Cocaine Hydrochloride (2 brand names, 1 dosage form, 1 route)
Available dosage forms: SOLUTION.
Routes of administration: NASAL.
Brand Names
- GOPRELTO
- NUMBRINO
Related Health Topics
Boxed Warning
WARNING: ABUSE AND DEPENDENCE CNS stimulants, including cocaine hydrochloride, have a high potential for abuse and dependence. (5.1)
Indications and Usage
NUMBRINO (cocaine hydrochloride) nasal solution is indicated for the induction of local anesthesia of the mucous membranes when performing diagnostic procedures and surgeries on or through the nasal cavities in adults.
Contraindications
NUMBRINO is contraindicated in: patients with a known history of hypersensitivity to cocaine hydrochloride, other ester-based local anesthetics, or any other component of the nasal solution [see Warnings and Precautions (5.5)].
Adverse Reactions
The following treatment-emergent adverse events are discussed in more detailed in other sections of the labeling: Increases in Blood Pressure and Heart Rate [see Warnings and Precautions (5.3)]
Mechanism of Action
Cocaine hydrochloride is a local anesthetic of the ester type. Cocaine hydrochloride prevents conduction in nerve fibers by reversibly blocking voltage-gated sodium channels and preventing the transient rise in sodium conductance necessary for generation of an action potential.
Overdosage
No cases of overdose with NUMBRINO were reported in clinical trials. Reported blood pressure and heart rate increases were greater with NUMBRINO nasal solution 10% than with NUMBRINO nasal solution 4%. In the case of an overdose, consult with a Certified Poison Control Center (1-800-222-1222) for up-to-date guidance and advice for treatment of overdosage. Individual patient response to cocaine varies widely. Toxic symptoms may occur idiosyncratically at low doses. Manifestations of cocaine overdose associated with illicit use of cocaine reported in literature and based on reports in FDA’s Adverse Events Reporting System (AERS) database include death, cardio-respiratory arrest, cardiac arrest, respiratory arrest, tachycardia, myocardial infarction, agitation, aggression, restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, panic states, hyperpyrexia, and rhabdomyolysis. Fatigue and depression usually follow the central nervous system stimulation. Other reactions include arrhythmias, hypertension or hypotension, circulatory collapse, nausea, vomiting, diarrhea, and abdominal cramps. Fatal poisoning is usually preceded by convulsions and coma. Because cocaine is significantly distributed to tissues and rapidly metabolized, dialysis and hemoperfusion are not effective. Acidification of the urine does not significantly enhance cocaine elimination.