Lappaconitine Hydrobromide

Lappaconitine Hydrobromide(LA) is a kind of diterpenoid alkaloid, labaconitine, which is extracted and isolated from the aconitum of ranunculus family. It is the first non-addictive analgesic drug for central nervous system in China. It has the effects of analgesia, antipyretic, detumescence and local anesthesia, and has the characteristics of non-addiction and less adverse reactions. Its analgesic effect is stronger than indomethacin and weaker than morphine. At present, its strong analgesic and immunomodulatory effects are mainly used in the clinical diagnosis and treatment activities of various specialties, and it is widely used in the late analgesia and perioperative analgesia of cancer.

Lappaconitine  is a popular product at KINTAI. After a decade of research and development, KINTAI has successfully overcome numerous core technical problems, achieving exceptional purity in every batch. We consistently adhere to stringent quality standards and maintain a customer-centric approach, ensuring that every product meets stringent pharmaceutical-grade standards. We provide global pharmaceutical companies with highly effective and safe botanical intermediates. As a trusted supplier of botanical active ingredients, we maintain our leading position in botanical extraction technology and are now the largest producer of 96%Lappaconitine  in China.Please feel free to contact us at health@kintaibio.com.

1. Analgesia

Laptopaconitine, my country's first non-addictive analgesic, is used to treat various mild to moderate pain conditions, such as cancer pain, postoperative pain, and sciatica. Clinically, lappaconitine's analgesic efficacy is seven times that of aminopyrine, and it has shown significant relief for toothache, trigeminal neuralgia, herpes zoster pain, and postoperative pain.

2. Anti-inflammatory

Laptopaconitine has a moderate anti-inflammatory effect and is commonly used in folk medicine to treat inflammatory conditions such as lupus erythematosus, rheumatism, and rheumatoid arthritis. Laptopaconitine can inhibit NO production by inhibiting the NF-κB pathway and the mitogen-activated protein kinase (MAPK) signaling pathway, thereby reducing the expression of inflammatory factors (TNF-α, IL-1β, IL-6) and chemokines (KC, MCP-1, MIP-1α), achieving anti-inflammatory effects.

3. Antiarrhythmic

Laptopaconitine's antiarrhythmic effect is a unique activity of lappaconitine. Lappaconitine belongs to the Class Ic antiarrhythmic natural product class. The antiarrhythmic activity of its derivatives is dependent on the halogen at the C-5' position of the aromatic group. The order of halogen substitution affecting biological activity is: Br > I > Cl. Lappaconitine hydrobromide is the most potent antiarrhythmic derivative.

4. Anti-tumor Effects

Lappaconitine sulfate can block A549 cells in the G0/G1 phase via the phosphoinositide 3-kinase/protein kinase B (PI3K/protein kinase B, PKB or AKT) signaling pathway, induce apoptosis, and inhibit cell viability and proliferation. The PI3K/AKT signaling pathway plays an important role in cell survival, proliferation, and growth.

5. Anti-epileptic Effects

Lappaconitine's inhibition of sodium currents is use-dependent and does not alter the voltage-dependence of sodium current activation and inactivation. Lappaconitine selectively reduces the duration of epileptiform discharges and bursts in neurons induced by bicuculline, aconitine, or Mg2+-free external solution. This suggests that the antiepileptic activity of lappaconitine may be mediated by inhibiting axonal conductance and reducing sodium currents.

1. Adverse Reactions

Occasionally, dizziness, palpitations, urticaria, chest tightness, and allergic rash may occur, generally resolving spontaneously.

The injection may cause local irritation.

2. Contraindications and Precautions

This product is contraindicated in patients with allergies.

Use with caution in patients with severe hepatic or renal insufficiency.

The safety of this drug in pregnant and lactating women is unknown; use should be carefully weighed against the risks.

Use with caution in patients with heart disease.

3. Drug Interactions

Combined use with other central nervous system depressants (such as sedatives and hypnotics) may enhance the depressant effect.

Combination use with other medications is recommended under a physician's supervision.

4. Special Notes

Slow onset of action: Compared to fast-acting opioids such as morphine, Lappaconitine Hydrobromide takes approximately 30 minutes to take effect after injection, making it unsuitable for extreme situations requiring immediate analgesia.

The formulation of lappaconitine  is primarily based on different dosage forms to meet diverse clinical needs. The following are its main dosage forms and formulation features:

1. Injection

This is the most classic and common dosage form, used for acute, moderate to severe pain.

Formula:

• Active ingredient: lappaconitine hydrobromide
• Solvent: Water for injection
• pH adjuster: Dilute hydrochloric acid or sodium hydroxide solution is commonly used to adjust the pH to an appropriate range (usually 4.0-6.0) to ensure drug stability and reduce irritation during injection.
• Possible excipients: Antioxidants (such as sodium bisulfite) are sometimes added to enhance stability.
• Common strengths: 4mg/2ml, 8mg/2ml, etc.
• Route of administration: Intramuscular injection or intravenous infusion.

2. Tablets/pills

This is used for the maintenance treatment of chronic, persistent pain and is convenient to administer.

Formula:

• Active ingredient: lappaconitine hydrobromide
• Bulker: Such as starch, lactose, and microcrystalline cellulose, used to increase tablet weight. Binders, such as polyvinylpyrrolidone (PVP) and starch slurry, are used to bind powders.
• Disintegrants, such as cross-linked sodium carboxymethyl cellulose and low-substituted hydroxypropyl cellulose, promote tablet disintegration in the gastrointestinal tract.
• Lubricants, such as magnesium stearate and talc, facilitate tablet compression.
• Common strength: 5 mg/tablet.

3. Patches (Transdermal Drug Delivery System)

This innovative dosage form provides sustained, stable analgesia and is particularly suitable for patients with chronic pain requiring long-term medication (such as cancer pain). It avoids first-pass hepatic effects and gastrointestinal side effects.

Formulation:

• Active ingredient: Lappaconitine hydrobromide
• Pressure-sensitive adhesives, such as polyacrylates, silicones, or polyisobutylenes, enable the patch to adhere to the skin and serve as a drug reservoir and release vehicle.
• Penetration enhancers, such as aminoketone and oleic acid, help the drug penetrate the stratum corneum.
• Backing layer: A water-impermeable film that prevents drug evaporation and external contamination. Anti-stick layer: A protective layer to be removed before use.
• Advantages: Stable blood drug concentration, long-lasting effect (lasting for more than 24 hours), easy to use, and good patient compliance.

Q1:What is lappaconitine hydrobromide used for?

A1:Lappaconitine hydrobromide is widely utilized in research focused on Pain Management.

Q2:What's your MOQ?

A2:Our MOQ is flexiable, please contact us to get more information.