Terconazole

Sample preparation Condition a 3 mL Bond-Elut CIS cartridge with 6 mL MeOH and 6 mL water. 1 mL Serum -t 250 )jlL 100 mM NaOH -t- 3 mL water, add to cartridge, wash with 9 mL water, wash with 200 p,L MeOH, elute with 1 mL MeOH. Evaporate eluent at 60°, resuspend in 200 pL mobile phase, centrifuge at 13000 g for 2 min, inject 20-40 pL. 

Mobile phase MeCN water 45 55 containing 500 pL/L diethylamine, pH adjusted to S.O with orthophosphoric acid 

Turner, CA. Ttirner, A. Wamock, D.W. High performance liquid chromatographic determination of ketoconazole in human serum. J.Antimicrob.Chemother., 1986, 18, 757-763 

Mobile phase MeOH .buffer 60 40 (Buffer was 25 mM KH2PO4 -I- 4 mM heptanesulfonic add, adjusted to pH 8.0 with 1 M NaOH.) 

Carver, P.L. Berardi, R.R. Knapp, M.J. Rider, J.M. Kauffman, C.A. Bradley, S.F. Atassi, M. In vivo interaction of ketoconazole and sucralfate in healthy volunteers. Antimicrob.Agents Chemother., 1994, 38, 326-329 

Molecular formula C2eH3,Cl2N503 Molecular weight 532.5 CAS Registry No. 67915-31-5 

---

Because of their limited, activity, small spectmm, and side effects, the older topical antimycotics have generally been surpassed by newer antimycotic chemotherapeutic agents. These newer antimycotics for topical use iaclude the imida2ole derivatives clotrimazole, miconazole, econazole, isoconazole, sulconazole, fenticonazole, oxiconazole, bifonazole, butoconazole, ziaoconazole, tioconazole, and the triazole derivative, terconazole (Table 2) (5—7). The iatroduction of the azole derivatives represents a milestone ia the treatment of mycoses. 

Insertion of a triazole ring in place of an imidazole ring is consistent in some cases with retention of antifungal activity. The synthesis of one such agent, azoconazole (64), proceeds simply by displacement of halide with 1,2,4-triazole. The route to terconazole (65) is rather like that to ketoconazole (34). ... 

CjHuO, 56-81-5) see Actinoquinol Itraconazole Ketoconazole Oxyquinoline Phanquinone Primaquine Terconazole glycerol... 

Terconazole (Terazol) Chlamydia 0.4% cream, 5 g intravaginally for 7 days ... 

Response rates are lower for non-albicans infections. Although an optimal regimen is unknown, use of intravaginal azole therapy for 7 to 14 days is recommended. Terconazole may prove more effective than other azoles in the treatment of non-albicans infections since C. glabrata and C. tropicalis are more susceptible to terconazole.17 For second-line therapy, boric acid 600 mg in a gelatin capsule administered vaginally twice daily for 2 weeks followed by once daily during menstruation is effective.18 Local irritation often limits the use of boric acid. Topical 4% flucytosine is also effective but use should be limited due to the potential for resistance. 

Clotrimazole 500 mg vaginal suppository once weekly Fluconazole 100 or 150 mg orally once weekly Terconazole 0.8% cream 5 g vaginally once weekly Monthly... 

Finally, reacting the mesylate (35.2.16) with the resulting l-isopropyl-4-(4-hydrox-yphenyl)piperazine (35.2.18) gives the desired terconazole [29-32]. 

---