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1. AUTOCOIDS

2. HISTAMINE INHIBITORS





B2 agonists
Cromolyn
Epinephrine
Glucocorticoids
Theophylline

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. 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. H1- Receptor Antagonists

1st Generation
 Cyproheptadine
 Diphenhydramine
 Meclizine
 Promethazine

2nd Generation
 Cetirizine

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. Question


DOC for Hay fever or urticaria?
DOC for prevention of motion sickness?

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. Cetirizine (Zyrtec)



Reduces histamine effects on SM and immune
cells
IgE immediate allergies, hay fever, urticaria
2nd generation H1 antagonist

10. H2 – Receptor Antagonists



Cemitidine
Famotidine
Ranitidine

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. 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. 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. 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. 5-HT Agonists





Buspirone
Ergonovine
Ergotamine
LSD
Metoclopramide

16. 5-HT1B/1D Agonists



Eletriptan
Sumatriptan
Zolmitriptan

17. 5-HT Antagonists





Butyrophenones
Cyproheptadine
Ketanserin
Ondasetron
Phenoxybenzamine

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. Question


What are the DOC for SEVERE ACUTE
MIGRAINE?
Treatment of CLUSTER HEADACHE?

Triptans, Sumatriptan

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. 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. 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. 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. Effects of Eicosanoids

Blood:
 TXA2
is powerful inducer of platelet aggregation
 PGI2 inhibits platelet aggregation
 LTB4 is a chemotactic agent

25. Lipid – Derived Autocoids

Prostaglandins
 Alprostadil
 Carboprost
Tromethamine
 Dinoprostone
 Epoprostenol
 Latanoprost
 Misoprostol

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. Alprostadil
PGE1 analog
 2nd line of defence against erectile dysfunction
 Toxicity: penile pain, prolonged erection, and
priaprism (persistant erection)

 “The
permanent boner” drug

28. Carboprost Tromethamine


PGF2alpha analog
2nd trimester abortion

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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