What Is Tioconazole?

Ticonazole has a molecular formula of C16H13Cl3N2OS, a molecular weight of 387.71100, a density of 1.44 g / cm3, a boiling point of 534.5ºC at 760 mmHg, and a flash point of 277 ° C.

Chinese name: Ticonazole
Foreign name: Tioconazole, Gyno-Trosyd

CAS number: 65899-73-2
Molecular formula: C16H13Cl3N2OS

Introduction to ticonazole compounds

Ticonazole Basic Information

Chinese name: thioconazole

Chinese alias: 1- [2-[(2-chloro-3-thienylmethoxy)]-2- (2,4-dichlorophenyl)] ethylimidazole; secconazole;

English name: 1- {2-[(2-chloro-3-thienyl) methoxy] -2- (2,4-dichlorophenyl) ethyl} imidazole

English alias: Tioconazole; Vagistat;

CAS number: 65899-73-2

Molecular formula: C ₁₆ H ₁₃ Cl ₃ N ₂ OS

Molecular weight: 387.71100

Structural formula:

Exact mass: 385.98100

PSA: 55.29000

LogP: 5.86290 ^[1]

Physicon Chemical Properties of Ticonazole

Density: 1.44g / cm ³

Boiling point: 534.5ºC at 760 mmHg

Flash point: 277ºC

Refractive index: 1.654 ^[1]

Ticonazole pharmacological action

This product is an imidazole broad-spectrum antifungal drug. This product has antibacterial activity against epidermal ringworm, candida albicans, yeast, etc .; it is equivalent to or stronger than miconazole and clotrimazole against pathogenic bacteria such as trichophyton, pityriasis versicolor and cutaneous candidiasis. It has strong antibacterial activity against Candida albicans, and its effect appears quickly. In vivo, it has fast effect on experimental Trichophyton infection and Candida vaginal infection, and the negative rate of treatment fungus is the same as clotrimazole. It also inhibits Gram-positive bacteria, Gram-negative bacteria, Haemophilus vaginalis, Trichomonas vaginalis and Chlamydia trachomatis. ^[2]

Ticonazole pharmacokinetics

20mg of hydrogen-3 labeled 1% cream is applied to normal skin and damaged skin of rats for 24 hours. The former shows a peak blood concentration after 24 hours and the value is extremely low, while the latter absorbs quickly, but the blood concentration is still low. Once a day, the drug was repeatedly used for 12 days. After 4 days of administration, the blood concentration reached the plateau value, and gradually decreased after stopping the drug. No accumulation effect was seen. The amount of migration into the body reached 16.1% after 24 hours on healthy skin and 36.7% on damaged skin, suggesting retention in the stratum corneum. Most of this product is excreted in the body after metabolism. ^[2]

Ticonazole indications

It is mainly used for vaginal fungal infections, such as those caused by Candida albicans, other Candida species and Trichomonas vaginalis. ^[2]

Ticonazole dosage usage

Local vaginal administration: suppositories, once per night before bedtime, using the attached dispenser, the course of treatment is 3, 6, or 14 days; ointment, once with the attached dispenser for intravaginal, if once a single dose If it is not cured, it can be used again after 1 week.

Do not use the various dosage forms of this product during menstruation. The drug should be discontinued when allergic symptoms appear. ^[2]

Ticonazole adverse reactions

Sometimes skin symptoms such as local irritation, itching, redness, puffiness, pimples, small blisters, scales, and cracks may appear. ^[2]

Ticonazole contraindications

It is contraindicated in patients with a history of allergies to imidazole antifungals. Pregnant women should avoid using this product. Not for cornea and conjunctiva. ^[2]

Ticonazole drug interactions

Combined with benzodiazepines, the latter can increase the blood concentration and increase the toxicity (central nervous system inhibition). Its mechanism of action is to inhibit the cytochrome P4503A enzyme. Therefore, the two should be avoided. The signs of possible toxicity should be monitored and the latter dose adjusted according to the dosage of this product. ^[2]

Ticonazole precautions

Sometimes the skin will experience local irritation, itching, redness, pimples, small blisters and other symptoms. Those who are allergic to this product or imidazole antifungal drugs are contraindicated. Avoid this product in the first trimester of pregnancy; stop using it during menstruation; rinse the vagina before topical application. ^[2]

Ticonazole Specifications

Suppository: 100mg × 3. Ointment: 2%, 20g.

Ticonazole Expert Reviews

This product is a synthetic broad-spectrum antifungal drug of imidazole, showing strong bactericidal activity against Candida albicans, and against pathogens such as ringworm, pityriasis versicolor, and skin candidiasis, and miconazole and clotrimazole. Have equal or greater effect. It is also effective against Trichomonas vaginalis. According to foreign reports, 395 cases of superficial mycosis were compared with clotrimazole in 21 hospitals in the United States and Switzerland, and 902 cases were subjected to general clinical trials. The results show that the double-blind, control group has a high final effectiveness. In the clotrimazole group, the effective rate for tinea corporis was 91%, the effective rate for ringworm and tinea pedis was 74%, and the effective rates for tinea versicolor and candidiasis were 94%. Domestic reports reported that 119 cases of itch and tinea corporis were treated with ticonazole cream, and 59 cases in the control group were treated with 25% benzoic acid ointment. Both groups were applied topically, twice daily. Results Among the 117 cases (excluding 2 cases that were not revisited) in the treatment group, the cure rates of tinea corporis and tinea corporis were 98.48% and 98.03%, respectively. The average days of cure were (6.66 ± 3.45) days and (6.86 ± 2.76) days. . Of the 56 cases actually completed in the control group (3 cases switched to other drugs due to drug stimulation), the cure rates of jock itch and body ringworm were 82.93% and 86.67%, respectively; the average cure days were (13.06 ± 7.03) days and (13.92 ± 5.6) days. The effect of the treatment group was significantly better than that of the control group. ^[3]