Pepsin is required for digestion in the stomach

Summary

Pepsin is a protease indicated in the treatment of digestive disorders.

Generic NamePepsinDrugBank Accession NumberDB13198Background

Pepsin is a potent enzyme in gastric juice that digests proteins such as those in meat, eggs, seeds, and dairy products 12.

Studies on gastric digestion from 1820-1840 led to the discovery of pepsin as the substance which, in the presence of stomach acid, causes nutrients including meat or coagulated egg whites to dissolve. Soon afterward, it was shown that these protein nutrients were cleaved by pepsin to products called peptones 2.

Pepsin is often used as a replacement enzyme for those with pancreatic insufficiency 11. Stimulation of the pancreas and therefore enzymatic digestion of food is a tightly controlled and is a hormonally mediated process. Any changes or conditions affecting metabolic steps for successful digestion and absorption negatively affect pancreatic enzymatic secretion, entry into the intestine, functionality once inside the intestine, and appropriate mixing with foods/nutrients. Many causes of pancreatic insufficiency require that enzyme replacement therapy is started, including cystic fibrosis, pancreatic cancer, acute and chronic pancreatitis, as well as pancreatic surgery 11.

Pepsin is approved by the FDA and is used in food at levels not to exceed current good manufacturing practice 17. Interestingly, it has been used as a marker for laryngopharyngeal reflux (LPR), which is a common illness of otolaryngology (ear, nose and throat specialist) visits 3.

Interestingly, recent research has suggested that pepsin participates in the digestion of nucleic acids 22.

TypeBiotechGroupsApproved, Experimental, InvestigationalBiologic ClassificationProtein Based Therapies
Other protein based therapiesProtein Chemical FormulaNot AvailableProtein Average WeightNot AvailableSequences

> Pepsin A Sus Scrofa (Pig)
MKWLLLLSLVVLSECLVKVPLVRKKSLRQNLIKNGKLKDFLKTHKHNPASKYFPEAAALI
GDEPLENYLDTEYFGTIGIGTPAQDFTVIFDTGSSNLWVPSVYCSSLACSDHNQFNPDDS
STFEATSQELSITYGTGSMTGILGYDTVQVGGISDTNQIFGLSETEPGSFLYYAPFDGIL
GLAYPSISASGATPVFDNLWDQGLVSQDLFSVYLSSNDDSGSVVLLGGIDSSYYTGSLNW
VPVSVEGYWQITLDSITMDGETIACSGGCQAIVDTGTSLLTGPTSAIANIQSDIGASENS
DGEMVISCSSIDSLPDIVFTINGVQYPLSPSAYILQDDDSCTSGFEGMDVPTSSGELWIL
GDVFIRQYYTVFDRANNKVGLAPVA

Download FASTA Format

Synonyms
  • Lactated pepsin
  • Pepsin A
  • Pepsin porcine
  • Pepsin, bovine
  • Pepsina
  • Saccharated pepsin
Indication

Used as a pancreatic enzyme replacement in pancreatic insufficiency 11. It is intended to mimic naturally produced human pepsin 14.

Pepsin powder is prepared from the gastric mucosa of pigs, cattle or sheep 19. In the laboratory, it is primarily used for the unspecific hydrolysis of proteins and peptides in acidic media. In addition, it provides limited hydrolysis of native immunoglobulins, yielding biologically active fragments 7.

In certain supplements, pepsin may be combined with betaine and HCl (hydrochloric acid) to aid in digestion in various gastrointestinal conditions 14, 6.

Pepsin is required for digestion in the stomach

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Associated Conditions
  • Diarrhea
  • Gastritis Chronic
  • Hypochlorhydria
  • Postoperative digestive insufficiency
Contraindications & Blackbox Warnings

Pepsin is required for digestion in the stomach

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Pharmacodynamics

Pepsin digests protein 12. It classified by the FDA that is characterizing enzyme activity is that of a peptide hydrolase 17.

Mechanism of action

Glands present in the mucous membrane lining of the stomach produce and store an inactive protein named pepsinogen. Impulses from the vagus nerve and the hormonal secretions of the hormones gastrin and secretin promote the release of pepsinogen into the stomach, where it is mixed with hydrochloric acid and quickly converted to the active enzyme pepsin. The digestive potency of pepsin is highest at the acidic pH of normal gastric juice. In the intestine, the gastric acids are then neutralized, and pepsin is no longer effective 12.

Pepsin, the proteolytic enzyme of the stomach is normally responsible for less than 20% of the protein digestion occuring the gastrointestinal tract. It is an endopeptidase enzyme that metabolizes proteins to peptides. It preferentially hydrolyzes peptide linkages where one of the amino acids is aromatic. Pepsin, like other protease enzymes, is produced from an inactive precursor, pepsinogen, which is stored in granule form in the chief cells of the stomach and are released by a process called exocytosis 16.

In the digestive tract, pepsin activity only contributes to the partial breakdown of proteins into smaller units called peptides, which then either are absorbed from the intestine into the bloodstream or are broken down further by pancreatic enzymes 12.

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Pepsin is the first of several enzymes that digest proteins. In the stomach, polypeptide chains bind in the deep active site groove of pepsin, and are then digested into smaller pieces. Following this, a variety of proteases and peptidases in the intestine complete the process. The small fragments, which are amino acids and dipeptides, are then absorbed by cells for use as metabolic energy or construction of new proteins 15.

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects

Pepsin is required for digestion in the stomach

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Toxicity

Oral LD50 Rat 90000 mg/kg MSDS

Chronic backflow of pepsin, acid, and other substances from the stomach into the esophagus, is the basis of reflux conditions, particularly gastroesophageal reflux disease (GERD) and laryngopharyngeal reflux. In the latter, pepsin and acid travel all the way up to the larynx, where they can lead to damage of the laryngeal mucosa and lead to symptoms ranging from hoarseness of the voice and chronic cough to laryngospasm (involuntary contraction of the vocal cords) as well as laryngeal cancer 12.

Though limited data is available on the toxicity of exogenous pepsin (not naturally produced in one's gastrointestinal tract), it can be extrapolated from the above-mentioned information that pepsin overdose may lead to mucosal tissue damage of the gastrointestinal tract.

PathwaysNot AvailablePharmacogenomic Effects/ADRs Not AvailableDrug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Not AvailableFood Interactions
  • Drink plenty of fluids.
  • Take before a meal.

Pepsin is required for digestion in the stomach

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Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Digestex Liquid 100 mg / 30 mL Oral Theralab Inc. 1981-04-25 2000-08-01
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Bemosin Tab Pepsin (130 mg) + Ammonium chloride (97.2 mg) + Betaine hydrochloride (130 mg) Tablet Oral Therapeutic Foods Co. 1988-12-31 2003-07-16
Betaine HCl and Pepsin Pepsin (135 mg) + Betaine hydrochloride (324 mg) Tablet Oral Rheingold Food International Ltd. 1985-12-31 2007-07-26
Betasin Tab Pepsin (130 mg / tab) + Ammonium chloride (97.2 mg / tab) + Betaine hydrochloride (130 mg / tab) Tablet Oral Bio Vita 1987-12-31 1996-09-09
Debiline Pepsin (50 mg) + Deoxycholic acid (100 mg) Tablet Oral Lab Nadeau LtÉe, Division Of Technilab Inc. 1951-12-31 1999-09-28
Debiline H Pepsin (50 mg / tab) + Deoxycholic acid (100 mg / tab) + Homatropine methylbromide (2.5 mg / tab) Tablet Oral Lab Nadeau LtÉe, Division Of Technilab Inc. 1951-12-31 1999-09-28
Duchol Ect Pepsin (200 mg) + Dehydrocholic acid (30 mg) + Deoxycholic acid (30 mg) + Pancrelipase (200 mg) + Sodium taurocholate (100 mg) Tablet, delayed release Oral Duchesnay Inc. 1977-12-31 2003-07-18
Dygest Pepsin (125 mg) + Betaine hydrochloride (90 mg) + Ox bile extract (75 mg) + Pancrelipase (200 mg) + Papain (100 mg) + Peppermint (50 mg) Tablet Oral Creative Nutrition Canada Corp. 1987-12-31 2007-07-11
Enzyme Tablets Pepsin (65 mg) + Betaine hydrochloride (65 mg) + Ox bile extract (8.125 mg) + Pancrelipase (100 mg) + Pancrelipase amylase (130 mg) + Papain (65 mg) Tablet Oral General Nutrition Canada Inc. 2001-10-20 2007-08-01
Glutamic Acid HCl Betaine HCl W Pepsin Pepsin (100 mg / tab) + Betaine hydrochloride (100 mg / tab) + Glutamic acid hydrochloride (200 mg / tab) Tablet Oral Nu Life Nutrition Ltd. 1963-12-31 2000-03-03
Glutamic Acid Hydrochloride Nu Life Pepsin (65 mg) + Glutamic acid hydrochloride (500 mg) Tablet Oral Nu Life Nutrition Ltd. 1963-12-31 2005-03-15
ATC CodesA09AC01 — Pepsin and acid preparations
  • A09AC — Enzyme and acid preparations, combinations
  • A09A — DIGESTIVES, INCL. ENZYMES
  • A09 — DIGESTIVES, INCL. ENZYMES
  • A — ALIMENTARY TRACT AND METABOLISM
A09AA03 — Pepsin
  • A09AA — Enzyme preparations
  • A09A — DIGESTIVES, INCL. ENZYMES
  • A09 — DIGESTIVES, INCL. ENZYMES
  • A — ALIMENTARY TRACT AND METABOLISM
Drug Categories

  • Alimentary Tract and Metabolism
  • Aspartic Acid Endopeptidases
  • Aspartic Acid Proteases
  • Digestives, Incl. Enzymes
  • Endopeptidases
  • Enzyme Preparations
  • Enzymes
  • Enzymes and Coenzymes
  • Gastrointestinal Agents
  • Hydrolases
  • Pepsin A, antagonists & inhibitors
  • Peptide Hydrolases

Chemical TaxonomyProvided by Classyfire DescriptionNot AvailableKingdomOrganic CompoundsSuper ClassOrganic AcidsClassCarboxylic Acids and DerivativesSub ClassAmino Acids, Peptides, and AnaloguesDirect ParentPeptidesAlternative ParentsNot AvailableSubstituentsNot AvailableMolecular FrameworkNot AvailableExternal DescriptorsNot AvailableAffected organisms
  • Humans and other mammals
UNIIGID333S43JCAS number9001-75-6General References
  1. Iannella G, Di Nardo G, Plateroti R, Rossi P, Plateroti AM, Mariani P, Magliulo G: Investigation of pepsin in tears of children with laryngopharyngeal reflux disease. Int J Pediatr Otorhinolaryngol. 2015 Dec;79(12):2312-5. doi: 10.1016/j.ijporl.2015.10.034. Epub 2015 Oct 30. [Article]
  2. Fruton JS: A history of pepsin and related enzymes. Q Rev Biol. 2002 Jun;77(2):127-47. [Article]
  3. Calvo-Henriquez C, Ruano-Ravina A, Vaamonde P, Martinez-Capoccioni G, Martin-Martin C: Is Pepsin a Reliable Marker of Laryngopharyngeal Reflux? A Systematic Review. Otolaryngol Head Neck Surg. 2017 Sep;157(3):385-391. doi: 10.1177/0194599817709430. Epub 2017 Jun 6. [Article]
  4. Petersen KU: Pepsin and Its Importance for Functional Dyspepsia: Relic, Regulator or Remedy? Dig Dis. 2018;36(2):98-105. doi: 10.1159/000481399. Epub 2017 Oct 5. [Article]
  5. Hedemann MS, Jensen BB: Variations in enzyme activity in stomach and pancreatic tissue and digesta in piglets around weaning. Arch Anim Nutr. 2004 Feb;58(1):47-59. [Article]
  6. Nutritional Interventions for Gastroesophageal Reflux, Irritable Bowel Syndrome, and Hypochlorhydria: A Case Report [Link]
  7. Pepsin, Sigma Aaldrich [Link]
  8. Effect of Pepsin on the Absorption of Food Vitamin B12 and Iron [Link]
  9. Pepsin [Link]
  10. Pepsin: science.gov topics [Link]
  11. Pancreatic Enzyme Replacement Therapy During Pancreatic Insufficiency [Link]
  12. Pepsin [Link]
  13. Gastritis [Link]
  14. Zypan [Link]
  15. PDB-pepsin [Link]
  16. NIH Dictionary- Pepsin [Link]
  17. Code of Federal Regulations, Pepsin [Link]
  18. Pepsin Drug Monograph [Link]
  19. Pepsin, Drugs.com [Link]
  20. Determining the Safety of Enzymes Used in Food Processing [Link]
  21. PEPSIN, SIGMA AALDRICH [Link]
  22. Digestion of Nucleic Acids Starts in the Stomach [Link]
External LinksPubChem Substance347911445RxNav8016WikipediaPepsinMSDSClinical Trials
PhaseStatusPurposeConditionsCount
Not Available Completed Not Available Abdominal Pain / Dyspepsia / Flatulence / Functional Gastrointestinal Disorders (FGID) / Nausea / Vomiting 1
Manufacturers

Not Available

Packagers

Not Available

Dosage Forms
FormRouteStrength
Liquid Oral 100 mg / 30 mL
Tablet, delayed release Oral
Tablet Oral
Tablet, film coated Oral
Tablet
PricesNot AvailablePatentsNot AvailableStateSolidExperimental Properties
PropertyValueSource
water solubility very soluble MSDS

Drug created at June 23, 2017 20:37 / Updated at June 05, 2021 09:12

What is the function of pepsin in stomach?

pepsin, the powerful enzyme in gastric juice that digests proteins such as those in meat, eggs, seeds, or dairy products. Pepsin is the mature active form of the zymogen (inactive protein) pepsinogen.

Where is pepsin in the digestive system?

Pepsin /ˈpɛpsɪn/ is an endopeptidase that breaks down proteins into smaller peptides. It is produced in the gastric chief cells of the stomach lining and is one of the main digestive enzymes in the digestive systems of humans and many other animals, where it helps digest the proteins in food.

How does pepsin digest proteins?

Pepsin cleaves peptide bonds in the amino-terminal side of the cyclic amino acid residues (tyrosine, phenylalanine, and tryptophan), breaking the polypeptide chains into smaller peptides (Fange and Grove, 1979).