Anti - Histamine

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Autacoid : Anti - Histamine

H
, Antagonists :

actions
• These
drugs competitively antagonize of
Histamine at H
, Receptors .

Classified into first


Generation & Second Generation
compounds ( on the basis of CNS penetration and

anticholinergic properties )

FA ] First Generation Anti - Histaminic


Can penetrate Blood brain barrier and result in

sedation &
Psychomotor impairment .


Have
Anticholinergic activity .
Uses :

conditions (
(a) via H
,
Blocking :
ci,
Allergic itching ,

urticaria ,
hay fever )
Iii ' Insect bite and to
prevent
adverse
effects due to

histamine releaser s .

(b) via
Anticholinergic properties :
ci, Common cold

dis Motion sickness

Liii , Parkinsonism
(in Acute muscular

dystonia .

(c) Other Uses : in


Idiopathic purilis
Cinnarizine
(
in is
useful in
Vertigo .

Adverse Effects :

( is Sedation

ciii
Psychomotor
iii,
Impairment
in
Anticholinergic effects
( dryness of mouth blurred vision
, ,
urinary
retention , constipation )
[ B.) Second Generation Anti -
Histamine :


59 As are those H, Receptor blockers marketed
after 1980 which have one or more
of
the
followings :

cis Absence
of Cms
depressant property
iii.
Higher H
,
selectivity No anticholinergic
: side
effe
cts
Additional
-

iii.
antiallergic mechanisms
apart
from histamine blockade : some also inhibit

late Phase Rkn


Allergic .
.

* Terfenadine - Fastest
acting antihistaminic
drugs .


In overdose ,
it
delayed rectifier
blocks cardiac

Kt channels and
may
result
Polymorphic
in

Ventricular
Tachycardia ( Prolong QT interval )
Astemizole Slowest and
iii. -

longest Acting agent .


c
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