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 oneIt is the 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)

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.

⚠ BOXED WARNING

Potential for abuse and dependence

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

Classes and tags

Clinical profile

Therapeutic safety burden3 / 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

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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