Local anesthetics

Local anesthetics are drugs that can inhibit the generation and conduction of nerve impulses in local medications. The chemical structure of these drugs and local anesthetic effects are closely related. The chemical structure must have three components:
①aromatic ring;
② the middle part, some are ester type (such as procaine), and some are amide type (such as lidocaine);
③ amine part, most  are tertiary amine, a few are amine.
The effects of local anesthetic on the nerve fiber tracts are first to inhibit the impulse conduction of sensory nerve, and then to inhibit the motor nerve, and its role is reversible.It causes a loss of sensation first to affect pain, followed by temperature sensation, and finally for the sense of touch and pressure.The effect of local anesthetic arises by drugs preventing sodium ion influx, making the nerve cell membrane cannot produce depolarization, blocking the generation of action potential and the conduction of nerve impulse. Local anesthetics act as a dissociative type on the inner side of the membrane. Since they are organic bases, they are high in the alkaline environment, and have a strong ability to pass through the cell membrane to the inside of the membrane. On the other hand, in an acidic environment ( e.g. in inflammatory conditions), their ability to pass through the membrane is poorer and the potency of local anesthesia diminishes. Local anesthetic effect mechanism is inconclusive. At present, it is believed that it may compete with calcium ions for phospholipids in the nerve cell membrane to form a more solid local complex which contains anesthetics and phospholipids, and prevent phospholipids from carrying sodium ions, thus hamper sodium ion influx.
The absorbed local anesthetic will produce excitatory effects and inhibition of the cardiovascular system on the central nervous system. The former showed convulsions, and then lead to bulbar paralysis, respiratory failure; the latter showed myocardial inhibition and vasodilation, severe cases of cardiovascular collapse and death. Therefore, when applying local anesthetics, we should prevent or reduce drug absorption into the blood.
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Structure Chemical Name CAS MF
Benzocaine Benzocaine 94-09-7 C9H11NO2
Benzocaine hydrochloride Benzocaine hydrochloride 23239-88-5 C9H11NO2.ClH
Tetracaine hydrochloride Tetracaine hydrochloride 136-47-0 C15H25ClN2O2
Ropivacaine mesylate Ropivacaine mesylate 854056-07-8 C18H30N2O4S
Benzyl alcohol Benzyl alcohol 100-51-6 C7H8O
Procaine hydrochloride Procaine hydrochloride 51-05-8 C13H21ClN2O2
Lidocaine Lidocaine 137-58-6 C14H22N2O
Ropivacaine hydrochloride Ropivacaine hydrochloride 132112-35-7 C17H26N2O.ClH.H2O
Bupivacaine hydrochloride Bupivacaine hydrochloride 14252-80-3 C18H28N2O.ClH
Propitocaine hydrochloride Propitocaine hydrochloride 1786-81-8 C13H21ClN2O
Proparacaine hydrochloride Proparacaine hydrochloride 5875-06-9 C16H27ClN2O3
Dyclonine hydrochloride Dyclonine hydrochloride 536-43-6 C18H28ClNO2
Lidocaine hydrochloride Lidocaine hydrochloride 73-78-9 C14H23ClN2O
Tetracaine Tetracaine 94-24-6 C15H24N2O2
Mepivacaine hydrochloride Mepivacaine hydrochloride 1722-62-9 C15H22N2O.ClH
Dibucaine hydrochloride Dibucaine hydrochloride 61-12-1 C20H30ClN3O2
Linocaine hydrochloride Linocaine hydrochloride 6108-05-0 C14H25ClN2O2
Ropivacaine Ropivacaine 84057-95-4 C17H26N2O
Elucaine Elucaine 25314-87-8 C19H23NO2
Cinchocaine Cinchocaine 85-79-0 C20H29N3O2
Trimecaine Trimecaine 616-68-2 C15H24N2O
Pribecaine Pribecaine 55837-22-4
Chloroprocaine hydrochloride Chloroprocaine hydrochloride 3858-89-7 C13H20Cl2N2O2
PROPARACAINE PROPARACAINE 298-50-0 C16H26N2O3
Ropivacaine hydrochloride Ropivacaine hydrochloride 98717-15-8 C17H27ClN2O
Oxybuprocaine Oxybuprocaine 99-43-4 C17H28N2O3
Bupivacaine Hydrochloride Bupivacaine Hydrochloride 73360-54-0 C18H31ClN2O2
Bupivacaine Bupivacaine 2180-92-9 C18H28N2O
DYCLONINE DYCLONINE 586-60-7 C18H27NO2
proxymetacaine proxymetacaine 499-67-2 C16H26N2O3
axybuprocaine hydrochloride axybuprocaine hydrochloride
CHLOROETHANE CHLOROETHANE 75-00-3 C2H5Cl
propoxycaine propoxycaine 86-43-1 C16H26N2O3
Prilocaine Prilocaine 721-50-6 C13H20N2O
Mepivacaine Mepivacaine 22801-44-1 C15H22N2O
Etidocaine Etidocaine 36637-18-0 C17H28N2O
PROCAINE PROCAINE 59-46-1 C13H20N2O2
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