Tapentadol


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Moderate to severe acute pain As immediate-release preparation: Initial: 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/day afterwards. Moderate to severe chronic pain; Neuropathic pain associated w/ diabetic peripheral neuropathy As modified-release preparation: Initial: 50 mg 12 hrly, increase by 100 mg every 3 days, if necessary. Max: 500 mg/day.
Dosage Details
Oral
Moderate to severe acute pain
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.
Adverse Reactions
Nausea, vomiting, dizziness, somnolence, constipation, pruritus, dry mouth, hyperhidrosis, fatigue, CNS depression, seizures, orthostatic hypotension, syncope.
Potentially Fatal: Resp depression.
Patient Counseling Information
May impair ability to drive or operate machinery.
MonitoringParameters
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.
Food Interaction
Enhanced sedative effect w/ alcohol. Decreased efficacy w/ St John’s wort.
Action
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

Click on icon to see table/diagram/image
Storage
Store up to 25°C. Protect tab from moisture.
MIMS Class
ATC Classification
N02AX06 - tapentadol ; Belongs to the class of other opioids. Used to relieve pain.
Disclaimer: This information is independently developed by MIMS based on Tapentadol from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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