GOPRELTO

GOPRELTO- cocaine hydrochloride solution
Genus Lifesciences Inc.

WARNING: ABUSE AND DEPENDENCE

CNS stimulants, including cocaine hydrochloride, have a high potential for abuse and dependence [see Warnings and Precautions (5.1).

1 INDICATIONS AND USAGE

GOPRELTO (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.

2 DOSAGE AND ADMINISTRATION

2.1 Important Dosage and Administration Instructions

  • GOPRELTO is for intranasal use only.
  • Do not apply GOPRELTO to damaged nasal mucosa.

2.2 Dosing Recommendation for Adults

The recommended dose of GOPRELTO is two soaked cottonoid pledgets placed in each nasal cavity, equivalent to 40 mg cocaine hydrochloride per pledget, for a total dose of 160 mg for four pledgets.

The total dose for any one procedure or surgery should not exceed 160 mg, or 3 mg/kg, cocaine hydrochloride.

The recommended size of cottonoid pledgets for use with GOPRELTO measure 1.3 cm × 4 cm (sold separately).

2.3 Preparation and Administration of GOPRELTO Pledgets

Pour the full contents of one 4 mL (160 mg) bottle of GOPRELTO into a small container. Soak four cottonoid pledgets until the solution is fully absorbed.

Following soaking, place two pledgets in each nasal cavity against the septum.

Leave pledgets in place for up to twenty minutes. Remove pledgets and continue with the procedure. Discard pledgets and dispose of any unused portion of solution in accordance with institutional procedures for CII products.

3 DOSAGE FORMS AND STRENGTHS

GOPRELTO (cocaine hydrochloride) nasal solution is provided as a 4% solution, 160 mg/4 mL (40 mg/mL), equivalent to 142.4 mg/4mL (35.6 mg/mL) cocaine free-base, and is a clear, green-colored solution in a single-use bottle.

4 CONTRAINDICATIONS

GOPRELTO is contraindicated in patients with a known history of hypersensitivity to cocaine hydrochloride, other ester-based anesthetics, or any other component of the product.

5 WARNINGS AND PRECAUTIONS

5.1 Potential for Abuse and Dependence

Central nervous system (CNS) stimulants, including cocaine hydrochloride, have a high potential for abuse and dependence [see Drug Abuse and Dependence (9.2, 9.3)].

5.2 Seizures

It has been reported in the literature that cocaine hydrochloride may lower the convulsive threshold. The risk may be higher in patients with a history of seizures or in patients with prior electroencephalogram (EEG) abnormalities without seizures, but has been reported in patients with no prior history or EEG evidence of seizures. Monitor patients for development of seizures.

5.3 Blood Pressure and Heart Rate Increases

As reported in the literature, cocaine hydrochloride causes an increase in observed blood pressure and heart rate. In the Phase 3 clinical study with GOPRELTO, increases in blood pressure and heart rate were observed for 60 minutes or longer following pledget removal. Monitor for vital sign changes, including heart rate and rhythm, after administration of GOPRELTO.

Avoid use of GOPRELTO in patients with a recent or active history of uncontrolled hypertension, unstable angina, myocardial infarction, coronary artery disease, or congestive heart failure. Avoid use of additional vasoconstrictor agents such as epinephrine or phenylephrine with GOPRELTO. If concomitant use is unavoidable, prolonged vital sign and ECG monitoring may be required [see Drug Interactions (7)].

5.4 Toxicology Screening

The cocaine hydrochloride in GOPRELTO may be detected in plasma for up to one week after administration. Cocaine hydrochloride and its metabolites may be detected in urine toxicology screening for longer than one week after administration.

6 ADVERSE REACTIONS

6.1 Clinical Trial Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

GOPRELTO has been evaluated in four Phase 1 studies and one Phase 3 study, which included 647 adult subjects who received a single topical intranasal 160 mg dose (four pledgets), of GOPRELTO. The randomized, double-blind, controlled Phase 3 study was conducted in adult patients undergoing diagnostic procedures and surgeries on or through the mucous membranes of the nasal cavities, of which 278 received GOPRELTO (4% solution), 275 received cocaine hydrochloride solution 8%, and 95 received placebo. Safety was evaluated for up to 7 days after dosing.

The most commonly reported adverse reactions (>1 patient) to occur in the Phase 3 study with GOPRELTO (4% solution) were headache and epistaxis. Two adverse reactions of headache were severe (Table 1).

No premature discontinuations due to an adverse event, serious adverse events, or deaths were reported in the Phase 3 clinical study.

Table 1: Common Adverse Reactions with GOPRELTO in > 1 Patient
System Organ Class / Preferred Term GOPRELTO 4%(N=278) Cocaine Hydrochloride Solution 8%(N=275) Placebo(N=95)
Nervous System Disorders
Headache 7 (3%) 4 (2%) 1 (1%)
Respiratory, Thoracic, and Mediastinal Disorders
Epistaxis 3 (1%) 2 (1%) 0
Psychiatric Disorders
Anxiety 0 2 (1%) 0

7 DRUG INTERACTIONS

7.1 Disulfiram

Published literature reported that disulfiram treatment increased plasma cocaine exposure, including both AUC and Cmax , by several fold after acute intranasal cocaine administration. Other literature reported that co-administration of disulfiram increased AUC of plasma cocaine by several fold after intravenous cocaine administration [see Clinical Pharmacology (12.3)].

Avoid using GOPRELTO in patients taking disulfiram. Consider using other local anesthetic agents.

7.2 Epinephrine, Phenylephrine

There are reports in the published literature of myocardial ischemia, myocardial infarction, and ventricular arrhythmias after concomitant administration of topical intranasal cocaine with epinephrine and phenylephrine during nasal and sinus surgery.

Avoid use of additional vasoconstrictor agents such as epinephrine and phenylephrine with GOPRELTO during nasal and sinus surgery. If concomitant use is unavoidable, prolonged vital sign and ECG monitoring may be required [see Warnings and Precautions (5.3)].

7.3 Inhibitors of plasma cholinesterase (pseudocholinesterase)

Cocaine has been described in literature to be primarily metabolized and inactivated by nonenzymatic ester hydrolysis and hepatic carboxylesterase, and also by plasma cholinesterase, hepatic carboxylesterase, and CYP3A4 [see Clinical Pharmacology (12.3)]. The pharmacokinetics of GOPRELTO in patients with reduced plasma cholinesterase activity has not been studied.

Plasma cholinesterase activity may be decreased by chronic administration of certain monoamine oxidase inhibitors, oral contraceptives, or glucocorticoids. It may also be diminished by administration of irreversible plasma cholinesterase inhibitors such as echothiophate, organophosphate insecticides, and certain antineoplastic agents. Patients with reduced plasma cholinesterase (pseudocholinesterase) activity may have reduced clearance and increased exposure of plasma cocaine after administration of GOPRELTO.

Since cocaine is metabolized by multiple enzymes, the effect of reduced plasma cholinesterase activity on cocaine exposure may be limited. No dosage adjustment of GOPRELTO is needed in patients with reduced plasma cholinesterase. Monitor patients with reduced plasma cholinesterase activity for adverse reactions such as headache, epistaxis, and clinically-relevant increases in heart rate or blood pressure.

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