Lansoprazole - The Long-Term and Well-Tolerated Therapy for GERD

How Does Lansoprazole Help Treat Gastroesophageal Disease (GERD)?

Lansoprazole is a proton pump inhibitor. It reduces the amount of acid produced by your stomach. The medication can treat ulcers present in your stomach and intestines. Lansoprazole is a prodrug, meaning that this proton pump inhibitor requires gastric acid secretion to be converted to sulfenamide or sulfenic acid. Once activated, it reacts with cysteine residues on the parietal H+ and K+ ATPase enzymes. This ability to bind covalently to their targets provides a prolonged inhibition of acid secretion. Therefore, the drug is taken before meals to control daytime gastric acidity. This not only reduces your acidity but also protects your food tract from ulceration. That is why taking Lansoprazole while you have ulcers or issues like heartburn is important.

Lansoprazole is available only by prescription and is a delayed-release medication that prevents breakdown by stomach acid and is released in the intestine. The proton pump inhibitor is approved by the Food and Drug Administration (FDA) to treat active ulcers (gastric and duodenal). It also treats erosive reflux esophagitis and gastroesophageal disease.

In Which Conditions Is Lansoprazole Used For?

Lansoprazole is indicated for the following:

1. The FDA approves the proton pump inhibitor for short-term treatment of active gastric ulcers and duodenal ulcers (soreness that occurs inside the stomach lining or the first part of the small intestine).

2. The drug relieves symptoms of heartburn and indigestion.

3. It is used to treat symptoms of erosive reflux esophagitis (inflammation of the esophageal mucosa) and GERD.

4. The proton pump inhibitor helps to treat ulcers on the lining of the stomach and intestine and decreases ulcer formation in people taking non-steroidal anti-inflammatory drugs.

5. Lansoprazole is prescribed to treat Zollinger-Ellison syndrome (a digestive disorder or condition that causes the stomach to produce too much gastric acid, resulting in tumor growth in the pancreas or the upper part of the small intestine).

6. Lansoprazole effectively eradicates H. pylori infection when combined with other medications, such as Amoxicillin and Clarithromycin.

Limitations:

Long-term therapy with Lansoprazole can increase the risk of developing stomach cancer.

Taking Lansoprazole for more than one year can increase the chances of specific side effects, such as bone fractures, especially in people with osteoporosis and vitamin B12 deficiency. Also, if you are still having an ulcer while taking Lansoprazole, please consult your doctor. In such cases, additional treatment or further examination may be needed.

Lansoprazole Dosing

1. Route of administration

The route of administration is Oral.

2. Dosage strengths

• Delayed-release capsules.

• 15 milligrams.

• 30 milligrams.

• Oral-disintegrating tablets.

• 15 milligrams.

• 30 milligrams.

• Oral suspension.

• 3 millimole/milliliter.

3. Dosage forms

Lansoprazole doses for GERD and for other gastric issues are as follows;

• Fifteen milligrams of Lansoprazole capsules are opaque, hard gelatin, pink and green colored with “15” imprinted.

• Thirty milligrams of Lansoprazole capsules are opaque hard gelatin, pink and black colored with “30” imprinted.

• Fifteen milligrams of Lansoprazole tablets are uncoated, orange to dark brown in color with a “15” imprint.

• Thirty milligrams of Lansoprazole tablets are uncoated, orange to dark brown in color, with “30” imprinted.

• The recommended dose is 30 milligrams, taken once daily for four to eight weeks.

Lansoprazole considerations:

1. Pregnancy-

Lansoprazole should be avoided during pregnancy, especially during the third trimester, as it may be associated with congenital disabilities.

2. Lactation-

There are no adequate studies to determine infant risk while using Lansoprazole during breastfeeding.

3. Pediatric patients-

Lansoprazole is not recommended for children younger than one year of age. The drug may be given to toddlers only if the benefits outweigh the risks.

4. Geriatric patients -

Long-term therapy with proton pump inhibitors such as Lansoprazole is related to an increased risk of hip, spine, or wrist fractures in adults over 65.

5. Renal impairment -

People with renal impairment are more likely to develop kidney damage or failure when given Lansoprazole in the long term.

6. Hepatic impairment -

If you are having liver issues, Lansoprazole is not for you. It can worsen your liver problem, leading to its malfunctioning. That is why it is not given to liver patients. Also, if it is given, the dose is reduced.

Lansoprazole Warnings and Contraindications

Contraindications

Lansoprazole is contraindicated in the following cases:

Pregnancy

Recent studies show that, during pregnancy, if you take it, it can lead to a birth defect in the child. As a result, during pregnancy, you should not take it.

Hypersensitivity

If patients have a known history of drug allergy, you should not prescribe it.

Colitis

If a patient has colitis or a history of colon inflammation, you should not prescribe it. It can lead to severe diarrhea in such cases.

Lansoprazole Warnings and Precautions

1. Clostridium difficile:

Some research shows proton pump inhibitors such as Lansoprazole may be linked with an increased risk of Clostridium difficile-associated diarrhea. It is usually observed in hospitalized patients. Close monitoring is recommended in patients with diarrhea and those taking antibacterial therapy.

2. Liver disease:

The liver primarily metabolizes Lansoprazole. Adjustment in the dose must be considered in patients with severe hepatic impairment.

3. Bone fractures:

Observational studies have shown that long-term use of Lansoprazole may be associated with an increased risk of osteoporosis-related hip, spine, or wrist fractures. These patients should be given low doses of Lansoprazole and treated for a short duration. If anyone takes Lansoprazole for a very long time, it can cause bone-related issues. This occurs due to the loss of bone mineral, which can lead to hip, spine, or wrist fractures.

4. Hypomagnesemia:

If anyone takes any proton pump inhibitor for more than three months, it can cause hypomagnesemia (an electrolyte disturbance caused when serum magnesium levels are lower than 1.46 mg/dl in the blood). It can be both symptomatic and nonsymptomatic. As a result, heart issues, unwanted muscle movement, and nerve problems may occur.

5. Vitamin B12 deficiency:

If anyone takes Lansoprazole for a very long time, it can lead to a vitamin deficiency. Long-term use can cause cyanocobalamin and vitamin B12 deficiency.

For patients (p)

Why Is Lansoprazole Prescribed for Gastroesophageal Reflux Disease?

Our stomachs produce acid, which helps in digestion. However, sometimes excessive acid production or backflow of acid in your esophagus can cause complications. It can lead to ulceration in your gastrointestinal tract or cause issues like heartburn. Lansoprazole, a proton pump inhibitor, helps lower the amount of acid production in your gut. Also, if you are suffering from issues like acid reflux or GERD, Lansoprazole can be effective for you.

Lansoprazole proper use:

• Usually, you take Lansoprazole once in the morning, on an empty stomach.

• The drug is available both over-the-counter and by prescription.

• Lansoprazole is most effective when taken at least 30 minutes before a meal or snack.

How should one take Lansoprazole?

• Lansoprazole is available as a tablet and capsule, which can be taken orally.

• You can take this in the morning on an empty stomach or 30 minutes before a meal.

• For the best result, you must take it at the same time every day.

• Lansoprazole is typically initiated at a low dose of 15 milligrams and gradually increased for more severe cases.

• Lansoprazole may be taken twice daily for 14 days when combined with other medications to eliminate Helicobacter pylori.

• You can see the benefits of this medicine after at least one or two weeks.

• Only stop the medicine suddenly after talking to the doctor.

• You do not have to break or chew the orally disintegrating tablets. Instead, the capsule is swallowed with a glass of water or milk.

What Should the Patient Discuss With His Doctor Before Beginning Lansoprazole Therapy?

As a patient, you should discuss any medical issues or concerns related to your medication before taking it.

• Allergies:

Inform the doctor if you have ever had an allergic reaction to Lansoprazole or other ingredients with the same formulation. Symptoms may include rash, facial swelling, throat tightness, or troubled breathing.

• Medical history:

Also, if you have issues like diabetes, heart issues, or urine problems, you should inform your doctor.

• Drug history:

Always provide the treating doctor with a complete list of all prescription and non-prescription medications you are taking, including any herbal supplements, nutritional supplements, and vitamins.

• Pregnancy:

If you are pregnant or planning to become pregnant soon, it is essential to inform your doctor. The use of Lansoprazole may harm the fetus and the mother. Using Lansoprazole during the third trimester of pregnancy may increase the risk of developing birth defects if one gets pregnant while on Lansoprazole; inform the doctor as soon as one finds out.

• Lactation:

The doctor must know if one is breastfeeding. The possibility of Lansoprazole passing into the breastmilk is unknown. However, it is likely to pass into the baby's bloodstream in small amounts.

• Older adults:

Prolonged use and high doses may increase the risk of bone fractures. Therefore, the doctor may prescribe low doses of Lansoprazole for treatment and for a short time.

Things to keep in mind: Before using Lansoprazole

1. Long-term therapy with proton pump inhibitors may be associated with an increased risk for osteoporosis-related hip, wrist, or spine fractures.

2. Prolonged use may cause hypomagnesemia (an electrolyte disturbance caused by low levels of serum magnesium in the blood).

Effectiveness of Lansoprazole:

There is no significant difference in the clinical effectiveness of other proton pump inhibitors, such as Omeprazole or Pantoprazole, in relieving heartburn symptoms and regurgitation.

The drug starts to work within two to three days and may take up to four weeks to completely control the acid symptoms.

Lansoprazole Side Effects

The common Lansoprazole side effects that occur with the use of Lansoprazole are as follows:

1. Diarrhea.

2. Constipation.

3. Abdominal pain.

4. Headache.

5. Feeling sick.

6. Itchy skin rashes.

7. Dry mouth or throat.

8. Nausea.

9. The severe side effects may include,

10. Chest pain.

11. Fast or irregular heart rate.

12. Watery or bloody diarrhea.

13. Jerky muscle movements.

14. Confusion.

15. Feeling jittery.

16. Seizures.

Can one stop taking Lansoprazole without the doctor's consent?

You should never stop taking Lansoprazole without first talking to your doctor. Consult a physician or visit the emergency room if you experience any side effects that require immediate attention.

Do not skip the dose or stop taking Lansoprazole suddenly. This can worsen the condition or make the symptoms return. Instead, the doctor will instruct on how to taper the dose gradually.

Stopping proton pump inhibitors can cause rebound acid hypersecretion and lead to the appearance of symptoms such as indigestion, heartburn, or regurgitation (a condition when digestive fluids and undigested food rise from the esophagus into the mouth).

Dietary restrictions to consider when taking Lansoprazole:

The patient may continue to follow their regular diet unless the doctor advises a change. No dietary restrictions are needed. The drug is taken 30 minutes before meals. This helps the body absorb the drug, making the medication more effective.

1. Caffeine-containing foods -

Avoid consuming caffeine-containing food items and beverages, such as tea, coffee, and chocolate, while taking Lansoprazole. Caffeine can decrease the effectiveness of the drug.

2. Fatty and spicy foods -

Try to eat small meals at once. Eat more often and avoid eating fatty and spicy foods.

3. Acidic foods -

Foods and drinks such as apples, lemons, grapefruit, oranges, tomatoes, carbonated drinks, and energy drinks can worsen the symptoms of GERD and heartburn and should be avoided.

Storage of Lansoprazole:

1. Store Lansoprazole at room temperature in a closed container, away from heat, moisture, and direct light.

2. Lansoprazole tablets should be stored in the original packaging or container with a tightly closed lid.

3. Keep this drug far from the reach of children and pets.

Disposal of Lansoprazole:

1. Lansoprazole should not be disposed of by flushing or throwing it out in regular garbage.

2. One may dispose Lansoprazole through the local medicine take-back program, which can be accessed or learned more about through a local pharmacist.

3. Ask the local pharmacist about other drug disposal options if the person cannot access a medicine take-back program.

Overdose:

1. In one of the reported cases, an individual had consumed almost 600 mg of Lansoprazole for more than a year, although there were no specific side effects.

2. If a person overdoses, contact a doctor immediately and do not take another tablet until the doctor tells you what to do.

3. Contact the doctor immediately if a person experiences severe abdominal pain, constipation, diarrhea, and nausea.

4. The drug is not usually eliminated with hemodialysis. In the event of an emergency, gastric emptying is performed. It is a procedure that induces vomiting in a patient, removes all particles from the stomach, and cleanses it thoroughly. In rare cases, charcoal may be administered if recommended.

5. Overdosing may cause a rare but severe cutaneous reaction called toxic epidermal necrolysis (TEN), characterized by blistering and peeling of the skin.

For Doctor

Indications

Lansoprazole is indicated for the following purposes:

1. It is indicated for the short-term treatment of healing and symptom relief in active duodenal ulcers and active benign gastric ulcers.

2. It is used for short-term treatment to heal all grades of erosive esophagitis and helps maintain the healing process.

3. The drug may be prescribed for treating pathological hypersecretory conditions, including Zollinger-Ellison syndrome.

4. Lansoprazole helps to reduce the risk of non-steroidal anti-inflammatories (NSAIDs) associated with gastric ulcers in patients with documented gastric ulcers. It is also used to heal NSAID-associated ulcers.

Pharmacology of Lansoprazole:

Description:

Lansoprazole is a white to brownish-white odorless crystalline powder. It is freely soluble in dimethylformamide, soluble in methanol, slightly soluble in ethyl acetate, and insoluble in water.

It is stable when exposed to light for up to two months.

Lansoprazole is a member of benzimidazole with selective and irreversible proton pump inhibitor activity.

Components:

1. Active ingredients:

Lansoprazole.

2. Inactive ingredients:

Sugar sphere, sucrose, methacrylic acid copolymer, hydroxypropyl cellulose, starch, magnesium carbonate, talc, polyethylene glycol, titanium dioxide, polysorbate 80, colloidal silicon dioxide.

Clinical pharmacology:

Mechanism of action:

Lansoprazole is an antisecretory compound called a substituted benzimidazole. These compounds suppress gastric secretion by specific inhibition of the H+ and K+ ATPase enzymes at the secretory surface of the gastric parietal cell. Lansoprazole blocks the final step of acid production. This effect is dose-dependent and inhibits the stimulated gastric acid secretion, irrespective of the stimulus.

Pharmacodynamics

After oral administration, Lansoprazole significantly decreases the basal acid output and increases the mean gastric pH.

1. Initial dose:

Increased gastric pH is observed within one to two hours after administering 30 mg of Lansoprazole and two to three hours after administering 15 mg of Lansoprazole.

2. Multiple dose:

Increased gastric pH was observed within the first hour after a dose of 30 mg of Lansoprazole and within one to two hours after a dose of 15 mg of Lansoprazole.

Pharmacokinetics

1. The mean Cmax is 1.7 hours after oral dosing, and the absolute bioavailability is over 80%. [Cmax- Maximum concentration achieved by a drug in the blood, cerebrospinal fluid, or target organ after administration of a dose]

2. Median Tmax- The presence of food diminishes by 50 to 70 percent. [Tmax- Time taken for a drug to reach maximum concentration after administration of a dose]

3. Pharmacokinetic changes - The dose is to be adjusted to individual requirements due to variations in the rate of metabolism.

A. Distribution

1. Steady-state plasma levels - 0.05 to 5.0 microgram per milliliter.

2. Time to approach steady-state levels - 1.7 hours.

3. Binding to plasma proteins- 97 %.

B. Metabolism

1. The liver mainly metabolizes Lansoprazole with enzymes CYP3A4 and CYP2C19.

2. Metabolic processes- 5-Hydroxylated sulfinyl and sulfone derivatives of Lansoprazole.

3. Active metabolites - Cyclic sulfenamide and disulfide metabolites.

4. Inactive metabolites - Sulphide and hydroxylated sulphone

C. Elimination

1. After Oral Administration -

2. 30% of the dose is excreted in the urine.

3. 70% is excreted in the feces.

4. The acid-inhibitory effect lasts for 24 hours.

5. Time is taken to return to normal levels - Two weeks.

6. Mean elimination half-life- Less than two hours.

Special Considerations

1. Hepatic impairment

Lansoprazole elimination half-life is significantly prolonged in patients with hepatic disease, and may show abnormal liver function tests with Lansoprazole use. Therefore, these patients may require a dose reduction of the proton pump inhibitor.

2. Bone fractures

Always use proton pump inhibitors such as Lansoprazole cautiously in patients with a risk of bone fractures or osteoporosis. Daily high doses of Lansoprazole increased the fracture risk in patients 50 years of age and older. Therefore, close monitoring of their bone status and adequate supplementation with vitamin D and calcium must be ensured.

3. Hypokalemia and hypocalcemia

Caution must be observed while using Lansoprazole in patients with a pre-existing risk of hypokalemia (low blood potassium levels) and hypocalcemia (low blood calcium levels). Prolonged therapy with Lansoprazole requires monitoring of calcium and potassium levels and should be discontinued if symptoms arise.

4. Infants

The safety and efficacy of Lansoprazole have not been established in neonates or infants and should be administered cautiously.

Drug interactions:

1. Erlotinib:

Lansoprazole decreases levels of Erlotinib by altering its solubility and reducing its bioavailability. Concomitant use of proton pump inhibitors such as Lansoprazole with Erlotinib should be avoided.

2. Mavacameten:

Lansoprazole with Mavacantem increases the drug's effect by affecting the hepatic enzyme CYP2C19 metabolism. The CYP2C19 inhibitors increase systemic exposure to Mavantem. As a result, it may cause heart failure due to systolic dysfunction.

3. Nelfinavir:

Lansoprazole with Nelfinavir is contraindicated as their combination may lead to loss of virologic response of Nelfinavir and the development of resistance.

4. Cabotegravir:

Concomitant use of Lansoprazole and Cabotegravir is contraindicated as it may lead to decreased absorption of the Cabotegravir (used in the treatment of the human immunodeficiency virus type-1 infection) or resistance.

5. Warfarin:

Combining Lansoprazole and Warfarin has been reported to result in an increased INR (International Normalized Ratio, based on the prothrombin test). This can lead to abnormal bleeding.

6. Tacrolimus:

Concomitant administration of Lansoprazole and Tacrolimus may increase whole blood levels, especially in transplant patients who are poor metabolizers of CYP2C19.

Conclusion:

Lansoprazole is a type of proton pump inhibitor that reduces the amount of acid your stomach produces. It is often used to treat ulcers in the stomach or intestines. You can take it by itself or mix it with other medications to help with heartburn that happens when acid flows back up from the stomach. It also helps prevent ulcers from forming in adults who have had them before or have had damage to their esophagus, and it reduces the risk of developing ulcers for those taking anti-inflammatory medications. For any issues related to Lansoprazole, you can talk to a gastro health specialist online.