Estradiol valerate
In addition to single-drug formulations, oral estradiol valerate is available in combination with the progestin dienogest as a combined oral contraceptive and intramuscular estradiol valerate is marketed in combination with the progestins hydroxyprogesterone caproate and norethisterone enantate as combined injectable contraceptives. Intramuscular estradiol valerate has also been marketed in combination with testosterone enantate, but this formulation has been discontinued. The availability of estradiol valerate-containing products varies throughout the world.
Pharmacokinetics of estradiol
Estradiol has been studied and used by intranasal administration. It was available as a cyclodextrin-containing nasal spray under the brand name Aerodiol in some countries, although this specific product was discontinued in 2007. The product was administered once per day as one 150-μg spray in each nostril (300 μg/day total). Intranasal estradiol has pharmacokinetics similar to those of sublingual and intravenous administration of estradiol, including a sharp peak and then rapid decline in estradiol levels. Despite the relatively short duration of intranasal estradiol, it has similar effectiveness to other, longer-lasting routes of administration in terms of relief of menopausal symptoms like hot flashes.