AUTOCOIDS
HISTAMINE INHIBITORS







B2 agonists
Cromolyn
Epinephrine
Glucocorticoids
Theophylline
HISTAMINE



Binds H1 – H4 (all G-protein coupled) receptors
H1 receptor: SM, brain




H2 receptor: gastric mucosa, c...
HISTAMINE


Neurons







Female Reproductive system






SM contraction (H1)  diarrhea

Heart




Gastric a...
H1- Receptor Antagonists


1st Generation
 Cyproheptadine
 Diphenhydramine
 Meclizine
 Promethazine



2nd Generatio...
H1-Receptor Antagonists





1st gen: strong sedative effects, enter CNS
2nd gen: much less sedating
MoA: Reversible c...
Question




DOC for Hay fever or urticaria?

DOC for prevention of motion sickness?
Diphenhydramine (Benadryl)






Reduces histamine effects on SM, immune
cells, and blocks muscarine and alphaadrenorec...
Cetirizine (Zyrtec)





Reduces histamine effects on SM and immune
cells
IgE immediate allergies, hay fever, urticaria...
H2 – Receptor Antagonists




Cemitidine
Famotidine
Ranitidine
H2 – Receptor Antagonists




MoA: - Competitive inhibitors of H2-receptors
in gut parietal cells  inhibits cAMP produc...
Serotonin  binds 5-HT receptors




Involved in migraines, gut, blood clotting,
carcinoid syndrome
90% stored in EC cel...
Serotonin







Chemoreceptor reflex and vomiting reflex
mediated by 5-HT3
Neurons: stimulates pain and itching
No ma...
Carcinoid Syndrome


Secondary to carcinoid tumors
 Discrete,

yellow, well-circumscribed tumors that
occur anywhere alo...
5-HT Agonists






Buspirone
Ergonovine
Ergotamine
LSD
Metoclopramide
5-HT1B/1D Agonists





Eletriptan
Sumatriptan
Zolmitriptan
5-HT Antagonists








Butyrophenones
Cyproheptadine
Ketanserin
Ondasetron
Phenoxybenzamine
5-HT Agonists


Triptans – orally administered
 5-HT1B/1D

(found in cerebral and meningeal
vessels) mediates vasoconstr...
Question




What are the DOC for SEVERE ACUTE
MIGRAINE?
Treatment of CLUSTER HEADACHE?



Triptans, Sumatriptan
Ergot Alkaloids









5-HT, dopamine, and alpha-receptor agonists
Oral bio of Ergotamine is little; Ergonovine is
...
Question


Drug for FIRST SIGN of migraine attack?
 Ergonovine/Ergotamine



Drug for hyperprolactinemia?
 bromocripti...
Eicosanoids








COX-1: - constitutively expressed; inhibited by
NSAIDS
COX-2: - inducible expression, inhibited by...
Effects of Eicosanoids


Vascular:
 PGE2

and PGI2 are potent arteriolar vasodilators
 TXA2  potent vasoconstrictor
 ...
Effects of Eicosanoids


Blood:
 TXA2

is powerful inducer of platelet aggregation
 PGI2 inhibits platelet aggregation
...
Lipid – Derived Autocoids


Prostaglandins
 Alprostadil
 Carboprost

Tromethamine
 Dinoprostone
 Epoprostenol
 Latan...
Lipid – Autocoid Inhibitors







Glucocorticoids – inhibit PLA2 and COX-2
Cromolyn
Montelukast
NSAIDS – inhibit CO...
Alprostadil
PGE1 analog
 2nd line of defence against erectile dysfunction
 Toxicity: penile pain, prolonged erection, an...
Carboprost Tromethamine



PGF2alpha analog
2nd trimester abortion
Dinoprostone






PGE2 analog
Vaginal adiministration
2nd trimester abortion, benign hydatidiform
mole, ripening of c...
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Pharmacology: Autocoid drugs flashcards

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  • Ergonovine/Ergotamine, bromocriptine (D2 receptor agonist) & cabergolide (ergot alkaloid), Ergonovine
  • Pharmacology: Autocoid drugs flashcards

    1. 1. AUTOCOIDS
    2. 2. HISTAMINE INHIBITORS      B2 agonists Cromolyn Epinephrine Glucocorticoids Theophylline
    3. 3. HISTAMINE   Binds H1 – H4 (all G-protein coupled) receptors H1 receptor: SM, brain   H2 receptor: gastric mucosa, cardiac muscle, mast cells, brain   Activates IP3/DAG Increases cAMP H3 receptor: presynaptic membranes in brain, myenteric plexus, other neurons  Inhibits cAMP production and Ca2+ influx   Decreases release of Nepi, serotonin, histamine, etc H4 receptor: leukocytes in BM and blood  Exerts chemotactic effects on eosinophils and mast cells
    4. 4. HISTAMINE  Neurons      Female Reproductive system    SM contraction (H1)  diarrhea Heart   Gastric acid secretion (H2) Intestines   Bronchoconstriction (H1) Stomach   Contraction of uterus (H1)  abortion in woman w/ anaphylactic rxn Respiratory System   Mediation of pain and itching (H1) Urticarial response to insect stings (H1) Inspiratory/expiratory centers (H1) Release of nt (H3) Increase HR, contractility, and pacemaker rate (H2) Metabolic (H3) CV system  Decrease systolic and diastolic bp due to vasodilation of arterioles and precapillary sphincters (H1 and H2)
    5. 5. H1- Receptor Antagonists  1st Generation  Cyproheptadine  Diphenhydramine  Meclizine  Promethazine  2nd Generation  Cetirizine
    6. 6. H1-Receptor Antagonists     1st gen: strong sedative effects, enter CNS 2nd gen: much less sedating MoA: Reversible competitive inhibition of H1 Effects: - inhibition of edema and itching Antinausea and antiemetic  Inhibition of bronchiolar and GI SM contraction   Therapeutic Uses: DOC in allergic rhinitis (Hay fever) and urticaria  Diphenydramine & Cetirizine  1st gen are good for prevention of motion sickness  Second choice for parkinsonism due to their central antimuscarinic effect 
    7. 7. Question   DOC for Hay fever or urticaria? DOC for prevention of motion sickness?
    8. 8. Diphenhydramine (Benadryl)    Reduces histamine effects on SM, immune cells, and blocks muscarine and alphaadrenoreceptors; highly sedative Uses: IgE immediate allergies, hay fever, urticaria, antiemetic, anti-motionsickness 1st gen H1 antagonist
    9. 9. Cetirizine (Zyrtec)    Reduces histamine effects on SM and immune cells IgE immediate allergies, hay fever, urticaria 2nd generation H1 antagonist
    10. 10. H2 – Receptor Antagonists    Cemitidine Famotidine Ranitidine
    11. 11. H2 – Receptor Antagonists   MoA: - Competitive inhibitors of H2-receptors in gut parietal cells  inhibits cAMP production  inhibits gastric acid secretion Therapeutic uses:  GERD, upset stomach (use prophylactically before meals)  Toxicity  Gynecomastia, galactorrhea, loss of libido, impotence  Leukopenia, thrombocytopenia
    12. 12. Serotonin  binds 5-HT receptors   Involved in migraines, gut, blood clotting, carcinoid syndrome 90% stored in EC cells of GI  Complex with ATP inside granules, released w/stimulus – thrombin, TXA2, reserpine (neurons)   In blood, stored in platelets Mediates inhibitory effects on behaviours: mood, sleep, appetite, temp regulation, pain perception, bp, vomiting
    13. 13. Serotonin     Chemoreceptor reflex and vomiting reflex mediated by 5-HT3 Neurons: stimulates pain and itching No major effects on respiratory system CV: - vascular SM contraction, vasoconstrictor of systemic vessels, induces platelet aggregation  5-HT2  Vasodilator in skeletal muscle and coronary muscles (NO-mediated)  GI: increased tone and peristalsis (5-HT2)
    14. 14. Carcinoid Syndrome  Secondary to carcinoid tumors  Discrete, yellow, well-circumscribed tumors that occur anywhere along the GI and lung  Neuroendocrine origin  overproduction of serotonin   Clinical presentation: flushing of skin (head, upper thorax), nausea, vomiting, 50% have cardiac abnormalities caused by 5-HT induced fibrosis of the tricuspid and pulmonary valves TIPS = Tricuspid Insufficiency, Pulmonary Stenosis  Affects  right side of heart Urine: 5 – HIAA (degradation product of 5-HT)
    15. 15. 5-HT Agonists      Buspirone Ergonovine Ergotamine LSD Metoclopramide
    16. 16. 5-HT1B/1D Agonists    Eletriptan Sumatriptan Zolmitriptan
    17. 17. 5-HT Antagonists      Butyrophenones Cyproheptadine Ketanserin Ondasetron Phenoxybenzamine
    18. 18. 5-HT Agonists  Triptans – orally administered  5-HT1B/1D (found in cerebral and meningeal vessels) mediates vasoconstriction  Inhibit vasodilator release from trigeminal nerve endings  Therapeutic uses  DOC for severe acute migrane  Treatment for cluster headache  Toxicity: cardiac arrhythmias, MI, paresthesias, dizziness, coronary vasoconstriction
    19. 19. Question   What are the DOC for SEVERE ACUTE MIGRAINE? Treatment of CLUSTER HEADACHE?  Triptans, Sumatriptan
    20. 20. Ergot Alkaloids      5-HT, dopamine, and alpha-receptor agonists Oral bio of Ergotamine is little; Ergonovine is high Induce mood changes, perceptual disorders, hallucinations Increased vasoconstriction due to alpha and 5HT receptor in the CV, GI, and Uterus Toxicity: prolonged vasospasm causing gangrene
    21. 21. Question  Drug for FIRST SIGN of migraine attack?  Ergonovine/Ergotamine  Drug for hyperprolactinemia?  bromocriptine (D2 receptor agonist) & cabergolide (ergot alkaloid)  Drug for postpartum bleeding?  Ergonovine
    22. 22. Eicosanoids     COX-1: - constitutively expressed; inhibited by NSAIDS COX-2: - inducible expression, inhibited by NSAIDS, glucocorticoids, and selective inhibitors Arachidonic Acid  PGG2  PGH2  other PGs, TXA2, tec MoA: IP3/DAG & Rho GTPase pathways, GPCR
    23. 23. Effects of Eicosanoids  Vascular:  PGE2 and PGI2 are potent arteriolar vasodilators  TXA2  potent vasoconstrictor  LTs strongly increase venule permeability  GI:  SM contraction by LTs and PGs  PGE2 and PGI2 have cytoprotective effects (secrete mucus/bicarbonate)  Respiratory:  Bronchial SM is relaxed by PGE2 and PGI2  LTs are powerful bronchoconstrictors
    24. 24. Effects of Eicosanoids  Blood:  TXA2 is powerful inducer of platelet aggregation  PGI2 inhibits platelet aggregation  LTB4 is a chemotactic agent
    25. 25. Lipid – Derived Autocoids  Prostaglandins  Alprostadil  Carboprost Tromethamine  Dinoprostone  Epoprostenol  Latanoprost  Misoprostol
    26. 26. Lipid – Autocoid Inhibitors       Glucocorticoids – inhibit PLA2 and COX-2 Cromolyn Montelukast NSAIDS – inhibit COX-1 and COX-2 Zafirlukast – blocks selective leukotriene rcpt Zileuton – inhibits 5-Lipoxygenase
    27. 27. Alprostadil PGE1 analog  2nd line of defence against erectile dysfunction  Toxicity: penile pain, prolonged erection, and priaprism (persistant erection)   “The permanent boner” drug
    28. 28. Carboprost Tromethamine   PGF2alpha analog 2nd trimester abortion
    29. 29. Dinoprostone     PGE2 analog Vaginal adiministration 2nd trimester abortion, benign hydatidiform mole, ripening of cervix to induce labor MoA: induction of uterine contractions and effects on cervical collagenase
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