Tapentadol is FDA approved for the treatment of moderate to severe acute pain. Due to the dual mechanism of action as an opioid agonist and norepinephrine reuptake inhibitor, there is potential for off-label use in chronic pain.
Tapentadol is a new molecular entity that is structurally similar to tramadol. Tapentadol is a centrally-acting analgesic with a dual-mode of action as an agonist at the mu-opioid receptor and as a norepinephrine reuptake inhibitor. These two actions are synergistic in pain relief. While its action reflects aspects of tramadol and morphine, its ability to control pain is more on the order of hydrocodone and oxycodone.
Its dual mode of action provides analgesia at similar levels of more potent narcotic analgesics such as hydrocodone, oxycodone, and meperidine with a more tolerable side effect profile. Clinical studies showed that tapentadol effectively relieves moderate to severe pain in various pain care settings
What should I discuss with my healthcare provider before taking tapentadol?
You should not use this medication if you are allergic to tapentadol, or if you have:
- severe asthma or breathing problems; or
- a blockage in your digestive tract (stomach or intestines).
Do not use tapentadol if you have taken an MAO inhibitor in the past 14 days. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, and tranylcypromine.
Tell your doctor if you have ever had:
- breathing problems, sleep apnea;
- a head injury, brain tumor, or seizures;
- drug or alcohol addiction, or mental illness;
- urination problems;
- liver or kidney disease; or
- problems with your gallbladder, pancreas, or thyroid.
If you use opioid medicine while you are pregnant, your baby could become dependent on the drug. This can cause life-threatening withdrawal symptoms in the baby after it is born. Babies born dependent on opioids may need medical treatment for several weeks.
You should not breast-feed while using this medicine.
Do not give tapentadol to a child.
How should I take tapentadol?
Take tapentadol exactly as prescribed by your doctor. Follow the directions on your prescription label and read all medication guides. Never use tapentadol in larger amounts, or for longer than prescribed. Tell your doctor if you feel an increased urge to take more of tapentadol.
Never share opioid medicine with another person, especially someone with a history of drug addiction. MISUSE CAN CAUSE ADDICTION, OVERDOSE, OR DEATH. Keep the medicine where others cannot get to it. Selling or giving away this medicine is against the law.
Stop taking all other medications that contain tapentadol or tramadol when you start taking tapentadol extended-release tablets.
Take tapentadol with a full glass of water at the same times each day, with or without food.
Do not crush, break, or open an extended-release pill. Swallow it whole to avoid exposure to a potentially fatal dose.
Tapentadol can cause constipation. Talk to your doctor before using a laxative or stool softener to treat or prevent this side effect.
Never crush a pill to inhale the powder or inject it into your vein. This could result in death.
You may have withdrawal symptoms if you stop using tapentadol suddenly. Ask your doctor before stopping the medicine.
Store at room temperature away from moisture and heat. Keep track of your medicine. You should be aware if anyone is using it improperly or without a prescription.
Do not keep leftover opioid medication. Just one dose can cause death in someone using this medicine accidentally or improperly. Ask your pharmacist where to locate a drug take-back disposal program. If there is no take-back program, flush the unused medicine down the toilet.
Usual Adult Dose for Pain:
Individualize therapy taking into consideration severity of pain, response to therapy, prior analgesic treatment experience, and risk factors for addiction, abuse, and misuse:
Initial dose: 50 to 100 mg orally every 4 to 6 hours as needed for pain
-Day 1: A second dose may be administered as soon as 1 hour after the first dose if needed
-Subsequent dosing: 50, 75, or 100 mg orally every 4 to 6 hours; adjust dosing to maintain adequate analgesia with acceptable tolerability
Maximum dose: 700 mg on day 1; 600 mg/day on subsequent days