Orlistat (Xenical) - Uses, Dose, Side effects, Brand Names

Xenical (Orlistat, Orslim) inhibits gastric and pancreatic lipases resulting in the inhibition of dietary fats absorption.

Orlistat Uses:

It is used as an adjunct to a low-calorie diet and exercise for the management of obesity.

It is available at a lower dose as OTC medicine for weight loss. For the treatment of obesity that may include losing weight and maintaining weight loss, higher doses may be used that require a prescription. It is only indicated for weight loss if the BMI is 30 kg/m² or more or if the BMI is 27 kg/m² or more in the presence of other risk factors like diabetes, hypertension, and dyslipidemia. It is among the five prescription weight loss pills approved by the AACE (American association of clinical endocrinologyy) and ACE (American college of Endocrinologist)

Orlistat (Xenical) Dose in Adults:

Xenical dose in the treatment of Obesity management: 

    • 120 mg thrice daily with each major meal that contains fats.
    • It should be taken during the meal or at least up to one hour after the meal.
    • If the meal is missed or does not contain any fats, the dose should be missed.
  • Alli (over the counter OTC labeling)

    • 60 mg thrice daily with each major meal that contains fats to the maximum dose of 180 mg/day).
  • Orlistat dose adjustment with concomitant therapy:

    • Cyclosporine:

      • Administer cyclosporine at least three hours after orlistat.
    • Levothyroxine:

      • Levothyroxine and orlistat should be taken at least four hours apart.
      • Thyroid functions should be monitored.

Orlistat (Xenical) dose in Childrens

Orlistat (Xenical) dose in the treatment of Obese children:

  • Children 12 years of age or older: Refer to adult dosing

Pregnancy Risk Factor X

  • Orlistat was not studied in pregnant women.
  • A healthy pregnancy is marked by a slight weight gain. Moderate weight gain should be ignored.
  • Orlistat is not recommended for use during pregnancy or during conception due to potential adverse effects.

Orlistat use during breastfeeding:

  • It is unknown if the drug will be excreted into breastmilk.
  • The drug is not well absorbed systemically and the manufacturer suggests that breastfeeding mothers avoid it.

Orlistat (Xenical) dose in Kidney disease:

  • The manufacturer has not recommended any dose adjustment in patients with renal disease.
  • The risk of oxalate nephropathy and oxalate nephrolithiasis exist.
  • Patients should be monitored for changing the deteriorating renal profile.

Orlistat (Xenical) Dose in liver disease:

  • Although, the drug is minimally absorbed, cases of liver failure have been reported with its use.
  • Patients with preexisting liver disease should avoid taking orlistat.
  • The manufacturer, however, has not recommended any adjustment in the dose in patients with liver disease.

Side effects of Orlistat (Xenical):

  • Cardiovascular:

    • Pedal Edema
  • Central Nervous System:

    • Headache
    • Fatigue
    • Anxiety
    • Sleep Disorder
  • Dermatologic:

    • Xeroderma
  • Endocrine & Metabolic:

    • Menstrual Disease
    • Hypoglycemia
  • Gastrointestinal:

    • Oily Rectal Leakage
    • Abdominal Distress
    • Abdominal Pain
    • Flatulence With Discharge
    • Bowel Urgency
    • Steatorrhea
    • Oily Evacuation
    • Frequent Bowel Movements
    • Nausea
    • Fecal Incontinence
    • Infectious Diarrhea
    • Rectal Pain
    • Gingival Disease
    • Cholelithiasis
    • Abdominal Distension
  • Genitourinary:

    • Urinary Tract Infection
    • Vaginitis
  • Infection:

    • Influenza
  • Neuromuscular & Skeletal:

    • Back Pain
    • Leg Pain
    • Myalgia
  • Otic:

    • Otitis
  • Respiratory:

    • Upper Respiratory Tract Infection
    • Lower Respiratory Tract Infection

Contraindications to Xenical (Orlistat):

  • Allergy reactions to orlistat and any component of the formulation
  • Pregnancy.
  • Chronic malabsorption syndrome.
  • Cholestasis

Warnings and precautions

  • Cholelithiasis

    • A higher risk of developing gallstones may be associated to weight loss that is rapid and significant.
  • Hepatotoxicity:

    • Orlistat has been linked to acute liver failure and cases hepatocellular necrosis. This may require liver transplantation.
    • Patients taking orlistat should report any clinical signs of liver disease, such as loss of appetite, itching and jaundice, dark urines, light-colored stool, right upper quadrant pain, nausea and vomiting.
    • In such cases, Orlistat should immediately be discontinued and liver function tests performed.
  • Increased urinary oxalate

    • Oxalate kidney stones can be a problem for patients. Patients may also develop oxalate renal disease. Orlistat could increase urinary oxalate excretion.
    • Renal failure may be caused by nephropathy or oxalate kidney stones.
    • Patients at high risk for renal failure should have their renal function monitored.
    • Patients suffering from hyperoxaluria and calcium oxalate renallithiasis need to be closely monitored.
  • Diabetes:

    • Diabetes patients should be closely monitored.
    • Because of impaired absorption, weight loss, or loss of calories, these patients may need to be adjusted in anti-diabetic medications.

Orlistat: Drug Interaction

Risk Factor C (Monitor therapy)

Amiodarone

Orlistat may decrease the serum concentration of Amiodarone.

Anticonvulsants

Orlistat may decrease the serum concentration of Anticonvulsants. Exceptions: Fosphenytoin; PENTobarbital; Thiopental.

Antiretroviral Agents

Orlistat may decrease the serum concentration of Antiretroviral Agents.

Propafenone

Orlistat may decrease the serum concentration of Propafenone.

Vitamin K Antagonists (eg, warfarin)

Orlistat may enhance the anticoagulant effect of Vitamin K Antagonists.

Risk Factor D (Consider therapy modification)

CycloSPORINE (Systemic)

Orlistat may decrease the serum concentration of CycloSPORINE (Systemic). Management: Administer orlistat at least 3 hours before or after oral cyclosporine. Monitor for decreased serum concentrations of oral cyclosporine, even with the recommended dose separation.

Levothyroxine

Orlistat may decrease the serum concentration of Levothyroxine. Management: Separate administration of oral levothyroxine and orlistat by a least 4 hours. Monitor patients closely for signs and symptoms of hypothyroidism.

Multivitamins/Fluoride (with ADE)

Orlistat may decrease the serum concentration of Multivitamins/Fluoride (with ADE). Specifically, orlistat may impair absorption of fat-solube vitamins. Management: Administer oral fat soluble vitamins (such as vitamins A, D, E, and/or K that are contained in many multivitamin products) at least 2 hours before or after the administration of orlistat.

Multivitamins/Minerals (with ADEK, Folate, Iron)

Orlistat may decrease the serum concentration of Multivitamins/Minerals (with ADEK, Folate, Iron). Specifically, orlistat may impair the absorption of fat-soluble vitamins. Management: Administer oral fat soluble vitamins (such as vitamins A, D, E, and/or K that are contained in many multivitamin products) at least 2 hours before or after the administration of orlistat.

Multivitamins/Minerals (with AE, No Iron)

Orlistat may decrease the serum concentration of Multivitamins/Minerals (with AE, No Iron). Specifically, orlistat may impair absorption of fat-solube vitamins. Management: Administer oral fat soluble vitamins (such as vitamins A, D, E, and/or K that are contained in many multivitamin products) at least 2 hours before or after the administration of orlistat.

Paricalcitol

Orlistat may decrease the serum concentration of Paricalcitol. Management: Monitor clinical response to paricalcitol closely when used with orlistat. When this combination must be used, consider administering paricalcitol at least 1 hour before or 4 to 6 hours after the administration of orlistat

Sincalide

Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction.

Vitamin D Analogs

Orlistat may decrease the serum concentration of Vitamin D Analogs. More specifically, orlistat may impair absorption of Vitamin D Analogs. Management: Monitor clinical response (including serum calcium) to oral vitamin D analogs closely if used with orlistat. If this combination must be used, consider giving the vitamin D analog at least 2 hrs before or after orlistat. Exceptions: Calcipotriene; Calcitriol (Topical); Tacalcitol.

Vitamins (Fat Soluble)

Orlistat may decrease the serum concentration of Vitamins (Fat Soluble). Management: Administer oral fat soluble vitamins at least 2 hours before or after the administration of orlistat. Similar precautions do not apply to parenterally administered fat soluble vitamins. Exceptions: Calcipotriene.

Monitor:

  • Body mass index (BMI)
  • Weight
  • Diet (calorie and fat intake)
  • Patients with diabetes should have a serum glucose checked.
  • Liver function tests in patients with clinical features of hepatic impairment or those with pre-existing hepatic impairment.
  • Renal functions should be monitored in patients with renal impairment.

How to administer Orlistat? How to take Xenical?

  • It is taken orally during a meal (or up to one hour after a meal).
  • It should be taken with major meals and fat-rich meals.
  • Xenical may inhibit the absorption of fat-soluble vitamins, therefore, the multivitamins should be taken at least 2 hours after or before the intake of orlistat.
  • If the meal does not contain fats or a meal is missed, orlistat should not be taken

Mechanism of action of Orlistat (Xenical MOA):

 

  • Xenical reverses the effects of gastric and pancreatic fat lipases. 
  • The body will not be able to absorb fats if it is blocked by lipase enzymes. Orlistat can inhibit up to 30% of dietary fats.

The Onset of action is 24-48 hours The duration of action of orlistat lasts for 48-72 hours It is minimally absorbed into the blood. More than 99% of the absorbed orlistat is protein-bound, mainly to albumin and lipoproteins. Metabolism: It is metabolized to inactive metabolites within the gastrointestinal wall. It has a Half-life elimination of 1-2 hours The time to reach peak serum concentration is about 8 hours Excretion: Most of the drug (97%) is excreted as unchanged in the feces.

International Brand Names of Orlistat:

  • Alli
  • Xenical
  • Aslene
  • Beacita
  • Bodyslend
  • Cuvarix
  • Digrasil
  • Eliza
  • Fatlose
  • Lakshmi
  • Lessfat
  • Lipidown
  • Lysta
  • Nofat
  • Obestat
  • Odistad
  • Oliet
  • Orlifit
  • Orlis
  • Orlist
  • Orly
  • Ornical
  • Orslim
  • Prolistat
  • Redustat
  • Sidelg
  • Slimfast
  • Verte
  • Viplena
  • Xenical
  • Xenista
  • Xenobese
  • Zero-X
  • Zerodown

Orlistat Brand Names in Pakistan:

Orlistat Capsules 20 mg

Orlical Envoy Pharma

 

Orlistat Capsules 60 Mg

Orlifit Getz Pharma Pakistan (Pvt) Ltd.
Osker Genix Pharma (Pvt) Ltd

 

Orlistat 120 mg Capsules

Abnil Agp (Private) Ltd.
Aptex Aptcure Private Limited
Fabecal Highnoon Laboratories Ltd.
Heptolic Brick Laboratories
Obestat Panacea Pharmaceuticals
Obistat Global Pharmaceuticals
Orlean Agp (Private) Ltd.
Orlifit Getz Pharma Pakistan (Pvt) Ltd.
Orlis Ferozsons Laboratoies Ltd.
Orlisat Obs
Orlit Genome Pharmaceuticals (Pvt) Ltd
Orlovit Consolidated Chemical Laboratories (Pvt) Ltd.
Orly Rotex Medica Pakistan (Pvt) Ltd
Orslim Pharmevo (Pvt) Ltd.
Osita Xenon Pharmaceuticals (Pvt) Ltd.
Osker Genix Pharma (Pvt) Ltd
Slimax Noa Hemis Pharmaceuticals
Slimtab Wilshire Laboratories (Pvt) Ltd.
Trimzak Schazoo Zaka
Xenical Roche Pakistan Ltd.
Zence English Pharmaceuticals Industries
Zenec Kurative Pak (Pvt) Ltd

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