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Antifungals

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ppt on fungal infections and treatment

ppt on fungal infections and treatment


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  • 1. ANTIFUNGAL AGENTS Introduction• Fungi are eukaryotic, heterotrophic organisms that live as saprobes or parasites.• Complex organisms in comparison to bacteria .• Have nucleus and well defined nuclear membrane, and chromosomes.• Have rigid cell wall composed of chitin (bacterial cell wall is composed of peptidoglycan)• Fungal cell membrane contains ergosterol , human cell mebmrane is composed of cholesterol• Antibacterial agents are not effective against fungi.• Fungal infections are also called as mycoses Dr Mrs Borkar 1
  • 2. ANTIFUNGAL AGENTS Introduction• Systemic fungal infections are a major cause of death in patients whose immune system is compromised – cancer or its chemotherapy, – organ transplantation – HIV-1 infection.• Superficial infections of the skin and other soft tissue structures.• Antifungal agents target – distinctive components of the fungal cell membrane – others alter cell wall synthesis – nucleic acid synthesis Dr Mrs Borkar 2
  • 3. ANTIFUNGAL AGENTS Types of Fungal Infections• Superficial : Affect skin – mucous membrane – Tinea versicolor – Dermatophytes : affect keratin layer of skin, hair, nail. e.g.tinea pedis, ring worm infection – Candidiasis : Yeast-like, oral thrush, vulvo-vaginitis , nail infections.• Deep Infections : – Affect internal organs as : lung ,heart , brain leading to pneumonia , endocarditis , meningitis. Dr Mrs Borkar 3
  • 4. ANTIFUNGAL AGENTS Mechanism of action of Antifungal agents• Disrupt fungal cell membrane – Polyenes – amphotericin, Nystatin – Azoles • Imidazole – Ketoconazole, Miconazole, Clotrimazole • Triazole – Fluconazole, Itraconazole – Allylamines - Terbinafin – Echinocandins - Capsofungin• Inhibit mitosis - Gresiofulvin• Inhibit DNA synthesis - Flucytosine• Miscellaneous – Tolnaftate – Cyclopirox Dr Mrs Borkar 4
  • 5. Cell Wall SynthesisMembrane function Capsofungin Amphotericin BNucleic acid synthesis Flucytosine Ergosterol synthesis Azoles Lanosterol synthesis Terbinafine Dr Mrs Borkar 5
  • 6. ANTIFUNGAL AGENTS Amphotericin B• Antifungal agent with the broadest spectrum of activity• Produced by Streptomyces nodosus.• Natural, Amphoteric polyene macrolide – – Amphoteric = can react as an acid as well as a base – polyene = many double bonds – macrolide = containing a large lactone ring• Heptaene macrolide - large lactone ring with multiple ketone and hydroxyl group)• Drug of choice for the vast majority of life-threatening systemic fungal infections• Interacts with ergosterols, forms pores that increase membrane permeability and allow leakage of intracellular ions & macromolecules from fungal cell ( cell death ). Dr Mrs Borkar 6
  • 7. ANTIFUNGAL AGENTS Amphotericin B• Broad range of pathogenic fungi• Protozoa, Leishmania braziliensis and Naegleria fowleri• No antibacterial activity• Amphotericin A & B are antifungal antibiotics.• Amphotericin A is not used clinically. Dr Mrs Borkar 7
  • 8. Mechanism of action of AmphotericinDr Mrs Borkar 8
  • 9. ANTIFUNGAL AGENTS Amphotericin - ADME• Poorly absorbed orally, useful for fungal infection of gastrointestinal tract.• For systemic infections given as slow I/V infusion.• Locally used in corneal ulcers, arthritis and candidial bladder irrigation• Highly protein bound - > 90%• Penetration through BBB is poor but increases in inflamed meninges.• Excreted slowly via kidneys, traces found in urine for months after cessation of drugs.• Half life 15 days Dr Mrs Borkar 9
  • 10. Amphotericin ADMEDr Mrs Borkar 10
  • 11. ANTIFUNGAL AGENTS Routes of Administration1. Slow IV infusion for systemic fungal disease.2. Intrathecal for fungal CNS infections.3. Topical drops & direct subconjunctival injection for Mycotic corneal ulcers & keratitis.4. Local injection into the joints in fungal arthritis.5. Bladder irrigation in Candiduria. Dr Mrs Borkar 11
  • 12. ANTIFUNGAL AGENTS Amphotericin – Liposomal Preparations• Packaged in a lipid- associated delivery system which acts as a reservoir• Large doses can be administered – 5 times• Reduces binding to human cell membrane• Clinically have more efficacy , less nephrotoxicity• More expensive Dr Mrs Borkar 12
  • 13. Liposomal preparations of Amphotericin Dr Mrs Borkar 13
  • 14. ANTIFUNGAL AGENTSAmphotericin B - Therapeutic Uses and Dosage• Usual dose is 0.5–0.6 mg/kg, administered in 5% glucose over 4 hours• Candida esophagitis, Rapidly progressive mucormycosis or invasive aspergillosis .• Coccidioides meningitis: Intrathecal infusion ; started with twice weekly schedule , increased to thrice weekly and continued on twice- weekly schedule.• Treatment of cryptococcal meningitis, Severe or rapidly progressing histoplasmosis, blastomycosis, coccidioidomycosis, penicilliosis marneffei, invasive aspergillosis, extracutaneous sporotrichosis, fusariosis, alternariosis, and trichosporonosis.• Given once weekly to prevent relapse in patients with AIDS who have been treated successfully for cryptococcosis or histoplasmosis. Dr Mrs Borkar 14
  • 15. ANTIFUNGAL AGENTS Amphotericin B - Adverse effects• Major acute reaction to intravenous is fever and chills, which typically end spontaneously in ~30 minutes and often abate with subsequent infusions.• Tachypnea and modest hypotension may occur, but true bronchospasm or anaphylaxis is rare.• Hypotension and hypoxia in preexisting cardiac or lung disease• Prophylactic use of IV glucocorticoids decreases reaction• Transient azotemia occurs in 80% of patients• Kidney function may be affected if other nephrotoxic agents like aminoglycoside are used concurrently.• Administration of 1 L of NS IV prior to amphotericin B administration is recommended for adults who can tolerate the Na+ load.• Azotemia occurs less frequentlyMrs Borkar lipid preparations of Dr with 15 amphotericin, and saline loading is not needed.
  • 16. ANTIFUNGAL AGENTS Amphotericin B - Adverse effects• Hypochromic, normocytic anemia is usual and reverses slowly following cessation of therapy.• It is due decreased production of erythropoietin and often responds to erythropoietin.• Headache, nausea, vomiting, malaise, weight loss, and phlebitis at peripheral infusion sites are common.• Arachnoiditis, manifested by fever and headache, can occur with intrathecal injection; it may be decreased by intrathecal administration of 10–15 mg of hydrocortisone.• Local injections of amphotericin B into a joint or peritoneal dialysate fluid commonly produce irritation and pain. 16 Dr Mrs Borkar
  • 17. ANTIFUNGAL AGENTS Amphotericin B - Adverse effectsImmediate reactions ( Infusion –related toxicity ).• Fever, muscle spasm, vomiting ,headache, hypotension.• Can be avoided by : – Slowing the infusion – Decreasing the daily dose – Premedication with antipyretics, antihistamincs or corticosteroids. – test dose.Slower Reactions:• Most serious is renal toxicity (nearly in all patients ).• Hypokalemia• Hypomagnesaemia• Impaired liver functions• Anemia, Thrombocytopenia Dr Mrs Borkar 17
  • 18. Dr Mrs Borkar 18
  • 19. ANTIFUNGAL AGENTS Flucytosine• Synthetic, water soluble, fluorinated pyrimidine analog• Often used in combination with amphotericin B and Itraconazole• Spectrum of antigungal activity is considerably less than that of amphotericin B.• Amphotericin B increases cell permeability , allowing more 5-FC to penetrate the cell, they are synergistic• Fungistatic• Has useful activity against Candida and Cryptococcus.• Acts by inhibiting synthesis of fungal DNA Dr Mrs Borkar 19
  • 20. ANTIFUNGAL AGENTS Flucytosine - ADME• Absorbed rapidly and well from the GI tract, widely distributed• Minimally bound to plasma proteins.• Penetrates well into CSF.• Mainly excreted unchanged through kidney• Half life drug normally is 3–6 hours but may reach 200 hours in renal failure.• Dose modification is necessary in renal dysfunction plasma concentrations should be measured periodically• Flucytosine is cleared by hemodialysis and peritoneal dialysis Dr Mrs Borkar 20
  • 21. ANTIFUNGAL AGENTS Flucytosine – Uses• Given orally at 100 mg/kg/day, in 4 divided doses and is used predominantly in combination with amphotericin B.• Severe deep fungal infections as in meningitis• Cryptococcal meningitis: begin with amphotericin B plus flucytosine and change to fluconazole after the patient has improved.• There is the risk of amphotericin induecd azotemia and flucytocine dose has to be reduced in this situation otherwise the combination will cause bone marrow suppression or colitis Dr Mrs Borkar 21
  • 22. ANTIFUNGAL AGENTS Flucytosine – Adverse effects• Hematologic : Leukopenia, thrombocytopenia, bone marrow depression• Allergic: Rash, nausea, vomiting, diarrhea, and enterocolitis• Hepatic: Elevation in hepatic transaminases but this reverses when therapy is stopped.• Toxicity is more frequent in patients with AIDS or azotemia.• Alopecia Dr Mrs Borkar 22
  • 23. ANTIFUNGAL AGENTS Nystatin/Nysfungin• Bacterial origin.• Isolated from Streptomyces noursei in 1950 by Elizabeth Lee Hazen and Rachel Fuller Brown,.• Polyene macrolide ,similar in structure & mechanism to amphotericin B.• Too toxic for systemic use.• Used only topically - available as creams, ointment , suppositories & other preparations. Dr Mrs Borkar 23
  • 24. ANTIFUNGAL AGENTS Nystatin/Nysfungin – Clinical uses• Prevent or treat superficial candidiasis of mouth, esophagus, intestinal tract.• Oral suspension of 100,000 U/ml 4 times a day and tablets 500,000 U are used to decrease GIT colonization with Candida• Vaginal candidiasis - pessaries used for 2 weeks• Can be used in combination with antibacterial agents & corticosteroids• In Cutaneous infection available in cream, ointment or powder form and applied 2-3 times a day Dr Mrs Borkar 24
  • 25. ANTIFUNGAL AGENTS Azole Antifungals• Bivalent chemical group composed of five-membered organic rings• Broad spectrum of activity - Antibacterial, antiprotozoal, anthelminthic and antifungal.• Group of synthetic fungistatic agents• Classification: according to the number of nitrogen atoms attached to the ring – Imidazoles (2 nitrogen atoms): Ketoconazole, Miconazole, Econazole, Clotrimazole, Bifonazole – Triazoles (3 nitrogen atoms): Itraconazole, Fluconazol, Vorionazole → systemic treatment Dr Mrs Borkar 25
  • 26. ANTIFUNGAL AGENTS Azole - antifungal activity• Cryptococci, Blastomyces, Histoplasma capsulatum, Coccidioides , Paracoccidioides brasiliensis, and dermatophytes.• Aspergillus spp., Scedosporium, apiospermum (Pseudallescheria boydii), Fusarium, and Sporothrix schenckii are intermediate in susceptibility.• C. krusei and the agents of mucormycosis are resistant. Dr Mrs Borkar 26
  • 27. ANTIFUNGAL AGENTSAzole Antifungals- Mechanism of Action • Inhibit the fungal cytochrome P450 enzyme • Responsible for converting lanosterol to ergosterol ( the main sterol in fungal cell membrane ). Dr Mrs Borkar 27
  • 28. ANTIFUNGAL AGENTS Azole Antifungals- Imidazoles• Contain 2 Nitrogen atoms attached to the ring• Reduce the formation of ergosterol in the cell membrae which become permeable to cellular constituents.• They lack selectivity, and also inhibits human gonadal and steroid synthesis leading to decreased testosterone and cortisol production• Ketoconazole,• miconazole,• clotrimazole,• isoconazole ,• Tioconazole Dr Mrs Borkar 28
  • 29. Mechanism of action KetoconazoleDr Mrs Borkar 29
  • 30. ANTIFUNGAL AGENTS Imidazole – Ketoconazole- ADME• Well absorbed orally as acidic environment favors its dissolution.• Bioavailability is impaired with food.• Cola drinks improve its absorption in patients with achlorhydria.• Metabolized extensively in liver and inactive products appear in the feces.• Moderate hepatic dysfunction has no effect on drug concentration.• 84 % is bound to plasma proteins.• Half life increases with dose• It does not enter CSF. Dr Mrs Borkar 30
  • 31. ANTIFUNGAL AGENTSImidazole – Ketoconazole – Adverse Effects• Inhibits adrenal and gonadal steroids which leads to menstrual irregularities, loss of libido, impotency and gynaecomastia in males.• Efficacy is poor in immunosuppressed patients and in meningitis.• Hepatotoxic - rare but may prove fatal.• Dose dependant nausea, anorexia ,vomiting• Hair loss• Fluid retention and hypertension.• Not used in Pregnancy, lactation ,hepatic dysfunction Dr Mrs Borkar 31
  • 32. Decrease in the ergosterol in the fungal membrane By ketoconazle reduces the fungicidal action of amphotericinDr Mrs Borkar 32
  • 33. ANTIFUNGAL AGENTS Imidazole – Ketoconazole – Clinical usesUsed topically or systematic (oral route only ) to treat1. Oral & vaginal candidiasis.2. Dermatophytosis.3. Systemic mycoses & mucocutaneous candidiasis. Dr Mrs Borkar 33
  • 34. Ketoconazole is not useful for fungal infections of UT as level of parent drug in urine is very lowDr Mrs Borkar 34
  • 35. ANTIFUNGAL AGENTS Imidazole – Clotrimazole• Bioavailability is low by taking orally.• Used topically.• Absorption less than 0.5 % from intact skin, 3-10 % from vagina• Activity in vagina remains for 3 days.• Stigma, erythema, edema, vesication, pruritus, urticaria mild vaginal burning sensation may occour.• Cure dermatophytes, cutaneous candidiasis and vulvovaginal candidiasis Dr Mrs Borkar 35
  • 36. ANTIFUNGAL AGENTS Azole Antifungals- Triazoles• Damage the fungal cell membrane by inhibiting enzyme desmethylase• They are selective• Penetrate to CNS• Resistant to degradation• Cause less endocrine disturbance.• Fluconazole,• itraconazole,• voriconazole Dr Mrs Borkar 36
  • 37. ANTIFUNGAL AGENTS Azole antifungals – Itraconazole• It is a synthetic triazole, new drug• Lacks endocrine side effects of ketoconazole.• Broad spectrum activity• Administered orally as well as I/V.• Food increases its absorption• Metabolized in liver to active metabolite• Highly lipid soluble ,well distributed to bone, sputum, adipose tissues.• Can not cross BBB Dr Mrs Borkar 37
  • 38. ANTIFUNGAL AGENTS Itraconazole- ADME• Food increases its absorption• Metabolized in liver extensively• It is highly lipid soluble and well distributed to bone, sputum and adipose tissue.• Highly bound to plasma protein• Half life is 30-40 hours• Does not penetrate CSF adequately• The capsule is better absorbed with food, but the oral solution is better absorbed in the fasting state Dr Mrs Borkar 38
  • 39. ANTIFUNGAL AGENTSAzole antifungals – Itraconazole - Therapeutic Uses• Available as a capsule and solutions for oral or intravenous administration• Oral solution is 60% more bioavailable than the capsules• IV only in serious infections.• Dose – Cap 200 to 400 mg/day • doses exceeding 200 mg/day are given in 2 divided doses • Loading dose: 200 mg 3 times daily can be given for the first 3 days• The only agent with significant activity against aspergillus species• It can safely be administered prophylactically in patients receiving bone marrow transplants Dr Mrs Borkar 39
  • 40. ANTIFUNGAL AGENTSAzole antifungals – Itraconazole - Therapeutic Uses• Dermatophytoses and onychomycosis.• Onychomycosis - 200 mg daily after food for 3 months• For deep mycoses, loading dose of 200 mg three times daily for 3 days. Thereafter, two 100-mg capsules are given twice daily with food.• Histoplasmosis : AIDS-associated histoplasmosis maintainance therapy - 200 mg once daily• It easily penetrate CSF and is a drug of choice in cryptococcal meningitis and coccido mycosis• Cryptococcosis: 400 mg daily for 8 weeks in meningitis, In AIDS 200 mg for life. Dr Mrs Borkar 40
  • 41. ANTIFUNGAL AGENTSAzole antifungals – Itraconazole - Therapeutic Uses • Itraconazole solution - for oropharyngeal and esophageal candidiasis. • Taken fasting in a dose of 100 mg once daily and swished vigorously in the mouth before swallowing to optimize topical effect. • 100 mg of the solution twice a day for 2–4 weeks. • Candidiasis: 200 mg on 1st day then 100 mg daily for 2 weeks. • Not effective in aspergillosis. • Used orally in dermatophytosis & vulvo-vaginal candidiasis. Dr Mrs Borkar 41
  • 42. ANTIFUNGAL AGENTS Itraconazole – Adverse Effects• Interact with many drugs• Interactions can cause serious toxicity• Fatal cardiac arrhythmias.• Congestive heart failure in patients with impaired ventricular function.• Hepatic failure and death. If symptoms of hepatotoxicity occur, the drug should be discontinued and liver function assessed.• Anaphylaxis and severe rash have rarely occurred. Dr Mrs Borkar 42
  • 43. ANTIFUNGAL AGENTS Itraconazole – Adverse Effects• Relative to capsules, the oral solution of itraconazole more frequently causes diarrhea, abdominal cramps, anorexia, and nausea.• Intravenous itraconazole has all the adverse effects of capsules but generally is well tolerated.• Chemical phlebitis: dedicated catheter port is required,• Infusion durations >1 hour are recommended.• Intravenous formulation is contraindicated in patients with a creatinine clearance <30 mL/min. Dr Mrs Borkar 43
  • 44. ANTIFUNGAL AGENTS Itraconazole – Adverse Effects• The adverse effects are related to dose and duration of use• In the absence of interacting drugs, itraconazole capsules are well tolerated at 200 mg daily.• GI distress occurs with use of 300 mg/day or more• In patients receiving 50–400 mg/day, nausea and vomiting, hypertriglyceridemia, hypokalemia, elevated serum aminotransferases, and rash occurred in few patients• Doses of 300 mg twice daily have led to adrenal insufficiency, lower limb edema, hypertension, and rhabdomyolysis• Doses above 400 mg/day are not recommended for long- term use Dr Mrs Borkar 44
  • 45. ANTIFUNGAL AGENTS Fluconazole - ADME• It is fluorinated bistriazole.• The widest therapeutic index of the azoles.• Excellent bioavailability by oral route.• Bioavailability not altered by food or gastric acidity• Not hepatotoxic• It can safely be administered prophylactically in patients receiving bone marrow transplants.• Maximum excretion by kidney• Half life is 25-30 hours. Dr Mrs Borkar 46
  • 46. ANTIFUNGAL AGENTS Fluconazole - ADME• Fluconazole is almost completely absorbed from the GI tract irrespective of food or gastric acidity.• Concentration in plasma is same by oral or I/v route.• Only 10% of drug in circulation is protein bound.• Readily diffuses into body fluids, including breast milk, sputum, saliva, and CSF. Dr Mrs Borkar 47
  • 47. ANTIFUNGAL AGENTS Fluconazole - Dosage• Tablets for oral administration• Powder for oral suspension• Intravenous solutions containing 2 mg/mL.• Dosage is 50–800 mg once daily for oral or intravenous administration.• Children are treated with 3–6 mg/kg once daily Dr Mrs Borkar 48
  • 48. ANTIFUNGAL AGENTS Fluconazole - Uses• Candidiasis - 200 mg on the first day and then 100 mg daily for at least 2 weeks, in oropharyngeal candidiasis.• single dose of 150 mg is effective in uncomplicated vaginal candidiasis.• 400 mg daily in deep candidiasis in allogeneic bone marrow transplant recipients• Systemic fungal infections – 400-800 mg q24h – > 800 mg q24h in unstable patient• Maintenance for cryptococcal meningitis - 400 mg/day, for the initial 8 weeks in the treatment in AIDS after the Dr Mrs Borkar 49 patient has been stabilized with intravenous amphotericin
  • 49. ANTIFUNGAL AGENTS Fluconazole – Adverse effects• Nausea and vomiting at doses >200 mg/day• Headache, skin rash, abdominal pain, and diarrhea• Reversible alopecia may occur with prolonged therapy• Rare deaths due to hepatic failure or Stevens- Johnson syndrome have occurred.• Highly teratogenic: Associated with skeletal and cardiac deformities in infants born to women taking high doses during pregnancy and should be avoided during pregnancy Dr Mrs Borkar 50
  • 50. ANTIFUNGAL AGENTS Griseofulvin• Fungistatic in vitro for various species of dermatophytes.• Inhibits fungal mitosis Dr Mrs Borkar 51
  • 51. ANTIFUNGAL AGENTS Griseofulvin - ADME• Entirely local action, no systemic absorption• Micronized and ultramicronized powders are used to facilitate dissolution• Half life in plasma of ~1 day.• Deposited in keratin precursor cells and persists in keratin to provide prolonged resistance to fungi.• The new growth of hair or nails is the first to become free of disease.• As the fungus-containing keratin is shed, it is replaced by normal tissue.• Griseofulvin is detectable in the stratum corneum within 4– Dr Mrs Borkar 52 8 hours of oral administration.
  • 52. ANTIFUNGAL AGENTS Griseofulvin - Uses• Mycotic infections of the hair (tinea capitis)• Tinea of the hands and beard• “Athlete’s foot” or epidermophytosis involving the skin and nails• Not effective in treatment of subcutaneous or deep mycoses Dr Mrs Borkar 53
  • 53. ANTIFUNGAL AGENTS Griseofulvin - Dosage• 5–15 mg/kg for children• 0.5–1 g for adults in 4 divided doses• Severe infections: 1.5–2 g daily for short periods• Best results are obtained• Treatment must be continued until infected tissue is replaced by normal hair, skin, or nails, which requires 1 month for scalp and hair ringworm, 6–9 months for fingernails, and at least a year for toenails. Dr Mrs Borkar 54
  • 54. ANTIFUNGAL AGENTS Griseofulvin – adverse effects• Headache, GI symptoms (e.g., nausea, vomiting, diarrhea, heartburn, flatulence), and rash.• More serious reactions include hepatotoxicity, serum sickness reaction, angioedema, and hematologic effects (e.g., leukopenia, neutropenia, punctate basophilia, and monocytosis).• Blood should be checked weekly during treatment.• Estrogen-like effects have been observed in children. Dr Mrs Borkar 55
  • 55. ANTIFUNGAL AGENTS Topical Antifungal Agents• Topical treatment is useful in superficial fungal infections confined to the stratum corneum, squamous mucosa, or cornea, including dermatophytosis (ringworm), candidiasis, tinea versicolor, piedra, tinea nigra, and fungal keratitis.• Unsuccessful for mycoses of the nails (onychomycosis) and hair (tinea capitis)• No place in subcutaneous mycoses, such as sporotrichosis and chromoblastomycosis.• Efficacy of topical agents depends not only on the type of lesion and the mechanism of drug action, but also on the viscosity, hydrophobicity, and acidity of the formulation. Dr Mrs Borkar 56
  • 56. ANTIFUNGAL AGENTS Topical Antifungal Agents• Regardless of formulation, penetration of topical drugs into hyperkeratotic lesions often is poor.• Removal of thick, infected keratin may be a useful adjunct to therapy.• Preferred formulations are – Creams – Solutions – Powders, whether applied by shake containers or aerosols, largely are used for the feet and moist lesions of the groin and other intertriginous areas Dr Mrs Borkar 57
  • 57. ANTIFUNGAL AGENTS Topical Antifungal Agents1. Topical azole derivatives2. Nystatin& Amphotericin3. Terbinafine4. Tolnaftate5. Naftifine6. Griseofulvin Dr Mrs Borkar 58
  • 58. ANTIFUNGAL AGENTS Topical Antifungal Agents• Used in superficial fungal infections: – Dermatophytosis ( ring worm) – Candidiasis – Fungal keratitis.• Not effective in mycoses of the nails & hair or subcutaneous mycoses.• Preferred formulation for cutaneous application is cream or solution. Dr Mrs Borkar 59
  • 59. ANTIFUNGAL AGENTS Topical Antifungal Agents - Azoles• Indications for topical use include – tinea corporis – tinea pedis – tinea cruris – tinea versicolor – cutaneous candidiasis.• Agents for topical use should be selected based on cost and availability.• They are applied twice daily for 3–6 weeks.• Preparations for cutaneous use are effective for Dr Mrs Borkar 60
  • 60. ANTIFUNGAL AGENTSTopical Antifungal Agents – Vaginal Applications • Creams, suppositories, and tablets for vaginal candidiasis • 5 gm, Used once daily for 1–7 days, preferably at bedtime to facilitate retention. • Three vaginal formulations— – clotrimazole tablets, – miconazole suppositories, – Terconazole cream • Come in both low- and high-dose preparations. • Shorter duration of therapy is recommended for the higher doses. • The action is local and only little is absorbed • Most common side effect is vaginal burning or itching. • A male sexual partner mayMrs Borkar Dr experience mild penile irritation.61

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