pharmacopeia
GET
/api/v1/drug/cocaine

Boxed warning

ABUSE AND DEPENDENCE CNS stimulants, including cocaine hydrochloride, have a high potential for abuse and dependence [see Warning and Precautions (5.1) . ] WARNING: ABUSE AND DEPENDENCE See full prescribing information for complete boxed warning. CNS stimulants, including cocaine hydrochloride, have a high potential for abuse and dependence. (5.1)

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Dopamine Uptake Inhibitors; Sodium Channel Interactions.

Dopamine Uptake

Indications

Sourced from openFDA
  • 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.

Contraindications

Sourced from openFDA
  • 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.contraindicated

Dosage & administration

Sourced from openFDA

• For intranasal use only. ( 2.1 ) • Recommended dose: two pledgets, each containing 40 mg of cocaine hydrochloride,applied to each nasal cavity. ( 2.2 ) • Do not apply to damaged nasal mucosa. ( 2.1 ) • Preparation and Application: – In a small container, soak four pledgets in the full contents (4 mL) of one bottle of GOPRELTO until the solution is fully absorbed. Each pledget absorbs 1 mL of solution, equivalent to 40 mg cocaine hydrochloride. ( 2.2 , 2.3 ) – Following soaking, place two pledgets in each nasal cavity against the septum. ( 2.3 ) – Leave pledgets in p lace for up to 20 minutes. ( 2.3 ) 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 x 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.

Warnings & precautions

Sourced from openFDA

• 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 ) 5.1 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.

Adverse reactions

Sourced from openFDA

The most common adverse reactions (>0.5%) occurring in patients treated with GOPRELTO (cocaine hydrochloride) nasal solution 4% were headache and epistaxis. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact LXO US., INC. at 1-844-800-8007 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 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.

Use in specific populations

Sourced from openFDA

• Pregnancy : May cause fetal harm. ( 8.1 ) • Lactation : Avoid breastfeeding for 48 hours after treatment. ( 8.2 ) • Hepatic Impairment : Monitor for adverse reactions such as headache, epistaxis, and clinically- relevant increases in heart rate or blood pressure. Do not administer a second dose within 24 hours of the first dose. ( 8.7 ) 8.1 Pregnancy Risk Summary In animal studies conducted in accordance with good laboratory practices, malformations including vertebral and rib abnormalities were reported when pregnant rabbits were treated with 16 mg/kg cocaine hydrochloride during organogenesis (8 times the adult human exposure following administration of pledgets containing 160 mg of cocaine) and increased pup mortality was noted when pregnant rats were exposed to cocaine hydrochloride during pregnancy at 47 times the adult human AUC exposures. Published rodent studies testing high exposures to cocaine during organogenesis report various malformations at 17 to 34 times the adult human AUC exposures following administration of pledgets containing 160 mg of cocaine. Data Human Data There are no available data on the use of intranasal cocaine hydrochloride solution in pregnant women to inform a drug-associated risk adverse developmental outcomes. There are published data describing adverse developmental outcomes in women with chronic cocaine abuse during pregnancy.

Overdosage

Sourced from openFDA

No cases of overdose with GOPRELTO were reported in clinical trials. Blood pressure and heart rate increases were greater with cocaine hydrochloride solution 8% than with GOPRELTO. In the case of an overdose, consult with a certified poison control center (1-800-222-1222) for up-to-date guidance and advice for treatment of overdosage. Individual patient response to cocaine varies widely. Toxic symptoms may occur idiosyncratically at low doses. Manifestations of cocaine overdose associated with illicit use of cocaine reported in literature and based on reports in FDA’s Adverse Events Reporting System (AERS) database include death, cardio-respiratory arrest, cardiac arrest, respiratory arrest, tachycardia, myocardial infarction, agitation, aggression, restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, panic states, hyperpyrexia, and rhabdomyolysis. Fatigue and depression usually follow the central nervous system stimulation. Other reactions include arrhythmias, hypertension or hypotension, circulatory collapse, nausea, vomiting, diarrhea, and abdominal cramps. Fatal poisoning is usually preceded by convulsions and coma.

Approval history

Sourced from openFDA
  • Dec 14, 2017NDANDA209963Lxo Ireland
  • Jan 10, 2020NDANDA209575Omnivium Pharms

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
406 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Completed Suicide9523%
  2. 2Cardiac Arrest9323%
  3. 3Respiratory Arrest8621%
  4. 4Toxicity To Various Agents6015%
  5. 5Drug Abuse5915%
  6. 6Product Use Issue409.9%
  7. 7Poisoning Deliberate389.4%
  8. 8Death297.1%
  9. 9Suicidal Ideation225.4%
  10. 10Suspected Suicide204.9%
  11. 11Drug Dependence194.7%
  12. 12Intentional Product Misuse194.7%
  13. 13Drug Interaction174.2%
  14. 14Pain174.2%
  15. 15Suicide Attempt174.2%

Literature

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Recent PubMed references pinned to Cocaine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 806 ClinicalTrials.gov registrations naming Cocaine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Cocaine work?
Mechanism-of-action classes: Dopamine Uptake Inhibitors; Sodium Channel Interactions.
What is Cocaine used for?
According to FDA labeling, Cocaine carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Cocaine?
Cocaine is classified as Analgesics and anesthetics, Anesthetics, local, Esters of benzoic acid, Local anesthetics, Dopamine Uptake Inhibitors, Sodium Channel Interactions, Decreased Sympathetic Norepinephrine Activity, Systemic Venous Vasoconstriction.
What are the brand names for Cocaine?
Cocaine is marketed under brand names including Goprelto, Numbrino.
What are the contraindications for Cocaine?
Cocaine labeling lists contraindications including: 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.. Always consult the full prescribing information and a clinician.
Note. Data for cocaine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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