Lidocaine capsule is an orally administered amide-type local anesthetic and antiarrhythmic agent widely used in clinical practice, with lidocaine as its core active ingredient and a molecular formula of C₁₄H₂₂N₂O. Characterized by rapid onset, stable therapeutic effects and manageable toxicity, it has become an indispensable clinical drug across multiple disciplines. Compared with injectable formulations, capsules offer the advantages of convenient oral administration and high patient compliance, delivering mild yet long-lasting effects while eliminating trauma and local irritation associated with injection delivery.
As a membrane stabilizer, its core pharmacological property lies in the reversible blockade of cell membrane sodium channels, conferring multiple bioactivities including local analgesia, antiarrhythmic action, anti-inflammatory effects and antinociceptive activity. It has a pKa value of 7.7 and moderate liposolubility under physiological pH conditions, enabling rapid penetration across biological membranes. Following gastrointestinal absorption, it distributes evenly throughout body tissues.
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Lidocaine COA
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| Certificate of Analysis | ||
| Compound name | Lidocaine | |
| Grade | Pharmaceutical grade | |
| CAS No. | 137-58-6 | |
| Quantity | Customized | |
| Packaging standard | Customized | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090088 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.27% |
| Loss on drying | ≤1.0% | 0.42% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.98% |
| Single impurity | <0.8% | 0.45% |
| Total microbial count | ≤750cfu/g | 400 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 550ppm |
| Storage | Store in a sealed, dark, and dry place below 2-8°C | |
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| Chemical Formula | C14H22N2O |
| Exact Mass | 234.17 |
| Molecular Weight | 234.34 |
| m/z | 234.17 (100.0%), 235.18 (15.1%), 236.18 (1.1%) |
| Elemental Analysis | C, 71.76; H, 9.46; N, 11.95; O, 6.83 |
Mechanism of Action and Clinical Applications
Core Pharmacological Mechanisms
The pharmacological activity of lidocaine capsule primarily stems from specific blockade of cell membrane sodium channels, complemented by auxiliary mechanisms including potassium channel modulation, anti-inflammatory effects and antithrombotic activity, whereby multi-target synergism yields therapeutic outcomes. As a weakly basic amide drug, its non-ionized form freely crosses biological barriers such as neuronal and cardiomyocyte membranes after oral absorption.
Upon entering cells, it ionizes into positively charged cations that reversibly bind to voltage-gated sodium channels on the inner side of cell membranes, locking the channels in an inactivated state and blocking sodium influx effectively.This action directly suppresses depolarization in neurons and cardiomyocytes, halting the generation and conduction of action potentials to fundamentally block pain signal transmission and correct abnormal cardiac electrical activity.
In terms of neural regulation, lidocaine precisely inhibits impulse conduction in peripheral sensory nerve fibers, exerting pronounced blockade of pain and temperature signals with minimal impact on motor nerves.
At therapeutic doses, it achieves selective analgesia without limb movement dysfunction. Additionally, it modulates signal transmission in nociceptors of the spinal dorsal horn to mitigate central sensitization, alleviating both acute pain and halting the progression of chronic pain. For cardiac electrophysiological regulation, the drug increases potassium permeability of cardiomyocyte membranes to facilitate potassium efflux, markedly reducing automaticity of Purkinje fibers, shortening action potential duration and absolute refractory period while prolonging the relative refractory period.
It effectively blocks reentrant cardiac electrical circuits and elevates ventricular fibrillation threshold, specifically correcting ventricular arrhythmias. Furthermore, modern pharmacological research confirms that lidocaine inhibits TLR receptors and nuclear factor signaling pathways to reduce pro-inflammatory cytokine release, delivering anti-inflammatory, anti-platelet aggregation and microcirculation-improving effects that further expand its clinical scope.
Applications in Pain Medicine
Pain intervention represents the primary clinical indication of ligoncaine capsules, covering acute pain, chronic pain and intractable neuropathic pain.
Its oral convenience renders it a preferred analgesic for outpatient and home-based pain management. For acute pain, it efficiently relieves discomfort induced by soft tissue injuries, mild postoperative trauma and mucosal inflammation. Compared with nonsteroidal anti-inflammatory drugs, it acts faster without adverse effects such as gastrointestinal mucosal injury and coagulation abnormalities, making it suitable for patients intolerant to conventional analgesics.
Prophylactic oral administration of ligoncaine capsules during the perioperative period preemptively blocks peripheral pain signaling, lowers the incidence of acute postoperative pain, reduces required opioid dosages and avoids opioid-related adverse reactions including addiction, nausea and vomiting, thereby optimizing perioperative analgesic regimens.
In chronic pain management, ligoncaine capsules demonstrate remarkable efficacy against intractable conditions such as postherpetic neuralgia, painful diabetic peripheral neuropathy and chronic neuropathic headaches.
Such chronic pain mostly arises from abnormal neuronal discharge, central sensitization and localized chronic inflammation. Through sustained blockade of aberrant sodium channels, suppression of pathological nerve impulses and alleviation of local inflammatory infiltration, lidocaine gradually relieves persistent dull, stabbing and burning pain, breaks the vicious cycle of pain, and improves patients' sleep quality and daily functioning. For mucosal-derived chronic pain including esophagitis and oral ulcers, the oral formulation targets submucosal nerve endings to precisely mitigate irritation-induced pain with mild, durable effects suitable for long-term low-dose maintenance therapy.
Unlike topical lidocaine preparations, capsules deliver uniform systemic action, eliminating uneven local dosing and limited coverage associated with external formulations for more consistent and comprehensive analgesia.
Applications in Cardiovascular Diseases
As a classic Class Ib antiarrhythmic agent, lidocaine capsule serves as a core oral medication for clinical management of ventricular arrhythmias, particularly ventricular electrical abnormalities secondary to organic heart diseases, featuring outstanding safety and target specificity.
Clinical studies indicate that therapeutic doses of lidocaine exert negligible effects on atrial and sinoatrial node electrical activity, acting selectively on ventricular Purkinje fibers and ventricular myocytes without triggering severe adverse reactions such as sinus bradycardia and atrioventricular block, rendering it compatible with most cardiovascular patients.
It is primarily indicated for ventricular premature beats and ventricular tachycardia stemming from acute myocardial infarction, myocarditis and myocardial ischemia, while also preventing ventricular fibrillation in high-risk populations.
Following acute myocardial infarction, ischemic myocardial regions develop disordered cardiomyocyte electrical activity generating abundant abnormal reentrant excitation, which readily triggers life-threatening malignant ventricular arrhythmias. Oral ligoncaine capsules rapidly stabilize ventricular myocyte membrane potential, suppress pathological automaticity and block reentrant conduction to resolve ventricular premature beats, halt ventricular tachycardia progression and reduce mortality from malignant arrhythmias post-infarction.
Long-term low-dose oral administration stabilizes cardiac electrical activity in patients with chronic heart failure and cardiomyopathy complicated by frequent ventricular premature beats, lowering arrhythmia frequency and improving patient prognosis. Moreover, perioperative oral administration during cardiac surgery provides prophylactic intervention against myocardial electrical disturbances, cutting postoperative ventricular arrhythmia incidence and safeguarding surgical safety. Notably, the drug exhibits no obvious therapeutic effect on supraventricular arrhythmias; strict differentiation of indications is required clinically to avoid indiscriminate medication.
Applications in Digestive Diseases
The application of ligoncaine capsules in gastroenterology centers on mucosal analgesia, inflammation relief and intervention for functional gastrointestinal disorders, making it a common adjuvant therapeutic agent in gastroenterology departments. Patients with reflux esophagitis and erosive gastritis present damaged, congested and edematous esophageal and gastric mucosa with exposed submucosal nerve endings, prone to acid and food irritation triggering acid regurgitation, heartburn, retrosternal pain and dull gastric pain.
After oral intake, lidocaine rapidly targets gastrointestinal mucosal nerve endings to block pain signal transmission and relieve heartburn and abdominal discomfort. It also reduces local pro-inflammatory cytokine release to alleviate mucosal congestion and edema, supporting mucosal repair.
For functional gastrointestinal disorders such as irritable bowel syndrome, patients frequently experience recurrent abdominal pain, bloating and defecation abnormalities due to heightened intestinal nerve sensitivity, with limited efficacy from conventional antispasmodics.
Lidocaine modulates neural conduction in intestinal smooth muscle to reduce intestinal nerve hypersensitivity, alleviating intestinal spasmodic pain and bloating without notable suppression of intestinal function or secondary constipation and aggravated distension.Additionally, oral ligoncaine capsules administered prior to gastroscopy, colonoscopy and other digestive endoscopies mildly block gastrointestinal mucosal nerves to mitigate nausea, abdominal pain and foreign body sensation caused by mechanical friction and stimulation during examinations, boosting patient tolerance, optimizing endoscopic experience and lowering complication risks.
Other Adjuvant Clinical Applications
Beyond its core therapeutic fields, lidocaine capsule possesses extensive adjuvant clinical value in perioperative systemic conditioning, auxiliary treatment of inflammatory disorders and neurological intervention owing to their multifaceted pharmacological activities. In perioperative systemic management, in addition to adjuvant analgesia, their anti-inflammatory and antithrombotic properties effectively reduce risks of postoperative systemic inflammatory response syndrome and deep vein thrombosis.
Surgical trauma triggers an inflammatory cascade leading to postoperative fever, tissue edema and slow recovery; lidocaine inhibits inflammatory pathway activation and suppresses secretion of pro-inflammatory mediators including tumor necrosis factor and interleukins to alleviate systemic inflammatory damage postoperatively, accelerating wound healing and physical recovery. Meanwhile, its anti-platelet aggregation and microcirculation-improving effects mitigate postoperative hypercoagulability to prevent thrombotic complications in bedridden patients.
In neurology, it serves as adjuvant therapy for certain neurological tremors and localized nerve spasms, relieving involuntary muscle tremors and focal spasmodic pain via blockade of abnormal neuronal discharge. In otorhinolaryngology, it alleviates persistent dull pain and foreign body sensation induced by chronic pharyngitis and external auditory canal inflammation to ameliorate patient discomfort.
Furthermore, clinical research demonstrates that long-term low-dose oral ligoncaine capsules assist in alleviating somatization symptoms in some patients with intractable chronic pain, relieving pain-induced anxiety and insomnia to achieve coordinated intervention for physical and psychological symptoms. Nevertheless, the drug exhibits dose-dependent toxicity; excessive intake may trigger adverse reactions such as dizziness, drowsiness and arrhythmias. Clinical administration demands strict control of dosage and treatment duration, with dose reduction as appropriate for patients with impaired hepatic or renal function.
The industrial synthesis of lidocaine adopts a classic amidation condensation route utilizing 2,6-dimethylaniline and diethylaminoethyl chloride as core raw materials. This mature process delivers high conversion rates and controllable impurities, suitable for large-scale pharmaceutical manufacturing and representing the mainstream synthetic pathway in the pharmaceutical industry to date.
The overall workflow comprises three stages: condensation reaction, purification and refining, and salt formation with purification, featuring mild reaction conditions without high-temperature and high-pressure equipment and low production costs.
First, anhydrous toluene serves as the reaction solvent. 2,6-dimethylaniline and diethylaminoethyl chloride are mixed at a fixed molar ratio with an appropriate acid-binding agent added. The mixture is stirred and heated to 80–90 °C for a 4–6 hour condensation reaction. The acid-binding agent neutralizes hydrogen chloride generated during the reaction to prevent acidic substances from inhibiting forward reaction progression, simultaneously minimizing byproduct formation and enhancing raw material utilization efficiency.
Upon reaction completion, the reaction mixture is cooled, left to stand and subjected to liquid-liquid separation to remove the lower acidic aqueous phase and retain the organic phase. Vacuum distillation eliminates toluene solvent and unreacted residual raw materials to yield crude lidocaine intermediate. The intermediate is then recrystallized using aqueous ethanol to remove residual impurities and byproducts and elevate drug purity.
Finally, purified lidocaine free base undergoes acid-base neutralization with an appropriate amount of hydrochloric acid to produce lidocaine hydrochloride. Subsequent low-temperature crystallization, filtration and drying yield high-purity active pharmaceutical ingredients, which are combined with excipients including starch and microcrystalline cellulose to formulate ligoncaine capsules.
The synthetic process delivers products with purity exceeding 99%, complying with pharmacopoeial pharmaceutical standards. Characterized by few reaction byproducts and straightforward downstream purification, it balances production efficiency and drug safety for widespread industrial mass production.
Frequently Asked Questions
What exactly does lidocaine do?
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Lidocaine belongs to the family of medicines called local anesthetics. This medicine prevents pain by blocking the signals at the nerve endings in the skin. This medicine does not cause unconsciousness as general anesthetics do when used for surgery. This medicine is available only with your doctor's prescription.
Is lidocaine a narcotic drug?
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Is lidocaine (Xylocaine) a narcotic? No, lidocaine (Xylocaine) isn't a narcotic. It's a local or regional anesthetic, which means it lowers your ability to feel pain in a specific area where it's injected. This medication works by preventing nerves from sending pain signals to the brain.
Is lidocaine a strong pain killer?
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Yes, lidocaine cream may cause a loss of feeling that numbs the skin in the application area. The numbing effect can relieve pain by stopping your nerves from sending pain signals.
Does lidocaine cause headaches?
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Rarely, some people may experience adverse reactions to the medications used in dental anesthesia (such as lidocaine), which can include headaches. One rare but important example is acute toxic methemoglobinemia, which can be triggered by the injection of lidocaine and some other dental anesthetic medications.
Does lidocaine heal or just numb?
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LIDOCAINE (LYE doe kane) treats pain. It numbs the area where it is applied, which blocks your nerves from sending pain signals to your brain.
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