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药品详细

Naphazoline(萘甲唑啉)

化学结构式图
中文名
萘甲唑啉
英文名
Naphazoline
分子式
C14H14N2
化学名
2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole
分子量
Average: 210.2744
Monoisotopic: 210.115698458
CAS号
835-31-4
ATC分类
R01A 未知;S01G 解充血药及抗过敏药;R01A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Naphazoline is a rapid acting sympathomimetic vasoconstrictor of occular artierioles. It acts to decrease congestion of the conjunctiva and is found in many over-the-counter eye drops.

生产厂家
  • Alcon laboratories inc
  • Allergan inc
  • Bausch and lomb pharmaceuticals inc
  • Novartis pharmaceuticals corp
  • Pharmafair inc
  • Taylor pharmaceuticals
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Naphthalenes
  • Phenethylamines
Substructures
  • Imidazolines
  • Carboxylic Acids and Derivatives
  • Naphthalenes
  • Benzene and Derivatives
  • Imidazoles
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamidines
  • Imines
适应症
药理
Indication Naphazoline is primarily indicated in conditions like Corneal vascularity, Hyperaemia, Itching, Nasal congestion, and can also be given in adjunctive therapy as an alternative drug of choice in Sinusitis
Pharmacodynamics Naphazoline is a direct acting sympathomimetic adrenergic alpha-agonist used to induce systemic vasoconstriction, thereby decreasing nasal congestion and inducing constriction around the conjunctiva. The sympathomimetic action of Naphazoline constricts the smaller arterioles of the nasal passages, producing a decongesting effect. Naphazoline ophthalmic causes constriction of blood vessels in the eyes. It also decreases itching and irritation of the eyes. aphazoline constricts the vascular system of the conjunctiva. It is presumed that this effect is due to direct stimulation action of the drug upon the alpha adrenergic receptors in the arterioles of the conjunctiva resulting in decreased conjunctival congestion. Naphazoline belongs to the imidazoline class of sympathomimetics.
Mechanism of action Naphazoline is a direct acting sympathomimetic drug, which acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. This activates the adrenal system to yield systemic vasoconstrction. In producing vasoconstriction, the result is a decrease in blood flow in the nasal passages and consequently decreased nasal congestion. The vasoconstriction means that there is less pressure in the capillaries and less water can filter out, thus less discharge is made.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Extended usage of Naphazoline can result in decreased effectiveness or a build up of tolerance against the drug. The number of receptors decreases, and when the administration of the drug is ceased, chronic congestion can occur; this is called rhinitis medicamentosa, commonly referred to as rebound congestion. Moreover long-term overdosing can cause degenerative changes in nasal mucous membranes that pose another health problem.
Affected organisms Not Available
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties Not Available
Predicted Properties
Property Value Source
water solubility 3.81e-02 g/l ALOGPS
logP 3.44 ALOGPS
logP 2.19 ChemAxon
logS -3.7 ALOGPS
pKa (strongest basic) 10.19 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 24.39 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 65.52 ChemAxon
polarizability 23.77 ChemAxon
药物相互作用
食物相互作用
Not Available

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