Cocaine

Cocaine naturally occurring chemical found in the leaves of Erythroxylum coca or coca plant. Cocaine is a highly addictive stimulant drug that directly affects the nervous system, including the brain. Risk for addiction is a common problem which prevents widespread clinical use. Powder cocaine (commonly referred to as coke), freebase and crack (crack cocaine) are all forms of the cocaine substance. Cocaine may also be used as a topical anesthetic is indicated for the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities.

Cocaine is available under the following different brand names: Cocaine topical.

Dosage Forms & Strengths

• 4% (pediatric and adult strength)
• 10%

Dosage Considerations for Topical Anesthesia

As local anesthetic for accessible mucous membranes (oral, nasal and laryngeal)

1-10% solution: Use lowest dose necessary to produce adequate anesthesia.

Do not exceed 3 mg/kg or 300 mg.

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

Reduce dose for elderly or debilitated patients.

Administration

Administer using cotton applicators or packs, instilled into a cavity, or as a spray.

Apply only on mucous membranes of mouth, laryngeal, or nasal cavities.

The fatal dose of cocaine has been approximated at 1.2 g., although severe toxic effects have been reported from doses as low as 20 mg.

Overdose

The symptoms of cocaine poisoning are referable to the CNS, namely the patient becomes excited, restless, garrulous, anxious and confused. Enhanced reflexes, headache, rapid pulse, irregular respiration, chills, rise in body temperature, mydriasis, exophthalmos, nausea, vomiting and abdominal pain are noticed. In severe overdoses, delirium, Cheyne-Stokes respiration, convulsions, unconsciousness, and death from respiratory arrest result. Acute poisoning by cocaine develops rapidly in time.

Common side effects associated with using cocaine include:

• Anxiety
• Apprehension
• Restlessness
• Nervousness
• Disorientation
• Excitement
• Confusion
• Restlessness
• Tremors, and possibly tonic-clonic convulsions
• Respiratory arrest
• Nausea
• Vomiting
• Chills
• Constricted pupils
• Ringing in the ears (tinnitus)
• Myocardial depression
• Slow heart rate
• Cardiac arrhythmias
• Low blood pressure (hypotension)
• Cardiovascular collapse
• Cardiac arrest
• Palpitation
• Fast heart rate
• Chest pain (angina)
• High blood pressure (epinephrine-containing solutions)
• Sloughing of corneal epithelium (eg, pitting, clouding, corneal ulceration)
• Serious toxic effects (eg, seizures, cardiac death) have been described following topical cocaine application used to anesthetize minor skin lacerations, especially on the face or scalp (eg, TAC [tetracaine 0.5%, epinephrine (Adrenalin) 1:2000, and cocaine 11.8%]); this risk is greater in pediatrics
• Coronary arteriosclerosis
• Irregular heart rate
• Seizure
• Swelling (edema)
• Asthma attacks
• Severe allergic reactions (anaphylaxis, sometimes fatal)

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring your health for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first. Alcohol should be avoided while using this drug.

Severe Interactions of Cocaine inlcude:

• Eliglustat
• Iobenguane I 123

Serious Interactions of Cocaine inlcude:

• Citalopram
• Desvenlafaxine
• Idelalisib
• Isocarboxazid
• Ivacaftor
• Linezolid
• Lorcaserin
• Methylene blue
• Phenelzine
• Procarbazine
• Tranylcypromine
• Vilazodone
• Vortioxetine

Moderate Interactions of Cocaine: Cocaine has a known moderate interaction with at least 73 different drugs.

Minor Interactions of Cocaine: Cocaine has mild interactions with at least 32 different drugs.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

This medication contains cocaine. Do not take cocaine if you are allergic to cocaine or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

Hypersensitivity to ester-type local anesthetics, para-aminobenzoic acid (PABA), or parabens
Ophthalmologic anesthesia (causing sloughing of the corneal epithelium)

Effects of Drug Abuse

None.

Short-Term Effects

None.

Long-Term Effects

User may develop tolerance if this drug is used as a sedative/hypnotic.

Cautions

Do not administer parenterally or apply to eye.

Do not dilute with epinephrine for topical application as "cocaine mud."

Serious toxic effects (eg, seizures, cardiac death) have been described in people following topical cocaine application used to anesthetize minor skin lacerations, especially on the face or scalp (eg, TAC [tetracaine 0.5%, epinephrine (Adrenalin) 1:2000, and cocaine 11.8%]); this risk is greater in pediatrics.

Use caution in patients with cardiovascular disease.

Avoid beta-blocker use when patients are being treated for cardiovascular complications caused by cocaine abuse.

Pregnancy and Lactation

Use cocaine with caution during pregnancy if prescribed and benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. Do not use cocaine during pregnancy for non-medicinal use. Cocaine enters breast milk; use while breastfeeding is contraindicated.