Term
| characteristics of a good topical drug? 4 |
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Definition
low molecular mass
adequate solubility in lipid and water
high partition coefficient
hydrated corneum |
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Term
| 4 abnormalities leading to acne. |
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Definition
Hyperkeratinization (caused by androgens
Sebum production (increased by androgens)
Bacteria (p. acnes) produces lipase to form FFA
Inflammatory - FFA cause immune response |
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Term
| Name some environmental factors that can increase acne |
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Definition
mechanical irritants such as helmets and headbands.
Occlusive materials such as lotions and cosmetics that are oil based |
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Term
benzoyl peroxide
MOA?
Uses?
SE? |
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Definition
keratolytic via solubilizing cell surface proteins.
Bacteriocidial - generates free radicals to kill P. acnes
Comedolytic - results from keratolytic features
Use - Acne. often included w/ erythromycin or clindamycin
SE - irritation, erythema, bleaching, or rarely contact dermatitis |
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Term
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Definition
only keratolytic via solubilizing intercellular adhesion proteins
SE - irritation, erythema, rare salicylism |
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Term
Topical Sulfur compounds
MOA
SE |
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Definition
keratolytic and desquamative
SE - skin staining, rotten egg odor, and comedogenic w/ long term use |
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Term
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Definition
inhibits DNA synthesis in bacteria, scavenges free radicles (anti-inflammatory), and keratolytic
SE - irritation, itching, HYPOPIGMENTATION. |
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Term
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Definition
steroid type drug that binds to RARs and RXRs in nucleus, dimerize, and bind to promoters. Binds and regulates cellular proliferation and differentiation
RAR --> therapeutic effects
RXRs --> SEs. |
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Term
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Definition
Binds to RARs --> exfoliative via increasing turnover. decreases cell adhesion. Prevents new comedone formation
SE - peeling, dryness, "appearance" of worse acne, degrades in UV light --> worse SE (thus apply at night
Also has anti-wrinkle effect via vasodilation and increase collagen |
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Term
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Definition
designed for acne to specifically target pilosebacious units. Binds to RARs.
SE - same as tretinoin but less severe. |
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Term
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Definition
prodrug converted to active via esterases --> exfoliative via promoting cellular differentiation by blocking ornithine decarboxylase. Also anti-inflammatory.
SE - same as tretinoin. category X |
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Term
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Definition
all cis retinoic acid. Given orally
Corrects all 4 abnormalities in acne.
Has the best results of any drug.
SE - common: dry skin, pruritis, dry eyes, alopecia. Serious: IBD, worsening lipid profile, psychological (depression/suicide), highly sunlight sensitive, category X, pseudotumor cerebri w/ tetracyclins. |
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Term
Erythromycin
Route of administration
MOA
SE |
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Definition
macrolide antibiotic. Topical and systemic
MOA - inhibits translocation via binding of the 50s ribosome
SE - liver enzyme inhibitor |
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Term
Clindamycin
route of administration
MOA
SE |
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Definition
not a macrolide. Topical and systemic
MOA - inhibits protein synthesis via binding to 50s ribosome and inhhibiting translocation and peptidyl transferase
SE - pesudomembranous colitis. |
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Term
tetracycline
route of administration
MOA
SE |
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Definition
topical or systemic
MOA - inhibits translation of mRNA into proteins via binding 30s ribosome
SE - alters normal intestinal flora, binds to calcium -> tooth/bone effects. Decreased absorption when used w/ antacids, dairy, and iron. Photosensitization. |
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Term
Doxycycline
Route of administration
MOA
SE |
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Definition
only systemically given
MOA - same as tetracyclin
SE - increased incidence of all the tetracycline side effects |
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Term
Minocycline
route of administration
MOA
SE |
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Definition
systemic only
MOA - same as tetracycline
SE - same as tetracycline w/ lower incidence. May develop ototoxicity (vestibular effects) |
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Term
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Definition
increase sex hormone binding globulin -> decreased free testosterone --> decreased sebum and hyperkeratinization. 2-4 months for results
SE - promotes clotting, MI in smokers, stroke, breast cancer. Relapse upon stopping |
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Term
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Definition
autoimmune activated Th1 cells are re-activated by APCs in the dermis -> psoriatic plaque from chemokines released affecting keratinocytes. lack of Th17 (Treg) also contribute. Triggered by infection, drugs, trauma, UV light, hypocalcemia. Very high cell turnover rate.
thick plaques, capillary dilation --> redness, neutrophil/lymphocyte infiltration, |
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Term
Psoriasis
What drugs used to treat? |
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Definition
emollients and keratolytics - salicylic acid.
Immunosuppresants - corticosteroids, cyclosporine A, alefacept, adilimumab, stelara (ustekinumab), vit d, retinoids, methotrexate. |
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Term
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Definition
bind to cytoplasmic glucocorticoid receptors and releases HSP 90. Translates to nucleus and binds to GRE to suppress inflammatory genes (IL-1,2,6) and upregulate anti-inflammatory genes.
Very High potency flourinated GCs should not be used on the face.
SEs - potential to suppress HPA axis. Iatrogenic cushings. Topical used may cause purpura, rosacea, dermatitis, skin atrophy |
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Term
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Definition
binds to cyclophilin to become a calcineurin inhibitor that stops transcription of NF-AT -> no IL-2 production -> no T cell activation
SE - nephrotoxic (additive w/ other drugs. ex. statins), HTN, and hirsutism |
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Term
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Definition
MOA - interferes w/ APC interaction -> reduction of activated lymphocytes
Use - moderate to severe plaque psoriasis
SE - CD4 lymphocyte count can drop (monitor the levels). Discontinue if below 250. |
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Term
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Definition
monoclonal humanized antibody
MOA - binds plasma membrane bound TNF-a --> lysis of T-cells
SE - allergic reactions, lymphoma, susceptible to infections (r/o TB before prescribing) |
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Term
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Definition
a retinoid. Prodrug converted to etritinate.
MOA - not known but normalizes growth of keratinocytes
Use - moderate to severe psoriasis
SE - similar to isoretinoin, more teratogenic, very fat soluble -> wait to donate blood or get pregnant. |
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Term
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Definition
MOA - antipruritic properites via phenolic compounds. epidermal hyperplasia followed by sytostatic effect and epidermal thinning.
Use - psoriasis, dermatitis, lichen simplex chronicus
SE - irritant, odor, phototoxicity |
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Term
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Definition
MOA - vit d3 analog. ointment. inhibits keratinocyte differentation and proliferation via decreasing Th1 stimulating cytokines (IL-2)
Use - moderate plaque psoriasis
SE - burning, itching, avoid mucous membranes (esp eyes), transient hypercalcemia |
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Term
| Methotrexate use in psoriasis. SE? |
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Definition
affects the rapidly dividing cells. beneficial via anti-inflammatory effects from decreased IL-1 production and death of active T cells.
SE - hepatic fibrosis, protein bound, BM suppression, megaloblastic anemia |
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Term
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Definition
UVB - often used first. short wavelength. Can be combined w/ other agents
PUVA - long wavelength, can cause skin cancer, need to use psoralen |
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Term
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Definition
facilitates GABA and inhibits NMDA.
Depresses cardiac contractility
Relaxes fascular smooth muscle, uterine smooth muscle, hypothermia
FAEE cause baby problems and cardiac fibrosis. detected in meconium
cross tolerance to benzo and barbituates
pancreatitis, peripheral neuropathies, gynectomastia, testes atrophy, edema |
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Term
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Definition
| lowers activity of receptors for glutamate. Used to maintain abstinence. |
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Term
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Definition
inhibit NE, dopa, and serotonin reuptake.
mixed with alcohol causes resp depression, MI. Cocaethylene causes hep failure, resp depression, stops ox phos, CV collapse.
ingested --> severe bowel gangrene
fetal complications - abortion, tremors, suckling failure, mental retard, visual probs, rupture of membranes, preterm, IUGR, abruptio placentae |
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Term
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Definition
| releases dopa and NE, rapid pulse, bronchial passage relaxation.more frequent lung infection, can produce anxiety, fear, panic. hands tremble. impairs memory, recal, attention. |
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Term
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Definition
| rapid emotional swings. Stimulates pre and post synaptic serotonin receptors |
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Term
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Definition
| pupillary dilation. Increased blood pressure, hyperreflexia |
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Term
| Name 3 dissociative agents |
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Definition
| PCP (phencyclidine) and ketamine, dextromethorphan |
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