Tìm theo
Lidocaine
Các tên gọi khác (7 ) :
  • 2-(Diethylamino)-2',6'-acetoxylidide
  • 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide
  • alpha-diethylamino-2,6-dimethylacetanilide
  • Lidocaine
  • Lidoderm
  • Lignocaine
  • α-diethylamino-2,6-dimethylacetanilide
Thuốc gây tê, mê
Thuốc Gốc
Small Molecule
CAS: 137-58-6
ATC: C01BB01, C05AD01, D04AB01, N01BB02, R02AD02, S01HA07, S02DA01, A01AD11
ĐG : 4uOrtho LLC , http://www.4udr.com
CTHH: C14H22N2O
PTK: 234.3373
A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of procaine but its duration of action is shorter than that of bupivacaine or prilocaine. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H22N2O
Phân tử khối
234.3373
Monoisotopic mass
234.173213336
InChI
InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17)
InChI Key
InChIKey=NNJVILVZKWQKPM-UHFFFAOYSA-N
IUPAC Name
2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide
Traditional IUPAC Name
lidocaine
SMILES
CCN(CC)CC(=O)NC1=C(C)C=CC=C1C
Độ tan chảy
68.5 °C
Độ sôi
159-160 °C at 2.00E+00 mm Hg
Độ hòa tan
4100 mg/L (at 30 °C)
logP
2.44
logS
-1.76
pKa (strongest acidic)
13.78
pKa (Strongest Basic)
7.75
PSA
32.34 Å2
Refractivity
73.93 m3·mol-1
Polarizability
27.77 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.21
pKa
8.01
Dược Lực Học : Lidocaine is an anesthetic 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 Lidocaine appears to be similar to that of procaine, procainamide and quinidine. Ventricular excitability is depressed and the stimulation threshold of the ventricle is increased during diastole. The sinoatrial node is, however, unaffected. In contrast to the latter 3 drugs, Lidocaine in therapeutic doses does not produce a significant decrease in arterial pressure or in cardiac contractile force. In larger doses, lidocaine may produce circulatory depression, but the magnitude of the change is less than that found with comparable doses of procainamide.
Cơ Chế Tác Dụng : A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of procaine but its duration of action is shorter than that of bupivacaine or prilocaine. [PubChem] Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action. Lidocaine alters signal conduction in neurons by blocking the fast voltage gated sodium (Na+) channels in the neuronal cell membrane that are responsible for signal propagation. With sufficient blockage the membrane of the postsynaptic neuron will not depolarize and will thus fail to transmit an action potential. This creates the anaesthetic effect by not merely preventing pain signals from propagating to the brain but by aborting their birth in the first place.
Dược Động Học :
▧ Absorption :
Information derived from diverse formulations, concentrations and usages reveals that lidocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon various factors such as the site of administration and the presence or absence of a vasoconstrictor agent.
▧ Volume of Distribution :
* 0.7 to 2.7 L/kg [healthy volunteers]
▧ Protein binding :
60-80%
▧ Metabolism :
Primarily hepatic.
▧ Route of Elimination :
Lidocaine and its metabolites are excreted by the kidneys.
▧ Half Life :
109 minutes
▧ Clearance :
* 0.64 +/- 0.18 L/min
Độc Tính : The oral LD 50 of lidocaine HCl in non-fasted female rats is 459 (346-773) mg/kg (as the salt) and 214 (159-324) mg/kg (as the salt) in fasted female rats. Symptoms of overdose include convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.
Chỉ Định : For production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.
Tương Tác Thuốc :
  • Acebutolol The beta-blocker, acebutolol, may increase the effect and toxicity of lidocaine.
  • Atazanavir Increased risk of cardiotoxicity and arrhythmias
  • Atenolol The beta-blocker, atenolol, may increase the effect and toxicity of lidocaine.
  • Bisoprolol The beta-blocker, bisoprolol, may increase the effect and toxicity of lidocaine.
  • Carvedilol The beta-blocker, carvedilol, may increase the effect and toxicity of lidocaine.
  • Cimetidine Increases the effect and toxicity of lidocaine
  • Darunavir Possible increase in lidocaine levels
  • Esmolol The beta-blocker, esmolol, may increase the effect and toxicity of lidocaine.
  • Etravirine Lidocaine, when used concomitantly with etravirine, may experience a decrease in serum concentration. It is recommended to monitor lidocaine therapy.
  • Labetalol The beta-blocker, labetalol, may increase the effect and toxicity of lidocaine.
  • Metoprolol The beta-blocker, metoprolol, may increase the effect and toxicity of lidocaine
  • Nadolol The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
  • Oxprenolol The beta-blocker increases the effect and toxicity of lidocaine
  • Penbutolol Penbutolol increases the volume of distribution of lidocaine in normal subjects. This could result in a requirement for higher loading doses of lidocaine.
  • Pindolol The beta-blocker increases the effect and toxicity of lidocaine
  • Propranolol The beta-blocker, propranolol, may increase the effect and toxicity of lidocaine.
  • Quinupristin This combination presents an increased risk of toxicity
  • Tacrine The metabolism of Tacrine, a CYP1A2 substrate, may be reduced by strong CYP1A2 inhibitors such as Lidocaine. Consider modifying therapy to avoid Tacrine toxicity. Monitor the efficacy and toxicity of Tacrine if Lidocaine is initiated, discontinued or if the dose is changed.
  • Tamoxifen Lidocaine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
  • Tamsulosin Lidocaine, a CYP3A4/2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4/2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Lidocaine is initiated, discontinued, or dose changed.
  • Telithromycin Telithromycin may reduce clearance of Lidocaine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Lidocaine if Telithromycin is initiated, discontinued or dose changed.
  • Terbinafine Terbinafine may reduce the metabolism and clearance of Lidocaine. Consider alternate therapy or monitor for therapeutic/adverse effects of Lidocaine if Terbinafine is initiated, discontinued or dose changed.
  • Thiothixene The strong CYP1A2 inhibitor, Lidocaine, may decrease the metabolism and clearance of Thiothixene, a CYP1A2 substrate. Consider alternate therapy or monitor for changes in Thiothixene therapeutic and adverse effects if Lidocaine is initiated, discontinued or dose changed.
  • Timolol The beta-blocker, timolol, may increase the effect and toxicity of lidocaine.
  • Tizanidine Lidocaine may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
  • Tolterodine Lidocaine may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
  • Tramadol Lidocaine may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Lidocaine may decrease the effect of Tramadol by decreasing active metabolite production.
  • Trazodone The CYP3A4 inhibitor, Lidocaine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Lidocaine is initiated, discontinued or dose changed.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of lidocaine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of lidocaine if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Aerosol - Topical
Aerosol, metered - Topical
Cream - Topical
Gel - Topical
Jelly - Topical
Jelly - Urethral
Liquid - Buccal
Liquid - Dental
Liquid - Infiltration
Liquid - Intravenous
Liquid - Oral
Liquid - Topical
Lotion - Topical
Ointment - Topical
Solution - Infiltration
Solution - Intramuscular
Solution - Intravenous
Solution - Oral
Solution - Topical
Spray - Topical
Swab - Topical
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : After Burn Double Strength Gel
  • Công ty :
    Sản phẩm biệt dược : After Burn Double Strength Spray
  • Công ty :
    Sản phẩm biệt dược : After Burn Gel
  • Công ty :
    Sản phẩm biệt dược : After Burn Spray
  • Công ty :
    Sản phẩm biệt dược : Akten
  • Công ty :
    Sản phẩm biệt dược : Alphacaine
  • Công ty :
    Sản phẩm biệt dược : Anestacon
  • Công ty :
    Sản phẩm biệt dược : Anestacon Jelly
  • Công ty :
    Sản phẩm biệt dược : DermaFlex
  • Công ty :
    Sản phẩm biệt dược : Dilocaine
  • Công ty :
    Sản phẩm biệt dược : Esracaine
  • Công ty :
    Sản phẩm biệt dược : L-Caine
  • Công ty :
    Sản phẩm biệt dược : Laryng-O-Jet
  • Công ty :
    Sản phẩm biệt dược : Lidoderm
  • Công ty :
    Sản phẩm biệt dược : Lidoject-1
  • Công ty :
    Sản phẩm biệt dược : Lidoject-2
  • Công ty :
    Sản phẩm biệt dược : Norwood Sunburn Spray
  • Công ty :
    Sản phẩm biệt dược : Solarcaine
  • Công ty :
    Sản phẩm biệt dược : Xylocaine
  • Công ty :
    Sản phẩm biệt dược : Xylocaine-MPF
  • Công ty :
    Sản phẩm biệt dược : Xylocard
  • Công ty :
    Sản phẩm biệt dược : Zilactin-L
  • Công ty :
    Sản phẩm biệt dược : Zingo
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00281
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3676
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505060
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00358
ChemSpider
http://www.chemspider.com/Chemical-Structure.3548.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/21695-075-30
PharmGKB
http://www.pharmgkb.org/drug/PA450226
Wikipedia
http://en.wikipedia.org/wiki/Lidocaine
RxList
http://www.rxlist.com/cgi/generic2/xylocaineinj.htm
Drugs.com
http://www.drugs.com/cdi/lidocaine-gel.html
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