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tapentadol (Nucynta)
FDA approved 2008
Indications:
- chronic pain
- osteoarthritis
- diabetic neuropathy [3]
Contraindications:
- significant respiratory depression
- acute or severe bronchial asthma
- hypercapnia in unmonitored settings or the absence of resuscitative equipment
Cautions
- renal insufficiency (severe)
- hepatic insufficiency (severe)
- seizures
Pregnancy-category: C
Dosage:
- start: 50 mg every 4-6 hours [2]
- if 1st dose fails to provide sufficient pain relief, a 2nd dose may be given 1 hour after the first [2]
- maximum: 600 mg/day (700 mg on 1st day) [2]
- 50-100 mg works about as well as oxycodone 10-15 mg for acute pain
Tabs: 50, 75, 100 mg
blister packs of 10 & bottles of 100
Pharmacokinetics:
- metabolized by glucuronidation (tapentadol glucuronide)
- does not inhibit or induce cyt P450 enzymes
Dosage adjustment in renal failure: none
Adverse effects:
- nausea, vomiting less than oxycodone [2]
- dizziness
- sleepiness
- risk of respiratory depression
- may increase risk of seizures
- may exaggerate increase in intracranial pressure caused by head injury or intracranial lesions
- abuse potential
Drug interactions:
- addictive depressive effects on the central nervous system when taken with alcohol, other opioids, or illicit drugs
Laboratory:
- tapentadol in tissue
- tapentadol in body fluid
- tapentadol in blood
- tapentadol in serum/plasma/blood
- tapentadol in serum/plasma
- tapentadol in saliva
- tapentadol in urine
Mechanism of action:
- centrally acting synthetic analgesic
- mu-opioid receptor agonist
- norepinephrine reuptake inhibitor
Note: Johnson & Johnson
Interactions
drug adverse effects of opiates
General
opioid receptor agonist (narcotic)
Database Correlations
PUBCHEM correlations
References
- FDA News
http://www.fda.gov/bbs/topics/NEWS/2008/NEW01916.html
- Prescriber's Letter 16(7): 2009
New Drug: Nucynta (Tapentadol)
Detail-Document#: 250711
(subscription needed) http://www.prescribersletter.com
- Deprecated Reference