NEUROSENSORY

(EYES & SKIN)

PHARMACOLOGY
dr. RAHMA TRILIANA, S.Ked., M.Kes., PhD
13 April 2018
 BASIC CONCEPT OF
PHARMACOLOGY
Drugs Input or

Storage &

Inactivation &
A-D-M-E

Mechanism of Drugs Actions

Window Therapy Drug effects

 DRUGS INPUT
• Determined by :
• Drugs properties (solubility, ionization)
• Therapeutic objectives (rapid onset, long-
term treatment, restriction of delivery to a
local site).
• Routes of administration
• Enteral
• Oral (Enteric-coated preparations &
Extended-release preparations)
• Sublingual/buccal
• Parenteral
• Intravenous (IV)
• Intramuscular (IM)
• Subcutaneous (SC) & Intracutaneus (IC)
• OTHERS
• Oral inhalation
• Nasal inhalation
• Intrathecal/intraventricular
• Topical
• Transdermal
• Rectal
 PROs & CONs of DRUGS
ROUTES OF ADMINISTRATION
 OCULAR
PHARMACOLOGY
 EYE BALL

ANATOMY &
HISTOLOGY
ANATOMY OF LACRYMAL SYSTEM
Autonomic
Innervation
By
Sympathetic
(a) & Para-
sympathetic
(b) Nervous
Systems.
ROUTE FOR EYE INJECTION
 Ocular Routes of Drug Administration
ROUTE ABSORPTION SPECIAL UTILITY LIMITATIONS & PRECAUTIONS
PATTERN
Topical Prompt, depending Convenient, Compliance, corneal and
on formulation economical, conjunctival toxicity, nasal
relatively safe mucosal toxicity, systemic side
effects from nasolacrimal
absorption
Subcon- Prompt or Anterior segment Local toxicity, tissue injury, globe
junctival, sustained, infections, Perforation, optic nerve trauma,
sub-Tenon's, & depending on posterior uveitis, central retinal artery and/or vein
formulation cystoid macular occlusion, direct retinal drug
retrobulbar
edema toxicity with inadvertent globe
injections perforation, ocular muscle
trauma, prolonged drug effect
Intraocular Prompt Anterior segment Corneal toxicity, intraocular
(intracameral) surgery, infections toxicity, relatively short duration
injections of action
Intravitreal Absorption Endophthalmitis, Retinal toxicity
injection or circumvented, retinitis, age-
device immediate local related macular
effect, potential degeneration
sustained effect
Absorption
pathways of an
ophthalmic drug
following topical
application to the
eye.
Solid black arrows  corneal
route
Dashed blue arrows 
conjunctival/scleral route
Black dashed arrow 
nasolacrimal absorption
pathway.
 COMMON
DRUGS FOR SKIN
DISEASES
AUTONOMIC PHARMACOLOGY
ADRENERGIC REC. CHOLINERGIC REC.
TISSUE
SUBTYPE RESPONSE SUBTYPE RESPONSE
Corneal epithelium 2 Unknown Ma Unknown

Corneal endothelium 2 Unknown Undefined Unknown

Iris radial muscle 1 Mydriasis

Iris sphincter muscle M3 Miosis

Trabecular meshwork 2 Unknown

Aqueous
Ciliary epithelium 2/2 production
Accommo
Ciliary muscle 2 Relaxation M3
dation
Lacrimal gland 1 Secretion M2, M3 Secretion

Retinal pigment H2O transport/

epithelium 1/2 unknown
 Effects of Pharmacological
Agents on the Pupil
CLINICAL DRUG PUPILLARY
SETTING RESPONSE
Normal Sympathomimetic drugs Dilation (mydriasis)

Normal Parasympathomimetic drugs Constriction (miosis)

Horner's syndrome Cocaine 4-10% No dilation

Preganglionic Horner's Hydroxyamphetamine 1% Dilation

Postganglionic Hydroxyamphetamine 1% No dilation

Horner's

Adie's pupil Pilocarpine 0.05-0.1%a Constriction

Normal Opioids (oral or intravenous) Pinpoint pupils

Anisocoria Evaluation Flowsheet
 Topical Antibacterial for Ophthalmic Use
GENERIC NAME FORMULATIONa INDICATIONS FOR USE
Azithromycin 1% solution Conjunctivitis
Bacitracin 500 units/g ointment Conjunctivitis, blepharitis, keratitis, keratoconjunctivitis, corneal ulcers,
blepharoconjunctivitis, meibomianitis, dacryocystitis

Besifloxacin 0.6% suspension Conjunctivitis

Chloramphenicol 1% ointment Conjunctivitis, keratitis
Ciprofloxacin 0.3% solution; Conjunctivitis, keratitis, keratoconjunctivitis, corneal ulcers, blepharitis,
hydrochloride 0.3% ointment blepharoconjunctivitis, meibomianitis, dacryocystitis

Erythromycin 0.5% ointment Superficial ocular infections; prophylaxis of ophthalmia neonatorum

Gatifloxacin 0.3% solution Conjunctivitis

Gentamicin sulfate 0.3% solution; Conjunctivitis, blepharitis, keratitis, keratoconjunctivitis, corneal ulcers,
0.3% ointment blepharoconjunctivitis, meibomianitis, dacryocystitis

Levofloxacin 0.5% solution Conjunctivitis

Levofloxacin 1.5% solution Corneal ulcers
Moxifloxacin 0.5% solution Conjunctivitis
Ofloxacin 0.3% solution Conjunctivitis, corneal ulcers
Sulfacetamide sodium 1%, 10%, 15%, and 10% Conjunctivitis, other superficial ocular infections
ointment
Polymyxin B combi. Solutions & ointments Conjunctivitis, blepharitis, keratitis
c
 Antiviral Agents for Ophthalmic Use
GENERIC NAME ROUTE INDICATIONS FOR USE
Trifluridine Topical (1% solution)
Herpes simplex keratitis and
keratoconjunctivitis
Acyclovir Oral, intravenous (200-mg Herpes zoster ophthalmicusa
capsules, 400- and 800-mg Herpes simplex iridocyclitis
tablets)
Valacyclovir Oral (500- and 1000-mg Herpes simplex keratitisa
tablets) Herpes zoster ophthalmicusa
Famciclovir Oral (125-, 250-, and 500-mg Herpes simplex keratitisa
tablets) Herpes zoster ophthalmicusa
Foscarnet Intravenous Cytomegalovirus retinitis
Intravitreala
Ganciclovir Intravenous, oral Cytomegalovirus retinitis
Intravitreal implant
Valganciclovir Oral Cytomegalovirus retinitis
Cidofovir Intravenous Cytomegalovirus retinitis
 Antifungal Agents for Ophthalmic Use
DRUG AGENT ADMINISTRATION INDICATIONS FOR USE
Amphotericin B 0.1-0.5% (most 0.15%) Yeast - fungal keratitis & endophthalmitis
topical solution
0.8-1 mg subconjunctival Yeast - fungal endophthalmitis
5-g intravitreal injection Yeast - fungal endophthalmitis
Intravenous Yeast -fungal endophthalmitis
Natamycin 5% topical suspension Yeast - fungal blepharitis, conjunctivitis,
keratitis
Fluconazole Oral, intravenous Yeast keratitis – endophthalmitis
Itraconazole Oral Yeast - fungal keratitis & endophthalmitis
Ketoconazole Oral Yeast keratitis & endophthalmitis
Miconazole 1% topical solution Yeast - fungal keratitis

5-10 mg subconjunctival Yeast - fungal endophthalmitis

10-g intravitreal injection Yeast -fungal endophthalmitis
 Autonomic Drugs for Ophthalmic Use
DRUG CLASS FORMULATION INDICATIONS OCULAR SIDE EFFECTS
Cholinergic agonists
Acetylcholine 1% solution Miosis in surgery Corneal edema
Carbachol 0.01-3% solution Miosis in surgery, Corneal edema, miosis, induced
glaucomaa myopia, decreased vision, brow
ache, retinal detachment
Pilocarpine 0.5%, 1%, 2%, 4%, & Glaucoma Same as for carbachol
6% solution; 4% gel
Anticholinesterase agents
Echo- 0.125% solution Glaucoma, Retinal detachment, miosis,
thiophate accommodative cataract, pupillary block
esotropia glaucoma iris cysts, brow ache,
punctal stenosis .
Muscarinic antagonists
Atropine 0.5%, 1%, and 2% Cycloplegia, mydriasis,b Photosensitivity, blurred vision
solution; 1% cycloplegic
ointment retinoscopy,a dilated
funduscopic exam
Scopolamine 0.25% solution Cycloplegia, mydriasisb Same as for atropine
Homatropine 2% and 5% solution
Cyclo- 0.5%, 1%, & 2%
pentolate solution
Tropicamide 0.5% & 1% solution
 Autonomic Drugs for Ophthalmic Use
DRUG CLASS FORMULATION INDICATIONS OCULAR SIDE EFFECTS
Sympathomimetic Agents
Dipivefrin 0.1% solution Glaucoma Photosensitivity,
conjunctival, hyperemia
hypersensitivity
Phenylephrine 0.12%, 2.5%, and 10% Mydriasis, Same as for dipivefrin
solution vasoconstriction,
decongestion
Apraclonidine 0.5% and 1% solution Ocular
hypertension
Brimonidine 0.1%, 0.15%, & 0.2% Glaucoma, ocular
solution hypertension
Naphazoline 0.012%, 0.03%, & 0.1% Decongestant
solution
Tetrahydrozoline 0.05% solution Decongestant
 and  Adrenergic antagonists
Betaxolol 0.25% & 0.5% suspension Glaucoma, ocular
Carteolol 1% solution hypertension
Levobunolol 0.25% & 0.5% Solution
Metipranolol 0.3% solution
Timolol 0.25% & 0.5% solution
and gel
 Immuno-modulatory Drugs for
Ophthalmic Therapy
• Glucocorticoids
• Managing ocular inflammatory diseases  ocular allergy, ocular
cicatricial pemphigoid, and post-operative inflammation
following refractive, corneal, and intraocular surgery.
• Delay the wound-healing post glaucoma to reduce potential
scarring of the surgical site..
• Treatment of Retinal Disease  age-related macular
degeneration, diabetic retinopathy, & cystoid macular edema.
• Given Systemic (oral/IV to treat optic neuritis), or topical (sub-
Tenon’s capsule injection, Intravitreal injection.
• Tappering off is needed!
• Topical glucocorticoid
• Dexamethasone, Prednisolone, Fluorometholone, Loteprednol,
Medrysone, Rimexolone
Immuno-modulatory Drugs for Ophthalmic Therapy--Cont

• Nonsteroidal Anti-Inflammatory Agents (NSAID)

• Decrease postoperative inflammation
• Decrease pain after corneal refractive surgery.
• Flurbiprofen, Ketorolac, Nepafenac, Diclofenac, Bromfenac
• Prostaglandin analogs (latanoprost, bimatoprost)

• Antihistamines (AH)
• Prevents histamine & other autacoids release from mast cells
• H-1 receptor antagonists  Allergic conjunctivitis.
• Pheniramine, Andantazoline
• Topical antihistamines
• Emedastine, Difumarate, Levocabastine hydrochloride, Cromolyn
sodium, Lodoxamide tromethamine,
Immuno-modulatory Drugs for Ophthalmic Therapy--Cont
• Mast-Cell Stabilizers
• Pemirolast, Nedocromil,
• Epinastine (AH1 & AH2), Olopatadine hydrochloride, ketotifen
fumarate, and azelastine  H-1 antagonists with mast cell–
stabilizing properties.
• Immunosuppressive And Antimitotic Agents
• Prevent suture breakdown, leakage, hypotony (low IOP).
• Reduce the risk of scarring after procedures of corneal opacities
removal
• Treat certain conjunctival and corneal tumors.
• Fluorouracil and mitomycin
• Immunomodulatory Agent
• Cyclosporine  Inhibits T-cell activation  decrease
inflammatory markers in the lacrimal gland, increased tear
production, and improved vision and comfort  chronic dry eye
associated with inflammation
Drugs & Agents Used in Ophthalmic Surgery
• ADJUNCTS IN ANTERIOR SEGMENT SURGERY
• Viscoelastic substances  to maintain spaces, moving tissue, and protecting surfaces.
• Hyaluronate, chondroitin sulfate, or hydroxypropylmethylcellulose
• OPHTHALMIC GLUE
• Management of corneal ulcerations and perforations.
• Cyanoacrylate tissue adhesive, Fibrinogen glue
• CORNEAL BAND KERATOPATHY
• Edetate disodium  Chelating agent
• ANTERIOR SEGMENT GASES
• Sulfur hexafluoride, perfluoropropane gases  vitreous substitutes during retinal surgery.
• SURGICAL HEMOSTASIS
• Controlling intraocular hemorrhage during vitrectomy, minimizing bleeding, hemostasis,
inproved clotting process
• Thrombin, fibrinogen, coagulation factor, Aminocaproic acid (topical).
• THROMBOLYTIC AGENTS
• Assist evacuation of a hyphema, subretinal clot, or nonclearing vitreous hemorrhage.
• Tissue plasminogen activator(t-PA
• BOTULINUM TOXIN TYPE A
• Preventing acetylcholine release  Regulation of nicotinic cholinergic postsynaptic
receptors, aberrant regeneration of motor nerve fibers at the neuromuscular junction.
• Treatment of strabismus, blepharospasm, meige’s syndrome, spasmodic torticollis
hemifacial spasm, and facial wrinkles.
• Side effect: Temporary paralysis, diplopia, ptosis.
 Vitreous Substitutes
Function:
1) Reattachment of retina after vitrectomy,
2) Membrane-peeling procedures for complicated proliferative vitreo-
retinopathy,
3) Traction retinal detachments
SUBSTANCES CHARACTERISTICS
Nonexpansile gases
Air e.g. Argon, Carbon dioxide, Duration of 5-7 days
Helium, Nitrogen, Krypton
Xenon Duration of 1 day
Expansile gases
Sulfur hexafluoride (SF6) Duration of 10-14 days
Perfluoromethane (CF4) Duration of 10-14 days
Perfluoroethane (C2F6) Duration of 30-35 days
Perfluoropropane (C3F8) Duration of 55-65 days
Silicone oils
Nonfluorinated silicone oils Viscosity range from 1000-30,000 cs
Fluorosilicone Viscosity range from 1000-10,000 cs
"High-tech" silicone oils May terminate as trimethylsiloxy or
polyphenylmethylsiloxane; viscosity not reported
 DERMATOLOGIC
PHARMACOLOGY
DERMATOLOGIC
PHARMACOOGY
 CUTANEOUS
DRUG DELIVERY
Schematic
Diagram of
Percutaneous
Absorption
Responses of Drugs applied to the
skin determine by:
 Regional variation in drug penetration
Scrotum, face, axilla, & scalp are more permeable than forearm.
 Concentration gradient
 Concentration gradient  the mass of drug transferred per unit time
Resistance to topical drugs sometimes can be overcome  concentrations.
 Dosing schedule
Skin acts is a reservoir for many drugs  “local half-life” may permit once-
daily application of drugs with short systemic half-lives.
 Vehicles and occlusion
Appropriate vehicle maximizes drug’s ability to penetrate the skin  vehicles
physical properties itself may have important therapeutic effects.
Occlusion (application of a plastic wrap to hold the drug and its vehicle in
close contact with the skin) is extremely effective in maximizing efficacy
 Medication in Skin Diseases:
• Systemic  as regular medication
• Oral
• Parenteral (IM, IV, IC, SC)
• Topical
• Active ingredients + vehicle for cutaneous application.
• Vehicle selection depend on:
• Solubility of active agent in the vehicle
• Rate of release of agent from the vehicle
• Ability of vehicle to hydrate stratum corneum  enhance
penetration
• Stability of agent in the vehicle
• Chemical & physical interactions of the vehicle, stratum corneum, &
active agent
Dermatologic Formulations:
• Wet dressings B • Drying preparations
L • For Acute inflammation (oozing,
• Lotions O vesiculation, & crusting)
C
• Tinctures K
• Gels
E
• Aerosols V Scalp & hairy areas.
A
• Powders P
O
• Foams
R
• Pastes A
• Lubricating preparations
T
• Creams • Chronic inflammation (xerosis,
I
scaling, & lichenification)
O
• Ointments. N
 Common Vehicles for Topically Applied Drugs
CREAM OINTMENT GEL/FOAM SOLUTION/
LOTION/FOAM
Physical Oil in water Water in oil Water-soluble Solution-dissolved drug
basis emulsion emulsion base
Lotion-suspended drug
Aerosol propellant with
drug
Foam drug with
surfactant as foaming
agent and propellant
Solubilizing >31% water (up <25% water Contains May be aqueous or
medium to 80%) water- soluble alcoholic
polyethylene
glycols
Advantage Leaves Protective oil film Concentrates
concentrated on skin drug at surface
drug at skin
surface
Advantages Spreads and Spreads easily Non staining Low residue on scalp
for patient removes easily Slows water Greaseless
No greasy feel evaporation
Clear
Cooling effect + appearance
 Common Vehicles for Topically Applied Drugs
CREAM OINTMENT GEL/FOAM SOLUTION/
Dis- Needs preservatives Greasy to very Needs LOTION/
advantages greasy preservatives FOAM
Stains clothes High alcohol
can be drying
Locations on Most locations Avoid Foams well for Solutions and
body intertriginous scalp and foams are well
areas other hairy accepted on
locations scalp
Occlusion Low Moderate to high
Increases skin
moisture
Composition Requires humectants Needs surfactants Microspheres
issues (glycerine, propylene to prevent phase or
glycol, polyethylene separation microsponges
glycols) to keep moist Hydrocarbon can be
when applied (VASELINE) formulated in
Oil phase with long-chain gels
alcohol for stability and
smooth feel
Has absorption bases—
hydrophilic petrolatum
Local Cutaneous Reactions to
Topical Medications
 COMMON
DRUGS FOR SKIN
DISEASES
FOLLOW THE TIMELINE
Empirical
Use of
Systemic
Antibiotics
Based on
Etiology

Diajarkan Lebih
Detail Di blok
Tropical
Medicine
(Sem 7)
Empirical
Use of
Systemic
Antibiotics
Based on
Etiology

Diajarkan
Lebih Detail
Di blok
Tropical
Medicine
(Sem 7)
Topical Antibiotics For Skin
Infections
• BACITRACIN
• Peptide antibiotics for gram-positive organisms
• In an ointment base alone or in combination with neomycin, polymyxin B, or
both.
• Microbial resistance may develop following prolonged use.
• SE: contact urticaria syndrome, anaphylaxis, allergic contact dermatitis,
immunologic allergic contact urticarial
• Poorly absorbed through the skin  Rare Systemic toxicity.
• GRAMICIDIN
• = Bacitracin
• Alone or in combination with neomycin, polymyxin, bacitracin, and nystatin.
• ONLY in topical use, High systemic toxicity  NEVER use as systemic drugs
• Sensitization is low after topical application in therapeutic concentrations 
low allergy incidence
 Topical Antibiotics For Skin Infections-Cont
• POLYMYXIN B SULFATE
• Peptide antibiotic
• For gram-negative organisms (Pseudomonas aeruginosa, Escherichia coli,
enterobacter, & klebsiella)
• Resistant for proteus, serratia, and ALL gram-positive organisms.
• Ssolution / ointment base.
• Low systemic absroption, but total daily dose in denuded skin / open wounds should
be < 200 mg
• Neurotoxic, nephrotoxic, Local complication is rare

• MUPIROCIN
• = pseudomonic acid A
• Unrelated to any topical antibacterial agents.
• For gram-positive aerobic bacteria  specially methicillin-resistant S aureus
(MRSA)
• Treatment of impetigo by S. Aureus and β-hemolytic streptococci group A.
• Also available in Intranasal ointment & Poorly absorbed in through skin 
Systemic toxicity
 Topical Antibiotics For Skin Infections-Cont
• RETAPAMULIN
• Semisynthetic pleromutilin
• Effective for uncomplicated superficial skin infection by group A β-hemolytic streptococci
and S aureus, Not for MRSA.
• For Impetigo in adult & pediatric patients > 9 months.
• 2 x /day for 5 days.
• Well tolerated, occasional local irritation, low allergic contact dermatitis .
• NEOMYCIN
• Aminoglycoside
• For gram-negative organisms (E coli, proteus, klebsiella, enterobacter).
• >> topical formulations, alone or in combination with polymyxin, bacitracin, or other.
• Available as a sterile powder for topical use. Systemic absorption is low
• SE: nephrotoxicity, neurotoxicity, &ototoxicity, Allergic contact dermatitis (in eczematous
dermatoses or in ointment).
• Sensitization has cross-sensitivity to streptomycin, kanamycin, paromomycin, & gentamicin.
• Water-soluble excreted in urine
• GENTAMICIN
• = Neomycin
• Shows greater activity for P aeruginosa
• Can be used for staphylococci and group A β-hemolytic strepto-cocci.
• Commonly used  in a hospital environment may lead to gentamicin-resistant organisms.
• Ointment / cream.
• Detectable in serum if applied in a water-miscible preparation to large areas of denuded skin e.g.
in burned patients.
 Topical Antibiotics For Acne
• Effectiveness of topical therapy < systemic for the same antibiotic.
• Topical therapy only for mild to moderate cases of inflammatory acne
• CLINDAMYCIN
• Inhibit Propionibacterium acnes
• Alone or in combination with benzoyl peroxide, & tretinoin
• As water-based gel, & lotion < iritative than hydroalcoholic vehicle, foam formulation10% of applied dose is absorbed
• SE: bloody diarrhea, pseudomembranous colitis, drying, skin irritation, burning & stinging sensation, allergic contact
dermatitis is rare
• ERYTHROMYCIN
• Marcolide
• Inhibit Propionibacterium acnes
• Alone or in combination with benzoyl peroxide
• Erythromycin base better than salt for skin penetration. Water-based gel is less drying & better tolerated.
• Can cause antibiotic-resistant to staphylococci. If occurred  discontinued, and changed to systemic antibiotic
• SE: Burning sensation, drying, irritation of the skin. Allergic contact dermatitis is rare.
• METRONIDAZOLE
• Effective for Acne rosacea due to inhibitory effects on Demodex brevis. May have anti-inflammatory property on
neutrophil cellular function.
• Water-based gel formulation
• Carcinogenic for skin, not for pregnant & breastfeeding women, or children
• SE: dryness, burning, and stinging, NOT for region near the eyes  excessive tearing.
• SODIUM SULFACETAMIDE
• Alone as lotion or wash or in combination with sulfur for acne vulgaris & rosacea.
• Inhibit P.acnes
• Topically sulfacetamide is absorbed percutaneously
• Contraindicated in patients with known hypersensitivity to sulfonamides.
 Recommended Cutaneous
Antifungal Therapy
CONDITION TOPICAL THERAPY ORAL THERAPY
Tinea corporis, localized Azoles, allylamines —
Tinea corporis, widespread — Griseofulvin, terbinafine,
itraconazole, fluconazole

Tinea pedis Azoles, allylamines Griseofulvin, terbinafine,

itraconazole, fluconazole

Onychomycosis — Griseofulvin, terbinafine,

itraconazole, fluconazole

Candidiasis, localized Azoles —

Candidiasis, widespread and — Ketoconazole, itraconazole,
mucocutaneous fluconazole

Tinea versicolor, localized Azoles, allylamines

Tinea versicolor, widespread — Ketoconazole, itraconazole,
fluconazole

Systemic therapy is needed for tinea capitis or follicular-based fungal

infections or in widespread cutaneous fungal infections.
 Antiviral in Skin Diseases
• Common viral infections of the skin:
• Verrucae (human papillomavirus [HPV]),
• Herpes simplex virus (HSV)
• Condyloma acuminatum (HPV),
• Molluscum contagiosum (poxvirus),
• Chicken pox (varicella-zoster virus [VZV]).
• Systemic Antiviral
• Acyclovir, famciclovir, & valacyclovir  HSV and VZV
• Cidofovir  acyclovir-resistant HSV or VZV and other cutaneous viral
infections
• Immune response modifier, Interferons refractory / recurrent warts
• Topical antiviral
• Acyclovir, docosanol, and penciclovir  treating mucocutaneous HSV.
• Podophyllin (25% solution) & podofilox 0.5% solution  condylomata.
Agents Used to Treat Infestations
• Infestations by ectoparasites  lice & scabies  disabling pruritus, secondary
infection, transmission of life-threatening illnesses (body louse)
• PERMETHRIN
• Synthetic pyrethroid  interferes with sodium transport proteins  neurotoxicity &
paralysis of parasites.
• Resistance in Cimex (bed bugs) & other insects  mutations of transport protein.
• Modeled after the natural insecticide in Chrysanthemum cinerariifolium.
• OK for > 2 months old infant,
• Scabies  5% cream
• Lice:
• Pyrethrins + piperonyl butoxide (lotion, gel, shampoo, and mousse)
• KLOUT shampoo (acetic acid + isopropanol).
• 1% cream / cream rinse, solutions for lice.
• LINDANE
• Hexachlorocyclo-hexane / organochloride compound  neuronal hyperstimulation
& paralysis of parasites.
• Neurotoxic in humans  2nd-line drug for pediculosis & scabies
• NOT for premature infants, patients with seizure disorders, children < 10 y.o, adults
weighing <110 pounds, or patients with skin disorders such as atopic dermatitis and
psoriasis
• Limited for single application.
 Agents Used to Treat Infestations
• MALATHION
• Organophosphate  bind acetylcholinesterase in lice  paralysis & death
• For head lice in children > 6 years of age.
• Formulation contains alcohol  flammable.
• For lice  5% lotion
• Inhibits closure of respiratory spiracles  obstruction of spiracles by vehicles 
lice asphyxiate. Less likely to cause resistance than traditional pesticides.
• IVERMECTIN
• Oral anthelmintic drug  effective for scabies and lice.
• Does not cross human blood-brain barrier of humans  no major CNS toxicity.
• SE: dizziness, somnolence, vertigo, tremor.
• Scabies and lice  ivermectin 200 g/kg, repeated in 1 week.
• Not for children weighing <15 kg.
• OTHER:
• Less effective  10% crotamiton cream and lotion,
• Sulfur (Extemporaneously compounded 5% precipitated sulfur in petrolatum
base)  for pregnancy or nursing mothers
• Use when lindane or permethrin is contraindicated.
ANTI-INFLAMMATORY
AGENTS
 Relative Efficacy of Some Topical
corticosteroids in various formulations
 Dermatologic
disorders ranked in
order of sensitivity
to Topical
Corticosteroids
 Agents for Treatment of Pruritus
• Pruritoceptive Pruritus: due to inflammation or other cutaneous
disease
• Emollients—Repair of barrier function
• Coolants (menthol, camphor, calamine)—Counter-irritants
• Capsaicin—Counter-irritant
• Antihistamines—Inhibit histamine-induced pruritus
• Topical steroids—Direct anti-pruritic and anti-inflammatory effects
• Topical immunomodulators—Anti-inflammatories
• Phototherapy—  mast cell reactivity and anti-inflammatory effects
• Thalidomide—Anti-inflammatory via suppression of TNF-
• Neuropathic Pruritus: due to disease of afferent nerves
• Carbamazepine—Block synaptic transmission & inhibit sodium channels
• Gabapentin—Suppresses neuronal hyperexcitability, inhibit voltage-
dependant calcium channels
• Topical anesthetics (EMLA, benzocaine, pramoxine)—Inhibit nerve
conduction via decreased nerve membrane permeability to sodium
 Agents for Treatment of Pruritus
• Neurogenic Pruritus: due to changes in the nervous system without
evidence of neural pathology
• Thalidomide—Central depressant
• Opioid-receptor antagonists (naloxone, naltrexone)— opioidergic tone
• Tricyclic antidepressants—Decrease pruritus signaling through alteration
in neurotransmitter concentrations
• Selective serotonin reuptake inhibitors (SSRIs)—Decrease pruritus signaling
through alteration in neurotransmitter concentrations

• Psychogenic Pruritus: due to psychological illness

• Anxiolytics (alprazolam, clonazepam, benzodiazepines)—Relieve stress-
reactive pruritus
• Antipsychotic agents (chlorpromazine, thioridazine, thiothixene,
olanzapine)—Relieve pruritus with impulsive qualities
• Tricyclic antidepressants—Relieve depression and insomnia related to
pruritus
• SSRIs—Relieve pruritus with compulsive qualities
ANTISEBORRHEA AGENTS
 Photochemotherapy Methods
PUVA PHOTODYNAMIC PHOTOPHERESIS
THERAPY
Target Broad cutaneous area Focal cutaneous sites Peripheral blood
leukocytes
Photosensitizing Methoxsalen, Trioxsalen Protoporphyrin IX Methoxsalen
agent Bergapten
Method of drug Oral, Topical lotion Topical cream or To isolated plasma
administration Bath water solution of a prodrug within photopheresis
device
FDA-approved Psoriasis Vitiligo Actinic keratosis Cutaneous T-cell
indications lymphoma
Act.wavelength UVA2 (320-340 nm) 417 nm and 630 nm UVA2 (320-340 nm)
Adverse effects Phototoxic reactions Phototoxic reactions Phototoxic reactions
(acute) Pruritus, Hypertrichosis Temporary GI disturbance
GI or CNS disturbance, dyspigmentation Hypotension
Bronchoconstriction Congestive heart
Hepatic toxicity failure
Retinal damage
Adverse Photoaging Potential scarring Loss of venous access
effects(chronic) Nonmelanoma skin ca after repeated
Melanoma, Cataracts venipuncture
Pregnancy Cb Cb FDA unrated
 KERATOLYTIC & DESTRUCTIVE
AGENTS
• Cause irritation to skin  Keratolytics
• SALICYLIC ACID
• PROPYLENE GLYCOL
• PODOPHYLLUM RESIN & PODOFILOX
• UREA
• SINECATECHINS
• FLUOROURACIL
• NONSTEROIDAL ANTI-INFLAMMATORY DRUGS
• AMINOLEVULINIC ACIDS
 AGENTS AFFECTING
PIGMENTATION
• Whitening lotion  reduce pigmentation
• Inhibition of enzyme tyrosinase  interfere with the
bio-synthesis of melanin.
• Hydroquinone
• Monobenzone
• Mequinol  Irreversible Depigmentation
• Repigmentation  vitiligo treatment
• Trioxsalen
• Methoxsalen
• Long Wave UV ight (UVA)
 AGENTS TO TREAT ACNE
• RETINOIC ACID & DERIVATIVES
• Tretinoin
• Adapalene  0.1% gel, cream, lotion, 0.3% gel.
• Tazarotene
• ISOTRETINOIN
• BENZOYL PEROXIDE
• AZELAIC ACID
 TRICHOGENIC &
ANTITRICHOGENIC AGENTS
• For alopecia androgenic or Alopecia areata
• Have anti-testosterone ability  feminization &
gynecomastie
• MINOXIDIL
• FINASTERIDE
• BIMATOPROST
• EFLORNITHINE