Yes

Local Anesthetic

Topical anesthesia for mucous membranes

C-II

C/X (if nonmedicinal use)

Hypersensitivity to cocaine or to any components of the topical solution; ophthalmologic anesthesia (causing sloughing of the corneal epithelium); pregnancy (nonmedicinal use)

For topical use only. Limit to office and surgical procedures only. Resuscitative equipment and drugs should be immediately available when any local anesthetic is used. Debilitated, elderly patients, acutely ill patients, and children should be given reduced doses consistent with their age and physical status. Use caution in patients with severely traumatized mucosa and sepsis in the region of the proposed application. Use with caution in patients with cardiovascular disease or a history of cocaine abuse. In patients being treated for cardiovascular complication of cocaine abuse, avoid beta-blockers for treatment.

>10%:

Central nervous system: CNS stimulation

Gastrointestinal: Loss of taste perception

Respiratory: Rhinitis, nasal congestion

Miscellaneous: Loss of smell

1% to 10%:

Cardiovascular: Heart rate (decreased) with low doses, tachycardia with moderate doses, hypertension, cardiomyopathy, cardiac arrhythmias, myocarditis, QRS prolongation, Raynaud's phenomenon, cerebral vasculitis, thrombosis, fibrillation (atrial), flutter (atrial), sinus bradycardia, congestive heart failure, pulmonary hypertension, sinus tachycardia, tachycardia (supraventricular), arrhythmias (ventricular), vasoconstriction

Central nervous system: Fever, nervousness, restlessness, euphoria, excitation, headache, psychosis, hallucinations, agitation, seizures, slurred speech, hyperthermia, dystonic reactions, cerebral vascular accident, vasculitis, clonic-tonic reactions, paranoia, sympathetic storm

Dermatologic: Skin infarction, pruritus, madarosis

Gastrointestinal: Nausea, anorexia, colonic ischemia, spontaneous bowel perforation

Genitourinary: Priapism, uterine rupture

Hematologic: Thrombocytopenia

Neuromuscular & skeletal: Chorea (extrapyramidal), paresthesia, tremors, fasciculations

Ocular: Mydriasis (peak effect at 45 minutes; may last up to 12 hours), sloughing of the corneal epithelium, ulceration of the cornea, iritis, mydriasis, chemosis

Renal: Myoglobinuria, necrotizing vasculitis

Respiratory: Tachypnea, nasal mucosa damage (when snorting), hyposmia, bronchiolitis obliterans organizing pneumonia

Miscellaneous: "Washed-out" syndrome

Symptoms of overdose include anxiety, excitement, confusion, nausea, vomiting, headache, rapid pulse, irregular respiration, delirium, fever, seizures, respiratory arrest, hallucinations, dilated pupils, muscle spasms, sensory aberrations, cardiac arrhythmias

Fatal dose: Oral: 500 mg to 1.2 g; severe toxic effects have occurred with doses as low as 20 mg

Since no specific antidote for cocaine exists, serious toxic effects are treated symptomatically. Maintain airway and respiration. Attempt delay of absorption (if ingested) with activated charcoal, gastric lavage or emesis. Seizures are treated with diazepam while propranolol or labetalol may be useful for life-threatening arrhythmias, agitation, and/or hypertension.

CYP3A3/4 enzyme substrate

Sympathomimetic amines may cause malignant arrhythmias; avoid concurrent use.

Store in well closed, light-resistant containers

Ester local anesthetic blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction; interferes with the uptake of norepinephrine by adrenergic nerve terminals producing vasoconstriction

Following topical administration to mucosa:

Peak action: Within 5 minutes

Duration: greater than or equal to 30 minutes, depending on dosage administered

Absorption: Well absorbed through mucous membranes; limited by drug-induced vasoconstriction; enhanced by inflammation

Distribution: Appears in breast milk

Metabolism: In the liver; major metabolites are ecgonine methyl ester and benzoyl ecgonine

Half-life: 75 minutes

Elimination: Primarily in urine as metabolites and unchanged drug (<10%); cocaine metabolites may appear in the urine of neonates for up to 5 days after birth due to maternal cocaine use shortly before birth

Dosage depends on the area to be anesthetized, tissue vascularity, technique of anesthesia, and individual patient tolerance; use the lowest dose necessary to produce adequate anesthesia should be used, not to exceed 1 mg/kg. Use reduced dosages for children, elderly, or debilitated patients.

Vital signs

Therapeutic: 100-500 ng/mL (SI: 330 nmol/L); Toxic: >1000 ng/mL (SI: >3300 nmol/L)

The prevalence of cocaine-induced cardiovascular events is increasing due to recreational use of cocaine. While cocaine is arrhythmogenic, it is also a potent vasospastic agent and may induce marked increases in blood pressure. In young patients presenting with acute myocardial infarction or with severe chest pain with EKG changes suggestive of ischemia, the possibility of antecedent cocaine use should be considered. Alpha blockade may be an option in treating cocaine-induced coronary artery spasm. There is some evidence that the vasospastic effects of cocaine may be enhanced when the drug is used in association with nicotine consumption. Cocaine may also be associated with cerebral vascular accidents in young patients without any previous risk factors.

CNS stimulation is common; may cause exacerbation of psychosis, nervousness, euphoria, restlessness, hallucinations, paranoia

Concurrent use with MAOIs may result in hypertensive crisis

Although plain local anesthetic is not contraindicated, vasoconstrictor is absolutely contraindicated in any patient under the influence of or within 2 hours of cocaine use

See Comments

When used orally, do not take anything by mouth until full sensation returns. Ocular: Use caution when driving or engaging in tasks that require alert vision (mydriasis may last for several hours). At time of use or immediately thereafter, report any unusual cardiovascular, CNS, or respiratory symptoms immediately. Following use, report skin irritation or eruption; alterations in vision, eye pain or irritation; persistent gastrointestinal effects; muscle or skeletal tremors, numbness, or rigidity; urinary or genital problems; or persistent fatigue. When used orally, do not take anything by mouth until full sensation returns. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not breast-feed.

Use only on mucous membranes of the oral, laryngeal, and nasal cavities, do not use on extensive areas of broken skin

Powder, as hydrochloride: 5 g, 25 g

Solution, topical:

As hydrochloride: 4% [40 mg/mL] (2 mL, 4 mL, 10 mL); 10% [100 mg/mL] (4 mL, 10 mL)

Viscous, as hydrochloride: 4% [40 mg/mL] (4 mL, 10 mL); 10% [100 mg/mL] (4 mL, 10 mL)

Tablet, soluble, for topical solution, as hydrochloride: 135 mg

Beckman KJ, Parker RB, Hariman RJ, et al, "Hemodynamic and Electrophysiological Actions of Cocaine. Effects of Sodium Bicarbonate as an Antidote in Dogs," Circulation, 1991, 83(5):1799-807.

Brogan WC 3d, Lange RA, Glamann DB, et al, "Recurrent Coronary Vasoconstriction Caused by Intranasal Cocaine; Possible Role for Metabolites," Ann Intern Med, 1992, 116(7):556-61.

Chasnoff IJ, Lewis DE, and Squires L, "Cocaine Intoxication in Breast-Fed Infants," Pediatrics, 1987, 80(6):836-8.

Fritsma GA, Leikin JB, Maturen AJ, et al, "Detection of Anticardiolipin Antibody in Patients With Cocaine Abuse," J Emerg Med, 1991, 9(Suppl 1):37-43.

Greenglass EJ, "The Adverse Effects of Cocaine on the Developing Human," Yaffe SJ and Arana JV, eds, Pediatric Pharmacology: Therapeutic Principles in Practice, 2nd ed, Philadelphia, PA: WB Saunders Co, 1992, 598-604.

Hollander JE, Burstein JL, Hoffman RS, et al, "Cocaine-Associated Myocardial Infarction," Chest, 1995, 107(5):1237-41.

Kain ZN, Kain TS, and Scarpelli EM, "Cocaine Exposure in Utero: Perinatal Development and Neonatal Manifestations - Review," Clin Toxicol, 1992, 30:607-36.

Nicholson KE and Rogers JE, "Cocaine and Adrenaline Paste: A Fatal Combination?" Br Med J, 1995, 311(6999):250-1.

Richards CF, Clark RF, Holbrook T, et al, "The Effect of Cocaine and Amphetamines on Vital Signs in Trauma Patients," J Emerg Med, 1995, 13(1):59-63.

Shannon RP, Manders WT, and Shen YT, "Role of Blood Doping in the Coronary Vasoconstrictor Response to Cocaine," Circulation, 1995, 92(1):96-105.

Trabulsy ME, "Cocaine Washed Out Syndrome in a Patient With Acute Myocardial Infarction," Am J Emerg Med, 1995, 13(5):538-9.