vonoprazan fumarate

Action and Spectrum

Actions and Spectrum 

Action: 

vonoprazan works selectively and irreversibly inhibits the proton pump, an enzyme called H+/K+-ATPase, in the stomach. This enzyme is responsible for the secretion of gastric acid into the stomach. By inhibiting this enzyme, the drug reduces acid production, effectively suppressing gastric acid secretion. 

Spectrum: 

vonoprazan is highly effective in reducing gastric acid secretion, and it has a broad spectrum of activity.  

Gastroesophageal Reflux Disease (GERD): vonoprazan can provide relief from the symptoms of GERD, such as heartburn, regurgitation, and difficulty swallowing. It helps in healing the esophageal mucosa that may have been damaged by excessive acid exposure. 

Gastric Ulcers: vonoprazan treats and prevents gastric ulcers caused by excessive acid secretion or infection with the bacteria Helicobacter pylori (H. pylori). It helps in reducing stomach acid levels, allowing the ulcers to heal. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: The utilization of this drug is contraindicated in individuals who exhibit a recognized hypersensitivity or allergic reaction to this medication or any of its constituent elements. Signs of a hypersensitivity reaction may include rash, itching, swelling, dizziness, or difficulty breathing. 

Severe liver impairment: The drug is primarily metabolized in the liver, and its safety and efficacy have not yet been adequately established in individuals experiencing severe liver impairment. Caution should be exercised in individuals with liver dysfunction; a healthcare professional may need to adjust the dosage accordingly. 

Pregnancy and breast-feeding: The safety of vonoprazan in pregnancy and breast-feeding has not been well established. It is commonly advised to not using this drug while pregnant. unless the potential benefits outweigh the risks. Similarly, it is advisable to consult a healthcare professional regarding the use of this drug while breast-feeding. 

Age restrictions: The effectiveness and safety of this medication in children have not been determined. and it is typically not recommended for use in children below a certain age. The specific age restrictions may vary depending on the country and local guidelines. 

Interactions with other medications: Drug may interact with certain medications, such as those metabolized by the liver enzymes CYP2C19 and CYP3A4. This includes drugs like warfarin, diazepam, phenytoin, and certain antiretroviral drugs. A healthcare professional should review a patient’s medication list to identify potential interactions before prescribing this drug. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

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:  

vonoprazan is a medication used in the treatment of acid-related gastrointestinal disorders, such as gastroesophageal reflux disease (GERD) and peptic ulcers. The drug class is proton pump inhibitors (PPIs), which reduce stomach acid production. 

Pharmacodynamics:  

vonoprazan acts by irreversibly binding to and inhibiting the enzyme H+/K+-ATPase (also known as the gastric proton pump) in the stomach’s parietal cells. The enzyme described here plays a critical function in the final phase of stomach acid synthesis. where it pumps hydrogen ions into the gastric lumen. By inhibiting this enzyme, vonoprazan suppresses gastric acid secretion more effectively than some other PPIs.  

Pharmacokinetics: 

Absorption 

The drug is Administered either in tablet form or as a suspension and is quickly absorbed into the body through the gastrointestinal system, with peak plasma concentrations typically reached within 1 to 2 hours after oral administration.  

Distribution 

The drug is extensively bound to plasma proteins, primarily albumin. A large volume characterizes the distribution of this drug. indicating that it distributes widely throughout the body. 

Metabolism 

drug undergoes hepatic metabolism primarily via the cytochrome P450 (CYP) enzyme system, specifically CYP3A4 and CYP2C19. It undergoes oxidative metabolism, primarily forming inactive metabolites. The main metabolite, vonoprazan sulfonamide, does not contribute significantly to the drug’s pharmacological activity. 

Excretion and Elimination 

 The primary route of excretion for this drug and its metabolites is through the kidneys. About 80% of the administered dose is eliminated through urine, with less than 1% of the dose being excreted without any alteration. 

Adminstartion

Administration:  

Dosage:  The drug is taken orally before a meal. The specific dosage and duration of treatment may vary depending on the individual’s condition and the healthcare provider’s recommendation.  

Always follow the prescribed dosage instructions provided by your doctor. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: vonoprazan 

Why do we use vonoprazan?  

Gastroesophageal Reflux Disease (GERD): The drug is effective in reducing the production of stomach acid and can provide relief from the symptoms of GERD, including heartburn, regurgitation, and difficulty swallowing. 

Gastric Ulcers: The drug can be prescribed to treat and prevent the recurrence of gastric ulcers, It helps by suppressing acid production and allowing the ulcers to heal. 

Duodenal Ulcers: Just like gastric ulcers, drug is employed for the treatment and prevention of duodenal ulcers, which are ulcers that occur in the duodenum, the initial part of the small intestine. 

Helicobacter pylori Infection: Drug is sometimes prescribed as part of a combination therapy to eradicate Helicobacter pylori bacteria, a common cause of peptic ulcers. It helps to suppress acid production and enhances the effectiveness of antibiotics in eliminating the infection. 

Zollinger-Ellison Syndrome: This is a rare condition characterized by the overproduction of stomach acid. This drug can be used to manage excessive acid secretion in individuals with Zollinger-Ellison Syndrome.