Prolex

Prolex Uses, Dosage, Side Effects, Food Interaction and all others data.

Prolex is chemically a novel substituted benzimidazole derivative, which suppresses the final step in gastric acid production by forming a covalent bond to two sites of H+/K+ATPase enzyme system at the secretory surface of the gastric parietal cell. This leads to inhibition of both basal and stimulated gastric effect that persists longer than 24 hours.

Prolex is quantitatively absorbed and its bioavailability does not change upon multiple dosing. Prolex is extensively metabolized in the liver. Almost 80% of an oral dose is excreted as metabolites in urine; the remainder is found in feces.

This drug acts to decrease gastric acid secretion, which reduces stomach acidity. Prolex administration leads to long-lasting inhibition of gastric acid secretion.

General Effects

Prolex has been shown to reduce acid reflux-related symptoms, heal inflammation of the esophagus, and improve patient quality of life more effectively than histamine-2 receptor antagonists (H2 blockers). This drug has an excellent safety profile and a low incidence of drug interactions. It can be used safely in various high-risk patient populations, including the elderly and those with renal failure or moderate hepatic dysfunction.

Trade Name Prolex
Availability Prescription only
Generic Pantoprazole
Pantoprazole Other Names Pantoprazol, Pantoprazole, Pantoprazolum
Related Drugs amoxicillin, omeprazole, famotidine, metronidazole, Nexium, Pepcid, Protonix, esomeprazole, sucralfate, Prilosec
Weight 10mg
Type Tablet, Dsr Capsule
Formula C16H15F2N3O4S
Weight Average: 383.37
Monoisotopic: 383.075133083
Protein binding

Approximately 98%

Groups Approved
Therapeutic Class Proton Pump Inhibitor
Manufacturer Unilex Lifesciences Pvt Ltd, Paramount Pharmaceuticals
Available Country India, Pakistan
Last Updated: September 19, 2023 at 7:00 am
Prolex
Prolex

Uses

Prolex is used where suppression of acid secretion is of therapeutic benefit. Prolex Is registered in the foltawing indications:

  • Peptic ulcer diseases (PUD)
  • Gastro-esophageal reflux diseases
  • Treatment of ulcer resistant to M2 blocker
  • Treatment of ulcer induced by NSAIDs
  • Gl bleeding from stress or acid peptic diseases
  • Eradication of Helicobacter pylori
  • Zollinger-Ellison syndrome
  • Prophylaxis for acid aspiration syndrome during induction of anesthesia

Prolex is also used to associated treatment for these conditions: Erosive Esophagitis, GERD With Erosive Esophagitis, Gastro-esophageal Reflux Disease (GERD), Healing, Heartburn, Helicobacter Pylori Infection, Stress Ulcers, Zollinger-Ellison Syndrome, Conditions where a reduction of gastric acid secretion is required, Pathological hypersecretory conditions

How Prolex works

Hydrochloric acid (HCl) secretion into the gastric lumen is a process regulated mainly by the H(+)/K(+)-ATPase of the proton pump, expressed in high quantities by the parietal cells of the stomach. ATPase is an enzyme on the parietal cell membrane that facilitates hydrogen and potassium exchange through the cell, which normally results in the extrusion of potassium and formation of HCl (gastric acid).

Proton pump inhibitors such as pantoprazole are substituted benzimidazole derivatives, weak bases, which accumulate in the acidic space of the parietal cell before being converted in the canaliculi (small canal) of the gastric parietal cell, an acidic environment, to active sulfenamide derivatives. This active form then makes disulfide bonds with important cysteines on the gastric acid pump, inhibiting its function. Specifically, pantoprazole binds to the sulfhydryl group of H+, K+-ATPase, which is an enzyme implicated in accelerating the final step in the acid secretion pathway. The enzyme is inactivated, inhibiting gastric acid secretion. The inhibition of gastric acid secretion is stronger with proton pump inhibitors such as pantoprazole and lasts longer than with the H(2) antagonists.

Dosage

Prolex dosage

Tablet:

The usual recommended adult oral dose is 40 mg given once daily, preferably in the morning with or without food. The duration of therapy is ranging from 2-8 weeks.

  • Duodenal ulcers: Prolex 40 mg tablet once daily for 2-4 weeks.
  • Gastric ulcer: Prolex 40 mg tablet once daily for 4-8 weeks.
  • Reflux esophagitis: Prolex 40 mg tabletonce daily for 4-8 weeks.
  • Ulcers induced by NSAIDs: Prolex 40 mg tablet once daily.
  • Maintenance therapy: Maintenance therapy should involve the lowest effective dose of the drug. Prolex both 20 mg & 40 mg doses are safe and effective in maintaining patients with healed reflux esophagitis and PUD in remission.

IV Injection:

  • Duodenal ulcer and gastric ulcer:40 mg once daily for 7-10 days
  • Gastroesophageal reflux disease associatedwith a history of erosive esophagitis:40 mg once daily for 7-10 days
  • Prevention of rebleeding in peptic ulcer:IV 80 mg, followed by 8 mg/hour infusion for 72 hours
  • Prophylaxis of acid aspiration:80 mg IV every 12 h for 24 h, followed by 40mg every 12 h
  • Long-term management of Zollinger-Ellison Syndrome and other pathological hypersecretory conditions: 80 mg IV every 12 hours, may increase to 80 mg every 8 hoursif needed, may titrate to higher doses depending on acid output.

DIRECTION FOR USE OF IV INJECTION: Prolex lyophilized powder and 0.9% Sodium Chloride Injection is for intravenous administration only and must not be given by any other route. Prolex IV injection should be given as a slow intravenous injection. The solution for IV injection is obtained by adding 10 ml 0.9% Sodium Chloride Injection to the vial containing powder. After reconstitution the injection should be given slowly over a period of at least 2 to 5 minutes. Use only freshly prepared solution. The reconstituted solution may be stored at room temperature (up to 30° C) for a maximum 4 hours.

DIRECTION FOR USE OF IV INFUSION: Prolex IV infusion should be given as an intravenous infusion over a period of approximately 15 minutes. Prolex IV infusion should be reconstituted with 10 ml of 0.9% Sodium Chloride Injection and further diluted (admixed) with 0.9% Sodium Chloride Injection or 5% Dextrose or Lactated Ringer's Injection to a final volume of 100 ml. The reconstituted solution may be stored at room temperature (up to 30° C) for a maximum 4 hours prior to further dilution. The admixed solution may be stored at room temperature (up to 30° C) and must be used within 24 hours from the time of initial reconstitution.

Side Effects

No potentially life-threatening effects have been reported with Prolex. Symptomatic adverse effects include headache and diarrhoea are two common reported adverse effects. Peripheral edema has been occasionally reported in female patients. Other side effects may include abdominal pain, dizziness, nausea, epigastric discomfort, flatulence, skin rash, pruritus etc.

Toxicity

Rat Oral LD 50 747 mg/kg

Tumorigenicity

Because of the chronic nature of GERD, there may be a potential for long-term administration of pantoprazole. In long-term rodent studies, pantoprazole was carcinogenic and its administration lead to rare types of gastrointestinal tumors. The relevance of these findings to tumor development in humans is unknown at this time.

Teratogenic Effects

This drug falls under pregnancy category B category. Reproduction studies have been performed in rats at oral doses up to 88 times the recommended human dose (RHD), as well as in rabbits at oral doses up to 16 times the RHD, and have shown no evidence of impaired fertility or harm to the fetus caused by pantoprazole. No adequate and well-controlled studies in pregnant women have been completed. Because animal reproduction studies are not always predictive of human response, this drug should only be used during pregnancy if clearly required.

Nursing Mothers

Prolex and its metabolites have been found to be excreted in the milk of rats. Prolex excretion in human milk has been found in a study performed with a single nursing mother after one 40 mg oral dose. The clinical relevance of this finding is not known, however, it is advisable to take note of this finding when considering pantoprazole use during nursing. Many drugs excreted in human breastmilk have a risk for serious adverse effects in nursing infants.

Precaution

Patients should be cautioned that Prolex tablet should not be split, crushed or chewed. The tablet should be swallowed whole, with or without food in the stomach. Concomitant administration of antacid does not affect the absorption of Prolex.

Interaction

There is no interaction with concomitantly administered antacids. No dosage adjustment is needed with combination use of the following drugs: Theophylline, Caffeine, Diazepam, Digoxin, Ethanol, Metoprolol, Nifedipine or Warfarin.

Food Interaction

  • Take with or without food. The absorption is unaffected by food.

Volume of Distribution

The apparent volume of distribution of pantoprazole is approximately 11.0-23.6 L, distributing mainly in the extracellular fluid.

Elimination Route

Prolex is absorbed after oral administration as an enteric-coated tablet with maximum plasma concentrations attained within 2 – 3 hours and a bioavailability of 77% that does not change with multiple dosing . Following an oral dose of 40mg, the Cmax is approximately 2.5 μg/mL with a tmax of 2 to 3 hours. The AUC is approximately 5 μg.h/mL. There is no food effect on AUC (bioavailability) and Cmax.

Delayed-release tablets are prepared as enteric-coated tablets so that absorption of pantoprazole begins only after the tablet leaves the stomach.

Half Life

About 1 hour

Clearance

Adults: With intravenous administration of pantoprazole to extensive metabolizers, total clearance is 7.6-14.0 L/h. In a population pharmacokinetic analysis, the total clearance increased with increasing body weight in a non-linear fashion.

Children: clearance values in the children 1 to 5 years old with endoscopically proven GERD had a median value of 2.4 L/h.

Elimination Route

After a single oral or intravenous (IV) dose of 14C-labeled pantoprazole to healthy, normal metabolizing subjects, about 71% of the dose was excreted in the urine, with 18% excreted in the feces by biliary excretion. There was no kidney excretion of unchanged pantoprazole.

Pregnancy & Breastfeeding use

There are no adequate or well-controlled studies in pregnant women. Prolex should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

It is not known whether Prolex is excreted in human breast milk. Prolex should be used during lactation only if the potential benefit justifies the potential risk.

Contraindication

It is contraindicated in patients with known hypersensitivity to Prolex.

Acute Overdose

There are no known symptoms of overdosage in humans. Since Prolex is highly protein bound, it is not readily dialyzable. Apart from symptomatic and supportive management, no specific therapy is recommended.

Storage Condition

Store in a cool, dry place and away from light. Keep out of the reach of children.

Innovators Monograph

You find simplified version here Prolex

Prolex contains Pantoprazole see full prescribing information from innovator Prolex Monograph, Prolex MSDS, Prolex FDA label

FAQ

What is Prolex used for?

Prolex is used to treat damage from gastroesophageal reflux disease (GERD), a condition in which backward flow of acid from the stomach causes heartburn and possible injury of the esophagus (the tube between the throat and stomach) in adults and children 5 years of age and older.

How does Prolex work?

Prolex is a type of medicine called a proton pump inhibitor (PPI). Proton pumps are tiny substances in the lining of the stomach that help it make acid to digest your food. Prolex prevents proton pumps from working properly. This reduces the amount of acid the stomach makes.

When will I feel better after taking Prolex?

You should start to feel better within 2 to 3 days. It may take up to 4 weeks for Prolex to work properly so you may still have some symptoms during this time. If you bought Prolex without a prescription, and feel no better after 2 weeks, tell your doctor. They may want to do tests or change you to a different medicine.

Is it safe to take Prolex for a long time?

If you take Prolex for more than 3 months, the levels of magnesium in your blood may fall. This can make you feel tired, confused and dizzy and cause muscle twitches, shakiness and an irregular heartbeat. If you get any of these symptoms, tell your doctor.

Taking Prolex for more than a year may increase your chances of certain side effects, including:

  • bone fractures
  • gut infections
  • vitamin B12 deficiency - symptoms include feeling very tired, a sore and red tongue, mouth ulcers, and pins and needles

If you take Prolex for longer than 1 year your doctor will regularly check your health to see if you should carry on taking it.

What are the side effects of taking Prolex?

Taking Prolex long-term may cause you to develop stomach growths called fundic gland polyps. Talk with your doctor about this risk.

Common side effects of Prolex include

  • injection site reactions (redness, pain, swelling),
  • headache,
  • nausea,
  • vomiting,
  • abdominal or stomach pain,
  • diarrhea,
  • gas,
  • dizziness,
  • joint pain,
  • weight changes,
  • drowsiness,
  • tired feeling, or
  • sleep problems (insomnia).

Does Prolex work immediately?

Prolex takes approximately two and a half hours to begin working, so it won't be effective for current symptoms. However, patients who need immediate relief from their acid reflux symptoms can combine pantoprazole with fast-acting Tums or Maalox to reduce the amount of acid.

Is drinking water good for acid reflux?

Frequently consuming water can make the digestion process better and curb GERD symptoms.

How safe is Prolex?

PPI have minimal side effects and few slight drug interactions and are considered safe for long term treatment. Prolex is significantly effective both for acute and long-term treatment with excellent control of relapse and symptoms. It is well tolerated even for long-term therapy and its tolerability is optimal.

Does Prolex work better than omeprazole?

Generally, pantoprazole and omeprazole are equally effective. Studies comparing pantoprazole and omeprazole have found pantoprazole as effective as omeprazole in treating GERD as well as treating stomach ulcers.

How long does it take for Prolex to leave the body?

Prolex is extensively metabolized in the liver through the cytochrome P-450 system, predominantly by CYP2C19 demethylation with subsequent sulfation and has a serum elimination half-life of about 1.1 hours.

What are the side effects of stopping Prolex?

Most patients have difficulty discontinuing their PPI's because the amount of acid in their digestive system surges when they stop taking the drug, and they're often left with symptoms like excruciating stomach pain and increased heartburn.

How long after taking Prolex can I eat?

Prolex oral granules should be taken 30 minutes before a meal.

How long does it take for stomach acid to return to normal?

For most people acid levels return to normal within one to two weeks.

Is Prolex safe in pregnancy?

Usually, Prolex is safe to take during pregnancy.

Is Prolex safe during breastfeeding?

Usually, Prolex is safe to take during breastfeeding.

Are there other medicines like Prolex?

There are 4 other medicines that are similar to Pantoprazole. They are:

  • lansoprazole
  • esomeprazole
  • omeprazole
  • rabeprazole

Can I take Prolex with an antacid?

You can take Prolex with an antacid (for example, Gaviscon) if you need to, but leave a gap of 2 hours between them.

Will Prolex affect my fertility?

There's no clear evidence to suggest that taking Prolex will reduce fertility in either men or women. But speak to a pharmacist or your doctor if you're trying to get pregnant. They may want to review your treatment.

Will Prolex affect my contraception?

Prolex does not affect any type of regular contraception, including the combined pill. But if Prolex makes you sick (vomit), your contraceptive pills may not protect you from pregnancy. If this happens, follow the instructions in the leaflet that comes with your contraceptive pills.

*** Taking medicines without doctor's advice can cause long-term problems.
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