Examples of Oral Antifungals
Griseofulvin
Terbinafine (Lamisil)
Itraconazole (Sporonox)
What do oral antifungals treat?
Scalp & nail fungal disorders
Medications to Treat Scalp Fungal Infections
1st: Griseofulvin
2nd: Terbinafine (Lamisil)
Medications to Treat Nail Fungal Infections
1st: Terbinafine (Lamisil)
2nd: itraconazole (Sporanox)
MOA of Griseofulvin
Inhibits fungal cell division
Binds to keratin making it resistant to fungal invasion
Administration of Griseofulvin
Take with a fatty meal: increases absorption, lessens GI upset
Distribution of Griseofulvin
Deposited in the keratin layer of skin, hair, & nails
Concentrates in liver, fat, & skeletal muscles
Where is griseofulvin metabolized?
Hepatically
2 Formulations of Griseofulvin
Microsize
Ultramicrosize
Contraindications with Griseofulvin
Liver failure Porphyria Pregnancy (Cat. X) Caution with penicillin allergy Breast feeding
SE of Griseofulvin
Photosensitivity SJS Toxic epidermal necrolysis Erythema multiforme Jaundice Elevated liver enzymes Granulocytopenia Dizziness Headache Fatigue N/V Drug induced lupus like syndrome
Drug Interactions with Griseofulvin
Multiple Warfarin Oral contraceptives Alcohol Barbiturates Cyclosporine
Monitoring with Griseofulvin
LFTs: liver failure
CBC: granulocytopenia
Renal function tests
MOA of Terbinafine (Lamisil)
Creates ergesterol deficiency within the fungal cell wall leading to cell death
Distribution of Terbinafine (Lamisil)
Sebum & skin
How is terbinafine (Lamisil) metabolized?
Hepatically
Drug Reactions with Terbinafine (Lamisil)
Many
Inhibit CYP450 enzymes
Terbinafine (Lamisil) SE
Headache
Diarrhea
Elevated liver enzymes
Monitoring for Terbinafine (Lamisil)
AST/ALT prior to initiation
CBC
Assess taste/smell disturbances
What is terbinafine used for?
Treat tinea capitis, and onychomycosis
Reasons to Treat Onychomycosis
Cosmetic reasons
DM & onychomycosis
Hx of lower extremity cellulitis & ipsilateral onychomycosis
Pain/discomfort secondary to infection
Black Box Warning for Itraconazole (Sporanox)
Negative inotropic effects have been observed following IV administration
Discontinue or reassess if S/S of HF occur during treatment
Contradictions for Itraconazole (Sporanox)
Ventricular dysfunction
CHF
Pregnancy
Concomitant use of other CYP450 drugs
How is itraconazole (Sporanox) metabolized?
Hepatically
Drug Interactions with Itraconazole (Sporanox)
PPIs Anxiolytics Pain medications Antiplatelet agents Antihypertensives Statins
Itraconazole (Sporanox) SE
Nausea Diarrhea Edema Headache Rash Abnormal LFTs Heart failure Arrhythmia Hearing loss Many others
Monitoring with Itraconazole (Sporanox)
Baseline LFTs
Monthly LFTs
Serum contraindications
5-Alpha-Reductase Inhibitor Medication for Fungal Infections
Finasteride (Propecia)
MOA of Finasteride (Propecia)
Inhibits the conversion of testosterone to dihydrotestosterone
What is finasteride (Propecia) first line for?
Androgenic alopecia in men
What is another name of medication for finasteride (Propecia)?
Proscar: BPH
Monitoring for Finasteride (Propecia)
Baseline PSA
PSA in 6 months
Reduces PSA my 50%
Finasteride (Propecia) SE
Orthostatic hypotension Dizziness Weakness Sexual dysfunction: decreased libido, ejaculatory dysfunction, erectile dysfunction Gynecomastia Testicular pain Depression
Why is finasteride (Propecia) hazardous?
Teratogenic
Women should avoid crushed/broken tablets
How is finasteride (Propecia) metabolized?
Hepatically
Antibiotics used in Dermatology
Cephalexin (Keflex) Mupirocin (Bactroban) Doxycycline Minocycline (Minocin) Clindamycin
Cephalexin (Keflex) Drug Class
1st generation cephalosporin
Beta-lactam antibiotic
Dermatology Indications for Cephalexin (Keflex)
Skin infections
Skin structure infections
Distribution of Cephalexin (Keflex)
Widely distributed to all tissues except CSF
What bugs does cqphalexin cover?
Staph
Strep
MOA of Cephalexin (Keflex)
Inhibits bacterial cell wall synthesis
Pregnancy Category of Cephalexin (Keflex)
Category B
Indications for Mupirocin (Bactroban)
Impetigo: ointment
Secondary infected skin lesions: cream
MRSA colonization: intranasal
MOA of Mupirocin (Bactroban)
Inhibits protein synthesis by binding to bacterial isoleucyl tRNA synthetase
Absorption of Mupirocin (Bactroban)
Ointment & cream: minimal systemic absorption
Intranasal: systemic absorption
MOA of Tetracyclines
Inhibition of protein synthesis by binding with the 30S ribosomal subunit
Alterations in the cytoplasmic membrane
Distribution of Tetracyclines
Throughout the body tissues & fluids
Poor CNS penetration
SE of Tetracyclines
Photosensitivity
Pregnancy Category of Tetracyclines
Category D
SE of Doxycyline
Photosensitivity
Nausea: empty stomach
Esophagitis: no fluids
Absorption of Doxycycline
Delayed with high stomach pH
Doxycycline Dermatologic Indications
Tick-borne rickettsial infections
Acne
Rosacea
Off-label use of Doxycycline
Animal & human bites
Cellulitis secondary to MRSA
Skin & soft tissue infections
Minocycline (Minocin) Dermatologic Indications
Acne
MRSA cellulitis: off-label
SE of Minocycline (Minocin)
Photosensitivity
Vertigo
Esophagitis: no liquids
GI upset: empty stomach
Dermatologic Indications for Clindamycin
Acne: only topical
Rosacea
Retinoid Acid Derivative Medication(s)
Isotrentinoin (Accutane) Absorica Amnesteem Claravis Myorisan Zenatone
Use for Isotrentinoin (Accutane)
Treatment of severe, recalcitrant, nodular acne
MOA of Isotrentinoin (Accutane)
Shrinks sebaceous glands
Decreases sebum production
Decreases # of sebum dependent bacteria acnes
Mucocutaneous SE of Isotrentinoin (Accutane)
Cheilitis Dry skin & mucous membranes Epistaxis Desquamation Photosensitivity Pruritis Corneal abrasion Cutaneous staph infections Temporary diffus alopecia or nail brittleness Depression Hypertriglyceridemia Elevated total & LDL cholesterol
Monitoring in Isotrentinoin (Accutane) Use
CBC
Fasting lipid profile
LFTs
Monthly pregnancy test
When would you discontinue Isotrentinoin (Accutane)?
TG >800
LFTs 3x upper limit of normal
Topical Calcineurin Inhibitor Medications
Tacrolimus (Protopic)
Pimecrolimus (Elidel)
Indications for Topical Calcineurin Inhibitors
Atopic dermatitis
Lichen planus
Vitiligo
Psoriasis
Black Box Warning for Topical Calcineurin Inhibitors
Rare cases of malignancy (skin & lymphoma)
Limited to short-term & intermittent
Contraindications for Topical Calcineurin Inhibitors
MOA of Topical Calcineurin Inhibitors
Suppresses cellular immunity
Recommendations for Topical Calcineurin Inhibitors
Alcohol ingestion = redness/flushing
Do not use under occlusive dressing
Sun protection
Tacrolimus (Protopic) SE
Headache
Skin burning at application site
Pruritus
Erythema
Pimecrolimus (Elidel) SE
Burning: less than Protopic
Presentation of Drug Induced Lupus like Syndrome
Arthralgia Myalgia Malaise Fever Rash Serositis
Treatment of Drug Induced Lupus like Syndrome
Discontinue drug
Symptomatic treatment with NSAIDs
Hydroxychloroquine >4-8 weeks
Systemic corticosteroid: severe symptoms or quick relief