Dexlansoprazole (Dexilant) 30 mg, 60 mg Capsules - Uses, Side effects

Dexlansoprazole (Dexilant) is a newer formulation of lansoprazole. It is a proton pump inhibitor that inhibits the release of gastric acid. It is used in the treatment of heartburn and other hypersecretory states.

Indications of Dexlansoprazole (Dexilant):

  • Erosive esophagitis:
    • It is effective in the healing of all grades of erosive esophagitis in patients ≥12 years of age for up to 8 weeks and to maintain healing of erosive esophagitis and relief of heartburn for up to 6 months in adults and 16 weeks in patients 12 to 17 years of age.
  • Gastroesophageal reflux disease:
    • It is indicated for the treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD) in patients ≥12 years of age for 4 weeks.
  • Off Label Use of Dexlansoprazole in Adults:
    • Stress ulcer prophylaxis in critically ill patients

 

Dexlansoprazole dose in adults:

Note: Doses more than 30 mg do not provide further benefit during maintainance phase.

Dexlansoprazole (Dexilant) dose in the treatment of Erosive esophagitis: 

  • Healing: 60 mg per oral once daily for up to 8 weeks.
  • Maintenance: 30 mg per oral once daily.

Dexlansoprazole (Dexilant) dose in the treatment of symptomatic gastroesophageal reflux disease:

  • 30 mg per oral once daily for 4 weeks.
  • Missed doses:
    • The dose should be taken as soon as possible in case of a missed dose, however, if the next scheduled dose is due, take the next dose on time and do not take the missed dose (do not take 2 doses at one time to make up for a missed dose).
  • Discontinuation of therapy:
    • In order to avoid worsening or rebound symptoms,a step-down approach is considered in some cases.
    • Dose reduction by 50% is considered over 2 to 4 weeks.
    • Alternate drugs should be used if the patient is already on the lowest possible dose.
    • Patients should be reassessed in case of worsening symptoms or withdrawal.

   Dexlansoprazole dose in children:

Note: Doses more than 30 mg do not provide further benefit during the maintenance phase.

Dexlansoprazole (Dexilant) dose in the treatment of erosive esophagitis: 

  • Healing:
    • Children ≥12 years of age and Adolescents: Refer to adult dosing.
  • Maintenance:
    • Children ≥12 years of age and Adolescents ≤17 years:
      • 30 mg once daily for up to 16 weeks.

Dexlansoprazole (Dexilant) dose in the treatment of symptomatic gastroesophageal reflux disease:

  • Children ≥12 years of age and Adolescents:
    • Oral: Refer to adult dosing.
    • Missed doses: Refer to adult dosing.

   Dexlansoprazole pregnancy risk category: B

  • Studies on animal reproduction did not show any adverse results.
  • There are many recommendations for treating GERD during pregnancy.
  • Lifestyle modifications are the first step in managing pregnancy. Then, you can add other medications.
  • When indicated by a physician, proton pump inhibitors should only be used.
  • Alternate agents may have more data available and be preferred.

Dexlansoprazole use during breastfeeding:

  • It is not known if Dexlansoprazole is secreted in breast milk.
  • The risk of infant exposure, benefits to the infant and mother's health are all factors that will influence the decision to continue or stop breastfeeding during therapy.

   Dexlansoprazole (Dexilant) Dose adjustment in kidney disease:

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); however, the pharmacokinetics of dexlansoprazole are not expected to be altered in patients with renal impairment.

  • Hemodialysis: Dexlansoprazole is not expected to be removed by hemodialysis.

   Dexlansoprazole (Dexilant) Dose adjustment in liver disease:

  • Mild impairment (Child-Pugh class A):
    • No dosage adjustment is necessary.
  • Moderate impairment (Child-Pugh class B):
    • Healing of erosive esophagitis:
      • 30 mg once daily for up to 8 weeks.
    • Gastroesophageal reflux disease or erosive esophagitis maintenance:
      • There are no dosage adjustments provided in the manufacturer's labeling.
  • Severe impairment (Child-Pugh class C):
    • Use is not recommended.

   Side Effects of Dexlansoprazole (Dexilant):

  • Cardiovascular:
    • Angina Pectoris
    • Bradycardia
    • Cardiac Arrhythmia
    • Chest Pain
    • Deep Vein Thrombosis
    • Edema
    • Hypertension
    • Palpitations
    • Tachycardia
  • Central Nervous System:
    • Headache
    • Abnormal Dreams
    • Anxiety
    • Chills
    • Depression
    • Dizziness
    • Falling
    • Feeling Abnormal
    • Insomnia
    • Memory Impairment
    • Migraine
    • Myocardial Infarction
    • Pain
    • Painful Defecation
    • Procedural Pain
    • Psychomotor Agitation
    • Seizure
    • Trigeminal Neuralgia
    • Vertigo
  • Dermatologic:
    • Acne Vulgaris
    • Dermatitis
    • Erythema
    • Pruritus
    • Skin Lesion
    • Skin Rash
    • Sunburn
    • Urticaria
  • Endocrine & Metabolic:
    • Change In Libido
    • Goiter
    • Heavy Menstrual Bleeding
    • Hot Flash
    • Hypercalcemia
    • Hypokalemia
    • Increased Gastrin
    • Increased Serum Glucose
    • Increased Serum Potassium
    • Increased Serum Total Protein
    • Menstrual Disease
    • Weight Gain
  • Gastrointestinal:
    • Abdominal Pain
    • Diarrhea
    • Flatulence
    • Abdominal Distress
    • Abdominal Tenderness
    • Abnormal Bowel Sounds
    • Abnormal Stools
    • Anorectal Pain
    • Barrett Esophagus
    • Bezoar Formation
    • Biliary Colic
    • Change In Appetite
    • Cholelithiasis
    • Colitis
    • Colonic Polyps
    • Constipation
    • Delayed Gastric Emptying
    • Duodenitis
    • Dysgeusia
    • Dyspepsia
    • Dysphagia
    • Enteritis
    • Eructation
    • Esophagitis
    • Gastric Polyp
    • Gastritis
    • Gastroenteritis
    • Gastroesophageal Reflux Disease
    • Gastrointestinal Disease
    • Gastrointestinal Hypermotility
    • Gastrointestinal Perforation
    • Gastrointestinal Ulcer
    • Halitosis
    • Hematemesis
    • Hematochezia
    • Hemorrhoids
    • Hiccups
    • Irritable Bowel Syndrome
    • Mucosal Inflammation
    • Mucus Stools
    • Oral Bullae
    • Oral Herpes Simplex Infection
    • Oral Paresthesia
    • Proctitis
    • Retching
    • Sore Throat
    • Vomiting
    • Xerostomia
  • Genitourinary:
    • Dysmenorrhea
    • Dyspareunia
    • Dysuria
    • Urinary Urgency
    • Vulvovaginal Infection
  • Hematologic & Oncologic:
    • Anemia
    • Decreased Platelet Count
    • Lymphadenopathy
    • Rectal Hemorrhage
  • Hepatic:
    • Abnormal Hepatic Function Tests
    • Decreased Serum Bilirubin
    • Hepatomegaly
    • Increased Serum Alkaline Phosphatase
    • Increased Serum Alanine Aminotransferase
    • Increased Serum Aspartate Aminotransferase
    • Increased Serum Bilirubin
  • Hypersensitivity:
    • Hypersensitivity Reaction
  • Infection:
    • Candidiasis
    • Influenza
    • Viral Infection
  • Neuromuscular & Skeletal:
    • Arthralgia
    • Arthritis
    • Asthenia
    • Bone Fracture
    • Joint Sprain
    • Muscle Cramps
    • Musculoskeletal Pain
    • Myalgia
    • Tremor
  • Ophthalmic:
    • Eye Irritation
    • Swelling Of Eye
  • Otic:
    • Otalgia
    • Tinnitus
  • Renal:
    • Increased Serum Creatinine
  • Respiratory:
    • Nasopharyngitis
    • Oropharyngeal Pain
    • Upper Respiratory Tract Infection
    • Asthma
    • Bronchitis
    • Cough
    • Dyspnea
    • Hyperventilation
    • Pharyngitis
    • Pulmonary Aspiration
    • Respiratory Congestion
    • Sinusitis
  • Miscellaneous:
    • Fever
    • Inflammation
    • Nodule

  Contraindications to Dexlansoprazole (Dexilant):

  • Hypersensitivity to dexlansoprazole, or any component thereof, is a known condition
  • Combination therapy with drugs that contain rilpivirine.

Warnings and precautions

  • Carcinoma
    • In humans, no occurrences of enterochromaffin-like (ECL) cell carcinoids, dysplasia, or neoplasia (such as those seen in studies of rodents exposed to lansoprazole) have been reported.
  • Clostridium difficile-associated diarrhea (CDAD), formerly Clostridium, is now Clostridioides
    • Patients receiving continuous PPI therapy are at greater risk for CDAD.
    • Patients admitted for persistent diarrhea are more likely to experience this.
    • It is important to use the lowest possible dose and for the shortest time period of PPI therapy.
  • Cutaneous and systemic Lupus Erythematosus
    • PPI can cause autoimmune diseases to become worse or new-onset. Most cases involved cutaneous lupus erythematosus, but also subacute CLE.
    • This is a condition that occurs within weeks to years of continuous therapy.
    • SLE is uncommon and can occur within days to years of starting therapy. It is most commonly seen in young adults and elderly patients.
    • Therapy should be stopped if you experience symptoms of CLE/SLE. A specialist evaluation is required.
    • Most patients experience improvement within 4-12 weeks after withdrawal.
  • Fractures
    • Proton pump inhibitors may cause osteoporosis-related fractures of bones in the hip, spine or wrist.
    • Patients on prolonged therapy (>1-year) or high-dose (multiple daily dosages) are at greater risk. Regular monitoring is required.
    • Vitamin D and calcium supplements should be taken in the lowest effective dose possible for the shortest time.
    • To minimize fracture risk, it is important to follow the appropriate guidelines.
  • Polyps of the fundic gland:
    • PPI can be used for longer periods of time than one year to increase your risk of developing fundic polyps.
    • This could present with nausea, vomiting, abdominal pain, GI bleeding and/or anemia in cases of ulcerated polyps.
    • A diagnosis of polyps can increase the likelihood of small intestinal obstruction.
    • To avoid polyps, the lowest dose and longest duration of PPI therapy should always be used.
  • Hypomagnesemia:
    • Hypomagnesemia can develop if you are on prolonged therapy for more than 3 months. This could lead to seizures, tetany and/or cardiac arrhythmias.
    • Magnesium supplementation can be used to correct hypomagnesemia. Stopping the drug within a week can return magnesium levels back to normal.
    • Concomitant digoxin, diuretics or other drugs that cause hypomagnesemia increase the risk.
    • Therefore, it is important to check serum magnesium levels before beginning prolonged PPI therapy.
  • Interstitial nephritis:
    • PPI may cause acute interstitial Nephritis secondary or idiopathic hypersensitivity reaction during any therapy.
    • Therapy should be stopped if acute interstitial Nephritis develops.
  • Vitamin B deficiency:
    • Chronic use of PPIs can lead to vitamin B malabsorption or subsequent vitamin B deficiency.
    • Females are at greater risk than those who are younger (30 years), and the risk is dose-related. 
    • Withdrawal therapy decreases the risk of developing withdrawal symptoms.
  • Gastric cancer:
    • If PPI is used to relieve symptoms, it cannot be ruled that there is gastric Ca.
  • Gastrointestinal infection (eg, Salmonella, Campylobacter):
    • Proton pump inhibitors can increase the risk of these infections.
  • Hepatic impairment
    • Patients with moderate hepatic impairment (Child Puugh class B) might need to reduce their doses.
    • Patients with severe hepatic impairment (Child Pugh class C) are not advised to use it.

Dexlansoprazole: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).

Amphetamine

The absorption of Amphetamine may be increased by Proton Pump Inhibitors.

Bisphosphonate Derivatives

The therapeutic effects of Bisphosphonate Derivatives may be diminished by Proton Pump Inhibitors.

Capecitabine

Proton Pump Inhibitors can reduce the therapeutic effects of Capecitabine.

Cefpodoxime

The serum concentration of Cefpodoxime may be decreased by Proton Pump Inhibitors.

Cysteamine (Systemic)

Cysteamine (Systemic) may be reduced by Proton Pump Inhibitors.

Dexmethylphenidate

The absorption of Dexmethylphenidate may be increased by proton pump inhibitors. Proton pump inhibitors can interfere with the normal release from extended-release capsules (FocalinXR brand). This could lead to both an increased (early) or decreased (later) absorption.

Dextroamphetamine

The absorption of Dextroamphetamine may be increased by Proton Pump Inhibitors. In particular, dextroamphetamine absorption rates from mixed amphetamine sodium extended release (XR capsules) may increase within the first hour after administration.

Doxycycline

The bioavailability and effectiveness of Doxycycline may be decreased by Proton Pump Inhibitors

Fluconazole

May increase serum concentrations of Proton Pump Inhibitors.

Indinavir

The serum level of Indinavir may be decreased by Proton Pump Inhibitors.

Iron Salts

Iron Salts may be less absorbed by Proton Pump Inhibitors. Exceptions: Ferric Carboxymaltose, Ferric Citrate, Ferric Gluconate, Ferric Gluconate and Ferric HydroxidePolymaltose Complex. Ferumoxytol. Iron Dextran Complex. Iron Isomaltoside. Iron Sucrose.

Methotrexate

Methotrexate serum concentrations may be increased by Proton Pump Inhibitors

Methylphenidate

The absorption of Methylphenidate may be increased by proton pump inhibitors. Proton pump inhibitors can interfere with the normal release from extended-release capsules (Ritalin LA) which may lead to both an increased (early) or decreased (later) absorption.

Multivitamins/Minerals (with ADEK, Folate, Iron)

Proton Pump Inhibitors may decrease the serum concentration of Multivitamins/Minerals (with ADEK, Folate, Iron). In particular, iron absorption may be reduced.

Mycophenolate

The serum concentrations of Mycophenolate may be decreased by Proton Pump Inhibitors. Concentrations of active mycophenolic acids may be decreased.

Raltegravir

The serum concentration of Raltegravir may be increased by Proton Pump Inhibitors.

Riociguat

Riociguat serum concentration may be decreased by Proton Pump Inhibitors

Saquinavir

The serum concentration of Saquinavir may be increased by Proton Pump Inhibitors.

SORAfenib

The absorption of SORAfenib may be decreased by using Proton Pump Inhibitors.

Tipranavir

This may decrease serum concentrations of Proton Pump Inhibitors. These data were derived from research using Ritonavir-boosted Tipranavir.

Voriconazole

Proton Pump Inhibitors may increase serum concentrations. The serum concentration of Voriconazole may be increased by Proton Pump inhibitors. Management: Patients who are taking omeprazole 40mg/day or more should reduce their omeprazole dosage by half before initiating voriconazole.

Risk Factor D (Regard therapy modification)

Atazanavir

Atazanavir serum concentration may be decreased by proton pump inhibitors. Management: Refer to the full drug interaction monograph.

Bosutinib

Bosutinib serum concentration may be decreased by proton pump inhibitors. Management: You may consider alternatives to proton pump inhibitors such as H2 receptor antagonists or antacids. Do not administer alternative agents for more than two hours after bosutinib.

Cefditoren

The serum concentration of Cefditoren may be decreased by proton pump inhibitors. Management: Avoid cefditoren if possible. If PPIs are not possible, consider alternative ways to reduce/control acid reflux such as diet modification or antimicrobial therapy.

Gefitinib

The serum concentration of Gefitinib may be decreased by proton pump inhibitors. Gefitinib Management: If possible, avoid the use of proton pump inhibitors (PPIs). Gefitinib may be administered 12 hours after the administration of the PPI, or 12 hours prior to the next dose.

Itraconazole

Itraconazole serum concentrations may be increased by Proton Pump inhibitors. Itraconazole serum concentration may be decreased by proton pump inhibitors. Administration: Sporanox brand Itraconazole should be administered at least two hours prior to or two hours after any proton pump inhibitors. PPIs may increase the exposure to Tolsura brand Itraconazole; reduce itraconazole dosage.

Ketoconazole (Systemic)

Proton Pump inhibitors may cause a decrease in serum Ketoconazole Systemic concentration. Proton Pump Inhibitors may have a higher serum concentration for Ketoconazole Systemic.

Ledipasvir

The serum concentration of Ledipasvir may be decreased by using Proton Pump inhibitors. Under fasted conditions, PPI doses equal to 20 mg of omeprazole may be administered with ledipasvir. Leadipasvir bioavailability may be reduced by administration of higher doses or combination of food and PPIs 2 hours after an initial PPI.

Mesalamine

Mesalamine may be less effective if it is inhaled by Proton Pump Inhibitors. Increases in the pH of the gastrointestinal tract may lead to premature release mesalamine from certain sustained-release mesalamine drugs. Management: Avoid concurrent administration of high dose proton pump inhibitors, (PPIs), and sustainedrelease mesalamines.

Nilotinib

The serum concentration of Nilotinib may be decreased by Proton Pump Inhibitors. Management: This combination should be avoided if possible as it is unlikely that a separation of doses will suffice to minimize the interaction.

Posaconazole

Posaconazole serum concentrations may be decreased by Proton Pump Inhibitors

Secretin

Secretin may be reduced by using Proton Pump Inhibitors. PPIs can cause gastrin secretion to increase in excess in response to secretin stimulation tests, which could lead to gastrinoma. Management: It is important to avoid secretin and proton pump inhibitors (PPIs). PPIs should be stopped several weeks before secretin administration. The duration of separation will be determined by the PPI. See full monograph for details.

Tacrolimus (Systemic)

The serum concentration of Tacrolimus may be increased by Proton Pump inhibitors (Systemic). Management: Tacrolimus dose adjustment may be required. It is possible for Rabeprazole and pantoprazole to interact with selected H2-receptor antagonists (e.g. ranitidine or fomotidine). Patients at greatest risk may be predicted by genetic testing.

Risk Factor X (Avoid Combination)

Acalabrutinib

The serum concentration of Acalabrutinib may be decreased by Proton Pump Inhibitors.

Alcohol (Ethyl)

Could lower the serum level of Dexlansoprazole.

Cefuroxime

The absorption of Cefuroxime may be decreased by Proton Pump Inhibitors

Dacomitinib

The serum concentration of Dacomitinib may be decreased by proton pump inhibitors. Management: Do not use dacomitinib concurrently with proton pump inhibitors. Antabics can be used. Histamine H2-receptor antagonists may be used (HR2A), provided that dacomitinib has been given at least 6 or 10 hours before the H2RA.

Dasatinib

Proton Pump inhibitors may reduce the serum level of Dasatinib. If you require acid-reducing therapy, an antacid can be taken 2 hours before or after Dasatinib administration.

Delavirdine

The serum concentration of Delavirdine may be decreased by proton pump inhibitors. Patients treated with Delavirdine should avoid prolonged therapy with proton pump inhibitors. Although the clinical impact of PPI therapy with Delavirdine for short term is not known, it should be done with caution.

Erlotinib

The serum concentration of Erlotinib may be decreased by Proton Pump Inhibitors

Nelfinavir

Proton pump inhibitors may lower serum levels of active metabolites of Nelfinavir. The serum concentrations of Nelfinavir may be decreased by Proton Pump inhibitors.

Neratinib

The serum concentration of Neratinib may be decreased by Proton Pump Inhibitors. Proton pump inhibitors can decrease neratinib sorption.

PAZOPanib

The serum concentration of PAZOPanib may be decreased by Proton Pump Inhibitors.

Rilpivirine

The serum concentration of Rilpivirine may be decreased by Proton Pump Inhibitors.

Risedronate

Risedronate's therapeutic effects may be diminished by Proton Pump Inhibitors. Risedronate serum concentration may be increased by Proton Pump inhibitors This is especially true for delayed-release risedronate.

Velpatasvir

Velpatasvir serum concentration may be decreased by Proton Pump Inhibitors

Monitoring parameters:

Magnesium levels before starting therapy and periodically thereafter) in patients on long-term treatment or those taking digoxin, diuretics, or other drugs that cause hypomagnesemia.   

How to administer Dexlansoprazole (Dexilant)?

  • It should be consumed orally, without chewing.
  • Patients who are unable to swallow the capsule can open it and sprinkle 1 tablespoon of applesauce on top.
  • You should throw away applesauce or granule mix. 
  • You can also open capsules for administration via an oral syringe or NG tube.

Administration via NG tube (>=16 French).

  • You can open the capsules and mix 20 ml water with them without crushing the granules.
  • The entire mixture should then be withdrawn into a catheter tip syringe
  • To prevent granules settling, gently swirl the syringe around. Then, inject mixture into the stomach using an NG tube (>=16 French).
  • Fill the syringe again with 10 ml water. Stir gently and flush the NG tube.
  • Repeat the process with a second rinse.
  • You should throw away water and granule mix.

Oral syringe:

  • Capsules must be opened and mixed in 20 ml water.
  • You should take the entire mixture into an oral syringe.
  • To prevent the granules settling, swirl the syringe gently and then immediately inject the mixture into your mouth.
  • Use 10 ml water to refill the syringe. Stir gently and then give it a good shake.
  • Repeat the process with a second rinse.
  • You should throw away water and granule mix.

Mechanism of action of Dexlansoprazole (Dexilant):

  • The proton pump inhibitors block the (H+ and K+) ATPase enzyme, which is the last step in the production of gastric acid.
  • This decreases the acid secretion within the gastric parietal cells.

Protein binding:

  • 96% to 99%.

Metabolism:

  • It is metabolized extensively in the liver via CYP2C19-mediated hydroxylation and CYP3A4-mediated oxidation followed by reduction to sulfate, glucuronide, and glutathione conjugates (inactive metabolites).

Bioavailability:

  • May be increased when administered with food.

Half-life elimination:

  • About 1 to 2 hours.

Time to peak serum concentration:

  • It has two distinct peaks secondary to the dual-release formulation:
  • The initial peak occurs between 1 and 2 hours and a second higher peak between 4 and 5 hours.

Excretion:

  • Urine (~51% as metabolites);
  • feces (~48%).

Note:

  • CYP2C19 polymorphism is expected to affect dexlansoprazole exposure.
  • In a study involving Japanese men following a single dose of dexlansoprazole, C and AUC were up to 2 times greater in intermediate metabolizers compared to extensive metabolizers.
  • In addition, mean C and mean AUC was up to 4 times greater and up to 12 times greater, respectively, in poor metabolizers compared to extensive metabolizers.

International Brands of Dexlansoprazole:

  • Dexilant
  • Apatrix
  • Desopra
  • Dexapol
  • Dexilant
  • Dexilant DR
  • Dexivant
  • Dexlan
  • Dexolant
  • Dexopral
  • Gladexa
  • Lantopep
  • Laxis
  • Ulcezole

Dexlansoprazole Brands in Pakistan:

  • Dextop 30 and 60 mg Capsules - Searle Pharmaceuticals
  • DDR 30 mg and 60 mg Capsules - Macter Pharmaceuticals
  • Delanzo 30 mg and 60 mg Capsules - Sami Pharmaceuticals
  • Dolgina 30 mg and 60 mg Capsules - Hilton Pharmaceuticals
  • Razodex 30 mg and 60 mg Capsules - Getz Pharmaceuticals
  • Dexxoo 30 mg and 60 mg Capsules - Horizon Pharmaceuticals
  • Daxila 30 mg and 60 mg Capsules - Scilife Pharmaceuticals
  • Dexlan 30 mg and 60 mg Capsules - IbnSina Pharmaceuticals
  • Kapdex 30 mg and 60 mg Capsules - Aspin Pharmaceuticals

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