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    Chapter 18

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    Jessie Marie Duhaylungsod
    1. Arachidonic acid undergoes oxygenation via three main pathways - cyclooxygenase, lipoxygenase, and epoxygenase - producing different eicosanoids including prostaglandins, thromboxanes, leukotrienes, and others. 2. These eicosanoids have diverse effects on organs and systems, such as regulating inflammation and pain, smooth muscle contraction, platelet aggregation, and renal, cardiovascular and respiratory function. 3. Nonsteroidal anti-inflammatory drugs work by inhibiting the cyclooxygenase pathway, thereby reducing prostaglandin production and downstream effects like inflammation, at the cost of potential gastrointestinal irritation. More selective cyclooxygenase-

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    Chapter 18

    Uploaded by

    Jessie Marie Duhaylungsod
    6 views5 pages
    1. Arachidonic acid undergoes oxygenation via three main pathways - cyclooxygenase, lipoxygenase, and epoxygenase - producing different eicosanoids including prostaglandins, thromboxanes, leukotrienes, and others. 2. These eicosanoids have diverse effects on organs and systems, such as regulating inflammation and pain, smooth muscle contraction, platelet aggregation, and renal, cardiovascular and respiratory function. 3. Nonsteroidal anti-inflammatory drugs work by inhibiting the cyclooxygenase pathway, thereby reducing prostaglandin production and downstream effects like inflammation, at the cost of potential gastrointestinal irritation. More selective cyclooxygenase-

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    PHARMACOLOGY NOTES

    Original Title

    CHAPTER 18

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    1. Arachidonic acid undergoes oxygenation via three main pathways - cyclooxygenase, lipoxygenase, and epoxygenase - producing different eicosanoids including prostaglandins, thromboxanes, leukotrienes, and others. 2. These eicosanoids have diverse effects on organs and systems, such as regulating inflammation and pain, smooth muscle contraction, platelet aggregation, and renal, cardiovascular and respiratory function. 3. Nonsteroidal anti-inflammatory drugs work by inhibiting the cyclooxygenase pathway, thereby reducing prostaglandin production and downstream effects like inflammation, at the cost of potential gastrointestinal irritation. More selective cyclooxygenase-

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    © All Rights Reserved
    Download as DOCX, PDF, TXT or read online from Scribd
    Download as docx, pdf, or txt
    6 views5 pages

    Chapter 18

    Uploaded by

    Jessie Marie Duhaylungsod
    1. Arachidonic acid undergoes oxygenation via three main pathways - cyclooxygenase, lipoxygenase, and epoxygenase - producing different eicosanoids including prostaglandins, thromboxanes, leukotrienes, and others. 2. These eicosanoids have diverse effects on organs and systems, such as regulating inflammation and pain, smooth muscle contraction, platelet aggregation, and renal, cardiovascular and respiratory function. 3. Nonsteroidal anti-inflammatory drugs work by inhibiting the cyclooxygenase pathway, thereby reducing prostaglandin production and downstream effects like inflammation, at the cost of potential gastrointestinal irritation. More selective cyclooxygenase-

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    © All Rights Reserved
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    of 5

    CHAPTER 18: THE EICOSANOIDS

    (PROSTAGLANDINS, THROMBOXANES,
    LEUKOTRIENES & RELATED COMPOUNDS)
    MEMBRANE PHOSPHOLIPIDS

    PLA2 - phospholipaseA2

    Arachidonic Acid- Undergo oxygenation

    Isoprosteine Epoxygenase Lipoxygenase Cyclooxygenase

    CYP450 (most
    abundant in liver
    PROSTANOIDS
    for drug HPETE
    metabolism) (hydroxypeeroxyeicosatetraeinoic
    acid)
    CYP450
    epoxygenase
    PGI TXA2 Prostacyclin

    HETE LEUKOTRIENE LIPOXIN

    NOTE!!
    Vasoconstrictors: Prostaglandin F, Isoprosteine,
    Thromboxane, HETE

    Mother compound & most abundant precursor of


    EICOSANOIDS: Arachidonic Acid (derived from Linoleic
    acid)
    CYCLOOXYGENASE PATHWAY
    Aka Prostaglandinendoperoxide Synthase Pathway

    COX 1- gives cytoprotection


    Older generation of anti- COX 1 blocker- remove cytoprotection,
    prostaglandin: block both/ non- irritate the stomach
    selective COX inhibitor w/c are
    irritant to the stomach
    Ex. Indomethacin, Ibuprofen COX 1/ PGH
    Synthase 1
    Present: COX2 selective inhibitor -cytoprotection
    Inhibit pain and inflammation without
    irritating the stomach
    Ex.-coxib, diclofenac (only COX2 not
    ending in -coxib) COX 2/ PGH
    Synthase 2
    -develop inflammation

    COX 2 selective blocker- reduce


    inflammation

    THROMBOXANE (TXA2)
    -powerful vasoconstrictor
    -platelet aggregator
    -mytogenic

    PROSTAGLANDIN
    -pain stimulant
    Anti-prostaglandin: pain reliever

    Misoprostol (PGE)
    BN: Cytotec
    -used to terminate pregnancy
    -developed because it can prevent stomach ulcers specifically peptic ulcer
    -cause contraction of uterus
    -contract GI tract
    -induce labor

    Latanaprost
    -used to treat glaucoma

    Alprostadil (PGE)
    BN: Caverject
    -affect penile erection (injected head of penis)
    -dilate the corpus cavernosum
    PROSTACYCLIN (PGI)
    -Vasodilator
    -Inhibit platelet aggregation

    EFFECTS ON ORGANS

    MUSCLE
    TXA: constriction on blood vessel
    PGF: vasoconstriction and mytogen effect
    PGE: vasodilator
    PGI: vasodilator

    GI TRACT & UTERUS


    PGF2: Contraction
    PGE2: Contraction, Erection on Penis
    TXA: Uterine contraction

    AIRWAYS
    TXA: constract respi. muscle
    PGF: contract respi. muscle
    PGE: relax respi. muscle
    PGI: relax respi. muscle

    PLATELET
    TXA: platelet aggregation
    PGI: inhibit platelet aggregation
    Renin- stimulates the liver to produce Angiotensinogen
    KIDNEYS
    PGE & PGI: Increase in renin release
    ANG I (goes to lungs)
    GLOMERULUS
    PGE & PGI: Vasodilating effect (increasing the
    Glomerular filtration= Increase urine production) ANG II (cause vasoconstriction)

    CNS
    PGE, PGI, PGF: Increase temperature
    PGD: Induces sleep

    NEUROTRANSMITTER Epinephrine & Norepinephrine:


    PGE: inhibit release of norepinephrine (vasodilation) Vasoconstrictor

    NSAIDS (non-steroidal anti-inflammatory


    BONE
    drug)- block prostaglandin
    Eicosanoids: increase bone turnover/ increase bone loss Effect on Epinephrine/ Norepi release:
    Increase
    Inhibit COX pathway: slowing of skeletal Effect on Blood Vessel: Constriction
    muscle healing

    Research studies on:


    EYE COX pathway inhibitor: reduce tumor

    Tumors are produced secondary to inflammation


    PG: increase the outflow of aqueous humor

    Inhibit COX pathway:decrease formation of nasal


    polyp

    LIPOOXYGENASE PATHWAY

    LEUKOTRIENE (LT)
    TRIAD of BRONCHIAL ASTHMA
    -BROnchoconstriction -constriction
    -MUcos secretion -mucus secretion
    -bronchial EDema -edema

    Tx of Bronchial Asthma:
    Block leukotriene

    APPROACHES TO BLOCK LEUKOTRIENE:


    1. Block Leukotriene Receptor (most common)
    Ex. of Leukotriene Receptor Blockers: Zafirlukast, Montelukast
    -Does not relieve bronchial asthma immediately/ not for immediate effect
    2. Block the Lipooxygenase
    3. Block PLA2
    4. Block 5-Lipooxygenase activating protein
    Ex. Zileuton

    EFFECTS of LEUKOTRIENE ON ORGANS

    RESPIRATORY CARDIOVASCULAR
    -constriction -chemoattractant
    -mucos secretion -vasodilation
    -edema (increase vascular permeability)
    EFFECTS of HETE ON ORGANS
    -stimulate release aldosterone
    -causes reabsorption of sodium
    -increase intravascular fluid

    EPOXYGENASE PATHWAY
    -Vasodilator

    ISOPROSTEINE PATHWAY
    -Vasoconstrictor

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