OXYMORPHONE G74 40MG

Product Description

Oxymorphone Hydrochloride 40 mg extended-release oral tablets deliver a high-potency semi-synthetic $\mu$-opioid receptor agonist engineered for 12-hour sustained analgesia. Chemically related to morphine and hydromorphone, oxymorphone exhibits an analgesic potency approximately three times greater than oral morphine, providing reliable pain control for refractory chronic conditions such as oncological malignancies or severe, non-malignant musculoskeletal trauma.

Clinical Profile & Physical Identification

• Active Ingredient: Oxymorphone Hydrochloride (40 mg)

• Physical Imprint: Round, yellow, film-coated biconvex tablet debossed with “G74” on one side and plain on the reverse (manufactured by Global Pharmaceuticals / Impax Laboratories).

• Mechanism of Action: Acts as a full agonist with high intrinsic affinity for central and peripheral $\mu$-opioid receptors, with secondary affinity for $\kappa$-opioid receptors. Binding stimulates intracellular inhibitory G-proteins, inhibiting adenylyl cyclase, reducing cyclic adenosine monophosphate (cAMP) synthesis, closing N-type voltage-operated calcium channels, and opening inwardly rectifying potassium channels. This hyperpolarizes ascending nociceptive projection neurons, dampening pain signal transmission across the spinal cord dorsal horn, thalamus, and periaqueductal gray.

• Pharmacokinetics & Absorption: Formulated for extended systemic delivery, providing stable therapeutic plasma concentrations over a 12-hour dosing interval. Mean oral bioavailability is approximately 10% due to extensive first-pass hepatic metabolism.

• Critical Food Effect: Co-administration with food significantly increases systemic exposure; a high-fat meal can elevate peak plasma concentration ($C_{\max}$) by up to 50% and total absorption ($\text{AUC}$) by 38%. Tablets must be taken on an empty stomach, at least one hour before or two hours after meals.

• Metabolism & Elimination: Primarily metabolized in the liver via glucuronidation to oxymorphone-3-glucuronide (inactive) and 6-hydroxyoxymorphone (minor active metabolite). Unlike many opioids, oxymorphone does not rely on cytochrome P450 enzymes (such as CYP2D6 or CYP3A4) for its primary metabolic clearance, reducing the risk of CYP-mediated pharmacokinetic drug-drug interactions. Exhibits an effective terminal elimination half-life of 9 to 11 hours with primary excretion in urine.

Indications & Opioid Tolerance Requirements

• Chronic Pain Indication: Reserved exclusively for patients with severe pain requiring daily, around-the-clock, long-term opioid analgesia where alternative treatment options (e.g., non-opioid analgesics or immediate-release opioids) are ineffective or poorly tolerated.

• Strict Opioid Tolerance Mandate: The 40 mg single-dose strength is indicated only for patients who are fully opioid-tolerant. Patients are considered opioid-tolerant if they have taken at least 60 mg oral morphine daily, 30 mg oral oxycodone daily, 20 mg oral oxymorphone daily, or an equianalgesic dose of another opioid continuously for one week or longer. Administration to opioid-naive individuals can cause fatal respiratory arrest.

• Dosage Form Integrity: Tablets must be swallowed whole with water. Crushing, chewing, snorting, or dissolving the tablet destroys the extended-release mechanism, precipitating rapid drug release (“dose dumping”) and lethal opioid toxicity.

Important Safety Information & Boxed Warnings

• Addiction, Abuse, and Misuse: Oxymorphone is a Schedule II controlled substance carrying high risks of addiction, abuse, and diversion, which can lead to overdose and death.

• Life-Threatening Respiratory Depression: Serious, life-threatening, or fatal respiratory depression may occur, particularly upon initiation of therapy or following dose titration.

• Accidental Ingestion: Accidental ingestion of even one 40 mg tablet, especially by children, can result in fatal respiratory depression.

• Concomitant CNS Depressant Risks: Co-administration with benzodiazepines, other sedatives, tranquilizers, or alcohol increases the risk of profound sedation, respiratory depression, coma, and death.

• Neonatal Opioid Withdrawal Syndrome (NOWS): Prolonged maternal use during pregnancy can result in life-threatening neonatal opioid withdrawal syndrome.