Dermatologic Agents

Chapter 13


Dermatologic Agents




DRUG OVERVIEW



























































































































































































































































Class Subclass Generic Name Trade Name
TOPICAL CORTICOSTEROIDS (SEE TABLE 13-2)
Immunosuppressive drugs   pimecrolimus Elidel image
    tacrolimus Protopic
ANTIINFECTIVES
Topical antibiotics   mupirocin image Bactroban image
    bacitracin Bacitracin, Baciguent
    erythromycin Akne-mycin
    gentamicin Garamycin
    nystatin image Mycostatin
    polymyxin B sulfate In Polysporin, Neosporin
    retapamulin Altabax
Topical antifungals Azoles clotrimazole Lotrimin, Mycelex, Lotrisone
    econazole Spectazole
    ketoconazole Nizoral
    miconazole Monistat-Derm
    oxiconazole Oxistat
    sertaconazole Ertaczo
    sulconazole Exelderm
  Allylamine/benzylamine derivatives butenafine Mentax
    naftifine Naftin
    terbinafine Lamisil image
  Hydroxypyridones ciclopirox Penlac, Loprox
  Others nystatin image Nystatin, Mycostatin
    haloprogin Halotex
    tolnaftate Tinactin
    selenium sulfide lotion 2.5% Selsun
Topical antivirals   acyclovir image Zovirax image
    penciclovir Denavir
    docosanol Abrevia
Scabicides/pediculicides   crotamiton Eurax
    ivermectin Stromectol, Sklice
    malathion Ovide
    permethrin Elimite, Nix
    lindane Kwell
    spinosad Natroba
ACNE PREPARATIONS
Antibacterial/keratolytic   benzoyl peroxide Benzac (prescription), many brands OTC
    metronidazole MetroGel
    clindamycin image Cleocin-T
Topical retinoid   tretinoin Retin-A, Avita
Oral retinoid   isotretinoin Generic
LOCAL ANESTHETICS Short acting procaine HCl Novocain
    chloroprocaine Nesacaine
  Intermediate acting lidocaine HCl Xylocaine
    mepivacaine HCl Carbocaine HCl
    prilocaine HCl Citanest
  Long acting bupivacaine HCl Marcaine, Sensorcaine,
    etidocaine Exparel LA
    tetracaine HCl Duranest
      Pontocaine HCl


image


image Top 100 drug.




INDICATIONS








Local Anesthetics




• Local anesthetics are indicated for a variety of uses, which include minor surgical procedures, suturing, and relief of itching or pain from wounds, burns, and/or hemorrhoids.


• Local anesthesia does not depress the patient’s level of consciousness, which makes its use much safer than general anesthesia. Local anesthetics may be applied as a powder, gel, lotion, ointment, spray, or injection into a small area. If a larger area is required for anesthesia, a nerve trunk (epidural, spinal) or a single nerve may be injected to provide for regional anesthesia. This discussion is not intended as a complete presentation but rather as a brief overview of common local anesthetics used in primary care.


• Local anesthetics may be combined with vasoconstrictors (epinephrine) to prolong action by decreasing systemic absorption. However, at the ends of arteries, such as in the fingers, toes, penis, and nose, vasoconstrictors are not safe for use. In those areas, gangrene may develop because of severe vasoconstriction.


• A number of local agents are used safely on mucous membranes, ulcers, or wounds. If agents are applied to the oral cavity, however, the patient may have difficulty swallowing. Therefore, food should be withheld for at least 1 hour to prevent aspiration. Use with caution in areas of inflammation.


• Do not use if solutions are discolored or if they contain precipitants. If the solution does not contain a preservative, it must be discarded after opening. Because some situations of severe anaphylaxis have resulted from the use of local anesthetics, have resuscitation equipment on hand before use or emergency backup plans when any anesthetic is used. Obtain the patient’s prior history of local anesthetic use before administration. Patient or guardian should sign a permission form before consenting to any procedure involving a local anesthetic.


This chapter discusses preparations used for skin, nail, and hair problems. These preparations are used for an extremely large array of dermatologic problems. See each section for more specific indications. General issues in topical medications are discussed; then corticosteroids, antiinfectives, acne medications, and local anesthesia are discussed, each in a separate section. The purpose of this chapter is to discuss the most common of the various available agents. It does not attempt to address all of the preparations or the myriad indications for these agents. This chapter focuses on the topical use of these products. See appropriate chapters for more information about drugs from specific drug categories.



Therapeutic Overview of Dermatologic Agents


Anatomy and Physiology


The primary function of the skin is as a barrier. It functions to protect and thermoregulate. The skin is involved in the immune response, biochemical synthesis, and sensory detection. The skin’s barrier function is compromised when the skin has been damaged or when inflammation is present.


The skin, the largest organ of the body, consists of three distinct layers: epidermis, dermis, and subcutaneous tissue (Figure 13-1). The epidermis is the outer layer of the skin. The thickness of the epidermis ranges from 0.05 mm on the eyelids to 1.5 mm on the palms and soles. Five layers make up the epidermis. Basal cells form a single layer of cells that make up the innermost layer of the epidermis. These basal cells divide to form keratinocytes. The other layers are formed as keratinocytes change until they migrate to the outer layer to become the major component of the stratum corneum. The stratum corneum provides protection to the skin by acting as a barrier. The thicker the epidermis, the greater the barrier protection.



The dermis, similar to the epidermis, varies in thickness, ranging from 0.3 mm on the eyelid to 3 mm on the back. Three types of connective tissue—collagen, elastic tissue, and reticular fibers—make up the dermis. Different from the epidermis, the dermis is made up of nerves, blood vessels, hair follicles, and apocrine and eccrine glands.


Subcutaneous tissue is the deepest layer. Distribution is dependent on sex characteristics. Age, heredity, and caloric intake also influence distribution. The subcutaneous tissue provides padding and insulation to the underlying structures.


New research has suggested that tattoo inks may include carcinogens (such as benzopyrene) and hormone disruptors (such as dibutyl phthalate, which can mimic estrogen or disrupt testosterone), and their injections into skin with small needles are linked to allergic rashes, chronic skin reactions, infection, and inflammation from sun exposure. The Food and Drug Administration has launched new studies to investigate the long-term safety of the inks, including what happens when they break down in the body or interact with light. It appears that when skin cells containing ink are killed by sunlight or laser light, the ink breakdown products could spread throughout the body. Research already has shown that tattoo inks migrate into people’s lymph nodes, but the connection of tattoo inks to malignancies such as melanoma, basal cell carcinomas, squamous cell carcinomas, and keratoacanthomas is not clear. The long-term health risks posed by tattoo inks are unknown. There may be potential effects on fetuses and infants—for example, in infant boys, feminization of the reproductive tract may occur with phthalate exposure.




Mechanism of Action


Topicals work by being absorbed into the skin. Their effect is local. The specific mechanisms of action are discussed in each separate section. Topical preparations are available in a bewildering array of products, including many combination products, corticosteroid products of different strengths, and antiinfectives of every kind. The primary care provider should become familiar with a few products and treatment measures rather than trying to master the complete array. Superficial skin infections and acne are commonly treated in primary care. If the patient does not respond to standard care, he is referred to a dermatologist. Primary care providers should be able to identify suspicious lesions and refer patients promptly to dermatology; such patients frequently require surgical treatment.


Where applicable, specific information regarding standard guidelines, evidence-based recommendations, cardinal points of treatment, pharmacologic treatment, and nonpharmacologic treatment is provided later in the chapter.


Topical therapy is unique because the skin is directly accessible for both diagnosis and therapy. Drugs used to treat skin problems can be applied directly to the site. All topical agents can also be absorbed systemically. Consider the adverse effects of the systemic medication when you are ordering topical agents.


Factors that affect the extent of drug absorption into the skin include the status of the skin, the characteristics of the drug, and the characteristics of the administration vehicle. Absorption is increased when the skin is broken or inflamed. In addition, absorption increases in cases in which skin integrity is compromised or the skin is thinner. Because of the vascular composition of the skin, mucous membranes absorb medication in high concentrations. The vehicle or base affects percutaneous absorption (Table 13-1). The vehicle may hydrate the outer layer of skin by preventing water loss. With improved hydration, the absorption of medication and the depth of penetration are enhanced.



TABLE 13-1


Characteristics of Vehicle of Selected Topical Products








































  Creams Ointments Gels Solutions and Lotions Aerosols
Base Mixture of several different organic oils and water Mixture of a limited number of organic compounds consisting primarily of petroleum jelly with little or no water Greaseless mixtures of propylene glycol, water, and alcohol Alcohol, water, and some chemicals Drug suspended in a base and delivered via a propellant (e.g., isobutane, propane)
Color White, somewhat greasy Translucent, greasy feeling persists on skin Clear with a gelatinous consistency Clear or milky  
Versatility Most frequent base prescribed, used on nearly all body areas, especially useful in the intertriginous areas (e.g., groin, genital area, axillae) Greater penetration, useful for drier lesions, enhanced potency Unpleasant sticky feeling, may be irritating Most useful for scalp because it penetrates the hair shaft Useful for applying to scalp via a long probe attached to a can
Miscellaneous Cosmetically more acceptable; can be drying after prolonged use, best used for acute exfoliative dermatitis Too occlusive for acute exudative eczematous inflammation; too occlusive for intertriginous areas Alcohol gels feel cool and are drying; useful in acute exudative inflammation (e.g., poison ivy); nonalcoholic gels are more lubricating and can be useful in drying scalp lesions; useful in scalp areas because other vehicles mat hair May be drying and irritating when used in intertriginous areas Convenient for patients who lack mobility and have difficulty in reaching lower legs; useful for moist lesions (e.g., poison ivy)


image


Absorption of topical medications is slow and incomplete compared with drugs given orally. For optimal absorption, apply them to moist skin either immediately after bathing or after wet soaks.


Prescribing the appropriate amount of topical medication is important. Too large a tube may be very costly to the patient, yet a small tube may not include enough medication to cover the entire area. To estimate the amount that should be prescribed, the rule of nines can be used (Figure 13-2).




Treatment Principles


How Topical Agents Are Used


Creams, Ointments, and Pastes











Topical Corticosteroids


For a listing, see Table 13-2.



TABLE 13-2


Topical Corticosteroids Ranked by Potency













































































































































































Group Generic Name Dosage Form Strength (%) Brand Name
I, Very High clobetasol propionate Cream, ointment 0.05 Temovate, generic
  betamethasone dipropionate Ointment 0.05 Diprosone, generic
  diflorasone diacetate Ointment 0.05 Psorcon E, generic
  halobetasol propionate Cream, ointment 0.05 Ultravate, generic
II, High amcinonide Cream, lotion, ointment 0.1 Amcinonide
  betamethasone dipropionate Cream 0.05 Diprosone
  betamethasone valerate Ointment 0.1 Valisone
  desoximetasone Cream, ointment 0.25 Topicort, generic
  diflorasone diacetate Gel 0.05 Psorcon E, generic
  fluocinolone acetonide Cream, ointment (emollient base) 0.05 Synalar, generic
  fluocinonide Cream 0.2 Lidex, generic
  halcinonide Cream, gel, ointment 0.05 Halog
  triamcinolone acetonide Cream, ointment
Cream, ointment
0.1
0.5
Kenalog, generic
Kenalog, generic
III, Medium betamethasone dipropionate Lotion 0.05 Maxivate, generic
  betamethasone valerate Cream 0.1 Beta-Val, generic
  clocortolone pivalate Cream 0.1 Cloderm
  desoximetasone Cream 0.05 Topicort LP, generic
  flurandrenolide Cream, ointment 0.025 Cordran SP (cream)
  fluticasone propionate Cream, ointment, 0.05 Cutivate, generic
  hydrocortisone butyrate Tape 4 mcg/cm2 Locoid, generic
  mometasone furoate Cream 0.05 Elocon, generic
  triamcinolone acetonide Ointment
Solution
Cream, ointment
Cream ointment, lotion
Cream, ointment, lotion
0.1
0.2%
0.1
0.025 or 0.1
0.05
Kenalog, generic
Aristocort
Generic
Generic
Kenalog
IV, Low alclometasone dipropionate Cream, ointment 0.05 Aclovate, generic
  desonide Cream 0.05 DesOwen, generic
  fluocinolone acetonide Cream, solution 0.01 Synalar, generic
  hydrocortisone Lotion 0.25 Generic
  hydrocortisone acetate Cream, ointment, lotion
Cream, ointment, lotion, solution
Cream, ointment, lotion
Cream, ointment
0.5
1
2.5
0.5, 1
Generic
Generic
Generic
Cortef, Lanacort 10 Crème, generic


image


Range: Group I (very potent) to Group IV (least potent). Note: Some of the drugs appear in more than one category.






Treatment Principles


Standardized Guidelines


No general standardized guidelines are found. There are some guidelines for treatment of specific diseases or skin conditions. See www.guidelines.gov for specific conditions. (See Table 13-4.)




Cardinal Points of Treatment




• Initiate therapy with an agent of the lowest potency needed, and use for as short a time as possible.


• Group I corticosteroids are used for severe dermatoses over nonfacial/nonintertriginous areas such as psoriasis, severe atopic dermatitis, or severe contact dermatitis. They are especially useful over the palms and soles, which tend to resist topical corticosteroid penetration because of skin thickness.


• Preparations of intermediate to potent strength are appropriate for mild to moderate nonfacial/nonintertriginous dermatoses.


• Eyelid and genital dermatoses should be treated with topical corticosteroids of mild strength.


• Preparations of mild to intermediate strength should be considered when large areas are treated because of the likelihood of systemic absorption.


• Treatment should be discontinued when the skin condition has resolved. Tapering the corticosteroid will prevent recurrence of the skin condition. Tapering is best performed by gradually reducing the potency and dosing frequency at 2-week intervals.


• Therapy may be continued for chronic diseases that are responsive to treatment; patients should be monitored for the development of adverse effects and/or tachyphylaxis (rapid development of a decreased response).


• Generic topical corticosteroids are effective for treatment of most skin disorders in the primary care setting. Generic medications often have slightly less potency or vehicles that are less cosmetically appealing, but the substantial cost savings may offset any differences in efficacy or feel.



Pharmacologic Treatment


Topical corticosteroids are ranked according to potency, with group I as the most potent and group VII as the least potent. It is usually sufficient to divide them into high-, medium-, and low-potency groups. Frequently, weaker strengths are used because they are considered to be safer. However, adequate strength is necessary for a therapeutic response. Weak OTC hydrocortisone is not effective against many dermatoses; a medium-strength steroid from class III or IV is often more effective. If the patient does not respond, treatment should be reevaluated.


Potency is the most important variable when a topical steroid corticosteroid is selected. A drug from each potency level should be chosen to meet the prescriptive needs of the patient. The potency of a steroid is not determined by its strength but by vasoconstrictor assays.



Vasoconstrictor assays measure skin blanching when an agent is applied to skin under occlusion. A difference in potency may be noted between generic and name brand corticosteroid equivalents. Pharmacists are allowed to substitute generic drugs unless the health care provider requests “No substitutions” or “Brand necessary.”


Use low-potency agents in children, on large areas, for mild conditions, and on body sites that are especially prone to corticosteroid damage, such as the face, scrotum, axilla, flexures, and skin folds.



Reserve high-potency agents for areas and conditions that are resistant to treatment with milder agents; these may be alternated with milder agents. Short-term intermittent therapy with the use of high-potency agents may be more effective and may cause fewer adverse effects than continuous treatment with low-potency agents. No fluorinated or high-potency corticosteroid should be used on the face.


For all groups, apply the product sparingly two to four times a day. Adequate results are usually achieved with twice-a-day application and a course of therapy of 2 to 6 weeks. To prevent rebound, do not discontinue treatment abruptly after long-term use of a potent agent. Instead, reduce the frequency of application, or use a lower-potency agent.


When desired results are not achieved, stop therapy for 4 to 7 days, and then resume treatment with a different agent. A more potent corticosteroid may be needed.


A drug from each potency level should be chosen to meet the prescriptive needs of the provider. Triamcinolone is commonly used because it is available generically and comes in a variety of strengths. Triamcinolone 0.5% is a good product of medium strength that is effective for many rashes seen in the office setting.



Group I


Topical corticosteroids in group I are super-potent agents. The amount of drug applied to the body per day and the duration of treatment must be carefully monitored. Per week, a maximum of 50 g of cream or ointment should be used. The duration of daily use of super-potent topical corticosteroids should not exceed 2 weeks, if possible. A period of 1 week is needed before a group I topical corticosteroid can be used again. This is called cyclic or pulse dosing. Diflorasone diacetate can be used under occlusion; betamethasone dipropionate cannot. Occlusive dressings should be used for no longer than 12 hours at a time. Renal suppression, skin atrophy, and other side effects are possible. Patients who use group I topical corticosteroids should be monitored closely for HPA suppression. Prescriptions should limit refills.







Patient Variables


Geriatrics






Pregnancy and Lactation




• Category C: No reports have described congenital anomalies or adverse effects associated with the use of corticosteroids during pregnancy. The use of group I through III corticosteroids in large amounts and with occlusive dressings for long periods of time has been shown to cause fetal abnormalities in animals, although none have been documented in humans.


• There is a significant association of fetal growth restriction with maternal exposure to potent/very potent topical corticosteroids, but not with mild/moderate topical corticosteroids.


• Effects on lactation are not known.


• Corticosteroids absorbed systemically can be detected in breast milk in quantities that are not likely to affect the infant.


• Use with caution.


• These drugs should not be applied to the nipples prior to nursing.




Specific Drugs


All Drugs in Class








Adverse Effects






Immunosuppressive Drugs


Specific Drugs



pimecrolimus (Elidel), tacrolimus (Protopic)













Treatment Principles




• Appropriate drug selection depends on diagnosis and culture whenever possible.


• Prolonged use of any of these topical agents may result in overgrowth of nonsusceptible organisms.


• Systemic antibiotics are needed for diffuse impetigo, cellulitis, and other more-than-superficial infections. Apply gauze dressing if indicated.


• Treatment should be reevaluated if no improvement is seen in 3 to 5 days (Table 13-3).


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Jul 22, 2016 | Posted by in PHARMACY | Comments Off on Dermatologic Agents

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