Tìm theo
Dipivefrin
Các tên gọi khác (9 ) :
  • (+-)-4-[1-Hydroxy-2-(methylamino)ethyl]-O-phenylene divavalate
  • 1-(3',4'-Dipivaloyloxyphenyl)-2-methylamino-1-ethanol
  • 4-[1-Hydroxy-2-(methylamino)ethyl]-O-phenylene divavalate
  • Dipivalyl Epinephrine
  • Dipivefrin
  • Dipivefrina
  • Dipivéfrine
  • Dipivefrinum
  • Pro-Epinephrine
adrenergic agonists, ophthalmics
Thuốc Gốc
Small Molecule
CAS: 52365-63-6
ATC: S01EA02
ĐG : Allergan Inc. , http://www.allergan.com
CTHH: C19H29NO5
PTK: 351.4373
Dipivefrin is a prodrug of adrenaline, which is used to treat glaucoma. It is available as ophthalmic solution (eye drops).
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H29NO5
Phân tử khối
351.4373
Monoisotopic mass
351.204573043
InChI
InChI=1S/C19H29NO5/c1-18(2,3)16(22)24-14-9-8-12(13(21)11-20-7)10-15(14)25-17(23)19(4,5)6/h8-10,13,20-21H,11H2,1-7H3
InChI Key
InChIKey=OCUJLLGVOUDECM-UHFFFAOYSA-N
IUPAC Name
2-[(2,2-dimethylpropanoyl)oxy]-5-[1-hydroxy-2-(methylamino)ethyl]phenyl 2,2-dimethylpropanoate
Traditional IUPAC Name
dipivefrin
SMILES
CNCC(O)C1=CC(OC(=O)C(C)(C)C)=C(OC(=O)C(C)(C)C)C=C1
Độ tan chảy
146-147
Độ hòa tan
Freely soluble as HCl salt
logP
1.7
logS
-3.8
pKa (strongest acidic)
14
pKa (Strongest Basic)
9.33
PSA
84.86 Å2
Refractivity
94.94 m3·mol-1
Polarizability
38.65 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Dipivefrin is a member of a class of drugs known as prodrugs. Prodrugs are usually not active in themselves and require biotransformation to the parent compound before therapeutic activity is seen. These modifications are undertaken to enhance absorption, decrease side effects and enhance stability and comfort, thus making the parent compound a more useful drug. Enhanced absorption makes the prodrug a more efficient delivery system for the parent drug because less drug will be needed to produce the desired therapeutic response. Dipivefrin is a prodrug of epinephrine formed by the diesterification of epinephrine and pivalic acid. The addition of pivaloyl groups to the epinephrine molecule enhances its lipophilic character and, as a consequence, its penetration into the anterior chamber.
Cơ Chế Tác Dụng : Dipivefrin is a prodrug of adrenaline, which is used to treat glaucoma. It is available as ophthalmic solution (eye drops). Dipivefrin is a prodrug with little or no pharmacologically activity until it is hydrolyzed into epinephrine inside the human eye. The liberated epinephrine, an adrenergic agonist, appears to exert its action by stimulating α -and/or β2-adrenergic receptors, leading to a decrease in aqueous production and an enhancement of outflow facility. The dipivefrin prodrug delivery system is a more efficient way of delivering the therapeutic effects of epinephrine, with fewer side effects than are associated with conventional epinephrine therapy.
Dược Động Học :
▧ Absorption :
Well absorbed following occular administration.
▧ Metabolism :
Dipivefrin is converted to epinephrine inside the human eye by enzyme hydrolysis.
Độc Tính : Oral LD50 in rat is 183 mg/kg.
Chỉ Định : Dipivefrin is a prodrug which is used as initial therapy for the control of intraocular pressure in chronic open-angle glaucoma.
Tương Tác Thuốc :
  • Desvenlafaxine Desvenlafaxine may increase the tachycardic and vasopressor effects of dipivefrin. Consider alternate therapy or monitor for increased sympathomimetic effects, such as increased blood pressure, chest pain and headache.
  • Venlafaxine Venlafaxine may increase the tachycardic and vasopressor effects of dipivefrin. Consider alternate therapy or monitor for increased sympathomimetic effects, such as increased blood pressure, chest pain and headache.
Liều Lượng & Cách Dùng : Liquid - Ophthalmic
Solution / drops - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Akorn
    Sản phẩm biệt dược : AKPro
  • Công ty : Allergan
    Sản phẩm biệt dược : D Epifrin
  • Công ty : Allergan
    Sản phẩm biệt dược : Diopine
  • Sản phẩm biệt dược : Pivalephrine
  • Công ty : Allergan
    Sản phẩm biệt dược : Propine
  • Công ty : Alcon
    Sản phẩm biệt dược : Thilodrin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00449
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3105
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504716
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06963
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02349
ChemSpider
http://www.chemspider.com/Chemical-Structure.2994.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0023-9208-10
PharmGKB
http://www.pharmgkb.org/drug/PA449364
Wikipedia
http://en.wikipedia.org/wiki/Dipivefrin
RxList
http://www.rxlist.com/cgi/generic2/dipivefrin.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/pro1356.shtml
Drugs.com
http://www.drugs.com/cdi/dipivefrin.html
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