Tioconazole

Tioconazole is an Antifungal agent belonging to the pharmacological class of Imidazole Antifungals.

Tioconazole has been approved to relieve symptoms and also for the treatment and maintenance of Vulvovaginal candidiasis

The common side effects of Tioconazole include Hives, Difficulty in breathing, Swelling of the face, lips, tongue, or throat, Headache, Vaginal/urethral burning/itching/pain, Increased urination.

Tioconazole is available in the form of Vaginal cream.

Tioconazole is approved in Germany, Japan, Malaysia, India, the U.K., the U.S., and China.

Tioconazole, belonging to the pharmacological class of Imidazole Antifungal, acts as an Antifungal agent.

Tioconazole exerts its action by interacting with 14-α demethylase, which is a cytochrome P-450 enzyme responsible for converting lanosterol to ergosterol—an essential component of the yeast membrane. By inhibiting this enzymatic process, tioconazole disrupts the synthesis of ergosterol, leading to an increase in cellular permeability.

Additionally, tioconazole may demonstrate further effects, such as inhibiting endogenous respiration, interacting with membrane phospholipids, impeding the transformation of yeasts to mycelial forms, reducing the uptake of purine, and interfering with triglyceride and/or phospholipid biosynthesis. Furthermore, it blocks the ion transport pathway known as the Gardos channel, thus hindering the movement of calcium as well as potassium ions across the cell membrane.

Tioconazole has been approved to relieve symptoms and also for the treatment and maintenance of Vulvovaginal candidiasis

Tioconazole is found to be available in the form of Vaginal cream.

Tioconazole can be used in the following treatment:

● Vulvovaginal candidiasis

Tioconazole can help to relieve symptoms and also for the treatment and maintenance of Vulvovaginal candidiasis.

Tioconazole is approved for use in the following clinical indications:

● Vulvovaginal candidiasis

● Vulvovaginal candidiasis: Tioconazole has demonstrated effectiveness as a single-dose treatment for vulvovaginal candidiasis. To administer, insert one full applicator intravaginally using the prefilled applicator provided. It is advisable to consider administering Tioconazole just before bedtime, which may be a preferred time for treatment.

Tioconazole is available in the following dosage forms and strengths:

● Vaginal Cream: 1% and 6.5%

Available as Vaginal cream.

Dosage Adjustments in Kidney Patients:

There are found to be no dosage adjustments in the manufacturer's labeling.

Dosage Adjustments in Hepatic Impairment Patients:

There are found to be no dosage adjustments in the manufacturer's labeling.

Dosage Adjustments in Pediatric Patients:

Tioconazole is not intended for use in children

When taking Tioconazole, there are certain dietary restrictions that should be followed to ensure the medication's effectiveness and safety:

● There are no specific food warnings associated with the use of Tioconazole. It is a topical antifungal agent meant for external use on the skin. Since it is not ingested or absorbed systemically, there is generally no interaction with food.

The dietary restriction should be individualized as per patient requirements.

 Tioconazole may be contraindicated under the following conditions:

● Hypersensitivity to the active substance i.e Tioconazole or to any of the excipients

No specific information has been found in the product monograph. 

The excretion of this drug in human milk is unknown. Since numerous drugs are excreted in human milk, nursing should be temporarily halted while administering Tioconazole .

Pregnancy warning

Pregnancy:

Pregnancy Category C

During the organogenesis period, pregnant rats were given Tioconazole hydrochloride at doses of 55, 110, and 165 mg/kg/day orally. There were no harmful effects on the growth or viability of their fetuses. Some fetuses showed a temporary drug-related increase in the incidence of dilated ureters, hydroureters, and hydronephrosis, but this effect disappeared in pigs raised to 21 days of age. However, when the drug was administered intravaginally in a 2% cream at approximately 10 mg/kg/day, these effects did not occur.

In rabbits receiving oral doses as high as 165 mg/kg/day or daily intravaginal application of approximately 2-3 mg/kg in a 2% tioconazole cream during organogenesis, no evidence of major structural anomalies or embryotoxic/teratogenic effects was found.

Tioconazole hydrochloride is an azole antimycotic agent that can cause difficult labor (dystocia) in rats if treatment is extended through parturition. Rats experienced prolonged pregnancy, in utero deaths, and impaired pup survival. The level at which no such effect was observed was 20 mg/kg/day orally and approximately 9 mg/kg/day intravaginally.

There are found to be no adequate and well-controlled studies in pregnant women. Therefore, Tioconazole -1 (tioconazole 6.5%) should be used during pregnancy only if the potential benefits outweighs the potential risk to the fetus.

There are certain food-related warnings and precautions to consider when using Tioconazole:

● There are no specific food warnings associated with the use of Tioconazole. It is a topical antifungal agent meant for external use on the skin. Since it is not ingested or absorbed systemically, there is generally no interaction with food.

The adverse reactions related to Tioconazole can be categorized as follows:

● Hives

● Difficulty in breathing

● Swelling of the face, lips, tongue, or throat

● Headache

● Vaginal/urethral burning/itching/pain

● Increased urination

No drug interactions have been reported in the product monograph.

The following are the side effects involving Tioconazole:

● Hives

● Difficulty in breathing

● Swelling of the face, lips, tongue, or throat

● Headache

● Vaginal/urethral burning/itching/pain

● Increased urination

The use of Tioconazole should be prudent in the following group of special populations:

Pregnancy:

Pregnancy Category C

During the organogenesis period, pregnant rats were given doses of 55, 110, as well as 165 mg/kg/day of tioconazole hydrochloride orally. No negative effects on fetal viability or growth were observed. However, a temporary increase in the incidence of dilated ureters, hydroureters, and hydronephrosis was seen in fetuses due to the drug. This effect was not evident in pigs raised to 21 days of age. No such effect occurred when the drug was administered intravaginally in a 2% cream at approximately 10 mg/kg/day.

Rabbits receiving oral doses as high as 165 mg/kg/day or daily intravaginal application of approximately about 2-3 mg/kg in a 2% tioconazole cream during organogenesis showed no evidence of major structural anomalies or embryotoxic/teratogenic effects.

Tioconazole hydrochloride, like other azole antimycotic agents, induced dystocia (difficult labor) in rats when treatment continued through parturition. This led to prolongation of pregnancy, in utero deaths, and impaired pup survival in rats. The level at which no such effect was observed was 20 mg/kg/day orally and approximately 9 mg/kg/day intravaginally.

There are found to be no sufficient and well-controlled studies in pregnant women. Therefore, Tioconazole -1 (tioconazole 6.5%) should only be used during pregnancy if the potential benefit outweighs the potential risk to the fetus.

Lactation:

The excretion of this drug in human milk is unknown. Since numerous drugs are excreted in human milk, nursing should be temporarily halted while administering Tioconazole.

Pediatric:

The safety and effectiveness of this treatment in children have not been confirmed or established.

Geriatric Use:

No information pertaining to use of drug in geriartic population has been found to be available.

The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of Tioconazole.

No information pertaining to the overdose maintenance or treatment has been found in the product monographs.

Pharmacodynamics:

Tioconazole is an imidazole antifungal agent with a broad-spectrum of activity, effectively inhibiting the growth of pathogenic yeasts in humans. In vitro studies have demonstrated that Tioconazole exhibits fungicidal activity against Candida albicans, various other Candida species, and Torulopsis glabrata.

The mechanism of action involves Tioconazole interfering with the production of crucial substances required to maintain the integrity of the fungal cell membrane. As a result, the growth and function of certain fungal organisms are disrupted.

It's important to note that Tioconazole is specifically effective against fungal infections and will not be effective for treating bacterial or viral infections.

Pharmacokinetics:

No data regarding detailed pharmacokinetics has been found.

1. https://go.drugbank.com/drugs/DB01007

2. https://www.webmd.com/drugs/2/drug-63478/tioconazole-1-vaginal/details

3. https://www.webmd.com/drugs/2/drug-63478/tioconazole-1-vaginal/details

4. https://www.drugs.com/cdi/tioconazole.html

5. https://www.rxlist.com/Tioconazole-drug.htm

6. https://pdf.hres.ca/dpd_pm/00064148.PDF