ATC Group: N01B Anesthetics, local

Articaine is a local anaesthetic of the amide type. Preclinical pharmacodynamic studies show that the mechanism of action of articaine is similar to that of other commonly used anaesthetics.

Benzocaine is a local anaesthetic of the ester type, acting to produce reversible loss of sensation by preventing or diminishing the generation and transmission of sensory nerve impulses near the site of application. Depolarisation of the neuronal membrane and ion exchange are reversibly inhibited.

Bupivacaine is an amide-type, long-acting local anesthetic. Bupivicaine reversibly binds to specific sodium ion channels in the neuronal membrane, resulting in a decrease in the voltage-dependent membrane permeability to sodium ions and membrane stabilization; inhibition of depolarization and nerve impulse conduction; and a reversible loss of sensation.

Capsaicin, or 6-nonenamide, N-[(4-hydroxy-3-methoxyphenyl) methyl]-8-methyl, (6E), is a highly selective agonist for the transient receptor potential vanilloid 1 receptor (TRPV1). The initial effect of capsaicin is the activation of TRPV1-expressing cutaneous nociceptors, which results in pungency and erythema due to the release of vasoactive neuropeptides.

Chloroprocaine is procaine in which one of the hydrogens ortho- to the carboxylic acid group is substituted by chlorine. Chloroprocaine, blocks the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse and by reducing the rate of rise of the action potential. Chloroprocaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine.

Cinchocaine is a local anaesthetic agent and is suitable for surface or spinal anaesthesia and for relaxing sphincteric spasms. It is an anaesthetic of the amide type. It is more toxic than cocaine by local application but its local anaesthetic action is greater so it can be used in lower concentrations. Its action is more prolonged than lignocaine.

Cocaine is a tropane alkaloid with central nervous systems (CNS) stimulating and local anesthetic activity. Cocaine binds to the dopamine, serotonin, and norepinephrine transport proteins and inhibits the re-uptake of dopamine, serotonin, and norepinephrine into pre-synaptic neurons. This leads to an accumulation of the respective neurotransmitters in the synaptic cleft and may result in increased postsynaptic receptor activation. The mechanism of action through which cocaine exerts its local anesthetic effects is by binding to and blocking the voltage-gated sodium channels in the neuronal cell membrane. By stabilizing neuronal membranes, cocaine inhibits the initiation and conduction of nerve impulses and produces a reversible loss of sensation.

Dyclonine effects surface anesthesia when applied topically to mucous membranes.

Chloroethane, commonly known by its old name ethyl chloride, is a chemical compound with chemical formula CH3CH2Cl, once widely used in producing tetraethyllead, a gasoline additive.

Eugenol is an aromatic oil extracted from cloves that is used widely as a flavoring for foods and teas and as an herbal oil used topically to treat toothache and more rarely to be taken orally to treat gastrointestinal and respiratory complaints.

Levobupivacaine is a long acting local anaesthetic and analgesic. It blocks nerve conduction in sensory and motor nerves largely by interacting with voltage sensitive sodium channels on the cell membrane, but also potassium and calcium channels are blocked. In addition, levobupivacaine interferes with impulse transmission and conduction in other tissues where effects on the cardiovascular and central nervous systems are most important for the occurrence of clinical adverse reactions.

Lidocaine, like other local anaesthetics, causes a reversible blockade of impulse propagation along nerve fibres by preventing the inward movement of sodium ions through the nerve membrane. Local anaesthetics of the amide-type are thought to act within the sodium channels of the nerve membrane.

Mepivacaine is an amide local anaesthetic. Mepivacaine has a rapid onset, a high potency of anaesthesia and a low toxicity.

Myrtecaine is a local anaesthetic. It is used to treat muscle strains, tendinitis or ligament sprains and joint pain. It is a surface anaesthetic, adds to the analgesic and anti-inflammatory actions of diethylamine salicylate by facilitating its penetration. Also myrtecaine has a muscle relaxant effect.

Prilocaine is a toluidine derivative and intermediate-acting amino amide with local anesthetic property. Prilocaine binds to the intracellular surface of sodium channels which blocks the subsequent influx of sodium into the cell. Action potential propagation and never function is, therefore, prevented. This block is reversible and when the drug diffuses away from the cell, sodium channel function is restored and nerve propagation returns.

Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation. Procaine is indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine.

Ropivacaine is a long-acting amide-type local anaesthetic with both anaesthetic and analgesic effects. At high doses ropivacaine produces surgical anaesthesia, while at lower doses it produces sensory block with limited and non-progressive motor block.

Tetracaine is a local anaesthetic and is believed to act by blocking nerve conduction mainly by inhibiting sodium ion flux across the axon membrane.