ACNE Pharmacotherapy Comparison Chart Prepared by Margaret Jin, BSP, PharmD Candidate , L. Regier, B. Jensen - © www.RxFiles.ca Feb 09 3,4,5,6,7,8,9 Basic Care Suggested Step-wise Approach for Initial Therapy {Step-down in treatment intensity for maintenance following remission} D/C acnegenic moisturizers/substances; Use oil free makeup Isotretinoin Accutane, Clarus {Avoid topicals as ↑ drying effect & not tolerated} D/C manual lesions manipulation Avoid stress, astringents, scrubs Systemic antibiotics◊ ± Topicals {Resistance concerns: systemic ABX “pulse therapy” for more severe/inflammatory acne} Shaving: shave area lightly, only once & follow grain of hair growth Women: Oral Contraceptives (COCs)◊ or Diane 35◊ {Spironolactone◊ may be an alternative}; ± Topicals Wash face: preferably once daily & no more than BID with… If papulopustular (inflammatory) +/- comedonal: Add topical ABX to BP 10(may need lower BP strength to ↓ dryness); ± retinoid mild soap (e.g., Glycerin Bar, Petrophyllic, Pears, Aveeno, Dove & e.g. combo topical products (Benzamycin, Clindoxyl / BenzaClin) ± retinoid* OR Stievamycin. To maintain, may step down to retinoid. Olay) and water or soapless cleanser (e.g., Cetaphil, Spectro Jel) If comedonal (white-blackheads): Start topical retinoid {tretinoin 0.025-0.05% has cost advantage; adapalene less irritating}; may add BP. Avoid Soaps: such as Dial, Irish Spring, Ivory, & Zest that are 1) General measures (discontinue drying agents); 2) Initiation of Benzoyl Peroxide (BP) 2.5% or 5% H O-based gel e.g. Panoxyl Aquagel or 4% Solugel; or lotion more irritating, & associated with erythema, dryness, & itching 1 2 {if starting at 2.5%, consider increase to 5% H 0-based BP; acetone- or alcohol-based gel option if oily skin.} Patient education important!!! Moisturizers – in dry seasons (e.g. Complex-15 Moisturizing Lotion) 2 Sunlight: evidence lacking 2; may be helpful for some; however, Severity MILD MODERATE SEVERE long-term exposure ↑ risk of skin cancer. Description 11 < 20 comedones (whitehead/blackhead), or 15-50 papules & pustules with comedone; cysts are Primarily nodules & cysts; also present are comedones, Diet: chocolate=MYTH; individualize diet recommendations <15 inflammatory papules, or a lesion count <30 rare; Total lesion count may range from 30-125 papules & pustules or total lesion count of > 125. Scarring. GENERAL APPROACH for topical therapies: Oily skin Æ Use solution or gel; Dry skin Æ Use cream or lotions. Potency of a given drug in various vehicles: Solution > gel > cream / lotion. Apply to affected areas, not just lesions!!! Context: affects 85% of those age 12-24; duration varies ~4+ yrs. Concerns include: scarring, pain, self esteem, social life, suicide. Contributing factors: hormonal, mechanical, contact, environmental, emotions, drugs. Family hx predictive of acne severity/duration. 12,13,14 Acne - TOPICALS www.RxFiles.ca Generic/TRADE g=generic avail. Side effects (SE)/ Response √ = therapeutic use / := Disadvantage / Comments / USUAL DOSE $ per Contraindications CI Time Drug Interactions DI / Monitor M pkg -Strength/forms, Pregnancy Category 15 Allow at least 8 wks! (≤ 5% OTC) 50% st Benzoyl Peroxide = BP Common: contact dermatitis , 8-12 weeks √1 line medication for mild-moderate acne vulgaris as monotherapy; low cost Apply to entire OTC: W χ 8% 20% 10-15 H2O-based: Solugel 4%, 8% gel; Benzac^ dryness & peeling appear after a for noted √In combination with other agents for mod-severe acne; helps prevent ABX resistance! affected area W W χ Wχ 14% 1% AC or W 5% , 10% gel; Desquam X 10% few days; erythema ; burning ; & 2% improvement; √Benzac AC gel for sensitive/dry skin & Benzac W (Water) for oily/normal skin. QHS or BID W χ gel; Panoxyl Aquagel 2.5%, 5% gel pruritus ; may bleach hair/clothes; (but covered on some drug plans) : BP >5% no more efficacious than 2.5-5% & more irritation Rx: χ⊗ odor on clothing & bed sheets. 2-4 weeks: 2.5% or 5%; Proactiv soln 2.5% (System: cleanser, toner, lotion, $$$) : Washes & Soaps least effective Æ little residual contact time 15-25 clinical Alcohol-based: Benzagel 5%W χ, 10% gel; {Temporary reduction in application may help.} H20 based C worsening DI: ↑ skin irritation or drying effect – concomitant topical medication, medicated 18bar Panoxyl 5%W χ, 10%W, 15%W, 20%W gel Irritation: ↑ conc. = ↑ irritation generally better may occur abrasive soaps & cleansers, soaps & cosmetics with strong drying effect; products W χ H2O-based < alcohol=acetone-based tolerated Acetone-based: Acetoxyl 2.5, 5, 10% gel before with high concentrations of alcohol, astringents, spices or lime; isotretinoin Lotion: Oxy 5W χ 2.5%; Benoxyl 5%W χ, 10%W; Serious: Allergic reactions & contact {if 2.5% ineffective, 1-2% improvement BP’s oxidizing action degrades antibiotics or retinoids: space admin times! W sensitization dermatitis Benzagel 5 . Select list above - see then ↑to 5%.} {Or use premixed combination products such as Clindoxyl, BenzaClin, Benzamycin} Antibacterial, Keratolytic Keratolytic Antibacterial, references for a more complete list To reduce irritation initially apply q2-3days then ↑ frequency as tolerated or OTC: 2.5, 4, & 5% W χ W W χ Wχ W χ W χ Rx: 8, 10, 15, 20% Less Useful: Soap: Panoxyl 5% , 10% ; Wash: Benzac W 5% , 10%; Benzagel 5% ; Desquam X 5% , 10% ; Panoxyl apply for 2 hrs for 4 nights, 4hrs for 4 nights, & then leave on all night if tolerated. st TRETINOIN = TRE Common: erythema, dryness, burning, ~12 weeks for √1 line medication for mild-moderate comedonal (blackheads/whiteheads) acne QHS TRE: C 0.025-0.05% 0.1% 25g Retin-A 0.01% crm, 0.025% crm, 0.05% crm, 0.1% crm, 0.01% gel, photosensitization (less with adapalene) max response; √Tretinoin has cost advantage; Adapalene has less irritation advantage Apply 30-45 min 16 ; 20g 0.025% gel Stieva-A 0.01% crm, 0.025% crm, 0.05% crm, 0.1% forte Irritation: TAZ > TRE* >ADA After successful course, consider step-down to less frequent (q2-3 night) maintenance tx after wash; start 21 {continue till no Micro crm, 0.01% gel, 0.025% gel, 0.05% gel, 0.025% soln; *(except Retin-A Micro) + ⊗χ TRE 0.025% Vitamin A esp. for TRE & TAZ tretinoin 0.01%, 0.025%, 0.05%, 0.1% $40/45g cr low conc. ; new lesions} :Use sunscreen SPF 15-30 {Retisol A: SPF-15 } Acid 0.01% crm, 0.025% crm, 0.05% crm, 0.1% crm, 0.01% gel, 0.025% {TAZ often reserved for tough skin areas, or a DI: ↑ skin irritation or drying effect– concomitant topical medication, medicated apply q2-3 nights gel, 0.05% gel {0.025-0.05% useful/tolerated} initially to ↓SE. ADA: desire for strong therapy despite irritation} 2-4 weeks: abrasive soaps & cleansers, soaps & cosmetics with strong drying effect; products 45g {Pregnancy: Motherisk deems fairly safe} May give ADA in 40 Retinoid clinical with high concentrations of alcohol, astringents, spices or lime; isotretinoin ADAPALENE = ADA Serious: rare true contact allergy less photosensitivity 16 AM ⊗ χ C worsening ↓ noninflammatory & inflammatory lesions counts by 38-71% Differin 0.1% crm & gel (XP 0.3% gel ) CI eczema; pregnancy; √ TAZ may be effective TAZ: Wχ 0.04% gel, 0.1% gel $35 (may be useful near eyes?; anti-aging?) 30g TAZAROTENE = TAZ sunburn may be less with adapalene may occur Retin-A Micro emollient, less penetrating/irritation with <5 min contact, 54 X -may wish to stop for 1 week before a sunny vacation Renova⊗χ 0.05% crm indicated for fine wrinkles, mottled hyperpigmentation & roughness of skin (not acne) Tazorac 0.05 & 0.1% crm, gel thus reducing irritation 60ml Clindamycin = CLI; Topical Soln : less irritating than BP & TRE, 8-12 weeks √Most effective for inflammatory lesions. Stop when/if no further inflammation. Dalacin T: BID 24 Common ⊗ Dalacin T, g 10mg/ml; Clindets 1% χ; erythema, peeling, itching, dryness & burning17 for noted Use in combination with BP to prevent bacterial resistance !!!18,19,20 Clindets: BID 4860s ⊗ rare CLI 1% Cream & SPF-15 Clindasol χ Serious: PMC improvement √Most effective when used in combination with BP or topical retinoids21,22,23,24 Clindets CI CLI – previous colitis, regional Erythromycin = ERY B {CLI may be preferred over ERY for prolonged effect &/or less resistance} Expert Opinion Antibiotic ⊗ χ enteritis, ulcerative colitis, PMC ERY: OD-BID 2625g Erysol 2% gel contains SPF-15 sunscreen ⊗ = 17 18,25 Benzamycin BP 5%/ERY 3% gel * As for individual ingredients above. 2-4 weeks for √BP combined with ERY or CLI has not shown resistance Similar or ↑ efficacy. Benzamycin: qHS- 46.6g * 60 corticosteroid BID ⊗ ⊗ {for Neomedrol : burning sensation, itching, noted Refrigerate Benzamycin (3 month expiry); Clindoxyl at room temp (4 mo. expiry) BenzaClin , Clindoxyl = BP 5%/CLI 1% gel * * 50g -50g Pump irritation, dryness, folliculitis, acneiform eruptions, improvement; BenzaClin: qHS-BID 58 : Combinations that are not generally recommended for long-term acne treatment: s χ W Stievamycin gel = TRE+ERY hypopigmentation; rare true contact allergy} 8-10 weeks ⊗χ NEOSPORIN 0.25%/ METHYLPREDNISOLONE 0.25%; OD-BID 75ml * Neo-Medrol Acne Lotion ; may exacerbate acne $24 Clindoxyl: qHS-BID 45g TRE 0.01%/ERY 4% C 53 Mild , ⊗ [BP/CLI combination no better than BP alone for optimal Sulfacet-R Lotion = SS 10%/Sul 5%; BID-TID; acne:less efficacious; useful: acne rosacea $33 25g Regular TRE 0.025%/ERY 4%, McKeage Combination for non-inflammatory acne ] results (tinted preparation may be useful as camouflage) Stievamycin: QHS 2225g Forte TRE 0.05%/ERY 4% Salicylic Acid = SAW χ 0.5, 1, 2 & 3.5% Oxy, Clearasil, Neutrogena, others Æ:Not commonly recommended (less potent than equal strength BP); option if retinoid intolerance e.g. skin irritation OD or BID 10-15 χ=Non-form Sk =Exception Drug Status Sk ⊗=not covered by NIHB W=covered by NIHB Δ=change ABX=antibiotic crm=cream DI=drug interaction H2O=water MET=methylprednisolone NEO=neomycin OTC= over-the-counter PMC= Pseudomembranous colitis SS=sodium sulfacetamide Sul=sulfur Rx=prescription ◊Adjunctive BP ± Retinoids ± topical Antibiotics is beneficial ^Benzac AC: ACrylates Polymer =microscopic beads that absorb excess oil while releasing a small amount of glycerine to moisturize the skin.