What type of drug is norbuprenorphine?

What type of drug is norbuprenorphine?

Norbuprenorphine is a major active metabolite of the opioid modulator buprenorphine. It is a μ-opioid, δ-opioid, and nociceptin receptor full agonist, and a κ-opioid receptor partial agonist.

What is another name for norbuprenorphine?

Norbuprenorphine

What is norbuprenorphine a metabolite of?

Norbuprenorphine, a metabolite of buprenorphine via CYP3A4 causes dose-dependent respiratory depression, perhaps mediated by opioid receptors in the lung rather than the brain, and is ten times more potent than buprenorphine [15].

How long is norbuprenorphine detectable in urine?

After Suboxone®completely leaves a person’s system, norbuprenorphine remains and exits the body through urine over the span of many days or weeks. Norbuprenorphine will usually exit the system 14 days after Suboxone® enters the body, but this process can be slower or faster depending on each individual person.

What is the half life of norbuprenorphine?

The overall, mean terminal elimination half-lives for buprenorphine and norbuprenorphine were 42 and 57 hours, respectively.

What does norbuprenorphine in urine mean?

The buprenorphine/norbuprenorphine ratio is extremely helpful in identifying situations of possible urine adulteration. High concentrations of buprenorphine with low concentrations of norbuprenorphine may indicate post-collection addition of the drug directly to the specimen.

What is the action of buprenorphine?

Mechanism of Action Buprenorphine is a partial agonist at the mu receptor, meaning that it only partially activates opiate receptors. It is also a weak kappa receptor antagonist and delta receptor agonist. It is a potent analgesic that acts on the central nervous system (CNS).

What is metabolite in pharmacology?

A metabolite is any substance produced during metabolism (digestion or other bodily chemical processes). The term metabolite may also refer to the product that remains after a drug is broken down (metabolized) by the body.

What’s the difference between norbuprenorphine and buprenorphine?

Unlike buprenorphine, which is a partial mu receptor agonist with slow receptor dissociation rates, norbuprenorphine in rats has rapid mu receptor binding and is a full agonist, causing full respiratory depression.

Is there norbuprenorphine in naloxone?

Buprenorphine is an opioid drug that has been used to treat opioid dependence on an outpatient basis, and is also prescribed for managing moderate to severe pain. Some formulations of buprenorphine also contain naloxone to discourage misuse. The major metabolite of buprenorphine is norbuprenorphine.

What receptors does buprenorphine bind to?

Martin and colleagues [56] originally described buprenorphine as a partial agonist at the mu opioid receptor. Subsequent studies showed that buprenorphine can also bind to kappa and delta opioid receptors (Tables 1 and ​ 2).

What is the mechanism of action of norbuprenorphine?

Norbuprenorphine is a major active metabolite of the opioid modulator buprenorphine. It is a μ-opioid, δ-opioid, and nociceptin receptor full agonist, and a κ-opioid receptor partial agonist. In rats, unlike buprenorphine, norbuprenorphine produces marked respiratory depression but with very little antinociceptive…

What is the difference between buprenorphine and norbuprenorphin?

Norbuprenorphine. Norbuprenorphine is the primary active metabolite of buprenorphine. Norbuprenorphine acts as a μ-opioid, δ-opioid, and nociceptin receptor full agonist, as well as a κ-opioid receptor partial agonist. Norbuprenorphine crosses the blood-brain-barrier similarly to buprenorphine and likely contributes to its effects.

Is norbuprenorphine a μ-opioid?

It is a μ-opioid, δ-opioid, and nociceptin receptor full agonist, and a κ-opioid receptor partial agonist. In rats, unlike buprenorphine, norbuprenorphine produces marked respiratory depression but with very little antinociceptive effect.

What is the active metabolite of buprenorphine?

Norbuprenorphine is the primary active metabolite of buprenorphine. Norbuprenorphine acts as a μ-opioid, δ-opioid, and nociceptin receptor full agonist, as well as a κ-opioid receptor partial agonist.