Definition Pharmaceutical agents are excreted primarily in the urine and, via the liver, in the bile in the stool. When excreted via the bile, they re-enter the small intestine, where they may be reabsorbed. They are transported back to the liver via the portal vein. This repetitive process is called the enterohepatic circulation. It prolongs … Enterohepatic Circulation
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)
Symptoms Increasing diffuse thinning of the hair occurs in the area of the middle parting. In this case, unlike androgenetic alopecia in men, not all hair is lost, but the scalp becomes visible over time. Often, a densely hairy strip remains frontally above the forehead. Dense hair is also still found on the sides and … Androgenetic Alopecia in Women
Products No finished drug products containing mestranol are commercially available in many countries. Structure and properties Mestranol (C21H26O2, Mr = 310.4 g/mol) is a methoxy derivative and a prodrug of ethinylestradiol. Effects Mestranol has contraceptive properties. Indications For hormonal contraception in combination with a progestin.
Products Gestodene is marketed in many countries exclusively in combination with ethinyl estradiol in the form of dragées and film-coated tablets as an oral contraceptive (“pill”). It has been approved in many countries since 1986. Structure and properties Gestodene (C21H26O2, Mr = 310.4 g/mol) exists as a white to yellowish crystalline powder that is practically … Gestodene
Products Drospirenone is commercially available as a fixed combination with ethinyl estradiol for contraception in the form of film-coated tablets (Yasmin, Yasminelle, YAZ, generics, auto-generics). Drospirenone is also used in combination with estradiol for hormone replacement therapy (Angeliq). Bayer’s originals Yasmin, Yasminelle and YAZ will go off the market in many countries in December 2021. … Drospirenone
Products Vaginal (contraceptive ring): NuvaRing (+ ethinyl estradiol) see under contraceptive ring. Implanted (plastic rods): Implanon Structure and properties Etonogestrel (3-keto-desogestrel, C22H28O2, Mr = 324.5 g/mol) is the biologically active metabolite of desogestrel (Cerazette), a progestin derived from 19-nortestosterone. Effects The contraceptive effects of etonogestrel (ATC G03AC08) are primarily due to inhibition of ovulation. Indications … Etonogestrel
Products Tibolone is commercially available in tablet form (Livial, Germany: Liviella). It has been approved in many countries since 1998. Generic versions were registered in 2014. Structure and properties Tibolone (C21H28O2, Mr = 312.4 g/mol) is structurally related to 19-nortestosterone. It carries an ethynyl group like ethynylestradiol. Effects Tibolone (ATC G03CX01) is a prodrug. The … Tibolone
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
Products Cyproterone acetate is commercially available in the form of dragées in combination with ethinyl estradiol (generics). The drug has been approved in many countries since 1987. This article refers to the original Diane-35 and corresponding generics. Other drugs containing cyproterone acetate are available for other indications. Bayer’s original Diane-35 goes off the market in … Cyproterone Acetate
Products The so-called four-period pill Seasonique was approved in many countries in 2016. It has been available in the United States since 2006, and in several European countries since 2015. One pack of Seasonique contains: 84 pink film-coated tablets containing ethinyl estradiol and levonorgestrel (for 12 weeks). 7 white film-coated tablets with low-dose ethinyl estradiol … Four Period Pill
Products Desogestrel is commercially available as a monopreparation in the form of film-coated tablets (Cerazette, 75 µg, generic). The active ingredient was approved in the 1980s. In 2014, generic versions were registered for the first time in many countries. Structure and properties Desogestrel (C22H30O, Mr = 310.5 g/mol) exists as a white crystalline powder that … Desogestrel: Drug Effects, Side Effects, Dosage and Uses
