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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
MPA is well absorbed orally, with blood levels peaking after 2–4 hours and a half-life of 12–17 hours. It can also be administered in a depot form (i.e., Depo-ProveraTM) by deep intramuscular injection (normally into the gluteal muscle) which provides a half-life of 40–50 days. As with most progestogens, side effects include GI disturbances (e.g., nausea), cardiovascular abnormalities (e.g., hypertension, palpitation, congestive heart failure), depression, fluid retention, breast and menstrual cycle irregularities in women, alopecia, sexual dysfunction, skin reactions, and weight changes. In addition to these general adverse effects, the glucocorticoid effects associated with MPA can lead to Cushingoid syndrome at higher doses. Also, rarely, vision disorders such as retinal thrombosis can occur, in which case treatment should be immediately discontinued. Medroxyprogesterone acetate should be avoided during conception or pregnancy, as genital malformations in the fetus may occur.
Essential Pharmacology of Abused Drugs
Published in Frank Lynn Iber, Alcohol and Drug Abuse as Encountered in Office Practice, 2020
Alcohol, unlike almost all other substances, is nearly completely metabolized to energy, with the products being carbon dioxide and water. The initial steps of oxidation occur predominantly in the liver with the formation of acetaldehyde followed by acetate. The acetate is then metabolized throughout the body.
Emergency contraception
Published in Suzanne Everett, Handbook of Contraception and Sexual Health, 2020
Ulipristal acetate prevents pregnancy by inhibiting or delaying ovulation depending when in the cycle it is administered. It is believed that ulipristal acetate can prevent ovulation after the luteal surge has started and delay follicular rupture up to five days later. If ulipristal acetate is administered after implantation has occurred, there is limited evidence on the effects on pregnancy and teratogenicity.
The pharmacotherapeutic management of premenstrual dysphoric disorder
Published in Expert Opinion on Pharmacotherapy, 2023
Nancy Ciccone, Maya B. Kovacheff, Benicio N. Frey
Ulipristal acetate is a selective progesterone receptor modulator that acts as a progesterone antagonist in the progesterone-responsive receptors in the brain, binding to progesterone receptors A and B with high affinity [64]. This medication induces ovulation suppression in approximately 80% of cases and is used for treatment of uterine fibroids. While the precise mechanisms of action in PMDD symptoms remain to be confirmed, both its effects on progesterone receptors and ovulation suppression are thought to be involved [65]. A recent proof-of-concept RCT found preliminary positive evidence especially for psychological symptoms, with a 41% mean decrease in DRSP scores in the ulipristal acetate group compared with 22% in those in the placebo group [65]. Of note, ulipristal acetate has been associated with liver failure, with a reported incidence rate of five acute liver failures among 765,000 patients, and no reports of liver failure in short-term clinical trials [66]
Fiber mixture-specific effect on distal colonic fermentation and metabolic health in lean but not in prediabetic men
Published in Gut Microbes, 2022
Emanuel E. Canfora, Gerben D.A. Hermes, Mattea Müller, Jacco Bastings, Elaine E. Vaughan, Marco A. van Den Berg, Jens J. Holst, Koen Venema, Erwin G. Zoetendal, Ellen E. Blaak
Evidence from acute human intervention studies supports the potential beneficial effect of acetate administration on substrate and energy metabolism. Acetate administered in the distal colon of normoglycaemic, overweight men increased fat oxidation and circulating peptide YY (PYY). In contrast, no effect on metabolic parameters was seen when acetate was administered in the proximal colon.17 In addition, another acute study demonstrated that distal colonic infusions of SCFA mixtures high in acetate increased fat oxidation, energy expenditure and circulating PYY and attenuated whole-body lipolysis in normoglycemic, overweight men.18 Thus, the administration/production site of acetate in the colon seems to be of major importance to elicit beneficial metabolic effects.
The contribution of gut bacterial metabolites in the human immune signaling pathway of non-communicable diseases
Published in Gut Microbes, 2021
F. Hosseinkhani, A. Heinken, I. Thiele, P. W. Lindenburg, A. C. Harms, T. Hankemeier
HDAC inhibition by SCFAs is not restricted to immune cells in the gut. SCFAs can be transported across the gut epithelium into the circulation, affecting distant organs. For instance, exposure of peripheral blood mononuclear cells and neutrophils to SCFAs in vitro can reduce NF-κB activity via HDAC inhibition and thereby down-regulate production of the pro-inflammatory cytokine tumor necrosis factor alpha (TNF-α).35 In the lungs, acetate and propionate control the hyperactivity of airways by inhibiting HDAC and reducing the action of T helper cell (Th-2) by increasing DC proliferation.18 Maternal acetate during pregnancy can protect the offspring against allergic airway disease,44 whereas HDAC inhibitors such as sodium butyrate markedly inhibit brain microglia-induced inflammation.45 Thus, the HDAC pathway actively contributes to the maintenance of immunological tolerance and control of pro-inflammatory cytokines. GPCR activation