https://interactions.guidetherapeutiquevih.com/en/interaction-details?id=7634
https://interactions.guidetherapeutiquevih.com/en/interaction-details?id=7634
No pharmaceutical opinion available for this interaction.
Rifampicin increases the metabolism (CYP 3A4) and decreases the plasma concentration of Atazanavir / ritonavir.
Possible decrease of clinical efficacy.
Risk of a possible development of resistance to antiretroviral class.
–
In patients without resistance to integrase inhibitors, dolutegravir 50 mg BID or raltegravir 800 mg BID : see dolutegravir + rifampicin or raltegravir + rifampicin.
Increased risk of hepatotoxicity.
Contraindicated. Use alternative.
Rifabutin either 150 mg QD, every 2 days or 3 times a week (see rifabutin with PIs) or choose an antibiotic that does not interact with PIs.
Hepatotoxicity: elevation of hepatic transaminases by 3 to 5 fold, fatigue, unusual weakness, nausea, vomiting, anorexia, abdominal pains, pale stools, dark urine, jaundice.
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| Reference number |
|---|
| Frequency |
| Duration (days) |
| HIV |
| Dose |
| AUC 0-24h |
| Cmin |
| Cmax |
| # patients |
| 1634 | 2396 |
|---|---|
| QD | QD |
| 10 | 8* |
| - | - |
| 600 mg | 600 mg** |
| 14 |
| 1634 | 2396 |
|---|---|
| QD | BID** |
| 10 | 11** |
| - | - |
| 400/200 mg | 300 mg**/100 mg** |
| + 10% * | |
| - 60% * | |
| - 18%* | |
| 14 |
Ref #1634: Rifampicin and desacetyl rifampicin exposures were comparable across different regimens of ATV/RTV, but were ~1.6 to 2.5 times higher that with rifampicin alone.
* Compared to atazanavir 400 mg daily.
Ref #2324 : Study with 10 patients HIV negative receiving ATV 300 mg BID (stade 1) + Rifampicin and ATV 400 mg + RIF 600 mg QD (stade 2) vs. ATV 300 mg BID. Despite the administration twice a day of atazanavir (300 mg BID), the Cmin of atazanavir was 44 ng/ml for patients receiving ATV 300 BID + RIF and 113 ng/ml for patients receiving ATV 400 + RIF compared to 811 ng/ml for patients receiving atazanavir 300 mg BID without rifampicin.
Ref #2323 : Study with 71 patients HIV negative receiving 300/100 mg QD of ATV/r vs. ATV/r + RIF 300/100/600 mg vs. ATV/r + RIF 300/200/600 mg vs. ATV/r + RIF 400/200/600 mg.
Results : Cmin of 707, 3 ng/mL in patients under ATV/r vs. 18.1 in ATV/r/RIF 300/100/600 mg vs. 42,7 in ATV/r/RIF 300/200/600 mg vs. 52,9 in ATV/r/RIF 400/200/600 mg.
Réf #2396: Study with 3 stages :
During the 1st stage *, rifampicin 600 mg once a day during 8 days. Stage 2 **: Rifampicin 600 mg + Atazanavir/ritonavir 300/100 mg BID during 11 days. Stage 3: Increase in dosage of atazanavir/ritonavir 400/100 mg BID.
Following this increase in dosage, 3 patients had an increase of transaminases and vomiting. The treatment had to be stopped.
Co-administration of rifampicin 600 mg QD with protease inhibitors such as lopinavir/ritonavir, darunavir/ritonavir and atazanavir alone also causes a decrease in AUC and Cmin of approximately 75% to 80%.
Ref #3116 : To increase the chance of achieving therapeutic serum levels and reduce the development of resistance and treatment failures some experts, as well as the CDC, recommend a 150mg QD dose. See rifabutin + PIs.