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atazanavir (Rx)Brand and Other Names:Reyataz

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 100mg
  • 150mg
  • 200mg
  • 300mg
more...

HIV-1 Infection

Treatment-naive

  • 400 mg PO qDay, OR
  • 300 mg PO with 100 mg ritonavir qDay
  • With 600 mg efavirenz: 400 mg PO with 100 mg ritonavir qDay administered at different times (ritonavir and atazanavir with food in morning; efavirenz on an empty stomach, preferably at bedtime)

Treatment-experienced or with tenofovir

  • 300 mg PO (with ritonavir 100 mg) PO qDay with tenofovir

Dosing during pregnancy and postpartum period

  • Administer atazanavir with ritonavir
  • Only administer to pregnant women with HIV-1 strains susceptible to atazanavir
  • Dosage adjustments are not required in pregnant patients except with the following exceptions: treatment-experienced pregnant women during the second or third trimester, when atazanavir is coadministered with either an H2-receptor antagonist or tenofovir, atazanavir 400 mg with ritonavir 100 mg once daily is recommended; insufficient data to recommend an atazanavir dose for use with both an H2-receptor antagonist and tenofovir in treatment-experienced pregnant women
  • No dose adjustment is required for postpartum patients; closely monitor patients for adverse events because atazanavir exposures may be increased during first 2 months after delivery

Dosage Modifications

Hepatic impairment

  • Child-Pugh score 7-9: 300 mg PO qDay
  • Child-Pugh score >9: Not recommended
  • Ritonavir boosting NOT recommended with Child-Pugh score 7 or above

Renal impairment

  • No dose adjustment necessary including those with severe renal impairment who are not managed with hemodialysis
  • Hemodialysis (treatment-naive): 300 mg PO (with ritonavir 100 mg) qDay
  • Antiretroviral-experienced patients: Not recommended

Dosage Forms & Strengths

capsule

  • 150mg
  • 200mg
  • 300mg

oral powder

  • 50mg/packet
more...

HIV-1 Infection

Oral capsules

  • 6-18 years (treatment naïve and treatment experienced)
    • 15 to <20 kg (33 to <44 lbs): 150 mg (+ 100 mg ritonavir) PO qDay
    • 20 to <40 kg (44 to <88 lbs): 200 mg (+ 100 mg ritonavir) PO qDay
    • ≥40 kg (≥88 lbs): 300 mg (+ 100 mg ritonavir) PO qDay
  • ≥13 years (treatment naïve and cannot tolerate ritonavir)
    • ≥40 kg (≥88 lbs): 400 mg PO qDay

Oral powder

  • Oral powder is for use in treatment-naive or treatment-experienced pediatric patients who are at least 3 months of age and weighing at least 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

Dosing Considerations

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

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Interactions

Interaction Checker

atazanavir and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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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: Nephrolithiasis

            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

            Inhibits CYP3A4 and UGT1A1

            • Do not coadminister with drugs highly dependent on CYP3A or UGT1A1 for clearance
            • Atazanavir may elevated plasma concentrations of the following drugs and lead to serious and/or life-threatening events
              • Alfuzosin
              • Irinotecan
              • Triazolam, midazolam PO
              • Ergot derivatives
              • Cisapride
              • Lovastatin
              • Simvastatin
              • Pimozide
              • Sildenafil (when used for PAH)
            • Coadministration with the following drugs that strongly induce CYP3A and may result in loss of therapeutic effect of atazanavir
              • Rifampin
              • St. John’s wort
              • Nevirapine

            Cautions

            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

            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

            Discontinue if severe rash develops

            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

            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

            Use caution in mild-moderate hepatic impairment

            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

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            Pregnancy & Lactation

            Pregnancy Category: B

            Administer atazanavir with ritonavir

            Only administer to pregnant women with HIV-1 strains susceptible to atazanavir

            Lactation: It is not known whether atazanavir is excreted in milk. Because of both the potential for HIV transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breast-feed if they are taking this drug.

            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 capsule or oral powder with food

            Do not open capsules

            Take atazanavir and ritonavir in a single dose

            When coadministered with H2-receptor antagonists or proton-pump inhibitors, dose separation may be required

            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)

            Instructions for mixing oral powder

            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
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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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