Autacoids

AUTACOIDS
=>

Local hormone
·

Ex:Histamine, Serotonin, Pl, Leukotrienes, PAF, angiotensit

-

HISTAMINE
=>

histidine
synthesized by decarboxylation of
-

-presentin most cell

of skin,
lung, live, placenta

->

Histamine liberators

~
~
~
~

E 3

· Betalistine:- Histamine analogu

head
-
Treat
veatigo
X: nausea, vomiting,
a che
-

Improve BFin inner ear

classification
=>

CANTIHISTAMINES)

& MOA blockers: block H,

of HI Competiterly receptors

Ac" -> Hi blockers cause:

P (NS 1, sedath, drowsiness, antiemetic, anti-parkinonian

② Anti
allogic
③ ac
Anticholinergic
A
-
- M
-
E
P.K oral, parenteral liver
- -
->
every Urine

Adverse effects:ICNS SE:sedat", drowsines, headach

<side effect ② GIT SE:nausea, vomitting, I appettite

③ Anticholinergic SE:Dry mouth, blurred vision

Teratogenic
④ effecti
5 Allergic rx
USES
=>

① Allergic diseases:Preventand treat

symptom of:
-

Pruvitis, urticaria, rhinitis, conjunctivitis

② Common cold:symptomatic relief by sedative, anticholinergic ac

③ Pre-auesthetic:Promethazine

Anti-emetic
④ (Anticholinergic ach)

* Promethazine, diphenhydramine.

⑦
Parkinsonism (Imbalance blu DA - Ach)
control
-used to tremor,
rigidity, sidorrhoea [auticholing is
and sedative properties]

CH, blockers:Used to control blood transfusion win, chils, rigors

⑦ vertigo:Cinnarizine, meclizine
⑧ sedative and
hypnotic
⑨ Acute
muscle dystonias:Due to
antipshycotici
 second
=>

gauration H, blockers
* Getrizine, levacltrizine
① No anticholinergic effecti
② No antiemetic effect
③ Dontcross BBB (no drowsiness)

⑭ Don'timpair
psychomotor performance
⑤
Expensive
i
Notmetabolized in
body ->
dalythmias
nasal spray
Uses
↑
=>

Allergic rhinitis,
① hay fees -> atrizine, mizolastine, azelastine

⑧ allergies -> abrizine, mizolastine

skin

③ Allergic conjunctivitis eye drops

-
 Degale of sedation H1 blockers:
of
·

->

High (Diphenhydramine, promethazine)

-->Moderate (meclizine, planiramine)

->
Mild (chlorpheniramine)

* Don'tprescribe antihistaminics to
drivers or
operators.

Anti
vertigo drugs
=>

① Cinnarizine
-

,stgen He blocker
-

Anticholinegic and vasodilator properties

entry of Catinto vestibular
x cells
-

② Antihistaminics, antichdinegics
-Labry inthe suppressant

③ Cortico steroids
-

I edence in labryinth

⑭
Furosemide
-causes drainage of third from inner ear

xpressure
-
 AUTACOIDS
Local hormones

HISTAMINE ANTI HISTAMINE

Histamine BiomenicAmine

Naturally present in animalplanttissue a venom

stinging secretion
Decarboxylation
of histidine Histamine
storedin granules
g mastcans Cliver lung skin placenta

MOMMY

I
r in capillary permeability

g Hareceptors Acamp a gastricacidsecretion

A
M
N
skingastric mucosa
my receptors I came chemotaxis
cytokinesecretion

AntigenAntibodyon Release
LiberatorsCW
of
histamine
Food
Bilesalts
Drugs Ggg Janina
urticaria
hypotension
mastcell concarria
ensuing
analoesemn
y

uset No valid clinical use

BETAHISTIDINE histamine analogue

Used orally to treat vertigo in meniere's disease

inner ear
Probably works by improving blood flow in
Sideeffect nausea vomiting headachepruritus
contraindication Asthma
peptic vicar
 ANTI HISTAMINES

off competitively blocks H receptor

t
Histamine
y Hireceptor a Antihistamine
agonist antagonist

FRST GENERATION H BLOCKER

Lesspotent
sedating
Antimuscarinic
armacological C's depression sedation drowsiness
actions
some are antiemetic local anaesthetic anti parkinsonism

Antiallergic type an suppression

Anticholinergic actions
drynessofmouth blurring g vision constipation urinary retention
Due to 0 dont give whiledriving on operating machines
kinetics
narmaco A oral parenteral
D widely
M Liver
E urine

averse common are sedation drowsiness lack cons

effect of headache fatigue lassitude

onside effect nausea vomiting epigastricdiscomfort

Anticholinergic dryness of mouth blurring constipation
effects a mouth

Teratogenic effect in some animals

Allergic ran rare contact dermatitis on topical admistration

uses Allergicdisease
common cold
Pre anaesthetic

Antiemetic
Parkinsonism

Bloodtransfusion a
vertigo in menieresdisease
sedative a hypnotic
 hyp
Acutemuscle dystonia

SECOND GENERATION HI BLOCKERS

morepotent
Nonsedating Edo not cross0003
Donot block muscarinic action eno anticholinergic effects
expensive

Mleused cerriz ne y thblocking effect minimaldrowsiness

inhibitrelease
g histamine not metabolized
lessside effects

set Allergicdisorders rhinitis

dermatitis
conjunctivitis
urticaria
eczema
drug a foodallergies

Allergicrhinitis Foremanme
hayfever cerrizine oral
Mizocaseinc
ruparabine
Nasalspray in allergicrhinitis
Azelastine
Eye drops in ameagre conjunctivitis

VERTIGO sensation
ofrotation movement ofone'sselfor surrounding
Anti vertigo drugs inanyplane

H blockers cinnaazine promeenazine Dimenhydrinate

anticholinergic hyoscine
phenothiazine procurorperazine sine first gen h blocker aentry a cartin resting
anticholinergic vasodilators
Hianalogue oceans
diuretics Furosemide Azerouamide antihistaminic
Benzodiazepine
Diazepam anticholinergic Labyrinth
Proaniorperasine suppressants
Tea Amirpenne
acucocorticons corticosteroids a oedemain iannone
Furosemide drainage g juicefrominnerear
5 HYDROXY TRYPTAMINE
Serotonin She neurotransmitter
synthesized from AA tryptophan

High conc in intestine platelets brain

Usedin migraine GI disorder sleep affective disorder

serotonin RECEPTORS
subtypes

All are a protein coupled except 5h3 ligandgatedion

channel

HT ANTAGONISTS
Hi receptor 5mean blocker
cypronepeadine
sedative antipruritic a anticholinergic effects
9 appetite
uses carcinoid a post gastrectomy dumpingsyndrome
sideeffects Drymouth weightgain drowsines

KETANSER N smear antagonist a x blocker

Antihypertensive effect

ON
DanseTron 5h5 receptor antagonist
Graniserron Antiemetics

Atypical antipsychotics sues blockers

schizophrenia

mermuseRIDE streams antagonist

Prophylaxis of migraine
causes abdominal pulmonary
Long term use fibrosis

purpura
Error Acracons naturally occur in fungusclaviceps
contraindicated in this no pro
renaldisease
DRUG THERAPY OF MIGRAINE

Migraine common debilitating condition

Migraine attack initial visual disturbance a severe usually throbbing

Laura
vomiting
headache
often with photophobia nausea

Nsaids alone or in combination

symptomatic relief
used in mild a moderate migraine
should not be taken on long term basis

American
Anti Treat nausea a vomiting associated with attack

Improve oral absorption of oral medications

formigraine

oral sublingual suppository

m fi n T at onset of pain or warning symptoms

absorption Modes Partial agonist at she receptors in cranial

Br
vasoconstrictoreffect

I
constriction
trendy
dilated cranial or
of
d inflammation
extravasation of plasma into perivassul

DIHYDROERGOTAMINE im iv see
12mgiriselim safer for parenteral use than ergotamine
 Sumatriptan
TRiPTANSy selective 5 HT Blip agonists Rizatriptan
Used in moderate a severe migraine tietriptan
Almotriptan
Zoimitriptan
Abnormal Cerebral Migraine Naratriptan
BV
dilation of ischaemia attack
Mjg Frovatriptan

Selective 547,011 constrict dilated Restor

Triptanis cerebral
agonists cranial or a blood
AV shunt flow

I 514T Vasoactive peptide release by acting

on 5 HT B12 receptors on presynaptic
nerveending

Inhibit extravasation of PP in perivascular spat

By inni