Raltegravir

Antacids

Combination not recommended.

No pharmaceutical opinion available for this interaction.

Mechanism

Cations by chelation may reduce the absorption of Raltegravir.

Raltegravir

Pharmacodynamic effects

Possible decrease of clinical efficacy.

Recommendations

Monitor for clinical efficacy.

Alternative solution(s)

Antacids

Pharmacodynamic effects

Recommendations

Association not recommended with raltegravir 400 mg BID or raltegravir HD 1200 mg QD.

See comments.

Alternative solution(s)

Calcium carbonate antacids with raltegravir 400 mg BID or H2 antagonists or inhibitors of proton pump receivers.

Monitor

Tests

Raltegravir plasma level

CD4+

Viral load HIV

Pharmacokinetic parameters

Comment

Ref #2416 : Monograph recommends not to give raltegravir or raltegravir HD with antacids containing aluminum or magnesium. Antacids with calcium carbonate are not recommended with raltegravir HD and they also reduced raltegravir Cmin but this decrease is considered clinically non-significant.

For more details, see raltegravir + Aluminium/Magnesium hydroxyde and raltegravir + calcium (antacid).

Reference
  • 2416
    Raltegravir (Isentress, Isentress HD), Merck, Quebec, Canada, 30 octobre 2023.
  • 2857
    Raltegravir (Isentress), European public assessment report (EPAR) Product Information, London, United Kingdom, sept 2013.
  • 2381
    Kiser JJ, Bumpass JB, Meditz A, et al. Effect of antacids on the pharmacokinetics of raltegravir in human immunodeficiency virus-seronegative volunteers. Antimicrob Agents Chemother 2010;54(12):4999-5003.
  • 2175
    Raltegravir (Isentress & ISentress HD), Prescribing Information, Merck & Co Inc, New Jersey USA, Jan 2019.
  • 3083
    Roberts JL, et al. Virologic failure with a raltegravir-containing antiretroviral regimen and concomitant calcium administration. Pharmacother, 2011, 31(10): 298e-302e.