DERMATOLOGY PHARM Flashcards by Rachael Petry

MOA: Competitively inhibits viral DNA poly; competes with dGTP for incorporation into viral DNA. Does not have 3’-OH so chain elongation is ceased.

Acyclovir

Valacyclovir

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MOA: Competitively inhibits viral DNA poly; competes with dGTP for incorporation into viral DNA. Has 3’—OH so synthesis of viral DNA is possible then it locks up.

Ganciclovir

Valganciclovir

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MOA: Competitively inhibits viral DNA poly; competes with dCTP for incorporation into viral DNA

Cidofovir

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MOA: Competitively inhibits viral DNA poly; competes with dGTP for incorporation into viral DNA

Famciclovir

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

Foscarnet

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Drug that treats:
Varciella zoster
Varciella chicken pox
HHV-8

Valacyclovir

Acyclovir just treats 2 varciellas

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Drug that treats:
HHV-6
HHV-8

Valganciclovir

Ganciclovir just does HHV-6 and is used off-label for HHV-8

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Drug that treats:
Pox virus family
HHV-6, -7, and -8

Cidofovir

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Drug that treats:
Varicella Zoster
HHV-8

Famciclovir

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Drug that treats:

HHV-6 only

Foscarnet

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Antiviral Drug with few side effects.

Famciclovir

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Antiviral Drug that causes:

NEUROTOXICITY (including seizures)

Aciclovir/Valaciclovir

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Antiviral Drug that causes:
PANCYTOPENIA (anemia, leucopenia, neutropenia, thrombocytopenia) and is a
TERATOGEN

Ganciclovir/

Valganciclovir

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Antiviral Drug that causes:

Nephrotoxicity (so monitor creatinine and urinary protein)

Cidofovir

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Antiviral Drug that causes:
Electrolyte imbalance (chelates calcium ions)

Foscarnet

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What drug do you give with cidofovir to reduce renal toxicity?

Probenecid (inhibits renal tubular secretion)

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MOA: Folate antagonist (bacteriostatic) that also inhibits 2nd messenger pathways involved in neutrophil chemotaxis

Dapsone

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MOA: Inhibition of bacterial and mycobacterial RNA synthesis (beta-subunit of DNA-dependent RNA-polymerase

Rifampin

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MOA: preferential binding (not intercalating) to mycobacterial guanine in DNA

Clofazimine

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MOA: Inhibits 50S ribosomal subunit

leprosy drug

Clarithromycin

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MOA: Inhibits 30S ribosomal subunit

(leprosy drug)

Minocycline

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MOA: Inhibits bacterial DNA gyrase

leprosy drug

Ofloxacin

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MOA: Inhibits NFKB mediated transcriptional upregulation and TNF-alpha production (blocks leukocyte migration)

Thalidomide

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Drugs that treat Tuberculoid leprosy.

Dapsone

Rifampin

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Drugs that treat Lepromatous leprosy.

Clofazimine Clarithromycin, Minocycline, Ofloxacin (if you cannot tolerate clofazimine)

Drug that is used to treat side effects of leprosy.

Thalidomide

Drug that is contraindicated in G6PD deficiency.

Dapsone

Leprosy drug that causes: - Hepatitis - Jaundice - Staining of body/fluids to a bronzing color - Feces may be black or tarry - Depression/suicide

Clofazimine

Leprosy drug that causes: - Hepatic toxicity - Discoloration of body fluids (red)

Rifampin

Leprosy drug that requires monitoring of LFTs, CBCs, and platelet count. Why?

Dapsone Causes dapsone syndrome (peripheral neuropathy, leukopenia, SJS, etc.)

``` Lepsory drug that: -TERATOGEN (X) -May increase HIV viral load -Somnolence > rash> H/A Peripheral Neuropathy ```

Thalidomide

Leprosy drug that has DDIs with rifampin, cimetidine (H2 blocker), omeprazole (proton pump inhibitors), and probenecid.

Dapsone

What leprosy drug gets widely distributed throughout the body (CNS, breast milk, etc.).

Rifampin

What leprosy drug is very lipophillic (can remain for a long time in fatty tissues and reticuloendothelial system).

Clofaziine

Which drugs have the BBW: Infection, including fungal/mycobacterial/viral, neoplasms, and Tb.

Adalimumab Etanercept Infliximab

MOA: Human mAb (with IgG1) targeted at TNF-alpha

Adalimumab (SC)

MOA: Receptor-Ab fusion protein (with p75 TNF receptor and Fc IgG1) targeted at TNF-alpha.

Etanercept (SC)

MOA: Chimeric mAb (with variable region of mouse mAb on human IgG1) targeted at TNF-alpha.

Infliximab (IV)

MOA: mAb directed at interleukin (binds to p40 subunit integral to IL-12 and IL-23 activation to suppress formation of pro-inflammatory Th1 and Th17.

Ustekinumab

MOA: acting upon nuclear receptors (RAR) and this causes transcriptional changes in a number of factors and produces epidermal hyperplasia and a sloughing off of the surface of the skin (peels off the surface layers leaving new skin underneath with lack of infection)

``` Acitretin (oral) Tazorotene (oral or topical) Tretinoin (topical) Adapalene (topical) Isotretinoin (topical) ```

MOA: Binds to Vit D receptor; complex associates with RXR-alpha and binds DNA vitamin D response elements to modulate epidermal differentiation and inflammation

Calcipotrene (topical)

MOA: Hormonally active form of Vitamin D3

Calcitrol (topical)

MOA: Topical pro-drug converted to benzid acid that works by free radical liberation that is lethal for P. acnes.

Benzoyl Peroxide

MOA: Inhibit protein synthesis (binds 50s ribosomal subunit) ACNE drug

Clindamycin/Erythromycin

MOA: Topical keratolytic that causes desquamation of horny layer of the skin.

Salicyclic Acid

MILD corticosteroid.

Hydrocortisone

Moderate corticosteroid.

Betamethasone valerate

Potent corticosteroid.

Fluocinonide

Very potent corticosteroid.

Clobetasol Proprionate

Drugs that treat acne and psoriasis.

Salicylic acid Acitretin Tazorotene Tretinoin

Drug that is contraindicated with immunosuppressives or concurrent vaccinations.

Adalimumab

Drug that is contraindicated with sepsis.

Etanercept

Drug that is contraindicated with heart failure and murine protein hypersensitivity.

Infliximab

Drug that is contraindicated with live virus vaccines and that you must pre-test for Tb with.

Ustekinumab

``` Acne drugs that are/cause: Teratogenic Hyperlipidemia Cause mucocutaneous/ musculoskeletal effects ```

Acitretin (oral) | Tazorotene (oral)

Drugs that increase the risk of sunburn, erythema, and burning.

Tazorotene (topical) Tretinoin (topical) Adapalene (topical) Isotretinoin (topical)

Acne drug that may lead to suicidal ideation.

Isotretinoin (topical)

Drug that is a topical irritant (reduced by concurrent corticosteroids); in EXCESS causes- hypercalcemia and hypercalcuria; increased susceptibility to UV-induced skin cancer

Calcipotrene

Drug that is way more potent on calcium metabolism when given systemically! Better tolerated in sensitive skin areas.

Calcitrol

Drug that causes: Drying of skin: peeling, erythema, irritation; bleach hair or colored fabrics; AVOID contact with eyes or mucous membranes

Benzoyl peroxide

Acne drug that must be given for a minimum of 4-8 weeks.

Clindamycin or Erythromycin

``` Drug that (with prolonged administration) leads to: -Tinitus and dizziness (early) -Seizures, Renal/liver failure, and organ edema (late) ```

Salicylic acid

Acne drugs that are category X teratogens.

Isotretinoin (oral) | tazarotnene (topical)

Hormonal contraceptives used for acne.

o Ortho Tri-cyclen o Estrostep o YAZ

Drugs for tinea (widespread)

Terbinafine Itraconazole Fluconazole Grisefulvin

Drugs for onchomycosis (widespread).

``` TGIF Terbinafine Grisefulvin Itraconazole Fluconazole ```

MOA: inhibits ergosterol formation.

"Azoles" (oral or topical) | Amorolfine (topical)

MOA: Inhibits the conversion of squalene to squalene epoxide (and overall ergosterol formation)

terbinafine

MOA: Inhibits microtubule formation to stops fungal mitosis

Griseofulvin

MOA: Selectively inhibits squalene 2,3-epoxidase enzyme. Produces antibacterial effects and anti-inflammatory effects (vasoconstriction) at higher concentrations.

Naftifine

MOA: Blocks fungal trans-membrane transport (depleting essential substrates and interfering with RNA and DNA synthesis)—high concentrations permit leakage of intracellular material.

Ciclopirox

Drugs for localized tinea.

``` TOPICAL: Azoles Terbinafine Naftifine Ciclopirox ```

Topical drugs for onchomycosis

Ciclopirox | Amorolfine

Antifungal that must be used very carefully in underlying heart problems and should NOT be used in hepatic toxicity (extensive hepatic and renal elimination) OR post-partum.

Itraconazole

Antifungal that must be dose adjusted for renal elimination.

Fluconazole

Antifungal that should not be used in hepatic texocity.

Griseofulvin

Azole with: Hepatotoxicity Adrenal insufficiency CYP inhibition**

Ketoconazole

``` Azole with: Hepatotoxicity CYP interactions Negative inotropic action Category C teratogenicity ```

Itraconazole

``` Azole with: Hepatotoxicity CYP interactions QT prolongation Category C teratogenicity Optic neuritis/Photosensitivity ```

Voriconazole

``` Azole with: Hepatotoxicity CYP interactions QT prolongation Category C teratogenicity ```

Fluconazole

Asoles that can cross CSF.

Voriconazole | Fluconazole

``` Azole with: Hepatotoxicity CYP interactions QT prolongation Category C teratogenicity ```

Posconazole

Azole that must be taken with full meal to have appropriate bioavailability.

Posconazole

What drug should NOT be combined with azoles (because it is useless).

naftifine

Antifungal that cross-reacts with beta lactams.

Griseofulvin

What drug requires routine CBCs when administering.

Terbinafine | causes transient lymphopenia and neutropenia with oral drug

MOA: Combines with keratin to produce fibrillar contraction and short term occlusion of eccrine and apocine sweat gland ducts.

aluminum chloride

MOA: Binds to cell membrane, internalized, cleaved into light and heavy chains→Blocks the exototic release of Ach (due to cleavage of SNAREs to inhibit the complex formation and fusion of vesicular membrane (VAMPs) with cellular membrane (SNAP25).

Botulinum toxin

MOA: Quaternary ammonium compound (antimuscarinic) | used for hyperhydrosis

Glycopyrrolate

MOA: Tertiary amine (antimuscarinic agent) | used for hyperhydrosis

Oxybutynin

MOA: Quaternary ammonium compound that blocks nicotinic and muscarinic receptors used for hyperhydrosis

Propantheline

Drug that: - Capable of causing muscular paralysis - (respiratory arrest and death - Typical anticholinergic effects (dry mouth, eye problems, etc.) - Contains albumin (allergy)

Botulinum toxin

Drug for hyperhydrosis that Crosses BBB (sedation and delirium).

Oxybutynin

List the drugs for Trichogenic Agents.

Minoxidil | Finasteride

Description: Topical agent used for hair re-growth.

Minoxidil

Description: Oral agent used for hair loss or at higher doses for treatment of BPH.

Finasteride

Description: Topical drug to reduce unwanted female facial hair. (Takes 6-8 weeks for effects to be noticeable).

Eflornithine

MOA: Unknown—may activate the hair follicle directly or stimulate follicular microcirculation. May also alter local androgen metabolism.

Minoxidil

MOA: Blocks 5 alpha-reductase activity to decrease scalp and serum DHT concentrations (without altering other hormones).

Finasteride

MOA: Inhibition of ornithine decarboxylase (a mandatory step in polyamine production)—so you get decreased hair follicle cell division and differentiation

Eflornithine

Description: Temporary relief of facial skin darkening by hormonal changes, pregnancy, OCs or HRT

Hydroquinolole Flucinolone Tretinoin

What type of drug is Hydroquinolole?

melanocyte inhibitor

What type of drug is Flucinolone?

steroid

What type of drug is Tretinoin?

retinoic acid analog

MOA: inhibition of melanin formation (blocking melanocyte enzymatic oxidation of tyrosine to 3,4-DOPA, and increased keratinocyte shedding from epidermis resulting in decreased epidermal melanin content).

Hydroquinolole | Tretinoin

MOA: Activation by exposure to UV light (resulting in conjugation of cross-linking of DNA and cell death. Leads to delayed erthema followed over several weeks by increased epidermal melanization and thickening of the stratum corneum.

Methoxsalen

What drug has: Loss of libido, sexual dysfunction, infertility, feminization

Finasteride

What drug has a DDI with saw palmetto?

Finasteride

List the PEDICULICIDAL DRUGS for lice.

permethrin lindane ivermectin

List the PEDICULICIDAL + OVICIDAL DRUG for lice.

malathion

MOA: Organophosphate insecticide that is metabolized to malaoxon in the louse and inhibits acetylcholinesterase and causes neuronal hyperstimulation and paralysis.

malathion

MOA: Synthetic pyrethrin that causes hyperexcitability and paralysis of louse by binding voltage-gated Na+ channels. → in RID and other OTC meds!

Permethrin

MOA: Neurotoxin that interferes with GABA neurotransmitter function by interacting with the GABA receptor-chloride channel complex at the picrotoxin binding site→ leads to hyperstimulation

Lindane

MOA: Oral and topical drug that causes hyperexcitability and paralysis by binding selectively and with high affinity to glutamate-gated Cl- ion channels present in invertebrate nerve and muscle cells.

Ivermectin

What drug has systemic toxicity if ingested (acts like a para-sympatetic agonist)?

Malathion

What drug has ashtma exacerbation (in patients allergic to ragweed or chrysanthemums).

Permethrin

What drug has the potential for neurotoxicity (seizures and death) and persistence in the environment?

Lindane

What drug may worsen bronchial asthma and can elevate liver transaminases?

Ivermectin

What drug is NOT for younger patients where the BBB is immature?

Ivermectin

What drug is rendered contraindicated in Knock-down resistance (kdr) mutations of louse sodium channels.

Permethrin

What drug has a BBW for skin diseases/conditions or neonatal prematurity will increase drug systemization and is NOT FOR patients with uncontrolled seizure disorders.

Lindane

Why is systemic absorption of Permethrin is NOT serious?

drug does not work on human sodium channels ONLY on lice sodium channels

Drug for BCC.

Vismodegib | Imiquimod

Drugs for actinic keratosis.

Imiquimod Diclofenac Trichloroacetic acid

Drugs for melanoma.

``` Aldesleukin Interferon Ipilimumab Sorafenib Trametinib Vemurafenib ```

MOA: Small molecule inhibitor of SMO used to block the Hedgehog pathway.

Vismodegib

MOA: Topical treatment for localized disease (immunostimulant that is a direct activator of TLR7 & TLR8→ Th1 immune response, blocker of adenosine receptors, and NF-kB activator (regulates cytokines like TNF and IL).) Negatively modulate GLI activity in BCC (inhibiting Hedge-hog pathway.

Imiquimod

MOA: NSAID: Inhibitor of PGE2 (inflammatory mediator)

Diclofenac | topical

MOA: Chemical peel that rapidly penetrates and cauterizes skin, keratin, and other tissue.

Trichloroacetic acid | topical

MOA: IL-2 agonist (stimulates cytokine cascades with various interferons, interleukins, and TNF); induces proliferation of B and T cells, monocytes, macrophages, and CTLs (indiscriminate stimulation).

Aldesleukin | IV or SC

MOA: Interferon-alpha agonist (bind to the cell surface receptor tyrosine kinases→ production of several enzymes which are thought to be responsible for the pleiotropic biologic effects of alpha-IFNs:

Interferon | IV or SC

MOA: Recombinant human antibody that blocks CTLA-4 and has anti-tumoral action by stimulating T cell function (CTLA-4 usually negatively effects T cell activation).

Ipilimumab

Cancer drug: Alopecia, GI toxicity, intrauterine fetal death, Weight loss and fatigue

Vismodegib

Cancer drug: Increases photosensitivity and can compromise birth control (condoms and diaphragm) integrity if used for HPV.

Imiquimod

Cancer drug: Itchy rash, dry skin, skin peeling, redness

Diclofenac | topical

Cancer drug: Burning, inflammation and localized tenderness

Trichloroacetic acid | topical

Cancer drug: Capillary leak syndrome (due to stimulation of NK cells or CD25 cells), hypotension, diminished mental status, dyspnea, etc.

Aldesleukin | IV or SC

Cancer drug: Flu-like symptoms, blood dyscrasias, alopecia, elevated hepatic enzymes, cough/dyspnea (do routine CBC, LFTs, CXRs and ECGs)

Interferon | IV or SC

Cancer drug: Dermatitis that can be as severe as TEN. Tiredness, diarrhea, itching, rash.

Ipilimumab

Cancer drug; Elevated hepatic enzymes, rash, hand and foot syndrome, anemia, bone marrow suppression (neutropenia), increased risk of hemorrhage

Sorafenib

Cancer drug: Elevated liver enzymes, rapid onset of rash, diarrhea, HTN, hemorrhage, RARE: retinal pigment epithelial detachment, ILD, cardiomyopathy

Trametinib

Cancer drug: Cutaneous squamous cell carcinoma; elevated creatinine, QT prolong, photosensitivity, SJS, ophthalmic issues. (need to do regular LFTs, ECGs, and electrolyte monitoring)

Vemurafenib

What cancer drug is a male and female teratogen?

Vismodegib

What cancer drug has a BBW: With significant CNS, cardiac, pulmonary (need regular CXRs), renal or hepatic disease and/or organ transplant.

Aldesleukin | IV or SC

What cancer drug has a BBW: Use cautioned in autoimmune and cardiac disease, depression, and infection

Interferon | IV or SC

What cancer drug should not be used in Adrenal insufficiency, diarrhea, Guillain-Barre syndrome, hepatitis, hyper/ hypothyroidism, hypopituitarism, myasthenia gravis, peripheral neuropathy, pregnancy, serious rash

Ipilimumab

do antibiotics

MOA: Rapid destruction of bacterial cell membranes that leads to depolarization (potassium efflux) and is bactericidal.

Dapatomycin

MOA: Binds 23S subunit of 50S to inhibit protein synthesis by ribosome.

Linezolid

MOA: Binds to ribosome peptidyl transferase domain to inhibit tRNA synthetase and block AA addition to the growing peptide chain. (Inhibits protein synthesis)

Streptogramins: Dalfopristin Quinupristin

MOA: Binds with HIGH affinity to 30s protein subunit to inhibit protein translation. NOT expelled by efflux pumps.

Tetracyclines like Glycycline Tigecycline

MOA: binds 50S ribosomal subunit to inhibit protein synthesis.

Clindamycin

MOA: binds reversibly to staph isoleucyl tRNA synthetase to inhibit protein and RNA synthesis.

Mupirocin

MOA: inhibits dephosphorylation of isoprenyl pyrophosphate carrier protein (so not movement of peptidoglycan building blocks of cell wall across the cell membrane)

Bacitracin

AE: Muscle pains/weakness (monitor CPK); DDI with statins

Daptomycin

AE: If used over 2 weeks, optic and peripheral neuropathy; DDI with SSRIs, MAOIs, PE, etc.

Linezolid

AE: Thrombophlebitis/pain at injection site, increased liver enzymes, joint/muscle pain; CYP450 inhibitor

Dalfopristin | Quinupristin

AE: GI problems, hepatic/pancreatic toxicity; sun sensitivity; teeth/bone alteration.

Blycycline | Tigecycline

AE: Pseudomembranous colitis from C diff, GI toxicity, hypersensitivity rash.

Clindamycin

AE: not many--not systemically absorbed.

Mupirocin

AE: nephrotoxic with parenteral use.

Bacitracin

What antibiotic needs to be dose adjusted for renal failure?

daptomycin

What drug loses action via point mutations in 23s.

linezolid

What drug loses action via changes in 23S and constitutive expression of "erm" MLSb phenotype

Dalfopristin | Quinupristin

What drug loses action via methylation of "erm" encoded genes that decrease affinity for ribosome?

Clindamycin

What antibiotics do you need to dose adjust for liver failure?

Glycycline/Tigecycline | Clindamycin

What antibiotics have absorption that is altered by food intake?

Linezolid | Clindamycin

What antibiotics are used topically?

Mupirocin | Bacitracin

What drugs are given in an IV 70:30 combination.

Dalfopristin (70): Quinupristin (30)

What drug is given in an ointment with neomycin and polymyxin B?

Bacitracin

What drug is widely absorbed but cannot penetrate the CSF?

clindamycin

What antibiotics cannot be used in patients under 18?

Glycycline | Tigecycline

What antibiotic cannot be used for lung infections because it is inactivated by surfactant?

daptomycin

What drug is given by slow IV infusion and is widely distributed into tissues?

Glycycline | Tigecycline