Dexolan

Dexolan Uses, Dosage, Side Effects, Food Interaction and all others data.

Dexolan belongs to a class of antisecretory compounds, the substituted benzimidazoles, that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase, at the secretory surface of the gastric parietal cell. Because this enzyme is regarded as the acid (proton) pump within the parietal cell, dexlansoprazole has been characterized as a gastric proton-pump inhibitor, in that it blocks the final step of acid production.

Dexolan is a proton pump inhibitor (PPI) and is included in the drug class of antisecretory compounds. It blocks the final step of gastric acid secretion by specific inhibition of the (H+, K+)-ATPase at the secretory surface of the parietal cells on gastric mucosa.

Trade Name Dexolan
Availability Prescription only
Generic Dexlansoprazole
Dexlansoprazole Other Names Dexlansoprazole
Related Drugs omeprazole, famotidine, pantoprazole, Nexium, Pepcid, Protonix, esomeprazole, Prilosec
Type Capsule
Formula C16H14F3N3O2S
Weight Average: 369.36
Monoisotopic: 369.075882366
Protein binding

Plasma protein binding of dexlansoprazole ranged from 96% to 99% in healthy subjects and was independent of concentration from 0.01 to 20 mcg/mL .

Groups Approved, Investigational
Therapeutic Class Proton Pump Inhibitor
Manufacturer Waterley Pharmaceuticals Pvt Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Dexolan
Dexolan

Uses

Healing of erosive esophagitis, maintenance of healed erosive esophagitis & symptomatic non-erosive GERD (NERD).

Dexolan is also used to associated treatment for these conditions: Erosive Esophagitis, Heartburn, Healed erosive esophagitis, Symptomatic non-erosive gastroesphageal reflux disease

How Dexolan works

Dexolan inhibits the H/K ATPase enzyme, which is involved in the secretion of hydrochloric acid, hydrolyzing ATP and exchanging H+ ions from the cytoplasm for K+ ions in the secretory canaliculus, which results in HCl secretion into the gastric lumen. Dexolan inhibits this effect of H/K ATPase by demonstrating a high degree of activation in the acidic environment. After passing through the liver and reaching the gastric parietal cells activated by a meal, PPIs undergo protonation in the acidic pH environment, followed by conversion to sulphenamide which represents the active form of the drug. Sulphenamide inhibits the activity of the proton pump and hence the transport of hydrogen ions into the gastric lumen via covalent binding to the SH groups of the cysteine residues of H/K ATPase . The delivery technology of dexlansoprazole MR is designed to release the drug in two separate pH-dependent phases, the first in the proximal duodenum (25% of total drug dose) and the second (75% of total drug dose) in the more distal small intestine. Dexolan reduces both basal and stimulated gastric acid secretion.

Dosage

Dexolan dosage

Healing of erosive esophagitis: 60 mg once daily for up to 8 week

Maintenance of healed erosive esophagitis & relief of heartburn: 30 mg once daily

Symptomatic non-erosive GERD (NERD): 30 mg once daily for 4 week

Side Effects

Diarrhea, abdominal pain, nausea, upper resp tract infection, vomiting, flatulence.

Toxicity

Oral LD50 value in mice, rats and dogs is > 5,000 mg/kg. Most commonly reported adverse reactions are diarrhea, abdominal pain, nausea, upper respiratory tract infection, vomiting, and flatulence. There are no reports of significant overdose but serious adverse events of hypertension have been reported in association with twice daily doses of DEXILANT 60 mg. Nonclicnial toxicology of dexlansopraole was assessed using lansoprazole studies. In two 24-month carcinogenicity studies involving rats, lansoprazole induced dose-related gastric ECL cell hyperplasia and ECL cell carcinoids and increased the incidence of intestinal metaplasia of the gastric epithelium in both sexes of rats. Dexolan is expected to have no effect on fertility and the reproductive system.

Precaution

Hepatic impairment. Gastric malignancy should be ruled out. Pregnancy and lactation. Not known whether distributed into breast milk; discontinue nursing or drug

Interaction

Drugs with pH-dependent absorption. Increased risk of hypomagnesaemia with diuretics and digoxin. May decrease plasma concentration of erlotinib, dasatinib and lapatinib. May decrease the bioavailability of itraconazole and ketoconazole. May increase plasma concentration of cilostazol and methotrexate. Reduced bioavailability with antacids and sucralfate.

Food Interaction

  • Avoid St. John's Wort. This may induce the CYP3A4 metabolism of dexlansoprazole, which may cause reduced efficacy.
  • Take with or without food. Dexolan's dual delayed release formulation allows it to be taken without regard to food in contrast to other PPIs.

Volume of Distribution

The apparent volume of distribution after multiple doses in symptomatic GERD patients was 40.3 L .

Elimination Route

After oral administration, the peak plasma concentration increases approximately dose proportionally. The dual delayed release formulation achieves two plasma concentration peaks, where the first peak occurs one to two hours after administration, followed by a second peak within four to five hours. The delivery technology of dexlansoprazole MR is designed to release the drug in two separate pH-dependent phases, the first in the proximal duodenum (25% of total drug dose) and the second (75% of total drug dose) in the more distal small intestine. The median time (Tmax) to peak plasma concentrations (Cmax) of 30 mg dexlansoprazole was 4 hours and ranged from 1 to 6 hours with the Cmax value of 688 ng/mL. AUC was found to be 3275 (ng∙h/mL).

Half Life

Dexolan is eliminated with a half-life of approximately one to two hours in healthy subjects and in patients with symptomatic GERD.

Clearance

Apparent clearance (CL/F) in healthy subjects was 11.4 to 11.6 L/hour, respectively, after five days of 30 or 60 mg once daily administration.

Elimination Route

Dexolan is cleared from the body by either fecal excretion (50.7%) or renal excretion (47.6%) following oral ingestion, with no unchanged drug detected in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category B. Either animal-reproduction studies have not demonstrated a fetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Contraindication

Dexolan is contraindicated in patients with known hypersensitivity to any component of the formulation. Hypersensitivity reactions, including anaphylaxis have been reported. Acute interstitial nephritis (AIN) has been reported with other proton pump inhibitors (PPIs), including lansoprazole of which dexlansoprazole is the R-enantiomer. Dexolan isalso contraindicated with rilpivirine-containing products.

Innovators Monograph

You find simplified version here Dexolan

Dexolan contains Dexlansoprazole see full prescribing information from innovator Dexolan Monograph, Dexolan MSDS, Dexolan FDA label

FAQ

What is the Dexolan used for?

Dexolan is a medication which reduces stomach acid. It is used to treat gastroesophageal reflux disease. Dexolan is used to treat certain conditions in which there is too much acid in the stomach. It is used to treat erosive esophagitis or "heartburn" caused by gastroesophageal reflux disease (GERD), a condition where the acid in the stomach washes back up into the esophagus.

How safe is Dexolan?

It has a good safety profile and carries a low risk of adverse interactions with other drugs. Dexolan may increase your risk of having fractures of the hip, wrist, and spine.

How does Dexolan work?

Dexolan works by decreasing the amount of acid made in the stomach.

What are the common side effects of Dexolan?

Common side effects of Dexolan are include:

  • Burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings
  • chest pain, discomfort, tightness, or heaviness
  • confusion
  • continuing stomach pain
  • diarrhea
  • difficult or labored breathing
  • fast, irregular, pounding, or racing heartbeat or pulse
  • fever
  • headache
  • incoherent speech
  • joint pain, stiffness, or swelling
  • lightheadedness, dizziness, or fainting
  • muscle pain, cramps, or weakness
  • nausea
  • numbness or tingling in the hands, feet, or lips
  • pain or discomfort in the arms, jaw, leg, back, or neck
  • pounding in the ears
  • rash, hives
  • shakiness in the legs, arms, hands, or feet
  • sweating
  • swelling of the eyelids, face, lips, hands, or feet
  • swollen, painful, or tender lymph glands in the neck, armpit, or groin
  • unusual bleeding or bruising
  • vomiting
  • vomiting of blood or material that looks like coffee grounds
  • watery or bloody diarrhea

Can I take Dexolan while pregnant?

This Dexolan should be used during pregnancy only if clearly needed. US FDA pregnancy category: Not assigned. Risk Summary: No data available on use of this drug in pregnant women to inform a drug-related risk.

Is Dexolan safe during breastfeeding?

No information is available on the use of Dexolan or lansoprazole during breastfeeding. However, lansoprazole has been used safely in newborn infants, so it is unlikely that the amount of Dexolan in breastmilk would be harmful.

Can I drink alcohol with Dexolan?

Dexolan orally disintegrating tablets should not be taken with alcohol. Alcohol may may affect how Dexolan orally disintegrating tablets works.

Can I take Dexolan on an empty stomach?

Dexolan may be taken with or without food. Take at around the same time every day.

How many time can I take Dexolan daily?

Dexolan is usually taken once a day.

How much Dexolan can I take daily?

The usual dosage of Dexolan for gastroesophageal reflux (GERD) is 30 mg once daily. You'll likely take this dosage for 4 weeks.

How long does Dexolan take to work?

Dexolan will start working within a few days. In a clinical study, 38% of people were heartburn-free after taking Dexilant for 3 days.

What is the half life of Dexolan?

The elimination half-life of Dexolan is approximately 1–2 hours in healthy subjects and in patients with symptomatic GERD; this is similar to other PPI.

How long can I take Dexolan?

Dexolan shouldn't be used for more than 8 weeks.

Is Dexolan safe for long-term use?

Taking Dexolan long-term may cause you to develop stomach growths called fundic gland polyps. Talk with your doctor about this risk. If you use Dexolan for longer than 3 years, you could develop a vitamin B-12 deficiency. Talk to your doctor about how to manage this condition if you develop it.

Who should not take Dexolan?

You should not take this medicine if you are allergic to Dexolan, or if: you had breathing problems, kidney problems, or a severe allergic reaction after taking this medicine in the past; or you also take a medicine that contains rilpivirine (Complera, Edurant, Odefsey).

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

Can I overdose on Dexolan?

If you take too much Dexolan call your healthcare provider or local Poison Control Center or seek emergency medical attention right away. If Dexolan is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur.

Does Dexolan cause heart problems?

Dexolan may cause a low level of magnesium in your blood. And if it isn't treated, this condition can lead to serious heart problems, such as an abnormal heart rhythm.

Can Dexolan cause kidney?

Dexolan can cause kidney problems. Long-term use of Dexolan or other PPIs may increase the risk of a serious kidney injury called acute interstitial nephritis (AIN). AIN is defined by inflammation in the tissue of the kidney. It can often be treated if caught early, but in rare cases it can cause permanent damage.

Can Dexolan cause liver problems?

Dexolan may also cause lupus, this is an autoimmune disease that results in pain and inflammation throughout the body. And some people with lupus experience heart- or liver-related problems. Other heart- and liver-related problems were also reported as rare side effects in studies of Dexolan.

Can Dexolan increase blood pressure?

Dexolan may cause high blood pressure. In clinical studies, less than 2% of people taking Dexolan had high blood pressure.

*** Taking medicines without doctor's advice can cause long-term problems.
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