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Benzhydrocodone API Manufacturers & Suppliers

General Description:

Benzhydrocodone, identified by CAS number 1259440-61-3, is a notable compound with significant therapeutic applications. 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 under the trade name Apadaz, marketed by KVK Tech and developed by KemPharm.

Indications:

This drug is primarily indicated for: Benzyhydrocodone is indicated, in combination with , for the short-term management of acute pain requiring opioid therapy. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Benzhydrocodone undergoes metabolic processing primarily in: Benzhydrocodone is rapidly metabolized to hydrocodone by intestinal enzymes. Hydrocodone undergoes oxidative metabolism by CYP3A4 and CYP2D6 which contribute to N-demethylation and O-demethylation respectively. The dealkylated metabolites undergo further 6-ketoreduction to the 6-α- and 6-β-hydroxy metabolites as well as glucuronide conjugation. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Benzhydrocodone are crucial for its therapeutic efficacy: 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. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Benzhydrocodone is an important consideration for its dosing schedule: The hydrocodone metabolite has a half life of elimination of 4.5 h. This determines the duration of action and helps in formulating effective dosing regimens.

Route of Elimination:

The elimination of Benzhydrocodone from the body primarily occurs through: The hydrocodone metabolite is eliminated through a mix of metabolism and renal excretion. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Benzhydrocodone is distributed throughout the body with a volume of distribution of: The hydrocodone metabolite of benzhydrocodone has an apparent volume of distribution of 714 L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Benzhydrocodone is a critical factor in determining its safe and effective dosage: The apparent clearance of the hydrocodone metabolite is 64.4 L/h. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Benzhydrocodone exerts its therapeutic effects through: Benzhydrocodone is rapidly metabolized to which acts on the central nervous system to produce analgesia. The action of hydrocodone in the brain can also produce euphoria, leading to addiction. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Benzhydrocodone functions by: Benzyhydrocodone is not reported to have pharmacological activity of its own and it not present in the plasma at detectable concentrations. Its active metabolite, is a mu-opioid receptor agonist. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Categories:

Benzhydrocodone is categorized under the following therapeutic classes: Opioids. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.