cyp

Oxazepam: Drug Effects, Side Effects, Dosage and Uses

Products Oxazepam is commercially available in tablet form (Seresta, Anxiolit). It has been approved in many countries since 1966. Structure and properties Oxazepam (C15H11ClN2O2, Mr = 286.7 g/mol) is a racemate. It exists as a white crystalline powder that is practically insoluble in water. Effects Oxazepam (ATC N05BA04) has antianxiety, sedative, sleep-inducing, anticonvulsant, and muscle … Oxazepam: Drug Effects, Side Effects, Dosage and Uses

Olodaterol

Products Olodaterol was approved in many countries in 2014 as a solution for inhalation (Striverdi). In 2016, a fixed-dose combination with tiotropium bromide was also marketed (Spiolto). Both drugs are administered with the Respimat. Respimat The Respimat is a new inhalation device that releases a visible spray, or aerosol. The droplets are fine and move … Olodaterol

Cytochrome P450 (CYP)

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)

Metabolism (Biotransformation)

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)

Apomorphine

Products Uprima sublingual tablets (2 mg, 3 mg) for erectile dysfunction are no longer marketed in many countries. The marketing authorization was not renewed by Abbott AG in 2006. Commercial reasons were cited, probably attributed to competition from phosphodiesterase-5 inhibitors (e.g., sildenafil, Viagra). It is also possible that a post-marketing study had played a role, … Apomorphine

Glucuronidation

Definition Glucuronidation refers to an intracellular metabolic reaction in which an endogenous or exogenous substrate is conjugated to glucuronic acid. The organism thereby makes the substrates more water soluble so that they can be rapidly excreted in the urine. Glucuronidation belongs to phase II metabolism (conjugations). UDP: uridine diphosphate UGT: UDP-glucuronosyltransferase Enzymes involved Glucuronidation is … Glucuronidation

Levetiracetam

Products Levetiracetam is commercially available as film-coated tablets, an oral solution, and an infusion concentrate (Keppra, generics). It has been approved in many countries since 2000 (United States: 1999). Starting in 2011, generics and new dosage forms entered the market (minipacks). Brivaracetam (Briviact) was developed by UCB as its successor. Structure and properties Levetiracetam (C8H14N2O2, … Levetiracetam

Ranolazine

Products Ranolazine is commercially available in the form of sustained-release tablets (Ranexa). It was approved in the United States as early as 2006, in the EU in July 2008, and in many countries in April 2010. Structure and properties Ranolazine or ()–(2, 6-dimethylphenyl)-4(2-hydroxy-3-(2-methoxyphenoxy)-propyl)-1-piperazine acetamide (C24H33N3O4, Mr = 427.54 g/mol) is a piperazine derivative and a … Ranolazine

Dexlansoprazole

Products Dexlansoprazole was approved in many countries in 2014 in the form of modified-release capsules (Dexilant). Generic versions were registered in 2020. Structure and properties Dexlansoprazole (C16H14F3N3O2S, Mr = 369.4 g/mol) is the pure -enantiomer of the racetmate lansoprazole (Agopton, both Takeda; generics). It exists as a white crystalline powder that is sparingly soluble in … Dexlansoprazole

St. John’s Wort Health Benefits

Products St. John’s wort and corresponding preparations are commercially available in the form of teas, film-coated tablets, dragées, capsules, and tinctures, among others (e.g., Jarsin, Rebalance, Remotiv, Ceres, Hyperiforce, Hyperiplant, Offenware). Stem plant Common St. John’s wort L. is a perennial plant of the St. John’s wort family, native to Europe and also common in … St. John’s Wort Health Benefits

Lumateperon

Products Lumateperone was approved in the United States in 2019 in capsule form (Caplyta). Structure and properties Lumateperone (C24H28FN3O, Mr = 393.5 g/mol) is present in the drug as lumate perontosylate. Like haloperidol (Haldol), for example, it belongs to the butyrophenone group. Effects Lumateperone has antipsychotic and antidepressant properties. Effects are attributed to antagonism at … Lumateperon