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Pharmacological Management of the Patient with Obesity
Published in James M. Rippe, Lifestyle Medicine, 2019
Magdalena Pasarica, Nikhil V. Dhurandhar
A three-year orlistat study involved 383 adults who had abdominal obesity and metabolic risk factors, including dyslipidemia, impaired fasting glucose, and diet-treated type 2 diabetes. The study aim was to investigate the effect of orlistat on weight regain and cardiovascular risk factors following a very-low-energy diet (VLED). Subjects who lost at least 5% of their body weight (309 of 383 subjects) were then randomized to receive lifestyle counseling together with a placebo or orlistat of 120 mg, three times a day for three years. Study results identified that compared to the placebo group, orlistat plus lifestyle intervention resulted in an additional 2.4 kg weight loss after VLED and a reduced occurrence of type 2 diabetes for up to three years. The authors concluded that orlistat may be a useful adjunct to conventional dietary and lifestyle treatment of high-risk subjects with obesity.39
Pharmacological Treatment of Obesity
Published in Emmanuel C. Opara, Sam Dagogo-Jack, Nutrition and Diabetes, 2019
Amie A. Ogunsakin, Ayotunde O. Dokun
Orlistat is a lipase inhibitor that reduces fat absorption from intestines. It was FDA approved in 1999. Orlistat, a semisynthetic derivative of lipstatin, is a potent and selective inhibitor of these enzymes, with little or no activity against amylase, trypsin, chymotrypsin, and phospholipases. Orlistat acts by binding covalently to the serine residue of the active site of gastric and pancreatic lipases (Figure 7.1). When administered with fat-containing foods, orlistat partially inhibits hydrolysis of triglycerides, thus reducing the subsequent absorption of monoacylglycerides and free fatty acids [60–62]. Orlistat blocks absorption of 25%–30% of fat calories and is not appreciably absorbed systemically. The drug is available over the counter at a dosage of 60 mg TID. The recommended prescription dosage is 120 mg TID, and this dose should not be exceeded, as there is no evidence from clinical trials that efficacy is greater at higher dosages. Orlistat 120 mg TID has been studied and approved for treatment of adolescents with obesity [23,31,33].
Obesity
Published in Andrew Stevens, James Raftery, Jonathan Mant, Sue Simpson, Health Care Needs Assessment, 2018
John Garrow, Carolyn Summerbell
Orlistat is a drug that inactivates the enzymes that digest fat in the human small intestine, and thus reduces fat absorption by about 30%. The results of RCTs are reviewed in section 6. In very large, multicentre, international trials orlistat has been shown to cause greater weight loss in obese subjects on a low-fat diet than that observed in control subjects; this difference is statistically significant (since the trials involved about 1000 subjects) but clinically not very impressive.
Evaluation of the toxicology, anti-lipase, and antioxidant effects of Callistemon citrinus in rats fed with a high fat-fructose diet
Published in Pharmaceutical Biology, 2022
Luis Gerardo Ortega-Pérez, Jonathan Saúl Piñón-Simental, Oliver Rafid Magaña-Rodríguez, Alejandro Lopéz-Mejía, Luis Alberto Ayala-Ruiz, Aram Josué García-Calderón, Daniel Godínez-Hernández, Patricia Rios-Chavez
One of the strategies in the prevention of obesity is to change lipid metabolism by inhibiting fat absorption (Gholamhose et al. 2009). Orlistat is one of the few drugs used for obesity treatment; it is a strong inhibitor of lipases, mainly pancreatic lipase, responsible for the digestion of dietary triacylglycerol into free fatty acids, and monoacylglicerol and diacylglycerol that can be absorbed by the organism (Zeng et al. 2018). However, orlistat can cause many side effects, some of them include oily spotting, increased bowel movements, abdominal pain, and headache among others. Mechanisms of action of phytochemicals comprise the following: inhibition of dietary lipid digestion via inhibition of pancreatic lipase activity, appetite regulation via hormones associated with food intake, and inhibition of white adipose tissue development via attenuation of oxidative stress in obesity (Sun et al. 2016).
Effect on the cardiovascular independent risk factor lipoprotein(a) in overweight or obese PCOS patients with ethinyl-estradiol/drospirenone alone or plus orlistat
Published in Gynecological Endocrinology, 2022
Muqing Gu, Xiangyan Ruan, Yanqiu Li, Tianhe Li, Chenghong Yin, Alfred O. Mueck
Combined oral contraceptives (COCs) are the first-line option for the long-term management of PCOS patients without fertility requirements. Fourth-generation COC formulations containing 20 μg ethinyl estradiol (EE) and 3 mg drospirenone (DRSP) worldwide are mostly used, and also widely used in China. Its beneficial effects include reducing acne, improving hirsutism, and correcting oligomenorrhea [7]. To manage overweight or obese PCOS patients, anti-obesity medications may be considered in addition to lifestyle changes. Orlistat is a reversible pancreatic lipase inhibitor that inhibits the absorption of 30% of ingested fat when eating a 30% fat diet. Orlistat is one of the most well-tolerated medications in this category [8]. Our previous research demonstrated that EE/cyproterone acetate (CPA) combined with orlistat is more effective than EE/CPA alone to reduce hyperandrogenism [9]. Another study showed that orlistat was associated with lower rates of overall major adverse cardiovascular events, new-onset heart failure, and mortality [10]. However, there are no studies on whether EE/DRSP and orlistat, commonly used in the long-term management of overweight or obese PCOS patients, affect cardiovascular risk factors, such as Lp(a) in PCOS patients. So, we designed this study to investigate the effect on the cardiovascular independent risk factor Lp(a) in overweight or obese PCOS patients with EE/DRSP alone or plus orlistat.
Pharmacotherapeutic options for prediabetes
Published in Expert Opinion on Pharmacotherapy, 2021
The lipase inhibitor orlistat works to lower weight by inducing fat malabsorption. It was studied in a 4 year trial of 3300 subjects with BMI of 30 kg/m2 or more [61]. Only 21% of the participants had abnormal glucose tolerance at baseline. Subjects received either 120 mg orlistat three times daily or placebo. After 4 years treatment, mean weight loss was significantly greater with orlistat (5.8 vs. 3.0 kg with placebo; P < 0.001), and the cumulative incidence of diabetes diagnosis was 9.0% with placebo and 6.2% with orlistat, corresponding to a risk reduction of 37.3% (P = 0.0032). However, the completion rate was only 52% for orlistat-treated subjects and even lower at 34% for the placebo cohort. The side effects of orlistat are due to fat malabsorption with greasy stools and occasional diarrhea.