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Oxistat

Generic Name: Oxiconazole Nitrate
Class: Azoles
ATC Class: G01AF17
VA Class: DE102
Chemical Name: 1-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-yl)ethanone (Z)-O-[(2,4-Dichlorophenyl)methyl]oxime mononitrate
Molecular Formula: C18H13C14N3O•HNO3
CAS Number: 64211-46-7

Introduction

Antifungal; azole (imidazole derivative).1 2 3 7 8 9 11 12 14 20 27 34 43

Uses for Oxistat

Dermatophytoses

Treatment of tinea corporis (body ringworm)1 20 24 25 28 and tinea cruris (jock itch)1 20 24 25 caused by Epidermophyton floccosum,1 20 25 27 28 Microsporum canis,20 25 27 28 M. gypseum,25 Trichophyton mentagrophytes,1 20 25 27 28 T. rubrum,1 20 25 27 28 or T. verrucosum.20 28

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Treatment of tinea pedis1 20 24 25 or tinea manuum24 25 caused by E. floccosum,20 25 27 28 M. canis,20 25 27 28 M. gypseum,25 T. mentagrophytes,1 20 25 27 28 T. rubrum,1 20 25 27 28 or T. verrucosum.20 28

Topical antifungals usually effective for treatment of uncomplicated tinea corporis or tinea cruris.35 36 39 40 41 An oral antifungal may be necessary when tinea corporis or tinea cruris is extensive, dermatophyte folliculitis is present, infection is chronic or does not respond to topical therapy, or patient is immunocompromised because of coexisting disease or concomitant therapy.35 36 39 40 41

Topical antifungals usually effective for treatment of uncomplicated tinea pedis or tinea manuum.36 39 41 An oral antifungal may be necessary for treatment of hyperkeratotic areas on the palms and soles, for chronic moccasin-type (dry-type) tinea pedis, and for tinea unguium (fingernail or toenail dermatophyte infections, onychomycosis).36 41

Pityriasis (Tinea) Versicolor

Treatment of pityriasis (tinea) versicolor caused by Malassezia furfur (Pityrosporum orbiculare or P. ovale).1

Topical antifungals usually effective; an oral antifungal (with or without a topical antifungal) may be necessary in patients who have extensive or severe infections or failed to respond to or have frequent relapses with topical therapy.37 38 40

Cutaneous Candidiasis

Treatment of cutaneous candidiasis caused by Candida albicans or C. tropicalis.27 28

Oxistat Dosage and Administration

Administration

Topical Administration

Apply topically to the skin as a 1% cream or lotion.1

Do not apply to the eye1 or administer intravaginally.1 32 33

Avoid contact with the nose, mouth, and other mucous membranes.1

Do not use with occlusive dressings or wrappings, unless otherwise directed by clinician.1

Shake lotion well before using.1

Apply a sufficient amount of cream or lotion; rub gently into affected area and immediately surrounding healthy skin.1

Dosage

Available as oxiconazole nitrate; dosage expressed in terms of oxiconazole.1

Pediatric Patients

Dermatophytoses
Tinea Corporis or Tinea Cruris
Topical

Apply 1% cream once or twice daily for 2 weeks.1

If clinical improvement does not occur after treatment, reevaluate diagnosis.1

Tinea Pedis
Topical

Apply 1% cream once or twice daily for 1 month.1

If clinical improvement does not occur after treatment, reevaluate diagnosis.1

Pityriasis (Tinea) Versicolor
Topical

Apply 1% cream once daily for 2 weeks.1

If clinical improvement does not occur after treatment, reevaluate diagnosis.1

Normalization of hyper- or hypopigmented patches on trunk, neck, arms, and upper thighs is variable and may take months.1

Adults

Dermatophytoses
Tinea Corporis or Tinea Cruris
Topical

Apply 1% cream or lotion once or twice daily for 2 weeks.1

If clinical improvement does not occur after treatment, reevaluate diagnosis.1

Tinea Pedis
Topical

Apply 1% cream or lotion once or twice daily for 1 month.1

If clinical improvement does not occur after treatment, reevaluate diagnosis.1

Pityriasis (Tinea) Versicolor
Topical

Apply 1% cream once daily for 2 weeks.1

If clinical improvement does not occur after treatment, reevaluate diagnosis.1

Normalization of hyper- or hypopigmented patches on trunk, neck, arms, and upper thighs is variable and may take months.1

Special Populations

No special population dosage recommendations at this time.1

Cautions for Oxistat

Contraindications

Known hypersensitivity to oxiconazole or any ingredient in the formulation.1

Warnings/Precautions

Warnings

Application Precautions

For external use only.1 Use only for topical application to the skin; not for ophthalmic1 or intravaginal use.1 32 33

Sensitivity Reactions

Hypersensitivity Reactions

Contact dermatitis reported following topical application of oxiconazole or other imidazole-derivative azole antifungals.1 21 22 47

If irritation or sensitivity occurs, discontinue the drug and initiate appropriate therapy.1

Possible cross-sensitization among the imidazoles.21 22 44 45 46 47 48

Specific Populations

Pregnancy

Category B.1

Lactation

Distributed into milk; caution if used in nursing women.1 32

Pediatric Use

Cream may be used in pediatric patients; has been used in children ≤10 years of age without unusual adverse effect.1

Safety and efficacy of lotion not established in children.1

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether safety and efficacy differ from that in younger adults.1

Available data to date indicate no difference in safety compared with younger adults; dosage adjustment not recommended.1

Common Adverse Effects

Pruritus, burning, irritation, stinging.1

Interactions for Oxistat

No formal drug interaction studies to date.1

Oxistat Pharmacokinetics

Absorption

Bioavailability

Only low concentrations absorbed systemically following topical application to skin.1

Distribution

Extent

Topical application to skin results in highest concentrations in epidermis and lower concentrations in upper and deeper corneum.1 In vitro on animal skin, oxiconazole 1% cream was retained in the horny layer of the epidermis for up to 96 hours after topical application.10 20

Distributed into milk.1 32

Not known whether systemically absorbed oxiconazole crosses the placenta.32 33

Elimination

Elimination Route

Systemically absorbed drug excreted in urine (<0.3% of topical dose).1

Stability

Storage

Topical

Cream and Lotion

15–30C;1 cream is stable for 24 months after the date of manufacture.32

Actions and Spectrum

  • Imidazole-derivative azole antifungal.1 2 3 7 8 9 11 12 14 20 27 34 43

  • Usually fungistatic;3 7 8 34 may be fungicidal at high concentrations or against very susceptible organisms.3 7 34

  • Presumably exerts its antifungal activity by altering cellular membranes, resulting in increased membrane permeability, secondary metabolic effects, and growth inhibition.3 4 5 9 Fungistatic activity may result from interference with ergosterol synthesis.1 4 5 9 34

  • Spectrum of antifungal activity includes many fungi, including yeasts and dermatophytes.1 2 3 7 11 12 14 20 34 Also has in vitro activity against some gram-positive bacteria.3 20

  • Dermatophytes: Active in vitro against Epidermophyton floccosum,1 3 7 Microsporum audouinii,1 7 M. canis,1 2 3 7 M. gypseum,1 3 7 Trichophyton mentagrophytes,1 2 3 6 7 16 T. rubrum,1 2 3 7 T. tonsurans,1 7 and T. violaceum.1

  • Candida: Active in vitro against Candida albicans,1 2 3 11 12 16 C. glabrata (Torulopsis glabrata),2 3 11 C. guilliermondii,3 C. krusei,2 3 C. parapsilosis,2 3 11 and C. tropicalis.2 3

  • Other fungi: Active in vitro against Malassezia furfur (Pityrosporum orbiculare).1 7 Also active in vitro against Aspergillus flavus,2 3 11 A. fumigatus,2 3 11 A. nidulans,3 A. niger,3 Cryptococcus neoformans,3 11 Epidermophyton floccosum,1 3 7 Exophiala werneckii,7 Petriellidium boydii,11 and Sporothrix schenkii.11

  • Bacteria: Active in vitro against Actinomadura madurae,3 Corynebacterium minutissimum,20 Nocardia asteroides,3 N. brasiliensis,3 and Streptomyces somaliensis.3

  • Cross-resistance can occur among the azole antifungals.7 32 Some C. albicans resistant to ketoconazole show cross-resistance to oxiconazole and other imidazole-derivative antifungals as well as to triazole derivatives.32

  • Some strains of M. furfur (Pityrosporum orbiculare) resistant to oxiconazole in vitro are cross-resistant to econazole.7

Advice to Patients

  • Importance of completing full course of treatment, even if symptoms improve.1

  • Importance of contacting clinician if skin condition worsens during therapy or if improvement does not occur after completing full course of therapy.1

  • Importance of applying to affected areas as directed and avoiding contact with eyes, nose, mouth, or mucous membranes.1

  • Importance of not using occlusive dressings, unless otherwise directed by clinician.1

  • Importance of washing hands after applying oxiconazole.1

  • Importance of discontinuing use and contacting clinician if treated area becomes irritated (e.g., itching, burning, blistering, swelling, oozing).1 32 33

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Oxiconazole Nitrate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Cream

1% (of oxiconazole)

Oxistat (with benzoic acid and propylene glycol)

GlaxoSmithKline

Lotion

1% (of oxiconazole)

Oxistat (with benzoic acid and propylene glycol)

GlaxoSmithKline

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2013. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Oxistat 1% Cream (PHARMADERM): 30/$108.63 or 90/$316.29

Oxistat 1% Cream (PHARMADERM): 60/$202.98 or 180/$599.99

Oxistat 1% Lotion (PHARMADERM): 30/$116.13 or 90/$343.08

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2013, Selected Revisions July 1, 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. GlaxoSmithKline Consumer Healthcare LP. Oxistat (oxiconazole nitrate) cream and lotion 1% prescribing information. Pittsburgh, PA; 2002 Aug.

2. Odds FC, Webster CE, Abbott AB. Antifungal relative inhibition factors: BAY I-9139, bifonazole, butoconazole, isoconazole, itraconazole (R 51211), oxiconazole, Ro 14- 4767/002, sulconazole, terconazole and vibunazole (BAY n-7133) compared in vitro with nine established antifungal agents. J Antimicrob Chemother. 1984; 14:105-14. [PubMed 6094418]

3. Polak A. Oxiconazole, a new imidazole derivative: evaluation of antifungal activity in vitro and in vivo. Arzneimittelforschung. 1982; 32:17-24. [PubMed 7037014]

4. Odds FC, Cheesman SL, Abbott AB. Suppression of ATP in Candida albicans by imidazole and derivative antifungal agents. Sabouraudia. 1985; 23:415-24. [PubMed 3913012]

5. Polak-Wyss A, Lengsfeld H, Oesterhelt G. Effect of oxiconazole and Ro 14-4767/002 on sterol pattern in Candida albicans. Sabouraudia. 1985; 23:433-42. [PubMed 3913013]

6. Hanel H, Raether W, Dittmar W. Evaluation of fungicidal action in vitro and in a skin model considering the influence of penetration kinetics of various standard antimycotics. Ann NY Acad Sci. 1988; 544:329-37. [PubMed 3214073]

7. Shadomy S, Wang H, Shadomy HJ. Further in vitro studies with oxiconazole nitrate. Diagn Microbiol Infect Dis. 1988; 9:231-7. [PubMed 3180708]

8. Beggs WH. Influence of growth phase on the susceptibility of Candida albicans to butoconazole, oxiconazole, and sulconazole. J Antimicrob Chemother. 1985; 16:397-9. [PubMed 3902762]

9. Hay RJ. Recent advances in the management of fungal infections. Q J Med. 1987; 64:631-9. [IDIS 236127] [PubMed 3328211]

10. Polak A. Antifungal activity of four antifungal drugs in the cutaneous retention time test. Sabouraudia. 1984; 22:501-3. [PubMed 6523308]

11. Gebhart RJ, Espinel-Ingroff A, Shadomy S. In vitro susceptibility studies with oxiconazole (Ro 13-8996). Chemotherapy. 1984; 30:244-7. [IDIS 187989] [PubMed 6086246]

12. Mallie M, Jouvert S, Bastide M et al. Activité comparée de huit composés azolés sur Candida albicans: pouvoir fongistatique et cytologie en microscopie électronique a balayage. Pathol Biol. 1988; 36:575-80. [PubMed 3043361]

13. Garuti L, Giovanninetti G, Ferranti A et al. Synthesis and antimycotic activity of some benzyloxyimino compounds. Pharmazie. 1987; 42:378-81. [PubMed 3671457]

14. Kerridge D. Mode of action of clinically important antifungal drugs. Adv Microbiol Physiol. 1986; 27:1-72.

15. Timm U, Zell M, Herzfeld L. Sensitive gas-liquid chromatographic method for the determination of oxiconazole in plasma. J Chromatogr. 1982; 229:111-20. [PubMed 7085818]

16. Dittmar W, Jovic N. Laboratory techniques alternative to in vivo experiments for studying the liberation, penetration and fungicidal action of topical antimycotic agents in the skin, including ciclopiroxolamine. Mykosen. 1987; 30:326-42. [PubMed 3657856]

17. Walters KA. Penetration of chemicals into, and through, the nail plate. Pharm Int. 1985; 6:86-9.

18. Stuttgen G, Bauer E. Permeation of labelled oxiconazole: comparison between the autoradiographic and the horizontal-slice technique in human skin. Mykosen. 1985; 28:138-47. [PubMed 3990703]

19. Stuttgen G, Bauer E. Bioavailability, skin- and nail penetration of topically applied antimycotics. Mykosen. 1982; 25:74-80. [PubMed 7062934]

20. Ramelet AA, Walker-Nasir E. One daily application of oxiconazole cream is sufficient for treating dermatomycoses. Dermatologica. 1987; 175:293-5. [PubMed 3319722]

21. Raulin C, Frosch PJ. Contact allergy to imidazole antimycotics. Contact Dermatitis. 1988; 18:76-80. [PubMed 2966706]

22. Raulin C, Frosch PJ. Contact allergy to oxiconazole. Contact Dermatitis. 1987; 16:39-40. [PubMed 3816206]

23. Gouveia DC, Jones da Silva C. Oxiconazole in the treatment of vaginal candidiasis: single dose versus 3-day treatment with econazole. Pharmatherapeutica. 1984; 3:682-5. [PubMed 6463068]

24. Wagner W. Comparison of clinical efficacy and tolerability of oxiconazole, one dose versus two doses daily. Mykosen. 1986; 29:280-4. [PubMed 3762589]

25. Arreaza de Arreaza F, De Torres ED, Maaz TB. Estudio comparativo doble ciego de RO-13-8996 con miconazole en relacion a su eficacia y tolerancia local en pacientes con dermatomicosis. Med Cutan Ibero Lat Am. 1984; 12:57-61. [PubMed 6376980]

26. Cetera C. Trattamento della candidiasi vaginale con un nuovo derivato imidazolico, l’oxiconazolo. Boll Chim Farm. 1985; 124(Suppl):13-20S. [PubMed 4015863]

27. Gip L. Comparison of oxiconazole (Ro 13-8996) and econazole in dermatomycoses. Mykosen. 1984; 27:295-302. [PubMed 6382000]

28. Wagner W, Reckers-Czaschka R. Oxiconazole in dermatomycosis: a double-blind, randomized comparison with bifonazol. Mykosen. 1987; 30:484-92. [PubMed 3325843]

29. Vanden Bossche H, Lauwers W, Willemsens G et al. Molecular basis for the antimycotic and antibacterial activity of N-substituted imidazoles and triazoles: the inhibition of isoprenoid biosynthesis. Pestic Sci. 1984; 15:188-98.

30. Thomas AH. Suggested mechanisms for the antimycotic activity of the polyene antibiotics and the N-substituted imidazoles. J Antimicrob Chemother. 1986; 17:269-79. [PubMed 3516967]

31. Sud IJ, Feingold DS. Mechanisms of action of the antimycotic imidazoles. J Invest Dermatol. 1981; 76:438-41. [IDIS 133194] [PubMed 7017013]

32. Vonderweidt J (Glaxo Inc, Research Triangle Park, NC): Personal communication; 1989 Jul 14.

33. Reviewers’ comments (personal observations); 1989 Jul.

34. Fromtling RA. Overview of medically important antifungal azole derivatives. Clin Microbiol Rev. 1988; 1:187-217. [PubMed 3069196]

35. Gupta AK, Einarson TR, Summerbell RC et al. An overview of topical antifungal therapy in dermatomycoses: a North American perspective. Drugs. 1998; 55:645-74. [PubMed 9585862]

36. Piérard GE, Arrese JE, Piérard-Franchimont C. Treatment and prophylaxis of tinea infections. Drugs. 1996; 52:209-24. [PubMed 8841739]

37. Sunenshine PJ, Schwartz RA, Janniger CK. Tinea versicolor: an update. Cutis. 1998; 61:65-72. [PubMed 9515210]

38. Assaf RR, Weil ML. The superficial mycoses. Dermatol Clin. 1996; 14:57-67. [PubMed 8821158]

39. Lesher JL. Recent developments in antifungal therapy. Dermatol Clin. 1996; 14:163-9. [PubMed 8821170]

40. Hay RJ. Dermatophytosis and other superficial mycoses. In: Mandel GL, Douglas RG Jr, Bennett JE, eds. Principles and practices of infectious disease. 4th ed. New York: Churchill Livingston; 1995: 2375-86.

41. Drake LA, Dincehart SM, Farmer ER et al. Guidelines of care for superficial mycotic infections of the skin: tinea corporis, tinea cruris, tinea faciei, tinea manuum, and tinea pedis. J Am Acad Dermatol. 1996; 34:282-6. [IDIS 363962] [PubMed 8642094]

42. Drake LA, Dinehart SM, Farmer ER et al. Guidelines of care for superficial mycotic infections of the skin: pityriasis (tinea) versicolor. J Am Acad Dermatol. 1996; 34:287-9. [IDIS 363963] [PubMed 8642095]

43. Reviewers’ comments (personal observations) on Sulconazole 84:04.08.

44. Bigardi AS, Pigatto PD, Altomare G. Allergic contact dermatitis due to sulconazole. Contact Dermatitis. 1992; 26:281-2. [PubMed 1395584]

45. Machet L, Vaillant L, Muller C et al. Contact dermatitis and cross-sensitivity from sulconazole nitrate. Contact Dermatitis. 1992; 26:352-3. [PubMed 1395603]

46. Jones SK, Kennedy CTC. Contact dermatitis from tioconazole. Contact Dermatitis. 1990; 22:122-3. [PubMed 2138969]

47. Baes H. Contact sensitivity to miconazole with ortho-chloro cross-sensitivity to other imidazoles. Contact Dermatitis. 1991; 24:89-93. [PubMed 1828223]

48. Marren P, Powell S. Contact sensitivity to tioconazole and other imidazoles. Contact Dermatitis. 1992; 27:129-30. [PubMed 1395626]

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