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Systemic Pharm II > Anti-Inflammatory > Flashcards

Anti-Inflammatory Flashcards

1
Q

Prostaglandin

A

lipid compounds that have hormone-like effects as local mediators

produced in minute quantities by almost all tissues and rapidly metabolized (don’t circulate in blood)

Arachnoid Acid is primary precursor of PLP of membranes

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2
Q

Production of Prostaglandins

A

Cycooxygenase Pathway
COX 1: gastric production, vascular homeostasis, platelet aggregation, kidney and reproductive function
COX 2: elevated prostaglandin in sites of chronic disease and inflammation

Lipoxygenase Pathway
Leukotrienes produced (tx asthma)
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3
Q

Prostaglandin Analogs

A

bind to membrane receptor and act as local signals with varying functions but play major role in modulating pain, inflammation, and fever

also controls uterine contractions, renal BF, and acid secretion/mucous production in GI tract

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4
Q

Misoprostol

A

PGE1 Analog ~ used to protect mucosal lining of stomach during chronic use of NSAIDS

decrease incidence of ulcers and constipation by binding to PGE receptors in parietal cells to decrease gastric acid and increase mucous production

AE: induce labor ** , D, Abdominal Pain, HA
- contraindicated in pregnancy

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5
Q

Iloprost

A

Prostacyclin Analog to increase cGMP causing vasodilation and mainly treats pulmonary HTN

inhalation only (short half life, needs frequent dosing)

AE: flush, HA, dizzy

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6
Q

Latanoprost

A

PGF analog

binds to prostaglandin FP receptor to increase uveoscleral outflow and DECREASE IOP (tx glaucoma)

AE: blur, increased iris pigmentation, increase pigment and number of lashes, eye redness and irritation

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7
Q

Travaprost

A

PGF analog PRODRUG

binds to prostaglandin FP receptor to increase uveoscleral outflow and DECREASE IOP (tx glaucoma)

AE: blur, increased iris pigmentation, increase pigment and number of lashes, eye redness and irritation

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8
Q

Bimatoprost

A

endogenous prostamides

binds to prostaglandin FP receptor to increase uveoscleral outflow and DECREASE IOP (tx glaucoma)

AE: blur, increased iris pigmentation, increase pigment and number of lashes, eye redness and irritation

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9
Q

Non-steroidal Anti-inflammatory drugs (NSAIDS)

A

inhibit COX enzymes which will decrease prostaglandin synthesis (PG etc)

anti-pyretic, anti-inflammatory, and analgesic but ulcers

  • PGE: thought to sensitize nerve endings to inflammatory chemical mediators (analgesic)
  • PGI: inhibits gastric acid secretion (increases acid)
  • PGE/F: stimulate mucous production (decrease protection)
  • PGE: increases set point for thermoregulatory center (no fever and resets body temp)

AE: ulcers + serious CV thrombotic events, MI, CVA

Contraindicated in post-op pain for CABG

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10
Q

Aspirin

A

prototype and ONLY NSAID to irreversibly inactivate COX

Esterases rapidly break down into salicylate

low dose decreases TXA and inhibits aggregation (prolongs bleeding) - DO NOT TAKE W/ anticoagulant

increases alveolar ventilation: elevates CO2 and increased respiration

Avoid in children with viral infections (reye syndrome)

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11
Q

Acetic and Propionic Acids

A

inhibit COX enzymes reversibly and nonspecifically with no effect on leukotrienes (less intense GI effects)

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12
Q

Indomethacin

A

Acetic and Propionic Acid / NSAID

highest incidence for GI issues + may cause ocular AE at large doses/long-term use

Blur, Whorl Keratopathy, Macular pigment changes

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13
Q

Ibuprofen

A

Acetic and Propionic Acid / NSAID

inhibit COX enzymes reversibly and nonspecifically with no effect on leukotrienes (less intense GI effects)

Max: 3200 mg/day

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14
Q

Diclofenac

A

Acetic and Propionic Acid / NSAID

inhibit COX enzymes reversibly and nonspecifically with no effect on leukotrienes (less intense GI effects)

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15
Q

Naproxen

A

Acetic and Propionic Acid / NSAID

inhibit COX enzymes reversibly and nonspecifically with no effect on leukotrienes (less intense GI effects)

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16
Q

Ketorolac

A

Acetic and Propionic Acid / NSAID

inhibit COX enzymes reversibly and nonspecifically with no effect on leukotrienes (less intense GI effects)

17
Q

Meloxicam

A

Oxicams/NSAID

long half life (1x/day dosing)

preferential for COX-2 but nonselective at high doses
- may have lesser AE

18
Q

Piroxicam

A

Oxicams/NSAID

long half life (1x/day dosing)

19
Q

Celecoxib

A

COX-2 Specific NSAID

theoretically less AE; no inhibition of platelet aggregation and COX-1 still provides GI protection

some of these showed high CV disease and CVA risk

20
Q

Acetaminophen

A

Tylenol / not NSAID - NOT ANTI-INFLAMMATORY

max 4g/day

inhibits prostaglandin synthesis (more activity in CNS so ONLY antipyretic and analgesic)

inactivated by chemicals in inflammatory cells/platelets
- poor anti-inflam or anti-platelet action

1st choice for children with viral infections or chicken pox

Metabolite: liver DAMAGE!! main AE

21
Q

Hydroxychloroquine

A

also known as Plaquenil

increases pH within inflammatory cells to interfere with antigen processing and decrease CD4

Treat RA, SLE, Anti-malarial

AE: GI, skin rash, Acne + Bull’s Eye Maculopathy

22
Q

Bull’s Eye Maculopathy

A

permanent loss of vision

RF: excessive daily dose of hydroxychloroquine by weight, duration of use, concomitant use of Tamoxifen, Retinal Disease

Recommendations:

  • Dose: <5mg/kg of weight
  • Baseline Screening within 1 year of starting treatment and annual screening after 5 years of use
  • – DFE + 10-2 VF + macular OCT
23
Q

Methotrexate

A

DMARD: immunosuppressant that inhibits dihydrofolate reductase and impairs DNA synthesis in immune cells

other meds can be added

lower dose than for cancer so less AE

24
Q

IL-1 and TNF

A

pro-inflammatory cytokines involved in RA secreted by synovial macrophages to stimulate release of collagenase (decrease collagen!!)

25
Q

Etanercept

A

TNF Inhibitor

subcutaneous/IV only

AE: high infection risk, no live vaccines, worsen pre-existing HF, increase risk of lymphoma/cancers

26
Q

Adalimumab

A

TNF Inhibitor

subcutaneous/IV only

AE: high infection risk, no live vaccines, worsen pre-existing HF, increase risk of lymphoma/cancers

27
Q

Infliximab

A

TNF Inhibitor

subcutaneous/IV only

AE: high infection risk, no live vaccines, worsen pre-existing HF, increase risk of lymphoma/cancers

28
Q

Golimumab

A

TNF Inhibitor (treat RA)

subcutaneous/IV only

AE: high infection risk, no live vaccines, worsen pre-existing HF, increase risk of lymphoma/cancers

29
Q

Certolizumab

A

TNF Inhibitor

subcutaneous/IV only

AE: high infection risk, no live vaccines, worsen pre-existing HF, increase risk of lymphoma/cancers

30
Q

Anakinra

A

IL-1 Antagonist

do NOT take with TNF inhibitor

Subcutaneous 1x/day

31
Q

Abatacept

A

inhibit t-cell activation to treat RA

32
Q

Tocilizumab

A

inhibit IL-6 to treat RA

33
Q

Tofacitinib

A

regulate immune cell function (oral)

Systemic Pharm II (17 decks)

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