PHARMACOLOGIC CLASS: Opioid
ACTIVE INGREDIENT: Tapentadol 50mg, 75mg, 100mg tabs.
INDICATION: Moderate to severe acute pain in patients ≥18 years of age.
PHARMACOLOGY: Tapentadol is a centrally-acting synthetic analgesic. Although its mechanism of action is unknown, analgesic efficacy is thought to be due to mu-opioid agonist activity and the inhibition of norepinephrine reuptake.
CLINICAL TRIALS: Two randomized, double-blind, placebo- and active-controlled studies were conducted to evaluate the efficacy and safety of tapentadol in the treatment of moderate to severe acute pain from first metatarsal bunionectomy and end-stage degenerative joint disease.
In the bunionectomy study, patients 18 to 80 years of age with moderate to severe pain following unilateral, first metatarsal bunionectomy surgery were given tapentadol 50mg, 75mg, 100mg, or placebo every 4 to 6 hours for 72 hours. The proportion of patients who showed reduction in pain intensity at 48 hours of 30% or greater, or 50% or greater were significantly higher inpatients treated with tapentadol at each dose versus placebo.
In the end-stage degenerative joint disease study, patients 18 to 80 years of age with moderate to severe pain from end stage degenerative joint disease of the hip or knee were given tapentadol 50mg, 75mg, or placebo every 4 to 6 hours for 10 days. The proportion of patients who showed reductions in pain intensity at 5 days of 30% or greater, or 50% or greater were significantlyhigher in patients treated with tapentadol at each dose versus placebo.
ADULTS: ≥18 years: 50–100mg every 4–6 hours depending upon pain intensity. First day of dosing: may give second dose one hour after first dose if adequate pain relief not attained with first dose; subsequent doses should be given every 4–6 hours. Max 700mg/day on the first day, 600mg/day on subsequent days. Moderate hepatic impairment: initially 50mg every 8 hours; max 3 doses/24 hours.
CHILDREN: <18 years: not recommended.
CONTRAINDICATIONS: Significant respiratory depression, acute or severe asthma or hypercapnia (in unmonitored settings or in the absence of resuscitative equipment). Paralytic ileus. During or within 14 days of MAOIs. Precautions: Severe renal or hepatic impairment: not recommended. Asthma. COPD. Cor pulmonale. Severe obesity. Sleep apnea syndrome. Myxedema. Kyphoscoliosis. CNS depression. Coma. Head injury. Increased intracranial pressure. Seizure disorders. Biliary tract disease. Acute pancreatitis. Drugabusers. Avoid abrupt cessation. Elderly. Debilitated. Pregnancy (Cat.C). Labor & delivery, nursing mothers: not recommended.
INTERACTIONS: See Contraindications. Additive CNS depression with other CNS depressants (eg, general anesthetics, phenothiazines, sedatives, hypnotics, alcohol); consider reducing dose. Serotonin syndrome possible with concomitant SSRIs, SNRIs, tricyclics, MAOIs, triptans, other drugs that impair metabolism of serotonin.
ADVERSE REACTIONS: GI upset, dizziness, somnolence; respiratory, CNS depression.
HOW SUPPLIED: Tabs—100
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