| Size | Price | Stock | Qty |
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| 1g |
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| 5g |
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| Other Sizes |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Systemic absorption of anaesthetic from the combination cream is directly related to the duration and surface area of application. Although peak plasma concentrations for lidocaine were measured, plasma levels for tetracaine could not be determined due to low levels (<0.9 ng/mL) Tetracaine is rapidly hydrolyzed in the plasma; therefore, volume of distribution could not be determined. Tetracaine is hydrolyzed rapidly in the plasma; therefore, clearance has not been determined. Metabolism / Metabolites Tetracaine is rapidly hydrolyzed by plasma esterases to the following primary metabolites: para-aminobenzoic acid and diethylaminoethanol. The activity of both metabolites is unspecified. Biological Half-Life Tetracaine is hydrolyzed rapidly in the plasma; therefore, half-life has not been determined. |
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No information is available on the use of tetracaine during breastfeeding. Based on the low excretion of other local anesthetics into breastmilk, a single dose of injected tetracaine during breastfeeding, such as for a dental procedure, is unlikely to adversely affect the breastfed infant. However, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. Topical application of tetracaine to the mother is unlikely to affect her breastfed infant if it is applied away from the breast. Only water-miscible cream or gel products should be applied to the breast because ointments may expose the infant to high levels of mineral paraffins via licking.[1] ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. Protein Binding Tetracaine is rapidly hydrolyzed in the plasma; therefore, protein binding could not be determined. |
| Additional Infomation |
Tetracaine is 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. It has a role as a local anaesthetic. It is a benzoate ester and a tertiary amino compound.
Tetracaine is an ester local anaesthetic currently available in combination with lidocaine as a cream and patch. Tetracaine is an Ester Local Anesthetic. The physiologic effect of tetracaine is by means of Local Anesthesia. Tetracaine is a benzoate ester with anesthetic properties. Upon administration, tetracaine reversibly binds voltage-gated sodium ion channels in neuronal cell membranes and inhibits sodium influx. This prevents the initiation and conduction of nerve impulses, and stabilizes neuronal membranes. This results in a loss of sensation, and thereby provides analgesia and anesthesia. A potent local anesthetic of the ester type used for surface and spinal anesthesia. See also: Tetracaine Hydrochloride (has salt form); Lidocaine; Tetracaine (component of); Benzocaine; Lidocaine; Tetracaine (component of) ... View More ... Drug Indication Ophthalmic tetracaine is indicated for the for procedures requiring a rapid and short- acting topical ophthalmic anesthetic. The combination lidocaine and tetracaine patch is indicated for local dermal analgesia for superficial dermatological procedures and superficial venous access. The combination lidocaine and tetracaine cream is intended to provide topical local analgesia for superficial dermatological procedures. FDA Label Mechanism of Action Tetracaine is an ester-type anesthetic and produces local anesthesia by blocking the sodium ion channels involved in the initiation and conduction of neuronal 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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