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Articaine

pharmaceutical raw materials
Articaine structure

Articaine 

structure
  • CAS No:

    23964-58-1

  • Formula:

    C13H20N2O3S

  • Chemical Name:

    Articaine

  • Synonyms:

    2-Thiophenecarboxylic acid,4-methyl-3-[[1-oxo-2-(propylamino)propyl]amino]-,methyl ester;2-Thiophenecarboxylic acid,4-methyl-3-[2-(propylamino)propionamido]-,methyl ester;Carticaine;Articaine;161449-10-1

  • Categories:

    Pharmaceutical Intermediates  >  Bulk Drug Intermediates

Description

4-methyl-3-[[1-oxo-2-(propylamino)propyl]amino]-2-thiophenecarboxylic acid methyl ester is a thiophenecarboxylic acid.|Articaine is a dental local anesthetic. Articaine is widely used around the world and is the most popular local anesthetic in many European countries.|The amide local anesthetics including lidocaine, bupivacaine and ropivacaine are commonly used for pain control during minor surgery or invasive procedures such as biopsies, small excisions or dental work. These local anesthetics have not been linked to serum enzyme elevations, but when given as constant infusions or repeated injections have been occasionally mentioned as possible causes of clinically apparent liver injury.|A thiophene-containing local anesthetic pharmacologically similar to MEPIVACAINE.

Articaine Basic Attributes

284.38

284.37

924-214-7

DTXSID7048536

N01BB58|N - Nervous system

2934990002

Characteristics

95.7

2.63360

White or white crystalline powder

1.178 g/cm3

175-176 °C

162-167 °C @ Press: 0.3 Torr

220.3ºC

1.556

5.79E-08mmHg at 25°C

Safety Information

NONH for all modes of transport

P301 + P312 + P330

H302

Toxicity

In clinical trials with the amide local anesthetics, serum aminotransferase and alkaline phosphatase elevations were rarely reported and were generally no more common than with placebo or comparator injections. Despite widespread use for many decades, the local amide anesthetics, when given as single or limited injections or infusions, have not been convincingly linked to instances of clinically apparent liver injury, and liver toxicity is not mentioned in product labels. Nevertheless, there have been several case series of jaundice arising a few days to as long as a month after use of bupivacaine given over several days as a constant infusion or as repeated injections into a localized area of pain. Some reports mentioned concurrent administration of an antibiotic such as cefazolin during the perioperative period, which might have accounted for the liver injury. However, in other reports, only bupivacaine was given. The liver injury was mixed or cholestatic and mild-to-moderate in severity, resolving within 1 to 2 months of onset without residual evidence of liver injury. In many instances, there was an accompanying low grade fever, rash or eosinophilia, suggesting a hypersensitivity reaction.

Drug Information

The amide local anesthetics including lidocaine, bupivacaine and ropivacaine are commonly used for pain control during minor surgery or invasive procedures such as biopsies, small excisions or dental work. These local anesthetics have not been linked to serum enzyme elevations, but when given as constant infusions or repeated injections have been occasionally mentioned as possible causes of clinically apparent liver injury.

Anesthetics, Local

Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate. (See all compounds classified as Anesthetics, Local.)

Articain

Articaine Use and Manufacturing

Uses

Articaine is an amide based short-acting local anesthetic use for regional anaesthesia in day-case settings such arthroscopy, hand , food surgery and in dentistry.

Pharmaceuticals

Computed Properties

Molecular Weight:284.38
XLogP3:2.8
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:7
Exact Mass:284.11946368
Monoisotopic Mass:284.11946368
Topological Polar Surface Area:95.7
Heavy Atom Count:19
Complexity:325
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Local anesthetics

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Registered Holders

  • Pcas

    United States United States
    Active
  • MOEHS IBERICA SL

    United States United States
    Active

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