Atazanavir

Atazanavir is a prescription medication used to treat the symptoms of HIV-1 Infection. Atazanavir may be used alone or with other medications.

• Atazanavir is available under the following different brand names: Reyataz 

Common side effects of Atazanavir include:

• fever,
• nausea,
• vomiting,
• stomach pain,
• diarrhea,
• headache,
• muscle pain,
• depressed mood,
• sleep problems (insomnia),
• numbness, tingling, or burning pain in the hands or feet, and
• changes in the shape or location of body fat (especially in the arms, legs, face, neck, breasts, and waist)

Serious side effects of Atazanavir include:

• hives,
• difficulty breathing,
• swelling of the face, lips, tongue, or throat,
• fever,
• sore throat,
• burning in the eyes,
• skin pain,
• red or purple skin rash that spreads and causes blistering and peeling,
• sudden dizziness,
• severe pain in the lower stomach or back,
• painful urination,
• blood in the urine,
• increased thirst,
• increased urination,
• dry mouth,
• fruity breath odor,
• headache,
• blurred vision,
• nausea,
• vomiting,
• upper stomach pain,
• itching,
• dark urine,
• clay-colored stools,
• yellowing of the skin or eyes (jaundice),
• night sweats,
• swollen glands,
• cold sores,
• cough,
• wheezing,
• diarrhea,
• weight loss,
• trouble speaking or swallowing,
• problems with balance or eye movement,
• weakness,
• prickly feeling,
• loss of bladder or bowel control,
• swelling in the neck or throat (enlarged thyroid),
• menstrual changes, and
• impotence

Rare side effects of Atazanavir include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Capsule

• 100 mg
• 150 mg
• 200 mg
• 300 mg

Oral powder

• 50 mg/packet

HIV-1 Infection

Adult dosage

Treatment-naïve (capsules)

• Recommended dose: 300 mg orally (with ritonavir 100 mg) once a day
• Unable to tolerate ritonavir: 400 mg orally once a day
• In combination with efavirenz: 400 mg orally (with ritonavir 100 mg) once a day

Treatment-experienced (capsules)

• Recommended dose: 300 mg orally (with ritonavir 100 mg) once a day
• In combination with H2-receptor antagonist (H2RA) and tenofovir DF: 400 mg orally (with ritonavir 100 mg) once a day
• Not recommended for treatment-experienced adults without ritonavir coadministration
• Dosing during pregnancy and the postpartum period
• Administer atazanavir with ritonavir
• Treatment-naïve and treatment-experienced: 300 mg orally (with ritonavir 100 mg) once a day
• Treatment-experienced during the second or third trimester when coadministered with either H2RA OR tenofovir DF: 400 mg orally (with ritonavir 100 mg) once a day
• 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

Pediatric dosage

Oral capsules

• Children between 6-18 years (treatment naïve and treatment-experienced)
• Children below 15 kg: Capsules not recommended
• Children between 15 to below 35 kg: 200 mg orally (with ritonavir 100 mg) once a day
• Children above 35: 300 mg orally (with ritonavir 100 mg) once a day
• Children above 13 years (treatment naïve and cannot tolerate ritonavir)
• Children above 40 kg: 400 mg orally once a day

Oral powder

• Children below 3 months or below 5 kg: Safety and efficacy not established
• Children above 3 months and weigh above 5 kg
• Children between 5 kg to below 15 kg: 200 mg (4 packets) plus 80 mg ritonavir orally once a day
• 15 kg to below 25 kg: 250 mg (5 packets) plus 80 mg ritonavir orally once a day
• Above 25 kg and unable to swallow capsule: 300 mg (6 packets) plus 100 mg ritonavir orally once a day
• NOTE: Children unable to tolerate 200 mg/day dose who weigh 5 kg to below 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 below 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

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Atazanavir has severe interactions with at least 36 other drugs.
• Atazanavir has serious interactions with at least 149 other drugs.
• Atazanavir has moderate interactions with at least 304 other drugs.
• Atazanavir has minor interactions with at least 93 other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

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
• Amiodarone
• Quinidine
• Dihydroergotamine
• Ergotamine
• Ergonovine
• Methylergonovine
• Lomitapide

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Atazanavir?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Atazanavir?”

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; because of limited clinical experience with preexisting conduction system disease (.g, marked first-degree AV block or second- or third-degree AV block), ECG monitoring should be considered
• 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 post-marketing 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 before 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 were 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
• Autoimmune disorders (such as Graves’ disease, polymyositis, Guillain-Barré syndrome, and autoimmune hepatitis) have also been reported to occur in the setting of immune reconstitution; however, time to onset is more variable and can occur many months after initiation of treatment
• Patients with hepatitis B or C infection are at risk of increased transaminases or hepatic decompensation; monitor hepatic laboratory tests before 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

Pregnancy and Lactation

• 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 the risk of major birth defects overall compared to the 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 further the 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 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 the 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 analogs 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 the development of severe hyperbilirubinemia during the first few days of life
• Lactation
  • The Centres 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 is available regarding atazanavir effects on milk production; atazanavir was present in the 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 the potential for serious adverse reactions in breastfed infants, advise women not to breastfeed