药品详细

Betamethasone(倍他米松)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

倍他米松

英文名

Betamethasone

分子式

C₂₂H₂₉FO₅

化学名

(1R,2S,10S,11S,13S,14R,15S,17S)-1-fluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one

分子量

Average: 392.4611
Monoisotopic: 392.199902243

CAS号

378-44-9

ATC分类

A07E Intestinal Antiinflammatory Agents;C05A 未知;D07A 未知;D07X 未知;H02A 未知;R01A 未知;R03B 未知;S01B 抗炎药;S01C 炎药组合;S02B 未知;S03B 未知

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724)

生产厂家

Actavis mid atlantic llc
Alpharma us pharmaceuticals division
Altana inc
Connectics corp
E fougera div altana inc
Glenmark generics inc usa
Parke davis div warner lambert co
Parke davis pharmaceutical research div warner lambert co
Perrigo new york inc
Pharmaderm div altana inc
Pharmafair inc
Savage laboratories inc div altana inc
Schering corp
Schering corp sub schering plough corp
Stat trade inc
Taro pharmaceuticals inc
Taro pharmaceuticals usa inc
Teva pharmaceuticals usa
Teva pharmaceuticals usa inc
Tj roaco ltd
Tolmar inc
Watson laboratories inc

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

Steroids and Steroid Derivatives

Substructures

Steroids and Steroid Derivatives
Hydroxy Compounds
Alkanes and Alkenes
Alkyl Halides
Alcohols and Polyols
Ketones

适应症

药理

Indication	Topical use (cream, lotion and ointment): for relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses Topical use (foam): relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses of the scalp Systemic use: for the treatment of edocrine disorders, rheumatic disorders, collagen diseases, dermatological diseases, allergic states, ophthalmic diseases, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, gastrointestinal diseases, tuberculous meningitis and trichinosis.
Pharmacodynamics	Betamethasone and its derivatives, betamethasone sodium phosphate and betamethasone acetate, are synthetic glucocorticoids. Used for its antiinflammatory or immunosuppressive properties, betamethasone is combined with a mineralocorticoid to manage adrenal insufficiency and is used in the form of betamethasone benzoate, betamethasone dipropionate, or betamethasone valerate for the treatment of inflammation due to corticosteroid-responsive dermatoses. Betamethasone and clotrimazole are used together to treat cutaneous tinea infections.
Mechanism of action	Betamethasone is a glucocorticoid receptor agonist. This leads to changes in genetic expression once this complex binds to the GRE. The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding. Betamethasone binds to plasma transcortin, and it becomes active when it is not bound to transcortin.
Absorption	Minimal if applied topically.
Volume of distribution	Not Available
Protein binding	64%
Metabolism	Hepatic
Route of elimination	Not Available
Half life	5.6 hours
Clearance	Not Available
Toxicity	Symptoms of overdose include burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, and miliaria.
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	232 °C	PhysProp
water solubility	66.5 mg/L (at 25 °C)	EPA
logP	1.94	HANSCH,C ET AL. (1995)
logS	-3.77	ADME Research, USCD

Predicted Properties

Property	Value	Source
water solubility	5.05e-02 g/l	ALOGPS
logP	1.93	ALOGPS
logP	1.68	ChemAxon
logS	-3.9	ALOGPS
pKa (strongest acidic)	12.42	ChemAxon
pKa (strongest basic)	-3.3	ChemAxon
physiological charge	0	ChemAxon
hydrogen acceptor count	5	ChemAxon
hydrogen donor count	3	ChemAxon
polar surface area	94.83	ChemAxon
rotatable bond count	2	ChemAxon
refractivity	102.49	ChemAxon
polarizability	40.88	ChemAxon

药物相互作用

Drug	Interaction
Acenocoumarol	The corticosteroid, betamethasone, alters the anticoagulant effect, acenocoumarol.
Acetylsalicylic acid	The corticosteroid, betamethasone, may decrease the effect of the salicylate, acetylsalicylic acid.
Ambenonium	The corticosteroid, betamethasone, may decrease the effect of the anticholinesterase, ambenonium.
Amobarbital	The barbiturate, amobarbital, may decrease the effect of the corticosteroid, betamethasone.
Anisindione	The corticosteroid, betamethasone, alters the anticoagulant effect of anisindione.
Aprobarbital	The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, betamethasone.
Bismuth Subsalicylate	The corticosteroid, betamethasone, may decrease the effect of the salicylate, bismuth subsalicylate.
Butabarbital	The barbiturate, butabarbital, may decrease the effect of the corticosteroid, betamethasone.
Butalbital	The barbiturate, butalbital, may decrease the effect of the corticosteroid, betamethasone.
Butethal	The barbiturate, butethal, may decrease the effect of the corticosteroid, betamethasone.
Dicumarol	The corticosteroid, betamethasone, alters the anticoagulant effect of dicumarol.
Dihydroquinidine barbiturate	The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, betamethasone.
Edrophonium	The corticosteroid, betamethasone, may decrease the effect of the anticholinesterase, edrophonium.
Ethotoin	The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, betamethasone.
Fosphenytoin	The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, betamethasone.
Heptabarbital	The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, betamethasone.
Hexobarbital	The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, betamethasone.
Indacaterol	Concomitant therapy may increase the risk of hypokalemia via intracellular shunting. Monitor for adverse effects and especially for cardiovascular effects associated with hypokalemia.
Magnesium salicylate	The corticosteroid, betamethasone, may decrease the effect of magnesium salicylate.
Mephenytoin	The enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, betamethasone.
Methohexital	The barbiturate, methohexital, may decrease the effect of the corticosteroid, betamethasone.
Methylphenobarbital	The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, betamethasone.
Midodrine	Increased arterial pressure
Pentobarbital	The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, betamethasone.
Phenobarbital	The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, betamethasone.
Phenytoin	The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, betamethasone.
Primidone	The barbiturate, primidone, may decrease the effect of the corticosteroid, betamethasone.
Pyridostigmine	The corticosteroid, betamethasone, may decrease the effect of the anticholinesterase, pyridostigmine.
Quinidine barbiturate	The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, betamethasone.
Rifampin	The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, betamethasone.
Salicylate-sodium	The corticosteroid, betamethasone, may decrease the effect of the salicylate, salicylate-sodium.
Salsalate	The corticosteroid, betamethasone, may decrease the effect of the salicylate, salsalate.
Secobarbital	The barbiturate, secobarbital, may decrease the effect of the corticosteroid, betamethasone.
Tacrine	Tacrine and Betamethasone may independently exacerbate muscle weakness in myasthenia gravis patients. Monitor for additive muscle weakness effects.
Talbutal	The barbiturate, talbutal, may decrease the effect of the corticosteroid, betamethasone.
Trastuzumab	Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Trisalicylate-choline	The corticosteroid, betamethasone, may decrease the effect of the salicylate, trisalicylate-choline.
Vecuronium	Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Betamethasone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
Warfarin	The corticosteroid, betamethasone, alters the anticoagulant effect of warfarin.

食物相互作用

Take with food to reduce irritation.

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