Terconazole

Terconazole Uses, Dosage, Side Effects, Food Interaction and all others data.

Terconazole disrupts ergosterol synthesis by binding to fungal cytochrome P450. It is active in vitro against Candida spp. and other fungi. It has some antibacterial activity in vitro but not against usual vag flora e.g, lactobacilli.

Terconazole is a triazole antifungal agent available for intravaginal use. It is structurally related to imidazole-derivative antifungal agents, although terconazole and other triazoles have 3 nitrogens in the azole ring. By inhibiting the 14-alpha-demethylase (lanosterol 14-alpha-demethylase), Terconazole inhibits ergosterol synthesis. Depletion of ergosterol in fungal membrane disrupts the structure and many functions of fungal membrane leading to inhibition of fungal growth.

Trade Name Terconazole
Generic Terconazole
Terconazole Other Names Terconazole
Type
Formula C26H31Cl2N5O3
Weight Average: 532.462
Monoisotopic: 531.180395297
Protein binding

94.9%

Groups Approved
Therapeutic Class Drugs used in Vaginal and Vulval condition
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Terconazole
Terconazole

Uses

Terconazole Vaginal Cream and Vaginal Suppositories are used for the local treatment of vulvovaginal candidiasis (moniliasis). As these products are effective only for vulvovaginitis caused by the genus Candida, the diagnosis should be confirmed by KOH smears and/or cultures.

Terconazole is also used to associated treatment for these conditions: Vulvovaginal Candidiasis

How Terconazole works

Terconazole may exert its antifungal activity by disrupting normal fungal cell membrane permeability. Terconazole and other triazole antifungal agents inhibit cytochrome P450 14-alpha-demethylase in susceptible fungi, which leads to the accumulation of lanosterol and other methylated sterols and a decrease in ergosterol concentration. Depletion of ergosterol in the membrane disrupts the structure and function of the fungal cell leading to a decrease or inhibition of fungal growth.

Dosage

Terconazole dosage

Terconazole Vaginal Cream 0.4%: One full applicator (5 g) of 7 Vaginal Cream (20 mg terconazole) should be administered intravaginally once daily at bedtime for seven consecutive days.

Terconazole Vaginal Cream 0.8%: One full applicator (5 g) of Vaginal Cream (40 mg terconazole) should be administered intravaginally once daily at bedtime for three consecutive days.

Terconazole Vaginal Suppositories 80 mg: One Vaginal Suppository (80 mg terconazole) should be administered intravaginally once daily at bedtime for three consecutive days.

May decrease absorption of ciprofloxacin, ciclosporin, mycophenolate, tacrolimus and levothyroxine. Sevelamer should be given 3 hr before or 1 hr after taking other drugs to minimise potential pharmacokinetic interaction.Before prescribing another course of therapy, the diagnosis should be reconfirmed by smears and/or cultures and other pathogens commonly associated with vulvovaginitis ruled out. The therapeutic effect of these products is not affected by menstruation.

Store at Controlled Room Temperature 15–30°C

Side Effects

Vulvovaginal burning, vulvar itching, dysmenorrhoea, genital, body and abdominal pain. Flu-like syndrome with headache, fever, chills and hypotension with doses >80 mg.

Toxicity

The oral LD50 values were found to be 1741 and 849 mg/kg for the male and female in rat.

Precaution

Discontinue use and do not retreat with terconazole if sensitization, irritation, fever, chills or flu-like symptoms are reported during use. The base contained in the suppository formulation may interact with certain rubber or latex products, such as those used in vaginal contraceptive diaphragms; therefore concurrent use is not recommended.

Interaction

May decrease absorption of ciprofloxacin, ciclosporin, mycophenolate, tacrolimus and levothyroxine. Sevelamer should be given 3 hr before or 1 hr after taking other drugs to minimise potential pharmacokinetic interaction.

Food Interaction

No interactions found.

Elimination Route

Following intravaginal administration of terconazole in humans, absorption ranged from 5-8% in three hysterectomized subjects and 12-16% in two non-hysterectomized subjects with tubal ligations

Half Life

6.9 hours (range 4.0-11.3)

Elimination Route

Following oral (30 mg) administration of 14C-labelled terconazole, excretion of radioactivity was both by renal (32-56%) and fecal (47-52%) routes.

Pregnancy & Breastfeeding use

Pregnancy Category C. There was no evidence of teratogenicity when terconazole was administered orally up to 40 mg/kg/day (25x the recommended intravaginal human dose of the suppository formulation, 50x the recommended intravaginal human dose of the 0.8% vaginal cream formulation, and 100x the intravaginal human dose of the 0.4% vaginal cream formulation) in rats, or 20 mg/kg/day in rabbits, or subcutaneously up to 20 mg/kg/day in rats.

Nursing Mothers: It is not known whether this drug is excreted in human milk. Animal studies have shown that rat offspring exposed via the milk of treated (40 mg/kg/orally) dams showed decreased survival during the first few post-partum days, but overall pup weight and weight gain were comparable to or greater than controls throughout lactation. Because many drugs are excreted in human milk, and because of the potential for adverse reaction in nursing infants from terconazole, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

Patients known to be hypersensitive to terconazole or to any of the components of the cream or suppositories.

Special Warning

Pediatric Use: Safety and efficacy in children have not been established.

Geriatric Use: Clinical studies of terconazole did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

Acute Overdose

Overdose of terconazole in humans has not been reported to date. In the rat, the oral LD 50 values were found to be 1741 and 849 mg/kg for the male and female, respectively. The oral LD 50 values for the male and female dog were @ 1280 and ≥ 640 mg/kg, respectively.

Innovators Monograph

You find simplified version here Terconazole

Terconazole contains Terconazole see full prescribing information from innovator Terconazole Monograph, Terconazole MSDS, Terconazole FDA label

FAQ

What is Terconazole used for?

Terconazole is an antifungal medicine. It is used to treat yeast infections of the vagina.

How quickly does Terconazole work?

Terconazole starts working within 5 to 10 hours after being inserted into the vagina. You may see improvement in symptoms within 1 or 2 days after starting this medication.

What are the side effects of Terconazole?

Common side effects may include:

  • headache;
  • body pain;
  • vaginal pain, burning, or itching;
  • stomach pain; or.
  • increased menstrual cramps.

How long should I use Terconazole for?

Terconazole vaginal is usually applied once daily at bedtime for 3 to 7 days in a row. Follow your doctor's instructions.

Can you use too much Terconazole?

Do not use in larger or smaller amounts or for longer than recommended. Do not take Terconazole vaginal by mouth. It is for use only in your vagina.

Is it safe to use Terconazole while pregnant?

Since Terconazole is absorbed from the human vagina, it should not be used in the first trimester of pregnancy unless the physician considers it essential to the welfare of the patient.Terconazole may be used during the second and third trimester if the potential benefit outweighs the possible risks to the fetus.

Do you have to use Terconazole at night?

Terconazole is usually used daily at bedtime for either 3 or 7 days.

Can I still use Terconazole during my period?

You can use the medication even if you are having your menstrual period.

Can sperm cause yeast infections?

But sometimes sexual activity can lead to vaginitis. Your partner's natural genital chemistry can change the balance of yeast and bacteria in your vagina. In rare cases, you can have an allergic reaction to your partner's semen.

Can I use Terconazole long time?

Keep using this medicine for the full time of treatment, even if your symptoms improve after the first few doses. Do not stop using the medicine if your menstrual period begins during your treatment time.

How much Terconazole do I use?


Adults one full applicator (5 grams) applied in the vagina once a day at bedtime for 3 or 7 consecutive days, as directed by your doctor.

What happens if I miss a day of Terconazole?

If you miss a dose, use it as soon as you can. If it is almost time for your next dose, use only that dose. Do not use double or extra doses.

When can I stop taking Terconazole?

Keep using this medicine for the full time of treatment, even if your symptoms improve after the first few doses. Do not stop using the medicine if your menstrual period begins during your treatment time

How long does yeast infection cream stay in?

Stay within the vagina to work without having to reapply every day for seven days.

Is Terconazole radioactive?

Terconazoleis extensively metabolized.Total radioactivity was eliminated from the blood with a harmonic half-life of 52.2 hours

What kind of yeast does Terconazole treat?

Terconazole is only effective for vaginal infections caused by a species of yeast called Candida. It is not effective for other infections, such as bacterial vaginosis.

Can I use Terconazole externally?

If you have itching/burning around the outside of the vagina, you may also apply Terconazole cream once daily to that area and rub in. Continue to use this medication every day until the full prescribed amount is finished, even if symptoms disappear after 1 to 2 days.

*** Taking medicines without doctor's advice can cause long-term problems.
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