cocaine

Cocaine is an ester anesthetic used topically to numb the mucous membranes of the oral, nasal and laryngeal cavities during procedures or surgeries in or through the nasal cavities.

Cocaine also constricts blood vessels locally, and is sometimes used off-label to stop nasal bleeding temporarily, before cauterization or packing. Other than its only approved clinical use, cocaine is abused and misused illegally because of its central nervous system (CNS) effects.

Cocaine produces anesthesia by blocking the conduction of signals in the nerve fibers. Cocaine blocks the sodium channels in the nerve cells (neurons), preventing sodium influx and generation of action potential. It also increases the levels of the neurotransmitter norepinephrine by preventing its uptake by nerve terminals. Norepinephrine makes the smooth muscles around blood vessels contract, producing vasoconstriction.

Systemic absorption of topical cocaine has effects on the cardiovascular system, increasing the heart rate and force of contraction, and peripheral vasoconstriction increases blood pressure. CNS stimulation increases dopamine, serotonin, and norepinephrine levels and produces euphoria and the potential for addiction. Cocaine’s topical anesthetic effect may last up to an hour depending on the concentration and dosage of the drug and the patient’s mucosal integrity. Systemic effects depend on the extent of systemic absorption.

• Do not use topical cocaine in patients who are hypersensitive to any of its components.
• CNS stimulants, including cocaine, have a high potential for abuse and can be diverted to illicit nonmedical uses. In order to minimize these risks, effective accounting procedures should be implemented, in addition to routine procedures for handling controlled substances.
• Cocaine increases  heart rate and blood pressure. Monitor vital signs in patients.
• Avoid use in patients with a history of cardiac conditions including:
  • Heart attack (myocardial infarction)
  • Coronary artery disease (CAD)
  • Congestive heart failure (CHF)
  • Abnormal ECG
  • Irregular heart rhythm (arrhythmia)
  • Uncontrolled high blood pressure (hypertension)
• Cocaine may lower seizure threshold. The risk of seizures may be higher in patients with a history of seizure or EEG abnormality without seizure, however, convulsions have been reported even in patients without a prior history or abnormal EEG. Monitor the patient for development of seizures.
• Do not use topical cocaine in pregnant women. Check pregnancy status before treating patients with pregnancy potential.
• Do not use topical cocaine for ophthalmic purposes, it can damage the cornea.
• Cocaine and its metabolites may be detected in the plasma and urine for up to a week.
• Avoid use of topical cocaine concurrently with:
  • CNS stimulants
  • Vasoconstricting agents
  • Drugs that increase levels of dopamine, serotonin and norepinephrine
  • Tricyclic and monoamine oxidase inhibitor (MAOI) antidepressants

Common side effects from systemic absorption of cocaine include:

• High blood pressure (hypertension)
• Rapid heart rate (tachycardia)
• Sinus tachycardia
• Slow heart rate (bradycardia)
• ECG abnormalities including:
  • Prolonged QT interval
  • Prolonged QRS duration
• Irregular heart rhythm (arrhythmia) in the atria and ventricles
• Impaired blood flow to the heart muscles (myocardial ischemia)
• Heart attack (myocardial infarction)
• Headache
• Nasal bleeding (epistaxis)
• Anxiety
• Tremor

Call your doctor immediately if you experience any of the following symptoms or serious side effects while using this drug:

• Serious heart symptoms include fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness;
• Severe headache, confusion, slurred speech, severe weakness, vomiting, loss of coordination, feeling unsteady;
• Severe nervous system reaction with very stiff muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, and feeling like you might pass out; or
• Serious eye symptoms include blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

Adult:

Topical Solution: Schedule II

• 4% (40 mg/mL)
• 10% (100 mg/mL)

Intranasal Solution: Schedule II

• 4% (Goprelto, Numbrino)

Nasal Cavity Anesthesia

Numbrino or Goprelto

• Indicated for induction of local anesthesia of the mucous membranes when performing diagnostic procedures and surgeries on or through the nasal cavities in adults
• Dose ranges from 40-160 mg, depending on nasal mucosal area to be anesthetized and the procedure to be performed
• A maximum of 2 soaked cotton or rayon pledgets may be placed in each nasal cavity, for a total dose of 160 mg (4% solution)
• Not to exceed 3 mg/kg for any 1 procedure or surgery

Mucous Membrane Anesthesia

• Indicated for local (topical) anesthesia for accessible mucous membranes of the oral, nasal, and laryngeal cavities
• 1-10% solution: Use lowest dose necessary to produce adequate anesthesia
• Do not exceed 3 mg/kg or 300 mg

Dosage Modifications

Hepatic impairment

• Insufficient data available to guide dosing
• Since cocaine is eliminated predominantly by metabolism, avoid in patients with hepatic impairment

Renal impairment

• Eliminated predominantly by metabolism, with little excreted unchanged in urine
• Not studied; titrate dose conservatively

Dosing Considerations

• Dosage variables include tissue vascularity, anesthetic technique and patient tolerance
• Reduce dose for elderly or debilitated patients

Pediatric:

Topical Solution: Schedule II

• 4% (40 mg/mL)

Mucous Membrane Anesthesia

• Indicated for local (topical) anesthesia of accessible mucous membranes of the oral, nasal, and laryngeal cavities
• Use lowest possible effective dose; solutions stronger than 4% not recommended because of increased risk/severity of toxicity

Dosing Considerations

• Dosage variables include tissue vascularity, anesthetic technique and patient tolerance

• Cocaine topical is used in clinical settings for anesthesia and there are no reports of overdose.
• Cocaine is a highly addictive substance, and misuse/abuse of cocaine can lead to dependence, addiction, overdose, convulsions, unconsciousness, coma and death.
• Cocaine overdose treatment is symptomatic and supportive care.

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

• Severe Interactions of cocaine include:
  • eliglustat
  • iobenguane I 123
• Serious Interactions of cocaine include:
  • abametapir
  • apalutamide
  • bupivacaine implant
  • citalopram
  • desvenlafaxine
  • fexinidazole
  • idelalisib
  • iobenguane I 131
  • isocarboxazid
  • linezolid
  • lonafarnib
  • lorcaserin
  • methylene blue
  • metoclopramide intranasal
  • phenelzine
  • procarbazine
  • pseudoephedrine
  • tranylcypromine
  • tucatinib
  • vilazodone
  • vortioxetine
  • voxelotor
• Cocaine has moderate interaction with at least 92 different drugs.
• Cocaine has mild interactions with at least 33 different drugs.

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.

• Topical cocaine may cause fetal harm, do not use in pregnant women.
• Cocaine is present in breast milk. Do not breastfeed during treatment. Pump and discard the breast milk for 48 hours after administration of topical cocaine.

• Cocaine is a Schedule II controlled substance, diversion of Schedule II products is subject to criminal penalty.
• Do not use cocaine for nonmedical purposes, it can lead to abuse, misuse, addiction, dependence and overdose that can be fatal.
• In case of overdose, seek immediate medical help or call Poison Control.
• If you are pregnant or suspect pregnancy, inform your doctor prior to ENT procedures that may require the use of cocaine as a topical anesthetic.
• Topical cocaine can increase heart rate and blood pressure. If these symptoms persist, notify your healthcare provider.
• Seek immediate medical help if you experience any hypersensitivity reactions.