Anti-obesity and cholesterol drugs
Ezetimibe
Ezetimibe

Dosage Forms:

  • 10 mg tablet

Drug Group

Anti-hypercholesterolemia

Mechanism

Ezetimibe is an inhibitor of intestinal cholesterol absorption. Ezetimibe localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to decrease in the delivery of intestinal cholesterol to the liver.

Indications

Primary hypercholesterolemia. Ezetimibe is indicated as adjunctive therapy to diet for the reduction of elevated total-cholesterol, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia and reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia.

Dosage and Administration:

  • Oral, 10 mg once daily with or without food.

Precautions and Warnings

When ezetimibe is co-administered with an HMG-CoA reductase inhibitor, liver function tests should be performed at initiation of therapy and according to the recommendations of the HMG-CoA reductase inhibitor. Due to the unknown effects of the increased exposure to ezetimibe in patients with moderate or severe hepatic insufficiency, ezetimibe is not recommended in these patients.

Side Effects

The most common adverse effects include headache, abdominal pain, and diarrhea; other gastro-intestinal disorders, myalgia, upper respiratory tract infection, back pain, coughing, dizziness, pharyngitis, sinusitis and urinal infection, hypersensitivity reactions including rash and angioedema, fatigue, chest pain, and arthralgia.
Interactions: Colestyramine: reduces the absorption of ezetimibe and should not be given at the same time of day. Cyclosporine: has been reported to increase the plasma concentration of ezetimibe and patients receiving both drugs should be carefully monitored. Fenofibrate: Concomitant administration increases total ezetimibe concentrations. Fibrates: Concomitant administration increases cholesterol excretion leading to cholelithiasis.

Pregnancy and Lactation

Pregnancy category C. It is not known whether ezetimibe is distributed into human breast milk. Therefore, ezetimibe should not be used in nursing mothers unless the potential benefit justifies the potential risk to the infant.

Packaging

  • 10 tablets in one blister. 3 blisters in a box.
Orlistat
Orlistat

Dosage Forms:

  • 60 mg and 120 mg capsules

Dosage Forms

60 mg and 120 mg capsules

Mechanism

Orlistat is a lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats.

Indications

Orlistat is indicated for obesity management including weight loss and weight maintenance when used in conjunction with a reduced-calorie diet. Orlistat is also indicated to reduce the risk for weight regain after prior weight loss.

Dosage and Administration:

  • Adult over 18 years, 120 mg taken immediately before, during, or up to 1 hour after each main meal (max. 120 mg 3 times daily); continue treatment beyond 12 weeks only if weight loss since start of treatment exceeds 5% (target for initial weight loss may be lower in patients with type 2 diabetes); Child over 12 years see BNF for Children Note If a meal is missed or contains no fat, the dose of orlistat should be omitted

Precautions and Warnings

Orlistat is contraindicated in patients with chronic malabsorption syndrome or cholestasis, and in patients with known hypersensitivity to orlistat or to any component of this product. Patients should be advised to adhere to dietary guidelines. Gastrointestinal events may increase when orlistat is taken with a diet high in fat.

Side Effects

Gastrointestinal symptoms were the most commonly observed treatment-emergent adverse events associated with the use of orlistat. These are: oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, increased defecation, and fecal incontinence. Other adverse effects are: influenza, upper respiratory infection, Lower Respiratory Infection, Back Pain, Pain Lower Extremities, Arthritis, Myalgia, Joint Disorder, Tendonitis, Headache, Dizziness, Fatigue, Sleep Disorder, Rash, Dry Skin, Menstrual Irregularity, Vaginitis, Urinary Tract Infection, Psychiatric Anxiety, Depression, Otitis, and Pedal Edema.
Interactions: Preliminary data from a orlistat and cyclosporine drug interaction study indicate a reduction in cyclosporine plasma levels when orlistat was co-administered with cyclosporine. A pharmacokinetic interaction study showed a 30% reduction in beta-carotene supplement absorption when concomitantly administered with orlistat. Orlistat inhibited absorption of a vitamin E acetate supplement by approximately 60%. As vitamin K absorption may be decreased with orlistat, patients on chronic stable doses of warfarin who are prescribed orlistat should be monitored closely for changes in coagulation parameters.

Pregnancy and Lactation

Category B. There are no adequate and well-controlled studies of orlistat in pregnant women. It is not known if orlistat is secreted in human milk. Therefore, orlistat should not be taken by nursing women.

Packaging:

  • 10 capsules in one blister. 2 blisters in a box.