PANZIM 10 000

Indications

• Exocrine pancreatic insufficiency
• Cystic fibrosis
• Chronic pancreatitis
• Post-surgical states involving the pancreas

Dosage

Children: Children aged 1–11 months: 1–2 capsules mixed with feeds. Children aged 1–17 years: 2–6 capsules to be taken with each meal, either swallowed whole or sprinkled on food.

Adults: Initially 1–2 capsules taken with each meal, and 1 capsule taken with snacks. Capsules may be swallowed whole or the contents mixed with a slightly acidic liquid or soft food, then swallowed immediately without chewing.

Mechanism of action

Pancreatin consists of a mixture of digestive enzymes including amylase, lipase, and proteases. These enzymes work in the gastrointestinal tract to break down carbohydrates, fats, and proteins into smaller molecules that can be easily absorbed by the body. The action of these enzymes is crucial, as their absence due to pancreatic insufficiency leads to malabsorption and nutrient deficiencies.

Pharmacodynamics

The pharmacodynamic effects of pancreatin are primarily seen in the gastrointestinal tract where it enhances digestion and nutrient absorption. By providing the necessary enzymes that are lacking in patients with pancreatic insufficiency, pancreatin helps alleviate symptoms such as steatorrhea (fatty stools), abdominal discomfort, and weight loss. It helps improve the overall nutritional status of patients.

Pharmacokinetics

Pancreatin is administered orally and is inactivated by gastric acid, making it necessary to take it with food or immediately before or after meals for optimal effect. The enzymes are released in the duodenum where they exert their action. The absorption of the resulting products of digestion occurs in the small intestine. The exact pharmacokinetic profile, including half-life and metabolism of the individual enzymes, varies and is often not detailed due to the complex nature of enzyme activity and digestion.

Adverse effects

• Abdominal distension
• Constipation
• Nausea
• Vomiting
• Skin reactions
• Fibrosing colonopathy

Interactions

• Pancreatin may reduce the effects of acarbose

Precautions

• Can irritate the perioral skin and buccal mucosa if retained in the mouth
• Excessive doses can cause perianal irritation

Pregnancy

Not known to be harmful.

Breast-feeding

Not known to be harmful.

Storage

Store in a cool, dry place. Keep the container tightly closed.

Formulations

• CREON® 10000
• CREON® 25000
• CREON® 40000
• PANCREX® V CAPSULES
• PANCREX® V POWDER
• PANCREX® V TABLETS
• PANCREX® V TABLETS FORTE
• CREON® MICRO

Indications

• Pancreatitis
• Salivary gland disorders
• Carbohydrate malabsorption syndromes

Dosage

Children: Refer to the BNF for Children for appropriate dosing information.

Adults: Refer to the specific guidelines and dosing recommendations in the BNF.

Mechanism of action

Amylase facilitates the breakdown of starch and glycogen into maltose and dextrins by cleaving the α-1,4-glycosidic bonds in these polysaccharides. Its action begins in the mouth with salivary amylase and continues in the small intestine with pancreatic amylase, where it further digests carbohydrates.

Pharmacodynamics

Amylase increases the rate of carbohydrate digestion, thereby influencing blood glucose levels. The enzyme's activity can be affected by pH levels, temperature, and the presence of inhibitors or activators. In clinical settings, elevated levels of amylase in the blood can indicate pancreatitis or other pancreatic disorders.

Pharmacokinetics

Amylase is absorbed and metabolized in the gastrointestinal tract. Its activity is measured through serum levels, with normal ranges indicating proper pancreatic function. The half-life of amylase in the bloodstream can vary based on individual metabolic rates and health conditions.

Pregnancy

Amylase is generally considered safe during pregnancy but should be used under medical supervision.

Breast-feeding

Amylase is excreted in breast milk; it is advisable to consult a healthcare provider before use while breastfeeding.

Storage

Store in a cool, dry place away from direct sunlight.

Indications

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

Dosage

Children: Refer to the BNF for Children for specific pediatric dosing guidelines, as it varies based on age, weight, and clinical conditions.

Adults: Refer to specific product guidelines or clinical protocols, as dosages may vary based on the formulation and clinical condition.

Mechanism of action

Lipase hydrolyzes triglycerides into diglycerides and free fatty acids. This process occurs in the presence of bile salts, which emulsify fats, allowing lipase to effectively access and break down lipid molecules. The free fatty acids produced can then be absorbed by the intestinal mucosa and transported into the bloodstream.

Pharmacodynamics

Lipase enhances the digestion of dietary fats, facilitating their absorption. The activity of lipase is pH-dependent, with optimal function occurring in the alkaline environment of the small intestine. The enzyme's activity can be influenced by factors such as dietary composition and the presence of bile salts. Elevated levels of lipase in the bloodstream can indicate pancreatic inflammation or damage, such as in cases of pancreatitis.

Pharmacokinetics

Lipase is not absorbed systemically; it functions locally in the gastrointestinal tract. The enzyme is secreted by the pancreas and acts in the small intestine. Its activity can be affected by gastrointestinal transit time and the presence of other digestive enzymes. The half-life of lipase in the gastrointestinal tract is dependent on dietary intake and gastrointestinal motility.

Adverse effects

• Abdominal cramping
• Diarrhea
• Nausea
• Vomiting
• Allergic reactions

Precautions

• Use with caution in patients with a history of pancreatitis
• Monitor for signs of allergic reactions
• Evaluate dietary fat intake in patients receiving lipase therapy

Pregnancy

Lipase is generally considered safe during pregnancy, but should be used under medical supervision.

Breast-feeding

Lipase can be used while breastfeeding, although it is advisable to consult a healthcare provider.

Storage

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

Formulations

• Capsules
• Tablets
• Powder for oral suspension

Indications

• HIV/AIDS
• Cancer
• Chronic pancreatitis
• Certain inflammatory diseases

Dosage

Children: Refer to the BNF for Children for specific paediatric dosing information regarding protease inhibitors.

Adults: Refer to the BNF for specific dosage recommendations for protease inhibitors based on the particular drug and condition being treated.

Mechanism of action

Proteases function by hydrolyzing the peptide bonds that link amino acids in proteins. This process is essential for the activation of many proteins and for the degradation of misfolded or damaged proteins. In antiretroviral therapy, protease inhibitors block the action of viral proteases, preventing the maturation of viral particles and thereby inhibiting viral replication.

Pharmacodynamics

Proteases exhibit a variety of pharmacodynamic effects depending on their specific type and target. For instance, HIV protease inhibitors prevent the cleavage of viral polyproteins, which is essential for the production of infectious viral particles. The inhibition of proteolytic activity can lead to accumulation of unprocessed protein precursors, ultimately reducing the viral load in patients with HIV.

Pharmacokinetics

The pharmacokinetic profile of proteases varies widely among different classes. Generally, they are absorbed following oral administration, but the extent of absorption can be affected by food intake. Many protease inhibitors undergo extensive hepatic metabolism, particularly via the cytochrome P450 enzyme system. The elimination half-life can range from several hours to days, depending on the specific protease. Renal excretion plays a significant role in the clearance of some proteases, while others may be predominantly excreted in the feces.

Pregnancy

Refer to specific product guidelines as data may vary.

Breast-feeding

Refer to specific product guidelines as data may vary.

Storage

Store at room temperature, away from moisture and light.