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Pantoprazole - all you need to know - luminant - updated for 2018
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Pantoprazole , first sold under the trademark Protonix , is used for the short-term treatment of erosive esophagitis associated with gastroesophageal reflux disease (GERD), maintenance of erosive esophagitis, and pathologic hypersecretion conditions including Zollinger-Ellison syndrome.

Some of the common side effects of using pantoprazole in adults include: headache, diarrhea, nausea, abdominal pain, vomiting, abdominal bloating, dizziness, and joint pain (& gt; 2%). The long-term use of pantoprazole may cause chronic inflammation of the stomach lining or atrophic gastritis, vitamin B-12 deficiency, and low magnesium.

Pantoprazole is a proton pump inhibitor that inhibits gastric acid secretion. It works on gastric parietal cells to inhibit irreversible (H/K) - ATPase function and suppress the production of stomach acid. It was first sold in 1994 in Germany and became available as a generic drug in 2010.


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Medical use

Pantoprazole is used for short-term treatment of erosion and esophageal ulceration for adults and patients aged 5 years and older who are caused by gastroesophageal reflux disease. It can be used as maintenance therapy for long-term use after the initial response is obtained, but there has been no controlled study of pantoprazole use for 12 months. Pantoprazole can also be used in combination with antibiotics to treat ulcers caused by Helicobacter pylori . It can also be used for long-term treatment of Zollinger-Ellison syndrome.

Pregnancy

US. Pregnancy Category B: In reproductive studies using larger doses than recommended doses in rats and rabbits, there is no obvious danger to infant development.

Breastfeeding

Pantoprazole has been found through breast milk. However, in rodent cancer studies, pantoprazole has been shown to potentially cause tumor growth. The clinical relevance of these findings is unknown, but risks and benefits are recommended for consideration in determining the use of therapies for mothers and children.

Children

Pantoprazole is only indicated for the short-term treatment of erosive esophagitis in children age 7 and older; and the safety and effectiveness of pantoprazole has only been established in the treatment of erosive esophagitis in children.

Elderly

The incidence of adverse events occurring in patients aged 65 years and older was similar to that in patients aged 65 and under.

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Adverse effects

  • Infection: Gastric acid plays a role in killing the ingested bacteria. The use of pantoprazole may increase the likelihood of developing infections such as pneumonia, especially in hospitalized patients.

General

  • Gastrointestinal: abdominal pain (6%), diarrhea (9%), flatulence (4%), nausea (7%), vomiting (4%)
  • Neurologic: headache (12%), dizziness (3%)
  • Neuromuscular and skeletal: arthralgia (3%)

Rare

  • Gastrointestinal: constipation, dry mouth, hepatitis
  • Blood problems: low white blood cell count, thrombocytopenia
  • Immunologic: Stevens-Johnson syndrome, toxic epidermal necrolysis
  • Metabolism: increased creatine kinase, elevated cholesterol levels, elevated liver enzymes (AST/ALT), swelling
  • Musculoskeletal: Musculoskeletal disorders, fractures and infections, Clostridium difficile infection , pelvic fractures associated with osteoporosis, rhabdomyolysis
  • Kidney: interstitial nephritis
  • Nutrition: can reduce the absorption of essential nutrients, vitamins, and minerals, including certain drugs, making users at high risk of pneumonia.

Long-term use

  • Osteoporosis and bone fractures have been observed in patients with high-dose and/or long-term proton pump inhibitors (more than 1 year).
  • Hypomagnesia has been observed in patients who use drugs such as pantoprazole when taken for a longer time (generally 1 year or more, although cases have been reported on a 3 month regimen).

Termination

In people in the PPI for more than six months, a pointed dose should be considered before discontinuation. For those who are to high-dose this can be done by 50 percent every week to the lowest dose. After a week, it can then be stopped.

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Interactions

  • Acidity: Because of its effect of reducing gastric acidity, the use of pantoprazole may affect the absorption of pH-sensitive drugs such as ampicillin ester, ketoconazole, atazanavir, iron salt, amphetamine, and mycophenolate mofetil.

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Pharmacology

The mechanism of action of pantoprazole is to inhibit the final step in gastric acid production. In stomach parietal cells, covalent pantoprazol binds the ATP H/K pump to inhibit gastric acid and basal acid secretion. Covalent bonds prevent acid secretion up to 24 hours and longer.

Pantoprazole is metabolized in the liver by cytochrome P450. Metabolism consists primarily of demetilation by CYP2C19 followed by sulfation. The other metabolic pathway is oxidized by CYP3A4. Pantoprazole metabolism is not considered to have pharmacological significance. Usually given with a prokinetic drug because it is not active in the acid environment of the stomach. Pantoprazole binds irreversibly to H K ATPase (proton pump) to suppress acid secretion. Due to the irreversible pump binding, new pumps must be made before acid production can proceed. The median half-life of the drug is about 2 hours.

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History

Pantoprazole was discovered by scientists at Byk Gulden, a subsidiary of Altana; drug discovery programs began in 1980 and produced pantoprazole in 1985 - the compound was actually made by chemists working on the improvement of a different chemical that has been selected as a development candidate. Byk Gulden partnered with Smith Kline & amp; France in 1984. The compound development name is BY1029 and SK & amp; F96022. In 1986 the company had created sodium salt, sodium sesquihydrate pantoprazole, and decided to develop it because it was more easily soluble and stable, and more compatible with other materials used in formulations. It was first marketed in Germany in 1994. Wyeth licensed US patents from Altana. and obtained marketing approval from the US FDA in 2000 under the trade name Protonix.

In 2004, worldwide drug sales reached $ 3.65 billion, about half in the US.

In 2007, Altana drug business was acquired by Nycomed. Nycomed was in turn acquired by Takeda in 2011 and Wyeth was acquired by Pfizer in 2009.

The patent protecting the drug was set to expire in 2010, but Teva Pharmaceutical filed YOU in 2007, and Wyeth and Nycomed sued Teva for patent infringement, but Teva decided to launch its "risky" generic drug that year, before the patent was canceled. Wyeth launched its official generic in 2008. The exclusivity of Pfizer and Takeda's patents has expired in 2010, and their administrative exclusivity for pediatric use ends in January 2011, and full generic competition begins. Litigation between Teva and Pfizer/Takeda was completed in 2013, with Teva paying a $ 2.15 billion patent holder on damage for the initial launch.

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Society and culture

By 2017, the drug is marketed under many brands worldwide, including as a combination drug with domperidone, a combination with itopride, in combination with clarithromycin and amoxicillin, in combination with levosulpiride, and in combination with naproxen.

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References


Pillbox - National Library of Medicine
src: pillbox.nlm.nih.gov


External links

  • Protonix label (Pantoprazole Sodium)

Source of the article : Wikipedia

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