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The duration of action of a single oral dose is longer than the half-life and may be up to 12 hours if the single dose is high enough (e.g., 80 mg). [72] Effective plasma concentrations are between 10 and 100 mg/L. [ citation needed ] Toxic levels are associated with plasma concentrations above 2000 mg/L. [ citation needed ]
0.5–5 mg/day Various: Estrogen: SC implant: 50–200 mg every 6–24 mos Estradiol valerate: Progynova: Estrogen: Oral: 2–10 mg/day Progynova: Estrogen: Sublingual: 1–8 mg/day Delestrogen [c] Estrogen: IM, SC: 2–10 mg/wk or 5–20 mg every 2 wks Estradiol cypionate: Depo-Estradiol: Estrogen: IM, SC: 2–10 mg/wk or 5–20 mg every 2 wks ...
For the drugs administered by oral and dermal route, the units of threshold dose are mg/kg body-weight/day (dose of the drug in mg per body weight in kg per day) or ppm (parts per million), while the threshold dose of drugs by inhalation delivery has the unit of mg/L 6h/day (amount of drug in mg in 1L of air, for 6 hours per day). [8]
In transgender women, estradiol valerate given by intramuscular injection is usually used at a dosage of 5 to 20 mg, but up to 30 to 40 mg, once every 2 weeks. [30] [31] [29] Estradiol valerate has also been used at a dose of 10 to 40 mg by intramuscular injection to limit bleeding in women with hemorrhage due to dysfunctional uterine bleeding.
Testosterone enanthate is purported to be slightly better with respect to even testosterone release, but this is probably more of a concern for bodybuilders who use the drugs at higher doses (250–1000 mg/week) than the replacement doses used by transgender men (50–100 mg/week).
The dose should be increased after a minimum of 3 days up to approximately 1.2 mg/kg daily (target dose) as a single or two divided doses (in the morning and late afternoon). For children older than 6 years old, over 70 kg, acute treatment should be started with 40 mg/day orally and increased up to 80 mg/day after a minimum of 3 days.
Pizotifen is able to dose-dependently and fully antagonize the discriminative stimulus effects of the serotonin–norepinephrine–dopamine releasing agent and serotonin 5-HT 2 receptor agonist MDMA in rodent drug discrimination tests. [10] Conversely, the related drug cyproheptadine was only partially effective and clozapine was ineffective. [10]
Rifapentine induces metabolism by CYP3A4, CYP2C8 and CYP2C9 enzymes. It may be necessary to adjust the dosage of drugs metabolized by these enzymes if they are taken with rifapentine. Examples of drugs that may be affected by rifapentine include warfarin, propranolol, digoxin, protease inhibitors and birth control pills. [2]