lafutidine

Action and Spectrum

Actions and spectrum: 

lafutidine is a medication primarily used to treat gastrointestinal conditions. It acts as an antagonist of histamine H2 receptors, which reduces production of stomach acid. This can help in treating conditions like peptic ulcers and gastroesophageal reflux disease (GERD). 

The spectrum of lafutidine’s action is within the gastrointestinal tract, where it helps to reduce gastric acid secretion and alleviate symptoms associated with excess stomach acid. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Constipation 

anorexia 

hyperuricaemia 

Gynaecomastia 

hallucinations 

blood dyscrasias 

Anaphylactic reactions 

increased LFT & total bilirubin 

Black Box Warning

Black Box Warning: 

There were no specific black box warnings associated with lafutidine. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: lafutidine should not be used in individuals who have a known hypersensitivity or allergy to the active ingredient or any of the components of the medication. 
• Pregnancy and Lactation: The use of lafutidine during pregnancy and lactation should be done under the guidance of a healthcare professional. 
• Children: lafutidine may not be recommended for use in very young children or infants without specific guidance from a healthcare provider. 
• Severe Liver Impairment: Patients with severe liver impairment may require dose adjustments or should avoid using lafutidine, as the drug is metabolized in the liver. 
• Renal Impairment: Individuals with severe kidney impairment may require dose adjustments or should avoid using lafutidine, as the drug is excreted through the kidneys.

Caution: 

• Elderly Patients: Elderly individuals may be more susceptible to certain side effects of lafutidine, so they should use it with caution.  
• Drug Interactions: lafutidine can interact with other medications. Patients who are taking other drugs, especially those that affect stomach acid production or absorption, should inform their healthcare provider to avoid potential interactions. 
• Allergic Reactions: Like any medication, allergic reactions are possible. Patients should be monitored for allergic reaction, like rash, swelling, itching, severe dizziness, or difficulty breathing. If any of these symptoms occur, medical attention should be sought immediately. 
• Pediatric Use: lafutidine may not be recommended for use in very young children or infants without specific guidance from a healthcare provider. 
• Long-Term Use: Prolonged use of acid-suppressing medications like lafutidine may be associated with certain risks, including decreased absorption of certain nutrients. The decision to use it long-term should be made by a healthcare provider. 

Comorbidities: 

• Peptic Ulcers: lafutidine can be used in the treatment of peptic ulcers, which often coexist with GERD or may have similar symptoms. 
• Hiatal Hernia: A hiatal hernia can contribute to GERD symptoms. It occurs when a portion of the stomach protrudes into the chest through the diaphragm. 
• Functional Dyspepsia: Some people with GERD also experience functional dyspepsia, which involves recurrent pain or discomfort in the upper abdomen. 
• Helicobacter pylori Infection: lafutidine may be part of a treatment regimen for H. pylori infection, which can contribute to peptic ulcers and GERD. 
• Asthma: There is a known association between GERD and asthma. lafutidine may be used in individuals with both conditions to help manage GERD-related asthma symptoms. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into breast milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

lafutidine is a medication used to treat gastroesophageal reflux disease (GERD) and related conditions. Its pharmacology primarily revolves around its action as an H2 receptor antagonist. lafutidine works by selectively blocking histamine H2 receptors in the stomach lining, which reduces the production of stomach acid.

This leads to decreased acidity in the stomach, alleviating symptoms like heartburn and acid reflux. Additionally, lafutidine may have cytoprotective effects on the stomach lining, helping to prevent damage caused by excess acid. It is well-absorbed after oral administration, and its effects typically last for several hours. lafutidine’s pharmacological profile makes it an effective option for managing acid-related gastrointestinal disorders.  

Pharmacodynamics: 

• Histamine Blockade: lafutidine selectively binds to histamine H2 receptors on the surface of parietal cells in the stomach lining. By doing so, it competitively inhibits the binding of histamine, a natural chemical messenger, to these receptors. 
• Reduction in Gastric Acid Secretion: When histamine binds to H2 receptors, it triggers a series of intracellular events that lead to the secretion of gastric acid. lafutidine’s blockade of these receptors prevents this cascade, reducing the production of stomach acid. 
• Decreased Acidic Environment: By inhibiting the production of gastric acid, lafutidine helps to raise the pH level in the stomach. This results in a less acidic environment, which can be beneficial for individuals with conditions like gastroesophageal reflux disease (GERD) or gastritis, as it reduces symptoms such as heartburn and acid reflux. 
• Cytoprotective Effects: Some studies suggest that lafutidine may have cytoprotective properties, which means it could help protect stomach lining from damage caused by excess acidity and various irritants. This can contribute to the healing of gastric ulcers and prevention of further damage.

Pharmacokinetics: 

Absorption 

lafutidine is well-absorbed after oral administration. It is absorbed from the gastrointestinal tract, particularly the small intestine. 

Distribution 

After absorption, lafutidine is distributed throughout the body via the bloodstream. It can enter various tissues, including the stomach lining, where it exerts its pharmacological effects on histamine H2 receptors. 

Metabolism 

lafutidine undergoes hepatic metabolism in the liver. The primary metabolic pathway involves cytochrome P450 enzymes, particularly CYP2C19 and CYP3A4. It is metabolized into several metabolites, including desalkyl lafutidine and N-oxide metabolites. 

Elimination and excretion 

The metabolites of lafutidine, along with any unmetabolized drug, are primarily excreted via the urine. The primary route of elimination for lafutidine and its metabolites. 

Adminstartion

Administration: 

• Dosage: The recommended dosage will depend on your age, weight, and the severity of your condition.  
• Timing: lafutidine is often taken before meals to help reduce stomach acid secretion and alleviate symptoms associated with conditions like GERD or peptic ulcers. 
• Duration: Follow the prescribed treatment duration recommended by your healthcare provider. Do not stop taking the medication prematurely, even if you start feeling better, unless advised by doctor. 
• Food Interaction: lafutidine is commonly taken before meals to enhance its effectiveness in reducing stomach acid. Follow your healthcare provider’s instructions regarding when to take it in relation to your meals. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: lafutidine 

Pronounced: (la-fyoo-ti-deen)  

Why do we use lafutidine? 

• Gastroesophageal Reflux Disease (GERD): lafutidine is often prescribed to manage the symptoms of GERD, where stomach acid flows back into esophagus, causing heartburn, regurgitation, and irritation of the esophageal lining. 
• Peptic Ulcers: It is used in the treatment of peptic ulcers, including gastric ulcers (in the stomach) and duodenal ulcers (in the first part of the small intestine). lafutidine helps in reducing acid secretion and promoting ulcer healing. 
• Gastritis: lafutidine can be prescribed to alleviate of gastritis, an inflammation of stomach lining that can cause abdominal pain, bloating, and discomfort. 
• Zollinger-Ellison Syndrome: In cases of Zollinger-Ellison syndrome, a rare condition characterized by excessive acid production in the stomach, lafutidine may be used to control acid secretion and manage symptoms. 
• Non-Ulcer Dyspepsia: In some cases of non-ulcer dyspepsia, a condition characterized by symptoms like bloating, abdominal discomfort, and pain without the presence of ulcers, lafutidine may be prescribed to alleviate symptoms.