Pantoprazole


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Gastro-oesophageal reflux disease 20-40 mg once daily for 4 weeks (increased to 8 weeks if necessary). Maintenance: 20-40 mg daily. Peptic ulcer 40 mg for 2-4 weeks for duodenal ulcer or 4-8 weeks for benign gastric ulcer. Prophylaxis of NSAID-induced ulcers 20 mg once daily. Zollinger-Ellison syndrome 40 mg bid (adjusted up to 240 mg/day if needed). Daily doses >80 mg should be given in 2 divided doses. IV Gastro-oesophageal reflux disease, Peptic ulcer 40 mg daily until PO can be resumed. Zollinger-Ellison syndrome 80 mg once or twice daily until PO can be resumed.
Dosage Details
Intravenous
Zollinger-Ellison syndrome
Adult: 80 mg once or twice daily as slow injection or short-term infusion over 2-15 minutes. Switch to oral therapy as soon as possible.

Intravenous
Gastro-oesophageal reflux disease, Peptic ulcer
Adult: 40 mg daily as slow injection or short-term infusion over 2-15 minutes. Switch to oral therapy as soon as possible.

Oral
Peptic ulcer
Adult: 40 mg once daily (increased up to 80 mg if necessary) for 2-4 weeks for duodenal ulcer or 4-8 weeks for benign gastric ulcer.

Oral
Gastro-oesophageal reflux disease
Adult: 20-40 mg once daily for 4 weeks (increased to 8 weeks if necessary). Maintenance: 20-40 mg daily. Alternatively, 20 mg daily on recurring symptoms.
Child: ≥5 years 15–40 kg: 20 mg once daily for up to 8 weeks; >40 kg: 40 mg once daily for up to 8 weeks.

Oral
Prophylaxis of NSAID-induced ulcers
Adult: 20 mg once daily.

Oral
Zollinger-Ellison syndrome
Adult: 40 mg bid (adjusted up to 240 mg/day if needed). Daily doses >80 mg should be given in 2 divided doses.
Special Patient Group
Pharmacogenomics:

CYP2C19 is one of the major enzymes in the metabolism of pantoprazole and it is known to exhibit genetic polymorphism due to its deficiency in some subpopulations.

CYP2C19 phenotypes are classified as ultrarapid metabolisers (carriers of 2 function alleles e.g. *17/*17), extensive metabolisers (e.g. CYP2C19 *1/*1), intermediate metabolisers (carriers of 1 non-function allele e.g. *1/*2, *1/*3, *17/*2, *17/*3), and poor metabolisers (carriers of 2 non-function alleles e.g. *2/*2, *2/*3, *3/*3).

Certain subpopulations lack CYP2C19 activity, these subpopulations are referred to as poor metabolisers. Approximately 3% of Caucasians and African-Americans, and 17-23% of Asians are poor metabolisers. Although these subpopulations have elimination half-life values of 3.5 to 10 hours in adults, they still have minimal accumulation with once-daily dosing. No dosage adjustment is needed in adult patients who are CYP2C19 poor metabolisers. Paediatric patients who are poor metaboliser exhibited greater than a 6-fold increase in AUC compared to extensive and intermediate metabolisers. Poor metabolisers exhibited approximately 10-fold lower apparent oral clearance compared to extensive metabolisers. Dose reduction should be considered in paediatric poor metaboliser patients.
Hepatic Impairment
Max: 20 mg daily.
Administration
Normal Release: May be taken with or without food.
Controlled-Release: Should be taken on an empty stomach. Take 1 hr before meals. Swallow whole, do not chew/crush.
Reconstitution
Reconstitute 40 mg vial with 10 mL 0.9% NaCl inj to make a final concentration of approx 4 mg/mL. IV Infusion: Further dilute with 100 mL of D5W, normal saline, or Lactated Ringer’s inj to achieve a concentration of approx. 0.4 mg/mL. For an 80 mg dose: Reconstitute two 40 mg vials and dilute 10mL of the reconstituted solution in 100 mL of IV infusion solutions.
Contraindications
Concomitant use with rilpivirine and atazanavir.
Special Precautions
Patient with gastric malignancy, risk factors for reduced vitamin B12 absorption or at risk for osteoporosis. Hepatic impairment. Pregnancy and lactation. CYP2C19 poor metabolisers.
Adverse Reactions
Significant: Hypomagnesaemia, cutaneous lupus erythematosus, SLE, osteoporosis-related fractures, fundic gland polyp, carcinoma, Clostridium difficile-associated diarrhoea, interstitial nephritis, Vitamin B12 deficiency (long-term therapy), gastrointestinal infection (e.g. salmonella, Campylobacter).
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, constipation, flatulence, abdominal pain, dyspepsia, dry mouth.
General disorders and administration site conditions: Asthenia, fatigue, malaise.
Hepatobiliary disorders: Increased liver enzymes.
Immune system disorders: Urticaria.
Metabolism and nutrition disorders: Peripheral oedema.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia.
Nervous system disorders: Headache, dizziness, vertigo.
Psychiatric disorders: Insomnia.
Reproductive system and breast disorders: Gynaecomastia.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Patient Counseling Information
This drug may cause dizziness or visual disturbances, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor bone loss, fractures, Clostridium difficile-associated diarrhoea (CDAD), serum Mg (at baseline and periodically), serum gastrin level concentrations.
Drug Interactions
May decrease plasma concentrations of rilpivirine and atazanavir. Increased risk of hypomagnesaemia with diuretics. Increased risk of digoxin-induced cardiotoxic effects. May increase INR and prothrombin time of warfarin. May increase plasma concentration of methotrexate. May decrease absorption of itraconazole, ketoconazole, posaconazole, erlotinib. May diminish the therapeutic effect of clopidogrel.
Food Interaction
St John’s wort may decrease serum levels of pantoprazole.
Lab Interference
May increase serum chromogranin A (CgA) levels causing false-positive result in diagnostic tests for neuroendocrine tumours and urine screening tests for tetrahydrocannabinol.
Action
Description: Pantoprazole is a substituted benzimidazole gastric antisecretory agent and is also known as proton pump inhibitor (PPI). It blocks the final step in gastric acid secretion by specific inhibition of H+/K+ adenosine triphosphatase (ATPase) enzyme system present on the secretory surface of the gastric parietal cell. Both basal and stimulated acid are inhibited.
Onset: 2.5 hours (oral); 15-30 minutes (IV).
Duration: 24 hours.
Pharmacokinetics:
Absorption: Rapidly absorbed. Time to peak plasma concentration: Approx 2-2.5 hours (oral). Bioavailability: Approx 77%.
Distribution: Enters breast milk. Volume of distribution: 11-23.6 L. Plasma protein binding: Approx 98% (mainly to albumin).
Metabolism: Extensive hepatic metabolism, mainly by CYP2C19 isoenzyme to desmethylpantoprazole and slightly by CYP3A4, CYP2D6 and CYP2C9 isoenzymes.
Excretion: Mainly via urine (approx 80%); faeces. Elimination half-life: Approx 1 hour.
Chemical Structure

Chemical Structure Image
Pantoprazole

Source: National Center for Biotechnology Information. PubChem Database. Pantoprazole, CID=4679, https://pubchem.ncbi.nlm.nih.gov/compound/Pantoprazole (accessed on Jan. 22, 2020)

Storage
Store between 20-25°C.
ATC Classification
A02BC02 - pantoprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
References
Annotation of DPWG Guideline for Pantoprazole and CYP2C19. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 12/12/2019.

Annotation of FDA Label for Pantoprazole and CYP2C19. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 12/12/2019.

Annotation of Swissmedic Label for Pantoprazole and CYP2C19. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 12/12/2019.

Anon. CYP2C19-Pantoprazole (Pharmacogenomics). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 12/12/2019.

Anon. Pantoprazole. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 01/03/2019.

Anon. Pantoprazole. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/03/2019.

Buckingham R (ed). Pantoprazole. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/03/2019.

Joint Formulary Committee. Pantoprazole. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/03/2019.

Pantoprazole Delayed Release Tablet (Teva Pharmaceuticals USA, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 12/12/2019.

Pantoprazole Sodium Injection, Powder, Lyophilized, for Solution (West-Ward Pharmaceuticals Corp). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/03/2019.

Pantoprazole Sodium Tablet, Delayed Release (Teva Pharmaceuticals USA, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/03/2019.

Disclaimer: This information is independently developed by MIMS based on Pantoprazole from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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