Tapentadol Contraindications, Pregnancy Category

Tapentadol is a centrally acting opioid analgesic of the benzenoid class with a dual mode of action as an agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor (NRI). Analgesia occurs within 32 minutes of oral administration and lasts for 4–6 hours.

It is similar to tramadol in its dual mechanism of action; namely, its ability to activate the mu opioid receptor and inhibit the reuptake of norepinephrine. Unlike tramadol, it has only weak effects on the reuptake of serotonin and is a significantly more potent opioid with no known active metabolites. Tapentadol is not a pro-drug and therefore does not rely on metabolism to produce its therapeutic effects; this makes it a useful moderate-potency analgesic option for patients who do not respond adequately to more commonly used opioids due to genetic disposition poor metabolizers of, as well as providing a more consistent dosage-response range among the patient population.

Tramadol has been found to possess the following actions

• Agonist of the μ-opioid receptor (MOR) and to a far lesser extent of the δ-opioid receptor (DOR) and κ-opioid receptor (KOR)
• Serotonin reuptake inhibitor (SRI) and norepinephrine reuptake inhibitor (NRI); hence, an SNRI
• Serotonin 5-HT_2C receptor antagonist
• M₁ and M₃ muscarinic acetylcholine receptor antagonist
• α7 nicotinic acetylcholine receptor antagonist
• NMDA receptor antagonist (very weak)
• TRPA1 inhibitor

Tapentadol Indications

• Cervical spondylosis
• Fibromyalgia
• Radiating pain due to nerve compression
• Demyelinating nerve pain
• Headache
• Lumbago
• Low back pain
• PLID
• Osteoarthritis
• Chest pain
• Ankylosing spondylitis
• Acute pain due to trauma
• Accidental pain due to a road traffic accident
• Acute abdominal pain due to gastritis/appendicitis
• Pain due to the especially musculoskeletal system
• Polyarthralgia
• Muscles stiffness in nerve diseases
• Morning stiffness
• Multiple joint pain
• Muscles stiffness in the spinal cord
• Pain caused by nonarticular rheumatism
• Periarthritis of scapulohumerals
• The immediate-release formulation of tapentadol is indicated for the relief of moderate to severe acute pain. The long-acting formulation serves as a continuous, around-the-clock analgesic that is indicated for the relief of moderate to severe chronic pain or neuropathic pain associated with diabetic peripheral neuropathy.

Therapeutic Uses of Tapentadol 

Tapentadol Contraindications

Tapentadol is contraindicated in those with hypersensitivity,

• Allergy to tapentadol  or any other ingredients in the medicine;
• Allergy to medicines called opioid antagonists (e.g. codeine, morphine);
• Consumed alcohol or taken another drug which affects your brain. These include:
• Some painkillers, including opioid pain killers;
• Hypnotic drugs;
• Psychotropic drugs;
• Used monoamine oxidase inhibitors (MAOIs) such as phenelzine  or tranylcypromine  in the past 14 days;
• Epilepsy;
• History of peptic ulcer disease,
• Gastrointestinal bleeding,
• Alcohol intolerance,
• Renal impairment,
• Angioedema, and asthma
• Acute intoxication with alcohol,
• Hypnotics,
• Opioids,
• Psychotropic medicinal products,
• Heart failure,
• Coagulation disorders,
• Renal impairment,
• Hepatic impairment.

Dosage of Tapentadol

Strengths: 50 mg, 75 mg, or 100 mg

Pain

Immediate release

• 50 mg, 75 mg, or 100 mg orally every 4 to 6 hours depending upon pain intensity, with or without food.
• On the first day of dosing, the second dose may be administered as soon as one hour after the first dose, if adequate pain relief is not attained with the first dose. Subsequent dosing is 50 mg, 75 mg, or 100 mg every 4 to 6 hours and should be adjusted to maintain adequate analgesia with acceptable tolerability. Daily doses greater than 700 mg on the first day of therapy and 600 mg on subsequent days have not been studied and are, therefore, not recommended.

Extended-release

• Initial: 50 mg twice daily (recommended interval: 12 hours); titrate in increments of 50 mg no more frequently than twice daily every 3 days to the effective dose (therapeutic range: 100 to 250 mg twice daily) (maximum dose: 500 mg/day)
• Initial: 50 mg titrated to an effective dose; titrate in increments of 50 mg no more frequently than twice daily every 3 days (therapeutic range: 100 to 250 mg twice daily) (maximum dose: 500 mg/day). Note: No adequate data on converting patients from other opioids to tapentadol extended release.
• Conversion from immediate release to extended release: Convert using same total daily dose but divide into two equal doses and administer twice daily (recommended interval: 12 hours) (maximum dose: 500 mg/day).

Side effects of Tapentadol

Drug Interactions of Tapentadol

Tapentadol may interact with following drugs, supplements & may change the efficacy of drugs

• anti-emetic medications (serotonin antagonists; e.g., granisetron, ondansetron)
• antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
• antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
• aminoglycoside antibiotics (e.g., amikacin, gentamicin, tobramycin)
• angiotensin-converting enzyme inhibitors (ACEIs; e.g., captopril, enalapril, ramipril)
• angiotensin receptor blockers (ARBs; e.g., candesartan, irbesartan, losartan)
• beta-adrenergic blockers (e.g., metoprolol, atenolol)
• baclofen
• barbiturates (e.g., butalbital, phenobarbital)
• benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
• calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
• celecoxib
• cilostazol
• clopidogrel
• corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
• cyclosporine
• diuretics (water pills; e.g., furosemide, hydrochlorothiazide, )
• 5-ASA medications (e.g. sulfasalazine)
• glucosamine
• haloperidol
• heparin
• methotrexate
• multivitamins
• other non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, ketorolac, naproxen)
• Omega-3 fatty acids
• phenytoin
• phenobarbital
• pentoxifylline
• quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
• selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine,fluoxetine, paroxetine, sertraline)
• serotonin/norepinephrine reuptake inhibitors (SNRIs; e.gduloxetine, )
• tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)

Pregnancy & Lactation of Tapentadol

 FDA Pregnancy Category C

Pregnancy

This medication should not be used during pregnancy, prior to or during labor. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

It is not known if tapentadol passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding.