OR-li-stat

Therapeutic Classification: weight control agents

Pharmacologic Classification: lipase inhibitors

• Obesity management (weight loss and maintenance) when used in conjunction with a reduced-calorie diet in patients with an initial BMI 30 kg/m² or 27 kg/m² in the presence of additional risk factors (diabetes, hypertension, hyperlipidemia).
• Reduces the risk of weight regain after prior loss.
• May delay onset of type 2 diabetes in patients with prediabetes.

• Decreases the absorption of dietary fat by reversibly inhibiting enzymes (lipases), which are necessary for the breakdown and subsequent absorption of fat.

• Weight loss and maintenance in obese patients.
• Delayed onset of type 2 diabetes.

Absorption: Minimal systemic absorption.

Distribution: Action is local, within the GI tract.

Protein Binding: Minimally absorbed drug is >99% bound to plasma proteins.

Metabolism/Excretion: Major route is fecal elimination of unabsorbed drug.

Half-life: 1–2 hr.

(effects on fecal fat)

†Following discontinuation.

Contraindicated in:

• Hypersensitivity
• Chronic malabsorption syndrome or cholestasis
• OB: Pregnancy (weight loss not recommended during pregnancy).

Use Cautiously in:

• Renal impairment
• History of hyperoxaluria or calcium oxalate nephrolithiasis
• Lactation: Lactation
• Pedi: Children <12 yr (safety and effectiveness not established).

With initial use; incidence decreases with prolonged use

GI: fecal urgency, flatus with discharge, ↑defecation, oily evacuation, oily spotting, fecal incontinence, HEPATOTOXICITY.

GU: nephrolithiasis, renal impairment/failure.

Drug-Drug:

• ↓absorption of some fat-solublevitamins, beta-carotene, amiodarone, levothyroxine (separate orlistat and levothyroxine by 4 hr), cyclosporine (give cyclosporine 3 hr after orlistat), anticonvulsants, and antiretrovirals.

• PO (Adults and Children 12 yr): 60–120 mg 3 times daily with each meal containing fat.

• Capsules: 60 mg^OTC; 120 mg;

• Monitor patients for weight loss and adjust concurrent medications (antihypertensives, antidiabetics, lipid-lowering agents) as needed.

• Monitor renal function periodically during therapy in patients with renal impairment or with a history of hyperoxaluria or calcium oxalate nephrolithiasis. Permanently discontinue if oxalate nephropathy develops.

• Do not confuse Xenical with Xeloda.
• PO: Administer one capsule 3 times daily with or up to 1 hr after a meal. If a meal is missed or contains no fat, dose of orlistat can be omitted.
  • A supplemental multivitamin containing vitamins A, D, E, K, and beta-carotene should be taken daily, at least 2 hr before or after orlistat dose.
• Psyllium 6 g with each dose or 12 g at bedtime may decrease GI side effects.

• Instruct patient to take orlistat with meals as directed. If a meal is missed or contains no fat, orlistat dose can be omitted. Do not take more than recommended dose; does not improve benefit.
• Instruct patient to adhere to a reduced-calorie diet. Daily intake of fat should be distributed over three main meals. Meals should contain no more than 30% fat. Taking orlistat with a meal high in fat may increase the GI side effects.
• Advise patient that regular physical activity, approved by a health care professional, should be used in conjunction with orlistat and diet.
• Inform patient of common GI side effects (oily spotting, gas with discharge, urgent need to go to the bathroom, oily or fatty stools, an oily discharge, increased number of bowel movements, inability to control bowel movements). Oil in bowel movement may be clear or have orange or brown colorations. GI side effects usually occur in first wk of treatment and are more increased following a meal high in fat. May lessen or disappear, or may continue for 6 mo or longer.
• Advise patient to notify health care professional if signs and symptoms of hepatotoxicity (weakness, fatigue, fever, jaundice, brown urine, abdominal pain, nausea, vomiting, light-colored stools, itching, loss of appetite) occur.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

• Slow, consistent weight loss when combined with a reduced-calorie diet.
• Delayed onset of type 2 diabetes.

Alli, Xenical