1st Generation Anti-histamine - Reversible competitive inhibitors of

the interaction of histamine with H1

receptors.
Efficacy
Pharmacodynamics:
-more likely to block autonomic
receptors.
-widely distributed throughout the
body, and enter the CNS readily.
(more lipid soluble; crosses blood-
brain barrier)
- has similarity of the general
structure to the structure of drugs
that have effects at muscarinic
cholinoceptor, alpha adrenoceptor,
serotonin, and local anesthetic
receptor sites.
-produce sedation and anti-
muscarinic effects (sleep aid; prevent
motion sickness)
-Certain H1 antagonists have potent
local anesthetics by blocking sodium
channels in excitable membranes in
the same fashion as procaine and
lidocaine.
-have alpha adrenolytic activity which
can decrease the vasoconstrictive
effect of adrenaline and
noradrenaline.

Pharmacokinetics:
-well-absorbed from GI tract.
- peak plasma concentrations: 23
hours, and
effects usually last 46 hours
- Peak concentrations are achieved
rapidly in the skin and persist even if
plasma
levels have declinedinhibition of
wheal and flare
- metabolized in liver by CYPs.
-eliminated more rapidly by children
than by adults
Clinical Use: used for supportive care
 of allergic manifestations, cutaneous
(urticaria) or mucous membranes.
Safety -Unsuitable for daytime use due to
sedative effects (most frequent side
effect) which may manifest as
diminished alertness, slowed reaction
times, and somnolence.

-Next most frequent side effects:

involve the GI tract and include loss
of appetite,nausea, vomiting,
epigastric distress, and constipation
or diarrhea.

-Other antimuscarinic effects:

include dryness of the mouth and
respiratory passages (sometimes
inducing cough), urinary retention or
frequency, and dysuria.

-At very high dose levels, marked

stimulation, agitation, and even
seizures may precede coma.
-excitation is common in children
rather than sedation
-may cause urinary retention and
blurred vision.
- cannot be tolerated or used safely
by many patients unless given only at
bedtime
-antihistamine hangovermay
appear in the morning, resulting in
sedation with or without psychomotor
impairment.
-severe systemic overdosage
resemble those of atropine
overdosage

Contraindication:
-Contraindicated in machine
operators because there is
interference with safe operation of
machinery, which
occur in about 50% of subjects
 Drug interaction:
Additive effect with other drugs with
CNS depressant effects and
antimuscarinic effects.

Suitability
Cost