Raltegravir

Aluminium / Magnesium hydroxide

Combination not recommended.

No pharmaceutical opinion available for this interaction.

Mechanism

Aluminium / Magnesium hydroxide could bind (chelation) to raltegravir and reduce its absorption .

Raltegravir

Pharmacodynamic effects

Possible decrease of clinical efficacy.

Recommendations

Monitor for clinical efficacy.

Alternative solution(s)

Aluminium / Magnesium hydroxide

Pharmacodynamic effects

Recommendations

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

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
Parameters
Reference number
# patients
Dose
Frequency
AUC
Cmax
Cmin
Raltegravir
2416 2416 2416 2416 2416 2416 2175 2175
25 23 23 16 16 19 17 18
400 mg 400 mg 400 mg 400 mg 400 mg 1200 mg 400 mg 400 mg
BID BID BID BID BID QD BID BID
- 49% - 51% - 30% - 13% - 11% - 14% - 19% - 32%
- 44% - 51% - 22% - 10% - 10% - 14% - 22% - 30%
- 63% - 56% - 57% - 50% - 49% - 58% - 60% - 62%
Aluminium / Magnesium hydroxide
2416 2416 2416 2416 2416 2416 2175 2175
25 23 23 16 16 19 17 18
20 ml * 20 ml ** 20 ml *** 20 ml † 20 ml †† 20 ml ° 20 ml ‡ 20 ml ‡‡
x 1 x 1 x 1 x 1 x 1 x 1 x 1 x 1
               
               
               
Comment

Ref #2416 :
* Taken with Raltegravir; ** Taken 2 hours before; *** Taken 2 hours after; † Taken 6 hours before; †† Taken 6 hours after; ° Taken 12 hours after.
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.

Ref #2175 : ‡ Taken 4 hours before; ‡‡ Taken 4 hours after.

See raltegravir + calcium (salts).

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.