pantoprazole

Absorption: Tablet is enteric-coated; absorption occurs only after tablet leaves the stomach.

Distribution: Unknown.

Protein Binding: 98%.

Metabolism/Excretion: Primarily metabolized by the CYP2C19 and CYP3A4 isoenzymes in the liver; the CYP2C19 isoenzyme exhibits genetic polymorphism (15–20% of Asian patients and 3–5% of Caucasian and Black patients may be poor metabolizers and may have significantly ↑ pantoprazole concentrations and an ↑ risk of adverse effects); inactive metabolites are excreted in urine (71%) and feces (18%).

Half-Life: 1 hr.

Time/Action Profile ⬆ ⬇

(effect on acid secretion)

ROUTE	ONSET‡	PEAK	DURATION‡
PO	2.5 hr	unknown	1 wk
IV	15–30 min	2 hr	unknown

‡Onset = 51% inhibition; duration = return to normal following discontinuation.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to pantoprazole or related drugs (benzimidazoles).

Use Cautiously in:

Patients using high doses for >1 yr (↑ risk of hip, wrist, or spine fractures and fundic gland polyps);
Patients using therapy for >3 yr (↑ risk of vitamin B₁₂ deficiency);
Pre-existing risk of hypocalcemia;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children;
Geri: Appears on Beers list. risk of Clostridioides difficile infection, pneumonia, GI malignancies, bone loss, and fractures in older adults. Avoid scheduled use for >8 wk in older adults unless for high-risk patients (e.g. oral corticosteroid or chronic NSAID use) or patients with erosive esophagitis, Barrett's esophagitis, pathological hypersecretory condition, or demonstrated need for maintenance therapy (e.g. failure of H2 antagonist).

Adv. Reactions/Side Effects ⬆ ⬇

Derm: ACUTE GENERALIZED EXANTHEMATOUS PUSTULOSIS, cutaneous lupus erythematosus, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS

Endo: hyperglycemia

F and E: hypocalcemia (especially if treatment duration ≥3 mo), hypokalemia (especially if treatment duration ≥3 mo), hypomagnesemia (especially if treatment duration ≥3 mo)

GI: abdominal pain, CLOSTRIDIOIDES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), diarrhea, eructation, flatulence, fundic gland polyps

GU: acute tubulointerstitial nephritis

Hemat: vitamin B₁₂ deficiency

MS: bone fracture

Neuro: headache

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS, ANGIOEDEMA, OR TUBULOINTERSTITIAL NEPHRITIS), systemic lupus erythematosis

Interactions ⬆ ⬇

Drug-drug:

May ↓ levels of atazanavir and nelfinavir; avoid concurrent use with either of these antiretrovirals.
May ↓ absorption of drugs requiring acid pH, including ketoconazole, itraconazole, ampicillin esters, iron salts, erlotinib, and mycophenolate mofetil; concomitant use with atazanavir not recommended.
May ↑ risk of bleeding with warfarin (monitor INR/PT).
Hypomagnesemia and hypokalemia ↑ risk of digoxin toxicity.
May ↑ methotrexate levels.

Route/Dosage ⬆ ⬇

Gastroesophageal Reflux Disease

PO (Adults ): Short-term treatment of erosive esophagitis associated with GERD: 40 mg once daily for up to 8 wk; Maintenance of healing of erosive esophagitis: 40 mg once daily.
PO (Children ≥5 yr): 15–39 kg: 20 mg once daily for up to 8 wk; ≥40 kg: 40 mg once daily for up to 8 wk.
IV (Adults ): 40 mg once daily for 7–10 days.

Gastric Hypersecretory Conditions

PO (Adults ): 40 mg twice daily, up to 120 mg twice daily.
IV (Adults ): 80 mg every 12 hr (up to 240 mg/day).

Availability ⬆ ⬇

(Generic available)

Delayed-release tablets: 20 mg; 40 mg
Delayed-release oral suspension: 40 mg/packet
Powder for injection: 40 mg/vial

Assessment ⬆ ⬇

Assess patient routinely for epigastric or abdominal pain and for frank or occult blood in stool, emesis, or gastric aspirate.

Lab Test Considerations:

May cause abnormal liver function tests, including ↑ AST, ALT, alkaline phosphatase, and bilirubin.
- May cause hypomagnesemia. Monitor serum magnesium prior to and periodically during therapy.

Implementation ⬆ ⬇

Do not confuse Protonix with Lotronex or protamine.
Patients receiving pantoprazole IV should be converted to PO dosing as soon as possible.
Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of CDAD. May begin up to several wk following cessation of therapy.
PO: DNC: May be administered with or without food. Do not break, crush, or chew tablets.
- Oral suspension: Sprinkle granules on 1 tsp of applesauce or apple juice approximately 30 min prior to a meal. Do not crush or chew granules. Take sips of water to make sure granules are washed down into the stomach. Granules may also be emptied into a small cup or teaspoon containing one teaspoon of apple juice. Stir for 5 sec (granules will not dissolve) and swallow immediately. To make sure that entire dose is taken, rinse container once or twice with apple juice to remove any remaining granules. Swallow immediately. Do not use with anything other that applesauce or apple juice. For patients who have a nasogastric tube or gastrostomy tube in place, remove plunger from the barrel of a 60 mL catheter-tip syringe. Discard plunger. Connect catheter tip of syringe to a 16 French (or larger) tube. Hold syringe attached to tubing as high as possible while giving pantoprazole. Empty contents of packet into the barrel of the syringe. Add 10 mL (2 tsp) of apple juice and gently tap and/or shake the barrel of the syringe to help rinse the syringe and tube. Repeat at least twice more using the same amount of apple juice (10 mL or 2 tsp) each time. No granules should remain in the syringe.
- Antacids may be used concurrently.

IV Administration:

IV: Reconstitution: Reconstitute each vial with 10 mL of 0.9% NaCl. Reconstituted solution is stable for 6 hr at room temperature.
Diluent: Administer undiluted.Concentration: 4 mg/mL.
Rate: Administer over at least 2 min.
Intermittent Infusion: Diluent: Dilute further with D5W, 0.9% NaCl, or LR.Concentration: 0.4–0.8 mg/mL. Diluted solution is stable for 24 hr at room temperature.
Rate: Administer over 15 min at a rate of <3 mg/min.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed for the full course of therapy, even if feeling better. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
Advise patient to avoid alcohol, products containing aspirin or NSAIDs, and foods that may cause an increase in GI irritation.
Advise patient to report onset of black, tarry stools; diarrhea; or abdominal pain to health care professional promptly. Instruct patient to notify health care professional immediately if rash, diarrhea, abdominal cramping, fever, or bloody stools occur and not to treat with antidiarrheals without consulting health care professional.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇