circulatory disorders:<\/i> often \u2013 drop in blood pressure (in some cases pronounced, up to collapse and loss of consciousness).<\/p>\n
<\/p>\n
Tizanidine is a centrally acting muscle relaxant. Its main site of action is in the spinal cord. By stimulating presynaptic alpha2<\/sub>receptors, it inhibits the release of excitatory amino acids that stimulate the N-methyl-D-aspartate (NMDA) receptors. As a result, polysynaptic excitation transmission at the level of the intermediate neurons of the spinal cord is inhibited. Since this mechanism is responsible for the excessive muscle tension, muscle tension is reduced after inhibition. In addition to its myorelaxant properties, tizanidine also exhibits a central, moderately pronounced analgesic effect.<\/p>\n Sirdalud\u00ae is effective in both acute painful muscle spasms and chronic spasticity of spinal and cerebral origin. It reduces spasticity and clonic spasms, reducing resistance to passive movements and increasing the volume of active movements.<\/p>\n The myorelaxing effect (measured with the Ashworth scale and the pendulum test) and the side effects (decrease in heart rate and blood pressure) of Sirdalud\u00ae depend on the plasma concentration of the drug.<\/p>\n Absorption.<\/i> Tizanidine is rapidly and almost completely absorbed. TMax<\/sub> in the plasma lies 1 hour after administration of the drug. Due to the important hepatic first-pass metabolism, the average bioavailability is approximately 34 %. CMax<\/sub> of tizanidine is 12.3 and 15.6 ng\/mL after a single and multiple dose of 4 mg, respectively.<\/p>\n Distribution.<\/i> The middle Vss<\/sub> after intravenous administration of tizanidine is 2.6 l\/kg. Binding to plasma proteins is 30 %.<\/p>\n Metabolism.<\/i> Tisanidine has been shown to be rapidly and extensively (about 95% %) metabolised in the liver. in vitro<\/i> it has been shown that tizanidine is primarily metabolised by the isoenzyme CYP1A2. The metabolites are inactive.<\/p>\n Excretion.<\/i> The middle T1\/2<\/sub> of tizanidine from systemic blood flow is 2-4 hours. The drug is excreted mainly through the kidneys (about 70 % of the dose) in the form of metabolites, of which about 4.5 % are unchanged.<\/p>\n effect of food.<\/i> Concomitant intake with food does not affect the pharmacokinetics of tizanidine. Although CMax<\/sub> although increased by a third when the tablet is taken after a meal, this is not considered clinically significant. No significant effect on absorbance (AUC) was observed.<\/p>\n Tizanidine in the dose range of 1 to 20 mg has linear pharmacokinetics.<\/p>\n Details of pharmacokinetics in different patient groups<\/i><\/p>\n Patients with impaired renal function.<\/i> In patients with renal impairment (creatinine Cl \u226425 mL\/min), the maximum mean plasma concentration is 2-fold higher than in healthy subjects, the final T1\/2<\/sub> reaches 14 hours, resulting in an increased (approximately 6-fold) systemic bioavailability of tizanidine (as measured by AUC).<\/p>\n Patients with impaired liver function.<\/i> No specific studies have been conducted in this patient category. Tizanidine is primarily metabolised in the liver by the cytochrome CYP1A2; therefore, hepatic impairment may result in increased systemic exposure.<\/p>","protected":false},"excerpt":{"rendered":" Durchblutungsst\u00f6rungen: h\u00e4ufig – Blutdruckabfall (in einigen F\u00e4llen ausgepr\u00e4gt, bis hin zu Kollaps und Bewusstlosigkeit). Pharmakologische Wirkungen Tizanidin ist ein zentral wirkendes Muskelrelaxans. Sein Hauptwirkungsort liegt im R\u00fcckenmark. Durch Stimulierung pr\u00e4synaptischer Alpha2-Rezeptoren hemmt es die Freisetzung von erregenden Aminos\u00e4uren, die die Rezeptoren f\u00fcr N-Methyl-D-Aspartat (NMDA-Rezeptoren) stimulieren. Infolgedessen wird die polysynaptische Erregungs\u00fcbertragung auf der Ebene der Zwischenneuronen […]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"crb-meta-links":"","crb-meta-show":"","crb-meta-show-edited":"","crb-meta-use-manual":"","footnotes":""},"categories":[3],"tags":[],"class_list":["post-3357","post","type-post","status-publish","format-standard","","category-artikel"],"yoast_head":"pharmacokinetics<\/h2>\n