Pancrelipase - Indications, Uses, Adverse Effects, and Safety Precautions

Overview:

Pancrelipase is a class of medications that are designed to treat malabsorption and abdominal pain due to chronic pancreatitis and exocrine pancreatic insufficiency. This drug can be used for all age groups. They are exogenous versions of digestive hormones and enzymes required for normal digestion. These enzymes are ingested with food to improve digestion, absorption, and abdominal pain in patients with chronic pancreatitis and exocrine pancreatic insufficiency. Manufacturers produced pancreatic enzyme products before the current United States Food and Drug Administration (FDA) and New Drug Approval (NDA) requirements were established. In 2005, the Food and Drug Administration requested the producers to submit a New Drug Approval to approve these products. This includes research concerning the bioavailability of pancreatic enzyme products, the improvement of fat absorption, and the onset of action, of this class of drugs.

For Patients:

What Is Exocrine Pancreatic Insufficiency?

Exocrine pancreatic insufficiency refers to poor absorption of fat, proteins, and a lesser amount of carbohydrates. Persons with exocrine pancreatic insufficiency have low vitamin levels, worse nutritional status, and quality of life. Pancreatic enzyme products have been used to treat this condition for the past three decades.

What Is Pancrelipase?

Pancrelipase is an enzyme that contains a mixture of pancreatic lipase, amylase, and protease. Lipase is a digestive enzyme involved in fat hydrolysis and degradation. Impairment in lipase metabolism leads to the malabsorption of fats. Amylase is a digestive enzyme that helps in the hydrolysis of starch and digestion. Impairment of amylase leads to carbohydrate malabsorption. Proteases are enzymes that are involved in protein and amino acid breakdown. Insufficient proteases cause poor absorption of amino acids and lower the breakdown of essential proteins.

What Is the Mechanism of Action?

Pancreatic enzyme products are exogenous versions of lipase, amylase, and protease enzymes that are derived from porcine pancreatic ducts. These enzymes act locally and break down fats, proteins, and carbohydrates. This mechanism takes place in the duodenum, which is the initial part of the small intestine where nutrients are absorbed, and macromolecules are degraded.

What Is the Dosage?

• Pancrelipase consists of three enzymes with different proportions; hence individuals should not switch between products or should not interchange.

• Individuals should take this medication with meals, or half doses can be taken with snacks.

• An Adult Dose: 500 to 2500 lipase units/kg/dose. It is taken orally with each meal or snack.

• The Pediatric Dose For One to Three Years: 1000 to 2500 lipase units/kg/dose orally with each meal or snack. Start with 1000 lipase units/kg/dose with each meal or snack. The maximum dose can be 6000 lipase units/kg/meal.

• For Ages Four to 11: 500 to 2500 lipase units/kg/dose. It is taken orally with each meal or snack. Start with 1000 lipase units/kg/dose with each meal or snack. The maximum dose can be 6000 lipase units/kg/meal.

• For Ages Twelve and Above: 500 to 2500 lipase units/kg/dose. It is taken orally with each meal or snack. Start with 500 lipase units/kg/dose with each meal or snack.

What Are the Adverse Effects of Pancrelipase?

• Headache.

• Oral irritation.

• Abdominal pain.

• Enlargement of lymph nodes.

• Nasal congestion.

• Neck pain.

• Cough.

• Dizziness.

• Decreased weight.

• Abnormal feces.

What Is the Most Important Information a Patient Should Be Aware Of?

Pancrelipase may increase bowel disorders called fibrosing colonopathy. The patient should call the healthcare professionals if they have unusual stomach pain.

What Should the Patient Tell the Healthcare Professionals Before Taking Pancrelipase?

• Any allergy to pig products.

• Having a history of intestinal blockage.

• Having kidney disorder.

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• Having trouble swallowing capsules.

• Pregnancy or planning to become pregnant.

• Breastfeeding mother.

How Should the Pancrelipase Be Taken Orally?

Infants (Up to Twelve Months):

• Pancrelipase should be administered immediately prior to each feeding. The recommended dose is 2000 to 4000 lipase units per breastfed or 120 mL of formula.

• Contents of the capsules should be administered directly to the mouth or can be given with a small amount of applesauce.

• Care should be taken not to crush or chew or retain in the mouth in order to avoid irritation of the oral mucosa.

Children and Adults:

• Pancrelipase should be taken with meals or snacks, with sufficient fluids.

• Capsules should be swallowed and should not be crushed or chewed.

• For patients who are unable to swallow as a whole, the contents of the capsules are added to a small amount of acidic food like applesauce with a pH of four or less at room temperature.

• Should hold the capsule upright so that one is able to read Pancrelipase on the capsule. Then twist the top portion of the capsule and sprinkle the contents onto the food.

• This food mixture should be swallowed immediately without crushing and followed with water or juice intake to ensure complete ingestion.

• Care should be taken so that no drug is retained in the mouth.

For Doctors:

What Are the Indications?

Pancrelipase delayed-release capsules are indicated for the treatment of exocrine pancreatic insufficiency due to cystic fibrosis.

How Is the Drug Administered?

• Pancrelipase is administered orally.

• Initially should start with a low dose, and gradually the dose should be increased.

• The dosage should be individualized according to the clinical symptoms, the degree of steatorrhea, and the diet fat content.

What Is the Recommended Dosage?

• Pancrelipase consists of three enzymes with different proportions; hence individuals should not switch between products or should not interchange.

• Individuals should take this medication with meals, or half doses can be taken with snacks.

• An adult dose is 500 to 2500 lipase units/kg/dose. It is taken orally with each meal or snack.

• The pediatric dose (for one to three years)is 1000 to 2500 lipase units/kg/dose. It is taken orally with each meal or snack. Start with 1000 lipase units/kg/dose with each meal or snack. The maximum dose can be 6000 lipase units/kg/meal.

• For ages 4 to 11 years: 500 to 2500 lipase units/kg/dose orally with each meal or snack. Start with 1000 lipase units/kg/dose with each meal or snack. The maximum dose can be 6000 lipase units/kg/meal.

• For ages twelve and above: 500 to 2500 lipase units/kg/dose. It is taken orally with each meal or snack. Start with 500 lipase units/kg/dose with each meal or snack.

What Are the Dose Limitations?

• The dosage should not exceed the recommended dosage.

• If symptoms persist, then the dose is increased by the healthcare professionals.

• Patients are instructed not to increase the dose on their own.

• Each individual response to a drug varies, and hence a range of doses is recommended.

• Changes in dose require several days to adapt.

• If doses need to be increased above 2500 lipase units/kg of body weight, further investigation is needed.

How Is the Drug Administered?

Infants (Up to Twelve Months):

• Pancrelipase should be administered immediately prior to each feeding. The recommended dose is 2000 to 4000 lipase units per breastfed or 120 mL of formula.

• Contents of the capsules should be administered directly to the mouth or can be given with a small amount of applesauce.

• Care should be taken not to crush or chew or retain in the mouth in order to avoid irritation of the oral mucosa.

Children and Adults:

• Pancrelipase should be taken with meals or snacks, with sufficient fluids.

• Capsules should be swallowed and should not crush or chew.

• For patients who are unable to swallow as a whole, the contents of the capsules are added to a small amount of acidic food like applesauce with a pH of four or less at room temperature.

• This food mixture should be swallowed immediately without crushing and followed with water or juice intake to ensure complete ingestion.

• Care should be taken so that no drug is retained in the mouth.

What Is the Dosage Strength, and How Is the Drug Supplied?

• Pancrelipase consists of lipase units as the main active ingredient. The other active ingredients include protease and amylase.

• Pancrelipase is a beige-white amorphous powder that is miscible in water and partially soluble or insoluble in alcohol and ether.

• 6,000 USP units of lipase, 19,000 USP units of protease, and 30,000 USP units of amylase capsules come as opaque orange caps with the imprint Pancrelipase 1206 and an opaque blue body.

• 12,000 USP units of lipase, 38,000 USP units of protease, and 60,000 USP units of amylase capsules come as opaque brown caps with the imprint Pancrelipase 1212 and a colorless transparent body.

• 24,000 USP units of lipase, 76,000 USP protease, and 1,20,000 USP amylase come as orange caps with the imprint Pancrelipase 1224 and a colorless transparent body.

How to Store the Drug?

• Pancrelipase should be stored at room temperature up to 25°C to 40°C for up to thirty days.

• It should be protected from moisture.

• Capsules should be discarded when exposed to high temperature and moisture conditions higher than 70 %.

• After opening, the cap should be tightly closed to prevent moisture contamination.

• Should keep out of reach of children.

What Are the Contraindications?

• There are no contraindications for this drug.

What Are the Warnings and Precautions?

1. Fibrosing Colonopathy:

• Fibrosing colonopathy is a rare but serious adverse reaction due to the use of high-dose pancreatic enzymes for a prolonged period in pediatric patients with cystic fibrosis.

• The underlying mechanism is unknown.

• In children less than twelve years of age, the colonic stricture is associated with doses of pancreatic enzymes exceeding 6,000 lipase units/kg body weight per meal.

• Patients with fibrosing colonopathy should be monitored for stricture formation as they are at high risk.

2. Potential Irritation to Oral Mucosa:

• Crushing or chewing the capsules results in disrupting the protective enteric coating that leads to an early release of enzymes, irritation of the oral mucosa, and loss of enzyme activity.

3. Potential for Risk of Hyperuricemia:

• Porcine-derived pancreatic enzyme products contain purines that increase blood uric acid levels; hence caution should be exercised while prescribing the drug.

4. Potential Viral Exposure From the Product Source:

• Since the presence of porcine viruses cannot be excluded, as they might infect humans.

• However, there is no report associated with the transmission of an infectious illness.

5. Allergic Reactions:

• Care should be taken while administering the drug to patients with known allergies to proteins of porcine origin.

• Rare allergic reactions include anaphylaxis, asthma, hives, and pruritus.

What Are the Adverse Effects of Pancrelipase?

• Headache.

• Oral irritation.

• Abdominal pain.

• Enlargement of lymph nodes.

• Nasal congestion.

• Neck pain.

• Cough.

• Dizziness.

• Decreased weight.

• Abnormal feces.

What Is the Postmarketing Experience?

There is no postmarketing experience with this drug.

What Are the Drug Interactions?

No studies have been conducted on interaction with other drugs.

What Are the Uses in a Specific Population?

• Pregnancy: Pregnancy C category. It is not known whether Pancrelipase causes fetal harm when administered to a pregnant woman. Patients should notify healthcare professionals if they are pregnant or trying to get pregnant while under treatment with Pancrelipase.

• Nursing Mothers: It is not evident that Pancrelipase is excreted in human milk. However, it is important to notify healthcare professionals if the patient is breastfeeding.

• Pediatric Use: A cross-over study including 32 patients with exocrine pancreatic insufficiency due to cystic fibrosis was assessed. This study includes twelve patients between 12 and 18 years of age. The safety and efficacy of these patients were similar to that of adult patients.

What Happens in Case of Overdosage?

• There have been no reports of overdose from clinical trials with Pancrelipase.

• High doses have been associated with fibrosing colonopathy, hyperuricosuria, and hyperuricemia.

What Is the Mechanism of Action?

• The pancreatic enzymes in the capsule are enteric-coated, resist destruction in gastric acid, and release most enzymes in vivo in the duodenum at a pH greater than 5.5.

• In the duodenum, these enzymes catalyze fats into monoglycerides, glycerol, and fatty acids.

• Catalyze proteins into peptides and amino acids.

• Catalyze starch into dextrins and short-chain sugars.

• Thereby these enzymes act as a replacement for digestive enzymes that are physiologically secreted by the pancreas.

What Are the Clinical Inferences?

• A cross-over study with 32 patients was assessed for the short-term efficacy and safety of Pancrelipase.

• This study includes patients 12 to 43 years with exocrine pancreatic insufficiency due to cystic fibrosis.

• The final count of patients was limited to 29.

• These patients were randomized to receive 4,000 lipase units/g fat ingested Pancrelipase for five to six days.

• All patients consumed a high-fat diet during the treatment periods.

• The coefficient of fat absorption between Pancrelipase and placebo treatment was determined by a 72-hour stool collection where fat excretion and ingestion were measured.

• The mean coefficient of fat absorption with Pancrelipase is 89 %, whereas 49 % with placebo treatment.