Pantoprazole Sodium

Trade Names:
Protonix
- Tablets, delayed-release 20 mg
- Tablets, delayed-release 40 mg
- Granules for oral suspension, delayed-release 40 mg

Trade Names:
Protonix IV
- Injection, lyophilized powder for solution 40 mg

Pharmacology

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Suppresses gastric acid secretion by blocking acid (proton) pump within gastric parietal cells.

Pharmacokinetics

Absorption

C _max is 2.5 mcg/mL (oral) and 5.52 mcg/mL (IV); bioavailability is approximately 77% (oral). T _max is 2.5 h (oral). Oral administration with food may delay absorption up to 2 h or longer.

Distribution

Pantoprazole distributes mainly in extracellular fluid. Vd is 11 to 23.6 L. Protein binding is approximately 98%, mainly to albumin.

Metabolism

Extensively metabolized in the liver through CYP-450. The main metabolic pathway is demethylation by CYP2C19 and oxidation by CYP3A4. No evidence of metabolites with pharmacologic activity. CYP2C19 displays genetic polymorphism because of deficiency in some populations (3% of white and black patients and 17% to 23% of Asian patients); these patients are known to be slow metabolizers of pantoprazole.

Elimination

Urine (71%), feces (18%); no renal excretion of unchanged drug. The t _½ is 1 h, and 3.5 to 10 h in slow metabolizers. Total Cl is 7.6 to 14 L/h.

Duration

More than 24 h.

Special Populations

No adjustment in dosage is needed.

Increase in serum elimination half-life to 7 to 9 h; AUC increases by 5- to 7-fold. No dosage adjustment is necessary.

Moderate increase in AUC (43%) and C _max (26%) after oral administration. No dosage adjustment is recommended.

A modest increase in AUC and C _max in women. No dosage adjustment is recommended.

Indications and Usage

Short-term (up to 8 wk) treatment in the healing and symptomatic relief of erosive esophagitis associated with gastroesophageal reflux disease (GERD); long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome; maintenance of healing of erosive esophagitis associated with GERD.

Short-term (7- to 10-day) treatment of GERD associated with a history of erosive esophagitis, as an alternative to oral therapy in patients unable to continue oral pantoprazole; hypersecretory conditions associated with Zollinger-Ellison syndrome or other neoplastic conditions.

Unlabeled Uses

Laryngitis (oral only).

Contraindications

Standard considerations.

Dosage and Administration

PO 40 mg/day.

PO Recommended starting dosage is 40 mg twice daily, adjusting the dose to the patient's needs and continuing therapy as long as clinically indicated. Dosages up to 240 mg/day have been used. IV 80 mg every 12 h; based upon individual patient needs, the dosage may be increased to 80 mg every 8 h. Daily dosages of more than 240 mg or administered for more than 6 days have not been studied.

PO 40 mg/day for up to 8 wk; an additional 8-wk course of treatment may be considered in patients who have not healed after 8 wk. IV 40 mg/day for 7 to 10 days.

General Advice

• Delayed-release oral suspension
• To administer in apple juice, empty contents of 1 packet of granules into a small cup containing 5 mL of apple juice. Stir for 5 sec and swallow immediately. To ensure complete delivery of the dose, rinse the container once or twice with apple juice to remove any remaining granules and have patient swallow immediately.
• For patients who have a nasogastric (NG) tube, separate the plunger from the barrel of a 2 oz (60 mL) catheter tip syringe. Connect the catheter tip of the syringe to a 16 French (or larger) NG tube. Hold the syringe attached to the tubing as high as possible during application to prevent any bending of the tubing and to provide smooth flow of the contents under gravity. Empty the contents of the packet into the barrel of the syringe. Add 10 mL of apple juice and gently tap and/or shake the barrel of the syringe to help rinse the syringe and NG tube. Repeat with at least 2 additional 10 mL aliquots of apple juice. No granules should remain in the syringe. Make sure NG tube is not clogged to ensure the patient receives the full dose.
• To administer in applesauce, open 1 packet and sprinkle intact granules on 1 teaspoonful of applesauce. Swallow within 10 min of preparation.
• Administer approximately 30 min prior to a meal.
• Administer only in apple juice or applesauce, not in water or other liquids or food.

• Delayed-release tablets
• May be used concomitantly with antacids.
• Administer without regard to meals but administer with food if GI upset occurs.
• Instruct patient to swallow tablet whole and not to split, chew, or crush the tablet.

• Injection
• For IV administration only. Not for intradermal, subcutaneous, IM, or intra-arterial administration.
• Discontinue IV as soon as oral therapy is feasible.
• Infuse prescribed dose through a dedicated line or Y-site over a period of 2 or 15 min as ordered. Flush IV line before and after administration of pantoprazole with dextrose 5% injection, sodium chloride 0.9% injection, or Ringer's lactate injection.
• For 2-min infusion of 40 mg dose, reconstitute 1 vial of powder for injection with 10 mL of sodium chloride 0.9% injection to produce a solution with a final concentration of 4 mg/mL. Infuse total volume over a period of 2 min.
• For 2-min infusion of 80 mg dose, reconstitute each of 2 vials of powder for injection with 10 mL of sodium chloride 0.9% injection to produce a solution with a final concentration of 4 mg/mL. Infuse total volume from both vials IV over a period of 2 min.
• For 15-min infusion of 40 mg dose, reconstitute 1 vial with 10 mL of sodium chloride 0.9% injection. Further dilute (admix) with 100 mL of dextrose 5% injection, sodium chloride 0.9% injection, or Ringer's lactate injection to a total volume of 110 mL, producing a solution with a final concentration of approximately 0.4 mg/mL. Administer at a rate of 7 mL/min over 15 min.
• For 15-min infusion of 80 mg dose, reconstitute each of 2 vials with 10 mL of sodium chloride 0.9% injection. Combine contents of 2 vials and further dilute (admix) with 80 mL of dextrose 5% injection, sodium chloride 0.9% injection, or Ringer's lactate injection to a total volume of 100 mL, producing a solution with a final concentration of approximately 0.8 mg/mL. Administer at a rate of 7 mL/min over 15 min.
• Do not administer if particulate matter, cloudiness, or discoloration is noted.
• Discard any unused reconstituted or admixed solution. Do not save for future use.

Storage/Stability

Store tablets and granules for oral suspension at 68° to 77°F. Store injection at 59° to 86°F. Protect powder for injection from light. Reconstituted solution may be stored for up to 6 h at room temperature prior to further dilution. Admixed solution may be stored for up to 24 h at room temperature prior to IV infusion.

Drug Interactions

Plasma concentrations may be reduced by pantoprazole. Coadministration with atazanavir is not recommended.

Plasma levels of certain azole antifungals may be reduced. Avoid this combination if possible.

Proton pump inhibitors may increase serum digoxin levels.

Absorption of these drugs may be affected.

May reduce pantoprazole plasma concentrations. Avoid combination if possible.

Incompatible with IV pantoprazole.

Enteric-coated salicylates may dissolve more rapidly, increasing gastric adverse reactions.

Increased INR and PT have been reported. Monitor INR and PT.

Laboratory Test Interactions

False-positive urine screening for tetrahydrocannabinol (THC).

Adverse Reactions

CNS

Headache (9%); anxiety, asthenia, dizziness, hypertonia, migraine (1% or more); insomnia (1%); anterior ischemic optic neuropathy, confusion, hypokinesia, speech disorder, tinnitus, vertigo (postmarketing).

Dermatologic

Rash (2%); severe dermatologic reactions (eg, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis) (postmarketing).

EENT

Pharyngitis, rhinitis (more than 1%); blurred vision (postmarketing).

GI

Diarrhea (6%); abdominal pain, flatulence (4%); nausea, vomiting (2%); constipation, dyspepsia, gastroenteritis, GI disorder, rectal disorder (1% or more); eructation (1%); increased salivation, pancreatitis (postmarketing).

Genitourinary

Urinary frequency, UTI (at least 1%); creatinine increased; interstitial nephritis (postmarketing).

Hematologic-Lymphatic

Pancytopenia (postmarketing).

Hepatic

Abnormal LFTs (2%); increased ALT (1% or more); hepatocellular damage leading to jaundice and hepatic failure (postmarketing).

Lab Tests

Elevated CPK (postmarketing).

Local

Injection-site reactions (including abscess, thrombophlebitis) (more than 1%).

Metabolic-Nutritional

Hyperlipidemia (at least 1%); hyperglycemia (1%); hypercholesterolemia, hyperuricemia.

Musculoskeletal

Arthralgia, back pain, neck pain (at least 1%); rhabdomyolysis (postmarketing).

Respiratory

Bronchitis, cough increased, dyspnea, sinusitis, upper respiratory tract infection (at least 1%).

Miscellaneous

Chest pain, flu syndrome, infection, pain (1% or more); anaphylaxis, angioedema (postmarketing).

Precautions

Pregnancy

Category B .

Lactation

Excreted.

Children

Safety and efficacy not established.

Hypersensitivity

Anaphylaxis has been reported with the use of IV pantoprazole.

Atrophic gastritis

May occur, particularly in patients who were once Helicobacter pylori positive.

Cyanocobalamin deficiency

May occur.

Gastric malignancy

Symptomatic response to therapy does not preclude the presence of gastric malignancy.

Prolonged use

In long-term rodent studies, pantoprazole was carcinogenic and caused rare types of GI tumors. The relevance of these findings to tumor development in humans is unknown.

Zinc deficiency

IV product contains edetate disodium. Consider zinc supplements in patients who are prone to zinc deficiency.

Overdosage

Symptoms

No adverse reactions were reported with pantoprazole 400 to 600 mg.

Patient Information

• Advise patient or caregiver that injection will be prepared and administered by a health care provider and is used temporarily when oral therapy is not feasible.
• Instruct patient to take tablets without regard to meals but to take with food if stomach upset occurs. Instruct patients to take oral suspension with applesauce or apple juice only, approximately 30 minutes before a meal.
• Instruct patient not to split, crush, or chew the tablet or granules for oral suspension.
• Remind patient that pantoprazole is to be taken every day and not as needed or only when symptoms are present.
• Remind patient that antacids may be taken concurrently with pantoprazole.
• Instruct patient to report any of the following to health care provider: bloody or coffee ground–like vomit; black, tarry stools; bothersome side effects (eg, constipation, gas, headache); increasing need for antacid use; recurrent heartburn; or recurrent indigestion or abdominal pain.

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