Derm Pharm Cards Part 1

Question 1

Botulinum toxin MAO

Answer 1

Hyperhydrosis tx

Purified protein from Clostridium botulinum

Heavy chain portion binds to cell membrane via an unidentified high affinity receptor molecule; internalized via endocytosis; light chain cleaves SNAP25 to prevent the fusion of Ach vesicles w/ cell membrane

Blocks N/M receptors to reduce wrinkles

Question 2

Glycopyrrolate

Propantheline

Answer 2

Quaternary ammonium cmpd, N/M block for hyperhydrosis, no BBB cross

Question 3

Propanolol

Answer 3

Hyperhydrosis tx

Beta blocker that reduces CNS stimulation

Question 4

Ditiazem

Answer 4

Hyperhydrosis tx

Blocks calcium ions involved in secretion

Question 5

Cyclovir MOA

Answer 5

Viral immediate early genes - thymidine kinases - phosphorylate the cyclovirs to activate them

All are renaly eliminated

Question 6

Cyclovir agents that are neurotoxic/ seizures

Answer 6

acyclovir

valacyclovir

Question 7

Cyclovir agents that cause anemia, leukopenia, neutropenia, thrombocytopenia

Answer 7

Gancyclovir

Valgancyclovir

Question 8

Variciella zoster & chicken pox - 2 therapies for pox, 3 for zoster

Answer 8

Acyclovir & Valacyclovir - pox & zoster

Famciclovir - zoster only

Question 9

Best tolerated cyclovir

Answer 9

Famcyclovir

Question 10

Anti-viral that causes electrolyte imbalance, chelates calcium

Answer 10

Forscarenet

Question 11

2 anti-virals that do not require intracellular phosphorylation

Answer 11

Forcarenet

cidofovir

Question 12

Taken w/ cidofovir to reduce renal toxicity

Answer 12

Probenecid

Question 13

MAO of Forscarenet

Answer 13

Selectively inhibits the viral-specific DNA polymerases and reverse transcriptases at pyrophosphate-binding site; blocks chain elongation

Question 14

MAO of cidofovir

Answer 14

Competitively inhibits viral DNA polymerase; competes with deoxycytosine triphospate for incorporation into viral DNA

(only Rx for HHV-7)

Question 15

Amorolfine MOA and use

Answer 15

Inhibits ergosterol synthesis

Clinical use: Topical therapy for Onchomycosis infections

Question 16

Ciclopirox MOA and use

Answer 16

Blocks fungal transmembrane transport which depletes essential substrates and interferes with RNA and DNA synthesis

Clinical use: Topical therapy for localized Tinea and Onchomychosis infections

Question 17

Naftifine

Answer 17

Inhibits ergosterol synthesis by inhibiting squalene epoxidase

Locally bactericidal against Gram+ and Gram- bacteria

Anti-inflammatory due to inhibition of PGs, LTs and histamine  vasoconstriction

Clinical use: Topical therapy for localized Tinea infections

Question 18

2 topical anti-fungals that we do not combine

Answer 18

Azoles & Naftifine because they both work by inhibiting ergosterol synthesis

Question 19

Fluconazole

Answer 19

Inhibit ergosterol synthesis by blocking 14-alpha demethylase, which is a CYP enzyme responsible for converting lanosterol to ergosterol

Clinical use: oral therapy for widespread Tinea infections, topical treatment for localized Tinea infections and oral therapy for Onychomycosis

Question 20

Azole w/ Renal Elimination

Answer 20

Fluconazole

Question 21

2 azoles to the CSF

Answer 21

Fluconazole & Voriconazole

Question 22

Itraconazole adverse effects

Answer 22

Hepatotoxicity

No QT prolongation

BBW: negative inotropic action  heart failure and ventricular dysfunction

Question 23

Terbinafine MAO & Adverse Effects

Answer 23

Inhibits ergosterol synthesis by inhibiting squalene epoxidase

Hepatotoxicity (rare), transient lymphopenia and neutropenia  requires routine CBCs

Avoid in immunosuppressed patients

Question 24

Posaconazole

Answer 24

Inhibit ergosterol synthesis by blocking 14-alpha demethylase, which is a CYP enzyme responsible for converting lanosterol to ergosterol

Must be taken with a full meal for adequate bioavailability

Question 25

Vorconazole unique adverse effects

Answer 25

genetic polymorphisms affect serum concentrations optic neuritis Photosensitizes the skin

Question 26

Daptomycin MAO, AEs? limitations?

Answer 26

Cyclic lipopeptide that rapidly disrupts bacterial cell membranes and results in depolarization and loss of membrane potential and K+ efflux Adverse affect- muscle pain or weakness, monitor serum creatine phosphokinase elevations Drug interactions with co-administration of statins Surfactant antagonizes daptomycin, so do not use in the treatment of pneumonia

Question 27

Linezolid static vs. cidal? Resistance? Caution use with?

Answer 27

Bacteriostatic in Staph and enterococci Bacteriocidal in Strep Resistance can develop by point mutations arising in the 23S RNA Non-selective inhibitor of monoamine oxidase, use caution with co-administration of pseudoephedrine, phenylpropanolamine, SSRIs, etc…  serotonin syndrome Decreased breakdown of tyramine absorbed from the diet  HTN oral - contains aspartame, caution w/ PKU

Question 28

Mupirocin MAO, vehicle, AEs, uses

Answer 28

Inihibits protein and RNA synthesis by binding reversibly to staphylococcal isoleucyl tRNA synthetase The vehicle used in mupirocin ointments is polyethylene glycol, which can cause renal failure tx topical for Staph/ Strep impetigo

Question 29

Bacitracin

Answer 29

Polypeptide that inhibits bacterial cell wall synthesis by inhibiting movement of peptidoglycan building blocks of cell wall from inside to outside the cell membrane by inhibiting dephosphorylation of isoprenyl pyrophosphate carrier protein Clinical use: Gram + cocci and bacilli Nephrotoxicity with parenteral use

Question 30

Dapsone MAO - 2

Answer 30

Inhibits folate synthesis via competitive antagonism of dihydropteroate synthetase Inhibits second messenger pathways involved in neutrophil chemotaxis (mechanism UNK)

Question 31

Dapsone - adverse rsns

Answer 31

hemolysis, methemoglobinemia, hepatitis, infectious mononucleosis, cholestatic jaundice, peripheral (motor) neuropathy, severe hypoalbuminemia, psychosis, leukopenia, agranulocytosis and maculopapular or exfoliative lesions SJS has been associated with dapsone syndrome as well Contraindicated in patients with G-6-PD deficiency Metabolized in liver to hydroxylamine  potent oxidant  hemolysis and methemoglobinemia Renal elimination  decreased renal function  increase risk of ADEs listed

Question 32

Dapsone syndrome

Answer 32

Type I - red rash on upper body/ forehead, give corticosteroids Type II - painful nodules/ neuropathy - give corticosteroids, clofazimine, thalidomide

Question 33

Clofazimine MAO

Answer 33

Binds to mycobacterial guanine and cytosine blocking the template function of the DNA and inhibiting bacterial proliferation Stains body fluids, feces may appear black or tarry and skin discoloration Highly lipophilic  long persistence

Question 34

3 TNF-alpha blockers | their black box warning?

Answer 34

Adalimumab Etanercept Infliximab (also Heart Failure & murine protein sensitivity) Infection, neoplasm, TB

Question 35

Ustekinuma

Answer 35

Monoclonal antibody that binds p40 subunit  disrupts IL-12 and IL-23 signal which are both over expressed in psoriasis plaques  suppresses formation of pro-inflammatory Th1 and Th17 cells

Question 36

Calcipotriene

Answer 36

Binds VitD receptor  complex associated with RXR  binds DNA vitamin D response element  modulation of epidermal differentiation and inflammation, leading to improvement in psoriatic plaques

Question 37

Calcitriol

Answer 37

Hormonally active form of VitD3 binds VitD receptor  complex associated with RXR  binds DNA vitamin D response element  modulation of epidermal differentiation and inflammation, leading to improvement in psoriatic plaques psoriasis in intertriginous and sensitive areas of skin

Question 38

Retinoids - MOA | Name 4 RAR;s

Answer 38

``` Targets RAR  affects cellular differentiation and proliferation first line for comedonal acne Adapalene Tretinoin, ATRA Isotretinoin Tazarotene ```

Question 39

2 retinoic acid receptors & their roles

Answer 39

RAR - affects differentiation and proliferation, useful in psoriasis and acne RXR -affects apoptosis, used for mycosis funoides & Kaposi sarcoma

Question 40

Benzoyl peroxide

Answer 40

Pro-drug converted in the skin to benzoic acid  liberation of free radical, which is lethal for nearby P. acnes

Question 41

Salicylic acid

Answer 41

Topical keratolytic  desquamation of horny layer of skin Clinical use: common and plantar warts, psoriasis, calluses, corns and acne

Question 42

salicylism

Answer 42

dizziness, tinnitus, CNS deficits, multi-organ failure and organ edema

Question 43

For fluorinated steroids only

Answer 43

Rosacea-like skin rash around the mouth Perioral dermatitis Do not apply fluorinated topical steroids to face

Question 44

Hydrocortisone

Answer 44

mild topical corticosteroid

Question 45

Betamethasone valerate

Answer 45

moderate corticosteroid; intralesional injection

Question 46

Flucinonide

Answer 46

potent topical corticosteroid

Question 47

Clobetasol propionate

Answer 47

very potent corticosteroid

Question 48

Aluminum Chloride

Answer 48

Hyperhydrosis tx Short term occlusion of eccrine/ apocrine ducts Combines with keratin to produce fibrilar contraction of duct

Question 49

Oxybutynin

Answer 49

Hyperhydrosis tx | Tertiary ammonium cmpd, cross BBB causing sedation and delirium

Question 50

Clonidine

Answer 50

Hyperhydrosis tx | Central alpha 2 agonist that lowers CNS stimulation

Question 51

Griseofulvin MAO & adverse rxns (2 unique)

Answer 51

Binds to tubulin  interfers with microtubule function  inhibiting mitosis Clinical use: oral therapy for widespread Tinea infections and oral therapy for Onychomycosis Because the drug is a product of penicillium, there is a potential cross-sensitivity to patients with beta-lactam hypersensitivity INDUCES CYP3A4

Question 52

Dalfopristin/Quinoprostin (70:30) -Synercid MAO

Answer 52

Protein synthesis inhibition by binding to the ribosome peptidyletransferase domain  inhibition of tRNA synthetase  amino acid addition to peptide chain is blocked

Question 53

Clindamycin antagonized by..

Answer 53

Erythromycin