Dolutegravir

Carbamazepine

Dosage adjustment is recommended.

No pharmaceutical opinion available for this interaction.

Mechanism

Carbamazepine may induce the metabolism (UGT 1A1 and CYP3A) and decrease the plasma concentration of Dolutegravir.

Dolutegravir

Pharmacodynamic effects

Possible decrease of clinical efficacy.

Recommendations

Tivicay : Increase dolutegravir dose to 50 mg BID.

Triumeq or Dovato : Administer an additional dose of 50 mg dolutegravir 12 hours after Triumeq or Dovato.

Monitor for clinical efficacy.

Avoid combination in patients with resistance to integrase inhibitors.

Juluca : Concomitant administration contraindicated.

Alternative solution(s)

Carbamazepine

Pharmacodynamic effects

Recommendations

Alternative solution(s)

Gabapentin, pregabalin, valproic acid, clobazam, levetiracetam, topiramate, lacosamide, clonazepam or lamotrigine.

Monitor

Tests

CD4+

Viral load HIV

Pharmacokinetic parameters
Parameters
Reference number
# patients
HIV
Dose
Frequency
Duration (days)
AUC
Cmax
Cmin
T1/2
Dolutegravir
3054
14
-
50 mg
QD
5
- 49%
- 33%
- 73%
- 43%
Carbamazepine
3054
14
-
100-300 mg *
BID
5
 
 
 
 
Comment

Ref #3054 : * Carbamazepine dose selection was based on consideration of the range of carbamazepine clinical doses as well as risk-benefit in studying in healthy subjects.
Dolutegravir co-administered with carbamazepine were well tolerated; both AEs leading to subject withdrawal occurred with carbamazepine alone, without dolutegravir.

Reference
  • 2868
    Dolutegravir (Tivicay), ViiV Healthcare, Quebec, Canada, 31 janv. 2020.
  • 3054
    Song I, Weller S, Patel J, Borland J, Wynne B et al. Effect of carbamazepine on dolutegravir pharmacokinetics and dosing recommendation. Eur J Clin Pharmacol 2016; 72: 665-670.
  • 3120
    Dolutégravir/abacavir/lamivudine (Triumeq), ViiV Healthcare, Québec, Canada, 31 janv. 2020.
  • 3441
    Dolutegravir/Rilpivirine (Juluca), ViiV Healthcare ULC, Quebec, Canada, 5 fév. 2020.
  • 3497
    Dolutegravir/Lamivudine (Dovato), ViiV Soins de santé ULC, Québec, Canada, 5 fév. 2020.