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Anti - Obesity

Orlistat STADA® 60mg/120 mg

Packaging:

Orlistat STADA®60 mg:    

Blister of 10 capsules. Box of 3 blisters, 6 blisters.                          

Blister of 21 capsules. Box of 2 blisters.

Orlistat STADA®120 mg:  

Blister of 21 capsules. Box of 2 blisters.

Compsition: 

Each Orlistat STADA® 60 mg capsule contains:

Orlistat (pellets)…………….……….....60 mg

Each Orlistat STADA® 120 mg capsule contains

Orlistat (pellets)……………………….120 mg

Shelf - Life:

24 months from the date of manufacturing.

 

  • Pharmacodynamics
  • Pharmacokinetics
  • Indications
  • Contraindications
  • Adverse Reactions
  • Dosage and Administration

  • Orlistat is a reversible inhibitor of lipases. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine residue site of gastric and pancreatic lipases. The inactivated enzymes are thus unavailable to hydrolyze dietary fat in the form of triglycerides into absorbable free fatty acids and monoglycerides. As undigested triglycerides are not absorbed, the resulting caloric deficit may have a positive effect on weight control. Systemic absorption of the drug is therefore not needed for activity.
  • Orlistat 60 mg taken three times daily blocks the absorption of approximately 25% of dietary fat. At the recommended therapeutic dose of 120 mg three times a day, orlistat inhibits dietary fat absorption by approximately 30%.
  • The effect of orlistat results in an increase in faecal fat as early as 24 to 48 hours after dosing. Upon discontinuation of therapy, faecal fat content returns to pre-treatment levels, usually within 48 to 72 hours.

  • Absorption: The extent of absorption of orlistat was minimal. Plasma concentrations of intact orlistat were non-measurable (< 5 ng/ml) eight hours following oral administration of orlistat. In general, at therapeutic doses, detection of intact orlistat in plasma was sporadic and concentrations were extremely low (< 10 ng/ml or 0.02 µmol), with no evidence of accumulation, which is consistent with minimal absorption.
  • Distribution: The volume of distribution cannot be determined because the drug is minimally absorbed and has no defined systemic pharmacokinetics. In vitro orlistat is > 99% bound to plasma proteins (lipoproteins and albumin were the major binding proteins). Orlistat minimally partitions into erythrocytes.
  • Metabolism: Based on a study in obese patients, of the minimal fraction of the dose that was absorbed systemically, two major metabolites, M1 (4-member lactone ring hydrolysed) and M3 (M1 with N-formyl leucine moiety cleaved), accounted for approximately 42% of the total plasma concentration. M1 and M3 have an open beta-lactone ring and extremely weak lipase inhibitory activity (1000- and 2500-fold less than orlistat respectively). In view of this low inhibitory activity and the low plasma levels at therapeutic doses (average of 26 ng/ml and 108 ng/ml respectively), these metabolites are considered to be pharmacologically inconsequential.
  • Elimination: Approximately 97% of the administered dose was excreted in faeces and 83% of that as unchanged orlistat. The cumulative renal excretion of total orlistat-related materials was < 2% of the given dose. The time to reach complete excretion (faecal plus urinary) was 3 to 5 days. The disposition of orlistat appeared to be similar between normal weight and obese volunteers. Orlistat, M1 and M3 are all subject to biliary excretion.

Orlistat is indicated in conjunction with a mildly hypocaloric diet for the treatment of obese patients as well as to reduce the risk for weight regain subsequent to initial loss in patients with a body mass index (BMI) greater or equal to 30 kg/m², or overweight patients (BMI) greater or equal to 27 kg/m²) with associated risk factors (e.g., hypertension, diabetes mellitus, hyperlipidemia).

  • Chronic malabsorption syndrome or cholestasis.
  • Known hypersensitivity to orlistat or any ingredient in the formulation.

Precautions:

  • Orlistat should be given with caution to patients with a history of hyperoxaluria or calcium oxalate nephrolithiasis. Adjustments to dosage of hypoglycaemics may be necessary in patients with type II diabetes because of improved metabolic control after weight loss in these patients. Supplements of fat-soluble vitamins may be necessary during long-term therapy, but they should be taken at least 2 hours before or after an orlistat dose or at bedtime. Hormonal contraceptive failure may occur in the event of severe diarrhoea with orlistat, and patients are advised to use an additional contraceptive method.

Drug Interactions:

  • Ciclosporin: A decrease in ciclosporin plasma levels has been observed in a drug-drug interaction study, when orlistat was administered concomitantly.
  • Acarbose: In the absence of pharmacokinetic interaction studies, the concomitant administration of orlistat with acarbose should be avoided.
  • Oral anticoagulants: When warfarin or other anticoagulants are given in combination with orlistat, international normalised ratio (INR) values should be monitored.
  • Fat soluble vitamins: Treatment with orlistat may potentially impair the absorption of fat-soluble vitamins (A, D, E and K).
  • Levothyroxine: Hypothyroidism has been reported in patients treated concomitanly with orlistat and levothyroxine postmarketing. Patients treated concomitanly with orlistat and levothyroxine should be monitored for changes in thyroid function. Administer levothyroxine and orlistat at least 4 hours apart.

Pregnancy and Lactation:

Pregnancy:

  • There are no adequate and well - controlled studies of orlistat in pregnant women. Orlistat is not recommended for use during pregnancy.

Lactation:

  • It is not known if orlistat is distributed in breast milk. Therefore, orlistat should not be taken by nursing women.
  • Effects on Ability to Drive and Use Machines: 
  • Orlistat has no influence on the ability to drive and use machines.

  • Gastrointestinal disturbances, including faecal urgency and incontinence, flatulence, and fatty stools or discharge, are the most frequently reported adverse effects during treatment with orlistat. They may be minimised by limiting the amount of fat in the diet.

Overdosage:

  • Single doses of 800 mg orlistat and multiple doses of up to 400 mg three times a day for 15 days have been studied in normal weight and obese subjects without significant adverse findings. Should a significant overdose of orlistat occur, it is recommended that the patient be observed for 24 hours. Systemic effects attributable to the lipase-inhibiting properties of orlistat should be rapidly reversible

Dosage:

  • Management of obesity and weight regain in adults and adolescents 12 years of age and older: 120 mg 3 times daily with each main meal containing fat.
  • Over weight adults 18 years of age and older: 60 mg 3 times daily with each meal containing fat.

Administration:

  • The capsule should be taken with water immediately before, during or up to 1 hour after each main meal. If a meal is missed or contains no fat, the dose of orlistat should be omitted.
  • Dosage exceeding 3 times daily have not been shown to provide additional benefit.
  • If patients have been unable to lose weight after 12 weeks of treatment with Orlistat STADA®, they should consult their doctor or a pharmacist. It may be necessary to discontinue treatment.

Remarks:

  • Diet and exercise are important parts of a weight loss programme. It is recommended that a diet and exercise programme is started before beginning treatment with Orlistat STADA®.
  • The patient should be on a nutritionally balanced, mildly hypocaloric diet that contains approximately 30% of calories from fat. The daily intake of fat, carbohydrate and protein should be distributed over three main meals.
  • The diet and exercise programme should continue to be followed when treatment with Orlistat STADA® is stopped.
  • The safety and effectiveness beyond 4 years have not been determined at this time.
  • Pediatric use: Safety and efficacy in children younger than 12 years of age not established.
  • There are limited data on the use of orlistat in the elderly. The effect of orlistat in individuals with hepatic and/or renal impairment has not been studied. However, as orlistat is minimally absorbed, no dosage adjustment is necessary in elderly and in individuals with hepatic and/or renal impairment.

Contact us

FACTORY 1: K63/1 Nguyen Thi Soc St., Xuan Thoi Dong, Hoc Mon, HCMC
Tel: +84 28 3718 2141 - Fax: +84 28 3718 2140

FACTORY 2: 40 Tu Do Avenue, VietNam-Singapore Industrial Park, Binh Duong
Tel: +84 274 376 7470 - Fax: +84 274 376 7469
Email : stada@stada.com.vn
Website: www.stada.com.vn



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