Dexlansoprazole

Registered South African indications:

• Erosive reflux oesophagitis
• Maintenance of healed erosive reflux oesophagitis and maintenance of relief of heartburn
• Symptomatic non-erosive gastro-oesophageal reflux disease (GORD)

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
  - Acute interstitial nephritis
  (See additional prescribing points)
• Coadministration with rilpivirine containing preparations

Cautions

• Pregnancy
• Breastfeeding
• Moderate to severe hepatic impairment
• Elderly
• Possibility of malignant gastric tumours
• Investigations for neuroendocrine tumours
• Risk factors for reduced vitamin B-12 absorption
• Prolonged use
• High doses
• Transplant patients who are intermediate or poor metabolisers of CYP2C19
• Fructose intolerance
• Glucose-galactose malabsorption
• Sucrase-isomaltase insufficiency
• May impair ability to drive and operate machinery

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

Erosive reflux oesophagitis

• Oral (cap): 60mg, dly; Treatment duration: 4 weeks

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For patients not fully healed within this time, the treatment may be continued at the same dose for another 4 weeks

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Maintenance of healed erosive reflux oesophagitis and maintenance of relief of heartburn

• Oral (cap): 30mg, dly; Treatment duration: Up to 6 months

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Therapy for up to 6 months where prolonged acid suppression is needed

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Symptomatic non-erosive gastro-oesophageal reflux disease (GORD)
- Short-term treatment of heartburn and acid regurgitation

• Oral (cap): 30mg, dly; Treatment duration: Up to 4 weeks

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Capsules should be swallowed whole with liquid. They can be taken with or without food. Capsules may also be opened, and granules mixed with one tablespoon apple sauce for administration. After preparing the mixture, the medicinal product should be administered immediately. Granules should not be chewed

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

Erosive reflux oesophagitis
Maintenance of healed erosive reflux oesophagitis and maintenance of relief of heartburn

Younger than 12 years

• Not established for use

Older than 12 years

• See adult dosage

Symptomatic non-erosive gastro-oesophageal reflux disease (GORD)
- Short-term treatment of heartburn and acid regurgitation

Younger than 12 years

• Not established for use

Older than 12 years

• Oral (cap): 30mg, dly; Treatment duration: Up to 4 months

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Therapy for up to 4 months where prolonged suppression is needed. Current evidence does not support a specific treatment period time. A decision should be taken by the clinician on a case by case basis

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Capsules should be swallowed whole with liquid. They can be taken with or without food. Capsules may also be opened, and granules mixed with one tablespoon apple sauce for administration. After preparing the mixture, the medicinal product should be administered immediately. Granules should not be chewed

Pregnancy

• Caution; not recommeneded
• There is limited amount of data from the use of dexlansoprazole in pregnant women
• 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 dexlansoprazole during pregnancy

Breastfeeding

• Caution; not recommended 
• It is not known whether dexlansoprazole is excreted in human breast milk
• Animal studies have shown excretion of lansoprazole in milk
• A risk to the newborns/ infants cannot be excluded
• Dexlansoprazole should not be used during breastfeeding

Fertility

• There was no evidence of impaired fertility following the administration of lansoprazole in animal studies
• Similar results could be expected with dexlansoprazole

Renal Impairment

• No dose adjustment recommended 
  Monitor renal function and check the urine for haematuria and/or proteinuria
  (See additional prescribing points)

Hepatic Impairment

• Mild: No dose adjustment recommended 
• Moderate: Caution; dose adjustment recommended 
  Max: 30mg/24hrs
• Severe: Caution; not recommended for use
  No studies have been conducted in patients with severe hepatic impairment, the use of dexlansoprazole is not recommended

Elderly

• Caution; dose adjustment recommended 
  Due to reduced clearance of dexlansoprazole in the elderly an adjustment of dose may be necessary based on individual requirements
  Max: 60mg/24hrs; unless there are compelling clinical indications

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Headache
• Insomnia
• Depression
• Dizziness
• Asthenia
• Seizures
• Paraesthesia

Cardiovascular Disorders

• Hypertension
• Hot flushes

Respiratory Disorders

• Cough

Gastrointestinal Disorders

• Diarrhoea
• Abdominal pain
  - Abdominal discomfort
• Nausea and vomiting
• Flatulence
• Constipation
• Benign fundic gland polyps
• Dry mouth
• Candidiasis
• Reduced absorption of vitamin B₁₂ (cyanocobalamin)
  - Hypochlorhydria
  - Achlorhydria
• Colitis
• Gastrointestinal infections
  - Clostridium difficile

Hepatobiliary Disorders

• Abnormal hepatic function test
• Drug-induced hepatitis

Genitourinary Disorders

• Acute interstitial nephritis

Endocrine and Metabolic Disorders

• Hypomagnesaemia
  (See additional prescribing points)
• Appetite changes

Musculoskeletal Disorders

• Fracture
  - Hip
  - Wrist
  - Spine
  (See additional prescribing points)

Skin and Subcutaneous Tissue Disorders

• Urticaria
• Pruritus
• Rash
• Subacute cutaneous lupus erythematosus
• Stevens-Johnson syndrome
• Toxic epidermal necrolysis

Immune, Blood and Lymphatic System Disorders

• Autoimmune haemolytic anaemia
• Idiopathic thrombocytopenic purpura
• Anaphylactic reaction
  - Anaphylactic shock
• Hypersensitivity
  - Acute interstitial nephritis
  (See additional prescribing points)
  - Idiopathic hypersensitivity reaction

Sensory Disorders

• Visual disturbance
• Auditory hallucinations
• Visual hallucinations
• Vertigo
• Blurred vision
• Deafness
• Altered taste

Others

• Increased Chromogranin A (CgA) level

• Rilpivirine containing preparations
• CYP2C19 inhibitors
• Fluvoxamine
• CYP2C19 inducers
• CYP3A4 inducers
• Rifampicin
• Sucralfate
• Antacids
• Medicinal agents with pH-dependent absorption
• HIV protease inhibitors
• Atazanavir
• Nelfinavir
• Ketoconazole
• Itraconazole
• Erlotinib
• Agents that cause hypomagnesaemia
• Diuretics
• Digoxin
• Tacrolimus
• Warfarin
• Methotrexate (high dose)
• Agents transported by P-glycoprotein

Other interactions

• St John’s wort

None routine. Specific cases may require

• Electrolytes
  - Serum calcium
  - Serum magnesium
  (See additional prescribing points)

Acute interstitial nephritis

• Acute interstitial nephritis (AIN) has been observed in patients taking proton pump inhibitors (PPIs) including dexlansoprazole
• Acute interstitial nephritis may occur at any point during PPI therapy and is generally attributed to an idiopathic hypersensitivity reaction
• Healthcare professionals should frequently monitor renal function and check the urine for haematuria and/ or proteinuria in patients on treatment with PPIs such as dexlansoprazole
• Discontinue dexlansoprazole if acute interstitial nephritis develops

Hypomagnesaemia

• Severe hypomagnesaemia has been reported in patients treated with PPIs like dexlansoprazole for at least three months, in most cases for a year
• Serious manifestations of hypomagnesaemia such as fatigue, delirium, seizures, dizziness and ventricular arrhythmia can occur, but they may begin insidiously and be overlooked in most affected patients, hypomagnesaemia improved after magnesium replacement and discontinuation of the PPI
• For patients expected to be on prolonged treatment or who take PPIs with digoxin or medicinal products that may cause hypomagnesaemia (e.g. diuretics), health care professionals should consider measuring magnesium levels before starting PPI treatment and periodically during treatment

Fractures

• Dexlansoprazole, especially if used in high doses and over long durations (>1 year), may modestly increase the risk of hip, wrist and spine fracture, predominantly in the elderly or in the presence of other recognised risk factors
• Patients on treatment for more than one year should take Vitamin D and calcium supplementation

Dexlansoprazole is the R-enantiomer of lansoprazole. It is a gastric proton pump inhibitor. It inhibits the final stage of gastric acid formation by inhibiting the activity of H+/K+ ATPase of the parietal cells in the stomach. The inhibition is dose dependent and reversible, and the effect applies to both basal and stimulated secretion of gastric acid. Dexlansoprazole is concentrated in the parietal cells and becomes active in their acidic environment, whereupon it reacts with the sulphydryl group of H+/K+ATPase causing inhibition of the enzyme activity.

Capsule 30mg

• Dexilant (Takeda) originator

Capsule 60mg

• Dexilant (Takeda) originator