Antihistamines

Many antihistamine drugs are available without a prescription. Examples include the firstgeneration antihistamines such as brompheniramine (Dimetapp, Bromphen, Dimetane, Nasahist),
chlorpheniramine (Chlor-Trimeton), clemastine (Allerhist, Tavist), and diphenhydramine
(Benadryl), and a second-generation antihistamineloratadine (Claritin). Loratadine (Claritin)
does not cause drowsiness.
Common prescription antihistamines (all second-generation antihistamines) include cetirizine
(Zyrtec), desloratadine (Clarinex), and fexofenadine (Allegra). These antihistamines (and
loratadine) are less likely to cause adverse effects like drowsiness or dry mouth.
Several antihistamine nasal sprays (for example, azelastine [Astelin]) are also available to treat
symptoms such as runny nose, sneezing, and itchy nose.

How antihistamines work: These drugs compete with histamine for histamine receptor
sites. By occupying the histamine receptor sites, they prevent histamine from causing
allergic symptoms. Antihistamines are most effective when taken continuously during the
allergy season.

Who should not use these medications: Antihistamines are contraindicated in

individuals allergic to them. They may cause unwanted side effects in the following:
o Individuals currently using a monoamine oxidase inhibitor (MAOI)
o Individuals with narrow-angle glaucoma
o Individuals who are breastfeeding

Use: Antihistamines come in tablet, chewable tablet, capsule, and liquid forms. How
often an antihistamine should be taken each day depends on the individual antihistamine's
characteristics and the type of preparation (that is, the dosage form).

Drug or food interactions: Avoid taking other drugs that cause drowsiness, such as
alcohol, sleep preparations, sedatives, or tranquilizers. Avoid taking MAOIs (for example,
isocarboxazid [Marplan], phenelzine sulfate [Nardil], or tranylcypromine [Parnate])
within 14 days of antihistamines. For drug interactions specific to a particular
antihistamine, talk with a doctor or pharmacist.

Side effects: Many antihistamines (particularly the first-generation agents) may cause the
following side effects:
o Drowsiness
o Dry mouth
o Urine retention
o Blurred vision
o Before driving a car or operating machinery, be sure to know if the antihistamine
affects the ability to concentrate and stay awake.
o Check with a doctor before taking antihistamines.

http://www.webmd.com/allergies/guide/antihistamines

A histamine antagonist is an agent that serves to inhibit the release or action of

histamine. Antihistamine can be used to describe any histamine antagonist, but it
is usually reserved for the classical antihistamines that act upon the H1 histamine
receptor. Antihistamines are used as treatment for allergies. Allergies are caused by
an excessive response of the body to allergens, such as the pollen released by
grasses and trees. An allergic reaction indicates an excessive release of histamines
by the body. Other uses of antihistamines are to help with normal symptoms of
insect stings even if there is no allergic reaction.

H1-receptor antagonists

In common use, the term antihistamine refers only to H1 antagonists, also known as H1
antihistamines. It has been discovered that these H1-antihistamines are actually inverse agonists
at the histamine H1-receptor, rather than antagonists per se.[1] Clinically, H1 antagonists are used
to treat allergic reactions.
Examples:

Diphenhydramine
Doxylamine (most commonly used as an OTC sedative)
Loratadine
Desloratadine
Fexofenadine
Pheniramine
Cetirizine
Promethazine
Chlorpheniramine
Levocetirizine
Quetiapine (antipsychotic)
Meclizine (most commonly used as an antiemetic)
Dimenhydrinate (most commonly used as an antiemetic)

H2-receptor antagonists

H2 antagonists, like H1 antagonists, are also inverse agonists and not true antagonists. H2
histamine receptors are found principally in the parietal cells of the gastric mucosa. H2
antagonists are used to reduce the secretion of gastric acid, treating gastrointestinal conditions
including peptic ulcers and gastroesophageal reflux disease.
Examples:

Cimetidine

Famotidine
Ranitidine
Nizatidine
Roxatidine
Lafutidine

Experimental: H3- and H4-receptor antagonists

These are experimental agents and do not yet have a defined clinical use, although a number of
drugs are currently in human trials. H3-antagonists have a stimulant and nootropic effect, and are
being investigated for the treatment of conditions such as ADHD, Alzheimer's Disease, and
schizophrenia, whereas H4-antagonists appear to have an immunomodulatory role and are being
investigated as antiinflammatory and analgesic drugs.

H3-receptor antagonists

Examples:

A-349,821
ABT-239
Ciproxifan
Clobenpropit
Thioperamide

H4-receptor antagonists

Thioperamide
JNJ 7777120
VUF-6002

Others
Inhibitors of histamine release

These agents (mast cell stabilizers) appear to stabilize the mast cells to prevent degranulation and
mediator release. Although this is an unlikely method of action.
Examples:

Cromoglicate (cromolyn)
Nedocromil

Other agents with antihistaminergic activity

Many drugs, used for other indications, possess unwanted antihistaminergic activity.
Large doses of vitamin C are known to alleviate shock by inhibiting deaminizing proteins that
release histamine.