ANTIBACTERIAL, ANTIFUNGAL,

ANTIVIRAL DRUG FOR SKIN

INFECTIONS

Herri S. Sastramihardja
 INTRODUCTION

Bacterial and fungal infection are common in dermatoses &

contaminated wounds e.g. wounds due to trauma
They may also occur in apparently clean wounds & are
especially dangerous in immunocompromised patients
TOPICAL ANTIBACTERIAL AGENTS (=AB)

THERAPEUTIC RATIONALE & MECHANISM

Ideally, a particular AB is selected on the basis of results of culture of
materials from the lession or wound
However, because pathogens isolated from most infected dermatoses are
group A-B- hemolytics Streptococci, Staphylococcus aureus, or mixture of
thee, presumptive therapy (i,e without a culture) is usually justified
High concentrations of AB are applied to relatively small areas to limit
systemic toxicity
Broad-spectrum coverage can be obtained by using prepackaged
topical AB preparations that contain several AB in fixed
concentration well above the therapeutic treshold.
If the response is delayed or inadequate, a culture should be
obtained to identify the organism & determine its sensitivity
MOA of AB drug are discussed next
INDICATIONS:

AB drugs are indicated for prevention of infection in clean

wounds & for early treatment of infected dermatoses & wounds
Bacitracin is also used to decrease colonization of the anterior
nares by Staphylococci
Tabel
 BACITRACIN

Contraindications & Warning

Allergic Hypersensitivity

Adverse Effect

Contact urticaria syndrome ( has been reported after

treatment with bacitracin)
 POLYMYXIN B-SULFATE

The only available topical preparations that contain polymyxin B

also contain AB that demonstrated activity agains Gr+ organism
Contraindication & Warning
• The daily dose applied to denude skin should not exceed 200 mg
because of the risk of neurotoxicity & Nephrotoxicity
NEOMYCIN & GENTAMYCIN

Contraindication & Warning

Allergic Hypersensitivity
Adverse Effects
Neomycin frequently caused sensitivity, particularly when applied
to eczematous dermatose
Gentamycin is applied to large areas of denuded skin (e.g. in burn
patients), serum concentration of drug may reach nephrotoxic, ototoxic,
neurotoxic levels.
 TOPICAL ANTIFUNGAL (=AF) AGENTS

THERAPEUTIC RATIONALE & MECHANISMS

Superficial infections of the non- hair-bearing skin by dermatophytes

or yeasts are generally successfully treated by topical therapy alone
Infections of the hair and nails respond poorly to topical therapy
alone & often necessitate treatment with orally administered agents
Chronic mucocutaneous Candidiasis is responsive to topical therapy
& requires long-term maintenance therapy with oral ketoconazole
 AMPHOTERIZIN B

Indication
• Cutaneous Candidiasis

Contraindication & Warning

• Allergic Hypersensitivity

Adverse Efects
• Yellowish discolouration of skin & nails

Interactions
• Should not be used concurently with imidazole agents (Clotrimazole,
Econazole, Ketoconazole, Miconazole) because their effects may
counteract each other
 CICLOPIROX OLAMINE

Indication
• Superficial dermatophyte infection

Contraindication & Warnings

• Allergic Hypersensitivity

Adverse Effects
• Pruritus
• Worsening of clinical disease secondary to infection
 IMIDAZOLE

Indication
• Superficial dermatophyte infections, cutaneous candidiasis, tinea
versicolor (All Imidazole antifungal agents)
• Clotrimazole & Miconazole also indicated for treatment of
vulvovaginal candidiasis

Contraindication & Warnings

• Allergic Hypersensitivity

Adverse Effects
• Local reactions to Imidazole drugs include stinging, pruritus,
erythema, local irritation.
 HALOPROGIN

Indication
• Superficial dermatophyte infections
• Tinea versicolor

Contraindication & Warnings

• Allergic Hypersensitivity

Adverse Effects
• Local irritation
• Burning sensation
• Vesiculation
• Exacerbation of the lessions
 NYSTATIN

Indication
• Cutaneous, oral, intstinal, vulvovaginal candidiasis

Contraindication & Warnings

• Allergic Hypersensitivity

Adverse Effects
• Diarrhea, nausea, vomiting (association with large doses)
 TOLNAFTATE

Indication
• Superficial dermatophyte infections,
• Tinea versicolor
• Not effective againts Candida

Contraindication & Warnings

• Allergic Hypersensitivity
• Recurrent of infection following cessation of therapy is common
• Infections of palms & soles are ususally unresponse to Tolnaftate alone

Adverse Effects
• Rarely cause irritation.
Hal 355
 GRISEOFULVIN (=GF)

Indication:
• Dermatophyte infections of the skin, hair, and nails
• Effective against Epidermophyton, Microsporum, Trichophyton species
• Ieffective against Candida & Pityrosporeus orbiculare

Pharmacokinetics
• Microsize GF orally (1 Gr) C max= 2 µg/ml3; Tmax= 4-6 hours
• Reduction particle size  Î absorption
• (1/2 dose VMS GF  C plasma = MSGF
• Transported by sweat + transepidermal fluid to stratum corneum (4-6
hours after oral)
Contraindication & Warnings
• Allergic hypersensitivity
• Cross reactivity with Penicillin (derived  Penicillin mold)
• Should not be used in porphiria or hepatic failure
• It’s safety on pregnancy is not established

Adverse Effects
• Headache, confusion
• Nausea, vomiting, diarrhea
• Photosensitivity
• Pheripheral neuritis
• Leukopenia & proteinuria (have been reported)

Interactions:

GF induced hepatic enzyme  Î rate of metabolsm of coumarin drugs

 KETOCONAZOLE

Indications
• Chronic mucocutaneous candidiasis
• Severe recalcitrant dermatophyte infections
• Chromomycosis

Pharmacokinetics
• Oral absorption requires an acidic gastric environment
• In achlorhydria, each tablet must be dissolved in 4 ml of 0,2
normal HCL prior to ingestion
 KETOCONAZOLE

Contraindincation & Warnings

• Allergic Hypersensitivity ( Anaphylaxis)
• Hepatic Dysfunction is a relative contraindication

Adverse Effects
• Hepatocellular hepatotoxicity (1/10.000)
• Nausea, vomiting ( ↓with food),
• Gynecomastia, impotence, ↓testosterone levels (in dose of 800 mg/
day)
 KETOCONAZOLE

Interactions
• Antacids, anticholinergic, H2 blockers (2 hours pre-K)
• Ketoconazole ↑anticoagulant effect of Coumarin
• Ketoconazole ↑blood level of Cyclosporine ↑nehrotoxicity
• Rifampin ↑metabolic clearance of Ketoconazole
 TOPICAL ANTIVIRAL AGENTS
ACYCLOVIR
Indication
• Primary & recurrent Herpes simplex Infections (HSI)
• HSI in immunocompromised patients

Pharmacokinetics
• Systemic absorption following topical application is minimal

Contraindication & Warnings

• Allergic hypersensitivity
 ACYCLOVIR

Adverse Effects
• Minimal for topical administration

Preparations available & dosage

• Acyclovir topical (e.g. Zovirax 5% ointment)
• (apply to lesions 6 times daily)
• Prescribing category-Rx:C
 PODOPHYLLUM RESIN

Indications
• Condyloma acuminatum
• Verucca vulgaris

Contraindication & Warnings

• Avoid during pregnancy
• Do not contact with the eyes

Adverse Effects
• Local irritation (common)
•  severe ulceration of surrounding tissue
• Residual post inflmmatory hyperpigmentation
Preparation available & dosage
• Podophyllum Resin (Pod.Ben-25, Podofin, Podoben: 25% tincture)
• Used once weekly (for 3-5 weeks), thin layer, allow it to dry.
• Wash tincture 2-3 hours after initial application 6-8 hours after
subsequent applications
• Prescribing category: RX do not use in pregnant women
 ANTIVIRAL SYSTEMIC AGENTS

While the majority of antiviral therapu rely on the production of active

or passive immunity
A few drugs are now available for the prophylaxis or treatment of viral
disease by nonimmunologic means
For examples for Herpes viruses:
• Acyclovir
• Ganciclovir
• Foscamet
• Cidofovir