CYP450 Cytochromes P450s are a family of enzymes that are of paramount importance in drug biotransformation. The most important isoenzymes for drug metabolism are: CYP1A1, CYP1A2 CYP2B6 CYP2C9, CYP2C19 CYP2D6 CYP2E1 CYP3A4, CYP3A5 and CYP3A7 The number after the abbreviation CYP stands for the family, the following letter for the subfamily and the last number … Cytochrome P450 (CYP)
Introduction Biotransformation is an endogenous pharmacokinetic process that leads to a change in the chemical structure of active pharmaceutical ingredients. The organism’s general goal in doing so is to make the foreign substances more hydrophilic and to direct them to excretion via the urine or stool. Otherwise, they could be deposited in the body and … Metabolism (Biotransformation)
Controlled release from the drug The special design of a drug can be used to achieve delayed, prolonged, continuous, and controlled release of the active ingredient over an extended period of time. This allows the timing, location, and rate of release to be influenced. Galenics Sustained-release drugs include sustained-release tablets, sustained-release capsules, sustained-release granules, and … Retardation
Products In many countries, there are currently no medicines approved that contain only cannabidiol. However, the active ingredient is a component of the cannabis oral spray Sativex, which is registered as a drug for MS treatment in many countries and also contains THC. The oral solution Epidiolex or Epidyolex was approved as a drug in … Cannabidiol
Products Nifedipine is commercially available in the form of sustained-release tablets (generics). It was first approved in the mid-1970s. Sales of the original Adalat were discontinued in many countries in 2019. Structure and properties Nifedipine (C17H18N2O6, Mr = 346.3 g/mol) is a dihydropyridine. It exists as a yellow crystalline powder that is practically insoluble in … Nifedipine: Drug Effects, Side Effects, Dosage and Uses
Products Isosorbide dinitrate is commercially available in many countries in the form of tablets, sustained-release tablets, sustained-release capsules, as an infusion concentrate, and as a spray (Isoket). The drug first came on the market in the 1940s. Structure and properties Isosorbide dinitrate (C6H8N2O8, Mr = 236.14 g/mol) exists as a white, fine, crystalline and odorless … Isosorbide Dinitrate
Products Estradiol is commercially available in tablet, transdermal patch, transdermal gel, vaginal ring, and vaginal tablet forms, among others. It is also combined fixed with progestogens. Structure and properties Estradiol (C18H24O2, Mr = Mr = 272.4 g/mol) exists as a white crystalline powder that is practically insoluble in water. Synthetic estradiol is bioidentical with human … Estradiol
Products Zaleplon was commercially available in capsule form (Sonata, 5 mg, 10 mg). It was approved in many countries in 1999. It was discontinued from distribution in April 2013. Structure and properties Zaleplon (C17H15N5O, Mr = 305.3 g/mol) is a pyrazolopyrimidine and exists as a white powder that is practically insoluble in water. It is … Zaleplon
Products Propranolol is commercially available in tablet, sustained-release capsule, and solution forms (Inderal, generic, hemangiol). It has been approved in many countries since 1965. Structure and properties Propranolol (C16H21NO2, 259.34 g/mol) is present in drugs as propranolol hydrochloride, a white powder that is soluble in water. Propranolol is a racemate. The -enantiomer is predominantly active. … Propranolol
Products Tipiracil is commercially available in the form of film-coated tablets in fixed combination with trifluridine (Lonsurf). The drug was approved in the United States in 2015, in the EU in 2016, and in many countries in 2017. Structure and properties Tipiracil (C9H12Cl2N4O2, Mr = 279.1 g/mol) is present in the drug as tipiracil hydrochloride. … Tipiracil
Products Tizanidine is commercially available in tablet and sustained-release capsule form (Sirdalud, Sirdalud MR, generics). It has been approved in many countries since 1983. Structure and properties Tizanidine (C9H8ClN5S, Mr = 253.7 g/mol) is present in drugs as tizanidine hydrochloride, a white crystalline powder that is somewhat soluble in water. It is an imidazoline and … Tizanidin
Products Nitrates are commercially available in the form of chewable capsules, transdermal patches, infusion preparations, ointment, sustained-release tablets, sustained-release capsules, and sprays. As the first representative, nitroglycerin was already produced in the 19th century and used for the treatment of angina pectoris. Nitrates are thus among the oldest synthetic drugs. Structure and properties Organic nitrates … Organic Nitrates
