Ceftriaxone
Ceftriaxone (Roche’s Rocephin, generics) is one of the most successful antibiotics on the market. The agent is a third-generation parenteral cephalosporin available for IV or IM administration that was first launched in 1982. Ceftriaxone has been available generically in Europe since 2002. In 2000, Cubist Pharmaceuticals announced that it had acquired the rights to oral ceftriaxone and was developing an alternate oral formulation. However, the company discontinued development in 2004 after human clinical trials showed highly variable bioavailability of the drug when administered orally.
Ceftriaxone has demonstrated a broad spectrum of activity against gram-positive and gram-negative bacteria, including S. aureus, S. pneumoniae, S. pyogenes, and other streptococci, E. coli, H. influenzae, H. parainfluenzae, K. pneumoniae, M. catarrhalis, and others. Ceftriaxone is indicated for lower respiratory tract infections caused by S. aureus, S. pneumoniae, H. influenzae, H. parainfluenzae, K. pneumoniae, and E. coli. The agent is one of the most widely used parenteral antibiotics for respiratory tract infections. The efficacy of ceftriaxone in the treatment of lower respiratory tract infections was evaluated in a comparative clinical study with cefonicid; 118 patients received 1 g of either Ceftriaxone or cefonicid, IV or IM, daily for 3 to 11 days (mean was seven days).
Clinical cure or improvement was noted in 93% of patients treated with ceftriaxone and 95% of patients treated with cefonicid. Bacteriologic cure or improvement was noted in 81% and 69% of cases, respectively. The agent is well tolerated in extensive clinical use. Local reactions have been reported following parenteral administration of antibiotics, including ceftriaxone. Pain, induration, and tenderness were reported in about 1% of cases. The frequency of side effects is comparable to frequency associated with other parenteral cephalosporins.
Cefdinir
Cefdinir (Abbott’s Omnicef, Fujisawa’s Cefzon) is a third-generation, oral cephalosporin available as a capsule and as an oral suspension. Cefdinir (Omnicef) was developed and launched by Fujisawa in Japan in 1991 as Cefzon. Warner-Lambert’ s Parke-Davis (now Pfizer) was the first to license Cefdinir (Omnicef) 300mg for the United States and Western Europe and began marketing Cefdinir in the United States in 1998, but Abbott obtained the exclusive marketing rights from Fujisawa and began marketing the drug as Omnicef in 2000.
The agent is expected to retain patent protection through 2007 in the United States. Cefdinir is indicated for treatment of adults and adolescents who have community-acquired pneumonia caused by penicillinase-susceptible S. pneumoniae and all strains of H. influenzae, H. parainfluenzae, and M. catarrhalis. Cefdinir is stable in the presence of many β-lactamase enzymes, effectively extending its spectrum of activity against a number of gram-positive and gram-negative bacteria resistant to penicillins and other cephalosporins.
Cefdinir has demonstrated clinical and bacteriologic activity against S. aureus, Staphylococcus epidermitis (in vitro), S. pneumoniae, S. pyogenes, E. coli (in vitro), H. influenzae, H. parainfluenzae, K. pneumoniae (in vitro), M. catarrhalis, and others. Cefdinir is not active against Pseudomonas species. A double-blind, controlled, Phase III clinical study enrolled a total of 690 patients in the United States to compare the efficacy of cefdinir and cefaclor for treatment of community-acquired pneumonia in adults and adolescents. One group of 347 patients received 300 mg of cefdinir twice daily for ten days; another group of 343 patients received 500 mg of cefaclor three times daily for ten days.
Clinical cure or improvement rates for cefdinir and cefaclor were similar: 89% (166/187) and 86% (160/186), respectively; bacteriologic eradication rates were 92% (238/260) and 93% (245/264), respectively. A Phase III comparative clinical trial showed that cefdinir had a statistically significant higher rate of adverse reactions (25.9%) than cephalexin (16.1 %). In particular, cefdinir causes more gastrointestinal discomfort (such as diarrhea) than other cephalosporins. The most frequently reported adverse reactions in U.S. clinical trials with a total of 3,841 cefdinir-treated adult patients were diarrhea (15%), vaginal moniliasis (4% of women), nausea (3%), and headache (2%). Most adverse events were mild and self-limiting in nature, with a low discontinuation rate (3%) due to associated adverse events. The most frequently reported adverse reactions in U.S. clinical trials with a total of 1,783 cefdinir-treated pediatric patients were diarrhea (8%), rash (3%), and vomiting (1%)