Statins

Products Most statins are commercially available in the form of film-coated tablets, and some are also available as capsules. The first active ingredient to be marketed was lovastatin from Merck in the United States in 1987. In many countries, simvastatin (Zocor) and, shortly thereafter, pravastatin (Selipran) were the first agents to be approved in 1990. … Statins

Ezetimibe

Products Ezetimibe is commercially available in tablet form, as a monopreparation (Ezetrol, generic), and as a fixed combination with simvastatin (Inegy, generic) and with atorvastatin (Atozet). Also released is a combination with rosuvastatin. Ezetimibe was approved in many countries and in the United States in 2002. Generic and auto-generics entered the market in November 2017. … Ezetimibe

Simvastatin: Effects, Uses & Risks

Simvastatin is a classic statin and is used as a cholesterol-lowering agent. It was approved in 1990 and is used relatively frequently. What is simvastatin? Simvastatin, chemically (1S,3R,7S,8S,8aR)-8-{2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl}-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl-2,2-dimethylbutanoate, is a drug used primarily as a cholesterol-lowering agent. Simvastatin is structurally derived from the naturally occurring monacolin K, also known as lovastatin. Simvastatin is partially synthetically … Simvastatin: Effects, Uses & Risks

Lipid-Lowering Agents

Products Lipid-lowering agents are mainly sold as tablets and capsules as monopreparations and combination preparations. Some other dosage forms exist, such as granules and injectables. Statins have established themselves as the most important group at present. Structure and properties The chemical structure of lipid-lowering agents is inconsistent. However, within the class, groups with comparable structures … Lipid-Lowering Agents

Simvastatin Lowers Cholesterol Levels

Simvastatin is a prescription drug from the group of statins that is used to lower cholesterol levels. This is intended to counteract deposits on the walls of blood vessels and reduce the risk of stroke or heart attack. However, taking simvastatin is associated with a wide variety of side effects. Some – such as nausea … Simvastatin Lowers Cholesterol Levels

Interactions

Definition When two or more drugs are combined, they may affect each other. This is especially true with regard to their pharmacokinetics (ADME) and effects and adverse effects (pharmacodynamics). This phenomenon is called interaction and drug-drug interaction. Interactions are usually undesirable because they can lead to, for example, loss of efficacy, side effects, poisoning, hospitalization, … Interactions

Interactions with Grapefruit Juice

Background That grapefruit juice can cause drug-drug interactions was discovered by chance in a clinical trial in 1989 and confirmed in an experiment by the same research group in 1991 (Bailey et al, 1989, 1991). This showed that simultaneous ingestion of grapefruit juice with the calcium channel blocker felodipine significantly increases the bioavailability of felodipine. … Interactions with Grapefruit Juice

Fenofibrate

Products Fenofibrate is commercially available in the form of capsules (lipanthyl). It has been approved in many countries since 1977. In 2014, a fixed combination with simvastatin was registered (Cholib); see Fenofibrate Simvastatin. Structure and properties Fenofibrate (C20H21ClO4, Mr = 360.8 g/mol) exists as a white crystalline powder that is practically insoluble in water. It … Fenofibrate

Pharmaceutical Active Ingredient

Definition Active ingredients are the active components of a drug that are responsible for its pharmacological effects. Drugs may contain a single active ingredient, multiple active ingredients, or complex mixtures such as herbal extracts. In addition to the active ingredients, a drug contains various excipients that should be as pharmacologically inert as possible. The percentage … Pharmaceutical Active Ingredient

Bempedoic Acid

Products Bempedoic acid was approved in the EU, the United States, and many countries in 2020 in the form of film-coated tablets (Nilemdo). The active ingredient is also combined fixed with ezetimibe (Nustendi film-coated tablets). Structure and properties Bempedoic acid (C19H36O5, Mr = 344.5 g/mol) exists as a white crystalline powder that is practically insoluble … Bempedoic Acid

Prodrugs

What are prodrugs? Not all active pharmaceutical ingredients are directly active. Some must first be converted to the active substance by an enzymatic or non-enzymatic conversion step in the body. These are the so-called . The term was introduced by Adrien Albert in 1958. It is estimated that up to 10% of all active ingredients … Prodrugs