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Active ingredient of drug Fluconazole

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Fluconazole is part of the triazole group and has antifungal activity based on strong selective inhibition of fungal sterol synthesis. Fluconazole has been shown to be effective against most of the following microorganisms in clinical and in vitro infections: Candida albicans, Candida parapsilosis, Candida glabrata (many strains are moderately susceptible), Candida tropicalis and Cryptococcus neoformans.

Diflucan - The Fungal infections killer

Since Alexander Fleming's discovery of penicillin, huge advances in pharmacology have been made and new antibiotics have been invented to detect more and more types of microorganisms. Fluconazole, one of the most effective antimycotics available in modern medicine, is one of the key agents in the entire antimicrobial era.

Although fungal diseases are not as common as bacterial or viral diseases, they occupy a special place among all pathologies. They are usually due to disorders in which an immunodeficiency exists, for. For example, HIV. However, they can also be caused by small microorganisms that infect our skin or nails.

Without a doubt, antimycotics are also necessary, even if our natural defenses are in good condition. For this reason, a whole generation of drugs has been developed in which fluconazole is one of the most important protagonists.

This antifungal drug is not only used on superficial lesions, but is also one of the most important weapons against serious systemic infections. Although there are several dosage forms, it should be noted that capsules, especially for superficial infections, and intravenous ampoules are most commonly used for the more complicated ones.

However, there are several forms of administration and we will explain the individual characteristics of fluconazole. It should also be noted that, as with most antifungals, there may be undesirable side effects, but they are easily counteracted by other drugs.

Action mechanism

Fluconazole, like many other antimycotics, has a classic mechanism of action: it inhibits a basic enzyme in the metabolism of fungi. Although the same enzyme is found in mammals, its effect is much lower and safe.Please remember that fluconazole is one of many FDA-approved drugs for many years. The inhibitory enzyme is 14-alpha-demethylase, which is responsible for modifying the formation of the structure in fungi. This enzyme is inhibited by the suppression of cytochrome p450, as in humans, resulting from the conversion of certain essential compounds in the fungus.

Theoretically, the fungus can not sufficiently synthesize its cytoplasmic membrane, which is fundamental for its continuous functioning, and accumulates sterols or molecules that it should not accumulate.

Depending on the dose of this drug, an effect may occur, ranging from static, in which the fungus is not killed, but prevents its replication, to fungicides, where it ends completely. The explanation lies in the fact that the higher the dose used, the more the enzyme is inhibited, and hence the greater the number of products that can kill the microorganism that can accumulate.

Pharmacokinetics - How does fluconazole move in the body?

It all depends on the route of administration. What we need to know is that its bioavailability, the amount of drug that remains after ingestion, is very high. Therefore, there should be no problem if we consume it with a diet or other medication.

In addition, the areas where fluconazole is most absorbed are urine and skin, where it can reach very high concentrations exceeding ten times the plasma concentrations. Nevertheless, it is a drug that penetrates very well in most of the body, even if the concentrations in other organs will never be so high.

The half-life and the manner in which the drug is excreted largely depend on urine and sweat, the two sites where it is most concentrated. Therefore, patients who do not have optimal kidney function or other kidney-affecting substances, such as warfarin, should not take this medicine.

Because of its very good distribution, fluconazole can be used in various infections and general problems. However, it must be made clear that all this must be done under the supervision of a specialist. Only doctors can and should prescribe this medicine.

Therapeutic advice

Although there are many indications, we limit ourselves to mention the most important ones. Remember that fluconazole is one of the most used drugs in the world. Therefore, it is not only the first choice for many diseases, but also the second choice for almost all fungal diseases. The most important indications include:

  1. candidiasis
  2. It is a disease that most often affects the mucous membranes. This is due to a group of fungi that invade the Candida species and can be mild or severe depending on the patient. Although it is more common to have a preference for the vagina and vaginal mucosa, as is the case for vaginal infections in every woman, this may also be the case in other areas.

    It is an opportunistic microorganism, like most fungi, which means it can infect atypically immunocompromised individuals, such as HIV patients.

    Instead of appearing easily on the lips or genitals, a Candida infection can easily occur in the mouth or mucous membrane of the esophagus.

    However, while talking about candida, fluconazole will still be an ideal drug for its treatment. It should even be mentioned that fluconazole is still at stake if local therapies can not cure candidiasis. Even some cases of Candida-related balanitis treated ineffectively with creams or vaginal candidiasis treated with eggs to which they have not responded may be the solution, in both cases of fluconazole. It can be considered as an option for women with recurrent genital infections (with more than 4 episodes per year).

  3. Meningitis
  4. There are several types of meningitis associated with inflammation of the meninges, one of the layers that line the nervous system. However, the treatment of fungal meningitis is one of the most complicated because patients usually suffer from very difficult conditions. Normally, the microorganism that infects this region is cryptococcus, a mushroom quite close to the nervous system. Although treatment with fluconazole is very effective, the duration of treatment is quite long and the patient may need many doses.

    Even sometimes - if fluconazole is not the first choice - this medicine can be used to treat cryptococcal meningitis in patients at high risk of relapse or relapse. In all cases, fluconazole will still be an effective drug for the treatment of these disorders.

  5. Dermatomycosis
  6. There is also the case of fungal infections of the skin, which are extremely common. We are not just talking about the famous "athlete's foot", which contains a fungus that infects the intertrigo of the fingers, but also those lesions that call the name "tinea corporis or cruris", all over the world. skin is affected.

    Although there is a topical treatment that patients usually respond to, it should be made clear that this is not the rule. The origin of this disease is related to the hygiene of the people affected. Normally, if you have poor hygiene, you are prone to dermatomycosis.

    Therefore, if a person has a long history of this condition (and simply does not want to receive or receive treatment), it becomes difficult to treat and does not respond adequately to topical treatment. This is where fluconazole comes in.

    This noble drug can eradicate any microorganism present in a patient for a long time, regardless of the extent of the infection. For this reason, it can also be applied to certain deep infections of the skin or nails when it has been determined that the cause is a fungus. There is no doubt that fluconazole is an excellent antifungal.

  7. Immunocompromised patient
  8. As mentioned above, most fungal infections are considered opportunistic. This means that they exploit the fact that the immunity of the host is weak or decaying to attack and form their colony.

    For this reason, in many cases, immunocompromised patients have different pathologies in almost all organs, particularly in the gastrointestinal tract. Depending on the microorganism and the complexity of the patient, fluconazole can be used both in capsule and ampoule (endovenous route). The truth is that this drug is effective enough to kill microorganisms that are trying to infect the host or have already established their colony. Fluconazole is a major pill in the treatment of fungal infections and has one of the highest efficacy rates of any antibiotic.

Dosage - How to take Diflucan

At the beginning of this section of the article, it should be noted that doses should always be handled by a physician. Only a health professional is trained to treat patients appropriately and to indicate the appropriate doses according to the pathology that affects them.

To give just a few examples, we can use the famous vaginal eggs for women with genital infections, with doses ranging from 150 to 300 mg, depending on the case. In addition, for some skin infections, as explained above, the same dosages can be used to eliminate microorganisms.

On the other hand, it is also possible to use fluconazole in two fundamental conditions that occur in several patients: as a prophylactic agent or as an initial broadband agent (unless the cause of infection is known). As a prophylactic agent, the dose of the previous one (150 to 300 mg) would be very similar for a broad spectrum that can increase considerably depending on the severity of the patient.

In some systemic infections, where the whole body is attacked by fungi, the doses can reach 600 mg per day, which is quite high. Even if it is a patient with meningitis caused by a fungal attack, this can be up to 800 mg / day. Of course, this limit must be determined taking into account the state of liver function and the kidneys that support the weight of their excretion.

The lowest doses range from 3 to 12 mg / day, depending on the cause for which it deserves to be used. In addition, sometimes "impregnation" boxes are used which are quite high, then "maintenance" boxes which correspond to the usual dosages described above.

The basis of this type of assay is the action of the antibiotic itself, which consists in rapidly increasing the blood concentration with a high dose of fluconazole and then only at maintaining the plasma concentrations. Here is how this medicine is used.

Contraindications - When fluconazole should NOT be taken

Allergic reactions

If you have never taken antifungals, it is best to start with small doses that you can control in case of an allergic reaction to the drug. Remember that many effects can not be controlled if you are allergic to the drug. Possible warning signs of allergy are: transient rash, Hamburian skin, glottal edema, shortness of breath (mild or severe) and generalized edema throughout the body. If you are allergic to fluconazole, you are probably allergic to other antifungals. So be careful.

Liver disease

Remember that the metabolism (the first stage of elimination) of the drug takes place in the liver. Therefore, the use of this type of medication can be fatal in patients who have difficulty treating normal liver metabolites. Fluconazole may also interact with other drugs that pass through the liver. Some enzymes are responsible for the metabolism of this drug, which can also become saturated by being metabolized into another drug. For this reason, you have to be very careful with combination therapies.

Some of the symptoms indicating that fluconazole has greater effects than expected on the liver are: yellowing of the skin or conjunctiva, extreme fatigue, loss of appetite, vomiting and even abdominal pain in the upper right (where the liver is located) is located).

Side effects

Like most medicines, fluconazole has side effects to watch for. Remember that it is difficult for any medicine to have no side effects because it often inhibits certain enzymes or factors that may affect the functioning of the rest of the body.

In the case of fluconazole, it should be noted that it inhibits an enzyme on fungi, which also exists in humans. Therefore, it is likely that our normal operation will be altered, as we have already mentioned. In fact, this enzyme is present at higher concentrations in the same liver and therefore represents a double and important risk for the liver.

  1. General
  2. Headache, diarrhea, general malaise, vomiting, nausea, etc. All of these side effects may be common after taking this medicine. This does not mean that one of the institutions mentioned above is seriously injured, but that the same effect of the drug causes this reaction.

    Remember that we are all different and that we may be more sensitive to certain medications than others. This has little to do with the effectiveness or severity of the pill itself, but with the ability to withstand the effects of the pill.

  3. Skin
  4. The skin may have mild reactions such as rashes. This is one of the areas (as indicated at the beginning) most strongly impregnated after the application of fluconazole. It is even probable that a certain amount of medicine is excreted by perspiration.

    However, these reactions may sometimes worsen or increase depending on their sensitivity. These include sweats, blisters, itching and even a sharp increase in sweating. These are rare effects that only occur in 1 in 100 patients.

    Even more rarely, but probably, a reddish or purple coloring can occur on the skin, which can be caused by a change in the number of platelets (which control the bleeding). In these cases, the drug can affect the viscosity of our blood.

  5. Neurological
  6. Muscle pain is the most common, but there are some important neurological symptoms to consider. One of the most striking is the inability to sleep or the abnormal perception of sensations, as if a limb or area of our body was sleeping.

    Apart from this, convulsions, numbness or nerve perforations are rarer. In some cases, there was even a decrease in taste or taste changes.

    Similarly, the patient is likely to experience tremor and somnolence after use. As we have pointed out throughout the article, the effects vary and manifest themselves differently in all patients. In addition, these are important, but quite rare.

Frequently Asked Questions about Diflucan

Is it ok if I take the pill with the food?

No, no In fact, it is absorbed very well when taken with food because its absorption mechanism is independent of the food present. It is safe to take with every meal.

How can I keep the medicine?

Ideally, it should be at room temperature and away from any child. It should be noted that things can change a bit depending on the presentation. For example, if it is a suspension, it must be stored in a cold place, but will not freeze. You must also have the bottle after two weeks, open bottle. For tablets, the most important thing is to protect them from moisture and heat. If you are dealing with eggs, prefer a single dose to avoid having to keep them.

What happens if I miss a dose?

Follow the instructions of your doctor carefully. If this is not possible, do not worry. Take the missed dose when several hours have passed.

Otherwise, it is best to wait for the next dose and prolong the treatment with another dose. Drug concentrations remain effective for a period slightly longer than the dose range recommended by your doctor.

What should I avoid while taking fluconazole?

In general, a lot of things. From alcohol to any type of drug metabolized by the liver, to anything that can make your condition worse. You must understand that fluconazole is a non-lethal drug, but that under certain circumstances it may cause side effects that may be more than "inconvenient".

What should I do if I get an overdose?

You must first visit an ambulance by going to the nearest medical center or calling the appropriate phone line. If this is not possible and little time has elapsed, vomit if possible. Ideally, however, you should contact a specialist for the exact procedure.

Fluconazole is one of the most important drugs of our time. It is without a doubt a cornerstone in the treatment of fungal infections and a medicine necessary for general medicine. In fact, there is still no good substitute for fluconazole, but the remaining antifungals are slightly less effective than fluconazole.

For this reason, it is important to understand that you should use this medicine with caution. Not because it can be deadly for us or because it's really a big threat, but can be understood as the "last line" of the fight against the most resistant mushrooms, so we should not abuse it, and let alone stop the treatment.

If you notice any side effects or unwanted side effects, we recommend that you contact your doctor immediately. Your health will always be the most important, and if we can not do it with Diflucan, we should change.


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