Dexlansoprazole


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Erosive oesophagitis Healing: 60 mg once daily for up to 8 weeks. Maintenance of healed oesophagitis: 30 mg once daily for up to 6 months. GERD 30 mg once daily for 4 weeks.
Dosage Details
Oral
Erosive oesophagitis
Adult: Healing: 60 mg once daily for up to 8 weeks. Maintenance of healed oesophagitis: 30 mg once daily for up to 6 months.
Child: ≥12 years Healing: Same as adult dose. Maintenance of healed oesophagitis: 30 mg once daily for up to 4 months.

Oral
Gastro-oesophageal reflux disease
Adult: 30 mg once daily for 4 weeks.
Child: ≥12 years Same as adult dose.
Special Patient Group
Pharmacogenomics:

CYP2C19 is one of the major enzymes in the metabolism of dexlansoprazole. CYP2C19 polymorphism affects dexlansoprazole exposure.

FDA-approved drug label indicates that the exposure to dexlansoprazole is higher in CYP2C19 intermediate and poor metabolisers as compared to extensive metabolisers. No recommended dose adjustment.
Hepatic Impairment
Moderate (Child-Pugh class B): 30 mg once daily for up to 8 weeks. Severe (Child-Pugh class C): Not recommended.
Administration
May be taken with or without food. Swallow whole. Alternatively, cap may be opened & entire contents sprinkled in a tablespoon of applesauce. Swallow immediately w/o chewing.
Contraindications
Concomitant use with rilpivirine.
Special Precautions
Patient with risk factors for osteoporosis; reduced body stores or risk factors for vitamin B12 malabsorption. Moderate to severe hepatic impairment. Children and elderly. Pregnancy and lactation. CYP2C19 poor metabolisers.
Adverse Reactions
Significant: Clostridioides difficile-associated diarrhoea, osteoporosis-related bone fracture, vitamin B12 deficiency, acute interstitial nephritis, subacute cutaneous and systemic lupus erythematosus, fundic gland polyps, hypersensitivity. Rarely, hypomagnesaemia.
Gastrointestinal disorders: Diarrhoea, abdominal pain, nausea, vomiting, flatulence.
Infections and infestations: Infection (e.g. Salmonella, Campylobacter).
Nervous system disorders: Headache.
Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection, nasopharyngitis.
MonitoringParameters
Monitor Mg levels prior to initiation of therapy and periodically thereafter (long-term treatments, or with risk for hypomagnesaemia).
Overdosage
Symptoms: Hypertension, hot flashes, contusion, oropharyngeal pain, weight loss. Management: Symptomatic and supportive treatment.
Drug Interactions
May decrease the serum concentration of atazanavir and nelfinavir. May increase the serum concentrations of methotrexate, tacrolimus and saquinavir. May reduce the absorption of pH-dependent drugs (e.g. ampicillin esters, ketoconazole, itraconazole, erlotinib, iron salts, dasatinib, nilotinib, mycophenolate mofetil).
Potentially Fatal: May decrease the serum concentration of rilpivirine.
Food Interaction
Decreased exposure with St. John’s wort.
Lab Interference
May increase serum chromogranin A (CgA) levels causing false-positive results in diagnostic test for neuroendocrine tumours. May cause hyper-response in gastrin secretion, falsely suggesting gastrinoma, with secretin stimulation test. May cause false-positive urine screening test for tetrahydrocannabinol (THC).
Action
Description: Dexlansoprazole is the R-isomer of lansoprazole. It suppresses gastric acid secretion by inhibiting the H+/K+ ATPase at the secretory surface of the gastric parietal cell, thus blocking the final step in gastric acid production.
Pharmacokinetics:
Absorption: Food increases bioavailability. Time to peak plasma concentration: Initial peak: 1-2 hours; second peak: 4-5 hours.
Distribution: Volume of distribution: 40 L (symptomatic GERD). Plasma protein binding: 96-99%.
Metabolism: Extensively metabolised in the liver into inactive metabolites by CYP2C19 and CYP3A4 enzymes via hydroxylation and oxidation respectively; followed by formation of sulphate, glucuronide, and glutathione conjugates.
Excretion: Via urine (approx 51% as metabolites); faeces (approx 48%). Elimination half-life: Approx 1-2 hours.
Chemical Structure

Chemical Structure Image
Dexlansoprazole

Source: National Center for Biotechnology Information. PubChem Database. Dexlansoprazole, CID=9578005, https://pubchem.ncbi.nlm.nih.gov/compound/Dexlansoprazole (accessed on Mar. 24, 2020)

Storage
Store below 30°C.
ATC Classification
A02BC06 - dexlansoprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
References
Annotation of FDA Label for Dexlansoprazole and CYP2C19. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 13/12/2019.

Annotation of HCSC FDA Label for Dexlansoprazole and CYP2C19. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 13/12/2019.

Annotation of Swissmedic Label for Dexlansoprazole and CYP2C19. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 13/12/2019.

Anon. Dexlansoprazole. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/12/2019.

Buckingham R (ed). Dexlansoprazole. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/12/2019.

Dexilant Delayed Release Capsule 30, 60 mg (Takeda Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 03/02/2020.

Dexilant Delayed-Release Capsule (Takeda Pharmaceuticals America, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 13/12/2019.

Disclaimer: This information is independently developed by MIMS based on Dexlansoprazole from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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