Tapentadol

Indications

Tapentadol is used for: Acute Moderate-to-Severe Pain, Musculoskeletal pain, Diabetic Peripheral Neuropathy

Adult Dose

Oral Moderate to severe acute pain Adult: Initially, 50 mg, 75 mg or 100 mg 4-6 hrly, depending on pain intensity. On day 1, a 2nd dose may be given 1 hr after the initial dose if pain relief is inadequate; subsequent dose may be given 4-6 hrly, adjust according to response. Max: 700 mg on day 1, 600 mg daily on subsequent days. Elderly: Initiate dosage at lower end of range Hepatic impairment Mild: Dosage adjustment not required Moderate: 50 mg q8hr initially; dosing frequency not to exceed 3 times daily; Severe: Not recommended

Child Dose

Safety and efficacy not established

Renal Dose

Renal impairment CrCl >30 mL/min : Dosage adjustment not required CrCl <30 mL/min: Not recommended

Administration

May be taken with or without food.

Contra Indications

Significant resp depression (in unmonitored settings or absence of resuscitative equipment), acute or severe bronchial asthma or hypercapnia, known or suspected paralytic ileus; acute intoxication w/ alcohol, hypnotics, centrally acting analgesics or psychotropic active substances. Concurrent or recent (w/in 2 wk) therapy w/ MAOIs.

Precautions

Patient w/ impaired resp function, head injury, brain tumours, biliary tract disease (including acute pancreatitis), history of seizure disorder. Avoid abrupt withdrawal. Moderate to severe hepatic impairment or severe renal impairment. Pregnancy and lactation.

Pregnancy-Lactation

Interactions

Potential severe adverse effects w/ MAOIs. CNS-active drugs; other serotonergic agents (including triptans, SSRIs, other SNRIs, lithium, sibutramine, fentanyl & its analogues, tramadol, dextromethorphan, tapentadol, meperidine, methadone, pentazocine or St. John's wort), drugs which impair serotonin (eg linezolid & methylene blue) or serotonin precursors (eg tryptophan supplements). Increased risk of QTc prolongation &/or ventricular arrhythmias w/ some antipsychotics & antibiotics. Decreased AUC & Cmax of indinavir. Increased AUC & Cmax of haloperidol. Increased plasma conc w/ ketoconazole. Increased plasma conc & reduced BP-lowering effect of metoprolol. Increased AUC of risperidone. Reduced metabolism w/ CYP2D6 inhibitors. Increased venlafaxine levels w/ CYP3A4 inhibitors.

Adverse Effects

Side effects of Tapentadol : >10% Nausea (30%),Dizziness (24%),Vomiting (18%),Somnolence (15%) 1-10% (selected) Constipation (8%),Pruritus (5%),Xerostomia (4%),Fatigue (3%),Hyperhidrosis (3%),Anorexia (2%),Dyspepsia (2%),Insomnia (2%)

Mechanism of Action

Mu-opioid agonist; inhibits ascending pain pathways, thus altering response to pain; produces analgesia, respiratory depression, and sedation; also inhibits reuptake of norepinephrine, which also affects ascending pain pathways.