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mepivacaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| local anaesthetics | 1700 | 96-88-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 2.40 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 5 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 23.19 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 55 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.95 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 6.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.30 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.561 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.531 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 40.551 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 11.482 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 63.210 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 74.820 | % | High | 1 |
| herg | hERG pIC50 | 4.228 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.614 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 9.162 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 57.430 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,MAPK7,MAPKAPK2,NTRK2,PDK2,PDK4,PIK3CB,PRKDC,SIK2,SIK3,TEK | 22 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,DDR1,EPHB4,ERBB2,GRK2,MAPK7,PDK4,SIK2,SIK3 | 11 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.650 | Moderate | 0.76 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.518 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 39.994 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 75.970 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.986 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 78.560 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 1.107 | % | Moderate | 0.76 |
| rh-clint | Rat hepatocyte intrinsic clearance | 31.261 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 90.660 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 77.250 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 887.156 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 6, 1960 | FDA | EASTMAN KODAK | |
| Dec. 23, 2022 | PMDA | NIPPON SHIKA YAKUHIN CO., LTD. |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Monoplegia | 85.32 | 51.39 | 17 | 1014 | 3657 | 90623759 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Anaphylactic shock | 67.59 | 38.93 | 21 | 558 | 23496 | 42597260 |
| Local anaesthetic systemic toxicity | 59.57 | 38.93 | 12 | 567 | 2288 | 42618468 |
| Drug ineffective | 48.34 | 38.93 | 50 | 529 | 630147 | 41990609 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Anaphylactic shock | 90.74 | 40.99 | 32 | 1499 | 51514 | 110536254 |
| Local anaesthetic systemic toxicity | 59.05 | 40.99 | 14 | 1517 | 5523 | 110582245 |
| Mycobacterium chelonae infection | 55.85 | 40.99 | 12 | 1519 | 3048 | 110584720 |
| Seizure | 41.76 | 40.99 | 30 | 1501 | 221155 | 110366613 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N01BB03 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Amides |
| ATC | N01BB53 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Amides |
| FDA CS | M0000897 | Amides |
| MeSH PA | D000777 | Anesthetics |
| MeSH PA | D000779 | Anesthetics, Local |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D018689 | Sensory System Agents |
| CHEBI has role | CHEBI:35480 | analgesic |
| CHEBI has role | CHEBI:36333 | local anaesthetic |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
| CHEBI has role | CHEBI:88188 | drug allergen |
| FDA EPC | N0000175682 | Amide Local Anesthetic |
| FDA PE | N0000175976 | Local Anesthesia |
Related Drugs by ATC class:
N01BB Amides 10 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Local anesthesia, by infiltration | indication | 44596000 | |
| Local anesthesia | indication | 386761002 | |
| Administration of Regional Anesthesia | indication | ||
| Administration of Local Anesthetic Nerve Block | indication | ||
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Deficiency of cholinesterase | contraindication | 360607009 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Horses | Local anesthetic for infiltration, nerve block, intra-articular and epidural anesthesia and topical and/or infiltration anesthesia of the laryngeal mucosa prior to ventriculectomy | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Carbocaine-V Sterile Aqueous Solution | Zoetis Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.06 | acidic |
| pKa2 | 7.81 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium channel protein type 5 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
| Sodium channel protein type 1 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
| Sodium channel protein type 2 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
| Sodium channel protein type 3 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
| Sodium channel protein type 4 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
| Sodium channel protein type 8 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
| Sodium channel protein type 9 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019815 | VUID |
| N0000147904 | NUI |
| D00738 | KEGG_DRUG |
| 1722-62-9 | SECONDARY_CAS_RN |
| 4018232 | VANDF |
| 4019815 | VANDF |
| C0025384 | UMLSCUI |
| CHEBI:6759 | CHEBI |
| CHEMBL1087 | ChEMBL_ID |
| DB00961 | DRUGBANK_ID |
| CHEMBL1200440 | ChEMBL_ID |
| D008619 | MESH_DESCRIPTOR_UI |
| 4062 | PUBCHEM_CID |
| 7224 | IUPHAR_LIGAND_ID |
| 988 | INN_ID |
| B6E06QE59J | UNII |
| 2021 | RXNORM |
| 1899 | MMSL |
| 5050 | MMSL |
| 64048 | MMSL |
| 73448 | MMSL |
| d01398 | MMSL |
| 001352 | NDDF |
| 004567 | NDDF |
| 391673008 | SNOMEDCT_US |
| 59560006 | SNOMEDCT_US |
| 65741009 | SNOMEDCT_US |
| B6E06QE59J | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Carbocaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0362-0753 | INJECTION, SOLUTION | 30 mg | SUBMUCOSAL | ANDA | 20 sections |
| Scandonest 3% Plain | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0362-1098 | injection, solution | 30 mg | SUBCUTANEOUS | ANDA | 19 sections |
| Mepivacaine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-6730 | INJECTION, SOLUTION | 30 mg | SUBMUCOSAL | ANDA | 20 sections |
| Mepivacaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43128-005 | injection, solution | 30 mg | SUBMUCOSAL | ANDA | 19 sections |
| Polocaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-4517 | INJECTION, SOLUTION | 10 mg | INFILTRATION | ANDA | 22 sections |
| Mepivacaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50227-1080 | INJECTION, SOLUTION | 30 mg | SUBMUCOSAL | ANDA | 20 sections |
| Mepivacaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51004-0005 | injection, solution | 30 mg | SUBMUCOSAL | ANDA | 19 sections |
| Polocaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51004-4411 | INJECTION, SOLUTION | 30 mg | SUBMUCOSAL | ANDA | 20 sections |
| POLOCAINE(R) -MPF (MEPIVACAINE HCI) | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1403 | INJECTION, SOLUTION | 10 mg | EPIDURAL | ANDA | 12 sections |
| POLOCAINE (MEPIVACAINE HCl) | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1534 | INJECTION, SOLUTION | 10 mg | INFILTRATION | ANDA | 12 sections |
| POLOCAINE (MEPIVACAINE HCl) | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1535 | INJECTION, SOLUTION | 20 mg | INFILTRATION | ANDA | 12 sections |
| Polocaine-MPF | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-260 | INJECTION, SOLUTION | 10 mg | EPIDURAL | ANDA | 22 sections |
| Polocaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-283 | INJECTION, SOLUTION | 10 mg | INFILTRATION | ANDA | 22 sections |
| Polocaine-MPF | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-293 | INJECTION, SOLUTION | 15 mg | EPIDURAL | ANDA | 22 sections |
| Polocaine-MPF | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-294 | INJECTION, SOLUTION | 20 mg | EPIDURAL | ANDA | 22 sections |
| Polocaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-296 | INJECTION, SOLUTION | 20 mg | INFILTRATION | ANDA | 22 sections |
| Polocaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66312-441 | INJECTION, SOLUTION | 30 mg | SUBMUCOSAL | ANDA | 20 sections |
| Mepivacaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66467-9760 | INJECTION, SOLUTION | 30 mg | SUBMUCOSAL | ANDA | 20 sections |
| Mepivacaine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66975-406 | INJECTION, SOLUTION | 30 mg | SUBMUCOSAL | ANDA | 20 sections |
| MEPIVACAINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67239-0201 | INJECTION, SOLUTION | 30 mg | SUBMUCOSAL | ANDA | 19 sections |