21.4 Cholesterol Absorption Inhibitors

Cholesterol absorption inhibitors are game-changers in managing high cholesterol. They work by blocking the uptake of cholesterol in your gut, reducing how much gets into your bloodstream. This clever trick helps lower your LDL (bad) cholesterol levels.

These meds are often used alongside statins or on their own if statins don't agree with you. While they can cause some tummy troubles, they're generally well-tolerated. Remember, they're just one part of the puzzle - a healthy diet and exercise are still key players in keeping your cholesterol in check.

Cholesterol Absorption Inhibitors

Key features and mechanism of action

• Cholesterol absorption inhibitors (CAIs) are lipid-lowering medications that selectively inhibit cholesterol absorption in the small intestine, reducing the amount absorbed from diet and bile
• CAIs target the Niemann-Pick C1-Like 1 (NPC1L1) protein responsible for cholesterol uptake from the intestinal lumen, decreasing absorption into enterocytes and delivery to the liver
• Decreased cholesterol absorption leads to compensatory increase in LDL receptor expression, enhancing LDL receptor-mediated clearance of LDL cholesterol from the bloodstream and ultimately lowering serum LDL cholesterol levels

Indications, side effects, and drug interactions

• Primary indications: adjunct to diet and exercise for reducing elevated LDL cholesterol in primary hyperlipidemia, combination therapy with statins for additional LDL cholesterol lowering, monotherapy for statin-intolerant patients or those with contraindications
• Common side effects: gastrointestinal disturbances (diarrhea, abdominal pain, flatulence), headache, myalgia, upper respiratory tract infections
• Potential drug interactions:
  • Cyclosporine: CAIs may decrease cyclosporine absorption and blood levels, requiring close monitoring
  • Fat-soluble vitamins (A, D, E, K): CAIs may reduce absorption, potentially necessitating supplementation or monitoring
  • Warfarin: CAIs may interfere with warfarin absorption, affecting INR and requiring close monitoring when initiating or discontinuing CAIs

Nursing considerations

• Patient assessment: obtain complete medical history (prior lipid-lowering therapy, medication allergies), assess baseline liver function tests and lipid profile before initiating therapy
• Dosing and administration: administer CAIs orally with or without food as prescribed, encourage same time daily dosing for optimal adherence
• Monitoring: regularly monitor lipid profile to assess therapeutic response and adjust therapy, periodically evaluate liver function tests for potential hepatic adverse effects
• Patient education: emphasize adherence to prescribed dosing regimen, advise reporting of unusual symptoms or side effects
• Lifestyle modifications: encourage heart-healthy diet low in saturated fats and cholesterol, promote regular physical activity and maintaining healthy body weight, address other cardiovascular risk factors (smoking cessation, blood pressure control)

Patient education plan

• Medication purpose: explain CAIs lower LDL cholesterol by reducing intestinal cholesterol absorption, used with healthy diet and exercise to manage hyperlipidemia
• Proper administration: instruct taking medication exactly as prescribed at same time daily, continue even if feeling well as hyperlipidemia is chronic
• Potential side effects and management: inform of common side effects (gastrointestinal disturbances, headache), encourage reporting severe or persistent side effects
• Drug interactions and precautions: advise informing healthcare provider about all medications, supplements, and herbal products, caution about reduced absorption of fat-soluble vitamins and cyclosporine
• Importance of follow-up: stress regular follow-up visits to monitor lipid levels and assess therapeutic response, encourage keeping all scheduled appointments and discussing concerns
• Lifestyle modifications: educate on significance of heart-healthy diet, regular exercise, maintaining healthy weight, provide resources and support for positive lifestyle changes to enhance CAI therapy effectiveness