Adult: As immediate-release preparation: Initially, 50 mg, 75 mg or 100 mg 4-6 hrly, depending on pain intensity. On day 1, a 2nd dose may be given 1 hr after the initial dose if pain relief is inadequate; subsequent dose may be given 4-6 hrly, adjust according to response. Max: 700 mg on day 1, 600 mg daily on subsequent days.
Oral Chronic pain, Neuropathic pain
Adult: Moderate to severe chronic pain; Neuropathic pain associated w/ diabetic peripheral neuropathy: As modified-release preparation: Initially, 50 mg 12 hrly, may increase by 100 mg every 3 days if pain relief is inadequate. Max: 500 mg daily.
Renal Impairment
Severe: Not recommended.
Hepatic Impairment
Moderate to severe acute pain:
Moderate: As immediate-release preparation: Initially, 50 mg, at intervals no less than 8 hrly. Max: 150 mg daily. Severe: Not recommended. Chronic pain; Neuropathic pain:
As modified-release preparation: Initially, 50 mg once daily, may be adjusted as tolerated. Max: 100 mg once daily. Severe: Not recommended.
Administration
May be taken with or without food.
Contraindications
Significant resp depression (in unmonitored settings or absence of resuscitative equipment), acute or severe bronchial asthma or hypercapnia, known or suspected paralytic ileus; acute intoxication w/ alcohol, hypnotics, centrally acting analgesics or psychotropic active substances. Concurrent or recent (w/in 2 wk) therapy w/ MAOIs.
Special Precautions
Patient w/ impaired resp function, head injury, brain tumours, biliary tract disease (including acute pancreatitis), history of seizure disorder. Avoid abrupt withdrawal. Moderate to severe hepatic impairment or severe renal impairment. Pregnancy and lactation.
Monitor resp and CV status, heart rate, BP; signs of misuse, abuse or addictions; signs/symptoms of hypoadrenalism or hypogonadism.
Overdosage
Symptoms: Vomiting, miosis, CV collapse, consciousness disorders up to coma, convulsions and resp depression up to resp arrest. Management: Re-establish a patent airway and institute assisted or controlled ventilation. GI decontamination w/ activated charcoal or by gastric lavage may be considered w/in 2 hr after intake. Pure opioid receptor antagonists (e.g. naloxone) may be given as antidote.
Drug Interactions
Increased risk of serotonin syndrome w/ other drugs that enhance monoaminergic neurotransmission (e.g. TCAs, triptans, SSRIs, serotonin and norepinephrine reuptake inhibitors). Enhanced sedative effect w/ benzodiazepines, barbiturates, antipsychotics, H1-antihistamines and other opioids. Increased potential for addiction w/ mixed μ-opioid agonists/antagonists (e.g. nalbuphine, pentazocine) or partial μ-opioid agonists (e.g. buprenorphine). Increased systemic exposure w/ strong inhibitors of UGT1A6, UGT1A9 and UGT2B7 isoenzymes. Decreased efficacy w/ strong enzyme inducers (e.g. rifampicin, phenobarbital). Potentially Fatal: Additive effect w/ MAOIs or w/in 2 wk after withdrawal.
Description: Tapentadol is a centrally-acting synthetic analgesic which inhibits ascending pain pathways by binding to μ-opiate receptor in the CNS and inhibiting norepinephrine reuptake, thus altering pain perception and response. Pharmacokinetics: Absorption: Rapidly and completely absorbed. Absolute bioavailability: Approx 32%. Time to peak plasma concentration: Approx 1.25 hr (immediate-release); 3-6 hr (long-acting formulations). Distribution: Widely distributed throughout the body. Plasma protein binding: Approx 20%. Metabolism: Extensively metabolised mainly via glucuronidation, and to a lesser extent, by CYP2C9, CYP2C19 and CYP2D6 isoenzymes, before further conjugation. Excretion: Via urine (approx 70% as conjugated metabolites and 3% as unchanged drug). Terminal half-life: Approx 4 hr.
Chemical Structure
Tapentadol Source: National Center for Biotechnology Information. PubChem Database. Tapentadol, CID=9838022, https://pubchem.ncbi.nlm.nih.gov/compound/Tapentadol (accessed on Jan. 23, 2020)
N02AX06 - tapentadol ; Belongs to the class of other opioids. Used to relieve pain.
References
Anon. Tapentadol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/03/2016.Buckingham R (ed). Tapentadol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/03/2016.McEvoy GK, Snow EK, Miller J et al (eds). Tapentadol Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 03/03/2016.Nucynta Solution (Janssen Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/03/2016.
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