atazanavir (Rx)

Brand and Other Names:Reyataz
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 100mg
  • 150mg
  • 200mg
  • 300mg

HIV-1 Infection

Indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection

Treatment-naïve (capsules)

  • Recommended dose: 300 mg PO (with ritonavir 100 mg) qDay
  • Unable to tolerate ritonavir: 400 mg PO qDay
  • In combination with efavirenz: 400 mg PO (with ritonavir 100 mg) qDay

Treatment-experienced (capsules)

  • Recommended dose: 300 mg PO (with ritonavir 100 mg) qDay
  • In combination with H2-receptor antagonist (H2RA) and tenofovir DF: 400 mg PO (with ritonavir 100 mg) qDay
  • Not recommended for treatment-experienced adults without ritonavir coadministration

Dosing during pregnancy and postpartum period

  • Administer atazanavir with ritonavir
  • Treatment-naïve and treatment-experienced: 300 mg PO (with ritonavir 100 mg) qDay
  • Treatment-experienced during the second or third trimester when coadministered with either H2RA OR tenofovir DF: 400 mg PO (with ritonavir 100 mg) qDay
  • Not recommended for treatment-experienced pregnant patients during the second and third trimester taking atazanavir with both tenofovir DF and H2RA
  • Post-partum patients: No dosage adjustment

Dosage Modifications

Hepatic impairment

  • For treatment naïve patients
  • Mild (Child-Pugh Class A): 400 mg PO qDay
  • Moderate (Child-Pugh Class B): 300 mg PO qDay
  • Severe (Child-Pugh Class C): Not recommended
  • Coadministration of atazanavir with ritonavir in patients with any degree of hepatic impairment is not recommended

Renal impairment

  • No dose adjustment necessary including those with severe renal impairment who are not managed with hemodialysis
  • Treatment-naïve patients with end-stage renal disease on hemodialysis: 300 mg PO (with ritonavir 100 mg) qDay
  • Antiretroviral-experienced patients: Not recommended

Dosing Considerations

Use of atazanavir with ritonavir in treatment-experienced patients should be guided by the number of baseline primary protease inhibitor resistance substitutions

Testing prior to initiation and during treatment

  • Perform renal laboratory testing (eg, serum creatinine, estimated CrCl, urinalysis with microscopic examination) in all patients prior to initiation of atazanavir and continued during treatment
  • Perform hepatic laboratory testing in patients with underlying liver disease prior to initiation of atazanavir and continued during treatment

Dosage Forms & Strengths

capsule

  • 150mg
  • 200mg
  • 300mg

oral powder

  • 50mg/packet

HIV-1 Infection

Also see Administration

Oral capsules

  • 6-18 years (treatment naïve and treatment experienced)
    • <15 kg: Capsules not recommended
    • 15 to <35 kg: 200 mg PO (with ritonavir 100 mg) qDay
    • ≥35: 300 mg PO (with ritonavir 100 mg) qDay
  • ≥13 years (treatment naïve and cannot tolerate ritonavir)
    • ≥40 kg: 400 mg PO qDay

Oral powder

  • <3 months or <5 kg: Safety and efficacy not established
  • ≥3 months and weigh ≥5 kg
    • 5 kg to <15 kg: 200 mg (4 packets) plus 80 mg ritonavir PO qDay
    • 15 kg to <25 kg: 250 mg (5 packets) plus 80 mg ritonavir PO qDay
    • ≥25 kg and unable to swallow capsule: 300 mg (6 packets) plus 100 mg ritonavir PO qDay
    • NOTE: Children unable to tolerate 200 mg/day dose who weigh 5 kg to <10 kg and have not previously taken an HIV protease inhibitor may take 150 mg (3 packets) daily with close HIV viral load monitoring
  • Weight 5 kg to <15 kg who do not tolerate 200 mg dose
    • Only patients weighing 5 to less than 10 kg who do not tolerate the 200 mg atazanavir dose and have not previously taken an HIV protease inhibitor, may take 150 mg (3 packets) with close HIV viral load monitoring

Dosing Considerations

Use of atazanavir with ritonavir in treatment-experienced patients should be guided by the number of baseline primary protease inhibitor resistance substitutions

Not recommended for use in pediatric patients <3 months due to the risk of kernicterus

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Interactions

Interaction Checker

and atazanavir

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            Adverse Effects

            Incidence based on combination therapy

            >10%

            Total bilirubin increased (35-49%)

            Fever (19%)

            Rash (3-21%)

            Cholesterol is increased (6-25%)

            Nausea (4-14%)

            CPK increased (6-11%)

            Cough (21%)

            Diarrhea (3-11%)

            1-10%

            Neutrophils decrease (6-10%)

            Jaundice (5-9%)

            Headache (1-7%)

            Peripheral neuropathy (1-4%)

            Insomnia (1-3%)

            Fever (2%)

            Vomiting (3-7%)

            Dizziness (1-2%)

            Myalgia (4%)

            Abdominal pain (2-4%)

            Depression (1-2%)

            <1%

            Prolonged PR interval

            New onset diabetes mellitus, exacerbation of diabetes mellitus & hyperglycemia

            Postmarketing Reports

            Body as a whole: Edema

            Cardiovascular system: Second-degree AV block, third-degree AV block, left bundle branch block, QTc prolongation

            Gastrointestinal system: Pancreatitis

            Hepatic system: Hepatic function abnormalities

            Hepatobiliary disorders: Cholelithiasis, cholecystitis, cholestasis

            Metabolic system and nutrition disorders: Diabetes mellitus, hyperglycemia

            Musculoskeletal system: Arthralgia

            Renal system: Chronic kidney disease, nephrolithiasis, interstitial nephritis, granulomatous interstitial nephritis

            Skin and appendages: Alopecia, angioedema, maculopapular rash, pruritus

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            Warnings

            Contraindications

            Previously demonstrated hypersensitivity including Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions

            Treatment-experienced patients with ESRD receiving hemodialysis

            Severe hepatic impairment (Child-Pugh Class C); hepatic impairment and concomitant ritonavir

            Indinavir; both atazanavir and indinavir are associated with indirect hyperbilirubinemia

            CYP3A4 inducers

            • May lead to lower exposure and loss of efficacy of atazanavir
            • Rifampin
            • St. John’s wort
            • Nevirapine

            CYP3A4 and UGT1A1 substrates

            • Do not coadminister with drugs highly dependent on CYP3A or UGT1A1 for clearance
            • Atazanavir may elevate plasma concentrations of the following drugs and lead to serious and/or life-threatening events
              • Alfuzosin
              • Irinotecan
              • Triazolam
              • Glecaprevir
              • Pibrentasvir
              • Midazolam PO
              • Ergot derivatives
              • Cisapride
              • Dronedarone
              • Lovastatin
              • Simvastatin
              • Lurasidone
              • Ranolazine
              • Pimozide
              • Grazoprevir
              • Colchicine
              • Sildenafil (when used for PAH)
              • Elbasvir/grazoprevir
              • Glecaprevir/pibrentasvir

            Cautions

            Also see Dosage Modifications

            Do not use proton-pump inhibitors in treatment-experienced patients

            Discontinue if severe rash; Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions reported, including drug rash, eosinophilia, and systemic symptoms (DRESS) syndrome; discontinue if severe rash develops

            Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” have been observed in patients receiving antiretroviral therapy

            Spontaneous bleeding may occur and additional factor VIII may be required

            PR interval prolongation may occur in some patients; ECG monitoring should be considered in patients with preexisting conduction system disease or when administered with other drugs that may prolong the PR interval

            Most patients experience asymptomatic increases in indirect bilirubin, which is reversible upon discontinuation; do not dose reduce; if concomitant transaminase increase occurs, evaluate for alternative etiologies

            Chronic kidney disease in HIV-infected patients treated with atazanavir, with or without ritonavir, has been reported during postmarketing surveillance; consider alternative therapy in patients at high risk for renal disease or with preexisting renal disease; conduct renal laboratory testing (including serum creatinine, estimated creatinine clearance, and urinalysis with microscopic examination) in all patients prior to and during therapy; expert consultation advised for patients who have confirmed renal laboratory abnormalities while on treatment; in patients with progressive kidney disease, consider discontinuing therapy

            Nephrolithiasis and cholelithiasis reported; consider temporary interruption or discontinuation

            Treatment-experienced patients with prior virologic failure: without ritonavir not recommended

            Patients receiving atazanavir may develop new onset or exacerbations of diabetes mellitus/hyperglycemia, immune reconstitution syndrome, and redistribution/accumulation of body fat

            Patients with hepatitis B or C infection are at risk of increased transaminases or hepatic decompensation; monitor hepatic laboratory tests prior to therapy and during treatment

            Most patients experience asymptomatic increases in indirect bilirubin, which is reversible upon discontinuation; do not dose reduce; if a concomitant transaminase increase occurs, evaluate for alternative etiologies.

            Oral powder contains phenylalanine which can be harmful to patients with phenylketonuria

            Drug interactions overview

            • Also see Contraindications
            • Initiation of atazanavir with ritonavir, a CYP3A inhibitor: Patients receiving medications metabolized by CYP3A, may increase plasma concentrations of medications metabolized by CYP3A
            • Initiation of CYP3A4 inducers/inhibitors may increase or decrease concentrations of atazanavir with ritonavir, respectively
            • Interactions may lead to clinically significant adverse reactions potentially leading to severe, life-threatening, or fatal events from greater exposures of concomitant medications; clinically significant adverse reactions from greater exposures of atazanavir with ritonavir, or loss of therapeutic effect of atazanavir with ritonavir and possible development of resistance
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            Pregnancy & Lactation

            Pregnancy

            There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to therapy during pregnancy; healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263

            Atazanavir has been evaluated in a limited number of women during pregnancy; available human and animal data suggest that atazanavir does not increase risk of major birth defects overall compared to background rate

            Therapy must be administered with ritonavir in pregnant women

            Dosage modifications

            • No dosage adjustment is required with the following exceptions
            • Treatment-experienced pregnant women during second or third trimester, when therapy is coadministered with either an H2-receptor antagonist or tenofovir DF, a dose of 400 mg with ritonavir 100 mg once daily recommended
            • There are insufficient data to recommend with both an H2-receptor antagonist and tenofovir DF in treatment-experienced pregnant women
            • No dosage adjustment is required for postpartum patients; however, patients should be closely monitored for adverse events because atazanavir exposures could be higher during first 2 months after delivery

            Maternal adverse reactions

            • Cases of lactic acidosis syndrome, sometimes fatal, and symptomatic hyperlactatemia have occurred in pregnant women receiving therapy in combination with nucleoside analogues, which are associated with an increased risk of lactic acidosis syndrome
            • Hyperbilirubinemia occurs frequently in patients who receive therapy; advise pregnant women of the potential risks of lactic acidosis syndrome and hyperbilirubinemia

            Fetal/Neonatal Adverse Reactions

            • All infants, including neonates exposed to therapy in utero, should be monitored for development of severe hyperbilirubinemia during first few days of life

            Lactation

            The Centers for Disease Control and Prevention recommend that HIV-1 infected mothers not breastfeed infants to avoid risking postnatal transmission of HIV-1

            Atazanavir has been detected in human milk; no data available regarding atazanavir effects on milk production; atazanavir was present in milk of lactating rats and was associated with neonatal growth retardation that reversed after weaning

            Because of both the potential for HIV-1 transmission and potential for serious adverse reactions in breastfed infants, advise women not to breastfeed

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Protease Inhibitor; inhibits cleavage of Gag-Pol polyprotein precursors, which in turn causes the formation of immature, noninfectious viral particles.

            Absorption

            Peak Plasma Time: 2-3 hr

            Distribution

            Protein Bound: 86%

            Metabolism

            Via hepatic P450 enzyme CYP3A4

            Enzymes inhibited: CYP3A4

            Elimination

            Half-life: 7-8 hr (unboosted therapy); 9-18 hr (boosted therapy)

            Excretion: 79% feces; 13% urine

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            Administration

            Oral Administration

            Take atazanavir and ritonavir in a single dose

            Capsules

            • Take capsule or oral powder with food
            • Do not open capsules
            • When coadministered with H2-receptor antagonists or proton-pump inhibitors, dose separation may be required

            Oral powder

            • Oral powder must be taken with ritonavir and is not recommended for use in children who weigh <5 kg or aged <3 months (risk of kernicterus)
            • Determine the number of packets that are needed
            • Prior to mixing, tap the packet to settle the powder
            • It is preferable to mix oral powder with food (eg, applesauce, yogurt)
            • Mixing oral powder with a beverage (milk, infant formula, or water) may be used for infants who can drink from a cup
            • For young infants (aged <6 months) who cannot eat solid food or drink from a cup, mix oral powder with infant formula and administer using an oral dosing syringe
            • Administration in infant formula using an infant bottle is not recommended because full dose may not be delivered
            • Administer ritonavir immediately following atazanavir oral powder administration
            • Administer the entire oral powder dose (mixed in the food or beverage) within 1 hr of preparation (may leave the mixture at room temperature during this 1 hr period)
            • Ensure that the patient eats or drinks all the food or beverage that contains the powder
            • Additional food may be given after consumption of the entire mixture
            • Mixing with food
              • Using a spoon, mix the recommended number of oral powder packets with a minimum of 1 tablespoon of food (eg, applesauce, yogurt)
              • Feed the mixture to the infant or young child
              • Add an additional 1 tablespoon of food to the small container, mix, and feed the child the residual mixture
            • Mixing with beverage
              • Using a spoon, mix the recommended number of oral powder packets with a minimum of 30 mL of beverage (eg, milk, water) in a small beverage cup
              • Have the child drink the mixture
              • Add an additional 15 mL more of beverage to the drinking cup, mix, and have the child drink the residual mixture
              • If water is used, food should also be taken at the same time
            • Mixing with infant formula
              • Using a spoon, mix the recommended number oral powder packets with 10 mL of prepared liquid infant formula
              • Draw up the full amount of the mixture into an oral syringe and administer into either right or left inner cheek of infant
              • Pour another 10 mL of formula into the medicine cup to rinse off remaining oral powder in cup, draw up residual mixture into the syringe and administer into either right or left inner cheek of infant

            Storage

            Capsules: Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F)

            Unused oral powder: Store <30°C (86°F); store in the original packet and do not open until ready to use

            Reconstituted oral powder: Once mixed with food or beverage, store at room temperature 20-30°C (68-86°F) for up to 1 hr prior to administration

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            Formulary

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
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