Camostat

Usage

• Camostat is prescribed for the remission of acute symptoms in chronic pancreatitis and for the treatment of postoperative reflux esophagitis.
• Pharmacological Classification: Serine protease inhibitor.
• Mechanism of Action: Camostat inhibits several serine proteases, including trypsin, kallikrein, and TMPRSS2. This action reduces the activity of pancreatic enzymes and diminishes pancreatic inflammation in chronic pancreatitis. It also inhibits TMPRSS2, which plays a role in viral cell entry, including SARS-CoV-2.

Alternate Names

• International/Regional Variations: Camostat mesilate (mesylate refers to the salt form).
• Brand Names: Foipan, Foypan.

How It Works

• Pharmacodynamics: Camostat reduces pancreatic enzyme activity, thereby decreasing inflammation in the pancreas. It also blocks the entry of certain viruses into host cells.
• Pharmacokinetics:
  • Absorption: Orally administered camostat is rapidly absorbed and metabolized to its active metabolite, 4-(4-guanidinobenzoyloxy)phenylacetate (GBPA).
  • Metabolism: Camostat mesylate is hydrolyzed by carboxyesterase to GBPA. GBPA is further hydrolyzed by arylesterase to 4-guanidinobenzoic acid (GBA).
  • Elimination: Primarily eliminated via renal excretion (89.8-95.6%) with a small amount excreted in feces (1.0-1.7%). The half-life is approximately 3.8-4.7 hours, and clearance is 4.5-7.3 mL/min/kg.
• Mode of Action: Camostat and GBPA competitively and reversibly bind to the active site of serine proteases. GBA binds covalently.
• Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Inhibits serine proteases such as trypsin, chymotrypsin, kallikrein, and TMPRSS2.

Dosage

Standard Dosage

Adults:

• Chronic Pancreatitis: 200 mg three times daily, taken after meals.
• Postoperative Reflux Esophagitis: 100 mg three times daily, taken after meals.

Children:

• Not recommended for patients under 18 years of age.

Special Cases:

• Elderly Patients: Dosage adjustments may be necessary based on renal and hepatic function.
• Patients with Renal Impairment: Dosage adjustments may be required.
• Patients with Hepatic Dysfunction: Dosage adjustments may be required.
• Patients with Comorbid Conditions: Use with caution in patients with severe chronic pancreatitis.

Clinical Use Cases

• Data regarding the dosage for intubation, surgical procedures, mechanical ventilation, ICU use, and emergency situations are not available.

Dosage Adjustments

• Dose adjustments may be necessary in patients with renal or hepatic dysfunction.

Side Effects

Common Side Effects:

• Rash
• Itching
• Nausea
• Stomach discomfort
• Abdominal bloating
• Diarrhea

Rare but Serious Side Effects:

• Anaphylaxis
• Thrombocytopenia
• Hepatic dysfunction
• Jaundice
• Hyperkalemia
• Angioedema
• Urticaria
• Leucopenia
• Erythrocytopenia
• Eosinophilia

Long-Term Effects:

• No specific long-term effects have been identified, but prolonged use should be monitored for potential adverse effects.

Adverse Drug Reactions (ADR):

• Anaphylaxis, thrombocytopenia, severe hepatic dysfunction, hyperkalemia.

Contraindications

• Hypersensitivity to camostat or any of its components.
• Severe chronic pancreatitis requiring suction of gastric juice or dietary restrictions.
• Pregnancy (high doses).

Drug Interactions

• May enhance the effects of anticoagulants like warfarin, increasing bleeding risk.
• May interact with other protease inhibitors.
• May interact with certain thrombogenic drugs.
• Consult a drug interaction database for specific interactions.

Pregnancy and Breastfeeding

• Pregnancy: High doses are contraindicated. Low doses should be used with caution and only if potential benefits outweigh risks.
• Breastfeeding: Not recommended unless potential benefits outweigh risks.

Drug Profile Summary

• Mechanism of Action: Serine protease inhibitor, inhibiting trypsin, kallikrein, TMPRSS2, etc.
• Side Effects: Rash, itching, nausea, abdominal discomfort, diarrhea; rarely: anaphylaxis, thrombocytopenia, hepatic dysfunction, jaundice, hyperkalemia.
• Contraindications: Hypersensitivity, severe chronic pancreatitis, pregnancy (high doses).
• Drug Interactions: Anticoagulants, other protease inhibitors, thrombogenic agents.
• Pregnancy & Breastfeeding: Use with caution if benefits outweigh risks.
• Dosage: Adults: 100-200 mg three times daily after meals. Not recommended for children under 18.
• Monitoring Parameters: Liver function tests, complete blood count, serum potassium levels.

Popular Combinations

• No established popular combinations are available.

Precautions

• General Precautions: Assess for allergies and renal/hepatic function before starting therapy.
• Specific Populations: Caution in pregnancy and breastfeeding. Not recommended for children.
• Lifestyle Considerations: No specific restrictions on alcohol, smoking, or diet are documented, but advise moderation.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Camostat?

A: For adults, 200 mg three times daily for chronic pancreatitis and 100 mg three times daily for postoperative reflux esophagitis, taken after meals. Not recommended for children under 18.

Q2: What is the mechanism of action of Camostat?

A: Camostat is a serine protease inhibitor. It inhibits trypsin, kallikrein, and TMPRSS2, reducing inflammation and viral cell entry.

Q3: What are the common side effects of Camostat?

A: Common side effects include rash, itching, nausea, abdominal discomfort, and diarrhea.

Q4: Is Camostat safe during pregnancy?

A: High doses are contraindicated in pregnancy. Low doses should be used with caution and only if the potential benefits outweigh the risks.

Q5: Can Camostat interact with other medications?

A: Yes, Camostat may interact with anticoagulants, other protease inhibitors, and thrombogenic drugs. Consult a drug interaction database for specific interactions.

Q6: What are the contraindications to using Camostat?

A: Contraindications include hypersensitivity to camostat, severe chronic pancreatitis requiring dietary restrictions, and pregnancy (high doses).

Q7: How is Camostat metabolized and eliminated?

A: Camostat is metabolized to GBPA and then to GBA. It is primarily eliminated via renal excretion.

Q8: Are there any long-term effects of using Camostat?

A: No specific long-term effects have been identified, but prolonged use should be monitored for potential adverse effects.

Q9: What should patients be monitored for while taking Camostat?

A: Patients should be monitored for liver function, complete blood count, and serum potassium levels.

This information is current as of February 16, 2025, and may be subject to change as new research emerges. Always consult the latest medical literature and guidelines for the most up-to-date information.