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xenicalXenical

Peripherally acting anti-obesity agent

 

1. Pharmaceutical Form

Capsule, hard

It is presented as turquoise cap and turquoise body bearing the imprint of "ROCHE XENICAL 120"

 

2. Qualitative and quantitative Composition

Active ingredient : orlistat

Capsules 120mg.

Excipients : Capsule filling : microcrystalline cellulose, sodium starch glycollate, povidone, sodium lauryl sulphate and talc.

Capsule shell : gelatine, indigo carmine ( E132 ) and titamium dioxide ( E171 )

 

3.Clinical Particulars

3.1 Therapeutic Indications

Xenical is indicated, in conjunction with a mildly hypocaloric diet for the treatment of obese ( BMI ≥ 30kg/m2 ) and overweight ( BMI ≥ 28kg/m2 ) patients, including patients with risk factors associated with obesity. Xenical is effective in weight loss, weight maintenance and prevention of weight regains. Treatment with Xenical results in an improvement of risk factors and comorbidities associated with obesity, including hypercholesterolemia, non-insulin dependent diabetes mellitus ( NIDDM ), impaired glucose tolerance, hyperinsulinemia, hypertension and in a reduction of visceral fat.

 

In type 2 diabetic patients who are overweight ( BMI ≥ 28kg/m2 ) or obese ( BMI ≥ 30kg/m2 ) Xenical, in conjunction with a mildly hypocaloric diet, provides additional glycemic control when used in combination with antidiabetic agents such as metformin, sulfonylurea and/or insulin.

 

Treatment with Xenical should only be started if diet alone has previously produced a weight loss of at least 2.5kg over a period of 4 consecutive weeks. 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 drug therapy.

 

3.2 Dosage and administration

3.2.1 Standard Dosage

The recommended dose of Xenical is one 120mg capsule with each main meal ( during or up to one hour after the meal ). If a meal is missed or contains no fat, the dose of Xenical may be omitted. 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.

 

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

 

3.2.2 Special Dosage Instruction

Clinical investigation in patients with hepatic and /or renal impairment and children under the age of 12 have not been undertaken.

 

3.3 Contraindications

Xenical is contraindicated in patients with chronic malabsorption syndrome, cholestasis and in patients with known hypersensitivity to orlistat or any of the other components contained in the medicinal product.

 

3.4 Special Warnings and Special Precautions For Use

The majority of patients in longterm studies of up to four years of treatment had vitamin A, D, E and K and beta-carotene levels within normal range. In order to ensure adequate nutrition, the use of a multivitamin supplement could be considered.

 

Patients should be advised to adhere to dietary guidelines ( see Dosage and administration ).

 

The possibility of experiencing gastrointestinal events ( see Undesirable effects ) may increase when Xenical is taken with a diet high in fat ( eg in a 2000 calorie/day diet, >30% of calories from fat equates to >67g of fat ). The daily intake of fat should be distributed over three main meals. If Xenical is taken with any one meal very high in fat, the possibility of gastrointestinal effects may increase.

 

Weight loss induced by Xenical is accompanied by improved metabolic control in type 2 diabetics which might allow or require reduction in the dose of oral hypoglycemic medication ( eg sulfonylureas ).

 

A reduction in cyclosporin plasma levels has been observed when Xenical is co-administered. Therefore it is recommended to monitor more frequently than usual the cyclosporin plasma levels when Xenical is co-administered ( see Interactions ).

 

Coagulation parameters should be monitored in patients treated with concomitant oral anticoagulants.

 

In a PK study, oral administration of amiodarone during orlistat treatment demonstrated a 25 - 30% reduction in the systemicexposure to amiodarone and desethylamiodarone. Due to the complex pharmacokinetics of amiodarone, the clinical effect of this is unclear. The effect of commencing orlistat treatment in patients on stable amiodarone therapy has not been studied. A potential reduced therapeutic efffect of amiodarone is possible.

 

Substantial weight loss can increase the risk of cholelithiasis. In a clinical trial of Xenical for the prevention of type 2 diabetes, the rates of cholelithiasis as an adverse event were 2.9% ( 47/1649 ) for patients randomized to Xenical and 1.8% ( 30/1655 ) for patients randomized to placebo. In this trail, the incidence of cholelithiasis ( gallstones ) was similar for Xenical and placebo at similar amounts of weight loss. No increase in cholelithiasis with xenical was seen in trials that were not evaluating the prevention of type 2 diabetes.

 

3.5 Interactions With Other Medicinal Products and Other Forms Of Interaction
No interactions based on specific drug-drug-interaction studies with amitriptyline, atorvastatin, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, pravastatin, warfarin, nifedipine Gastrointestinal Therapeutic System, nifedipine slow release, sibutramine or alcohol have been observed.


However, when warfarin or other anticoagulants are given in combination with orlistat, international normalized ratio (INR) values should be monitored.


Decreases in the absorption of vitamin D, E and G3-carotene have been observed when co-administered with Xenical. If a multivitamin supplement is recommended, it should be taken at least two hours after the administration of Xenical or at bedtime. A reduction in cyclosporin plasma levels has been observed when Xenical is co-administered. Therefore it is recommended to monitor more frequently than usual the cyclosporin plasma levels when Xenical is co-administered (see Special Warnings and Special Precautions For Use).


In a PK study, oral administration of amiodarone during orlistat treatment demonstrated a 25 - 30% reduction in the systemic exposure to amiodarone and desethylamiodarone. Due to the complex pharmacokinetics of amiodarone, the clinical effect of this is unclear. The effect of commencing orlistat treatment in patients on stable amiodarone therapy has not been studied. A reduced therapeutic effect of amiodarone is possible.

 

3.6 Pregnancy and Lactation
In animal reproductive studies, no embryotoxic or teratogenic effects were observed with orlistat.
In absence of a teratogenic effect in animals, no malformative effect is expected in human beings. However, Xenical is not rec
ommended for use during pregnancy in the absence of clinical data. The secretion of orlistat in human breast milk has not been investigated. Xenical should not be taken during breast-feeding.

 

3.7 Effects on Ability to Drive and Use Machine

No information available


3.8 Undesirable effects


3.8.1 Experience from clinical trials
Adverse reactions to Xenical are largely gastrointestinal in nature and related to the pharmacologic effect of the drug in preventing the absorption of ingested fat. Commonly observed events are oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, increased defecation and fecal incontinence.

 

The incidence of these increases the higher the fat content of the diet. Patients should be counseled as to the possibility of gastrointestinal effects occurring and how best to handle them such as reinforcing the diet, particularly the percentage of fat it contains.


Consumption of a diet low in fat will decrease the likelihood of experiencing adverse gastrointestinal events and this may help patients monitor and regulate their fat intake. These adverse gastrointestinal reactions are generally mild and transient. They occurred early in treatment (within 3 months) and most patients experienced only one episode.

 

Treatment-emergent GI-adverse events that occurred commonly among patients treated with Xenical were: abdominal pain/discomfort, flatulence, liquid stools, soft stools, rectal pain/discomfort, tooth disorder, gingival disorder.

 

Other events observed were: upper respiratory infection, lower respiratory infection; influenza; headache; menstrual irregularity; anxiety; fatigue; urinary tract infection.


Unique treatment adverse events observed in obese type 2 diabetic patients were hypoglycemia (very common) and abdominal distension (common). Weight loss induced by Xenical is accompanied by improved metabolic control in type 2 diabetics which might allow or require reduction in the dose of hypoglycemic medication (see Special Warnings and Special Precautions for Use).


In a 4 year clinical trial, the general pattern of adverse events distribution was similar to that reported for the 1 year and 2 year studies with the total incidence of gastrointestinal related adverse events occurring in year 1 decreasing year on year over the four year period.


In type 2 diabetic patients, adverse event reporting was comparable to that reported in overweight and obese patients. The only unique treatment adverse events that occurred at a frequency of >2% and with an incidence ? 1% above placebo were hypoglycemia (which may occur as a result of improved glycaemic control) and abdominal distention.


3.8.2 Post-marketing experience
Rare cases of hypersensitivity have been reported. Main clinical symptoms are pruritus, rash, urticaria, angioedema, bronchospasm and anaphylaxis.


Very rare cases of bullous eruption, increase in liver transaminases and in alkaline phosphatase and exceptional cases of hepatitis that may be serious have been reported during the post marketing. No causal relationship or physiopathological mechanism between hepatitis and orlistat therapy has been established.


Reports of decreased prothrombin, increased INR and unbalanced anticoagulant treatment resulting in change of haemostatic parameters have been reported in patients treated concomitantly with orlistat and anticoagulants during post-marketing.


3.9 Overdose
Single doses of 800 mg Xenical and multiple doses of up to 400 mg t.i.d. for 15 days have been studied in normal weight and obese subjects without significant adverse findings. In addition, doses of 240 mg t.i.d. have been administered to obese patients for 6 months without significant increase of adverse findings. Orlistat overdose cases received during post-marketing reported either no adverse events or adverse events that are similar to those reported with recommended dose. Should a significant overdose of Xenical 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.

 

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