Diflucan – The Fungus Killer
Since Alexander Fleming discovered penicillin, enormous advances have been made in pharmacology, inventing new antibiotics capable of covering more and more species of microorganisms. One of the most important of the entire antimicrobial era is Fluconazole, one of the most potent antifungals available in modern medicine.
Although fungal diseases are not as frequent as bacterial or viral diseases, they have a special place among all pathologies. They are usually due to disorders where there is a deficit in immunity, such as HIV, although it can also be caused by small microorganisms that infect our skin or nails.
Undoubtedly, antifungals are also necessary, even though our natural defenses are in good condition. For this reason, a whole generation of drugs has been created where Fluconazole is one of the most important protagonists.
This antifungal is not only used for superficial lesions but is one of the most important weapons against serious systemic infections. Although it has several forms of presentation, it is necessary to clarify that the most used are the capsules, especially for superficial infections, and intravenous ampoules, for the most complicated.
However, there are several ways of presentation and we will clarify each of the features of Fluconazole. It is also necessary to note that, like most antifungals, there can be several undesirable adverse effects, but they are easily counteracted with other drugs.
Mechanism of Action
Fluconazole, like many other antifungals, has a classic mechanism of action: it inhibits a fundamental enzyme in the metabolism of fungi. Although this same enzyme also inhabits mammals, its action is much weaker and does not represent a risk. Remember that fluconazole is one of many drugs approved by the FDA many years ago.
The inhibiting enzyme is 14 alpha demethylase, which is responsible for modifying the formation of structures within fungi. This enzyme is inhibited by the suppression of cytochrome p450, like the one found in humans, which is given by the conversion of certain essential compounds within the fungus.
In theory, what happens is that the fungus can no longer adequately synthesize its cytoplasmic membrane, fundamental for it to continue functioning, and begins to accumulate sterols or molecules that it should not.
Depending on the dose of this drug used, we could have an effect that ranges from static, where the fungus is not killed, but stops its proliferation, to fungicide, where it ends completely. The explanation lies in the fact that the higher the dose used, the more enzyme will be inhibited, and therefore the greater the number of products that will end up killing the microorganism will be able to accumulate.
Pharmacokinetics - How Does Fluconazole Moves in The Body?
It all depends on the route of administration. What we do need to know is that its bioavailability, the amount of drug that remains after it is absorbed orally, is very high, so there should be no problems if we consume it with any food or another drug.
In addition, the areas where fluconazole is most absorbed are urine and skin, where it can reach very high concentrations that exceed up to 10 times those found in plasma. Even so, this is a medicine that penetrates very well in almost all the body, although the concentrations found in other organs will never be so high.
The half-life and the way in which the drug is eliminated depends largely on urine and sweat, the two places where it is most concentrated. Therefore, patients who do not have optimal kidney function or those who are ingesting other substances that affect the kidneys, such as Warfarin, should not take this drug.
As the distribution is very good, fluconazole can be used for a large number of infections and general problems. However, it is necessary to clarify that all this must occur under the supervision of a specialist. Only doctors can and should prescribe this medicine.
Although there are many indications, we will limit ourselves to mentioning the most important ones. Remember that fluconazole is one of the most widely used medicines in the world, so it is not only the first choice for many diseases, but also the secondary choice for almost all fungal diseases. Among the most relevant indications we have:
This is a disease which most often affects the mucous membranes. It is due to a group of fungi that enter the Candida spp and can be mild or severe depending on the patient. Although it is more common to have a predilection for the vagina and vaginal mucous membranes, as it happens with vaginal infections that occur in any woman, it could also be seen in other areas.
This is an opportunistic microorganism, like most fungi, which means that it can infect atypical in people who have compromised immunity, such as HIV patients. Instead of appearing slightly on the lips or genitals, candida infection may show up in the oral or esophageal mucosa without any problems.
Whatever the case while we are talking about candida, fluconazole will always be an ideal drug for its treatment. It is even necessary to mention that when local therapies cannot cure candidiasis, it will always be the turn of fluconazole.
Even some cases of balanitis due to candida that was treated ineffectively with creams or vaginal candidiasis that was treated with eggs to which it did not respond, in both cases fluconazole could be the answer. It may be considered an option for women who have recurrent genital infections (with more than 4 episodes per year).
There are several types of meningitis, which refers to inflammation of the meninges which is one of the layers lining the nervous system. However, fungal meningitis is one of the most complicated to treat, since patients are usually in very delicate conditions.
Normally, the microorganism that infects this area is the cryptococcus, a fungus quite close to the nervous system. Although treatment with fluconazole is highly effective, the therapeutic period is quite long, and the patient may require many doses.
Even sometimes - when fluconazole is not the first choice - this drug may be used to treat cryptococcal meningitis in patients who are at high risk of relapse or who have relapsed. Whatever the case, fluconazole will always be an effective drug for treating these conditions.
There is also the case of fungal skin infections, which are extremely common. We are not only talking about the famous "athlete's foot", in which there is a fungus that is infecting the intertrigo of the fingers, but also those lesions that respond to the name of "tinea corporis or cruris", where any other area of the skin is affected.
Although there is a topical treatment to which patients usually respond, it is necessary to clarify that this is not the rule. The origin of this disease has to do with the hygiene of those who suffer from it. Normally, when your hygiene is poor, it makes you prone to suffer from dermatomycosis.
Therefore, when a person has a long time with this pathology (and simply has not wanted to receive or seek treatment), it becomes difficult to treat and does not respond adequately to topical therapy. This is where fluconazole comes in.
This noble medicine can wipe out any microorganism that has long resided in any patient, regardless of the magnitude of the infection. For this reason, it can even be used in some deep dermal or nail infections, when it has been determined that the cause is a fungal agent. Without a doubt, fluconazole is an excellent antifungal.
4. Immunosuppressed Patient
As mentioned above, most fungal infections are classified as opportunistic. This means that they take advantage of the fact that the immunity of the host is low or decayed in order to attack and form their colony.
For this reason, in many cases with immunosuppressed patients there are different pathologies in almost all organs, especially the gastrointestinal tract. Depending on the microorganism and how complicated the patient is, fluconazole could be used in both capsules and ampoules (endovenous route).
The truth is that this drug ends up being effective enough to kill all those microorganisms that are trying to infect the host or that have already created their colony. Fluconazole is a mainstay in the treatment of fungal infections and has one of the highest effectiveness rates of all antibiotics.
Dosage - How to Take Diflucan
It is worth noting, to begin with this section of the article, that doses should always be handled by a physician. Only a health specialist is trained to treat patients properly and to indicate the corresponding doses according to the pathology that is affecting them.
Just to give some examples, we can use the famous vaginal ova for women who have infections in their genitals, where the doses can be between 150 and 300mg depending on the case. In addition, in some skin infections, as explained above, the same doses may be used to eliminate the microorganisms.
On the other hand, it is also possible to use fluconazole in two fundamental states that occur in several patients: as a prophylactic or as an initial broad-spectrum agent (when the cause of the infection is not known). As a prophylactic agent, the dose would be quite like the previous one (150-300mg), however, when it comes to broad spectrum could increase a lot depending on the severity of the patient.
Some systemic infections, where the whole body is under the effects of some fungus, doses could reach 600mg a day, which is quite high. Even when it comes to patients with meningitis due to fungus, this could be as high as 800mg/day. Of course, this limit must be imposed considering the state of liver function and the kidneys, which are the ones that will bear the weight of its elimination.
Finally, as for the smallest, doses range from 3 to 12mg/day, depending on the cause that merits its use. In addition, sometimes "impregnation" doses are used, which are quite high, and then "maintenance" doses are used, which correspond to the common doses described above.
The basis for this type of dosage lies in the effect of the antibiotic itself. The aim is to increase blood concentrations rapidly, through a high dose of fluconazole, and then only maintain plasma levels. This is how to use this medicine.
Contraindications - When NOT to take Fluconazole
If you have never taken antifungals before, it is best to start with small doses that you can control in case you have an allergic reaction to the medication. Remember, there are many effects that cannot be controlled when you are allergic to the drug.
Among the possible warning signs that you are allergic are: the presence of a fleeting skin rash, hambones all over the skin, edema of the glottis, inability to breathe (whether mild or severe), as well as a generalized edema throughout the body. If you are allergic to fluconazole, you are probably allergic to other antifungal medications, so be careful.
Remember that the metabolism (the first step for elimination) of the drug occurs in the liver, so it can be lethal to use this type of medication in patients who have problems processing normally substances that have hepatic metabolism.
Fluconazole may also interact with other medications that have their passage through the liver. There are specific enzymes that are responsible for metabolizing this drug which can also be saturated by having to metabolize to a different drug. For this reason, great care must be taken in combination therapies.
Some of the symptoms that indicate that Fluconazole may be having a greater than expected impact on the liver are: yellowing of the skin or ocular conjunctiva, extreme fatigue, loss of appetite, vomiting and even pain in the right upper abdominal region (where the liver is located).
Like most drugs, fluconazole also has several adverse effects to watch out for. Remember, it is difficult for a drug (whatever it is) not to have some undesirable effect, since it often inhibits certain enzymes or factors that can affect the functioning of the rest of the body.
In the case of fluconazole, it is necessary to remember that it inhibits an enzyme on fungi that is also found in humans. Therefore, it is likely to impede our normal functioning as we have been mentioning. In fact, this enzyme is found in greater concentration in the same liver, so it represents a double and important hepatic risk.
Headache, diarrhea, general malaise, vomiting, nausea, etc. All these may be common effects that occur after the intake of this medicine. It does not mean that it causes real damage to any of the organs we have mentioned, but that the same effect of the medicine causes this reaction.
Let us remember that we are all different and may be more sensitive than others to certain drugs. It does not have much to do with the potency or severity of the pill itself, but with the ability we must withstand the effects of the pill.
Mild reactions, such as rashes, may occur on the skin. This is one of the areas (as mentioned at the beginning) that is most impregnated after the use of fluconazole. It is even likely that a certain amount of medication will be eliminated through sweating.
However, sometimes these reactions can worsen or have a greater impact on the patient, depending on their sensitivity. This is when welts, blisters, itching, and even a profuse increase in sweating begin to appear. These are rare effects that occur in only 1 out of 100 patients.
Now, even rarer but probable, a reddish or purple coloration may appear on the skin, which may be caused by alterations in the number of platelets (which control bleeding). In these cases, the drug may be affecting the viscosity of our blood.
Most often there is muscle pain, however, there are several important symptoms to be aware of in the neurological sphere. One of the most prominent is the inability to sleep or abnormal perception of sensations, as if a limb or an area of our body were asleep.
Apart from this, more rare adverse effects are likely to include seizures, out-of-place numbness, or nerve punctures. In some cases, there has even been a decrease in taste or changes in the sensation of taste.
Similarly, it is likely that the patient will experience tremors and have a kind of drowsiness after the use of this. As we have emphasized throughout the article, the effects are different and manifest differently in all patients. In addition, the latter are important, but quite rare.
Frequently Asked Questions about Diflucan
Is it okay if I take the pill with the food?
No, none. In fact, it absorbs very well when taken with food because the absorption mechanism is independent of the food present. It is quite safe to take with any food.
How can I store the medicine?
Ideally, it should be at room temperature, away from any child. It is necessary to mention that, depending on the presentation, things may change a little. For example, if it is a suspension, it should be stored in a cold place, but it does not reach freezing point. Also, after two weeks with the bottle open, you should discard it.
When it comes to tablets, the most important thing is to keep them away from moisture and heat. If you are dealing with eggs, prefer those of a single dose so that you do not need to keep it.
What happens if I miss a dose?
Follow your doctor's instructions carefully. If this is not possible, do not be alarmed. Take the missed dose if many hours have passed. Otherwise, it is best to wait for the next dose and extend the treatment for one more dose. Drug concentrations will remain effective for a period slightly longer than the dose interval recommended by your doctor.
What should I avoid while taking fluconazole?
In general, many things. From alcohol and any type of drug that is metabolized in the liver, to anything else that can cause your general condition to get worse. You need to understand that fluconazole is a non-lethal medication, but that, under certain circumstances, it may cause side effects that can be much more than "annoying".
What should I do if I get an overdose?
First, you should seek emergency medical attention, either by going to the nearest medical center or by calling the appropriate telephone lines. If this is not possible, and only a short time has passed, encourage vomiting if possible. Ideally, however, you should contact a specialist to find out exactly how to proceed.
Fluconazole is one of the most important medicines of our time. It is undoubtedly a cornerstone in the treatment of fungal infections and a necessary drug for general medicine. In fact, there are still no good substitutes for fluconazole, but the rest of the antifungals are a little less effective than fluconazole.
For this reason, it is necessary to understand that we must be careful when using this drug. Not because it can be lethal for us or because it really represents a major threat, but it can be understood as almost the "last line" of battle against the most resistant mushrooms, so we should not abuse its use, let alone not comply with the treatment.
Finally, if you notice any adverse effects that are harmful or that you do not like, we recommend that you do not hesitate to consult your doctor. Your health will always be the most important thing, and if we can't achieve it with Diflucan, we'd better change.
By: Dr. Amy Lewis