AMBEZIM-G

Indications

• Pancreatic insufficiency
• Protein malabsorption
• Digestive disorders involving protein digestion

Dosage

Children: Refer to specific product guidelines for dosing information, as it may vary

Adults: Refer to specific product guidelines for dosing information, as it may vary based on formulation and clinical condition.

Mechanism of action

Chymotrypsin acts by cleaving peptide bonds on the carboxyl side of aromatic amino acids such as phenylalanine, tryptophan, and tyrosine. The enzyme's active site contains a catalytic triad of serine, histidine, and aspartate residues, which facilitate the hydrolysis of peptide bonds. The enzyme-substrate complex formation is key to its activity, where the substrate binds to the active site, enabling the enzymatic cleavage of peptide bonds, resulting in the production of smaller peptides and free amino acids.

Pharmacodynamics

Chymotrypsin enhances the digestive process by increasing the availability of amino acids from dietary proteins. This enzymatic activity is particularly vital in individuals with pancreatic insufficiency, where the lack of endogenous enzyme production leads to malabsorption and nutritional deficiencies. The efficacy of chymotrypsin in protein digestion can contribute to improved nutritional status and overall health in affected individuals.

Pharmacokinetics

Chymotrypsin is administered orally or via injection, depending on the formulation. After administration, it is absorbed into the bloodstream and its effects can be observed in the gastrointestinal tract. The enzyme's activity is dependent on the pH of the environment, with optimal activity occurring in alkaline conditions. Chymotrypsin is eventually inactivated and metabolized in the body, with its products excreted through urine. The half-life of chymotrypsin varies based on the route of administration and the formulation used.

Contra-indications

• Hypersensitivity to chymotrypsin or any component of the formulation
• Active bleeding or conditions associated with bleeding
• Severe renal impairment
• History of gastrointestinal bleeding

Adverse effects

• Allergic reactions including rash, pruritus, and anaphylaxis
• Gastrointestinal disturbances such as nausea and diarrhea
• Injection site reactions including pain and swelling
• Increased risk of bleeding

Interactions

• Anticoagulants may have enhanced effects leading to increased bleeding risk
• Corticosteroids may interfere with the anti-inflammatory effects of chymotrypsin

Precautions

• Use with caution in patients with liver disease
• Monitor for signs of bleeding in patients on anticoagulants
• Assess for allergies prior to administration

Pregnancy

Safety during pregnancy has not been established, consult a healthcare provider before use.

Breast-feeding

Chymotrypsin is excreted in breast milk, caution is advised when administering to nursing mothers.

Storage

Store at room temperature, protect from light and moisture, keep out of reach of children.

Formulations

• Tablets
• Powder for reconstitution
• Injectable solution

Indications

• Pancreatic insufficiency
• Malabsorption syndromes
• Cystic fibrosis
• Chronic pancreatitis

Dosage

Children: Refer to the BNF for Children for appropriate dosing information tailored to paediatric patients.

Adults: Refer to the prescribing information or BNF for specific dosing guidelines based on the condition being treated and the formulation used.

Mechanism of action

Trypsin acts by cleaving peptide bonds in proteins, particularly at the carboxyl side of lysine and arginine residues. This enzymatic activity is essential for protein digestion, leading to the conversion of proteins into smaller peptides and free amino acids, which can be readily absorbed by the intestinal mucosa. The activation of trypsinogen to trypsin is catalyzed by the enzyme enteropeptidase, which is secreted by the intestinal mucosa.

Pharmacodynamics

The pharmacodynamic effects of trypsin are primarily related to its role in protein digestion. It aids in the breakdown of complex protein structures into smaller peptides, which enhances nutrient absorption. Additionally, trypsin may influence various physiological processes by modulating protein signaling pathways, although these effects are less well-characterized compared to its digestive role.

Pharmacokinetics

Trypsin is typically administered exogenously in a proteolytic enzyme supplement form, particularly for conditions associated with pancreatic insufficiency. When taken orally, it is subject to degradation in the gastrointestinal tract; hence, it is often encapsulated to protect it from gastric acid. Its absorption is generally poor, and any systemic effects are limited due to rapid inactivation in the systemic circulation. Clinical studies indicate that trypsin may be absorbed in small amounts, but its primary use remains local to the gastrointestinal tract.

Contra-indications

• Hypersensitivity to trypsin or any of its components
• Active gastrointestinal bleeding
• Severe renal impairment
• History of pancreatitis

Adverse effects

• Gastrointestinal disturbances such as nausea, vomiting, and diarrhea
• Allergic reactions including rash and urticaria
• Increased risk of bleeding
• Local irritation at the site of administration

Interactions

• Anticoagulants may have enhanced effects when used with trypsin due to its proteolytic activity
• Corticosteroids may interfere with the action of trypsin
• Other proteolytic enzymes may have additive effects

Precautions

• Use with caution in patients with a history of allergies
• Monitor for signs of bleeding in patients with clotting disorders
• Evaluate renal function before initiating therapy
• Caution in patients with a history of gastrointestinal disorders

Pregnancy

There are no well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether trypsin is excreted in human milk. Caution should be exercised when administering to nursing women.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Enteric-coated tablets
• Capsules
• Powder for reconstitution