Atazanavir

What is Atazanavir?

• Atazanavir (Reyataz) is a protease inhibitor used in combination with other antiretroviral agents for the treatment of HIV-1 infection.

Atazanavir structure

Atazanavir ball-and-stick

Atazanavir-skeletal

What are the uses of this medicine?

• Atazanavir (Reyataz) is a prescription medicine that is used to treat human immunodeficiency virus-1 (HIV-1) infection, in combination with other HIV-1 medicines in adults and children 3 months of age and older and who weigh at least 11 pounds (5 kg). HIV-1 is the virus that causes AIDS (Acquired Immunodeficiency Syndrome).

How does this medicine work?

• Atazanavir is an HIV-1 antiretroviral drug.
• Atazanavir (ATV) is an azapeptide HIV-1 protease inhibitor (PI).
• The compound selectively inhibits the virus-specific processing of viral Gag and Gag-Pol polyproteins in HIV-1 infected cells, thus preventing formation of mature virions.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergic to atazanavir or any of the ingredients in REYATAZ.

are taking any of the following medicines. Taking REYATAZ with these medicines may affect how REYATAZ works. REYATAZ may cause serious or life-threatening side effects, or death when used with these medicines:

• alfuzosin
• amiodarone (when REYATAZ is used with ritonavir)
• cisapride
• elbasvir and grazoprevir

• ergot medicines including:

1. dihydroergotamine
2. ergonovine
3. ergonovine ergotamine
4. methylergonovine

• glecaprevir and pibrentasvir
• indinavir
• irinotecan
• lurasidone (when REYATAZ is used with ritonavir)
• lomitapide
• lovastatin
• midazolam, when taken by mouth for sedation
• nevirapine
• pimozide
• quinidine (when REYATAZ is used with ritonavir)
• rifampin
• sildenafil, when used for the treatment of pulmonary arterial hypertension
• simvastatin
• St. John’s wort
• triazolam

What drug interactions can this medicine cause?

• Coadministration of REYATAZ can alter the concentration of other drugs and other drugs may alter the concentration of atazanavir.
• Coadministration with alfuzosin, amiodarone (if REYATAZ is coadministered with ritonavir), quinidine (if REYATAZ is coadministered with ritonavir), triazolam, orally administered midazolam, ergot derivatives, rifampin, irinotecan, lurasidone (if REYATAZ is coadministered with ritonavir), lovastatin, simvastatin, lomitapide, indinavir, cisapride, pimozide, St. John’s wort, nevirapine, elbasvir/grazoprevir, glecaprevir/pibrentasvir, and sildenafil when dosed as REVATIO® is contraindicated.

Is this medicine FDA approved?

• Atazanavir was approved for use in the United States in 2003 for the treatment of HIV infection and is typically given in combination with low “booster” doses of ritonavir or with the pharmacologic enhancer cobicistat, which improve its pharmacokinetics by inhibiting its metabolism by CYP 3A4.

How should this medicine be used?

• Renal laboratory testing should be performed in all patients prior to initiation of REYATAZ and continued during treatment with REYATAZ.
• Hepatic testing should be performed in patients with underlying liver disease prior to initiation of REYATAZ and continued during treatment with REYATAZ.

Recommended dosage:

• Treatment-naive adults: REYATAZ 300 mg with ritonavir 100 mg once daily with food or REYATAZ 400 mg once daily with food.
• Treatment-experienced adults: REYATAZ 300 mg with ritonavir 100 mg once daily with food.
• Pediatric patients: REYATAZ capsule dosage is based on body weight not to exceed the adult dose and must be taken with food.
• REYATAZ oral powder: Must be taken with ritonavir and food and should not be used in pediatric patients who weigh less than 5 kg.
• Pregnancy: REYATAZ 300 mg with ritonavir 100 mg once daily with food, with dosing modifications for some concomitant medications.

Dosage in Patients with Renal Impairment:

• For patients with renal impairment, including those with severe renal impairment who are not managed with hemodialysis, no dose adjustment is required for REYATAZ.
• Treatment-naive patients with end-stage renal disease managed with hemodialysis should receive REYATAZ 300 mg with ritonavir 100 mg.

Dosage Adjustments in Patients with Hepatic Impairment:

• Mild hepatic impairment: 400 mg
• Moderate hepatic impairment: 300 mg
• Severe hepatic impairment: REYATAZ with or without ritonavir is not recommended.

Administration:

• REYATAZ must be used with other HIV-1 medicines.
• Take REYATAZ 1 time each day.
• REYATAZ comes as capsules and oral powder.
• Take REYATAZ capsules and oral powder with food.
• Swallow the capsules whole. Do not open the capsules.
• REYATAZ oral powder must be mixed with food or liquid. Your child’s healthcare provider will prescribe the right dose of REYATAZ based on your child’s weight. See the detailed “Instructions for Use” that comes with REYATAZ oral powder for information about the correct way to mix and give a dose of REYATAZ oral powder to your child.
• REYATAZ oral powder must be taken with ritonavir.
• If you miss a dose of REYATAZ, take it as soon as you remember. Then take the next dose at your regular time. Do not take 2 doses at the same time.
• If you take too much REYATAZ, call your healthcare provider or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 150 mg, 200 mg, 300 mg.
• Oral powder: 50 mg packet.

This medicine is available in fallowing brand namesː

• REYATAZ

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea
• headache
• stomach-area pain
• vomiting
• trouble sleeping
• numbness, tingling, or burning of hands or feet
• dizziness
• muscle pain
• diarrhea
• depression
• fever

REYATAZ can cause serious side effects, including:

• heart rhythm change
• Skin rash
• Liver problems
• Chronic kidney disease
• Kidney stones
• Gallbladder stones
• Yellowing of your skin or the white part of your eyes
• hyperglycemia
• Immune Reconstitution Syndrome
• Changes in body fat
• Increased bleeding problems in people with hemophilia

What special precautions should I follow?

• 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.
• In controlled clinical trials, rash (all grades, regardless of causality) occurred in approximately 20% of subjects with HIV-1 infection treated with REYATAZ. Discontinue if severe rash develops.
• 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.
• Phenylalanine can be harmful to patients with phenylketonuria (PKU). REYATAZ oral powder contains phenylalanine (a component of aspartame). Each packet of REYATAZ oral powder contains 35 mg of phenylalanine. REYATAZ capsules do not contain phenylalanine.
• 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.
• Chronic kidney disease has been reported during postmarketing surveillance in patients with HIV-1 infection treated with atazanavir, with or without ritonavir. Consider alternatives in patients at high risk for renal disease or with preexisting renal disease. Monitor renal laboratory tests prior to therapy and during treatment. Consider discontinuation of REYATAZ in patients with progressive renal disease.
• Nephrolithiasis and cholelithiasis have been reported. Consider temporary interruption or discontinuation.
• The concomitant use of REYATAZ with ritonavir and certain other medications may result in known or potentially significant drug interactions. Consult the full prescribing information prior to and during treatment for potential drug interactions.
• Patients receiving REYATAZ may develop new onset or exacerbations of diabetes mellitus/hyperglycemia, immune reconstitution syndrome, and redistribution/accumulation of body fat.
• Spontaneous bleeding may occur and additional factor VIII may be required.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• asymptomatic bifascicular block
• PR interval prolongation
• jaundice
• hyperbilirubinemia
• PR interval prolongation

Management of overdosage:

• Treatment of overdosage with REYATAZ should consist of general supportive measures, including monitoring of vital signs and ECG, and observations of the patient’s clinical status.
• If indicated, elimination of unabsorbed atazanavir should be achieved by emesis or gastric lavage.
• Administration of activated charcoal may also be used to aid removal of unabsorbed drug.
• There is no specific antidote for overdose with REYATAZ. Since atazanavir is extensively metabolized by the liver and is highly protein bound, dialysis is unlikely to be beneficial in significant removal of this medicine.

Can this medicine be used in pregnancy?

• Available human and animal data suggest that atazanavir does not increase the risk of major birth defects overall compared to the background rate.
• There is a pregnancy exposure registry that monitors pregnancy outcomes in patients exposed to REYATAZ during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263.

Can this medicine be used in children?

• REYATAZ is indicated in combination with other antiretroviral agents for the treatment of pediatric patients with HIV-1 infection, 3 months of age and older weighing at least 5 kg.
• REYATAZ is not recommended for use in pediatric patients below the age of 3 months due to the risk of kernicterus.

What are the active and inactive ingredients in this medicine?

• Active ingredient: atazanavir sulfate
• Inactive ingredients:
• REYATAZ capsules: crospovidone, lactose monohydrate, and magnesium stearate. The capsule shells contain gelatin, FD&C Blue No. 2, titanium dioxide, black iron oxide, red iron oxide, and yellow iron oxide. The capsules are printed with ink containing shellac, titanium dioxide, FD&C Blue No. 2, isopropyl alcohol, ammonium hydroxide, propylene glycol, n-butyl alcohol, simethicone, and dehydrated alcohol.
• REYATAZ oral powder: aspartame, sucrose, and orange-vanilla flavor.

Who manufactures and distributes this medicine?

Distributed by:

• Bristol-Myers Squibb Company, Princeton, NJ USA.

What should I know about storage and disposal of this medication?

• Store REYATAZ oral powder at a temperature of 68°F to 86°F (20°C to 30°C).
• Store REYATAZ oral powder in the original packet. Do not open until ready to use.
• After REYATAZ oral powder is mixed with food or liquid, it may be kept at a temperature of 68°F to 86°F (20°C to 30°C) for up to 1 hour. Take REYATAZ oral powder within 1 hour after mixing with food or liquid.
• Keep REYATAZ oral powder and all medicines out of the reach of children.

Antiviral agents

Drugs for HIV Infection, in the Subclass Antiretroviral Agents

• Fusion Inhibitors (HIV)
  • Enfuvirtide, Maraviroc

• Integrase Inhibitors (HIV)
  • Dolutegravir, Elvitegravir, Raltegravir

• Monoclonal Antibodies
  • Ibalizumab

• Nonnucleoside Reverse Transcriptase Inhibitors (HIV)
  • Delavirdine, Efavirenz, Etravirine, Nevirapine, Rilpivirine

• Nucleoside Analogues (HIV)
  • Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zidovudine

• Protease Inhibitors (HIV)
  • Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir,Ritonavir, Saquinavir, Tipranavir

Drugs for Hepatitis B

• • Alpha Interferon, Adefovir, Emtricitabine, Entecavir, Lamivudine, Telbivudine, Tenofovir

Drugs for Hepatitis C

• Interferon Based Therapies
  • Alpha Interferon and Peginterferon, Ribavirin

HCV NS5A Inhibitors

• Daclatasvir, Elbasvir, Ledipasvir, Ombitasvir, Pibrentasvir, Velpatasvir

HCV NS5B (Polymerase) Inhibitors

• Dasabuvir, Sofosbuvir

HCV Protease Inhibitors

• Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir

Combination Therapies

• Epclusa, Harvoni, Mavyret, Technive, Viekira Pak, Vosevi, Zepatier

Drugs for Herpes Virus Infections (HSV, CMV, others)

• Acyclovir, Cidofovir, Famciclovir, Foscarnet, Ganciclovir, Valacyclovir, Valganciclovir

Drugs for Influenza

• Amantadine, Oseltamivir, Peramivir, Rimantadine, Zanamivir

• Dailymed label info on Atazanavir
• FDA Atazanavir

Atazanavir Resources
Latest articles Most recent articles Ongoing trials	Wikipedia