KONTAB

Indications

• Osteoarthritis
• Sinusitis
• Postoperative inflammation
• Wound healing
• Digestive disorders

Dosage

Children: Refer to specific product guidelines for paediatric doses, as bromelain usage in children should be approached with caution and under medical supervision.

Adults: Refer to specific product guidelines for dosing, as bromelain is available in various formulations. Doses may range widely based on the indication and formulation.

Mechanism of action

Bromelain acts by breaking down proteins into smaller peptides and amino acids, which aids in digestion. It also has anti-inflammatory effects by inhibiting the activity of pro-inflammatory mediators, including bradykinin and prostaglandins. Additionally, bromelain may enhance the absorption of certain antibiotics and improve the bioavailability of other therapeutic agents.

Pharmacodynamics

Bromelain exhibits anti-inflammatory and analgesic properties, which are beneficial in reducing swelling, bruising, and pain. Its proteolytic activity can promote the degradation of fibrin, a protein involved in blood clotting, thereby assisting in the reduction of inflammation and promoting healing. Its effects on the immune system also contribute to its therapeutic potential.

Pharmacokinetics

Bromelain is absorbed in the gastrointestinal tract, with its bioavailability influenced by the presence of food. Its systemic effects may vary based on the formulation and dosage. The elimination of bromelain occurs primarily through the renal pathway, and its half-life is not well established due to variations in individual metabolism and formulation.

Adverse effects

• Gastrointestinal disturbances (nausea, diarrhea, abdominal pain)
• Allergic reactions (skin rash, itching, anaphylaxis in sensitive individuals)
• Increased bleeding risk (due to its fibrinolytic activity)

Interactions

• Anticoagulants (increased risk of bleeding)
• Antiplatelet drugs (may enhance effects)
• Antibiotics (may enhance absorption and effects)

Precautions

• Use with caution in individuals with a history of allergies to pineapples or other bromelain sources
• Caution in patients with bleeding disorders or those undergoing surgery

Pregnancy

There is insufficient reliable information regarding the safety of bromelain during pregnancy. It should be used with caution and only if clearly needed.

Breast-feeding

Limited information is available; consult a healthcare provider before use.

Storage

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

Formulations

• Oral tablets
• Capsules
• Powder

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