GASFREE ®– Dexlansoprazole INN

Chemical Name: 2-[(R)-[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl]-1H-benzimidazole

Description: Dexlansoprazole is a new generation proton pump inhibitor (PPI) used for the management of symptoms associated with gastroesophageal reflux disease (GERD) and erosive esophagitis. The active ingredient is released in two phases at different pH values and at different time points, resulting in two peak concentrations in the blood; 25% of the dose is released at pH 5.5 in the proximal duodenum, while the remaining 75% is released at pH 6.75 in the distal small intestine. As a result, dexlansoprazole has a peak concentration within 1-2 hours after dosing and another within 4-5 hours. Dexlansoprazole targets the (H+, K+)-ATPase enzyme, which is involved in the secretion of hydrochloric acid through the exchange of H+ ions from the cytoplasm for K+ ions. Normally functioning (H+, K+)-ATPase stimulates hydrochloric acid secretion into the gastric lumen thereby increasing stomach acidity and lowering pH.
Dexlansoprazole targets the (H+, K+)-ATPase enzyme, which is involved in the secretion of hydrochloric acid through the exchange of H+ ions from the cytoplasm for K+ ions. Normally functioning (H+, K+)-ATPase stimulates hydrochloric acid secretion into the gastric lumen thereby increasing stomach acidity and lowering pH.

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GASFREE ®– Dexlansoprazole INN

COMPOSITION
GASFREE® 30 Capsule: Each dual delayed release capsule contains Dexlansoprazole INN 30 mg as enteric coated pellets.
GASFREE® 60 Capsule: Each dual delayed release capsule contains Dexlansoprazole INN 60 mg as enteric coated pellets.

PHARMACOLOGY
GASFREE® (Dexlansoprazole) dual delayed release capsule is a PPI that suppresses gastric acid secretion by specific inhibition of the (H+/K+)-ATPase in the gastric parietal cell. By acting specifically on the proton pump, Dexlansoprazole blocks the final step of acid production. It is the R-enantiomer of Lansoprazole (A racemic mixture of the R- and S-enantiomers). GASFREE® is supplied as a Dual Delayed Release (DDR) formulation in a capsule for oral administration. GASFREE® capsule contains a mixture of two types of enteric coated granules with different pH-dependent dissolution profiles. The formulation of GASFREE® (Dexlansoprazole) utilizing Dual Delayed Release technology results in plasma concentration-time profile with two distinct peaks: the first peak occurs 1 to 2 hours after administration, followed by a second peak within 4 to 5 hours. No accumulation of Dexlansoprazole occurs after multiple once daily doses of Dexlansoprazole 30 mg or 60 mg. After oral administration of Dexlansoprazole 30 mg or 60 mg to healthy subjects, mean Cmax and AUC values of Dexlansoprazole increase approximately dose proportionally. Dexlansoprazole is extensively metabolized in the liver and excreted by urine

INDICATION
• Healing of Erosive Esophagitis: GASFREE® (Dexlansoprazole) is indicated for healing of all grades of Erosive Esophagitis (EE) for up to 8 weeks.
• Maintenance of Healed Erosive Esophagitis: GASFREE® (Dexlansoprazole) is indicated to maintain healing of EE and relief of heartburn for up to 6 months.
• Symptomatic Non-Erosive Gastroesophageal Reflux Disease: GASFREE® (Dexlansoprazole) is indicated for the treatment of heartburn associated with symptomatic Non-Erosive Gastroesophageal Reflux Disease (GERD) for upto 4 weeks.

DOSAGE AND ADMINISTRATION
GASFREE® (Dexlansoprazole) dosing recommendations
Indication Dose Frequency
Maintenance of Healed EE and relief of heartburn 30 mg Once daily
Symptomatic Non-Erosive GERD 30 mg Once daily for 4 weeks
Healing of EE 60 mg Once daily for 8 weeks
Important Administration Information:
• GASFREE® (Dexlansoprazole) can be taken without regard to food or the timing of food.
• GASFREE® (Dexlansoprazole) should be swallowed whole.
Alternatively, GASFREE® (Dexlansoprazole) capsules can be administered as follows:
– Open capsule. – Sprinkle intact granules on one table spoon.
– Swallow immediately. Granules should not be chewed.
Missed Dose: If a capsule is missed at its usual time, it should be taken as soon as possible. But if it is too close to the time of the next dose, only the prescribed dose should be taken at the appointed time. A double dose should not be taken. or as directed by the physicians.

SIDE EFFECT
Diarrhoea, abdominal pain, nausea, upper respiratory tract infection, vomiting & flatulence.

PRECAUTION
Gastric malignancy, Clostridium difficile associated diarrhoea, bone fracture, hypomagnesemia. concomitant use of Dexlansoprazole with Methotrexate.

CONTRAINDICATION
Dexlansoprazole is contraindicated in patients with known hypersensitivity to any component of the formulation.

DRUG INTERACTION
Atazanavir, Warfarin, Tacrolimus, Clopidogrel & Methotrexate.

USE IN PREGNANCY AND LACTATION
Dexlansoprazole is probably safe for use during pregnancy, although the full risks are currently unknown. As many drugs are excreted in human milk, Dexlansoprazole should not be given to nursing mothers unless its use is considered essential

USE IN CHILDREN & ADOLESCENTS
Safety and effectiveness of Gasfree (Dexlansoprazole) in patients below 18 years of age have not been established yet.

OVERDOSAGE
There have been no reports of significant overdose of Dexlansoprazole. Multiple doses of Dexlansoprazole 120 mg and a single dose of Dexlansoprazole 300 mg did not result in any severe adverse events

STORAGE
Store below 30ºC Temperature in a dry place. Keep away from light. Keep out of the reach of children.

PACKAGING
GASFREE® 30 Capsule: Each box contains 30 capsules in Alu-Alu blister strip
GASFREE® 60 Capsule: Each box contains 30 capsules in Alu-Alu blister strip

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