Endos

Endos Uses, Dosage, Side Effects, Food Interaction and all others data.

Docusate acts primarily by increasing the penetration of fluid into the faeces. It may also have effects on intestinal fluid secretion, and probably act both as stimulant and faecal softening agent. It also softens ear wax through penetration into the dry matrix of the ceruminous mass, reducing it into semi-solid debris.

Docusate sodium is a laxative and an anionic detergent that supposedly promotes incorporation of water and fats into stool through a reduction in surface tension, resulting in softer fecal mass . Docusate's onset of action is 6-72 hours orally and 2-15 minutes rectally . The effects of docusate are thought to be exerted locally in the jejunum.

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

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 .

Pepsin is often used as a replacement enzyme for those with pancreatic insufficiency . 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 .

Trade Name Endos
Generic Docusate + Diastase + Pepsin
Weight 100mg
Type Capsule
Therapeutic Class
Manufacturer Geno Pharmaceuticals Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Endos
Endos

Uses

Docusate is used for Constipation, Bowel evacuation, Softening of ear wax, Constipation

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

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

Pepsin powder is prepared from the gastric mucosa of pigs, cattle or sheep . 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 .

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

Endos is also used to associated treatment for these conditions: Constipation, Occasional Constipation, Bowel preparation therapyDiarrhoea, Gastritis Chronic, Hypochlorhydria, Postoperative digestive insufficiency

How Endos works

Recent studies suggest that docusate's mechanism of action is due largely to it's surfactant effect in the intestines, which allow fat and water into the feces to soften the stool.

Docusate’s mechanism of action was investigated in 1985 on healthy patients. Docusate was added directly to the jejunum based on calculated concentrations of docusate in the jejunum. At this concentration, there was an increase in secretion of water, sodium, chloride, and potassium as well as a decrease in absorption of glucose and bicarbonate. Based on in vitro data, the authors suggested this effect was due to an increase in intracellular cyclic AMP either directly through docusate or E series prostaglandins.

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 .

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 .

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 .

Dosage

Endos dosage

Constipation:

  • Adult: 50-300 mg daily in divided doses. Max: 500 mg daily.
  • Child: ≥12 yr Same as adult dose.

Bowel evacuation:

  • Adult: As adjunct to abdominal radiological procedures: 400 mg given with barium meal.
  • Child: ≥12 yr Same as adult dose.

Side Effects

Anorectal pain or bleeding (rectal). Rarely, diarrhoea, abdominal cramps, nausea, skin rash.

Toxicity

Docusate is not known to be carcinogenic or cause reproductive toxicity. It was not mutagenic in the Ames assay . Acute oral LD50 in rat is 1900 mg/kg .

Oral LD50 Rat 90000 mg/kg

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 .

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.

Precaution

Rectal admin in patient with haemorrhoids or anal fissures. Children. Pregnancy and lactation.

Interaction

May enhance GI uptake of other drugs (e.g. liquid paraffin). May increase effects of anthraquinone laxatives. Increased incidence of adverse effects in GI mucosa with aspirin.

Elimination Route

Docusate is not absorbed systemically. As the actions of docusate are local and it is not absorbed, the pharmacokinetic parameters are not available.

Elimination Route

If docusate is systemically absorbed, it undergoes biliary excretion .

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

Presence of abdominal pain, nausea, vomiting, intestinal obstruction. Perforation of ear drum or ear inflammation (otic).

Acute Overdose

Symptoms: Oral: Excessive loss of water and electrolytes. Otic: Skin irritation.

Management: Oral: Encourage patient to drink plenty of fluid. Replenish electrolyte loss where appropriate. Otic: Symptomatic treatment.

Storage Condition

Store between 15-30° C. Protect from freezing, heat, humidity and light.

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