Tramadol Hydrochloride / Acetaminophen

Pronunciation

Pronunciation: TRAM-a-dol HYE-droe-KLOR-ide/a-SEET-a-MIN-oh-fen
Class: Nonnarcotic analgesic combination

Trade Names

Ultracet
- Tablets acetaminophen 325 mg/tramadol 37.5 mg

Tramacet (Canada)

Pharmacology

Acetaminophen

Inhibits prostaglandin in CNS and reduces fever through direct action on hypothalamic heat-regulating center.

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Tramadol

Exact mechanism is unknown; however, it binds to certain opioid receptors and inhibits reuptake of norepinephrine and serotonin.

Indications and Usage

Short-term (5 days or less) management of acute pain.

Contraindications

Any situation in which opioids are contraindicated, including acute intoxication with any of the following: alcohol, centrally acting analgesics, hypnotics, narcotics, opioids, or psychotropic drugs; hypersensitivity to any component of the product or opioids.

Dosage and Administration

Adults

PO 2 tablets (tramadol 37.5 mg/acetaminophen 325 mg per tablet) every 4 to 6 h as needed for pain relief (max, 8 tablets/day).

Renal function impairment

In patients with CrCl less than 30 mL/min, it is recommended that the dosing interval be increased not to exceed 2 tablets every 12 h.

General Advice

  • For oral use only.
  • Do not exceed recommended dosage.
  • Should be taken without regard to food; instruct patient to take with food if GI upset occurs.

Storage/Stability

Store between 59° and 86°F.

Drug Interactions

Alcohol

Should not be used concomitantly with alcohol.

CNS depressants (eg, anesthetic agents, narcotics, opioids, phenothiazines, sedative-hypnotics, tranquilizers)

Use with caution and in reduced doses.

Cyclobenzapride, 5HT 1 agonists (eg, sumatriptan), linezolid, lithium, MAOIs (eg, isocarboxazid), neuroleptics (eg, carbamazepine), promethazine, SNRIs (eg, duloxetine), SSRIs (eg, fluoxetine), St. John's wort, tricyclic antidepressants (TCAs) (eg, amitriptyline), triptans (eg, sumatriptan)

Use with caution because of increased risk of adverse effects, including seizures and serotonin syndrome. Concomitant use with carbamazepine is not recommended.

CYP3A4 inhibitors (eg, erythromycin, ketoconazole), CYP2D6 inhibitors (eg, amitriptyline, fluoxetine, paroxetine, quinidine)

Plasma concentrations of tramadol may be increased, increasing the risk for serious adverse reactions (eg, seizures).

Digoxin

Digoxin toxicity has been reported rarely in postmarketing surveillance.

Warfarin

Anticoagulant effect of warfarin may be altered; increased monitoring of INR may be needed.

Laboratory Test Interactions

Acetaminophen may cause more than a 20% decrease in mean glucose as measured with Chemstrip bG home blood glucose system.

Adverse Reactions

Cardiovascular

Arrhythmia, hypertension, hypotension, palpitation, tachycardia.

CNS

Somnolence (6%); anorexia, dizziness (3%); insomnia (2%); anxiety, asthenia, confusion, euphoria, fatigue, headache, nervousness, tremor (at least 1%); convulsions, hallucination, paroniria.

Dermatologic

Increased sweating (4%); pruritus (2%); rash (at least 1%).

GI

Constipation (6%); diarrhea, nausea (3%); dry mouth (2%); abdominal pain, dyspepsia, flatulence, vomiting (at least 1%).

Genitourinary

Prostatic disorder (2%); albuminuria, impotence, oliguria, urinary retention.

Miscellaneous

Hot flushes (at least 1%); abnormal hepatic function, allergic reactions, anemia, dyspnea.

Precautions

Warnings

This product contains acetaminophen. Acetaminophen has been associated with cases of acute liver failure, at times resulting in liver transplant and death. Most of the cases of liver injury are associated with the use of acetaminophen at doses that exceed 4,000 milligrams per day, and often involve more than one acetaminophen-containing product.


Pregnancy

Category C .

Lactation

Excreted. Use is not recommended.

Children

Safety and efficacy have not been established.

Elderly

Use with caution, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease and multiple drug therapy.

Renal Function

Renal impairment results in decreased rate and extent of excretion of tramadol and its active metabolite. Adjust dosage in patients with CrCl less than 30 mL/min.

Hepatic Function

Use is not recommended in patients with hepatic impairment.

Abdominal conditions

Assessment of patients with acute abdominal conditions may be more difficult.

Acetaminophen- or tramadol-containing products

Do not use concurrently with other acetaminophen- or tramadol-containing products because of increased risk of hepatotoxicity.

Anaphylactoid reactions

Serious and rarely fatal anaphylactoid reactions may occur.

Dependence

Morphine-type psychic and physical dependence may occur with tramadol.

Head injury

Use with caution in patients with increased intracranial pressure or head injury.

Respiratory depression

Use with caution in patients at risk of respiratory depression.

Seizures

Seizures may occur with doses within or above the recommended dosage range. The risk of seizures may be increased in patients with epilepsy; history of seizures; risk of seizures (eg, head trauma); metabolic disorders; alcohol and drug withdrawal; CNS infections; and concomitant use of SSRIs, TCAs, other tricyclic compounds, other opioids, MAOIs, neuroleptics, and/or other drugs that reduce the seizure threshold.

Serotonin syndrome

Potentially life-threatening serotonin syndrome may develop, particularly when combined with serotonergic agents (eg, MAOIs, SNRIs, SSRIs, TCAs, triptans).

Suicide risk

Do not use in patients who are suicidal or prone to addiction.

Withdrawal

Symptoms (eg, anxiety, insomnia, pain, sweating, rigors, tremors) may occur if this drug is discontinued abruptly.

Overdosage

Symptoms

Acetaminophen

Anorexia, coagulation defects, diaphoresis, hepatic centrilobular necrosis (leading to hepatic failure and death), hypoglycemia, malaise, nausea, pallor, renal tubular necrosis, vomiting.

Tramadol

Bradycardia, cardiac arrest, cold and clammy skin, constricted pupils, death, hypotension, respiratory depression, seizures, skeletal muscle flaccidity, somnolence progressing to stupor or coma.

Patient Information

  • Advise patient to take without regard to meals, but to take with food if GI upset occurs.
  • Caution patient to not take more tablets than prescribed or more frequently than prescribed. Serious toxicity may develop if the prescribed dose is exceeded or doses are taken too close together.
  • Advise patients that medication is for short-term (5 days or less) use only and if symptoms persist to contact their health care provider regarding other therapies for pain control.
  • Instruct patient to avoid taking acetaminophen, other acetaminophen-containing products, tramadol, or other tramadol-containing products.
  • Instruct patient to avoid alcoholic beverages and other depressants while taking this medication.
  • Advise patient that drug may impair judgment, thinking, or motor skills or cause dizziness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
  • Inform patients that medication may cause seizures and/or serotonin syndrome with concomitant use of serotonergic agents (including SNRIs, SSRIs, and triptans) or drugs that significantly reduce the metabolic Cl of tramadol.

Copyright © 2009 Wolters Kluwer Health.

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