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药品详细

Minoxidil (米诺 )

化学结构式图
中文名
米诺
英文名
Minoxidil
分子式
Not Available
化学名
2,6-diamino-4-(piperidin-1-yl)pyrimidin-1-ium-1-olate
分子量
Average: 209.2483
Monoisotopic: 209.127660127
CAS号
38304-91-5
ATC分类
C02D 未知;D11A 未知
药物类型
small molecule
阶段
商品名
Alopexil;Alostil;Apo-Gain;Gen-Minoxidil;Loniten;Lonolox;Minodyl;Minoxigaine;Minoximen;Normoxidil;PDP;Pierminox;Prexidil;Regaine;Rogaine;Rogaine Extra Strength for Men;Rogaine for Men;Rogaine for Women;Theroxidil;Tricoxidil;Trocoxidil;
同义名
Minossidile [Italian];Minoxidilum [INN-Latin];
基本介绍

A potent direct-acting peripheral vasodilator (vasodilator agents) that reduces peripheral resistance and produces a fall in blood pressure. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371)

生产厂家
  • Actavis mid atlantic llc
  • Avacor products llc
  • Bausch and lomb pharmaceuticals inc
  • Copley pharmaceutical inc
  • Harmony laboratories
  • Hi tech pharmacal co inc
  • Johnson and johnson group consumer companies
  • L perrigo co
  • Mutual pharmaceutical co inc
  • Novex pharma
  • Par pharmaceutical inc
  • Perrigo co
  • Perrigo new york inc
  • Pharmacia and upjohn co
  • Quantum pharmics ltd
  • Royce laboratories inc
  • Sight pharmaceuticals inc
  • Teva pharmaceuticals usa inc
  • Usl pharma inc
  • Watson laboratories inc
  • Wockhardt eu operations (swiss) ag
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Olsen EA, Whiting D, Bergfeld W, Miller J, Hordinsky M, Wanser R, Zhang P, Kohut B: A multicenter, randomized, placebo-controlled, double-blind clinical trial of a novel formulation of 5% minoxidil topical foam versus placebo in the treatment of androgenetic alopecia in men. J Am Acad Dermatol. 2007 Aug 28;. Pubmed
剂型
Form Route Strength
Liquid Topical
Solution Topical
Tablet Oral
规格
Unit description Cost Unit
Rogaine ex-str starter kit 28.32 USD kit
Minoxidil powder 2.07 USD g
Loniten 10 mg Tablet 1.52 USD tablet
Minoxidil 10 mg tablet 1.32 USD tablet
Minoxidil 2.5 mg tablet 0.7 USD tablet
Loniten 2.5 mg Tablet 0.39 USD tablet
Rogaine 5 % foam 0.27 USD g
化合物类型
Type small molecule
Classes
  • Pyrimidines and Derivatives
  • Piperidines
Substructures
  • Hydroxy Compounds
  • Aliphatic and Aryl Amines
  • Pyrimidines and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Cyanamides
  • Piperidines
适应症
ANTIHYPERTENSIVES 降血压;
药理
Indication For the treatment of severe hypertension and in the topical treatment (regrowth) of androgenic alopecia in males and females and stabilisation of hair loss in patients with androgenic alopecia.
Pharmacodynamics Minoxidil is an orally effective direct acting peripheral vasodilator that reduces elevated systolic and diastolic blood pressure by decreasing peripheral vascular resistance. Minoxidil is also used topically to treat androgenetic alopecia. Microcirculatory blood flow in animals is enhanced or maintained in all systemic vascular beds. In man, forearm and renal vascular resistance decline; forearm blood flow increases while renal blood flow and glomerular filtration rate are preserved. The predominant site of minoxidil action is arterial. Venodilation does not occur with minoxidil; thus, postural hypotension is unusual with its administration. The antihypertensive activity of minoxidil is due to its sulphate metabolite, minoxidil sulfate.
Mechanism of action Minoxidil is thought to promote the survival of human dermal papillary cells (DPCs) or hair cells by activating both extracellular signal-regulated kinase (ERK) and Akt and by preventing cell death by increasing the ratio of BCl-2/Bax. Minoxidil may stimulate the growth of human hairs by prolonging anagen through these proliferative and anti-apoptotic effects on DPCs. Minoxidil, when used as a vasodilator, acts by opening adenosine triphosphate-sensitive potassium channels in vascular smooth muscle cells. This vasodilation may also improve the viability of hair cells or hair follicles.
Absorption Minoxidil is at least 90% absorbed from the GI tract in experimental animals and man.
Volume of distribution Not Available
Protein binding Minoxidil does not bind to plasma proteins.
Metabolism

Approximately 90% of the administered drug is metabolized, predominantly by conjugation with glucuronic acid at the N-oxide position in the pyrimidine ring, but also by conversion to more polar products. Known metabolites exert much less pharmacologic effect than minoxidil itself.
Route of elimination Not Available
Half life 4.2 hours
Clearance Not Available
Toxicity Oral LD50 in rats has ranged from 1321-3492 mg/kg; in mice, 2456-2648 mg/kg. Side effects include cardiovascular effects associated with hypotension such as sudden weight gain, rapid heart beat, faintness or dizziness.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Melting point 248 oC
Experimental Properties
Property Value Source
water solubility 2200 mg/L PhysProp
logP 0.6 PhysProp
pKa 4.61 Various sources
Predicted Properties
Property Value Source
water solubility 1.99e+01 g/l ALOGPS
logP 1.24 ALOGPS
logP 1.30 ChemAxon Molconvert
logS -1.02 ALOGPS
pKa 18.78 ChemAxon Molconvert
hydrogen acceptor count 5 ChemAxon Molconvert
hydrogen donor count 2 ChemAxon Molconvert
polar surface area 93.63 ChemAxon Molconvert
rotatable bond count 1 ChemAxon Molconvert
refractivity 60.74 ChemAxon Molconvert
polarizability 21.93 ChemAxon Molconvert
药物相互作用
Drug Interaction
Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
食物相互作用
  • Take without regard to meals.

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