Tìm theo
Phentolamine
Các tên gọi khác (10 ) :
  • 2-(N-(m-Hydroxyphenyl)-P-toluidinomethyl)imidazoline
  • Fentolamina
  • Phentolamin
  • Phentolamine
  • Phentolamine mesylate
  • Phentolaminum
  • Regitina
  • Regitine
  • Rogitine
  • Vesomax
antihypertensive agents, adrenergic alpha antagonists
Thuốc Gốc
Small Molecule
CAS: 50-60-2
ATC: C04AB01, V03AB36
ĐG : Bedford Labs , http://www.bedfordlabs.com
CTHH: C17H19N3O
PTK: 281.3523
A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of raynaud disease and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H19N3O
Phân tử khối
281.3523
Monoisotopic mass
281.152812245
InChI
InChI=1S/C17H19N3O/c1-13-5-7-14(8-6-13)20(12-17-18-9-10-19-17)15-3-2-4-16(21)11-15/h2-8,11,21H,9-10,12H2,1H3,(H,18,19)
InChI Key
InChIKey=MRBDMNSDAVCSSF-UHFFFAOYSA-N
IUPAC Name
3-[(4,5-dihydro-1H-imidazol-2-ylmethyl)(4-methylphenyl)amino]phenol
Traditional IUPAC Name
phentolamine
SMILES
CC1=CC=C(C=C1)N(CC1=NCCN1)C1=CC(O)=CC=C1
Độ tan chảy
174.5 °C
Độ hòa tan
2.72e-01 g/l
logP
3.3
logS
-3
pKa (strongest acidic)
9.78
pKa (Strongest Basic)
9.02
PSA
47.86 Å2
Refractivity
84.25 m3·mol-1
Polarizability
31.37 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Phentolamine is indicated for the control of episodes of hypertension and sweating that occur with a disease called pheochromocytoma. If tachycardia is excessive, it may be necessary to use a beta-blocking agent concomitantly. Phentolamine is a long-acting, adrenergic, alpha-receptor blocking agent which can produce and maintain "chemical sympathectomy" by oral administration. It increases blood flow to the skin, mucosa and abdominal viscera, and lowers both supine and erect blood pressures. It has no effect on the parasympathetic system. Phentolamine works by blocking alpha receptors in certain parts of the body. Alpha receptors are present in the muscle that lines the walls of blood vessels. When the receptors are blocked by Phentolamine, the muscle relaxes and the blood vessels widen. This widening of the blood vessels results in a lowering of blood pressure.
Cơ Chế Tác Dụng : A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of raynaud disease and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease. [PubChem] Phentolamine produces its therapeutic actions by competitively blocking alpha-adrenergic receptors (primarily excitatory responses of smooth muscle and exocrine glands), leading to a muscle relaxation and a widening of the blood vessels. This widening of the blood vessels results in a lowering of blood pressure. The action of phentolamine on the alpha adrenergic receptors is relatively transient and the blocking effect is incomplete. The drug is more effective in antagonizing responses to circulating epinephrine and/or norepinephrine than in antagonizing responses to mediator released at the adrenergic nerve ending. Phentolamine also stimulates β-adrenergic receptors and produces a positive inotropic and chronotropic effect on the heart and increases cardiac output.
Dược Động Học :

▧ Route of Elimination :
10-13% of the drug is excreted unchanged in urine, and the fate of the remainder of the drug is unknown.
▧ Half Life :
19 minutes
Chỉ Định : Used as an aid for the diagnosis of pheochromocytoma, and may be administered immediately prior to or during pheochromocytomectomy to prevent or control paroxysmal hypertension resulting from anesthesia, stress, or operative manipulation of the tumor. Phentolamine has also been used to treat hypertensive crisis caused by sympathomimetic amines or catecholamine excess by certain foods or drugs in patients taking MAO inhibitors, or by clonidine withdrawal syndrome. Other indications include the prevention of dermal necrosis and sloughing following IV administration or extravasation of norepinephrine, decrease in impedance to left ventricular ejection and the infarct size in patients with MI associated with left ventricular failure, treatment of erectile dysfunction through self-injection of small doses combined with papaverine hydrochloride into the corpus cavernosum, and as an adjunct to the management of cocaine overdose to reverse coronary vasoconstriction following use of oxygen, benzodiazepines,and nitroglycerin.
Tương Tác Thuốc :
  • Tadalafil Tadalafil may enhance the hypotensive effect of Phentolamine. Monitor for hypotension during concomitant therapy.
  • Tamsulosin Concomitant use of alpha1-adrenergic antagonists, Tamsulosin and Phentolamine, may result in additive antihypertensive effects. Combination therapy is not recommended.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Vardenafil Additive hypotensive effects of the PDE5 inhibitor, Vardenafil, and alpha1-blocker, Phentolamine, may occur. Monitor for hypotension during concomitant therapy.
Liều Lượng & Cách Dùng : Solution - Intravenous
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Septodont
    Sản phẩm biệt dược : OraVerse
  • Công ty : Novartis
    Sản phẩm biệt dược : Regitin
  • Công ty : Novartis
    Sản phẩm biệt dược : Regitina
  • Công ty : Novartis
    Sản phẩm biệt dược : Regitine
  • Công ty : Paladin
    Sản phẩm biệt dược : Rogitine
  • Công ty : Grupo Cimed
    Sản phẩm biệt dược : Vigamed
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00692
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5775
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506535
ChemSpider
http://www.chemspider.com/Chemical-Structure.5571.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50008789
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0083-6830-02
PharmGKB
http://www.pharmgkb.org/drug/PA450926
Wikipedia
http://en.wikipedia.org/wiki/Phentolamine
RxList
http://www.rxlist.com/cgi/generic3/phentol.htm
Drugs.com
http://www.drugs.com/cons/phentolamine-injection.html
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