Last update July 12, 2023

Raltegravir (RAL)

Compatible

Safe product and/or breastfeeding is the best option.

An antiretroviral integrase inhibitor. Indicated in combination with two other antiretroviral drugs for the treatment of infection by the human immunodeficiency virus (HIV-1) and in the prophylaxis of vertical transmission (pregnancy/breastfeeding) (Puthanakit 2018, Westling 2012) and accidental post-exposure. Oral administration in 2 daily doses.

It is excreted in breast milk in a clinically insignificant amount and plasma levels in infants were very low or below the limit of detection. (Aebi 2022, Feiterna 2020)

It is a well-tolerated drug with low frequency of serious side effects (MSD 2019, AEMPS2018, Clarke 2018, Ribera 2010), including in neonates, infants and children (Clarke 2018, Ripamonti 2016, Nachman 2015 and 2014).

It is used in nonpreterm newborns and from 3 kg of weight (Trahan 2019, MSD 2019, AEMPS 2018). The WHO provides for neonatal use (Clarke 2018, WHO 2016, WHO 2014). It is recommended after 2 to 4 weeks of life in the non-occupational post-exposure prophylaxis guidelines for HIV (CDC 2016, WHO 2014).

In preterm infants it has a longer elimination half-life, between 15 and 22 hours (Kreutzwiser 2017)

"Individuals with HIV who are on ART with a sustained undetectable viral load and who choose to breastfeed should be supported in this decision". (Panel 2022 p ix)


See below the information of these related products:

Alternatives

We do not have alternatives for Raltegravir (RAL) since it is relatively safe.

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

Jose Maria Paricio, Founder & President of APILAM/e-Lactancia

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Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.
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Other names

Raltegravir (RAL) is also known as


Raltegravir (RAL) in other languages or writings:

Group

Raltegravir (RAL) belongs to this group or family:

Tradenames

Main tradenames from several countries containing Raltegravir (RAL) in its composition:

Pharmacokinetics

Variable Value Unit
Molecular weight 483 daltons
Protein Binding 83 %
pKa 5.62 -
Tmax 1.7 - 3 hours
T½ 9 (7 - 12) hours
M/P ratio 0.39 (0.39–0.42) -
Theoretical Dose 0.1 - 0.32 mg/Kg/d
Relative Dose 0.8 - 5.35 %

References

  1. Panel on Treatment of HIV During Pregnancy and Prevention of Perinatal Transmission. Recommendations for the Use of Antiretroviral Drugs During Pregnancy and Interventions to Reduce Perinatal HIV Transmission in the United States. Department of Health and Human Services. 2024 Abstract Full text (link to original source)
  2. Aebi-Popp K, Kahlert CR, Crisinel PA, Decosterd L, Saldanha SA, Hoesli I, Martinez De Tejada B, Duppenthaler A, Rauch A, Marzolini C; Swiss Mother and Child HIV Cohort Study (SHCS). Transfer of antiretroviral drugs into breastmilk: a prospective study from the Swiss Mother and Child HIV Cohort Study. J Antimicrob Chemother. 2022 Nov 28;77(12):3436-3442. Abstract Full text (link to original source)
  3. Feiterna-Sperling C, Bukkems VE, Teulen MJA, Colbers AP; PANNA network.. Low raltegravir transfer into the breastmilk of a woman living with HIV. AIDS. 2020 Oct 1;34(12):1863-1865. Abstract Full text (link to original source)
  4. Trahan MJ, Lamarre V, Metras ME, Kakkar F. Use of Triple Combination Antiretroviral Therapy With Raltegravir as Empiric HIV Therapy in the High-risk HIV-exposed Newborn. Pediatr Infect Dis J. 2019 Apr;38(4):410-412. Abstract
  5. MSD. Raltegravir (Isentress). Drug Summary. 2019 Full text (in our servers)
  6. AEMPS - MSD. Raltegravir (Isentress). Ficha técnica. 2018 Full text (in our servers)
  7. Clarke DF, Penazzato M, Capparelli E, Cressey TR, Siberry G, Sugandhi N, Mirochnick M; WHO Paediatric Antiretroviral Working Group.. Prevention and treatment of HIV infection in neonates: evidence base for existing WHO dosing recommendations and implementation considerations. Expert Rev Clin Pharmacol. 2018 Jan;11(1):83-93. Abstract
  8. Puthanakit T, Thepnarong N, Chaithongwongwatthana S, Anugulruengkitt S, Anunsittichai O, Theerawit T, Ubolyam S, Pancharoen C, Phanuphak P. Intensification of antiretroviral treatment with raltegravir for pregnant women living with HIV at high risk of vertical transmission. J Virus Erad. 2018 Apr 1;4(2):61-65. Abstract Full text (link to original source) Full text (in our servers)
  9. Kreutzwiser D, Sheehan N, Dayneka N, Lemire B, Wong A, Samson L, Brophy J. Therapeutic drug monitoring guided raltegravir dosing for prevention of vertical transmission in a premature neonate born to a woman living with perinatally acquired HIV. Antivir Ther. 2017;22(6):545-549. Abstract
  10. WHO - World Health Organization Consolidated Guidelines on the Use of Antiretroviral Drugs for Treating and Preventing HIV Infection: Recommendations for a Public Health Approach. Guideline. 2016 Abstract Full text (link to original source) Full text (in our servers)
  11. CDC - Centers for Disease Control and Prevention, U.S. Department of Health and Human Services. Updated Guidelines for Antiretroviral Postexposure Prophylaxis After Sexual, Injection Drug Use, or Other Nonoccupational Exposure to HIV— United States. nPEP Guidelines Update. 2016 Full text (link to original source) Full text (in our servers)
  12. Ripamonti D, Tatarelli P, Mangili G, Gotta C, Benatti SV, Bruzzone B, Callegaro A, Viscoli C, Ruggeri M, Di Biagio A. Potential role of raltegravir-based therapy to induce rapid viral decay in highly viraemic HIV-infected neonates. J Chemother. 2016 Aug;28(4):337-40. Abstract
  13. Nachman S, Alvero C, Acosta EP, Teppler H, Homony B, Graham B, Fenton T, Xu X, Rizk ML, Spector SA, Frenkel LM, Worrell C, Handelsman E, Wiznia A. Pharmacokinetics and 48-Week Safety and Efficacy of Raltegravir for Oral Suspension in Human Immunodeficiency Virus Type-1-Infected Children 4 Weeks to 2 Years of Age. J Pediatric Infect Dis Soc. 2015 Dec;4(4):e76-83. Abstract Full text (link to original source) Full text (in our servers)
  14. Nachman S, Zheng N, Acosta EP, Teppler H, Homony B, Graham B, Fenton T, Xu X, Wenning L, Spector SA, Frenkel LM, Alvero C, Worrell C, Handelsman E, Wiznia A; International Maternal Pediatric Adolescent AIDS Clinical Trials (IMPAACT) P1066 Study Team.. Pharmacokinetics, safety, and 48-week efficacy of oral raltegravir in HIV-1-infected children aged 2 through 18 years. Clin Infect Dis. 2014 Feb;58(3):413-22. Abstract
  15. Westling K, Pettersson K, Kaldma A, Navér L. Rapid decline in HIV viral load when introducing raltegravir-containing antiretroviral treatment late in pregnancy. AIDS Patient Care STDS. 2012 Dec;26(12):714-7. Abstract
  16. Ribera E, Tuset M, Martín M, del Cacho E. Características de los fármacos antirretrovirales. [Characteristics of antiretroviral drugs]. Enferm Infecc Microbiol Clin. 2011 May;29(5):362-91. Abstract

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