Orlistat 120mg Capsules
It is used to help with weight loss in certain people.It is used to reduce the risk of gaining weight again after weight loss.
Drug Class
Anti-obesity agent
Pharmacologic Class
Gastrointestinal lipase inhibitor
Pregnancy Category
Not available
FDA Approved
Apr 1999
DEA Schedule
Not Controlled
Overview
What is this medicine?
Orlistat is a medication that helps you lose weight by blocking some of the fat you eat from being absorbed by your body. This fat then passes out of your body in your stool. It works best when combined with a reduced-calorie, low-fat diet and regular exercise.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from this medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely.
Take this medication with each main meal that contains fat, or up to 1 hour after the meal.
If you miss a meal or if the meal does not contain fat, you can skip a dose.
If you take vitamins, take them at least 2 hours before or 2 hours after taking this medication. Consider taking your vitamins at bedtime.
Note that this medication may interfere with the absorption of other oral medications. If you take other medications by mouth, discuss with your doctor whether you should take them at a different time than this medication.
Following Your Treatment Plan
In addition to taking your medication as directed, be sure to follow the diet and exercise plan recommended by your doctor.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry place, away from the bathroom.
Keep the lid tightly closed to maintain the medication's effectiveness.
What to Do If You Miss a Dose
If you miss a dose, skip it and return to your regular dosing schedule.
Do not take two doses at the same time or take extra doses to make up for a missed dose.
To get the most benefit from this medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely.
Take this medication with each main meal that contains fat, or up to 1 hour after the meal.
If you miss a meal or if the meal does not contain fat, you can skip a dose.
If you take vitamins, take them at least 2 hours before or 2 hours after taking this medication. Consider taking your vitamins at bedtime.
Note that this medication may interfere with the absorption of other oral medications. If you take other medications by mouth, discuss with your doctor whether you should take them at a different time than this medication.
Following Your Treatment Plan
In addition to taking your medication as directed, be sure to follow the diet and exercise plan recommended by your doctor.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry place, away from the bathroom.
Keep the lid tightly closed to maintain the medication's effectiveness.
What to Do If You Miss a Dose
If you miss a dose, skip it and return to your regular dosing schedule.
Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Adhere to a reduced-calorie, low-fat diet (approximately 30% of calories from fat) to minimize gastrointestinal side effects and maximize weight loss.
- Take a multivitamin supplement containing fat-soluble vitamins (A, D, E, K, and beta-carotene) at least 2 hours before or after taking Orlistat, or at bedtime, as Orlistat can reduce their absorption.
- Engage in regular physical activity as part of a comprehensive weight management program.
- Distribute daily fat intake over three main meals; avoid high-fat snacks between meals.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
120 mg three times daily with each main meal containing fat
Dose Range:
120 - 120 mg
Condition-Specific Dosing:
obesity:
120 mg three times daily with each main meal containing fat. Doses should be taken during or up to 1 hour after the meal. If a meal is missed or contains no fat, the dose should be omitted.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (not recommended for children under 12 years)
Adolescent:
120 mg three times daily with each main meal containing fat (for adolescents 12-16 years with obesity, in conjunction with a reduced-calorie diet)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended
Moderate:
No specific adjustment recommended
Severe:
No specific adjustment recommended (due to minimal systemic absorption, but caution advised)
Dialysis:
No specific adjustment recommended
Hepatic Impairment:
Mild:
No specific adjustment recommended
Moderate:
No specific adjustment recommended
Severe:
Caution advised; no specific dose adjustment recommended due to minimal systemic absorption, but cases of severe liver injury have been reported rarely.
Pharmacology
Mechanism of Action
Orlistat is a potent, specific, and long-acting inhibitor of gastrointestinal lipases (gastric and pancreatic lipases). It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine site of these enzymes. This inactivates the lipases, preventing the hydrolysis of dietary triglycerides into absorbable free fatty acids and monoglycerides. The undigested triglycerides are then excreted in the feces, leading to a reduction in caloric intake from fat.
Pharmacokinetics
Absorption:
Bioavailability:
<1%
Tmax:
Not applicable (minimal systemic absorption)
FoodEffect:
Should be taken with meals containing fat for optimal effect.
Distribution:
Vd:
Not applicable (minimal systemic absorption)
ProteinBinding:
Not applicable (minimal systemic absorption)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 1-2 hours (for systemically absorbed drug, which is minimal)
Clearance:
Not applicable (minimal systemic absorption)
ExcretionRoute:
Fecal (approximately 97% of the dose is excreted in feces, with 83% as unchanged drug)
Unchanged:
83%
Pharmacodynamics
OnsetOfAction:
Within 24-48 hours (onset of fat malabsorption)
PeakEffect:
Within 24-48 hours (maximal fat excretion)
DurationOfAction:
Continues as long as treatment is maintained with fat-containing meals
Confidence:
Medium
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of kidney problems, including:
+ Inability to pass urine
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Signs of liver problems, such as:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of gallstones, including:
+ Sudden pain in the upper right belly area, right shoulder area, or between the shoulder blades
+ Yellow skin or eyes
+ Fever with chills
Back pain, belly pain, or blood in the urine, which may indicate a kidney stone
Black, tarry, or bloody stools
Pain while urinating
Frequent urination
Severe groin or thigh pain
Swelling
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Stomach pain or diarrhea
Loss of bowel control
Gas with discharge, oily spotting, and urgent need to have a bowel movement
Fatty or oily stools
Upset stomach
Headache
Fatigue or weakness
Changes in menstrual period
* Symptoms of a common cold
This is not an exhaustive list of possible side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of kidney problems, including:
+ Inability to pass urine
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Signs of liver problems, such as:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of gallstones, including:
+ Sudden pain in the upper right belly area, right shoulder area, or between the shoulder blades
+ Yellow skin or eyes
+ Fever with chills
Back pain, belly pain, or blood in the urine, which may indicate a kidney stone
Black, tarry, or bloody stools
Pain while urinating
Frequent urination
Severe groin or thigh pain
Swelling
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Stomach pain or diarrhea
Loss of bowel control
Gas with discharge, oily spotting, and urgent need to have a bowel movement
Fatty or oily stools
Upset stomach
Headache
Fatigue or weakness
Changes in menstrual period
* Symptoms of a common cold
This is not an exhaustive list of possible side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe or persistent stomach pain
- Dark urine
- Yellowing of your skin or the whites of your eyes (jaundice)
- Itching
- Loss of appetite
- Unusual tiredness or weakness
- Severe diarrhea
- Oily spotting or discharge from your rectum
- Increased gas with discharge
- Fecal urgency or incontinence
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Gallbladder disease
+ Malabsorption syndrome
+ Poor eating habits
* If you are pregnant or think you may be pregnant. Note that this medication is contraindicated during pregnancy and should not be taken if you are pregnant.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Gallbladder disease
+ Malabsorption syndrome
+ Poor eating habits
* If you are pregnant or think you may be pregnant. Note that this medication is contraindicated during pregnancy and should not be taken if you are pregnant.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you are currently taking a medication to treat seizures, consult with your doctor, as this drug may affect your seizure control. Immediately contact your doctor if you experience an increase in the frequency or severity of seizures while taking this medication.
This medication has been associated with liver problems, which can be severe and, in rare cases, may lead to liver transplant or death. If you have any concerns or questions, discuss them with your doctor.
If you have diabetes and are taking medications to lower your blood sugar, consult with your doctor, as weight loss caused by this medication may increase your risk of hypoglycemia (low blood sugar). Be aware of the signs of low blood sugar, which include dizziness, headache, drowsiness, weakness, shaking, rapid heartbeat, confusion, hunger, and sweating. If you experience any of these symptoms, contact your doctor immediately.
Adhere to the prescribed dosage, as taking more than the recommended amount may increase your risk of severe side effects. Do not exceed the dosage instructed by your doctor.
If you are breastfeeding, consult with your doctor to discuss any potential risks to your baby, as you will need to weigh the benefits and risks of continuing to take this medication while nursing.
This medication has been associated with liver problems, which can be severe and, in rare cases, may lead to liver transplant or death. If you have any concerns or questions, discuss them with your doctor.
If you have diabetes and are taking medications to lower your blood sugar, consult with your doctor, as weight loss caused by this medication may increase your risk of hypoglycemia (low blood sugar). Be aware of the signs of low blood sugar, which include dizziness, headache, drowsiness, weakness, shaking, rapid heartbeat, confusion, hunger, and sweating. If you experience any of these symptoms, contact your doctor immediately.
Adhere to the prescribed dosage, as taking more than the recommended amount may increase your risk of severe side effects. Do not exceed the dosage instructed by your doctor.
If you are breastfeeding, consult with your doctor to discuss any potential risks to your baby, as you will need to weigh the benefits and risks of continuing to take this medication while nursing.
Overdose Information
Overdose Symptoms:
- Exacerbation of common gastrointestinal side effects (e.g., severe oily spotting, flatulence with discharge, fecal urgency, abdominal discomfort).
What to Do:
Due to minimal systemic absorption, systemic toxicity following an overdose is unlikely. However, if an overdose is suspected, contact a poison control center (e.g., 1-800-222-1222) or seek emergency medical attention. Supportive care and symptomatic treatment for gastrointestinal symptoms may be necessary.
Drug Interactions
Major Interactions
- Cyclosporine
- Warfarin (and other oral anticoagulants)
- Levothyroxine
Moderate Interactions
- Fat-soluble vitamins (A, D, E, K, and beta-carotene)
- Amiodarone
- Antiepileptic drugs (e.g., valproate, lamotrigine)
Minor Interactions
- Oral contraceptives (potential for reduced efficacy if severe diarrhea occurs)
Monitoring
Baseline Monitoring
Weight and BMI
Rationale: To establish baseline and monitor treatment efficacy.
Timing: Prior to initiation of therapy.
Dietary fat intake assessment
Rationale: To counsel patient on appropriate diet to minimize GI side effects and optimize efficacy.
Timing: Prior to initiation of therapy.
Liver function tests (LFTs)
Rationale: Although rare, cases of severe liver injury have been reported. Baseline LFTs may be considered, especially in patients with pre-existing liver conditions.
Timing: Prior to initiation of therapy (if clinically indicated).
Routine Monitoring
Weight and BMI
Frequency: Monthly for first 3-6 months, then quarterly or as clinically indicated.
Target: Goal of 5-10% weight loss within 6-12 months.
Action Threshold: Consider discontinuation if <5% weight loss after 12 weeks.
Dietary adherence and GI symptoms
Frequency: At each follow-up visit.
Target: Not applicable
Action Threshold: Counsel patient on diet modification if severe or persistent GI side effects occur.
Fat-soluble vitamin levels (A, D, E, K)
Frequency: Periodically, especially with long-term use or if deficiency suspected.
Target: Within normal limits.
Action Threshold: Supplementation if levels are low, ensuring separation from Orlistat dose.
INR (for patients on warfarin)
Frequency: Regularly, as per standard warfarin monitoring guidelines, with increased vigilance upon initiation or discontinuation of Orlistat.
Target: Individualized therapeutic range.
Action Threshold: Adjust warfarin dose as needed to maintain target INR.
Symptom Monitoring
- Severe or persistent abdominal pain
- Dark urine
- Yellowing of skin or eyes (jaundice)
- Itching
- Loss of appetite
- Severe diarrhea
- Oily spotting or discharge from the rectum
- Increased flatulence with discharge
- Fecal urgency or incontinence
Special Patient Groups
Pregnancy
Orlistat is generally not recommended during pregnancy. Weight loss during pregnancy is not advised, and based on animal data, Orlistat may cause fetal harm. The benefits of weight loss in obesity do not outweigh the potential risks during pregnancy.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm based on animal data; weight loss not recommended.
Second Trimester:
Potential for fetal harm based on animal data; weight loss not recommended.
Third Trimester:
Potential for fetal harm based on animal data; weight loss not recommended.
Lactation
It is not known whether Orlistat is excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Generally not recommended.
Infant Risk:
Moderate risk (L3) - no human data, animal data suggests excretion into milk, potential for adverse effects on infant.
Pediatric Use
Orlistat 120mg (Xenical) is approved for use in adolescents aged 12 to 16 years with obesity, in conjunction with a reduced-calorie diet. It is not recommended for children under 12 years of age. Close monitoring of growth and development is important.
Geriatric Use
No specific dose adjustment is required for elderly patients. However, caution should be exercised due to potential for polypharmacy and comorbidities. Monitor for potential drug interactions and ensure adequate fat-soluble vitamin intake.
Clinical Information
Clinical Pearls
- Orlistat's efficacy is directly linked to dietary fat intake; patients must adhere to a reduced-calorie, low-fat diet to achieve optimal results and minimize GI side effects.
- The characteristic GI side effects (e.g., oily spotting, flatulence with discharge, fecal urgency) are a sign that the drug is working and that the patient may be consuming too much fat.
- Advise patients to take a multivitamin containing fat-soluble vitamins at a different time of day (e.g., bedtime) to ensure adequate absorption.
- Counsel patients on the importance of lifestyle modifications (diet and exercise) as Orlistat is an adjunct to, not a replacement for, these changes.
- Patients should be advised to carry extra clothing or pads if they experience significant oily spotting or fecal incontinence, especially during the initial weeks of therapy.
Alternative Therapies
- Other pharmacologic agents for weight management (e.g., phentermine/topiramate, naltrexone/bupropion, liraglutide, semaglutide)
- Lifestyle interventions (dietary modification, increased physical activity, behavioral therapy)
- Bariatric surgery (for severe obesity)
Cost & Coverage
Average Cost:
$50 - $200+ per 90 capsules (generic)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (for generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.