Products Rivaroxaban is commercially available in the form of film-coated tablets (Xarelto, Xarelto vascular). It was approved in 2008 as the first agent in the direct factor Xa inhibitor group. Low-dose Xarelto vascular, 2.5 mg, was registered in many countries in 2019. Structure and properties Rivaroxaban (C19H18ClN3O5S, Mr = 435.9 g/mol) is a pure -enantiomer … Rivaroxaban
Products Mirabegron is commercially available in the form of sustained-release film-coated tablets (Betmiga, USA: Myrbetriq). It was approved in the US and EU in 2012 and in many countries in 2014. Mirabegron was the first agent from the beta3 agonist group to be approved for the treatment of irritable bladder. It was originally intended to … Mirabegron
Intestinal absorption After ingestion of a drug, the active ingredient must first be released. This process is called release (liberation), and it is a prerequisite for subsequent absorption. Absorption (formerly: resorption) is the passage of an active pharmaceutical ingredient from the digestive pulp into the bloodstream in the stomach and intestines. Absorption occurs primarily in … Absorption
Products Pasireotide is commercially available as an injectable (Signifor, Signifor LAR). It was approved in the EU and many countries in 2012. Structure and properties Pasireotide (C59H67N9O9, Mr = 1046.2 g/mol) is present in the drug as pasireotide diaspartate or as pasireotide pamoate. It is a cyclohexapeptide and an analog of the hormone somatostatin. Somatostatin … Pasireotide
Definition and mechanisms A pharmacokinetic booster is an agent that improves the pharmacokinetic properties of another agent. It is a desirable drug interaction It can exert its effects at different levels (ADME): Absorption (uptake into the body). Distribution (distribution) Metabolism and first-pass metabolism (metabolization). Elimination (excretion) Pharmacokinetic enhancers can increase absorption, increase distribution to an … Pharmacokinetic Booster
Products Sofosbuvir is commercially available in the form of film-coated tablets (Sovaldi). It was approved in the United States and EU in 2013 and in many countries in 2014. The very high price of the drug has been a source of debate. Sofosbuvir is also combined fixed with ledipasvir (Harvoni). Cheaper generics are available in … Sofosbuvir
Products Carvedilol is commercially available in tablet form (Dilatrend, generic). It has been approved in many countries since 1995. Carvedilol is also combined with ivabradine fixed (Carivalan). Structure and properties Carvedilol (C24H26N2O4, Mr = 406.5 g/mol) is a racemate, with both enantiomers participating in the pharmacological effects. It exists as a white crystalline powder that … Carvedilol
Products Medicines containing colchicine are no longer on the market in many countries. Drugs are available abroad that can be imported. It may also be possible to prepare an extemporaneous formulation in a pharmacy (difficulties: toxicity, substance). Stem plant Colchicine is the main alkaloid of the autumn crocus (Colchicaceae), which contains it particularly abundantly in … Colchicine
Products Carfilzomib was approved in many countries in 2015 as a powder for the preparation of an infusion solution (Kyprolis). Structure and properties Carfilzomib (C40H57N5O7, Mr = 719.9 g/mol) exists as a crystalline substance that is practically insoluble in water. It is a peptide derivative, a tetrapeptide epoxyketone. Epoxyketones are derivatives of epoxomicin, a natural … Carfilzomib
Products Olaparib was approved in the United States and EU in 2014 and in many countries in 2015 in capsule form (Lynparza). Later, film-coated tablets were also registered. Structure and properties Olaparib (C24H23FN4O3, Mr = 434.5 g/mol) Effects Olaparib (ATC L01XX46) has antitumor and cytotoxic properties. The effects are due to inhibition of PARP (poly-(ADP-ribose) … Olaparib
Products Elbasvir was approved in many countries in 2016 as a fixed-dose combination with the protease inhibitor grazoprevir in film-coated tablet form (Zepatier). Structure and properties Elbasvir (C49H55N9O7, Mr = 882.0 g/mol) Effects Elbasvir (ATC J05AX68) has antiviral properties. The effects are due to binding to the viral protein NS5A (Non-Structural Protein 5A). Unlike other … Elbasvir
Products Eletriptan is commercially available in the form of film-coated tablets (Relpax, generics). It has been approved in many countries since 2000. Structure and properties Eletriptan (C22H26N2O2S, Mr = 382.5 g/mol) is a lipophilic methylpyrrolidinyltryptamine substituted with a sulfonylbenzene. It is present in drugs as eletriptan hydrobromide, a white powder that is readily soluble in … Eletriptan
