Тетракаин

Химические свойства

White or light-yellow, waxy solid. Very slightly soluble in water; soluble in alcohol, ether, benzene, chloroform.

Использование

Tetracaine has been used as an anesthetic and to lower the glucose synthesis in upper small intestinal infusions. It has also been used to inhibit ryanodine receptors (RyRs) in rats.

Определение

ChEBI: A benzoate ester in which 4-N-butylbenzoic acid and 2-(dimethylamino)ethanol have combined to form the ester bond; a local ester anaesthetic (ester caine) used for surface and spinal anaesthesia.

Биологические функции

Tetracaine hydrochloride (Pontocaine) is an ester of PABA that is an effective topical local anesthetic agent and also is quite commonly used for spinal (subarachnoid) anesthesia. Epinephrine is frequently added to prolong the anesthesia.Tetracaine is considerably more potent and more toxic than procaine and cocaine. It has approximately a 5-minute onset and 2 to 3 hours of action.

Общее описание

Tetracaine was developed to address the low potency andshort duration of action of procaine and chloroprocaine. The addition of the butyl side chain on the para nitrogen increasesthe lipid solubility of the drug and enhances the topical potencyof tetracaine. The plasma half-life is 120 to 150 seconds.Topically applied tetracaine to unbroken skin requires 30 to 45minutes to confer topical anesthesia. Tetracaine 4% gel is superiorthan eutectic mixture with lidocaine (EMLA) (an emulsionof lidocaine and prilocaine) in preventing pain associatedwith needle procedures in children. Tetracaine metabolism issimilar to procaine ester metabolism yielding parabutylaminobenzoicacid and dimethylaminoethanol and conjugatesexcreted in the urine. The pKa of the dimethylated nitrogen is8.4 and tetracaine is formulated as a hydrochloride salt with apH of 3.5 to 6.0. The increased absorption from topical siteshas resulted in reported toxicity. Overdoses of tetracaine mayproduce central nervous system (CNS) toxicity and seizure activitywith fatalities from circulatory depression reported.No selective cardiac toxicity is seen with tetracaine althoughhypotension has been reported. Tetracaine is employed for infiltrationanesthesia, spinal anesthesia, or topical use.