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OSD Drugs > Derm & Musculoskeletal Drugs > Flashcards

Derm & Musculoskeletal Drugs Flashcards

These are all of the drugs- except the corticosteroids.

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
Q

Methotrexate

A

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
Q

Methoxsalen

A

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
Q

Etanercept

A

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
Q

Infliximab

A

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
Q

Benzoyl Peroxide

A

Class: Acne drug

MOA:

  • bacteriostatic
  • combined with erythromycin or clindamycin to prevent development of resistance.
30
Q

Clindamycin

A

Class: Acne drug

MOA:

  • Antibiotic
  • Binds 50S ribosome to suppress protein synthesis

AE:
-Increased risk for CDIFF infection

31
Q

Doxycycline

A

Class: Acne drug

MOA:
-Binds 30S subunit and inhibits protein synthesis

Note:
-Also used in Rx for Ricketsia Rickettsii

32
Q

Metronidazole

A

Class: Acne drug

MOA:

  • Anti-Inflammatory
  • Inhibits nucleic acid synthesis by disrupting DNA

Rx:
-ACNE ROSACEA

33
Q

Acitretin

A

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
Q

Adapalene

A

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
Q

Isotretinoin

A

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
Q

Tretinoin

A

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
Q

Calcipotriene

A

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
Q

Ketoconazole

A

Class: Antifungal

MOA:
-Blocks 14-a-demethylase to block ergosterol synthesis and inhibit cell wall formation

39
Q

Mycostatin

A

Class: Antifungal

MOA:

  • Binds ergosterol in fungal cell wall.
  • Same as Nystatin

AE:
-Can bind human Cholesterol at high doses

40
Q

Clotrimazole

A

Class: Antifungal

MOA:
-Blocks 14-a-demethylase to block ergosterol synthesis and inhibit cell wall formation

41
Q

Econazole

A

Class: Antifungal

MOA:
-Blocks 14-a-demethylase to block ergosterol synthesis and inhibit cell wall formation

42
Q

Itraconazole

A

Class: Antifungal

MOA:
-Blocks 14-a-demethylase to block ergosterol synthesis and inhibit cell wall formation

43
Q

Terbinafine

A

Class: Antifungal

MOA:

  • Inhibits squalene epoxidase
  • Thus, Reduces ergosterol synthesis and inhibits fungal cell wall formation.

Note: Oral or topical.

44
Q

Acyclovir

A

Class: Antiviral

MOA:
-Interferes with DNA polymerase to inhibit DNA replication via chain termination.

Rx:
-Herpes

45
Q

Neomycin

A

Class: Antibiotic

MOA:

  • Aminoglycoside
  • Binds 30S subunit of ribosome

AE:
-Contact Dermatitis

46
Q

Erythromycin

A

Class: Antibiotic

MOA:
-Binds 50S ribosome to suppress protein synthesis

47
Q

Bacitracin

A

Class: Antibiotic

MOA:
-Targets Gram (+)

AE:

  • Contact Dermatitis
  • Nephrotox when given IM
48
Q

Mupirocin

A

Class: Antibiotic

MOA:
-Reversibly binds isoleucyl tRNA synthetase.

Note: Ointment; derived from Pseudomonas

49
Q

Cephalexin

A

Class: Antibiotic
-First generation cephalosporin

MOA:

  • Binds penicillin binding proteins to arrest bacterial cell wall synthesis
  • Inhibit bacterial replication.

AE:
-Diarrhea

50
Q

Cefazolin

A

Class: Antibiotic
-First generation cephalosporin

MOA:

  • Binds penicillin binding proteins to arrest bacterial cell wall synthesis
  • Inhibit bacterial replication.

AE:
-Diarrhea

51
Q

Polymyxin B

A

Class: Peptide antibiotic

Rx:
-Gram (-)

AE:

  • Nephrotoxicity
  • Neurotoxicity
52
Q

Imiquimod

A

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
Q

Topical 5-fluorouracil

A

Class: Anti-wart agent & Miscellaneous

MOA:

  • Inhibits thymidylate synthetase
  • Pyrimidine antimetabolite.
54
Q

Liquid nitrogen

A

Class: Miscellaneous

MOA:
-Cryotherapy for removal of skin lesions

Rx:

  • Warts
  • AK

AE:
-Blistering

55
Q

Permethrin

A

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.

OSD Drugs (4 decks)

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