Drug Detail:Pantoprazole (Pantoprazole (oral/injection) [ pan-toe-pra-zole ])
Drug Class: Proton pump inhibitors
1. How it works
- Pantoprazole is an acid-suppressing agent that may be used to treat conditions associated with excessive stomach acid production, such as gastroesophageal reflux (GERD), stomach ulcers, erosive esophagitis, and Zollinger-Ellison syndrome.
- Pantoprazole works by irreversibly blocking the actions of an enzyme responsible for acid production, called H+/K+ ATPase (also known as the gastric proton pump). The proton pump is located in the parietal cells of the stomach wall. Both baseline gastric acid secretion and stimulated gastric acid secretion are decreased in a dose-related manner (higher dosages cause a more pronounced decrease in stomach acid). Decreasing the production of stomach acid allows damaged tissue in the esophagus, stomach, and duodenum to heal.
- Pantoprazole belongs to the class of medicines known as proton pump inhibitors (PPIs).
2. Upsides
- Oral pantoprazole may be used for the short-term treatment of erosive or non-erosive gastroesophageal reflux disease (GERD) in adults and children over the age of 5 years. May also be used for the maintenance healing of erosive esophagitis to reduce relapse rates of daytime and nighttime heartburn symptoms in adults. Erosive esophagitis is a severe inflammation of the lining of the esophagus - the tube that carries food from the mouth to the stomach, and GERD is also known as heartburn.
- Both oral and IV pantoprazole may be useful for the treatment of hypersecretory conditions such as Zollinger-Ellison syndrome in adults.
- IV pantoprazole may be used short-term to treat gastroesophageal reflux disease associated with a history of erosive esophagitis.
- May be used off-label for aspiration prophylaxis in patients undergoing anesthesia, for Barrett's esophagus, for functional dyspepsia, for helicobacter pylori eradication, for primary prevention of NSAID-induced ulcers, for stress ulcer prophylaxis, and peptic ulcer disease. Many of these off-label uses feature in international and national guidelines.
- When used to treat GERD, guidelines recommend a 4- to 8-week treatment course; if an improvement is seen after 4 to 8 weeks consider a possible wean. May be used for up to 12 months to maintain the healing of erosive esophagitis.
- No dosage adjustment is recommended for people with kidney disease, liver disease, or the elderly.
- Available as oral delayed-release tablets, delayed-release oral granules, enteric-coated tablets, and as an intravenous (IV) powder for reconstitution for injection.
- A 2 mg/mL pantoprazole oral suspension may be made by crushing twenty pantoprazole 40mg tablets and mixing them to a fine powder, adding 340mL of sterile water, and 16.8g of sodium bicarbonate powder, and stirring with a magnetic stirrer for about 20 minutes until all the tablet remains have disintegrated. The mixture should be transferred to an amber-colored bottle and labeled "shake well" and "refrigerate". The mixture is stable for 62 days when it is refrigerated. Removing the Protonix imprint from the tablets by rubbing them with a paper towel impregnated with ethanol before crushing them improves the look of the product.
- Based on available data, pantoprazole is considered acceptable to use during pregnancy if lifestyle interventions have not been successful at improving symptoms.
- Generic pantoprazole is available.
3. Downsides
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Headache, dizziness, nausea or vomiting, abdominal pain, diarrhea, joint pain, and flatulence, are the most common side effects reported.
- May also interfere with some laboratory tests.
- May mask the symptoms of gastric cancer. An endoscopy may be necessary for some people (especially seniors) before pantoprazole treatment to rule out malignancy, or for those who don't respond to treatment or relapse soon after pantoprazole is discontinued.
- PPIs (including pantoprazole) have been associated with an increased risk of osteoporosis-related fractures of the hip, wrist, or spine. People on high-dose or long-term therapy are more at risk.
- Has also been associated with other conditions such as lupus erythematosus, magnesium deficiency, and fundic gland polyps.
- Prolonged treatment (greater than 24-36 months) may cause vitamin B12 deficiency. The risk is greater in women, people aged less than 30, and with higher dosages.
- Administration of PPIs (such as pantoprazole), has been associated with acute interstitial nephritis, a severe inflammation of the kidneys. May occur on medication initiation or at any point of therapy. Symptoms include fever, rash, and generalized aches and pains. Discontinue pantoprazole and seek medical advice.
- Has been associated with a greater risk of Clostridium difficile-associated diarrhea. See your doctor if you develop diarrhea that does not improve.
- Should not be used in people with previous hypersensitivity to pantoprazole or other substituted benzimidazole proton pump inhibitors.
- Dosing in obese children should be based on lean body weight.
- May interact with some other medications including methotrexate, rilpivirine, and other antisecretory agents. Pantoprazole can also reduce the absorption of drugs that are dependent on a certain gastric pH for their absorption.
- IV pantoprazole contains EDTA and zinc supplementation may be needed in people prone to zinc deficiency.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Tips
- Usually taken once daily.
- Swallow tablets whole; do not split, crush, or chew. Pantoprazole is best taken before breakfast or 30 to 60 minutes before a meal. If administering twice daily take the first dose before breakfast and the second dose before dinner.
- Delayed-release granules should be sprinkled on one teaspoonful of apple sauce or apple juice and then swallowed whole. This preparation should be taken within ten minutes of making and sips of water drunk immediately afterward to ensure the granules are washed into the stomach. Administer approximately 30 minutes before a meal.
- Take pantoprazole exactly as directed. Do not take more or less than prescribed. Talk to your doctor or pharmacist before taking other medications brought over the counter including supplements.
- See your doctor if you develop any unexplained fever, rash (particularly one that gets worse after you have been in the sun), new or worsening joint pain, persistent diarrhea, or generalized aches and pains.
- Also, see your doctor if you develop any muscle cramps, spasms, or weakness; jitteriness; abnormal heartbeat; dizziness; seizures; or any other symptoms of concern.
- Pantoprazole is normally taken short-term (up to 8 weeks) unless it is being used for hypersecretory conditions such as Zollinger-Ellison syndrome in adults. Talk to your doctor about how long you need to stay on pantoprazole.
- People taking pantoprazole long-term are at an increased risk of osteoporosis-related fractures of the hip, wrist, or spine; magnesium deficiency; and vitamin B12 deficiency. Talk to your doctor about taking supplements to counteract these effects.
5. Response and effectiveness
- The onset of action for acid secretion is 2.5 hours for oral pantoprazole and 15 to 30 minutes for IV pantoprazole (maximum effect 2 hours). The time to peak is 0.34 hours for the IV and 2.54 hours for the oral.
- Pantoprazole lasts for 24 hours (oral and IV).
- Poor metabolizers of CYP2C19 have an approximately 10-fold lower oral clearance compared to extensive metabolizers. People with liver disease have a 5 to 7-fold increase in the AUC (area under the curve).
6. Interactions
Medicines that interact with pantoprazole may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with pantoprazole. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with pantoprazole include:
- aminophylline or theophylline
- ampicillin
- astemizole
- bisphosphonates, such as alendronate, etidronate, or risedronate
- clopidogrel
- delavirdine
- digoxin
- diuretics
- H2 receptor antagonists (such as famotidine)
- HIV medications (eg, atazanavir, indinavir, ritonavir, or saquinavir)
- iron supplements
- methotrexate
- medications that rely on a certain gastric pH for absorption, such as ampicillin, dasatinib, erlotinib, iron salts, ketoconazole/itraconazole, mycophenolate mofetil, or nilotinib
- medications that affect either CYP3A4 or CYP2C19 hepatic enzymes, such as erythromycin, fluconazole, fluvoxamine, itraconazole, ketoconazole, or voriconazole
- misoprostol
- octreotide
- sucralfate
- tacrolimus
- warfarin (monitor INR and prothrombin time).
In addition, pantoprazole may affect some diagnostic tests, for example, those for neuroendocrine tumors or the secretin stimulation test. There have also been reports of false-positive urine screening tests for tetrahydrocannabinol (THC) in patients receiving PPIs, such as pantoprazole.
Note that this list is not all-inclusive and includes only common medications that may interact with pantoprazole. You should refer to the prescribing information for pantoprazole for a complete list of interactions.