Tetracaine HCl Local Anesthetic Powder Tetracaine Hydrochloride 202-316-6

Tetracaine HCL

Chemical Names: Tetracaine hydrochloride; Tetracaine HCl; Butethanol; Butylocaine; Anethain
CAS number: 136-47-0;
Molecular Formula: C15H25ClN2O2
Molecular Weight: 300.827 g/mol

Tetracaine (also known as amethocaine) is a local anesthetic of the ester anesthetic group. It is mainly used topically in ophthalmology and as an antipruritic, and it has been used in spinal anesthesia.

In biomedical research, tetracaine is used to alter the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores. Tetracaine is an allosteric blocker of channel function. At low concentrations, tetracaine causes an initial inhibition of spontaneous calcium release events, while at high concentrations, tetracaine blocks release completely.

Tetracaine is the T in TAC, a mixture of 5 to 12% tetracaine, 0.05% adrenaline, and 4 or 10% cocaine hydrochloride used in ear, nose, and throat surgery and in the emergency department where numbing of the surface is needed rapidly, especially when children have been injured in the eye, ear, or other sensitive locations.

 

Pharmacodynamic properties
Tetracaine hydrochloride is used as a local anaesthetic which acts by reversibly blocking the propagation and conduction of nerve impulses along nerve axons. Tetracaine stabilises the nerve membrane, preventing the increase in sodium permeability necessary for the production of an action potential.

Pharmacokinetic properties
Tetracaine is a weak base (pKa 8.5), therefore, significant changes in the rate of ionised lipid soluble drug uptake may occur with changes in the acid base balance.
In vitro studies have shown that tetracaine has a high affinity for melanin, therefore, differences in duration of action may be expected between deeply pigmented eyes and less pigmented eyes.
The primary site of metabolism for tetracaine is the plasma. Pseudocholinesterases in the plasma hydrolyse tetracaine to 4-aminobenzoic acid. Unmetabolised drug is excreted in the urine.

Preclinical safety data
No adverse safety issues were detected during the development of this formulation. The active ingredient is well established in clinical ophthalmology.

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