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There are several notable drug interactions with progesterone. Certain selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine , paroxetine , and sertraline may increase the GABA A receptor-related central depressant effects of progesterone by enhancing its conversion into 5α-dihydroprogesterone and allopregnanolone via activation ...
Progesterone interacts with membrane progesterone receptors, but interaction of progestins with these receptors is less clear. [165] [166] In addition to their progestogenic activity, many progestogens have off-target activities such as androgenic, antiandrogenic, estrogenic, glucocorticoid, and antimineralocorticoid activity. [1] [2] [47]
A selective progesterone receptor modulator (SPRM) is an agent that acts on the progesterone receptor (PR), the biological target of progestogens like progesterone.A characteristic that distinguishes such substances from full receptor agonists (e.g., progesterone, progestins) and full antagonists (e.g., aglepristone) is that their action differs in different tissues, i.e. agonist in some ...
Progesterone is a progestogen, or an agonist of the nuclear progesterone receptors (PRs), the PR-A, PR-B, and PR-C. [1] In one study, progesterone showed EC 50 Tooltip half-maximal effective concentration values of 7.7 nM for the human PR-A and 8.0 nM for the human PR-B. [5] In addition to the PRs, progesterone is an agonist of the membrane progesterone receptors (mPRs), including the mPRα ...
Drug-drug interactions among COCPs and other medications of the user that decrease contraceptive estrogen and/or progestogen levels. [ 44 ] In any of these instances, a backup contraceptive method should be used until hormone active pills have been consistently taken for 7 consecutive days or drug-drug interactions or underlying illnesses have ...
Norgestimate is a progestogen, or an agonist of the progesterone receptor. [1] The relative binding affinities of norgestimate and its active metabolites for the progesterone receptor compared to promegestone (100%) are 15% for norgestimate, 10% for norelgestromin, 150% for levonorgestrel, and 135% for levonorgestrel acetate. [1]
The drug was first marketed, by Parke-Davis as Norlestrin in the United States, in March 1964. [11] [12] This was a combination formulation of 2.5 mg NETA and 50 μg ethinylestradiol and was indicated as an oral contraceptive. [11] [12] Other early brand names of NETA used in oral contraceptives included Minovlar and Anovlar. [11]
Unlike progesterone, hydroxyprogesterone caproate and its metabolites are not anticipated to interact with non-genomic receptors such as membrane progesterone receptors or the GABA A receptor. [23] In accordance, hydroxyprogesterone caproate is not thought to possess the neurosteroid activities of progesterone or its associated sedative effects.
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