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The mean absolute bioavailability of a 100 mg oral dose is approximately 75%. The mean peak plasma concentration of racemic Estradiol and M1 occurs at two and three hours, respectively, after administration in healthy adults.
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Although Estradiol is known to exhibit a local anaesthetic effect, how Estradiol exerts this effect is not understood fully.
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Intramuscular (i.m.) Estradiol increases gastric pH during anaesthesia similar to famotidine.
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Use Estradiol with caution in the ELDERLY; they may be more sensitive to its effects.Estradiol should not be used in CHILDREN younger than 16 years old;
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Estradiol can impair thinking and the physical abilities required for driving or operating machinery. Estradiol should be avoided in patients intoxicated with alcohol,
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Respiratory depression should be treated as an overdose.
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Estradiol had only slight thermoregulatory effects. Its use is thus unlikely to provoke hypothermia or to facilitate fever.
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Estradiol is well absorbed orally with an absolute bioavailability of 75%. Estradiol has a volume of distribution of approximately 2.7 L/kg and is only 20% bound to plasma proteins.
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