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Beige Solid

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Hydrocodone is a powerful anticough drug that is widely used for suppressing the cough reflex. It is widely used in effective commercial anticough drugs in combination with guaiphenesin (entuss), with homatropine (hycodan), with phenylpropanolamine (hycomine), phenyltoloxamine (tussionex), and pseudoephedrine and guaiphenesin (tussened).

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ChEBI: A morphinane-like compound that is a semi-synthetic opioid synthesized from codeine.

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Hydrocodone is the 3 methoxy version of hydromorphone.The loss of the 3-OH group yields a compound that is approximately4 to 5 times less potent than hydromorphone, thusabout equal to morphine. Unlike codeine, the agonist activityof hydrocodone does not require 3-O-demethylation, althoughit does occur via CYP2D6 representing 4.6% of totalclearance. The protected 3-position has better brain penetration,and the 7,8-dihydro-6-keto C ring contributes to the increasedbinding of the compound to the μ-receptor.
There are no pure hydrocodone products available on theU.S. market. All FDA-approved products containing hydrocodoneare combination products. Like codeine, hydrocodoneis marketed as an antitussive agent. It is availablecombined with the anticholinergic agent homatropineas a syrup and a tablet. The addition of the anticholinergicagent is to discourage abuse. It is also available in a delayedrelease suspension form (Tussionex). This formulation usesa sulfonated styrene divinylbenzene copolymer complexedwith hydromorphone and chlorpheniramine that acts as acation-exchange resin slowly releasing the drugs over a 12-hour period. Hydrocodone is also marketed in combinationwith acetaminophen (Vicodin, Lortab) or aspirin (LortabASA) for the treatment of pain. The dose of acetaminophenconsumed by the patient must be closely monitored, andprescriptions that allow for greater than 4 grams of acetaminophenper 24-hour period should not be dispensed.

Safety Profile

Poison by intravenous and subcutaneous routes. When heated to decomposition it emits toxic fumes of NOx.

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