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Cocaine Hydrochloride Topical Solution, 4% and 10%

DEA Controlled Substance Schedule C-II

Disclaimer: This drug has not been found by FDA to be safe and effective, and this labeling has not been approved by FDA

NOT FOR INJECTION OR OPHTHALMIC USE

TABLE OF CONTENTS

1. DESCRIPTION 8. ADVERSE REACTIONS
2. INDICATIONS AND USAGE 9. DRUG ABUSE AND DEPENDENCE
3. DOSAGE AND ADMINISTRATION 10. OVERDOSAGE
4. CONTRAINDICATIONS 11. DRUG INTERACTIONS
5. MECHANISM OF ACTION 12. PHARMACOKINETICS
6. USE IN SPECIFIC POPULATIONS 13. HOW SUPPLIED/STORAGE AND HANDLING
7. WARNINGS AND PRECAUTIONS  

 

1. DESCRIPTION

Cocaine hydrochloride, or ecgonine methyl ester benzoate hydrochloride, is an alkaloid ester extracted from the leaves of plants including coca. Cocaine hydrochloride has the following structural formula:

C17H21NO4•HCl

Molecular Weight 339.81

Each mL contains: Cocaine hydrochloride 40 mg (4%) or 100 mg (10%) as aqueous solution.

The topical solution contains the following inactive ingredients: citric acid, D&C Yellow No. 10, FD&C Green No. 3, sodium benzoate, and water.

NOTE (for Glass Bottle): External surface of unopened bottle may be sterilized by ethylene oxide only. Do not steam autoclave. Cocaine hydrochloride USP is a crystalline, granular, or powder substance having a saline, slightly bitter taste that numbs tongue and lips. Cocaine hydrochloride is a local anesthetic.

2. INDICATIONS AND USAGE

Cocaine hydrochloride topical solution is a local (topical) anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse.

3. DOSAGE AND ADMINISTRATION

The dosage varies and depends upon the area to be anesthetized, vascularity of the tissues, individual tolerance, and the technique of anesthesia. The lowest dosage needed to provide effective anesthesia should be administered. Dosages should be reduced for children and for elderly and debilitated patients. Cocaine hydrochloride topical solution can be administered by means of cotton applicators or packs, instilled into a cavity, or as a spray.

4. CONTRAINDICATIONS

Cocaine hydrochloride is contraindicated in patients with a known history of hypersensitivity to the drug or to the components of the topical solution.

5. MECHANISM OF ACTION

Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake

6. USE IN SPECIFIC POPULATIONS

6.1 Usage in Pregnancy

Pregnancy Category C

Animal reproduction studies have not been conducted with cocaine. It is also not known whether cocaine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Cocaine should be given to a pregnant woman only if needed.

7. WARNINGS AND PRECAUTIONS

WARNINGS

RESUSCITATIVE EQUIPMENT AND DRUGS SHOULD BE IMMEDIATELY AVAILABLE WHEN ANY LOCAL ANESTHETIC IS USED.

PRECAUTIONS

The safety and effectiveness of cocaine hydrochloride topical solution depends on proper dosage, correct technique, adequate precautions, and readiness for emergencies. Standard textbooks should be consulted for specific techniques and precautions for various anesthetic procedures.

The lowest dosage that results in effective anesthesia should be used to avoid high plasma levels and serious adverse effects.

Debilitated, elderly patients, acutely ill patients, and children should be given reduced doses commensurate with their age and physical status.

Cocaine hydrochloride topical solution should be used with caution in patients with severely traumatized mucosa and sepsis in the region of the proposed application. Use with caution in persons with known drug sensitivities.

8. ADVERSE REACTIONS

Adverse reactions may be due to high plasma levels as a result of excessive and rapid absorption of the drug. Reactions are systemic in nature and involve the central nervous system and/or the cardiovascular system. A small number of reactions may result from hypersensitivity, idiosyncrasy or diminished tolerance on the part of the patient.

CNS reactions are excitatory and/or depressant, and may be characterized by nervousness, restlessness and excitement. Tremors and eventually clonic-tonic convulsions may result. Emesis may occur. Central stimulation is followed by depression, with death resulting from respiratory failure.

Small doses of cocaine slow the heart rate, but after moderate doses, the rate is increased due to central sympathetic stimulation. Cocaine is pyrogenic, augmenting heat production in stimulating muscular activity and causing vasoconstriction which decreases heat loss. Cocaine is known to interfere with the uptake of norepinephrine by adrenergic nerve terminals, producing sensitization to catecholamines, causing vasoconstriction and mydriasis.

Cocaine causes sloughing of the corneal epithelium, causing clouding, pitting, and occasionally ulceration of the cornea. The drug is not meant for ophthalmic use.

9. DRUG ABUSE AND DEPENDENCE

9.1 Controlled Substance

Cocaine hydrochloride is an opioid agonist and is a Schedule II controlled substance. Cocaine hydrochloride can be abused and is subject to criminal diversion.

9.2 Abuse

Drug addiction is characterized by compulsive use, use for non-medical purposes, and continued use despite harm or risk of harm. Drug addiction is a treatable disease, utilizing a multi-disciplinary approach, but relapse is common.

“Drug seeking” behavior is very common in addicts and drug abusers. Drug-seeking tactics include emergency calls or visits near the end of office hours, refusal to undergo appropriate examination, testing or referral, repeated “loss” of prescriptions, tampering with prescriptions and reluctance to provide prior medical records or contact information for other treating physician(s). “Doctor shopping” to obtain additional prescriptions is common among drug abusers and people suffering from untreated addiction.

Abuse and addiction are separate and distinct from physical dependence and tolerance. Physicians should be aware that addiction may not be accompanied by concurrent tolerance and symptoms of physical dependence. The converse is also true. In addition, abuse of opioids can occur in the absence of true addiction and is characterized by misuse for nonmedical purposes, often in combination with other psychoactive substances. Careful record-keeping of prescribing information, including quantity, frequency, and renewal requests is strongly advised.

Cocaine hydrochloride topical solution is intended for local (topical) use only. Abuse of cocaine poses a risk of overdose and death. The risk is increased with concurrent abuse of alcohol and other substances. Parenteral drug abuse is commonly associated with transmission of infectious diseases such as hepatitis and HIV.

Proper assessment of the patient, proper prescribing practices, periodic re-evaluation of therapy, and proper dispensing and storage are appropriate measures that help to limit abuse of opioid drugs.

Infants born to mothers physically dependent on opioids will also be physically dependent and may exhibit respiratory difficulties and withdrawal symptoms. [see Use in Specific Populations].

10. OVERDOSAGE

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.

Symptoms

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 is rapid in developing.

Treatment

The specific treatment of acute cocaine poisoning is the intravenous administration of a short-acting barbiturate or diazepam. Artificial respiration may be necessary. It is important to limit absorption of the drug. If entrance of the drug into circulation can be checked, and respiratory exchange maintained, the prognosis is favorable since cocaine is eliminated fairly rapidly.

11. DRUG INTERACTIONS

No drug interaction information is available.

12. PHARMACOKINETICS

No pharmacokinetic information is available.

13. HOW SUPPLIED/STORAGE AND HANDLING

1) How Available:

a) Brand name: COCAINE HYDROCHLORIDE, by LANNETT CO.

b) Generic drugs: None.

2) How Supplied:

4% Cocaine Hydrochloride Topical Solution, clear, blue-green solution.

NDC 0527-1728-74: Unit-of-Use Glass Bottle filled to contain 4 mL, one 4 mL bottle per carton.

NDC 0527-1728-73: Multi-Dose Bottle of 10 mL.

10% Cocaine Hydrochloride Topical Solution, clear, blue-green solution.

NDC 0527-1729-74: Unit-of-Use Glass Bottle filled to contain 4 mL, one 4 mL bottle per carton.

NDC 0527-1729-73: Multi-Dose Bottle of 10 mL.

DEA Order Form Required.

3) Storage:

Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature].

Avoid freezing.

Keep out of reach of children.

Rx only

Rev 03/08