Tìm theo
Procainamide
Các tên gọi khác (6 ) :
  • Biocoryl
  • p-Amino-N-(2-diethylaminoethyl)benzamide
  • p-Aminobenzoic diethylaminoethylamide
  • Procainamida
  • Procainamide
  • Procainamidum
Thuốc chống loạn nhịp
Thuốc Gốc
Small Molecule
CAS: 51-06-9
ĐG : E.R. Squibb and Sons LLC
CTHH: C13H21N3O
PTK: 235.3253
A derivative of procaine with less CNS action. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H21N3O
Phân tử khối
235.3253
Monoisotopic mass
235.168462309
InChI
InChI=1S/C13H21N3O/c1-3-16(4-2)10-9-15-13(17)11-5-7-12(14)8-6-11/h5-8H,3-4,9-10,14H2,1-2H3,(H,15,17)
InChI Key
InChIKey=REQCZEXYDRLIBE-UHFFFAOYSA-N
IUPAC Name
4-amino-N-[2-(diethylamino)ethyl]benzamide
Traditional IUPAC Name
procainamide
SMILES
CCN(CC)CCNC(=O)C1=CC=C(N)C=C1
Độ tan chảy
165-169 °C
Độ hòa tan
5050 mg/L
logP
0.88
logS
-1.9
pKa (strongest acidic)
15.75
pKa (Strongest Basic)
9.04
PSA
58.36 Å2
Refractivity
72.25 m3·mol-1
Polarizability
27.69 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
9.32
Dược Lực Học : Procainamide is an agent indicated for production of local or regional anesthesia and in the treatment of ventricular tachycardia occurring during cardiac manipulation, such as surgery or catheterization, or which may occur during acute myocardial infarction, digitalis toxicity, or other cardiac diseases. The mode of action of the antiarrhythmic effect of Procainamide appears to be similar to that of procaine and quinidine. Ventricular excitability is depressed and the stimulation threshold of the ventricle is increased during diastole. The sinoatrial node is, however, unaffected.
Cơ Chế Tác Dụng : A derivative of procaine with less CNS action. [PubChem] Procainamide is sodium channel blocker. It stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action.
Dược Động Học :
▧ Absorption :
75 to 95%
▧ Volume of Distribution :
* 2 L/kg
▧ Protein binding :
15 to 20%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Trace amounts may be excreted in the urine as free and conjugated p-aminobenzoic acid, 30 to 60 percent as unchanged PA, and 6 to 52 percent as the NAPA derivative.
▧ Half Life :
~2.5-4.5 hours
Độc Tính : LD50=95 mg/kg (rat, IV); LD50=312 mg/kg (mouse, oral); LD50=103 mg/kg (mouse, IV); LD50=250 mg/kg (rabbit, IV)
Chỉ Định : For the treatment of life-threatening ventricular arrhythmias.
Tương Tác Thuốc :
  • Amiodarone Amiodarone may increase serum levels and toxicity of procainamide.
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Cimetidine The histamine H2-receptor antagonist, cimetidine, may increase the effect of procainamide.
  • Ciprofloxacin Ciprofloxacin may increase the effect of procainamide.
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Dihydroquinidine barbiturate Quinidine increases the effect of procainamide
  • Donepezil Possible antagonism of action
  • Fingolimod Pharmacodynamic synergist. Contraindicated. Increased risk of bradycardia, AV block, and torsade de pointes.
  • Galantamine Possible antagonism of action
  • Levofloxacin Levofloxacin may increase the effect of procainamide.
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Mesoridazine Increased risk of cardiotoxicity and arrhythmias
  • Ofloxacin Ofloxacin may increase the effect of procainamide.
  • Quinidine Quinidine increases the effect of procainamide
  • Quinidine barbiturate Quinidine increases the effect of procainamide
  • Ranitidine The histamine H2-receptor antagonist, ranitidine, may increase the effect of procainamide.
  • Ranolazine Possible additive effect on QT prolongation
  • Rivastigmine Possible antagonism of action
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Telavancin Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Terbinafine Terbinafine may reduce the metabolism and clearance of Procainamide. Consider alternate therapy or monitor for therapeutic/adverse effects of Procainamide if Terbinafine is initiated, discontinued or dose changed.
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
  • Thioridazine Increased risk of cardiotoxicity and arrhythmias
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimethoprim Trimethoprim may reduce the clearance of Procainamide. Alternative treatments should be considered. If Trimethoprim is initiated or the dose is increased, monitor for increased toxicity of Procainamide (e.g. QTc intervals, EKG, serum drug concentrations). If Trimethoprim is discontinued or the dose decreased, monitor for reduced effects of Procainamide.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Vardenafil Increased risk of cardiotoxicity and arrhythmias
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Capsule - Oral
Solution - Intramuscular
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Biocoryl
  • Công ty :
    Sản phẩm biệt dược : Procan
  • Công ty :
    Sản phẩm biệt dược : Procanbid
  • Công ty :
    Sản phẩm biệt dược : Procapan
  • Công ty :
    Sản phẩm biệt dược : Pronestyl
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01035
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4913
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507313
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07401
ChemSpider
http://www.chemspider.com/Chemical-Structure.4744.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0003-0758-50
PharmGKB
http://www.pharmgkb.org/drug/PA451108
Wikipedia
http://en.wikipedia.org/wiki/Procainamide
RxList
http://www.rxlist.com/cgi/generic3/procain.htm
Drugs.com
http://www.drugs.com/cdi/procainamide.html
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