Topical Antimicrobials

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Topical Antibacterials - Skin Savers

  • Mupirocin:
    • MOA: Inhibits bacterial isoleucyl-tRNA synthetase.
    • Spectrum: Gram(+) cocci, including MRSA.
    • Uses: Impetigo, folliculitis, eradication of nasal MRSA.
  • Fusidic Acid:
    • MOA: Inhibits protein synthesis (blocks EF-G). Steroid-like structure.
    • Spectrum: Potent against Staphylococci (including some MRSA).
    • Uses: Staphylococcal skin infections (impetigo, infected eczema). Good skin penetration.
  • Retapamulin:
    • MOA: Pleuromutilin; inhibits protein synthesis at 50S ribosomal subunit (P site).
    • Spectrum: S. aureus, S. pyogenes.
    • Uses: Impetigo.
  • Neomycin, Polymyxin B, Bacitracin (Triple Antibiotic Ointment):
    • MOA: Neomycin (30S inhibitor), Polymyxin B (damages cell membrane), Bacitracin (inhibits cell wall synthesis).
    • Spectrum: Broad (Gram +ve & -ve).
    • Uses: Minor skin trauma. ⚠️ High risk of allergic contact dermatitis (esp. Neomycin).
  • Clindamycin (Topical):
    • MOA: Lincosamide, binds 50S ribosome.
    • Uses: Acne vulgaris, bacterial vaginosis.
  • Erythromycin (Topical):
    • MOA: Macrolide, binds 50S ribosome.
    • Uses: Acne vulgaris. Widespread resistance.
  • Metronidazole (Topical):
    • MOA: Disrupts bacterial DNA synthesis.
    • Uses: Rosacea, bacterial vaginosis, infected ulcers.
  • Silver Sulfadiazine:
    • MOA: Silver ions (antimicrobial) + sulfadiazine (folate synthesis inhibitor).
    • Uses: Prevention/treatment of burn wound infections. Can cause transient leukopenia.

⭐ Mupirocin is a key agent for decolonizing MRSA from the nares, often used pre-operatively to reduce surgical site infections (SSIs).

Topical Antifungals - Fungus Fighters

  • Azoles: Inhibit fungal P450 enzyme (14-α-demethylase) → ↓ergosterol synthesis. Broad spectrum.
    • Imidazoles: Clotrimazole, Miconazole, Ketoconazole (also for seborrheic dermatitis, Pityriasis versicolor).
    • Triazoles (newer): Luliconazole, Efinaconazole (onychomycosis).
  • Allylamines: Inhibit squalene epoxidase → squalene accumulation (toxic) & ↓ergosterol. Fungicidal.
    • Terbinafine: Excellent for dermatophytes (tinea pedis, cruris, corporis).
    • Naftifine, Butenafine.
  • Polyenes: Bind to ergosterol in fungal cell membrane → form pores → leakage.
    • Nystatin: Candida infections (oral thrush, vaginal, intertrigo). Not absorbed.
    • Amphotericin B (topical): Cutaneous/mucocutaneous candidiasis.
  • Other Antifungals:
    • Ciclopirox Olamine: Unique MoA (chelates trivalent cations); broad spectrum. Nail lacquer.
    • Tolnaftate: Distorts hyphae; dermatophytes only (tinea).
    • Amorolfine: Inhibits ergosterol synthesis (different enzymes than azoles). Nail lacquer.

⭐ Terbinafine typically requires shorter treatment duration (e.g., 1-2 weeks for tinea corporis/cruris) compared to many azoles for similar dermatophyte infections.

Fungal cell structure with antifungal drug targets

Topical Antivirals & Antiparasitics - Virus & Vermin Vanquishers

Antivirals:

  • Acyclovir (5% cr/oint): Herpes simplex, VZV. Guanosine analog → inhibits DNA pol. Apply 5-6x/day.
  • Penciclovir (1% cream): Herpes labialis. Like acyclovir. Apply q2h awake.
  • Imiquimod (5% cream): HPV warts, actinic keratosis, sBCC. TLR7 agonist. Apply 3x/wk up to 16 wks (warts).
  • Podophyllotoxin (0.5% sol/gel): HPV warts. Antimitotic. BID x3d, 4d off. ⚠️ Teratogenic.

Antiparasitics:

  • Permethrin (5% cream): Scabies, pediculosis. Neurotoxin (Na+ ch. blocker).
    • Scabies: Apply neck-down, wash 8-14h. Repeat 1 wk if needed.
    • Lice: Apply, wash 10 min.

    ⭐ Permethrin 5% cream: DoC for scabies; single overnight (8-14h) application often curative.

  • Lindane (GBHC 1%): Scabies, pediculosis (2nd line). CNS stimulant. Wash 8-12h (scabies). ⚠️ Neurotoxic (kids).
  • Ivermectin (0.5%-1%): Pediculosis capitis, rosacea (Demodex). Glu-Cl- ch. modulator. Lice: 1 app, wash 10 min.
  • Crotamiton (10%): Scabies (↓effective), antipruritic.
  • Benzyl Benzoate (25%): Scabies. Irritant. Apply 24h.
  • Malathion (0.5%): Pediculosis. Organophosphate. Flammable. Apply 8-12h.

Sarcoptes scabiei mite and eggs

High‑Yield Points - ⚡ Biggest Takeaways

  • Mupirocin: Targets isoleucyl-tRNA synthetase; effective for MRSA (impetigo, nasal carriage).
  • Retapamulin: Binds 50S ribosomal subunit (L3 protein); treats impetigo (S. aureus, S. pyogenes).
  • Fusidic acid: Steroidal antibiotic inhibiting protein synthesis (EF-G); for Staphylococcal skin infections.
  • Triple antibiotic (Neomycin, Bacitracin, Polymyxin B): Neomycin is a common cause of contact dermatitis.
  • Topical Clindamycin: Used for acne vulgaris; systemic absorption carries a rare risk of pseudomembranous colitis.
  • Silver sulfadiazine: For burn wound prophylaxis; combines silver ions and sulfadiazine (folate inhibitor).

Practice Questions: Topical Antimicrobials

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A patient develops an infection of methicillin resistant Staphylococcus aureus. All of the following can be used to treat this infection except

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Flashcards: Topical Antimicrobials

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_____ is an FDA-approved drug that acts by stimulating Toll-like receptors 7 and 8

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_____ is an FDA-approved drug that acts by stimulating Toll-like receptors 7 and 8

Imiquimod

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