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It is a gastric and pancreatic lipase inhibitor that limits the absorption of dietary fat by 30% ^{(Guerciolini 1997)}. Oral administration three times a day.

At latest update, relevant information on excretion into breast milk was not found.

However, because of pharmacokinetic data (a moderately high molecular-weight, a virtually nil absorption, and very high protein-binding-capacity), excretion of Orlistat into breast milk in significant levels is unlikely.

Orlistat has virtually no intestinal absorption ^{(Zhi 1995)}. Plasma ^{(AEMPS 2014)} and breast milk ^{(Musatadi 2021)} concentrations have been found at insignificant levels (<10 and <3 micrograms/L, respectively).

On long-standing basis, it may affect absorption of liposoluble vitamins (A, D, E, K), beta-carotenes and colesterol ^{(Mittendorfer 2001, Melia 1996)}. This would be a reason to recommend a varied diet which should be rich in consumption of fruits, vegetables. Vitamin supplementation should also be considered. Nutritional status of the nursing mother should be monitored.

Expert authors consider the use of orlistat to be safe or very probably safe during breastfeeding. ^{(Hale, LactMed, Briggs 2015)}

There is good quality evidence that exclusive breastfeeding helps to regain pre-pregnancy weight earlier than if breastfeeding is partial (mixed) or there is no breastfeeding, and that prolonged breastfeeding helps maintain that loss and as well as body fat loss.^{(Jayasinghe 2021, Schalla 2017, López 2016, Jarlenski 2014, Sámano 2013, Neville 2014, Hatsu 2008, Dewey 2004, 2001 y 1993, Kramer 1993)}