https://interactions.guidetherapeutiquevih.com/en/interaction-details?id=9783
https://interactions.guidetherapeutiquevih.com/en/interaction-details?id=9783
No pharmaceutical opinion available for this interaction.
Carbamazepine can induce the metabolism (CYP 3A4) and decrease the plasma concentration of Elvitegravir / Cobicistat.
Elvitegravir / Cobicistat may possibly inhibit the metabolism (CYP 3A4) and consequently increase the plasma concentration of Carbamazepine.
Possible decrease of clinical efficacy.
Risk of a possible development of resistance to antiretroviral class.
Monitor for signs and symptoms of therapeutic failure.
–
Possible increase of adverse effects.
Contraindicated. Use alternative.
As clinically indicated : brivaracetam, gabapentin, lacosamide, lamotrigine, levetiracetam, pregabalin, rufinamide, topiramate, vigabatrin, zonisamide.
Carbamazepine adverse effects : disorientation, ataxia, lethargy, drowsiness, nausea, vomiting, headache, diplopia, dizziness, leukopenia and hyponatremia.
Carbamazepine
Viral Load
CD4+
Elvitegravir plasma level
| Reference number |
|---|
| # patients |
| HIV |
| Dose |
| Frequency |
| Duration (days) |
| AUC |
| Cmax |
| Cmin |
| 3069 |
|---|
| 12 |
| - |
| 150/150 mg |
| QD |
| 10 |
| - 69%/- 84% |
| - 97%/- 90% |
| - 45%/- 72% |
| 3069 |
|---|
| 12 |
| - |
| 200 mg |
| BID |
| 10 |
| + 43% * |
| + 51% * |
| + 40% * |
Ref #3069 : * Carbamazepine10,11-epoxyde AUC -35%, Cmax -41% and Cmin -27%.
Importantly, elvitegravir Cmin, the parameter best associated with antiviral activity, was below the IC95 (45 ng/mL) in 11 of 12 subjects. These study findings are consistent with the current dosing recommendation that carbamazepin be avoided with elvitegravir and cobicistat containing regimens.
Ref #1304 : Reported case of a 20-year-old patient who developed vomiting, dizziness, elevated liver enzymes, and increased carbamazepine concentration by 87% following the addition of one dose of ritonavir 200 mg. Symptoms started within 12 hours after the first dose of ritonavir. In order to obtain a concentration within the therapeutic index, the dose of carbamazepine was reduced from 750 to 280 mg QD. Several other cases of acute toxicity to carbamazepine 2 to 4 days after the addition of ritonavir have been reported. See ritonavir + carbamazepine.
Ref #2090: Another case reported of a 50 year man who developed excessive drowsiness following the introduction of lopinavir/ritonavir and it was found that his serum carbamazepine concentration had increased by 46%. His antiretroviral therapy was then changed to nelfinavir 1250 mg BID but 3 days later the same symptoms appeared with 53% increase in carbamazepine. The symptoms of carbamazepine toxicity disappeared after a carbamazepine dose reduction of 33%. See lopinavir/ritonavir + carbamazepine.