Orlistat

Registered South African indications: 

• Obese patients with a Body Mass Index (BMI) ≥ 30kg/m²
• Overweight patients with a BMI ≥ 27kg/m² in the presence of other risk factors

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Breastfeeding
• Chronic malabsorption syndrome
• Cholestasis
• Must not be used in patients with eating disorders (e.g. bulimia) other than obesity
• Not to be used in patients younger than 12 years
• Should not be co-administered with ciclosporin, acarbose and amiodarone

Contraindications registered in other jurisdictions

• Hypersensitivity to the active substance or to any of the excipients
• Chronic malabsorption syndrome
• Cholestasis
• Breastfeeding

• Pregnancy
• Renal impairment
• Hepatic impairment
• Elderly
• Volume depletion
• Diet high in fat (>30%)
• Hypothyroidism
• Epilepsy
• Patients on Antiretrovirals for HIV

Forms avail. in SA and covered in this monograph: cap

South African registered indications and dosages

Obese patients with a Body Mass Index (BMI) ≥ 30kg/m²
​​Overweight patients with a BMI ≥ 27kg/m² in the presence of other risk factors

• Oral (cap): 120mg, with each main meal (during or up to one hour after the meal); If a meal is missed or contains no fat, the dose should be omitted

Should be administered in conjunction with a nutritionally balanced, reduced energy diet that contains approximately 30% of calories from fat. It is recommended that the diet should be rich in fruit and vegetables. The daily intake of fat, carbohydrate and protein should be distributed over three main meals

Doses above 120mg three times daily have not been shown to provide additional benefit

Treatment should be discontinued after 12 weeks if a patient has been unable to lose at least 5% of their body weight as measured at the start of therapy

Contraindicated for children below 12 years

Pregnancy 

South African recommendations

• Caution; not recommended
• Orlistat is not recommended for use in pregnancy

Recommendations in other jurisdictions

• Caution
• For orlistat no clinical data on exposed pregnancies are available. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development
• Caution should be exercised when prescribing to pregnant women

Breastfeeding

Recommendations below are applicable to South Africa and other jurisdictions

• Contraindicated
• As it is not known whether orlistat is secreted into human milk, orlistat is contraindicated during breastfeeding

Fertility

Recommendations below are applicable to South Africa and other jurisdictions

• No information available

• Caution; no dose adjustment recommended

• Caution; no dose adjustment recommended

• Caution; no dose adjustment recommended

Central Nervous System Disorders

• Headache
• Anxiety
• Fatigue

Respiratory Disorders

• Upper respiratory infection
• Lower respiratory infection

Gastrointestinal Disorders

• Abdominal pain
• Oily spotting from the rectum
• Flatus with discharge
• Faecal urgency
• Fatty/oily stool
• Flatulence
• Liquid stools
• Oily evacuation
• Increased defecation
• Rectal pain
• Soft stools
• Faecal incontinence
• Abdominal distension
• Tooth disorder
• Gingival disorder
• Rectal bleeding
• Diverticulitis
• Pancreatitis

Hepatobiliary Disorders

• Cholelithiasis
• Hepatitis
• Increased liver transaminases
• Increased alkaline phosphatase

Genitourinary Disorders

• Urinary tract infection
• Menstrual irregularity
• Oxalate nephropathy

Endocrine and Metabolic Disorders

• Hypoglycemia

Skin and Subcutaneous Tissue Disorders

• Bullous eruptions

Immune, Blood and Lymphatic System Disorders

• Infections and infestations
• Influenza
• Hypersensitivity 
• Decreased prothrombin
• Increased internationalized ratio 

• Amiodarone
• Acarbose
• Ciclosporin
• Antidiabetic agents
• Contraceptives
• Oral anticoagulants
• Antiepileptic agents
• Antiretrovirals
• Fat soluble vitamins
• Iodine salts
• Levothyroxine

None routine. Specific cases may require

• Renal function
• Hepatic function
• Serum glucose
• Thyroid function

Orlistat is a specific and long-acting inhibitor of gastrointestinal lipases. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the serine residue of the active site of the gastric and pancreatic lipases. The inactivated enzyme is thus unable to hydrolyse dietary fat, in the form of triglycerides, into absorbable free fatty acids and monoglycerides. Undigested triglycerides are not absorbed.

Capsule 120mg

• Xenical (Pharmaco) originator
• Xenical with complete kit  (Pharmaco) originator