Sertaconazole is a synthetic imidazole derivative, containing a benzothiophene ring, with antifungal, antibacterial, anti-inflammatory, and anti-pruritic activity. Besides its ability to inhibit the synthesis of ergosterol, the benzothiophene ring of sertaconazole is able to insert into the fungal cell wall instead of tryptophan. This increases the permeability of the cell wall. In addition, sertaconazole suppresses the release of cytokines.
Sertaconazole nitrate is an antifungal medication of the imidazole class. It is available in topical formulations for the treatment of skin infections such as athlete’s foot.
Sertaconazole Nitrate is the nitrate salt form of sertaconazole, a synthetic imidazole derivative with the antifungal property. Sertaconazole nitrate inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols and the inhibition of ergosterol synthesis, an essential component of the cell membrane of fungi. This leads to a disruption of cell membrane permeability and leakage of adenine triphosphate (ATP) and other constituents from fungal cells.
Mechanism of Action of Sertaconazole
Sertaconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Sertaconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.
Indications of Sertaconazole
- For the topical treatment of interdigital tinea pedis in immunocompetent patients 12 years of age and older, caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
- Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues.
- Interdigital Tinea Pedis
Contraindications Of Sertaconazole
- Have known hypersensitivity to other azole medicines such as sertaconazole ;
- Are taking terfenadine, if 400 mg per day multidose of sertaconazole is administered;
- Concomitant administration of sertaconazole and quinidine, especially when Sertaconazole is administered in high dosages;
- Take SSRIs such as fluoxetine or sertraline.
Dosage of Sertaconazole
Strengths: 2%
Tinea Pedis
- Apply topically twice a day for 4 weeks.
Pediatric Dose for Tinea Pedis
- 12 years or older: Apply topically twice a day for 4 weeks.
Side Effects of Sertaconazole
Most Common
- Blistering, burning, crusting, dryness or flaking of skin
- itching, redness, skin rash, swelling, or soreness at the application site
- darkening of skin
- dry skin
- flushing and redness of the skin
- scaling, severe redness, soreness or swelling of the skin
- peeling or loosening of the skin
- skin tenderness
- unusually warm skin
Common
- Abdominal or stomach pain
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- Nausea
- liver problems,
- stomach pain,
- vomiting,
- Dizziness
- Burning, itching, stinging, redness, or other sign of irritation at the application site, rash
- a headache,
- increased intracranial pressure,
- meningeal signs,
- reversible hair loss or thinning, and
- fever.
Common
- chills or fever
- a headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- liver problems–nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes)
- decreased amount of urine
Rare
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- burning,
- stinging,
- severe pain in your upper stomach spreading to your back, nausea and vomiting;
- signs of congestive heart failure–shortness of breath (even with mild exertion), cough with mucus, fast heartbeats, swelling, rapid weight gain, sleep problems; or.
Interactions Of Sertaconazole
Sertaconazole may interact with following drugs, supplyments & may change the efficacy of drugs
- medications that use the enzyme such as budesonide, cyclosporine, darifenacin, dihydroergotamine, fentanyl pimozide, quinidine, sirolimus, tacrolimus, terfenadine, fluticasone, eletriptan, lovastatin quetiapine, sildenafil, and simvastatin
- medications that block the enzyme CYP3A4 such as some macrolide antibiotics (clarithromycin, telithromycin), some HIV protease inhibitors (indinavir, nelfinavir, ritonavir, saquinavir), some HCV protease inhibitors (boceprevir, telaprevir), some azole antifungals (ketoconazole, itraconazole, posaconazole, voriconazole), conivaptan, delavirdine, and nefazodone
- medications that increase the activity of the enzyme CYP3A4 such as carbamazepine , phenobarbital, phenytoin , rifampin and nimodipine
- methylprednisolone
- midazolam
- triazolam
- digoxin
- warfarin
- phenytoin
- rifampin
- alcohol
Pregnancy & Lactation of Sertaconazole
FDA Pregnancy Category C
Pregnancy
Sertaconazole falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. There are no well-controlled studies that have been done in humans with Sertaconazole, though. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.
Lactation
It is not known if into human milk. Because many medications can cross into human milk and because of the possibility of serious adverse reactions in nursing infants with the use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using ketoconazole.
References
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