tapentadol (Nucynta)
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Introduction
FDA approved 2008
Indications
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
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
Dosage adjustment in renal failure
none
Pharmacokinetics
- metabolized by glucuronidation (tapentadol glucuronide)
- does not inhibit or induce cyt P450 enzymes
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 adverse effects of opiates
- drug adverse effects of psychotropic agents
- drug adverse effects of sedatives
Drug interactions
- addictive depressive effects on the central nervous system when taken with alcohol, other opioids, or illicit drugs
- drug interaction(s) of benzodiazepine with opiates
- drug interaction(s) of Z-drugs with opiates
- drug interaction(s) of alcoholic beverage with opiates
- drug interaction(s) of pregabalin with opiates
- drug interaction(s) of gabapentin with opiates
Laboratory
Mechanism of action
- centrally acting synthetic analgesic
- mu-opioid receptor agonist
- norepinephrine reuptake inhibitor
Notes
Johnson & Johnson
More general terms
References
- ↑ FDA News http://www.fda.gov/bbs/topics/NEWS/2008/NEW01916.html
- ↑ 2.0 2.1 2.2 2.3 2.4 Prescriber's Letter 16(7): 2009 New Drug: Nucynta (Tapentadol) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=250711&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 3.0 3.1 Deprecated Reference