Orlistat Actavis

Orlistat Actavis Uses, Dosage, Side Effects, Food Interaction and all others data.

Orlistat Actavis is a reversible inhibitor of gastrointestinal lipase. 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 lipase. 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.

Orlistat Actavis helps with weight reduction and maintenance by inhibiting the absorption of dietary fats via the inhibition of lipase enzymes.

Trade Name Orlistat Actavis
Availability Rx and/or OTC
Generic Orlistat
Orlistat Other Names Orlipastat, Orlipastatum, Orlistat, Tetrahydrolipstatin
Related Drugs phentermine, semaglutide, Wegovy, Saxenda, liraglutide, Alli
Type
Formula C29H53NO5
Weight Average: 495.7348
Monoisotopic: 495.392373811
Protein binding

Orlistat is >99% bound to plasma proteins (mainly lipoproteins and albumin).

Groups Approved, Investigational
Therapeutic Class Appetite suppressant drugs/Anti-obesity drugs
Manufacturer
Available Country Switzerland
Last Updated: September 19, 2023 at 7:00 am
Orlistat Actavis
Orlistat Actavis

Uses

Orlistat Actavis is used for obesity management including weight loss and weight maintenance when used in conjunction with a reduced-calorie diet. Orlistat Actavis is also used for the reduction of the risk of weight regain after prior weight loss. Orlistat Actavis 120 mg is used for obese patients with an initial body mass index (BMI) ≥30 kg/m2 or ≥27 kg/m2 in the presence of other risk factors (eg, hypertension, diabetes, dyslipidemia) and Orlistat Actavis 60 mg is used for overweight & obese patients with an initial body mass index (BMI) ≥25 kg/m2.

Orlistat Actavis is also used to associated treatment for these conditions: Weight Gain, Weight Reduction

How Orlistat Actavis works

Orlistat Actavis is a potent and selective inhibitor of various lipase enzymes responsible for the metabolism of fat. It acts in the gastrointestinal (GI) tract via covalent binding to the serine residues located on the active site of both gastric and pancreatic lipase. When orlistat is taken with food containing fat, it partially inhibits the hydrolysis of triglycerides. This decreases absorption of monoaclglycerides and free fatty acids, contributing to weight maintenance and weight loss.

Dosage

Orlistat Actavis dosage

The recommended dose of Orlistat Actavis is one 60 mg or 120 mg capsule three times a day with each main meal containing fat (during or up to 1 hour after the meal). The patient should be on a nutritionally balanced, reduced-calorie diet that contains approximately 30% of calories from fat. The daily intake of fat, carbohydrate, and protein should be distributed over three main meals. If a meal is occasionally missed or contains no fat, the dose of Orlistat Actavis can be omitted.

Because Orlistat Actavis has been shown to reduce the absorption of some fat-soluble vitamins and beta-carotene, patients should be counseled to take a multivitamin containing fat-soluble vitamin to ensure adequate nutrition. The vitamin supplement should be taken at least 2 hours before or after the administration of Orlistat Actavis, such as at bedtime.

Side Effects

Commonly-observed adverse events associated with the use of Orlistat Actavis include oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, increased defecation, fecal incontinence.

Toxicity

The oral LD50 of orlistat is >5000 mg/kg in rats. Single orlistat doses of 800 mg and multiple doses of up to 400 mg three times a day for 15 days have been administered to healthy weight and obese subjects without clinically significant adverse findings. In addition, doses of 240 mg three times a day have been given to obese patients for 6 months without a significant adverse effects. Post-marketing reports of overdoses cases indicate no adverse events or adverse events that are similar to those reported with the recommended dose. If a significant overdose with orlistat occurs, the patient should be observed for at least 24 hours. Based on the results of clinical studies, systemic effects caused by orlistat are likely to be rapidly reversible.

Precaution

Patients should be advised to adhere to dietary guidelines. gastrointestinal events may increase when orlistat is taken with a diet high in fat (>30% of calories from fat). The daily intake of fat should be distributed over three main meals. If a meal is missed, the dose of orlistat may be omitted.

Interaction

May reduce the absorption of iodine salts and/or levothyroxine, fat-soluble vit (A, D, E, K) and beta carotene. May decrease plasma levels of ciclosporin and amiodarone. May decrease the efficacy of antiepileptic drugs (e.g. valproate, lamotrigine), antiretrovirals, antidepressants, antipsychotics (including lithium). Additive effect on glycaemic control with antidiabetics. May cause hormonal contraceptive failure. May enhance the anticoagulant effect of warfarin.

Food Interaction

  • Take with food. Take with meals or up to 1 hour after a meal. Doses may be skipped for missed meals or fat-free meals.

Orlistat Actavis multivitamins interaction

[Minor] Orlistat Actavis decreases the absorption of fat-soluble vitamins.

Studies have shown a 30% reduction in beta-carotene absorption and a 60% reduction in tocopherol acetate absorption when coadministered with orlistat.

Vitamin supplements should be taken at least two hours before or after orlistat administration.

Volume of Distribution

Volume of distribution cannot be obtained because the absorption of orlistat is minimal. Orlistat Actavis is minimally distributed to erythrocytes and is primarily bound to proteins.

Elimination Route

The systemic absorption and exposure of orlistat is low, however, systemic absorption of the drug is not required for orlistat activity. After an oral dose with 360 mg of radiolabeled orlistat, plasma radioactivity achieved a peak at about 8 hours. Plasma concentrations of unchanged parent drug were close to the lower end of detection limits (15

Half Life

The half-life of orlistat of the small amount of absorbed orlistat ranges between 1-2 hours.

Elimination Route

After single oral dose of radiolabled orlistat in both normal weight and obese volunteers fecal excretion of the unabsorbed drug was found to be the major route of elimination with 11,20 Fecal elimination of orlistat is estimated between 95-97%. Complete excretion by both routes occurs within in 3 to 5 days.

Pregnancy & Breastfeeding use

Pregnancy Category X. Orlistat Actavis is contraindicated during pregnancy, because weight loss offers no potential benefit to a pregnant woman and may result in fetal harm.

It is not known whether Orlistat Actavis is present in human milk or not. Caution should be exercised when Orlistat Actavis is administered to a nursing woman.

Contraindication

Orlistat Actavis is contraindicated in Pregnancy, Patients with chronic malabsorption syndrome, Patients with cholestasis, Patients with known hypersensitivity to Orlistat Actavis or to any component of this product.

Special Warning

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

Acute Overdose

Single doses of 800 mg 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. If 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

Storage Condition

Store below 25°C; excursions permitted to 15° to 30°C. Keep the medicine out of reach of children.

Innovators Monograph

You find simplified version here Orlistat Actavis

Orlistat Actavis contains Orlistat see full prescribing information from innovator Orlistat Actavis Monograph, Orlistat Actavis MSDS, Orlistat Actavis FDA label

FAQ

What is Orlistat Actavis used for?

Orlistat Actavis is used with an individualized low-calorie, low-fat diet and exercise program to help people lose weight. Prescription Orlistat Actavis  is used in overweight people who may also have high blood pressure, diabetes, high cholesterol, or heart disease.

How safe is Orlistat Actavis?

The Food and Drug Administration published a safety review of orlistat in 2010 because of rare reports of serious liver injury in people using it. The FDA found no evidence to confirm that Orlistat Actavis was the cause of the reported liver injuries.

How does Orlistat Actavis work?

Orlistat Actavis works by blocking the receptors in the brain that dopamine acts on. This prevents the excessive activity of dopamine and helps to control psychotic illness.

What are the common side effects of Orlistat Actavis?

Common side effects of Orlistat Actavis are include:

  • Abdominal or stomach pain or discomfort
  • back pain
  • difficulty with moving
  • gas with leaky bowel movements
  • inability to hold bowel movement
  • increases in bowel movements
  • loss of bowel control
  • oily bowel movements
  • oily spotting of underclothes

Is Orlistat Actavis safe during pregnancy?

Orlistat Actavis should not be used during pregnancy as it may harm your unborn baby. Weight loss offers no potential benefit to a pregnant woman and may result in fetal harm.

Is Orlistat Actavis safe during breastfeeding?

It is unlikely that Orlistat Actavis will be absorbed by the infant in amounts that would adversely affect the breastfed infant.

Can I drink alcohol with Orlistat Actavis?

Orlistat Actavis does not interact with alcohol, so it is safe to drink alcohol while taking Orlistat Actavis.

Can I drive after taking Orlistat Actavis ?

You may feel less alert, drowsy or sleepy and have blurred vision while taking this medicine. If this happens, do not drive or use any tools or machines.

When should be taken of Orlistat Actavis?

You should take it with liquids during the meal or up to 1 hour after eating. If you occasionally miss a meal or eat a meal that contains no fat, you should skip the dose of Orlistat Actavis.

Can I take Orlistat Actavis on empty stomach?

Orlistat Actavis only works when there are fats in what you eat, so if you miss a meal or if you eat a meal which is fat-free then do not take a dose of Orlistat Actavis.

How long does Orlistat Actavis take to work?

You can expect to see results in 1-3 months; aiming to lose 5% of your starting body weight in 3 months.

What is the half life of Orlistat Actavis?

The half-life of the absorbed orlistat is in the range of 1 to 2 hours.

How long does Orlistat Actavis take to work?

You should not take Orlistat Actavis for more than six months over the counter.

What happen if I forget to take Orlistat Actavis?

If you forget to take a dose at the right time, take it as soon as you remember, then go on as before. However, do not take a double dose to make up for a forgotten tablet.

What happen If I stop taking Orlistat Actavis?

Keep taking Orlistat Actavis until your doctor tells you to stop. Do not stop taking your medicine just because you feel better as your illness may get worse or come back. Unless your doctor tells you otherwise, Orlistat Actavis should not be stopped suddenly as this may cause withdrawal effects such as muscle stiffness or unusual body movements.

Can I overdose on Orlistat Actavis ?

Yes, you can overdose on Orlistat Actavis. Although the symptoms of such an overdose are not known, they are probably the same as the side effects. This includes: nausea, vomiting, diarrhea, gas, abdominal distress, oily feces and incontinence of feces.

Does Orlistat Actavis effect fertility?

In Orlistat Actavis group, significant improvement was observed in lipid profile at the end of 3 months. Conception rates were 40% and 16.7% and 3.3% in Orlistat Actavis, metformin group and control group respectively.

Can Orlistat Actavis affects my heart ?

Treatment with Orlistat Actavis in conjunction with diet promotes significantly greater weight loss and cardiovascular risk factor reduction than diet alone amongst obese patients at high risk of future coronary events.

Can Orlistat Actavis affect my kidneys?

Orlistat Actavis use has been limited by troublesome but benign gastrointestinal side effects, it has more recently been associated with acute kidney injury (AKI).

Can Orlistat Actavis affects my liver?

The liver injury that occurs during Orlistat Actavis therapy ranges in severity from minor serum aminotransferase elevations to acute symptomatic hepatitis to severe acute liver failure that can be fatal or require emergency liver transplantation. There is no known therapy for orlistat induced liver injury.

Is Orlistat Actavis good for weight loss?

Orlistat Actavis promotes weight loss by decreasing the amount of dietary fat absorbed in your intestines.

Is Orlistat Actavis harmful?

More specifically, the use of Orlistat Actavis has been associated with several mild-to-moderate gastrointestinal adverse effects, such as oily stools, diarrhoea, abdominal pain and faecal spotting.

Can Orlistat Actavis affect periods?

Women may also notice irregularities in the menstrual cycle while taking Orlistat Actavis. Side effects are most common in the first few weeks after beginning the drug.

Does Orlistat Actavis cause depression?

Evidence suggested one in 10 people taking the Orlistat Actavis, whose Orlistat Actavis name is Acomplia, may develop mental side-effects including low mood and depression, anxiety, irritability, nervousness and sleep disorders.

Can Orlistat Actavis cause weight gain?

Orlistat Actavis can cause weight gain also with other side effects.

*** Taking medicines without doctor's advice can cause long-term problems.
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