Octreotide

Registered South African indications:

• Acromegaly
• Vasoactive intestinal peptide tumours (VIPomas)
• Bleeding oesophageal varices
• Carcinoid tumours

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients 

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Severe hepatic impairment (LAR)
• Growth hormone-secreting pituitary tumours
• Females of childbearing potential with acromegaly
• Prolonged therapy
• Risk factors for bradycardia  
• Diabetes mellitus
• Thyroid dysfunction
• History of vitamin B12 deficiency

Forms avail. in SA and covered in this monograph: inj, microencapsulated long-acting formulation injection (LAR)

Acromegaly

• SC (inj): Initial: 0.05-0.1mg, 8-12hrly; Maintenance dose: 0.3mg, dly; Max: 1.5mg/24hrs
• IM (LAR): Initial: 20mg, 4 weekly for 3 months; Titration based on clinical symptoms and biochemical parameters 

Dose adjustment should be based on assessment of the effects of the level of growth hormone and insulin-like growth factor

Gastro-enteropancreatic endocrine tumours

• SC (inj): Initial: 0.05mg, 12-24hrly; Maintenance: 0.1-0.2mg, 8hrly
• IM (LAR): Initial: 20mg, 4 weekly for 3 months; Titration based on clinical symptoms and biochemical parameters

Switching from SC injection to LAR formulation: Patients on treatment with subcutaneously administered octreotide should continue at the previously effective dosage for 2 weeks after the first injection of octreotide LAR

Bleeding gastro-oesophageal varices

• IV (inj): 25μg/hr, for 5 days

Carcinoid tumours

Consult specialist for dosages and regimens

Not established for use in children below 18 years

Pregnancy

• Caution
• There is a limited amount of data (less than 300 pregnancy outcomes) from the use of octreotide in pregnant women, and in approximately one third of the cases, the pregnancy outcomes are unknown. The majority of reports were received after post-marketing use of octreotide and more than 50% of exposed pregnancies were reported in patients with acromegaly. Most women were exposed to octreotide during the first trimester of pregnancy at doses ranging from 100-1200 micrograms/day of octreotide (s.c) or 10-40 mg/month of octreotide (i.m). Congenital anomalies were reported in about 4% of pregnancy cases for which the outcome is known. No causal relationship to octreotide is suspected for these cases
• Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of octreotide during pregnancy

Breastfeeding

• Caution; not recommended
• It is unknown whether octreotide is excreted in human breast milk. Animal studies have shown excretion of octreotide in breast milk. Patients should not breastfeed during octreotide treatment

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Mild to moderate (Child-Pugh class A and B): No dose adjustment recommended
• SC/IV: Severe (Child-Pugh Class C): No dose adjustment recommended
  Max: 0.3mg/24hrs 
• IM (LAR): Severe (Child-Pugh Class C): Caution; dose adjustment recommended
  IM (LAR): Initial: 10mg every 4 weeks; Titrate based on response

Elderly

• No dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Headache
• Dizziness
• Asthenia

Cardiovascular Disorders

• Bradycardia
• Tachycardia

Respiratory Disorders

• Dyspnoea

Gastrointestinal Disorders

• Diarrhoea
• Abdominal pain
• Nausea and vomiting
• Constipation
• Flatulence
• Dyspepsia
• Abdominal bloating
• Steatorrhoea
• Discolouration of faeces

Hepatobiliary Disorders

• Cholelithiasis
• Cholecystitis
• Biliary sludge
• Hyperbilirubinaemia

Endocrine and Metabolic Disorders

• Thyroid dysfunction
• Hyperglycaemia
• Hypoglycaemia
• Impaired glucose tolerance
• Anorexia
• Dehydration

Skin and Subcutaneous Tissue Disorders

• Pruritus
• Rash
• Alopecia
• Injection site reactions

• Beta blockers
• Calcium channel blockers
• Agents that control fluid and electrolyte balance 
• Insulin
• Antidiabetic agents
• Ciclosporin  
• Cimetidine
• Bromocriptine
• CYP3A4 substrates

• Thyroid function
• Hepatic function
• Blood glucose
• Serum vitamin B12
• Insulin-like growth factor
• Expansion of growth hormone-secreting pituitary tumour

Adminstration guidelines

• IV infusion: Dilute 500μg octreotide with 60ml 0.9% sodium chloride or 5% dextrose-containing solutions

Injection 0.05mg/ml, Injection 0.1mg/ml, Injection 0.2mg/ml - EML (Tertiary)

Octreotide is a synthetic octapeptide analogue of somatostatin. It inhibits pathologically increased secretion of growth hormone (GH) and of peptides and serotonin produced within the gastro-enteropancreatic (GEP) endocrine system. It also inhibits release of GH stimulated by arginine, exercise- and insulin-induced hypoglycaemia; postprandial release of insulin, glucagon, gastrin, other peptides of the GEP endocrine system; arginine-stimulated release of insulin and glucagon and thyrotropin-releasing hormone-stimulated release of thyroid-stimulating hormone.

Injection (per 1ml) 0.05mg

• Sandostatin (Novartis) originator

Injection (per 1ml) 0.1mg

• Sandostatin (Novartis) originator

Injection (per 1ml) 0.2mg

• Sandostatin (Novartis) originator

Injection (per 5ml) 10mg

• Sandostatin LAR prefilled syringe (Novartis) originator

Injection (per 5ml) 20mg

• Octreotide Teva 20 (Teva Pharmaceuticals)
• Sandostatin LAR prefilled syringe (Novartis) originator

Injection (per 5ml) 30mg

• Octreotide Teva 30 (Teva Pharmaceuticals)
• Sandostatin LAR prefilled syringe (Novartis) originator