Reyataz (Atazanavir) - Complete Drug Information

Reyataz (Generic Atazanavir) is an anti-retroviral drug that belongs to the protease inhibitors.

  • It is used in the treatment of HIV-1 infection with other antiretroviral agents in patients ≥3 months weighing more than 5 kg

  • It is not recommended in pediatric patients <3 months due to the risk of kernicterus

Atazanavir Dose in Adults

Reyataz (Atazanavir) dose in the Treatment of HIV-1 infection:

  • Antiretroviral-naive patients:

    • dosage is Atazanavir 300 mg orally once daily plus ritonavir 100 mg or
    • cobicistat 150 mg orally once daily or
    • atazanavir 400 mg orally once daily in patients who are unable to tolerate ritonavir.
  • Antiretroviral-experienced patients:

    • Atazanavir 300 mg orally once daily plus ritonavir 100 mg or
    • cobicistat 150 mg orally once daily.
    •  Atazanavir is not given without ritonavir in antiretroviral-experienced patients with prior virologic failure.
  • Pregnant patients, antiretroviral-naive or experienced:

    • Atazanavir 300 mg orally once daily is given along with ritonavir 100 mg once daily.
    • Some experts increase the dose to atazanavir 400 mg once daily plus ritonavir 100 mg once daily in the second and third trimesters.
    • It should not be used if both tenofovir disoproxil fumarate and an H2 antagonist are used.
    • Postpartum dosage adjustment is not required.
    • Observe patient for side effects, especially within 2 months after delivery.

Dosage adjustments for concomitant therapy:

  • Coadministration with efavirenz:

    • Antiretroviral-naive patients:

      • Atazanavir 400 mg + ritonavir 100 mg + efavirenz 600 mg
      • All are given once daily but at different times
      • Atazanavir and ritonavir should be given with food and efavirenz on an empty stomach.
    • Antiretroviral-experienced patients:

      • Synchronous use not recommended due to decreased atazanavir exposure.
  • Administration with didanosine buffered or enteric-coated formulations:

    • Give atazanavir 2 hours before or 1 hour after didanosine
  • Coadministration with H2 antagonists:

    • Antiretroviral-naive patients:

      • Atazanavir 300 mg + ritonavir 100 mg
      • It is given simultaneously, or at least 10 hours after an H2 antagonist equivalent dose of less than 80 mg famotidine/day
    • Patients unable to tolerate ritonavir:

      • Atazanavir 400 mg once daily
      • It is given at least 2 hours before or at least 10 hours after an H2 antagonist equivalent daily dose of less than 40 mg famotidine
    • Antiretroviral-experienced patients:

      • Atazanavir 300 mg + ritonavir 100 mg
      • It is given simultaneously  or at least 10 hours after an H2 antagonist equivalent dose of ≤40 mg famotidine/day
    • Antiretroviral-experienced pregnant patients in the second or third trimester:

      • Atazanavir 400 mg + ritonavir 100 mg is given simultaneously with, or at least 10 hours after an H antagonist.
  • Co-administration with proton pump inhibitors:

    • Antiretroviral-naive patients:

      • Atazanavir 300 mg plus ritonavir 100 mg is given 12 hours after a proton pump inhibitor equivalent dose of ≤20 mg omeprazole/day
    • Antiretroviral-experienced patients:

      • Concurrent use not advised.
  • Co-administration with tenofovir disoproxil fumarate:

    • Antiretroviral-naive patients:

    • Antiretroviral-experienced patients:

      • Atazanavir 300 mg + ritonavir 100 mg given with tenofovir disoproxil fumarate 300 mg
      • If H2 antagonist coadministered then  increase atazanavir to 400 mg (plus ritonavir 100 mg) once daily
    • Antiretroviral-experienced pregnant patients in the second or third trimester:

      • Atazanavir 400 mg + ritonavir 100 mg.

Atazanavir Dose in Childrens

Reyataz (Atazanavir) dose in the treatment of HIV-1 infection:

  • It should be used in combination with other antiretroviral agents.
  • ritonavir-boosted regimen (preferred regimen): Antiretroviral-naïve and experienced patients:

  • Oral powder:

    • Infants ≥3 months, Children, and Adolescents: Oral:
    • 5 - 15 kg:

      • Atazanavir 200 mg along with ritonavir 80 mg once daily.
      • In antiretroviral-naïve patients weighing 5 -10 kg unable to tolerate this dose, can use atazanavir 150 mg + ritonavir 80 mg once daily with close HIV viral load monitoring.
    • 15 to <25 kg:

      • Atazanavir 250 mg  plus ritonavir 80 mg once daily
    • ≥25 kg:
      • Atazanavir 300 mg plus ritonavir 100 mg once daily

Oral capsule:

  • Children ≥6 years and Adolescents <18 years weighing ≥15 kg: Oral:
    • 15 kg to <35 kg:
      • Atazanavir 200 mg plus ritonavir 100 mg once daily
    • ≥35 kg:
      • Atazanavir 300 mg along with ritonavir 100 mg once daily
  • Adolescents ≥18 years:

    • Atazanavir 300 mg orally once daily along with ritonavir 100 mg or cobicistat 150 mg once daily
  • Ritonavir unboosted regimen:

    • The ritonavir-boosted atazanavir dosing regimen is favored
    • Guidelines do not recommend unboosted regimens.
    • The oral powder is not used for unboosted regimens.
  • Antiretroviral-naïve patients: Oral capsule:

    • Adolescents weighing ≥40 kg who are not able to tolerate ritonavir: Oral:

      • 13 to <18 years:

        • Atazanavir 620 mg/m /dose once daily (without ritonavir);
        • Plasma concentrations should be monitored to ensure adequate concentrations are achieved.
  • Adolescents ≥18 years:
    • Atazanavir 400 mg once daily
  • Dosing adjustments for concomitant therapy:

    • Coadministration with didanosine buffered or enteric-coated formulations:

      • Infants ≥3 months, Children, and Adolescents:
        • Give atazanavir 2 hours before or 1 hour after didanosine​​​​​​​
  • Coadministration with H2 -receptor antagonists:

    • Antiretroviral-naïve patients:

      • Infants ≥3 months, Children, and Adolescents:
        • The daily dose of atazanavir plus ritonavir should be given at the same time or at least 10 hours after, the H - receptor antagonist
    • Patients unable to tolerate ritonavir:

      • Adolescents ≥18 years:
        • Atazanavir 400 mg is given once daily given at least 2 hours before or at least 10 hours after an H antagonist
    • Antiretroviral-experienced patients:

      • Infants ≥3 months, Children, and Adolescents:
        • The daily dose of atazanavir is given along with ritonavir simultaneously with, or at least 10 hours after, the H -receptor antagonist
  • Coadministration with proton pump inhibitor:

    • Antiretroviral-naïve patients:

      • Infants ≥3 months, Children, and Adolescents:
        • The daily dose of atazanavir is given along with ritonavir 12 hours after the proton pump inhibitor
    • Antiretroviral-experienced patients:

      • Concurrent use not advised
  • Co-administration with efavirenz:

    • Adolescents ≥18 years:
      • Antiretroviral-naive patient:

        • Atazanavir 400 mg is given along with ritonavir 100 mg given + efavirenz 600 mg
        • All are given  once daily but at different times
        • Atazanavir and ritonavir should be given with food and efavirenz on an empty stomach.
      • Antiretroviral-experienced patients:

        • Concurrent use not advised due to decreased atazanavir exposure
  • Coadministration with tenofovir disoproxil fumarate:

    • Adolescents ≥18 years:
      • Antiretroviral-naïve patients:

      • Antiretroviral-experienced patients:

        • Atazanavir 300 mg plus ritonavir 100 mg given with tenofovir 300 mg

Reyataz (Atazanavir) pregnancy Risk Factor: B

  • Atazanavir crosses the human placenta at very low levels.
  • Cord blood concentrations were reported to be between 13% and 21% of maternal serum concentrations during delivery.
  • There has been no evidence of an increased risk for teratogenic effects.
  • Preterm births are more likely to occur when a mother is taking antiretroviral medication.
  • There has been an increase in stillbirths, low birth weights, and infants of small gestational age have been observed.
  • Because of the potential for adverse neonatal outcomes, maternal ART should never be stopped.
  • All infants who have been exposed to antiretroviral medication should be followed up for a long time.
  • Children with significant organ system abnormalities (especially the heart or CNS) should be examined for possible mitochondrial dysfunction.
  • Protease inhibitors are used to treat hyperglycemia, diabetes mellitus new onset, and diabetic ketoacidosis. It isn't known if this increases with pregnancy.
  • Neonatal exposure to atazanavir in utero can lead to hyperbilirubinemia and hypoglycemia.
  • Atazanavir, when combined with low-dose ritonavir, is the preferred protease inhibitor for HIV infected pregnant women who are antiretroviral naive (initial treatment), who have received ART therapy previously but need to restart, who have poor tolerance or poor virologic responses to current regimens, and who are not yet pregnant but trying to conceive.
  • Atazanavir is not used in treatment-experienced pregnant females using both H - receptor blockers and tenofovir.
  • Experts recommend that you take higher doses in the second and third trimesters.
  • It is possible to monitor therapeutic drug use.
  • To keep HIV-positive pregnant women under the age of 18 from contracting perinatal HIV, it is strongly recommended that they receive ART.
  • Monitoring during pregnancy is more frequent than monitoring in nonpregnant women.
  • All HIV-positive females should continue ART postpartum. ART can also be modified after birth

Reyataz (Atazanavir) use during breastfeeding:

  • Atazanavir can be found in breast milk and is 13% higher than in maternal plasma.
  • The risk of HIV transmission after birth does not disappear with infant or maternal antiretroviral treatment.
  • To reduce the risk of HIV transmission, pregnant women with HIV should stop breastfeeding.

Atazanavir Dose in Renal Disease:

  • Mild to severe impairment:

    • No dosage adjustment required.
  • ESRD receiving IHD:

    • In patients with ESRD managed with hemodialysis, atazanavir is not mainly removed during hemodialysis.
  • Antiretroviral-naive patients:

    • Atazanavir 300 mg plus ritonavir 100 mg once daily
  • Antiretroviral-experienced patients:

    • Not used.

Atazanavir Dose in Liver Disease:

  • Atazanavir: Antiretroviral-naive patients:

    • Mild impairment (Child-Pugh class A):

      • Atazanavir 400 mg once daily
    • Moderate impairment (Child-Pugh class B):

      • Atazanavir 300 mg once daily
    • Severe impairment (Child-Pugh class C):

      • Use is not recommended.
  • Atazanavir/ritonavir:

    • Mild to severe impairment: Use is not recommended (has not been studied).

Common Side Effects of Reyataz (Atazanavir) Include:

  • Dermatologic:

    • Skin Rash
  • Endocrine & Metabolic:

    • Increased Serum Cholesterol
    • Increased Amylase
  • Gastrointestinal:

    • Nausea
  • Hepatic:

    • Increased Serum Bilirubin
    • Jaundice
  • Neuromuscular & Skeletal:

    • Increased Creatine Phosphokinase
  • Respiratory:

    • Cough
  • Miscellaneous:

    • Fever

Less common side effects of Reyataz (Atazanavir) Include:

  • Cardiovascular:

    • Peripheral Edema
    • First Degree Atrioventricular Block
    • Second Degree Atrioventricular Block
  • Central Nervous System:

    • Headache
    • Peripheral Neuropathy
    • Insomnia
    • Depression
    • Dizziness
  • Endocrine & Metabolic:

    • Increased Serum Triglycerides
    • Hyperglycemia
    • Hypoglycemia
  • Gastrointestinal:

    • Vomiting
    • Diarrhea
    • Increased Serum Lipase
    • Abdominal Pain
  • Hematologic & Oncologic:

    • Decreased Neutrophils
    • Decreased Hemoglobin
    • Decreased Platelet Count
  • Hepatic:

    • Increased Serum ALT
    • Increased Serum AST
  • Neuromuscular & Skeletal:

    • Myalgia
    • Limb Pain
  • Respiratory:

    • Nasal Congestion
    • Oropharyngeal Pain
    • Rhinorrhea
    • Wheezing

Contraindication to Reyataz (Atazanavir) Include:

  • Hypersensitivity to atazanavir (or any other component of the medicine) can result in Stevens-Johnson Syndrome, erythema multife, and skin eruptions.
  • Therapy along with with alfuzosin, cisapride, elbasvir/grazoprevir, glecaprevir/ pibrentasvir, ergot derivatives, indinavir, irinotecan, lovastatin, lurasidone (when atazanavir is coadministered with ritonavir), midazolam (oral), nevirapine, pimozide, rifampin, sildenafil (when used for pulmonary artery hypertension [eg, Revatio]), simvastatin, St. John's wort, or triazolam

Warnings and precautions

  • Elevated Bilirubin

    • Asymptomatic increases in unconjugated bilirubin can occur frequently during therapy. They are easily reversed once treatment is stopped.
    • If bilirubin elevations are associated with jaundice, scleral inflammation or jaundice, consider alternative treatment.
    • If transaminase elevations occur, consider other causes.
  • Fat redistribution

    • It can lead to redistribution and accumulation of fat (eg central obesity, buffalo-hump, peripheral waste, breast enlargement or cushingoid appearance).
  • Hypersensitivity reactions

    • A number of hypersensitivity events are also caused by protease inhibitors.
    • If severe rash occurs or moderate symptoms are present, it is a good idea to discontinue treatment.
  • Immune reconstitution syndrome:

    • Some patients may develop immune reconstitution syndrome, which can cause an inflammatory response to an infection.
    • This could occur during initial HIV treatment, or activation of autoimmune disorders later on in therapy.
  • Nephrolithiasis/cholelithiasis:

    • Postmarketing surveillance can reveal gallstones and renal problems.
    • If symptoms persist, you may consider a temporary or permanent suspension of therapy.
  • Conductivity abnormalities

    • It can extend the PR interval
    • Patients with conduction abnormalities or medications that prolong AV conduction should have their ECG monitored.
  • Diabetes:

    • There are also changes in glucose tolerance, hyperglycemia and exacerbation or new-onset diabetes mellitus.
  • Hemophilia A and B:

    • Patients with hemophilia A and B should not use it.
  • Hepatic impairment

    • Hepatitis can also be caused by protease inhibitors.
    • Patients with severe hepatic impairment should not use this product.
    • When hepatic impairment exists, it is not recommended that patients take it with ritonavir.
  • Renal impairment

    • Postmarketing surveillance has shown cases of chronic kidney disease.
    • Patients at risk of renal impairment or who have preexisting renal disease should consider alternative therapies.
    • Before starting treatment, it is important to have renal laboratory testing done (serum creatinine and estimated CrCl)
    • It is not recommended for use in treatment-experienced patients with ESRD on hemodialysis.
    • Patients with progressive kidney disease should stop receiving therapy.

Atazanavir: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy)

Abacavir Protease Inhibitors may decrease the serum concentration of Abacavir.
Alosetron CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alosetron.
Amiodarone Atazanavir may increase the serum concentration of Amiodarone.
AmLODIPine CYP3A4 Inhibitors (Strong) may increase the serum concentration of AmLODIPine.
Antidiabetic Agents Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents.
Apixaban CYP3A4 Inhibitors (Strong) may increase the serum concentration of Apixaban.
Benperidol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Benperidol.
Benzhydrocodone CYP3A4 Inhibitors (Strong) may increase the serum concentration of Benzhydrocodone. Specifically, the concentration of hydrocodone may be increased.
Betamethasone (Ophthalmic) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Betamethasone (Ophthalmic).
Bictegravir CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bictegravir.
Bortezomib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bortezomib.
Brentuximab Vedotin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Brentuximab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be increased.
Brinzolamide CYP3A4 Inhibitors (Strong) may increase the serum concentration of Brinzolamide.
Budesonide (Nasal) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Nasal).
Budesonide (Oral Inhalation) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Oral Inhalation).
Calcifediol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Calcifediol.
Cannabidiol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cannabidiol.
Cannabis CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cannabis. More specifically, tetrahydrocannabinol and cannabidiol serum concentrations may be increased.
Cinacalcet CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cinacalcet.
Clofazimine May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
CloZAPine CYP3A4 Inhibitors (Strong) may increase the serum concentration of CloZAPine. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Codeine CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Codeine.
Corticosteroids (Orally Inhaled) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Corticosteroids (Orally Inhaled). Management: Orally inhaled fluticasone propionate with a strong CYP3A4 inhibitor is not recommended. Exceptions: Beclomethasone (Oral Inhalation); Triamcinolone (Systemic).
Corticosteroids (Systemic) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Corticosteroids (Systemic). Exceptions: MethylPREDNISolone; PrednisoLONE (Systemic); PredniSONE.
Cyclophosphamide Protease Inhibitors may enhance the adverse/toxic effect of Cyclophosphamide. Specifically, the incidences of neutropenia, infection, and mucositis may be increased.
CYP3A4 Inducers (Moderate) May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
CYP3A4 Inhibitors (Moderate) May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors).
Dapsone (Systemic) May enhance the adverse/toxic effect of Atazanavir. Specifically, the risk of hyperbilirubinemia may be increased.
Deferasirox May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Dexamethasone (Ophthalmic) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dexamethasone (Ophthalmic).
Disulfiram Atazanavir may diminish the therapeutic effect of Disulfiram.
Dofetilide CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
Doxercalciferol CYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Doxercalciferol.
Dronabinol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dronabinol.
Dutasteride CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dutasteride.
Enfuvirtide Protease Inhibitors may increase the serum concentration of Enfuvirtide. Enfuvirtide may increase the serum concentration of Protease Inhibitors.
Estazolam CYP3A4 Inhibitors (Strong) may increase the serum concentration of Estazolam.
Estrogen Derivatives CYP3A4 Inhibitors (Strong) may increase the serum concentration of Estrogen Derivatives.
Evogliptin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Evogliptin.
Fosnetupitant May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Fostamatinib CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Fostamatinib.
Galantamine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Galantamine.
Gefitinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Gefitinib.
HYDROcodone CYP3A4 Inhibitors (Strong) may increase the serum concentration of HYDROcodone.
Ifosfamide CYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Ifosfamide.
Imatinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Imatinib.
Imidafenacin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Imidafenacin.
Lacosamide CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lacosamide.
LamoTRIgine Atazanavir may decrease the serum concentration of LamoTRIgine.
Levobupivacaine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Levobupivacaine.
Lumefantrine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lumefantrine.
Minocycline May decrease the serum concentration of Atazanavir.
Minoxidil (Systemic) Atazanavir may increase the serum concentration of Minoxidil (Systemic).
Naldemedine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Naldemedine.
Nalfurafine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Nalfurafine.
Netupitant May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Orlistat May decrease the serum concentration of Antiretroviral Agents.
Ospemifene CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ospemifene.
Oxybutynin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Oxybutynin.
Parecoxib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Parecoxib.
Paricalcitol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Paricalcitol.
Pimecrolimus CYP3A4 Inhibitors (Strong) may decrease the metabolism of Pimecrolimus.
Pitavastatin Atazanavir may increase the serum concentration of Pitavastatin.
Posaconazole May increase the serum concentration of Atazanavir.
Pranlukast CYP3A4 Inhibitors (Strong) may increase the serum concentration of Pranlukast.
Praziquantel CYP3A4 Inhibitors (Strong) may increase the serum concentration of Praziquantel.
PrednisoLONE (Systemic) CYP3A4 Inhibitors (Strong) may increase the serum concentration of PrednisoLONE (Systemic).
PredniSONE CYP3A4 Inhibitors (Strong) may increase the serum concentration of PredniSONE.
Propafenone CYP3A4 Inhibitors (Strong) may increase the serum concentration of Propafenone. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
QuiNIDine Atazanavir may increase the serum concentration of QuiNIDine.
Ramelteon CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ramelteon.
Retapamulin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Retapamulin. Management: Avoid this combination in patients less than 2 years old. No action is required in other populations.
Rilpivirine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Rilpivirine.
RomiDEPsin CYP3A4 Inhibitors (Strong) may increase the serum concentration of RomiDEPsin.
Rosiglitazone Atazanavir may increase the serum concentration of Rosiglitazone.
Sarilumab May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Siltuximab May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
SORAfenib CYP3A4 Inhibitors (Strong) may increase the serum concentration of SORAfenib.
Tacrolimus (Topical) Protease Inhibitors may decrease the metabolism of Tacrolimus (Topical).
Talazoparib BCRP/ABCG2 Inhibitors may increase the serum concentration of Talazoparib.
Tasimelteon CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tasimelteon.
Tetrahydrocannabinol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tetrahydrocannabinol.
Tetrahydrocannabinol and Cannabidiol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tetrahydrocannabinol and Cannabidiol.
Tocilizumab May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
TraMADol CYP3A4 Inhibitors (Strong) may increase the serum concentration of TraMADol.
Tricyclic Antidepressants Protease Inhibitors may increase the serum concentration of Tricyclic Antidepressants.
Valproate Products Protease Inhibitors may decrease the serum concentration of Valproate Products.
Vilanterol May increase the serum concentration of CYP3A4 Inhibitors (Strong).
Vindesine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vindesine.
Vinorelbine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vinorelbine.
Warfarin Atazanavir may increase the serum concentration of Warfarin.
Zidovudine Protease Inhibitors may decrease the serum concentration of Zidovudine.
Zolpidem CYP3A4 Inhibitors (Strong) may increase the serum concentration of Zolpidem.

Risk Factor D (Consider therapy modification)

Abemaciclib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Abemaciclib. Management: In patients taking abemaciclib at a dose of 200 mg or 150 mg twice daily, reduce the dose to 100 mg twice daily when combined with strong CYP3A4 inhibitors. In patients taking abemaciclib 100 mg twice daily, decrease the dose to 50 mg twice daily.
Alitretinoin (Systemic) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alitretinoin (Systemic). Management: Consider reducing the alitretinoin dose to 10 mg when used together with strong CYP3A4 inhibitors. Monitor for increased alitretinoin effects/toxicities if combined with a strong CYP3A4 inhibitor.
Almotriptan CYP3A4 Inhibitors (Strong) may increase the serum concentration of Almotriptan. Management: Limit initial almotriptan adult dose to 6.25 mg and maximum adult dose to 12.5 mg/24-hrs when used with a strong CYP3A4 inhibitor. Avoid concurrent use in patients with impaired hepatic or renal function.
ALPRAZolam CYP3A4 Inhibitors (Strong) may increase the serum concentration of ALPRAZolam. Management: Consider using an alternative agent that is less likely to interact. If combined, monitor for increased therapeutic/toxic effects of alprazolam if combined with a strong CYP3A4 inhibitor.
Antacids May decrease the absorption of Atazanavir.
ARIPiprazole CYP3A4 Inhibitors (Strong) may increase the serum concentration of ARIPiprazole. Management: See full interaction monograph for details.
ARIPiprazole Lauroxil CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of ARIPiprazole Lauroxil. Management: Please refer to the full interaction monograph for details concerning the recommended dose adjustments.
AtorvaSTATin Protease Inhibitors may increase the serum concentration of AtorvaSTATin. Management: See full monograph for recommended dose limits. Avoid atorvastatin with tipranavir/ritonavir.
Bedaquiline CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bedaquiline. Management: Limit duration of concurrent use of bedaquiline with CYP3A4 inhibitors to no more than 14 days, unless the benefit of continued use outweighs the possible risks. Monitor for toxic effects of bedaquiline. Exceptions discussed in separate monographs.
Bosentan May decrease the serum concentration of Atazanavir. Atazanavir may increase the serum concentration of Bosentan. Management: Concurrent use of atazanavir (without ritonavir) and bosentan is not recommended. Bosentan dose adjustments are required when used together with atazanavir/ritonavir.
Brexpiprazole CYP3A4 Inhibitors (Strong) may increase the serum concentration of Brexpiprazole. Management: Reduce brexpiprazole dose to 50% of usual with a strong CYP3A4inhibitor; reduce to 25% of usual if used with both a moderate CYP3A4 inhibitor and a CYP2D6 inhibitor, or if a strong CYP3A4 inhibitor is used in a CYP2D6 poor metabolizer.
Brigatinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Brigatinib. Management: Avoid concurrent use of brigatinib with strong CYP3A4 inhibitors when possible. If combination cannot be avoided, reduce the brigatinib dose by approximately 50%, rounding to the nearest tablet strength (ie, from 180 mg to 90 mg, or from 90 mg to 60 mg).
Budesonide (Topical) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Topical). Management: Per US prescribing information, avoid this combination. Canadian product labeling does not recommend strict avoidance. If combined, monitor for excessive glucocorticoid effects as budesonide exposure may be increased.
BusPIRone CYP3A4 Inhibitors (Strong) may increase the serum concentration of BusPIRone. Management: Limit the buspirone dose to 2.5 mg daily and monitor patients for increased buspirone effects/toxicities if combined with strong CYP3A4 inhibitors.
Cabazitaxel CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cabazitaxel. Management: Concurrent use of cabazitaxel with strong inhibitors of CYP3A4 should be avoided when possible. If such a combination must be used, consider a 25% reduction in the cabazitaxel dose.
Cabozantinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cabozantinib. Management: Avoid use of a strong CYP3A4 inhibitor with cabozantinib if possible. If combined, cabozantinib dose adjustments are recommended and vary based on the cabozantinib product used and the indication for use. See monograph for details.
Calcium Channel Blockers (Nondihydropyridine) Protease Inhibitors may decrease the metabolism of Calcium Channel Blockers (Nondihydropyridine). Increased serum concentrations of the calcium channel blocker may increase risk of AV nodal blockade. Management: Avoid concurrent use when possible. If used, monitor for CCB toxicity. The manufacturer of atazanavir recommends a 50% dose reduction for diltiazem be considered. Saquinavir, tipranavir, and darunavir/cobicistat use with bepridil is contraindicated.
CarBAMazepine May increase the metabolism of Protease Inhibitors. Protease Inhibitors may decrease the metabolism of CarBAMazepine.
Cariprazine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cariprazine. Management: Cariprazine dose reductions of 50% are required; specific recommended management varies slightly for those stable on cariprazine versus those just starting cariprazine. See prescribing information or full interaction monograph for details.
Ceritinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ceritinib. Management: If such combinations cannot be avoided, the ceritinib dose should be reduced by approximately one-third (to the nearest 150 mg). Resume the prior ceritinib dose after cessation of the strong CYP3A4 inhibitor. Exceptions discussed in separate monographs.
Cilostazol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol. Management: Consider reducing the cilostazol dose to 50 mg twice daily in adult patients who are also receiving strong inhibitors of CYP3A4.
Cladribine BCRP/ABCG2 Inhibitors may increase the serum concentration of Cladribine. Management: Avoid concomitant use of BCRP inhibitors during the 4 to 5 day oral cladribine treatment cycles whenever possible. If combined, consider dose reduction of the BCRP inhibitor and separation in the timing of administration.
Clarithromycin Protease Inhibitors may diminish the therapeutic effect of Clarithromycin. Specifically, certain protease inhibitors may decrease formation of the active 14-hydroxyclarithromycin metabolite, which may negatively impact clarithromycin effectiveness vs. H. influenzae and other non-MAC infections. Protease Inhibitors may increase the serum concentration of Clarithromycin. Clarithromycin dose adjustment in renally impaired patients may be needed. Clarithromycin may increase the serum concentration of Protease Inhibitors. Management: Saquinavir is contraindicated with clarithromycin. Avoid clarithromycin adult doses over 1000 mg/day with a protease inhibitor. Further dose reductions may be needed with impaired renal function. Consider alternative antimicrobial for a non-MAC infection.
Colchicine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Colchicine. Management: Colchicine is contraindicated in patients with impaired renal or hepatic function who are also receiving a strong CYP3A4 inhibitor. In those with normal renal and hepatic function, reduce colchicine dose as directed. See full monograph for details.
Copanlisib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Copanlisib. Management: If concomitant use of copanlisib and strong CYP3A4 inhibitors cannot be avoided, reduce the copanlisib dose to 45 mg. Monitor patients for increased copanlisib effects/toxicities.
Crizotinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Crizotinib. Management: Avoid concomitant use of crizotinib and strong CYP3A4 inhibitors whenever possible. If combined use cannot be avoided, decrease the crizotinib dose to 250 mg daily. Exceptions are discussed in separate monographs.
CycloSPORINE (Systemic) Protease Inhibitors may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Protease Inhibitors.
CycloSPORINE (Systemic) CYP3A4 Inhibitors (Strong) may increase the serum concentration of CycloSPORINE (Systemic).
CYP3A4 Inducers (Strong) May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling.
CYP3A4 Inhibitors (Strong) May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors).
CYP3A4 Substrates (High risk with Inhibitors) CYP3A4 Inhibitors (Strong) may decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Exceptions: Alitretinoin (Systemic); AmLODIPine; Benzhydrocodone; Buprenorphine; Gefitinib; HYDROcodone; Praziquantel; Telithromycin; Vinorelbine.
Daclatasvir CYP3A4 Inhibitors (Strong) may increase the serum concentration of Daclatasvir. Management: Decrease the daclatasvir dose to 30 mg once daily if combined with a strong CYP3A4 inhibitor. No dose adjustment is needed when daclatasvir is used with darunavir/cobicistat.
Dasatinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib. Management: This combination should be avoided if possible. If combined, dasatinib dose reductions are recommended. See full monograph for details. Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Deflazacort CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Deflazacort. Management: Administer one third of the recommended deflazacort dose when used together with a strong or moderate CYP3A4 inhibitor.
Delamanid CYP3A4 Inhibitors (Strong) may increase the serum concentration of Delamanid. Management: Increase ECG monitoring frequency if delamanid is combined with strong CYP3A4 inhibitors due to the risk for QTc interval prolongation. Continue frequent ECG assessments throughout full delamanid treatment period. Exceptions discussed separately.
Delavirdine Protease Inhibitors may decrease the serum concentration of Delavirdine. Delavirdine may increase the serum concentration of Protease Inhibitors.
Didanosine May decrease the serum concentration of Atazanavir. Specifically, the buffered formulation of didanosine may decrease atazanavir absorption. Atazanavir may decrease the serum concentration of Didanosine. Reported with enteric coated didanosine capsules. Management: To avoid therapeutic failure of atazanavir the drug should be administered 2 hours before or 1 hour after didanosine. This recommendation applies to both buffered didanosine products and enteric coated didanosine products.
DOCEtaxel CYP3A4 Inhibitors (Strong) may increase the serum concentration of DOCEtaxel. Management: Avoid the concomitant use of docetaxel and strong CYP3A4 inhibitors when possible. If combined use is unavoidable, consider a 50% docetaxel dose reduction and monitor for increased docetaxel toxicities.
DOXOrubicin (Conventional) CYP3A4 Inhibitors (Strong) may increase the serum concentration of DOXOrubicin (Conventional). Management: Seek alternatives to strong CYP3A4 inhibitors in patients treated with doxorubicin whenever possible. One U.S. manufacturer (Pfizer Inc.) recommends that these combinations be avoided.
Drospirenone CYP3A4 Inhibitors (Strong) may increase the serum concentration of Drospirenone. Management: Drospirenone use is contraindicated specifically when the strong CYP3A4 inhibitors atazanavir and cobicistat are administered concurrently. Caution should be used when drospirenone is coadministered with other strong CYP3A4 inhibitors.
Duvelisib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Duvelisib. Management: Reduce the dose of duvelisib to 15 mg twice a day when used together with a strong CYP3A4 inhibitor.
Efavirenz May decrease the serum concentration of Atazanavir. Management: When used with efavirenz, the adult atazanavir dose should be 400 mg daily, boosted with ritonavir 100 mg daily or cobicistat 150 mg daily, for treatment-naive patients only; treatment-experienced patients should not use atazanavir with efavirenz.
Eliglustat CYP3A4 Inhibitors (Strong) may increase the serum concentration of Eliglustat. Management: Use should be avoided under some circumstances. See full drug interaction monograph for details.
Eluxadoline Atazanavir may increase the serum concentration of Eluxadoline. Management: Decrease the eluxadoline dose to 75 mg twice daily if combined with atazanavir and monitor patients for increased eluxadoline effects/toxicities.
Elvitegravir Atazanavir may increase the serum concentration of Elvitegravir. Specifically, atazanavir/ritonavir may increase the concentration of elvitegravir. Management: When elvitegravir is combined with atazanavir/ritonavir, the dose of elvitegravir should be reduced to 85 mg once daily and the dose of atazanavir/ritonavir should be 300 mg/100 mg once daily. Avoid the use of atazanavir/cobicistat and elvitegravir.
Encorafenib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Encorafenib. Management: Avoid concomitant use of encorafenib and strong CYP3A4 inhibitors whenever possible. If concomitant administration is unavoidable, decrease the encorafenib dose to onethird of the encorafenib dose used prior to initiation of the strong CYP3A4 inhibitor.
Enzalutamide May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring.
Erlotinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Erlotinib. Management: Avoid use of this combination when possible. When the combination must be used, monitor the patient closely for the development of severe adverse reactions, and if such severe reactions occur, reduce the erlotinib dose (in 50 mg decrements).
Estrogen Derivatives (Contraceptive) Protease Inhibitors may decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Use oral contraceptives containing at least 35mcg ethinyl estradiol with atazanavir/ritonavir, or no more than 30mcg in patients receiving atazanavir alone. Use of an alternative, non-hormonal contraceptive is recommended with other protease inhibitors.
Eszopiclone CYP3A4 Inhibitors (Strong) may increase the serum concentration of Eszopiclone. Management: Limit the eszopiclone dose to 2 mg daily when combined with strong CYP3A4 inhibitors and monitor for increased eszopiclone effects and toxicities (eg, somnolence, drowsiness, CNS depression).
Etizolam CYP3A4 Inhibitors (Strong) may increase the serum concentration of Etizolam. Management: Consider use of lower etizolam doses when using this combination; specific recommendations concerning dose adjustment are not available. Monitor clinical response to the combination closely.
Etravirine Atazanavir may increase the serum concentration of Etravirine. Etravirine may decrease the serum concentration of Atazanavir. Management: The combination of etravirine and atazanavir should be avoided unless atazanavir is boosted with ritonavir. The use of cobicistat instead of ritonavir has not been evaluated and is not recommended.
FentaNYL CYP3A4 Inhibitors (Strong) may increase the serum concentration of FentaNYL. Management: Monitor patients closely for several days following initiation of this combination, and adjust fentanyl dose as necessary.
Fesoterodine CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Fesoterodine. Management: Avoid fesoterodine doses greater than 4 mg daily in adult patients who are also receiving strong CYP3A4 inhibitors.
Fluticasone (Oral Inhalation) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Fluticasone (Oral Inhalation). Management: Use of orally inhaled fluticasone propionate with strong CYP3A4 inhibitors is not recommended. Use of orally inhaled fluticasone furoate with strong CYP3A4 inhibitors should be done with caution. Monitor patients using such a combination more closely.
Fluvastatin Atazanavir may increase the serum concentration of Fluvastatin.
Garlic May decrease the serum concentration of Protease Inhibitors. Management: Concurrent use of garlic supplements with protease inhibitors is not recommended. If this combination is used, monitor closely for altered serum concentrations/effects of protease inhibitors, and particularly for signs/symptoms of therapeutic failure.
Gilteritinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Gilteritinib. Management: Consider alternatives to the use of a strong CYP3A4 inhibitor with gilteritinib. If the combination cannot be avoided, monitor more closely for evidence of gilteritinib toxicities.
Glasdegib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Glasdegib. Management: Consider alternatives to this combination when possible. If the combination must be used, monitor closely for evidence of QT interval prolongation and other adverse reactions to glasdegib.
GuanFACINE CYP3A4 Inhibitors (Strong) may increase the serum concentration of GuanFACINE. Management: Reduce the guanfacine dose by 50% when initiating this combination.
Histamine H2 Receptor Antagonists May decrease the serum concentration of Atazanavir. Management: Specific dose limitations and administration guidelines exist; consult full interaction monograph or atazanavir prescribing information.
Iloperidone CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolites P88 and P95 may be increased. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Iloperidone. Management: Reduce iloperidone dose by half when administered with a strong CYP3A4 inhibitor.
Ivacaftor CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ivacaftor. Management: Ivacaftor dose reductions are required; consult full monograph content for specific age- and weight-based recommendations.
Ivosidenib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ivosidenib. Management: Avoid use of a strong CYP3A4 inhibitor with ivosidenib whenever possible. When combined use is required, reduce the ivosidenib dose to 250 mg once daily. Drugs listed as exceptions are discussed in further detail in separate drug interaction monographs.
Ixabepilone CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ixabepilone.
Larotrectinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Larotrectinib. Management: Avoid use of strong CYP3A4 inhibitors with larotrectinib. If this combination cannot be avoided, reduce the larotrectinib dose by 50%. Increase to previous dose after stopping the inhibitor after a period of 3 to 5 times the inhibitor half-life.
Levomilnacipran CYP3A4 Inhibitors (Strong) may increase the serum concentration of Levomilnacipran. Management: Do not exceed a maximum adult levomilnacipran dose of 80 mg/day in patients also receiving strong CYP3A4 inhibitors.
Lorlatinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lorlatinib. Management: Avoid use of lorlatinib with strong CYP3A4 inhibitors. If the combination cannot be avoided, reduce the lorlatinib dose from 100 mg once daily to 75 mg once daily, or from 75 mg once daily to 50 mg once daily.
Lorlatinib May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences.
Lurasidone Atazanavir may increase the serum concentration of Lurasidone. Management: Atazanavir labeling recommends reducing the lurasidone dose as directed by the lurasidone labeling for moderate CYP3A4 inhibitors when used together with lurasidone.
Manidipine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Manidipine. Management: Consider avoiding concomitant use of manidipine and strong CYP3A4 inhibitors. If combined, monitor closely for increased manidipine effects and toxicities. Manidipine dose reductions may be required.
Maraviroc CYP3A4 Inhibitors (Strong) may increase the serum concentration of Maraviroc. Management: Reduce the adult dose of maraviroc to 150 mg twice daily when used with a strong CYP3A4 inhibitor. Do not use maraviroc with strong CYP3A4 inhibitors in patients with Clcr less than 30 mL/min.
Meperidine Protease Inhibitors may enhance the adverse/toxic effect of Meperidine. Protease Inhibitors may decrease the serum concentration of Meperidine. Concentrations of the toxic Normeperidine metabolite may be increased.
MethylPREDNISolone CYP3A4 Inhibitors (Strong) may increase the serum concentration of MethylPREDNISolone. Management: Consider methylprednisolone dose reduction in patients receiving strong CYP3A4 inhibitors and monitor for increased steroid related adverse effects.
Midostaurin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Midostaurin. Management: Seek alternatives to the concomitant use of midostaurin and strong CYP3A4 inhibitors if possible. If concomitant use cannot be avoided, monitor patients for increased risk of adverse reactions. Exceptions are discussed in separate monographs.
MiFEPRIStone CYP3A4 Inhibitors (Strong) may increase the serum concentration of MiFEPRIStone. Management: Limit mifepristone adult dose, when used for treatment of hyperglycemia in Cushing's syndrome, to a maximum of 600 mg/day when combined with a strong CYP3A4 inhibitor. Monitor for increased mifepristone toxicity regardless of dose or indication.
MiFEPRIStone May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus.
Mirodenafil CYP3A4 Inhibitors (Strong) may increase the serum concentration of Mirodenafil. Management: Consider using a lower dose of mirodenafil when used with strong CYP3A4 inhibitors. Monitor for increased mirodenafil effects/toxicities with the use of this combination.
Mitotane May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane.
Nefazodone Protease Inhibitors may increase the serum concentration of Nefazodone. Management: Consider alternatives to, or reduced doses of, nefazodone in patients treated with HIV protease inhibitors. Monitor patients receiving these combinations closely for toxic effects of nefazodone.
Nilotinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Nilotinib. Management: Avoid if possible. If combination needed, decrease nilotinib to 300 mg once/day for patients with resistant or intolerant Ph+ CML or to 200 mg once/day for patients with newly diagnosed Ph+ CML in chronic phase. Exceptions discussed in separate monograph.
Olaparib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Olaparib. Management: Avoid use of strong CYP3A4 inhibitors in patients being treated with olaparib, if possible. If such concurrent use cannot be avoided, the dose of olaparib should be reduced to 100 mg twice daily.
Ombitasvir, Paritaprevir, Ritonavir, and Dasabuvir Atazanavir may increase the serum concentration of Ombitasvir, Paritaprevir, Ritonavir, and Dasabuvir. Specifically, the paritaprevir component may increase significantly. Management: These agents can be combined if the atazanavir dose is 300 mg daily, atazanavir is administered in the morning at the same time as the ombitasvir/paritaprevir/ritonavir/dasabuvir combination product, and atazanavir is given without additional ritonavir.
OxyCODONE CYP3A4 Inhibitors (Strong) may enhance the adverse/toxic effect of OxyCODONE. CYP3A4 Inhibitors (Strong) may increase the serum concentration of OxyCODONE. Serum concentrations of the active metabolite oxymorphone may also be increased.
Panobinostat CYP3A4 Inhibitors (Strong) may increase the serum concentration of Panobinostat. Management: Reduce the panobinostat dose to 10 mg when it must be used with a strong CYP3A4 inhibitor.
Pimavanserin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Pimavanserin. Management: Decrease the pimavanserin dose to 10 mg daily when combined with strong CYP3A4 inhibitors.
Piperaquine CYP3A4 Inhibitors (Strong) may enhance the QTc-prolonging effect of Piperaquine. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Piperaquine. Management: Avoid concomitant use of piperaquine and strong CYP3A4 inhibitors when possible. If the combination cannot be avoided, frequent ECG monitoring is recommended due to the risk for QTc prolongation. Exceptions are discussed separately.
Pitolisant May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Combined use of pitolisant with a CYP3A4 substrate that has a narrow therapeutic index should be avoided. Other CYP3A4 substrates should be monitored more closely when used with pitolisant.
PONATinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib. Management: Per ponatinib U.S. prescribing information, the adult starting dose of ponatinib should be reduced to 30 mg daily during treatment with any strong CYP3A4 inhibitor.
Progestins (Contraceptive) Atazanavir may increase the serum concentration of Progestins (Contraceptive). However, atazanavir may lead to decreased ethinyl estradiol concentrations and decreased effectiveness of oral contraceptive products. Management: Consider an alternative or additional method of contraception, particularly with combined estrogen/progestin products. Depot medroxyprogesterone acetate may be used without a need for additional contraception.
Protease Inhibitors May increase the serum concentration of other Protease Inhibitors. Management: Atazanavir--indinavir combination contraindicated. Tipranavir/ritonavir or atazanavir/ritonavir not recommended with other protease inhibitors (PI). Darunavir/cobicistat not recommended with PI that require boosting.Other combos may require dose changes.
Proton Pump Inhibitors May decrease the serum concentration of Atazanavir. Management: See full drug interaction monograph for details.
QUEtiapine CYP3A4 Inhibitors (Strong) may increase the serum concentration of QUEtiapine. Management: In quetiapine treated patients, reduce quetiapine to one-sixth of regular dose after starting strong CYP3A4 inhibitor. In those on strong CYP3A4 inhibitors, start quetiapine at lowest dose and up-titrate as needed. Exceptions discussed separately.
Reboxetine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Reboxetine.
Ribociclib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ribociclib. Management: Avoid use of ribociclib with strong CYP3A4 inhibitors when possible; if combined use cannot be avoided, reduce ribociclib dose to 400 mg once daily. Exceptions are discussed in separate monographs.
Rifabutin Atazanavir may increase serum concentrations of the active metabolite(s) of Rifabutin. Atazanavir may increase the serum concentration of Rifabutin. Management: Reduce rifabutin doses. Clinical guidelines recommend 150 mg daily or 300 mg 3 times per week with atazanavir/ritonavir. Atazanavir labeling recommends a decrease of at least 75%, to 150 mg every other day or 150 mg 3 times per week for adults.
Riociguat Protease Inhibitors may increase the serum concentration of Riociguat. Management: Consider starting with a reduced riociguat dose of 0.5 mg three times a day (for adults). Patients receiving such a combination should also be monitored extra closely for signs or symptoms of hypotension.
Rosuvastatin Protease Inhibitors may increase the serum concentration of Rosuvastatin. Management: Start at the lowest rosuvastatin dose and monitor for toxicity. See full drug interaction monograph for details.
Ruxolitinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ruxolitinib. Management: This combination should be avoided under some circumstances. See monograph for details.
SAXagliptin CYP3A4 Inhibitors (Strong) may increase the serum concentration of SAXagliptin. Management: Saxagliptin U.S. product labeling recommends limiting saxagliptin adult dose to 2.5 mg/day when used with a strong CYP3A4 inhibitor. Monitor for increased saxagliptin levels/effects. A similar recommendation is not made in the Canadian product labeling.
Sildenafil Protease Inhibitors may increase the serum concentration of Sildenafil. Management: Erectile dysfunction: sildenafil max = 25 mg/48 hrs with ritonavir, atazanavir, or darunavir; starting dose = 25 mg with other protease inhibitors (adult doses). Contraindicated if sildenafil being used for pulmonary arterial hypertension.
Sildenafil CYP3A4 Inhibitors (Strong) may increase the serum concentration of Sildenafil. Management: Use of sildenafil for pulmonary hypertension should be avoided with strong CYP3A4 inhibitors. When used for erectile dysfunction, starting adult dose should be reduced to 25 mg. Maximum adult dose with ritonavir or cobicistat is 25 mg per 48 hours.
Sirolimus CYP3A4 Inhibitors (Strong) may increase the serum concentration of Sirolimus. Management: Consider avoiding concurrent use of sirolimus with strong CYP3A4 inhibitors in order to minimize the risk for sirolimus toxicity. Concomitant use of sirolimus and voriconazole or posaconazole is contraindicated.
Stiripentol May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring.
SUFentanil CYP3A4 Inhibitors (Strong) may increase the serum concentration of SUFentanil. Management: If a strong CYP3A4 inhibitor is initiated in a patient on sufentanil, consider a sufentanil dose reduction and monitor for increased sufentanil effects and toxicities (eg, respiratory depression).
Tacrolimus (Systemic) Protease Inhibitors may decrease the metabolism of Tacrolimus (Systemic).
Tacrolimus (Systemic) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tacrolimus (Systemic). Management: Monitor clinical tacrolimus response closely and frequently monitor tacrolimus serum concentrations with concurrent use of any strong CYP3A4 inhibitor. Tacrolimus dose reductions and/or prolongation of the dosing interval will likely be required.
Tadalafil CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tadalafil. Management: Recommendations regarding use of tadalafil in patients also receiving strong CYP3A4 inhibitors may vary based on indication and/or international labeling. Consult appropriate product labeling.
Temsirolimus Protease Inhibitors may enhance the adverse/toxic effect of Temsirolimus. Levels of sirolimus, the active metabolite, may be increased, likely due to inhibition of CYP-mediated metabolism.
Temsirolimus CYP3A4 Inhibitors (Strong) may increase the serum concentration of Temsirolimus. Management: Avoid concomitant use of temsirolimus and strong CYP3A4 inhibitors whenever possible. If combined, decrease temsirolimus dose to 12.5 mg per week and monitor patients for increased temsirolimus effects and toxicities.
Tenofovir Disoproxil Fumarate May decrease the serum concentration of Atazanavir. Atazanavir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Management: Must use boosted atazanavir in adults; give combo (atazanavir/ritonavir or atazanavir/cobicistat with tenofovir) as a single daily dose with food. Pediatric patients, pregnant patients, and users of H2blockers require other dose changes.
Tezacaftor CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tezacaftor. Management: When combined with strong CYP3A4 inhibitors, tezacaftor/ivacaftor (100 mg/150 mg) should be administered in the morning, twice a week, approximately 3 to 4 days apart. No evening doses of ivacaftor (150 mg) alone should be administered.
Tofacitinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tofacitinib. Management: Tofacitinib dose reductions are recommended when combined with strong CYP3A4 inhibitors. Recommended dose adjustments vary by tofacitinib formulation and therapeutic indication. See full monograph for details.
Tolterodine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tolterodine. Management: The maximum recommended adult dose of tolterodine is 2 mg/day when used together with a strong CYP3A4 inhibitor.
Toremifene CYP3A4 Inhibitors (Strong) may increase the serum concentration of Toremifene. Management: Use of toremifene with strong CYP3A4 inhibitors should be avoided if possible. If coadministration is necessary, monitor for increased toremifene toxicities, including QTc interval prolongation. Exceptions are discussed in separate monograph.
TraZODone Atazanavir may increase the serum concentration of TraZODone. Management: Consider using a lower dose of trazodone when used in combination with atazanavir.
Valbenazine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Valbenazine. Management: Reduce the valbenazine dose to 40 mg daily when combined with strong CYP3A4 inhibitors.
Vardenafil CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vardenafil. Management: Recommendations regarding concomitant use of vardenafil with strong CYP3A4 inhibitors may vary depending on brand name (e.g., Levitra, Staxyn) or by international labeling. See full drug interaction monograph for details.
Vemurafenib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vemurafenib. Management: Avoid concurrent use of vemurafenib with strong CYP3A4 inhibitors when possible. Consider use of an alternative that is not a strong inhibitor of CYP3A4 as clinically appropriate. Exceptions are discussed in separate monographs.
Venetoclax CYP3A4 Inhibitors (Strong) may increase the serum concentration of Venetoclax. Management: This combination is contraindicated during venetoclax initiation and ramp-up in patients with CLL/SLL. Reduced venetoclax doses are required during ramp-up for patients with AML, and reduced doses are required for all patients during maintenance therapy.
Vilazodone CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vilazodone. Management: Limit maximum adult vilazodone dose to 20 mg daily in patients receiving strong CYP3A4 inhibitors. The original vilazodone dose can be resumed following discontinuation of the strong CYP3A4 inhibitor.
Zopiclone CYP3A4 Inhibitors (Strong) may increase the serum concentration of Zopiclone. Management: The initial starting adult dose of zopiclone should not exceed 3.75 mg if combined with a strong CYP3A4 inhibitor. Monitor patients for signs and symptoms of zopiclone toxicity if these agents are combined.
Zuclopenthixol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Zuclopenthixol. Management: Consider zuclopenthixol dosage reduction with concomitant use of a strong CYP3A4 inhibitor (eg, ketoconazole) in poor CYP2D6 metabolizers or with strong CYP2D6 inhibitors (eg, paroxetine). Monitor for increased zuclopenthixol levels/toxicity.

Risk Factor X (Avoid combination)

Acalabrutinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Acalabrutinib.
Ado-Trastuzumab Emtansine CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Ado-Trastuzumab Emtansine. Specifically, strong CYP3A4 inhibitors may increase concentrations of the cytotoxic DM1 component.
Alfuzosin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alfuzosin.
Alfuzosin Protease Inhibitors may increase the serum concentration of Alfuzosin.
Aprepitant CYP3A4 Inhibitors (Strong) may increase the serum concentration of Aprepitant.
Astemizole CYP3A4 Inhibitors (Strong) may increase the serum concentration of Astemizole. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Asunaprevir CYP3A4 Inhibitors (Strong) may increase the serum concentration of Asunaprevir.
Asunaprevir OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Asunaprevir.
Avanafil CYP3A4 Inhibitors (Strong) may increase the serum concentration of Avanafil.
Axitinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Axitinib. Management: Avoid concurrent use of axitinib with any strong CYP3A inhibitor whenever possible. If a strong CYP3A inhibitor must be used with axitinib, a 50% axitinib dose reduction is recommended.
Barnidipine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Barnidipine.
Belinostat Atazanavir may increase the serum concentration of Belinostat.
Blonanserin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Blonanserin.
Bosutinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bosutinib.
Bromocriptine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Bromocriptine.
Budesonide (Systemic) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Systemic).
Buprenorphine May decrease the serum concentration of Atazanavir. Atazanavir may increase the serum concentration of Buprenorphine. Management: Avoid this combination in patients unboosted atazanavir due to possible decreased atazanavir concentrations. This combination is not contraindicated in patients also receiving ritonavir, but monitoring for buprenorphine toxicity is recommended.
Cisapride Protease Inhibitors may increase the serum concentration of Cisapride. This may result in QTc prolongation and malignant cardiac arrhythmias. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Cobimetinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Cobimetinib.
Conivaptan CYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
Conivaptan May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Dabrafenib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dabrafenib.
Dapoxetine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dapoxetine.
Domperidone CYP3A4 Inhibitors (Strong) may increase the serum concentration of Domperidone. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Dronedarone CYP3A4 Inhibitors (Strong) may increase the serum concentration of Dronedarone. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Elagolix OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix.
Eletriptan CYP3A4 Inhibitors (Strong) may increase the serum concentration of Eletriptan.
Eplerenone CYP3A4 Inhibitors (Strong) may increase the serum concentration of Eplerenone.
Ergot Derivatives Protease Inhibitors may increase the serum concentration of Ergot Derivatives. Exceptions: Cabergoline; Nicergoline; Pergolide.
Everolimus CYP3A4 Inhibitors (Strong) may increase the serum concentration of Everolimus.
Flibanserin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Flibanserin.
Fluticasone (Nasal) CYP3A4 Inhibitors (Strong) may increase the serum concentration of Fluticasone (Nasal).
Fosaprepitant CYP3A4 Inhibitors (Strong) may increase the serum concentration of Fosaprepitant.
Fusidic Acid (Systemic) May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Glecaprevir and Pibrentasvir Atazanavir may increase the serum concentration of Glecaprevir and Pibrentasvir.
Grazoprevir Atazanavir may increase the serum concentration of Grazoprevir.
Halofantrine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Halofantrine. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Ibrutinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ibrutinib. Management: Avoid concomitant use of ibrutinib and strong CYP3A4 inhibitors. If a strong CYP3A4 inhibitor must be used short-term (eg, anti-infectives for 7 days or less), interrupt ibrutinib therapy until the strong CYP3A4 inhibitor is discontinued.
Idelalisib May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Indinavir Atazanavir may enhance the adverse/toxic effect of Indinavir. Indinavir may enhance the adverse/toxic effect of Atazanavir.
Irinotecan Products CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Irinotecan Products. Specifically, serum concentrations of SN-38 may be increased. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Irinotecan Products.
Irinotecan Products UGT1A1 Inhibitors may increase serum concentrations of the active metabolite(s) of Irinotecan Products. Specifically, concentrations of SN-38 may be increased. UGT1A1 Inhibitors may increase the serum concentration of Irinotecan Products.
Isavuconazonium Sulfate CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Isavuconazonium Sulfate. Specifically, CYP3A4 Inhibitors (Strong) may increase isavuconazole serum concentrations. Management: Combined use is considered contraindicated per US labeling. Lopinavir/ritonavir (and possibly other uses of ritonavir doses less than 400 mg every 12 hours) is treated as a possible exception to this contraindication despite strongly inhibiting CYP3A4.
Ivabradine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ivabradine.
Lapatinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lapatinib. Management: If an overlap in therapy cannot be avoided, consider reducing lapatinib adult dose to 500 mg/day during, and within 1 week of completing, treatment with the strong CYP3A4 inhibitor.
Lercanidipine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lercanidipine.
Lomitapide CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lomitapide.
Lovastatin Protease Inhibitors may increase the serum concentration of Lovastatin.
Lovastatin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lovastatin.
Macitentan CYP3A4 Inhibitors (Strong) may increase the serum concentration of Macitentan.
Midazolam Protease Inhibitors may increase the serum concentration of Midazolam. Management: Oral midazolam contraindicated with all protease inhibitors. IV midazolam contraindicated with fosamprenavir and nelfinavir; other protease inhibitors recommend caution, close monitoring, and consideration of lower IV midazolam doses with concurrent use.
Naloxegol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Naloxegol.
Neratinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Neratinib.
Nevirapine Atazanavir may increase the serum concentration of Nevirapine. Nevirapine may decrease the serum concentration of Atazanavir.
NiMODipine CYP3A4 Inhibitors (Strong) may increase the serum concentration of NiMODipine.
Nisoldipine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Nisoldipine.
Ombitasvir, Paritaprevir, and Ritonavir Atazanavir may increase the serum concentration of Ombitasvir, Paritaprevir, and Ritonavir. Specifically, the paritaprevir component may increase significantly.
PACLitaxel (Conventional) Atazanavir may increase the serum concentration of PACLitaxel (Conventional). Management: Use of paclitaxel or other narrow therapeutic index CYP2C8 substrates with atazanavir without concurrent ritonavir is not recommended. If paclitaxel is used with ritonavir-boosted atazanavir, no significant interaction is expected.
Palbociclib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Palbociclib.
PAZOPanib BCRP/ABCG2 Inhibitors may increase the serum concentration of PAZOPanib.
Pimozide Protease Inhibitors may increase the serum concentration of Pimozide.
Pimozide CYP3A4 Inhibitors (Strong) may increase the serum concentration of Pimozide.
Radotinib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Radotinib.
Ranolazine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ranolazine.
Red Yeast Rice CYP3A4 Inhibitors (Strong) may increase the serum concentration of Red Yeast Rice. Specifically, concentrations of lovastatin and related compounds found in Red Yeast Rice may be increased.
Regorafenib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Regorafenib.
Repaglinide Atazanavir may increase the serum concentration of Repaglinide. Management: Use of repaglinide or other narrow therapeutic index CYP2C8 substrates with atazanavir without concurrent ritonavir is not recommended. If repaglinide is used with ritonavir-boosted atazanavir, no significant interaction is expected.
Revefenacin OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentrations of the active metabolite(s) of Revefenacin.
RifAMPin May decrease the serum concentration of Atazanavir.
Rupatadine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Rupatadine.
Salmeterol CYP3A4 Inhibitors (Strong) may increase the serum concentration of Salmeterol.
Saquinavir May increase the serum concentration of Atazanavir. Atazanavir may increase the serum concentration of Saquinavir.
Silodosin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Silodosin.
Simeprevir CYP3A4 Inhibitors (Strong) may increase the serum concentration of Simeprevir.
Simeprevir Protease Inhibitors may increase the serum concentration of Simeprevir. Simeprevir may increase the serum concentration of Protease Inhibitors.
Simvastatin Protease Inhibitors may increase the serum concentration of Simvastatin.
Simvastatin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Simvastatin.
Sonidegib CYP3A4 Inhibitors (Strong) may increase the serum concentration of Sonidegib.
St John's Wort May decrease the serum concentration of Atazanavir.
Suvorexant CYP3A4 Inhibitors (Strong) may increase the serum concentration of Suvorexant.
Tamsulosin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tamsulosin.
Terfenadine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Terfenadine. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Ticagrelor CYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Ticagrelor. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ticagrelor.
Tipranavir May decrease the serum concentration of Protease Inhibitors.
Tolvaptan CYP3A4 Inhibitors (Strong) may increase the serum concentration of Tolvaptan.
Topotecan BCRP/ABCG2 Inhibitors may increase the serum concentration of Topotecan.
Trabectedin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Trabectedin.
Triazolam CYP3A4 Inhibitors (Strong) may increase the serum concentration of Triazolam.
Udenafil CYP3A4 Inhibitors (Strong) may increase the serum concentration of Udenafil.
Ulipristal CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ulipristal. Management: This is specific for when ulipristal is being used for signs/symptoms of uterine fibroids (Canadian indication). When ulipristal is used as an emergency contraceptive, patients receiving this combo should be monitored for ulipristal toxicity.
VinCRIStine (Liposomal) CYP3A4 Inhibitors (Strong) may increase the serum concentration of VinCRIStine (Liposomal).
Vinflunine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vinflunine.
Vorapaxar CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vorapaxar.
Voriconazole Atazanavir may decrease the serum concentration of Voriconazole. Atazanavir may increase the serum concentration of Voriconazole. Voriconazole may decrease the serum concentration of Atazanavir. Management: Voriconazole should not be used in a patient who is being treated with ritonavir-boosted atazanavir unless the benefits of the combination outweigh the potential risks. Extra monitoring for both loss of effectiveness and toxicity is warranted.
Voxilaprevir Atazanavir may increase the serum concentration of Voxilaprevir.

Monitor:

  • Viral load
  • CD4
  • serum glucose level
  • LFT (before initiation and as indicated in patients with existing liver disease),
  • bilirubin (as clinically indicated);
  • drug levels (with certain concomitant medications),
  • ECG monitoring in patients with preexisting prolonged PR interval or with concurrent AV nodal blocking drugs;
  • serum creatinine level,
  • estimated CrCL,
  • urinalysis along with microscopic examination (before initiation and as clinically indicated).

How to take Atazanavir (Reyataz)?

  • Administer with food. Give atazanavir 2 hours prior or 1 hour after didanosine buffered formulations, capsules, other buffered medications, or antacids.
  • Administer atazanavir (with ritonavir) at the same time, or at least 10 hours after, H -receptor antagonists
  • Administer atazanavir (without ritonavir) at least 2 hours prior or at least 10 hours after H -receptor antagonist.
  • Administer atazanavir (with ritonavir) 12 hours after giving proton pump inhibitor.

Additional formulation specific information:

  • Oral capsules: Swallow capsules whole, should not be opened

Oral powder: Mixing with food:

  • While using a spoon, mix the recommended number of oral powder packets with a minimum of one tablespoon of food in a small container.
  • Then feed the mixture to the patient.
  • Mix an additional one tablespoon of food to the container, and give the patient the residual mixture.

Mix the medicine with a beverage such as milk or water in a small drinking cup:

  • While using a spoon, mix the advised number of oral powder packets with a minimum of 30 mL of the beverage in a  cup.
  • Give the patient to drink the mixture.
  • Add 15 mL more of beverage to the cup
  • Then mix, and have the patient drink the remaining mixture.
  • If water is used, food should be eaten at the same time.

Mixed the drug with food or beverage and give the entire dose within 60 minutes of preparation (may leave the mixture at room temperature during this 60 minute period). Ensure that the patient eats or drinks all the food or beverage which contains the powder. Additional food can be given after consumption of the entire mixture. Give ritonavir after oral powder administration.

Mechanism of action of Atazanavir (Reyataz):

  • Atazanavir binds with the protease activity and inhibits cleavage viral GagPol polyprotein precursors into functional proteins necessary for HIV infection.
  • This results in the formation of non-infectious, immature viral particles.

Absorption:

  • Rapid; increased with food

Distribution:

  • CSF: Plasma concentration ratio (range): 0.0021 - 0.0226

Protein binding:

  • 86%; it binds to both alpha -acid glycoprotein and albumin (similar affinity)

Metabolism:

  • Mainly Hepatic by cytochrome P450 isoenzyme CYP3A;
  • also undergoes biliary elimination;
  • It undergoes major biotransformation pathways like mono-oxygenation and deoxygenation;
  • Minor pathway metabolism of the parent drug or metabolites include glucuronidation, N-dealkylation, hydrolysis, and oxygenation with dehydrogenation; 2 minor inactive metabolites have been seen

Half-life elimination:

  • Unboosted therapy: 7 - 8 hours;
  • Boosted therapy (with ritonavir): 9 - 18 hours;
  • 12 hours in patients with hepatic impairment

Time to peak, plasma:

  • 2 to 3 hours

Excretion:

  • Via Feces (79%, 20% of total dose as unchanged drug)
  • Via urine (13%, 7% of total dose as unchanged drug)

International Brands of Atazanavir:

  • Atavir-A
  • MYLAN-Atazanavir
  • Reyataz
  • TEVA-Atazanavir
  • Atazor
  • Reyataz

Atazanavir Brands in Pakistan:

 No brands available in Pakistan

Comments

NO Comments Found