Tetracaine targets voltage-gated sodium channels (Nav channels) in neuronal cell membranes. It reversibly binds to these channels, inhibiting sodium influx. This inhibition prevents the initiation and conduction of nerve impulses, and stabilizes neuronal membranes. Tetracaine also alters the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores. It blocks voltage-sensitive release of Ca2+ from sarcoplasmic reticulum. By blocking sodium channels, tetracaine provides local anesthesia.

In vitro, Tetracaine is used as a research tool for studying excitation-contraction (E-C) coupling in skeletal and cardiac muscle. It is also used for studying the impact of drugs on tumor-necrosis-factor (TNF)-mediated cytotoxicity and TNF-induced arachidonic acid release. Tetracaine's effects on sodium channels and calcium release channels can be studied using electrophysiological techniques. It is a potent local anesthetic that blocks nerve conduction in a concentration-dependent manner.

In vivo, Tetracaine is used clinically as a local anesthetic. It is applied topically to mucous membranes for minor operations in the mouth or nose. It is used as a topical ophthalmic anesthetic and for spinal anesthesia. Tetracaine provides rapid and effective local anesthesia by blocking nerve impulse conduction. Its effects are reversible and localized to the site of application. Tetracaine is an approved drug for these indications.

In vitro assays for Tetracaine measure its effects on voltage-gated sodium channels and calcium release channels. Electrophysiological techniques, such as patch-clamp, are used to measure sodium currents in neurons or cells expressing Nav channels. Tetracaine is applied, and the inhibition of sodium currents is measured. The IC50 is determined from dose-response curves. Ryanodine receptor binding assays can be performed to study Tetracaine's effects on calcium release. These assays confirm the compound's mechanism of action.

In vitro cell-based assays for Tetracaine are used to study its effects on neuronal excitability and calcium signaling. Neuronal cultures or cell lines are treated with Tetracaine, and the inhibition of action potentials is measured using multi-electrode arrays or patch-clamp. Intracellular calcium levels can be measured using fluorescent dyes to assess the compound's effects on calcium release. Cell viability assays are used to assess cytotoxicity. These assays confirm the compound's local anesthetic activity.

In vivo animal experiments for Tetracaine are conducted in animal models of pain and anesthesia. In a typical study, Tetracaine is administered topically or by injection, and the loss of sensation is assessed using behavioral tests, such as the tail-flick or hot-plate test. The compound's duration of action and potency are compared to other local anesthetics. These studies confirm the in vivo efficacy of Tetracaine as a local anesthetic.

Absorption, Distribution and Excretion
Systemic absorption of anesthetics in compound creams is directly related to the time and area of administration. Although the peak plasma concentration of lidocaine was determined, the plasma concentration of tetracaine was too low (<0.9 ng/mL) to be determined. Tetracaine is rapidly hydrolyzed in plasma; therefore, its volume of distribution could not be determined. Tetracaine is rapidly hydrolyzed in plasma; therefore, its clearance has not been determined. Metabolisms/Metabolites Tetracaine is rapidly hydrolyzed in plasma by esterases to the following major metabolites: para-aminobenzoic acid and diethylaminoethanol. The activities of these two metabolites have not been determined. Biological Half-Life Tetracaine is rapidly hydrolyzed in plasma; therefore, its half-life has not been determined.

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Tetracaine has a molecular weight of 264.36 g/mol and a molecular formula of C15H24N2O2. It has a CAS registry number of 94-24-6 and an FDA UNII Code of 0619F35CGV. It is a solid compound. It is soluble in water and organic solvents. For storage, it is recommended to keep the compound at room temperature. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been characterized in the context of its clinical use. Tetracaine is rapidly metabolized by plasma esterases.

Effects During Pregnancy and Lactation
◉ Overview of medication use during lactation There is currently no information available regarding the use of tetracaine during lactation. Given the low levels of other local anesthetics in breast milk, a single injection of tetracaine during lactation (e.g., for dental procedures) is unlikely to have adverse effects on a breastfed infant. However, other medications may be preferred, especially in newborns or preterm infants. If tetracaine is applied to areas away from the breast, it is unlikely to affect the breastfed infant. Only water-soluble creams or gels should be applied to the breast, as ointments may expose the infant to high concentrations of mineral oil through licking. [1] ◉ Effects on breastfed infants No relevant published information was found as of the revision date. ◉ Effects on lactation and breast milk No relevant published information was found as of the revision date.

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Protein binding
Tetracaine is rapidly hydrolyzed in plasma; therefore, protein binding cannot be determined.

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Tetracaine is an approved drug and its safety profile has been established. Common side effects include local irritation, allergic reactions, and systemic toxicity if absorbed in large amounts. As a sodium channel blocker, it can cause cardiac and neurological effects at high doses. It should be used with caution in patients with hypersensitivity to ester-type local anesthetics. For research use, standard laboratory safety precautions should be followed when handling Tetracaine.

Tetracaine is a benzoic acid ester formed by the combination of 4-n-butylbenzoic acid and 2-(dimethylamino)ethanol; it is a local ester anesthetic (tetracaine) used for surface and spinal anesthesia. It is a local anesthetic. It is a benzoic acid ester and tertiary amine compound. Tetracaine is an ester-based local anesthetic, currently used in combination with lidocaine in the form of creams and patches. Tetracaine is an ester-based local anesthetic. The physiological effect of tetracaine is achieved through local anesthesia. Tetracaine is a benzoic acid ester with anesthetic properties. After administration, tetracaine reversibly binds to voltage-gated sodium ion channels on the neuronal cell membrane, inhibiting sodium ion influx. This prevents the generation and conduction of nerve impulses and stabilizes the neuronal cell membrane. This leads to loss of sensation, thereby achieving analgesia and anesthesia. A potent ester-based local anesthetic used for surface and spinal anesthesia. See also: Tetracaine Hydrochloride (in salt form); Lidocaine; Tetracaine (ingredient); Benzocaine; Lidocaine; Tetracaine (ingredient)... See more...

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Drug Indications
Ophthalmic Tetracaine is indicated for surgical procedures requiring rapid, short-acting local ocular anesthesia. Lidocaine and Tetracaine Combination Patch is indicated for local analgesia in superficial dermatological procedures and superficial venous punctures. Lidocaine and Tetracaine Combination Cream is intended to provide local analgesia for superficial dermatological procedures.
FDA Label

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Mechanism of Action
Tetracaine is an ester anesthetic that produces local anesthesia by blocking sodium ion channels involved in the initiation and conduction of nerve impulses.

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Tetracaine is an approved drug used as a topical local anesthetic. It is a benzoate ester that reversibly binds voltage-gated sodium ion channels in neuronal cell membranes, inhibiting sodium influx. This prevents the initiation and conduction of nerve impulses, resulting in a loss of sensation. Tetracaine is used as a topical ophthalmic anesthetic and for spinal anesthesia, and as a surface anesthetic of mucous membranes. It is also used as a research tool for studying E-C coupling and TNF-mediated cytotoxicity.

264.183

94-24-6

Tetracaine hydrochloride;136-47-0

5411

White to off-white solid powder

1.0±0.1 g/cm3

389.4±27.0 °C at 760 mmHg

43 °C

189.3±23.7 °C

0.0±0.9 mmHg at 25°C

1.538

3.65

1

4

9

19

249

0

O=C(C1C=CC(NCCCC)=CC=1)OCCN(C)C

GKCBAIGFKIBETG-UHFFFAOYSA-N

InChI=1S/C15H24N2O2/c1-4-5-10-16-14-8-6-13(7-9-14)15(18)19-12-11-17(2)3/h6-9,16H,4-5,10-12H2,1-3H3

2-(dimethylamino)ethyl 4-(butylamino)benzoate

Tetracaine Pontocaine Amethocaine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 43 mg/mL (~162.66 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (9.46 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (9.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)