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Articaine Hcl Powder compound is a white crystalline powder, and its chemical formula is methyl 4 -methyl-3-[ [1-oxo-2-(propaneamino) propyl] amino]-2-thiophene carboxylate. Articaine HCl, chemical formula C13H20N2O3S · HCl, CAS 23964-57-0. It is a local anesthetic widely used in dental and other surgical procedures. It is the hydrochloride form of Articaine and has a series of unique chemical properties. It is a four ring structure consisting of a benzene ring, a thiophene ring, a methylpropylamino carboxylyl group, and an alkyl group. It has one chiral carbon atom, so there are two Enantiomer: (S)-Articaine HCl and (R)-Articaine HCl. It is in the form of a hydrochloride and therefore has acidity. When Articaine HCl is dissolved in water, it will completely dissociate into positively charged Articaine cations and chloride ions (Cl-). This dissociation process is a Reversible reaction, depending on the acid-base equilibrium in the solution. Different Enantiomer have different optical rotation properties, among which (S)-Articaine HCl has specific optical rotation. The solubility may vary at different pH values. Under acidic conditions, solubility may slightly decrease, while in alkaline environments, solubility may be higher. Therefore, when preparing and using drugs, it is necessary to adjust the pH value of the solution according to specific needs and conditions.
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Chemical Formula |
C13H20N2O3S |
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Exact Mass |
284 |
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Molecular Weight |
284 |
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m/z |
C, 54.91; H, 7.09; N, 9.85; O, 16.88; S, 11.27 |
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Elemental Analysis |
C, 52.39; H, 6.60; N, 6.11; O, 27.91; S, 6.99 |
Articaine HCl has anesthetic and analgesic effects. Its molecular structure is as follows:
Hydrogen and ion bonds
There are hydrogen and ion bonds in Articaine HCl molecules. Hydrogen bond is a weak bond formed by the hydrogen atom in Articaine and Electronegativity atoms in other molecules (such as oxygen, nitrogen, etc.). These hydrogen bonds contribute to the interaction between Articaine and other molecular structures, such as drug receptor binding. At the same time, the cationic part of Articaine HCl forms ionic bonds with the anionic part (such as chloride ions).
Structural features
- Organic part:
The organic part of Articaine HCl is composed of benzene ring, thiophene ring, methylpropylamino carboxylyl group, and alkyl group. There is a methyl group and a propylamino carboxyl group connected to the benzene ring. There is a methyl group attached to the thiophene ring. Alkyl groups are attached to carbon atoms on the thiophene ring. These organic groups endow Articaine HCl with drug activity and biological characteristics.
- Cation part:
Articaine HCl is a hydrochloride formed by the reaction of Articaine with hydrochloric acid. It contains a positively charged Articaine cation and a chloride ion (Cl -). This cationic part is responsible for interacting with the anesthesia target site to produce local anesthesia effects.
Stereoscopic structure
Articaine HCl molecule contains chiral carbon atoms, so there are two Enantiomer: (S) - Articaine HCl and (R) - Articaine HCl. These two isomers are mirror symmetric in spatial configuration and share the same chemical composition, but their chemical and biological properties may differ slightly.
As for articaine, so far, animal experiments of two species have been carried out. Animal experiments show that articaine has good tolerance, and no teratogenic effect has been found in the study. Note that the product contains pyrosulfite may cause allergic reactions or aggravate allergies, athletes need to pay attention to the active ingredients of this drug can cause positive urine test results of stimulants. Moreover, articaine hcl and epinephrine can be mixed to produce septocaine.
What are the side effects?
Articaine Hcl, Articaine hydrochloride is a local anesthetic used in dentistry. Its powder form is usually used for formulation in scientific research or specific medical environments. However, regarding the side effects of articaine hydrochloride powder, as it is mainly used for local anesthesia after preparing the solution, its side effects are usually related to the use of the prepared solution rather than the powder form itself. However, considering the potential risks of powder processing and preparation, as well as the potential side effects of using the prepared solution, the following are its side effects:
Potential risks in powder processing and preparation
Skin and eye contact
During the processing and preparation of Articaine Hcl powder, if it accidentally comes into contact with the skin or eyes, it may cause irritation and discomfort. Skin contact may cause redness, swelling, itching, or pain. Eye contact may cause stinging, tearing, and blurred vision.
Inhalation and Swallowing
Inhaling powder of articaine hydrochloride may cause irritation to the respiratory tract, leading to coughing, difficulty breathing, or asthma. Swallowing powder may cause gastrointestinal discomfort, such as nausea, vomiting, and abdominal pain.
Allergic reactions
Some individuals may experience allergic reactions to articaine hydrochloride or its components, manifested as rash, urticaria, difficulty breathing, laryngeal edema, etc. Severe allergic reactions can lead to anaphylactic shock, which is life-threatening.
Potential side effects of using formulated articaine hydrochloride solution
- Local tissue damage: Improper injection techniques or excessive dosage during local anesthesia may lead to local tissue damage, such as hematoma, nerve damage, and infection.
- Inefficient anesthesia effect: Due to individual differences, injection sites, or injection depths, the anesthesia effect may not be ideal, and patients may still feel pain or discomfort.
- Allergic reactions: The prepared solution of articaine hydrochloride may also cause allergic reactions, with symptoms similar to powder contact but possibly more severe.
- Central nervous system suppression: Excessive use of articaine hydrochloride may lead to central nervous system suppression, manifested as confusion, drowsiness, coma, and even respiratory arrest. This may be due to the drug entering the central nervous system through the bloodstream, causing a blocking effect on nerve conduction.
- Muscle tremors: Articaine hydrochloride may have an impact on central motor neurons, leading to muscle tremors. Tremors may exacerbate local discomfort and affect the accuracy of surgery or treatment.
- Slow heart rate: Articaine hydrochloride may directly act on the heart or indirectly affect the heart through the central nervous system, leading to a decrease in heart rate. A significant decrease in heart rate may lead to insufficient blood supply to the brain, posing a risk of fainting or cardiac arrest.
- Blood pressure drop: Articaine hydrochloride has the effect of dilating blood vessels, which may reduce peripheral resistance and lead to a decrease in blood pressure. Long term hypotension may cause insufficient blood supply to organs, and in severe cases, shock symptoms may occur.
- Dyspnea: In rare cases, articaine hydrochloride may cause respiratory distress, which may be due to allergic reactions or central nervous system suppression.
- Apnea: In extreme cases, articaine hydrochloride may cause apnea, which is typically associated with severe central nervous system suppression.
- Taste changes: After using articaine hydrochloride, some patients may experience taste changes such as decreased or abnormal taste.
- Nausea and vomiting: Some patients may experience symptoms of nausea and vomiting after using articaine hydrochloride.
Precautions and preventive measures for articaine hydrochloride
Drug preparation
Articaine Hcl powder should be prepared under sterile conditions to ensure the purity and safety of the drug. When preparing, follow the instructions of a doctor or pharmacist to avoid excessive or insufficient dosage.
Drug use
Before using articaine hydrochloride, patients should be carefully asked about their allergy and medication history to avoid potential allergic reactions. Proper injection techniques and depth should be followed during use to reduce the risk of local tissue damage. During use, the patient's vital signs and reactions should be closely monitored in order to promptly detect and address potential side effects.
Drug storage
Articaine hydrochloride should be stored in a cool and dry place, away from direct sunlight and high temperatures. During the storage process, the packaging and expiration date of the medication should be regularly checked to ensure its quality and safety.
Patient education
Before using articaine hydrochloride, the patient should be provided with a detailed explanation of the drug's use, possible side effects, and precautions. Encourage patients to promptly report any discomfort or abnormal reactions during use.
- The demand in the dental field is increasing: With the growth of the global population and the improvement of oral health awareness, the demand for dental treatment is constantly increasing. As an effective local anesthetic for dentistry, the market demand for articaine hydrochloride will continue to grow. It has the advantages of good diffusion, fast anesthesia effect, and long duration, making it the preferred anesthetic drug in dental clinics and hospitals.
- Academic research and institutional demand: The academic community and research institutions are increasingly interested in the study of articaine hydrochloride, in order to explore its more applications in pain control, pharmacological mechanisms, and other areas.
- Global market size: The global market size of articaine hydrochloride is growing year by year and is expected to maintain a stable compound growth rate in the coming years.
- Production process optimization: With the continuous progress of chemical synthesis and pharmaceutical technology, the production process of articaine hydrochloride will be more efficient and environmentally friendly, thereby reducing production costs and improving market competitiveness.
- Research and development of new formulations: In order to meet the needs of different patients, the development of new formulations such as sustained-release and controlled release formulations will become an important direction for the future research and development of articaine hydrochloride.
- Medical policy promotion: Governments around the world continue to attach increasing importance to oral healthcare and have introduced a series of policy measures to promote its development. This will be beneficial for the market promotion and application of oral healthcare products such as articaine hydrochloride.
- Drug regulatory policies: With the continuous improvement and strictness of drug regulatory policies, the production, sales, and use of drugs such as articaine hydrochloride will become more standardized, which is conducive to ensuring patient medication safety and product quality.
- Intense market competition: Currently, there are multiple domestic and foreign companies competing in the market for articaine hydrochloride, and the phenomenon of product homogenization is quite serious. Therefore, enterprises need to strengthen technological innovation and brand building, improve product added value and market competitiveness.
- Environmental Protection and Sustainable Development Challenges: With the increasing global awareness of environmental protection, the production and use of chemical drugs such as articaine hydrochloride need to pay more attention to environmental protection and sustainable development. Enterprises need to adopt environmentally friendly production processes and waste disposal technologies to reduce environmental pollution.
Articaine Hcl Powder, also known as Hoe-045, is a potent local anesthetic belonging to the amide class. It exists as a white to off-white crystalline powder. This compound is an amide-based local anesthetic with an ester group, which allows it to reversibly bind to the α-subunit of voltage-gated sodium channels within nerve fibers, thereby inhibiting neural conduction and providing analgesia.
Articaine hydrochloride is primarily used for local anesthesia in dental procedures such as tooth extractions, endodontic treatments, and periodontal therapies. It is effective in blocking nerve conduction along the injected site, ensuring pain relief during these procedures.
When administered, Articaine hydrochloride is usually injected as a 4% solution. The injection speed should not exceed 1 ml per minute to avoid adverse reactions. For mandibular molar endodontic treatments where local infiltration anesthesia may not provide complete analgesia, an additional 0.2 to 0.3 ml of the solution can be injected directly into the periodontal ligament space of the affected tooth to enhance pain relief.
Articaine hydrochloride should be stored at 4°C in a sealed container, away from moisture and light. For solutions prepared for experimental use, storage conditions vary depending on the solvent used. For instance, in DMSO or water, the solution can be stored at -80°C for up to 6 months or at -20°C for 1 month, provided it remains sealed and protected from moisture and light.
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