Pantoprazole (Dosing, Interaction, Side Effect, Administration, Etc..)

DRUG CLASS:
Gastric Acid Secretion Inhibitor
Proton Pump Inhibitor

DOSING:
Adult Dose:
Important Note:
Beers Criteria: Use caution or avoid use as potentially inappropriate in older adults.

Drug-induced gastrointestinal disturbance; Prophylaxis - Non-steroidal anti-inflammatory drug adverse reaction:
20 to 40 mg orally once daily for 6 months (off-label dosage)

Duodenal ulcer disease:
40 to 80 mg orally once daily for 4 to 8 weeks (

study dosage

)
40 mg IV once daily over 2 to 15 minutes for 6 days; 20 mg OR 80 mg was used in a few patients (study dosage)

Erosive esophagitis; Maintenance therapy - Gastroesophageal reflux disease:
40 mg orally once daily

Erosive esophagitis – Gastroesophageal reflux disease:
40 mg orally once daily for up to 8 weeks; if not healed; an additional 8-week course may be initiated
40 mg IV infusion once daily for 7 to 10 days

Gastric hypersecretion; Pathological:
Initial; 40 mg orally twice daily; titrate to patient response; doses up to 240 mg daily and over 2 years duration have been administered
80 mg IV infusion every 12 hours; can increase to every 8 hours; doses up to 240 mg/day and up to 6 days duration have been studied.

Gastroesophageal reflux disease:
Mild: 20 mg orally once daily for 8 weeks (study dosage).

Helicobacter pylori gastrointestinal tract infection:
(

Guideline Dosage

):
Clarithromycin triple regimen:
40 to 80 mg orally twice daily in combination with clarithromycin 500 mg orally twice daily and either amoxicillin 1 g orally twice daily or metronidazole 500 mg orally 3 times per day; continue regimen for 14 days

Bismuth quadruple regimen:
40 mg orally twice daily in combination with tetracycline 500 mg orally 4 times per day; metronidazole 250 mg orally 4 times per day or 500 mg orally 3 or 4 times per day; and either bismuth subcitrate 120 to 300 mg orally 4 times per day or bismuth subsalicylate 300 mg orally 4 times per day; continue regimen for 10 to 14 days

Concomitant regimen:
40 mg orally twice daily in combination with amoxicillin 1 g orally twice daily; clarithromycin 500 mg orally twice daily; and metronidazole or tinidazole 500 mg orally twice daily; continue regimen for 10 to 14 days

Sequential regimen:
40 mg orally twice daily plus amoxicillin 1 g orally twice daily for 5 to 7 days; then follow with clarithromycin 500 mg twice daily; metronidazole or tinidazole 500 mg twice daily; and

pantoprazole 40 mg

twice daily for 5 to 7 days

Hybrid regimen:
40 mg orally twice daily plus amoxicillin 1 g orally twice daily for 7 days; then follow with amoxicillin 1 g twice daily; clarithromycin 500 mg twice daily; metronidazole or tinidazole 500 mg twice daily; and

pantoprazole 40 mg twice daily

for 7 days

Levofloxacin triple regimen:
40 mg orally twice daily in combination with amoxicillin 1 g orally twice daily and levofloxacin 500 mg orally once daily; continue regimen for 10 to 14 days

Levofloxacin sequential regimen:
40 to 80 mg orally twice daily plus amoxicillin 1 g orally twice daily for 5 to 7 days; then follow with amoxicillin 1 g orally twice daily; metronidazole or tinidazole 500 mg orally twice daily;

pantoprazole 40 mg orally twice daily

; and levofloxacin 500 mg orally once daily for 5 to 7 days

LOAD regimen:
80 mg orally once daily in combination with levofloxacin 250 mg orally once daily; doxycycline 100 mg orally once daily; and nitazoxanide 500 mg twice daily; continue regimen for 7 to 10 days.

Recurrent gastrointestinal bleeding; Prophylaxis:
80 mg IV bolus followed by 8 mg/hour IV for 72 hours (study dosage).

Zollinger-Ellison syndrome:
80 mg IV infusion every 12 hours; can increase to every 8 hours; doses up to 240 mg/day and up to 6 day duration has been studied
Initial; 40 mg orally twice daily; titrate to patient response; doses up to 240 mg daily and over 2 years duration have been administered.

Pediatric Dose:
Important Note:
Beers Criteria: Use caution or avoid use as potentially inappropriate in older adults.

General Dosage Information:
Safety and efficacy not established in children.

Erosive esophagitis - Gastroesophageal reflux disease:
(5 years and older; 15 to less than 40 kg)
20 mg orally once daily for up to 8 weeks

(5 years and older; 40 kg and greater)
40 mg orally once daily for up to 8 weeks

Gastroesophageal reflux disease:
(5 to 11 years)
Initial; 20 mg (0.6 to 0.9 mg/kg) orally once daily; increase to 40 mg once daily (1.2 mg/kg or greater) if symptoms do not improve (study dosage).







MECHANISM OF ACTION:

Pantoprazole sodium

is a proton pump inhibitor (PPI) that covalently binds to the (H(+); K(+))-ATPase enzyme system at the secretory surface of the gastric parietal cell. This action suppresses the final step in gastric acid production and leads to inhibition of both basal and stimulated acid secretion

INDICATIONS:
FDA-LABELED INDICATIONS:
Erosive esophagitis; Maintenance therapy - Gastroesophageal reflux disease
Erosive esophagitis - Gastroesophageal reflux disease
Gastric hypersecretion; Pathological
Zollinger-Ellison syndrome

NON-FDA LABELED INDICATIONS:
Drug-induced gastrointestinal disturbance; Prophylaxis - Non-steroidal anti-inflammatory drug adverse reaction
Duodenal ulcer disease
Gastroesophageal reflux disease
Helicobacter pylori gastrointestinal tract infection
Recurrent gastrointestinal bleeding; Prophylaxis

ADVERSE EFFECT:
Common:
Gastrointestinal:
Abdominal pain (3%)
Diarrhea (4%)
Flatulence (4%)

Neurologic:
Headache (5%)

Serious:
Dermatologic:
Cutaneous lupus erythematosus.

Gastrointestinal:
Atrophic gastritis
Clostridium difficile diarrhea

Hematologic:
Thrombocytopenia (less than 1%)

Immunologic:
Stevens-Johnson syndrome
Toxic epidermal necrolysis

Musculoskeletal:
Disorder of muscle
Fracture of bone
Osteoporosis-related
Hip fracture
Rhabdomyolysis

Renal:
Interstitial nephritis

CONTRAINDICATION:
Rilpivirine(theoretical)

DRUG INTERACTION:
Antiretrovirals:
The effect of PPIs on antiretroviral drugs is variable. The clinical importance and the mechanisms behind these interactions are not always known.
Decreased exposure of some antiretroviral drugs (e.g., rilpivirine atazanavir, and nelfinavir) when used concomitantly with

pantoprazole

may reduce antiviral effect and promote the development of drug resistance.
Increased exposure of other antiretroviral drugs (e.g., saquinavir) when used concomitantly with pantoprazole may increase toxicity

Warfarin:
Increased INR and prothrombin time in patients receiving PPIs, including

pantoprazole sodium

, and warfarin concomitantly. Increases in INR and prothrombin time may lead to abnormal bleeding and even death.

Methotrexate:
Concomitant

use of pantoprazole sodium

with methotrexate (primarily at high dose) may elevate and prolong serum concentrations of methotrexate and/or its metabolite hydroxymethotrexate, possibly leading to methotrexate toxicities. No formal drug interaction studies of high-dose methotrexate with PPIs have been conducted.

Drugs Dependent on Gastric pH for Absorption (e.g., iron salts, erlotinib, dasatinib, nilotinib, mycophenolate mofetil, ketoconazole)

Pantoprazole sodium

can reduce the absorption of other drugs due to its effect on reducing intragastric acidity

False Positive Urine Tests for THC:
There have been reports of false positive urine screening tests for tetrahydrocannabinol (THC) in patients receiving PPIs, including pantoprazole.

Major:
Acalabrutinib (probable)
Atazanavir (theoretical)
Bosutinib (theoretical)
Capecitabine (probable)
Cilostazol (theoretical)
Citalopram (theoretical)
Dasatinib (theoretical)
Erlotinib (probable)
Eslicarbazepine Acetate (theoretical)
Gefitinib (theoretical)
Ketoconazole (theoretical)
Ledipasvir (theoretical)
Methotrexate (probable)
Mycophenolate Mofetil (probable)
Nelfinavir (probable)
Neratinib (probable)
Nilotinib (theoretical)
Pazopanib (established)
Saquinavir (theoretical)
Secretin Human (theoretical)
Sunitinib (probable)
Velpatasvir (theoretical)
Vismodegib (theoretical)

Moderate:
Levothyroxin(Probable)
Warfarin(Probable)

PHARMACOKINETICS:
Absorption:
ORAL;

DELAYED RELEASE TABLETS

:
Bioavailability: Approximately 77%

Effect of food:
Food may delay its absorption up to 2 hours or longer
With high fat meal: Cmax and AUC decreased by 51% and 29%

Time for Maximum Plasma Concentration (Tmax):
2.5 hr
1.5 to 2 hours (Pediatrics)
ORAL; FOR-DELAYED-RELEASE SUSPENSION:
Effect of food: Administer 30 minutes before a meal
Time for Maximum Plasma Concentration (Tmax): 2 to 2.5 hours

Distribution:
Plasma Protein binding: about 98% to primarily albumin

Volume of Distribution (Vd):
Extensive metabolizers (IV): approximately 11 L to 23.6 L
Pediatrics (oral): 0.21 to 0.43 L/kg

Metabolism:
Hepatic:
Cytochrome P450 CYP2C19
Minor metabolism from CYP3A4; 2D6; and 2C9

Excretion:
Fecal: (oral or IV; normal metabolizers); 18%
Renal: (oral or IV; normal metabolizers); approximately 71%; none as unchanged
Dialyzable: no (hemodialysis)

Total body clearance:
IV: 7.6 to 14 L/hour
Oral; Pediatrics: 0.18 to 2.08 L/hr/kg

Elimination:
Oral or IV: 1 hour
Oral or IV: Slow metabolizers; 3.5 to 10 hours
Pediatrics: 0.7 to 5.34 hours

PRECAUTION:
Beers Criteria:
Avoid scheduled

use of proton pump inhibitors

for longer than 8 weeks in older adults; due to risk of Clostridium difficile infection and bone loss and fractures; unless needed for high-risk patients (e.g.; oral corticosteroids; chronic NSAID use); erosive esophagitis; Barrett esophagitis; pathological hypersecretory condition; or need for maintenance treatment (e.g.; due to failure of drug discontinuation or histamine-2 blockers).

Dermatologic:
New or worsening cutaneous lupus erythematosus has been reported within weeks to years after continuous drug therapy; avoid using for longer than medically indicated and discontinue use if suspected.

Endocrine and metabolic:
Hypomagnesemia has been reported in patients treated with proton pump inhibitors for at least 3 months; tetany; arrhythmias; and seizures may occur; monitoring recommended with

prolonged use

or concomitant drugs that may cause hypomagnesemia; discontinuation may be required.

Predisposition to zinc deficiency; consider zinc supplementation when treated with IV pantoprazole; use caution with coadministration of other IV EDTA-containing products.

Vitamin B12 deficiency may occur with prolonged use (eg greater than 1 to 2 years); monitoring recommended.

Gastrointestinal:
Symptomatic response does not preclude gastric malignancy
Clostridium difficile-associated diarrhea may occur; especially in hospitalized patients;

use lowest dose

and shortest treatment duration.

Hematologic:
Thrombophlebitis has been reported with IV administration.

Hepatic:
Mild; transient transaminase elevations have been reported with IV administration.

Immunologic:
Anaphylaxis and other serious reactions; including erythema multiforme; Stevens-Johnson syndrome; and toxic epidermal necrolysis have been reported with IV administration.

New or worsening systemic lupus erythematosus has been reported within weeks to years of treatment initiation; avoid using for longer than medically indicated and discontinue use if suspected.
Lab interference:
Gastric acid suppression may increase serum chromogranin A (CgA) levels; withhold pantoprazole for 14 days prior to CgA testing neuroendocrine tumor assessment.

Musculoskeletal:

Osteoporosis-related bone fracture of hip; wrist; or spine may occur; especially with higher (multiple daily) doses or longer duration of therapy (1 year or longer); use lowest dose and shortest treatment duration.
Renal: Acute interstitial nephritis; typically associated with idiopathic hypersensitivity; has been reported; discontinuation required Concomitant use: Use with atazanavir or nelfinavir not recommended.

PREGNANCY CATEGORY:
B (FDA)
B3 (AUS)

BREAST FEEDING:
Infant Risk cannot be ruled out

MONITORING:
GERD:
Decreased abdominal and gastroesophageal discomfort may indicate efficacy

Peptic ulcer:
Endoscopic improvement may indicate efficacy
Negative urea breath (UB) test 4 to 6 weeks after completion of therapy

Serum magnesium:
Routine screening is not necessary; consider screening prior to initiation and periodically during prolonged therapy

Serum vitamin B12:
Although no routine screening is needed; may consider screening every 1 to 2 years for deficiency in patients receiving prolonged therapy.

HOW TO TAKE OR ADMINISTRATION:
General Information
Intravenous administration should be discontinued as soon as an oral route is possible
Parenteral routes other than the IV route are not recommended

Intravenous:
Administer through a dedicated line or through a Y-site; flush before and after administration with 5% dextrose injection, 0.9% sodium chloride injection, or Lactated Ringer's injection

Injection is NOT compatible with midazolam and may not be compatible with products containing zinc; compatible solutions include 5% Dextrose Injection, 0.9% Sodium Chloride Injection, or Lactated Ringer's Injection

(15-minute infusion) reconstitute the appropriate number of vials with 10 mL of 0.9% sodium chloride injection and then dilute to a total volume of 100 mL with 5% dextrose injection, 0.9% sodium chloride injection, or lactated Ringer's injection to a final concentration of approximately 0.4 mg/mL for a 40 mg dose and 0.8 mg/mL for an 80 mg dose; administer IV over a period of 15 minutes at a rate of approximately 7 mL/min

(2-minute infusion) reconstitute the appropriate number of vials with 10 mL of 0.9% sodium chloride injection for each vial to a final concentration of approximately 4 mg/mL; administer total volume IV over a period of at least 2 minutes
reconstituted and diluted solutions do not need to be protected from light

Nasogastric:
(Delayed release suspension)
Concomitant administration of antacids does not affect absorption

Remove plunger from the barrel of a 60 mL catheter tip syringe; connect catheter tip syringe to a 16 French (or larger) nasogastric tube; hold the syringe attached to the tubing as high as possible during process to prevent any bending of the tubing; empty granules into the barrel of syringe; add 10 mL of apple juice; gently tap and/or shake the barrel of the syringe; rinse and tap and/or shake again with apple juice; repeat with at least 2 additional 10 mL aliquots of apple juice; no granules should remain in the syringe

Oral:
(Delayed-release tablets)
Take with or without food; concomitant administration of antacids does not affect absorption
Swallow tablets whole, do not split, crush, or chew

(Delayed release suspension)
Sprinkle intact granules on 1 teaspoonful of applesauce or apple juice, swallow within 10 minutes of preparation and 30 minutes prior to a meal; rinse the container 1 or 2 times with apple juice and swallow to remove any remaining granules; do not chew or crush

DOSAGE FORM:
Intravenous Powder for Solution:
40 MG

Oral Tablet; Enteric Coated:
20 MG
40 MG.

TREATMENT:
MANAGEMENT OF MILD TO MODERATE TOXICITY:
Treatment is symptomatic and supportive. Correct any significant fluid and/or electrolyte abnormalities in patients with severe diarrhea and/or vomiting.

MANAGEMENT OF SEVERE TOXICITY:
Treatment is symptomatic and supportive. Significant toxicity is not expected after an overdose.

PATIENT COUNSELING OR CLINICAL TEACHING:
Counsel patient to report symptoms of cutaneous or systemic lupus erythematosus
Advise patient that drug may increase risk for osteoporosis-related fractures of the hip; wrist; or spine with multiple daily doses that are continued for longer than a year
Warn patient to report diarrhea that does not improve; especially with persistent watery stools; fever; and abdominal pain

Oral side effects

may include abdominal pain; nausea; diarrhea; vomiting; flatulence; dizziness; headaches; fever; rash; and arthralgia
Injection

side effects

may include injection site reactions (e.g.; thrombophlebitis; abscess)
Tell patient to immediately report signs/symptoms of hypomagnesemia (e.g.; dizziness; palpitations; tetany; seizures.
Instruct patient using delayed-release oral suspension to mix with 1 teaspoonful of apple juice or applesauce and take at least 30 minutes before a meal
Counsel patient using nasogastric tube to mix delayed-release oral suspension with 2 teaspoonfuls of apple juice in syringe and take at least 30 minutes before a meal




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For the Registered Medical Practitioner Only. We are not recommended for self medication. self medication is may harmful for health. We are only Provide information about medicine.