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Antihistamines

Actions of histamine on H1 and H2 receptors


Increase production of nasal and bronchial mucus
(H1)
Constriction of bronchioles results in symptoms
of asthma (H1)
Action on sensory nerve endings causes itching
and pain (H1)

Lowers systemic blood pressure by reducing


peripheral resistance (H1,H2)
Reddening of the skin due to local vasodilation
(H1,H2)
Stimulation of gastric Hcl secretion(H2 )

Histamine antagonists
adrenaline
antihistamines
corticosteroids

It is the main physiological antagonist that antagonizes the effects of histamine by


producing opposite effects. It causes bronchodilatation and vasoconstriction
Blocks histamine receptors and prevent histamine from reaching its sites of
actions. (used in acute and chronic allergic conditions)
They stabilize mast cells and prevent the formation and release of histamine.they
are used in severe acute conditions (with adrenaline)and in chronic conditions
with antihistamines

First generation ( sedating)


Clemastine
Doxylamine
Mequitazine(primalan)R
Dimetindene
Cyclizine(emetrex)R
Dimenhydrinate

Chlorpheniramine
Chlorphenoxamin
e
Pheniramine(avil)R
Cyproheptadine
Diphenhydramine
promethazine

Chlorphenoxamine(allergex)R

Second generation ( nonsedating)


Fexofenadine
Acrivastine
Desloratadine
Loratadine
Ebastine

Desloratadine (desa)R

Cetirizine
Levocetirizine
terfenadine

acrivastine(semprex)R

pharmacokinetics
.the onset of action occurs within 1 to 3 hours-1
The duration of action for many oral H1 antihistamines is at least 24 hours,facilitating once-daily -2
dosing. They are most effective when used prophylactically before allergen exposure rather than as
.needed
. Tolerance to the action of H1 antihistamines has not been observed-3

Therapeutic uses
Allergic and inflammatory-1
conditions (allergic rhinitis and
urticaria)

Motion sikness and nausea-2


Treatment on insomnia-3
Diphenhydramine(sultan)R
Diphenhydramine
Dimenhydrinate(dramenex)R
Doxylamine(donormyl)R
R
Cyclizine(emetrex)
Promethazine(phenergan)R
antihistamines are frequently used in combination preparations for the treatment of coughs and -4
colds The mechanism of their antitussive action may involve reduction in cholinergic nerve
transmission or may simply result from their sedative effects
.cyproheptadine is used for prophylaxis of migraine and also increase appetite -5
antihistamines are the drugs of choice in controlling the symptoms of allergic rhinitis and urticaria, because histamine is the principal mediator However, the H1 receptor blockers are ineffective in
.treating bronchial asthma, because histamine is only one of several mediators of that condition
although the margin of safety is high and chronic toxicity is rare, acute poisoning is common .especially in young children

Adverse effects of sedating antihistamines


First-generation H1 -receptor blockers have a low specificity; that is, they interact not only with
histamine receptors but also with muscarinic cholinergic receptors, -adrenergic receptors, and
serotonin receptors The extent of interaction with these receptors and, as a result, the nature of the
side effects vary with the structure of the drug. Some side effects may be undesirable, and others may
have therapeutic value

cholinergic

-adrenergic

dry mouth
urinary retention
sinus tachycardia

hypotension
dizziness
reflex tachycardia

serotonin
appetite

Histamine H1
allergic inflammation,
itching,rhionrrhea
neurotransmission in
the CNS
sedation

Sedating antihistamines should be avoided in severe liver disease as they increase risk of coma
Most manufactures of antihistamines advise avoiding use during pregnancy however, there is no
evidence of teratogenicity except for hydroxyzine and loratadine


drug
Active constituent

pirafene

tavegyl

avil

chlorpheniramine

clemastine

pheniramine

drug

Fenistil
zyrtec

Active constituent
Dimetindene
3
Cetrizine

dose
3-1 30 10

4-3 45 30 3
5 10 6 3
2.5 2.5

10=(1) 20 =
Active constituent
Chlorpheniramine
Clemastine
Cyproheptadine
Dimenhydrinate

drug

dose

Allergyl ,anallerge,pirafene

3



5 2.5 3 1
5
6 3
7 2
2 14 7
3 2

) ..
)
(
5 3-6)..
(
2.5
2-5
5
6-11

12

5

Tavegyl

Triactin
3 2
Dramenex

Cetirizine

Zyrtec,cetrak,histazine,tomazine

Ebastine

Evastine,ebastel,astin,bastab

Loratadine
Fexofenadine

Claritine,lorano,loratan,mosedin
Alertam,allerfen,fastel,telfast.rapido

() ( )