TAPAL 50
TAPENTADOL HYDROCHLORIDE
What it does
Tapentadol is a strong pain relief medication that belongs to the opioid class. It helps manage moderate to severe pain.
Commonly used for: moderate to severe pain, pain management
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Source: Pharmacy and Poisons Board · fetched 2026-01-28 19:58:01 · updated 2026-09-25 02:29:58
Drug Interactions
62Pharmacodynamic Warnings
Tapentadol appears in TABLE 11: Drugs with CNS depressant effects
Severe (6)
Opioids - decreases concentration
Brigatinib potentially decreases the concentration of opioids (alfentanil, fentanyl). Avoid. Also see TABLE 6 p. 1518
Opioids - increases exposure
Ceritinib is predicted to increase the exposure to opioids (alfentanil, fentanyl). Avoid. Theoretical → Also see TABLE 6 p. 1518
Opioids - increases risk of cnstoxicity
Ritonavir increases the risk of CNS toxicity when given with opioids (pethidine). Avoid.
Opioids - decreases exposure
Lorlatinib is predicted to decrease the exposure to opioids (alfentanil, fentanyl). Avoid.
Opioids - increases risk of adverse effects
Selegiline increases the risk of adverse effects when given with opioids (pethidine). Avoid. Also see TABLE 13 p. 1520
Opioids - increases exposure
Selpercatinib is predicted to increase the exposure to opioids (alfentanil, buprenorphine). Avoid.
Moderate (31)
Opioids - increases exposure
Dronedaroneispredictedtoincreasetheexposuretoopioids (alfentanil,buprenorphine,fentanyl,oxycodone).Monitorand adjustdose.oStudy →AlsoseeTABLE6p.1518
Opioids - increases concentration
Amiodarone is predicted to increase the concentration of opioids (fentanyl). Monitor and adjust dose. Also see TABLE 6 p. 1518.
Opioids - decreases concentration
Carbamazepine decreases the concentration of opioids (tramadol). Adjust dose.
Opioids - increases exposure
Miconazole is predicted to increase the exposure to opioids (alfentanil). Use with caution and adjust dose.
Opioids - increases exposure
Antifungals, azoles (fluconazole, isavuconazole, posaconazole) are predicted to increase the exposure to opioids (alfentanil, buprenorphine, fentanyl, oxycodone). Monitor and adjust dose.
Unknown (25)
Drugs That Cause Serotonin Syndrome - increases risk of serotonin syndrome
Tapentadol is predicted to increase the risk of serotonin syndrome when given with drugs that cause serotonin syndrome (see TABLE 13 p. 1520).
Drugs That Cause Serotonin Syndrome - increases risk of serotonin syndrome
Opioids (tapentadol) are predicted to increase the risk of serotonin syndrome when given with drugs that cause serotonin syndrome (see TABLE 13 p. 1520). Theoretical drugs that reduce serum potassium.
Opioids - additive effect
Clozapine can cause constipation, as can opioids; concurrent use might increase the risk of developing intestinal obstruction. Also see TABLE 11 p. 1519
Opioids - increases exposure
Asciminibispredictedtoincreasetheexposuretoopioids (alfentanil).rTheoretical
Opioids - increases exposure
Bictegravirispredictedtoincreasetheexposuretoopioids (methadone).oTheoretical
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: class
About this medicine
Tapentadol is a strong pain relief medication that belongs to the opioid class. It helps manage moderate to severe pain.
What it treats
- moderate to severe pain
- pain management
How it works
Tapentadol works by changing how the brain and nervous system respond to pain.
Who it's for
This medication is for adults who need relief from significant pain.
Drug class
Opioids
Cautions
- • Be careful if you are also taking other medications that can slow down your brain activity.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Tapentadol
BNF-referencedTapentadol is a synthetic analgesic classified as an opioid. It is primarily used for the management of moderate to severe pain that cannot be adequately controlled by other analgesics. Tapentadol exhibits a dual mechanism of action, providing effective pain relief while minimizing some common side effects associated with traditional opioids.
Indications
- Moderate to severe acute pain that can be managed only with opioid analgesics
- Severe chronic pain requiring opioid treatment
Dosage
Children: In children aged 1 to 11 years, the dose is 1.35 to 4.3 mg/kg, and for those aged 12 to 17 years, the dose is 7.
Adults: For immediate-release tablets, the initial dose is 50 mg every 4–6 hours, adjusted according to response, with a maximum allowable dose of 500 mg per day. For modified-release tablets, the initial dose is 50 mg every 12 hours, adjusted as needed.
Mechanism of action
Tapentadol is a selective mu-opioid receptor agonist, which binds with high affinity to mu-opioid receptors, producing analgesia. Additionally, it inhibits the reuptake of noradrenaline, increasing its levels and activating alpha-2 adrenergic receptors, further contributing to its analgesic effects. It also has weak serotonin reuptake inhibition, but this does not contribute to its analgesic action.
Pharmacodynamics
Tapentadol operates as an opioid agonist, leading to effects such as miosis, reduced gastrointestinal motility, and peripheral vasodilation. Respiratory depression is a significant concern, as it decreases the responsiveness of the brainstem respiratory centers to carbon dioxide and electrical stimulation. Tapentadol also has a potential for misuse and abuse, which can lead to a risk of overdose and death, particularly when combined with other central nervous system depressants.
Pharmacokinetics
Tapentadol is rapidly absorbed following oral administration, with peak plasma concentrations typically occurring within 1 to 3 hours. It undergoes extensive hepatic metabolism, primarily via glucuronidation. The elimination half-life ranges from 4 to 5 hours, and the drug is predominantly excreted through urine as metabolites. Caution is advised in patients with hepatic or renal impairment, as dose adjustments may be necessary.
Contra-indications
- Severe renal impairment
- Severe hepatic impairment
- Hypersensitivity to tapentadol or any excipients
Adverse effects
- Nausea
- Vomiting
- Constipation
- Dizziness
- Somnolence
- Fatigue
- Headache
- Anxiety
- Sexual dysfunction
- Cognitive impairment
- Visual impairment
- Seizures (in overdose)
- Mood changes
- Ureteral spasm
- Muscle rigidity
Interactions
- Drugs that cause serotonin syndrome (increased risk)
- CNS depressants (increased risk of respiratory depression)
- Monoamine oxidase inhibitors (MAOIs)
- Other opioids
Precautions
- Caution in patients with a history of substance use disorder
- Caution in patients with respiratory depression
- Caution in patients with head injury or increased intracranial pressure
- Avoid abrupt discontinuation in long-term users to prevent withdrawal symptoms
- Monitor for signs of misuse, abuse, and addiction
Pregnancy
Use only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects on fetal development.
Breast-feeding
Present in breast milk but not known to be harmful. Caution is advised.
Storage
Store below 25°C. Keep out of reach of children. Protect from light.
Formulations
- Immediate-release tablets (50 mg, 100 mg, 150 mg, 200 mg)
- Modified-release tablets (50 mg, 100 mg, 150 mg, 200 mg)
- Oral solution (tapentadol hydrochloride 25 mg/5 ml)
- Solution for injection (tapentadol hydrochloride 50 mg/1 ml)
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Tapentadol
PubChem CID 9838022Molecular formula: C14H23NO
Mechanism of action
Tapentadol is a centrally-acting synthetic analgesic. Although their clinical relevance is unclear, tapentadol is believed to have two main mechanisms of action. Tapentadol is a selective mu-opioid receptor (MOR) agonist: it binds to MOR with an affinity greater than or equal to ten-fold affinity compared to delta- and kappa-opioid receptors. Tapentadol also inhibits noradrenaline reuptake, thereby increasing noradrenaline levels and activating alpha-2 receptors to promote analgesia. Tapentadol is a weak serotonin reuptake inhibitor; however, this action does not contribute to its analgesic effect. Treatments for neuropathic pain are either not fully effective or have problematic side effects. Combinations of drugs are often used. Tapentadol is a newer molecule that produces analgesia in various pain models through two inhibitory mechanisms, namely central mu-opioid receptor (MOR) agonism and noradrenaline reuptake inhibition. These two components interact synergistically, resulting in levels of analgesia similar to opioid analgesics such as oxycodone and morphine, but with more tolerable side effects. The right central nucleus of the amygdala (CeA) is critical for the lateral spinal ascending pain pathway, regulates descending pain pathways and is key in the emotional-affective components of pain. Few studies have investigated the pharmacology of limbic brain areas in pain models. Here we determined the actions of systemic tapentadol on right CeA neurones of animals with neuropathy and which component of tapentadol contributes to its effect. Neuronal responses to multimodal peripheral stimulation of animals with spinal nerve ligation or sham surgery were recorded before and after two doses of tapentadol. After the higher dose of tapentadol either naloxone or yohimbine were administered. Systemic tapentadol resulted in dose-dependent decrease in right CeA neuronal activity only in neuropathy. Both naloxone and yohimbine reversed this effect to an extent that was modality selective. The interactions of the components of tapentadol are not limited to the synergy between the MOR and a2-adrenoceptors seen at spinal levels, but are seen at this supraspinal site where suppression of responses may relate to the ability of the drug to alter affective components of pain.
Pharmacodynamics
Tapentadol is an opioid agonist that exerts physiological effects commonly caused by the opioid drug class. These effects include miosis, reduced gastrointestinal motility, and peripheral vasodilation. Tapentadol produces respiratory depression by reducing the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide tension and electrical stimulation. Tapentadol has a high potential for misuse and abuse, which can lead to the development of substance use disorder. Abuse of tapentadol poses a risk of overdose and death, which increases with alcohol or other central nervous system depressants.
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
This drug in other countries
The same active ingredient registered across other registries we cover - including different brands.