Drugs online research references
Antimicrob Agents Chemother. 1994 Sep;38(9):1937-43.
Characteristics of murine model of genital infection with Chlamydia trachomatis and effects of therapy with tetracyclines, amoxicillin-clavulanic acid, or azithromycin.
Beale AS, Upshon PA.
SmithKline Beecham Pharmaceuticals, Brockham Park, Betchworth, Surrey, United Kingdom.
Following intravaginal inoculation of progesterone-treated outbred mice with Chlamydia trachomatis MoPn, 4 to 6 log10 inclusion-forming units were recovered in vaginal swabs for 21 days but all animals were culture negative after 28 days. Serum antibody titers were elevated and remained high for at least 70 days. Between 28 and 70 days, upper tract infection (inflammation and distension of the uterine horns, occlusion of oviducts with inflammatory exudate, pyosalpinx, and hydrosalpinx) was seen in > 80% of the animals. Mice were dosed orally, commencing at 7 days after infection, with minocycline, doxycycline, or amoxicillin-clavulanate. Further groups received azithromycin either as a single high dose or as lower once-daily doses. In addition, minocycline and amoxicillin-clavulanate were administered at 24 h after infection, and this early treatment prevented elevation of antibody titers whereas delayed therapy did not. Vaginal swabs from mice in all treatment regimens were culture negative except for 25% of mice receiving either early amoxicillin-clavulanate or low-dose azithromycin, which yielded low numbers (20 to 70 inclusion-forming units) of chlamydiae. Numbers of fertile mice in the early treatment regimens and their litter sizes were similar to those of noninfected controls, although 25% of amoxicillin-clavulanate-treated mice had unilateral hydrosalpinges. In comparison, 88% of untreated mice developed hydrosalpinges and only 25% conceived. Delayed dosing did not affect the outcome of amoxicillin-clavulanate therapy but did diminish the protective efficacy of minocycline such that 50% of treated mice had either unilateral hydrosalpinges or ovarian abscesses. Doxycycline and azithromycin were highly effective in restoring fertility. This model makes possible the study of both short- and long-term outcomes of chlamydial infection.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7811001&dopt=Abstract
Antimicrob Agents Chemother. 1994 Sep;38(9):2218-20.
N,N-dimethylglycyl-amido derivative of minocycline and 6-demethyl-6-desoxytetracycline, two new glycylcyclines highly effective against tetracycline-resistant gram-positive cocci.
Goldstein FW, Kitzis MD, Acar JF.
Laboratoire de Microbiologie Medicale, Hopital Saint-Joseph, Paris, France.
The in vitro activities of the N,N-dimethylglycyl-amino derivative of minocycline (DMG-MINO) and 6-dimethyl-6-dexoxytetracycline (DMG-DMDOT), members of a new generation of tetracyclines, were evaluated by an agar dilution method and were compared with those of tetracycline and minocycline against 224 tetracycline-resistant and 73 tetracycline-susceptible recent clinical isolates of gram-positive cocci, including multiple-antibiotic-resistant methicillin-resistant Staphylococcus aureus and penicillin-resistant Streptococcus pneumoniae. The MICs of DMG-MINO and DMG-DMDOT were up to 500- to 2,000-fold lower than those of tetracycline against methicillin-resistant S. aureus and Streptococcus pneumoniae (MIC for 50% of strains tested [MIC50], < 0.06 microgram/ml). Against Streptococcus groups A, B, C, and G and Enterococcus faecalis, the MIC50 was 0.5 microgram/ml. MIC50s were greater only for coagulase-negative staphylococci (2 micrograms/ml). These data indicate that DMG-MINO and DMG-DMDOT are very potent drugs, and further in vitro and in vivo studies are warranted.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7811053&dopt=Abstract
Arzneimittelforschung. 1976 Apr;26(4):556-60.
[Activity in vitro and pharmacokinetics of minocycline (author's transl)]
[Article in German]
Simon C, Malerczyk V, Preuss I, Schmidt K, Grahmann H.
The in vitro activity of doxycycline and minocycline (Klinomycin) was determined by serial dilution test in 100 strains of E. coli, 101 strains of enterobacter, 91 tetracycline-sensitive and 52 tetracycline-resistant strains of staphylococci. Only staphylococci were more sensitive against minocycline than against doxycycline whereas other species showed nearly the same sensitivity against both antibiotics. After i.v. infusion of 200 mg minocycline (during 1 h) mean serum levels fell from 3.5 mug/ml to 0.6 mug/ml (after 24 h). Half-life was calculated as 15.7 h, urine recovery as 5.9%. After oral application of 200 mg minocycline serum level peaks were 2.7 mug/ml, serum levels after 24 h 0.7 mug/ml. At repeated administrations daily dosage of 100 mg was too low of 200 mg sufficient to obtain the same serum levels as after the initial dose of 200 mg. CSF levels after oral administration of 0.4 g minocycline were 0.74 +/- 0.09 mug/ml (in serum at the same time 2.2 +/- 0.2 mug/ml). Half-life of minocycline in chronic renal failure (7 adult patients) was not prolonged (15--20 h). Minocycline is especially suitable for treatment of infections of unknown bacterial origin (including such caused by staphylococci). I.v. infusion is indicated only in unconscious or vomiting patients.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=782466&dopt=Abstract
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