Professional Documents
Culture Documents
Submitted to-
Dept. of VPT
Submitted by-
2020-VL-40,44,46
What are autacoids?
CHEMICAL
STRUCTURE
Peptide
Lipid
Amine autacoids
derived
autacoids autacoids
Kinins(Bradykini
n and Kallidin Eicosanoids(
Histamine PG, LT, TXA)
Angiotensins
Platelet
Serotonin/ Tachykinins activating
5HT
factor
Cytokines
Amine autacoids
Histamine
Extrusion of
Chemical, Rise in contents of
mechanical, granules by
physiological intracellular exocytosis
stimulation Ca2+ level (degranulation
)
Metabolism & excretion-
● Excreted through
urin.
Mechanism of action-
1. On CVS-
● Dilation of smaller blood vessels, decrease Peripheral
resistance and fall in BP.
● Capillary permeability- increases, resulting oedema
formation.
● In Heart- produces both chronotropic & inotropic effect.
● Triple response- I/D,
Reddening- vasodialtory effect.
Wheal- increase in capillary permeability
Flare- stimulation of axonal reflexes, causes
Vasodilation indirectly
Contd.
02 Inflammation-
03 Gastric secretion
04 Neurotransmission
06 Regulation of microcirculation
1. BETAZOLE
2. PENTAGASTRIN
3.BETAHISTINE
Histamine blocking drugs-
Works in 3 way
1. Prevention or reduction of histamine release
from sensitized mast cells.
2. Use of physiological antagonists.
3. Histamine receptor antagonists- competitively
blocking,
H1 receptor antagonist-
● based on sedation-
● First generation
1. High sedation - Eg:
Diphenhydramine ,Dimenhydramine,Promethazine
2. Moderate sedation - Eg: Pheniramine, Antazoline,
Trimeprazine, Cyproheptadine
3. Low sedation - Eg: Chlorpheniramine, Mepyramine
● Second generation
1. No sedation - Eg:
Terfenadine,Astemizole,Loratadine,Cetirizine
2. Anti vertigo - Eg: Cinnarizine
PHARMACOLOGICAL ACTIONS OF ANTIHISTAMINES
● serotonin/5-hydroxytryptamine /5HT-
biogenic amines
● Chemical name- β-
aminoethyl 5-hydroxyindole.
● Primarily found- GIT, platelets, CNS.
● Act as a neurotransmitter in the CNS
● Regulation of smooth muscle function in GIT & CVS,&
in platelets formation.
● enteramine/vasotonin.
● 80% - enterochromaffin cells of GI tract.
● Precursor for melatonin
Synthesis-
Stored
mainly on
enterochro
mafin cells &
neuron.
Metabolism-
5-HIAA, major
metabolite of
serotonin -
excreted in
urine serve as
indicator
Mechanism of action
● Receptor mediated.
Physiological and pharmacological effects
1. On cardiovascular system
● Arterioles are constricted by its action on the smooth
muscles.
● In rapid intravenous injection - a triphasic curve in
blood pressure
early sharp fall - stimulation of coronary
chemoreceptor
an brief rise - vasoconstriction
prolonged fall - arteriolar dilation and extravasation of
fluid.
Physiological and pharmacological effects
3.On glands-
● inhibits gastric secretion and increases mucous production.
● ulcer protective effect.
4.On platelets-
● change in the shape of platelets and is a weak aggregator.
● Neurotransmitter-
● Inflammation and allergy
● Gastrointestinal function- regulation of peristalsis
● Nausea and vomiting- mainly through 5HT3 receptors
● Haemostasis- platelet aggregation and
vasoconstriction.
● Carcinoid syndrome- tumour of enterochromaffin
cells.
Serotonin receptor agonists-