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Pantoprazole

Pantoprazole is an inhibitor of H + / K + ATPase (proton pump) , a blocker of hydrochloric acid secretion . Antiulcer drug. The original molecule under the trade name Controlok was developed by Takeda (formerly Nycomed). It is also sold under the trademarks PanGastro , Sanpraz , Pantap, Ulsepan.

Pantoprazole
Pantoprazole Enantiomers Strutural Formulae.png
Chemical compound
IUPAC( RS ) -5- (difluoromethoxy) - 2 - [(3,4-dimethoxypyridin-2-yl) methylsulfinyl] - 3 H- benzoimidazole
Gross formulaC 16 H 15 F 2 N 3 O 4 S
Molar mass383.371 g / mol
Cas
PubChem
Drugbank
Classification
ATX
Pharmacokinetics
Bioavailable77%
Metabolismhepatic (CYP2C19 and CYP3A4)
The half-life.1 hour
Excretionwith urine
Route of administration
internal, intravenous
Other names
"Control", "Pantap", "Ulsepan."

Content

Pharmacological action

Inhibitor of H + / K + ATPase . It blocks the final stage of the secretion of hydrochloric (hydrochloric) acid , reduces the level of basal and stimulated (regardless of the type of stimulus) secretion of hydrochloric (hydrochloric) acid in the stomach. In case of duodenal ulcer associated with Helicobacter pylori , a decrease in gastric secretion increases the sensitivity of the microorganism to antibiotics.

Does not affect the motility of the digestive tract . Secretory activity is normalized 3-4 days after the end of the drug.

Pharmacokinetics

Suction

After taking the drug inside, pantoprazole is rapidly absorbed from the digestive tract. Cmax is reached after 2.5 hours and amounts to 2-3 mg / l, while the Cmax value remains unchanged when taken repeatedly. Bioavailability of 65-77%.

Withdrawal

The elimination half-life (T 1/2 ) is about 1 hour. The half-life does not reflect the duration of the drug.

Indications

- peptic ulcer of the stomach or duodenum in the acute phase;

- erosive gastritis (including those associated with Helicobacter pylori );

- erosive and ulcerative lesions of the stomach and duodenum associated with NSAIDs ;

- reflux esophagitis ;

- eradication of Helicobacter pylori in combination with two antibiotics;

- Zollinger-Ellison syndrome and other pathological conditions associated with increased gastric secretion.

Dosage

With peptic ulcer of the stomach and duodenum, erosive gastritis, the drug is prescribed at 40-80 mg / day. The course of treatment for exacerbation of duodenal ulcer is 2 weeks, and gastric ulcer - 4-8 weeks.

For the prevention of exacerbations of gastric ulcer and duodenal ulcer, 20 mg / day are prescribed.

To eradicate Helicobacter pylori, 40 mg are taken 2 times / day in combination with antimicrobial agents. The course of therapy is 7-14 days.

With erosive and ulcerative lesions of the stomach and duodenum associated with NSAIDs, 40-80 mg / day are prescribed. The course of treatment is 4-8 weeks. For the prevention of erosive lesions against the background of prolonged use of NSAIDs - 20 mg / day.

With reflux esophagitis, 20-40 mg / day is prescribed. The course of therapy is 4-8 weeks. To prevent exacerbations, take 20 mg / day.

In patients with severe hepatic impairment, the dose should be reduced to 40 mg once every 2 days, and it is necessary to monitor blood biochemical parameters. With an increase in the activity of liver enzymes, the drug should be discontinued.

Tablets are taken orally as a whole (without crushing or dissolving), washed down with a sufficient amount of liquid. The drug is recommended to be taken 1 hour before breakfast, with a frequency of administration 2 times a day, the second dose - 1 hour before dinner.

Side effect

From the side of the central nervous system : headache; very rarely - depression , weakness, dizziness, visual impairment.

From the digestive system: diarrhea , nausea , pain in the upper abdomen, constipation , flatulence ; in isolated cases - severe hepatocellular damage to the liver with jaundice , impaired liver function.

Allergic reactions: skin rash, itching, flushing of the skin, anaphylactic reactions (up to shock).

Other: painful tension of the mammary glands, hyperthermia .

Contraindications

- dyspepsia of neurotic origin;

- children's age (due to lack of data on the use of the drug in pediatric practice);

- Hypersensitivity to pantoprazole.

With caution, a drug is prescribed for liver failure.

Pregnancy and lactation

With caution, the drug is prescribed during pregnancy and during lactation (breastfeeding). The experience with pantoprazole in pregnant women is limited. There is no data on the allocation of pantoprazole with breast milk.

Special instructions

Before and after the end of therapy, endoscopic monitoring (if necessary, with a biopsy ) is required to exclude malignant neoplasms of the stomach or esophagus, since the use of the drug may delay the correct diagnosis.

Overdose

Symptoms of an overdose in humans are not known. Treatment: there is no specific antidote. In case of an overdose of the drug, accompanied by the usual signs of intoxication, detoxification measures are used. The treatment is symptomatic.

Drug Interactions

With the simultaneous use of pantoprazole can reduce the absorption of drugs, the bioavailability of which depends on the pH of the stomach (for example, ketoconazole).

External links

  • Official website of the manufacturer
  • Pantoprazole Information at DrugLib

See also

  • Proton pump inhibitors
Source - https://ru.wikipedia.org/w/index.php?title=Pantoprazole&oldid=95131874


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Clever Geek | 2019