Moxifloxacin hydrochloride CAS NO.186826-86-8

moxifloxacin hydrochloride basic information

fluoroquinolone antibiotics pharmacological effects pharmacokinetics indications dosage adverse reactions precautions application

product name:	moxifloxacin hydrochloride
synonyms:	avalox;bay-12-8039;(1's,6's)-1-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride;1-cyclopropyl-6-fluoro-1,4-dihydro- 8-methoxy-7- [(4as,7as)-octahydro-6h-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid hydrochloride;1-cyclopropyl-7-[(s,s)-2,8-diaza-bicyclo[4.3.0]non-8-yl]-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3-quinoline carboxylic acid hydrochloride;actira;proflox;moxifloxacin hcl
cas:	186826-86-8
mf:	c21h25clfn3o4
mw:	437.89
einecs:
product categories:	active pharmaceutical ingredients;moxifloxacin;api;aricept
mol file:	186826-86-8.mol

moxifloxacin hydrochloride usage and synthesis

fluoroquinolone antibiotics	moxifloxacin hydrochloride developed by the german bayer , is a fluoroquinolone antibiotic , moxifloxacin hydrochloride is used for the treatment of staphylococcus aureus, haemophilus influenzae, streptococcus pneumoniae, moraxella catarrhalis mucositis, caused by klebsiella pneumoniae causing social acquired pneumonia, acute exacerbation of chronic bronchitis, acute sinusitis, etc.
pharmacological effects	this product’s mechanism of action and in vitro antimicrobial spectrum are similar to other fluoroquinolones, but the antibacterial activity of gram-positive bacteria and anaerobic bacteria is similar to trovafloxacin , better than some older varieties. compared with other fluoroquinolones,there is little gram-positive bacteria resistant to the chemicals or drug resistance is very slow, and there is a cross resistant between it and the other fluoroquinolones in gram-negative bacteria and enterococci . but the product at least is effective in staphylococcus aureus isolates beads grla, grlb, gyra or gyrb, this product of 0.5 ~ 2 mg / l could inhibit ciprofloxacin-resistant staphylococcus aureus, followed in descending order by mic ciprofloxacin, ofloxacin, levofloxacin, sparfloxacin, moxifloxacin. figure 1 the structural formula of moxifloxacin hydrochloride
pharmacokinetics	45 cases of healthy volunteers were involved after oral administration of a single dose of 50 ~ 800mg, the area under the curve and peak plasma concentrations of the drug (auc) increased linearly with dose. the recommended dose of oral 400mg, average cmax was 2.5mg / l, peak time (tmax) to 1.5h, auc was 26.9mg · h / l. healthy volunteers repeated 400mg oral once a day for10d, cmax was 4.52mg / l, treatment 10d accumulation was 1.59. the oral bioavailability of 89%, the apparent volume of distribution was 3.55l / kg, plasma protein binding rate was 48%. when this product was 400mg intravenous injection, cmax was 3.62mg / l, auc was 34.6mg · h / l. 13 cases of healthy volunteers were involved after a single oral or intravenous injection of this product 400mg, 24h, the skin blister fluid concentrations was about 2-fold of serum concentration of it , suggesting that the product is easier to penetrate into the interstitial tissue. 18 patients before undergoing bronchoscopy took single oral dose of this product 400mg, after 1h, bronchial epithelial cell fluid and bronchial biopsy tissue concentrations were 24.4,5.5mg / l, more than plasma concentrations ;after 12h, the product stored in macrophages cells reached an extremely high concentration (113.6mg / l). 34 cases of chronic sinusitis patients were treated with oral administration of five doses of 400mg, the maxillary sinus mucosa concentrations was more than the plasma concentration; after 3h of the last dose ,the maximum plasma concentration was 7.47mg / kg, 36h of 1.25mg / kg, which prompted it is effective after the dose. healthy volunteers single oral dose of 400mg of the product, the total clearance and renal clearance were hourly 14.9,3.03l. this product did not seem to metabolize by p450 . in vitro by human liver cells it was metabolized as n- sulphate and acyl glucuronide metabolite inactive. healthy volunteers after oral administration of 400mg / d , the mean elimination half-life (t1 / 2β) of the first day was 9.3h , while the first 10 days was 11.95h. another study showed that the average t1 / 2βwas about 10 ~ 16h. a single oral or intravenous injection of this product 400mg, the reabsorption rate of urine was 19% to 20% and 22%, respectively. the above information is edited by the chemicalbook of tian ye.
indications	this product can be used in the treatment of staphylococcus aureus, haemophilus influenzae, streptococcus pneumoniae, moraxella catarrhalis mucositis, klebsiella pneumoniae causing social acquired pneumonia, acute exacerbation of chronic bronchitis, acute sinusitis, etc.
dosage	[preparation specifications] oral tablets or injections. this product is recommended daily dose of 400mg, orally or intravenously.
adverse reactions	side effects of this product are mostly mild and transient , 3.8% of the patient discontinued treatment due to adverse events . the most common adverse reactions are nausea (7.2%) and diarrhea (5.7%). dizziness is 2.8%. in healthy volunteers, no changes in vital signs, hematology, blood biochemistry and electrocardiogram. studies have shown that the product is different from lomefloxacin , no drug-induced light toxicity.
precautions	similar to other fluoroquinolones , the product (400mg) in combination with antacids, bioavailability will fall significantly, auc and cmax fall down 45% and 40% respectively when compared with alone, but using the moxifloxacin hydrochloride 2h before taking antacids or using antacids 4h after using this service, the absorption of the drug has no effect. if the product in combination with iron ,absorption rate decreases, auc and cmax are reduced by 39% and 59%. the product has no interaction with theophylline, probenecid, ranitidine and warfarin .
application	fluoroquinolone antibiotics for the treatment of community-acquired pneumonia, acute exacerbation of chronic bronchitis, urinary and reproductive tract infections, acute sinusitis. significant effects, little side effects.
usage	acetylcholinesterase inhibitor (reversible), cognitive enhancer
usage	an antibacterial agent that inhibits the activities of topo ii (dna gyrase) and topoisomerase iv

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