Derm & Musculoskeletal Drugs Flashcards

These are all of the drugs- except the corticosteroids. (55 cards)

1
Q

Acetaminophen

A

Class: Weak COX Inhibitor

  • Strong analgesic (non-opioid)
  • Antipyretic
  • Very weak antiinflammatory activity

Rx:

-Analgesia in children

AE:

-Fatal liver disease if overdose

Note: AM404 is active metabolite, which:

  • Agonist at TRPV1 channel
  • Agonist Cannabinoid CB1 receptor
  • Inhibits endogenous cellular CB uptake
  • Inhibits COX-1 and COX-2.
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2
Q

Aspirin

A

Class: Nonselective / COX-1 Inhibitors
-Class 3 NSAID

MOA:

  • Irreversible acetylation (inactivation) of COX (non-selective).
  • Analgesia, antipyresis, antiinflammation, inhibits thrombosis (post-MI).

AE:

  • GI Irritation
  • Asthma Exacerbation
  • Gestation Prolongation
  • Renal Function Inhibition
  • Gout Exacerbation
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3
Q

Diclofenac

A

Class: Nonselective / COX-1 Inhibitors

Phase 1: Competitive, time dependent, reversible COX inhibitor.
Phase 2: with time, conformational change with tighter binding. Class 2 NSAID.

AE:
-Increase COX-1 selectivity increases risk of ulcer and GI risks.

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4
Q

Etodolac

A

Class: Nonselective / COX-1 Inhibitors

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5
Q

Ibuprofen

A

Class: Nonselective / COX-1 Inhibitors
-Class 1 NSAID

MOA:

  • Competitive, reversible COX inhibitor
  • Competes with arachidonic acid for COX active site.

AE:
-Increase COX-1 selectivity increases risk of ulcer and GI risks.

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6
Q

Indomethacin

A

Class: Nonselective / COX-1 Inhibitors
-Class 2 NSAID

MOA:

  • Phase 1: Competitive, time dependent, reversible COX inhibitor.
  • Phase 2: with time, conformational change with tighter binding.

AE:
-Increase COX-1 selectivity increases risk of ulcer and GI risks.

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7
Q

Ketorolac

A

Class: Nonselective / COX-1 Inhibitors

MOA:

  • Effective perenteral opioid alternative, COX-1 selective.
  • Analgesia with minimal toxicity, for use IM (slower) or IV (faster)
  • Prolonged IM effect allowing longer dosing interval.

AE:

  • Not for use >5 days, high GI ulcer risk (25% at 1 week)
  • Avoid using pre-surgery (platelet inhibition and delayed healing).
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8
Q

Naproxen

A

Class: Nonselective / COX-1 Inhibitors
-Class 1 NSAID

MOA:

  • Competitive, reversible COX inhibitor
  • Competes with arachidonic acid for COX active site.

AE:
-Increase COX-1 selectivity increases risk of ulcer and GI risks.

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9
Q

Celecoxib

A

Class: COX-2 Inhibitors

MOA:

  • Inhibits COX-2 prostaglandins that mediate inflammation, fever, and pain
  • Does not block the GI/renal injuring PGs (COX-1).

AE:

  • Increase COX-2 selectivity increases risk of:
  • Thrombosis and CV
  • CHF
  • Hypertension
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10
Q

Diclofenac

A

Class: COX-2 Inhibitors

MOA:

  • Inhibits COX-2 prostaglandins that mediate inflammation, fever, and pain
  • Does not block the GI/renal injuring PGs (COX-1).

AE:

  • Increase COX-2 selectivity increases risk of:
  • Thrombosis and CV
  • CHF
  • Hypertension
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11
Q

Etodolac

A

Class: COX-2 Inhibitors

MOA:

  • Inhibits COX-2 prostaglandins that mediate inflammation, fever, and pain
  • Does not block the GI/renal injuring PGs (COX-1).

AE:

  • Increase COX-2 selectivity increases risk of:
  • Thrombosis and CV
  • CHF
  • Hypertension
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12
Q

Hydroxycholorquine

A

Class: DMARD

MOA:

  • Antimalarial
  • Unknown mechanism, accumulates in lysosome.
  • Decreases neutrophils chemotaxis, phagocytosis and superoxide synthesis.
  • Inhibits TLR-9 signaling.

Rx:

  • RA
  • SLE

AE:

  • GI Irritation
  • Macular Toxicity (requires annual eye exam)
  • Myopathy
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13
Q

Leflunomide

A

Class: DMARD

MOA: Pyrimidine synthesis inhibitor

Rx:
-RA (Not Useful at all)

Note: Useless drug in RA. This is known in France as “Le Fluke-o-mide”

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14
Q

Methotrexate

A

Class: DMARD

MOA:

  • Dihydrofalte reductase inhibitor
  • Thus, blocks Purine Synthesis
  • Very potent antiinflammatory, used with anti-TNFs.
  • Decreases Joint pain

Note: If no response alone, can add sulfasalazine and hydrochlorquine, leflunomide, anti-TNF agent, anakinra, abatacept.

Triple therapy = MTX + SSZ + HCQ (not as good as anti-TNF).

Rx:

  • RA
  • Psoriasis

AE:

  • Hepatotoxicity,
  • cytopenia
  • stomatitis
  • GI irritation

Note: Can decrease AE’s with folic acid or leucovorin after MTX dose.

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15
Q

Sulfasalazine

A

Class; DMARD
-5-ASA

MOA:
-sulfapyridine and salicylate bound by axo group. Unknown mechanism.

Rx:

  • RA
  • IBD
  • Spolyloarthropathy

AE:

  • Hypospermia (from sulfapyridine metabolite)
  • GI irritation
  • Headache
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16
Q

Etanercept

A

Class: DMARD
-Biologic

MOA:

  • TNF-a receptor decoy
  • Etanercept Intercepts TNF

Rx:

  • RA
  • Psoriasis

AE:

  • Opportunistic Infection (TB; can’t form granulomas)
  • Serious Infection (avoid in Chronic Infection; HBV, Immunosuppressed)
  • Demyelination (Avoid in MS, Optic Neuritis)
  • CHF (Avoid in CHF patients)
  • Lupus
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17
Q

Anakinra

A

Class: DMARD
-Biologic

MOA:
-IL-1 receptor antagonist

Rx: RA
-Note Effective for RA

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18
Q

Infliximab

A

Class: DMARD

MOA:
-Neutralizes soluble and cell-bound TNF-a and beta

AE:

  • Opportunistic Infection (TB; can’t form granulomas)
  • Serious Infection (avoid in Chronic Infection; HBV, Immunosuppressed)
  • Demyelination (Avoid in MS, Optic Neuritis)
  • CHF (Avoid in CHF patients)
  • Lupus
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19
Q

Allopurinol

A

Class: Anti-Gout Agent

MOA:

  • Xanthine oxidase inhibitor (Hypoxanthine analogue)
  • Metabolized to Oxipurinol, which is the clinically effective XO inhibitor.

Note:

  • Has short t1/2
  • But Oxipurinol has t1/2 = 14-26 hours (prolonged if decreased GFR).
  • Max effect in 4-14 days.

Rx:

  • Gout
  • Not for Acute Gout
  • Urate Nephrolithiasis

AE:

  • Stevens-Johnson Syndrome
  • Hypersensitivity (more common if on diuretics; 25% mortality)
  • Myelosuppression
  • Hepatotox
  • Nephrotox
  • Vasculitis

DDIs:

  • Azothioprine
  • Warfarin
  • 6MP
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20
Q

Colchicine

A

Class: Anti-Gout agent

Readily bioavailable (<50%) PO following jejunal and ileal uptake.

MOA:

  • Binds Tubulin and forms complex; prevents elongation/contraction of Dynamin tubulin Polymers
  • Promotes depolymerization (high concentration)
  • Blocks cell division, signal transduction, gene expression
  • Arrests growth (low concentration)
  • Disrupts Phagocytosis by PMN

Rx:

  • Actue Gout (within 24-36hrs)
  • Prophylaxis of Gout during initiation of Urate lowering drugs

AE:

  • Narrow therapeutic-toxicity window
  • Avoid use in Hepatic and Renal patients

Note:

  • Major elimination via ABCB1 (GI tract)
  • Minor elimination by CYP3A4 (enteric and hepatic cytochrome).
  • Renal Elimination also

Note: Alkaloid derivative of meadow saffron.

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21
Q

Probenecid

A

Class: Anti-Gout agent
-Uricosuric

MOA:

  • Targets URAT-1 urate transporter in proximal tubule.
  • Inhibits urate-anion exchange at proximal tubule to block reabsorption

Note:

  • Rapid hepatic metabolism and urinary excretion.
  • Take with fluids, alkalinize urine
  • Monitor urate, CBC, LFTs, creatinine.

AE:

  • Pregnancy risk factor B
  • Rash
  • Nephrotic Syndrome
  • Stones
  • Aplastic Anemia
  • Hemolytic Anemia
  • Leukopenia
  • Hepatic Necrosis

DDI:

  • Salicylates (inhibits uricosuric effect)
  • Beta lactams
  • NSAIDS
  • Increased Methotrexate Tox
  • Dapsone
  • Acyclovir
  • Heparin
  • Loop Diuretics
  • Quinolones
  • Benzodiazapines
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22
Q

Febuxostat

A

Class: Anti-Gout agent

MOA:

  • Nonpurine analogue inhibitor of xanthine oxidase
  • Can inhibit oxidized and reduced XO forms.

Rx:

  • Prophylaxis for Gout
  • Used with NSAIDs or Colchicine for up to 6months.

Contraindicated:

  • Azathioprine
  • 6MP
  • Monitor LFTs
  • CVA

Note:

  • Metabolized hepatically
  • Activity is not altered in mild to moderate renal insufficiency.
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23
Q

Tacrolimus

A

Class: Calcineurin Inhibitor
-Anti-inflammatory ointment/cream

MOA:

  • Binds FK506
  • Forms complex that inhibits calcineurin and blocks cytokine production.

Rx:
-Atopic Dermatitis

AE:

  • Vitiligo
  • Granuloma facialis
  • Eye lid and intertrigenous regions of body
24
Q

Pimecrolimus

A

Class: Calcineurin Inhibitor
-Anti-inflammatory ointment/cream

MOA:

  • Binds FK506
  • Forms complex that inhibits calcineurin and blocks cytokine production.

Rx:
-Atopic Dermatitis

AE:

  • Skin cancer and Lymphoma
  • Black box warning - avoid long term use.
25
Methotrexate
Class: RA and Psoriasis agents MOA: - Dihydrofalte reductase inhibitor - Thus, blocks Purine Synthesis - Very potent antiinflammatory, used with anti-TNFs. - Decreases Joint pain Note: -For RA, if no response alone, can add sulfasalazine and hydrochlorquine, leflunomide, anti-TNF agent, anakinra, abatacept. Triple therapy = MTX + SSZ + HCQ (not as good as anti-TNF). Rx: - RA - Psoriasis AE: - Hepatotoxicity, - cytopenia - stomatitis - GI irritation Note: Can decrease AE's with folic acid or leucovorin after MTX dose. AE: -
26
Methoxsalen
Class: Psoriasis Agent MOA: - Photosensitizer (makes cells more susceptible to UV radiation damage) - Preferentially taken up by epidermal cells and binds DNA Rx: -Psoriasis AE: -Erythema
27
Etanercept
Class: Psoriasis agent and DMARD -Biologic MOA: - TNF-a receptor decoy - Etanercept Intercepts TNF Rx: - RA - Psoriasis AE: - Opportunistic Infection (TB; can't form granulomas) - Serious Infection (avoid in Chronic Infection; HBV, Immunosuppressed) - Demyelination (Avoid in MS, Optic Neuritis) - CHF (Avoid in CHF patients) - Lupus
28
Infliximab
Class: Psoriasis and DMARD MOA: -Neutralizes soluble and cell-bound TNF-a and beta AE: - Opportunistic Infection (TB; can't form granulomas) - Serious Infection (avoid in Chronic Infection; HBV, Immunosuppressed) - Demyelination (Avoid in MS, Optic Neuritis) - CHF (Avoid in CHF patients) - Lupus
29
Benzoyl Peroxide
Class: Acne drug MOA: - bacteriostatic - combined with erythromycin or clindamycin to prevent development of resistance.
30
Clindamycin
Class: Acne drug MOA: - Antibiotic - Binds 50S ribosome to suppress protein synthesis AE: -Increased risk for CDIFF infection
31
Doxycycline
Class: Acne drug MOA: -Binds 30S subunit and inhibits protein synthesis Note: -Also used in Rx for Ricketsia Rickettsii
32
Metronidazole
Class: Acne drug MOA: - Anti-Inflammatory - Inhibits nucleic acid synthesis by disrupting DNA Rx: -ACNE ROSACEA
33
Acitretin
Class: Acne drug -Retinoid (unstable in sunlight) MOA: - Functional vitamin A analogue - Acts at retinoic acid receptor, retinoid X receptor. - Alters gene expression by binding nuclear receptor. Results in: - Differentiation of epidermis - Modulates proliferation - Prevents keratinization and Follicle plugging (=anti-acne), - Antiinflammatory and Apoptotic AE: - Teratogenic - Drying and Itching - Photosensitization
34
Adapalene
Class: Acne drug -Retinoid (unstable in sunlight) MOA: - Functional vitamin A analogue - Acts at retinoic acid receptor, retinoid X receptor. - Alters gene expression by binding nuclear receptor. Results in: - Differentiation of epidermis - Modulates proliferation - Prevents keratinization and Follicle plugging (=anti-acne), - Antiinflammatory and Apoptotic AE: - Teratogenic - Drying and Itching - Photosensitization
35
Isotretinoin
Class: Acne drug -Retinoid (unstable in sunlight) Note: Oral Form of Tretinoin -ISO for I-SwallO MOA: - Functional vitamin A analogue - Acts at retinoic acid receptor, retinoid X receptor. - Alters gene expression by binding nuclear receptor. Results in: - Differentiation of epidermis - Modulates proliferation - Prevents keratinization and Follicle plugging (=anti-acne), - Antiinflammatory and Apoptotic AE: - SERIOUS Teratogenic - Drying and Itching - Photosensitization (decreased Keratin) Baby AE: - Craniofacial - CNS - Cardiac
36
Tretinoin
Class: Acne drug -Retinoid (unstable in sunlight) MOA: - Functional vitamin A analogue - Acts at retinoic acid receptor, retinoid X receptor. - Alters gene expression by binding nuclear receptor. Results in: - Differentiation of epidermis - Modulates proliferation - Prevents keratinization and Follicle plugging (=anti-acne), - Antiinflammatory and Apoptotic AE: - Teratogenic - Drying and Itching - Photosensitization (decreased Keratin)
37
Calcipotriene
Class: Anti Psoriasis MOA: - Vitamin D analogue - Inhibits keratinocyte proliferation and promotes differentiation (=slows growth). - Steroid-alternative. Rx: -Psoriasis AE: -Calcium and Bone Metabolism (high doses)
38
Ketoconazole
Class: Antifungal MOA: -Blocks 14-a-demethylase to block ergosterol synthesis and inhibit cell wall formation
39
Mycostatin
Class: Antifungal MOA: - Binds ergosterol in fungal cell wall. - Same as Nystatin AE: -Can bind human Cholesterol at high doses
40
Clotrimazole
Class: Antifungal MOA: -Blocks 14-a-demethylase to block ergosterol synthesis and inhibit cell wall formation
41
Econazole
Class: Antifungal MOA: -Blocks 14-a-demethylase to block ergosterol synthesis and inhibit cell wall formation
42
Itraconazole
Class: Antifungal MOA: -Blocks 14-a-demethylase to block ergosterol synthesis and inhibit cell wall formation
43
Terbinafine
Class: Antifungal MOA: - Inhibits squalene epoxidase - Thus, Reduces ergosterol synthesis and inhibits fungal cell wall formation. Note: Oral or topical.
44
Acyclovir
Class: Antiviral MOA: -Interferes with DNA polymerase to inhibit DNA replication via chain termination. Rx: -Herpes
45
Neomycin
Class: Antibiotic MOA: - Aminoglycoside - Binds 30S subunit of ribosome AE: -Contact Dermatitis
46
Erythromycin
Class: Antibiotic MOA: -Binds 50S ribosome to suppress protein synthesis
47
Bacitracin
Class: Antibiotic MOA: -Targets Gram (+) AE: - Contact Dermatitis - Nephrotox when given IM
48
Mupirocin
Class: Antibiotic MOA: -Reversibly binds isoleucyl tRNA synthetase. Note: Ointment; derived from Pseudomonas
49
Cephalexin
Class: Antibiotic -First generation cephalosporin MOA: - Binds penicillin binding proteins to arrest bacterial cell wall synthesis - Inhibit bacterial replication. AE: -Diarrhea
50
Cefazolin
Class: Antibiotic -First generation cephalosporin MOA: - Binds penicillin binding proteins to arrest bacterial cell wall synthesis - Inhibit bacterial replication. AE: -Diarrhea
51
Polymyxin B
Class: Peptide antibiotic Rx: -Gram (-) AE: - Nephrotoxicity - Neurotoxicity
52
Imiquimod
Class: Immune Modulator MOA: - Binds TLR-7, to induce cytokines (INF-a and TNF-a). - Antiviral and anti-tumor immune modulator AE: - Incites immune response, therefore Flu-like symptoms - Erythema - Irritation - Ulceration
53
Topical 5-fluorouracil
Class: Anti-wart agent & Miscellaneous MOA: - Inhibits thymidylate synthetase - Pyrimidine antimetabolite.
54
Liquid nitrogen
Class: Miscellaneous MOA: -Cryotherapy for removal of skin lesions Rx: - Warts - AK AE: -Blistering
55
Permethrin
Class: Antiparasitic MOA: - Synthetic pyrethroid, <2% absorbed percutaneously. - Paralyzes mite by sodium channel disruption. NOTE: Only acts on mite (not eggs), so must give multiple treatments.