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Tetracaine

S01H - Local anesthetics ATC S01HA03 Small molecule approved 2005 Topical First-in-class Natural product

JFDA label: Minims Tetracaine Hcl 0.5%

Mechanism of Action

Blocker of Sodium channel alpha subunit — Sodium channel alpha subunit blocker

TargetActionGene / class
Sodium channel alpha subunit efficacy BLOCKER

Indications

Approved

  • Hemorrhoids — hemorrhoid
  • Pain — pain
  • Pruritus — Pruritus

Off-label

  • Carpal Tunnel Syndrome
  • Cataract
  • Myofascial Pain Syndromes
  • Neuralgia, Postherpetic
  • Shoulder Impingement Syndrome
  • Skin Diseases
  • Tendinopathy
  • Wounds and Injuries

Contraindications

Source: openFDA

  • Spinal anesthesia with tetracaine hydrochloride is contraindicated in patients with known hypersensitivity to tetracaine hydrochloride or to drugs of a similar chemical configuration (ester-type local anesthetics), or aminobenzoic acid or its derivatives; and in patients for whom spinal anesthesia as a technique is contraindicated. The decision as to whether or not spinal anesthesia should be used for an individual patient should be made by the physician after weighing the advantages with the risks and possible complications. Contraindications to spinal anesthesia as a technique can be found in standard reference texts, and usually include generalized septicemia, infection at the site of injection, certain diseases of the cerebrospinal system, uncontrolled hypotension, etc. Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Cardiac disorders (1)

Not Known Cardiac arrest

Vascular disorders (1)

Not Known Hypotension

Nervous system disorders (6)

Not Known Convulsion · Dizziness · Loss of consciousness · Paralysis · Somnolence · Tremor

Immune system disorders (2)

Not Known Anaphylactic shock · Hypersensitivity

Gastrointestinal disorders (2)

Not Known Nausea · Vomiting

Skin and subcutaneous tissue disorders (1)

Not Known Urticaria

Psychiatric disorders (1)

Not Known Agitation

Eye disorders (1)

Not Known Vision blurred

Ear and labyrinth disorders (1)

Not Known Tinnitus

General disorders and administration site conditions (14)

Not Known Arachnoiditis · Chills · Conjunctival hyperaemia · Corneal oedema · Iritis · Keratitis · Meningism · Necrosis · Nervousness · Oedema · Pain · Post lumbar puncture syndrome · Tension · Vasodilation procedure

Dosing

Source: openFDA

Dosage and Administration As with all anesthetics, the dosage varies and depends upon the area to be anesthetized, the number of neuronal segments to be blocked, individual tolerance, and the technique of anesthesia. The lowest dosage needed to provide effective anesthesia should be administered. For specific techniques and procedures, refer to standard textbooks. Suggested Dosage for Spinal Anesthesia Using 1% Tetracaine HCl Injection, USP Extent of Anesthesia Dose of solution (mL) Volume of spinal fluid (mL) Site of injection (lumbar interspace) Perineum 0.5 (= 5 mg)* 0.5 4 th Perineum and lower extremities 1.0 (= 10 mg) 1.0 3 rd or 4 th Up to costal margin(= 15 mg to 20 mg)** 1.5 to 2.0 1.5 to 2.0 2 nd , 3 rd , or 4 th * For vaginal delivery (saddle block), from 2 mg to 5 mg in dextrose. **Doses exceeding 15 mg are rarely required and should be used only in exceptional cases. Inject solution at rate of about 1 mL per 5 seconds. The extent and degree of spinal anesthesia depend upon dosage, specific gravity of the anesthetic solution, volume of solution used, force of the injection, level of puncture, position of the patient during and immediately after injection, etc. When spinal fluid is added to 1% tetracaine hydrochloride injection, some turbidity results, the degree depending on the pH of the spinal fluid, the temperature of the solution during mixing, as well as the amount of drug and diluent employed. Liberation of base (which is completed within the spinal canal) is held to be essential for satisfactory results with any spinal anesthetic. The specific gravity of spinal fluid at 25°C/25°C varies under normal conditions from 1.0063 to 1.0075. The 1% concentration in saline solution has a specific gravity of 1.0060 to 1.0074 at 25°C/25°C. A hyperbaric solution may be prepared by mixing equal volumes of the 1% solution and Dextrose Solution 10%. Examine vials carefully before use. Do not use solution if crystals, cloudiness, or discoloration is observed. This formulation of tetracaine hydrochloride does not contain antimicrobial or bacteriostatic agents; therefore, unused portions should be discarded. Sterilization of Vials The tetracaine hydrochloride injection is sterile within an undamaged vial. To destroy bacteria on the exterior of vials use heat sterilization (autoclaving) before opening. Immersion in antiseptic solution is not recommended. Autoclave at 15-pounds pressure, at 121°C (250°F), for 15 minutes. Autoclaving increases likelihood of crystal formation. Unused autoclaved vials should be discarded. Under no circumstances should unused vials which have been autoclaved be returned to stock .

Warnings & Precautions

Source: openFDA

Warnings & Precautions

USED. Large doses of local anesthetics should not be used in patients with heartblock. Reactions resulting in fatality have occurred on rare occasions with the use of local anesthetics, even in the absence of a history of hypersensitivity. Methemoglobinemia Cases of methemoglobinemia have been reported in association with local anesthetic use. Although all patients are at risk for methemoglobinemia, patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition. If local anesthetics must be used in these patients, close monitoring for symptoms and signs of methemoglobinemia is recommended. Signs and symptoms of methemoglobinemia may occur immediately or may be delayed some hours after exposure and are characterized by a cyanotic skin discoloration and abnormal coloration of the blood. Methemoglobin levels may continue to rise; therefore, immediate treatment is required to avert more serious central nervous system and cardiovascular adverse effects, including seizures, coma, arrhythmias, and death. Discontinue tetracaine hydrochloride and any other oxidizing agents. Depending on the severity of the symptoms, patients may respond to supportive care, i.e., oxygen therapy, hydration. More severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.

Pregnancy & Lactation

Pregnancy

Lactation

Probably Compatible Hale L2

However, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.

Chemistry & Properties

2D structure
FormulaC15H24N2O2
Molecular weight264.37 g/mol
IUPAC name2-(dimethylamino)ethyl 4-(butylamino)benzoate
CAS94-24-6
PubChem CID5411
InChIKeyGKCBAIGFKIBETG-UHFFFAOYSA-N
logP2.62 (XLogP 3.7)
Polar surface area41.57 Ų
H-bond acceptors / donors4 / 1
Drug-likeness (QED)0.58
Lipinski violations0
SMILESCCCCNc1ccc(C(=O)OCCN(C)C)cc1

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability70.0%
Half-life0.782 h
Volume of distribution5.315 L/kg
Protein binding78.7%
BBB penetrantYes

Enzyme interactions

EnzymeRoleDetail
CYP1A2Substrate
CYP2B6Inhibitor
CYP2C19Substrate

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MDR1 (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (32, DDInter)

Interacting drugSeverityManagement
Bupivacaine (liposome) major
Nitrous acid major
Alprazolam moderate
Benzocaine (topical) moderate
Chlordiazepoxide moderate
Cinchocaine (topical) moderate
Clobazam moderate
Clonazepam moderate
Clorazepic acid moderate
Cocaine (nasal) moderate
Cocaine (topical) moderate
Diazepam moderate
Estazolam moderate
Flurazepam moderate
Halazepam moderate
Lidocaine (ophthalmic) moderate
Lidocaine (topical) moderate
Lorazepam moderate
Midazolam moderate
Oxazepam moderate
Oxybuprocaine (ophthalmic) moderate
Proparacaine (ophthalmic) moderate
Quazepam moderate
Remimazolam moderate
Sulfadiazine moderate
Sulfadoxine moderate
Sulfamethoxazole moderate
Sulfasalazine moderate
Temazepam moderate
Tilmanocept moderate
Triazolam moderate
Hyaluronidase minor

Registered Products (3)

BrandForm / strengthPackAgentCitizen (JOD)
Atracaine Solution 0.5 % 15 ml Amman Pharmaceutical Indusries
Minims Tetracaine Hcl Solution 0.5 % 0.5 ml Petra Drug Store
Minims TetracaineHcl 1% e/d Ophthalmic Solution 1 % 0.5 ml Petra Drug Store