Pharmacology
Mechanism of Action
Induces hyperketonemia to provide an alternative energy substrate to glucose in the brain of patients with Alzheimer disease
Pharmacokinetics/Pharmacodynamics
Metabolism
Processed by lipases in the gut to medium-chain fatty acids (MCFAs); MCFAs under obligate oxidation in the liver and beta-oxidation in the liver mitochondria to form acetyl-CoA and acetoacetyl-CoA. Acetyl-CoA and acetoacetyl-CoA when in excess are combined to form 3-hydroxy-3-methyl-glutaryl-CoA (HMG-CoA) which forms acetoacetate and beta-hydroxybutyrate (ie, ketone bodies) by HMG-CoA lyase.
Use: Labeled Indications
Alzheimer disease: For clinical dietary management of the metabolic processes associated with mild to moderate Alzheimer disease (AD). Caprylidene is a medical food containing a proprietary formulation of medium-chain triglycerides (MCTs), specifically caprylic triglyceride.
Note: A medical food is formulated to be administered enterally under the supervision of a physician and is intended for the specific dietary management of a disease or condition for which distinctive nutritional requirements are established by medical evaluation. Medical foods are not drugs and, therefore, are not subject to any FDA regulatory requirements that specifically apply to drugs (eg, premarket review or approval or proof of safety and efficacy).
Contraindications
Allergy to milk or soy
Dosage and Administration
Dosing: Adult
Alzheimer disease (AD): Oral: Initial: 10 g once daily for 2 days; increase dose in 10 g increments every 2 days until reaching 40 g once daily on day 7; titrate slower if the patient experiences adverse events; Maintenance: 40 g once daily
Note: If adverse events occur, discontinue caprylidene until symptoms resolve (generally within 2 to 3 days). Over-the-counter medications such as simethicone, antacids, and antidiarrheals may be useful for treating mild to moderate GI side effects. Restart caprylidene with the initial dose.
Administration
Oral: The contents of each packet of caprylidene should be added to 4 to 8 oz (118 to 236 mL) of water or other liquids, shaken or blended until fully mixed, and consumed 15 to 30 minutes after a full meal (preferably breakfast or lunch). Consumption following meals containing fats and proteins or adding ice to the drink may slow the digestion of MCTs and reduce the likelihood of developing GI symptoms; tolerability can also be improved if the drink is sipped over 30 minutes instead of consumed all at once.
Storage
Store at 15°C to 30°C (59°F to 86°F), sealed and protected from light and moisture. Reconstituted product may be refrigerated and stored for up to 24 hours. Refrigerated product should be re-blended and thoroughly mixed prior to consumption.
Drug Interactions
There are no known significant interactions.
Adverse Reactions
>10%: Gastrointestinal: Diarrhea (10% to 24%), nausea (10% to 20%), abdominal distention (17%), flatulence (15% to 17%)
1% to 10%:
Cardiovascular: Hypertension (5%)
Central nervous system: Dizziness (7%), headache (6%), fatigue (4%), pain (4%)
Gastrointestinal: Abdominal pain (10%), dyspepsia (9%)
Respiratory: Cough (4%), rhinitis (4%)
<1%, postmarketing, and/or case reports: Abdominal distress, GI inflammation (exacerbation), increased blood urea nitrogen, increased serum creatinine, increased serum triglycerides, increased uric acid, syncope
Warnings/Precautions
Concerns related to adverse effects:
- Ketoacidosis: Use with caution in patients at risk for ketoacidosis such as patients with a history of alcohol abuse and poorly controlled diabetes.
Disease-related concerns:
- Cardiovascular disease: Use with caution in patients with a history of bradycardia, hypotension, or among patients taking medications that may induce these effects (eg, antihypertensives and cholinesterase inhibitors); fainting and dizziness has been infrequently reported among these groups. Use a gradual dose titration in patients at risk and emphasize administration after meals.
- Gastrointestinal disease: Gastrointestinal (GI) adverse effects (eg, abdominal cramping, diarrhea, dyspepsia) may result due to the rapid hydrolysis of medium-chain triglycerides in the gut and the resultant accumulation of high concentration of medium-chain fatty acids in the small intestine. Severe episodic diarrhea may occur with overusage. Use with caution in patients with a history of GI inflammatory conditions such as irritable bowel syndrome, diverticular disease, chronic gastritis, and severe gastroesophageal reflux disease. OTC medications such as simethicone, antacids, and antidiarrheals may be useful for treating mild to moderate GI effects; advise patients to see healthcare provider if symptoms persist.
- Metabolic syndrome: Elevated triglyceride values have been observed in patients with probable metabolic syndrome. Periodically monitor triglyceride levels in patients who meet at least 3 of the following 5 criteria indicative of metabolic syndrome: Elevated waist circumference (≥40 inches in men, ≥35 inches in women), blood pressure ≥130/85 mm Hg, triglyceride ≥150 mg/dL, reduced fasting HDL (<40 mg/dL in men, <50 mg/dL in women), and fasting glucose ≥100 mg/dL.
- Renal impairment: Use with caution in patients with a history of renal dysfunction; mild increases in blood urea nitrogen (BUN), creatinine, or uric acid were reported in clinical trials. Routine renal function monitoring is recommended in patients with a history of renal dysfunction.
Dosage form specific issues:
- Component ingredients: Product contains caseinate (milk-derived protein), whey (milk), and lecithin (soy). Do not use in patients allergic to these component ingredients or milk or soy.
Monitoring Parameters
Periodic triglyceride levels in patients who meet criteria indicative of metabolic syndrome; routine renal function tests in patients with a history of renal dysfunction; periodic monitoring of hepatic function in patients with hepatic cirrhosis
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience diarrhea, abdominal cramps, nausea, passing gas, or headache. Have patient report immediately to prescriber severe dizziness or passing out (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
