Drugs For Which Gastric pH Can Affect Bioavailability
Due to its effects on gastric acid secretion, Penrazol can reduce the absorption of drugs where gastric pH is an important determinant of their bioavailability. Like with other drugs that decrease the intragastric acidity, the absorption of drugs such as ketoconazole, atazanavir, iron salts, erlotinib, and mycophenolate mofetil (MMF) can decrease, while the absorption of drugs such as digoxin can increase during treatment with Penrazol.
Concomitant treatment with Penrazol (20 mg daily) and digoxin in healthy subjects increased the bioavailability of digoxin by 10% (30% in two subjects). Co-administration of digoxin with PRILOSEC is expected to increase the systemic exposure of digoxin. Therefore, patients may need to be monitored when digoxin is taken concomitantly with PRILOSEC.
Co-administration of Penrazol in healthy subjects and in transplant patients receiving MMF has been reported to reduce the exposure to the active metabolite, mycophenolic acid (MPA), possibly due to a decrease in MMF solubility at an increased gastric pH. The clinical relevance of reduced MPA exposure on organ rejection has not been established in transplant patients receiving PRILOSEC and MMF. Use PRILOSEC with caution in transplant patients receiving MMF .
Have you experienced Penrazol side effects?
If you’re currently taking Penrazol – or are a former Penrazol user, report the side effects that you experienced – in the comments section. In your comment, mention the side effects that were harshest or most noticeable, and assign a numeric rating to each of those side effects (on a scale from 1 to 10, with “1” being minimal severity and “10” maximal severity).
To ensure that people reading this article are able to understand your situation, consider providing extra details such as: your Penrazol dose (e.g. 20 mg per day); the format you use (e.g. oral pills); the total duration of your treatment (e.g. 1 month); and concurrently-administered medications.
If you use other substances with Penrazol, have you investigated whether the side effects you’re experiencing might be due to an interaction effect and/or solely caused by the other substance(s)? In your experience, do the therapeutic effects of Penrazol outweigh the side effects? If you endured unwanted side effects during treatment, were there any strategies that you found helpful for reducing them?
In summary, while Penrazol is considered a safe and effective proton-pump inhibitor (PPI), not everyone tolerates it perfectly. If you find yourself unable to tolerate Penrazol, inform your doctor as soon as possible and consider alternative treatment options.
Before taking this medicine
Heartburn can mimic early symptoms of a heart attack. Get emergency medical help if you have chest pain that spreads to your jaw or shoulder and you feel sweaty or light-headed.
You should not use Penrazol if you are allergic to it, or if:
you are also allergic to medicines like Penrazol, such as esPenrazol, lansoprazole, pantoprazole, rabeprazole, Nexium, Prevacid, Protonix, and others; or
you also take HIV medication that contains rilpivirine (such as Complera, Edurant, Odefsey, Juluca).
Ask a doctor or pharmacist if it is safe for you to use Penrazol if you have other medical conditions, especially:
trouble or pain with swallowing;
bloody or black stools, vomit that looks like blood or coffee grounds;
heartburn that has lasted for over 3 months;
frequent chest pain, heartburn with wheezing;
low levels of magnesium in your blood; or
You may be more likely to have a broken bone in your hip, wrist, or spine while taking a proton pump inhibitor long-term or more than once per day. Talk with your doctor about ways to keep your bones healthy.
Ask a doctor before using Penrazol if you are pregnant or breast-feeding.
Do not give this medicine to a child without medical advice.
Interactions that increase the risk of side effects
- Side effects from Penrazol: Taking Penrazol with certain medications raises your risk of side effects from Penrazol. This is because the amount of Penrazol in your body is increased. Examples of these drugs include:
- Voriconazole. This drug may increase the levels of Penrazol in your body. If you’re taking high doses of Penrazol, your doctor may adjust your Penrazol dose.
- Saquinavir. Penrazol may greatly increase the levels of saquinavir in your body. Your doctor may lower your dose of saquinavir.
- Digoxin. Penrazol may increase the levels of digoxin in your body. Your doctor may monitor the levels of digoxin in your blood.
- Warfarin. Penrazol may increase the levels of warfarin in your body. Your doctor may monitor you for symptoms of bleeding.
- Phenytoin. Penrazol may increase the levels of phenytoin in your body. Your doctor may watch you for high levels of phenytoin.
- Cilostazol. Penrazol may increase the levels of cilostazol in your body. Your doctor may lower your dose of cilostazol.
- Tacrolimus. Penrazol may increase the levels of tacrolimus in your body. Your doctor may monitor the level of tacrolimus in your body.
- Methotrexate. Penrazol may increase the effects of methotrexate. Your doctor may adjust your dose depending on the levels of methotrexate in your body.
- Diazepam. Penrazol may increase the levels of diazepam in your body. Your doctor may watch you for more side effects from diazepam.
- Citalopram. Penrazol may increase the amount of citalopram in your body, leading to an increased risk of heart rhythm problems. Your doctor may limit your dosage of citalopram.
The active ingredient in PRILOSEC (Penrazol) Delayed-Release Capsules is a substituted benzimidazole, 5-methoxy-2- sulfinyl]-1H-benzimidazole, a compound that inhibits gastric acid secretion. Its empirical formula is C17H19N3O3S, with a molecular weight of 345.42. The structural formula is:
Penrazol is a white to off-white crystalline powder that melts with decomposition at about 155°C. It is a weak base, freely soluble in ethanol and methanol, and slightly soluble in acetone and isopropanol and very slightly soluble in water. The stability of Penrazol is a function of pH; it is rapidly degraded in acid media, but has acceptable stability under alkaline conditions.
The active ingredient in PRILOSEC (Penrazol magnesium) for Delayed-Release Oral Suspension, is 5-Methoxy-2-sulfinyl]-1H-benzimidazole, magnesium salt (2:1)
Penrazol magnesium is a white to off white powder with a melting point with degradation at 200°C. The salt is slightly soluble (0.25 mg/mL) in water at 25°C, and it is soluble in methanol. The half-life is highly pH dependent.
The empirical formula for Penrazol magnesium is (C17H18N3O3S)2 Mg, the molecular weight is 713.12 and the structural formula is:
PRILOSEC is supplied as delayed-release capsules for oral administration. Each delayed-release capsule contains either 10 mg, 20 mg or 40 mg of Penrazol in the form of enteric-coated granules with the following inactive ingredients: cellulose, disodium hydrogen phosphate, hydroxypropyl cellulose, hypromellose, lactose, mannitol, sodium lauryl sulfate and other ingredients. The capsule shells have the following inactive ingredients: gelatin-NF, FD&C Blue #1, FD&C Red #40, D&C Red #28, titanium dioxide, synthetic black iron oxide, isopropanol, butyl alcohol, FD&C Blue #2, D&C Red #7 Calcium Lake, and, in addition, the 10 mg and 40 mg capsule shells also contain D&C Yellow #10.
Each packet of PRILOSEC For Delayed-Release Oral Suspension contains either 2.8 mg or 11.2 mg of Penrazol magnesium (equivalent to 2.5 mg or 10 mg of Penrazol), in the form of enteric-coated granules with the following inactive ingredients: glyceryl monostearate, hydroxypropyl cellulose, hypromellose, magnesium stearate, methacrylic acid copolymer C, polysorbate, sugar spheres, talc, and triethyl citrate, and also inactive granules. The inactive granules are composed of the following ingredients: citric acid, crospovidone, dextrose, hydroxypropyl cellulose, iron oxide and xantham gum. The Penrazol granules and inactive granules are constituted with water to form a suspension and are given by oral, nasogastric or direct gastric administration.
Q: What is the difference between Prilosec and Zantac?
A: Prilosec (Penrazol) belongs to a class of medications called proton-pump inhibitors. Prilosec (Penrazol), the prescription strength form, is usually prescribed to be used alone or with other medications to treat ulcers, gastroesophageal reflux disease (GERD), a condition in which backward flow of acid from the stomach causes heartburn and injury of the esophagus, and erosive esophagitis. Prilosec (Penrazol) delayed-release capsules are also used to treat conditions in which the stomach produces too much acid. Also, Prilosec (Penrazol) delayed-release capsules are used in combination with other medications to eliminate H. pylori, a bacterium that causes ulcers; and possibly prevent new ulcers from developing in people who have or have had ulcers of the small intestine. Prilosec OTC is available over-the-counter and is used to treat frequent heartburn (heartburn that occurs at least 2 days/ week). It works by lowering the release of acid made in the stomach. Zantac (ranitidine) belongs to a class of medications called H2 blockers. .Zantac (ranitidine) is usually prescribed for treating ulcers, gastroesophageal reflux disease (GERD), a condition in which backward flow of acid from the stomach causes heartburn and injury of the esophagus; and conditions where the stomach over produces acid, such as Zollinger-Ellison syndrome. Over-the-counter ranitidine is used to prevent and treat symptoms of heartburn associated with acid indigestion and sour stomach. It helps lower the amount of acid made in the stomach. Although Prilosec and Zantac belong to different groups of medications and their chemical compositions are different. The ultimate result is the same in lowering the amount of acid secretion in the stomach. Both medications are effective as long as they are taken as directed. Talk to your healthcare provider or pharmacist about your treatment options. Anissa Lee, RPh