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 |
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