Classifications: anesthetic, local; Therapeutic:topical anesthetics
Pregnancy Category: C
Controlled Substance: Schedule II
4%, 10% topical solution
Alkaloid obtained from leaves of Erythroxylon coca. Topical application blocks nerve conduction and produces surface anesthesia accompanied by local vasoconstriction. Exerts
adrenergic effect by potentiating action of endogenous (and injected) epinephrine and norepinephrine, possibly by inhibiting
reuptake of catecholamines into sympathetic nerve terminals. Topical form of cocaine is a local anesthetic.
Systemic absorption produces descending CNS stimulation, with intense, short-lived euphoria accompanied by indifference
to pain or hunger and with illusions of great strength, endurance, and mental capacity, all the basis for drug abuse.
Surface anesthesia of ear, nose, throat, rectum, and vagina. Ophthalmic use largely abandoned because of its tendency to
cause corneal sloughing. Sometimes used as ingredient in Brompton's cocktail.
Hypersensitivity to local anesthetics; sepsis in region of proposed application; acute MI, history of cardiac arrhythmias,
cardiac disease; seizures or seizure disorders; thyrotoxicosis cerebrovascular disease; Tourette's syndrome; MAOI therapy;
pregnancy (category C), lactation.
History of drug sensitivities, history of drug abuse.
Route & Dosage
Adult: Topical 110% solution (use >4% solution with caution), max single dose of 1 mg/kg
- Exercise caution to ensure that drug is taken as prescribed.
- Preserve in tightly closed, light-resistant containers.
Adverse Effects (≥1%) Body as a Whole:
Formication ("cocaine bugs"), hypersensitivity reactions. CV:
Tachycardia, ventricular fibrillation, MI,
angina pectoris. GI:
Nausea, vomiting, anorexia, abdominal pain. CNS: CNS stimulation
and CNS depression (respiratory and circulatory failure). Respiratory: pneumonia
, lung damage (chronic cocaine smoking). Special Senses:
Runny nose, perforated nasal septum; clouding, pitting, and ulceration of cornea.
Interactions Drug: Epinephrine
entails risk of severe hypertension and arrhythmias; mao inhibitors
potentiate pharmacologic effects of cocaine.
Readily absorbed from mucous membranes; absorption limited by vasoconstriction. Onset:
1 min. Peak:
15120 min. Duration:
30 min2 h. Distribution:
Crosses placenta; distributed into breast milk. Metabolism:
Hydrolyzed in serum
In urine; detectable for up to 30 h. Half-Life:
Assessment & Drug Effects
- When used for anesthesia of throat, cocaine causes temporary paralysis of cilia of respiratory tract cells, reducing protection
against aspiration. It also may interfere with pharyngeal stage of swallowing. Give nothing by mouth until sensation returns.
- Monitor cardiovascular status, especially in patients with known cardiac disease. Report promptly cardiac arrhythmias.
Patient & Family Education
- Promptly report angina or chest pain or respiratory distress.