Omeprazole

Registered South African indications:

• Duodenal ulcer
• Gastric ulcer 
• Reflux oesophagitis
• Zollinger-Ellison syndrome
• Functional dyspepsia
• Symptomatic relief of heartburn in gastro-oesophageal reflux disease (GORD)
• Helicobacter pylori-positive duodenal ulcers (as part of an eradication programme with appropriate antibiotics)
• Non-steroidal anti-inflammatory drug (NSAID)-associated gastric and/or duodenal ulcer and erosions
• Reduction of the risk to develop gastric and/or duodenal ulcer/erosions in those on NSAID treatment
• Reduction of the risk of relapse for a previously healed gastric and/or duodenal ulcer/erosions in those on NSAID treatment

Contraindications

South African recommendations

• Hypersensitivity to omeprazole, substituted benzimidazoles or to any excipients
• Pregnancy
• Lactation
• Concomitant use with atazanavir and nelfinavir
• Concomitant use with indinavir (20mg tab)

Recommendations in other jurisdictions

• Hypersensitivity to the active substance, 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
• Galactose intolerance (certain oral formulations)
  - Galactosaemia
• Fructose intolerance (certain oral formulations)
• Glucose-galactose malabsorption (certain oral formulations)
• Sucrase-isomaltase insufficiency (certain oral formulations)
• Lapp lactase deficiency (certain oral formulations)
• Lactase intolerance (certain oral formulations)

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
• Galactose intolerance (certain oral formulations)
• Total/ Lapp lactase deficiency (certain oral formulations) 
• Glucose-galactose malabsorption (certain oral formulations) 
• Fructose intolerance (certain oral formulations)
• Sucrase-isomaltase insufficiency (certain oraal formulations)

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

Dosages below include:

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

South African registered indications and dosages

Duodenal ulcer

• Oral (cap, tab): 20mg, dly; Treatment duration: 2-4 weeks

- When refractory to other treatment regimens

• Oral (cap, tab): 40mg, dly

Prevention of relapse of duodenal ulcer

• Oral (cap, tab): 10mg, dly; Increase to 20-40mg, dly, if needed

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The above recommended dosage regimens for duodenal ulcer are inclusive of Helicobacter pylori (H. pylori)-positive duodenal ulcers as part of the eradication programme with appropriate antibiotics

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Gastric ulcer
Reflux oesophagitis

• Oral (cap, tab): 20mg, dly; Treatment duration: 4-8 weeks

- When refractory to other treatment regimens

• Oral (cap, tab): 40mg, dly

Long-term management of reflux oesophagitis

• Oral (cap): 20mg, dly; Increase to 20-40mg, dly, if needed
• Oral (tab): 10mg, dly;  Increase to 20-40mg, dly, if needed

Severe or symptomatic recurrent reflux oesophagitis

• Oral (cap, tab): 20mg, dly

NSAID-associated gastro-duodenal lesions with or without continued NSAID treatment

• Oral (cap, tab): 20mg, dly; Treatment duration: 4 weeks; If not fully healed after initial course: Treatment duration: Continue for additional 4 weeks

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If symptom control has not been achieved after the additional 4 weeks of treatment with the prescribed daily dose, further investigation is recommended

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Reduction of the risk to develop gastric and/or duodenal ulcer/erosions in those on NSAID treatment
Reduction of the risk of relapse for a previously healed gastric and/or duodenal ulcer/erosions in those on NSAID treatment
Dyspeptic symptoms

• Oral (cap, tab): 20mg, dly

Symptomatic gastro-oesophageal reflux disease
Functional dyspepsia

• Oral (cap, tab): 10-20mg, dly; Individual dose adjustments should be considered

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If symptom control has not been achieved after 2 weeks of treatment with 20mg daily further investigation is recommended

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Zollinger-Ellison Syndrome

• Oral (cap, tab): Initial: 60mg, dly; Adjust to higher daily doses as individually needed

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In patients with Zollinger-Ellison syndrome the dose should be individually adjusted and treatment continued as long as clinically indicated

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Patients with severe disease and inadequate response to other therapies have been effectively controlled with more than 90% maintained on doses of 20-120mg daily

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When doses exceed 80mg daily, the dose should be divided and given twice daily

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Doses recommended to be given in the morning and swallowed whole with half a glass of liquid. The tablets/ capsules should not be chewed or crushed

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Indications and dosages registered in other jurisdictions

Duodenal ulcer

• Oral (cap, tab): 20mg, dly; Treatment duration: 2 weeks; If not fully healed after initial course: Treatment duration; Continue for an additional 2 weeks

- Poorly responsive duodenal ulcer

• Oral (cap, tab): 40mg, dly; Treatment duration: ≤4 weeks

Prevention of relapse of duodenal ulcers
- In H. pylori negative patients or when H. pylori eradication is not possible

• Oral (cap, tab): 20mg, dly; Min dose: 10mg, dly

- Treatment failure in H. pylori negative patients or when H. pylori eradication is not possible

• Oral (cap, tab): 40mg, dly

Gastric ulcer

• Oral (cap, tab): 20mg, dly; Treatment duration: 4 weeks; If not fully healed after initial course: Treatment duration: Continue for additional 4 weeks

- Poorly responsive gastric ulcer

• Oral (cap, tab): 40mg, dly; Treatment duration: ≤8 weeks

NSAID-associated gastric and duodenal ulcers

• Oral (cap, tab): 20mg, dly; Treatment duration: 4 weeks; If not fully healed after initial course: Treatment duration: Continue for additional 4 weeks

Prevention of relapse of gastric ulcer
- Poorly responsive gastric ulcer

• Oral (cap, tab): 20mg, dly; Increase to 40mg, dly, if needed

Prevention of NSAID-associated duodenal and gastric ulcers in those at risk
- Age >60
- Previous history of gastric and duodenal ulcers
- Previous history of upper GI bleeding

• Oral (cap, tab): 20mg, dly

H. pylori eradication in peptic ulcer disease  (Additional agent(s) required)

• Oral (cap, tab): 20mg, 12hrly; Treatment duration: 7 days
  OR
• Oral (cap, tab): 40mg, dly; Treatment duration: 7 days

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In each regimen, if the patient is still H. pylori positive, therapy may be repeated

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For the eradication of H. pylori the selection of antibiotics should consider the individual patient's drug tolerance, and should be undertaken in accordance with national, regional and local resistance patterns and treatment guidelines

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Reflux oesophagitis

• Oral (cap, tab): 20mg, dly; Treatment duration: 4 weeks; If not fully healed after initial course: Treatment duration: Continue for additional 4 weeks

- Severe oesophagitis

• Oral (cap, tab): 40mg, dly; Treatment duration: ≤8 weeks

Long-term management of healed reflux oesophagitis

• Oral (cap, tab): 10mg, dly; Increase to 20-40mg, dly, if needed

Symptomatic gastro-oesophageal reflux disease

• Oral (cap, tab): 20mg, dly; Min dose: 10mg, dly; Individual dose adjustment should be considered; Treatment duration: 4 weeks

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If symptom control has not been achieved after 4 weeks treatment with 20mg daily, further investigation is recommended

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Zollinger-Ellison syndrome

• Oral (cap, tab): Initial: 60mg, dly; Adjust to higher daily doses as individually needed; Treatment duration: Continued for as long as clinically indicated

---

Patients with severe disease and inadequate response to other therapies have been effectively controlled with more than 90% maintained on doses of 20-120mg daily

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When doses exceed 80mg daily, the dose should be divided and given twice daily

Paed. forms avail. in SA and covered in this monograph: cap, tab

Paed. dosages below include:

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

South African registered indications and dosages

Severe ulcerative reflux oesophagitis resistant to previous medical treatment
- Short term therapy

Younger than 1 year

• No information available

1 year and older

• 10-20kg: Oral (cap, tab): 10mg, dly; Increase to 20mg, dly if needed; Treatment duration: ≤3 months
• >20kg: Oral (cap, tab): 20mg, dly; Increase to 40mg, dly if needed; Treatment duration: ≤3 months

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Note: Above recommendations are applicable to certain formulations. Please refer to the product Professional Information before a clinical decision is made

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There is very limited experience with the use of omeprazole in children

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Indications and dosages registered in other jurisdictions

Reflux oesophagitis

Oral (cap)

• Younger than 1 year: No information available
• Between 1-2 years: 10-20kg: 10mg, dly; Increase to 20mg, dly if needed; Treatment duration: 4-8 weeks
• Older than 2 years: >20kg: 20mg, dly; Increase to 40mg, dly if needed; Treatment duration: 4-8 weeks

Symptomatic treatment of heartburn and acid regurgitation in gastro-oesophageal reflux disease

Oral (cap)

• Younger than 1 year: No information available
• Between 1-2 years: 10-20kg: 10mg, dly; Increase to 20mg, dly if needed; Treatment duration: 2-4 weeks
• Older than 2 years: >20kg: 20mg, dly; Increase to 40mg, dly if needed; Treatment duration: 2-4 weeks

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If symptom control has not been achieved after 2–4 weeks the patient should be investigated further

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Gastro-resistant tab: This formulation is not suitable for children

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Duodenal ulcer caused by Helicobacter pylori (Additional agents required)

Oral (cap)

• Younger than 4 years: No information available
• 4 years and older: 15-30kg: 10mg, 12hrly; Treatment duration: 7 days
• 4 years and older: >30kg: 20mg, 12hrly; Treatment duration: 7 days

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Treatment should be supervised by a specialist

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When selecting appropriate combination therapy, consideration should be given to official national, regional and local guidance regarding bacterial resistance, duration of treatment (most commonly 7 days but sometimes up to 14 days), and appropriate use of antibacterial agents

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

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.

Tablet 10mg

• Losec Mups (AstraZeneca) originator

Tablet 20mg 

• Corpocid 
• Losec Mups (AstraZeneca) originator (Discontinued)

Capsule 10mg 

• Altosec (Pharmacare)
• DRL-Omeprazole  (Dr Reddy's)
• Omez (Dr Reddy's)
• Rapacid (Adcock)

Capsule 20mg 

• Altosec (Pharmacare)
• Adco-Omeprazole (Adcock) (Discontinued: 29/07/2020)
• DRL-Omeprazole (Dr Reddy's)
• Lokit (Teva Pharmaceuticals)
• Lokit OTC (Teva Pharmaceuticals)
• Nozer (Dezzo trading)
• Omez (Dr Reddy's)
• Omiflux (Sandoz)
• Omiloc  (Sandoz)
• Probitor (Sandoz)
• Sandoz Omeprazole (Sandoz)
• Omez OTC 20 (Dr Reddy's)

Capsule 40mg 

• DRL-Omeprazole (Dr Reddy's)
• Omez (Dr Reddy's)