| Size | Price | Stock | Qty |
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| 1g |
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| 5g |
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| Other Sizes |
| ADME/Pharmacokinetics |
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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| Toxicity/Toxicokinetics |
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. Protein binding Tetracaine is rapidly hydrolyzed in plasma; therefore, protein binding cannot be determined. |
| Additional Infomation |
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...
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 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. |
| Exact Mass |
264.183
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|---|---|
| CAS # |
94-24-6
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| Related CAS # |
Tetracaine hydrochloride;136-47-0
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| PubChem CID |
5411
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
389.4±27.0 °C at 760 mmHg
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| Melting Point |
43 °C
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| Flash Point |
189.3±23.7 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.538
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| LogP |
3.65
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
19
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| Complexity |
249
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=CC(NCCCC)=CC=1)OCCN(C)C
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| InChi Key |
GKCBAIGFKIBETG-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
2-(dimethylamino)ethyl 4-(butylamino)benzoate
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| Synonyms |
Tetracaine Pontocaine Amethocaine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 43 mg/mL (~162.66 mM)
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|---|---|
| Solubility (In Vivo) |
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. 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. View More
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. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02863679 | COMPLETED | Drug: Tetracaine hydrochloride gel | Hysteroscopy | Wenzhou Medical University | 2016-05 | Not Applicable |
| NCT03749915 | UNKNOWN STATUS | Device: Pain Ease Cold Spray Drug: Ametop |
Analgesia Topical Anesthetic |
University of British Columbia | 2018-11-20 | Not Applicable |
| NCT02750137 | COMPLETED | Drug: Tetracaine | Adverse Drug Event | KK Women's and Children's Hospital | 2014-08 | |
| NCT02771392 | UNKNOWN STATUS | Drug: Ophthalmic Tetracaine Other: Normal Saline |
Corneal Abrasion | New York Presbyterian Brooklyn Methodist Hospital | 2016-06 | Phase 2 Phase 3 |
| NCT01864213 | COMPLETED | Drug: Ametop cream | Pain | University of British Columbia | 2013-05 | Phase 1 |
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