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NAMA : Susiyanti Basri

NIM : 012221038

A. Dermatology Pharmacology

1. Drungs applied to the skin :


- Regional variation in drug penetration: Daerah kulit
mempengaruhi penetrasi obat
Mis : kulit scrotum, muka, axilla dan scalp lebih permeabel
dibanding kulit lengan, sehingga membutuhkan obat yang
lebih sedikit Untuk menghasilkan efek yang sama (equivalent)
- Concentration gradient:
Peningkatan gradient konsentrasi akan meningkatkan transfer
massa obat per satuan waktu
- Dosing schedule:
Sifat fisik kulit  reservoir obat mempengaruhi half life : half
life pendek bisa lebih memanjang
Mis : kortikosteroid cukup efektif diberikan 1 x sehari, dimana
pada kondisi Lain diberikan beberapa kali
- Vehicles :
Vehicles memaksimalkan kemampuan obat .

2. Penggunaan topikal :
 Kandungan bahan aktif dalam vehicle memfasilitasi aplikasi ke
kulit :
- Kelarutan bahan aktif dalam vehicle
- Kecepatan lepasnya bahan aktif dari vehicle
- Kemampuan vehicle membasahi stratum corneum
meningkatkan penetrasi
- S agen terapi dalam vehicle
- Interaksi secara kimia dan fisika dari vehicle dengan stratum
corneum dan bahan aktif obat
 Formulasi obat kulit sesuai dengan vehicle, diklasifikasikan sbb :
- Tincture, wet dressings, lotions, gels, aerosols, powders,
pastes, creams, and ointments
 Kemampuan vehicle mencegah evaporasi / penguapan obat
kulit :
- Tinctures, wet dressings > ointments
 Inflamasi akut dengan oozing, vesikulasi dan crustae baik
diterapi dengan bentuk kering seperti tincture. Wet dressing dan
lotions
 Inflammation kronis dengan xerosis, scaling, dan lichenification,
diterapi dengan bentuk sediaan preparat lubrikan seperti cream
dan ointment
 Tincture, lotions, gels, and aerosols scalp dan area berambut
 Emulsified vanishing type creams intertriginous areas tanpa
maserasi
 Emulsifying agents are used to provide homogeneous, stable
preparations Antibakter

3. Antibakteri
a. Preparant antibakteri topikal
 mencegah infeksi pada luka bersih.
 Terapi awal infeksi dermatosis
 Mengurangi kolonisasi staphylococci pada nares,
deodorisasi axila dan penatalak-sanaan jerawat
b. Bacitracin & Gramicidin
 Indikasi : bakteri gram positif :

Streptococci, pneumococci, and staphylococci, sebagian


besar anaerobic cocci, neisseriae, tetanus bocilli dan
diphtheria bacilli

Ointment : tunggal atau kombinasi dengan neomycin,


polymixin B

Penggunaan lama  resisten Efek samping : urtikaria 


anafilaksis jarang kontak dermatitis

Absorbsi melalui kulit sedikit, toksisitas sistemik jarang

Sediaan :
Penggunaan topikal. Kombinasi dengan neomycin,
polymyxin, bacitracin dan nystatin Penggunaan topikal
terbatas karena ada toksisitas sistemik. Sensitisasi
penggunaan topikal jarang

Polymyxin B Sulfate Indikasi :


Kuman Gram-negative : Pseudomonas aeruginosa,
Escherichia coli, enterobacter, and klebsiella. Gram
positif resisten
Preparat topikal : bentuk larutan atau ointment
Neomycin & Gentamicin
Topical Antibiotics in Acne Clindamycin
Erythromycin Metronidazole
Sodium Sulfacetamide

4. Anti Jamur
- Superficial fungal infections caused by dermatophytic
fungi
- Terapi topikal :clotrimazole, miconazole, econazole,
ketoconazole,oxiconazole, sulconazole, Ciclopirox
olamine, naftifine, terbinafine dan tolnaftate
- Terapi oral :griseofulvin, terbinafine, ketoconazole,
fluconazole, and itraconazole

a. Superficial candida species :


Topikal :
- Clotrimazole, miconazole, econazole,
ketoconazole, oxiconazole, ciclopirox olamine,
nystatin atau amphotericin B.
- Chronic generalized mucocutaneous candidiasis is
responsive to long-term therapy with oral
ketoconazole.
b. Topical Antifungal Preparations
Topical Azole Derivatives Ciclopirox Olamine Naftifine &
Terbinafine Butenafine. Tolnaftate. Nystatin &
Amphotericine B
c. Oral Antifungal agents
Oral azole derivatives, Griseofulvin, Terbinafine, Nystatin
and amphotericin B

5. Nystatin and Amphotericin B


- Nystatin and amphotericin B are useful in the topical therapy of
C albicans infections but ineffective against dermatophytes.
- Nystatin is limited to topical treatment of cutaneous and mucosal
candida infections because of its narrow spectrum and
negligible absorption from the gastrointestinal tract following oral
administration.
- Amphotericin B has a broader antifungal spectrum and is used
intravenously in the treatment of many systemic mycoses
- Adverse effects associated with oral administration of nystatin
include mild nausea, diarrhea, and occasional vomiting.
- Topical application is nonirritating, and allergic contact
hypersensitivity is exceedingly uncommon.
- Topical amphotericin B is well tolerated and only occasionally
locally irritating. Hypersensitivity is very rare. The drug may
cause a temporary yellow staining of the skin,

B. TOPICAL ANTIVIRAL AGENTS


1. herpez simplex
Acyclovir, Valacyclovir, Penciclovir, & Famciclovir
Ectoparasiticides Penyakit scabies
Permethrin, Lindane (hexachlorocyclohexane) Crotamiton, Sulfur
Malathion
2. Permethrin

Permethrin is neurotoxic to Pediculus humanus, Pthirus pubis, and


Sarcoptes scabiei.

Less than 2% of an applied dose is absorbed percutaneously. Residual


drug persists up to 10 days following application.

It is recommended that permethrin 1% cream rinse (Nix) be applied


undiluted to affected areas of pediculosis for 10 minutes and then
rinsed off with warm water.

For the treatment of scabies, a


Single application of 5% cream (Elimite) is applied to the body from the
neck down, left on for 8–14 hours, and then washed off.

Adverse reactions to permethrin include transient burning, stinging, and


pruritus. Cross-sensitization to pyrethrins or chrysanthemums may
occur.

3. Agents Affecting Pigmentation


 Hydroquinone & Monobenzone
- Reduce hyperpigmentation of the skin. Topical
hydroquinone  temporary lightening,
Monobenzone  irreversible depigmentation.
- Mechanism of action  inhibition of the enzyme
tyrosinase, interfering with the biosynthesis of
melanin.
- Monobenzone may be toxic to melanocytes,
resulting in permanent depigmentation
Hydroquinone and monobenzone may cause local
irritation and allergy
 Trioxsalen & Methoxsalen  psoralen
- Repigmentation of depigmented macules of vitiligo
- The major long-term risks of psoralen
photochemotherapy are cataracts and skin cancer.
 Sunscreens
- Topical medications useful in protecting against
sunlight contain either chemical compounds that
absorb ultraviolet light, called sunscreens
- Opaque materials such as titanium dioxide that
reflect light, called sunshades
- The three classes of chemical compounds most
commonly used in sunscreens :
- P-aminobenzoic acid (PABA) and its esters
benzophenones, dibenzoylmethanes.
 Drugs for Psoriasis
Acitretin
- Tidak boleh untuk orang hamil – tidak boleh jadi
donor darah
 Tazarotene Calcipotriene

4. Antiinflamasi Kortikosteroid
 ermatologic Disorders Responsive to Topical
Corticosteroids Ranked in Order of Sensitivity.
- Very responsive
- Atopic dermatitis
- Seborrheic dermatitis
- Lichen simplex chronicus
- Pruritus ani
- Later phase of allergic contact dermatitis
- Later phase of irritant dermatitis
- Nummular eczematous dermatitis
- Stasis dermatitis
- Psoriasis, especially of genitalia and face
 Less responsive
Discoid lupus erythematosus
Psoriasis of palms and soles
Necrobiosis lipoidica diabeticorum
Sarcoidosis
Lichen striatus
Pemphigus
Familial benign pemphigus
Vitiligo
Granuloma annulare
 Least responsive: intralesional injection required
- Keloids
- Hypertrophic scars
- Hypertrophic lichen planus
- Alopecia areata
- Acne cysts
- Prurigo nodularis
- Chondrodermatitis nodularis chronica helicis
 Adverse Effects
All absorbable topical corticosteroids possess the potential to suppress the pituitary-
adrenal axis
Penggunaan topikal yang lama pada anak  growth retardation
Adverse local effects of topical corticosteroids :
Atrophy, which may present as depressed, shiny, often wrinkled “cigarette paper”-
appearing skin, tendency to develop purpura and ecchymosis; steroid rosacea, with
persistent erythema, pustules, and papules in central facial distribution; perioral
dermatitis, steroid acne, alterations of cutaneous infections, hypopigmentation and
increased intraocular pressure; and allergic contact dermatitis.

Keratolytic & Destructive Agents


Salicylic Acid
Mekanisme kerja belum jelas. Obat melarutkan protein di permukaan sel  sehingga
stratum corneum intak deskuamasi “keratotic debris”.
Salicylic acid is keratolytic in concentrations of 3–6%.
In concentrations greater than 6%, it can be destructive to tissues
Efek samping :
Penggunaan topikal local irritation, acute inflammation, and even ulceration with
the use of high concentrations of salicylic acid

Propylene Glycol
Propylene glycol effective keratolytic agent for the removal of hyperkeratotic debris.
Efek samping : iritasi, orang dengan dermatitis eksim sensitif

Antipruritic Agents
Doxepin
Mekanisme belum jelas  diduga antihistamin H1 dan H2 dan efek antikolinergik
Efek amping : rasa terbakar Kontraindikasi : glaukoma, retensi urin

Pramoxine
Antiseborrhea Agents
Table : Antiseborrhea Agents.
Betamethasone valerate foam (Luxiq) Chloroxine shampoo (Capitrol)
Coal tar shampoo (Ionil-T, Pentrax, Theraplex-T, T-Gel) Fluocinolone acetonide
shampoo (FS Shampoo) Ketoconazole shampoo (Nizoral)
Selenium sulfide shampoo (Selsun, Exsel)
Zinc pyrithione shampoo (DHS-Zinc, Theraplex-Z)
Antibacterials; These medicines, includingmupirocin or clindamycin, are often used
to treat or prevent infection.

Anthralin (Drithocreme, Micanol, and others): These drugs, though not often used,
help to reduce inflammation and can help treat psoriasis.
Salicylic acid: This drug is sold in lotions, gels, soaps, shampoos, and patches.
Salicylic acid is the active ingredient in many skin care products for the treatment of
acne and warts.
Some common oral treatments for skin conditions include:

Benzoyl peroxide: Creams and other products containing benzoyl peroxide are used
to treat acne.

Coal tar: This topical treatment is available with and without a prescription, with
strengths ranging from 0.5% to 5%. Coal tar is used to treat conditions including
Seborrheic dermatitis (usually in shampoos) or psoriasis. Currently, coal tar is
seldom used because it can be slow acting and can cause severe staining of
personal clothing and bedding.

Antifungal agents: Terbinafine, clotrimazole, and ketoconazole are a few examples


of common topical antifungal drugs used to treat skin conditions such asringworm
and athlete’s foot.

Corticosteroids: These are used to treat skin conditions including eczema.


Corticosteroids come in many different forms including foams, lotions, ointments,
and creams.

Retinoids: These medications (such as Retin-A and Tazorac) are gels or creams
derived from vitamin A and are used to treat conditions
Including acne. Contraindication : pregnant

Antibiotics: Oral antibiotics are used to treat many skin conditions. Common
antibiotics
Include erythromycin, tetracycline, and dicloxacillin.
Antifungal agents: Common oral antifungal drugs
Include ketoconazole and fluconazole. These drugs can be used to treat more
severe fungal infections.

Antiviral agents: Common antiviral agents include valacyclovir, acyclovir, and


famciclovir. Antiviral treatments are used for skin conditions including those related
To herpes.

Corticosteroids: These medications, including prednisone, can be helpful in treating


skin conditions linked to autoimmune diseases including vasculitis and inflammatory
diseases such as eczema. Dermatologists prefer topical steroids to avoid side
effects; however, short-term use of prednisone is sometimes necessary.

Immunosuppressants: Immunosuppressants, such


As azathioprine andmethotrexate, can be used to treat conditions including severe
cases of psoriasis and eczema.

Biologics: These new therapies are the latest methods being utilized to treat
psoriasis and other conditions. Examples of biologics
Include Enbrel, Humira, Remicade, and Stelara.

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