Moxifloxacin - malangizo azomwe angagwiritsidwe ntchito

Kufotokozera kogwirizana ndi 30.01.2015

  • Dzina lachi Latin: Moxifloxacine
  • Code ya ATX: J01MA14
  • Chithandizo: Moxifloxacin (Moxifloxacin)
  • Wopanga: Vertex (Russia), Macleods Pharmaceutical (India).

Piritsi 1 moxifloxacin hydrochloride 400 mg

Cellulose, lactose monohydrate, hydroxypropyl cellulose, magnesium stearate, hypromellose, polyethylene glycol, titanium dioxide, talc, iron oxide ofiira, monga okonda.

Pharmacodynamics ndi pharmacokinetics

Mankhwala

Mankhwala antibacterial kuchokera pagulu la IV mbadwo wa quinolones (trifluoroquinolone), amachita bactericidal. Imalowa mu cell ya tizilomboti totseka ndipo timabisika nthawi imodzi enzymekuchita nawo kubwereza kwa DNA ndikuwongolera zomwe zimapangidwa ndi DNA, zomwe zimabweretsa kusintha kwakukulu mu khoma la maselo, kusokoneza kwa mapangidwe a DNA ndi kufa kwa tizilomboti.

Moxifloxacin amawonetsa bactericidalkuchitapo kanthu poyerekezera ndi tizilombo toyambitsa matenda, gram-positive ndi gram-tizilombo tating'onoting'ono. Kugwiritsa ntchito motsutsana ndi anaerobes, osagwira asidi komanso mabakiteriya atypical. Ndi imodzi mwa yogwira staphylococci, kuphatikiza ndi methicillin zosagwira staphylococci. Kuchita mycoplasmas wamkulu Levofloxacinndi chlamydia - Ofloxacin.

Palibe kukana ndi penicillin, aminoglycosides, macrolidesndi cephalosporins. Kuchulukana kwa mankhwala kumakhala kochepa, kukana kumayamba pang'onopang'ono. Mankhwala alibe photosensitizing. Zotsatira za mankhwalawa zimagwirizana mwachindunji ndi kukhudzidwa kwake magazi ndipo minofu ndipo imatsatana ndi kutulutsa pang'ono poizonichifukwa chake palibe chiopsezo chotukuka kuledzera motsutsana ndi maziko a chithandizo.

Pharmacokinetics

Moxifloxacin pambuyo m`kamwa makonzedwe kwathunthu odzipereka. Bioavailability ndi 91%. Kuchuluka kwa mankhwalawa kumawonedwa pambuyo pa maola 0.5-4, ndipo patatha masiku atatu a kudya pafupipafupi, mulingo wake wokhazikika umatheka. Mankhwalawa amagawidwa mu minofu, ndipo chidwi chake chimatsimikizika mu kupuma komanso khungu. Nthawi T 1/2 - maola 12. Imafufutidwa ndi impso komanso kudzera m'mimba.

Zizindikiro zogwiritsidwa ntchito

  • Chifuwa chachikulu (kuphatikiza mankhwala ena a anti-TB, ngati mankhwala a mzere wachiwiri),
  • matenda opuma: hr bronchitis pachimake, sinusitis, chibayo,
  • matenda amkati ndi m'mimba,
  • matenda a pakhungu ndi minofu yofewa.

Contraindication

  • zolemetsa kulephera kwa chiwindi,
  • Hypersensitivity
  • pseudomembranous colitis,
  • wazaka 18
  • chizolowezi chodwala,
  • mimba.

C imayikidwa mosamala pakukweza nthawi ya Q-T, myocardial ischemia, makamaka bradycardia, hypokalemia, pamene akumwabe corticosteroids.

Zotsatira zoyipa

  • Kupweteka kwam'mimba kusanza, kusanza, kudzimbidwa,kuchuluka kwa transaminase, kamwa yowuma, matenda a anorexia, candidiasis pamlomo wamkamwagastritis, dysphagia,kusintha kwamitundu
  • chizungulire, asthenia, kusowa tulo, mutu, kumverera nkhawa, paresthesia. Osowa kwambiri - zovuta kumayankhula, kuyerekezera, kukokana,chisokonezo,
  • Kusintha kwa kukoma
  • tachycardiakupweteka pachifuwa, kuchuluka HEREKutalika kwa Q-T,
  • kupuma movutikiraosowa - zolanda mphumu ya bronchial,
  • arthralgiakupweteka kumbuyo
  • nyini candidiasiskuwonongeka kwaimpso,
  • zotupa, urticaria,
  • leukopenia, eosinophilia, kuchepa magazi, thrombocytosis, hyperglycemia.

Kuchita

Maantacididi, ma multivitaminindi mchere komanso Ranitidine amalepheretsa mayamwidwe ndikuchepetsa kuchuluka kwa mankhwalawa mu plasma. Ayenera kutumikiridwa maola 2 atatha kumwa mankhwala. Kukonzekera kwazitsulo, sucralfate kuchepetsa kwambiri bioavailability, ayenera kugwiritsidwa ntchito pambuyo maola 8.

Kugwiritsa ntchito nthawi yomweyo kwa ena quinoloneszimawonjezera chiopsezo chowonjezera nthawi ya Q-T kangapo. Moxifloxacin amakhudza pang'ono pharmacokinetics Digoxin.

Mukutenga Warfarin muyenera kuwongolera zizindikiro za coagulation. Phwando corticosteroids chiopsezo chowonjezeka cha tendon ndi mawonekedwe a tendovaginitis.

Mankhwala

Mankhwala


Moxifloxacin ndi mankhwala osiyanasiyana a bactericidal antibacterial, 8-methoxyphoroquinolone. Mphamvu ya bactericidal ya moxifloxacin imachitika chifukwa cha kuletsa kwa bakiteriya topoisomerases II ndi IV, komwe kumayambitsa kusokonezeka kwa njira zobwereza, kukonza ndi kusindikiza kwa DNA biosynthesis yama cell tizilombo tating'onoting'ono ndipo, chifukwa chake, pakufa kwa maselo okhala ndi ma cell ochepa.
Ma proteinicidal osachepera moxifloxacin nthawi zambiri amatha kuyerekeza ndi ma inhibitory concentrations (MICs).
Njira zopewera


Njira zomwe zimatsogolera pakupanga kukana kwa penicillins, cephalosporins, aminoglycosides, macrolides ndi tetracyclines sizimakhudzana ndi antibacterial zochita za moxifloxacin. Palibe kutsutsana kwapakati pa magulu awa a antibacterial mankhwala ndi moxifloxacin. Pakadali pano, sipanakhalepo zochitika za kukana kwa plasmid. The pafupipafupi kukula kwa kukana ndi ochepa kwambiri (10 -7 -10 -10). Kukana kwa Moxifloxacin kumayamba pang'onopang'ono kudzera pakusintha kambiri. Kuchulukanso kwa moxifloxacin pama cellorganic oyenda pansipa MIC amaphatikizidwa ndi kuwonjezeka pang'ono chabe kwa MIC. Milandu yotsutsana ndi quinolones imadziwika. Komabe, tizilombo tating'onoting'ono tokhala ndi gramu komanso anaerobic osagwirizana ndi ma quinolones ena timawaganizirabe moxifloxacin.
Kukhazikitsidwa kuti kuwonjezeranso kwa gulu la methoxy mu mawonekedwe a C8 ku moxifloxacin mamolekedwe a moxifloxacin kumawonjezera ntchito ya moxifloxacin ndikuchepetsa mapangidwe a mabakiteriya osintha a mabakiteriya oyenera. Kuphatikizidwa kwa gulu la bikcloamine paudindo C7 kumalepheretsa kukhazikika kwa yogwira ntchito, njira yotsutsana ndi fluoroquinolones.
Moxifloxacin mu vitro yogwira polimbana ndi tizilombo tating'onoting'ono ta gramu-gramu komanso gramu-zabwino, anaerobes, mabakiteriya osagwira asidi komanso mabakiteriya atypical monga Mycoplasma spp., Chlamydia spp., Legionella $ pp.komanso mabakiteriya osagonjetsedwa ndi ß-lactam ndi macrolide maantibayotiki.
Zokhudza matumbo microflora


M'maphunziro awiri omwe adachitika pa odzipereka, kusintha kwa microflora yam'mimba kunawonekera pambuyo pakukonzekera kwa moxifloxacin. Kutsika kwazowonetseratu kunadziwika. Escherichia coli, Bacillus spp., Bacteroides vulgatus, Enterococcus spp., Klebsiella spp.komanso anaerobes Bifidobacterium spp., Eubacterium spp., Peptostreptococcus spp. Kusintha kumeneku kunasinthidwa mkati mwa milungu iwiri. Zoopsa Clostridium Hardile sanapezeke.
Mu Mayeso a Vitro Sensitivity


Mphamvu ya antibacterial zochita za moxifloxacin imaphatikizanso zotsatirazi:

Zomvera Wotengeka pang'onoKutsutsa
Zabwino
Gardnerella vaginalis
Streptococcus chibayo
(kuphatikiza tizilombo ta penicillin ndi mabakiteriya okhala ndi maantibayotiki ambiri), komanso tizilombo ta mankhwala awiri kapena angapo, monga penicillin (MIC> 2 mg / ml), IIep cephalosporins (mwachitsanzo cefuroxime), macrolides, tetracyclines, trimethoprim / sulfamethoxazole
Streptococcus pyogene
(gulu A) *
Gululi Streptococcus milleri (S. anginosus * S. constellatus * ndi interrnedius *)
Gululi Streptococcus viridans (S. viridans, S. mutans, S. mitis, S. sanguinis, S. salivarius, S. thermophilics, S. constellatus)
Streptococcus agalactiae
Streptococcus dysgalactiae
Staphylococcus aureus
(kuphatikiza mitsempha yokhala ndi methicillin)
Staphylococcus aureus
(methicillin / ofloxacin immune bacteria) *
Coagulonegative Staphylococci (S .. cohnii, S. epidermic! Ndi, S. haemolyticus, S. hominis, S. saprophytic us, S s ​​imulans)michere yokhala ndi methicillinCoagul yogwira staphylococci (S.cohnii, S. epidermic / ndiye, S. haemolyticus, S. nyanga mu,, S.saprophytics, S. simulans)methicillin kugonjetsedwa tizilombo ta
Enterococcus faecalis* ((Ndi zovuta zokha za vancomycin ndi glamicin)
Enterococcus avium *
Enterococcus faecium *
Zabwino
Haemophilus influenzae
(kuphatikiza zingwe zopanga ndi mafuta osatulutsa)
Haemophillus parainfluenzae*
Moraxella catarrhalis (kuphatikiza zingwe zopanga ndi mafuta osatulutsa)
Bordetella pertussis
Legionella pneumophilaEscherichia coli *
Acinetobacter baumaniiKlebsiella pneumoniae *
Klebsiella oxytoca
Cikrobacter freundii *
Enterо bader spp. (E.aerogene, E.intermedins, E.sakazakii)
Enterobacter cloacae *
Pantoea agglomerans
Pseudomonas aeruginosa
Pseudomonas fluorescens
Burkholderia cepacia
Stenotrophomonas maltophilia
Proteus mirabilis *
Proteus vulgaris
Morganella morganii
Neisseria gonorrhoeae *
Providencia spp. (P. rettgeri, P. Stuartii)
Anaerobes
Bacteroides spp. (B.fragi / ni * B. Distasoni * Mu thetaiotaomicron *, B. ovatus *, B. yunifolomu ndi *, B. vulgaris *)
Fusobacterium spp.
Peptos treptococcus spp. *
Porphyromonas spp.
Prevotella spp.
Propionibacterium spp.
Clostridium spp. *
Zachikale
Chlamydia pneumoniae *
Chiamydia trachomatis *
Mycoplasma pneumoniae *
Mycoplasma hominis
Mycoplasma genitalium
CoxieIla burnettii
Legionella pneumohila
* Kuzindikira kwa moxifloxacin kumatsimikiziridwa ndi zidziwitso zamankhwala.

Kugwiritsidwa ntchito kwa moxifloxacin sikulimbikitsidwa pochiza matenda omwe amayamba chifukwa cha methicillin tizilombo ta S. aureus (MRSA). Pankhani ya matenda okayikiridwa kapena kutsimikiziridwa oyambitsidwa ndi MRSA, mankhwala omwe ali ndi antibacterial mankhwala oyenera ayenera kuyikidwa.
Kwa zovuta zina, kufalikira kwa kukhudzika komwe kumachitika kungasiyane ndi dera komanso nthawi. Pankhaniyi, poyesa kumva kupsinjika, ndikofunikira kukhala ndi chidziwitso chakudziko chokana, makamaka pochiza matenda oopsa.
Ngati odwala akuchipatala, m'chipindacho ndimomwe amapangira pharmacokinetic curve (AUC) / MHK90 zopitilira 125, ndi kuchuluka kwa plasma concentration (Cmax) / MIC90 ili pamtundu wa 8-10 - izi zikuwonetsa kusintha kwamankhwala. Muzochitika kunja, magawo okhala ndi izi nthawi zambiri amakhala otsika: AUC / MIC90>30-40.

Parame (mtengo wapakati) AUIC * (h)Cmax / MIC90
(kulowetsedwa kwa 1 h)
MIC90 0.125 mg / ml31332,5
MIC90 0.25 mg / ml15616,2
MIC90 0,5 mg / ml788,1
* AUIC - dera lomwe lili pansi pa chipondacho (ratio (AUC) / MMK)90).

Pharmacokinetics
Zogulitsa
Pambuyo pa kulowetsedwa kamodzi kwa moxifloxacin pa mlingo wa 400 mg wa 1 h, C max amafikira kumapeto kwa kulowetsedwa ndipo pafupifupi 4.1 mg / l, omwe amafanana ndi kuwonjezeka kwa pafupifupi 26% poyerekeza ndi phindu la chidziwitso ichi mukamamwa moxifloxacin pakamwa. Kuwonekera kwa moxifloxacin, wokhazikika ndi chisonyezo cha AUG, kumapitirira pang'ono poyerekeza ndi kuyamwa kwa moxifloxacin. Mtheradi bioavailability pafupifupi 91%. Pambuyo mobwerezabwereza kulowetsedwa kwa moxifloxacin pa mlingo wa 400 mg kwa ola limodzi, pazowonjezera zochepa komanso zochepa zomwe zimayambira kuchokera ku 4.1 mg / L mpaka 5.9 mg / L komanso kuchokera ku 0.43 mg / L mpaka 0,84 mg / L, motero. Chiyero chokhazikika cha 4.4 mg / L chimakwaniritsidwa kumapeto kwa kulowetsedwa.
Kugawa
Moxifloxacin imagawiridwa mwachangu mu minofu ndi ziwalo ndipo zimamangiriza kumaproteni amwazi (makamaka albin) ndi pafupifupi 45%. Kuchuluka kwa magawidwe kumakhala pafupifupi 2 l / kg.
Kuzungulira kwa moxifloxacin, ochulukitsa omwe ali m'madzi am'magazi, amapangika m'matumbo am'mapapu (kuphatikizapo epithelial fluid, alveolar macrophages), mu sinuses (maxillary and ethmoid sinuses), mu mphuno zamkamwa, poyang'ana kutupa (pazomwe zili ndi matuza zotupa za pakhungu). Pazipinda zamkati komanso malovu, moxifloxacin imatsimikiziridwa mwaulere, osaphatikizidwa ndi mapuloteni, pamsasa wambiri kuposa plasma wamagazi. Kuphatikiza apo, ma moxifloxacin amadziwika kwambiri pamatumbo am'mimba, zotupa za peritoneal, komanso ziwalo zoberekera wamkazi.
Kupenda
Moxifloxacin akudutsa gawo lachiwiri ndipo amamuchotsa kuchokera ku thupi ndi impso, matumbo, osasinthika komanso mawonekedwe osakanikirana a mankhwala a Soffo (Ml) ndi glucuronides (M2).
Moxifloxacin sanapangidwe biocransformed ndi microsomal cytochrome P450 system. Ma metabolabolites Ml ndi M2 amapezeka m'magazi am'magazi mozama kuposa gawo lawolo. Malinga ndi zotsatira za maphunziro oyamba, zimatsimikiziridwa kuti ma metabolites awa samakhala ndi vuto lililonse mthupi poteteza komanso kulolera.
Kuswana
Hafu ya moyo wa moxifloxacin ndi pafupifupi maola 12. Pafupifupi chilolezo chotsatira pambuyo pa 400 mg ndi 1 79-246 ml / min. Chilolezo cha renal ndi 24-53 ml / min. Izi zikuwonetsa kubwezeretsanso kwakanthawi kwa moxifloxacin.
Mulingo woyambira wopanga gawo ndi gawo 2 metabolites pafupifupi 96-98%, zomwe zikuwonetsa kusowa kwa metabolid oxidative. Pafupifupi 22% ya mlingo umodzi (400 mg) umatuluka osagwirizana ndi impso, pafupifupi 26% - ndi matumbo.
Pharmacokinetics m'magulu osiyanasiyana odwala
Zaka, jenda komanso fuko
Kafukufuku wa pharmacokinetics a moxifloxacin mwa abambo ndi amayi adawonetsa kusiyana kwa 33% malinga ndi AUC ndi Cmax. Kudziwika kwa moxifloxacin sikudalira jenda. Kusiyana kwa AUC ndi Cmax kunachitika makamaka pakusiyana kwa kulemera kwa thupi kuposa jenda ndipo sikofunika kuchipatala.
Panalibe kusiyana kwakukulu kachipatala mu pharmacokinetics ya moxifloxacin mwa odwala amitundu yosiyanasiyana ndi mibadwo yosiyana.
Ana
Ma pharmacokinetics a moxifloxacin mwa ana sanaphunzire.
Kulephera kwina
Panalibe kusintha kwakukulu mu pharmacokinetics ya moxifloxacin odwala omwe ali ndi vuto la Impso (kuphatikiza odwala omwe ali ndi chilolezo cha creatinine 2) komanso odwala omwe akupitilira hemodialysis wopitilira nthawi yayitali.
Kuwonongeka kwa chiwindi

Panalibe kusiyana kwakukulu pakuchitika kwa moxifloxacin mwa odwala omwe ali ndi vuto la chiwindi (Makulidwe a ana-Pugh A ndi gulu la B) poyerekeza ndi odzipereka athanzi komanso odwala omwe ali ndi vuto lolimba la chiwindi (kuti mugwiritse ntchito odwala omwe ali ndi matenda a cirrhosis, onaninso gawo la "Malangizo apadera" )

Mlingo ndi makonzedwe


Mlingo wovomerezeka wa moxifloxacin: 400 mg (250 ml ya njira yothetsera kulowetsedwa) 1 kamodzi patsiku ndi matenda omwe tawonetsedwa pamwambapa. Musapitirire mlingo woyenera.
Kutalika kwa mankhwala


Kutalika kwa mankhwalawa kumatsimikiziridwa ndi malo komanso kuuma kwa matendawa komanso matenda.

  • Chibayo chodziwika ndi anthu ammudzi: kutalika kwa mankhwala ophatikizidwa ndi moxifloxacin
  • Matenda ovuta a pakhungu ndi mapangidwe anthawi zonse: Kutalika kokwanira kwa mankhwala ndi moxifloxacin ndi masiku 7 mpaka 21,
  • Zovuta zam'mimba zam'mimba matenda: kutalika kokwanira kwa mankhwala ndi moxifloxacin ndi masiku 5 mpaka 14.
Musapitirire nthawi yolimbikitsidwa. Malinga ndi maphunziro azachipatala, kutalika kwa mankhwalawa ndi moxifloxacin kumatha kufika masiku 21.
Odwala okalamba


Kusintha kwa dongosolo la odwala okalamba sikofunikira.
Ana


Kuchita bwino ndi chitetezo cha kugwiritsa ntchito moxifloxacin mwa ana ndi achinyamata sichinakhazikitsidwe.
Kuchepa kwa chiwindi (Mwana ndi Pgh mkalasi L ndi B)


Odwala omwe ali ndi vuto la chiwindi safunika kusintha mtundu wa mankhwalawa (kuti mugwiritse ntchito odwala omwe ali ndi chiwindi, onani gawo la "Special Instructions").
Kulephera kwina


Odwala omwe ali ndi vuto la impso (kuphatikizira omwe ali ndi vuto laimpso kulephera kwa mawonekedwe a 30 ml / mphindi / 1.73 m 2), komanso mwa odwala omwe akupitilira hemodialysis ndi kupitilira kwa nthawi yayitali. .
Gwiritsani ntchito odwala a mitundu yosiyanasiyana


Kusintha kwa regimen ya kuchuluka sikofunikira.
Njira yogwiritsira ntchito


Mankhwala chikuyendetsedwera kudzera mu mawonekedwe a kulowetsedwa osachepera mphindi 60, onse osachiritsika komanso osakanikirana ndi izi:

  • madzi a jakisoni
  • 0,9% sodium kolorayidi njira,
  • 1M sodium chloride solution,
  • 5% dextrose solution,
  • 10% yankho la dextrose,
  • 40% dextrose yankho,
  • 20% xylitol yankho,
  • yankho la ringer
  • yankho la ringer
Ngati mankhwala a moxifloxacin, njira yothetsera kulowetsedwa, amagwiritsidwa ntchito molumikizana ndi mankhwala ena, ndiye kuti aliyense ayenera kupatsidwa mankhwala mosiyanasiyana.
Kusakaniza kwa yankho la mankhwalawa ndi mayankho omwe ali pamwambapa kumakhalabe kosatha kwa maola 24 kutentha kwa chipinda.
Popeza njira yothetsera vutoli siitha kugundidwa kapena kuzirala, siyitha kusungidwa mufiriji. Pakazizira, mpweya umatha kukhala womwe umasungunuka kutentha kwa firiji. Njira yothetsera vutoli iyenera kusungidwa mu ma CD ake. Yankho lomveka lokha liyenera kugwiritsidwa ntchito.

Zotsatira zoyipa


Simungathe kulowetsamo yankho la moxifloxacin nthawi imodzi ndi njira zina zosagwirizana ndi izo, zomwe zimaphatikizapo:

  • 10% sodium kolorayidi njira,
  • 20% sodium kolorayidi njira,
  • 42% sodium bicarbonate solution,
  • 84% sodium bicarbonate solution.

Malangizo apadera

Zokhudza mphamvu pakutha kuyendetsa magalimoto ndi zida

Fluoroquinolones, kuphatikiza moxifloxacin, imatha kuchepetsa mphamvu ya odwala kuyendetsa magalimoto ndi kuchita zina zomwe zingakhale zoopsa zomwe zimafunikira chidwi chochulukirapo komanso kuthamanga kwa zochitika zama psychomotor chifukwa chazovuta zamkati wamanjenje komanso kuwonongeka kwa mawonekedwe.

Wopanga

Wogwirizira Sitifiketi Yoyang'anira
LLC PROMOMED RUS, Russia,
101000, Moscow, Arkhangelsky Lane, 1, nyumba 1

Adilesi yovomerezeka:
Russia, Republic of Mordovia,
430030, Saransk, St. Vasenko, 1 5A.

Adilesi ya malo opangira:
Russia, Republic of Mordovia,
430030, Saransk, St. Vasenko, 15A.

Tchulani, adilesi ndi nambala yafoni ya bungwe lovomerezeka loyitanirana (kutumiza madandaulo ndi zodandaula):
LLC PROMOMED RUS, Russia,
129090, Moscow, Prospect Mira, d. 13, p. 1.

Kupanga ndi mawonekedwe a kumasulidwa

Moxifloxacin amapezeka m'mitundu itatu: yankho la kulowetsedwa, mapiritsi olimbitsa pakamwa komanso madontho amaso. Mawonekedwe awo:

Mapiritsi achikasu a Biconvex

The kuchuluka kwa moxifloxacin hydrochloride, mg

Yellow iron oxide, calcium stearate, titanium dioxide, chimanga wowuma, talc, croscarmellose sodium, macrogol, polyvinyl mowa, mannitol, opadra, cellcrystalline cellulose, povidone, hydroxypropyl cellulose, hypromellose, polyethylene glycol

Sodium Chloride, Sodium Hydroxide, Hydrochloric Acid, Madzi

Sodium hydroxide, sodium chloride, hydrochloric acid, boric acid, madzi

Matumba a ma PC 5, 1 kapena matuza awiri mumphika

Mabotolo 250 ml

5 ml mabotolo opopera a polyethylene

Mlingo ndi makonzedwe

Mitundu yosiyanasiyana ya kumasulidwa kwa mankhwalawa imasiyana m'njira zogwiritsira ntchito. Mapiritsiwo adapangira kuti pakhale pakamwa, yankho limaperekedwa kwa makolo, ndipo madontho amapaka m'maso ndi matenda opatsirana omwe amafananirako. Mlingo umatengera kuuma kwa matendawa, mtundu wake, machitidwe a wodwala. Zambiri zimaperekedwa mu malangizo.

Pa nthawi yoyembekezera

Pakubala kwa mwana, kumwa mankhwala opatsirana kumapangidwa, pokhapokha ngati phindu la mayiyo silipitirira chiopsezo kwa mwana wosabadwayo. Kafukufuku wokhudza chitetezo cha mankhwalawa panthawi yomwe ali ndi pakati sanachitike. Popereka mankhwala pakupatsa mkaka, kuyamwitsa mwana kuyenera kuthetsedwa, chifukwa zomwe zimapangidwira zimalowa mkaka wa m'mawere ndipo zimasokoneza thanzi la mwana.

Kuyanjana kwa mankhwala osokoneza bongo

Musanayambe mankhwala ndi Moxifloxacin, kuyanjana kwa mankhwala ndi mankhwala ena kuyenera kuphunzira. Kuphatikiza ndi zotsatira:

  1. Maantacid okhala ndi mankhwala a magnesium kapena aluminium hydroxide, sucralfate, zinc ndi iron amachepetsa kuyamwa kwa mankhwalawa.
  2. Mankhwalawa amathandizira kuchuluka kwa digoxin, kumachepetsa mphamvu ya glibenclamide.
  3. Ranitidine amachepetsa kuyamwa kwa ma antibayotiki m'magazi, angayambitse candidiasis.
  4. Kuphatikiza kwa mankhwalawo ndi fluoroquinolones ena, Penicillin amathandizira pazomwe zimachitika.

Bongo

Kuchuluka kwa mlingo wa mankhwalawo kumaonekera ndi zotsatira zoyipa. Mankhwala osokoneza bongo akachitika, muyenera kusamba m'mimba, kusiya kumwa mankhwalawa, kugwiritsa ntchito mankhwalawa kuti muchotse poizoni (Smecta, kaboni yodziyambitsa, Enterosgel, Sorbex). Ndi kuledzera, kuyamwa kwamankhwala osokoneza bongo, kugwiritsa ntchito mankhwala osokoneza bongo, ma multivitamini amaloledwa.

Zotsatira za pharmacological

Moxifloxacin ndi mankhwala odana ndi bakiteriya okhala ndi mawonekedwe osiyanasiyana a fluoroquinolone. Moxifloxacin amawonetsa ntchito mu vitro motsutsana ndi zolengedwa zambiri zama gramu zabwino ndi gramu-hasi, anaerobic, acid osagwira ndi mabacteria atypical, mwachitsanzo Chlamidia spp., Mycoplasma spp. ndi Legionella spp. Mphamvu ya bactericidal ya mankhwalawa imachitika chifukwa cha kuletsa kwa bakiteriya topoisomerases II ndi IV, zomwe zimayambitsa kuphwanya kwa biosynthesis ya DNA ya khungu loyang'aniridwa ndipo, monga chotsatira, ku imfa ya maselo okhala ndi ma cell ochepa. Zozungulira zochepa za bactericidal za mankhwala nthawi zambiri zimakhala zofanana ndi kuchepa kwake kwakanthawi.

Moxifloxacin ali ndi bactericidal kwambiri mabakiteriya osagwirizana ndi ma p - lactam maantibayotiki ndi macrolides.

Njira zomwe zimatsogolera pakupanga kukana kwa penicillin, cephalosporins, aminoglycosides, macrolides ndi ma tetracyclines saphwanya antibacterial zochita za moxifloxacin. Palibe kutsutsana kwapakati pa magulu awa a antibacterial mankhwala ndi moxifloxacin. Kutsutsa kwapakati kwa Plasmid sikunawonedwe. Kuchulukana kwathunthu kumakhala kochepa kwambiri (10 '- 10 "). Kukaniza moxifloxacin kumayamba pang'onopang'ono kudzera pakusintha kambiri. Kuwonetsedwa mobwerezabwereza kwa moxifloxacin kuzinthu zamagetsi zomwe zimayang'aniridwa pansipa ndi zochepa za inhibitory concentration (MIC) zimayendera limodzi ndi kuwonjezeka pang'ono kwa MIC. Pali zochitika zotsutsa ma quinolones. Komabe, tizilombo tating'onoting'ono tokhala ndi gramu komanso anaerobic osagwirizana ndi ma quinolones ena timawaganizirabe moxifloxacin.

Mphamvu ya antibacterial zochita za moxifloxacin imaphatikizanso zotsatirazi:

1. galamu HIV - Streptococcus pneumoniae (kuphatikizapo tizilombo ta penicillin ndi macrolides ndi tizilombo ta ndi kukana angapo mankhwala) * Streptococcus pyogenes (Gulu A) * Streptococcus milleri, Streptococcus mitis, Streptococcus agalactiae * Streptococcus dysgalactiae, Streptococcus anginosus * Streptococcus constellatus *, Staphylococcus aureus (kuphatikiza methicillin-tiziwalo tatswiri) *, Staphylococcus cohnii, Staphylococcus epermidis (kuphatikiza methicillin-tiziwikidwe tating'ono), Staphylocococ haemolyticus, Staphylocococecococococcusocinocococcus womvera vancomycin ndi gentamicin) *.

2. Gram-hasi - Haemophillus fuluwenza (kuphatikiza zingwe zomwe zimatulutsa komanso zosapanga (3-lactamases) *, Haemophillus parainfluenzae *, Klebsiella pneumoniae *, Moraxella catarrhalis (kuphatikiza mitundu yopangira ndi yopanda kupanga (3-lactamases) *, Escherobacteria coli * , Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogene, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazaki, Proteus mirabilis *, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providencia stuartii.

3. anaerobes - Bacteroides distasonis, Bacteroides eggerthii, Bacteroides fragilis * Bacteroides ovatum, Bacteroides thetaiotaomicron * Bacteroides uniformis, Fusobacterium spp, Peptostreptococcus spp * Porphyromonas spp, Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas Magnus, Prevotella spp, .... Propionibacterium spp., Clostridium perfringens *, Clostridium ramosum.

4. Atypical - Chlamydia pneumoniae *, Mycoplasma pneumoniae *,

Legionella pneumophila *, Coxiella bumetti.

* - kuzindikira kwa moxifloxacin kumatsimikiziridwa ndi deta yamankhwala.

Moxifloxacin sakhala wogwira ntchito motsutsana ndi Pseudomonas aeruginosa, Pseudomonas fluorescens, Burkholderia cepacia, Stenotrophomonas maltophilia.

Pharmacokinetics

Pambuyo limodzi kulowetsedwa kwa moxifloxacin pa 400 mg wa 1 ora, pazipita ndende ya mankhwala (Cmosamala) imatheka kumapeto kwa kulowetsedwa ndipo pafupifupi 4.1 mg / l, yomwe ikufanana ndikuwonjezeka pafupifupi 26% poyerekeza ndi mtengo wa chizindikirocho mukamamwa mankhwala mkati. Kuwonekera kwa mankhwalawa, wotsimikiziridwa ndi AUC (dera lomwe limaphatikizidwa ndi nthawi yotsalira), limapitirira pang'ono pakumwa mankhwala mkati. Mtheradi bioavailability pafupifupi 91%.

Pambuyo mobwerezabwereza kulowetsedwa kwa yankho la moxifloxacin pa mlingo wa 400 mg kwa ola limodzi, kuchuluka kwake ndi kutsika kwa plasma kokhazikika (400 mg kamodzi tsiku lililonse) kumakwaniritsidwa kuchokera ku 4.1 mpaka 5.9 mg / l ndikuchokera 0,43 mpaka 0.84 mg / l, motero. Munthawi yokhazikika, zotsatira za yankho la moxifloxacin mkati mwa nthawi yayitali pafupifupi 30% kuposa pambuyo poyambira mlingo woyamba. Pakati pazokhazikika za 4,4 mg / L zimatheka kumapeto kwa kulowetsedwa.

Moxifloxacin imagawiridwa mwachangu mu minofu ndi ziwalo ndipo zimamangiriza kumaproteni amwazi (makamaka albin) ndi pafupifupi 45%. Kuchuluka kwa magawidwe kumakhala pafupifupi 2 l / kg.

Moxifloxacin amakumana ndi gawo la biotransformation la gawo lachiwiri ndipo amamuchotsa kuchokera ku thupi ndi impso, komanso ndowe, zonse zosasinthika komanso mawonekedwe osakanikirana a sulfo mankhwala ndi glucuronides. Moxifloxacin sanapangidwe biocransformed ndi microsomal cytochrome P450 system. Hafu ya moyo wa mankhwala pafupifupi maola 12. Nthawi zonse chilolezo chitatha pa 400 mg kuchokera pa 179 mpaka 246 ml / min. Pafupifupi 22% ya mlingo umodzi (400 mg) umachotsedwa mu mkodzo, pafupifupi 26% - yokhala ndi ndowe.

Njira zopewera kupewa ngozi

Nthawi zina, mankhwalawa atagwiritsidwa ntchito koyamba moxifloxacin, hypersensitivity ndi thupi lawo siligwirizana. Nthawi zambiri, zotsatira za anaphylactic zimatha kupitilira mpaka pakubwezeretsa pangozi ya anaphylactic, ngakhale atangoyamba kugwiritsa ntchito mankhwalawa. Milandu iyi, moxifloxacin iyenera kusiyidwa ndipo njira zoyenera zothandizira zimatengedwa (kuphatikizapo anti-shock).

Pogwiritsa ntchito moxifloxacin mwa odwala ena, kuwonjezedwa kwa nthawi ya QT kungaoneke.

Popeza azimayi amakonda kuwonjezera nthawi ya QT poyerekeza ndi abambo, amatha kukhala osamala ndi mankhwala omwe amawonjezera nthawi ya QT. Odwala okalamba amamveranso chidwi ndimankhwala omwe amakhudza nthawi ya QT.

Kuchulukitsa kwa nthawi ya QT kumatha kuwonjezeka ndi kuchuluka kwa mankhwalawa, chifukwa chake simuyenera kupitilira muyeso wopatsidwa komanso kulowetsedwa (400 mg mu mphindi 60). Komabe, odwala chibayo palibe kulumikizana pakati pa kuchuluka kwa moxifloxacin m'madzi a m'magazi komanso kutalika kwa nthawi ya QT. Kutalika kwa nthawi ya QT kumalumikizidwa ndi chiwopsezo chowonjezeka cha chamitsempha yama cell, kuphatikiza polymorphic ventricular tachycardia. Palibe mwa 9,000 odwala omwe amathandizidwa ndi moxifloxacin omwe anali ndi vuto la mtima kapena milandu yoopsa yokhudzana ndi kukulitsa nthawi ya QT. Komabe, mwa odwala omwe ali ndi vuto lodziwika kuti ali ndi vuto losagwirizana, kugwiritsa ntchito moxifloxacin kungakulitse chiopsezo cha ventricular arrhythmias.

Pankhaniyi, makonzedwe a moxifloxacin ayenera kupewedwa kwa odwala omwe ali ndi nthawi yayitali ya QT, hypokalemia yopanda dongosolo, komanso omwe amalandila antiarrhythmic mankhwala a kalasi IA (quinidine, procainamide) kapena kalasi III (amiodarone, sotalol), popeza momwe amagwiritsira ntchito moxifloxacin mwa izi odwala ndi organic.

Moxifloxacin ayenera kuikidwa mosamala, popeza

kuchuluka kwa moxifloxacin sikungaphatikizidwe pazinthu zotsatirazi:

Odwala omwe amalandira chithandizo chamankhwala omwe amakulitsa nthawi ya QT (cisapride, erythromycin,

antipsychotic mankhwala, tricyclic antidepressants),

- Odwala omwe ali ndi vuto lodziwika kuti ali ndi vuto lotchedwa bradycardia, pachimake myocardial ischemia,

- odwala omwe ali ndi matenda a cirrhosis, popeza kukhalapo kwa nthawi yayitali ya QT mwa iwo sikungathere kunja,

- mwa amayi kapena odwala okalamba, omwe amatha kukhala osamala ndi mankhwala omwe amawonjezera nthawi ya QT. Nkhani za chitukuko cha chiwindi cha hepatitis, chomwe chingayambitse chiwopsezo cha moyo, kuphatikizapo imfa, zanenedwapo. Ngati zizindikiro za kulephera kwa chiwindi zikuwonekera, odwala ayenera kufunsa dokotala nthawi yomweyo asanapitirize chithandizo.

Milandu yokhudzana ndi kukhudzana kwa khungu lamphongo, mwachitsanzo, Stevens-Johnson syndrome kapena poermal necrolysis yoopsa (yomwe ikhoza kuwononga moyo), akuti. Ngati pakhungu pakukhudzana ndi / komanso pakhungu pakhungu lanu, muyenera kufunsa dokotala nthawi yomweyo musanapitirize chithandizo. Kugwiritsa ntchito mankhwala a quinolone kumalumikizidwa ndi chiopsezo chogwira gwiridwe. Moxifloxacin iyenera kugwiritsidwa ntchito mosamala kwa odwala omwe ali ndi matenda amkatikati mwa mitsempha komanso mikhalidwe yomwe akukayikira pakukhudzidwa kwapakati pamitsempha yamagetsi, poganiza kuti pakubwera kugunda kotsitsimula, kapena kutsitsa poyambira kuti agwire.

Kugwiritsa ntchito mitundu yotakata ya antibacterial, kuphatikiza moxifloxacin, kumalumikizidwa ndi chiopsezo chotenga pseudomembranous colitis yokhudzana ndi kumwa maantibayotiki. Kuzindikiritsa izi kuyenera kukumbukiridwa mwa odwala omwe amatenga matenda otsekula m'mimba panthawi ya mankhwala a moxifloxacin. Pankhaniyi, chithandizo choyenera chikuyenera kuperekedwa nthawi yomweyo. Odwala omwe ali ndi matenda otsegula m'mimba amatsutsana ndi mankhwala omwe amaletsa matumbo kuyenda.

Moxifloxacin ayenera kugwiritsidwa ntchito mosamala odwala omwe ali ndi Gravis myasthenia gravis, chifukwa mankhwalawa angakulitse zizindikiro za matendawa.

Pochita mankhwala ndi fluoroquinolones, kuphatikizapo moxifloxacin, makamaka okalamba komanso odwala omwe amalandila glucocorticosteroids, kukulitsa kwa tendonitis ndi kupindika kwa tendon ndikotheka. Pazizindikiro zoyambirira za kupweteka kapena kutupa pamalo ovulala, mankhwalawa amayenera kuyimitsidwa ndikugwedezedwa.

Kwa odwala omwe ali ndi zovuta zotupa za ziwalo zamkati (mwachitsanzo, zimagwirizanitsidwa ndi tubo-ovarian kapena pelvic abscesses) omwe amathandizidwa ndi chithandizo chamkati, kugwiritsa ntchito moxifloxacin mu mapiritsi a 400 mg sikulimbikitsidwa.

Pogwiritsa ntchito quinolones, mawonekedwe a photosensitivity amadziwika. Komabe, pa preclinical, maphunziro azachipatala, komanso kugwiritsa ntchito moxifloxacin pochita, palibe zotsatira zamtundu wa photosensitivity zomwe zimawonedwa. Komabe, odwala omwe amalandila moxifloxacin ayenera kupewa kuwala kwa dzuwa mwachindunji ndi ma radiation a ultraviolet.

Kwa odwala omwe ali ndi chakudya chochepa cha sodium (chifukwa cha kulephera kwa mtima, kulephera kwa impso, ndi nephrotic syndrome), mankhwala ena owonjezera a sodium ndi kulowetsedwa amayenera kukumbukiridwa.

Kusiya Ndemanga Yanu