The representative of proton pump inhibitors - esomeprazole has something to say

In recent years, proton pump inhibitors have been widely used to treat acute and chronic acid-related diseases of the digestive system, including gastroesophageal reflux disease, peptic ulcer, upper gastrointestinal bleeding, Helicobacter pylori infection, etc. However, due to the lack of clinical application standards for drugs, the clinical application of proton pump inhibitors has problems such as over-indications, over-dosage, over-treatment, and improper combination of drugs. In order to further standardize the clinical application of proton pump inhibitors, in 2020, the National Health Commission formulated the "Guidelines for the Clinical Application of Proton Pump Inhibitors". On February 25 this year, the State Drug Administration issued the "Announcement on the Revision of the Instructions for Proton Pump Inhibitors", which uniformly revised the contents of the instructions for 10 proton pump inhibitors, including omeprazole oral monopreparation, omeprazole injection, and esomeprazole sodium for injection. The revision items include [Adverse Reactions], [Precautions], [Drug Interactions], etc. This shows that the rational application of proton pump inhibitors has received attention at the national level.

So, what should we pay attention to when using proton pump inhibitors?

Today, we sent a member of the proton pump inhibitor family, esomeprazole, as a representative to talk about how to use it reasonably. Please welcome with applause~~

Some people say that I am the "guardian angel" of the stomach! I am used for gastritis, acid reflux, ulcers, and stomachaches... Actually, I am not that magical!

First, introduce yourself

I am the S-isomer of omeprazole, a weakly alkaline drug, and am often used clinically to inhibit gastric acid secretion. I inhibit the H+/K+-ATPase (proton pump), which inhibits both basal gastric acid secretion and stimulated gastric acid secretion. As a member of the proton pump inhibitors, my advantage is that I have a strong acid-suppressing effect and a long-lasting effect.

What diseases can I treat?

Because I have a strong inhibitory effect on gastric acid secretion, I am widely used to treat gastric diseases caused by excessive gastric acid. I have two dosage forms, oral and injection.

Oral dosage forms are mainly used for:

1. Gastroesophageal reflux disease;

2. Combined use with appropriate antimicrobial therapy can eradicate Helicobacter pylori infection and promote the healing of duodenal ulcers associated with Helicobacter pylori infection; prevent the recurrence of peptic ulcers associated with Helicobacter pylori infection;

3. Patients who require continuous NSAID treatment; Treatment of gastric ulcers associated with NSAID use.

Injectable dosage forms are mainly used for:

1. As an alternative treatment for gastroesophageal reflux disease when oral therapy is not suitable;

2. Used for acute gastric or duodenal ulcer bleeding that is not suitable for oral therapy;

3. Used to reduce the risk of rebleeding after endoscopic treatment of bleeding gastric and duodenal ulcers in adults.

Someone said that I have difficulty swallowing. Can I break it into pieces and eat it?

NO! NO! NO!

Since I am a weakly alkaline drug, in order to avoid being destroyed by gastric acid, my oral dosage form is often in the form of an enteric-coated preparation. Enteric-coated preparations are best swallowed whole and cannot be chewed or crushed. But if swallowing is difficult, you can dissolve me in water and drink it immediately or within 30 minutes after dispersion; you can also mix me with applesauce and take it. The reason why it is so special is that I have a special MUPS dosage form (full name: multiple unit pellet system, literally translated as multiple unit microcapsule system), and my inner coating remains intact in water, so I can be used for nasogastric administration in clinical practice.

Everyone says I have to eat it before meals, right?

YES! YES! YES!

My absorption site is in the intestines, so taking it on an empty stomach can avoid the effects of food. Moreover, I am most effective in inhibiting the acid secretion of parietal cells caused by food stimulation. The number of H+/K+-ATPase in the human stomach parietal cells is the highest after a long period of fasting, so if you take the medicine once a day, it is most appropriate to take me 30 to 60 minutes before breakfast. If you need to take it in divided doses, you can take it before breakfast and before dinner respectively.

Special population, can you use me?

Will my work affect my other medications?

I am a CYP2C19 inhibitor, and potential interactions between me and other drugs metabolized by CYP2C19 should be considered, such as clopidogrel, voriconazole, diazepam, citalopram, imipramine, phenytoin, clomipramine, cilostazol, etc. Therefore, it is not recommended to use me in combination with these drugs.

Can I take it long term?

Continuous use for more than 6 months is considered long-term use. If I use it beyond the period, the following may occur:

1. Increased infection - Since gastric acid itself has a strong inhibitory and inactivating effect on bacteria, when the acidic environment in the stomach is destroyed, it gives bacteria an opportunity to multiply, increasing the risk of gastrointestinal infections, such as gastrointestinal candidiasis and Clostridium difficile-associated diarrhea; if gastric juice containing bacteria refluxes into the pharynx or is even accidentally inhaled into the respiratory tract, it will increase the risk of lung infection.

2. Increased risk of fractures - Long-term use of me will destroy the acidic environment of the stomach and duodenum, which is not conducive to calcium absorption. Long-term use can cause bone loss and lead to osteoporosis, increasing the incidence of fractures, such as hip, wrist or spinal fractures.

3. Affects the absorption of vitamins - Gastric acid is very important for the absorption of vitamin B12, vitamin C, folic acid, etc., especially vitamin B12. Most current studies have shown that I will hinder the absorption of vitamin B12 in protein-bound form.

4. Hypomagnesemia - There are reports that long-term use of me can cause hypomagnesemia, and patients may experience clinical manifestations such as tetany, convulsions, dizziness, fatigue, etc. If prolonged treatment is required or combined medication such as digoxin or drugs that can cause hypomagnesemia (such as diuretics) is used, blood magnesium concentrations should be monitored regularly.

5. Others: such as atrophic gastritis, abnormal liver function, myalgia, hair loss, interstitial nephritis, myocardial infarction, anorexia, emotional indifference, increased risk of gastric cancer, etc.

Xiao Ai, I am not omnipotent. I can only play the most effective role if used reasonably under the guidance of doctors and pharmacists.

Author: Wang Jinmei, Chief Pharmacist of Zhengzhou Central Hospital

Review expert: He Meng, deputy chief pharmacist of Zhengzhou Central Hospital

Zhang Kai, deputy chief pharmacist of Zhengzhou Central Hospital