Oxycodone and Acetaminophen

OXYCODONE AND ACETAMINOPHEN- oxycodone hydrochloride and acetaminophen tablet
Alvogen, Inc.

5-325-label7.5-325-label10-325-labeloxy-hcl-structure

WARNING: ADDICTION, ABUSE, AND MISUSE; RISK EVALUATION AND MITIGATION STRATEGY (REMS); LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION; NEONATAL OPIOID WITHDRAWAL SYNDROME, CYTOCHROME P450 3A4 INTERACTION; HEPATOTOXICITY, and RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS

Addiction, Abuse, and Misuse
Oxycodone and acetaminophen tablets exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death. Assess each patient’s risk prior to prescribing oxycodone and acetaminophen tablets, and monitor all patients regularly for the development of these behaviors and conditions [see WARNINGS].

Opioid Analgesic Risk Evaluation and Mitigation Strategy (REMS):
To ensure that the benefits of opioid analgesics outweigh the risks of addiction, abuse, and misuse, the Food and Drug Administration (FDA) has required a REMS for these products [see Warnings]. Under the requirements of the REMS, drug companies with approved opioid analgesic products must make REMS-compliant education programs available to healthcare providers. Healthcare providers are strongly encouraged to

  • complete a REMS-compliant education program,
  • counsel patients and/or their caregivers, with every prescription, on safe use, serious risks, storage, and disposal of these products,
  • emphasize to patients and their caregivers the importance of reading the Medication Guide every time it is provided by their pharmacist, and
  • consider other tools to improve patient, household, and community safety.

Life-Threatening Respiratory Depression
Serious, life-threatening, or fatal respiratory depression may occur with use of oxycodone and acetaminophen tablets. Monitor for respiratory depression, especially during initiation of oxycodone and acetaminophen tablets or following a dose increase [see WARNINGS].

Accidental Ingestion
Accidental ingestion of oxycodone and acetaminophen tablets, especially by children, can result in a fatal overdose of oxycodone and acetaminophen tablets [see WARNINGS].

Neonatal Opioid Withdrawal Syndrome
Prolonged use of oxycodone and acetaminophen tablets during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated, and requires management according to protocols developed by neonatology experts. If opioid use is required for a prolonged period in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available [see WARNINGS].

Cytochrome P450 3A4 Interaction
The concomitant use of oxycodone and acetaminophen tablets with all cytochrome P450 3A4 inhibitors may result in an increase in oxycodone plasma concentrations, which could increase or prolong adverse reactions and may cause potentially fatal respiratory depression. In addition, discontinuation of a concomitantly used cytochrome P450 3A4 inducer may result in an increase in oxycodone plasma concentration. Monitor patients receiving oxycodone and acetaminophen tablets and any CYP3A4 inhibitor or inducer [see CLINICAL PHARMACOLOGY, WARNINGS, PRECAUTIONS; Drug Interactions].

Hepatotoxicity
Acetaminophen has been associated with cases of acute liver failure, at times resulting in liver transplant and death. Most of the cases of liver injury are associated with the use of acetaminophen at doses that exceed 4000 mg per day, and often involve more than one acetaminophen-containing product.

Risks From Concomitant Use With Benzodiazepines Or Other CNS Depressants
Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death [see WARNINGS, PRECAUTIONS; Drug Interactions].

  • Reserve concomitant prescribing of oxycodone and acetaminophen tablets and benzodiazepines or other CNS depressants for use in patients for whom alternative treatment options are inadequate.
  • Limit dosages and durations to the minimum required.
  • Follow patients for signs and symptoms of respiratory depression and sedation.

DESCRIPTION

Oxycodone and Acetaminophen is available in tablets for oral administration.

Each tablet for oral administration contains:

Oxycodone Hydrochloride, USP……………………………… 5 mg*
(*5 mg oxycodone hydrochloride is equivalent to 4.4815 mg of oxycodone.)
Acetaminophen, USP……………………………………………. 325 mg

Oxycodone Hydrochloride, USP……………………………… 7.5 mg*
(*7.5 mg oxycodone hydrochloride is equivalent to 6.7228 mg of oxycodone.)
Acetaminophen, USP……………………………………………. 325 mg

Oxycodone Hydrochloride, USP……………………………… 10 mg*
(*10 mg oxycodone hydrochloride is equivalent to 8.9637 mg of oxycodone.)
Acetaminophen, USP……………………………………………. 325 mg

Inactive Ingredients

All strengths of Oxycodone and Acetaminophen Tablets, USP contain the inactive ingredients crospovidone, lactose monohydrate, povidone, pregelatinized corn starch, and stearic acid. The 5 mg/325 mg tablets contain FD&C Blue No. 1 Aluminum Lake as a colorant. The 7.5 mg/325 mg tablets contain FD&C Yellow No. 6 Aluminum Lake as a colorant. The 10 mg/325 mg tablets contain D&C Yellow No. 10 Aluminum Lake as a colorant.

Oxycodone and acetaminophen tablets contain oxycodone, 14-hydroxydihydrocodeinone, a semisynthetic opioid analgesic which occurs as a white to off-white fine crystalline powder. The molecular formula for oxycodone hydrochloride is C18 H21 NO4 ∙ HCl and the molecular weight is 351.82. It is derived from the opium alkaloid, thebaine, and may be represented by the following structural formula:

oxy-hcl-structure
(click image for full-size original)

Oxycodone and acetaminophen tablets contain acetaminophen, 4′-hydroxyacetanilide, a non-opiate, non-salicylate analgesic and antipyretic which occurs as a white, odorless, crystalline powder. The molecular formula for acetaminophen is C8 H9 NO2 and the molecular weight is 151.17. It may be represented by the following structural formula:

apap-structure
(click image for full-size original)

CLINICAL PHARMACOLOGY

Mechanism of Action

Oxycodone is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can interact with other opioid receptors at higher doses. The principal therapeutic action of oxycodone is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with oxycodone. Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression.

The precise mechanism of the analgesic action is unknown. However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug.

The precise mechanism of the analgesic properties of acetaminophen is not established but is thought to involve central actions.

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