Tìm theo
Mepivacaine
Các tên gọi khác (8 ) :
  • (+-)-1-Methyl-2',6'-pipecoloxylidide
  • 1-methyl-2',6'-pipecoloxylidide
  • Carbocaine
  • DL-Mepivacaine
  • Mepivacaina
  • Mepivacainum
  • N-(2,6-Dimethylphenyl)-1-methyl-2-piperidinecarboxamide
  • N-(2,6-Dimethylphenyl)-1-methylpiperidine-2-carboxamide
Thuốc gây tê, mê
Thuốc Gốc
Small Molecule
CAS: 96-88-8
ATC: N01BB03
ĐG : American Dental Cooperative Inc. , http://www.gotoadc.com
CTHH: C15H22N2O
PTK: 246.348
A local anesthetic that is chemically related to bupivacaine but pharmacologically related to lidocaine. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H22N2O
Phân tử khối
246.348
Monoisotopic mass
246.173213336
InChI
InChI=1S/C15H22N2O/c1-11-7-6-8-12(2)14(11)16-15(18)13-9-4-5-10-17(13)3/h6-8,13H,4-5,9-10H2,1-3H3,(H,16,18)
InChI Key
InChIKey=INWLQCZOYSRPNW-UHFFFAOYSA-N
IUPAC Name
N-(2,6-dimethylphenyl)-1-methylpiperidine-2-carboxamide
Traditional IUPAC Name
mepivacaine
SMILES
CN1CCCCC1C(=O)NC1=C(C)C=CC=C1C
Độ tan chảy
150.5 °C
Độ hòa tan
7000 mg/L (at 23 °C)
logP
1.95
logS
-1.55
pKa (strongest acidic)
13.62
pKa (Strongest Basic)
7.25
PSA
32.34 Å2
Refractivity
76.32 m3·mol-1
Polarizability
28.61 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
7.7
Dược Lực Học : Mepivicaine is a local anesthetic of the amide type. Mepivicaine as a reasonably rapid onset and medium duration and is known by the proprietary names as Carbocaine and Polocaine. Mepivicaine is used in local infiltration and regional anesthesia. Systemic absorption of local anesthetics produces effects on the cardiovascular and central nervous systems. At blood concentrations achieved with normal therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal.
Cơ Chế Tác Dụng : A local anesthetic that is chemically related to bupivacaine but pharmacologically related to lidocaine. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168) Local anesthetics block the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: pain, temperature, touch, proprioception, and skeletal muscle tone.
Dược Động Học :
▧ Absorption :
Absorbed locally. The rate of systemic absorption of local anesthetics is dependent upon the total dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic solution.
▧ Protein binding :
Mepivacaine is approximately 75% bound to plasma proteins. Generally, the lower the plasma concentration of drug, the higher the percentage of drug bound to plasma.
▧ Metabolism :
Rapidly metabolized, with only a small percentage of the anesthetic (5 percent to 10 percent) being excreted unchanged in the urine. The liver is the principal site of metabolism, with over 50% of the administered dose being excreted into the bile as metabolites.
▧ Route of Elimination :
It is rapidly metabolized, with only a small percentage of the anesthetic (5 percent to 10 percent) being excreted unchanged in the urine.The liver is the principal site of metabolism, with over 50% of the administered dose being excreted into the bile as metabolites.
▧ Half Life :
The half-life of mepivacaine in adults is 1.9 to 3.2 hours and in neonates 8.7 to 9 hours.
Độc Tính : The mean seizure dosage of mepivacaine in rhesus monkeys was found to be 18.8 mg/kg with mean arterial plasma concentration of 24.4 µg/mL. The intravenous and subcutaneous LD 50 in mice is 23 mg/kg to 35 mg/kg and 280 mg/kg respectively.
Chỉ Định : For production of local or regional analgesia and anesthesia by local infiltration, peripheral nerve block techniques, and central neural techniques including epidural and caudal blocks.
Liều Lượng & Cách Dùng : Liquid - Infiltration
Solution - Infiltration
Solution - Subcutaneous
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Mepivacaine hcl powder
    Giá bán buôn : USD >318.33
    Đơn vị tính : g
  • Biệt dược thương mại : Carbocaine 2% vial
    Giá bán buôn : USD >0.19
    Đơn vị tính : ml
  • Biệt dược thương mại : Polocaine 2% vial
    Giá bán buôn : USD >0.24
    Đơn vị tính : ml
  • Biệt dược thương mại : Polocaine 1% vial
    Giá bán buôn : USD >0.25
    Đơn vị tính : ml
  • Biệt dược thương mại : Carbocaine 1% vial
    Giá bán buôn : USD >0.26
    Đơn vị tính : ml
  • Biệt dược thương mại : Mepivacaine hcl 3% cartridge
    Giá bán buôn : USD >0.46
    Đơn vị tính : ml
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Carbocaine
  • Công ty :
    Sản phẩm biệt dược : Isocaine
  • Công ty :
    Sản phẩm biệt dược : Polocaine
  • Công ty :
    Sản phẩm biệt dược : Scandicaine
  • Công ty :
    Sản phẩm biệt dược : Scandonest Plain
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00961
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4062
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507857
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07528
ChemSpider
http://www.chemspider.com/Chemical-Structure.3922.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0186-0412-01
PharmGKB
http://www.pharmgkb.org/drug/PA164748741
Wikipedia
http://en.wikipedia.org/wiki/Mepivacaine
RxList
http://www.rxlist.com/cgi/generic2/mepivacaine.htm
Drugs.com
http://www.drugs.com/cdi/mepivacaine.html
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