Cocaine (Topical Anesthetic): Medical Uses, Dosage, Side Effects & More

 

Learn everything about medical-grade Cocaine, including its introduction, mechanism of action, pharmacokinetics, clinical indications, side effects, interactions, dosage, brand names, and pricing. An essential guide for medical professionals and students.

Table of Contents:

1. Introduction  

2. Mechanism of Action  

3. Pharmacokinetics and Dynamics  

4. Indications  

5. Drug of Choice  

6. Contraindications  

7. Side Effects  

8. Drug Interactions  

9. Dosage  

10. Brand Names & Price  

11. Conclusion

1. Introduction:

Cocaine is a *Schedule II controlled substance* with legitimate *medical applications*. It is primarily used as a *topical anesthetic and vasoconstrictor* in ENT procedures (especially nasal surgeries). Unlike its illicit form, *medical cocaine is purified and strictly regulated*.

2. Mechanism of Action:

Cocaine blocks the reuptake of *norepinephrine, dopamine, and serotonin* at nerve terminals. It also *inhibits sodium channels*, resulting in local anesthesia. Its *vasoconstrictive* action helps reduce bleeding during surgeries.

3. Pharmacokinetics and Dynamics:

- *Absorption:* Rapidly absorbed via mucosal surfaces  

- *Onset:* Within 1–5 minutes (topical)  

- *Duration:* 30–60 minutes  

- *Metabolism:* Hepatic via plasma esterases  

- *Half-life:* 0.8–1.5 hours  

- *Excretion:* Renal

4. Indications:

- Local anesthesia in *nasal, laryngeal, and oral* procedures  

- Reduction of bleeding during *ENT surgeries*  

- Occasionally used for *diagnostic nasal blocks*

5. Drug of Choice:

Cocaine is often preferred in *nasal surgeries* due to its *dual action*—local anesthesia and vasoconstriction—making it a *drug of choice* in certain ENT settings.

6. Contraindications:

- Hypersensitivity to cocaine  

- Hypertension  

- Cardiac arrhythmias  

- Hyperthyroidism  

- Pregnancy  

- Patients with history of *substance abuse*

7. Side Effects:

- *Common:* Irritation, headache, dry nose  

- *Systemic:* Tachycardia, hypertension, dizziness  

- *Serious:* Arrhythmias, seizures, myocardial infarction, CNS stimulation

- *Addiction Risk*: High if abused outside medical settings

8. Drug Interactions:

- *MAO inhibitors* – hypertensive crisis  

- *Beta-blockers* – increased risk of unopposed alpha activity  

- *Sympathomimetics* – additive cardiovascular effects  

- Avoid with *alcohol* or other CNS stimulants

9. Dosage:

- Typically used as a *4% or 10% topical solution*

- *Adult dosage:* Not to exceed *200 mg* of cocaine per procedure  

- Apply directly to the mucosa under supervision

10. Brand Names & Price:

Brand Names:

  - Goprelto®️ (Cocaine hydrochloride topical solution)  

  - Numbrino®️  

- *Forms Available:* 4% and 10% solutions  

Price: 

Goprelto can cost 150–250 per vial (under regulated conditions)

11. Conclusion:

Though controversial, *Cocaine remains a vital tool* in ENT procedures due to its unique combination of anesthetic and vasoconstrictive properties. Its *clinical use must be closely monitored*, and it should only be handled by trained professionals under strict medical guidelines.