Classifications: antibiotic; antituberculosis agent; Therapeutic: antibiotic; antituberculosis agent
Pregnancy Category: C
150 mg tablets
Rifamycin derivative similar to rifampin. Inhibits DNA-dependent RNA polymerase activity in susceptible bacterial cells,
thereby suppressing RNA synthesis. Inhibits the growth of Mycobacterium tuberculosis.
Effective against Mycobacterium tuberculosis, indicated by improvement in clinical S&S (e.g., fever, cough, pleuritic pain,
fatigue) and on chest x-ray.
Pulmonary tuberculosis in conjunction with at least one other antitubercular agent.
Hypersensitivity to any rifamycins (e.g., rifampin, rifabutin, rifapentine); porphyria; pregnancy (category C); lactation.
Patients with abnormal liver function tests or hepatic disease; older adults; HIV disease or concurrent use of protease
inhibitors. Safe use in children <12 y not established.
Route & Dosage
|Tuberculosis: Short-Course Therapy
Adult: PO 600 mg twice weekly (at least 72 h apart) x 2 mo, then 600 mg once weekly x 4 mo
- Give with an interval of NO LESS than 72 h between doses.
- Give with food to minimize GI upset.
- Store at 15°30° C (59°86° F) in a tightly closed container and protect from excess moisture.
Adverse Effects (≥1%)CNS:
Headache, dizziness. CV:
Increased liver function tests (ALT, AST), anorexia, nausea, vomiting, dyspepsia, diarrhea. GU: Hyperuricemia,
pyuria, proteinuria, hematuria, urinary casts. Hematologic:
Neutropenia, lymphopenia, anemia, leukopenia, thrombocytosis. Respiratory:
Rash, pruritus, acne
. Body as a Whole:
Decreased levels of indinavir
and possibly other protease inhibitors
; increased metabolism and decreased activity of oral contraceptives
, phenytoin, disopyramide, mexiletine, quinidine, tocainide, warfarin, fluconazole, itraconazole, ketoconazole, diazepam, beta blockers
, calcium channel blockers
, haloperidol, sulfonylureas
, cyclosporine, tacrolimus, levothyroxine, narcotic analgesics
, quinine, reverse transcriptase inhibitors
, tricyclic antidepressants
, sildenafil, theophylline.
Approximately 70% absorbed. Peak:
56 h. Distribution:
97.7% protein bound. Metabolism:
Hydrolyzed by esterase enzyme to active metabolite in liver; inducer of cytochromes P450 3A4 and 2C8/9. Elimination:
70% in feces, 17% in urine. Half-Life:
Assessment & Drug Effects
- Lab tests: Sputum smear and culture, CBC, baseline liver functions (especially serum transaminases) to rule out preexisting
hepatic disease and serum creatinine and BUN.
- Monitor carefully for S&S of toxicity with concurrent use of oral anticoagulants, digitalis preparations, or anticonvulsants.
Patient & Family Education
- Follow strict adherence to the prescribed dosing schedule to prevent emergence of resistant strains of tuberculosis.
- Be aware that food may be useful in preventing GI upset.
- Report immediately any of the following to the physician: fever, weakness, nausea or vomiting, loss of appetite, dark urine
or yellowing of eyes or skin, pain or swelling of the joints, severe or persistent diarrhea.
- Use or add barrier contraceptive if using hormonal contraception.