For people who often suffer from stomach problems, there are so many prazoles! Which one should I choose?

There are so many types of prazole, which one should I choose?

In daily life, people who often suffer from stomach problems may be familiar with "prazole" drugs. In pharmacies, you can often see omeprazole, rabeprazole, lansoprazole, esomeprazole... There are many types of drugs called prazole. Faced with so many prazoles, many patients are at a loss when choosing. Which one should I choose? Which prazole is suitable for me?

What are proton pump inhibitors? What are their indications?

Omeprazole, rabeprazole, lansoprazole and other drugs called "prazoles" are all proton pump inhibitors (PPIs). Proton pump inhibitors are currently the most widely used drugs in the treatment of gastric acid-related diseases in the clinic, with the most outstanding acid-suppressing effect, and are the drugs with the strongest acid-suppressing effect to date. Proton pump inhibitors are weakly alkaline benzimidazole derivatives that can quickly pass through the gastric wall cell membrane, accumulate in the strongly acidic secretory tubules, and convert into sulfonamide compounds. They covalently bind to the sulfhydryl group of H+/K+-ATPase to form a disulfide bond, inactivating the proton pump, thereby inhibiting central or peripherally mediated gastric acid secretion.

How many categories are proton pump inhibitors divided into? What are the representative drugs?

Irreversible proton pump inhibitors can be divided into two generations according to their development and metabolic characteristics.

The first generation takes longer to take effect than the second generation, and the efficacy is not strong enough. It requires multiple doses (i.e., several days) to achieve the maximum acid suppression effect, and has a significant nocturnal breakthrough phenomenon (NAB). It may not be able to suppress acid stably for 24 hours. The time of taking the medicine and the time of eating may affect the efficacy and pharmacokinetic parameters, and there are large individual differences in pharmacokinetics.

1. Duodenal ulcer

Cure rate: pantoprazole, rabeprazole, esomeprazole ≈ omeprazole

Lansoprazole＞omeprazole (within 2 weeks), lansoprazole≈omeprazole (within 4 weeks)

Pain relief: pantoprazole, rabeprazole, esomeprazole > omeprazole

2. Omeprazole is the first-line treatment for gastroesophageal reflux

Efficacy: Esomeprazole>Omeprazole≈Lansoprazole, Pantoprazole, Rabeprazole

Acid suppression: Esomeprazole > Rabeprazole > Lansoprazole, Pantoprazole > Omeprazole

3. HP

Eradication rate: lansoprazole > omeprazole > rabeprazole, pantoprazole, esomeprazole

95.5% 79—96% 85% 85% 85%

Ulcer healing rate: Rabeprazole > Omeprazole ≈ Esomeprazole

The current recommended regimen for eradicating Helicobacter pylori in China is: PPI + bismuth + 2 antibacterial drugs, with a course of 14 days. Because CYP2C19 has genetic polymorphism (fast metabolizer, medium metabolizer, slow metabolizer), rabeprazole and esomeprazole are less affected by CYP2C19 genetic polymorphism and can be used first.

4. Duration

Esomeprazole＞rabeprazole＞omeprazole＞lansoprazole＞pantoprazole

Time to take medicine

Gastric acid can destroy PPIs. Oral preparations are all enteric-coated and cannot be chewed or crushed before taking. The number of newly formed proton pumps on gastric wall cells is the highest in the morning, so it is recommended to take it in the morning. Meals can activate proton pumps, so it is recommended to take it 0.5-1h before breakfast. If taken twice a day, the other dose should be taken 0.5-1h before dinner.

Therefore, for people who often suffer from stomach problems, the use of proton pump inhibitors should be carried out under the guidance of doctors, and the right medicine should be used to achieve twice the result with half the effort. In addition, the use of proton pump inhibitors should also pay attention to its adverse reactions, such as common adverse reactions such as digestive system, infection, trace element deficiency, osteoporosis, increased risk of myocardial infarction, etc., causing kidney damage such as acute interstitial nephritis and chronic kidney disease has gradually attracted the attention of experts and scholars, and long-term use of drugs can lead to the risk of atrophic gastritis and hypergastrinemia, which should also be taken seriously.

References:

[1]Xu Tao. A simple comparative analysis of common proton pump inhibitors in China. Chinese Journal of Modern Drug Application, 2015, 9(12): 257-258.

[2] Expert consensus on optimizing the use of proton pump inhibitors (2020)

Author: Yu Hong, Chief Pharmacist, Sports New City Branch, Dalian Women and Children's Medical Center (Group)

Reviewer: Li Ling, Chief Pharmacist, Sports New City Branch, Dalian Women and Children's Medical Center (Group)