Product Information
Registration Status: ActiveSIN14607P
NUCYNTA IR TABLET 50mg is approved to be sold in Singapore with effective from 2014-08-09. It is marketed by MUNDIPHARMA PHARMACEUTICALS PTE LTD, with the registration number of SIN14607P.
This product contains Tapentadol 50mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Janssen Ortho LLC in PUERTO RICO.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Opioid analgesic for treatment of moderate to severe pain. FDA approved on Nov 20, 2008.
Indication
The immediate-release formulation of tapentadol is indicated for the relief of moderate to severe acute pain. The long-acting formulation serves as a continuous, around-the-clock analgesic that is indicated for the relief of moderate to severe chronic pain or neuropathic pain associated with diabetic peripheral neuropathy.
Mechanism of Action
Tapendadol causes large increases in levels of extracellular norepinephrine (NE) due to a dual mechanism of action involving mu opioid receptor (MOR) agonism as well as noradrenaline reuptake inhibition.
Pharmacokinetics
- Absorption
- Bioavailability, immediate release (IR), 86 mg: 32%; Bioavailability, extended release (ER), 86 mg: 32%; Cmax, IR: 64.2 ng/mL; Cmax, ER: 22.5 ng/mL; T max, IR: 1.5 hours; T max, ER: 5.0 hours; Tapentadol accumulates following multiple repeat doses.
- Distribution
- Following IV administration, volume of distribution is 540 ± 98 L.
- Metabolism
- 97% of the dose is metabolized mostly via conjugation with glucuronic acid to produce glucuronides. Tapentadol is also metabolized into N-desmethyl tapentadol (13%) by CYP2C9 and CYP 2C19. CYP2D6 is involved in the formation of the metabolite, hydroxy tapentadol (2%). All metabolites are inactive.
- Elimination
Clearance
Total clearance = 1530 ± 177 ml/min.
Toxicity
Oral, rabbit: LD50 = 3200 mg/kg; Oral, mouse: LD50 = 300 mg/kg; Oral, rat: LD50: 980 mg/kg; The most common reasons for discontinuation due to adverse events were dizziness, nausea, vomiting, somnolence, and headache.
Active Ingredient/Synonyms
Tapentadol | Tapentadol |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.