Tìm theo
Brimonidine
Các tên gọi khác (5 ) :
  • 5-Bromo-6-(2-imidazolin-2-ylamino)quinoxaline
  • Brimonidina
  • Brimonidine
  • Brimonidinum
  • Bromoxidine
antihypertensive agents, adrenergic alpha 2 receptor agonists, eent preparations
Thuốc Gốc
Small Molecule
CAS: 59803-98-4
ATC: S01EA05
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C11H10BrN5
PTK: 292.135
Brimonidine is a drug used to treat glaucoma. It acts via decreasing aqueous humor synthesis. [Wikipedia] A topical gel formulation, marketed under the name Mirvaso, was FDA approved on August 2013 for the treatment of rosacea.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C11H10BrN5
Phân tử khối
292.135
Monoisotopic mass
291.011957992
InChI
InChI=1S/C11H10BrN5/c12-9-7(17-11-15-5-6-16-11)1-2-8-10(9)14-4-3-13-8/h1-4H,5-6H2,(H2,15,16,17)
InChI Key
InChIKey=XYLJNLCSTIOKRM-UHFFFAOYSA-N
IUPAC Name
5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine
Traditional IUPAC Name
brimonidine
SMILES
BrC1=C(NC2=NCCN2)C=CC2=NC=CN=C12
Độ tan chảy
207.5 °C
Độ hòa tan
Soluble (1.5 mg/mL)
logP
1.7
logS
-3.3
pKa (Strongest Basic)
8.32
PSA
62.2 Å2
Refractivity
68.49 m3·mol-1
Polarizability
25.74 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Brimonidine significantly lowers intraocular pressure with minimal effects on cardiovascular and pulmonary parameters. It lowers intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow.
Cơ Chế Tác Dụng : Brimonidine is a drug used to treat glaucoma. It acts via decreasing aqueous humor synthesis. [Wikipedia] A topical gel formulation, marketed under the name Mirvaso, was FDA approved on August 2013 for the treatment of rosacea. Brimonidine is an alpha adrenergic receptor agonist (primarily alpha-2). It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that Brimonidine has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow. The topical gel reduces erythema through direct vasocontriction.
Dược Động Học :
▧ Absorption :
Minimal systemic absorption occurs after ocular insertion. When the topical gel was applied to adult patients with facial erythema associated with rosacea, the plasma maximum concentration (Cmax) and area under the concentration-time curve (AUC) were 46 ± 62 pg/mL and 417 ± 264 pg.hr/mL, respectively. These values were reached on Day 15 of treatment.
▧ Metabolism :
Metabolized primarily by the liver.
▧ Route of Elimination :
Urinary excretion is the major route of elimination of the drug and its metabolites.
▧ Half Life :
2 hours [ophthalmic solution]
Độc Tính : Oral LD50 is 50 mg/kg in mice and 100 mg/kg in rats. Common adverse reactions of the topical gel formulation include erythema, flushing, skin burning sensation, and contact dermatitis.
Chỉ Định : The ophthalmic solution is indicated for patients with open-angle glaucoma or ocular hypertension to lower intraocular pressure. The topical gel is indicated for the treatment of persistent (nontransient) facial erythema of rosacea in adults 18 years or older.
Tương Tác Thuốc :
  • Aliskiren Monitor therapy because of enhanced hypotensive effect.
  • Droperidol Droperidol may enhance the CNS depressant effect of brimonidine. Consider therapy modification.
  • Isocarboxazid MAO Inhibitors like isocarboxazid may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
  • Linezolid MAO Inhibitors like linezolid may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
  • Methotrimeprazine Brimonidine may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of brimonidine. Consider therapy modification.
  • Moclobemide MAO Inhibitors like moclobemide may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
  • Phenelzine MAO Inhibitors like phenelzine may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
  • Procarbazine MAO Inhibitors like procarbazine may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
  • Rasagiline MAO Inhibitors like rasagiline may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
  • Selegiline MAO Inhibitors like selegiline may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
  • Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the alpha2-agonist, Brimonidine. Concomitant therapy is contraindicated.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Liều Lượng & Cách Dùng : Gel - Topical - 0.33%
Solution - Ophthalmic - 0.1%, 0.15%
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00484
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2435
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507305
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07886
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02076
ChemSpider
http://www.chemspider.com/Chemical-Structure.2341.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/60758-866-05
PharmGKB
http://www.pharmgkb.org/drug/PA448665
Wikipedia
http://en.wikipedia.org/wiki/Brimonidine
RxList
http://www.rxlist.com/cgi/generic3/alphagan-p.htm
Drugs.com
http://www.drugs.com/cdi/brimonidine.html
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