Pantoprazole, Uses, Dosage, Side Effects, Interactions, Pregn

Pantoprazole, Uses, Dosage, Side Effects, Interactions, Pregn

Pantoprazole is a substituted benzimidazole and proton pump inhibitor with antacid activity. Pantoprazole is a lipophilic weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulphenamide, which forms an irreversible covalent bond with two sites of the H+/K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production.
Pantoprazole is a proton pump inhibitor (PPI) and a potent inhibitor of gastric acidity which is widely used in the therapy of gastroesophageal reflux and peptic ulcer disease. Pantoprazole therapy is associated with a low rate of transient and asymptomatic serum aminotransferase elevations and is a rare cause of clinically apparent liver injury.

The stability of the compound in aqueous solution is pH-dependent. The rate of degradation increases with decreasing pH. At ambient temperature, the degradation half-life is approximately 2.8 hours at pH 5 and approximately 220 hours at pH 7.8. Pantoprazole sodium sesquihydrate is a white to off-white crystalline powder and is racemic. Pantoprazole has weakly basic and acidic properties. Pantoprazole sodium sesquihydrate is freely soluble in water, very slightly soluble in phosphate buffer at pH 7.4, and practically insoluble in n-hexane.

Mechanism of Action of Pantoprazole

Pantoprazole is a substituted benzimidazole which inhibits the secretion of hydrochloric acid in the stomach by specific blockade of the proton pumps of the parietal cells. Pantoprazole is converted to its active form in the acidic environment in the parietal cells where it inhibits the H+, K+-ATPase enzyme, i.e. the final stage in the production of hydrochloric acid in the stomach. The inhibition is dose-dependent and affects both basal and stimulated acid secretion. In most patients, freedom from symptoms is achieved within 2 weeks. As with other proton pump inhibitors and H2 receptor inhibitors, treatment with pantoprazole reduces acidity in the stomach and thereby increases gastrin in proportion to the reduction in acidity. The increase in gastrin is reversible. Since pantoprazole binds to the enzyme distal to the cell receptor level, it can inhibit hydrochloric acid secretion independently of stimulation by other substances (acetylcholine, histamine, gastrin). The effect is the same whether the product is given orally or intravenously.

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Pantoprazole is a proton pump inhibitor. It accumulates in the acidic compartment of parietal cells and is converted to the active form, a sulfanilamide, which binds to hydrogen-potassium-ATP-ase at the secretory surface of gastric parietal cells. Inhibition of hydrogen-potassium-ATPase blocks the final step of gastric acid production, leading to inhibition of both basal and stimulated acid secretion. The duration of inhibition of acid secretion does not correlate with the much shorter elimination half-life of pantoprazole. 
Pantoprazole is a proton pump inhibitor (PPI) that suppresses the final step in gastric acid production by forming a covalent bond to two sites of the (H+,K+ )- ATPase enzyme system at the secretory surface of the gastric parietal cell. This effect is dose- related and leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus.
Pantoprazole is a proton pump inhibitor. It accumulates in the acidic compartment of parietal cells and is converted to the active form, a sulfanilamide, which binds to hydrogen-potassium-ATP-ase at the secretory surface of gastric parietal cells. Inhibition of hydrogen-potassium-ATPase blocks the final step of gastric acid production, leading to inhibition of both basal and stimulated acid secretion. The duration of inhibition of acid secretion does not correlate with the much shorter elimination half-life of pantoprazole. 

Indications of Pantoprazole

Pentoprazole is used to treat conditions caused by too much acid production in the stomach, such as

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Therapeutic Uses of Pantoprazole [FDA Level]

Therapeutic Indications of Pantoprazole

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Contra Indications of Pantoprazole

Taking a proton pump inhibitor such as pantoprazole may increase your risk of bone fracture in the hip, wrist, or spine. This effect has occurred mostly in people who have taken the medicine long term or at high doses, and in those who are age 50 and older.

Dosage of Pantoprazole

Strengths: 2.5 mg; 2 mg/mL; 10 mg;20 mg, 40 mg;  20, 40 mg I.V injection

Gastroesophageal Reflux Disease

  • Oral: 40 mg orally once a day
  • Duration of therapy: 8 weeks
  • Parenteral: 40 mg IV once a day, given over at least 2 minutes OR over 15 minutes
  • Duration of therapy: 7 to 10 days

Erosive Esophagitis

  • Treatment: 40 mg orally once a day
  • Duration of therapy: 8 weeks
  • Maintenance: 40 mg once daily

Zollinger-Ellison Syndrome

  • Oral: 40 mg orally 2 times a day
  • Maximum dose: 240 mg/day

Parenteral

  • Initial dose: 80 mg IV every 12 hours, given over at least 2 minutes OR over 15 minutes
  • Maintenance dose: 80 mg IV every 8 to 12 hours, given over at least 2 minutes OR over 15 minutes
  • Maximum dose: 240 mg/day
  • The maximum duration of therapy: 6 days

 Pediatric Gastroesophageal Reflux Disease

5 years and older

  • 15 to less than 40 kg: 20 mg orally once a day
  • 40 kg and greater: 40 mg orally once a day
  • Duration of therapy: Up to 8 weeks

Side Effects of Pantoprazole

The most common

More common

Rare

Drug Interactions of Pantoprazole 

Pantoprazole may interact with following drugs, supplements, & may change the efficacy of the drug

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Pregnancy Catagory of Pantoprazole 

FDA Pregnancy Category B

Pregnancy

A moderate amount of data on pregnant women (between 300-1000 pregnancy outcomes) indicate no malformative or feto/ neonatal toxicity of Pantoprazole. Animal studies have shown reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of Pantoprazole during pregnancy.

Lactation

Animal studies have shown excretion of pantoprazole in breast milk. There is insufficient information on the excretion of pantoprazole in human milk but excretion into human milk has been reported. A risk to the newborns/infants cannot be excluded. Therefore, a decision on whether to discontinue breastfeeding or to discontinue/abstain from Pantoprazole therapy should take into account the benefit of breastfeeding for the child and the benefit of Pantoprazole therapy for the woman. There was no evidence of impaired fertility following the administration of pantoprazole in animal studies

Before taking this medicine

Heartburn is often confused with the first symptoms of a heart attack. Seek emergency medical attention if you have chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, and a general ill feeling.

You should not use this medicine if

  • you are allergic to pantoprazole or to similar medicines such as lansoprazole (Prevacid), esomeprazole (Nexium), omeprazole (Prilosec, Zegerid), or rabeprazole (AcipHex); or
  • you also take medicine that contains rilpivirine (Edurant, Complera, Odefsey).

To make sure pantoprazole is safe for you, tell your doctor if you have:

  • severe liver disease;
  • low levels of magnesium in your blood;
  • lupus;
  • osteoporosis; or
  • low bone mineral density (osteopenia).
  • It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.
  • Pantoprazole can pass into breast milk and may harm a nursing baby. You should not breast-feed while using this medicine.
  • Pantoprazole is not approved for use by anyone younger than 5 years old.

References

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