Monograph
N02AX06 - Tapentadol |
Propably not porphyrinogenic |
PNP |
Rationale
Studies have shown that tapentadol has no clinically relevant potential for induction or inhibition of CYP enzymes and is therefore probably not porphyrinogenic. Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Chemical description
Tapentadol is an μ-opioid agonist with noradrenaline reuptake inhibiting properties.
Therapeutic characteristics
Tapentadol is an analgesic used for the relief of moderate to severe acute pain in adults.
It is administered orally.
Common adverse reactions of tapentadol that can be confused with an acute porphyric attack are nausea, vomiting and constipation. Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Metabolism and pharmacokinetics
Tapentadol is mainly metabolized by conjugation with glucuronic acid to produce glucuronides. A smaller portion of the drug is metabolized to N-desmethyl tapentadol (13%) by CYP2C9 and CYP2C19 and to hydroxy tapentadol (2%) by CYP2D6, which are further metabolized by conjugation.
In vitro studies has not revealed any clinical significant potential of tapentadol to either inhibit or induce cytochrome P450 enzymes. One in vitro study showed inhibition of CYP 2D6 to a limited extent, but at clinically irrelevant concentrations.
References
| # |
Citation details |
PMID |
|---|
| * | Scientific articles |
| 1. |
Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes.
Kneip C, Terlinden R et al. Drug Metab Lett. 2008 Jan;2(1):67-75. |
19356073 |
| 2. |
Tapentadol: an initial analysis.
Prommer EE. J Opioid Manag. 2010 May-Jun;6(3):223-6. |
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| * | Drug reference publications |
| 3. |
Sweetman SC, editor. Martindale: The complete drug reference. Tapentadol. Pharmaceutical Press 2009.
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| * | Government bodies |
| 4. |
Food and Drug Administration. FDA labelling information. FDA web site,
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| * | Summary of Product Characteristics |
| 5. |
The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). (Palexia).
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