Diflucan (Fluconazole)

Diflucan (a.k.a. fluconazole after its active component) is referred to the drug family of antifungal antibiotics commonly applied for curing the symptoms of any fungus-caused infections that can appear and spread practically on any part of a human body including throat, lungs, bladder, genital area, the blood, mouth esophagus and skin.

Healthcare providers advise therapy with the use of Diflucan in cases when a fungal infection develops in people with very weak immune system that can be causes by AIDS/HIV, transplantation of bone marrow or any kind of cancer.

Being the "pioneer" in a brand new sub-category of the antifungal agents developed on the basis of the synthetic form of triazole this medication can be applied in three different forms:
  • As orally taken tabs (strengths - 200, 150, 100 and 50 mg)
  • As an orally taken suspension (powder) with strengths 40 mg/ml and 10mg/ml
  • As a sterile solution for IV administration (in a glass) and in plastic containers Viaflex Plus (strength - 2mg per ml)

The brand medication known as Diflucan can be released only by Pfizer Inc. The generic forms of Diflucan are also available on the market and they are made by various Indian and U.S. manufacturers.

This drug is classified to the family of medicines that were joined under one title - "azole" antifungals. Like other preparations from its class this medication acts as an inhibitor of enzymes produced by fungal cells in a body in order to release ergosterol (responsible for the development of the new fungal cell membranes). In such way Diflucan decreases the release of ergosterol and slows down the growth of fungal cells.


Uses

According to the official press release, there are only few FDA-confirmed indications for the use of this preparation. Being an antifungal medicine created as a treatment of the Candida fungus Diflucan can be applied for curing people suffering from painful bone marrow transplantation and requiring the protection from Candida infections. This medical preparation is also assigned in the cases of cryptococcal meningitis.

Like with any brand preparations there are also few off-label indications Diflucan has. For example, it can be recommended when there is an urgent need to treat any infections triggered by another type of fungus.

Since fluconazole (the active component of Diflucan) stands for an antifungal agent applied only by a prescription it is strongly recommended it only according to its FDA-confirmed uses:
Candida fungus
Candida fungus
 

1. As monotherapy for curing certain fungal infections triggered by Candida fungus:
  • Infections in mouth or throat
  • Peritonitis (when infection spread in the lining of the abdominal cavity)
  • Yeast infections of vagina in females
  • UTI (urinary tract infection in males and females)
  • Candidemia (a fungal bloodstream infection)
  • Disseminated candidiasis (a widespread fungal infection that can infect any part of a body)

2. As a preventive measure against the development of infections triggered by Candida fungus in patients that are going through a recovery process after a bone marrow transplantation/chemotherapy/radiation.

3. As monotherapy for curing the symptoms of cryptococcal meningitis (a certain kind of a fungal infection that develops and spreads in the brain and spinal cord).

A common procedure when a healthcare provider assigns a broad-spectrum antifungal medication while running tests for detection of a fungus or bacteria causing the symptoms of the infection in a patient's body. After getting the test results a doctor usually indicated what specific antifungal meds a person should use.
Cryptococcal meningitis
Cryptococcal meningitis
 


When children can use Diflucan?


This medical preparation was allowed by the FDA for the use by children who are at least 6 months old. In this scenario, the antifungal agent's use is safe and efficient. Before an oral administration discuss with your child's therapist all pros and cons of applying Diflucan.

Non-confirmed/off-label indications


In certain cases your therapist may assign using Diflucan for curing indications that were not listed among FDA-confirmed uses. Off-label uses of Diflucan are considered when this preparation is applied as monotherapy for treating any kind of fungal infection caused by other type of fungus than Candida.


Dosage

The commonly assigned daily dosage of Diflucan is 150 mg when it comes to the treatment of vaginal yeast infection. In order to treat the thrush developed in a mouth or throat it is required to administer at least 200 mg of Diflucan orally per the first day of therapy following with the daily dosage of 100 mg taken per every 24 hours within 2-3 weeks. As for the treatment by Diflucan of Candida fungus related infections a healthcare provider should adjust the dosage according to the state of the infection with every particular patient. As a preventive measure from fungal infections people who are going through the recovery process from a bone marrow transplantation/chemotherapy/radiation should take at least 400 mg of Diflucan per day.

Diflucan dosage
Diflucan dosage
 
The main factors that can impact on the prescribed dosage of Fluconazole:
  • Your current medical condition and other maladies/diseases
  • The type of a fungal infection you have
  • Age and weight (especially in children)
  • Other drugs and supplements you are currently using or have recently stopped to use

The standard warning on dosage intake: never adjust the daily dosage of the medication on your own. Appeal to a therapist to get instructions on how to administer Diflucan.

General Facts for people about Diflucan dosage:

  • This medication is only available for the intake in such forms as an orally taken pill, a liquid/suspension and in few injectable forms
  • You are free to take this antifungal agent regardless mealtime at any time of the day
  • Before applying Diflucan as an oral suspension you are to shake the bottle with the medicine before each intake
  • In order to let the medication be effective you are to use as it was assigned to you
  • If you have a doubt how to apply this drug please consult any healthcare provider

Dosing rules for treating vaginal yeast infections


You need to remember that Diflucan can be applied only by adults for such treatment. The average assigned dose of Fluconazole per day to treat vaginal yeast infections is no more than 150 mg you ought to apply only by mouth. Bear in mind that Diflucan can't be administered topically. It fights with fungus only through bloodstream.

Dosage of Diflucan for cryptococcal meningitis


In order to cure the symptoms of this inflectional disease with Diflucan you are to be an adult (older than 18 years), since this drug is not allowed for children with cryptococcal meningitis. Start from 500 mg applied on the first day of the treatment and then decrease the daily dosage to 200 mg used each day within 10-12 weeks. As a preventive measure against relapsing of this disease in patients with HIV/AIDS it is advised to apply 200 mg on a daily basis according to doctor's prescriptions.

Dosage guidelines for Candida infections


Since Candida fungus can spread anywhere in a body - bloodstream, abdominal area or UT - there is no an average dosage regulation for treating all these kinds of the same fungal infection. Healthcare providers may prescribe a daily dose varying from 50 to 400 mg.
Diflucan injection
Diflucan injection


Various types and strengths


You will be able to buy Diflucan in the following strengths:
  • As 200 mg, 150 mg, 100 mg and 50 mg pills for the oral administration
  • As powder for suspension taken orally this drug is offered in the concentration of 10 mg/40 mg per each mL
  • As an injection form Diflucan is accessible in different package sizes with the concentration of 2 mg per each mL

You can use this antifungal agent only for oral administration or injections.


Warnings and Precautions

Diflucan warnings
Diflucan warnings
Hepatic injuries and Fluconazole: People who suffer from any condition related to liver insufficiency should avert using Diflucan. This drug has been forbidden because it may trigger a severe hepatic toxicity that can lead to fatal consequences including death. In addition, it is not quite understandable for now how Diflucan can cause hepatoxicity since such adverse reactions doesn't depend on the duration of treatment, dosage, sex or age of a patient. People who had problems with liver earlier should go through tests in order to prevent the development of more serious hepatic injuries. Immediately discontinue applying this medical preparation if you have a liver insufficiency of any kind.

Anaphylaxis in certain cases can also occur if you use Diflucan.

Dermatologic problems related to Diflucan: People who simultaneous have a rare exfoliative skin condition and AIDS with malignancy should prevent applying Diflucan since such combination can lead to fatality. People who started to use Diflucan with such diagnoses have to be thoroughly monitored after the treatment's discontinuation.

When Diflucan is forbidden to be applied:
  • When a patient has a QT prolongation syndrome revealed during electrocardiogram. This condition may get worse if Diflucan is applied;
  • This drug is not allowed for people with various proarrythmic conditions;
  • The combined application of Fluconazole and Erythromycin can lead to cardiotoxicity and to a sudden heart failure;
  • People with renal problems should prevent applying Diflucan as well;
  • This drug can become a potential CYP34A4 and CYP2C9 inhibitor. Patients who used other medications having the same effects have to go through tests before starting to administer Diflucan;
  • People with lactose intolerance, Lapp lactase deficiency and glucose-glactose malabsorption have to avert applying this medication as well;
  • Sucrose is contained in powder of Diflucan applied as an orally taken suspension and that is why people who have glucose malabsorption, hereditary fructose or sucrose deficiency have to prevent using this medication;
  • Generic Diflucan is also supplied as a syrup containing glycerol. This component may lead to such by-effects as stomach upset, diarrhea or headache.

Since the use of this antifungal drug may lead to seizures and dizziness, please discontinue the treatment with this preparation prior to driving any kind of motor vehicles.


Side Effects

The following section will disclose some of the main adverse reactions (so far not all of them) which may occur after the oral administration of Diflucan.

As you already know all medical preparations and supplement have a row of adverse reactions that may or may not reveal. In the most cases, people with fungal infections who are applying Diflucan tolerate it quite well without any negative consequences to their health. Frequently people who suffer adverse reactions caused by this drug can be treated from them quite easily under the surveillance of a healthcare provider.
Diflucan side effects
Diflucan side effects
 

During the clinical trials when the side effects of Diflucan were compared to adverse reactions of other antifungal preparations were revealed and documented the following most frequent by-effects of Fluconazole:
  • Nausea (was registered in 7 % of people taking participation in the clinical trials of Diflucan)
  • Headache (13%)
  • Diarrhea (3%)
  • Stomach (abdominal) ache (6%)
  • Vomiting (1.7%)
  • Heartburn or any indigestion problems (1%)
  • Dizziness (1%)
  • Changes in taste (1%)

Most dangerous adverse reactions


Few adverse reactions caused by this medication can be referred to life-threatening that is why it is essential to report about them as soon as you notice them. These by-effects are:
  • Arrhythmia (irregular heart beating)
  • Convulsions
  • Allergic reactions revealed via such symptoms as:
    • rash
    • hives
    • swelling of mouth, lips or throat
    • itching
    • difficulties in breathing like wheezing
  • Any signs of a sudden liver damage:
    • jaundice (yellowing of eyes or skin)
    • stomach pain (in upper-right abdominal area)
    • darkened urine
    • elevated level of liver enzymes (can be checked with a special blood test)

Bear in mind that the described side effects of Diflucan may or may not occur to you during treatment. Your therapist can't predict what problems you may have after using Diflucan but he can assist in overcoming them. Immediately go to consult a doctor if you notice any signs of by-effects after taking this medical preparation.


Mechanism of action

Fluconazole formula
Fluconazole formula
 
Fluconazole that makes the active component of Diflucan is referred to the class of imidazole and triazole antifungal drugs that can inhibit Cytochrome P450 enzymes making in such way fungal demethylase more sensitive than mammalian demethylase activity. Such inhibition leads to the conversion of lanosterol to ergosterol (stands for the main vital component of any fungal cytoplasmic membrane). Despite the fact Fluconazole is mainly fungistatic it can also effectively act like a fungicidal agent against some organisms (only taken in dose-adjusted manner) like Cryptococcus.

It will be essential to mention, that when Fluconazole was in the process of development by Pfizer's scientists the primal decision was to avert adding to it such function as production of chiral centers in order to prevent encounter of subsequent purification and synthesis and in such way avoid difficulties related to the accompanying variations of such biological effect. Later a certain quantity of similar compounds was determined to act like potent teratogens and then being discarded.


History

Ken Richardson
Ken Richardson
 
Fluconazole that is the basis of Diflucan was at first discovered and researched in 1981 by Ken Richardson who made a real breakthrough in applying antifungal medications against infections caused by various types of fungi. Being more effectual than previous antifungal agents Fluconazole became the medication of priority choice when it came to the treatment of infections triggered by superficial and natural kinds of fungi. Comparing to another popular antifungal drug Amphotericin B, Fluconazole has minimal adverse reactions and is offered in two forms - as oral pills/suspension and in injections. It is also more suitable for patients since its once-per-day-dosage guidelines and the absence of hospitalization.

The launch of Diflucan at the market happened at the very appropriate time - when the fungal infections threatening to life were extremely widespread and there was no a single medicine capable to cope with the most of them without hospitalization. Besides fungal infections were common among people who went through bone marrow transplantation, had severe burns, who had chemotherapy or AIDS- in other words, were vulnerable to fatal fungal infections due to the weak immune system.

About Ken Richardson - the inventor of Fluconazole


Ken Richardson got his first degree in chemistry at Trent Polytechnic in 1965 and his Ph.D at the University of Nottingham in 1969. He made a prodocotroal friendship with Robert B. Woodward from Harvard's laboratory who won the Nobel Prize because of his outstanding accomplishments in organic chemistry. Dr. Richardson started the brilliant career in Groton at Pfizer's Central Research Laboratories and then was promoted to work in Sandwich (England) at the biggest Pfizer's Research Center.

His discovery remains one of the most essential researches and inventions in the history of antifungal medicine. Dr. Richardson's true legacy lies in saving many lives of people who suffered from horrible and mostly deadly fungal infections and with the discovery of Diflucan managed to continue living safe and sound for many years.


Generic Diflucan

Generic fluconazole
Generic fluconazole
 
Pfizer is the manufacturer of an antifungal medication Fluconazole with the brand title Diflucan. But the patent for this title have expired few years ago so it became legal to produce cheaper generic versions of Fluconazole under other generic titles. In the most cases generic versions of this drug canbe found in 4 strengths as orally administered tabs and you can buy generic Diflucan as an oral suspension or an injectable form but unlike brand forms of Diflucan these forms will be available only in one strength. Bear in mind that most generic Diflucan version are equivalent to the brand medication according to the FDA. But some generics received BX rating which means they can't be applied in the same way as Diflucan.

Right now there are only few manufacturers have license to produce generic versions of Diflucan and they are:
  • Ranbaxy Pharmaceuticals, Inc.
  • Apotex
  • Dr. Reddy's Laboratories
  • Teva Specialty Pharmaceuticals
  • Baxter Healthcare
  • Roxane Laboratories, Inc.

Is generic Fluconazole as efficient as brand Diflucan?


All generics of brand medications are tested in the same way as other drugs by the U.S. FDA. Generic versions of brand medicines receive a special rating denoting their efficacy comparing to the authentic brand medical products. For example, AB or AP rating denotes that the FDA found a generic version a of drug as good as a brand titled medication with the same active components applied for curing the same diseases or disorders.

Most Fluconazole based generics received the FDA rating of AP or AB (denoting they are practically identical by efficacy with Diflucan), but some of them received BX rating meaning they act less efficiently than brand Diflucan. According to the state laws, a pharmacist can't offer you a BX-rated generic as a replacement of Diflucan.

All generics including those rated with AP or AB can contain inactive elements different from the content of Diflucan. These inactive components can be dyes, fillers or other compounds that may trigger allergies in hypertensive to such substances people.

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