Період Напіввиведення Препаратів

Testosterone ester mixtures have been widely used for substitution therapy of
male hypogonadism (e.g. TestovironRDepot 50: 20mg testosterone propionate and
55 mgtestosterone enanthate; TestovironRDepot 100: 25mg testosterone propionate
and 100 mg testosterone enanthate; SustanonR 250: 30 mg testosterone propionate,
60 mg testosterone phenylpropionate, 60 mg testosterone isocaproate and 100 mg
testosterone decanoate). These combinations are used following the postulate that
the so-called short-acting testosterone ester (e.g testosterone propionate) is the
effective testosterone for substitution during the first days of treatment and the
so-called long-acting testosterone (e.g. testosterone enanthate) warrants effective
substitution for the end of injection interval. However, this assumption is not
supported by the pharmacokinetic parameters of the individual testosterone esters.
Both testosterone propionate and testosterone enanthate cause highest testosterone
serum concentrations shortly after injection (Fig. 14.4 and Fig. 14.6). Accordingly,
addition of testosterone propionate to testosterone enanthate only increases the
initial undesired testosterone peak and worsens the pharmacokinetic profile that
ideally should follow zero-order kinetics (Fig. 14.9). The computer simulation
agrees well with the limited published single-dose testosterone values that have
been measured in hypogonadal patients treated with the combination of testosterone
propionate and testosterone enanthate.Maximal increases of approximately
40 nmol/l testosterone over basal values are described one day after intramuscular
administration of a testosterone ester combination of 115.7 mg testosterone enanthate
and 20 mg testosterone propionate to three hypogonadal patients (Fukutani
et al. 1974).
A comparison of computer-simulated testosterone serum concentrations after
multiple-dose injections of TestovironR Depot 100 (110 mg testosterone enanthate
and 25 mg testosterone propionate = 100 mg unesterified testosterone) every 10 d
and 139 mg testosterone enanthate (= 100 mg unersterified testosterone) every
10 d is shown in Fig. 14.10. As can be expected by the single-dose kinetics of the
individual esters, injection of the testosterone ester mixture (upper panel) produces
amuch wider fluctuation of testosterone serumconcentrations relative to injection
of testosterone enanthate alone (lower panel). This simulation shows that injections
of testosterone enanthate alone produce amore favourable pharmacokinetic profile
in comparison to injections of testosterone propionate and testosterone enanthate
ester mixtures in comparable doses. For treatment of male hypogonadism there is
no advantage in combining the available short- and long-acting testosterone esters.

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Омнадрен 250 є сумішшю ефірів тестостерону, які після внутрішньом`язового введення повільно всмоктуються з різною швидкістю, що дозволяє зберігати відносно постійний рівень тестостерону в крові.