We carried out fundamental studies to evaluate the usefulness of Cefixime (CFIX) in maxillofacial surgery, and obtained the following results.
1) The mean values of concentrations of CFIX after administration of 200mg P.O. to non-fasted patients were 2.42μg/ml (5 hr), 1.79μg/ml (7 hr) in serum, 0.95μg/ml (5 hr), and 0.65μg/ml (7 hr) in blood in wound. Gingival concentrations of CFIX were 0.21-1.17μg/g except 6 N.D.
2) The antibacterial activity of CFIX against 65 Streptococcus sp. clinically isolated was equivalent to those of Ampicillin (ABPC), Cefteram (CFTM), Cefuroxime (CXM) Ofloxacin (OFLX) and superior to that of Cefaclor (CCL) at MIC₈₀, but against 30 Staphyloccoccus sp. CFIX showed inferior antibacterial activity to other antibiotics. Among all antibiotics, CFIX showed the strongest antibactrial activity against arerobic gram-negative organisms.
3) It was considered that CFIX was effective in the treatment of mild and moderate oral infections.

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Cefotaxime was administered to 21 cases in oral regions and studied on laboratory parameters concerning peripheral blood: blood plateret counts, prothorombin time (PT), hapaplastin test (HPT), active partial thromboplastin time (APTT) and protein induced by vitamin K absence (PIVKA II) . The results obtained were summarized as follows,
Clinical bleeding symptoms were not observed in any of these cases.
1. blood plateret counts: Abnormal values were not observed.
2. Coaguration system (PT, HPT, APTT, PIVKA II) : Significant changes were not found in these values.
We have concluded that incidences of abnormal hemostatic test following CTX administration are rare. It was suggestted that CTX is one of the reliable antibiotics in oral regions.

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Levofloxacin (LVFX), levo-isomer of ofloxacin (OFLX), was administered to New Zea-land White rabbits at a dose of 20mg/kg and pharmacokinetic characteristics of the tissues related to the field of oral surgery was investigated, and compared with those of OFLX. In addition, clinical efficacy of LVFX was evaluated in the patients with odontogenic infections.
LVFX had higher concentration in serum, tongue, sub mandibular gland and parotid gland, but lower in mandible, than OFLX.
Clinical efficacy rate according to the numerical rating on the 3rd day was 57.1% (4/7) with a dosage of 100mg t.i.d, and 60.0% (3/5) with 100mg b.i.d. Except for 1 patient with elevation of eosinocyte, no abnormal laboratory changes nor adverse reactions were observed.
Clinical usefulness evaluated by the doctors in charge was 75%.
These results suggested that LVFX is an useful antimicrobial agent in the treatment of odontogenic infections.

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The success or failure of surgical operations depends partly on the prevention of postoperative infections. Recently, prophylactic method of infections is the administrations of antibiotics.
Preventive effects of postoperative infections by means of Ceftizoxime (CZX) that has broad spectrum and few side effects were investigated. Fever index as the index of prophylactic effects to infection, and other findings, such as clinical and laboratory test results, were assessed to determine the prophylactic usefullness of CZX to postoperative infection. The result was that the postoperative infection was judged, by the chief physiciens to have occured in one out of the 40 cases under study by the judgement of chief physicians. On compairing the Fever index of the infected case with that of the uninfected case, the latter was more high. As for the relationship between Fever index, operative backgrounds and the other findings, considerable correration index between he operative time, the amount of bleeeding and Fever index were seen.
The results of our study indicate that CZX is a useful enough antibiotic to prophylaxis of ostoperative infections and that Fever index can be used as an index of preventive effects of postoperative infection.

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The therapeutic regimen of levofloxacin in odontogenic infection and in chemoprophylaxis of exodontia was studied. Application of salivary drug concentration for therapeutic drug monitoring was also examined.
1) Normal meal intake had almost no effect on the absorption of orally administered lavo-floxacin.
2) When the blood concentration of exodontia wound was set at 1.56μg/ml (MIC₉₀) as the chemoprophylactic target level, the percentage of cases, in which the concentrations achieved were over the target level were 61.1% (11/18 cases) and 56.4% (22/39 cases) during 30-180 minutes after administration of levofloxacin (200mg) in fasting and non-fasting volunteers, respectively.
3) Saliva and serum levels of levofloxacin were almost equal after orlal administration, in-dicating that saliva concentration could be useful for therapeutic drug monitoring.

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In 17 patients with cystic diseases of the jaw bone. The drug levels in serum and cyst tissue were determined after a one-shot intravenous injection of 1 g of cefuzonam sodium (CZON) . We also assessed the effect of this drug in preventing postoperative infection and its adverse effects for this group. Through these examinations, we evaluated the clinical usefulness and safety of this drug. The following results were obtained.
1. When passed 35-75 minutes (mean: about 56 minutes) after a one-shot injection, the serum drug level was 25.1±9.1, ug/ml and the cyst tissue drug level was 18.8+5.3, ug/mg (n=17) .
2. The percentage of cyst tissue drug level relative to the serum drug level ranged from 53.2% to 137.5%.
3. In a subjective assessment of the drug's efficacy, its effectiveness rate was 82.4%. No adverse reactions to the drug were observed.

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局所麻酔剤であるプロカインおよびプロカインアミドのウシ血漿アミンオキシダーゼの活性に及ぼす影響を基質にベンジルアミンおよびキヌラミンを用いて調べた。プロカインおよびプロカインアミドの両方とも強くアミンオキシダーゼの活性を阻害し, ともに非競合阻害であった。ベンジルアミンを基質に用いたとき, Km値は0.75mMで, Ki値はプロカインに対して0.12mM, プロカインアミドに対して0.43mMであった。
プロカインやプロカインアミドの構成成分であるp-アミノ安息香酸, N, N-ジエチルアミノエタノールおよびN, N-ジエチルアミノエチルアミンはアミンオキシダーゼ活性をほとんど阻害しないことがわかった。

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Serum and tissue concentrations of fleroxacin (FLRX), a new quinolone antimicrobial agnt, were measured in W ister Strain rats after oral administration at a dose of 10mg/kg. FLRX was detected in serum, gingiva, tongue, mandibular bone, cervical lymphnode, submandibular bone, gland, kidney and liver. Samples were taken at 0.25h, 0.5h, 1h, 2h, 4h, 6h, and 8h, after administration.
The concentrations were determined by bioassay, and a paper disk method was adopted using Escherrichia coli NIHJ JC-2 was the test organism.
The serum and all tissue concentrations reached a peak the 30 minutes and the peak concentration of FLRX was 4.51μg/ml in serum, 2.8μg/g in gingiva, 2.12μg/g in tonve, 3.22μg/g in mandibular bone, 3.5μg/g in cervical lymph node, 5.2μg/g in submandibular gland, 6.34μg/g in kidney, and 14.5μg/g in liver. The ratios of the above tissue levels to the serum level were 0.62, 0.47, 0.71, 0.78, 1.15, 1.41, and 3.22.

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