 0.2mg/kg is an option. It may be repeated in 4 to 12 hours if needed.

What is 2nd pass metabolism?

However, significant hepatic extraction still occurs because of second pass metabolism, whereby a fraction of venous blood travels through the hepatic portal vein and hepatocytes.

What does CYP2C19 rapid metabolizer mean?

In people who are rapid metabolizers, the CYP2C19 enzyme has high activity. People who are rapid metabolizers break down some medicines quickly and may need different doses or a different medicine. About 29% of our patients are rapid metabolizers.

Does diazepam have a high first pass metabolism?

How is benzodiazepine metabolized?

All benzodiazepines are metabolized by the liver. However, some benzodiazepines (i.e. – lorazepam, oxazepam, and tamazepam) do not go through cytochrome P450 metabolism (Phase I metabolism), and are only metabolized via glucuronidation (Phase II metabolism).

How much diazepam can a dog have?

Dosing Information of Diazepam for Dogs and Cats The typical dose administered to dogs is 0.25 to 1 mg per pound (0.5 to 2 mg/kg) and 0.25 to 0.5 mg per pound (0.5 to 1 mg/kg) in cats, intravenous as needed or as often as every six hours or as a constant rate infusion (a slow drip through the intravenous line).

How does diazepam work?

Diazepam is a type of medicine called a benzodiazepine. It works by increasing the activity of a neurotransmitter called GABA in the brain. Neurotransmitters are chemicals that are stored in nerve cells in the brain and nervous system. They are involved in transmitting messages between the nerve cells.

Is diazepam for dogs the same as humans?

As diazepam is also used for humans, many people wonder if they can give human diazepam to their dog. The answer is no.

What is the function of diazepam?

Diazepam is used to relieve anxiety and to control agitation caused by alcohol withdrawal.

Where does Phase 1 and 2 metabolism occur?

The enzymes involved in Phase I reactions are primarily located in the endoplasmic reticulum of the liver cell, they are called microsomal enzymes. Phase II metabolism involves the introduction of a hydrophilic endogenous species, such as glucuronic acid or sulfate, to the drug molecule.

Which drugs are metabolised by CYP2C19?

CYP2C19 catalyzes the metabolism of several drugs, including proton pump inhibitors (PPIs) (e.g., omeprazole, lansoprazole, pantoprazole), antidepressants (e.g., citalopram and amitriptyline), antiplatelet drugs (e.g., clopidogrel), antifungals (e.g., voriconazole), and anticancer compounds (e.g., cyclophosphamide).

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