Clinical equivalence of intranasal and oral 17β-estradiol for postmenopausal symptoms

Mattsson, Lars; Christiansen, Claus; Colau, J. C.; Palacios, Santiago; Kenemans, P.; Bergeron, Christine; Chevallier, Olivier; Holst, T. von; Gangar, K. F.

doi:10.1067/mob.2000.104843

Cited by 64 publications

(27 citation statements)

References 18 publications

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“…25 Given with oral dydrogesterone in a sequentially combined fashion, 24 weeks of intranasal 300 g E 2 did not show significant changes from baseline in antithrombin or D-dimer. 25 Increased resistance to APC is associated with an increased VTE risk. 8,9 APC resistance was measured with the ETPbased APC resistance test.…”

Section: Discussionmentioning

confidence: 99%

“…An intranasal spray has shown to be effective in climacteric symptom relief and a well-tolerated alternative route for E 2 administration (Aerodiol; Servier) 25 with an attractive theoretical advantage of less stimulation of the breast and endometrium, 26 leading to less breakthrough bleeding and mastalgia. 25 In addition to the E 2 -only spray, an intranasal spray for continuous combined 17␤-E 2 plus norethisterone (E 2 /NET) administration has been developed.…”

mentioning

confidence: 99%

“…25 In addition to the E 2 -only spray, an intranasal spray for continuous combined 17␤-E 2 plus norethisterone (E 2 /NET) administration has been developed. Because the hepatic metabolism is largely bypassed, it is plausible that, like HT with transdermal E 2 , 3 intranasal administration may have limited effect on VTE risk.…”

mentioning

confidence: 99%

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Less Effect of Intranasal Than Oral Hormone Therapy on Factors Associated With Venous Thrombosis Risk in Healthy Postmenopausal Women

Hemelaar

Rosing²,

Kenemans³

et al. 2006

ATVB

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Objective-To compare the effects of intranasal and oral administration of 17␤-estradiol (E 2 ) and norethisterone (acetate) [NET(A)] in healthy postmenopausal women on activated protein C (APC) resistance and other hemostatic parameters associated with venous thrombosis. Methods and Results-In this 2-center, randomized, double-blind, 1-year trial, 90 postmenopausal women (56.6Ϯ4.7 years of age) received daily either an intranasal spray with 175 g/275 g E 2 /NET (nϭ47) or 1 mg/0.5 mg oral E 2 /NETA (nϭ43). Normalized APC sensitivity ratios (nAPCsr) were determined with a thrombin generation-based APC resistance test. After 1 year, the increase in nAPCsr was smaller in the intranasal than in the oral group: 11% (95% CI, 1% to 22%) versus 53% (95% CI, 37% to 72%). Overall, the decrease in antithrombin and increase in prothrombin fragment 1ϩ2 (F1ϩ2) were smaller and the decrease in free protein S larger in the intranasal compared with the oral group after 1 year. In both groups, the decreases in protein C and prothrombin, and the increase in D-dimer were similar. Conclusion-Compared

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Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

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Less Effect of Intranasal Than Oral Hormone Therapy on Factors Associated With Venous Thrombosis Risk in Healthy Postmenopausal Women

Hemelaar

Rosing²,

Kenemans³

et al. 2006

ATVB

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“…It displays completely different pharmacokinetics of plasma estradiol levels (Devissaguet et al 1999), leading to a transient exposure to high estradiol levels and introducing the new concept of pulsed estrogen therapy. In clinical trials, pulsed estrogen therapy has demonstrated a clinical efficacy similar to reference compounds on climacteric symptoms (Studd et al 1999, Lopes et al 2000 and bone (Garnero et al 1999) and has been shown to be safe on some estradiol target organs (Mattsson et al 2000), especially the endometrium (Gompel et al 2000).…”

Section: Discussionmentioning

confidence: 99%

Comparative activity of pulsed or continuous estradiol exposure on gene expression and proliferation of normal and tumoral human breast cells

Cavaillès

Gompel²,

Portois³

et al. 2002

Journal of Molecular Endocrinology

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Intranasal administration of hormone replacement therapy presents an original plasma kinetic profile with transient estrogen levels giving rise to the concept of pulsed therapy. To further understand the molecular effects of this new therapy, we have compared the effects of pulsed and continuous estradiol treatments on two critical aspects of estradiol action: gene expression and cell proliferation. Cells were stimulated with estradiol as 1-h pulsed or 24-h continuous treatments at concentrations such that the 24-h exposure (concentration×time) was identical in both conditions. In MCF7 cells, the transcriptional activity of estrogen receptors (ER) on a transiently transfected responsive estrogen response element-luciferase reporter construct was shown to be drastically (∼10-fold) and similarly stimulated after both treatments. Moreover, the increased mRNA expression of three representative estradiol-sensitive genes (pS2, cathepsin D, progesterone receptor), evaluated by Northern blot, was identical after 1-h pulse with 7 nM estradiol or continuous treatment with 0·29 nM estradiol with the same kinetic profile over 48 h. Proliferation was quantified by a histomorphometric method on primary cultures of human normal breast cells from reduction mammoplasties and using a fluorescence DNA assay in six human breast cancer cell lines which were ER positive or negative. After a 7-day treatment period, estradiol had no effect on the proliferation of the three ER negative cell lines (BT20, MDA MB231, SK BR3) but significantly stimulated the proliferation of the normal cells and of the three tumoral hormone-sensitive cell lines (MCF7, T47D, ZR 75-1); both hormone treatments producing the same increases in cell growth. In conclusion, we have shown that the genomic or proliferative effects of estradiol were identical with pulsed or continuous treatments, thus indicating that estrogenic effects are not strictly related to concentrations but rather to total hormone exposure.

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“…Intranasal estradiol valerate was as effective as oral administration in alleviating postmenopausal symptoms but produced less frequent mastalgia and uterine bleeding. 76 Intranasal desmopressin acetate was as effective for nocturnal enuresis as the oral drug but at a dose one-tenth that of the oral drug. 77 Intranasal desmopressin is the preferred route for management of central diabetes insipidus.…”

Section: Commentmentioning

confidence: 99%

Intranasal Theophylline Treatment of Hyposmia and Hypogeusia

Henkin¹,

Schultz²,

Minnick-Poppe³

2012

Arch Otolaryngol Head Neck Surg

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To determine whether intranasal theophylline methylpropyl paraben can correct hyposmia and hypogeusia. Design:We performed an open-label pilot study in patients with hyposmia and hypogeusia under the following 3 conditions: (1) before treatment, (2) after oral theophylline anhydrous treatment, and (3) after intranasal theophylline treatment. Under each condition, we performed subjective evaluations of taste and smell functions, quantitative measurements of taste (gustometry) and smell (olfactometry), and measurements of serum theophylline level and body weight.Setting: The Taste and Smell Clinic in Washington, DC.Patients: Ten patients with hyposmia and hypogeusia clinically related to the effects of viral illness, allergic rhinitis, traumatic brain injury, congenital hyposmia, and other chronic disease processes were selected.Interventions: Oral theophylline anhydrous, 200 to 800 mg/d for 2 to 12 months, was administered to each patient. This treatment was discontinued for 3 weeks to 4 months when intranasal theophylline methylpropyl paraben, 20 µg/d in each naris, was administered for 4 weeks.Main Outcome Measures: At termination of each condition, taste and smell function was determined subjectively, by means of gustometry and olfactometry, with measurement of serum theophylline levels and body weight.Results: Oral theophylline treatment improved taste and smell acuity in 6 patients after 2 to 12 months of treatment. Intranasal theophylline treatment improved taste and smell acuity in 8 patients after 4 weeks, with improvement greater than after oral administration. No adverse effects accompanied intranasal drug use. Body weight increased with each treatment but was greater after intranasal than after oral administration.Conclusions: Intranasal theophylline treatment is safer and more effective in improving hyposmia and hypogeusia than oral theophylline anhydrous treatment.

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Clinical equivalence of intranasal and oral 17β-estradiol for postmenopausal symptoms

Cited by 64 publications

References 18 publications

Less Effect of Intranasal Than Oral Hormone Therapy on Factors Associated With Venous Thrombosis Risk in Healthy Postmenopausal Women

Less Effect of Intranasal Than Oral Hormone Therapy on Factors Associated With Venous Thrombosis Risk in Healthy Postmenopausal Women

Comparative activity of pulsed or continuous estradiol exposure on gene expression and proliferation of normal and tumoral human breast cells

Intranasal Theophylline Treatment of Hyposmia and Hypogeusia

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