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)
Products Mesalazine is commercially available as film-coated tablets, enteric-coated sustained-release tablets, granules, sustained-release granules, clysms, and suppositories (e.g., Asacol, Mezavant, Pentasa, Salofalk). It has been approved in many countries since 1984. Structure and properties Mesalazine (C7H7NO3, Mr = 153.1 g/mol) corresponds to 5-aminosalicylic acid (5-ASA). The active ingredient exists as powders or crystals that are … Mesalazine
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
Products Ixazomib was approved in capsule form in the United States in 2015, in the EU in 2016, and in many countries in 2017 (Ninlaro). Structure and properties Ixazomib is present in drugs in the form of the prodrug ixazomib citrate (C14H19BCl2N2O4, Mr = 361.0 g/mol) is present. In the body, it is hydrolyzed to … Ixazomib
Structure and properties Many active pharmaceutical ingredients are present in the drug as organic salts. This means that the active ingredient is ionized and its charge is neutralized by a counterion (English ). For example, naproxen is present in the over-the-counter pain reliever as a sodium salt. In this form, it is referred to as … Active Ingredient Salts
Products Eslicarbazepine has been approved in tablet form in the EU since 2009, in the United States since 2013, and in many countries in 2020 (Zebinix, Aptiom). Structure and properties Eslicarbazepine (C15H14N2O2, Mr = 254.3 g/mol) is present in drugs in the form of the prodrug eslicarbazepine acetate, which is hydrolyzed in the body after … Eslicarbazepine
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
Products Candesartan is commercially available in tablet form (Atacand, Blopress, generics). It is also combined fixed with hydrochlorothiazide (Atacand plus, Blopress plus, generics). Candesartan has been approved in many countries since 1997. In 2020, a fixed combination with amlodipine was also released. Structure and Properties Candesartan (C24H20N6O3, Mr = 440.45 g/mol) is administered in the … Candesartan
Products Proton pump inhibitors (PPIs) are commercially available in many countries in the form of film-coated tablets, MUPS tablets, capsules, as granules for preparation of an oral suspension, and as injectable and infusion preparations. The first active ingredient from this group to be approved in many countries was omeprazole (Antra, Losec), developed by Astra in … Proton Pump Inhibitors
Products In many countries, vitamin B12 is available as a monopreparation in the form of injectables and as a dietary supplement. Vitamin B12 is also combined with other vitamins, minerals, trace elements, and amino acids. Low- and high-dose preparations are available. Structure and properties Vitamin B12 is a water-soluble B-group vitamin that contains cobalt as … Vitamin B12
Products Tedizolid is commercially available as an infusion preparation and in tablet form (Sivextro). It was approved in the United States in 2014 and in many countries and the EU in 2015. Structure and properties Tedizolid (C17H15FN6O3, Mr = 370.3 g/mol) is present in the drug in the form of the prodrug tedizolid phosphate, a … Tedizolid
Products Dabigatran is commercially available in capsule form (Pradaxa). It has been approved in many countries since 2012. It was first approved in 2008. Structure and properties Dabigatran (C25H25N7O3, Mr = 471.5 g/mol) is present in drugs as mesilate and in the form of the prodrug dabigatran etexilate, which is metabolized in the organism by … Dabigatran
