FDA

Goprelto

Approved 14 Dec 2017NasalSolution

Indications

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. GOPRELTO (cocaine hydrochloride) nasal solution is an ester local anesthetic 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.

( 1 )

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. Known hypersensitivity to cocaine hydrochloride, other ester-based anesthetics, or any other component of GOPRELTO. ( 4 )

Warnings and precautions

Seizures : GOPRELTO may lower the convulsive threshold. Monitor patients for development of seizures. ( 5.2 )
Blood Pressure and Heart Rate Increases : Monitor vital signs, including heart rate and rhythm, in patients after receiving 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. ( 5.3 )

5.1Potential 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 )].

5.2Seizures

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.

5.3Blood 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.

At a glance

Brand name: Goprelto
Active substance: cocaine hydrochloride
Route: Nasal
Dosage form: Solution
Applicant: Lxo Ireland
Status: Prescription
FDA approval: 14 Dec 2017
Application: NDA209963-001

Indications

( 1 )

Warnings and precautions

Seizures : GOPRELTO may lower the convulsive threshold. Monitor patients for development of seizures. ( 5.2 )
Blood Pressure and Heart Rate Increases : Monitor vital signs, including heart rate and rhythm, in patients after receiving 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. ( 5.3 )

5.1Potential 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 )].

5.2Seizures

5.3Blood Pressure and Heart Rate Increases

Interactions

Disulfiram : Increases plasma cocaine exposure. Avoid using GOPRELTO in patients taking disulfiram. ( 7 )
Epinephrine, Phenylephrine : There have been reports of myocardial ischemia, myocardial infarction, and ventricular arrhythmias with concomitant use during nasal surgery. Avoid use of additional vasoconstrictor agents with GOPRELTO. If concomitant use is unavoidable, prolonged vital sign and ECG monitoring may be required. ( 5.3 , 7 )

7.1Disulfiram

Published literature reported that disulfiram treatment increased plasma cocaine exposure, including both AUC and C max , 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.

7.2Epinephrine, 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 ) ].

7.3Inhibitors

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.

Goprelto

Indications

Contraindications

Warnings and precautions

5.1Potential for Abuse and Dependence

5.2Seizures

5.3Blood Pressure and Heart Rate Increases

At a glance

Two medicines in one question?

Goprelto

Indications

Contraindications

Warnings and precautions

5.1Potential for Abuse and Dependence

5.2Seizures

5.3Blood Pressure and Heart Rate Increases

At a glance

Two medicines in one question?

5.4Toxicology Screening

Interactions

7.1Disulfiram

7.2Epinephrine, Phenylephrine

7.3Inhibitors

Adverse reactions

6.1Clinical Trial Experience

Composition

Official product information