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Lipid & Cholesterol Lowering Drugs:
Pitavastatin May Be the Best Statin Option for PLWH
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Taken together, pitavastatin might be an optimum treatment option for adults with HIV-associated dyslipidaemia who have a high risk of cardiovascular disease, and subsequently the preliminary results in abstracts from the INTREPID study are cited in the 2015 National Lipid Association Part 2 recommendations that
Pitavastatin versus pravastatin in adults with HIV-1 infection and dyslipidaemia (INTREPID): 12 week and 52 week results of a phase 4, multicentre, randomised, double-blind, superiority trial
2022 Lancet HIV Aberg et al.
Taken together, pitavastatin might be an optimum treatment option for adults with HIV-associated dyslipidaemia who have a high risk of cardiovascular disease, and subsequently the preliminary results in abstracts from the INTREPID study are cited in the 2015 National Lipid Association Part 2 recommendations that pitavastatin is a preferred statin in the treatment of dyslipidaemia for people living with HIV…..because its metabolism is not cytochrome P450 dependent, pitavastatin can be used in the setting of complex background ART.
The use of statins in the setting of ART has been challenging because of drug interactions, which are sometimes unpredictable, leading to intolerance or reduced efficacy. Protease inhibitors, non-nucleoside reverse transcriptase inhibitors, and most statins are metabolised via the cytochrome P450 (CYP) enzyme system. Simvastatin and lovastatin are contraindicated with protease inhibitors, atorvastatin doses should not exceed 20 mg/day if given with protease inhibitors, and rosuvastatin requires a dose reduction with selected protease inhibitors. Pitavastatin is primarily metabolised by glucuronidation with only marginal metabolism by CYP2C9 and to a lesser extent CYP2C8, and there are no contraindications or dose limitations with pitavastatin and protease inhibitor therapy. Pravastatin is also not dependent on CYP metabolism. Pitavastatin 4 mg and pravastatin 40 mg are both classified as moderate-intensity statins and share similar potency.
At the time of this study, pravastatin was a commonly used drug in the management of dyslipidaemia in people living with HIV, on the basis of drug interaction data in the absence of randomised, double-blind comparative trials of statins in this population.
The REPRIEVE trial (NCT02344290) is investigating the effect of statin therapy (pitavastatin) for the primary prevention of cardiovascular disease in adults with HIV who do not have a clinical indication for taking statins.
The risk for myocardial infarction is 1⋅5-2⋅0 times higher in people with HIV than in those who are uninfected, and dyslipidaemia has been reported in up to 80% of individuals with HIV. Increases in lipid concentrations associated with specific ARTs, notably the protease inhibitors, are less commonly observed with newer medications.
Neither ageing alone nor traditional cardiovascular disease risk factors fully explain the excess cardiovascular risk noted in people with HIV. Possible mechanisms working separately or in combination include chronic immune activation and inflammation caused by the HIV infection itself as well as associated senescence and dysregulation of the immune system.
A unique pathophysiology of atherosclerosis in the setting of HIV highlights the need for tailored primary cardiovascular disease prevention strategies in this population. Regardless of the biological cause of dyslipidaemia, the challenge is how best to manage this disorder in people living with HIV.
Importantly, with respect to safety, there were no significant changes in the variables of insulin resistance for either treatment at week 12 or week 52 in this population, which is at greater risk for incident diabetes. This finding is further evidence that statins differ in their extent of risk for such a side-effect of statin therapy.
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https://www.trihealth.com/institutes-and-services/trihealth-heart-institute/heart-health/heart-medications/lipid-lowering-agents
Cholesterol-Lowering Drugs
https://my.clevelandclinic.org/health/drugs/8744-cholesterol-lowering-drugs
Some people have a genetic predisposition to high blood cholesterol levels. If you're one of them, you may need medication in addition to diet to reduce your cholesterol.
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What types of drugs are used to lower cholesterol?
Your liver produces cholesterol, which you also get from food that comes from animals (such as meat and dairy products.) You might have a genetic issue that leads to high blood cholesterol levels, or your cholesterol might be high due to food choices and lack of physical activity. You can improve cholesterol levels with a healthy diet and exercise, but if your cholesterol level doesn't drop low enough to be healthy, your healthcare provider might prescribe medications to reduce the cholesterol levels.
Cholesterol medications list
Types of cholesterol-lowering drugs include:
• Statins.
• PCSK9 inhibitors.
• Fibric acid derivatives (also called fibrates).
• Bile acid sequestrants (also called bile acid resins).
• Nicotinic acid (also called niacin).
• Selective cholesterol absorption inhibitors.
• Omega-3 fatty acids and fatty acid esters.
• Adenosine triphosphate-citrate lyase (ACL) inhibitors.
Your healthcare provider will discuss these options with you and together you can decide which type of high cholesterol medication, if any, would be best for you.
Statins
Statins are one of the better-known types of cholesterol-lowering drugs. Providers choose these for the majority of people because they work well. Statins decrease cholesterol output by blocking the HMG CoA reductase enzyme that the liver uses to make cholesterol. Statins are also called HMG CoA reductase inhibitors.
Statins also:
• Improve the function of the lining of the blood vessels.
• Reduce inflammation (swelling) and damage.
• Reduce the risk of blood clots by stopping platelets from sticking together.
• Make plaques (fatty deposits) less likely to break away and cause damage.
These additional benefits help prevent cardiovascular disease (CVD) in people who have had events like heart attacks and in people who are at risk.
What are the side effects of statins?
Like any other drugs, statins may produce unwanted side effects. These may include:
• Constipation or nausea.
• Headaches and cold-like symptoms.
• Sore muscles, with or without muscle injury.
• Liver enzyme abnormalities.
• Increased blood glucose levels.
• Reversible memory issues.
If you can't take statins because of the side effects, you're statin-intolerant. With certain statins, you should avoid grapefruit products because they can increase side effects. You should limit the amount of alcohol that you drink because combining alcohol and statin usage can increase your risk of liver damage. You may want to talk with your provider or pharmacist if you're concerned about any other types of interactions.
PCSK9 inhibitors
PCSK9 inhibitors attach to a particular liver cell surface protein, which results in lowered LDL ("bad") cholesterol. This class of drug can be given with statins and is usually for people at high risk of heart disease who have not been able to lower their cholesterol enough in other ways.
What are some possible side effects of PCSK9 inhibitors?
Possible side effects include:
• Pain, including muscle pain (myalgia) and back pain.
• Swelling at the injection site.
• Cold-like symptoms.
Cost may be another drawback as these products can be expensive.
Fibric acid derivatives (fibrates)
Fibric acid derivatives make up another class of cholesterol meds that reduce blood lipid (fat) levels, especially triglycerides. Your body creates triglycerides (fats) from food when you consume calories but don't burn them.
Fibric acid derivatives may also increase the level of HDL, also called the "good" cholesterol, while lowering liver production of LDL, the "bad" cholesterol. People who have severe kidney disease or liver disease should not take fibrates.
What are some possible side effects of fibric acid derivatives?
Possible side effects of fibrates include:
• Constipation or diarrhea.
• Weight loss.
• Bloating, belching or vomiting.
• Stomachache, headache or backache.
• Muscle pain and weakness.
Bile acid sequestrants (also called bile acid resins)
This class of cholesterol medication works inside the intestine by attaching to bile, a greenish fluid made of cholesterol your liver produces to digest food. The binding process means that less cholesterol is available in the body. Resins decrease LDL cholesterol and give a slight boost to HDL cholesterol levels.
What are the possible side effects of bile acid resins?
Possible side effects of bile acid sequestrants include:
• Sore throat, stuffy nose.
• Constipation, diarrhea.
• Weight loss.
• Belching, bloating.
• Nausea, vomiting, stomach pain.
If your high cholesterol medication is a powder, never take it dry. It must always be mixed with at least three to four ounces of liquid such as water, juice or a noncarbonated beverage.
If you take other medications besides these, make sure you take the other drugs one hour before or four hours after taking the bile acid resin.
Selective cholesterol absorption inhibitors
This class of medication (ezetimibe) works in your intestine to stop your body from absorbing cholesterol. These inhibitors reduce LDL cholesterol, but may also reduce triglycerides and increase HDL "good" cholesterol. They can be combined with statins.
Possible side effects include:
• Diarrhea.
• Fatigue.
• Joint pain.
Nicotinic acid
Nicotinic acid, also called niacin, is a B-complex vitamin. You can get over-the-counter versions of this, but some versions are prescription only. Niacin decreases LDL cholesterol and triglycerides and increases HDL. If you have gout or severe liver disease, you should not take niacin.
What are the possible side effects of niacin?
The main side effect of niacin is flushing of the face and upper body, which might be lessened if you take it with meals. You might have less flushing if you take aspirin about 30 minutes before taking niacin.
Other side effects include:br clear="all" />
• Skin issues, such as itching or tingling.
• Headache.
• Stomach upset.
• Can lead to increased blood sugars.
• Coughing.
Omega-3 fatty acid esters and polyunsaturated fatty acids (PUFAs)
These kinds of drugs, used to lower triglycerides, are commonly called fish oils. Some products are available as over-the-counter items, while others are prescription-only (ethyl eicosapentaenoic acid). Here are two things to consider: Fish oils might interfere with other medications, and some people are allergic to fish and shellfish.
What are the possible side effects of omega-3 products?
Possible side effects of omega-3 products include:
• Belching.
• Skin issues like rash or itching.
• Gas.
• Fishy taste.
• Increased bleeding time.
Adenosine triphosphate-citric lyase (ACL) inhibitors
Bempedoic acid works in the liver to slow down cholesterol production. It should be taken with statin medications, but you'll need to limit your dosage if you take it with simvastatin or pravastatin.
What are the possible side effects of bempedoic acid?
Some possible side effects of bempedoic acid include:
• Upper respiratory infection.
• Stomach, back or muscle pain.
• Increased levels of uric acid.
• Tendon injury.
What about using red rice yeast or plant stanols (phytosterols) instead of prescription drugs to lower cholesterol?
Many people say they prefer to take "natural" medicines over prescription drugs. However, just because something is natural doesn't mean that it's safe. The United States doesn't regulate supplements as closely as medicines. Supplements can also interfere in dangerous ways with medications that you already take.
However, red rice yeast extract does contain the same chemical that's in certain prescription statins like lovastatin. In some cases, you and your healthcare provider might agree that you should try the supplement with monitoring.
Plant stanols are another nonprescription choice for lowering cholesterol. Plant stanols stop your body from absorbing cholesterol in your intestines. You can buy capsules or get plant stanols in some margarine substitutes.
How to take your cholesterol-lowering medicines
When you're taking medicines, it's important to follow your healthcare provider's advice carefully. If you don't take medicines exactly as prescribed, they can harm you. For example, you could unknowingly counteract one medicine by taking it with another one. Medicines can make you feel sick or dizzy if not taken properly.
Taking your cholesterol meds correctly
Medicine can only help you reduce cholesterol if you take it correctly.
• You should take all medicines the way your provider instructs you to do.
• Don't decrease your medication dosage to save money. You must take the full amount to get the full benefits. If your medicines are too expensive, ask your provider or pharmacist about finding financial assistance. Some companies provide discounts for certain medications.
• Don't hesitate to let your provider know if you don't think the medication is working or if you have side effects of cholesterol medicine that concern you.
Working with your pharmacy
Your pharmacy can be your partner in ensuring you're sticking with your cholesterol meds.
• Fill your prescriptions regularly, and don't wait until you're out of something to get a refill.
• You can ask your healthcare provider or pharmacist any questions you have.
• Let them know if you have problems getting to the pharmacy to pick up your medicines or if the instructions are too complicated.
• If you have trouble understanding your provider or pharmacist, ask a friend or family member to be with you when you ask questions. You need to know what medicines you take and what they do.
Keeping track of your high cholesterol medication
There are now many ways to keep track of medication schedules.
• It might help to have a routine of taking your medicines at the same time every day.
• You can have a pillbox marked with the days of the week that you fill at the start of the week.
• Some people keep a medication calendar or journal, marking down the time, date and dose.
• Make use of smartphone apps and pillboxes with alarms you can set.
• If you forget to take a dose, take it as soon as you remember. However, if it's almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Don't take two doses to make up for the dose you missed.
When traveling, keep your medicines with you so you can take them as scheduled. On longer trips, take an extra week's supply of medicines and copies of your prescriptions in case you need to get a refill.
Always discuss any new medication with your provider, including over-the-counter drugs and herbal or dietary supplements. Your high cholesterol medication dose might have to be adjusted. Make sure you tell your dentist and other providers what medications you're taking, especially before having surgery with a general anesthetic.
All of your cholesterol meds will be more effective if you continue to follow a low cholesterol diet. Your healthcare provider may be able to refer you to a dietitian for help in designing a diet especially for you, such as a Mediterranean diet, and encouraging you to stay with it. Exercise also helps with cholesterol levels.
A note from Cleveland Clinic
You may need medications to improve your cholesterol numbers. There are several options, but many of them will work better if you eat healthily and exercise. Remember to discuss any new medication with your provider. This includes over-the-counter products like herbs or dietary supplements.
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