Anti Allergic Drugs

ANTI-ALLERGIC DRUGS
Mechanism of Allergy
Common Symptoms Of An Allergic Reaction
1. Allergic rhinitis (Itchy, runny or blocked nose, Sneezing)

2. Itchy, red, watering eyes (Conjunctivitis)
3. Wheezing
4. Chest tightness
5. Shortness of Breath
6. Raised, itchy, red rash (Hives)
7. Swollen lips, tongue, eyes or face
8. Vomiting or Diarrhea
9. Dry, red and cracked skin
10. Occasionally, a severe reaction called Anaphylaxis.
Histamine and its Receptors
HISTAMINE is nitrogenous compound involved in

 Local immune response
 Regulation of GIT function
 Act as neurotransmitter in brain
 Involved in inflammatory response
Four types of HISTAMINE RECEPTORS are identified

 H1 (Present in Bronchial smooth muscle, Heart, Mucous membrane, Eye, Central
nervous system and Blood vessels)
 H2 (Present in Gastric parietal cells, Blood vessels, Bronchial smooth muscles)
 H3 (Present in CNS and nerve endings)
 H4 (Present in Leukocytes)
H1 and H2 are best understood and involved in the allergic response.
Physiological Function of Histamine
On Binding with H1 receptor, Histamine causes

 Increased production of nasal and bronchial mucus (Respiratory symptoms)
 Bronchoconstriction (Asthma like symptoms)
 Intestinal muscle constriction (Intestinal cramps and diarrhea)
 Sensory nerve endings stimulation (itching or pain)
 Positive inotropic effect
 Wheal and Flare response (Dilation and increased permeability of capillaries result in
protein and fluid leakage into the tissue)
On binding with H2 receptor, Histamine causes

 Stimulate gastric acid secretion
 Positive inotropic and chronotropic effect
 Itching
 Wheal and Flare response (Dilation and increased permeability of capillaries result in
protein and fluid leakage into the tissue)
Ocular Allergy Manifestation of Histamine
Histamine release in eye produces characteristic

manifestations of ocular allergy that includes
 Itching (Due to stimulation of Conjunctival nerve)

 Tearing
 Chemosis
 Lid edema
 Dilation of conjunctival blood vessel
 Papillary reaction (small round bumps (papillae) develop on the
underside of the eyelid)
Treatment Options for Allergic Eye Diseases
Following are the treatment options that have

proven useful for alleviating the signs and symptoms
associated with ocular allergic reactions.
 Topical Decongestants,
 Topical and Oral Antihistamines,
 Mast Cell Stabilizers,
 Certain Non-steroidal Anti-inflammatory Agents
1. DECONGESTANTS
The synthetic adrenergic agonists—phenylephrine,

naphazoline, oxymetazoline, and
tetrahydrozoline—are available as ocular
decongestants.
These agents provide only symptomatic relief, because
they have no effect on the conjunctival response to
antigen.
At the concentrations used for ocular decongestion,
phenylephrine causes vasoconstriction by direct
stimulation of α-adrenergic receptors on the
conjunctival vasculature. The resultant clinical effect is
usually a decrease in conjunctival hyperemia and edema.
Cont…
Newer drugs i.e. oxymetazoline, tetrahydrozoline etc

exhibit greater α- than β-adrenergic receptor activity. After
topical application to the eye, they induce a marked
vasoconstriction.
These newer drugs seem to have a clinical advantage over
phenylephrine in that they are less likely to induce rebound
congestion and pupillary dilation.
SIDE EFFECTS:
 Transient stinging
 Pupillary dilation, Rebound congestion (Phenyephrine)
 Blurred vision
2. ANTIHISTAMINES
 ORAL H1 ANTIHISTAMINES
 The first-generation H1 antihistamines, also referred to as
sedating antihistamines, and the second-generation
antihistamines, the less or non-sedating antihistamines, are
among the most frequently used oral medications for ocular
allergies.
 Classification:
First Generation H1 Second Generation H1
Antagonist (Sedating) Antagonist (Non-Sedating)
Chlorpheniramine Cetrizine
Cyclizine Fexofenadine
Dimenhydrinate Loratidine
Cont…
Difference between first and second generation

Antihistamines
First Generation Antihistamines Second Generation Antihistamines
Can cross blood brain barrier Cant cross blood brain barriers
CNS depressing effect Less CNS depressing effect
Highly sedative drugs Less or no sedation
Has autonomic effect No autonomic effect

Cont…
 These compounds do not influence the formation or release of

histamine; rather, they block the receptor-mediated response
of a target tissue.
 The first generation antihistamines has the ability to cross
blood brain barrier and have CNS depressant effect but second
generation antihistamines do not able to cross BBB and thus
causing no or less CNS depression.
 CLINICAL USES:
 Oral antihistamines provide symptomatic relief of nasal and
conjunctival itching, sneezing, congestion, and watery and red eyes.
 Oral antihistamines are therefore effectively used in patients with
moderate to severe eyelid edema and chemosis.
Cont…
SIDE EFFECTS:
 Increased sedation (In case of First generation antihistamines)
 Headache
 Muscarinic blockade (Dry mouth, Urinary retention, Constipation,
Mydriasis)
 GIT Disturbance
 Palpitation
Cont…
TOPICAL H1 ANTIHISTAMINE
Antihistamines currently available for topical
ophthalmic use include
 The first-generation agents pheniramine maleate and antazoline
phosphate.
 The second-generation antihistamines azelastine and ketotifen.
CLINICAL USES:
 The combination of antazoline phosphate and naphazoline
formulation significantly inhibited signs and symptoms of
itching, redness, chemosis, lid swelling, and tearing.
Cont…
SIDE EFFECTS:
 Burning, stinging and discomfort on instillation
 Mydriasis
 Keratopathy (antazoline-naphazoline)
3. MAST CELL STABILIZERS
Drugs included in this group

 Cromolyn sodium
 Nedocromil
These agents inhibit mast cell degranulation and

release of mediators of allergic disease by preventing
calcium influx across mast cell membranes.
They also act by inhibition of the activation of other
cell types, including neutrophils, monocytes, and
eosinophils.
Clinical Uses and Side effects of Mass Cell Stabilizer
Mast cell stabilizers may be used in the treatment of all

types of allergic eye diseases, including allergic
conjunctivitis etc.
The typical dosage for mast cell stabilizers is four times a
day, with a maintenance dose of twice a day. Nedocromil
is the exception, because there is a more rapid response,
and dosage is twice a day.
Pemirolast is used to treat the itch in allergic conjunctivitis.
Mast cell stabilizers have very low incidence of SIDE
EFFECTS and relatively safe to use. But sometime
HEADACHE may occur.
OTHER AGENTS
Some Steroidal and Non-steroidal anti-inflammatory

drugs can also be beneficial for allergic
conjunctivitis.
KETOROLAC (NSAIDs) and LOTEPREDNOL

(Steroid) are beneficial in treating different type of
ocular allergic symptoms.

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ANTI-ALLERGIC DRUGS

1. Allergic rhinitis (Itchy, runny or blocked nose, Sneezing)

HISTAMINE is nitrogenous compound involved in

Four types of HISTAMINE RECEPTORS are identified

On Binding with H1 receptor, Histamine causes

On binding with H2 receptor, Histamine causes

Histamine release in eye produces characteristic

 Itching (Due to stimulation of Conjunctival nerve)

Following are the treatment options that have

The synthetic adrenergic agonists—phenylephrine,

Newer drugs i.e. oxymetazoline, tetrahydrozoline etc

Difference between first and second generation

First Generation Antihistamines Second Generation Antihistamines

CNS depressing effect Less CNS depressing effect

Highly sedative drugs Less or no sedation

Has autonomic effect No autonomic effect

 These compounds do not influence the formation or release of

Drugs included in this group

These agents inhibit mast cell degranulation and

Mast cell stabilizers may be used in the treatment of all

Some Steroidal and Non-steroidal anti-inflammatory

KETOROLAC (NSAIDs) and LOTEPREDNOL

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