Farmakologik xususiyatlari
Levofloksatsin - sintetik antibakterial preparat keng spektrli ta'sirga ega florokinolonlar guruhidan bo'lib, faol modda sifatida levofloksatsin - ofloksatsinning levovratsiyalovchi izomeri mavjud. Levofloksatsin DNK-girazani bloklaydi, superspiralizatsiyani va DNK uzilishlarini bog'lashni buzadi, DNK sintezini inhibe qiladi, sitoplazmada, hujayra devorida va membranalarda chuqur morfologik o'zgarishlarni keltirib chiqaradi.
Levofloksatsin ko'p mikroorganizmlar shtammlariga nisbatan in vitro va in vivo sharoitlarda faol. Aerob grammusbat mikroorganizmlar: Corynebacterium diphtheriae, Enterococcus faecalis, Enterococcus spp, Listeria monocytogenes, Staphylococcus koagulaza-negativ methi-S(I), Staphylococcus aureus methi-S, Staphylococcus epidermidis methi-S, Staphylococcus spp (CNS), Streptococci guruh C va G, Streptococcus agalactiae, Streptococcus pneumoniae peni I/S/R, Streptococcus pyogenes, Viridans streptococci peni-S/R. Aerob grammanfiy mikroorganizmlar: Acinetobacter baumannil, Acinetobacter spp, Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter spp, Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae ampi-S/R, Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella oxytoca, Klebsiella pneumoniae, Klebsiella spp, Moraxela catarrhalis ?+/?-, Morganella morganii, Neisseria gonorrhoeae non PPNG/PPNG, Neisseria meningitidis, Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida, Pasteurella spp, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Providencia spp, Pseudomonas aeruginosa, Pseudomonas spp, Salmonella spp, Serratia marcescens, Serratia spp. Anaerob mikroorganizmlar: Bacteroides fragilis, Bifidobacterium spp, Clostridium perfringens, Fusobacterium spp, Peptostreptococcus, Propionibacterum spp, Veilonella spp. Boshqa mikroorganizmlar: Bartonella spp, Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Legionella spp, Mycobacterium spp, Mycobacterium leprae, Mikobakterium tuberkulosi, Mycoplasma hominis, Mycoplasma pneumoniae, Ricketsia spp, Ureaplasma urealyticum.
Farmakokinetika
IV 60 daqiqalik infuziya orqali 500 mg levofloksatsin berilgandan so'ng, sog'lom ko'ngilli shaxslarda plasmaning o'rtacha pik konsentratsiyasi 6,2 mkg/ml ni tashkil etdi. 500 mg levofloksatsin bir martalik qabul qilinganda farmakokinetik xususiyatlar mos ravishda: Cmax 6,2±1,0 mkg/ml, Tmax - 1,0±0,1 soat, yarim chiqarilish davri 6,4±0,7 soat.
Levofloksatsinning farmakokinetikasi chiziqli xarakterga ega va bir martalik va ko'p martalik kiritishda bashorat qilinadi. Levofloksatsinning plasmadagi konsentratsiya profili IV kiritishdan so'ng tabletkali qabul qilishdagi kabi, shuning uchun, og'zaki va IV kiritish yo'llari o'zaro almashtirilishi mumkin. Levofloksatsinning o'rtacha taqsimlanish hajmi bir martalik va ko'p martalik 500 mg IV dozadan so'ng 89 dan 112 l gacha. Plazma oqsillari bilan bog'lanish 30-40% ni tashkil etadi. Levofloksatsinning o'rtacha oxirgi yarim chiqarilish davri bir martalik yoki ko'p martalik dozadan so'ng 6 dan 8 soatgacha.
Levofloksatsin organlar va to'qimalarga yaxshi kiradi: o'pka, bronxlarning shilliq qavati va balg'am, siydik-tashqarish tizimi organlari, jumladan, prostata bezi, suyak to'qimasi, orqa miya suvi, polimorfnuklear leykotsitlar, alveolyar makrofaglar. Levofloksatsin asosan siydik bilan o'zgarmagan holda chiqariladi. Jigarida kichik qismi oksidlanadi va/yoki dezasetilatsiyalanadi. Og'zaki qabul qilingandan so'ng taxminan 87% qabul qilingan dozadan 48 soat ichida o'zgarmagan holda siydik bilan chiqariladi. 72 soat davomida najasda 4% dan kam aniqlangan.