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Purity: ≥98%
Tetracaine HCl (also called Amethocalne; Butylocaine; Curtacain; Decicain; Gingicain; PantocaineM; Intercaine; Leocaine; Menonasal; Niphanoid), the hydrochloride salt form of tetracaine, is a local anaesthetic and a channel function allosteric inhibitor. Tetracaine is used as a local anesthetic to numb the throat, nose, or eyes. It can also be applied topically to reduce pain before beginning an intravenous. Tetracaine works by preventing the sarcoplasmic reticulum's voltage-sensitive Ca2+ release. Additionally, tetracaine inhibits both Na+ CP types IV α and X α.
| Targets |
Calcium channel
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| ln Vitro |
Tetracaine hydrochloride (Amethocaine hydrochloride) is applied to modify the activity of ryanodine receptors, or calcium release channels, which regulate the release of calcium from intracellular reserves. Tetracaine hydrochloride inhibits channel function allosterically. Tetracaine inhibits spontaneous calcium release events initially at low concentrations and completely blocks release at high concentrations[1][2].
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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. |
| 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. |
| References | |
| 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. |
| Molecular Formula |
C15H25CLN2O2
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| Molecular Weight |
300.82
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| Exact Mass |
300.16
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| Elemental Analysis |
C, 59.89; H, 8.38; Cl, 11.78; N, 9.31; O, 10.64
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| CAS # |
136-47-0
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| Related CAS # |
Tetracaine; 94-24-6
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| PubChem CID |
5411
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| Appearance |
White to off-white solid powder
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| Boiling Point |
389.4ºC at 760 mmHg
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| Melting Point |
149°C
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| Flash Point |
189.3ºC
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| Vapour Pressure |
2.87E-06mmHg at 25°C
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| LogP |
3.492
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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 |
Cl[H].O(C(C1C([H])=C([H])C(=C([H])C=1[H])N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O)C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
PPWHTZKZQNXVAE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H24N2O2.ClH/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;1H
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| Chemical Name |
2-(dimethylamino)ethyl 4-(butylamino)benzoate;hydrochloride
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| Synonyms |
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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 Note: (1). This product is not stable in solution, please use freshly prepared working solution for optimal results. (2). Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3242 mL | 16.6212 mL | 33.2425 mL | |
| 5 mM | 0.6648 mL | 3.3242 mL | 6.6485 mL | |
| 10 mM | 0.3324 mL | 1.6621 mL | 3.3242 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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 | May 2016 | Not Applicable |
| NCT01304316 | Completed | Drug: Tetracaine HCl 3% and Oxymetazoline HCl 0.05% |
Anesthesia | St. Renatus, LLC | September 2010 | Phase 2 |
| NCT01710787 | Completed | Drug: Tetracaine HCl 3% Drug: Placebo |
Anesthesia | St. Renatus, LLC | October 2012 | Phase 3 |
| NCT01807624 | Completed | Drug: Tetracaine HCl 3% and Oxymetazoline HCl 0.05% |
Anesthesia | St. Renatus, LLC | March 2013 | Phase 2 |
| NCT01952990 | Completed | Drug: Tetracaine HCl 3% and Oxymetazoline HCl 0.05% |
Anesthesia | St. Renatus, LLC | September 2013 | Phase 2 |
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