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Anti histamines:

Histamine is present in mast cells and release in response to specific antigens. These drugs block the release of histamine. Classification: Sedative 1st generation diphenhydramine dimenhydrinate promethazine 25-50 mg 10 mg 25-50mg 25-50mg Oral IM Oral, IM Oral ,IM

Less sedative 1st generation pheniramine chlorpheniramine cyclizine meclizine Newer non sedatives 2nd generation terfenadine astemizole loratadine cetrizine fexofenadine acrevastine

25-50 mg 4-20mg 50 mg 25-50 mg 5 mg 5 mg 10 mg 10 mg 120 mg 8 mg

oral Oral ,IM oral oral oral oral oral oral oral oral

H1-receptor antagonists In common use, the term antihistamine refers only to compounds that inhibit action at the H 1 receptor (and not H2, etc). Rather than "true" antagonists, H1-antihistamines are actually agonists at the histamine H1-receptor. Clinically, H1 antagonists are used to treat allergic reactions. Sedation is a common side-effect, and s3ome H1 antagonists, such as diphenhydramine and doxylamine, are also used to treat insomnia. Second-generation antihistamines cross the bloodbrain barrier to a much lower degree than the first ones. The main benefit is that they primarily affect peripheral histamine receptors, and therefore have a much lower sedative effect. High doses can still induce the CNS drowsiness.

Examples: Acrivastine Azelastine Bilastine Brompheniramine Buclizine Bromodiphenhydramine

H2-receptor antagonists They act on H2 histamine receptors found principally in the parietal cells of the gastric mucosa, which are part of the endogenous signaling pathway for gastric acid secretion. Normally, histamine acts on H2 to stimulate acid secretion; drugs that block H2 signaling thus reduce the secretion of gastric acid. H2 antagonists are among first-line therapy to treat gastrointestinal conditions including peptic ulcers and gastroesophageal reflux disease. Examples:

Cimetidine Famotidine Lafutidine Nizatidine Ranitidine Roxatidine

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 effect, and are being investigated for the treatment of conditions such as ADHD, Alzheimer's disease, and schizophrenia, whereas H4antagonists appear to have an immunomodulatory role and are being investigated as antiinflammatory and analgesic drugs. H3-receptor antagonists. Eg. A-349,821 Ciproxifan Clobenpropit Conessine Thioperamide

H4-receptor antagonists Examples:


Thioperamide JNJ 7777120 VUF-3 6002

USES: Antihistamines are used to treat rash, hives, watery eyes, runny nose, itching, and sneezing due to allergies or the common cold. They may also be used to treat motion sickness, anxiety, or as a sleep aid (for insomnia). DRUG INTERACTIONS: Tell your doctor of all the medications you may use (both prescription and nonprescription), especially of: sleeping pills, sedatives, tranquilizers, muscle relaxants, medication for depression, seizure medications, narcotic pain relievers, other medications for colds/hay fever/allergies. Because this medication may affect allergy testing, you may have to stop using this medication for several days before the tests are performed. Consult your doctor about this. Do not start or stop any medicine without doctor or pharmacist approval. Pharmacokinetics:

well absorbed

well distributed

liver metabolism

excreted by kidneys

Mechanism of action: these drugs block action of histamine, thereby cause bronchdilation. These drugs dry the secretions so they decrease mucous production in respiratory tract.

Side Effects of Antihistamines Antihistamines can cause side effects, and some cause more side effects than others. Drugs such as Benadryl, older group known as "first-generation" antihistamines. They tend to cause more side effects, particularly drowsiness. Newer-generation antihistamines such as Allegra, Clarinex, and Zyrtec and have fewer side effects, so they may be a better choice for some people. Some of the main side effects of antihistamines include:

Dry mouth Drowsiness Dizziness Nausea and vomiting Restlessness or moodiness (in some children)

Trouble urinating or not being able to urinate Blurred vision Confusion