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looking forward to [100/mm:<750/mm 3 in those> <1 year,> <500/mm 3 in those 1 2 years,> <75/mm 3 in those 2 6 years, or> <50/mm 3 in those 6 years of age. 72 The safety of discontinuing primary MAC prophylaxis in HIV-infected infants and children receiving potent antiretroviral therapy has not been extensively studied. 72 Primary Prevention of MAC in Adolescents with Advanced HIV Infection Oral 300 mg once daily. 72 Used alone or in conjunction with azithromycin. 72 USPHS/IDSA recommends initiation of primary prophylaxis against MAC if CD4 + T-cell count is> <50/mm 3 . 72 Primary MAC prophylaxis may be discontinued if there is immune recovery in response to antiretroviral therapy with an increase in CD4 + T-cell count to> 100/mm 3 sustained for 3 months. 72 Reinitiate prophylaxis if CD4 + T-cell count decreases to <50 100/mm 3 . 72 Prevention of MAC Recurrence (Secondary Prophylaxis) in HIV-infected Children Oral 5 mg/kg (up to 300 mg) once daily. 72 Used in conjunction with clarithromycin (or azithromycin) and ethambutol. 72 Secondary prophylaxis to prevent MAC recurrence in HIV-infected children usually continued for life. 72 The safety of discontinuing secondary MAC prophylaxis in children whose CD4 + T-cell count increases in response to antiretroviral therapy has not been studied. 72 Prevention of MAC Recurrence (Secondary Prophylaxis) in HIV-infected Adolescents Oral 300 mg once daily. 72 f Used in conjunction with clarithromycin (or azithromycin) and ethambutol. 72 f Secondary prophylaxis to prevent MAC recurrence usually continued for life in HIV-infected individuals. 72 f Consideration can be given to discontinuing secondary MAC prophylaxis after 12 months in those who remain asymptomatic with respect to MAC and have an increase in CD4 + T-cell count to> 100/mm 3 that has been sustained for 6 months. 72 f Reinitiate prophylaxis if CD4 + T-cell count decreases to <100/mm 3 . 72 f Treatment of Disseminated MAC in HIV-infected Infants and Children Oral 10 20 mg/kg (up to 300 mg) once daily recommended by CDC and others. g Used in conjunction with clarithromycin (or azithromycin) and ethambutol. g Treatment of Disseminated MAC in HIV-infected Adolescents Oral 300 mg once daily. 60 f Used in conjunction with clarithromycin (or azithromycin) and ethambutol. 60 f Tuberculosis Treatment of Active (Clinical) Tuberculosis Oral Children> <15 years of age or weighing 40 kg : 10 20 mg/kg (up to 300 mg) once daily or 2 or 3 times weekly. 67 g Adolescents 15 years of age: 5 mg/kg (up to 300 mg) once daily or 2 or 3 times weekly. 65 66 67 82 Latent Tuberculosis Infection (LTBI) Oral Adolescents: 300 mg once daily for 4 months. 72 Adults Mycobacterium avium Complex (MAC) Infections Primary Prevention in Adults with Advanced HIV Infection Oral 300 mg once daily. 1 60 72 Alternatively, 150 mg twice daily with food may be used in patients experiencing nausea, vomiting, or other GI upset. 1 Used alone 1 60 72 or in conjunction with azithromycin. 72 Primary prophylaxis against MAC should be initiated if CD4 + T-cell count is> <50/mm 3 . 72 Primary MAC prophylaxis may be discontinued if there is immune recovery in response to antiretroviral therapy and an increase in CD4 + T-cell count to> 100/mm 3 has been sustained for 3 months. 72 Reinitiate prophylaxis if CD4 + T-cell count decreases to <50 100/mm 3 . 72 Prevention of MAC Recurrence (Secondary Prophylaxis) in HIV-infected Adults Oral 300 mg once daily. 72 f Used in conjunction with clarithromycin (or azithromycin) and ethambutol. 72 f Secondary prophylaxis to prevent MAC recurrence usually continued for life in HIV-infected individuals. 72 f Consideration can be given to discontinuing secondary MAC prophylaxis after 12 months in those who remain asymptomatic with respect to MAC and have an increase in CD4 + T-cell count to> 100/mm 3 that has been sustained for 6 months. 72 f Reinitiate prophylaxis if CD4 + T-cell count decreases to <100/mm 3 . 72 f Initial Treatment of Pulmonary MAC Infections (Fibrocavitary or Severe Nodular/bronchiectatic Disease) Caused by Macrolide-susceptible Strains Oral 150 300 mg once daily in conjunction with ethambutol (15 mg/kg once daily) and either clarithromycin (0.5 1 g daily) or azithromycin (250 mg once daily) recommended by ATS and IDSA. 60 Continue until patient has been culture negative on treatment for 1 year. 60 Consideration can be given to including amikacin or streptomycin 3 times weekly during the first 2 3 months of treatment for extensive, especially fibrocavitary, disease or when previous therapy has failed. 60 Treatment of Disseminated MAC in HIV-infected and Other Adults Oral 300 mg once daily in conjunction with ethambutol (15 mg/kg once daily) in conjunction with either clarithromycin (500 mg twice daily) or azithromycin (500 mg once daily) recommended by ATS, CDC, and IDSA. 60 f Rifabutin dosages of 300 450 mg once daily have been used. 60 Dosage may need to be adjusted in HIV-infected patients depending on the drugs included in the antiretroviral regimen. 60 (See Specific Drugs under Interactions.) Tuberculosis Treatment of Active (Clinical) Tuberculosis Oral 5 mg/kg (up to 300 mg) once daily or 2 or 3 times weekly. 65 66 67 82 f o Latent Tuberculosis Infection (LTBI) Oral 5 mg/kg (up to 300 mg) once daily for 4 months. 72 73 Prescribing Limits Pediatric Patients Mycobacterium avium Complex (MAC) Infections Prevention of MAC Recurrence (Secondary Prophylaxis) in HIV-infected Children Oral Maximum 300 mg once daily. 72 Treatment of Disseminated MAC in HIV-infected Infants and Children Oral Maximum 300 mg once daily. g Tuberculosis Treatment of Active (Clinical) Tuberculosis in Children or Adolescents Oral Maximum 300 mg per dose in once-daily or 2- or 3-times weekly regimens. 65 66 67 82 g Adults Tuberculosis Treatment of Active (Clinical) Tuberculosis Oral Maximum 300 mg per dose in once-daily or 2- or 3-times weekly regimens. 65 66 67 82 f Special Populations Hepatic Impairment Dosage reductions may be needed in patients with severe hepatic impairment. 82 (See Hepatic Impairment under Cautions.) Renal Impairment Cl cr> <30 mL/minute: Reduce dose by 50%. 1 f To prevent inadequate dosage, some experts prefer to use usual dosage and monitor plasma rifabutin concentrations. f Mild to moderate renal impairment: Dosage adjustment not required. 1 82 Geriatric Patients Select dosage with caution. 1 Cautions for Rifabutin Contraindications Known hypersensitivity to rifabutin or other rifamycins (rifampin, rifapentine). 1 Warnings/Precautions Warnings Precautions Related to Treatment of MAC Infections Should not be used for prevention of MAC infection in patients with active TB. 1 If rifabutin monotherapy is used for prevention of MAC infection in patients with active TB, M. tuberculosis resistant to both rifabutin and rifampin may emerge. 1 There is no evidence that rifabutin is effective for prevention of M. tuberculosis infections. 1 Individuals requiring prophylaxis against M. tuberculosis (i.e., treatment of latent tuberculosis infection) and prophylaxis against MAC may receive isoniazid and rifabutin concomitantly. 1 HIV-infected individuals frequently have TB and may present with atypical or extrapulmonary findings. 1 The tuberculin skin test (TST) for diagnosis of TB may be nonreactive in such patients despite presence of active disease. 1 In addition to chest radiographs and sputum cultures, blood culture, urine culture, or biopsy of suspicious lymph nodes may be useful in the diagnosis of TB in HIV-infected individuals. 1 Any patient developing symptoms consistent with active TB while receiving rifabutin for MAC prophylaxis should be evaluated immediately so that those with active disease can be given an effective multiple-drug regimen for treatment of TB. 1 Precautions Related to Treatment of Tuberculosis Should not be used alone for the treatment of active TB; must be used in conjunction with other antituberculosis agents. 82 Clinical specimens for microscopic examination and mycobacterial cultures and in vitro susceptibility testing should be obtained prior to initiation of antituberculosis therapy and periodically during treatment to monitor therapeutic response. 82 The antituberculosis regimen should be modified as needed. 82 Patients with positive cultures after 4 months of treatment should be considered to have failed treatment (usually as the result of noncompliance or drug-resistant TB). 82 Compliance with the full course of antituberculosis therapy and all drugs included in the multiple-drug regimen is critical. 82 Missed doses increase the risk of treatment failure and increase the risk that M. tuberculosis will develop resistance to the antituberculosis regimen. 82 To ensure compliance, ATS, CDC, IDSA, and AAP recommend that directly observed (supervised) therapy (DOT) be used for treatment of active (clinical) TB and for treatment of LTBI whenever possible, especially when intermittent regimens are used, when the patient is immunocompromised or infected with HIV, or when drug-resistant M. tuberculosis is involved. 73 82 f g m o Sensitivity Reactions Dermatologic Reactions. Rash reported frequently. 1 2 23 General Precautions Discoloration of Body Tissues or Fluids Orange or yellow skin discoloration may occur. 1 27 30 Urine, feces, saliva, sputum, sweat, or tears may have a brown-orange coloration. 1 23 Soft contact lenses may become permanently stained. 1 Hematologic Effects Neutropenia reported frequently; thrombocytopenia reported rarely. 1 Consider monitoring hematologic status periodically during therapy. 1 Ocular Effects Uveitis, which may be unilateral or bilateral 27 30 31 32 and is characterized by pain, redness, and possible temporary or permanent loss of vision, 27 31 32 33 reported occasionally. 1 27 30 31 32 33 34 Corneal deposits were reported in some HIV-infected children who were receiving rifabutin as part of a multiple-drug regimen for MAC prophylaxis. 1 These were tiny, almost transparent, asymptomatic peripheral and central corneal deposits that did not impair vision. 1 If uveitis occurs, temporarily interrupt rifabutin therapy and obtain ophthalmic evaluation. 1 33 In mild cases, rifabutin can be reinstituted; if signs and symptoms of uveitis recur, discontinue immediately. 1 33 Permanent discontinuance may be necessary if uveitis is severe. 27 Musculoskeletal Effects Myalgia, arthralgia, myositis reported. 1 23 26 Specific Populations Pregnancy Category B. 1 ATS, CDC, and IDSA state that data are insufficient to recommend use of rifabutin in pregnant women. 82 Lactation Not known whether rifabutin is distributed into milk. 1 Discontinue nursing or the drug. 1 Pediatric Use Safety and efficacy for prophylaxis of MAC infection in children have not been established. 1 Has been used for primary or secondary prophylaxis of MAC infections in HIV-infected children . 72 Has been used in a limited number of children (concomitantly with other antimycobacterial agents) for the treatment of MAC infection . 1 g Adverse effects reported in children (e.g., leukopenia, neutropenia, rash) are similar to those observed in adults. 1 In addition, corneal deposits were reported in some children. 1 (See Ocular Effects under Cautions.) Geriatric Use Insufficient experience in patients 65 years of age to determine whether geriatric patients respond differently than younger adults. 1 Select dosage with caution, starting at the low end of the dosage range, because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy. 1 Hepatic Impairment Use close clinical and laboratory monitoring when used in patients with hepatic impairment. 82 Dosage reduction may be needed in severe impairment. 82 Renal Impairment Dosage adjustment recommended in patients with substantial renal impairment. 1 (See Renal Impairment under Dosage and Administration.) Common Adverse Effects Rash, GI effects (abdominal pain, nausea, vomiting, diarrhea, dyspepsia, eructation, taste perversion), neutropenia, headache, discolored urine. 1 23 Interactions for Rifabutin Metabolized by CYP3A. 1 Induces CYP3A; induces hepatic enzymes to a lesser extent than rifampin. 1 81 Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes Pharmacokinetic interactions likely with drugs that are inhibitors, inducers, or substrates of CYP3A with possible alteration of the metabolism of rifabutin and/or other drug. 1 Specific Drugs Drug Interaction Comments Antifungals, azoles Fluconazole: Increased rifabutin concentrations and AUC; no change in fluconazole pharmacokinetics; 1 increased incidence of uveitis if high rifabutin dosage used 1 Itraconazole: Decreased itraconazole concentrations and AUC; possible loss of antifungal effects 1 Posaconazole: Decreased posaconazole concentrations and AUC; increased rifabutin concentrations and AUC; j k possible increased risk of rifabutin-associated adverse effects j Fluconazole: Monitor patients receiving rifabutin concomitantly with fluconazole 1 Posaconazole: Avoid concomitant use of rifabutin and posaconazole unless benefits outweigh risks; j k if concomitant use considered necessary, monitor frequently for adverse effects associated with rifabutin (e.g., uveitis, leukopenia) j k Atazanavir Increased concentrations and AUC of rifabutin and rifabutin metabolite 80 81 Reduce rifabutin dosage up to 75% of usually recommended dosage (i.e., use 150 mg every other day or 3 times weekly) 80 81 Co-trimoxazole Decreased AUC of co-trimoxazole; no change in rifabutin pharmacokinetics 1 Dapsone Decreased dapsone AUC 1 Darunavir Increased rifabutin concentrations; decreased darunavir concentrations i Reduce rifabutin dosage to 150 mg once every other day i 81 Delavirdine Decreased delavirdine concentrations and AUC; increased rifabutin concentrations and AUC 1 81 Concomitant use not recommended 1 81 Didanosine Pharmacokinetic interaction unlikely 1 Efavirenz Decreased rifabutin concentrations; no change in efavirenz AUC 81 Increase rifabutin dosage to 450 600 mg once daily or 600 mg 3 times weekly; efavirenz dosage adjustment not needed 81 Erlotinib Possible decreased erlotinib AUC h Avoid concomitant use if possible h Estrogens/Progestins Hormonal contraceptives: Decreased concentrations of estrogen and/or progestin; decreased efficacy of the hormonal contraceptive 1 Use nonhormonal methods of contraception 1 Ethambutol Pharmacokinetic interaction unlikely 1 Fosamprenavir Studies using amprenavir indicate slightly decreased amprenavir AUC and increased rifabutin concentrations and AUC d Rifabutin 150 mg every other day with ritonavir-boosted fosamprenavir: slightly increased amprenavir concentrations d If fosamprenavir used without ritonavir, reduce rifabutin dosage by at least 50% of usually recommended dosage (i.e., use 150 once daily or 300 mg 3 times weekly) 81 d If ritonavir-boosted fosamprenavir used, reduce rifabutin dosage by at least 75% of the usual dosage of 300 mg daily (i.e., maximum dosage of 150 mg every other day or 3 times weekly) 81 d Monitor for neutropenia by performing weekly CBC and as clinically indicated d Indinavir Increased rifabutin AUC; decreased indinavir AUC 1 61 Reduce rifabutin dosage by 50%; 1 use rifabutin 150 mg once daily or 300 mg 3 times weekly and increase indinavir dosage to 1 g every 8 hours 61 81 If ritonavir-boosted indinavir used, reduce rifabutin dosage to 150 mg once every other day or 3 times weekly and use usual boosted dosage of indinavir 81 Isoniazid Pharmacokinetic interaction unlikely 1 Lopinavir Fixed combination of lopinavir and ritonavir: Increased concentrations of rifabutin and rifabutin metabolite 48 81 Reduce rifabutin dosage by at least 75% (maximum dosage of 150 mg every other day or 3 times weekly) and use usual dosage of fixed combination of lopinavir and ritonavir; 48 81 further rifabutin dosage reductions may be necessary 48 Monitor closely for adverse effects 48 Macrolides Clarithromycin: Increased rifabutin AUC; decreased clarithromycin AUC; 1 increased incidence of uveitis if high rifabutin dosage used 33 Clarithromycin: Monitor patients receiving rifabutin and clarithromycin; 1 decreased rifabutin dosage of 150 mg daily may be necessary 60 Maraviroc Potential induction of maraviroc metabolism 81 Maraviroc dosage may need adjustment; monitor virologic response 81 Methadone Pharmacokinetic interaction unlikely 1 Nelfinavir Increased rifabutin concentrations and AUC; decreased nelfinavir concentrations and AUC 1 62 81 Reduce rifabutin dosage by 50%; 1 use nelfinavir 1.25 mg twice daily with rifabutin 150 mg once daily or 300 mg 3 times weekly 62 81 Nevirapine Increased rifabutin concentrations (high interindividual variability, some patients may experience large increases in rifabutin exposure); 76 decreased nevirapine concentrations 76 81 Caution advised; monitor for rifabutin toxicity; 76 dosage adjustment not needed if HIV PIs are not included in the regimen 81 Raltegravir Possible decreased raltegravir concentrations 81 If used with rifabutin, consider possibility of pharmacokinetic interaction if optimal virologic response is not achieved 81 Ritonavir Increased rifabutin concentrations and AUC; 1 81 possible increased incidence of uveitis 1 Reduce rifabutin dosage to 150 mg once every other day or 3 times weekly and use usual ritonavir dosage; further rifabutin dosage reduction may be needed 63 81 Manufacturer of rifabutin states concomitant use not recommended 1 Saquinavir Decreased saquinavir AUC 1 81 Rifabutin should not be used in patients receiving unboosted saquinavir; 81 in patients receiving ritonavir-boosted saquinavir, a rifabutin dosage of 150 mg once every other day or 3 times weekly is recommended 81 Theophylline Pharmacokinetic interaction unlikely 1 Tipranavir Increased rifabutin concentrations; 81 l no change in tipranavir concentrations l Reduce rifabutin dosage by 75% (i.e., use 150 mg once every other day or 3 times weekly); 81 l further rifabutin dosage reduction may be needed l Monitor closely for adverse effects l Zidovudine Slightly decreased concentrations and AUC of zidovudine; no change in rifabutin pharmacokinetics 1 38 39 Rifabutin Pharmacokinetics Absorption Bioavailability Readily absorbed from GI tract; peak plasma concentrations achieved within 2 4 hours. 1 Absolute bioavailability in HIV-positive patients was 20%. 1 Food High-fat meal slows the rate but not the extent of absorption. 1 Special Populations Compared with patients who have Cl cr 61 74 mL/minute, AUC is 71% higher in those with Cl cr> <30 mL/minute and 41% higher in those with Cl cr 30 61 mL/minute. 1 (See Renal Impairment under Dosage and Administration.) Steady-state pharmacokinetics more variable in geriatric individuals> 70 years of age than in younger adults. 1 Distribution Extent Widely distributed. 1 Intracellular concentrations higher than plasma concentrations; concentrations in lung tissue higher than plasma concentrations. 1 Distributed into CNS when meninges are inflamed. 82 Plasma Protein Binding 85%. 1 Special Populations Plasma protein binding not influenced by hepatic or renal impairment. 1 Elimination Metabolism Metabolized by CYP3A. 1 Metabolized to 5 metabolites; 1 metabolite has antimicrobial activity equal to that of rifabutin. 1 Elimination Route Excreted in urine (53%) principally as metabolites and excreted in feces (30%). 1 Removal by hemodialysis unlikely. 1 Half-life 45 hours (range: 16 69 hours). 1 Stability Storage Oral Capsules 25 C (may be exposed to 15 30 C); tight container. 1 Actions and Spectrum A spiropiperidyl rifamycin structurally and pharmacologically similar to other rifamycins (rifampin, rifapentine). 2 3 4 5 6 7 8 16 Inhibits DNA-dependent RNA polymerases in susceptible Escherichia coli and Bacillus subtilis . 1 Not known whether rifabutin inhibits DNA-dependent RNA polymerases in M. avium complex (MAC). 1 Mycobacterium : Active in vitro and in clinical infections against M. avium complex (MAC) and M. tuberculosis . 1 2 4 6 7 8 9 10 11 12 13 14 Active in vitro against M. gordonae , 1 60 M. haemophilum , 60 M. kansasii , 1 60 and M. marinum . 1 60 q Has some activity against M. leprae . 1 15 Spectrum of activity against gram-positive and gram-negative bacteria similar to that of rifampin. 2 16 Cross-resistance occurs between rifabutin and other rifamycins (rifampin, rifapentine). 1 82 M. tuberculosis resistant to rifampin usually are resistant to both rifabutin and rifapentine; only rarely are rifampin-resistant strains susceptible to rifabutin. 82 Advice to Patients Advise patients that poor compliance with antituberculosis regimens can result in treatment failure and development of drug-resistant TB, which can be life-threatening and lead to other serious health risks. 82 Importance of completing full course of therapy; importance of not missing any doses. 1 Advise patient of the signs and symptoms of MAC infections and TB; importance of consulting clinician if new symptoms consistent with either disease occur. 1 Possibility of uveitis; importance of consulting clinician if signs or symptoms of an inflammatory ocular condition occur (e.g., eye pain, redness, loss of vision). 1 Possibility of arthralgias or myositis; importance of consulting clinician if signs or symptoms of these disorders occur (e.g., joint stiffness, swelling, tenderness, paresthesia). 1 Advise patient that rifabutin may impart a brown-orange color to urine, feces, saliva, sputum, sweat, tears, and skin. 1 23 Soft contact lenses may become permanently stained. 1 Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, as well as any concomitant illnesses. 1 Advise that reliability of systemic hormonal contraceptives may be affected; alternative contraceptives should be considered. 1 Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. 1 Importance of informing patients of other important precautionary information. 1 (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Rifabutin Routes Dosage Forms Strengths Brand Names Manufacturer Oral Capsules 150 mg Mycobutin Pfizer AHFS DI Essentials. Copyright 2017, Selected Revisions January 1, 2008. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. Use is not currently included in the labeling approved by the US Food and Drug Administration. References 1. Pfizer. Mycobutin (rifabutin) capsules USP prescribing information. New York, NY; 2006 Feb. 2. O Brien RJ, Lyle MA, Snider DE Jr. Rifabutin (ansamycin LM 427): a new rifamycin-S derivative for the treatment of mycobacterial diseases. Rev Infect Dis . 1987; 9:519-30. [PubMed 3037676] 3. Farr BM, Mandell GL. Rifamycins. In: Mandell GL, Douglas RG Jr, Bennett JE, eds. Principles and practice of infectious diseases. 3rd ed. New York: Churchill Livingstone Inc; 1991:295- 303. 4. Dickinson JM, Mitchison DA. In vitro activity of new rifamycins against rifampicin-resistant M. tuberculosis and MAIS-complex mycobacteria. Tubercle . 1987; 68:177- 82. [PubMed 2834842] 5. Ungheri D, Della Bruna C, Sanfilippo A. Studies on the mechanism of action of the spiropiperidylrifamycin LM 427 on rifampicin-resistant M. tuberculosis . Drugs Exp Clin Res . 1984; 10:681-9. 6. Heifets LB, Iseman MD, Lindholm-Levy PJ. Bacteriostatic and bactericidal effects of rifabutine? (ansamycin LM427) on Mycobacterium avium clinical isolates. In: Casal M, ed. Mycobacteria of clinical interest. Amsterdam: Elsevier Science Publishers; 1986:180-3. 7. Heifets LB, Iseman MD. Determination of in vitro susceptibility of mycobacteria to ansamycin. Am Rev Respir Dis . 1985; 132:710-1. [PubMed 3929660] 8. Woodley CL, Kilburn JO. In vitro susceptibility of Mycobacterium avium complex and Mycobacterium tuberculosis strains to a spiro-piperidyl rifamycin. Am Rev Respir Dis . 1982; 126:586-7. [PubMed 6289711] 9. Masur H. Effect of combined clofazimine and ansamycin therapy on Mycobacterium avium Mycobacterium intracellulare bacteremia in patients with AIDS. J Infect Dis . 1987; 155:127-9. [PubMed 3794396] 10. Perumal VK, Nguyen KC, Iseman M et al. Dynamic and in vivo chemotherapeutic activities of ansamycin on Mycobacterium avium-intracellulare . Am Rev Respir Dis . 1984; 129(Suppl 4 Part 2):186. 11. Adria Laboratories. Rifabutin clinical protocol. 1990 Jan 20. 12. Saito H, Sato K, Tomioka H. Comparative in vitro and in vivo activity of rifabutin and rifampicin against Mycobacterium avium complex. Tubercle . 1988; 69:187-92. [PubMed 2855458] 13. Klemens SP, Cynamon MH. In vivo activities of newer rifamycin analogs against Mycobacterium avium infection. Antimicrob Agents Chemother . 1991; 35:2026- 30. [PubMed 1662021] 14. Orme IM. Antimycobacterial activity in vivo of LM427 (rifabutin). Am Rev Respir Dis . 1988; 138:1254-7. [PubMed 2849349] 15. Franzblau SG. In vitro activities of aminoglycosides, lincosamides, and rifamycins against Mycobacterium leprae . Antimicrob Agents Chemother . 1992; 35:1232-4. 16. Sanfilippo A, Della Bruna C, Marsili L et al. Biological activity of a new class of rifamycins. J Antibiot . (Tokyo). 1980; 33:1193-8. 17. Food and Drug Administration. Orphan designations pursuant to Section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act (P.L. 97-414), to June 28, 1996. Rockville, MD; 1996 Jul. 18. Gordin F, Nightingale S, Wynne B et al. Rifabutin monotherapy prevents or delays Mycobacterium avium complex (MAC) bacteremia in patients with AIDS. Int Conf AIDS . Jul 19-24, 1992. Abstract No. PoB 3081. 19. Cameron W, Sparti P, Pietroski N et al. Rifabutin therapy for the prevention of M. avium complex (MAC) bacteremia in patients with AIDS and CD4 less than or equal to 200. Int Conf AIDS . Jul 19-24, 1992. Abstract No. WeB 1055. 20. Council of State and Territorial Epidemiologists; AIDS Program, Center for Infectious Diseases. Revision of CDC surveillance case definition for acquired immunodeficiency syndrome. MMWR Morb Mortal Wkly Rep . 1987; 36(Suppl 1S):1-15S. [PubMed 3099157] 21. Horsburgh CR, Wynne B, Bianchine J et al. Epidemiology of Mycobacterium avium complex (MAC) bacteremia in patients enrolled in a placebo controlled study. Int Conf AIDS . Jul 19-24, 1992. Abstract No. PoB 3109. 22. Narang PK, Lewis RC, Bianchine JR. Rifabutin absorption in humans: relative bioavailability and food effect. Clin Pharmacol Ther . 1992; 52:335-41. [PubMed 1330396] 23. Nightingale SD, Cameron DW, Gordin FM et al. Two controlled trials of rifabutin prophylaxis against Mycobacterium avium complex infection in AIDS. N Engl J Med . 1993; 329:828-33. [PubMed 8179648] 24. Masur H, Public Health Service Task Force on Prophylaxis and Therapy for Mycobacterium Avium Complex. Recommendations on prophylaxis and therapy for disseminated Mycobacterium avium complex disease in patients infected with the human immunodeficiency virus. N Engl J Med . 1993; 329:898-904. [PubMed 8395019] 25. Brogden RN, Fitton A. Rifabutin: a review of its antimicrobial activity, pharmacokinetic properties and therapeutic efficacy. Drugs . 1994; 47:983-1009. [PubMed 7521834] 26. Bourget-Letarte H, Dugas A, Sahai J et al. Clinical tolerance of daily oral rifabutin, an investigational antimycobacterial drug, in AIDS patients. Int Conf AIDS . Jul 19-24, 1992. Abstract No. PoB 3146. 27. Siegal FP, Eilbott D, Burger H et al. Dose-limiting toxicity of rifabutin in AIDS-related complex: syndrome of arthralgia/arthritis. AIDS . 1990; 4:433-41. [PubMed 2164820] 28. Morris JT, Kelly JW. Rifabutin-induced ageusia. Ann Intern Med . 1993; 119:171-2. [PubMed 8390142] 29. McBride MO, Coker RJ, Horner PJ et al. Diarrhoea associated with Clostridium difficile in AIDS patients receiving rifabutin. Lancet . 1994; 343:417. [PubMed 7905569] 30. Shafran SD, Deschnes J, Miller M et al. Uveitis and pseudojaundice during a regimen of clarithromycin, rifabutin, and ethambutol. N Engl J Med . 1994; 330:438-9. [PubMed 8284019] 31. Frank MO, Graham MB, Wispelway B. Rifabutin and uveitis. N Engl J Med . 1994; 330:868. [PubMed 8114854] 32. Fuller JD, Stanfield LED, Craven DE. Rifabutin prophylaxis and uveitis. N Engl J Med . 1994; 330:1315-6. [PubMed 8145794] 33. Centers for Disease Control and Prevention. Uveitis associated with rifabutin therapy. MMWR Morb Mortal Wkly Rep . 1994; 43:658. [PubMed 8072478] 34. Giacchino R, Tasso L, Losurdo G et al. Safety of rifabutin in a three-month-old infant. Pediatr Infect Dis J . 1994; 13:164. [PubMed 8190549] 35. US Public Health Service Task Force on Prophylaxis and Therapy for Mycobacterium avium Complex. Recommendations on prophylaxis and therapy for disseminated Mycobacterium avium complex for adults and adolescents infected with human immunodeficiency virus. MMWR Recomm Rep . 1993; 42(RR-9):14-20. [PubMed 8393134] 36. Anon. Updated guidelines for the use of rifabutin or rifampin for the treatment and prevention of tuberculosis among HIV-infected patients taking protease inhibitors or nonnucleoside reverse transcriptase inhibitors. MMWR Morb Mortal Wkly Rep . 2000; 49:185-9. [PubMed 11795500] 37. GlaxoSmithKline. Agenerase (amprenavir) capsules prescribing information. Research Triangle Park, NC; 2002 Oct 38. Gallicano K, Sahai J, Swick L et al. Effect of rifabutin on the pharmacokinetics of zidovudine in patients infected with human immunodeficiency virus. Clin Infect Dis . 1995; 21:1008-11. [PubMed 8645788] 39. Li RC, Nightingale S, Lewis RC et al. Lack of effect of concomitant zidovudine on rifabutin kinetics in patients with AIDS-related complex. Antimicrob Agents Chemother . 1996; 40:1397-1402. [PubMed 8726008] 40. Sahai J, Narang PK, Hawley-Foss N et al. A phase I evaluation of concomitant rifabutin and didanosine in symptomatic HIV-infected patients. J Acquir Immune Defic Syndr Hum Retrovirol . 1995; 9:274-9. [PubMed 7788425] 41. Reviewers comments (personal observations) on Antituberculosis Agents General Statement 8:16.04. 42. Abbott. Biaxin (clarithromycin) Filmtab tablets and granules for oral suspension prescribing information. North Chicago, IL; 1996 Apr. 43. Horsburgh CR Jr. Advances in the prevention and treatment of Mycobacterium avium disease. N Engl J Med . 1996; 335:428-30. [PubMed 8663875] 44. Havlir DV, Dube MP, Sattler FR et al. Prophylaxis against disseminated Mycobacterium avium complex with weekly azithromycin, daily rifabutin, or both. N Engl J Med . 1996; 335:392-8. [PubMed 8676932] 45. Moore RD, Chaisson RE. Survival analysis of two controlled trials of rifabutin prophylaxis against Mycobacterium avium complex in AIDS. AIDS . 1995; 9:1337-42. [PubMed 8605053] 46. Pfizer. Zithromax (azithromycin) capsules, tablets, and oral suspension) prescribing information. New York, NY; 1996 Jun. 47. Horsburgh CR Jr. Advances in the prevention and treatment of Mycobacterium avium disease. N Engl J Med . 1996; 335:428-30. [PubMed 8663875] 48. Abbott Laboratories. Kaletra (lopinavir/ritonavir) oral tablets and solution prescribing information. North Chicago, IL; 2007 Jan. 49. Havlir DV, Dube MP, Sattler FR et al. Prophylaxis against disseminated Mycobacterium avium complex with weekly azithromycin, daily rifabutin, or both. N Engl J Med . 1996; 335:392-8. [PubMed 8676932] 50. Pierce M, Crampton S, Henry D et al. A randomized trial of clarithromycin as prophylaxis against disseminated Mycobacterium avium complex infection in patients with advanced acquired immunodeficiency syndrome. N Engl J Med . 1996; 335:384-91. [PubMed 8663871] 51. Sun E, Heath-Chiozzi M, Cameron DW et al. Concurrent ritonavir and rifabutin increase risk of rifabutin-associated adverse event. Presented at the XI International Conference on AIDS. Vancouver, BC, July 8, 1996. Abstract B171. 52. The Indinavir (MK 639) Pharmacokinetic Study Group. Indinavir (MK 629) drug interaction studies. Presented at the XI International Conference on AIDS. Vancouver, BC, July 8, 1996. 53. Griffith DE, Brown BA, Girard WM et al. Adverse events associated with high-dose rifabutin in macrolide-containing regimens for the treatment of M. avium complex definitely


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