Effects of local anesthetics on contractions of pregnant and non-pregnant rat myometrium in vitro. 2014

Jin-Song Wei, and Zhe-Bin Jin, and Zhi-Qiang Yin, and Qiang-Min Xie, and Ji-Qiang Chen, and Zi-Gang Li, and Hui-Fang Tang
Chinese Medicine Hospital of Jingshan County Department of Medicine Hubei, Jinshan China.

In order to determine whether local anesthetics directly affect the propagation and strength of myometrial contractions, we compared the effects of bupivacaine, ropivacaine, lidocaine and tetracaine on the contractions of myometrium isolated from pregnant and non-pregnant rats. Full-thickness myometrial strips were obtained from 18- to 21-day pregnant and non-pregnant Sprague-Dawley rats and incubated in an organ bath. When spontaneous contractions became regular, strips were exposed to cumulative concentrations of the four local anesthetics ranging from 0.01 to 300 μmol/L and the amplitude and frequency of contraction were recorded. All four compounds caused a concentration-dependent inhibition of the contractility of pregnant and non-pregnant uterine muscle. In pregnant myometrium, the concentration that caused 50% inhibition (IC(50)) was 100 μmol/L for bupivacaine, 157 μmol/L for ropivacaine, > 1000 μmol/L for lidocaine, and 26.3 μmol/L for tetracaine. In non-pregnant myometrium, the IC(50) was 26.9 μmol/L for bupivacaine, 40 μmol/L for ropivacaine, 384 μmol/L for lidocaine, and 7.4 μmol/L for tetracaine. These results suggested that local anesthetics do inhibit myometrial contractions in pregnant and non-pregnant rats in a concentration-dependent manner.

UI MeSH Term Description Entries
D008012 Lidocaine 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. Lignocaine,2-(Diethylamino)-N-(2,6-Dimethylphenyl)Acetamide,2-2EtN-2MePhAcN,Dalcaine,Lidocaine Carbonate,Lidocaine Carbonate (2:1),Lidocaine Hydrocarbonate,Lidocaine Hydrochloride,Lidocaine Monoacetate,Lidocaine Monohydrochloride,Lidocaine Monohydrochloride, Monohydrate,Lidocaine Sulfate (1:1),Octocaine,Xylesthesin,Xylocaine,Xylocitin,Xyloneural
D011247 Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH. Gestation,Pregnancies
D002045 Bupivacaine A widely used local anesthetic agent. 1-Butyl-N-(2,6-dimethylphenyl)-2-piperidinecarboxamide,Bupivacain Janapharm,Bupivacain-RPR,Bupivacaina Braun,Bupivacaine Anhydrous,Bupivacaine Carbonate,Bupivacaine Hydrochloride,Bupivacaine Monohydrochloride, Monohydrate,Buvacaina,Carbostesin,Dolanaest,Marcain,Marcaine,Sensorcaine,Svedocain Sin Vasoconstr,Bupivacain RPR
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D005260 Female Females
D000077212 Ropivacaine An anilide used as a long-acting local anesthetic. It has a differential blocking effect on sensory and motor neurons. 1-Propyl-2',6'-pipecoloxylidide,AL 381,AL-381,LEA 103,LEA-103,Naropeine,Naropin,Ropivacaine Hydrochloride,Ropivacaine Monohydrochloride,Ropivacaine Monohydrochloride, (S)-isomer,1 Propyl 2',6' pipecoloxylidide,AL381,LEA103
D000577 Amides Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed) Amide
D000779 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. Anesthetics, Conduction-Blocking,Conduction-Blocking Anesthetics,Local Anesthetic,Anesthetics, Topical,Anesthetic, Local,Anesthetics, Conduction Blocking,Conduction Blocking Anesthetics,Local Anesthetics,Topical Anesthetics
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013748 Tetracaine A potent local anesthetic of the ester type used for surface and spinal anesthesia. Tetrakain,Amethocaine,Ametop,Dicaine,Pantocaine,Pontocaine,Tetracaine Monohydrochloride,Tetrracaine Hydrochloride,Hydrochloride, Tetrracaine

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