Antifungal, Azole (Vaginal)

Antifungal azole medicines contain an azole ring which prevents the growth of many different types of fungi.

Overview

These medications are typically classified into one of two groups: those with two nitrogens within the azole ring and those with three nitrogens in the azole ring, which are also known as triazoles. The most common of these triazoles used in the treatment of vaginal yeast infection is flucanozole.

Like all other antifungal drugs, azole medicines work by exploiting certain differences between human and fungal cells in order to destroy a fungal organism with as little adverse effects on the host as possible. Antifungal azole medications function by inhibiting lanosterol 14-alpha-demethylase, which is a cytochrome P450-dependent enzyme. This enzyme helps to convert lanosterol to ergosterol, which is the main sterol in fungal cell membranes. The depletion of ergosterol helps to damage the membranes of the cell, which ultimately results in its death.

The majority of research into the azole class of antifungal medications took place in the 1990s, and this served to expand the options for the safe treatment of a number of endemic and opportunistic fungal infections. Many of today's antifungal azoles are particularly adept at treating vaginal fungal issues.

Conditions treated:

  • Vaginal candidiasis

Type of medicine:

  • Azole antifungal

Side effects:

Along with the required effects, azole medications for the treatment of vaginal antifungal infections can potentially cause a number of unwanted side effects. The most common side effects experienced by patients undergoing treatment with azole antifungals include: dry mouth, fever, decreased level of urination, increased thirst, irregular heartbeat, appetite loss, changes in mood, muscle cramps or pain, vomiting or nausea, difficulty breathing, unusual weakness or tiredness and/or a numbness or tingling sensation in the feet, hands or lips.

As the patient continues to be treated with the medicine as prescribed, many (if not all) of the previously mentioned side effects should begin to subside. Side effects which worsen in intensity or persist over a prolonged period of time warrant following up by the patient with their doctor as soon as possible, in order to rule out any potential harmful effects or allergies. For symptoms which merely cause mild discomforts, such as dry mouth or increased thirst, patients are advised to suck on sugar-free candy or ice cubes, or chew sugar-free gum. Regular glasses of water should also be consumed (eight glasses per day on average).

The majority of patients will only experience very minimal effects while being treated with antifungal azole medication – if they observe any side effects whatsoever. The drug is designed to alleviate a number of the aforementioned symptoms and is typically prescribed as the benefits of treatment with azoles greatly outweigh the risk of experiencing any potential side effects.

Some patients have described a decreased interest in sexual intercourse when using antifungal azole medicines. In some cases, this could be a direct side effect and in others, it may be psychological due to the nature in which antifungal azoles are applied vaginally.

Approximately 11% of patients in studies have reported experiencing nausea, diarrhea, gastroenteritis, constipation and other gastrointestinal conditions. Most of these conditions can be combated with an over the counter medication which does not interact with the azole the patient is currently being treated with.

Other side effects which are experienced rarely, albeit often enough to warrant mentioning, include the following: blurred vision, chills, chest pain, abdominal cramps, dark-colored stools, sold sweats, cloudy urine, coughing, diarrhea, dizziness (especially when getting up from a prone position quite suddenly), headaches, drowsiness, rashes or itching, mental changes, nervousness, pounding in the ears, noisy breathing and/or shivering.

Because antifungal azoles have the potential to affect the psychology of the patient, he or she may experience mood swings, hallucinations, memory issues, confusion, and/or depression. Because of the potential for confusion to arise or motor skills to be affected (particularly during the early stages of treatment with this medicine), patients are advised to refrain from driving or operating heavy machinery until a qualified healthcare professional has ascertained that they are safe to do so while undergoing treatment with an antifungal azole.

In some instances, patients have reported allergic reactions to the medicine. In this instance, medical assistance should be sought.

Dosage:

As with all medicines, it is incredibly important to take antifungal azoles as advised by a doctor. This means that patients should refrain from increasing doses or increasing the frequency of doses without the say-so of a qualified healthcare professional. In addition to this, patients should stop taking the medication when advised to do so by a doctor, even if they have a supply of the drug remaining.

Adult dosage for vaginal candidiasis (yeast infection):

Azole antifungal cream should be applied to the skin in and around the vaginal area in order to reduce symptoms of itching, burning and redness that are associated with a vaginal yeast infection. Before applying the first dose of azole antifungal cream, patients should be aware that this medication can only be used to treat yeast infection, and will be ineffective against other types of infection (such as bacterial vaginosis). Patients who have chills, flu-like symptoms, abdominal pain or foul-smelling vaginal discharge should not use this medication, and should instead contact a doctor who will be able to advise on a more suitable prescription medication.

Azole antifungal medications are available over the counter. If the patient is self-treating, they are advised to thoroughly read the information leaflet provided with the product. The leaflet will typically direct the patient to apply a liberal amount of the cream to the vaginal area once or twice daily, for a period of approximately seven days (or until the symptoms have subsided).

If applying more than one dose per day on the advice of a pharmacist or doctor, patients are advised to space out the doses as evenly as possible in order to increase efficacy and to prevent any irritation caused by excess application of the cream.

Interactions:

All drugs have the potential to interact with other medicines and chemicals within the human body, resulting in changes in the way one or more drugs function. These interactions can, for example, cause a medication to no longer be an effective treatment. In some instances, interactions between drugs can cause potentially harmful side effects. With this in mind, it is imperative that patients keep a detailed list of all medications they are currently taking – and this extends to over the counter remedies, vitamins and herbal supplements as well as prescription medicines.

Below is a list of some of the major medications known to have interacted negatively with antifungal azoles. Patients who are currently undergoing treatment with any of these drugs are advised to notify their doctor before starting treatment with any form on antifungal agent:

  • A-Cof DH (guaifenesin / hydrocodone)
  • A-D Anti-Diarrheal (loperamide)
  • A-G Tussin (chlorpheniramine / hydrocodone / pseudoephedrine)
  • A-Methapred (methylprednisolone)
  • abemaciclib
  • Abstral (fentanyl)
  • AccessPak for HIV PEP Expanded with Kaletra (emtricitabine / lopinavir / ritonavir / tenofovir)
  • acetaminophen / caffeine / chlorpheniramine / hydrocodone / phenylephrine
  • acetaminophen / hydrocodone
  • acetaminophen / oxycodone
  • Acetocot (triamcinolone)
  • Actiq (fentanyl)
  • Adalat (nifedipine)
  • Adalat CC (nifedipine)
  • Addyi (flibanserin)
  • Adempas (riociguat)
  • Adlone-40 (methylprednisolone)
  • Adlone-80 (methylprednisolone)
  • Advair Diskus (fluticasone / salmeterol)
  • Advair HFA (fluticasone / salmeterol)
  • Advicor (lovastatin / niacin)
  • Afeditab CR (nifedipine)
  • Afinitor (everolimus)
  • Afinitor Disperz (everolimus)
  • AirDuo Respiclick (fluticasone / salmeterol)
  • Alfenta (alfentanil)
  • alfentanil
  • alfuzosin
  • Aliqopa (copanlisib)
  • Alor 5 / 500 (aspirin / hydrocodone)
  • alprazolam
  • Alprazolam Intensol (alprazolam)
  • Altocor (lovastatin)
  • Altoprev (lovastatin)
  • Alunbrig (brigatinib)
  • Ambi 5 / 15 / 100 (guaifenesin / hydrocodone / phenylephrine)
  • Amiodarone
  • amlodipine
  • Anaplex HD (brompheniramine / hydrocodone / pseudoephedrine)
  • Anexsia (acetaminophen / hydrocodone)
  • Anolor DH5 (acetaminophen / hydrocodone)
  • Anti-Diarrheal (loperamide)
  • apixaban
  • Arava (leflunomide)
  • Aristocort (triamcinolone)
  • Aristocort For Injection (triamcinolone)
  • Aristopak (triamcinolone)
  • Aristospan (triamcinolone)
  • Aristospan Intra-Articular (triamcinolone)
  • Aristospan Intralesional (triamcinolone)
  • ArmonAir RespiClick (fluticasone)
  • Arnuity Ellipta (fluticasone)
  • artemether / lumefantrine
  • aspirin / hydrocodone
  • aspirin / oxycodone
  • Hydro-PC II (chlorpheniramine / hydrocodone
  • Halfan (halofantrine)
  • halofantrine
  • Hecoria (tacrolimus)
  • Hexatussin (chlorpheniramine / hydrocodone / pseudoephedrine)
  • Hi-Tuss HC (chlorpheniramine / hydrocodone / phenylephrine)
  • Highland HC (chlorpheniramine / hydrocodone / phenylephrine)
  • Hismanal (astemizole)
  • Histex HC (carbinoxamine / hydrocodone / pseudoephedrine)
  • Histinex D (hydrocodone / pseudoephedrine)
  • Histinex HC (chlorpheniramine / hydrocodone / phenylephrine)
  • Histinex PV (chlorpheniramine / hydrocodone / pseudoephedrine)
  • Histussin D (hydrocodone / pseudoephedrine)
  • Histussin HC Liquid (chlorpheniramine / hydrocodone / phenylephrine)
  • Histussin HC Syrup (dexbrompheniramine / hydrocodone / phenylephrine)
  • homatropine / hydrocodone
  • Hy-KXP (hydrocodone / potassium guaiacolsulfonate)
  • Hy-Phen (acetaminophen / hydrocodone)
  • Hycet (acetaminophen / hydrocodone)
  • Hyco-DH (hydrocodone / phenylephrine / pyrilamine)
  • Hycoclar Tuss (guaifenesin / hydrocodone)
  • Hycoclear (guaifenesin / hydrocodone)
  • Hycodan (homatropine / hydrocodone)
  • Hycofenix (guaifenesin / hydrocodone / pseudoephedrine)
  • Hycomal DH (hydrocodone / phenylephrine / pyrilamine)
  • Hycomine (hydrocodone / phenylpropanolamine)
  • Hycomine Compound (acetaminophen / caffeine / chlorpheniramine / hydrocodone / phenylephrine)
  • Hycomine Pediatric (hydrocodone / phenylpropanolamine)
  • Hycophen (hydrocodone / phenylpropanolamine)
  • Hycophen Pediatric (hydrocodone / phenylpropanolamine)
  • Hycosin Expectorant (guaifenesin / hydrocodone)
  • Hycotuss Expectorant (guaifenesin / hydrocodone)
  • Hydex PD (dexchlorpheniramine / hydrocodone / phenylephrine)
  • Hydro GP (guaifenesin / hydrocodone / phenylephrine)
  • Hydro-DP (diphenhydramine / hydrocodone / phenylephrine)
  • Chlorphen HD (chlorpheniramine / hydrocodone / phenylephrine)
  • chlorpheniramine / guaifenesin / hydrocodone / pseudoephedrine
  • chlorpheniramine / hydrocodone
  • chlorpheniramine / hydrocodone / phenylephrine
  • chlorpheniramine / hydrocodone / pseudoephedrine
  • cilostazol
  • cisapride
  • Clinacort (triamcinolone)
  • Clinalog (triamcinolone)
  • Co-Gesic (acetaminophen / hydrocodone)
  • Co-Tuss V Expectorant (guaifenesin / hydrocodone)
  • Co-Tussin (guaifenesin / hydrocodone)
  • Coartem (artemether / lumefantrine)
  • cobimetinib
  • Codal-DH Syrup (hydrocodone / phenylephrine / pyrilamine)
  • Codamine (hydrocodone / phenylpropanolamine)
  • Codamine Pediatric (hydrocodone / phenylpropanolamine)
  • CodiCLEAR DH (guaifenesin / hydrocodone)
  • Codimal DH (dexchlorpheniramine / hydrocodone / phenylephrine)
  • Codituss DH (hydrocodone / phenylephrine / pyrilamine)
  • Codotuss (guaifenesin / hydrocodone)
  • colchicine
  • colchicine / probenecid
  • Colcrys (colchicine)
  • ColdCough HCM (hydrocodone / pseudoephedrine)
  • Combunox (ibuprofen / oxycodone)
  • Comtussin HC (chlorpheniramine / hydrocodone / phenylephrine)
  • Condasin (guaifenesin / hydrocodone)
  • conivaptan
  • copanlisib
  • Cordarone (amiodarone)
  • Norco (acetaminophen / hydrocodone)
  • Paracetamol (acetaminophen)
  • Singulair (montelukast)
  • Spiriva (tiotropium)
  • Symbicort (budesonide / formoterol)
  • Synthroid (levothyroxine)
  • Ventolin (albuterol)
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D3 (cholecalciferol)
  • Zyrtec (cetirizine)
  • Co-trimoxazole (sulfamethoxazole / trimethoprim)
  • CoQ10 (ubiquinone)
  • Cymbalta (duloxetine)
  • Fish Oil (omega-3 polyunsaturated fatty acids)
  • Nexium (esomeprazole)

In addition to these medications, patients are advised to inform their healthcare provider fi they are currently taking any medicines or substances which could potentially induce drowsiness. This includes sleeping pills, cough suppressants which contain codeine and hydrocodone, as well as recreational substances like marijuana or alcohol. Each of these substances could affect concentration levels, and patients are advised not to drive or otherwise carry out tasks which require complex movements or concentration (such as working at height on scaffolding) until a physician has ascertained that the patient is at little or no risk of experiencing interactions associated with these medicines.

Warnings:

Before taking any antifungal azoles, patients are advised to inform their doctors if they have any allergies – including those directly involving azoles and antifungal agents as well as general allergic reactions. Some antifungal azoles can contain inactive ingredients which have the propensity to cause reactions and other issues.

Azole creams should only be used to treat yeast infection, and should not be used at a later stage to treat another infection unless advised by a qualified healthcare professional. When undergoing treatment with antifungal azole creams, patients are advised to avoid wearing tight jeans, pantyhose, bathing suits or leisure wear for long periods after exercise. Cotton underwear is advised, and should be changed daily in order to prevent the return of infection.

Patients with a history of liver or kidney disease should make their healthcare provider aware of this before commencing treatment with antifungal azoles, as in some instances reports of decreased liver and kidney function have been associated with antifungal azole use, particularly in higher doses over prolonged periods.

Some antifungal azoles, such as fluconazole, can potentially cause a condition which affects the rhythm of the heart. This is known as QT prolongation. QT prolongation has the potential to cause serious, although rarely fatal, irregular fast heartbeats and symptoms such as severe dizziness and fainting which may require immediate medical attention. The risk of QT prolongation can potentially be increased in patients suffering from heart problems, or with a family history of heart problems.

Low levels of magnesium or potassium in the blood can also put patients at risk of QT prolongation This risk is increased if the patient is taking diuretic medication which reduces swelling and water levels in the body. Many diuretics are prescribed to treat edema associated with congenital heart problems, and patients should advise their doctor if suffering from one of these conditions.

After applying an azole antifungal cream to the vagina, great care should be taken by the patient to ensure that their hands are sufficiently washed. This is because yeast infections are highly contagious and could easily be spread to other parts of the body, or passed on to other people. Another reason for thoroughly washing the hands is because azole antifungal creams can be harmful if they get into the eyes. In the event of this medicine making contact with the eye, the patient is advised to wash the affected eye and surrounding area with large amounts of water until sufficiently rinsed. If eye irritation persists, the patient is advised to contact their doctor.

Antifungal azole creams can be dangerous if swallowed. If the patient or someone the patient knows accidentally swallows a reasonable amount of the cream, the potential for overdose arises. In this instance, the patient should contact their local poison control center or emergency services immediately.

Pregnant women are advised to use antifungal azoles only if clearly needed. This is because many antifungal azoles have the potential to harm unborn babies if applied in high doses during the first trimester of pregnancy. Pregnant women currently experiencing vaginal yeast infections are therefore advised to use other medications which can be applied in or around the vagina – the risks and benefits of which should be discussed with a doctor before committing to any treatment.

Some antifungal azoles are known to pass into breast milk. Studies have yet to be undertaken to ascertain the effects, although experts agree that these compounds are unlikely to harm a nursing infant.

Patients who have been using this medicine for more than seven days without any signs of improvement are advised to contact their doctor. In the event of infection returning within two months of treatment, patients are also advised to contact their doctor, who may suggest an alternative or additional medication in order to treat infection.

Storage:

Antifungal azoles should be stored in a cool and dry place. Unless specified on the label, antifungal medications should not be kept in the refrigerator and should instead be kept at room temperature. Patients should ensure that all medicines are stored out of the reach of children or pets, in order to prevent any accidental ingestion.

After a course of treatment, patients who have a supply of antifungal azole cream remaining should dispose of their unwanted medication safely and hygienically. Most pharmacies are able to provide information on the correct disposal of prescription medications, and some may even operate a take-back scheme where they will safely dispose, reuse or recycle any unwanted medicines.

Unused antifungal azole creams should never be poured down the sink, toilet or drain, as the medicine can inadvertently harm animals or make its way into the water supply as a result.

Summary:

Antifungal azoles are available as topical creams which can be used to treat a variety of symptoms, internally and externally, related to vaginal yeast infection. These medicines are cost-effective, and the development of antifungals with higher resistance and greater efficacy during the 1990's has meant that the widespread use of modern antifungal azoles is now commonplace throughout the United States, Asia and Europe.

These creams are marketed in the US under a variety of brand names, including Clotrimazole, and many are available over the counter in order to provide fast and effective relief of the symptoms of yeast infection. In some instances, topical creams are packaged together with an oral tablet which is used to treat internal infection. In order for this medicine to work most effectively, patients and doctors should work together in order to gain an understanding of the optimal dose and frequency.

Although there is a small potential for some patients with pre-existing conditions to experience unpleasant or potentially harmful side effects, antifungal azoles are generally regarded as safe for use and are an integral drug found in clinics and pharmacies across the developed world.

Antifungal azoles can also be used to treat symptoms associated with AIDS and HIV-related illnesses, although care should be taken with regard to dosage levels in such patients, in order to avoid potentially harmful side effects.

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Last Reviewed:
December 24, 2017
Last Updated:
April 04, 2018
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