Tìm theo
Clonidine
Các tên gọi khác (6 ) :
  • 2-[(2,6-Dichlorophenyl)imino]imidazoline
  • 2,6-Dichloro-N-2-imidazolidinylidenebenzenamine
  • Chlofazoline
  • Clonidin
  • Clonidina
  • Clonidinum
antihypertensive agents, sympatholytics, analgesics, adrenergic alpha 2 receptor agonists
Thuốc Gốc
Small Molecule
CAS: 4205-90-7
ATC: C02AC01, N02CX02, S01EA04, S01EA03
ĐG : AAIPharma Inc. , http://www.aaipharma.com
CTHH: C9H9Cl2N3
PTK: 230.094
Clonidine, an imidazoline-derivative hypotensive agent is a centrally-acting α2-adrenergic agonist. It crosses the blood-brain barrier and acts in the hypothalamus to induce a decrease in blood pressure. It may also be administered as an epidural infusion as an adjunct treatment in the management of severe cancer pain that is not relieved by opiate analgesics alone. Clonidine may be used for differential diagnosis of pheochromocytoma in hypertensive patients. Other uses for clonidine include prophylaxis of vascular migraine headaches, treatment of severe dysmenorrhea, management of vasomotor symptoms associated with menopause, rapid detoxification in the management of opiate withdrawal, treatment of alcohol withdrawal used in conjunction with benzodiazepines, management of nicotine dependence, topical use to reduce intraocular pressure in the treatment of open-angle and secondary glaucoma and hemorrhagic glaucoma associated with hypertension, and in the treatment of attention-deficit hyperactivity disorder (ADHD). Clonidine also exhibits some peripheral activity.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H9Cl2N3
Phân tử khối
230.094
Monoisotopic mass
229.017352717
InChI
InChI=1S/C9H9Cl2N3/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9/h1-3H,4-5H2,(H2,12,13,14)
InChI Key
InChIKey=GJSURZIOUXUGAL-UHFFFAOYSA-N
IUPAC Name
N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine
Traditional IUPAC Name
clonidine
SMILES
ClC1=CC=CC(Cl)=C1NC1=NCCN1
Độ tan chảy
305
Độ hòa tan
Appreciable
logP
1.59
logS
-2.7
pKa (Strongest Basic)
8.16
PSA
36.42 Å2
Refractivity
59.09 m3·mol-1
Polarizability
21.7 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.59
pKa
8.05 (at 25 °C)
Dược Lực Học : Clonidine is an α-adrenergic agent that acts specifically on α2-receptors. α2-receptors regulate a number of signaling pathways mediated by multiple Gi proteins, Gαi1, Gαi2, and G&alphai3. Stimulation of α2-receptors mediates effects such as inhibition of adenylyl cyclase, stimulation fo phospholipase D, stimulation of mitogen-activated protein kinases, stimulation of K+ currents and inhibition of Ca2+ currents. Three G-protein coupled α2-receptor subtypes have been identified: α2A, α2B, and α2C. Each subtype has a unique pattern of tissue distribution in the central nervous system and peripheral tissues. The α2A-receptor is widely distributed throughout the central nervous system; it is found in the locus coeruleus, brain stem nuclei, cerebral cortex, septum, hypothalamus, and hippocampus. α2A-receptors are also expressed in the kidneys, spleen, thymus, lung and salivary glands. The α2C-receptor is primarily expressed in the central nervous system, including the striatum, olfactory tubercle, hippocampus and cerebral cortex. Low levels of the α2C-subtype are also found in the kidneys. The α2B-receptor is located primarily in the periphery (kidney, liver, lung and heart) with low levels of expression in the thalamic nuclei of the central nervous system. The α2A- and α2C-receptors are located presynaptically and inhibit the released of noradrenaline from sympathetic nerves. Stimulation of these receptors decreases sympathetic tone, resulting in decreases in blood pressure and heart rate. Sedation and analgesia is mediated by centrally located α2A-receptors, while peripheral α2B-receptors mediate constriction of vascular smooth muscle. α2A-Receptors also mediate essential components of the analgesic effect of nitrous oxide in the spinal cord. Clonidine stimulates all three α2-receptor subtypes with similar potency. Its actions in the nervous system decreases blood pressure in patients with hypertension and decreases sympathetic overactivity in patients undergoing opioid withdrawal. Clonidine is also a potent sedative and analgesic and can prevent post-operative shivering in intensive and post-operative care. Its use in differential diagnosis of pheochromocytoma owes to the fact that hypertension in patients with pheochromocytoma is refractory to antihypertensive treatment with clonidine.
Cơ Chế Tác Dụng : Clonidine, an imidazoline-derivative hypotensive agent is a centrally-acting α2-adrenergic agonist. It crosses the blood-brain barrier and acts in the hypothalamus to induce a decrease in blood pressure. It may also be administered as an epidural infusion as an adjunct treatment in the management of severe cancer pain that is not relieved by opiate analgesics alone. Clonidine may be used for differential diagnosis of pheochromocytoma in hypertensive patients. Other uses for clonidine include prophylaxis of vascular migraine headaches, treatment of severe dysmenorrhea, management of vasomotor symptoms associated with menopause, rapid detoxification in the management of opiate withdrawal, treatment of alcohol withdrawal used in conjunction with benzodiazepines, management of nicotine dependence, topical use to reduce intraocular pressure in the treatment of open-angle and secondary glaucoma and hemorrhagic glaucoma associated with hypertension, and in the treatment of attention-deficit hyperactivity disorder (ADHD). Clonidine also exhibits some peripheral activity. See Pharmacology section above.
Dược Động Học :
▧ Absorption :
Well absorbed following oral administration. Bioavailability following chronic administration is approximately 65%.
▧ Protein binding :
20-40%, primarily to albumin
▧ Metabolism :
Hepatic. Metabolized via minor pathways. The major metabolite, p-hydroxyclonidine, is present in concentrations less than 10% of those of unchanged clonidine in urine. Four metabolites have been detected, but only p-hydroxyclonidine has been identified.
▧ Half Life :
6-20 hours; 40-60% is excreted in urine unchanged, 20% is excreted in feces. Less than 10% is excreted by p-hydroxyclonidine.
Độc Tính : Oral LD50 is 150 mg/kg in rat and 30 mg/kg in dog. Symptoms of overdose include constriction of pupils of the eye, drowsiness, high blood pressure followed by a drop in pressure, irritability, low body temperature, slowed breathing, slowed heartbeat, slowed reflexes, and weakness.
Chỉ Định : May be used as an adjunct in the treatment of hypertension, as an epidural infusion as an adjunct treatment in the management of severe cancer pain that is not relieved by opiate analgesics alone, for differential diagnosis of pheochromocytoma in hypertensive patients, prophylaxis of vascular migraine headaches, treatment of severe dysmenorrhea, management of vasomotor symptoms associated with menopause, rapid detoxification in the management of opiate withdrawal, treatment of alcohol withdrawal used in conjunction with benzodiazepines, management of nicotine dependence, topical use to reduce intraocular pressure in the treatment of open-angle and secondary glaucoma and hemorrhagic glaucoma associated with hypertension, and in the treatment of attention-deficit hyperactivity disorder (ADHD).
Tương Tác Thuốc :
  • Acebutolol Increased hypertension when clonidine stopped
  • Amitriptyline The tricyclic antidepressant, amitriptyline, decreases the effect of clonidine.
  • Amoxapine The tricyclic antidepressant, amoxapine, decreases the effect of clonidine.
  • Atenolol Increased hypertension when clonidine stopped
  • Betaxolol Increased hypertension when clonidine stopped
  • Bevantolol Increased hypertension when clonidine stopped
  • Bisoprolol Increased hypertension when clonidine stopped
  • Carteolol Increased hypertension when clonidine stopped
  • Carvedilol Increased hypertension when clonidine stopped
  • Clomipramine The tricyclic antidepressant, clomipramine, may decrease the effect of clonidine.
  • Desipramine The tricyclic antidepressant, desipramine, decreases the effect of clonidine.
  • Doxepin The tricyclic antidepressant, doxepin, decreases the effect of clonidine.
  • Esmolol Increased hypertension when clonidine stopped
  • Imipramine The tricyclic antidepressant, imipramine, decreases the effect of clonidine.
  • Labetalol Increased hypertension when clonidine stopped
  • Metoprolol Increased hypertension when clonidine stopped
  • Milnacipran Because Savella inhibits norepinephrine reuptake, co-administration with clonidine may inhibit clonidine's anti-hypertensive effect.
  • Mirtazapine Possible hypertensive crisis
  • Nadolol Increased hypertension when clonidine stopped
  • Nortriptyline The tricyclic antidepressant, nortriptyline, decreases the effect of clonidine.
  • Oxprenolol Increased hypertension when clonidine stopped
  • Penbutolol Increased hypertension when clonidine stopped
  • Pindolol Increased hypertension when clonidine stopped
  • Practolol Increased hypertension when clonidine stopped
  • Propranolol Increased hypertension when clonidine stopped
  • Protriptyline The tricyclic antidepressant, protriptyline, decreases the effect of clonidine.
  • Sotalol Increased hypertension when clonidine stopped
  • Timolol Increased hypertension when clonidine stopped
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Trimipramine Trimipramine may reduce the antihypertensive effect of the alpha2-agonist, Clonidine. Trimipramine may also increase the rebound hypertensive effect of Clonidine. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Clonidine if Trimipramine is initiated, discontinued or dose changed. Clonidine should be withdrawn very gradually to reduce the risk of hypertensive crisis.
Liều Lượng & Cách Dùng : Injection, solution - Epidural - 100 mcg/ml
Injection, solution, concentrate - Epidural - 500 mcg/ml
Patch - Transdermal - 0.1 mg/24 hours
Patch - Transdermal - 0.2 mg/24 hours
Patch - Transdermal - 0.3 mg/24 hours
Tablet - Oral - 0.025 mg
Tablet - Oral - 0.1 mg
Tablet - Oral - 0.2 mg
Tablet - Oral - 0.3 mg
Dữ Kiện Thương Mại
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Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00575
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2803
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508119
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00281
ChemSpider
http://www.chemspider.com/Chemical-Structure.2701.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/49884-774-86
PharmGKB
http://www.pharmgkb.org/drug/PA449051
Wikipedia
http://en.wikipedia.org/wiki/Clonidine
RxList
http://www.rxlist.com/cgi/generic/clonidin.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cat1072.shtml
Drugs.com
http://www.drugs.com/clonidine.html
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