by Agent G

Created on: July 22, 2009

Hydrocodone is an analgesic (pain reliever) and antitussive (cough suppressant). Hydrocodone is the most frequently prescribed opiate in the United States with nearly 130 million prescriptions for hydrocodone-containing products dispensed in 2006. Studies indicate that hydrocodone is as effective, or more effective, than codeine for cough suppression and nearly equipotent to morphine for pain relief.

Hydrocodone is an analgesic (pain reliever) and antitussive (cough suppressant). Hydrocodone is the most frequently prescribed opiate in the United States with nearly 130 million prescriptions for hydrocodone-containing products dispensed in 2006. Hydrocodone has been clinically proven to be as effective, or more effective, than codeine for cough suppression and nearly equipotent to morphine for pain relief. Although hydrocodone is marketed under many trade names, Vicodin. Lorcet, and Lortab are the most familiar.

Indication

Hydrocodone is indicated for moderate to sever acute pain. When being used as an analgesic, hydrocodone is always coformulated with acetaminophen, ibuprofen, or aspirin to treat pain. Used as an antitussive, hydrocodone is combined with phenylephrine, pseudoephedrine, phenylpropanolamine, guaifenesin, pyrilamine, pheniramine, or chlorpheniramine.

Side effects

Side effects of hydrocodone include effects on the CNS including drowsiness, mental clouding, lethargy, impairment of mental and physical performance, anxiety, fear, dysphoria, psychic dependence, and mood changes. Due to its effect on smooth muscle, prolonged use of any opioid, including hydrocodone can cause constipation and uninary retention. Overdosing may lead to respiratory depression. Naloxone, an opioid antagonist, can reverse the effects of hydrocodone in the event of an overdose.

Mechanism of Action

Hydrocodone acts on the central nervous system (CNS) and smooth muscle to provide analgesia as an opioid agonist. It is a semi-synthetic opioid most closely related to codeine in structure and morphine in producing opiate-like effects. Hydrocodone acts as a weak agonist at OP1, OP2, and OP3 opiate receptors within the CNS. Hydrocodone primarily affects OP3 receptors. OP3 receptors couple with G-protein receptors and function as modulators of synaptic transmission via G-proteins that activate effector proteins. Hydrocodone binding stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface

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