Dyslipidaemias Flashcards
What is the drug class of choice for treating hypercholesterolaemia and moderate hypertriglyceridaemia?
Statins
What lipid-regulating drug is given in addition to statins for severe hypercholesterolemia or hypertriglyceridemia?
Ezetimibe
- oral: 10 mg daily
What drug class is more effective than statins at reducing triglyceride concentration?
Fibrates (e.g. fenofibrate)
What drug would you add to statin therapy if triglycerides remain high even after the LDL-cholesterol concentration has been reduced adequately?
Fenofibrate
- Oral capsules: maximum 200 mg daily with concomitant statin
- Oral tablets: 160 mg daily
Fibrates are more effective than statins in reducing triglyceride concentration
Patients with familial hypercholesterolaemia are at high risk of premature (?)
coronary heart disease
What is the definition of ‘high-intensity statin’?
The dose at which a reduction in LDL-cholesterol of greater than 40% is achieved
What is first-line therapy in all patients with familial hypercholesterolemia?
High-intensity statin
+ lifestyle changes
What is the target reduction of LDL-cholesterol concentration in a patient with familial hypercholesterolemia?
Greater than 50% from baseline
For patients with primary heterozygous familial hypercholesterolaemia who have contra-indications to, or are intolerant of statins, what drug is the used as monotherapy?
Ezetimibe
- Oral: 10 mg daily
For patients with familial hypercholesterolaemia and in whom statins or ezetimibe are inappropriate, what two other drug classes can be considered?
Fibrates (fenofibrate)
Bile acid sequestrant (e.g. colestyramine or colestipol hydrochloride)
Which side effect is a patient taking a combination of statin with a fibrate at increase risk of?
Muscle-related side-effects (including rhabdomyolysis)
Should be used under specialist supervision
Which drug should NOT be combined with a statin because of the very high risk of rhabdomyolysis?
Gemfibrozil
Which two drugs can be considered for patients with primary heterozygous familial hypercholesterolemia whose LDL-cholesterol has NOT been adequately controlled on maximum tolerated lipid-lowering therapy?
Alirocumab
Evolocumab
What reduction of LDL cholesterol would you expect in the patient is taking 20 mg daily dose of atorvastatin?
43%
What reduction of LDL cholesterol would you expect in the patient is taking 80 mg daily dose of atorvastatin?
55%
Why is high-dose simastatin (80mg) NOT considered in the majority of patients?
Increased risk of myopathy
The 80 mg dose should be considered only in patients with severe hypercholesterolaemia and high risk of cardiovascular complications who have not achieved their treatment goals on lower doses, when the benefits are expected to outweigh the potential risks.
(drug?) and (drug?) bind to a pro-protein involved in the regulation of LDL receptors on liver cells; receptor numbers are increased, which results in increased uptake of LDL-cholesterol from the blood.
Alirocumab
Evolocumab
Alirocumab and evolocumab bind to a pro-protein involved in the regulation of (?) receptors on liver cells; receptor numbers are increased, which results in increased uptake of LDL-cholesterol from the blood.
LDL
Alirocumab and evolocumab binds to a pro-protein involved in the regulation of LDL receptors on liver cells; receptor numbers are increased, which results in increased uptake of (?) from the blood.
LDL-cholesterol
What are the two indications for the use of alirocumab?
- Primary hypercholesterolaemia or mixed dyslipidaemia in patients who have not responded adequately to other appropriate measures
- Established atherosclerotic cardiovascular disease
- Subcutaenous injection: Initially 75 mg every 2 weeks; increased if necessary to 150 mg every 2 weeks, alternatively 300 mg every 4 weeks, patients requiring an LDL-C reduction of greater than 60% may be initiated on 150 mg every 2 weeks or 300 mg every 4 weeks, dose adjustments should be made at 4 to 8 weekly intervals.
What are the common side effects of alirocumab?
- Nasal complaints
- Oropharyngeal pain
- Pulmonary reaction
- Skin reactions
Can alirocumab be used during pregnancy?
No unless clinical condition requires treatment
Maternal toxicity in animal studies
What is the route of administration of alirocumab?
Subcutaneous injection
What are the 4 indications for use of evolocumab?
- Primary hypercholesterolaemia or mixed dyslipidaemia in patients who have not responded adequately to other appropriate measures
- Established atherosclerotic cardiovascular disease
- Homozygous familial hypercholesterolemia
- Homozygous familial hypercholesterolemia in patients on apheresis
What is the route of administration of evolocumab?
Subcutaneous injection
What are the common side effects of evolocumab? (6)
- Arthralgia
- Back pain
- Hypersensitivity
- Increased risk of infection
- Nausea
- Skin reactions
Can pregnant women take evolocumab?
No unless essential
Should patients with moderate to severe hepatic impairment use evolocumab?
Use with caution
Risk of reduced efficacy
Name two bile acid sequestrants
Colestipol hydrochloride
Colestyramine
(drug class?) act by binding bile acids, preventing their reabsorption; this promotes hepatic conversion of cholesterol into bile acids; the resultant increased LDL-receptor activity of liver cells increases the clearance of LDL-cholesterol from the plasma.
Bile acid sequestrants
Bile acid sequestrants act by binding bile acids, preventing their (?); this promotes hepatic conversion of cholesterol into bile acids; the resultant increased LDL-receptor activity of liver cells increases the clearance of LDL-cholesterol from the plasma.
reabsorption