1/2 - Creams, Ointments & Transdermal Products Theory Flashcards by Karlo Sison

Functions of the skin

DRY SKIN

Impedes Electrical Current

ELECTRICAL BARRIER

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What type of steroid?

used for atopic dermatitis / severe dermatitis

xerotic/nummular eczema

lichen sclerosis

SCABIES

Moderate Steroids

5-4-3

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Topical Antiseptic, Antibiotics, or Disinfectant?

Bacitracin + Polymyxin + NEOMYCIN

BPN

USA triple antibiotic =

NEOSPORIN

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broad category

may be applied topically, but have

SYSTEMIC EFFECTS (enter skin)

usually through lymphatic transport when applied topically

Anti-BIOTICS

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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

5 v 4

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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

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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

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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

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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

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REMOVE SKIN/HAIR

Thioglycolate breaksdown Di-sulfide bonds in keratin

Hair is weakened, making it easier to slough off

DEPILATORIES

THIOGLYCOLATE

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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

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Outer most layer of the skin

Stratum Corneum

Barrier layer, comprimised primarily of keratin protein

10um in thickness

MOSTLY DEAD TISSUE

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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

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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

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Functions of the skin

4.2 - 5.6 pH

of acid mantle is low enough to be BACTERIOSTATIC

MICROBIAL BARRIER

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Topical Antiseptic, Antibiotics, or Disinfectant?

Bacitracin + Polymyxin + GRAMICIDIN

BPG

Canadian TRIPLE ANTIBIOTIC

polysporin complete*
has gramicidin instead of neomycin*

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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)

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SEBUM / COMEDO

SOAP + WATER

removes sebum+acne ,

prevents formation of COMEDO

Comedo = black/whiteheads, pores that are blocked by sebum

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Main Drugs that use TRANSFERMAL DELIVERY

for SYSTEMIC EFFECTS

Patches

NICOTINE / NITROGLYCERIN

Clonidine / ESTRADIOL

/ Scopalomine / FENTANYL

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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
COLD INCORPORATION
- levigate drug INTO prepared ointment/cream base
Importance of GEOMETRIC PROPORTIONS
Neutrolization of carbopol genls

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Steroid Class? / Allergy Group?

Betamethasone DiPropionate

0.05% - diprosone vs Dermovate

only (di)PROPIONATE that HAS an allergy CLASS

3 / 1

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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%

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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

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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

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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? ## Footnote **Mupirocin**

**RX ONLY** **Topical ANTIBIOTIC**

Steroid Class? / Allergy Group? ## Footnote **Betamethasone Dipropionate 0.05%**

**3 - C** ## Footnote 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)* ## Footnote 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** ## Footnote 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**

*infuruoate**D*** **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? ## Footnote **Hydrocortisone Valerate 0.2%** **Hydrocortisone Butyrate 0.1%** **Mometasone Furoate 0.1%**

**4 - D** ## Footnote 4 is a MIX of **B & D** valerate is higher strength vs the class 5, still D allergy

Steroid Class? / Allergy Group? ## Footnote **Desonide 0.05%** **Cream/Lotion vs Ointment**

**B** ## Footnote **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** ## Footnote *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-**B**ounce" **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? ## Footnote **_HyDrocortisone VALERATE_** **0.2% Cream vs Ointment** **_HyDrocortisone Butyrate_**

hy**D**rocortisone, *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**

**_DERMI_****_S_** 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 wate**r 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** ## Footnote _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? ## Footnote **Mometasone Furoate 0.1%**

**3 - D** ## Footnote 3 is a mix of BDC

**_Keratolytics_** ## Footnote **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** ## Footnote 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 **i****nducing 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_** ## Footnote **_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_**