Cocaine

NUMBRINO

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Cocaine ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Cocaine ballicule

What it isDopamine, norepinephrine, and serotonin reuptake inhibitor plus sodium-channel blocker; topical ENT anesthesia.

Why this oneThe only local anesthetic that also vasoconstricts, reducing bleeding during nasal procedures.

What limits itCoronary vasospasm, arrhythmia, seizure, and addiction are major hazards; avoid unopposed beta blockade during acute toxicity.

Cocaine molecular structure (skeletal formula) — Molecular structure: Cocaine

FDA-approved for

topical anesthesia (ENT) (1884)

Principal riskCoronary vasospasm; beta blockers are avoided in cocaine chest pain

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Sedation liability0 / 4

QT / Torsades2 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryN/A (post-2015 labeling)

Defining liabilitySympathomimetic cardiovascular toxicity and abuse potential

FDA label

Read the full label on DailyMed ↗

BOXED WARNING CNS stimulant with high potential for abuse and dependence.

FDA dosing	Population	Start	Target	Max
Nasal mucosal anesthesia for diagnostic procedures/surgery	Adult	40-160 mg topical (4% solution via pledgets), single application	40-160 mg per procedure	160 mg total (2 pledgets/nostril); not to exceed 3 mg/kg

Renal Not studied; use a conservative initiation approach and monitor for HR/BP increases

Hepatic Avoid in hepatic impairment (not studied)

Total dose for any one procedure must not exceed 3 mg/kg

Instructions

Intranasal/topical use only; not for injection or ophthalmic use
Do not apply to damaged nasal mucosa
Apply via cotton/rayon pledgets (1 mL each); max 2 pledgets per nostril; leave in place up to 20 minutes
Remove pledgets immediately upon any sign/symptom of an adverse event
Do not substitute for other intranasal cocaine products
Avoid concomitant vasoconstrictors (epinephrine, phenylephrine)

Available strengths

sol 4 %

Contraindications

Hypersensitivity to cocaine or other ester-type local anesthetics

Cautions

Seizures (lowers convulsive threshold)
Blood pressure and heart rate increases; avoid in recent/active MI, CAD, CHF, arrhythmia, abnormal ECG, uncontrolled hypertension, thyrotoxicosis
Potentiates concomitantly administered sympathomimetic amines
Corneal sloughing/ulceration if used in the eye
Abuse and dependence

Adverse reactions

Hypertension
Tachycardia
Sinus tachycardia
Bradycardia
QT/QRS prolongation
Headache
Seizure
Anxiety

Pregnancy No data with NUMBRINO; chronic cocaine abuse in pregnancy associated with reduced fetal growth and adverse outcomes

Lactation Breastfeeding not recommended during treatment; pump and discard breast milk for 48 hours after use

Cost

Cocaine (NUMBRINO)

Strength		#/mo	generic $/unit	CostPlus
4 %	sol	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Cocaine is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Serotonin and MAOI

Provisional washout figures

SRI significance2 / 4

Serotonin release0 / 4

Elevating mechanismSRI

Evidence confidenceModerate

InterpretationInhibits SERT as well as DAT and NET; does not belong in an MAOI-compatible group.

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Self-check

What distinguishes cocaine from other local anesthetics in nasal procedures?
It also vasoconstricts, reducing bleeding.
Which blockade should be avoided during acute cocaine toxicity?
Unopposed beta blockade.