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Tetracaine powder is the shape of tetracaine in the laboratory,The researchers determined its accurate chemistry. The relevant information is as follows. it is a white to light yellow crystalline powder with the molecular formula C15H24N2O2 and a molecular weight of 264.36. It is usually stable at room temperature, but may decompose under extreme conditions such as high temperature or strong light irradiation. The melting point is between 149 ° C and 153 ° C. Its melting point is high enough to ensure its stability under common usage conditions. In addition, the high melting point makes Tetracaine easier to store. The boiling point is relatively high, at 490.74 ° C. This means that high-temperature conditions can be used during the preparation or separation process to remove pollutants.
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CF |
C15H24N2O2 |
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EM |
264 |
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MW |
264 |
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m/z |
264 (100.0%), 265 (16.2%), 266 (1.2%) |
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EA |
C, 68.15; H, 9.15; N, 10.60; O, 12.10. |
chemical property
Stability:
Tetracaine powder is relatively stable at room temperature, but easily decomposes under conditions such as high temperature, strong acid, and strong alkali.
Solubility:
Tetracaine can dissolve in solvents such as water, ethanol, ether, and acetone, but is not easily soluble in organic solvents such as petroleum ether, benzene, and dichloromethane.
Acidity and alkalinity:
Tetracaine is a weakly alkaline substance with a pKa value of approximately 8.5.
Oxidation-reduction properties:
Tetracaine molecules have carbonyl and aromatic ring structures, which can undergo oxidation-reduction reactions.
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Tetracaine powder has been used for various purposes since the 1930s, but currently the most common use is as a local anesthetic for short-term surgeries on ophthalmic surfaces, such as eye, ear, and nose surgeries. In addition, it is also used for spinal anesthesia. The World Health Organization (WHO) lists it as an essential drug and compared to other local anesthetics, its price is relatively cheap.
1.Mechanism of Action
It mainly works by blocking intracellular sodium channels. The drug passes through the lipid bilayer in a non ionized form and dissociates into an ionized form (cation/conjugated acid), which then acts on the alpha subunit of the sodium channel. When specific neural Na/K channels are used, drugs act as allosteric inhibitors of sodium channels, binding and activating more quickly. This blockade must occur on three consecutive nodes of the axon to block nerve conduction. During this process, sodium influx was prevented, thereby preventing cell depolarization and the development of any potential action potentials.
2.Administration method
Its pKa value is 8.46 (at room temperature of 25 degrees Celsius), which is moderate, although the drug has a relatively fast onset, especially for spinal cord administration. Tetracaine has high lipid solubility, with a relative value of 80, making it one of the strongest local anesthetics. Its protein binding rate is moderate, at 75%, allowing for a relative action duration of up to 200 minutes. Drugs are mainly hydrolyzed by plasma acetylcholinesterase (but acetylcholinesterase) to produce alcohol and p-aminobenzoic acid (PABA). A small portion is metabolized through red blood cell cholinesterase. Only a very small amount of unmetabolized tetracaine is excreted in the urine. Its pH value is 4.5 to 6.5.
3.The Influence of Eyes
Corneal injury
Not suitable for injection or intraocular use. Using it may cause damage to corneal endothelial cells.
Corneal toxicity
Long term use or abuse may lead to corneal epithelial toxicity and may manifest as epithelial defects, which may develop into permanent corneal damage.
Corneal damage caused by loss of sensation
Patients should not touch their eyes for at least 10-20 minutes after using anesthesia, as accidental injury may occur due to loss of eye sensation.
4.Excessive use
Long term use of local eye anesthetics, including it, may lead to permanent corneal opacities and ulcers, accompanied by visual loss.
Substitute
Lidocaine
Lidocaine is a commonly used local anesthetic with the characteristics of rapid onset, strong blockade, and rapid recovery, suitable for spinal anesthesia. In some cases, lidocaine is used as a substitute for it, especially in outpatient surgeries.
Bupivacaine
Bupivacaine is a long-acting local anesthetic with a lower risk of transient neurological symptoms (TNS) after spinal anesthesia compared to lidocaine.
Levobupivacaine
As a purified isomer of bupivacaine, levobupivacaine is also used for local anesthesia and has a lower risk of TNS compared to lidocaine.
Prilocaine
Propavacaine is another local anesthetic that reduces the risk of TNS compared to lidocaine.
Procaine
Procaine is a local anesthetic with a lower risk of TNS compared to lidocaine.
Ropivacaine
Ropivacaine is another long-acting local anesthetic with a lower risk of TNS compared to lidocaine.
2-Chloroprocaine
2-chloroprocaine is a rapidly acting local anesthetic with no significant difference in the risk of TNS compared to lidocaine.
Mepivacaine
Mexicaine is another local anesthetic, and there is no significant difference in the risk of TNS compared to lidocaine.
Safety and Danger
1.Toxicity intensity
- The toxicity of this substance is 10 times higher than that of procaine, and its pharmacological strength is also about 10 times that of procaine.
- The incidence of toxic reactions is also higher than that of procaine, often caused by high doses, rapid absorption, or improper handling, such as accidental injection into blood vessels resulting in high blood drug concentrations.
2.Toxicity performance
- Central nervous system toxicity: When its concentration is too high or it is used for too long, it is easy to enter the central nervous system through the blood-brain barrier, causing toxic reactions. When there is mild overdose or mild poisoning, patients may exhibit symptoms such as irritability, multilingualism, numbness at the base of the tongue, and nystagmus. As toxicity worsens, patients may experience symptoms such as dizziness, vertigo, chills, tremors, panic, and in severe cases, seizures, coma, respiratory failure, and decreased blood pressure.
- Cardiovascular toxicity: It may affect the normal electrophysiological activity of the heart by interfering with sodium ion channels on the myocardial cell membrane. In the early stages, patients may exhibit increased heart rate and blood pressure. As toxicity progresses, bradycardia, decreased blood pressure, respiratory depression, and severe arrhythmias such as premature ventricular contractions, frequent premature ventricular contractions, and ventricular fibrillation may occur.
- Allergic reactions: During use, some patients may experience allergic reactions such as hives, difficulty breathing, and other symptoms. Severe allergic reactions may even lead to sudden death.
Applicatian Restrictions
Storage method:
Temperature and lighting
Tetracaine powder 0.5% should be stored in an environment between 2 ° C and 25 ° C (36 ° F and 77 ° F). It is necessary to avoid direct sunlight and protect the medication from direct sunlight.
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package
Medicines should be stored in tightly sealed and light resistant containers.
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inspect
Before use, the solution should be checked for crystallization, turbidity, or discoloration. If these situations occur, they should not be used.
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Disposable
This product is intended for single patient use, with each DROP-TAINER ® The dispenser contains 4 mL of medication, and the remaining unused portion should be discarded after use as this product does not contain preservatives.
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Usage Guide:
- Administration method: Usually, it is used as eye drops and dripped into the eye as needed. Unused parts should be discarded after each use to ensure sterility.
- Aseptic operation: When administering drugs in a sterile field, standard aseptic techniques should be used to open the packaging, and DROP-TAINER can be used ® The dispenser is placed on a sterile surface.
- Avoid contact: Do not touch the tip of the dropper to avoid contaminating the solution.
- Avoid intracorneal injection: It should not be administered through intracorneal injection or intraocular use. Using it may cause damage to corneal endothelial cells.
- Avoid long-term use: Long term use or abuse may lead to corneal epithelial toxicity and may manifest as epithelial defects, which may develop into permanent corneal damage.
- Avoid touching eyes after use: Patients should not touch their eyes for at least 10-20 minutes after using anesthesia, as accidental injury may occur due to loss of eye sensation.
- Medication for medical professionals: It should be taken under the direct supervision of medical professionals. This medication is not suitable for patients to take on their own.
adverse reaction
Tetracaine Powder, as a local anesthetic, is widely used in the medical field for surface anesthesia, infiltration anesthesia, conduction anesthesia, and epidural anesthesia. It achieves temporary sensory loss in local tissues or regions by blocking the transmission of nerve impulses, thereby reducing or eliminating pain. However, like other drugs, tetracaine may also cause a series of adverse reactions during use, which may involve multiple systems and pose a potential threat to the patient's health.
Pharmacological characteristics and mechanism of action
Pharmacological characteristics
Tetracaine belongs to ester local anesthetics, which have the characteristics of fast onset, long action time, and strong penetration. Its chemical structure determines that it is easily hydrolyzed by esterases in the body, thereby losing its anesthetic activity. This characteristic enables tetracaine to quickly take effect when applied locally, but also limits its feasibility for systemic use, as high doses or rapid absorption may lead to toxic reactions.
Mechanism of action
Tetracaine inhibits sodium ion channels on the membrane of nerve cells, preventing the influx of sodium ions and thus blocking the transmission of nerve impulses. This process results in temporary loss of pain, touch, and temperature sensation in local tissues or areas, achieving anesthesia effects. However, when the drug concentration is too high or absorbed too quickly, this inhibitory effect may extend to the central nervous system, causing a wider range of adverse reactions.
Types and mechanisms of adverse reactions
Central nervous system response
Dizziness and headache: These are common mild central nervous system reactions after using lidocaine powder. Medications may enter the bloodstream through local absorption, affecting brain function and causing symptoms such as dizziness and headache. These reactions usually occur in the early stages of drug action and gradually alleviate with drug metabolism.
Tinnitus and blurred vision: Some patients may report tinnitus or blurred vision, which may be related to the indirect effects of medication on the auditory and visual nerves. These symptoms are usually mild and transient.
Convulsion: When the concentration of lidocaine is too high or absorbed too quickly, it may cause convulsions. This is due to the excessive inhibition of the central nervous system by drugs, which leads to abnormal firing of neurons. Convulsions may manifest as systemic convulsions accompanied by loss of consciousness, and in severe cases can be life-threatening.
Respiratory depression: In extreme cases, lidocaine may inhibit the respiratory center, leading to a decrease in respiratory rate, shallower amplitude, and even respiratory pauses. This reaction is usually related to drug overdose or rapid absorption, which requires emergency treatment to avoid hypoxia and carbon dioxide retention.
Cardiovascular system response
Blood pressure drop: Tetracaine may cause a decrease in blood pressure by dilating blood vessels or inhibiting myocardial contractility. This reaction is particularly common during anesthesia induction, possibly due to the direct effect of the drug on vascular smooth muscle or inhibition of the sympathetic nervous system. A decrease in blood pressure may lead to dizziness, fatigue, and even fainting.
Cardiac arrhythmia: Some patients may experience cardiac arrhythmia, including tachycardia, bradycardia, or arrhythmia, after using lidocaine. This may be related to the direct impact of drugs on the cardiac conduction system or through reflex mechanisms such as compensatory heart rate acceleration caused by a decrease in blood pressure. Cardiac arrhythmia may increase the risk of cardiovascular events and requires close monitoring.
Allergic reactions
- Mild allergy
Skin itching and erythema: Some patients may experience allergic reactions to lidocaine or its excipients, manifested as skin itching, erythema, or urticaria. These symptoms usually appear within minutes to hours after drug exposure and can be relieved by antihistamines.
Local edema: Allergic reactions may cause edema at the injection site or surrounding tissues, which may be related to increased vascular permeability.
- Severe allergy (anaphylactic shock)
Dyspnea and laryngeal edema: In rare cases, patients may experience severe allergic reactions, known as anaphylactic shock. This manifests as difficulty breathing, laryngeal edema, rapid drop in blood pressure, and even loss of consciousness. Allergic shock requires immediate emergency treatment, including adrenaline injection and maintaining airway patency.
Local tissue reactions
Injection site pain: Tetracaine powder may cause injection site pain during injection, which may be related to the stimulation of local tissue by the drug or injection technique. The degree of pain varies from person to person and can usually be alleviated by slowing down the injection speed or using a thinner needle.
Localized inflammation or necrosis: In rare cases, lidocaine may cause inflammation or necrosis of local tissues. This may be related to high drug concentration, improper injection techniques, or the patient's special sensitivity to the drug. Local inflammation manifests as redness, swelling, and thermal pain, while necrosis may lead to tissue ulcers and scar formation.
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