Details
| Stereochemistry | UNKNOWN |
| Molecular Formula | C17H28N2O.ClH |
| Molecular Weight | 312.878 |
| Optical Activity | ( - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCCN(CC)C(CC)C(=O)NC1=C(C)C=CC=C1C
InChI
InChIKey=LMWQQUMMGGIGJQ-UHFFFAOYSA-N
InChI=1S/C17H28N2O.ClH/c1-6-12-19(8-3)15(7-2)17(20)18-16-13(4)10-9-11-14(16)5;/h9-11,15H,6-8,12H2,1-5H3,(H,18,20);1H
DescriptionCurator's Comment: description was created based on several sources, including
http://www.kiessig.com/drugs/druginfo.aspx?id=1218 | http://www.kiessig.com/drugs/druginfo.aspx?id=1218 | https://www.ncbi.nlm.nih.gov/pubmed/8799190 | https://www.ncbi.nlm.nih.gov/pubmed/8085162
Curator's Comment: description was created based on several sources, including
http://www.kiessig.com/drugs/druginfo.aspx?id=1218 | http://www.kiessig.com/drugs/druginfo.aspx?id=1218 | https://www.ncbi.nlm.nih.gov/pubmed/8799190 | https://www.ncbi.nlm.nih.gov/pubmed/8085162
Etidocaine, marketed under the trade name Duranest, is a local anesthetic given by injection during surgical procedures and labor and delivery. Etidocaine has a long duration of activity, and the main disadvantage of using during dentistry is increased bleeding during surgery. Etidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL4187 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | DURANEST Approved UseINDICATIONS AND USAGE. Duranest (Etidocaine HCl) Injections are indicated for infiltration anesthesia, peripheral nerve blocks (e.g., brachial plexus, intercostal, retrobulbar, ulnar, inferior alveolar), and central neural block (i.e., lumbar or caudal epidural blocks). Launch Date1976 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
12.5 μg/mL |
20 mL single, peridural dose: 20 mL route of administration: Peridural experiment type: SINGLE co-administered: EPINEPHRINE |
ETIDOCAINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.8 μg × h/mL |
20 mL single, peridural dose: 20 mL route of administration: Peridural experiment type: SINGLE co-administered: EPINEPHRINE |
ETIDOCAINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.7 h |
20 mL single, peridural dose: 20 mL route of administration: Peridural experiment type: SINGLE co-administered: EPINEPHRINE |
ETIDOCAINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
6% |
20 mL single, peridural dose: 20 mL route of administration: Peridural experiment type: SINGLE co-administered: EPINEPHRINE |
ETIDOCAINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| A double-blind trial of bupivacaine (Marcain) and etidocaine (Duranest) in extradural block for surgical induction of labour. | 1975 Dec |
|
| Relative neural toxicity of local anesthetics. | 1993 May |
|
| Pain of injection and duration of anesthesia for intradermal infiltration of lidocaine, bupivacaine, and etidocaine. | 1994 Jul |
|
| From cocaine to ropivacaine: the history of local anesthetic drugs. | 2001 Aug |
|
| Molecular determinants of voltage-dependent gating and binding of pore-blocking drugs in transmembrane segment IIIS6 of the Na(+) channel alpha subunit. | 2001 Jan 5 |
|
| Cardiac toxicity of local anesthetics in the intact isolated heart model: a review. | 2002 Nov-Dec |
|
| Local anesthesia: advances in agents and techniques. | 2002 Oct |
|
| Peribulbar anaesthesia using a combination of lidocaine, bupivocaine and clonidine in vitreoretinal surgery. | 2002 Sep |
|
| [Local anesthetics. Differences and similarities in the "-cains"]. | 2003 Apr |
|
| Toxicity of local anaesthetics. | 2003 Mar |
|
| Lipid rescue resuscitation from local anaesthetic cardiac toxicity. | 2006 |
|
| Update on local anesthetics: focus on levobupivacaine. | 2008 Apr |
|
| Direct vasocontractile activities of bupivacaine enantiomers on the isolated rat thoracic aorta. | 2010 |
|
| Use of local anaesthetics and adjuncts for spinal and epidural anaesthesia and analgesia at German and Austrian University Hospitals: an online survey to assess current standard practice. | 2010 Apr 17 |
|
| Progress in analgesia for labor: focus on neuraxial blocks. | 2010 Aug 9 |
|
| The efficacy of ilioinguinal and iliohypogastric nerve block for postoperative pain after caesarean section. | 2010 Jan |
|
| Intravenous lipid emulsion in clinical toxicology. | 2010 Oct 5 |
Patents
Sample Use Guides
The maximum dose to be employed as a single injection should be determined on the basis of the status of the patient and the type of regional anesthetic technique to be performed. Although single injections of 450 mg have been employed for regional anesthesia without adverse effects, at present it is strongly recommended that the maximal dose as a single injection should not exceed 400 mg (approximately 8.0 mg/kg or 3.6 mg/lb based on a 50 kg person) with epinephrine 1:200,000 and 300 mg (approximately 6 mg/kg or 2.7 mg/lb based on a 50 kg person) without epinephrine.
Route of Administration:
Intramuscular
Rat brain type IIA Na+ channels expressed in Xenopus oocytes were stimulated infrequently (1 pulse per 20 s, all currents were elicited by 15-ms pulses to 0 mV.) This tonic block mainly reflects drug binding to resting channels, the channel state that predominated at the holding potential of -90 mV. Etidocaine (200 mkM) decrease activities of WT Type IIA Na+ channels on ~40%.
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YGD0Y35434
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1290125-23-3
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37498
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38188-14-6
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SUBSTANCE RECORD
