1/2 - Creams, Ointments & Transdermal Products Theory Flashcards
Functions of the skin
DRY SKIN
Impedes Electrical Current
ELECTRICAL BARRIER
What type of steroid?
used for atopic dermatitis / severe dermatitis
xerotic/nummular eczema
lichen sclerosis
SCABIES
Moderate Steroids
5-4-3
Topical Antiseptic, Antibiotics, or Disinfectant?
Bacitracin + Polymyxin + NEOMYCIN
BPN
USA triple antibiotic =
NEOSPORIN
broad category
may be applied topically, but have
SYSTEMIC EFFECTS (enter skin)
usually through lymphatic transport when applied topically
Anti-BIOTICS
Steroid Class? / Allergy Group?
Triamcinolone Acetonide
0.025%
0.1% - Cream/lotion vs OINTMENT
0.5%
“Ace-Bounce”
ALL Allergy group B -
6-5v4-3
6
5 v 4
3
Moisturizer for SENSITIVE skin
Moisturizers hold water in the outermost layer of skin
temporary barrior, usually contain combo of humectants + Emollients
SHOULD NOT CONTAIN
ACIDS / Fragrances + Dyes
SHOULD contain
Soothing agents = Aloe / Chamomile
Topical Antiseptic, Antibiotics, or Disinfectant?
Hydrogen Peroxide 3-6%
- DO NOT ADVICE*
- less preferable than GENTLE HAND WASHING*, can induce scarring / delay healing
Phenol & Related Phenolics
Thymol / tricolsan* - rmoved
many of these products had endocrine effects or allergenic
ANTISEPTICS
not generally adviced to use tho
salty ikky sweat, ikky=eccy
SALTY sweat glands
About 99% water, pH of 5
Concentrated in Palms & Soles
Functions as heat control for humans and MOST animals (not in hooved animals)
<1/10000 of total surface area
ECCRINE
Sweat Glands
Topical Antiseptic, Antibiotics, or Disinfectant?
Silver Sulfadiazine
sulfa drug to prevent infection in BURNS
Benzoyl Peroxide +/- Clinda or Erythromycin
treat ACNE, gram POSITIVE propionibacterium acne
TOPICAL ANTIBIOTICS
REMOVE SKIN/HAIR
Thioglycolate breaksdown Di-sulfide bonds in keratin
Hair is weakened, making it easier to slough off
DEPILATORIES
THIOGLYCOLATE
1 of 3 active ingredients in SUNSCREENS
NEWER agens mainly in Europe / Australia / Japan
not in USA
Designed to improve UVA BLOCKING
longer wave length ~320-400nm
does not protect SUNBURN, but does prevent long term skin dmg –> photodermatitus / melanoma
UV-Absorbing
COLLOIDAL SOLIDS
Outer most layer of the skin
Stratum Corneum
Barrier layer, comprimised primarily of keratin protein
10um in thickness
MOSTLY DEAD TISSUE
What type of steroid?
Utilized for thin-skinned / sensitive areas
especially areas under occlusion
armpit / groin / buttock / breast folds
Weaker TOPICAL Steroids
7-6-5
Type of Semi-Solid - topical dosage form
Hydrocarbon-based, with dissolved or suspended drugs
addition of high melting waxes to liquid mineral oil or petrolatum
addition of polyetheline into mineral oil
OINTMENTS
Adv: excellent moisturizing materials, adhesive, hard to remove, good vehicles for dry skin
DisAdv: greasy, may stain, not good solvents -> lessen drug availability
Functions of the skin
4.2 - 5.6 pH
of acid mantle is low enough to be BACTERIOSTATIC
MICROBIAL BARRIER
Topical Antiseptic, Antibiotics, or Disinfectant?
Bacitracin + Polymyxin + GRAMICIDIN
BPG
Canadian TRIPLE ANTIBIOTIC
- polysporin complete*
- has gramicidin instead of neomycin*
Topical Antiseptic, Antibiotics, or Disinfectant?
Sodium Chloride
HIGH concentrations >> 0.9% are damaging to living cells
Sodium + Calcium Hypochlorite
chlorine Bleach, useful as a DISINFECTANT, no longer used as a topical antiseptic
FIRST IS ANTISEPTIC
second was antiseptic, now just a disinfectant (non-living surfaces)
SEBUM / COMEDO
SOAP + WATER
removes sebum+acne ,
prevents formation of COMEDO
Comedo = black/whiteheads, pores that are blocked by sebum
Main Drugs that use TRANSFERMAL DELIVERY
for SYSTEMIC EFFECTS
Patches
NICOTINE / NITROGLYCERIN
Clonidine / ESTRADIOL
/ Scopalomine / FENTANYL
How are SEMISOLID dosage forms PREPARED?
-
FUSION METHOD -
- Heat to >70*C, emulsify @ HIGH temps
- Congeal upon cooling
- Creams = water phase is SLIGHTLY hotter than oil
- Heat to >70*C, emulsify @ HIGH temps
-
COLD INCORPORATION
- levigate drug INTO prepared ointment/cream base
- Importance of GEOMETRIC PROPORTIONS
- Neutrolization of carbopol genls
Steroid Class? / Allergy Group?
Betamethasone DiPropionate
0.05% - diprosone vs Dermovate
C
only (di)PROPIONATE that HAS an allergy CLASS
3 / 1
Steroid Class? / Allergy Group?
Fluocinonide 0.5%
Halcinonide 0.5%
Amcinonide 0.5%
Desoximetasone 0.25%
no allergy group
2 - B
ALL Class 2 are allergy group B
ALL 0.5%
except for the non-allerrgy group desoximetasone = 0.25%
Moisturizer for MATURE / OLD skin
Moisturizers hold water in the outermost layer of skin
temporary barrior, usually contain combo of humectants + Emollients
typically Water in Oil = W/o
with PETROLATUM BASE, just like VERY DRY SKIN
but also have ANTIOXIDANTS to combat
wrinkles / prevent flaking + scaling
Steroid Class? / Allergy Group?
Fluocinolone Acetonide 0.01-0.2%
Triamcinolone Acetonide OINTMENT 0.1%
Fluradrenolide 0.05%
no allergy group
4 - B
4 is a MIX of B & D
Triamcinolone Cream/Lotion = 5, Triamcinolone OINTMENT = 4
Steroid Class? / Allergy Group?
Clobetasol Propionate 0.05%
Betamethasone Dipropionate 0.05%
Halobetasol proprionate 0.05%
Diflorasone Diacetate 0.05%
1 - D
All 1’s are D’s, MOST POTENT
up to 600x stronger thatn group 7 (hydrocortisone)
except for the 2 withought allergy groups
DRUG used to stop hair loss and promote hair growth
side effect = initial hair loss
stimulates hair follicle activity, could lead to the shedding of OLD hairs. before NEW HAIR can grow
MINOXIDIL
rogaine
Main drugs that use TRANSDERMAL DELIVERY for
LOCAL EFFECTS
extending beyond the skin
Muscle/Joint Pain Relief:
Menthol / methyl salicylate
Camphor / capsaicin
Local analgesics
Topical Antiseptic, Antibiotics, or Disinfectant?
Mupirocin
RX ONLY
Topical ANTIBIOTIC
Steroid Class? / Allergy Group?
Betamethasone Dipropionate 0.05%
3 - C
Group 3 are allergy class B D or C
ADVANTAGES
of percutaneous drug delivery
AVOIDS 1st Pass Metabolism
Avoids stability/BV issues of oral drugs
Prolonged therapy + Reduces Dose
Controlled / Convenient -> Compliance
Nocturnal Treatment
Accomodates for drug w/ short half life
How do drugs move through the skin?
D-Ni-P
Passive-Non-Ionic Diffusion
Diffusion - follows a conc gradient from high-> low
Passive - not active, NO energy
Non-Ionic - ONLY uncharged molecules can cross membranes
Absorbs or reflects some of the sun’s
UV radiation on the skin, protects against sunburn
mainly against UV-B spectrum = effective spectrum
SUNSCREEN
aka sunblock / sun tan lotion / sunburn cream / block out
type of LOTION / SPRAY / GEL / other
What type of steroid?
Used on the face / eyelids / diaper area / perianal skin
interigo of groin / body folds
Weaker Steroids
7-6-5?
Steroid Class? / Allergy Group?
Triamcinolone Acetonide Lotion/Cream 0.1%
Fluocinolone Acetonide 0.025%
Desonide OINTMENT 0.05%
Hydrocortisone Valerate 0.2%
Fluticasone propionate 0.05%
does not have an allergy class
5 - B + 1 D (Valerate)
All B except valerate (D)
mainly the same drugs, just greater strength vs class 6
Desonide OINTMENT = 6 ,desonide cream/lotion = 5
Triamcinolone Cream/Lotion = 5, Triamcinolone OINTMENT = 4
Moisturizer for NORMAL skin
Moisturizers hold water in the outermost layer of skin
temporary barrior, usually contain combo of humectants + Emollients
Oil in Water = O/W Emulsions
light-weight oily component such as cetyl alcohol o rcyclomethicone
Therapeutic Effect on the STRATUM CORNEUM (SC)
Removal of Thickened SC
lysis of covalent bonds of keratim protein
disintegration / SLOUGHING of DEAD SKIN
KERATOLYTICS
Steroid Class? / Allergy Group?
Mometasone Furoate
0.1% Cream/lotion vs Ointment
infuruoateD
D
4 / 3
Functions of the skin
Helps keep body at 37*C = 98.6*F
Vessels DILATE to cool
CONTRACT to CONSERVE
MOST HEAT IS LOSS @ THE HEAD
THERMAL BARRIER
Temperature regulating
Physical factors
that affect the DEVELOPMENT of
transdermal drug delivery systems
PROMPT onset
Adequate rate of delivery + duration
Controlled delivery, to lessen variability
lessen environmental effect
Efficient use of drug by body
Steroid Class? / Allergy Group?
Hydrocortisone Valerate 0.2%
Hydrocortisone Butyrate 0.1%
Mometasone Furoate 0.1%
4 - D
4 is a MIX of B & D
valerate is higher strength vs the class 5, still D allergy
Steroid Class? / Allergy Group?
Desonide 0.05%
Cream/Lotion vs Ointment
B
6 & 5
Type of Semi-Solid - topical dosage form
white semisolids, emulsions
only O/W, not w/o
prepared by fusion,
Higher concentration of INTERNAL PHASE –> MORE VISCOUS
CREAMS
Adv: water washable / soluble, volatile components evaporate, vanishing cream
UVA vs UVB
UVA does NOT cause sunburn
Causes longer term skin damage
Photodermatitus + Melanoma
PPD = persistent pigment darkening
rating measures UVA exposure protection from TANNING
Hydrocortisone creams & ointments
Class? / Allergy Group?
Treatment of rash / eczema / dermatitis
weakest topical steroid, poor lipid permeability for mucous membranes
THE REFERENCE
A-7
least potent
SPF
Sun Protection Factor
Measures the effectiveness of a product at blocking
UVB
SPF 15 = user wearing product can
Expose skin 15x as long as unprotected expsure
TIME BASED / COMPLEXTION OF SKIN
Classified as a COSMETIC
most are alcohol-based liquid products, some gel formulations
Contain perfume fragrances / natural essential oils inteded to MASK the odor of perspiration
corn starch + baking soda also recommended
DEODORANTS
in comparison to antipersperants**, deodorants DO NOT have Al or Zr
Broad Category
System that retain their shape until acted upon, in which they deform and deformations are permenant
Toothpaste / Ointments / Pastes / Creams (O/W)
Gels / Rigid Foams
type of topical/cutaneous dosage forms
SEMISOLIDS
Steroid Class? / Allergy Group?
Fluocinolone ACEtonide
0.01%
0.025% Cream
0.01-0.2% Ointment?
FluocinoNIDE
“Ace-Bounce”
B - 6-5-4-2
6
5
4
2
Type of Semi-Solid - topical dosage form
Emulsification of AIR or other gasses in a LIQUID PHASE
some can be “quick-breaking” –> become liquid or powder RAPIDLY
RIGID FOAMS
aerosol shaving creams / medicated foams
What type of steroid?
used for Psoriasis / severe Poison Ivy Exposure
lichen planus / discoid lupus / chapped feet
alopecia areata / nummular eczema
STRONG STEROIDS
1-2-3
Topical Antiseptic, Antibiotics, or Disinfectant?
Bacitracin + Polymyxin
BP
Polysporin
topical ANTIBIOTIC
Steroid Class? / Allergy Group?
HyDrocortisone VALERATE
0.2% Cream vs Ointment
HyDrocortisone Butyrate
hyDrocortisone, except for the OG one that is A
D
5 v 4
4
oily hairy bum, SEBum
Secrete SEBUM, oily skin lubricant
Maintains acid pH = 5 at skin surface = acid mantle
Comprises only 1/1000 of the total SURFACE AREA
SEBACEOUS GLANDS
associated with HAIR FOLLICLES
Inner-most layer of sikin
DERMIS
Primarily collagen / reticulum / elastin proteins
Semi-gel matrix of mucopolysaccharide ground substance
network of NERVES / Micro-circulation
Lymphatic circulation
Topical Antiseptic, Antibiotics, or Disinfectant?
Lower Aliphatic Alcohols
Ethanol 70-90% / isopropanol 70-80% - MORE EFFECTIVE
Quartenary Amonium surfactants
BAC / CTAB / CPC / BZT
Types of topical ANTISEPTICS
Keratolytics
for ACNE
Sulfur + Salicylic acid
ROSORCINOL
used in 5-10% in ointments for chronic skin diseases such as:
Psoriasis / Hidradenitis supporativa / ECZEMA
1 of 3 active ingredients in SUNSCREENS
Listings vary by GEOPOLITICAL region
More effective for blocking UVB
UVB = shorter wavelength, blocks the outer skin
from SUNBURN
UV-Absorbing Dissolved Substances
Transepidermal Route
Primary Route of Percutaneous Absorption
High skin permeability = good LIPID & Water Solubility
Lipid Zone - slowest, rate limiting
Stratum corneum, packed with KERATIN
drugs must transverse through lipid channels
Aqueous Zone
Pass through epidermis –> circulatory system
must diffuse through the largely aqeuous epidermal region = 99% of cross section
BIOLOGICAL Factors
that affect the DEVELOPMENT of
transdermal drug delivery systems
May see local irritation from device
Allergic skin RXNS
METABOLISM of drug in skin
Variability in system ELIMINATION
Vasoconstriction activity, further delays absorption
Favorable DRUG CHARACTERISTICS
for percutaneous drug delivery systems
POTENT, IV dose <10mg qd
Adequate Solubility in mineral oil & water, logP ~ 1
low MW, <800 amu
low melting point
PK/Pkdynamics properties well known
Moisturizer for DRY skin
Moisturizers hold water in the outermost layer of skin
temporary barrior, usually contain combo of humectants + Emollients
typically WATER IN OIL = W/O
have antioxidants / grape seed oil / dimethicone
AyPO = AyBO
Secrete MILKY SUBSTANCE** = **B-O
contains proteins / lipoproteins / lipids
Bacterial action on the secretions –> body odor
Located in axillae = armpits / anogenital regions** / **nipples
APOCRINE
SWEAT GLANDS
broad category
topical products applied to the skin to
kill harmful microorganisms
- NOT absorbed through the skin*
- can also be used as disinfectants*
Anti-SEPTICS
broad category
Steroid Class? / Allergy Group?
Triamcinolone Acetonide 0.025%
Fluocinolone Acetonide 0.01%
Desonide CREAM/LOTION 0.05%
Aclometasone Dipropionate 0.05%
does not have an allergy class
6 - B
all class 6’s are allergy group B
these are all the LOWER STRENGTH VERSIONS
same drugs/allergy group as group 5, just lower % strength
Steroid Class? / Allergy Group?
Mometasone Furoate 0.1%
3 - D
3 is a mix of BDC
Keratolytics
Salicylic Acid
Allantoin, Lactic Acid, Urea
REMOVE EXCESS DEAD SKIN ON SURACE
used to remove warts and other skin lesions
Soften keratin, improve natural moisturization
relieve dry skin
Sulfur added -> secondary treatment for dandrugg / seborrheic dermatitis
Broad Category
agents applied to NON-LIVING SURFACES
to kill microrganisms that would be harmful to living tissue
can also be an antiseptic
DISINFECTANT
Steroid Class? / Allergy Group?
Triamcinolone Acetonide 0.5%
Fluticasone propionate 0.005%
not in an allergy class
3 - B
Group 3 is one of each B / D / C
Type of Semi-Solid - topical dosage form
Clear - Whitish, but TRANSLUCENT
semisolid system w/ cross-linked polymer w/ concentration <10%, generally 0.5% to 2%
natural gums
GELS
JELLIES
Therapeutic Effect on the STRATUM CORNEUM (SC)
MOISTURIZING ABILITY
re-hydrate tissue, apply water-impermeable film
containign fatty acids + fatty acid esters
EMOLLIENCY
Topical Antiseptic, Antibiotics, or Disinfectant?
IODINE
Povidine Triiodine = Betadine, SAFER & MORE PREFERRED. delays release of iodine that promotes wound healing
Alcoholic solution** = tincture of iodine, NO LONGER RECOMMENDED for minor wounds due to **inducing scarring / delaying healing**
ANTISEPTIC
Type of Semi-Solid - topical dosage form
- like ointments* w/ HIGH concentration of *INSOLUBLE solids*
ex. Starch / ZnO / Talc
protective barrier / water impereable film
less greasy
film/ opaque
PASTES
Types of Drug Delivery systems to deliver:
LOCAL/Topical ANESTHETICS
used to numb body parts
to REDUCE PAIN & relieve ITCHING
Creams / Ointments
Aerosols / Sprays
Lotions / Gels
Percutaneous Absorption
ISSUES
NOT a frequently used route
Drug absorbed slowly
Incomplete absorption
Inefficient route
Variation in delivery
Patient Counseling for Topical Steroids
Important to counsel, excessive use –> dangerous side effects
Patient allergic to one steroid in a Group A-D are allergic to ALL OTHER STEROIDS IN THAT SAME GROUP (A-D)
if allergic:
recommend SUBSTITUTE in SAME CLASS
Middle layer of tissue
Stratum Germinativum
Viable Epidermis
Living tissue, germative layer produces more stratum germinativum
100um in thickness
Antiperspirant
or
Antiperspirant / Deodorant combintation
CLASSIFIED AS** **DRUGS
Al / Zr Salts
do chemical reversible DAMAGE to glands
Aluminum based complexes react w/ electrolytes in sweat to form a gel-plug in the duct of the sweat gland
Topical Steroids
Goal is to select the:
Least Potent (Class 1) steroid that will do that job
in the allergy Group (a-d) which the patient is not sensitive
Classified by US FDA into SEVEN CLASSES
based on POTENCY compared to Hydrocortisone = REFERENCE
1 = MOST POTENT, 7 = least potent
Also classified into FOUR GROUPS based on ALLERGY
A / B / C / D
steroids in SAME GROUP = CROSS REACTIVE, can be reactive to more than 1 group
Steroids WITHOUT Allergy Groups
Alclometasone Diproprionate 0.05%
Fluticasone Propionate 0.05% + 0.005%
Fluranderenolide 0.05%
Desoximetasone 0.25%
Halobetasol Proprionate
Diflorasone Diacetate
almost all PROP-ionates do NOT have allergy groups, exception is BETAmethasone 0.05/0.05 = class C
6
5/3
4
2
1/1
Functions of the skin
Prmarily to UV RADIATION of the sun
Role of Melanocytes to produce MELANIN to
LESSEN Burning
RADIATION BARRIER
Moisturizer for OILY skin
Moisturizers hold water in the outermost layer of skin
temporary barrior, usually contain combo of humectants + Emollients
typically OIL IN WATER = O/W
Need to be NON-COMODOGENIC = will NOT clog pores
help prevent acne recurrence
Topical Antiseptic, Antibiotics, or Disinfectant?
Boric Acid
for opthalmics, also effective against yeast
Chlorhexidine Digluconate
cationic surfactants –> surgical swags / mouthwash
ANTISEPTIC
Moisturizer for VERY DRY skin
Moisturizers hold water in the outermost layer of skin
temporary barrior, usually contain combo of humectants + Emollients
typically w/o
WATER IN OIL w/ PETROLATUM BASE
1 of 3 active ingredients in SUNSCREENS
Metals
TiO2
ZnO
Topical Antiseptic, Antibiotics, or Disinfectant?
Manuka Honey
Natural source of methylglyoxal, which has AB properties
Polyhexanide
PHMB
Octenidine Dihydrochloride
cationic surfactant with broader spectrum of AB action
ANTI SEPTIC
Containment of body fluids & Tissues
Barrier function
Receptor of external stimuli
Regulate body temperature
Synthesis and metabolism function
disposes of biochemical wastes
Sexual Attraction / Blood Pressure regulation
Skin functions
Functions of the skin
need to partition across the
STRATUM CORNEUM
via pore routes, need HIGH LIPID SOLUBILITY
and sufficient water solubility
CHEMICAL BARRIER