Statin-induced Myopathy

-
 Statins are commonly used drugs for lowering LDL/bad cholesterol and preventing the risk of atherosclerosis, heart disease, and stroke. Statins are also known as HMG-Coenzyme A reductase inhibitors. They work by inhibiting the rate-limiting step in cholesterol synthesis, i.e., by inhibiting the enzyme HMG-Coenzyme A reductase (needed by the liver to produce cholesterol). 

There are different types of Statins available (Lovastatin, Simvastatin, Pravastatin, Atorvastatin, Rosuvastatin, and Fluvastatin). The most potent statin is Rosuvastatin, followed by Atorvastatin.  

The CYP3A4 metabolizes Atorvastatin, Simvastatin, and Lovastatin. 

The CYP2C9 metabolizes Rosuvastatin and Fluvastatin. 

Pravastatin is not metabolized by the CYP enzymes. 


Despite the numerous benefits of Statins, there are some risks involved with the use of statins as well. One of them is Statin-induced myopathy. It is a muscle disorder characterized by muscle pain, weakness, and muscle cramps, with symptoms starting after the initiation of Statin use. If left untreated, it can progress to Rhabdomyolysis - a medical emergency in which damaged muscle breaks down rapidly, releasing harmful proteins in the bloodstream and leading to kidney damage. The management of Statin-induced myopathy includes immediate reporting of symptoms of muscle pain, weakness, and cramps, which begin after starting statins to your healthcare provider. This is followed by the analysis of Creatine Kinase levels in the blood. CK levels give an estimate of the intensity of muscle damage. Based on the CK levels, the dose of statins may be reduced, switched to a different statin, or statins may be stopped temporarily, and CK levels are monitored. The Statins may be reintroduced at a lower dose after CK levels have returned to normal, or non-statin medications may be used to lower cholesterol.


Some individuals may be at a higher risk for Statin-induced myopathy, i.e., females, the elderly, individuals with a small body frame, individuals with renal disease, diabetes, and hypothyroidism. Some drug-drug interactions may also increase the risk of statin-induced myopathy. For example, using Grapefruit juice (CYP3A4 inhibitor) along with Atorvastatin, Simvastatin, and Lovastatin (metabolized by CYP3A4) may reduce the metabolism of these statins and increase the concentration of Statins, thereby increasing the risk of statin-induced myopathy. Similarly, it is best to avoid the use of statins with Fibrates (Gemfibrozil) and other CYP3A4 inhibitors(Grapefruit juice, Amiodarone, Azoles, Ritonavir, Clarithyromycin, Erythromycin, Verapamil, Diltiazem) and CYP2C9 inhibitors (Amiodarone, Fluconazole, Metronidazole, Sulfamethoxazole).




Comments

Post a Comment

Popular posts from this blog

Popping Painkillers. Is it safe?

-
Painkillers are the most commonly used OTC drugs. Though they are considered safe enough to be dispensed OTC (Over-the-counter) without needing a prescription, they certainly have side effects and long-term toxicity. Painkillers belong to the class of drugs known as NSAIDs (Non- steroidal anti-inflammatory drugs). These drugs treat fever, and pain and reduce inflammation in the body. NSAIDs/ Painkillers work by preventing the body from producing Prostaglandins. Prostaglandins cause inflammation and pain by dilating blood vessels and raising temperature.  Many people doubt how painkillers know where the pain is, painkillers like NSAIDs block the Cox enzyme thereby blocking the prostaglandins, and prostaglandins send signals of pain to the brain. Thus by blocking prostaglandins, pain signals to the brain are blocked, and all kinds of pain are reduced. Other types of drugs used for pain include narcotics and anesthesia. These drugs change the brain’s perception of pain, but today we a...
Read more

Gut Health and its impact on Mental health

-
We have all heard the statement "You are what you eat". This isn't just a blanket statement, but the impact of food on gut health and thereby its impact on mental health, emotions, and overall well-being is tremendous. If you've ever had a gut-wrenching feeling or have felt butterflies in your stomach, you know there is a connection between emotions and the gut. This is why you may feel nauseous in stressful situations or have diarrhea before an important exam or interview. This connection between the gut and brain is called the Gut-Brain axis. It is a connection between the CNS of the brain and the Enteric nervous system (ENS) of the gut. The gut is also known as the second brain. This connection is evident in diseases like Irritable Bowel Syndrome (IBS) and Inflammatory Bowel Disease (IBD) where psychological stress or anxiety can worsen the gut symptoms. On the other hand, studies have found that anxiety, depression, and autism spectrum disorders are linked with Ga...
Read more

PCOS Epidemic

-
  PCOS is the abbreviation of Polycystic ovary syndrome. It is when the ovaries produce too much androgen leading to hormonal imbalance in women.  As a result, women with PCOS experience irregular menstrual cycles, missed periods, no ovulation, or unpredictable ovulation. The ovaries develop small fluid-filled sacs called cysts which contain the undeveloped follicles. These follicles mature and release egg - ovulation. Thus there is no ovulation or unpredictable ovulation with PCOS. In addition to this PCOS also causes acne, weight gain, increased facial and body hair, fatigue, hair fall, mood swings, pigmentation of skin, etc. Insulin resistance is also seen in PCOS, and it can increase the risk of diabetes, hypertension, and cardiovascular diseases. PCOS can happen in young girls as well, anytime after puberty. PCOS affects about 3.7%-22.5% i.e. 1.3 crore to 7.9 crore women in India and 4%-20% i.e. 8 crore to 40 crore women worldwide. These are huge numbers. There is an ongo...
Read more