Overview
11 DESCRIPTION Tapentadol extended-release tablet is an opioid agonist, supplied in extended-release film-coated tablets for oral administration, containing 58.24, 116.48, 174.72, 232.96, and 291.20 mg of tapentadol hydrochloride in each tablet strength, corresponding to 50, 100, 150, 200, and 250 mg of tapentadol free-base, respectively.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Tapentadol is a centrally-acting synthetic analgesic. The exact mechanism of action is unknown. Although the clinical relevance is unclear, preclinical studies have shown that tapentadol is a mu-opioid receptor (MOR) agonist and a norepinephrine reuptake inhibitor (NRI). Analgesia in animal models is derived from both of these properties. 12.2 Pharmacodynamics Effects on the Central Nervous System (CNS) Tapentadol produces respiratory depression, by direct action on the brainstem respiratory centers. The respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide tension and electrical stimulation. Tapentadol causes miosis, even in total darkness.
Indications
- 1 INDICATIONS AND USAGE Tapentadol extended-release tablets are indicated for the management of: Severe and persistent pain in adults that requires an extended treatment period with a daily opioid analgesic and for which alternative treatment options are inadequate. Severe and persistent neuropathic pain associated with diabetic peripheral neuropathy (DPN) in adults that requires an extended treatment period with a daily opioid analgesic and for which alternative treatment options are inadequate.
Common Doses
- 500 mg
- 50 mg
- 100 mg
- 600 mg
Dosage
2 DOSAGE AND ADMINISTRATION Tapentadol extended-release tablets should be prescribed only by healthcare professionals who are knowledgeable about the use of extended-release/long-acting opioids and how to mitigate the associated risks. ( 2.1 ) Use the lowest effective dosage for the shortest duration of time consistent with individual patient treatment goals. Reserve titration to higher doses of tapentadol extended-release tablets for patients in whom lower doses are insufficiently effective and in whom the expected benefits of using a higher dose opioid clearly outweigh the substantial risks...
Black Box Warning
WARNING: SERIOUS AND LIFE-THREATENING RISKS FROM USE OF TAPENTADOL EXTENDED-RELEASE TABLETS Addiction, Abuse, and Misuse Because the use of tapentadol extended-release tablets expose 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 and reassess all patients regularly for the development of these behaviors and conditions [see Warnings and Precautions (5.1) ] .
Contraindications
- 4 CONTRAINDICATIONS Tapentadol extended-release tablets are contraindicated in patients with: Significant respiratory depression Acute or severe bronchial asthma or hypercarbia in an unmonitored setting or in the absence of resuscitative equipment Known or suspected gastrointestinal obstruction, including paralytic ileus Hypersensitivity (e.g., anaphylaxis, angioedema) to tapentadol or to any other ingredients of the product [see Adverse Reactions (6.
Side Effects
- 6 ADVERSE REACTIONS The following serious adverse reactions are described, or described in greater detail, in other sections: Addiction, Abuse, and Misuse [see Warnings and Precautions (5.1) ] Life-Threatening Respiratory Depression [see Warnings and Precautions (5.2) ] Interaction with Benzodiazepine or Other CNS Depressants [see Warnings and Precautions (5.3) ] Neonatal Opioid Withdrawal Syndrome [see Warnings and Precautions (5.4) ] Opioid-Induced Hyperalgesia and Allodynia [see Warnings and Precautions (5.6) ] Serotonin Syndrome [see Warnings and Precautions (5.
Interactions
- 7 DRUG INTERACTIONS Table 3 includes clinically significant drug interactions with tapentadol extended-release tablets. Table 3. Clinically Significant Drug Interactions with tapentadol extended-release tablets Alcohol Clinical Impact: Concomitant use of alcohol with tapentadol extended-release tablets can result in an increase of tapentadol plasma levels and potentially fatal overdose of tapentadol. Intervention: Instruct patients not to consume alcoholic beverages or use prescription or non-prescription products containing alcohol while on tapentadol extended-release tablet therapy [see...