cocaine (Rx)

Brand and Other Names:Cocaine topical, Goprelto, more...Numbrino
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

topical solution: Schedule II

  • 4% (40mg/mL)
  • 10% (100mg/mL)

intranasal solution: Schedule II

  • 4% (Goprelto, Numbrino)

Nasal Cavity Anesthesia

Numbrino or Goprelto

  • Indicated for induction of local anesthesia of the mucous membranes when performing diagnostic procedures and surgeries on or through the nasal cavities in adults
  • Dose ranges from 40-160 mg, depending on nasal mucosal area to be anesthetized and the procedure to be performed
  • A maximum of 2 soaked cotton or rayon pledgets may be placed in each nasal cavity, for a total dose of 160 mg (4% solution)
  • Not to exceed 3 mg/kg for any 1 procedure or surgery

Mucous Membrane Anesthesia

Indicated for local (topical) anesthesiatic for accessible mucous membranes of the oral, nasal, and laryngeal cavities

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

Do not exceed 3 mg/kg or 300 mg

Dosage Modifications

Hepatic impairment

  • Insufficient data available to guide dosingSince cocaine is eliminated predominantly by metabolism, avoid in patients with hepatic impairment

Renal impairment

  • Eliminated predominantly by metabolism, with little excreted unchanged in urine
  • Not studied; titrate dose conservatively

Dosing Considerations

Dosage variables include tissue vascularity, anesthetic technique and patient tolerance

Reduce dose for elderly or debilitated patients

Dosage Forms & Strengths

topical solution: Schedule II

  • 4% (40mg/mL0

Mucous Membrane Anesthesia

Indicated for local (topical) anesthesia of accessible mucous membranes of the oral, nasal, and laryngeal cavities

Use lowest possible effective dose; solutions >4% not recommended because of increased risk/severity of toxicity

Dosing Considerations

Dosage variables include tissue vascularity, anesthetic technique and patient tolerance

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Interactions

Interaction Checker

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            Contraindicated (2)

            • eliglustat

              cocaine increases levels of eliglustat by affecting hepatic enzyme CYP2D6 metabolism. Contraindicated. If coadministered with strong or moderate CYP2D6 inhibitors, reduce eliglustat dose from 84 mg BID to 84 mg once daily in extensive and intermediate metabolizers; eliglustat is contraindiated if strong or moderate CYP2D6 inhibitors are given concomitantly with strong or moderate CYP3A inhibitors.

            • iobenguane I 123

              cocaine decreases effects of iobenguane I 123 by receptor binding competition. Contraindicated. If clinically appropriate, discontinue drugs that compete for NE receptor sites for at least 5 half-lives; may cause false-negative imaging results.

            Serious - Use Alternative (22)

            • abametapir

              abametapir will increase the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

            • apalutamide

              apalutamide will decrease the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

            • bupivacaine implant

              cocaine, bupivacaine implant. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid additional local anesthetic administration within 96 hr following bupivacaine implantation. If use of additional local anesthetics is unavoidable based on clinical need, monitor for neurologic and cardiovascular effects related to local anesthetic systemic toxicity.

            • citalopram

              citalopram and cocaine both increase serotonin levels. Avoid or Use Alternate Drug. Combination may increase risk of serotonin syndrome or neuroleptic malignant syndrome-like reactions.

            • desvenlafaxine

              cocaine and desvenlafaxine both increase serotonin levels. Avoid or Use Alternate Drug.

            • fexinidazole

              fexinidazole will increase the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

            • idelalisib

              idelalisib will increase the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates

            • iobenguane I 131

              cocaine will decrease the level or effect of iobenguane I 131 by Other (see comment). Avoid or Use Alternate Drug. Based on the mechanism of action of iobenguane, drugs that reduce catecholamine uptake or that deplete catecholamine stores may interfere with iobenguane uptake into cells, and thus, reduce iobenguane efficacy. Discontinue interfering drugs for at least 5 half-lives before administration of either the dosimetry or an iobenguane dose. Do not administer these drugs until at least 7 days after each iobenguane dose.

            • isocarboxazid

              isocarboxazid and cocaine both increase serotonin levels. Contraindicated.

            • linezolid

              linezolid and cocaine both increase serotonin levels. Avoid or Use Alternate Drug. Linezolid may increase serotonin as a result of MAO-A inhibition. Cocaine inhibits presynaptic reuptake of serotonin. Monitor for CNS toxicity.

            • lonafarnib

              cocaine will increase the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of lonafarnib (a sensitive CYP3A substrate) with weak CYP3A inhibitors is unavoidable, reduce to, or continue lonafarnib at starting dose. Closely monitor for arrhythmias and events (eg, syncope, heart palpitations) since lonafarnib effect on QT interval is unknown.

              lonafarnib will increase the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.

            • lorcaserin

              cocaine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • methylene blue

              methylene blue and cocaine both increase serotonin levels. Avoid or Use Alternate Drug. Methylene blue may increase serotonin as a result of MAO-A inhibition. Cocaine inhibits presynaptic reuptake of serotonin. Monitor for CNS toxicity.

            • metoclopramide intranasal

              cocaine will increase the level or effect of metoclopramide intranasal by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug. Concurrent use of metoclopramide intranasal and strong CYP2D6 inhibitors is not recommended since the metoclopramide intranasal dose cannot be adjusted.

            • phenelzine

              phenelzine and cocaine both increase serotonin levels. Contraindicated.

            • procarbazine

              procarbazine and cocaine both increase serotonin levels. Contraindicated.

            • pseudoephedrine

              cocaine increases effects of pseudoephedrine by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Avoid or Use Alternate Drug.

            • tranylcypromine

              tranylcypromine and cocaine both increase serotonin levels. Contraindicated.

            • tucatinib

              tucatinib will increase the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

            • vilazodone

              cocaine, vilazodone. Either increases toxicity of the other by serotonin levels. Avoid or Use Alternate Drug. Concomitant therapy should be discontinued immediately if signs or symptoms of serotonin syndrome emerge and supportive symptomatic treatment should be initiated. .

            • vortioxetine

              cocaine increases levels of vortioxetine by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug. Decrease vortioxetine dose by 50% when coadministered with strong CYP2D6 inhibitors.

            • voxelotor

              voxelotor will increase the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

            Monitor Closely (91)

            • 5-HTP

              5-HTP and cocaine both increase serotonin levels. Use Caution/Monitor.

            • almotriptan

              almotriptan and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • amifampridine

              cocaine increases toxicity of amifampridine by Other (see comment). Modify Therapy/Monitor Closely. Comment: Amifampridine can cause seizures. Coadministration with drugs that lower seizure threshold may increase this risk.

            • amitriptyline

              amitriptyline and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • amoxapine

              amoxapine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • atogepant

              cocaine will increase the level or effect of atogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • avapritinib

              cocaine will increase the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • axitinib

              cocaine increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • brexpiprazole

              cocaine will decrease the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

            • bupivacaine implant

              cocaine, bupivacaine implant. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Local anesthetics may increase the risk of developing methemoglobinemia when concurrently exposed to drugs that also cause methemoglobinemia.

            • buspirone

              buspirone and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • cenobamate

              cenobamate will decrease the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

            • chloramphenicol

              chloramphenicol will increase the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • clomipramine

              clomipramine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • codeine

              cocaine decreases effects of codeine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Prevents conversion of codeine to its active metabolite morphine.

            • desipramine

              desipramine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • dexfenfluramine

              cocaine and dexfenfluramine both increase serotonin levels. Use Caution/Monitor.

            • dextroamphetamine

              cocaine and dextroamphetamine both increase serotonin levels. Use Caution/Monitor.

            • dextromethorphan

              cocaine and dextromethorphan both increase serotonin levels. Modify Therapy/Monitor Closely.

            • dihydroergotamine

              cocaine and dihydroergotamine both increase serotonin levels. Use Caution/Monitor.

            • dihydroergotamine intranasal

              cocaine and dihydroergotamine intranasal both increase serotonin levels. Use Caution/Monitor.

            • disulfiram

              disulfiram increases levels of cocaine by unknown mechanism. Use Caution/Monitor.

            • doxepin

              doxepin and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • droxidopa

              cocaine and droxidopa both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor. May increase risk for supine hypertension

            • duloxetine

              duloxetine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • elagolix

              elagolix will decrease the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered.

            • eletriptan

              eletriptan and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • eluxadoline

              cocaine increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.

            • ergotamine

              cocaine and ergotamine both increase serotonin levels. Use Caution/Monitor.

            • escitalopram

              escitalopram and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • fedratinib

              fedratinib will increase the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

            • fenfluramine

              cocaine and fenfluramine both increase serotonin levels. Use Caution/Monitor.

            • finerenone

              cocaine will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or weak CYP3A4 inhibitors. Adjust finererone dosage as needed.

            • flibanserin

              cocaine will increase the level or effect of flibanserin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Increased flibanserin adverse effects may occur if coadministered with multiple weak CYP3A4 inhibitors.

            • fluoxetine

              fluoxetine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • fluvoxamine

              fluvoxamine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • frovatriptan

              frovatriptan and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • iloperidone

              iloperidone increases levels of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.

            • imipramine

              imipramine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • ioflupane I 123

              cocaine decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.

            • isavuconazonium sulfate

              cocaine will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • isoniazid

              cocaine and isoniazid both increase serotonin levels. Use Caution/Monitor.

            • L-tryptophan

              cocaine and L-tryptophan both increase serotonin levels. Use Caution/Monitor.

            • letermovir

              letermovir increases levels of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • levomilnacipran

              levomilnacipran and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • lithium

              cocaine and lithium both increase serotonin levels. Use Caution/Monitor.

            • lofepramine

              lofepramine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • lofexidine

              cocaine will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

            • lomitapide

              cocaine increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lomitapide dose should not exceed 30 mg/day.

            • lsd

              cocaine and lsd both increase serotonin levels. Use Caution/Monitor.

            • maprotiline

              maprotiline and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • meperidine

              cocaine and meperidine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • methylphenidate

              cocaine increases effects of methylphenidate by pharmacodynamic synergism. Use Caution/Monitor. Risk of acute hypertensive episode.

            • midazolam intranasal

              cocaine will increase the level or effect of midazolam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of mild CYP3A4 inhibitors with midazolam intranasal may cause higher midazolam systemic exposure, which may prolong sedation.

            • milnacipran

              milnacipran and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • mirtazapine

              cocaine and mirtazapine both increase serotonin levels. Use Caution/Monitor.

            • mitotane

              mitotane decreases levels of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.

            • morphine

              cocaine and morphine both increase serotonin levels. Use Caution/Monitor.

            • naratriptan

              naratriptan and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • nefazodone

              nefazodone and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • nelfinavir

              nelfinavir will increase the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor.

            • nortriptyline

              nortriptyline and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • oliceridine

              cocaine will increase the level or effect of oliceridine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. If concomitant use is necessary, may require less frequent oliceridine dosing. Closely monitor for respiratory depression and sedation and titrate subsequent doses accordingly. If inhibitor is discontinued, consider increase oliceridine dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal.

            • paroxetine

              paroxetine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • pentazocine

              cocaine and pentazocine both increase serotonin levels. Use Caution/Monitor.

            • pitolisant

              cocaine will increase the level or effect of pitolisant by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. If coadministered with strong CYP2D6 inhibitors, initiate pitolisant at 8.9 mg/day and increase after 7 days to maximum of 17.8 mg/day. For patients currently taking pitolisant, reduce pitolisant dose by half upon initiating strong CYP2D6 inhibitors.

            • protriptyline

              protriptyline and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • rasagiline

              rasagiline and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • ritonavir

              ritonavir will increase the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor.

            • rizatriptan

              rizatriptan and cocaine both increase serotonin levels. Use Caution/Monitor.

            • rucaparib

              rucaparib will increase the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

            • SAMe

              cocaine and SAMe both increase serotonin levels. Use Caution/Monitor.

            • selegiline

              selegiline and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • selegiline transdermal

              selegiline transdermal and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • sertraline

              sertraline and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • solriamfetol

              cocaine and solriamfetol both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.

            • St John's Wort

              cocaine and St John's Wort both increase serotonin levels. Modify Therapy/Monitor Closely.

            • stiripentol

              stiripentol, cocaine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

            • sumatriptan

              sumatriptan and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • sumatriptan intranasal

              sumatriptan intranasal and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • tamoxifen

              cocaine, tamoxifen. affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. CYP2D6 inhibition decreases metabolism of tamoxifen to hydroxytamoxifen, and N-desmethyl tamoxifen to endoxifen (active metabolites with 100-fold greater affinity for estrogen receptor); decreased endoxifen levels may result in poor clinical outcome.

            • tamsulosin

              cocaine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • tazemetostat

              tazemetostat will decrease the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              cocaine will increase the level or effect of tazemetostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tinidazole

              cocaine will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tramadol

              cocaine and tramadol both increase serotonin levels. Use Caution/Monitor.

            • trazodone

              trazodone and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • trimipramine

              trimipramine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • valbenazine

              cocaine will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.

            • venlafaxine

              venlafaxine and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            • zolmitriptan

              zolmitriptan and cocaine both increase serotonin levels. Modify Therapy/Monitor Closely.

            Minor (31)

            • acebutolol

              acebutolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • amobarbital

              amobarbital will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • armodafinil

              armodafinil will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • atenolol

              atenolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • betaxolol

              betaxolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • bisoprolol

              bisoprolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • butabarbital

              butabarbital will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • butalbital

              butalbital will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • carvedilol

              carvedilol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • celiprolol

              celiprolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • chloramphenicol

              chloramphenicol will increase the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • efavirenz

              efavirenz will increase the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • esmolol

              esmolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • labetalol

              labetalol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • metoprolol

              metoprolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • modafinil

              modafinil will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • nadolol

              nadolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • nebivolol

              nebivolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • nilotinib

              nilotinib will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • penbutolol

              penbutolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • pentobarbital

              pentobarbital will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • phenobarbital

              phenobarbital will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • pindolol

              pindolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • primidone

              primidone will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • propranolol

              propranolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • ribociclib

              ribociclib will increase the level or effect of cocaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • ruxolitinib

              cocaine will increase the level or effect of ruxolitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • secobarbital

              secobarbital will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • sorafenib

              sorafenib will increase the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • sotalol

              sotalol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

            • timolol

              timolol increases effects of cocaine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.

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            Adverse Effects

            >10%

            Hypertension (78%)

            1-10%

            Tachycardia (5%)

            Headache (3%)

            Bradycardia (3%)

            Sinus tachycardia (2%)

            QT prolonged (3%)

            QRS prolonged (2%)

            Epistaxis (1%)

            Postmarketing Reports

            Nervous system disorders: Headache, seizure

            Cardiac disorders: Hypertension, tachycardia, atrial and ventricular arrhythmias, myocardial ischemia and infarction

            Psychiatric disorders: Anxiety

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            Warnings

            Black Box Warning

            CNS stimulants, including cocaine hydrochloride, have a high potential for abuse and dependence

            Contraindications

            Hypersensitivity to cocaine, other ester-type local anesthetics, or other product ingredients

            Cautions

            CNS stimulants, including cocaine hydrochloride, have a high potential for abuse and dependence

            May lower convulsive threshold; risk may be higher in patients with history of seizures or with prior EEG abnormalities without seizures, but has been reported in patients with no prior history or EEG evidence of seizures; monitor for development of seizures

            Increases blood pressure and heart rate; monitor for changes in vital signs, including heart rate and rhythm; avoid with history of MI, CAD, CHF, arrhythmia, abnormal ECG, or uncontrolled hypertension

            Not for ophthalmic use; can cause sloughing of the corneal epithelium; pitting and ulceration of the cornea reported

            Toxicology screening

            • The time after cocaine administration for which cocaine and its metabolites can be detected in plasma and urine depends on the sensitivity of the utilized assay method
            • Plasma: May be detected for up to 1 week after administration
            • Urine: May be detected >1 week after administration

            Drug interaction overview

            • Avoid use of additional vasoconstrictor agents (eg, epinephrine, phenylephrine); if unavoidable, prolonged vital sign and ECG monitoring may be required
            • Cocaine is a sympathetic neuronal catecholamine reuptake inhibitor, which may potentiate the actions of concomitantly administered sympathomimetic amines
            • Concurrent use of other CNS stimulants may result in excessive stimulation, leading to nervousness, irritability, or possibly convulsions, or cardiac arrhythmias
            • Disulfiram treatment increases plasma cocaine exposure (AUC and Cmax), by several folds after acute intranasal or IV cocaine administration; avoid use in patients taking disulfiram
            • Postganglionic blocking agents (eg, reserpine) potentiate cocaine-induced sympathetic stimulation; concurrent use may increase the risk of hypertension and cardiac arrhythmias that may be life-threatening
            • Tricyclic antidepressants may increase activity of the sympathetic nervous system, which may also be increased by cocaine administration
            • MAO inhibitor effects and toxicity may be potentiated by cocaine
            • Cholinesterase inhibitors
              • Cocaine is primarily metabolized and inactivated by nonenzymatic ester hydrolysis and hepatic carboxylesterase, and also by plasma cholinesterase, hepatic carboxylesterase, and CYP3A4
              • Plasma cholinesterase activity may be decreased by chronic administration of certain monoamine oxidase inhibitors, oral contraceptives, glucocorticoids, antimyasthenics (neostigmine), cyclophosphamide, and possibly thiotepa
              • May also be diminished by administration of irreversible plasma cholinesterase inhibitors (eg, echothiophate, organophosphate insecticides, and certain antineoplastic agents)
              • Patients with reduced plasma cholinesterase (pseudocholinesterase) activity may have reduced clearance and increased exposure of plasma cocaine
              • Because cocaine is metabolized by multiple enzymes, the effect of reduced plasma cholinesterase activity on cocaine exposure may be limited; no dosage adjustment of is needed in patients with reduced plasma cholinesterase
              • Monitor patients with reduced plasma cholinesterase activity for adverse reactions (eg, increased heart rate or blood pressure)
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            Pregnancy & Lactation

            Pregnancy

            Data are not available on the use of cocaine for mucosal anesthesia in pregnant women to identify a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

            Adverse maternal and fetal/neonatal outcomes have been seen in women with chronic cocaine abuse during pregnancy including congenital malformations, prematurity, miscarriage, premature rupture of membranes, and gestational hypertension

            Cocaine crosses the placenta by simple diffusion and accumulates in the fetus after repeated use

            Applicability of findings from these studies of chronic abuse in pregnancy to a single topical exposure is limited

            Fertility

            • Published animal studies suggest that cocaine can alter female reproductive hormone levels, disrupt the estrous cycle, and reduce ovulation at doses ~1-2 times the human reference dose based on BSA

            Lactation

            Because of the potential for serious adverse reactions in breastfed infants, advise a lactating woman that breastfeeding is not recommended during treatment with and to pump and discard breastmilk for 48 hr after use

            Based on case reports in published literature, cocaine is present in human milk at widely varying concentrations

            Based on its pharmacochemical characteristics, high concentrations of cocaine are expected in breast milk with systemic exposure

            The applicability of these findings to a single topical exposure with limited systemic absorption is unclear

            No studies have evaluated cocaine concentrations in milk after topical administration

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Local ester-type anesthetic; prevents conduction in nerve fibers by reversibly blocking voltage-gated sodium channels and preventing the transient rise in sodium conductance necessary for generation of an action potential

            Absorption

            Significant absorption from mucosa

            160-mg nasal mucosa dose over 20 min

            • Estimated systemic absorption: 23.44%
            • Peak plasma time: 30 min
            • Peak plasma concentration: 142.68 ng/mL (mean); 142.7 ng/mL (median)

            Distribution

            Protein Bound: 84-92%

            Vd: 2 L/kg

            Metbolism

            Metabolized by hydrolysis to benzoylecgonine (major, but inactive metabolite) by hepatic carboxylesterase-1

            Also metabolized by hydrolysis to ecgonine methyl ester (major, but inactive metabolite) by plasma butyrylcholinesterase and hepatic carboxylesterase-2

            N-demethylated by CYP3A4 to produce norcocaine (active metabolite); total systemic exposure of norcocaine is <1% that observed with cocaine

            Elimination

            Half-life: 1.5 hr

            Excreted almost exclusively in urine as metabolites

            <5% eliminated unchanged in urine

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            Administration

            Intranasal preparation

            Numbrino or Goprelto

            • Draw up 4 mL into a syringe calibrated in mL
            • Recommended size of the cotton or rayon pledgets for use measure 0.5 x 3 inches (sold separately)
            • Each pledget absorbs 1 mL (40 mg) of nasal solution
            • Stack four pledgets and apply 2 mL of solution to the top of the stacked pledgets; turn the stacked pledgets over and apply 2 mL of solution to the other side
            • Evenly distribute solution on all pledgets
            • Place 1 or 2 pledgets in each nasal cavity, for a maximum of 2 pledgets used per nostril
            • Leave pledgets in place for up to 20 minutes, remove pledgets and continue with the procedure
            • Discard pledgets, and dispose of any unused pledgets and remaining solution in accordance with institutional procedures for CII products
            • Pledgets should be removed immediately upon any sign or symptom of an adverse event

            Intranasal application

            Use product specific for intranasal use only

            Do not apply to damaged nasal mucosa

            Unless the FDA has determined that these products can be substituted, do not substitute for other intranasal cocaine products because this may result in different local and/or systemic exposures

            Mucous membrane application

            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

            Storage

            All formulations

            • Store at 20-25ºC (68-77ºF) with excursions permitted to 15-30ºC (59-86ºF)
            • Avoid freezing
            • Keep out of reach of children
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            Images

            No images available for this drug.
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            Patient Handout

            A Patient Handout is not currently available for this monograph.
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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.