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Flusol

Flusol - General Information

Triazole antifungal agent that is used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS. [PubChem]

 

Pharmacology of Flusol

Flusol, a synthetic antifungal agent of the imidazole class, is used to treat vaginal candidiasis.

 

Flusol for patients

DIFLUCAN (fluconazole tablets)

This leaflet contains important information about DIFLUCAN (dye-FLEW-kan). It is not meant to take the place of your doctor's instructions. Read this information carefully before you take DIFLUCAN. Ask your doctor or pharmacist if you do not understand any of this information or if you want to know more about DIFLUCAN.

What Is DIFLUCAN?

DIFLUCAN is a tablet you swallow to treat vaginal yeast infections caused by a yeast called Candida. DIFLUCAN helps stop too much yeast from growing in the vagina so the yeast infection goes away.

DIFLUCAN is different from other treatments for vaginal yeast infections because it is a tablet taken by mouth. DIFLUCAN is also used for other conditions. However, this leaflet is only about using DIFLUCAN for vaginal yeast infections. For information about using DIFLUCAN for other reasons, ask your doctor or pharmacist. See the section of this leaflet for information about vaginal yeast infections.

What is a Vaginal Yeast Infection?

It is normal for a certain amount of yeast to be found in the vagina. Sometimes too much yeast starts to grow in the vagina and this can cause a yeast infection. Vaginal yeast infections are common. About three out of every four adult women will have at least one vaginal yeast infection during their life.

Some medicines and medical conditions can increase your chance of getting a yeast infection. If you are pregnant, have diabetes, use birth control pills, or take antibiotics you may get yeast infections more often than other women. Personal hygiene and certain types of clothing may increase your chances of getting a yeast infection. Ask your doctor for tips on what you can do to help prevent vaginal yeast infections.

If you get a vaginal yeast infection, you may have any of the following symptoms:

• itching

• a burning feeling when you urinate

• redness

• soreness

• a thick white vaginal discharge that looks like cottage cheese

What To Tell Your Doctor Before You Start DIFLUCAN?

Do not take Diflucan if you take certain medicines. They can cause serious problems.

Therefore, tell your doctor about all the medicines you take including:

• diabetes medicines you take by mouth such as glyburide, tolbutamide, glipizide

• blood thinners such as warfarin

• cyclosporine (used to prevent rejection of organ transplants)

• rifampin or rifabutin (used for tuberculosis)

• astemizole (used for allergies)

• tacrolimus (used to prevent rejection of organ transplants)

• phenytoin (used for seizures)

• theophylline (used for asthma)

• cisapride (Propulsid; used for stomach acid problems)

Since there are many brand names for these medicines, check with your doctor or pharmacist if you have any questions.

• are taking any over-the-counter medicines you can buy without a prescription, including natural or herbal remedies

• have any liver problems.

• have any other medical conditions

• are pregnant, plan to become pregnant, or think you might be pregnant. Your doctor will discuss whether DIFLUCAN is right for you.

• are breast-feeding. DIFLUCAN can pass through breast milk to the baby.

• are allergic to any other medicines including those used to treat yeast and other fungal infections.

• are allergic to any of the ingredients in DIFLUCAN. The main ingredient of DIFLUCAN is fluconazole. If you need to know the inactive ingredients, ask your doctor or pharmacist.

Who Should Not Take DIFLUCAN?

To avoid a possible serious reaction, do NOT take DIFLUCAN if you are taking cisapride (Propulsid) since it can cause changes in heartbeat in some people if taken with DIFLUCAN.

How Should I Take DIFLUCAN

Take DIFLUCAN by mouth with or without food. You can take DIFLUCAN at any time of the day.

DIFLUCAN keeps working for several days to treat the infection. Generally the symptoms start to go away after 24 hours. However, it may take several days for your symptoms to go away completely. If there is no change in your symptoms after a few days, call your doctor.

Just swallow 1 DIFLUCAN tablet to treat your vaginal yeast infection.

What Should I Avoid While Taking DIFLUCAN?

Some medicines can affect how well DIFLUCAN works. Check with your doctor before starting any new medicines within seven days of taking DIFLUCAN.

What Are The Possible Side Effects of DIFLUCAN?

Like all medicines, DIFLUCAN may cause some side effects that are usually mild to moderate.

The most common side effects of DIFLUCAN are:

headache

• diarrhea

• nausea or upset stomach

dizziness

• stomach pain

• changes in the way food tastes

Allergic reactions to DIFLUCAN are rare, but they can be very serious if not treated right away by a doctor. If you cannot reach your doctor, go to the nearest hospital emergency room. Signs of an allergic reaction can include shortness of breath; coughing; wheezing; fever; chills; throbbing of the heart or ears; swelling of the eyelids, face, mouth, neck, or any other part of the body; or skin rash, hives, blisters or skin peeling.

Diflucan has been linked to rare cases of serious liver damage, including deaths, mostly in patients with serious medical problems. Call your doctor if your skin or eyes become yellow, your urine turns a darker color, your stools (bowel movements) are light-colored, or if you vomit or feel like vomiting or if you have severe skin itching.

In patients with serious conditions such as AIDS or cancer, rare cases of severe rashes with skin peeling have been reported. Tell your doctor right away if you get a rash while taking DIFLUCAN.

DIFLUCAN may cause other less common side effects besides those listed here. If you develop any side effects that concern you, call your doctor. For a list of all side effects, ask your doctor or pharmacist.

What To Do For An Overdose

In case of an accidental overdose, call your doctor right away or go to the nearest emergency room.

How To Store DIFLUCAN

Keep DIFLUCAN and all medicines out of the reach of children.

General Advice About Prescription Medicines

Medicines are sometimes prescribed for conditions that are mentioned in patient information leaflets. Do not use DIFLUCAN for a condition for which it was not prescribed. Do not give DIFLUCAN to other people, even if they have the same symptoms you have. It may harm them.

This leaflet summarizes the most important information about DIFLUCAN. If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about DIFLUCAN that is written for health professionals.

You can also visit the DIFLUCAN Internet site at www.diflucan.com.

 

Flusol Interactions

Clinically or potentially significant drug interactions between DIFLUCAN and the following agents/classes have been observed. These are described in greater detail below:

DIFLUCAN and the following agents/classes have been observed. These are described in greater detail below:

Oral hypoglycemics
Coumarin-type anticoagulants
Phenytoin
Cyclosporine
Rifampin
Theophylline
Terfenadine
Cisapride
Astemizole
Rifabutin
Tacrolimus
Short-acting benzodiazepines

Oral hypoglycemics: Clinically significant hypoglycemia may be precipitated by the use of DIFLUCAN with oral hypoglycemic agents; one fatality has been reported from hypoglycemia in association with combined DIFLUCAN and glyburide use. DIFLUCAN reduces the metabolism of tolbutamide, glyburide, and glipizide and increases the plasma concentration of these agents. When DIFLUCAN is used concomitantly with these or other sulfonylurea oral hypoglycemic agents, blood glucose concentrations should be carefully monitored and the dose of the sulfonylurea should be adjusted as necessary.

Coumarin-type anticoagulants: Prothrombin time may be increased in patients receiving concomitant DIFLUCAN and coumarin-type anticoagulants. In post-marketing experience, as with other azole antifungals, bleeding events (bruising, epistaxis, gastrointestinal bleeding, hematuria, and melena) have been reported in association with increases in prothrombin time in patients receiving fluconazole concurrently with warfarin. Careful monitoring of prothrombin time in patients receiving DIFLUCAN and coumarin-type anticoagulants is recommended. (See CLINICAL PHARMACOLOGY: Drug Interaction Studies.)

Phenytoin: DIFLUCAN increases the plasma concentrations of phenytoin. Careful monitoring of phenytoin concentrations in patients receiving DIFLUCAN and phenytoin is recommended. (See CLINICAL PHARMACOLOGY: Drug Interaction Studies.)

Cyclosporine: DIFLUCAN may significantly increase cyclosporine levels in renal transplant patients with or without renal impairment. Careful monitoring of cyclosporine concentrations and serum creatinine is recommended in patients receiving DIFLUCAN and cyclosporine. (See CLINICAL PHARMACOLOGY: Drug Interaction Studies.)

Rifampin: Rifampin enhances the metabolism of concurrently administered DIFLUCAN. Depending on clinical circumstances, consideration should be given to increasing the dose of DIFLUCAN when it is administered with rifampin.

Theophylline: DIFLUCAN increases the serum concentrations of theophylline. Careful monitoring of serum theophylline concentrations in patients receiving DIFLUCAN and theophylline is recommended.

Terfenadine: Because of the occurrence of serious cardiac dysrhythmias secondary to prolongation of the QTc interval in patients receiving azole antifungals in conjunction with terfenadine, interaction studies have been performed. One study at a 200-mg daily dose of fluconazole failed to demonstrate a prolongation in QTc interval. Another study at a 400-mg and 800-mg daily dose of fluconazole demonstrated that DIFLUCAN taken in doses of 400 mg per day or greater significantly increases plasma levels of terfenadine when taken concomitantly. The combined use of fluconazole at doses of 400 mg or greater with terfenadine is contraindicated. The coadministration of fluconazole at doses lower than 400 mg/day with terfenadine should be carefully monitored.

Cisapride: There have been reports of cardiac events, including torsade de pointes in patients to whom fluconazole and cisapride were coadministered. A controlled study found that concomitant fluconazole 200 mg once daily and cisapride 20 mg four times a day yielded a significant increase in cisapride plasma levels and prolongation of QTc interval.The combined use of fluconazole with cisapride is contraindicated.

Astemizole: The use of fluconazole in patients concurrently taking astemizole or other drugs metabolized by the cytochrome P450 system may be associated with elevations in serum levels of these drugs. In the absence of definitive information, caution should be used when coadministering fluconazole. Patients should be carefully monitored.

Rifabutin: There have been reports of uveitis in patients to whom fluconazole and rifabutin were coadministered. Patients receiving rifabutin and fluconazole concomitantly should be carefully monitored.

Tacrolimus: There have been reports of nephrotoxicity in patients to whom fluconazole and tacrolimus were coadministered. Patients receiving tacrolimus and fluconazole concomitantly should be carefully monitored.

Short-acting Benzodiazepines: Following oral administration of midazolam, fluconazole resulted in substantial increases in midazolam concentrations and psychomotor effects. This effect on midazolam appears to be more pronounced following oral administration of fluconazole than with fluconazole administered intravenously. If short-acting benzodiazepines, which are metabolized by the cytochrome P450 system, are concomitantly administered with fluconazole, consideration should be given to decreasing the benzodiazepine dosage, and the patients should be appropriately monitored.

Fluconazole tablets coadministered with ethinyl estradiol- and levonorgestrel-containing oral contraceptives produced an overall mean increase in ethinyl estradiol and levonorgestrel levels; however, in some patients there were decreases up to 47% and 33% of ethinyl estradiol and levonorgestrel levels. The data presently available indicate that the decreases in some individual ethinyl estradiol and levonorgestrel AUC values with fluconazole treatment are likely the result of random variation. While there is evidence that fluconazole can inhibit the metabolism of ethinyl estradiol and levonorgestrel, there is no evidence that fluconazole is a net inducer of ethinyl estradiol or levonorgestrel metabolism. The clinical significance of these effects is presently unknown.

Physicians should be aware that interaction studies with medications other than those listed in the CLINICAL PHARMACOLOGY section have not been conducted, but such interactions may occur.

 

Flusol Contraindications

DIFLUCAN (fluconazole) is contraindicated in patients who have shown hypersensitivity to fluconazole or to any of its excipients. There is no information regarding cross-hypersensitivity between fluconazole and other azole antifungal agents. Caution should be used in prescribing DIFLUCAN to patients with hypersensitivity to other azoles. Coadministration of terfenadine is contraindicated in patients receiving DIFLUCAN (fluconazole) at multiple doses of 400 mg or higher based upon results of a multiple dose interaction study.

Coadministration of cisapride is contraindicated in patients receiving DIFLUCAN (fluconazole).

 

Additional information about Flusol

Flusol Indication: For the treatment of fungal infections.
Mechanism Of Action: Flusol interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Flusol may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.
Drug Interactions: Alfentanil Increases the effect and toxicity of alfentanil
Alprazolam Increases the effect of the benzodiazepine
Amitriptyline The imidazole increases the effect and toxicity of the tricyclic
Anisindione Increases the anticoagulant effect
Atorvastatin Increased risk of myopathy/rhabdomyolysis
Carbamazepine Increases the effect of carbamazepine
Celecoxib Increases the effect of celecoxib
Chlordiazepoxide Increases the effect of the benzodiazepine
Cilostazol Decreases the effect of cilostazol
Cisapride Increased risk of cardiotoxicity and arrhythmias
Clonazepam Increases the effect of the benzodiazepine
Clorazepate Increases the effect of the benzodiazepine
Cyclophosphamide Reduces metabolism and clearance of cyclophosphamide
Cyclosporine Increases the effect of the immunosuppressant
Diazepam Increases the effect of the benzodiazepine
Dicumarol Increases the anticoagulant effect
Dihydroergotamine Possible ergotism and severe ischemia with this combination
Eplerenone This CYP3A4 inhibitor increases the effect and toxicity of eplerenone
Ergotamine Possible ergotism and severe ischemia with this combination
Estazolam Increases the effect of the benzodiazepine
Ethotoin Increases the effect of hydantoin
Everolimus The imidazole increases everolimus levels/toxicity
Fentanyl The imidazole increases levels/toxicity of fentanyl
Flurazepam Increases the effect of the benzodiazepine
Fluvastatin Increases the effect and toxicity of fluvastatin
Fosphenytoin Increases the effect of hydantoin
Halazepam Increases the effect of the benzodiazepine
Haloperidol The imidazole increases the effect and toxicity of haloperidol
Imipramine The imidazole increases the effect and toxicity of the tricyclic
Lovastatin Increased risk of myopathy/rhabdomyolysis
Mephenytoin Increases the effect of hydantoin
Midazolam Increases the effect of the benzodiazepine
Acenocoumarol Increases the anticoagulant effect
Nortriptyline The imidazole increases the effect and toxicity of the tricyclic
Phenytoin Increases the effect of hydantoin
Pimozide Increased risk of cardiotoxicity and arrhythmias
Quazepam Increases the effect of the benzodiazepine
Ramelteon This imidazole increases the levels/toxicity of ramelteon
Ranolazine Increased levels of ranolazine - risk of toxicity
Rifabutin Increases levels/toxicity of rifabutin
Rifampin Decreases the effect of imidazole
Simvastatin Increased risk of myopathy/rhabdomyolysis
Tacrolimus Increases the effect of the immunosuppressant
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Tolterodine Increases the effect and toxicity of tolterodine
Triazolam Increases the effect of the benzodiazepine
Valdecoxib The imidazole increases the effect and toxicity of valdecoxib
Vinblastine Increases the effect and toxicity of anticancer agent
Vincristine Increases the effect and toxicity of anticancer agent
Warfarin Increases the anticoagulant effect
Food Interactions: Take without regard to meals.
Generic Name: Fluconazole
Synonyms: Not Available
Drug Category: Antifungals
Drug Type: Small Molecule; Approved

Other Brand Names containing Fluconazole: Biocanol; Biozolene; Diflucan; Elazor; Flucazol; Flucostat; Flukezol; Flunizol; Flusol; Pritenzol; Triflucan;
Absorption: 90%
Toxicity (Overdose): Symptoms of overdose include hallucinations and paranoid behavior.
Protein Binding: 11 to 12%
Biotransformation: Hepatic
Half Life: 30 hours (range 20-50 hours)
Dosage Forms of Flusol: Solution Intravenous
Powder, for solution Oral
Liquid Intravenous
Tablet Oral
Capsule Oral
Chemical IUPAC Name: 2-(2,4-difluorophenyl)-1,3-bis(1,2,4-triazol-1-yl)propan-2-ol
Chemical Formula: C13H12F2N6O
Fluconazole on Wikipedia: https://en.wikipedia.org/wiki/Fluconazole
Organisms Affected: Fungi