Drugs online research references
Obstet Gynecol. 1993 Jun;81(6):919-21.
The need for adjustment of dosage regimen of penicillin V during pregnancy.
Heikkila AM, Erkkola RU.
Department of Obstetrics and Gynecology, Turku University Central Hospital, Finland.
OBJECTIVE: To determine whether the normal regimen of dosage of oral penicillin V is relevant during pregnancy. METHODS: Twelve pregnant and six nonpregnant women volunteered for the study. Six women were in the second trimester of pregnancy (mean +/- standard deviation 19 +/- 7 weeks' gestation) and six women were in the third trimester (35 +/- 2 weeks). All of the women took 1 x 10(6) IU phenoxymethylpenicillin orally, and multiple blood and urine samples were obtained. Assays were performed by means of a disk agar diffusion method. The results were compared by Mann-Whitney U test. RESULTS: Compared with nonpregnant women, pregnant women had smaller area under the curve values (433 +/- 93 minutes.IU/mL, P < .05 in the second trimester; 550 +/- 220 minutes.IU/mL in the third trimester) and a shorter half-life (57 +/- 56 minutes in the second trimester; 34 +/- 21 minutes, P < .05 in the third trimester). Plasma and renal clearances were faster in the pregnant women. CONCLUSION: Elimination of penicillin V is enhanced during pregnancy, necessitating either a shorter dosing interval (6-8 hours) or an increased dose with the standard dosing interval.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8497356&dopt=Abstract
Clin Infect Dis. 1996 May;22(5):788-93.
Treatment of erythema migrans in pregnancy.
Maraspin V, Cimperman J, Lotric-Furlan S, Pleterski-Rigler D, Strle F.
Department of Infectious Diseases, University Medical Centre, Ljubljana, Slovenia.
The course of the illness and the outcome of pregnancy were investigated in a prospective study of 58 consecutively enrolled pregnant women with typical erythema migrans at the University Medical Centre of Ljubljana, Slovenia. Thirteen patients (22.4%) acquired borrelial infection in the first trimester of pregnancy, 27 (46.6%) in the second trimester, and 18 (31%) in the third trimester. All patients were treated for 14 days: 2 (3.4%) with phenoxymethylpenicillin (1 million IU thrice per day), 3 (5.2%) with benzylpenicillin (10 million units twice per day), and 53 (91.4%) with ceftriaxone (2 g daily). For 51 of the 58 women (87.9%), the pregnancies were normal and the infants were born at term, were clinically healthy, and had normal psychomotor development. Of the remaining 7 pregnancies, 1 ended with a missed abortion and 5 with preterm birth; 1 of the preterm babies had heart abnormalities. One child born at term was found to have urologic abnormalities at 7 months of age. A causal relationship between borrelial infection and fetal adverse effects has not been proven, and for at least some such cases a reasonable explanation (not associated with Lyme borreliosis) was found.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8722932&dopt=Abstract
Bioorg Med Chem. 1996 Apr;4(4):521-2.
New drugs--reports of new drugs recently approved by the FDA. Dirithromycin.
Shinkai I, Ohta Y.
Merck Research Laboratories, Rahway NJ 07065-0900, USA.
Dirithromycin is a semisynthetic derivative of erythromycin, a 14-membered ring macrolide antibiotic. The drug is converted during absorption and distribution, to an active metabolite 9-(S)-erythromycylamine, which is the predominant compound found in plasma and extravascular tissues. High tissue concentration of erythromycylamine is achieved after oral doses of dirithromycin, with slow release back into the circulation. The mechanism of action of dirithromycin is like that of erythromycin and other macrolides. These compounds inhibit RNA-dependent protein synthesis. It has recently been suggested that all macrolides stimulate dissociation of peptidyl-tRNA from ribosomes during the elongation phase, leading to inhibited protein synthesis. The antimicrobial spectrum of dirithromycin is similar to that of erythromycin, although the drug offers no significant advantage with regard to MIC values. In vitro against Gram-positive isolates, dirithromycin exhibits similar potency to that of clarithromycin, erythromycin, roxithromycin, and clindamycin. In vivo, dirithromycin is active against penicillin-susceptible Staphylococcus aureus, beta-hemolytic streptococci, and Streptococcus pneumoniae. Dirithromycin is as effective as penicillin VK against streptococcal pharyngitis and tonsilitis, and as effective as erythromycin against acute superimposed chronic bronchitis and skin and soft-tissue infections. In comparison with other newer macrolides, dirithromycin has shown similar or lesser in vitro activity. In particular, Haemophilus influenzae, Bacteroides spp., Peptococcus-Peptostreprococcus spp., Clostridium perfringens, Legionella spp., Neisseria gonorrhoeae, and Chlamydia trachomatis were all less sensitive to dirithromycin than azithromycin or clarithromycin. Once-daily oral administration of dirithromycin (500 mg) has been demonstrated to be similar in efficacy to erythromycin (250 mg, 4 times daily), each for approximately 7 days, in the treatment of acute bronchitis or acute-exacerbations of chronic bronchitis in controlled studies. Proven or presumed pathogen eradication rates were 83 and 86% for acute bronchitis patients treated with dirithromycin and erythromycin, respectively. Corresponding bacteriological response rates in acute exacerbations of chronic bronchitis were 75 to 84% with dirithromycin and 75 to 82% with erythromycin. Both agents achieved clinical cure or improvement in over 85% of the patients with either condition. The main advantage of dirithromycin over erythromycin appears to be once-daily administration. Lilly launched dirithromycin in September 1993, in Spain, received approval from FDA in August 1995, and launched it during October 1995.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8735838&dopt=Abstract
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