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FORBICAL 120 MG Capsules

Quick Overview

Our aim is to reach out to the globe with in shortest possible time frame.

To promote this objective, not only we distribute and market our range of products globally through our distribution channels but we also undertake ‘contract manufacturing’& ‘formulation development ’of our wide range of generic products such as FORBICAL 120 MG which contains Orlistat 120mg

FORBICAL 120 MG Capsules

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Details

For the use of Registered Medical Practitioner or a Hospital or a Laboratory only.

Orlistat Capsules 120 mg

 

FORBICAL 120

Composition

Each Capsule contains:

Orlistat             120 mg (As Pellets)

Excipients              q.s.

Approved Colour Used for Capsule Shells

 

Chemical Name

(S)-2-formylamino-4-methyl-pentanoic acid (S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]-dodecyl ester.

 

Category

Long-acting inhibitor of gastrointestinal lipases.

 

Pharmacology

Pharmacodynamics

Orlistat is a reversible inhibitor of gastrointestinal 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. At the recommended therapeutic dose of 120 mg three times a day, orlistat inhibits dietary fat absorption by approximately 30%. Ethanol does not affect orlistat's effect on preventing the absorption of fat.

 

Pharmacokinetic

Absorption: Reported studies in normal weight and obese volunteers have shown that the extent of absorption of Orlistat was minimal. Plasma concentrations of intact Orlistat were non-measurable (<5 mg/ml) 8 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 mg/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 active substance 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 animal data, it is likely that the metabolism of Orlistat  occurs mainly within the gastrointestinal wall. 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 (1,000 and 2,500-fold less than Orlistat, respectively). In view of this low inhibitory activity and the low plasma levels at therapeutic doses (average of 26 mg/ml and 108 mg/ml, respectively), these metabolites are considered to be pharmacologically inconsequential.

 

Elimination: Reported studies in normal weight and obese subjects have shown that faecal excretion of the unabsorbed active substance was the major route of 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.

 

Indications

Orlistat is indicated in conjunction with a mildly hypocaloric lower-fat diet for the treatment of obese patients with a body mass index (BMI) greater or equal to 30 kg/m², or overweight patients (BMI > 28 kg/m²) with associated risk factors.

 

Treatment with Orlistat should be discontinued after 12 weeks if patients have been unable to lose at least 5 % of the body weight as measured at the start of therapy.

 

Contraindications

Orlistat is contraindicated in hypersensitivity to the active substance or to any of the excipients. Orlistat is also contraindicated in Concurrent treatment with ciclosporin, chronic malabsorption syndrome, Cholestasis, Pregnancy, Breast-feeding and concurrent treatment with warfarin or other oral anticoagulants.

 

Pregnancy and Lactation

Pregnancy

Pregnancy Category X

 

Orlistat is contraindicated during pregnancy, because weight loss offers no potential benefit to a pregnant woman and may result in fetal harm. A minimum weight gain, no weight loss, is currently recommended for all pregnant women, including those who are already overweight or obese, due to the obligatory weight gain that occurs in maternal tissues during pregnancy.

 

Nursing Mothers

It is not known if orlistat is present in human milk. Caution should be exercised when orlistat is administered to a nursing woman.

 

Pediatric Use

Safety and effectiveness in pediatric patients below the age of 12 have not been established.

 

Effect to drive and use the machine

Orlistat has no influence on the ability to drive and use machines.

 

Warning and Precaution

Patients should be advised to adhere to the dietary recommendations they are given. The possibility of experiencing gastrointestinal symptoms may increase when Orlistat is taken with an individual meal or a diet high in fat.

 

Treatment with Orlistat may potentially impair the absorption of fat-soluble vitamins (A, D, E & K). For this reason, a multivitamin supplement should be taken at bedtime. As weight loss may be accompanied by improved metabolic control in diabetes, patients who are taking a medicinal product for diabetes should consult a doctor before starting treatment with Orlistat, in case it is necessary to adjust the dose of the antidiabetic medicinal product. Weight loss may be accompanied by an improvement in blood pressure and cholesterol levels. Patients who are taking a medicinal product for hypertension or hypercholesterolemia should consult a doctor or pharmacist when taking Orlistat, in case it is necessary to adjust the dose of these medicinal products.

 

Patients who are taking amiodarone should consult a doctor before starting treatment with Orlistat.

Cases of rectal bleeding have been reported in patients taking  Orlistat. If this occurs, the patient should consult a doctor. The use of an additional contraceptive method is recommended to prevent possible failure of oral contraception that could occur in case of severe diarrhoea. Patients with kidney disease should consult a doctor before starting treatment with Orlistat, as the use of Orlistat may rarely be associated with hyperoxaluria and oxalate nephropathy.

 

Hypothyroidism and/or reduced control of hypothyroidism may occur when Orlistat and levothyroxine are co-administered. Patients taking levothyroxine should consult a doctor before starting treatment with Orlistat, as Orlistat and levothyroxine may need to be taken at different times and the dose of levothyroxine may need to be adjusted.

 

Patients taking an antiepileptic medicinal product should consult a doctor before starting treatment with Orlistat, as they should be monitored for possible changes in the frequency and severity of convulsions. If this occurs, consideration could be given to administering Orlistat and antiepileptic medicinal products at different times.

 

Interactions

Ciclosporin: A decrease in ciclosporin plasma levels has been observed in a drug-drug interaction study and also reported in several cases, when Orlistat was administered concomitantly. This could potentially lead to a decrease of immunosuppressive efficacy. Concurrent use of Orlistat and ciclosporin is contraindicated.

 

Oral anticoagulants: When warfarin or other oral anticoagulants are given in combination with Orlistat, international normalised ratio (INR) values could be affected. Concurrent use of Orlistat and warfarin or other oral anticoagulants is contraindicated.

 

Oral contraceptives: The absence of an interaction between oral contraceptives and Orlistat has been demonstrated in specific drug-drug interaction studies. However, Orlistat may indirectly reduce the availability of oral contraceptives and lead to unexpected pregnancies in some individual cases. An additional contraceptive method is recommended in case of severe diarrhoea.

 

Levothyroxine: Hypothyroidism and/or reduced control of hypothyroidism may occur when Orlistat and  levothyroxine are taken at the same time. This could be due to a decreased absorption of iodine salts and/or levothyroxine.

 

Antiepileptic medicinal products: Convulsions have been reported in patients treated concomitantly with Orlistat and antiepileptic medicinal products e.g. valproate, lamotrigine, for which a causal relationship to an interaction cannot be excluded. Orlistat may decrease the absorption of antiepileptic medicinal products, leading to convulsions.

 

Fat soluble vitamins: Treatment with Orlistat may potentially impair the absorption of fat-soluble vitamins (A, D, E & K). In the reported study, the vast majority of subjects receiving up to 4 full years of treatment with Orlistat  in clinical studies had vitamin A, D, E and K and beta-carotene levels that stayed within normal range. However, patients should be advised to use a multivitamin supplement at bedtime to help ensure adequate vitamin intake.

 

Acarbose: In the absence of pharmacokinetic interaction studies, Orlistat  is not recommended to be used by patients receiving acarbose.

 

Amiodarone: A decrease in plasma levels of amiodarone, when given as a single dose, has been observed in a limited number of healthy volunteers who received Orlistat concomitantly. The clinical relevance of this effect in patients receiving amiodarone treatment remains unknown. Patients who are taking amiodarone should consult a doctor before starting treatment with Orlistat. The dose of amiodarone may need to be adjusted during treatment with Orlistat.

 

Adverse Reactions

Adverse reactions to Orlistat are largely gastrointestinal in nature and related to the pharmacologic effect of the medicinal product on preventing the absorption of ingested fat.

 

Consumption of a diet low in fat will decrease the likelihood of experiencing adverse gastrointestinal reactions.

 

Dosage and Administration

Adults:  The recommended dose of orlistat is one 120 mg capsule taken with water immediately before, during or up to one hour after each main meal. If a meal is missed or contains no fat, the dose of orlistat should be omitted.

 

Doses of orlistat above 120 mg three times daily have not been shown to provide additional benefit.

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 usually returns to pre-treatment levels, within 48 to 72 hours.

While taking Orlistat, the patient should be on a nutritionally balanced, mildly hypocaloric diet that contains approximately 30% of calories from fat (e.g. in a 2,000 kcal/day diet, this equates to <67 g of fat). The daily intake of fat, carbohydrate and protein should be distributed over three main meals.

The diet and exercise program should continue to be followed when treatment with Orlistat is stopped.

If patients have been unable to lose weight after 12 weeks of treatment with Orlistat, they should consult their doctor or a pharmacist. It may be necessary to discontinue treatment.

Diet and exercise are important parts of a weight loss program. It is recommended that a diet and exercise program is started before beginning treatment with Orlistat.

 

Special populations: Orlistat should not be used in children and adolescents below 18 years of age due to insufficient data on safety and efficacy.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.

 

Overdosage

Reported overdosage cases have shown either no adverse reactions that are similar to those reported with recommended doses of orlistat.

 

In the event of an overdose, medical advice should be sought. Should a significant overdose of Orlistat occur, it is recommended that the patient be observed for 24 hours. Based on human and animal studies, any systemic effects attributable to the lipase-inhibiting properties of Orlistat should be rapidly reversible.

Presentation

 

90 capsules in HDPE container

 

Storage

Store below 30°C. Protect from light and moisture.

Keep out of reach of children.

Last update: June 2014.