What Are the Uses of Omeprazole and Lansoprazole?

The main ingredient of this product is lansoprazole.
Chemical name: 2-[[[3-methyl-4- (2,2,2-trifluoroethoxy) -2-pyridyl] methyl] sulfinyl-1H-benzimidazole.
Chemical Structure:

Lansoprazole for injection is indicated for duodenal ulcers with bleeding that are not suitable for oral therapy.

Drug Name

Lansoprazole for injection

Drug type

Prescription drugs, medicines for medical workers' injuries

Use classification

Drugs that inhibit gastric acid secretion

Lansoprazole for injection

The main ingredient of this product is lansoprazole.
Chemical name: 2-[[[3-methyl-4- (2,2,2-trifluoroethoxy) -2-pyridyl] methyl] sulfinyl-1H-benzimidazole.
Chemical Structure:

Molecular formula: C ₁₆ H ₁₄ F ₃ N ₃ O ₂ S
Molecular weight: 369.36
The auxiliary material is mannitol, and the pH value is adjusted with an appropriate amount of sodium hydroxide.

Lansoprazole properties for injection

This product is white or off-white loose block or powder.

Lansoprazole indications for injection

It is used for duodenal ulcer with bleeding which is not applicable for oral therapy.

Lansoprazole specifications for injection

30mg.

Lansoprazole for injection

Intravenous infusion: Usually 30 mg once for adults, dissolved with 100 ml of 0.9% sodium chloride injection, twice a day, the recommended intravenous infusion time is 30 minutes, and the treatment course does not exceed 7 days.
Note when using:
(1) This product should be equipped with a filter with a pore size of 1.2 m when used in a static drop in order to remove the sediment that may be generated during the infusion. These deposits can cause small blood vessel embolism with serious consequences.
(2) In the case of high risk of spurting or gushing massive bleeding, vascular exposure, etc., endoscopic hemostasis measures should be adopted first.
(3) This product is only for intravenous infusion. It should be used as soon as possible after dissolution. Avoid infusion with liquids and other drugs other than 0.9% sodium chloride injection.
(4) If the hemostatic effect is achieved within the first 3 days after treatment with this product, oral medication should be used instead of intravenous administration without restriction.

Lansoprazole for injection adverse reactions

In domestic clinical research, this product is administered twice a day with 30 mg intravenous drip, 5 days course of treatment. Four (3.64%) adverse reactions occurred in 127 subjects, mainly leukocytopenia (1.82%), a slight increase in transaminase (0.91%), and a rash (0.91%). Leukopenia was normal after one week, and transaminase was slightly elevated after ten days.
After being marketed abroad, more than 1,000 patients were well tolerated after using lansoprazole for injection. In 161 patients in 4 clinical trials in the United States, lansoprazole for injection was used, and more than 1% of the adverse reactions were nausea (1.3%), headache (1%), pain at the injection site (1%); less than 1% The adverse reactions were abdominal pain, diarrhea, indigestion, vomiting, dizziness, paresthesia, abnormal taste, rash, and vasodilation. No adverse effects were observed compared with oral administration.
Clinical study data of 221 subjects in Japan using lansoprazole for injection reported that 31 cases (14.0%) had abnormal clinical laboratory test values, mainly due to increased ALT (6.2%) and increased AST (5.7%). , LDH increased (2.0%), -GTP increased (1.5%) and other abnormal values.
The following adverse reactions are seen with oral lansoprazole, but intravenous injections are also possible:
1. Close observation should be made during treatment, if any of the following serious adverse reactions should be discontinued in time and treatment.
(1) Allergic reactions (general rash, facial edema, dyspnea, etc.) (<0.1%), and even cause shock (<0.1%);
(2) pancytopenia and agranulocytosis, hemolysis (<0.1%), as well as granulocytopenia, thrombocytopenia, and anemia (0.1 to <5%);
(3) Severe liver damage with jaundice, elevated AST and ALT (<0.1%);
(4) Toxic epidermal necrolysis (Lyell syndrome), cutaneous mucosal eye syndrome (Stevens-Johnson syndrome) (<0.1%);
(5) Interstitial pneumonia (<0.1%), fever, cough tenderness, dyspnea, abnormal breathing sounds in the lungs (twisted sounds), etc., should promptly stop medication, perform chest x-ray examination, and give adrenocortical hormone And so on.
2. Other adverse reactions; discontinue medication when the following adverse reactions occur, and appropriate treatment if necessary.

Lansoprazole contraindication for injection

1. Patients who are allergic to lansoprazole and any of the ingredients in the prescription are prohibited from using this product.
2. Patients who are using atazanavir sulfate are prohibited from using this product.

Lansoprazole for injection matters needing attention

1. The following patients should be used with caution:
(1) Patients with a previous history of drug allergy;
(2) Patients with liver injury (due to delayed metabolism and excretion of this drug);
2. The treatment of this product will cover the symptoms of gastrointestinal tumors, and the drug should be used after excluding malignant tumors.
3. Observe the condition closely during the treatment of this product, and switch to other therapies when the treatment fails.
4. This product has no more than 7 days of medication experience.
5. Oproprazole, a similar proton pump inhibitor, has been reported to cause visual impairment in foreign countries, and this product is unclear.
6. In animal experiments, after long-term use of this product in rats, benign testicular mesenchymal tumors, carcinoid tumors and retinal atrophy appeared. But similar phenomenon did not appear in the carcinogenicity test of mice and the toxicity test of dogs and monkeys.

Lansoprazole for injection for pregnant and lactating women

The Lansoprazole oral administration test in rats showed that the Lansoprazole drug concentration in fetal plasma was higher than the maternal plasma concentration. In addition, the rabbit (oral 30mg / kg / day) test showed an increase in fetal mortality. For pregnant women and women who may become pregnant, it is recommended to use this product only when the benefits of treatment outweigh the risks.
In a rat oral lansoprazole trial, lansoprazole was secreted through breast milk. It is recommended that lactating women avoid using this product as much as possible, and should stop breastfeeding when medication is necessary.

Lansoprazole for injection for children

The safety of children using this product has not been determined, and no experience has been used.

Lansoprazole for injection

Generally, the physiological function of the elderly is reduced, so medication should be used with caution.

Lansoprazole drug interactions for injection

Lansoprazole is metabolized by the liver cytochrome P450 enzyme system, especially the CYP3A4 and CYP2C19 enzymes. Lansoprazole can significantly inhibit gastric acid secretion for a long time, so theoretically it can promote or inhibit the absorption of some combined drugs.
1. Contraindications

2. Compatibility note

Lansoprazole for drug overdose

There is currently no clinical experience with drug overdose for reference, but lansoprazole cannot be cleared from the circulatory system by hemodialysis.

Lansoprazole for injection pharmacology and toxicology

Pharmacological effects:
Lansoprazole is a proton pump inhibitor. The drug is distributed in the acidic environment of gastric mucosal parietal cells, and then converted into an active metabolite. This metabolite binds to the thiol group of the H +, K + -ATPase present in the acid-generating site and inhibits acid secretion by inhibiting the activity of the H +, K + -ATPase.
Lansoprazole inhibits gastric acid secretion in a dose-dependent manner. It inhibits gastric acid secretion caused by basal and stimulus within 24 hours after drug administration. Healthy adults were given 30 mg once a day, and intravenously twice a day, showing sustained gastric acid secretion inhibition.
It has been reported that under acidic conditions, blood coagulation and platelet aggregation are greatly impaired. The fibrin formed by blood coagulation can be dissolved by pepsin under acidic conditions. This medicine improves the blood coagulation and platelet aggregation function by increasing the pH in the stomach, inhibits the activity of pepsin, and exerts the effect of suppressing bleeding. In addition, under acidic conditions, the repair of damaged mucosa of the stomach is inhibited. This medicine increases the pH in the stomach by inhibiting acid secretion, and promotes the repair of damaged mucosa.

Toxicology research:
Genotoxicity: Ames test. The results of rat liver cell extra-synthetic DNA synthesis test, mouse micronucleus test, and rat bone marrow cell chromosome aberration test were all negative. In vitro human lymphocyte chromosome aberration test results were positive.
Reproductive toxicity: Rats and rabbits received lansoprazole intravenously at a dose of 30 mg / kg / day (equivalent to 8 and 16 times the human clinical recommended dose based on body surface area). No adverse effects on fertility and embryos were found .
Carcinogenicity study: SD rats received lansoprazole at 5-150 mg / kg / day for 24 consecutive months (calculated based on body surface area, which is equivalent to 1 to 40 times the clinically recommended dose of 30 mg / d for patients weighing 5 kg). The results showed Lansoprazole induces gastrointestinal chromaffin-like (ECL) cell proliferation and benign ECL cell tumors in a dose-dependent manner; the incidence of intestinal epithelialization in the gastric epithelium of test animals is increased. The incidence of testicular mesenchymal adenoma in male rats increased in a dose-dependent manner. Rats administered at a dose of 15 to 150 mg / kg / day (calculated based on body surface area, which is equivalent to 4 to 40 times the human clinically recommended dose). These The incidence of adenomas exceeds the natural incidence of this germline rat (1.4 to 10%). In a one-year toxicity study, testicular mesenchymal adenomas occurred in one of 30 rats administered at a dose of 50 mg / kg / day (corresponding to 13 times the human clinically recommended dose based on body surface area).
CD-1 mice received 15 to 600 mg / kg / day of lansoprazole orally (corresponding to 2 to 80 times the human clinically recommended dose based on body surface area) for 24 consecutive months. As a result, lansoprazole induced ECL in a dose-dependent manner. Cell proliferation, liver tumor incidence increased in administration mice. The incidence of tumors in male mice of the 300 and 600 mg / kg / day group and female mice of the 150-600 mg / kg / day group exceeded the historical tumors of the germline mice. Range of incidences. When lansoprazole was administered at 75-600 mg / kg / day, testicular adenomas developed in mice.

Lansoprazole for injection pharmacokinetics

When lansoprazole is administered intravenously, there are individual differences in serum concentrations. Intravenous injection of 30 mg (30 min) of lansoprazole in healthy people showed a double exponential decrease in blood concentration, a terminal half-life of 1.3 (± 0.5) h, and a peak plasma concentration (Cmax) of 1705 (± 292) ng / ml, AUC It was 3192 (± 1745) ng · h / ml, and lansoprazole 30 mg was administered orally or intravenously once a day. The pharmacokinetic parameters after 7 days did not change with time.

Twelve healthy adult men were divided into fast metabolizer group and slow metabolizer group according to CYP2C19 genotype, 30 mg once, twice a day, and intravenous drip for 5 days. The main pharmacokinetic parameters are shown in the table.

For patients with different degrees of chronic liver disease, the average drug half-life of oral lansoprazole was extended from 1.5 hours to 3.2-7.2 hours. In patients with liver injury, the AUC can increase to 500% when compared with healthy people. Therefore, the intravenous dose of patients with severe liver injury should be reduced.
Oral lansoprazole studies suggest that there is no difference in the pharmacokinetics of patients with gender and renal insufficiency, so intravenous doses do not need to be adjusted.

The apparent distribution volume of sub-Bransoprazole is about 15.7 (± 1.9) L, which is mainly distributed in extracellular fluid. The plasma protein binding rate was 97%. When the blood drug concentration was 0.05-5.0 g / ml, the plasma protein binding was constant.

The plasma elimination half-life of metabolizing lansoprazole has nothing to do with the effect of inhibiting gastric acid secretion. The elimination half-life of lansoprazole is less than 2 hours, and the effect of inhibiting gastric acid secretion is at least 24 hours.
Lansoprazole is metabolized by the cytochrome P450 enzyme system, especially the CYP2C19 and CYP3A4 enzymes. It is reported that there is a genetic polymorphism in CYP2C19, and about 10-20% of the Asian Mongolian race is of the slow metabolizer type. Lansoprazole is extensively metabolized in the liver, and two major metabolites (hydroxylated sulfinyl and sulfo derivatives) are detected in plasma. These metabolites are only converted into two active components that inhibit H +, K + -ATPase in the tubules of gastric parietal cells, but they are not detected in the systemic circulation.

The mean clearance of lansoprazole after intravenous injection was 11.1 (± 3.8) L / h. Healthy adult men, 30 mg intravenously once, no prototype drug in urine, all metabolites, the cumulative excretion rate in the urine 24 hours after the end of administration is 12-17%. An oral 14C-labeled lansoprazole study showed that about one third of the dose (radioactive) was excreted through the urine, and about two thirds of the radioactive material appeared in the feces, suggesting that the metabolites of lansoprazole pass Bile and urine excretion.

Lansoprazole for injection storage

Protected from light and sealed.

Lansoprazole for injection

(1) 1 bottle / box of vials.
(2) 2 vials / box.

Lansoprazole for injection

24 months.

Lansoprazole for injection

State Food and Drug Administration Standard YBH02092012