ACTIVE INGREDIENT: Tramadol HCl 100mg, 200mg, 300mg; ext-rel tabs.

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INDICATION: Moderate to moderately severe chronic pain when around-the-clock treatment for an extended time is needed.

PHARMACOLOGY: Tramadol is a morphine (mu-) opioid agonist that also inhibits the reuptake of serotonin and norepinephrine. Ryzolt is a once-daily formulation of tramadol that has both immediate-release and extended-release characteristics. The tablets provide a continuous release of tramadol over 24 hours. Both the parent drug and a metabolite (M1) whose formation is dependent on the CYP2D6 enzyme have been shown to be active moieties. The activity profiles of the parent drug differ from those of this metabolite, soboth polymorphism (individual variations in the activity of the enzyme) and concomitant drug therapy may alter the effects of the drug. The impact of these changes on the safety and efficacy is not known.

CLINICAL TRIALS: The efficacy of this product was demonstrated in a double-blind, placebo-controlled randomized withdrawal design study. Patients who experienced a reduction in pain and who tolerated Ryzolt during an open-label titration period were randomized to Ryzolt or placebo for 12 weeks. Following a washout period, patients randomized to Ryzolt were titrated to either 200mg/day or 300mg/day and maintained on that dose for 12 weeks. Patients given Ryzolt had a greater improvement in pain intensity at the end of the treatment period compared to those randomized to placebo.

ADULTS: Swallow whole. Take once daily (allow 24 hours in between doses). Not currently on tramadol: 100mg once daily; may increase every 2–3 days by 100mg/day. Usual range: 200–300mg/day. Currently on immediate-release tramadol: Switch to ext-rel at same daily dose or rounded down to nearest 100mg increment. Max 300mg/day.Withdraw gradually.

CHILDREN: <16yrs: not recommended.

CONTRAINDICATIONS: Significant respiratory depression, acute or severe bronchial asthma, or hypercapnia in unmonitored settings or without resuscitative equipment.

PRECAUTIONS: Do not give to opioid-dependent patients. Respiratory depression. Increased intracranial pressure. Head injury. Seizure disorders. Suicidal ideation. Acute abdomen. Hepatic or severe renal impairment (CrCl<30mL/min): not recommended. Drug abusers. Avoid abrupt cessation. Elderly (esp. >75yrs). Labor & delivery, pregnancy (Cat.C), nursing mothers: not recommended.

INTERACTIONS: Concomitant other forms of tramadol. Do not take with MAOIs, alcohol, carbamazepine. Potentiated by alcohol, other CNS depressants (reduce dose). Increased risk of seizures and/or serotonin syndrome with SSRIs, SNRIs, tricyclics, cyclobenzaprine, promethazine, opioids, MAOIs, naloxone, triptans, linezolid, lithium, neuroleptics, others that lower seizure threshold. May be affected by CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, amitriptyline) or CYP3A4 inhibitors (eg, ketoconazole, erythromycin)or inducers (eg, rifampin, St. John’s wort). Monitor digoxin, warfarin.

ADVERSE REACTIONS: GI upset, constipation, dizziness, drowsiness, anorexia, sweating, dry mouth, vertigo, insomnia; anaphylaxis.

HOW SUPPLIED: Tabs—30, 90

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