(atorvastatin · DailyMed)
Atorem 20
Atorvastatin Calcium eq to Atorvastatin 20 mg,Calcium Carbonate gm/ml,Lactose Monohydrate gm/ml,Magnesium Stearate gm/ml,Microcrystalline Cellulose (Avicel PH 101) gm/ml,Microcrystalline cellulose gm/ml,Polysorbate 80 gm/ml,Purified Water gm/270ml
What it does
Atorvastatin is a medication used to lower cholesterol levels in the blood.
Commonly used for: high cholesterol (hyperlipidemia), prevention of heart disease, prevention of stroke
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Answers come only from this medicine's registration record, BNF monograph and interaction data - not medical advice.
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Sourcing - Kenya onlyRegistration & product details
Source: Tanzania Medicines and Medical Devices Authority · fetched 2026-03-11 23:48:04 · updated 2026-09-24 03:00:47
Drug Interactions
127Pharmacodynamic Warnings
Atorvastatin appears in TABLE 1: Drugs that cause hepatotoxicity
Severe (7)
Atorvastatin - increases exposure
Darolutamide is predicted to increase the exposure to statins (atorvastatin, fluvastatin, rosuvastatin). Avoid.
Atorvastatin - increases exposure
Posaconazole is predicted to increase the exposure to statins (atorvastatin). Avoid.
Atorvastatin - increases exposure
Tedizolid is predicted to increase the exposure to statins (atorvastatin, fluvastatin, rosuvastatin). Avoid.
Statins - increases exposure
Darolutamide is predicted to increase the exposure to statins (atorvastatin, fluvastatin, rosuvastatin). Avoid.
Statins - increases exposure
Posaconazole is predicted to increase the exposure to statins (atorvastatin). Avoid.
Statins - increases exposure
Tedizolid is predicted to increase the exposure to statins (atorvastatin, fluvastatin, rosuvastatin). Avoid.
Statins - increases exposure
Voxilaprevir with sofosbuvir and velpatasvir markedly increases the exposure to statins (rosuvastatin). Avoid.
Moderate (40)
Atorvastatin - increases exposure
Amiodarone is predicted to increase the exposure to statins (atorvastatin). Monitor and adjust dose.
Atorvastatin - increases exposure
Dronedarone slightly increases the exposure to statins (atorvastatin). Monitor and adjust dose.
Atorvastatin - decreases exposure
Carbamazepine is predicted to decrease the exposure to statins (atorvastatin). Monitor and adjust dose. Also see TABLE 1 p. 1517.
Atorvastatin - decreases exposure
Eslicarbazepine is predicted to decrease the exposure to statins (atorvastatin). Monitor and adjust dose.
Atorvastatin - increases exposure
Fluconazole is predicted to increase the exposure to statins (atorvastatin, simvastatin). Monitor and adjust dose. Also see TABLE 1 p. 1517.
Unknown (80)
Aliskiren - increases exposure
Atorvastatin slightly to moderately increases the exposure to aliskiren.
Atorvastatin - decreases exposure
Apalutamide is predicted to decrease the exposure to statins (atorvastatin).
Atorvastatin - decreases exposure
Enzalutamide is predicted to decrease the exposure to statins (atorvastatin, simvastatin).
Atorvastatin - decreases exposure
Phenytoin moderately decreases the exposure to statins (atorvastatin).
Atorvastatin - decreases exposure
Oxcarbazepine is predicted to decrease the exposure to statins (atorvastatin, simvastatin).
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact
About atorvastatin
Atorvastatin is a medication used to lower cholesterol levels in the blood.
What it treats
- high cholesterol (hyperlipidemia)
- prevention of heart disease
- prevention of stroke
How it works
Atorvastatin works by blocking a substance your body needs to make cholesterol, which helps reduce the amount of cholesterol in your blood.
Who it's for
It is suitable for adults who have high cholesterol or are at risk of heart disease.
Drug class
Statins
Cautions
- • Be cautious if you are taking other medications that can harm the liver.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About carbonate
Carbonate is used to help manage acidity in the stomach and can be found in various over-the-counter products.
What it treats
- stomach acidity
- indigestion
- heartburn
How it works
Carbonate helps neutralize stomach acid, providing relief from discomfort caused by excess acidity.
Who it's for
Adults and children experiencing symptoms of stomach acidity or indigestion.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About cellulose
Cellulose is a type of fiber that helps with digestion and promotes bowel health.
What it treats
- constipation
- irregular bowel movements
How it works
Cellulose adds bulk to the stool, making it easier to pass through the intestines.
Who it's for
Suitable for people looking to improve their digestive health.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About lactose
Lactose is a sugar found in milk and dairy products. It is often used as an excipient in medications.
What it treats
- lactose intolerance
- as a filler in tablets and capsules
How it works
Lactose helps improve the texture and stability of medications and is sometimes used as a sweetener.
Who it's for
Individuals who require lactose as part of their medication or those who consume dairy products.
Cautions
- • May cause digestive issues in people with lactose intolerance.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About microcrystalline
Microcrystalline is a type of substance often used in medicines to help with various health issues. It is commonly used as a filler or binder in tablets and capsules.
What it treats
- stomach issues
- constipation
- weight management
How it works
It helps to improve the texture of medicines and can assist in the absorption of other ingredients in the body.
Who it's for
Adults and children who need help with specific health conditions, as directed by a healthcare professional.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About polysorbate
Polysorbate is a substance often used as an emulsifier, helping to mix ingredients that usually don't blend well together in medications and food products.
What it treats
- used in various medications and food products to stabilize mixtures
How it works
It helps to keep ingredients mixed evenly, preventing separation and improving texture.
Who it's for
Suitable for individuals who need products containing polysorbate for various health or dietary reasons.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About purified
Purified ingredients are often used in various medicines to ensure safety and effectiveness by removing impurities.
What it treats
- various medical conditions
How it works
Purified ingredients help in delivering the intended effects of the medicine without the risk of contaminants.
Who it's for
People who need medications with safe and effective ingredients.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Atorvastatin
BNF-referencedAtorvastatin is a statin medication used to lower cholesterol levels and reduce the risk of cardiovascular disease. It works by inhibiting HMG-CoA reductase, an enzyme involved in the synthesis of cholesterol in the liver.
Indications
- Hyperlipidaemia
- Primary prevention of cardiovascular disease
- Secondary prevention of cardiovascular events
Dosage
Children: Refer to the BNF for Children for specific dosing information.
Adults: Initial dose is typically 10-20 mg once daily, which can be adjusted based on lipid levels and tolerability. Maximum dose is 80 mg once daily.
Mechanism of action
Atorvastatin competitively inhibits HMG-CoA reductase, leading to decreased cholesterol synthesis and increased uptake of LDL cholesterol from the blood.
Pharmacodynamics
Atorvastatin reduces total cholesterol, LDL cholesterol, and triglycerides while increasing HDL cholesterol. The effects are dose-dependent, and it may also provide vascular protection.
Pharmacokinetics
Atorvastatin is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1 to 2 hours. It undergoes extensive first-pass metabolism in the liver, primarily by CYP3A4. The elimination half-life is approximately 14 hours, and it is excreted mainly in bile.
Contra-indications
- Active liver disease
- Unexplained persistent elevations in serum transaminases
- Pregnancy
Adverse effects
- Myopathy
- Rhabdomyolysis
- Hepatotoxicity
- Severe cutaneous adverse reactions (SCARs)
- Hypoglycaemia
- Peripheral oedema
- Cough
- Dyspnoea
- Weight loss
Interactions
- darolutamide: Severe (increases exposure)
- posaconazole: Severe (increases exposure)
- tedizolid: Severe (increases exposure)
- amiodarone: Moderate (increases exposure)
- dronedarone: Moderate (increases exposure)
- carbamazepine: Moderate (decreases exposure)
- eslicarbazepine: Moderate (decreases exposure)
- fluconazole: Moderate (increases exposure)
- diltiazem: Moderate (increases exposure)
- cobicistat: Moderate (increases exposure)
Precautions
- Caution in patients with a history of haemorrhagic stroke
- Caution in hepatic impairment
- Patient counselling advised for muscle effects
Pregnancy
Manufacturer advises against use due to potential risk of fetal congenital anomalies.
Breast-feeding
Manufacturer advises to avoid; no information available.
Storage
Store in a cool, dry place away from direct sunlight.
Formulations
- Atorvastatin 10 mg tablets
- Atorvastatin 20 mg tablets
- Atorvastatin 30 mg tablets
- Atorvastatin 60 mg tablets
- Atorvastatin 80 mg tablets
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: carbonate
BNF-referencedCarbonate is a polyatomic ion with the molecular formula CO3^2-. It plays a critical role in various biological processes, including the regulation of pH in biological systems and the formation of bicarbonate, which is essential for maintaining acid-base balance. Carbonates are commonly found in nature and are involved in buffering systems in blood and other bodily fluids.
Mechanism of action
Carbonate ions participate in buffering reactions that help maintain pH homeostasis in biological systems. They can react with acids to form bicarbonate and carbon dioxide, thus neutralizing excess acidity in the body. This mechanism is crucial in processes such as respiration and metabolism.
Pharmacodynamics
As a buffer, carbonate helps to stabilize pH levels in different biological environments, preventing excessive acidity or alkalinity that could impair cellular functions. It is involved in the transport of carbon dioxide in the blood and plays a role in maintaining the acid-base equilibrium necessary for physiological processes.
Pharmacokinetics
Carbonate ions are readily absorbed in the gastrointestinal tract when ingested and can be found in various body fluids. They are involved in the bicarbonate buffering system, where they are converted to bicarbonate (HCO3-) and carbon dioxide (CO2) through reactions with acids. The kidneys regulate the levels of bicarbonate and carbonate in the body, excreting or reabsorbing them as needed to maintain homeostasis.
Pregnancy
There is no specific information available regarding the use of carbonate compounds during pregnancy. Consult a healthcare provider for advice.
Breast-feeding
There is no specific information available regarding the use of carbonate compounds while breastfeeding. Consult a healthcare provider for advice.
Storage
Store in a cool, dry place away from direct sunlight. Keep out of reach of children.
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: cellulose
Cellulose is a complex carbohydrate and a key structural component of the plant cell wall. It is an indigestible polysaccharide made up of linear chains of glucose molecules linked by β-1,4-glycosidic bonds. As a dietary fiber, cellulose contributes to digestive health by promoting bowel regularity and is commonly used as a laxative and bulking agent in various food products and pharmaceuticals.
Indications
- Constipation
- Dietary fiber supplementation
- Irritable bowel syndrome
- Diverticular disease
- Weight management
Dosage
Children: Refer to appropriate guidelines for specific dosage; generally taken with adequate fluid intake.
Adults: Refer to appropriate guidelines for specific dosage; generally taken with adequate fluid intake.
Mechanism of action
Cellulose acts primarily as a bulk-forming laxative. It absorbs water in the intestines, which increases stool bulk and stimulates peristalsis, thus facilitating bowel movements. Additionally, cellulose is not digestible by human enzymes, leading to fermentation by gut bacteria, which may enhance gut health and alter gut microbiota composition.
Pharmacodynamics
Cellulose increases stool weight and frequency of bowel movements. It works by retaining water in the intestines, leading to softer stools and improved passage through the gastrointestinal tract. The bulking effect of cellulose can help alleviate constipation and promote overall digestive health. It may also play a role in cholesterol reduction and glycemic control through its effects on digestion and absorption of nutrients.
Pharmacokinetics
Cellulose is not absorbed into the bloodstream due to its indigestible nature. Instead, it passes through the gastrointestinal tract, where it adds bulk to the stool. Its fermentation by colonic bacteria produces short-chain fatty acids, which may have beneficial effects on colon health. The onset of action for cellulose as a laxative can vary but is generally within 24 to 72 hours after ingestion.
Adverse effects
- Bloating
- Flatulence
- Diarrhea
- Abdominal discomfort
Precautions
- Use with caution in patients with a history of gastrointestinal disorders.
- Monitor for potential allergic reactions in sensitive individuals.
Pregnancy
Cellulose is generally considered safe during pregnancy as it is a non-toxic, indigestible fiber.
Breast-feeding
Cellulose is also considered safe during breastfeeding; it is excreted in breast milk in negligible amounts.
Storage
Store in a cool, dry place away from direct sunlight.
Formulations
- Powder
- Capsules
- Tablets
- Granules
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: lactose
BNF-referencedLactose is a disaccharide sugar composed of galactose and glucose, primarily found in milk and dairy products. It serves as a source of energy and is metabolized by the enzyme lactase. In individuals with lactase deficiency, lactose can lead to gastrointestinal symptoms such as bloating, diarrhea, and abdominal pain.
Indications
- Lactose intolerance
- As a filler or excipient in pharmaceutical formulations
Dosage
Children: Refer to the BNF for Children for specific dosing information based on age and clinical context.
Adults: Refer to the BNF for specific dosing information based on clinical context.
Mechanism of action
Lactose is metabolized in the intestine by the enzyme lactase into its constituent monosaccharides, glucose and galactose. In individuals with lactase deficiency, unabsorbed lactose passes into the colon, where it is fermented by bacteria, leading to gas production and osmotic effects that contribute to diarrhea.
Pharmacodynamics
The pharmacodynamics of lactose are primarily related to its effects on gastrointestinal function. In healthy individuals, lactose is effectively broken down into glucose and galactose, which are absorbed and utilized for energy. In individuals with lactose intolerance, the unabsorbed lactose can cause osmotic diarrhea and colonic fermentation, leading to discomfort and symptoms associated with lactose intolerance.
Pharmacokinetics
Lactose is not absorbed in the gastrointestinal tract until it is hydrolyzed into glucose and galactose by lactase. The absorption of glucose and galactose occurs in the small intestine. The half-life is not applicable as lactose is not typically administered as a medication but is rather ingested as a natural component of food. Its metabolism primarily occurs in the intestine.
Adverse effects
- Bloating
- Diarrhea
- Abdominal pain
- Flatulence
Precautions
- Use with caution in patients with lactose intolerance.
- Consider potential for gastrointestinal upset in sensitive individuals.
Pregnancy
Lactose is generally considered safe for use during pregnancy. However, consult a healthcare professional for individual advice.
Breast-feeding
Lactose is safe to use while breastfeeding, as it is a natural sugar present in breast milk.
Storage
Store in a cool, dry place, away from direct sunlight.
Formulations
- Powder
- Granules
- Tablets
- Syrup
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: microcrystalline
Microcrystalline cellulose is a refined wood pulp, commonly used as an excipient in pharmaceutical formulations. It serves as a bulking agent and stabilizer in tablets and capsules, improving the physical properties of the drug formulation. It is characterized by its ability to absorb moisture and provide a suitable texture for various dosage forms.
Indications
- Used as an excipient in tablet formulations
- Used as a bulking agent in capsule formulations
- Used in food products as a thickener or stabilizer
Dosage
Children: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.
Adults: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.
Mechanism of action
Microcrystalline cellulose acts as a non-digestible filler that enhances the flow properties of powders during the manufacturing of tablets and capsules. It does not have a direct pharmacological action on the body but ensures that the active ingredients are effectively delivered to the patient.
Pharmacodynamics
As a non-active ingredient, microcrystalline cellulose does not exert pharmacodynamic effects typical of active pharmaceutical ingredients. Its primary role is to provide a stable and consistent matrix for the drug, facilitating the release of the active compound once ingested.
Pharmacokinetics
Microcrystalline cellulose is not absorbed in the gastrointestinal tract; it passes through the digestive system largely unchanged. It adds bulk to the stool, which may aid in promoting regular bowel movements. The substance is excreted in feces, where it contributes to dietary fiber intake.
Pregnancy
Data regarding the use of microcrystalline cellulose during pregnancy is limited. It is advisable to consult with healthcare professionals before use.
Breast-feeding
Microcrystalline cellulose is considered safe during breastfeeding, as it is not absorbed systemically.
Storage
Store in a cool, dry place away from direct sunlight and moisture.
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: polysorbate
Polysorbate is a non-ionic surfactant and emulsifier used in various pharmaceutical formulations. It is derived from sorbitol and fatty acids and is known for its capacity to enhance the solubility of hydrophobic compounds in aqueous solutions. Polysorbate is commonly utilized in the preparation of oral, parenteral, and topical pharmaceutical products, as well as in food and cosmetic industries.
Indications
- Emulsifying agent in drug formulations
- Stabilizer for parenteral preparations
- Solubilizer for hydrophobic drug compounds
- Ingredient in topical formulations
Dosage
Children: Refer to specific product guidelines, as dosing varies based on formulation and intended use.
Adults: Refer to specific product guidelines, as dosing varies based on formulation and intended use.
Mechanism of action
Polysorbate functions primarily as an emulsifying agent. It reduces the surface tension between immiscible liquids, allowing them to mix more easily. This property is particularly useful in stabilizing emulsions and suspensions, facilitating the delivery of active pharmaceutical ingredients in various formulations.
Pharmacodynamics
Polysorbate does not exert pharmacological effects in the traditional sense, as it does not bind to specific receptors to elicit a physiological response. Instead, it plays a crucial role in modifying the physical properties of drug formulations, thereby enhancing drug delivery and absorption. Its ability to solubilize drugs enhances their bioavailability, particularly for poorly soluble compounds.
Pharmacokinetics
Polysorbate is generally considered to be non-toxic and is not absorbed to a significant extent when administered orally. It is metabolized by the liver and excreted primarily through the gastrointestinal tract. The pharmacokinetic profile may vary depending on the route of administration and the specific formulation in which it is used.
Adverse effects
- Allergic reactions
- Skin irritation
- Gastrointestinal disturbances
Precautions
- Use cautiously in patients with known allergies to polysorbates or related compounds
- Monitor for allergic reactions in susceptible individuals
Pregnancy
Polysorbate is generally considered safe for use during pregnancy, but consult with a healthcare provider for specific cases.
Breast-feeding
Polysorbate is considered safe during breastfeeding, but consult with a healthcare provider for individual advice.
Storage
Store at room temperature, away from direct sunlight and moisture.
Formulations
- Polysorbate 20
- Polysorbate 80
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: purified
Purified refers to a substance that has been processed to remove impurities, contaminants, or unwanted substances, resulting in a more concentrated and effective form of the original compound. In pharmacology, purified compounds are often used to enhance therapeutic efficacy and reduce adverse effects. The purification process can apply to a variety of substances, including drugs, biological products, and chemical compounds.
Dosage
Children: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.
Adults: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.
Mechanism of action
The mechanism of action for purified compounds varies widely depending on the specific substance. Generally, purified drugs exert their effects by interacting with specific biological targets, such as receptors, enzymes, or ion channels, leading to a desired therapeutic effect. This interaction can involve binding to receptors to activate or inhibit signaling pathways, modulating enzymatic activity, or altering physiological processes.
Pharmacodynamics
Pharmacodynamics describes the effects of a drug on the body and the relationship between drug concentration and effect. For purified drugs, this can involve dose-response relationships and the time course of their action. The purified form often enhances potency and reduces variability in response among patients, which can lead to more predictable therapeutic outcomes. The overall effect is determined by the drug's affinity for its target, the efficacy of the drug-receptor interaction, and the downstream signaling pathways activated as a result of this interaction.
Pharmacokinetics
Pharmacokinetics involves the absorption, distribution, metabolism, and excretion (ADME) of a drug. For purified substances, absorption can be more efficient due to the absence of impurities that may affect solubility or stability. Distribution may also be enhanced, leading to higher bioavailability. Metabolism can be influenced by the structure of the purified compound, as it may be metabolized more readily by liver enzymes. Excretion typically occurs through the kidneys or liver, depending on the molecular characteristics of the purified drug.
Pregnancy
Consult with a healthcare professional, as the safety of purified forms of medications during pregnancy may vary depending on the specific substance.
Breast-feeding
Consult with a healthcare professional, as the safety of purified forms of medications during breastfeeding may vary depending on the specific substance.
Storage
Store in a cool, dry place, away from light and moisture, and keep out of reach of children.
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Atorvastatin
PubChem CID 60823Molecular formula: C33H35FN2O5
Mechanism of action
Atorvastatin is a statin medication and a competitive inhibitor of the enzyme HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis. Atorvastatin acts primarily in the liver, where decreased hepatic cholesterol concentrations stimulate the upregulation of hepatic low-density lipoprotein (LDL) receptors, which increases hepatic uptake of LDL. Atorvastatin also reduces Very-Low-Density Lipoprotein-Cholesterol (VLDL-C), serum triglycerides (TG) and Intermediate Density Lipoproteins (IDL), as well as the number of apolipoprotein B (apo B) containing particles, but increases High-Density Lipoprotein Cholesterol (HDL-C). _In vitro_ and _in vivo_ animal studies also demonstrate that atorvastatin exerts vasculoprotective effects independent of its lipid-lowering properties, also known as the pleiotropic effects of statins. These effects include improvement in endothelial function, enhanced stability of atherosclerotic plaques, reduced oxidative stress and inflammation, and inhibition of the thrombogenic response. Statins were also found to bind allosterically to β2 integrin function-associated antigen-1 (LFA-1), which plays an essential role in leukocyte trafficking and T cell activation. In animal models, Lipitor lowers plasma cholesterol and lipoprotein levels by inhibiting 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase and cholesterol synthesis in the liver and by increasing the number of hepatic low-density lipoprotein (LDL) receptors on the cell surface to enhance uptake and catabolism of LDL; Lipitor also reduces LDL production and the number of LDL particles. Lipitor reduces LDL-cholesterol (LDL-C) in some patients with homozygous familial hypercholesterolemia (FH), a population that rarely responds to other lipid-lowering medication(s). Lipitor is a selective, competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of sterols, including cholesterol. Cholesterol and triglycerides circulate in the bloodstream as part of lipoprotein complexes. With ultracentrifugation, these complexes separate into HDL (high-density lipoprotein), IDL (intermediate-density lipoprotein), LDL (low-density lipoprotein), and VLDL (very-low-density lipoprotein) fractions. Triglycerides (TG) and cholesterol in the liver are incorporated into VLDL and released into the plasma for delivery to peripheral tissues. LDL is formed from VLDL and is catabolized primarily through the high-affinity LDL receptor. Clinical and pathologic studies show that elevated plasma levels of total cholesterol (total-C), LDL-cholesterol (LDL-C), and apolipoprotein B (apo B) promote human atherosclerosis and are risk factors for developing cardiovascular disease, while increased levels of HDL-C are associated with a decreased cardiovascular risk. Statins are largely used in clinics in the treatment of patients with cardiovascular diseases for their effect on lowering circulating cholesterol. Lectin-like oxidized low-density lipoprotein (LOX-1), the primary receptor for ox-LDL, plays a central role in the pathogenesis of atherosclerosis and cardiovascular disorders. We have recently shown that chronic exposure of cells to lovastatin disrupts LOX-1 receptor cluster distribution in plasma membranes, leading to a marked loss of LOX-1 function. Here we investigated the molecular mechanism of statin-mediated LOX-1 inhibition and we demonstrate that all tested statins /including atorvastatin/ are able to displace the binding of fluorescent ox-LDL to LOX-1 by a direct interaction with LOX-1 receptors in a cell-based binding assay. Molecular docking simulations confirm the interaction and indicate that statins completely fill the hydrophobic tunnel that crosses the C-type lectin-like (CTLD) recognition domain of LOX-1. Classical
Pharmacodynamics
Atorvastatin is an oral antilipemic agent that reversibly inhibits HMG-CoA reductase. It lowers total cholesterol, low-density lipoprotein-cholesterol (LDL-C), apolipoprotein B (apo B), non-high density lipoprotein-cholesterol (non-HDL-C), and triglyceride (TG) plasma concentrations while increasing HDL-C concentrations. High LDL-C, low HDL-C and high TG concentrations in the plasma are associated with increased risk of atherosclerosis and cardiovascular disease. The total cholesterol to HDL-C ratio is a strong predictor of coronary artery disease, and high ratios are associated with a higher risk of disease. Increased levels of HDL-C are associated with lower cardiovascular risk. By decreasing LDL-C and TG and increasing HDL-C, atorvastatin reduces the risk of cardiovascular morbidity and mortality. Elevated cholesterol levels (and high low-density lipoprotein (LDL) levels in particular) are an important risk factor for the development of CVD. Clinical studies have shown that atorvastatin reduces LDL-C and total cholesterol by 36-53%. In patients with dysbetalipoproteinemia, atorvastatin reduced the levels of intermediate-density lipoprotein cholesterol. It has also been suggested that atorvastatin can limit the extent of angiogenesis, which can be useful in the treatment of chronic subdural hematoma. **Myopathy/Rhabdomyolysis** Atorvastatin, like other HMG-CoA reductase inhibitors, is associated with a risk of drug-induced myopathy characterized by muscle pain, tenderness, or weakness in conjunction with elevated levels of creatine kinase (CK). Myopathy often manifests as rhabdomyolysis with or without acute renal failure secondary to myoglobinuria. The risk of statin-induced myopathy is dose-related, and the symptoms of myopathy are typically resolved upon drug discontinuation. Results from observational studies suggest that 10-15% of people taking statins may experience muscle aches at some point during treatment. **Liver Dysfunction** Statins, like some other lipid-lowering therapies, have been associated with biochemical abnormalities of liver function. Persistent elevations (> 3 times the upper limit of normal [ULN] occurring on two or more occasions) in serum transaminases occurred in 0.7% of patients who received atorvastatin in clinical trials. This effect appears to be dose-related. **Endocrine Effects** Statins are associated with a risk of increased serum HbA1c and glucose levels. An _in vitro_ study demonstrated a dose-dependent cytotoxic effect on human pancreatic islet β cells following treatment with atorvastatin. Moreover, insulin secretion rates decreased relative to control. HMG-CoA reductase inhibitors interfere with cholesterol synthesis and may theoretically interfere with the production of adrenal and/or gonadal steroids. Clinical studies with atorvastatin and other HMG-CoA reductase inhibitors have suggested that these agents do not affect plasma cortisol concentrations, basal plasma testosterone concentration, or adrenal reserve. However, the effect of statins on male fertility has not been fully investigated. The effects of statins on the pituitary-gonadal axis in premenopausal women are unknown. **Cardiovascular** Significant decreases in circulating ubiquinone levels in patients treated with atorvastatin and other statins have been observed. The clinical significance of a potential long-term statin-induced deficiency of ubiquinone has not been established. It has been reported that a decrease in myocardial ubiquinone levels could lead to impaired cardiac function in patients with borderline congestive heart failure. **Lipoprotein A** In some patients, the beneficial effect of lowered total cholesterol and LDL-C levels may be partly blunted by the concomitant increase in Lp(a) lipoprotein concentrations. Present knowledge suggests the importance of high Lp(a) levels as an emerging risk factor for coronary heart disease. Further studies have demonstrated statins affect Lp(a) levels diffe
Biological pathways
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
Molecular reference: carbonate
PubChem CID 19660Molecular formula: CO3-2
Biological pathways
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
Molecular reference: lactose
PubChem CID 6134Molecular formula: C12H22O11
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
This drug in other countries
The same active ingredient registered across other registries we cover - including different brands.