Adult: For moderate to severe cases: As conventional tab or oral solution: Initially, 50-100 mg 4-6 hourly as needed. On the 1st day, an additional dose may be given 1 hour after the initial dose if pain control is not achieved. Max: 700 mg daily on the 1st day and 600 mg daily on subsequent days. Dose and dosing intervals are individualised based on patient-specific factors (e.g. pain severity, degree of opioid experience or tolerance). Use the lowest effective dose for the shortest possible duration. Dosage and treatment recommendations may vary among countries and individual products (refer to specific product guidelines). Child: ≥2 years weighing >16 kg: As conventional oral solution: 1.25 mg/kg 4 hourly for up to 3 days. Max: 7.5 mg/kg daily. For children with high BMI, the calculated maximum dose for a body weight at the 97.5th percentile for the given age must not be exceeded. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
Oral Chronic pain
Adult: For severe cases: As extended-release tab: Initially, 50 mg 12 hourly, may increase in increments of 50 mg bid every 3 days. Max: 500 mg daily. Dose and dosing intervals are individualised based on patient-specific factors (e.g. pain severity, degree of opioid experience or tolerance). Use the lowest effective dose for the shortest possible duration. Dosage and treatment recommendations may vary among countries and individual products (refer to specific product guidelines).
Oral Neuropathic pain associated with diabetic peripheral neuropathy
Adult: For severe and persistent cases in patients who require an extended treatment period with a daily opioid analgesic and for whom alternative treatment options are ineffective, not tolerated or inadequate. As extended-release tab: Initially, 50 mg 12 hourly, may increase in increments of 50 mg bid every 3 days. Max: 500 mg daily. Dose and dosing intervals are individualised based on patient-specific factors (e.g. pain severity, degree of opioid experience or tolerance). Use the lowest effective dose for the shortest possible duration. Treatment recommendations may vary among countries and individual products (refer to specific product guidelines).
Renal Impairment
Severe: Not recommended.
Hepatic Impairment
Acute pain:
Moderate (Child-Pugh class B): As conventional tab: Initially, 50 mg up to 8 hourly. As conventional oral solution: Initially, 25 mg up to 8 hourly. Max: 150 mg in 24 hours. Severe (Child-Pugh class C): As conventional tab or oral solution: Not recommended.
Chronic pain; Neuropathic pain associated with diabetic peripheral neuropathy:
Moderate (Child-Pugh class B): As extended-release tab: Initially, 50 mg once daily. Max: 100 mg daily. Severe (Child-Pugh class C): As extended-release tab: Not recommended.
Administration
Tapentadol May be taken with or without food.
Contraindications
Significant respiratory depression, acute or severe bronchial asthma or hypercapnia (in unmonitored settings or absence of resuscitative equipment); known or suspected gastrointestinal obstruction (including paralytic ileus). Concomitant use with or within 14 days after MAOI therapy.
Special Precautions
Patient with personal or family history of substance use disorders; mental health conditions (e.g. major depression, anxiety, personality disorders, PTSD); impaired respiratory functions; elevated intracranial pressure, head injury, brain tumours; history of seizure disorder or any condition that may increase the risk of seizures; biliary tract disease (including acute pancreatitis); hypovolaemia, CV disease (e.g. acute MI), adrenal insufficiency (including Addison's disease), prostatic hyperplasia or urinary stricture, sleep-related disorders (e.g. sleep apnoea). Cachectic or debilitated patients. Avoid abrupt withdrawal. Avoid use in patients with impaired consciousness or coma. Concomitant use with benzodiazepines and other CNS depressants. Mild to moderate renal and moderate hepatic impairment; not recommended for severe renal and hepatic impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Drug tolerance, physical and psychological dependence, opioid use disorder; withdrawal symptoms (after abrupt discontinuation); sleep-related breathing disorders (e.g. central sleep apnoea, sleep-related hypoxaemia); opioid-induced hyperalgesia; severe hypotension (including orthostatic hypotension and syncope); may cause or exacerbate pre-existing seizures, spasm of sphincter of Oddi. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, constipation, dyspepsia, dry mouth. General disorders and administration site conditions: Fatigue, asthenia, feeling of body temperature change. Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Muscle spasms. Nervous system disorders: Headache, dizziness, somnolence, tremor. Psychiatric disorders: Abnormal dreams, anxiety, confusional state, hallucination, sleep disorder. Skin and subcutaneous tissue disorders: Rash, pruritus, hyperhidrosis. Vascular disorders: Flushing. Potentially Fatal: Respiratory depression.
This drug may cause drowsiness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor respiratory and mental status (particularly during initiation or after dose increase); blood pressure, heart rate, and bowel function. Assess for signs or symptoms of misuse, abuse or substance use disorder.
Overdosage
Symptoms: Vomiting, constricted pupils, convulsions, skeletal muscle flaccidity, cold and clammy skin, CV collapse, somnolence leading to stupor or coma, and respiratory depression leading to respiratory arrest. In some cases, bradycardia, hypotension, hypoglycaemia, atypical snoring, and pulmonary oedema. Management: Supportive treatment. Re-establish a patent airway and institute assisted or controlled ventilation. In case of circulatory shock and pulmonary oedema, may employ other supportive measures (e.g. oxygen, vasopressors). Pure opioid receptor antagonists (e.g. naloxone) may be given as an antidote for respiratory depression. May consider gastrointestinal decontamination using activated charcoal or by performing gastric lavage within 2 hours following intake; ensure that the airway is secured before attempting gastrointestinal decontamination.
Drug Interactions
Concomitant use with or within the last 14 days after MAOI therapy may result in adverse CV effects (e.g. hypertensive crisis). May precipitate withdrawal symptoms and reduce efficacy with mixed agonist/antagonist analgesics (e.g. pentazocine, nalbuphine, butorphanol) or partial agonist analgesics (e.g. buprenorphine). Increased risk of seizure with other agents that may lower seizure threshold (e.g. SSRIs, SNRIs, TCAs, antipsychotics). Increased risk of urinary retention and severe constipation with anticholinergic agents. May reduce the efficacy of diuretics. May reduce efficacy with strong enzyme inducers (e.g. rifampicin, phenobarbital). May increase systemic exposure with strong UGT inhibitors (e.g. ketoconazole, fluconazole, meclofenamic acid). Potentially Fatal: Concomitant use with benzodiazepines or CNS depressants (e.g. anxiolytics, tranquillisers, general anaesthetics, antipsychotics, H1 antihistamines, other opioids) may result in profound sedation, respiratory depression and coma. Increased risk of serotonin syndrome with serotonergic agents (e.g. SSRIs, SNRIs, TCAs, triptans) and agents that impair serotonin metabolism (e.g. MAOIs).
Food Interaction
Additive CNS depressant effect with alcohol. Increased plasma concentration with high-fat/calorie meal. May reduce efficacy with St. John's wort.
Action
Description: Mechanism of Action: Tapentadol is a strong opioid analgesic with mainly μ-agonistic opioid and norepinephrine reuptake inhibition properties. It inhibits the ascending pain pathways by binding to μ-opiate receptors in the CNS, leading to alteration of perception of and response to pain. Pharmacokinetics: Absorption: Rapidly and completely absorbed. Increased plasma concentration with high-fat/calorie meal. Bioavailability: Approx 32%. Time to peak plasma concentration: Approx 1.25 hours (conventional form); 3-6 hours (extended-release tab). Distribution: Widely distributed throughout the body. Plasma protein binding: Approx 20%. Metabolism: Extensively metabolised mainly via glucuronidation into glucuronides (major metabolite: tapentadol-O-glucuronide), and to a lesser extent by CYP2C9, CYP2C19, and CYP2D6 isoenzymes into N-desmethyl tapentadol before further conjugation. Undergoes extensive first-pass metabolism. Excretion: Via urine (99%; approx 70% as conjugated forms, 3% as unchanged drug). Terminal elimination half-life: 4 hours (conventional form); approx 5-6 hours (extended-release tab).
Chemical Structure
Tapentadol Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 9838022, Tapentadol. https://pubchem.ncbi.nlm.nih.gov/compound/Tapentadol. Accessed May 27, 2025.
Storage
Store between 15-30°C. Protect the tab from moisture.
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