Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C18H28N2O.ClH |
| Molecular Weight | 324.889 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCCCN1CCCC1C(=O)NC2=C(C)C=C(C)C=C2C
InChI
InChIKey=NFEZGTHMTGKIBG-UHFFFAOYSA-N
InChI=1S/C18H28N2O.ClH/c1-5-6-9-20-10-7-8-16(20)18(21)19-17-14(3)11-13(2)12-15(17)4;/h11-12,16H,5-10H2,1-4H3,(H,19,21);1H
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C18H28N2O |
| Molecular Weight | 288.4277 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
Bumecaine (Pyromecaine) is a local anesthetic and anti-arrhythmic drug. It is indicated as an agent for superficial anesthesia during medical and diagnostic procedures in dentistry, ophthalmology, otorhinolaryngology, surgery, bronchology, gastroenterology, urology. The experiments on the isolated neurons in the rat spinal ganglions have shown that interaction of pyromecaine with inactivated Na+ channels makes a considerable contribution to the blocking effect of anesthesia. Oral administration of pyromecaine pills considerably depresses platelet aggregation and even causes platelet disaggregation. Possible side effects are: general weakness, nausea, vomiting, headache, dizziness, fainting, a drop in blood pressure. Quinidine increases the risk of side effects.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Sodium channels |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Bumecain Approved UsePyromecaine is prescribed as an anesthetic for superficial anesthesia during medical and diagnostic procedures in dentistry, ophthalmology, otorhinolaryngology, surgery, bronchology, gastroenterology, urology. Pyromecaine is also used as an antiarrhythmic agent. |
|||
| Primary | Bumecain Approved UsePyromecaine is prescribed as an anesthetic for superficial anesthesia during medical and diagnostic procedures in dentistry, ophthalmology, otorhinolaryngology, surgery, bronchology, gastroenterology, urology. Pyromecaine is also used as an antiarrhythmic agent. |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.61 μg/mL |
50 mg single, intravenous dose: 50 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
BUMECAINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1.22 μg/mL |
100 mg single, intravenous dose: 100 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
BUMECAINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
34.2 μg × min/mL |
50 mg single, intravenous dose: 50 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
BUMECAINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
68.7 μg × min/mL |
100 mg single, intravenous dose: 100 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
BUMECAINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.3 h |
50 mg single, intravenous dose: 50 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
BUMECAINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1.75 h |
100 mg single, intravenous dose: 100 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
BUMECAINE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| [A morphological evaluation of the tissue status of the oral mucosa after anesthesia applied with dicaine and pyromecaine solutions]. | 1990-11-01 |
|
| [The action of aqueous solutions of dicaine and pyromecaine on the epithelium of the oral mucosa]. | 1990-05-01 |
|
| [The Ca2+ reactivity and the subunit composition of myocardial actomyosin during the pyromecaine and pyrroxan treatment of experimental ischemia]. | 1990-01-01 |
|
| [Interaction of quinidine, lidocaine, tricaine and pyromecaine with heparin]. | 1989-07-01 |
|
| [Effect of anti-angina therapy on phospholipid levels of the myocardium in ischemic lesions]. | 1988-10 |
|
| [Anti-arrhythmia properties of pyromecaine]. | 1983-09-01 |
| Substance Class |
Chemical
Created
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Edited
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Mon Mar 31 21:06:38 GMT 2025
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| Record UNII |
PBE1H9OIFQ
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| Record Status |
Validated (UNII)
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DTXSID00940679
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19089-24-8
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167785
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