Enzyme preparations

Principles of therapy and classification

Digestive disorders, or maldigestion, most commonly arise due to functional insufficiency of the gastrointestinal organs. This condition is termed secondary enzymopathy, with replacement therapy serving as the primary treatment method. In congenital (primary) enzymopathies, strict dietary therapy with the exclusion of the non-tolerated substrate takes precedence.

Depending on their composition, all enzyme agents are divided into two large groups:

1. Containing bile and gastric mucosal extracts (Panzinorm, Festal, Digestal, Enzistal).
2. Bile-free, which include pure pancreatin preparations (Meзим, Creon, Triferment), as well as plant- and fungal-derived enzymes (Orazase, Solizym).

Bile-containing preparations

These agents exert a complex effect: they not only compensate for secretory deficiency but also produce a mild laxative effect, making them ideal for patients prone to constipation.

• Gastric mucosal extract ensures proteolysis via pepsin and cathepsin, and also contains peptides that stimulate the production of endogenous gastrin.
• Bile acids emulsify fats, improve the absorption of fat-soluble vitamins, and activate pancreatic lipase.

A prominent representative of this group is Panzinorm. This is a bilayer preparation that mimics the physiology of digestion. Its outer layer dissolves in the stomach (releasing gastric extracts and amino acids), while the inner, acid-resistant layer dissolves in the intestine (releasing pancreatin and bile).

Another popular preparation is Festal. In addition to enzymes and bile, it contains hemicellulase, which breaks down plant fiber. This facilitates enzyme access to food and reduces flatulence. It is important to remember that bile-containing preparations are contraindicated in severe liver damage (especially with hyperbilirubinemia) and intestinal obstruction.

Monocomponent preparations (bile-free)

The basis of this group is animal-derived pancreatin, obtained from the pancreas of cattle. It contains amylase, proteases, and lipase.

The key rule: the dosage of pancreatin is always calculated based on the lipase content and directly depends on the degree of exocrine insufficiency. The daily dose can reach 5–10 g. Preparations (e.g., Meзим or Triferment) are generally well tolerated and are prescribed before meals.

A special place is held by Creon—microgranulated pancreatin. Its microgranules mix evenly with the food bolus (chyme) in the stomach, but dissolve exclusively in the small intestine at pH 5.0 and above. Like other enzymes, Creon is strictly contraindicated in acute pancreatitis.

Fungal and plant-derived enzymes

If animal pancreatin is not suitable or a specific action is required, alternative agents are used:

• Orazase (from the culture of the fungus Aspergillus oryzae). Contains an acid-resistant complex for breaking down proteins and carbohydrates. Activated in the alkaline environment of the intestine. Possesses a unique property—it exerts a spasmolytic effect on intestinal smooth muscle.
• Solizym (from the fungus Penicillium solitum). A narrow-spectrum preparation that hydrolyzes fats only. Normalizes blood lipid levels. There is also a combined form—Somilase (Solizym + $\alpha$-amylase), which additionally breaks down carbohydrates.
• Nigedase (from Nigella damascena seeds). A plant-based preparation with an exclusively lipolytic effect. Its activity depends on gastric acidity: in case of reduced acidity, it is recommended to take the preparation with gastric juice. Due to the absence of proteases and amylases, it is advisable to combine nigedase with pancreatin administration.

Class and exam questions

What else to study on this topic

• Features of enzyme use in gastritis with hypo- and hyperacidity.
• The mechanism of action of hemicellulase and its effect on gas formation in the intestine.
• Pharmacokinetics of bilayer preparations using Panzinorm as an example.
• Specific contraindications: why enzyme preparations must not be prescribed in acute pancreatitis.
• Tactics for combining plant lipases (nigedase) with protease- and amylase-containing preparations.

Other topics in the section «Drugs Affecting Digestive System Functions»

Prepared by WhiteCoat Pro faculty in accordance with the medical school curriculum. For educational purposes only.