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Orlistat : 

Orlistat Drug Review HOD Medicine Dr K.A.S Murthy Chairperson Dr Vijay Cheluvaraj By Dr.Abhijit Bhograj

Introduction : 

Introduction Primary used as an anti obesity drug. Secondary use as a Drug in the prevention of onset of T2DM in obese patients . Coronary arteriosclerosis Prophylaxis. Anti hypertensive co therapy. Hyperlipidemia.

Slide 3: 

Works by inhibiting gastric and pancreatic lipases. When lipase activity is blocked, triglycerides from the diet are not hydrolyzed into absorbable free fatty acids and are excreted undigested . Orlistat prevents approximately 30% of dietary fat from being absorbed.

Action/Pharmacology/Drug Dynamics : 

The drugs systemic absorption is minimal . T max is 8 hours More than 99% of the drug is protein bund to plasma , mainly albumin and lipoprotein. Metabolism occur in the GI wall forming 2 metabolites M1 and M3. The absorbed drug has a half life of 1-2 h The metabolites have a half life of 3-13 h The metabolites are excreted in bile while 97% of the drug is eliminated through feces less than 2% of the drug is eliminated in the urine . Action/Pharmacology/Drug Dynamics

Contraindications/ Precautions : 

Contraindications/ Precautions Contraindications A)  Cholestasis B)  Chronic malabsorption syndrome C)  Hypersensitivity to orlistat products Precautions A)  Clinically significant GI disease B)  Exclude any organic causes of obesity before treatment C)  Patients at risk for fat-soluble vitamin deficiency

Side Effects : 

Side Effects Gastrointestinal (GI) symptoms were the most commonly observed treatment-emergent adverse events associated with the use of Orlistat in the seven double-blind placebo-controlled clinical trials. Overall, approximately 50% of all episodes of GI adverse events associated with orlistat treatment lasted for less than 1 week, and a majority lasted for no more than 4 weeks Commonly observerd non GI side effects include Influenza symptoms 40%Headache 30% ,back pain14%

Slide 8: 

The US Food and Drug Administration's Adverse Event Reporting System has received 32 reports of serious liver injury, including 6 cases of liver failure, and 27 hospitalizations in patients receiving orlistat therapy. The most commonly reported adverse events in the 32 reports were jaundice, weakness, and abdominal pain. No definitive association between liver injury and orlistat has been established

Interactions : 

Interactions Beta-carotene –Plasma concentration may be reduced by the use of orlistat Fat Soluble Vitamins – 30% reduction in beta carotene supplement absorption was shown when administered with orlistat . Vit E vit D and A are all effected to some extent orlistat and cyclosporine drug interaction study indicate a reduction in cyclosporine plasma levels Warfarin – Vit K levels tend to decline in patients taking orlistat with the result that a lower dose of warfarin is required . patients on warfarin have to have their coagulation parameters monitored closely.

Slide 11: 

Concomitant use of levothyroxine and orlistat may decrease levothyroxine efficacy by binding to and delaying or preventing levothyroxine absorption, potentially resulting in hypothyroidism. If concurrent use is necessary, separate administration of these agents by at least 4 hours and monitor for changes in thyroid function

Monitoring Parameters : 

Monitoring Parameters Total, low-density lipoprotein, high-density lipoprotein, and very-low-density lipoprotein cholesterol levels, and serum triglycerides periodically during treatment   Body weight   Laboratory Parameters   Plasma levels of vitamins A, D, and E   In patients receiving higher doses of orlistat (ie, 360 mg daily or greater) for any duration, or during prolonged periods of administration of lower doses (eg, longer than 2 months), particularly in patients at risk of deficiency (eg, poor dietary habits)   Physical Findings should be watched for Signs/symptoms of orlistat gastrointestinal adverse events

Dosage : 

Dosage Adult and children > 12 years - 120 mg TID 1hour After taking food . Patients should be on nutritionally balanced ,reduced calorie diet that contains 30% calories from fat . Daily Fat ,Carbs and protein intake should be distributed over 3 main meals. If a meal is missed or contains no fat the orlistat dose should be omitted . Suplimentation of Multivitamins should be taken at least 2h before or after taking orlistat

Literature : 

Literature Long-term changes in blood pressure following orlistat and sibutramine treatment: a meta-analysis- The objective of this study was to estimate the effects on systolic (SBP) and diastolic blood pressure (DBP) of orlistat and sibutramine Weight reduction is known to decrease blood pressure by reductions in blood volume, left ventricular mass, cardiac output, sympathetic activity, renin activity, aldosterone and insulin levels. Orlistat in the prevention of diabetes in the obese patient XENDOS study – this study shows that Free fatty acids are increased in obesity and reduce insulin clearance and increase hepatic glucose production Orlistat is an inhibitor of lipase activity, with proved efficacy in body weight reduction and long-term management of obesity and more favorable effects on carbohydrate metabolism.

Slide 15: 

Orlistat and LDL Cholesterol 2006 Annual Scientific Meeting of NAASO, The Obesity Society, Found that orlistat (60 mg) in conjunction with a reduced-calorie diet, provided greater reductions in LDL cholesterol and weight loss when compared with placebo and a reduced-calorie diet. The results were based on two multi-center, double-blind, randomized, placebo-controlled clinical trials of 576 patients which were conducted over a 2-year period.

Orlistat for Nonalcoholic Fatty Liver Clin Gastroenterol Hepatol. 2006 May;4(5):639-44 : 

Orlistat for Nonalcoholic Fatty Liver Clin Gastroenterol Hepatol. 2006 May;4(5):639-44 A double-blind randomized placebo-controlled trial . 52 patients with NAFLD and confirmed by liver biopsy . The patients were randomized to receive either orlistat (120 mg 3 times daily for 6 months) or placebo. Fifty-two patients were recruited and 44 completed the study. Serum glucose and insulin levels were significantly higher in the orlistat group, which also presented a higher degree of fibrosis. Serum ALT levels decreased significantly in orlistat group (48% vs 26%). There was a statistically significant reversal of fatty liver in the orlistat group. Orlistat improves serum ALT levels and steatosis in NAFLD patients.

The efficacy of orlistat vs. sibutramine in the treatment of obesity: A systematic literature reviewLindsay Kloer PA-S*, Sue Nyberg MHS, PA-C : 

The efficacy of orlistat vs. sibutramine in the treatment of obesity: A systematic literature reviewLindsay Kloer PA-S*, Sue Nyberg MHS, PA-C There were 18 randomized controlled trials demonstrating the effectiveness of both medications to produce weight loss. Orlistator & sibutramine both showed 5-10% weight loss. 10 level 1 randomized controlled trials demonstrating the management of the weight loss for up to 2 years, both orlistat or sibutramine can be used in the long-term management of weight loss. Conclusion: Both medications are effective, selection of which medication to prescribe is primarily determined which has least side effect on the patient

Indian Brands : 

Indian Brands Average cost Rs 400 – 250 for 10 caps 120mg COBESE cap® [ Ranbaxy ] OBELIT tab® [ Intas ]   ORLICA cap® [ Torrent (Azuca)] ORLIMAC tab® [ Macleods ]  ORLITROY cap® [ Troikaa ]  REESHAPE cap® [ Meyer ]  TROYSLIM cap® [ Troikaa ]  VYFAT cap® [ Intas ]  ZEROFAT HG-cap® [ Mankind (Discovery) ]

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