tapentadol

medtigo

tapentadol

Brand Name :

Nucynta, Nucynta ER

Synonyms :

tapentadol

Class :

Opioid analgesics

Action and Spectrum

Mechanism of action

Mu-opioid agonists are a class of drugs that bind to mu-opioid receptors in the body. They treat pain by inhibiting the ascending pain pathways in the body, which alters the body’s response to pain. These drugs can produce analgesia, respiratory depression, and sedation. They also inhibit the reuptake of norepinephrine, which further affects the ascending pain pathways. Examples of mu-opioid agonists include morphine, fentanyl, and oxycodone.

Spectrum

It is a centrally acting analgesic drug that has a unique mechanism of action. It is a dual-acting drug that acts as a mu-opioid receptor agonist and a norepinephrine reuptake inhibitor (NRI). The mu-opioid receptor agonist activity relieves pain by inhibiting the ascending pain pathways. In contrast, the NRI activity enhances the pain-relieving effects of the mu-opioid receptor agonist by increasing the levels of norepinephrine in the brain.

This dual mechanism of action results in a broad spectrum of activity for tapentadol, making it practical for treating acute and chronic pain. It is used to treat moderate to severe pain, including pain from osteoarthritis, lower back pain, and postoperative pain. It is available as an oral tablet and an extended-release oral tablet.

Dosing & Uses

Drug Interaction

Adverse Reaction

Frequency defined:

>10%

Dizziness

Somnolence

Nausea

vomiting

1-10%

Pruritis

Fatigue

Anorexia

Insomnia

Constipation

Xerostomia

Hyperhidrosis

Dyspepsia

Post-marketing reports

Angioedema

Headache

Palpitations

Panic attack

Diarrhea

Black Box Warning

Black box warning

The FDA issued a black box warning for tapentadol in 2013 regarding the risk of severe respiratory depression, which can be fatal, particularly when the drug is combined with other medications that also cause respiratory depression, such as sedatives, anxiolytics, and other opioids.
The warning also highlights the risk of accidental overdose and death, particularly in patients with impaired consciousness or sleep apnea.
It is important to note that tapentadol is a potent opioid analgesic and should be used with caution in patients with a history of substance abuse or addiction and those with respiratory problems or sleep apnea.
It is recommended that patients be informed of the risk of respiratory depression and potentially fatal outcomes. They should be closely monitored when taking the drug, particularly when starting treatment and when the dose is increased.

Contraindication / Caution

Contraindications

Hypersensitivity to tapentadol or any of its components
Severe respiratory depression or severe chronic obstructive pulmonary disease (COPD)
Acute or severe bronchial asthma
Known or suspected gastrointestinal obstruction
Head injury, intracranial pressure, or raised intracranial pressure
Patients who have a history of opioid abuse or dependence
Patients treated with monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuing treatment with MAOIs
Pregnancy and breastfeeding, as the safety of tapentadol during pregnancy and breastfeeding has not been established

Caution

Respiratory depression: It can cause respiratory depression, mainly when used in combination with other medications that also cause respiratory depression, such as sedatives, anxiolytics, and other opioids. Patients should be closely monitored for respiratory depression, especially when starting treatment and increasing the dose.
Risk of addiction, abuse, and misuse: It is a potent opioid analgesic and has a risk of addiction, abuse, and misuse. It should be used with caution in patients with a history of substance abuse or addiction and those with respiratory problems or sleep apnea.
Gastrointestinal effects: It may cause constipation, nausea, vomiting, and other gastrointestinal effects. Patients should be advised to drink fluids and eat a diet high in fiber to help prevent constipation.
Risk of overdose: It has a risk of accidental overdose and death, particularly in patients with impaired consciousness or sleep apnea. Patients should be informed of the risk of overdose and potentially fatal outcomes.
CNS effects: It may cause drowsiness, dizziness, and other effects. Patients should be advised to avoid driving or operating heavy machinery until they know how the drug affects them.
Seizures: It may increase the risk of seizures. Patients should be advised to avoid tapentadol if they have a history of convulsive disorders or epilepsy

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available

Lactation: Excretion of the drug in human breast milk is known

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology

The mu-opioid receptor agonist activity of tapentadol provides pain relief by inhibiting the ascending pain pathways in the spinal cord and brain, reducing pain perception. This activity is similar to other opioid analgesics, such as morphine and fentanyl.

The NRI activity of tapentadol enhances the pain-relieving effects of the mu-opioid receptor agonist activity by increasing the levels of norepinephrine in the brain. Norepinephrine is a neurotransmitter that helps to modulate pain perception. It can also have a positive effect on mood, which may also contribute to the overall effectiveness of tapentadol in treating pain

Pharmacodynamics

It is a centrally-acting analgesic drug that belongs to the class of opioid agonists. It acts on the mu-opioid receptor and the norepinephrine reuptake inhibitor (NRI) to produce its analgesic effect. The drug’s dual mechanism of action provides a balance between pain relief and reduced risk of side effects such as respiratory depression, compared to traditional opioid analgesics. It is indicated for the management of moderate to severe pain. It is available in both immediate-release and extended-release formulations

Pharmacokinetics

Absorption: 

It is well absorbed from the gastrointestinal tract with peak plasma concentrations occurring within 2-3 hours of oral administration. The bioavailability of the immediate-release formulation is about 50-60%

Distribution: 

It is highly protein bound (about 99%) and has a volume of distribution of about 3 L/kg

Metabolism: 

It is metabolized primarily by the liver, primarily via the cytochrome P450 (CYP) enzyme, CYP2D6. The main metabolite is O-desmethyltapentadol (ODT), which is also an active compound

Elimination/Excretion: 

tapentadol and its metabolites are primarily excreted in the urine, with a small portion excreted in the feces. The elimination half-life of the drug is about 3-4 hours

Adminstartion

Administration

It is available in immediate and extended-release formulations and can be administered orally. The immediate-release tablet can be taken with or without food, while the extended-release tablet should be taken with food.
The usual starting dose for adults for moderate to severe pain is an immediate-release tablet: 50-100 mg every 4-6 hours as needed, or the extended-release tablet: Once daily, starting with 50-100mg and titrated up to a maximum of 250mg per day.
The dose should be adjusted based on the patient’s response and tolerance to the medication. The maximum recommended daily dose for adults is 600 mg for immediate release and 500mg for extended release.
It’s important to note that tapentadol should be used only in patients for whom alternative treatment options are ineffective, not tolerated, or would be inadequate to provide sufficient pain management. And not to exceed the recommended maximum daily dose

Patient Information Leaflet

Patient information leaflet

Generic Name: tapentadol

Pronounced: (ta-PEN-ta-dol)

Why do we use tapentadol?

It is a centrally-acting analgesic drug that is used for the management of moderate to severe pain. It is approved for use in adults for the management of acute and chronic pain, including:

Acute pain: It is indicated for managing acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.
Chronic pain: It is indicated for managing chronic pain in adults who require around-the-clock pain treatment for an extended period.
Neuropathic pain: It is also indicated for the management of neuropathic pain associated with diabetic peripheral neuropathy or postherpetic neuralgia

tapentadol

No data available for drug.

DRUG INTERACTION

tapentadol

&

tapentadol +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

tapentadol

No data available for drug.

DRUG INTERACTION

tapentadol

&

tapentadol +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

tapentadol

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology

Adminstartion

Patient Information Leaflet