Benzhydrocodone

Benzhydrocodone Uses, Dosage, Side Effects, Food Interaction and all others data.

Benzhydrocodone is a benzylic prodrug of hydrocodone. It was developed in an effort to reduce parenteral bioavailability of the active metabolite as a deterrent to abuse. Benzhydrocodone is indicated for use in the short-term management of pain. It was first approved by the FDA in February 2018 in combination with acetaminophen under the trade name Apadaz, marketed by KVK Tech and developed by KemPharm.

Benzhydrocodone is rapidly metabolized to hydrocodone which acts on the central nervous system to produce analgesia. The action of hydrocodone in the brain can also produce euphoria, leading to addiction.

Trade Name Benzhydrocodone
Generic Benzhydrocodone
Benzhydrocodone Other Names Benzhydrocodone
Type
Formula C25H25NO4
Weight Average: 403.478
Monoisotopic: 403.178358289
Groups Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Benzhydrocodone
Benzhydrocodone

Uses

Benzyhydrocodone is indicated, in combination with acetaminophen, for the short-term management of acute pain requiring opioid therapy.

Benzhydrocodone is also used to associated treatment for these conditions: Pain, Acute

How Benzhydrocodone works

Benzyhydrocodone is not reported to have pharmacological activity of its own and it not present in the plasma at detectable concentrations. Its active metabolite, hydrocodone is a mu-opioid receptor agonist.

Toxicity

Overdosage with benzhydrocodone presents as opioid intoxication including respiratory depression, somnolence, coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, pulmonary edema, bradycardia, hypotension, partial or complete airway obstruction, atypical snoring, and death.

In case of oversdosage the foremost priority is the maintenance of a patent and protected airway with the provision of assisted ventilation if necessary. Supportive measures such as IV fluids, supplemental oxygen, and vasopressors may be used to manage circulatory shock. Advanced life support may be necessary in the case of cardiac arrest or arrhythmias. Opioid antagonists such as naloxone may be used to reverse the respiratory and circulatory effects of hydrocodone. Emergency monitoring is still required after naloxone administration as the opioid effects may reappear. Additionally, if used in an opioid tolerant patient, naloxone may produce opioid withdrawal symptoms.

Food Interaction

  • Avoid alcohol. Ingesting alcohol may increase the CNS depressive effects of benzhydrocodone. Apadaz also contains acetaminophen, which, when combined with alcohol, may increase the risk of hepatotoxicity.
  • Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

Volume of Distribution

The hydrocodone metabolite of benzhydrocodone has an apparent volume of distribution of 714 L.

Elimination Route

The absorption profile of benzhydrocodone meets the FDA bioequivalence requirements for similar hydrocodone immediate-release products. Benzhydrocodone itself is rapidly metabolized by intestinal enzymes to the active metabolite, hydrocodone, with no detectable benzhydrocodone reaching circulation. Single oral doses of 6.67 mg benzhydrocodone produces a Cmax of 19.18 ng/mL with a Tmax of 1.25 h and an AUC of 125.73 h*ng/mL. Administration with food may slightly delay absorption but has no significant effect on AUC.

Half Life

The hydrocodone metabolite has a half life of elimination of 4.5 h.

Clearance

The apparent clearance of the hydrocodone metabolite is 64.4 L/h.

Elimination Route

The hydrocodone metabolite is eliminated through a mix of metabolism and renal excretion.

Innovators Monograph

You find simplified version here Benzhydrocodone

*** Taking medicines without doctor's advice can cause long-term problems.
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