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Biochem Drugs > Eicosanoid metabolism > Flashcards

Eicosanoid metabolism Flashcards

1
Q

Aspirin

A
  • Inhibits TXA2
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2
Q

NSAID

A
  • Aspirin inhibits both COX-1 & COX-2
    • covalent acetylation of SER530
  • Celecoxib inhibits COX-2
    • Rx: arthritis & menstrual cramps
  • Irreversible inhibition
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3
Q

Asthma Rx

A

Inhibition of leukotriene synthesis

  • Corticosteroid inhibition of PLA2
  • 5’Lipoxygenase inhibition, eg. Benoxaprofen, Zileuton

Inhibition Leukotriene Receptor

  • Cysteinyl-Leukotriene Receptor antagonists
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4
Q

Corticosteroids

A
  • anti-inflammtory preventing bronchoconstriction
  • Genetic level MOA
  • Induces release of phosphorylated formm of Annexin-1 protein involved in inhibiting PLA2
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5
Q

Leukotriene Receptor antagonists

A
  • Cysteinyl-Leukotriene (CysLT) receptors have imp. actions in cardio & resp systems
  • CysLT receptor antagonists prevents bronchoconstriction
    • Zafirlukast
    • Montelukast
    • Lukast
    • Less effective than Salbutamol, a ß-AR agonist
    • Zileutin inhibits LOX-5 reducing formation of LTB4 & CysLT
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6
Q

Zileuton

A
  • LOX-5 blocker
  • reduces formation of LTB4 & CysLT (LTC4, LTD4 & LTE4)
  • Leukocytes
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7
Q

TXA2

A
  • produced primarily by platelets
  • promotes platelet aggregation
  • decreases formation of cAMP
  • vasoconstriction
  • bronchoconstriction
  • mobilizes intracellular Ca2+
  • contraction of smooth muscle
  • lymphocyte proliferation
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8
Q

PGE2

A
  • produced by most tissues especially the kidney
  • vasodilation
  • relaxes smooth muscle
  • used to induce labour
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9
Q

PGF2alpha

A
  • produced by most tissues
  • vasoconstriction
  • contraction of smooth muscle
  • stimulates uterine contractions
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10
Q

PGI2

A
  • produced primarily by endothelium of vessels
  • vasodilation
  • inhibits platelet aggregation
  • increases formation of cAMP
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11
Q

EPA is a precursor for?

A
  • series-3 PG which includes PGE3
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12
Q

Arachidonic acid is a precursor for?

A
  • Series-2 eicosanoids including PGE2, PGI2 & TXA2
    *
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13
Q

SC-558

A
  • Strong inhibitor of COX-2
  • Weak inhibitor of COX-1
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14
Q

Cysteinyl-leukotrenes

A
  • LTC4
  • LTD4
  • LTE4
  • more potent than histamine in stimulating smooth muscle contraction of bronchi & intestines
    *
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15
Q

Slow-Reacting Substance of Anaphylaxis (SRS-A)

A
  • mixture of leukotrienes LTC4, LTD4 & LTE4
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16
Q

Leukotriene receptors

A
  • Cysteinyl-leukotriene receptors (CysLT) imp. actions in cardiovascular & respiratory systems

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