Derm/Musc Drugs Flashcards Preview

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Flashcards in Derm/Musc Drugs Deck (67)
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1
Q

Acetaminophen

What is the active metabolite

Agonist & inhibitor at what receptor?

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.
2
Q

Aspirin

A

Class: Nonselective / COX-1 Inhibitors

MOA:

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

AE:

  • GI irritation
  • Asthma Exacerbation
  • prolonged bleeding time
  • prolonged gestation
  • inhibits renal function
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.

4
Q

Etodolac

A

Inhibits COX-2 prostaglandins that mediate inflammation, fever, and pain without blocking the GI/renal injuring PGs (COX-1).

5
Q

Ibuprofen

A

competitive, reversible COX inhibitor, competes with arachidonic acid for COX active site. Class 1 NSAID.

6
Q

Indomethacin

A

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

7
Q

Ketorolac

A

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

8
Q

Naproxen

A

competitive, reversible COX inhibitor, competes with arachidonic acid for COX active site. Class 1 NSAID.

9
Q

Celecoxib

A

Inhibits COX-2 prostaglandins that mediate inflammation, fever, and pain without blocking the GI/renal injuring PGs (COX-1).

10
Q

Diclofenac

A

Inhibits COX-2 prostaglandins that mediate inflammation, fever, and pain without blocking the GI/renal injuring PGs (COX-1).

11
Q

Hydroxycholorquine

A

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

12
Q

Leflunomide

Mechanism?

AE

A

Pyrimidine synthesis inhibitor - inhibits dihydrochloorate (rUMP synthesis) - wich inhibits autoreactive T cells activation and auto-antibodies by B cells

AE - Diarrhea, Elevation of liver enzymes

***Cholestiramine increases clearence

13
Q

Methotrexate

A

Very potent antiinflammatory, used with anti-TNF’s to prevent anti-anti-TNF Abs. Inhibits DHF to THF converison by DHF reductase, to block purine synthesis. Strong effecton decreasing joint pain index. Increase dose if disease not well-controlled. If no responde alone, can add sulfasalazine and hydrochlorquine, leflunomide, anti-TNF agent, anakinra, abatacept. Triple therapy = MTX + SSZ + HCQ (not as good as anti-TNF).

14
Q

Sulfasalazine

A

sulfapyridine and salicylate bound by axo group. Unknown mechanism.

15
Q

Etanercept

A

soluble TNF receptor bound to TNF-a, mimics cel-surface receptor.

16
Q

Anakinra

A

Use as a Disease Modifying Anti-Rheumatic Drug

IL-1 receptor antagonist

17
Q

Golimumab

A

Neutralizes soluble and cell-bound TNF-a/b.

18
Q

Adalimumab

A

Neutralizes soluble and cell-bound TNF-a/b.

19
Q

Infliximab

Mechanism

AE?

Major complication

A

Neutralizes soluble and cell-bound TNF-a

AE - Upper Respiratory Infection, nausea, cough, headache

***TB reaction

20
Q

Allopurinol

A

Xanthine oxidase inhibitor (hypoxanthine analogue), metabolized to oxipurinol, which is the clinically effective XO inhibitor. Has a short t1/2, but oxipurinol has t1/2 = 14-26 hours (prolonged if decreased GFR). Max effect in 4-14 days.

21
Q

Colchicine

Mechanism?

AE?

A

Alkaloid derivative of meadow saffron. . Readily bioavailable (> binds soluble, non-polymerized tubulin, forms complex preventing elongation/contraction of dynamic tublin polymers >> blocks cell division, signal transduction, regulation of gene expression, migration, and secretion. Arrests growth (low concentration) and promotes depolymerization (high concentration) and arrests cell at metaphase = antiinflammatory and PMN phagocytosis disruption. Also binds leukocyte membrane proteins. Biliary and stool excretion (enterohepatic circulation), with major eleimination by ABCB1 (GI tract), minor elimination by CYP3A4 (enteric and hepatic cytochrome). Also Renal elimination.

AE - Nausea Vomiting Diarrhea, hair loss , myopathy**, bone marrow suppresion

22
Q

Probenecid

AE?

A

Targets URAT-1 urate transporter in proximal tubule = uricosuric. Oral, well-absorbed, t1/2= 6-12 hours, rapid hepatic metabolism and urinary excretion. Inhibits urate-anion exchange at proximal tubule to block reabsorption. Ineffective at CrCl <60 ml/min. Take with fluids, alkalinize urine, monitor urate, CBC, LFTs, creatinine.

AE: GI irritation, rash

P works in the P(roximal tubule)

23
Q

Febuxostat

A

Oral, nonpurine analogue inhibitor of xanthine oxidase. Can inhibit oxidized and reduced XO forms. T1/2 4-18 hours, metabolized hepatically. Activity is not altered in mild to moderate renal insufficiency.

24
Q

Hydrocortisone

A

Synthetic cortisol, ~90% circulates bound to corticosteroid binding globulin, 5-10% circulates free. Metabolized by liver, 60-90 min t1/2. 30% excreted in urine as dihydroxy ketones. Binds cytosolic receptor, dimerizes, translocates to nucleus where binds glucocorticoid response elements to upregulate or repress transcription of many proteins (20-30%), with variable action depending on cell type. Can also activate signaling pathways before entering nucleus = rapid steroid actions (prior to transcriptional changes). Example is phosphorylation and release of annexin-1, a potent antiinflammatory agents that blocks the mobilization of lymphocytes and release of inflam mediators.

25
Q

Prednisone

A

Oral available, 4x antiinflammatory with less (0.3x) mineralocorticoid activity cf. hydrocortisone/cortisol. Short/medium-acting duration.

26
Q

Prednisolone

A

Oral, injectable. 5x antiinflammatory with less (0.3x) mineralocorticoid activity cf. hydrocortisone/cortisol. Short/medium-acting duration.

27
Q

Triamcinolone

A

Oral, injectable, topical. Intermediate duration. 5x antiinflammatory with 5^3 topical activity and no (0) mineralocorticoid activity cf. hydrocortisone/cortisol

28
Q

Betamethasone

A

Oral, injectable, topical. Long duration. 25-40x antiinflammatory with 10x topical activity and no (0) mineralocorticoid activity cf. hydrocortisone/cortisol

29
Q

Dexamethasone

A

Oral, injectable, topical. Long duration. 30x antiinflammatory with 10x topical activity and no (0) mineralocorticoid activity cf. hydrocortisone/cortisol

30
Q

Fludrocortisone

A

Oral. 10x antiinflammatory with 0 topical activity and 250x mineralocorticoid activity cf. hydrocortisone/cortisol

31
Q

Clobetasol

A

Superpotent, Class I steroid. Binds receptor and translocates to nucleus for many functions. Vasoconstriction activite correlates with clinical efficacy. Available as lotion, spray, or shampoo.

32
Q

Triamcinolone

A

Upper-middle strength, Class III steroid. Available as ointment, cream, foam.

33
Q

Desonide

A

Mild strength, Class VI steroid. Available as gel.

34
Q

Hydrocortisone

A

Synthetic cortisol, ~90% circulates bound to corticosteroid binding globulin, 5-10% circulates free. Metabolized by liver, 60-90 min t1/2. 30% excreted in urine as dihydroxy ketones. Binds cytosolic receptor, dimerizes, translocates to nucleus where binds glucocorticoid response elements to upregulate or repress transcription of many proteins (20-30%), with variable action depending on cell type. Can also activate signaling pathways before entering nucleus = rapid steroid actions (prior to transcriptional changes). Example is phosphorylation and release of annexin-1, a potent antiinflammatory agents that blocks the mobilization of lymphocytes and release of inflam mediators.

35
Q

Tacrolimus

A

Antiinflammatory ointment/cream, binds FK506 forming complex that inhibits calcineurin and blocks cytokine production.

36
Q

Pimecrolimus

AE?

A

Antiinflammatory ointment/cream, binds FK506 forming complex that inhibits calcineurin and blocks cytokine production.

Risk of Cancer (lymphoma, skin cancer) and vitiligo

37
Q

Methotrexate

Mechanism?

A

Very potent antiinflammatory, used with anti-TNF’s to prevent anti-anti-TNF Abs in Rheumatoid Arthritis. Inhibits DHF to THF converison by DHF reductase, to block purine synthesis. Strong effecton decreasing joint pain index. Increase dose if disease not well-controlled. If no responde alone, can add sulfasalazine and hydrochlorquine, leflunomide, anti-TNF agent, anakinra, abatacept. Triple therapy = MTX + SSZ + HCQ (not as good as anti-TNF).

38
Q

Methoxsalen

A

Photosensitizer, preferentially taken up by epidermal cells and binds DNA, making more susceptible to UV radiation damage.

39
Q

Etanercept

A

soluble TNF receptor bound to TNF-a, mimics cel-surface receptor.

40
Q

Infliximab

A

Neutralizes soluble and cell-bound TNF-a/b.

41
Q

Benzoyl Peroxide

A

bacteriostatic, combined with erythromycin or clindamycin to prevent development of resistance.

42
Q

Clindamycin

A

Binds 50S ribosome to suppress protein synthesis, antibiotic

43
Q

Doxycycline

A

Binds 30S subunit and inhibits protein synthesis in susceptible bacteria.

44
Q

Metronidazole

Mechanism?

A

for Rosea

Inhibits nucleic acid synthesis by disrupting DNA, anti-inflammatory

45
Q

Acitretin

A

Retinoid, unstable in sunlight. Functional vitamin A analogue acts at retinoic acid receptor, retinoid X receptor. Alters gene expression by binding nuclear receptor. Differentiates epidermis, modulates proliferation, prevents keratinization, prevents follicle plugging (=anti-acne), antiinflammatory, apoptotic

46
Q

Adapalene

A

Retinoid, unstable in sunlight. Functional vitamin A analogue acts at retinoic acid receptor, retinoid X receptor. Alters gene expression by binding nuclear receptor. Differentiates epidermis, modulates proliferation, prevents keratinization, prevents follicle plugging (=anti-acne), antiinflammatory, apoptotic

47
Q

Isotretinoin

A

Oral tretinoin

48
Q

Tretinoin

A

First generation retinoid, unstable in sunlight (unlike 3rd generation retinoids). Functional vitamin A analogue acts at retinoic acid receptor, retinoid X receptor. Alters gene expression by binding nuclear receptor. Differentiates epidermis, modulates proliferation, prevents keratinization, prevents follicle plugging (=anti-acne), antiinflammatory, apoptotic

49
Q

Calcipotriene

A

Vitamin D analgue inhibits keratinocyte proliferation and promotes differentiation (=slows growth). Steroid-alternative.

50
Q

Ketoconazole

A

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

51
Q

Mycostatin

A

Same as Nystatin, binds ergosterol in fungal cell wall.

52
Q

Clotrimazole

A

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

53
Q

Econazole

A

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

54
Q

Itraconazole

A

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

55
Q

Terbinafine

A

Inhibits squalene epoxidase, reducing ergosterol synthesis and inhibiting fungal cell wall formation. Oral or topical.

56
Q

Acyclovir

What enzyme does it need for function?

A

Interferes with DNA polymerase to inhibit DNA replication via chain termination - needs thymidine kinase

57
Q

Neomycin

A

Aminoglycoside, binds 30S subunit of ribosome

58
Q

Erythromycin

A

Binds 50S ribosome to suppress protein synthesis, antibiotic

59
Q

Bacitracin

A

TMP/SMX

60
Q

Mupirocin

A

Ointment, derived from Pseudomonas. Reversibly binds isoleucyl tRNA synthetase.

61
Q

Cephalexin

A

First generation cephalosporin, binds penicillin binding proteins to arrest bacterial cell wall synthesis and inhibit bacterial replication.

62
Q

Cefazolin

A

First generation cephalosporin, binds penicillin binding proteins to arrest bacterial cell wall synthesis and inhibit bacterial replication.

63
Q

Polymyxin B

A

Peptide antibiotic

64
Q

Imiquimod

A

Antiviral and anti-tumor immune modulator, binds TLR-7, to induce cytokines (INF-a and TNF-a).

65
Q

Topical 5-fluorouracil

A

inhibits thymidylate synthetase >> pyrimidine antimetabolite.

66
Q

Liquid nitrogen

A

Cryotherapy for removal of skin lesions

67
Q

Permethrin

A

Synthetic pyrethroid, <2% absorbed percutaneously. Paralyzes mite by sodium channel disruption. Only acts on mite (not eggs), so must give multiple treatments.