Bronchodilation following inhaled tiotropium is the result of local rather than a systemic effect.
It has been shown that significant increases deca durabolin injection pulmonary function minutes after the single dose for 24 hours. Pharmacodynamic balance is achieved within the first week, and expressed bronhodilyatiruyuschy effect was observed on day 3. Spiriva significantly increases the morning and evening peak expiratory stream velocity, measured by patients. Bronhodilyatiruyuschy effect Spiriva, estimated during the year, did not reveal the manifestations of tolerance.
Spiriva significantly reduces the number of exacerbations is increasing and the period until the first exacerbation compared to placebo.
Spiriva significantly improves the quality of life. This improvement is observed throughout the entire period of treatment.
It has been shown that the Spiriva significantly reduces hospitalizations associated exacerbations and increases the time until the first admission.
Quaternary ammonium compound, sparingly soluble in water . Absorption Inhalation route of administration, the absolute bioavailability of tiotropium is 19.5%, indicating that the fraction of drug that reaches the lungs, high bioavailability. Based on the chemical structure of the compound (quaternary ammonivoe connection), tiotropium is poorly absorbed from the gastrointestinal tract. For this reason, eating does not affect the absorption of tiotropium. Admission into the solutions of tiotropium have an absolute bioavailability equal to 2-3%. Tiotropium maximum concentration in plasma after inhalation achieved after 5 minutes. . Studies have shown that tiotropium does not penetrate the blood-brain barrier.
The biotransformation. The extent of biotransformation is small. This is confirmed by the fact that after intravenous administration to healthy young volunteers detected in urine 74% unmodified substance.Tiotropium cleaved neferment¬nym way to alcohol and N-metilskopina ditienilglikolivoy acids which do not bind to muscarinic receptors.
In studies showed that the drug is metabolized by cytochrome the process depends on the oxidation and subsequent conjugation with glutathione to form various metabolites. Violation of metabolism may occur when using inhibitors (quinidine, ketoconazole and gestodene). Therefore, deca durabolin injection are included in the drug metabolism. Tiotropium even sverhterapevticheskih concentrations did not inhibit cytochrome human liver microsomes.
Excretion. The terminal half-life after inhalation of tiotropium is 5-6 days. Total clearance when administered intravenously to healthy young volunteers is 880ml / min, and individual variability of 22%.Tiotropium after intravenous administration is mainly excreted by the kidneys in unchanged form (74%). After dry powder inhalation renal excretion of 14% of the dose remaining unabsorbed portion is output from the intestine. Renal clearance of tiotropium exceeds the creatinine clearance, indicating that tubular secretion of the drug. After prolonged administration of the drug once a day by patients , pharmacokinetic equilibrium is reached after 2-3 weeks, with no further accumulation is observed.
Tiotropium has a linear pharmacokinetics in the therapeutic range after intravenous administration and dry powder inhalation deca durabolin price.
Elderly patients: In elderly patients there is a decrease of tiotropium renal clearance , that can be explained by a decrease in kidney function. After inhalation Tiotropium excretion in the urine is reduced from 14% (young healthy volunteers) to 7% deca durabolin injection, however plasma concentrations did not significantly changed in elderly patients , given the inter – and intraindividual variability (43% increase in the AUC0- 4 after inhalation of dry powder.
Patients with impaired renal function: As with the other tools, Rui-egestas mainly kidneys, reducing kidney function resulted in increased drug concentration in blood plasma and reduced renal clearance following intravenous administration and inhalation administration. Mild decrease in renal function (creatinine clearance of 50-80 ml / min) often observed in elderly patients, increased tiotropium plasma concentrations slightly ). Patients with moderate or severe degree of decrease in renal function (creatinine clearance <50 ml / min) after intravenous administration of tiotropium observed a twofold increase in the blood plasma concentration (82% increase AUC0-4), compared with the concentrations in the blood plasma determined after inhalation of dry powder.
Patients with impaired liver function: It is assumed that hepatic impairment will not have a significant effect on the pharmacokinetics of tiotropium as tiotropium is mainly excreted by the kidneys and the formation of pharmacologically inactive metabolites is not associated with an enzymatic process. anabolic steroids online shop
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