Minoxidil

Các tên gọi khác (14 ) :

2,4-Diamino-6-piperidinopyrimidine 3-oxide
6-Piperidin-1-ylpyrimidine-2,4-diamine 3-oxide
Alostil
Apo-gain
Loniten
Lonolox
Minossidile
Minoxidil
Minoxidilum
Minoximen
Normoxidil
Regaine
Rogaine
Tricoxidil

Thuốc Gốc

Small Molecule

CAS: 38304-91-5

ATC: C02DC01, D11AX01

ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com

CTHH: C₉H₁₅N₅O

PTK: 209.2483

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)

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₉H₁₅N₅O

Phân tử khối

209.2483

Monoisotopic mass

209.127660127

InChI

InChI=1S/C9H15N5O/c10-7-6-8(12-9(11)14(7)15)13-4-2-1-3-5-13/h6H,1-5,10H2,(H2,11,12)

InChI Key

InChIKey=ZFMITUMMTDLWHR-UHFFFAOYSA-N

IUPAC Name

2,6-diamino-4-(piperidin-1-yl)pyrimidin-1-ium-1-olate

Traditional IUPAC Name

rogaine

SMILES

NC1=CC(=NC(N)=[N+]1[O-])N1CCCCC1

Độ tan chảy

248 °C

Độ hòa tan

2200 mg/L

logP

1.24

logS

-1

pKa (strongest acidic)

14.22

pKa (Strongest Basic)

4.34

PSA

93.63 Å²

Refractivity

60.74 m³·mol^-1

Polarizability

21.93 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Ghose Filter

true

pKa

4.61

Dược Lực Học : 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.

Cơ Chế Tác Dụng : 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) 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.

Dược Động Học :

▧ Absorption :
Minoxidil is at least 90% absorbed from the GI tract in experimental animals and man.
▧ 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.
▧ Half Life :
4.2 hours

Độc Tính : 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.

Chỉ Định : 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.

Tương Tác Thuốc :

Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

Liều Lượng & Cách Dùng : Liquid - Topical
Solution - Topical
Tablet - Oral

Dữ Kiện Thương Mại

Giá thị trường

Biệt dược thương mại : Minoxidil 10 mg tablet

Giá bán buôn : USD >1.32

Đơn vị tính : tablet
Biệt dược thương mại : Loniten 10 mg Tablet

Giá bán buôn : USD >1.52

Đơn vị tính : tablet
Biệt dược thương mại : Minoxidil powder

Giá bán buôn : USD >2.07

Đơn vị tính : g
Biệt dược thương mại : Rogaine ex-str starter kit

Giá bán buôn : USD >28.32

Đơn vị tính : kit
Biệt dược thương mại : Rogaine 5 % foam

Giá bán buôn : USD >0.27

Đơn vị tính : g
Biệt dược thương mại : Loniten 2.5 mg Tablet

Giá bán buôn : USD >0.39

Đơn vị tính : tablet
Biệt dược thương mại : Minoxidil 2.5 mg tablet

Giá bán buôn : USD >0.7

Đơn vị tính : tablet

Nhà Sản Xuất

Công ty : McNeil

Sản phẩm biệt dược : Alostil
Công ty : Apotex

Sản phẩm biệt dược : Apo-Gain
Công ty :

Sản phẩm biệt dược : Avogain
Công ty :

Sản phẩm biệt dược : Lipogaine
Công ty : Pfizer

Sản phẩm biệt dược : Loniten
Công ty : Pfizer

Sản phẩm biệt dược : Lonolox
Công ty :

Sản phẩm biệt dược : Minodyl
Công ty :

Sản phẩm biệt dược : Minoxigaine
Công ty : Menarini

Sản phẩm biệt dược : Minoximen
Công ty : Dr. Reddy's

Sản phẩm biệt dược : Mintop
Công ty : McNeil

Sản phẩm biệt dược : Regaine
Công ty : Johnson & Johnson

Sản phẩm biệt dược : Rogaine
Công ty : Ei

Sản phẩm biệt dược : Theroxidil
Công ty :

Sản phẩm biệt dược : Tricoxidil
Công ty :

Sản phẩm biệt dược : Vanarex

Đóng gói

Công ty : Amerisource Health Services Corp.

Website : http://www.amerisourcebergen.com
Công ty : Atlantic Biologicals Corporation

Website : http://www.atlanticbiologicals.com
Công ty : Comprehensive Consultant Services Inc.
Công ty : Dept Health Central Pharmacy
Công ty : Heartland Repack Services LLC
Công ty : Johnson & Johnson Healthcare

Website : http://www.jnjcanada.com
Công ty : Kaiser Foundation Hospital
Công ty : Major Pharmaceuticals

Website : http://www.majorpharmaceuticals.com
Công ty : Medisca Inc.

Website : http://www.medisca.com
Công ty : Murfreesboro Pharmaceutical Nursing Supply

Website : http://www.unitdosesupply.com
Công ty : Mutual Pharmaceutical Co.
Công ty : Nucare Pharmaceuticals Inc.

Website : http://www.nucarerx.com
Công ty : Par Pharmaceuticals

Website : http://www.parpharm.com
Công ty : Patheon Inc.

Website : http://www.patheon.com
Công ty : Perrigo Co.

Website : http://www.perrigo.com
Công ty : Pharmaceutical Utilization Management Program VA Inc.
Công ty : Pharmacia Inc.

Website : http://www.pharmaciaupjohn.com
Công ty : Physicians Total Care Inc.

Website : http://www.physicianstotalcare.com
Công ty : Prepak Systems Inc.

Website : http://www.prepaksys.com
Công ty : Remedy Repack

Website : http://www.remedyrepack.com
Công ty : Southwood Pharmaceuticals

Website : http://www.southwoodhealthcare.com
Công ty : Vangard Labs Inc.
Công ty : Watson Pharmaceuticals

Website : http://www.watson.com

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00350

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4201

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508344

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D00418

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/53489-386-01

PharmGKB

http://www.pharmgkb.org/drug/PA450521

Wikipedia

http://en.wikipedia.org/wiki/Minoxidil

RxList

http://www.rxlist.com/minoxidil-drug.htm

Drugs.com

http://www.drugs.com/cdi/minoxidil.html

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