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Atazanavir Sulfate

Class: HIV Protease Inhibitors
VA Class: AM800
Chemical Name: (3S,8S,9S,12S) - 3,12 - Bis(1,1 - dimethylethyl) - 8 - hydroxy - 4,11 - dioxo - 9 - (phenylmethyl) - 6 - {[4 - (2 - pyridinyl)phenyl]methyl{ - 2,5,6,10,13 - pentaazatetradecanedioic acid dimethyl ester, sulfate (1:1)
Molecular Formula: C₃₈H₅₂N₆O₇•H₂SO₄
CAS Number: 22997597-7
Brands: Reyataz

Introduction

Antiretroviral; HIV protease inhibitor (PI).¹

Uses for Atazanavir Sulfate

Treatment of HIV Infection

Treatment of HIV-1 infection in conjunction with other antiretrovirals.¹ ² ³ ⁴ ⁷ ¹⁴ ²⁰⁰ ²⁰¹

Usually used in conjunction with low-dose ritonavir (ritonavir-boosted atazanavir) in PI-based regimens that include a PI and 2 nucleoside reverse transcriptase inhibitors (NRTIs).¹ ²⁰⁰ ²⁰¹

For initial treatment in HIV-infected adults and adolescents, some experts state that ritonavir-boosted atazanavir is a preferred PI for use in PI-based regimens in conjunction with 2 NRTIs.²⁰⁰

For initial treatment in HIV-infected children, some experts state that ritonavir-boosted atazanavir in conjunction with 2 NRTIs is a preferred PI-based regimen in those ≥6 years of age.²⁰¹

Atazanavir (without low-dose ritonavir) can be used in adults and adolescents ≥13 years of age who cannot tolerate ritonavir,¹ ²⁰⁰ ²⁰¹ but should not be used in antiretroviral-experienced (previously treated) patients with prior virologic failure.¹

Postexposure Prophylaxis of HIV

Postexposure prophylaxis of HIV infection† in health-care workers and others exposed occupationally via percutaneous injury or mucous membrane or nonintact skin contact with blood, tissues, or other body fluids associated with a risk for transmission of the virus.¹⁸ Used in conjunction with other antiretrovirals.¹⁸

Postexposure prophylaxis of HIV infection† in individuals who have had nonoccupational exposure to blood, genital secretions, or other potentially infectious body fluids of a person known to be infected with HIV when that exposure represents a substantial risk for HIV transmission.¹⁷ Used in conjunction with other antiretrovirals.¹⁷

Atazanavir Sulfate Dosage and Administration

Administration

Oral Administration

Administer orally once daily with food.¹ ²⁰⁰

Usually administered with low-dose ritonavir (ritonavir-boosted atazanavir);¹ ²⁰⁰ ²⁰¹ may be used without low-dose ritonavir in adults and adolescents ≥13 years of age unable to tolerate ritonavir.¹ ²⁰⁰ ²⁰¹

If used with a histamine H₂-receptor antagonist in antiretroviral-naive or antiretroviral-experienced adults, administer ritonavir-boosted atazanavir simultaneously with, and/or at least 10 hours after, the histamine H₂-receptor antagonist.¹ (See Specific Drugs under Interactions.)

If used with a histamine H₂-receptor antagonist in antiretroviral-naive adults unable to tolerate ritonavir, administer atazanavir at least 2 hours before and 10 hours after the histamine H₂-receptor antagonist.¹ (See Specific Drugs under Interactions.)

If used with a proton-pump inhibitor in antiretroviral-naive adults, administer proton-pump inhibitor approximately 12 hours before ritonavir-boosted atazanavir.¹ (See Specific Drugs under Interactions.)

Dosage

Available as atazanavir sulfate;¹ dosage expressed in terms of atazanavir.¹

Must be given in conjunction with other antiretrovirals.¹ ²⁰⁰ If used with efavirenz, ritonavir, or tenofovir, dosage adjustment may be necessary.¹ ²⁰⁰ If used with didanosine, administer at separate times.¹ ²⁰⁰ (See Specific Drugs under Interactions.)

Pediatric Patients

Treatment of HIV Infection

Antiretroviral-naive Children

Oral

Dosage of Ritonavir-boosted Atazanavir for Antiretroviral-naive Pediatric Patients 6 Years to <18 Years of Age1
Body Weight	Atazanavir Dosage	Ritonavir Dosage
15 to <25 kg	150 mg once daily	80 mg once daily
25 to <32 kg	200 mg once daily	100 mg once daily
32 to <39 kg	250 mg once daily	100 mg once daily
≥39 kg	300 mg once daily	100 mg once daily

Adolescents ≥13 years of age who weigh ≥39 kg and are unable to tolerate ritonavir: Recommended dosage of atazanavir (without low-dose ritonavir) is 400 mg once daily.¹

Antiretroviral-experienced Children

Oral

Dosage of Ritonavir-boosted Atazanavir for Antiretroviral-experienced Pediatric Patients 6 Years to <18 Years of Age1
Body Weight	Atazanavir Dosage	Ritonavir Dosage
25 to <32 kg	200 mg once daily	100 mg once daily
32 to <39 kg	250 mg once daily	100 mg once daily
≥39 kg	300 mg once daily	100 mg once daily

Adults

Treatment of HIV Infection

Antiretroviral-naive Adults

Oral

300 mg once daily boosted with low-dose ritonavir (100 mg once daily).¹ For adults unable to tolerate ritonavir, recommended dosage of atazanavir (without low-dose ritonavir) is 400 mg once daily.¹

If tenofovir is included in the regimen, use 300 mg of atazanavir once daily boosted with low-dose ritonavir (100 mg once daily).¹

If efavirenz is included in the regimen, use 400 mg of atazanavir once daily boosted with low-dose ritonavir (100 mg once daily).¹

If a histamine H₂-receptor antagonist or proton-pump inhibitor is given concomitantly, use 300 mg of atazanavir once daily boosted with low-dose ritonavir (100 mg once daily).¹ (See Specific Drugs under Interactions.)

If a histamine H₂-receptor antagonist is given concomitantly and patient cannot tolerate ritonavir, use 400 mg of atazanavir once daily.¹ (See Specific Drugs under Interactions.)

Antiretroviral-experienced Adults

Oral

300 mg once daily boosted with low-dose ritonavir (100 mg once daily).¹

If a histamine H₂-receptor antagonist is given concomitantly, use 300 mg of atazanavir once daily boosted with low-dose ritonavir (100 mg once daily).¹ (See Specific Drugs under Interactions.)

If tenofovir is included in the regimen and a histamine H₂-receptor antagonist is given concomitantly, use 400 mg of atazanavir once daily boosted with low-dose ritonavir (100 mg once daily).¹ (See Specific Drugs under Interactions.)

Dosage recommendations not established for use with efavirenz in antiretroviral-experienced adults.¹

Postexposure Prophylaxis of HIV†

Occupational Exposure†

Oral

400 mg once daily.¹⁸ If tenofovir included in the regimen, use 300 mg of atazanavir once daily boosted with low-dose ritonavir (100 mg once daily).¹⁸

Initiate postexposure prophylaxis as soon as possible following exposure (within hours rather than days) and continue for 4 weeks, if tolerated.¹⁸

Nonoccupational Exposure†

Oral

400 mg once daily.¹⁷ If tenofovir included in the regimen, use 300 mg of atazanavir once daily boosted with low-dose ritonavir.¹⁷

Initiate postexposure prophylaxis as soon as possible following exposure (preferably ≤72 hours after exposure) and continue for 28 days.¹⁷

Prescribing Limits

Pediatric Patients

Treatment of HIV Infection

Oral

300 mg once daily boosted with low-dose ritonavir (100 mg once daily).¹

Special Populations

Hepatic Impairment

Oral

Patients with moderate hepatic impairment (Child-Pugh class B) without prior virologic failure: Consider reduced dosage of 300 mg once daily (without ritonavir).¹ ²⁰⁰ Do not use in those with severe hepatic impairment (Child-Pugh class C).¹

Ritonavir-boosted atazanavir not recommended in patients with hepatic impairment.¹

Renal Impairment

Oral

Patients with renal impairment, including those with severe renal impairment not undergoing hemodialysis: Dosage adjustments not needed.¹ ²⁰⁰

Antiretroviral-naive patients with end-stage renal disease undergoing hemodialysis: 300 mg once daily boosted with low-dose ritonavir (100 mg once daily).¹ ²⁰⁰

Antiretroviral-experienced patients with end-stage renal disease undergoing hemodialysis: Atazanavir (with or without low-dose ritonavir) not recommended.¹ ²⁰⁰

Geriatric Patients

Dosage adjustments based solely on age not required in patients ≥65 years of age.¹

Pregnant and Postpartum Women

300 mg once daily boosted with low-dose ritonavir (100 mg once daily).¹ Do not use atazanavir without low-dose ritonavir.¹ Monitor closely for adverse effects, especially during first 2 months after delivery.¹ (See Pregnancy under Cautions.)

Antiretroviral-experienced pregnant women in second or third trimester also receiving either a histamine H₂-receptor antagonist or tenofovir: Increase atazanavir dosage to 400 mg once daily boosted with ritonavir (100 mg once daily).¹ Dosage recommendations not available for antiretroviral-experienced pregnant women receiving both a histamine H₂-receptor antagonist and tenofovir.¹

Cautions for Atazanavir Sulfate

Contraindications

History of clinically important hypersensitivity reaction (e.g., Stevens-Johnson syndrome, erythema multiforme, toxic skin eruptions) to atazanavir or any ingredient in the formulation.¹
Concomitant use with drugs highly dependent on CYP3A or uridine diphosphate-glucuronosyltransferase (UGT) 1A1 for metabolism and for which elevated plasma concentrations are associated with serious and/or life-threatening events or possible loss of virologic response (e.g., alfuzosin, cisapride, ergot alkaloids, indinavir, irinotecan, lovastatin, oral midazolam, pimozide, rifampin, sildenafil used for treatment of pulmonary arterial hypertension [PAH], simvastatin, St. John’s wort [Hypericum perforatum], triazolam).¹ (See Specific Drugs under Interactions.)

Warnings/Precautions

Interactions

Concomitant use with certain drugs is contraindicated or requires particular caution.¹ (See Specific Drugs under Interactions.)

When ritonavir-boosted atazanavir is used, the usual cautions, precautions, and contraindications associated with ritonavir should be considered.¹

Cardiovascular Effects

Abnormalities in AV conduction (including prolongation of PR interval) reported.¹ Cardiac conduction abnormalities generally are asymptomatic and limited to first-degree AV block.¹

Use with caution in patients with preexisting cardiac conduction abnormalities (e.g., marked first-degree AV block; second- or third-degree AV block) because of lack of clinical experience.¹

Caution advised if used with other drugs that prolong PR interval (e.g., some β-adrenergic blocking agents, some calcium-channel blocking agents, digoxin, fixed combination of lopinavir and ritonavir [lopinavir/ritonavir]).¹ ²⁰⁷ (See Specific Drugs under Interactions.)

Sensitivity Reactions

Dermatologic Reactions

Rash (generally mild to moderate maculopapular eruptions) reported frequently.¹ Median time to onset is 7.3 weeks; median duration is 1.4 weeks.¹ Stevens-Johnson syndrome, erythema multiforme, and toxic skin eruptions reported.¹

Discontinue atazanavir in patients who develop severe rash.¹

Hyperbilirubinemia

Reversible, asymptomatic elevations in indirect (unconjugated) bilirubin occur in most patients since atazanavir is a competitive inhibitor of UGT 1A1 (an enzyme that catalyzes the glucuronidation of bilirubin).¹

Total bilirubin concentrations ≥2.6 times ULN reported in 35–49% of patients; long-term safety data not available for patients with persistent elevations in total bilirubin >5 times ULN.¹

If increases in serum AST and/or ALT occur with hyperbilirubinemia, evaluate for etiologies other than hyperbilirubinemia.¹

If jaundice or scleral icterus resulting from elevated bilirubin causes cosmetic concerns, alternative antiretroviral therapy can be considered; reduction of atazanavir dosage not recommended since efficacy data not available.¹

Hyperbilirubinemia reported in pregnant women receiving atazanavir.¹ Neonates exposed in utero also at risk; monitor for severe hyperbilirubinemia during first few days of life.¹

Nephrolithiasis

Nephrolithiasis reported in postmarketing surveillance.¹ If nephrolithiasis occurs, temporarily interrupt or discontinue atazanavir.¹

Hyperglycemic and Diabetogenic Effects

Hyperglycemia, new-onset diabetes mellitus, or exacerbation of preexisting diabetes mellitus reported with PIs; diabetic ketoacidosis has occurred.¹

Immune Reconstitution Syndrome

During initial treatment, patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium complex [MAC], M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jiroveci [formerly P. carinii]); this may necessitate further evaluation and treatment.¹

Adipogenic Effects

Possible redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement (“buffalo hump”), peripheral wasting, facial wasting, breast enlargement, and general cushingoid appearance.¹

Hemophilia A and B

Spontaneous bleeding noted with PIs; causal relationship not established.¹

Caution in patients with a history of hemophilia type A or B.¹ Increased hemostatic (e.g., antihemophilic factor) therapy may be needed.¹

HIV Resistance

Possibility of HIV-1 resistant to atazanavir.¹ ⁹ ¹¹

Varying degrees of cross-resistance occur among the various PIs.¹ Resistance to atazanavir may not preclude subsequent use of other PIs.¹

Specific Populations

Pregnancy

Category B.¹

Antiretroviral Pregnancy Registry at 800-258-4263 or .¹ ²⁰²

In pregnant or postpartum women, administer only as ritonavir-boosted atazanavir.¹ ²⁰² Use in pregnant women only if clearly needed and when HIV-1 is susceptible to atazanavir.¹ Some experts state that ritonavir-boosted atazanavir is an alternative PI (not preferred PI) for use in pregnant women.²⁰² Dosage adjustments may be necessary.¹ (See Pregnant and Postpartum Women under Dosage.)

Limited data suggest atazanavir does not elevate risk of major birth defects.¹

Lactic acidosis, sometimes fatal, and symptomatic hyperlactatemia reported in pregnant women receiving atazanavir in conjunction with NRTIs.¹

Hyperbilirubinemia reported in pregnant women receiving ritonavir-boosted atazanavir.¹ Bilirubin concentrations ≥4 mg/dL reported within 24 hours of birth in some neonates born to women who received the drug during pregnancy.¹ Monitor neonates exposed to atazanavir in utero for development of severe hyperbilirubinemia during first few days of life.¹

Monitor postpartum women closely for adverse effects during first 2 months after delivery; atazanavir concentrations and AUC may be increased during postpartum period.¹ (See Special Populations under Pharmacokinetics: Absorption.)

Lactation

Distributed into milk in low concentrations.²⁰² (See Distribution under Pharmacokinetics.)

Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.¹ ²⁰⁰

Pediatric Use

Should not be used in neonates and infants <3 months of age because of risk of kernicterus.¹ Closely monitor any infant exposed to the drug in utero.¹ (See Pregnancy under Warnings/Precautions.)

Safety, efficacy, and pharmacokinetic profile not established in children 3 months to <6 years of age.¹

Adverse effects in children 6–18 years of age similar to those reported in adults.¹

Geriatric Use

Insufficient experience in those ≥65 years of age to determine whether they respond differently than younger adults.¹

Use with caution and monitor because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.¹

Hepatic Impairment

Principally metabolized and eliminated by the liver; increased plasma atazanavir concentrations expected in patients with moderate to severe hepatic impairment.¹

Use with caution in those with mild to moderate hepatic impairment.¹ Consider dosage adjustments in those with moderate hepatic impairment (Child-Pugh class B).¹ (See Hepatic Impairment under Dosage and Administration.)

Do not use in those with severe hepatic impairment (Child-Pugh class C).¹

Those with HBV or HCV infection and those with marked increases in AST or ALT prior to atazanavir therapy may be at increased risk for further elevations in hepatic enzymes or for hepatic decompensation.¹ Perform liver function testing prior to and periodically during atazanavir therapy in such individuals.¹

Ritonavir-boosted atazanavir not recommended in those with hepatic impairment.¹

Renal Impairment

Plasma concentrations in individuals with severe renal impairment not undergoing dialysis generally are similar to those in individuals with normal renal function.¹ Dosage adjustment not needed.¹

Atazanavir boosted with low-dose ritonavir can be used in antiretroviral-naive patients with end-stage renal disease who are undergoing hemodialysis.¹

Do not use atazanavir (with or without low-dose ritonavir) in antiretroviral-experienced patients with end-stage renal disease undergoing hemodialysis.¹ ²⁰⁰

Common Adverse Effects

Headache, nausea, jaundice/scleral icterus, abdominal pain, rash, vomiting, diarrhea, insomnia, peripheral neurologic symptoms, dizziness, myalgia, depression, fever.¹

Interactions for Atazanavir Sulfate

Atazanavir metabolized by CYP3A.¹

Atazanavir inhibits CYP3A, CYP2C8, and UGT1A1.¹

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Pharmacokinetic interactions likely with drugs that are inducers of CYP3A4 or substrates of CYP3A with possible alteration in metabolism and concentrations of atazanavir and/or the other drug.¹

Pharmacokinetic interactions possible with drugs that are CYP3A or 2C8 substrates.¹

Drugs Metabolized by Uridine Diphosphate-glucuronosyltransferase 1A1

Pharmacokinetic interactions possible with drugs that are UGT 1A1 substrates.¹

Specific Drugs

Drug	Interaction	Comments
Abacavir	No in vitro evidence of antagonistic antiretroviral effects¹
Acetaminophen	Pharmacokinetic interaction unlikely¹
Alfuzosin	Possible increased alfuzosin concentrations; may result in hypotension¹	Concomitant use contraindicated¹
Antacids	Possible decreased atazanavir concentrations¹ ²⁰⁰	Take atazanavir at least 2 hours before or 1 hour after antacids¹ ²⁰⁰
Antiarrhythmic agents (amiodarone, systemic lidocaine, quinidine)	Possible increased antiarrhythmic agent concentrations; potential for serious and/or life-threatening effects¹	Use concomitantly with caution; monitor serum concentrations of antiarrhythmic agent¹
Anticoagulants, oral (e.g., warfarin)	Potential for increased warfarin plasma concentrations and serious and/or life-threatening bleeding episodes¹	Monitor INR¹
Anticonvulsants (carbamazepine, phenobarbital, phenytoin)	Possible decreased atazanavir concentrations²⁰⁰	Monitor anticonvulsant concentrations and virologic response; consider use of an alternative anticonvulsant, monitoring atazanavir concentrations, and use of ritonavir-boosted atazanavir²⁰⁰
Antidepressants, tricyclics	Possible increased concentrations of tricyclic antidepressants and potential for serious and/or life-threatening effects¹	Monitor tricyclic antidepressant concentrations¹
Antifungals, azoles	Fluconazole: No clinically important pharmacokinetic interactions with ritonavir-boosted atazanavir¹ Itraconazole: Possible pharmacokinetic interaction with ritonavir-boosted atazanavir;¹ ²⁰⁰ increased itraconazole and atazanavir concentrations²⁰⁰ Ketoconazole: No clinically important increases in atazanavir concentrations if atazanavir used without ritonavir;¹ possible increased ketoconazole concentrations with ritonavir-boosted atazanavir¹ Posaconazole: Increased atazanavir concentrations if used with atazanavir (with or without low-dose ritonavir)³² ²⁰⁰ Voriconazole: Possible increased atazanavir concentrations if atazanavir used without ritonavir; decreased antifungal concentrations with ritonavir-boosted atazanavir¹	Itraconazole: Caution if itraconazole dosage >200 mg daily is used with ritonavir-boosted atazanavir;¹ monitor itraconazole concentrations in those receiving >200 mg daily²⁰⁰ Ketoconazole: Caution if ketoconazole dosage >200 mg daily is used with ritonavir-boosted atazanavir¹ Posaconazole: If used with atazanavir (with or without low-dose ritonavir), monitor for atazanavir-associated adverse effects³² ²⁰⁰ Voriconazole: Monitor for toxicities if atazanavir used without ritonavir;²⁰⁰ concomitant use of ritonavir-boosted atazanavir and voriconazole not recommended unless potential benefits outweigh risk¹ ²⁰⁰ and voriconazole concentration monitoring considered²⁰⁰
Antimycobacterials (rifabutin, rifampin, rifapentine)	Rifabutin: Increased rifabutin concentrations and AUC¹ ²⁰⁰ Rifampin: Substantially decreased atazanavir concentrations; possible loss of virologic response and development of resistance¹	Rifabutin: If used with atazanavir (with or without low-dose ritonavir), reduce rifabutin dosage (use 150 mg every other day or 3 times weekly);¹ ²⁰⁰ monitor for rifabutin-associated adverse effects (e.g., neutropenia)¹ Rifampin: Concomitant use contraindicated¹ Rifapentine: Concomitant use not recommended²⁰⁰
Atovaquone and Proguanil	Ritonavir-boosted atazanavir: Decreased atovaquone and proguanil concentrations²⁰⁰	Consider alternative for malaria prophylaxis, if possible²⁰⁰
Benzodiazepines	Midazolam or triazolam: Possible increased plasma concentrations of midazolam or triazolam; potential for serious and/or life-threatening effects (e.g., prolonged or increased sedation or respiratory depression)¹ Alprazolam or diazepam: Possible increased benzodiazepine concentrations²⁰⁰ Lorazepam, oxazepam, temazepam: No data, but may have less potential for pharmacokinetic interaction with PIs compared with other benzodiazepines²⁰⁰	Oral midazolam or triazolam: Concomitant use contraindicated¹ ²⁰⁰ Parenteral midazolam: Consider reduced midazolam dosage, particularly if multiple doses are administered;¹ some experts state a single parenteral midazolam dose can be used with caution in a monitored situation for procedural sedation²⁰⁰ Alprazolam or diazepam: Consider alternative benzodiazepine with less potential for interaction (e.g., lorazepam, oxazepam, temazepam)²⁰⁰
β-Adrenergic blocking agents (atenolol)	Increased plasma concentrations and AUC of atenolol; no effect on PR interval observed¹	Use concomitantly with caution;¹ atenolol dosage adjustment not needed¹
Bosentan	Possible increased bosentan concentrations and decreased atazanavir concentrations¹ ²⁰⁰	Do not use atazanavir without low-dose ritonavir in patients receiving bosentan¹ ²⁰⁰ In patients already receiving ritonavir-boosted atazanavir for ≥10 days, initiate bosentan using dosage of 62.5 mg once daily or every other day based on individual tolerability¹ ²⁰⁰ In patients already receiving bosentan, discontinue bosentan for at least 36 hours prior to initiating ritonavir-boosted atazanavir; after ≥10 days of ritonavir-boosted atazanavir, resume bosentan using dosage of 62.5 mg once daily or every other day based on individual tolerability¹ ²⁰⁰
Buprenorphine	Atazanavir or ritonavir-boosted atazanavir: Increased buprenorphine and norbuprenorphine concentrations;¹ possible decreased atazanavir concentrations when used without low-dose ritonavir¹	Do not use atazanavir without low-dose ritonavir in patients receiving buprenorphine;¹ ²⁰⁰ monitor for sedation and adverse cognitive effects and consider reduced buprenorphine dosage¹ ²⁰⁰
Calcium-channel blocking agents (diltiazem, felodipine, nicardipine, nifedipine, verapamil)	Diltiazem: Increased diltiazem concentrations and AUC if used with atazanavir (without low-dose ritonavir);¹ ²⁰⁰ concomitant use with ritonavir-boosted atazanavir not evaluated¹ Felodipine, nicardipine, nifedipine, verapamil: Possible increased concentrations and AUC of calcium-channel blocking agent¹ Possible additive effect on PR interval¹	Diltiazem: Use concomitantly with caution; ECG monitoring recommended; consider reducing diltiazem dosage by 50%¹ ²⁰⁰ Felodipine, nicardipine, nifedipine, verapamil: Use concomitantly with caution; ECG monitoring recommended; consider dosage titration of the calcium-channel blocker¹ ²⁰⁰
Cisapride	Possible increased cisapride plasma concentrations;¹ potential for serious and/or life-threatening effects (e.g., cardiac arrhythmias)¹	Concomitant use contraindicated¹
Colchicine	Increased colchicine concentrations¹	Patients with renal or hepatic impairment: Avoid concomitant use of colchicine and atazanavir (with or without low-dose ritonavir)¹ Colchicine for treatment of gout flares: In those receiving atazanavir (with or without ritonavir), use initial colchicine dose of 0.6 mg followed by 0.3 mg 1 hour later and repeat dose no earlier than 3 days later¹ ²⁰⁰ Colchicine for prophylaxis of gout flares: In those receiving atazanavir (with or without ritonavir), decrease colchicine dosage to 0.3 mg once daily in those originally receiving 0.6 mg twice daily or decrease dosage to 0.3 mg once every other day in those originally receiving 0.6 mg once daily¹ ²⁰⁰ Colchicine for treatment of familial Mediterranean fever (FMF): In those receiving atazanavir (with or without ritonavir), use maximum colchicine dosage of 0.6 mg daily (may be given as 0.3 mg twice daily)¹ ²⁰⁰
Corticosteroids	Fluticasone nasal spray/oral inhalation: Increased fluticasone concentrations with atazanavir (with or without low-dose ritonavir) resulting in decreased cortisol concentrations¹ Dexamethasone: Potential decreased atazanavir concentrations²⁰⁰	Fluticasone nasal spray/oral inhalation: Consider alternative to fluticasone in patients receiving atazanavir without ritonavir, especially when long-term corticosteroid therapy is anticipated; concomitant use with ritonavir-boosted atazanavir not recommended unless potential benefits outweigh risk of systemic corticosteroid adverse effects¹ Dexamethasone: Use caution; consider alternative corticosteroids if long-term systemic therapy anticipated²⁰⁰
Co-trimoxazole	Pharmacokinetic interactions unlikely¹
Dapsone	Pharmacokinetic interactions unlikely¹
Darunavir		Usual dosage of ritonavir-boosted darunavir can be used concomitantly with atazanavir 300 mg once daily²⁰⁰ ²⁰⁴
Delavirdine	No in vitro evidence of antagonistic antiretroviral effects¹
Didanosine	Buffered didanosine: Decreased atazanavir concentrations and AUC;¹ decreased didanosine concentrations and AUC¹ Didanosine delayed-release capsules: Decreased didanosine concentrations and AUC if given with atazanavir and food;¹ ²⁰⁰ no change in atazanavir concentrations²⁰⁰ No in vitro evidence of antagonistic antiretroviral effects¹	Administer atazanavir (with food) 2 hours before or 1 hour after buffered or delayed-release didanosine preparations (without food)¹ ²⁰⁰
Digoxin	Potential additive effect on PR interval¹	Use concomitantly with caution¹
Efavirenz	Decreased atazanavir concentrations and AUC;¹ ²⁰⁰ no change in efavirenz concentrations²⁰⁰ No in vitro evidence of antagonistic antiretroviral effects¹	Do not use atazanavir without low-dose ritonavir in patients receiving efavirenz¹ In antiretroviral-naive adults, a regimen of atazanavir 400 mg, ritonavir 100 mg, and efavirenz 600 mg given once daily with food is recommended¹ ²⁰⁰ Concomitant use of atazanavir and efavirenz in antiretroviral-experienced adults not recommended¹ ²⁰⁰
Emtricitabine	No in vitro evidence of antagonistic antiretroviral effects¹
Enfuvirtide	No in vitro evidence of antagonistic antiretroviral effects¹
Ergot alkaloids (dihydroergotamine, ergonovine, ergotamine, methylergonovine)	Possible increased plasma concentrations of ergot alkaloids and potential for serious and/or life-threatening effects such as ergot toxicity (peripheral vasospasm, ischemia of the extremities and other tissues)¹	Concomitant use contraindicated¹ ²⁰⁰ If treatment of uterine atony and excessive postpartum bleeding is indicated in a woman receiving atazanavir, use methylergonovine maleate (Methergine) only if alternative treatments cannot be used and if potential benefits outweigh risks; use methylergonovine at lowest dosage and shortest duration possible²⁰²
Estrogens/Progestins	Oral hormonal contraceptives containing ethinyl estradiol and norgestimate or norethindrone: Possible increase or decrease in plasma concentrations of ethinyl estradiol and increase in progestin concentrations¹ ²⁰⁰	Ritonavir-boosted atazanavir: Use an oral contraceptive containing at least 35 mcg of ethinyl estradiol¹ ²⁰⁰ Atazanavir (without low-dose ritonavir): Use an oral contraceptive containing no more than 30 mcg of ethinyl estradiol¹ ²⁰⁰
Etravirine	Atazanavir or ritonavir-boosted atazanavir: Increased etravirine concentrations and decreased atazanavir concentrations²⁰⁰ ²¹⁴	Concomitant use with atazanavir (with or without low-dose ritonavir) not recommended²⁰⁰ ²¹⁴
Fosamprenavir	Ritonavir-boosted fosamprenavir: Decreased atazanavir concentrations; no change in amprenavir concentrations²⁰⁵ Fosamprenavir (without low-dose ritonavir): No data²⁰⁵ In vitro evidence of synergistic antiretroviral effects²⁰⁵	Appropriate dosages for concomitant use with fosamprenavir (with or without low-dose ritonavir) with respect to safety and efficacy not established²⁰⁰ ²⁰⁵
Histamine H₂-receptor antagonists	Famotidine: Decreased atazanavir concentrations with possible loss of therapeutic effect and development of resistance when atazanavir (without ritonavir) is administered at the same time as the histamine H₂-receptor antagonist ¹	Antiretroviral-naive and antiretroviral-experienced patients: Administer atazanavir 300 mg and ritonavir 100 mg once daily with food simultaneously with, and/or at least 10 hours after, the histamine H₂-receptor antagonist¹ Antiretroviral-naive patients unable to tolerate ritonavir: Administer atazanavir 400 mg once daily at least 2 hours before and 10 hours after the histamine H₂-receptor antagonist¹ Antiretroviral-naive patients: Dosage of histamine H₂-receptor antagonist should not exceed famotidine 40 mg twice daily (or equivalent)¹ Antiretroviral-experienced patients: Dosage of histamine H₂-receptor antagonist should not exceed famotidine 20 mg twice daily (or equivalent)¹ If used concomitantly with tenofovir and a histamine H₂-receptor antagonist in antiretroviral-experienced patients, a regimen of atazanavir 400 mg, tenofovir disoproxil fumarate 300 mg, and ritonavir 100 mg once daily with food is recommended¹ ²⁰⁰ Antiretroviral-experienced pregnant women in second and third trimester: Increase dosage of atazanavir to 400 mg once daily with ritonavir 100 mg once daily¹ Dosage recommendations not available for antiretroviral-experienced pregnant women receiving atazanavir and both tenofovir and a histamine H₂-receptor antagonist ¹
HMG-CoA reductase inhibitors	Atorvastatin, lovastatin, simvastatin, rosuvastatin: Possible decreased clearance and increased plasma concentrations of HMG-CoA reductase inhibitor with potential for increased risk of myopathy (including rhabdomyolysis)¹ ²⁰⁰ Fluvastatin or pravastatin: Interaction not expected¹ Pitavastatin: Possible increased pitavastatin concentrations²⁰⁰	Lovastatin or simvastatin: Concomitant use contraindicated¹ Atorvastatin or rosuvastatin: Use lowest possible initial dose of HMG-CoA reductase inhibitor with careful monitoring or consider using fluvastatin or pravastatin¹ ²⁰⁰ Pitavastatin: Dosage adjustments not needed if used with atazanavir (without ritonavir);²⁰⁰ some experts do not recommend concomitant use with ritonavir-boosted atazanavir²⁰⁰
Immunosuppressive agents (cyclosporine, sirolimus, tacrolimus)	Potential for increased plasma concentrations of cyclosporine, sirolimus, or tacrolimus¹	Monitor plasma concentrations of the immunosuppressive agent¹
Indinavir	Potential for additive hyperbilirubinemia¹ ²⁰⁰ No in vitro evidence of antagonistic antiretroviral effects¹	Concomitant use contraindicated¹
Irinotecan	Possible interference with metabolism of irinotecan; increased risk of irinotecan toxicity¹	Concomitant use contraindicated¹ ²⁰⁰
Lamivudine	No in vitro evidence of antagonistic antiretroviral effects¹
Lopinavir	Prolonged PR interval reported with both atazanavir and lopinavir²⁰⁷ In vitro evidence of additive to synergistic antiretroviral effects;²⁰⁷ no in vitro evidence of antagonism¹	Use concomitantly with caution and clinical monitoring²⁰⁷ Some experts recommend a dosage of atazanavir 300 mg once daily and lopinavir 400 mg/ritonavir 100 mg twice daily²⁰⁰
Macrolides (azithromycin, clarithromycin, erythromycin)	Azithromycin: Pharmacokinetic interactions unlikely¹ Clarithromycin: Increased plasma concentrations and AUC of atazanavir;¹ increased clarithromycin plasma concentrations and decreased 14-hydroxyclarithromycin plasma concentrations;¹ increased clarithromycin concentrations may cause QTc prolongation¹ Erythromycin: Pharmacokinetic interactions unlikely¹	Clarithromycin: Consider reducing clarithromycin dosage by 50%;¹ ²⁰⁰ consider alternative to clarithromycin¹ ²⁰⁰ for indications other than Mycobacterium avium complex (MAC)¹
Maraviroc	Atazanavir or ritonavir-boosted atazanavir: Increased maraviroc concentrations²⁰⁰ ²²⁴	Atazanavir or ritonavir-boosted atazanavir: Recommended dosage of maraviroc is 150 mg twice daily²⁰⁰
Methadone	Atazanavir: Pharmacokinetic interactions unlikely¹ ²⁰⁰ Ritonavir-boosted atazanavir: Decreased R-methadone (active isomer) concentrations²⁰⁰	Ritonavir-boosted atazanavir: Dosage adjustment of methadone not needed; closely monitor for signs of opiate withdrawal and adjust methadone dosage if needed²⁰⁰
Nelfinavir	No in vitro evidence of antagonistic antiretroviral effects¹
Nevirapine	Possible decreased atazanavir concentrations and increased nevirapine concentrations¹ ²⁰⁰ No in vitro evidence of antagonistic antiretroviral effects¹	Atazanavir (with or without low-dose ritonavir): Concomitant use not recommended¹ ²⁰⁰
Paclitaxel	Atazanavir (without low-dose ritonavir): Possible increased paclitaxel concentrations¹ Ritonavir-boostedatazanavir: Clinically important interaction not expected¹	Atazanavir (without low-dose ritonavir): Use concomitantly with caution¹
Pimozide	Atazanavir (with or without low-dose ritonavir): Potential for serious and/or life-threatening effects (e.g., cardiac arrhythmias)¹	Concomitant use contraindicated¹ ²⁰⁰
Proton-pump inhibitors	Omeprazole: Substantially decreased atazanavir concentrations¹ Possible loss of virologic response and development of atazanavir resistance¹	Antiretroviral-naive patients: Administer atazanavir 300 mg and ritonavir 100 mg once daily with food; administer the proton-pump inhibitor approximately 12 hours before ritonavir-boosted atazanavir;¹ dosage of proton-pump inhibitor should not exceed omeprazole 20 mg daily (or equivalent)¹ Antiretroviral-experienced patients: Concomitant use of proton-pump inhibitors not recommended¹
Raltegravir	Atazanavir or ritonavir-boosted atazanavir: Increased raltegravir concentrations;²⁰⁰ ²²⁵ concomitant use well tolerated²⁰⁰ ²²⁵ In vitro evidence of additive or synergistic antiretroviral effects²²⁵	Dosage adjustment of raltegravir not needed when used with atazanavir (with or without ritonavir)²⁰⁰ ²²⁵
Repaglinide	Atazanavir (without low-dose ritonavir): Possible increased repaglinide concentrations¹ Ritonavir-boostedatazanavir: Clinically important interaction not expected¹	Atazanavir (without low-dose ritonavir): Use concomitantly with caution¹
Rilpivirine	Atazanavir or ritonavir-boosted atazanavir: Possible increased rilpivirine concentrations; not expected to affect atazanavir concentrations²²⁶ No in vitro evidence of antagonistic antiretroviral effects²²⁶
Ritonavir	Increased atazanavir concentrations and AUC ;¹ ²⁰⁰ concomitant low-dose ritonavir used to therapeutic advantage (ritonavir-boosted atazanavir)¹ ¹³ ²⁰⁰ Possibility of additional pharmacokinetic interactions if ritonavir-boosted atazanavir used with other PIs¹ Prolonged PR interval reported with both atazanavir and ritonavir²⁰⁹ No in vitro evidence of antagonistic antiretroviral effects¹	Recommended dosage is atazanavir 300 mg once daily and ritonavir 100 mg once daily with food;¹ ²⁰⁰ safety and efficacy of concomitant use of ritonavir dosages >100 mg once daily not established¹ Use concomitantly with caution and clinical monitoring²⁰⁹ Concomitant use of ritonavir-boosted atazanavir with other PIs not recommended¹
St. John’s wort (Hypericum perforatum)	Possible decreased atazanavir concentrations; possible loss of virologic response and increased risk of atazanavir resistance¹	Concomitant use contraindicated¹ ²⁰⁰
Salmeterol	Atazanavir (with or without low-dose ritonavir): Possible increased salmeterol concentrations and increased risk of QT interval prolongation, palpitations, and sinus tachycardia¹	Concomitant use not recommended¹ ²⁰⁰
Saquinavir	Ritonavir-boosted saquinavir: Increased saquinavir concentrations and AUC; no change in atazanavir concentrations²¹⁰ Prolonged PR interval reported with both drugs; potential additive effects on PR interval²¹⁰ In vitro evidence of synergistic antiretroviral effects;²¹⁰ no in vitro evidence of antagonism¹	Appropriate dosage for concomitant use with respect to safety and efficacy not established¹ ²⁰⁰ Ritonavir-boosted saquinavir: Use concomitantly with caution and clinical monitoring²¹⁰
Sildenafil	Possible increased sildenafil concentrations and increased risk of sildenafil-associated adverse effects (hypotension, syncope, visual changes, priapism)¹ ²⁰⁰	Sildenafil (Revatio) for treatment of PAH: Concomitant use with atazanavir (with or without ritonavir) contraindicated¹ ²⁰⁰ Sildenafil for treatment of erectile dysfunction: Use with caution and with reduced sildenafil dosage (do not exceed 25 mg every 48 hours);¹ ²⁰⁰ closely monitor for adverse effects¹ ²⁰⁰
Stavudine	No in vitro evidence of antagonistic antiretroviral effects¹
Tadalafil	Possible increased tadalafil concentrations and increased risk of tadalafil-associated adverse effects (hypotension, syncope, visual changes, priapism)¹ ²⁰⁰	Tadalafil (Adcirca) for treatment of PAH: In patients already receiving atazanavir (with or without low-dose ritonavir) for ≥1 week, use initial tadalafil dosage of 20 mg once daily and increase to 40 mg once daily based on individual tolerability¹ ²⁰⁰ Avoid use of tadalafil (Adcirca) for treatment of PAH during initiation of atazanavir (with or without low-dose ritonavir) therapy;¹ ²⁰⁰ in a patient already receiving tadalafil (Adcirca) for treatment of PAH, discontinue tadalafil for at least 24 hours before starting atazanavir (with or without low-dose ritonavir); tadalafil can be restarted after ≥1 week of atazanavir (with or without low-dose ritonavir) therapy using initial tadalafil dosage of 20 mg once daily and increasing dosage to 40 mg once daily based on individual tolerability¹ ²⁰⁰ Tadalafil for treatment of erectile dysfunction: Use with caution and reduced tadalafil dosage (initial dose of 5 mg; do not exceed a single dose of 10 mg in 72 hours);¹ ²⁰⁰ closely monitor for adverse effects¹
Telaprevir	Ritonavir-boosted atazanavir: Decreased telaprevir concentrations and increased atazanavir concentrations¹⁸⁴
Tenofovir	Atazanavir and ritonavir-boosted atazanavir: Decreased atazanavir concentrations and AUC (minimum atazanavir plasma concentration higher with ritonavir-boosted atazanavir than with atazanavir); increased tenofovir concentrations and AUC¹ ²⁰⁰ No in vitro evidence of antagonistic antiretroviral effects¹	Do not use tenofovir in conjunction with atazanavir without low-dose ritonavir¹ ²⁰⁰ ²²¹ If ritonavir-boosted atazanavir is used with tenofovir, recommended dosage is atazanavir 300 mg, tenofovir disoproxil fumarate 300 mg, and ritonavir 100 mg once daily with food¹ ²⁰⁰ ²²¹ Monitor for tenofovir toxicity;¹ ²⁰⁰ discontinue tenofovir if adverse effects occur If used concomitantly with tenofovir and a histamine H₂-receptor antagonist in antiretroviral-experienced patients, a regimen of atazanavir 400 mg, tenofovir disoproxil fumarate 300 mg, and ritonavir 100 mg once daily with food is recommended¹ ²⁰⁰ Antiretroviral-experienced pregnant women in second or third trimester: Increase dosage of atazanavir to 400 mg with ritonavir 100 mg once daily¹ Dosage recommendations not available for antiretroviral-experienced pregnant women receiving both tenofovir anda histamine H₂-receptor antagonist ¹
Tipranavir	Ritonavir-boosted atazanavir: Decreased atazanavir concentrations and increased tipranavir concentrations²¹¹	Concomitant use with ritonavir-boosted tipranavir not recommended²¹¹
Trazodone	Atazanavir (with or without low-dose ritonavir): Possible increased trazodone concentrations¹	Use concomitantly with caution; consider using decreased trazodone dosage¹
Vardenafil	Possible increased vardenafil concentrations and increased risk of vardenafil-associated adverse effects (hypotension, syncope, visual changes, priapism)¹ ²⁰⁰	If used in patients receiving ritonavir-boosted atazanavir, use with caution and with reduced vardenafil dosage (do not exceed 2.5 mg every 72 hours); closely monitor for adverse effects¹ ²⁰⁰ If used in patients receiving atazanavir (without ritonavir), use with caution and with reduced vardenafil dosage (do not exceed 2.5 mg every 24 hours); closely monitor for adverse effects¹
Zidovudine	No change in zidovudine AUC, but possible decreased zidovudine concentrations²⁰⁰ No in vitro evidence of antagonistic antiretroviral effects¹

Atazanavir Sulfate Pharmacokinetics

Absorption

Bioavailability

Atazanavir: Rapidly absorbed following oral administration;¹ peak plasma concentrations attained approximately 2–2.5 hours after a dose.¹

Ritonavir-boosted atazanavir: Peak plasma concentrations attained approximately 2.7–3 hours after a dose.¹

Food

Food increases bioavailability and reduces pharmacokinetic variability.¹

Administration of atazanavir with a light meal (357 kcal, 8.2 g fat, 10.6 g protein) increases AUC by 70% and peak plasma concentration by 57% compared with fasting.¹ A high-fat meal (721 kcal, 37.3 g fat, 29.4 g protein) increases AUC by 35% with no increase in peak plasma concentration.¹

Administration of ritonavir-boosted atazanavir with a light meal (336 kcal, 5.1 g fat, 9.3 g protein) increases AUC by 33% and peak plasma concentration by 40% compared with fasting.¹ A high-fat meal (951 kcal, 54.7 g fat, 35.9 g protein) does not affect AUC compared with fasting.¹

Plasma Concentrations

Nonlinear pharmacokinetics with greater than dose-proportional increases in plasma concentrations and AUC.¹

Steady-state concentrations attained between days 4–8 with an accumulation of approximately 2.3-fold.¹

Special Populations

Hepatic Impairment: Following a single 400-mg dose of atazanavir, AUC increased 42% in adults with moderate to severe hepatic impairment (Child-Pugh class B and C) compared with healthy adults.¹

Renal Impairment: Plasma concentrations in adults with severe renal impairment not undergoing dialysis generally are similar to those in adults with normal renal function.¹ When administered before or after dialysis, plasma concentrations are lower than those in adults with normal renal function (mechanism of this change unknown).¹

Postpartum women: Atazanavir steady-state peak plasma concentrations and AUC are approximately 28–43% higher during postpartum period (4–12 weeks) compared with historical data in HIV-infected, nonpregnant patients.¹

Distribution

Extent

Low concentrations attained in CSF and semen after oral administration.¹

Crosses the placenta.¹ ²⁰² When ritonavir-boosted atazanavir used in pregnant women, atazanavir concentrations in cord blood approximately 12–19% of maternal plasma concentrations at delivery.¹ ²⁰²

Distributed into milk in low concentrations.²⁰²

Plasma Protein Binding

86% bound to serum proteins; binding independent of concentration.¹

Binds to both α-1-acid glycoprotein (89%) and albumin (86%).¹

Elimination

Metabolism

Extensively metabolized and eliminated in liver.¹ CYP3A involved in metabolism of the drug.¹

Elimination Route

Approximately 79% of a dose eliminated in feces and 13% eliminated in urine as metabolites and unchanged drug.¹

Not removed by hemodialysis.¹

Half-life

Atazanavir: 6.5–7.9 hours.¹

Ritonavir-boosted atazanavir: 8.6–18.1 hours.¹

Special Populations

No clinically important differences in pharmacokinetics in those >65 years of age compared with younger adults.¹

Atazanavir: Half-life is 12.1 hours in those with moderate to severe hepatic impairment.¹

Stability

Storage

Oral

Capsules

25°C (may be exposed to 15–30°C).¹

Actions and Spectrum

Pharmacologically related to other PIs (e.g., darunavir, fosamprenavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir, tipranavir); differs structurally from these drugs and also differs pharmacologically and structurally from other currently available antiretrovirals.¹
Active against HIV-1;¹ not active against HIV-2.¹²
Inhibits replication of HIV-1 by interfering with HIV protease.¹
HIV-1 with reduced susceptibility to atazanavir have been selected in vitro and have emerged during therapy with the drug.¹ ¹¹
Varying degrees of cross-resistance occur among PIs.¹

Advice to Patients

Critical nature of compliance with HIV therapy.¹ ²⁰⁰ Use in conjunction with other antiretrovirals—not for monotherapy.¹ ²⁰⁰ Importance of taking as prescribed; do not alter or discontinue antiretroviral regimen without consulting clinician.¹
Antiretroviral therapy is not a cure for HIV infection; opportunistic infections and other complications associated with HIV disease may still occur.¹
Advise patients that sustained decreases in plasma HIV RNA have been associated with reduced risk of progression to AIDS and death.¹
Importance of continuing to practice safer sex (e.g., using latex or polyurethane condoms to minimize sexual contact with body fluids) and never reusing or sharing needles.¹
Importance of taking with food to enhance absorption.¹
If a dose is missed, it should be taken as soon as it is remembered and the next dose taken at the regularly scheduled time; if a dose is skipped, the next dose should not be doubled.¹
Advise patients that ECG changes (PR prolongation) have occurred; importance of consulting clinician if dizziness or lightheadedness occurs.¹
Possibility of asymptomatic increases in indirect bilirubin that may be accompanied by yellowing of the skin or whites of the eyes;¹ alternative antiretroviral therapy can be considered if these cosmetic changes are a concern.¹
Redistribution/accumulation of body fat may occur, with as yet unknown long-term health effects.¹
Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements (e.g., St. John's wort), and any concomitant illnesses.¹
Advise patients receiving a selective PDE5 inhibitor (e.g., sildenafil, tadalafil, vardenafil) that they may be at increased risk of PDE5 inhibitor-associated adverse effects (e.g., hypotension, syncope, visual changes, prolonged penile erection) and that any symptoms should be promptly reported to clinician.¹ Should not be used in patients receiving sildenafil for treatment of PAH.¹
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹ ²⁰⁰
Importance of advising 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.

Atazanavir Sulfate
Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules	100 mg (of atazanavir)	Reyataz	Bristol-Myers Squibb
		150 mg (of atazanavir)	Reyataz	Bristol-Myers Squibb
		200 mg (of atazanavir)	Reyataz	Bristol-Myers Squibb
		300 mg (of atazanavir)	Reyataz	Bristol-Myers Squibb

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 10/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Reyataz 150MG Capsules (B-M SQUIBB U.S. (PRIMARY CARE)): 30/$557.97 or 90/$1,616.92

Reyataz 200MG Capsules (B-M SQUIBB U.S. (PRIMARY CARE)): 60/$1,048.99 or 180/$3,058.08

Reyataz 300MG Capsules (B-M SQUIBB U.S. (PRIMARY CARE)): 30/$1,037.97 or 90/$3,067.86

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Bristol-Myers Squibb. Reyataz (atazanavir sulfate) capsules prescribing information. Princeton, NJ; 2011 Feb.

2. Sanne I, Piliero P, Squires K et al. Results of a phase 2 clinical trial at 48 weeks (A1424-007); a dose-ranging, safety, and efficacy comparative trial of atazanavir at three doses in combination with didanosine and stavudine in antiretroviral-naive subjects. J Acquir Immune Defic Syndr. 2003; 32:18-29. [IDIS 492665] [PubMed 12514410]

3. Haas DW, Zala C, Schrader S et al. Therapy with atazanavir plus saquinavir in patients failing highly active antiretroviral therapy: a randomized comparative pilot trial. AIDS. 2003; 17:1339-49. [PubMed 12799555]

4. Piliero PJ. Atazanavir: a novel HIV-1 protease inhibitor. Expert Opin Investig Drugs. 2002; 11:1295-1301 [PubMed 12225250]

7. Squires K, Lazzarin A, Gatell JM et al. Comparison of once-daily atazanavir with efavirenz, each in combination with fixed-dose zidovudine and lamivudine, as initial therapy for patients infected with HIV. J Acquir Immune Defic Syndr. 2004; 36:1011-9. [PubMed 15247553]

8. Wood R, Phanuphak P, Cahn P et al. Long-term efficacy and safety of atazanavir with stavudine and lamivudine in patients previously treated with nelfinavir or atazanavir. J Acquir Immune Defic Syndr. 2004; 36:684-92. [PubMed 15167287]

9. Murphy RL. Reviving protease inhibitors: new data and more options. J Acquir Immune Defic Syndr. 2003; 33(suppl 1):S43-52. [IDIS 511780] [PubMed 12946064]

11. Colonno RJ, Thiry A, Limoli K et al. Activities of atazanavir 9BMS-232632) against a large panel of human immunodeficiency virus type 1 clinical isolates resistant to one or more approved protease inhibitors. Antimicrob Agents Chemother. 2003; 47:1324-3. [PubMed 12654666]

12. Bristol-Myers Squibb, Princeton, NJ: Personal Communication.

13. Hodder S. Dear healthcare provider letter: important new pharmacokinetic data for Reyataz (atazanavir sulfate) in combination with Viread (tenofovir disoproxil fumarate). Princeton, NJ: Bristol-Myers Squibb; 2003 Aug 8.

14. Goldsmith DR, Perry CM. Atazanavir. Drugs. 2003; 63:1679-93. [PubMed 12904086]

17. Centers for Disease Control and Prevention. Antiretroviral postexposure prophylaxis after sexual, injection-drug use, or other nonoccupational exposure to HIV in the United States: Recommendations from the U.S. Department of Health and Human Services. MMWR Recomm Rep. 2005; 54 (No. RR-2):1-19.

18. Center for Disease Control and Prevention. Updated U.S. public health service guidelines for the management of occupational exposures to HIV and recommendations for postexposure prophylaxis. MMWR Recomm Rep. 2005; 54(No. RR-9):1-17.

21. AstraZeneca. Crestor (rosuvastatin calcium) prescribing information. Wilmington, DE; 2005 Dec.

28. Molina JM, Andrade-Villanueva J, Echevarria J et al. Once-daily atazanavir/ritonavir versus twice daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1 infected patients: 48 week efficacy and safety results of the CASTLE study. Lancet. 2008; 372:646-55. [PubMed 18722869]

29. Molina JM, Andrade-Villanueva J, Echevarria J et al. Once-daily atazanavir/ritonavir compared with twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 96-week efficacy and safety results of the CASTLE study. J Acquir Immune Defic Syndr. 2010; 53:323-32. [PubMed 20032785]

30. Johnson M, Grinsztejn B, Rodriguez C et al. Atazanavir plus ritonavir or saquinavir, and lopinavir/ritonavir in patients experiencing multiple virological failures. AIDS. 2005; 19:685-94. [PubMed 15821394]

31. Johnson M, Grinsztejn B, Rodriguez C et al. 96-week comparison of once-daily atazanavir/ritonavir and twice-daily lopinavir/ritonavir in patients with multiple virologic failures. AIDS. 2006; 20:711-8. [PubMed 16514301]

32. Schering Corp. Noxafil (poscaconazole) oral solution prescribing information. Whitehouse Station, NJ; 2010 Sep.

35. Murphy RL, Sanne I, Cahn P et al. Dose-ranging, randomized, clinical trial of atazanavir with lamivudine and stavudine in antiretroviral-naive subjects: 48-week results. AIDS. 2003; 17:2603-14. [PubMed 14685054]

184. Vertex Pharmaceuticals. Incivek (telaprevir) tablets prescribing information. Cambridge, MA; 2011 May.

200. Panel on Antiretroviral Guidelines for Adults and Adolescents, US Department of Health and Human Services (DHHS). Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (January 10, 2011). Updates available at DHHS AIDS Information (AIDSinfo) website.

201. Panel on Antiretroviral Therapy and Medical Management of HIV-infected Children. Guidelines for the use of antiretroviral agents in pediatric HIV infection (August 11, 2011). Updates available at HHS AIDS Information (AIDSinfo) website.

202. Panel on Treatment of HIV-Infected Pregnant Women and Prevention of Perinatal Transmission, US Department of Health and Human Services (DHHS). Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States (May 24, 2010). Updates available at DHHS AIDS Information (AIDSinfo) website.

204. Tibotec. Prezista (darunavir) tablets prescribing information. Raritan, NJ; 2010 Dec.

205. ViiV Healthcare. Lexiva (fosamprenavir calcium) tablets and oral suspension prescribing information. research Triangle Park, NC; 2011 May.

207. Abbott Laboratories. Kaletra (lopinavir/ritonavir) tablets and oral solution prescribing information. North Chicago, IL; 2011 Feb.

209. Abbott Laboratories. Norvir (ritonavir) tablets and oral solution prescribing information. North Chicago, IL; 2010 Apr.

210. Genentech USA. Invirase (saquinavir mesylate) capsules and tablets prescribing information. South San Francisco, CA; 2010 Oct.

211. Boehringer Ingelheim. Aptivus (tipranavir) capsules and oral solution prescribing information. Ridgefield, CT; 2011 Apr.

214. Tibotec Therapeutics. Intelence (etravirine) tablets prescribing information. Raritan, NJ; 2010 Dec.

221. Gilead Sciences. Viread (tenofovir disoproxil fumarate) tablets prescribing information. Foster City, CA; 2010 Oct.

224. ViiV Healthcare. Selzentry (maraviroc) tablets prescribing information. New York, NY; 2011 Jun.

225. Merck Sharp & Dohme Corp. Isentress (raltegravir) tablets prescribing information. Whitehouse Station, NJ; 2011 Feb.

226. Tibotec Therapeutics. Edurant (rilpivirine) tablets prescribing information. Raritan, NJ; 2011 May.

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