Summary of Use during Lactation

Saquinavir is no longer marketed in the United States. No published information is available on the use of saquinavir during breastfeeding. Saquinavir is not a recommended agent during breastfeeding.[1,2] Achieving and maintaining viral suppression with antiretroviral therapy decreases breastfeeding transmission risk to less than 1%, but not zero. Individuals with HIV who are on antiretroviral therapy with a sustained undetectable viral load and who choose to breastfeed should be supported in this decision. If a viral load is not suppressed, banked pasteurized donor milk or formula is recommended.[3,4]

Drug Levels

Maternal Levels. Relevant published information was not found as of the revision date.

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Relevant published information was not found as of the revision date.

Effects on Lactation and Breastmilk

Gynecomastia has been reported among men receiving highly active antiretroviral therapy. Gynecomastia is unilateral initially, but progresses to bilateral in about half of cases. No alterations in serum prolactin were noted and spontaneous resolution usually occurred within one year, even with continuation of the regimen.[5-7] Some case reports and in vitro studies have suggested that protease inhibitors might cause hyperprolactinemia and galactorrhea in some male patients,[8,9] although this has been disputed.[10] The relevance of these findings to nursing mothers is not known. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

References

1.

AIDSinfo. Panel on treatment of pregnant women with HIV infection and prevention of perinatal transmission. Recommendations for use of antiretroviral drugs in transmission in the United States, 2018: Counseling and management of women living with HIV who breastfeed.

2.

World Health Organization. HIV and infant feeding: Update. 2007. http://whqlibdoc​.who​.int/publications/2007​/9789241595964_eng.pdf

3.

World Health Organization. Consolidated guidelines on HIV prevention, testing, treatment, service delivery and monitoring: recommendations for a public health approach. 2021. https://www​.who.int/publications​/i/item/9789240031593 [PubMed: 34370423]

4.

Department of Health and Human Services. Recommendations for the use of antiretroviral drugs during pregnancy and interventions to reduce perinatal HIV transmission in the United States. Infant feeding for individuals with HIV in the United States. 2023. https:​//clinicalinfohivgov​/en/guidelines​/perinatal/infant-feeding-individuals-hiv-united-states?view=full

5.

García-Benayas T, Blanco F, Martin-Carbonero L, et al. Gynecomastia in HIV-infected patients receiving antiretroviral therapy. AIDS Res Hum Retroviruses 2003;19:739-41. [PubMed: 14585204]

6.

Pantanowitz L, Evans D, Gross PD, Dezube BJ. HIV-related gynecomastia. Breast J 2003;9:131-2. [PubMed: 12603389]

7.

Evans DL, Pantanowitz L, Dezube BJ, Aboulafia DM. Breast enlargement in 13 men who were seropositive for human immunodeficiency virus. Clin Infect Dis 2002;35:1113-9. [PubMed: 12384846]

8.

Hutchinson J, Murphy M, Harries R, Skinner CJ. Galactorrhoea and hyperprolactinaemia associated with protease-inhibitors. Lancet 2000;356:1003-4. [PubMed: 11041407]

9.

Orlando G, Brunetti L, Vacca M. Ritonavir and saquinavir directly stimulate anterior pituitary prolactin secretion, in vitro. Int J Immunopathol Pharmacol 2002;15:65-8. [PubMed: 12593790]

10.

Montero A, Bottasso OA, Luraghi MR, et al. Galactorrhoea, hyperprolactinaemia, and protease inhibitors. Lancet 2001;357:473-5. [PubMed: 11273087]

Substance Name

Saquinavir

CAS Registry Number

127779-20-8

Drug Class

Breast Feeding

Lactation

Milk, Human

Anti-Infective Agents

Anti-HIV Agents

Antiviral Agents

Anti-Retroviral Agents

HIV Protease Inhibitors