Pronunciation: di-JES-tiv EN-zimes
Class: Digestive enzymes

Trade Names

Bio-Zyme
- Tablets, oral lipase 3,250 units/protease 40,625 units/amylase 40,625 units

Creon
- Capsules, delayed-release, oral lipase 6,000 units/protease 19,000 units/amylase 30,000 units
- Capsules, delayed-release, oral lipase 12,000 units/protease 38,000 units/amylase 60,000 units
- Capsules, delayed-release, oral lipase 24,000 units/protease 76,000 units/amylase 120,000 units

Hi-Vegi-Lip
- Tablets, oral lipase 4,800 units/protease 60,000 units/amylase 60,000 units (pancreatin 600 mg)

Pancreatin Quadruple Strength
- Capsules, oral lipase 4,000 units/protease 50,000 units/amylase 50,000 units

Pancreaze
- Capsules, delayed-release, oral lipase 4,200 units/protease 10,000 units/amylase 17,500 units
- Capsules, delayed-release, oral lipase 10,500 units/protease 25,000 units/amylase 43,750 units
- Capsules, delayed-release, oral lipase 16,800 units/protease 40,000 units/amylase 70,000 units
- Capsules, delayed-release, oral lipase 21,000 units/protease 37,000 units/amylase 61,000 units

Pancrelipase
- Capsules, delayed-release, oral lipase 5,000 units/protease 17,000 units/amylase 27,000 units

Tyler Similase Jr
- Capsules, oral lipase 465 units/protease 7,250 units/amylase 3,350 units

Tyler Panplex 2-Phase
- Tablets, oral lipase 1,008 units/protease 12,600 units/amylase 12,600 units

Zenpep
- Capsules, delayed-release, oral lipase 5,000 units/protease 17,000 units/amylase 27,000 units
- Capsules, delayed-release, oral lipase 10,000 units/protease 34,000 units/amylase 55,000 units
- Capsules, delayed-release, oral lipase 15,000 units/protease 51,000 units/amylase 82,000 units
- Capsules, delayed-release, oral lipase 20,000 units/protease 68,000 units/amylase 109,000 units

Cotazym (Canada)
Creon 5 Minimicrospheres (Canada)
Creon 10 Minimicrospheres (Canada)
Creon 20 Minimicrospheres (Canada)
Creon 25 Minimicrospheres (Canada)

Pharmacology

Enzymes catalyze the hydrolysis of fats to monoglyceride, glycerol, and free fatty acids; proteins into peptides and amino acids; and starches into dextrins and short-chain sugars in the duodenum and proximal small intestine.

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Pharmacokinetics

Absorption

Pancreatic enzymes are enteric-coated to minimize destruction or inactivation in gastric acid. Most of the enzymes are released at an approximate pH of 5.5 or greater. Pancreatic enzymes are not absorbed from the GI tract in appreciable amounts.

Indications and Usage

Treatment of exocrine pancreatic insufficiency caused by cystic fibrosis, chronic pancreatitis, pancreatectomy, or other conditions (all products except Hi-Vegi-Lip ); as a digestive enzyme aid ( Hi-Vegi-Lip only).

Contraindications

None well documented.

Dosage and Administration

Pancreatic insufficiency
Adults and Children 4 y and older

PO Initial dose is lipase 500 units/kg per meal (max, lipase 2,500 units/kg per meal [or less than lipase 10,000 units/kg per day] or lipase 4,000 units/g fat ingested per day). If symptoms and signs of steatorrhea persist, the dosage may be increased.

Enzyme doses expressed as lipase units/kg per meal should be decreased in older patients because they weigh more but tend to ingest less fat per kg of body weight.

Adults with chronic pancreatitis or pancreatectomy ( Creon only)

PO Lipase 72,000 units per meal while consuming at least 100 g of fat per day. Lower starting dose recommended is lipase 500 units/kg per meal.

Older than 12 mo and younger than 4 y

PO Initial dosage is lipase 1,000 units/kg per meal (max, lipase 2,500 units/kg per meal [or less than lipase 10,000 units/kg per day] or lipase 4,000 units/g fat ingested per day). If symptoms and signs of steatorrhea persist, the dosage may be increased.

Infants up to 12 mo

PO Lipase 2,000 to 4,000 units per 120 mL of formula or per breast-feeding. Administer immediately prior to each feeding.

Dietary Supplement
Children Tyler Similase Jr

PO 1 to 2 capsules at the beginning of each meal.

Adults Bio-Zyme

PO 2 tablets before each meal, up to 12 tablets/day.

Hi-Vegi-Lip , Pancreatin Quadruple Strength

PO 1 tablet or capsule daily preferably with each meal.

Tyler Panplex 2-Phase

PO 1 to 2 tablets 3 times daily with meals.

General Advice

• Initiate therapy at the lowest recommended dose and gradually increase. Individualize the dosage based on clinical symptoms, the degree of steatorrhea present, and the fat content of the diet.
• Advise patients not to crush or chew tablets, capsules, or capsule contents. Swallow whole.
• Give with meals or snacks with sufficient liquid.
• If patient has difficulty swallowing capsule, open capsule and add to a small amount of acidic soft food with a pH of 4.5 or less (eg, commercially available bananas, pears, or applesauce) at room temperature. Have patient swallow immediately without crushing or chewing. Follow with a glass of juice or water. Care should be taken to ensure that no drug is retained in the mouth.
• For infants up to 12 mo of age, contents of the capsules may also be administered directly to the mouth or with a small amount of acidic soft food. Do not mix contents of the capsules in formula or breast milk.
• Usually, half of the prescribed dose for an individualized meal should be given with each snack. The total daily dose should reflect approximately 3 meals plus 2 or 3 snacks per day.
• Pancrelipase products are not interchangeable.

Storage/Stability

Store between 68° and 77°F. Do not store above 77°F. Protect from heat and moisture. For Creon , temperature excursions are permitted between 77° and 104°F for up to 30 days; discard if exposed to higher temperature and moisture conditions higher than 70%.

Drug Interactions

None well documented.

Adverse Reactions

The following adverse reactions are compiled from the different pancrelipase products. The highest percentages are listed.

CNS

Headache (15%); dizziness (4%).

Dermatologic

Skin disorders (eg, pruritus, rash, urticaria) (postmarketing).

EENT

Blurred vision (postmarketing).

GI

Vomiting (6%); abdominal pain, abnormal feces, flatulence, frequent bowel movements (4%); constipation, distal intestinal obstruction, fibrosing colonopathy, nausea (postmarketing).

Hypersensitivity

Severe allergic reactions, including anaphylaxis, asthma, hives, and pruritus (postmarketing).

Lab Tests

Asymptomatic elevations of liver enzymes (postmarketing).

Metabolic-Nutritional

Hyperglycemia (8%); hypoglycemia (4%).

Musculoskeletal

Muscle spasm, myalgia (postmarketing).

Respiratory

Cough (6%); nasopharyngitis (4%).

Miscellaneous

Contusion, early satiety (6%); recurrence of preexisting carcinoma (postmarketing).

Precautions

Monitor Monitor the degree of steatorrhea present and clinical symptoms.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Doses exceeding lipase 6,000 units/kg per meal have been associated with fibrosing colonopathy and colonic strictures in children younger than 12 y.

Hypersensitivity

Use with caution in patients with allergy to proteins of porcine origin. Rare, severe allergic reactions, including anaphylaxis, asthma, hives, and pruritus, have been reported.

Renal Function

Use with caution.

Fibrosing colonopathy

Has been reported and most commonly in children with cystic fibrosis. Monitor these patients closely because they may be at risk of stricture formation.

Hyperuricemia

Use with caution in patients with gout or hyperuricemia because of the risk of increased blood uric acid levels.

Irritation to oral mucosa

Because irritation of the oral mucosa can occur, make sure none of the drug is retained in the mouth.

Viral transmission

Some of the products are sourced from pancreatic tissue from swine used for food consumption; therefore, there is a theoretical risk for transmission of viral disease, including diseases caused by novel or unidentified viruses.

Overdosage

Symptoms

Abdominal pain, elevated AST, elevated ALT, elevated serum phosphate, elevated hematocrit, hyperuricosuria, hyperuricemia.

Patient Information

• Tell patient not to change brands without notifying their health care provider. Products are not bioequivalent.
• Advise patient to take with meals or snacks and with sufficient liquid.
• Advise patient to not crush or chew the tablets, capsule, or capsule contents, but to swallow whole. The capsule may be opened and the contents added to soft, acidic foods.
• Advise patient to follow dosing instructions carefully, as doses exceeding lipase 6,000 units/kg per meal have been associated with colonic strictures in children younger than 12 y.
• Advise patient to contact their health care provider immediately if symptoms of an allergic reaction (eg, anaphylaxis, asthma, hives, pruritus) develop.
• Instruct patients to notify their health care provider if they are pregnant, thinking of becoming pregnant, or are breast-feeding during therapy.

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