Last update April 2, 2023

C37 H48 N4 O5

Compatible

Safe substance and/or breastfeeding is the best option.

Antiviral HIV protease inhibitor (PI). It is used, boosted with Ritonavir, in the treatment of HIV/AIDS. It has been used experimentally in the treatment of the COVID-19 coronavirus (Li 2020, Lim 2020, SEFH 2020). Oral administration in two daily doses.

Lopinavir pharmacokinetic data (moderately high molecular weight and very high percentage of protein binding) explain the negligible transfer into milk observed. (Oumar 2018, Ramírez 2018, Corbett 2014, Shapiro 2013, Palombi 2012, Rezk 2008)

The plasma levels of infants whose mothers took Lopinavir were undetectable (Oumar 2018, Corbett 2014, Gandhi 2013, Shapiro 2013) or very low. (Gandhi 2013, Shapiro 2013, Palombi 2012)

For Ritonavir, the commentary and bibliography can be consulted in the ritonavir file

According to the policy adopted by the health authorities of each country, breastfeeding in mothers with HIV/AIDS is or is not advised. With current combination antiretroviral therapy, the HIV viral load can be made undetectable, reducing the risk of HIV transmission through breastfeeding to levels similar to those of formula feeding.


See below the information of these related products:

Alternatives

We do not have alternatives for C37 H48 N4 O5 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

Your contribution is essential for this service to continue to exist. We need the generosity of people like you who believe in the benefits of breastfeeding.

Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Group

C37 H48 N4 O5 belongs to this group or family:

Tradenames

Main tradenames from several countries containing C37 H48 N4 O5 in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 25 %
Molecular weight 629 daltons
Protein Binding 98 - 99 %
VD 0.9 - 1.8 l/Kg
pKa 13.39 -
Tmax 4.4 hours
5 - 6 hours
M/P ratio 0.2 - 0.4 -
Theoretical Dose 0.1 - 0.28 mg/Kg/d
Relative Dose 0.23 - 2.1 %

References

  1. Lim J, Jeon S, Shin HY, Kim MJ, Seong YM, Lee WJ, Choe KW, Kang YM, Lee B, Park SJ. Case of the Index Patient Who Caused Tertiary Transmission of COVID-19 Infection in Korea: the Application of Lopinavir/Ritonavir for the Treatment of COVID-19 Infected Pneumonia Monitored by Quantitative RT-PCR. J Korean Med Sci. 2020 Feb 17;35(6):e79. Consulted on Feb. 20, 2020 Abstract
  2. SEFH - Sociedad Española de Farmacia Hospitalaria. Procedimientos de farmacia hospitalaria para la gestión del tratamiento con antivirales en la enfermedad por el nuevo coronavirus sars-cov-2 (COVID-19). Recomendaciones de la Sociedad Española de Farmacia Hospitalaria. None 2020 Full text (in our servers)
  3. Li H, Wang YM, Xu JY, Cao B. [Potential antiviral therapeutics for 2019 Novel Coronavirus]. Zhonghua Jie He He Hu Xi Za Zhi. 2020 Feb 5;43(0):E002. Abstract
  4. Oumar AA, Bagayoko-Maiga K, Bahachimi A, Maiga M, Cere MC, Diarra Z, Chatelut E, Sylla M, Murphy RL, Dao S, Gandia P. Efavirenz and Lopinavir Levels in HIV-Infected Women and Their Nursing Infants, in Mali. J Pharmacol Exp Ther. 2018 Sep;366(3):479-484. Abstract
  5. Ramírez-Ramírez A, Sánchez-Serrano E, Loaiza-Flores G, Plazola-Camacho N, Rodríguez-Delgado RG, Figueroa-Damián R, Domínguez-Castro M, López-Martínez M, Flores-García Z, Hernández-Pineda J. Simultaneous quantification of four antiretroviral drugs in breast milk samples from HIV-positive women by an ultra-high performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method. PLoS One. 2018 Jan 19;13(1):e0191236. Abstract Full text (link to original source)
  6. Cohan D, Natureeba P, Koss CA, Plenty A, Luwedde F, Mwesigwa J, Ades V, Charlebois ED, Gandhi M, Clark TD, Nzarubara B, Achan J, Ruel T, Kamya MR, Havlir DV. Efficacy and safety of lopinavir/ritonavir versus efavirenz-based antiretroviral therapy in HIV-infected pregnant Ugandan women. AIDS. 2015 Jan 14;29(2):183-91. Abstract Full text (link to original source)
  7. Corbett AH, Kayira D, White NR, Davis NL, Kourtis AP, Chasela C, Martinson F, Phiri G, Musisi B, Kamwendo D, Hudgens MG, Hosseinipour MC, Nelson JA, Ellington SR, Jamieson DJ, van der Horst C, Kashuba A; BAN Study Team.. Antiretroviral pharmacokinetics in mothers and breastfeeding infants from 6 to 24 weeks post-partum: results of the BAN Study. Antivir Ther. 2014;19(6):587-95. Abstract Full text (link to original source)
  8. Gandhi M, Mwesigwa J, Aweeka F, Plenty A, Charlebois E, Ruel TD, Huang Y, Clark T, Ades V, Natureeba P, Luwedde FA, Achan J, Kamya MR, Havlir DV, Cohan D; Prevention of Malaria and HIV disease in Tororo (PROMOTE) study.. Hair and plasma data show that lopinavir, ritonavir, and efavirenz all transfer from mother to infant in utero, but only efavirenz transfers via breastfeeding. J Acquir Immune Defic Syndr. 2013 Aug 15;63(5):578-84. Abstract
  9. Shapiro RL, Rossi S, Ogwu A, Moss M, Leidner J, Moffat C, Lockman S, Moyo S, Makhema J, Essex M, Capparelli E. Therapeutic levels of lopinavir in late pregnancy and abacavir passage into breast milk in the Mma Bana Study, Botswana. Antivir Ther. 2013;18(4):585-90. Abstract Full text (link to original source)
  10. Palombi L, Pirillo MF, Andreotti M, Liotta G, Erba F, Sagno JB, Maulidi M, Ceffa S, Jere H, Marchei E, Pichini S, Galluzzo CM, Marazzi MC, Vella S, Giuliano M. Antiretroviral prophylaxis for breastfeeding transmission in Malawi: drug concentrations, virological efficacy and safety. Antivir Ther. 2012;17(8):1511-9. Abstract Full text (link to original source)
  11. Rezk NL, White N, Bridges AS, Abdel-Megeed MF, Mohamed TM, Moselhy SS, Kashuba AD. Studies on antiretroviral drug concentrations in breast milk: validation of a liquid chromatography-tandem mass spectrometric method for the determination of 7 anti-human immunodeficiency virus medications. Ther Drug Monit. 2008 Oct;30(5):611-9. Abstract Full text (link to original source)

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