Last Updated on February 19, 2017 by Dr.Derek Fhisher

Diflucan Fluconazole 50, 150, 100, 200 mg
Most popular brand: Diflucan
Active ingredient: Fluconazole
Available dosage forms: 50, 150, 100, 200 mg
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Fluconazole general information

Anti-fungal treatments, for example fluconazole, nystatin and ketoconazole could possibly be prescribed. When somebody is diagnosed with a fungal infection, the medical provider recommends the usage of antifungal medicines for example fluconazole, ketoconazole, Itraconazole, or terbinafine. Any antibiotics should be discontinued. Antifungal medicines should just be taken after consultation by means of your healthcare provider.

Chronic yeast infection can lead to a big selection of symptoms. Treatment will be different agreeing with the kind of infection. Mentioned here are certain signs and symptoms that can warn you about the beginning of onychomycosis.

When pregnant, you’re susceptible to several infections and sexually transmitted diseases as your own immune system isn’t working to its complete capacity. It may be a significant vaginal infection or vaginal inflammation for example trichomonas, or bacterial vaginosis, all which need appropriate medication. Among the most typical factors behind galactorrhea are tumors within the pituitary gland.

You should try and hold your diabetes in order. Following a fitness regimen is going to keep you physically fit. Such individuals must make some lifestyle-related changes, including following a wholesome diet and a fitness regimen. They aren’t only effective, but also don’t cause almost any side consequences!

The intensity of the poisoning symptoms is contingent on the exposure time plus volume of spores that somebody is exposed to. Rather, factors for example taking steroids (which weaken the immune system), antibiotics, and similar substances create the essential conditions where the fungi grows. Therefore, it is very important to take precautions to prevent sulfa drugs side outcomes. Use of particular medications to treat a specific disease can lead to an allergic reaction, which might manifest in a type of mouth blister.

Facial fungal rash is actually inflammation of the skin in your face, which results from a fungal infection. As the rash begins to heal, the skin has a tendency to turn into dry and flaky. Take advantage of these measures and remove the yeast infection on face.

Symptoms of vaginal thrush could include itching as well as inflammation round the genitals, soreness, and pain. If there’s constipation, the body might produce more levels of mucus so the hardened stools may be softened. Together with that, there’ll be a few other symptoms like flu, fever, abdominal malady, vomiting, or constipation. Often it might also be because of an amoeba infection named, trichomoniasis.

It truly is advised to speak with your doctor to prevent withdrawal symptoms. Therefore, it is extremely important to ask your doctor, if you’re already on some drug or medication, to prevent such side results. Ask your physician or pharmacist in case you have any query. Right Along with the test, then, other factors really have to be considered prior to a diagnosis might be made.

Thus, let’s find out whether this medicine may be taken when pregnant. In most containers, the pill is provided only once to cure the patient. Nonetheless, certain conditions may necessitate the utilization of medications while pregnant.

When the presence of the Candida infection was established there are quite a few methods to alleviate symptoms and bring the Candida in check. In the event the other party has a healthy immune system, but the Candida is going to be killed along with the person won’t suffer any symptoms. Even with the unpleasant complications due to thrush infection, it’s not considered essentially as dangerous. Aside from physical troubles, it may likewise result in abnormal behavior and disorders linked to attention span, hyperactivity, anxiety and impulse.

Fluconazole (Fluconazole): instruction, and the use of a formula

Code CAS

substance Characteristics Fluconazole

Antifungal triazole derivatives from the group.

The crystalline powder of white or almost white, odorless, with a characteristic flavor, it is soluble in water and isopropyl alcohol and sparingly soluble in ethanol and chloroform, soluble in acetone and slightly soluble in methanol (injection izoosmotichen). The molecular weight of 306,3.


Mode of action – antifungal.

Blocks number of cytochrome P450 – dependent enzymes and highly selective inhibits the synthesis of sterols in cell membranes of fungi. Effective with infections caused by fungi genus Candida spp. Cryptococcus neoformans, Microsporum spp. Trichophyton spp., as well as infections caused by pathogens Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum .

The pharmacokinetic characteristics similar to fluconazole at / in the introduction and by ingestion.

Once inside well absorbed from the gastrointestinal tract. Bioavailability is 90%, it does not affect food intake on absorption. Binding to plasma proteins ; 11 – 12%. C max and AUC proportional to dose. C max is achieved through the 1 – 2 h after administration. The equilibrium concentration of ; for 5 – 10 days of treatment (when receiving 50 – 1 400 mg once a day). Introduction of the treatment on the first day loading dose of 2 times the normal daily dose, achieves a level close to the equilibrium concentration of the second day. The apparent volume of distribution close to the total water content in the body. It penetrates into all body fluids, it passes through the BBB. Meningitis caused by fungi Fluconazole level in the cerebrospinal fluid reaches approximately 80% of plasma levels. In healthy volunteers, fluconazole concentration in saliva was equal to or slightly higher than its level in plasma is dose dependent way and the duration of administration. In patients with bronchiectasis sputum concentration of fluconazole after 4 and 24 h after a single oral dose of 150 mg was similar to plasma. After receiving a single oral dose of 150mg fluconazole concentration ratio vaginal tissue / plasma was 0,94 – 1,14 during the first 48 hours (n = 27), the ratio of vaginal fluid / plasma ; 0,36 – 0,71 during the first 72 hours (n = 14). The ratio of the concentrations of fluconazole urine / plasma and normal skin / plasma reached 10.

Write mainly kidneys in healthy volunteers, 80% of fluconazole excreted unchanged, about 11% ; in the form of metabolites. T 1/2 ; about 30 hours (in the range of 20 – 50 h). The pharmacokinetics of fluconazole significantly depends on renal function. T 1/2 is inversely proportional to creatinine clearance.

When receiving fluconazole in healthy volunteers at doses ranging from 200 mg to 400 mg once daily for 14 days had little effect on the testosterone concentration was observed, endogenous corticosteroids and ACTH – stimulated cortisol response. When receiving 50 mg per day did not change fluconazole testosterone concentration in the blood of men and steroid content in women of childbearing age.

carcinogenicity, mutagenicity, effects on fertility

No evidence of carcinogenicity studies fluconazole in mice and rats receiving inside it for 24 months in the doses of 2.5; 5 and 10 mg / kg / day (approximately 2 – 7 times the recommended human dose). In male rats at doses of 5 and 10 mg / kg / day there was an increase in the incidence of hepatocellular adenomas.

There were no mutagenicity of fluconazole in a number of tests in vitro and in vivo .

There was no effect on the fertility of male and female rats with daily oral administration at dosages of 5, 10 or 20 mg / kg or parenteral administration of doses of 5, 25 or 75 mg / kg, while at oral doses of 20 mg / kg was observed a small start delay delivery. In the perinatal research at / in rats doses of fluconazole 5, 20 and 40 mg / kg in a few females who received doses of 20 and 40 mg / kg (approximately 5 – 15 times higher than recommended for humans), the birth was difficult and protracted. This effect was not observed at doses of 5 mg / kg. Violations of labor accompanied by a slight increase in the frequency of occurrence of stillborn pups and decrease of neonatal survival. The impact on labor in rats is consistent with the specific estrogensnizhayuschim effects caused by high doses of fluconazole. Similar hormonal changes in women treated with fluconazole, are not found.

Teratogenic effects of . In two studies with oral fluconazole in pregnant rabbits during the period of organogenesis at dosages of 5, 10, 20, 25 and 75 mg / kg was observed violation gain animal body weight at all doses and miscarriages at a dose of 75 mg / kg (approximately 20 – 60 times higher than the recommended doses for humans), with adverse fetal disorders not observed. In several studies in which fluconazole was used inside in pregnant rats during organogenesis, disorders weight gain and placental weight were increased at a dose of 25 mg / kg. At doses of 5 or 10 mg / kg of fetal disorders was not observed; at doses of 25 and 50 mg / kg and higher was an increase in the number of anatomical changes in the fetus (additional edges, expansion of the renal pelvis), delayed ossification. At doses ranging from 80 mg / kg (approximately 20 – 60 times the recommended dose for humans) and 320 mg / kg in rats increased embrioletalnost and fetal disorders including wavy ribs and cleft palate craniofascial ossification disorders. These effects are consistent with inhibition of estrogen synthesis in rats and may be the result of the well-known effect of low estrogen on pregnancy, organogenesis and childbirth.

Application of the substance Fluconazole

Cryptococcosis: cryptococcal meningitis, an infection of the skin and lungs; prevention of relapse of cryptococcosis in patients with AIDS; generalized candidosis: candidemia, disseminated candidiasis and other forms of invasive Candida infections (lesion of the peritoneum, endocardium, eyes, respiratory and urinary tract); candidiasis of the mucous membranes of the oral cavity and pharynx, esophagus, bronchopulmonary candidiasis, candiduria, candidiasis of the skin and mucous membranes, atrophic oral candidiasis (associated with wearing dentures), prevention of relapse of oropharyngeal candidiasis in patients with AIDS; Genital candidiasis: vaginal (acute or recurrent), including relapse prevention, candida balanitis; prevention and treatment of fungal infection of malignancy (treatment with cytostatics and / or radiation therapy), antibiotic therapy, treatment of immunosuppressive agents after transplantation; fungal infections of the skin (feet, body, groin), pityriasis versicolor, onychomycosis, candidiasis of the skin; deep endemic mycoses (coccidioidomycosis, paracoccidioidomycosis, sporotrichosis, histoplasmosis) in patients with intact immune systems.


Hypersensitivity, concomitant use of terfenadine, with repeated use of fluconazole doses of 400 mg and above; joint application with drugs. that prolong the QT interval and are metabolized by CYP3A4 (such as cisapride, astemizole, quinidine) ; see. “Interaction».

Restrictions on the use

Known hypersensitivity to other azole derivatives, as there is no information regarding cross-hypersensitivity between fluconazole and other azole antifungal agents (be careful).

Application of pregnancy and breastfeeding

When pregnancy is possible only in life-threatening severe infections, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies of the safety in pregnant women have not performed). There are reports of various congenital disorders in babies whose mothers for 3 months or more were treated with high doses of fluconazole ; 400 – 800 mg / day over coccidioidomycosis, although the cause – effect relationship of these cases with taking fluconazole is unclear.

Category effects on the fetus by FDA ; C.

At the time of treatment should stop breastfeeding (fluconazole concentrations in breast milk compared to plasma).

Side effects of substance Fluconazole

Patients treated with a single dose for vaginal candidiasis

In comparative clinical trials in the United States in patients with vaginal candidiasis (n = 448) received a single dose of 150 mg fluconazole, the total incidence of adverse effects possibly associated with drug intake, was 26%; in patients treated with the reference drug (n = 448) – 16%. The most common side effects associated with taking fluconazole were headache (13%), nausea (7%), abdominal pain (6%), diarrhea (3%), dyspepsia (1%), dizziness (1%) dysgeusia (1%). Most side effects were mild or moderate in severity. Very rarely observed in market research angioedema and anaphylactic reactions.

In patients treated with multiple doses for other infections

In the clinical trials, approximately 16% of the 4048 patients treated with fluconazole for 7 days or more, adverse reactions were observed. Treatment was discontinued due – to the occurrence of adverse events in 1.5%, from – for abnormalities in laboratory tests ; in 1.3% of patients.

During treatment with fluconazole clinically significant side effects were observed more frequently in HIV – infected patients (21%), as opposed to non – HIV – infected (13%). The number of patients who discontinued treatment due – to the occurrence of adverse effects was similar in both groups (1,5%).

The side effects that have been observed in clinical trials in the treatment of fluconazole in more than 1% of cases within 7 days or more and have been associated with taking medication (n = 4048): nausea (3.7%), headache (1 , 9%), rash (1.8%), vomiting (1.7%), abdominal pain (1.7%) and diarrhea (1,5%).

Side Effects, whose connection with the treatment of fluconazole likely: hepatotoxicity, immunological reactions.

The combined data from clinical trials and marketing experience indicate that treatment with fluconazole is accompanied by rare cases of serious toxic reactions on the part of the liver, including fatal outcome. There was no apparent relationship flukonazolassotsiirovannoy hepatotoxicity with a total daily dose, duration of therapy, sex, age of the patient. Hepatotoxic action of Fluconazole is usually (but not always) is reversible, the symptoms disappear after cessation of therapy. To prevent serious reactions on the part of the liver should be carefully monitored patients during therapy with fluconazole revealed violations of liver function tests. Treatment with fluconazole should be discontinued in the event of clinically significant symptoms of developing liver disease, which may be associated with fluconazole therapy.

The reactions on the part of the liver may have different expressions, from a small transient increase in liver transaminases to clinical hepatitis, cholestasis, fulminant hepatic failure, including fatal outcome. Cases of fatal hepatic reactions were mainly in patients with severe underlying disease (AIDS. Neoplastic disease) and is often treated with polimedikamentoznuyu therapy.

There was a statistically significant increase in median AST levels from the base in two comparative trials evaluating the effectiveness of fluconazole in the prevention of relapse of cryptococcal meningitis. Increased serum transaminases more than 8 times higher than the upper limit of normal were observed in approximately 1% of patients treated with fluconazole. These cases have been observed in patients with severe underlying disease (AIDS. Malignancies), most of whom were receiving multiple concomitant drug therapy, including many drugs with known hepatotoxic. The frequency increase of transaminase level was higher in patients receiving fluconazole concurrently with one or more of the following: rifampin, phenytoin, isoniazid, valproic acid, oral hypoglycemic agents – sulfonylurea derivatives.

Immunological response: reported rare cases of anaphylaxis.

The side effects, communication has not been established with fluconazole treatment.

From the CNS: convulsions.

Dermatologic: exfoliative skin conditions including Stevens – Johnson and toxic epidermal necrolysis; alopecia.

exfoliative skin disorders during treatment with fluconazole is rare in patients with severe underlying diseases (AIDS. Neoplastic diseases) they had rarely fatal. If during treatment with fluconazole skin symptoms appear, requires careful patient monitoring and with an increase in symptomatic treatment with fluconazole should be discontinued.

Hematopoietic and lymphatic: leukopenia, including neutropenia and agranulocytosis, thrombocytopenia.

Metabolic: hypercholesterolemia, hypertriglyceridemia, hypokalemia.

Side effects observed in children

In clinical trials, the Phase 2 and 3 in the US and Europe in 577 patients aged 1 day & minus; 17, fluconazole-treated at doses up to 15 mg / kg / day up to 1,616 days, the side effects were observed in children in 13% of cases; in patients treated with the reference drug (n = 451) ; 9% of cases. The most common side effects were marked by the following: vomiting (5.4%), abdominal pain (2.8%), nausea (2.3%), diarrhea (2.1%). Treatment was discontinued due – to the occurrence of adverse effects in 2.3% of patients, – for abnormalities in laboratory tests (in most cases ; increase in transaminases and alkaline phosphatase) ; in 1.4% of patients.


Fluconazole increases T 1/2 from the plasma of oral hypoglycemic drugs ; sulfonylureas (possible symptomatic hypoglycemia). Increases concentration of phenytoin (optionally simultaneous use of both drugs phenytoin concentrations should be monitored and to adjust the dose to provide a therapeutic concentration in serum). Against the backdrop of increased fluconazole (slowing biotransformation) serum concentrations of theophylline (should closely monitor the concentration of theophylline in the blood and adjust therapy accordingly if necessary). With simultaneous use of zidovudine with fluconazole observed increase in C max of zidovudine by 84%, AUC ; 74%, T 1/2 is prolonged by approximately 128%; may increase the side effects of zidovudine (you may need to decrease the dose of zidovudine). Fluconazole increases the AUC of saquinavir by approximately 50%, C max ; approximately 55% and decreases clearance of saquinavir by approximately 50% (may require dose adjustment of saquinavir).

Fluconazole increases plasma concentrations of sirolimus presumably – for the inhibition of metabolism of sirolimus, mediated by CYP3A4 and P – glycoprotein (while the application may require a dosage adjustment of sirolimus).

Fluconazole may significantly increase the cyclosporine blood levels in patients with kidney transplantation with or without renal dysfunction (requires monitoring of cyclosporine concentrations and creatinine levels in the blood).

In a joint application of fluconazole and anticoagulants of the coumarin type may be extended PT. therefore the development of possibly bleeding (hematoma, bleeding from the nose and gastrointestinal tract hematuria and melena.); we recommend careful monitoring of PV. you may need to change the dose of warfarin. Rifampicin increases the metabolism of fluconazole: the AUC is reduced by 25%, T 1/2 ; 20% (it should be possible to increase the dose of fluconazole).

When receiving fluconazole (100 mg), together with hydrochlorothiazide (50 mg) for 10 days fluconazole blood of healthy volunteer plasma (n = 13) increased by about 40%, and renal clearance was reduced by 30%.

With the simultaneous use of fluconazole and rifabutin serum concentrations of rifabutin increased. There have been reports of uveitis development. Patients simultaneously receiving rifabutin and fluconazole should be carefully observed.

Fluconazole may increase systemic exposure of NSAIDs. are metabolized by CYP2C9 (including naproxen, lornoxicam, meloxicam, diclofenac); It recommends frequent monitoring of patients for early detection of side effects and NSAID – mediated toxicity; you may need a dose adjustment of NSAIDs.

At the same time taking fluconazole (200 mg daily) and celecoxib (200 mg) C max increased by 68%, AUC ; 134%; when co-administered may need to reduce the dose of celecoxib by half.

The use of fluconazole concurrently with drugs. metabolized with participation of cytochrome system P450 (including cisapride, astemizole, quinidine) may increase serum levels of these funds (in the absence of accurate information necessary to exercise caution and carefully monitor the condition of patients).

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