Omeprazole

Registered South African indications:

• Gastro-oesophageal reflux disease (GORD) as an alternative to oral therapy and for the shortest possible time
• Short-term maintenance of haemostasis and prevention of rebleeding in those who have undergone therapeutic endoscopy for acute bleeding gastric or duodenal ulcers

Contraindications

South African recommendations

• Hypersensitivity to esomeprazole, substituted benzimidazoles or to any of the excipients
• Children
• Concomitant use with nelfinavir and atazanavir
• Concomitant use with clopidogrel
• Pregnancy
• Lactation

Recommendations in other jurisdictions

• Hypersensitivity to omeprazole, substituted benzimidazoles or to any of the excipients
• Concomitant use with nelfinavir

Cautions

South African recommendations

• Renal impairment
• Hepatic impairment 
  - Chronic hepatic disease, current or history thereof
• Elderly 
• Gastric malignancy
• Risk factors for reduced vitamin B₁₂ absorption on long-term therapy
• Prolonged use
• Risk factors for fractures
• Risk of osteoporosis 
• Sun exposure
• Subacute cutaneous lupus erythematosus after previous treatment
• Pre-existing gastrointestinal infections
• Mild gastrointestinal complaints
  - Nervous dyspepsia
• Diabetes mellitus
• Coadministration of agents that may cause hypomagnesaemia

Recommendations in other jurisdictions

• Hepatic impairment 
• Elderly 
• Gastric malignancy 
• Vitamin B₁₂ deficiency
• Risk factors for reduced vitamin B₁₂ absorption on long-term therapy
• High doses and prolonged use
  - Especially when exceeding a treatment period of 1 year
• Risk factors for fractures
• Risk of osteoporosis 
• Sun exposure
• Subacute cutaneous lupus erythematosus after previous treatment
• Pre-existing gastrointestinal infections
• Coadministration with clopidogrel
• Coadministration of agents that may cause hypomagnesaemia

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

Dosages below include:

• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

South African registered indications and dosages

Gastro-oesophageal reflux disease (GORD) as an alternative to oral therapy and for the shortest possible time
- Erosive reflux oesophagitis

• IV: 40mg, dly; Treatment duration: 4 weeks; If oesophagitis has not healed or symptoms are persistent: Treatment duration: Continue for additional 4 weeks

- Long-term management of those with healed oesophagitis to prevent relapse
- Severe symptoms of reflux disease

• IV: 20mg, dly

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When oral therapy is possible or appropriate, intravenous therapy should be discontinued and oral therapy should be continued

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Short-term maintenance of haemostasis and prevention of rebleeding in those who have undergone therapeutic endoscopy for acute bleeding gastric or duodenal ulcers

• IV: 80mg, bolus infusion over 30min; Then: 8mg/hr, as a continuous infusion given over 3 days

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The parenteral treatment period should be followed by acid-suppression therapy with 40mg esomeprazole orally once daily for 4 weeks

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Indications and dosages registered in other jurisdictions

Alternative to oral therapy for
- Duodenal ulcers
- Prevention of relapse of duodenal ulcers
- Gastric ulcers
- Prevention of relapse of gastric ulcers
- Helicobacter pylori (H. pylori) eradication in peptic ulcer disease (Additional agents required)
- NSAID-associated gastric and duodenal ulcers
- Prevention of NSAID-associated gastric and duodenal ulcers in patients at risk
- Reflux esophagitis
- Long-term management of those with healed reflux esophagitisr
- Symptomatic gastro-esophageal reflux disease

• IV: 40mg, dly as an infusion over 20-30min

Zollinger-Ellison syndrome

• IV: Initial: 60mg, dly as an infusion over 20-30min; Adjust to higher daily doses as individually needed

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When doses exceed 60mg daily, the dose should be divided and given twice daily

Paed. dosages below include:

• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

South African registered indications and dosages

Contraindicated

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Indications and dosages registered in other jurisdictions

No established for use in children

Pregnancy

International manufacturer recommendations

• Safe
• Results from three prospective epidemiological studies (more than 1000 exposed outcomes) indicate no adverse effects of omeprazole on pregnancy or on the health of the foetus/newborn child. Omeprazole can be used during pregnancy

South African manufacturer recommendations

• Contraindicated
• Safety in pregnancy has not been established

Breastfeeding

International manufacturer recommendations

• Compatible
• Omeprazole is excreted in breast milk but is not likely to influence the child when therapeutic doses are used

South African manufacturer recommendations

• Contraindicated 

• Safety in breastfeeding has not been established. Omeprazole is excreted in breast milk

Fertility

International manufacturer recommendations

• Animal studies with the racemic mixture omeprazole, given by oral administration do not indicate effects with respect to fertility

South African manufacturer recommendations

• No information available

Renal Impairment

International manufacturer recommendations

• No dose adjustment recommended 

South African manufacturer recommendations

• Caution; no dose adjustment recommended 
  The long-term safety of omeprazole in patients with renal impairment has not been established (tab) 

Hepatic Impairment

International manufacturer recommendations

• Caution; dose adjustment recommended 
  IV/Oral (cap, tab): 10-20mg, dly 

South African manufacturer recommendations

• Caution; dose adjustment recommended 
  Oral (cap): 10-20mg, dly 
  Oral (tab): 20mg, dly
  The long-term safety of omeprazole in patients with hepatic impairment has not been established (tab) 
  IV: No information available

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Not porphyrinogenic (NP)

Drugs in Sport

• Permitted - No warnings 

Central Nervous System Disorders

• Insomnia
• Agitation
• Confusion
• Depression
• Aggression
• Hallucinations
• Headache
• Dizziness
• Paraesthesia
• Somnolence

Respiratory Disorders

• Bronchospasm

Gastrointestinal Disorders

• Abdominal pain
• Constipation
• Diarrhoea
• Flatulence
• Nausea and vomiting
• Dry mouth
• Stomatitis
• Gastrointestinal candidiasis
• Microscopic colitis

Hepatobiliary Disorders

• Increased liver enzymes
• Hepatitis with or without jaundice
• Hepatic failure
• Encephalopathy (in patients with pre-existing liver disease)

Genitourinary Disorders

• Interstitial nephritis
• Gynaecomastia

Endocrine and Metabolic Disorders

• Hyponatraemia
• Hypomagnesaemia
  - May be associated with hypokalaemia
  - Severe hypomagnesaemia may result in hypocalcaemia

Musculoskeletal Disorders

• Fracture of the hip, wrist or spine
• Arthralgia
• Myalgia
• Muscular weakness

Skin and Subcutaneous Tissue Disorders

• Dermatitis
• Pruritus
• Rash
• Urticaria
• Alopecia
• Photosensitivity
• Erythema multiforme
• Stevens-Johnson syndrome
• Toxic epidermal necrolysis
• Subacute cutaneous lupus erythematosus
• Increased sweating

Immune, Blood and Lymphatic System Disorders

• Leukopenia
• Thrombocytopenia
• Agranulocytosis
• Pancytopenia
• Hypersensitivity reactions
  - Fever
  - Angioedema
  - Anaphylactic reaction
  - Shock
• Peripheral oedema

Sensory Disorders

• Blurred vision
• Vertigo
• Taste disturbance

• Nelfinavir
• Atazanavir
• Indinavir
• Digoxin
• Clopidogrel
• Posaconazole
• Erlotinib
• Ketoconazole
• Itraconazole
• CYP2C19 substrates
  - Warfarin
  - Vitamin K antagonists
  - Cilostazol
  - Diazepam
  - Phenytoin
• CYP2C19 inhibitors
• CYP2C19 inducers
• CYP3A4  inhibitors
• Clarithromycin
• Voriconazole
• CYP3A4 inducers
• Rifampicin
• Saquinavir
• Tacrolimus
• Methotrexate
• Diuretics

Other interactions

• St John's wort
• Laboratory tests
  - Investigations for neuroendocrine tumours (See additional prescribing points)

• Magnesium levels 

Specific cases may require

• Susceptibility testing (in patients who fail H. pylori-eradication regimen)
• Signs and symptoms of
  - Cutaneous lupus erythematosus or systemic lupus erythematosus
• C. difficile associated diarrhoea
• Bone loss and fractures

Interference with laboratory tests

• Increased Chromogranin A (CgA) level may interfere with investigations for neuroendocrine tumours
• To avoid this interference, omeprazole treatment should be stopped for at least 5 days before CgA measurements
• If CgA and gastrin levels have not returned to reference range after initial measurement, measurements should be repeated 14 days after cessation of proton pump inhibitor treatment

Omeprazole, a racemic mixture of two enantiomers reduces gastric acid secretion through a highly targeted mechanism of action. It is a specific inhibitor of the acid pump in the parietal cell. It is rapidly acting and provides control through reversible inhibition of gastric acid secretion with once daily dosing. Omeprazole is a weak base and is concentrated and converted to the active form in the highly acidic environment of the intracellular canaliculi within the parietal cell, where it inhibits the enzyme H⁺ K⁺-ATPase - the acid pump. This effect on the final step of the gastric acid formation process is dose-dependent and provides for highly effective inhibition of both basal acid secretion and stimulated acid secretion, irrespective of stimulus.

Injection (per 10ml) 40mg

• Accord Omeprazole (Accord)
• Altosec (Pharmacare) (Discontinued 6 Sept 2019)
• Omeprazole Safeline Injection (Safeline)