Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (2)
- eliglustat
cocaine topical 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 topical 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 (21)
- apalutamide
apalutamide will decrease the level or effect of cocaine topical 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 topical, 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 topical both increase serotonin levels. Avoid or Use Alternate Drug. Combination may increase risk of serotonin syndrome or neuroleptic malignant syndrome-like reactions.
- desvenlafaxine
cocaine topical and desvenlafaxine both increase serotonin levels. Avoid or Use Alternate Drug.
- fexinidazole
fexinidazole will increase the level or effect of cocaine topical 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 topical 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 topical 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 topical both increase serotonin levels. Contraindicated.
- linezolid
linezolid and cocaine topical 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 topical 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 topical 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 topical and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.
- methylene blue
methylene blue and cocaine topical 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 topical 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 topical both increase serotonin levels. Contraindicated.
- procarbazine
procarbazine and cocaine topical both increase serotonin levels. Contraindicated.
- pseudoephedrine
cocaine topical increases effects of pseudoephedrine by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Avoid or Use Alternate Drug.
- tranylcypromine
tranylcypromine and cocaine topical both increase serotonin levels. Contraindicated.
- tucatinib
tucatinib will increase the level or effect of cocaine topical 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 topical, 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 topical 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 topical 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 (93)
- 5-HTP
5-HTP and cocaine topical both increase serotonin levels. Use Caution/Monitor.
- almotriptan
almotriptan and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- amifampridine
cocaine topical 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- amoxapine
amoxapine and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- atogepant
cocaine topical will increase the level or effect of atogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- avapritinib
cocaine topical will increase the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- axitinib
cocaine topical increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- brexpiprazole
cocaine topical 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 topical, 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- cenobamate
cenobamate will decrease the level or effect of cocaine topical 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 topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- clomipramine
clomipramine and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- codeine
cocaine topical 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- dexfenfluramine
cocaine topical and dexfenfluramine both increase serotonin levels. Use Caution/Monitor.
- dextroamphetamine
cocaine topical and dextroamphetamine both increase serotonin levels. Use Caution/Monitor.
- dextroamphetamine transdermal
cocaine topical will increase the level or effect of dextroamphetamine transdermal by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Initiate with lower doses and monitor patients for signs and symptoms of serotonin syndrome, particularly during dextroamphetamine initiation and after a dosage increase. If serotonin syndrome occurs, discontinue dextroamphetamine transdermal and CYP2D6 inhibitor.
- dextromethorphan
cocaine topical and dextromethorphan both increase serotonin levels. Modify Therapy/Monitor Closely.
- dihydroergotamine
cocaine topical and dihydroergotamine both increase serotonin levels. Use Caution/Monitor.
- dihydroergotamine intranasal
cocaine topical and dihydroergotamine intranasal both increase serotonin levels. Use Caution/Monitor.
- disulfiram
disulfiram increases levels of cocaine topical by unknown mechanism. Use Caution/Monitor.
- doxepin
doxepin and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- droxidopa
cocaine topical 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- elagolix
elagolix will decrease the level or effect of cocaine topical 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- eluxadoline
cocaine topical 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 topical 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 topical and ergotamine both increase serotonin levels. Use Caution/Monitor.
- escitalopram
escitalopram and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- fedratinib
fedratinib will increase the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- fenfluramine
cocaine topical and fenfluramine both increase serotonin levels. Use Caution/Monitor.
- finerenone
cocaine topical 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 topical 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- fluvoxamine
fluvoxamine and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- frovatriptan
frovatriptan and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- iloperidone
iloperidone increases levels of cocaine topical 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- ioflupane I 123
cocaine topical 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 topical will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- isoniazid
cocaine topical and isoniazid both increase serotonin levels. Use Caution/Monitor.
- L-tryptophan
cocaine topical and L-tryptophan both increase serotonin levels. Use Caution/Monitor.
- lenacapavir
lenacapavir will increase the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir (a moderate CYP3A4 inhibitor) may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.
- letermovir
letermovir increases levels of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- levomilnacipran
levomilnacipran and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- lithium
cocaine topical and lithium both increase serotonin levels. Use Caution/Monitor.
- lofepramine
lofepramine and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- lofexidine
cocaine topical 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 topical increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lomitapide dose should not exceed 30 mg/day.
- lsd
cocaine topical and lsd both increase serotonin levels. Use Caution/Monitor.
- maprotiline
maprotiline and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- meperidine
cocaine topical and meperidine both increase serotonin levels. Modify Therapy/Monitor Closely.
- methylphenidate
cocaine topical increases effects of methylphenidate by pharmacodynamic synergism. Use Caution/Monitor. Risk of acute hypertensive episode.
- midazolam intranasal
cocaine topical 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- mirtazapine
cocaine topical and mirtazapine both increase serotonin levels. Use Caution/Monitor.
- mitotane
mitotane decreases levels of cocaine topical 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 topical and morphine both increase serotonin levels. Use Caution/Monitor.
- naratriptan
naratriptan and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- nefazodone
nefazodone and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- nelfinavir
nelfinavir will increase the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor.
- nortriptyline
nortriptyline and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- oliceridine
cocaine topical 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- pentazocine
cocaine topical and pentazocine both increase serotonin levels. Use Caution/Monitor.
- pitolisant
cocaine topical 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- rasagiline
rasagiline and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- ritonavir
ritonavir will increase the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor.
- rizatriptan
rizatriptan and cocaine topical both increase serotonin levels. Use Caution/Monitor.
- rucaparib
rucaparib will increase the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- SAMe
cocaine topical and SAMe both increase serotonin levels. Use Caution/Monitor.
- selegiline
selegiline and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- selegiline transdermal
selegiline transdermal and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- sertraline
sertraline and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- solriamfetol
cocaine topical and solriamfetol both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- St John's Wort
cocaine topical and St John's Wort both increase serotonin levels. Modify Therapy/Monitor Closely.
- stiripentol
stiripentol, cocaine topical. 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- sumatriptan intranasal
sumatriptan intranasal and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- tamoxifen
cocaine topical, 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 topical increases levels of tamsulosin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- tazemetostat
tazemetostat will decrease the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
cocaine topical will increase the level or effect of tazemetostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - tinidazole
cocaine topical will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tramadol
cocaine topical and tramadol both increase serotonin levels. Use Caution/Monitor.
- trazodone
trazodone and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- trimipramine
trimipramine and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- valbenazine
cocaine topical 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 topical both increase serotonin levels. Modify Therapy/Monitor Closely.
- zolmitriptan
zolmitriptan and cocaine topical both increase serotonin levels. Modify Therapy/Monitor Closely.
Minor (37)
- acebutolol
acebutolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- acetazolamide
acetazolamide will increase the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- amobarbital
amobarbital will decrease the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- armodafinil
armodafinil will decrease the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- atenolol
atenolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- betaxolol
betaxolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- bisoprolol
bisoprolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- butabarbital
butabarbital will decrease the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- butalbital
butalbital will decrease the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- carvedilol
carvedilol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- celiprolol
celiprolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- chloramphenicol
chloramphenicol will increase the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- efavirenz
efavirenz will increase the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- esmolol
esmolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- labetalol
labetalol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- larotrectinib
larotrectinib will increase the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- levoketoconazole
levoketoconazole will increase the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- metoprolol
metoprolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- modafinil
modafinil will decrease the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- nadolol
nadolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- nebivolol
nebivolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- nilotinib
nilotinib will decrease the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- penbutolol
penbutolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- pentobarbital
pentobarbital will decrease the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- phenobarbital
phenobarbital will decrease the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- pindolol
pindolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- primidone
primidone will decrease the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- propranolol
propranolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- ribociclib
ribociclib will increase the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ruxolitinib
cocaine topical will increase the level or effect of ruxolitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ruxolitinib topical
cocaine topical will increase the level or effect of ruxolitinib topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- secobarbital
secobarbital will decrease the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- sorafenib
sorafenib will increase the level or effect of cocaine topical by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.
- sotalol
sotalol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
- timolol
timolol increases effects of cocaine topical by pharmacodynamic synergism. Minor/Significance Unknown. Risk of angina.
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
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
Reduced plasma cholinesterase activity
- Cocaine has been described in literature to be primarily metabolized and inactivated by non-enzymatic ester hydrolysis and hepatic carboxylesterase, and also by plasma cholinesterase,hepatic carboxylesterase, and CYP3A4
- Genetic abnormalities of plasma cholinesterase (eg, patients who are heterozygous or homozygous for atypical plasma cholinesterase gene), disease conditions such as malignant tumors, severe liver or kidney disease, decompensated heart disease, infections, burns, anemia, peptic ulcer, or myxedema or other physiological states such as pregnancy may lead to reduced plasma cholinesterase activity
- Patients with reduced plasma cholinesterase (pseudocholinesterase) activity may have reduced clearance and increased exposure of plasma cocaine after administration of this drug
- Since cocaine is metabolized by multiple enzymes, effect of reduced plasma cholinesterase activity on cocaine exposure may be limited; no dosage adjustment of this drug needed inpatients 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
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
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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)
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
Animal data
- Animal studies conducted in accordance with good laboratory practices, malformations including vertebral and rib abnormalities reported when pregnant rabbits treated with16 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 47times adult human AUC exposures
- Published rodent studies testing high exposures to cocaine during organogenesis report various malformations at 17-34 times adult human AUC exposures following administration of pledgets containing 160 mg of cocaine
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
Based on limited case reports in published literature, cocaine is present in human milk at widely varying concentrations; based on pharmacochemical characteristics, high concentrations of cocaine are expected in breast milk with systemic exposure
Applicability of these findings to single topical exposure with limited systemic absorption is unclear; no studies have evaluated cocaine concentrations in milk after topical administration of this drug
Cocaine is detected in human breastmilk in chronic abuse situations and is expected to be at higher concentrations in milk than in maternal blood based on its physicochemical characteristics
Breastfeeding immediately after administration of this medication could result in infant plasma concentrations approximately half anticipated maximum maternal plasma concentrations at clinical dose of 160 mg
The effects of this cocaine plasma concentration in an infant are unknown, but no level of cocaine exposure is considered safe for breastfed infant
Adverse reactions have occurred in infants ingesting cocaine through breastmilk, including vomiting, diarrhea, convulsions, hypertension, tachycardia, agitation, and irritability
Long-term effects on infants exposed to cocaine through breast milk are unknown; there are no data on effects of this drug on milk production
Because of potential for serious adverse reactions in breastfed infants, advise nursing women that breastfeeding is not recommended during treatment and to pump and discard breastmilk for 48 hours after use
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.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
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
Images
Formulary
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