Pharmacokinetic indices for the respective drugs were comparable after administration of beclomethasone dipropionate and formoterol as monotherapies and as part of a combined preparation.
For beclomethasone dipropionate when administered as part of a combined of the drug to its active metabolite beclomethasone-17-monopropionata and value of the maximum concentration plasma is slightly lower, while the absorption is faster than the monopreparation beclomethasone dipropionate.
for formoterol when administered as part of a combined plasma drug coincided with that of the single agent, but systemic activity was slightly higher than that of single agent.
No data obtained what is trenbolone regarding pharmacokinetic or pharmacodynamic interactions between and formoterol:
BDP under the action of esterase is converted to the active metabolite beclomethasone-17-monopropionat .
Inhaled rapidly absorbed light; intense absorption precedes its conversion BDP its active metabolite beclomethasone-17-monopropionata . Systemic bioavailability provided by 36% due to light, and also due to the suction organs of the gastrointestinal tract ingested dose inhalation portion. The bioavailability of ingested is negligible, however, presystemic conversion causes that 41% BDP digested . There is almost a linear increase in systemic effects with increasing inhaled dose. The absolute bioavailability following inhalation is approximately 2% and 62% of the nominal dose in relation to the unmodified , respectively.
The connection to plasma proteins is high enough.
Metabolism is characterized by a very high rate of clearance from the systemic circulation through the action of esterase present in most tissues. The main metabolite of BDP – active metabolite what is trenbolone Less active metabolites are beclomethasone monopropionatand beclomethasone (, which are also formed by metabolism, but their role in systemic exposure is very low. Excretion main part excreted in feces as polar metabolites. Renal excretion of the its metabolites is negligible. The respectively. A special population Liver failure does not alter the pharmacokinetics and safety profile BDP due to the fact that the latter is subjected to rapid metabolism The polar metabolites by the action of enzymes present in the gastro-intestinal tract, blood plasma, lung and liver. The pharmacokinetic properties patients with renal failure has not been studied. Considering that both what is trenbolone and its metabolites in the urine almost not allocated, there is no reason to assume increased systemic action of the drug on the body of patients suffering from renal failure.
Formoterol Absorption and distribution of inhaled formoterol is absorbed into the lungs and gastrointestinal tract. Part inhalation dose that is swallowed, depending on the type of inhalation device and inhalation technique. So when using a metered dose inhaler multidose it can be up to 90%. Therefore swallowed fraction must be considered in the inhalation route of administration of the drug. At least 65% of an oral dose of formoterol is absorbed through the digestive tract, with 70% of this volume it undergoes first-pass metabolism. The maximum concentration of unchanged formoterol in plasma observed for 0.5. 1 hour after oral administration. Communication with plasma proteins of formoterol is from 61-64%, with the affinity to albumin – 34%. The range of therapeutic dosages affinity saturation is not observed.When perroralnom reception hours. Inhalation 12-96 mcg of formoterol fumarate absorption of formoterol is linear. Metabolism Metabolism Formoterol is carried out, in particular, due to the direct conjugation fenolgidroksilnoy group. The conjugates of glucuronic acid is not active. The second important pathway formoterol – O-dimetelirovanie by conjugation at two phenolic hydroxyl groups. Cytochrome P450 enzymes, is involved in the O-demetelirovanii formoterol. There is reason to assume that formoterol metabolism is carried out mainly in the liver. Formoterol does not inhibit what is trenbolone enzymes at therapeutically relevant concentrations. Excretion Total formoterol renal excretion following inhalation of a single dose via metered dry powder inhaler increases linearly in the dose range 12-96 mg. Indicators and excretion of unchanged total formoterol, on average, are 8 and 25%, respectively. Based on the measurement of plasma concentrations of formoterol after single inhalation of a dose of 120 mg in 12 healthy volunteers was designated , which was 10 hours. The ratio (R, R) – and (S, S) enantiomers of unchanged drug in renal excretion is respectively 40 and 60%. The relative ratio of these two parameters is not changed within the range of dosages investigated; . no evidence of accumulation of one enantiomer relative to the other after receiving repeated doses in healthy volunteers after oral administration (40-80 mg), 6.10% of the dose was found in the urine as unchanged drug; 8% of the dose was present in the form of glucuronides. Total 67% of the oral dose excreted by the kidneys formoterol (mainly as metabolites), the remainder of the dose – via the intestine. Renal clearance of formoterol is 150 ml / min. personal trainer for bodybuilding laser lipo machine bodybuilding magazine free