Usage
- Centbucridine is a local anesthetic used for topical, infiltration, and nerve block anesthesia. It’s indicated for various surgical procedures, including ophthalmic and dental surgeries. It’s also utilized in wound healing gels combined with Feracrylum.
- Pharmacological Classification: Local anesthetic.
- Mechanism of Action: Centbucridine blocks nerve conduction by inhibiting sodium channels, thus preventing the transmission of pain signals.
Alternate Names
- 4-N-butylamino-1,2,3,4-tetrahydroacridine hydrochloride
- Brand names include Hemolok AR Gel, Sepgard AR Gel, and Supraheal AR Gel.
How It Works
- Pharmacodynamics: Centbucridine reversibly binds to sodium channels within nerve fibers, inhibiting sodium ion influx. This prevents depolarization and blocks nerve impulse conduction, effectively inhibiting pain signal transmission. It also exhibits some vasoconstrictor properties.
- Pharmacokinetics:
- Absorption: Rapid absorption from the administration site.
- Metabolism: Not extensively studied.
- Elimination: Not extensively studied. Details on elimination pathways (renal/hepatic excretion) and CYP enzyme metabolism are lacking in the current literature.
- Mode of Action: Sodium channel blocker.
- Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Binds to sodium channels, inhibiting nerve impulse transmission. No documented CYP450 interactions have been identified.
Dosage
Standard Dosage
Adults:
- Infiltration Anesthesia: 0.5% solution, 2 mg/kg up to a maximum of 20 mg.
- Topical Anesthesia (Ophthalmic): 0.5% or 1% solution, single drop instillation.
Children:
- Limited data available. Dosing should be adjusted based on weight and age under specialist guidance with close monitoring for variations in drug metabolism.
Special Cases:
- Elderly Patients: Dose adjustment may be necessary based on individual health and organ function. Initiate with lower doses and monitor closely.
- Patients with Renal Impairment: Dose modification is recommended based on creatinine clearance.
- Patients with Hepatic Dysfunction: Adjustment may be necessary due to potential altered metabolism. Commence with lower doses and monitor closely.
- Patients with Comorbid Conditions: Caution and potential dose modifications for patients with diabetes, cardiovascular diseases, or other relevant comorbidities.
Clinical Use Cases
- Intubation: Limited data; lower doses advised.
- Surgical Procedures (Minor): 0.5% solution for infiltration anesthesia.
- Mechanical Ventilation: No specific recommendations.
- Intensive Care Unit (ICU) Use: No specific recommendations.
- Emergency Situations: No specific recommendations.
Dosage Adjustments
- Consider modifications for patients with renal/hepatic impairment, metabolic disorders, or genetic polymorphisms affecting drug metabolism.
Side Effects
Common Side Effects:
- Burning sensation (especially with topical use)
- Dizziness
- Headache
- Pins and needles sensation
- Muscle twitchiness
- Continued numbness in the affected area
Rare but Serious Side Effects:
- Systemic toxicity (with high doses or inadvertent intravascular injection)
- Allergic reactions, including anaphylaxis
- Seizures
- Cardiac arrest
Long-Term Effects:
- No long-term side effects specifically reported.
Adverse Drug Reactions (ADR):
- Anaphylaxis (rare but serious)
Contraindications
- Known hypersensitivity to centbucridine or any formulation component.
Drug Interactions
- Other local anesthetics: Additive effects may occur if used concurrently.
- Medications affecting cardiac conduction: Use with caution in patients taking antiarrhythmic medications.
- Epsilon aminocaproic acid (EACA): Contraindicated for concomitant use with centbucridine + feracrylum combination.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: No official FDA classification assigned. Use with caution during pregnancy, especially in the first trimester, due to limited data on fetal risks.
- Breastfeeding: No specific data available regarding breast milk excretion. Use with caution and monitor the infant for adverse effects. Topical application of centbucridine + feracrylum is considered probably safe.
Drug Profile Summary
- Mechanism of Action: Sodium channel blocker, inhibiting nerve impulse transmission.
- Side Effects: Burning sensation, rare systemic toxicity, allergic reactions.
- Contraindications: Hypersensitivity to centbucridine, concomitant EACA use (when used in combination with feracrylum).
- Drug Interactions: Other local anesthetics, medications affecting cardiac conduction, EACA (with feracrylum combination).
- Pregnancy & Breastfeeding: Use with caution. Topical feracrylum + centbucridine combination probably safe during lactation.
- Dosage: Refer to the detailed dosage section above.
- Monitoring Parameters: Vital signs, especially respiratory and cardiovascular function.
Popular Combinations
- Feracrylum: Used in wound healing gels. Combines the antiseptic and hemostatic properties of feracrylum with the local anesthetic and antimicrobial effects of centbucridine.
Precautions
- General Precautions: Assess patient history for allergies and contraindications. Monitor vital signs during and after administration.
- Pregnant Women: Use with caution, especially during the first trimester.
- Breastfeeding Mothers: Use cautiously and monitor infant for side effects. Topical combination probably safe.
- Children & Elderly: Adjust dose based on age and weight. Monitor closely.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Centbucridine?
A: Refer to the detailed dosage section above, which covers adult, pediatric, and special population dosing.
Q2: What are the primary uses of Centbucridine?
A: Primarily used as a local anesthetic for infiltration, topical (especially ophthalmic), and nerve block anesthesia. Also used in wound healing gels combined with Feracrylum.
Q3: Is Centbucridine safe during pregnancy?
A: Use with caution, especially during the first trimester. Limited data on fetal risks is available. Consult specialized resources for further guidance.
Q4: Can I use Centbucridine if I am breastfeeding?
A: Use with caution while breastfeeding and monitor the infant for any adverse effects. Consult a healthcare professional. Topical application of centbucridine + feracrylum gel is considered probably safe.
Q5: What are the common side effects?
A: Burning sensation (particularly with topical use), dizziness, headache, pins and needles sensation, muscle twitchiness, and persistent numbness.
Q6: Are there any serious side effects I should be aware of?
A: Although rare, systemic toxicity (with high doses or inadvertent intravascular injection) and allergic reactions, including anaphylaxis, can occur. Seizures and cardiac arrest have also been reported in extremely rare cases.
Q7: Does Centbucridine interact with other medications?
A: Yes, additive effects may occur if used concurrently with other local anesthetics. Caution is advised with medications affecting cardiac conduction. EACA is contraindicated with the centbucridine + feracrylum combination.
Q8: What is the mechanism of action of Centbucridine?
A: It acts as a sodium channel blocker, inhibiting nerve impulse transmission by preventing depolarization.
A: Detailed information on its metabolism and elimination pathways is currently limited.
