Single‐Dose Pharmacokinetics of Sublingual Versus Oral Administration of Micronized 17β‐Estradiol

@article{Price1997SingleDosePO,
  title={Single‐Dose Pharmacokinetics of Sublingual Versus Oral Administration of Micronized 17$\beta$‐Estradiol},
  author={Thomas M Price and Keith L. Blauer and M. D. Hansen and Frank Z. Stanczyk and Rogerio A. Lobo and G. William Bates},
  journal={Obstetrical \& Gynecological Survey},
  year={1997},
  volume={89},
  pages={340–345}
}
Objective To investigate the pharmacokinetic profiles of different doses of micronized 17β-estradiol administered by oral or sublingual routes. Methods Single doses of micronized 17β-estradiol were administered orally (1 mg, 0.5 mg) or sublingually (1 mg, 0.5 mg, 0.25 mg) to six postmenopausal women in a randomized clinical trial. We calculated pharmacokinetic parameters for estradiol (E2) and estrone (E1) of maximum serum concentration, time to maximum serum concentration, terminal half-life… Expand
Pharmacokinetic profile of nomegestrol acetate and 17β-estradiol after multiple and single dosing in healthy women.
TLDR
These data demonstrate that NOMAC/E2 has a pharmacokinetic profile consistent with once-daily dosing, and are demonstrated to be compatible with pill-free intervals. Expand
Pharmacokinetics of Sublingual vs. Oral Estradiol in Transgender Women.
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Oral Estradiol administered sublingually has a different pharmacokinetic profile, with higher serum estradiol levels and AUC (0-8h) than traditionally administered oral E2, and multi-daily dosing may be necessary to suppress testosterone levels with sublingual estradio. Expand
Bioavailability of norethisterone acetate alone and in combination with estradiol administered in single or multiple oral doses to postmenopausal women.
TLDR
The most abundant metabolite of E2 was the E1S/E1G fraction, which may have served as the main source of E3 and other estrogens due to metabolic interconversions during the absorption and elimination phases, and the bioavailability of NET was not influenced by its combination with 1 mg E2. Expand
Pharmacokinetics of Estradiol Valerate 2mg + Dienogest 2mg (Climodien® 2/2) after Single and Repeated Oral Administration in Healthy Postmenopausal Women
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Pharmacology of estrogens and progestogens: influence of different routes of administration
  • H. Kuhl
  • Medicine
  • Climacteric : the journal of the International Menopause Society
  • 2005
This review comprises the pharmacokinetics and pharmacodynamics of natural and synthetic estrogens and progestogens used in contraception and therapy, with special consideration of hormoneExpand
Sublingual Route of Drug Delivery System: A Review
TLDR
This review highlights the different sublingual dosage forms, factors affecting theSublingual absorption, advantages, various in vitro and in vivo evaluation parameters and commercially available sublingUAL dosage forms. Expand
Comparison of pharmacokinetics of a conjugated equine estrogen preparation (premarin) and a synthetic mixture of estrogens (C.E.S.) in postmenopausal women.
Objective To compare the pharmacokinetics and relative bioavailabilities of key estrogen components of Premarin (Wyeth-Ayerst, Canada) with those of a generic conjugated estrogen preparation, C.E.S.Expand
The acute effects of sublingual 17beta-estradiol on the cardiovascular system.
TLDR
It appears that sublingual estradiol at 1 or 2 mg may improve ischemia and exercise performance in women with coronary artery disease, and augment the aortic and brachial blood flow as a result of vasodilation, whereas larger doses (4 mg) may lead to a decrease in myocardial contractility and aortIC blood flow, and a slight drop in blood pressure. Expand
SUBLINGUAL MUCOSA AS A ROUTE FOR SYSTEMIC DRUG DELIVERY
Drug delivery via the oral mucous membrane is considered to be a promising alternative to the oral route. Sublingual route is a useful when rapid onset of action is desired with better patientExpand
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