Antazoline

Last updated
Antazoline
Antazoline.svg
Clinical data
Trade names Vasocon-a
AHFS/Drugs.com Micromedex Detailed Consumer Information
Routes of
administration
Topical (nasal, eye drops)
ATC code
Identifiers
  • N-(4,5-Dihydro-1H-imidazol-2-ylmethyl)-N-(phenylmethyl)aniline
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.001.904 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C17H19N3
Molar mass 265.360 g·mol−1
3D model (JSmol)
  • N\1=C(\NCC/1)CN(c2ccccc2)Cc3ccccc3
  • InChI=1S/C17H19N3/c1-3-7-15(8-4-1)13-20(14-17-18-11-12-19-17)16-9-5-2-6-10-16/h1-10H,11-14H2,(H,18,19) Yes check.svgY
  • Key:REYFJDPCWQRWAA-UHFFFAOYSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Antazoline is a 1st generation antihistamine with anticholinergic properties used to relieve nasal congestion and in eye drops, usually in combination with naphazoline, to relieve the symptoms of allergic conjunctivitis. [1] To treat allergic conjunctivitis, antazoline can be combined in a solution with tetryzoline. [2] The drug is a Histamine H1 receptor antagonist: [3] selectively binding to but not activating the receptor, thereby blocking the actions of endogenous histamine and subsequently leading to the temporary relief of the negative symptoms brought on by histamine.

Related Research Articles

Conjunctivitis Inflammation of the eye

Conjunctivitis, also known as pink eye, is inflammation of the outermost layer of the white part of the eye and the inner surface of the eyelid. It makes the eye appear pink or reddish. Pain, burning, scratchiness, or itchiness may occur. The affected eye may have increased tears or be "stuck shut" in the morning. Swelling of the white part of the eye may also occur. Itching is more common in cases due to allergies. Conjunctivitis can affect one or both eyes.

Mastocytosis Medical condition

Mastocytosis, a type of mast cell disease, is a rare disorder affecting both children and adults caused by the accumulation of functionally defective mast cells and CD34+ mast cell precursors.

H1 antagonists, also called H1 blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines; other agents may have antihistaminergic action but are not true antihistamines.

Diphenhydramine Antihistamine medication

Diphenhydramine is an antihistamine mainly used to treat allergies. It can also be used for insomnia, symptoms of the common cold, tremor in parkinsonism, and nausea. It is used by mouth, injection into a vein, injection into a muscle, or applied to the skin. Maximal effect is typically around two hours after a dose, and effects can last for up to seven hours.

Allergic rhinitis Human disease

Allergic rhinitis, also known as hay fever, is a type of inflammation in the nose which occurs when the immune system overreacts to allergens in the air. Signs and symptoms include a runny or stuffy nose, sneezing, red, itchy, and watery eyes, and swelling around the eyes. The fluid from the nose is usually clear. Symptom onset is often within minutes following allergen exposure and can affect sleep, and the ability to work or study. Some people may develop symptoms only during specific times of the year, often as a result of pollen exposure. Many people with allergic rhinitis also have asthma, allergic conjunctivitis, or atopic dermatitis.

Chlorphenamine

Chlorphenamine, also known as chlorpheniramine, is an antihistamine used to treat the symptoms of allergic conditions such as allergic rhinitis. It is taken by mouth. The medication takes effect within 6 hours and lasts for about a day.

Tetryzoline

Tetryzoline is a drug used in some over-the-counter eye drops and nasal sprays.

Hives Skin disease characterized by red, raised, and itchy bumps

Hives, also known as urticaria, is a kind of skin rash with red, raised, itchy bumps. They may also burn or sting. Often the patches of rash move around. Typically they last a few days and do not leave any long-lasting skin changes. Fewer than 5% of cases last for more than six weeks. The condition frequently recurs.

Cetirizine Antihistamine medication

Cetirizine, sold under the brand name Zyrtec among others, is a second-generation antihistamine used to treat allergic rhinitis, dermatitis, and urticaria. It is taken by mouth. Effects generally begin within an hour and last for about a day. The degree of benefit is similar to other antihistamines such as diphenhydramine.

Cromoglicic acid

Cromoglicic acid (INN) — also referred to as cromolyn (USAN), cromoglycate, or cromoglicate — is traditionally described as a mast cell stabilizer, and is commonly marketed as the sodium salt sodium cromoglicate or cromolyn sodium. This drug prevents the release of inflammatory chemicals such as histamine from mast cells.

Allergic conjunctivitis Medical condition

Allergic conjunctivitis (AC) is inflammation of the conjunctiva due to allergy. Although allergens differ among patients, the most common cause is hay fever. Symptoms consist of redness, edema (swelling) of the conjunctiva, itching, and increased lacrimation. If this is combined with rhinitis, the condition is termed allergic rhinoconjunctivitis (ARC).

Clemastine Allergy medication

Clemastine, also known as meclastin, is a first-generation H1 histamine antagonist (antihistamine) with anticholinergic properties (drying) and sedative side effects. Like all first-generation antihistamines, it is sedating.

Olopatadine

Olopatadine, sold under the brand name Opatanol among others, is a medication used to decrease the symptoms of allergic conjunctivitis and allergic rhinitis. It is used as eye drops or as a nasal spray. The eye drops generally result in an improvement within half an hour.

Post-nasal drip Medical condition

Post-nasal drip (PND), also known as upper airway cough syndrome (UACS), occurs when excessive mucus is produced by the nasal mucosa. The excess mucus accumulates in the back of the nose, and eventually in the throat once it drips down the back of the throat. It can be caused by rhinitis, sinusitis, gastroesophageal reflux disease (GERD), or by a disorder of swallowing. Other causes can be allergy, cold, flu, and side effects from medications.

Ketotifen

Ketotifen, sold under the brand name Zaditor among others, is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer. It is most commonly sold as a salt with fumaric acid, ketotifen fumarate, and is available in two forms. In its ophthalmic form, it is used to treat allergic conjunctivitis. In its oral form, it is used to prevent asthma attacks or anaphylaxis, as well as various mast cell, allergic-type disorders.

Nedocromil

Nedocromil sodium is a medication considered as mast cell stabilizer which act to prevent wheezing, shortness of breath, and other breathing problems caused by asthma. It is administered by an inhaler under the brand name Tilade, and as an eye drop under the brand name Alocril. The effects of nedocromil versus asthma are gradual rather than fast-acting and it is not indicated for acute respiratory distress compared to fast acting bronchodilators like albuterol or other well-known inhaler medications). Liquid preparations of nedocromil are available in the UK under the name Rapitil for use for allergic eye reactions. Nedocromil sodium has been shown to be effective in alleviating symptoms of allergic conjunctivitis.

Emedastine

Emedastine (trade name Emadine) is a second generation antihistamine used in eye drops to alleviate the symptoms of allergic conjunctivitis. It acts as a H1 receptor antagonist. It works by blocking the action of histamine that causes allergic symptoms. It is used in form of the difumarate. The emedastine difumarate is a white, crystalline, water-soluble fine powder. Emedastine eye drops is usually applied twice a day to the affected eye. When the patients with allergic conjunctivitis were treated with 0.05% emedastine difumarate ophthalmic solution for six weeks, the signs and symptoms such as redness, itching and swelling of the eyes were relieved. Emedastine appears to be devoid of effects on adrenergic, dopaminergic and serotonin receptors. This drug was developed by Alcon, which is global medical company specializing in eye care products.

Mast cell stabilizer

Mast cell stabilizers are medications used to prevent or control certain allergic disorders. They block mast cell degranulation, stabilizing the cell and thereby preventing the release of histamine and related mediators. One suspected pharmacodynamic mechanism is the blocking of IgE-regulated calcium channels. Without intracellular calcium, the histamine vesicles cannot fuse to the cell membrane and degranulate.

Antihistamine Drug that binds to but does not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists

Antihistamines are drugs which treat hay fever and other allergies. Typically, people take antihistamines as an inexpensive, not patented (generic), drug that can be bought without a prescription and relieves from nasal congestion, sneezing, or hives caused by pollen, dust mites, or animal allergy with few side effects. Antihistamines are usually for short-term treatment. Chronic allergies increase the risk of health problems which antihistamines might not treat, including asthma, sinusitis, and lower respiratory tract infection. Consultation of a medical professional is recommended for those who intend to take antihistamines for longer-term use.

Pemirolast

Pemirolast (INN) is a mast cell stabilizer used as an anti-allergic drug therapy. It is marketed under the tradenames Alegysal and Alamast.

References

  1. Abelson MB, Allansmith MR, Friedlaender MH (1980). "Effects of topically applied ocular decongestant and antihistamine". Am J Ophthalmol. 90 (2): 254–7. doi:10.1016/s0002-9394(14)74864-0. PMID   7425039.
  2. Castillo M, Scott NW, Mustafa MZ, Mustafa MS, Azuara-Blanco A (2015). "Topical antihistamines and mast cell stabilisers for treating seasonal and perennial allergic conjunctivitis" (PDF). Cochrane Database Syst Rev. 6: CD009566. doi:10.1002/14651858.CD009566.pub2. hdl: 2164/6048 . PMID   26028608.
  3. Noguchi, Seiji; Inukai, Toshiya; Kuno, Takayoshi; Tanaka, Chikako (June 1992). "The suppression of olfactory bulbectomy-induced muricide by antidepressants and antihistamines via histamine H1 receptor blocking". Physiology & Behavior. 51 (6): 1123–1127. doi:10.1016/0031-9384(92)90297-f. PMID   1353628.