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Marcaine with Epinephrine
bupivacaine/ epinephrine
Black Box Warnings .
Obstetrical Use
contraindicated for obstetrical paracervical block; 0.75% conc. (except hyperbaric form) not recommended for obstetrical anesthesia; cardiac arrest w/ difficult resuscitation or death during epidural anesthesia in obstetric pts has occurred; systemic toxicity from accidental intravascular inj. can cause seizures and cardiac arrest; reserve 0.75% conc. for surgical procedures requiring high degree of muscle relaxation and prolonged effect
Adult Dosing .
Dosage forms: INJ (0.25%/1:200,000): 2.5 mg per mL; INJ (0.5%/1:200,000): 5 mg per mL
Special Note
- [formulation clarification]
- Info: not interchangeable w/ bupivacaine liposomal; do not substitute on a mg to mg basis; some concentrations methylparaben-free (MPF)
- [dosing clarification]
- Info: dose based on bupivacaine component
local anesthesia
- [infiltration, dental]
- Dose: 9 mg (0.5%/1:200,000) via infiltration x1 for single site; Max: 90 mg/procedure; Info: may repeat dose x1 after 2-10min; onset 2-10min, peak 30-45min, duration 3-6h
- [infiltration, all other procedures]
- Dose: up to 225 mg (0.25%/1:200,000) via infiltration x1; Max: 400 mg/24h; Info: may repeat dose q3h prn; onset 2-10min, peak 30-45min, duration 3-6h
regional anesthesia
- [peripheral nerve block, dental]
- Dose: 9 mg (0.5%/1:200,000) perineurally x1 for single site; Max: 90 mg/procedure; Info: may repeat dose x1 after 2-10min; onset 2-10min, peak 30-45min, duration 3-6h
- [peripheral nerve block, all other procedures]
- Dose: 25-225 mg (0.5%/1:200,000) perineurally x1; Max: 400 mg/24h; Alt: 12.5-225 mg (0.25%/1:200,000) perineurally x1; Info: may repeat dose q3h prn; onset 2-10min, peak 30-45min, duration 3-6h
- [caudal block]
- Dose: 75-150 mg (0.5%/1:200,000 MPF) intracaudally x1; Max: 400 mg/24h; Alt: 37.5-75 mg (0.25%/1:200,000 MPF) intracaudally x1; Info: may repeat dose q3h prn; onset 2-10min, peak 30-45min, duration 3-6h
- [lumbar block]
- Dose: 50-100 mg (0.5%/1:200,000 MPF) epidurally x1; Max: 400 mg/24h; Alt: 25-50 mg (0.25%/1:200,000 MPF) epidurally x1; Info: may repeat dose q3h prn; onset 2-10min, peak 30-45min, duration 3-6h
epidural test dose
- [10-15 mg (0.5%/1:200,000 MPF) epidurally x1]
- Info: give before initial full dose and any repeat full doses
renal dosing
- [see below]
- renal impairment: not defined, caution advised
- HD/PD: not defined
hepatic dosing
- [see below]
- mild impairment: not defined, caution advised; moderate-severe impairment: consider decr. usual dose
Peds Dosing .
- Dosage forms: INJ (0.25%/1:200,000): 2.5 mg per mL; INJ (0.5%/1:200,000): 5 mg per mL
Special Note
- [formulation clarification]
- Info: not interchangeable w/ bupivacaine liposomal; do not substitute on a mg to mg basis; some concentrations methylparaben-free (MPF)
- [dosing clarification]
- Info: dose based on bupivacaine component
local anesthesia
- [infiltration, 12 yo and older]
- Dose: up to 225 mg (0.25%/1:200,000) via infiltration x1; Max: 3 mg/kg/dose; 400 mg/24h; Info: may repeat dose q3h prn; onset 2-10min, peak 30-45min, duration 3-6h
regional anesthesia
- [peripheral nerve block, 12 yo and older]
- Dose: 25-225 mg (0.5%/1:200,000) perineurally x1; Max: 3 mg/kg/dose; 400 mg/24h; Alt: 12.5-225 mg (0.25%/1:200,000) perineurally x1; Info: may repeat dose q3h prn; onset 2-10min, peak 30-45min, duration 3-6h
- [caudal block, 12 yo and older]
- Dose: 75-150 mg (0.5%/1:200,000 MPF) intracaudally x1; Max: 3 mg/kg/dose; 400 mg/24h; Alt: 37.5-75 mg (0.25%/1:200,000 MPF) intracaudally x1; Info: may repeat dose q3h prn; onset 2-10min, peak 30-45min, duration 3-6h
- [lumbar block, 12 yo and older]
- Dose: 50-100 mg (0.5%/1:200,000 MPF) epidurally x1; Max: 3 mg/kg/dose; 400 mg/24h; Alt: 25-50 mg (0.25%/1:200,000 MPF) epidurally x1; Info: may repeat dose q3h prn; onset 2-10min, peak 30-45min, duration 3-6h
epidural test dose
- [12 yo and older]
- Dose: 10-15 mg (0.5%/1:200,000 MPF) epidurally x1; Info: give before initial full dose and any repeat full doses
renal dosing
- [see below]
- renal impairment: not defined, caution advised
- HD/PD: not defined
hepatic dosing
- [see below]
- mild impairment: not defined, caution advised; moderate-severe impairment: consider decr. usual dose
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- hypersensitivity to amide anesthetics
- intra-articular continuous infusion use
- IV regional anesthesia use
- paracervical block use, obstetrical
- intrathecal use
- caudal use (methylparaben-containing form)
- epidural use (methylparaben-containing form)
- dental use (peds pts)
- caution: hypersensitivity to sulfites
- caution: elderly pts
- caution: debilitated pts
- caution: illness, acute
- caution: hepatic impairment
- caution: renal impairment
- caution: cardiac impairment
- caution: HTN
- caution: CAD
- caution: PVD
- caution: cerebrovascular dz
- caution: diabetes mellitus
- caution: hyperthyroidism
- caution: G6PD deficiency
- caution: pulmonary impairment
- caution: head admin.
- caution: neck admin.
Drug Interactions .
Overview
bupivacaine
local anesthetic
- bradycardia
- displaces liposomal agent
- hypotensive effects
- methemoglobinemia
- potentiates neuromuscular blockade
epinephrine
alpha/beta agonist
- COMT substrate
- hyperglycemic effects
- hypertensive effects
- hypokalemia
- interferes w/ radiolabeled norepinephrine analog effect
- tachycardia
Contraindicated
- lidocaine topical
- phenelzine
- prilocaine topical
Avoid/Use Alternative
- albuterol
- aldesleukin
- amitriptyline
- amoxapine
- amphetamine
- arsenic trioxide
- articaine
- brigatinib
- carvedilol
- ceritinib
- chloroprocaine
- chlorpromazine
- clomipramine
- clozapine
- cocaine
- crizotinib
- desipramine
- diethylpropion
- doxepin
- dronabinol
- epinephrine inhaled
- esmolol
- etrasimod
- fexinidazole
- fingolimod
- fluphenazine
- formoterol inhaled
- furosemide
- haloperidol
- imipramine
- iobenguane I 131
- isocarboxazid
- isoproterenol
- labetalol
- linezolid
- lofexidine
- mepivacaine
- methamphetamine
- midodrine
- nadolol
- nortriptyline
- olanzapine
- ozanimod
- perphenazine
- pimozide
- pindolol
- ponesimod
- procarbazine
- prochlorperazine
- promethazine
- propranolol
- protriptyline
- rasagiline
- ropivacaine
- safinamide
- selegiline
- selegiline transdermal
- siponimod
- thioridazine
- timolol
- tranylcypromine
- trifluoperazine
- trimipramine
- yohimbe
Monitor/Modify Tx
- abiraterone acetate
- acarbose
- acebutolol
- acetazolamide
- adenosine
- albuterol inhaled
- alectinib
- alfentanil
- alfuzosin
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- aloe
- alogliptin
- amantadine
- amifostine
- amiloride
- aminophylline
- amiodarone
- amlodipine
- amphotericin
- angiotensin II
- apomorphine
- apraclonidine ophthalmic
- arformoterol inhaled
- aripiprazole
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- aripiprazole lauroxil
- armodafinil
- asciminib
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- atazanavir
- atenolol
- atomoxetine
- atracurium
- atropine ophthalmic
- avanafil
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- brexpiprazole
- brimonidine ophthalmic
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- buprenorphine
- bupropion
- butorphanol
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- clonidine
- codeine
- coenzyme Q-10
- colesevelam
- copanlisib
- corticotropin
- cortisone
- cyclosporine
- danazol
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- dexamethasone
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- dextroamphetamine
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- magnesium citrate
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- magnesium sulfate
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- mefenamic acid
- mefloquine
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- meperidine
- metformin
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- methohexital
- methoxy polyethylene glycol-epoetin beta
- methyldopa
- methylene blue injection
- methylergonovine
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- moexipril
- molindone
- morphine
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- naproxen
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- nattokinase
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- niacin (vitamin B3)
- nicardipine
- nifedipine
- nilotinib
- nimodipine
- niraparib
- nisoldipine
- nitric oxide
- nitrite
- nitroglycerin
- nitroprusside
- norepinephrine
- octreotide
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- olmesartan medoxomil
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- opicapone
- opium
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- oxymorphone
- oxytocin
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- pancuronium
- pasireotide
- pazopanib
- pentamidine
- pentazocine
- pentobarbital
- perindopril
- pexidartinib
- phendimetrazine
- phenobarbital
- phenoxybenzamine
- phentermine
- phentolamine
- phenylephrine
- phenylephrine injection
- phenylephrine nasal
- phenylephrine ophthalmic
- phenylephrine rectal
- phenytoin
- pioglitazone
- piroxicam
- polyethylene glycol
- polyethylene glycol/electrolytes
- ponatinib
- posaconazole
- pralsetinib
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- pramlintide
- praziquantel
- prazosin
- prednisolone
- prednisone
- procainamide
- propafenone
- propofol
- pseudoephedrine
- pyridostigmine
- quetiapine
- quinapril
- quinidine (antiarrhythmic)
- quinine
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- sildenafil
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- sodium phenylbutyrate
- sodium phosphate (bowel prep)
- sodium polystyrene sulfonate
- sodium thiosulfate
- solriamfetol
- sorafenib
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- sotalol
- sparsentan
- spironolactone
- succinylcholine
- sufentanil
- sugammadex
- sulfate bowel prep
- sulindac
- sumatriptan
- sunitinib
- tacrolimus
- tadalafil
- tafasitamab
- tagraxofusp
- tamsulosin
- tapentadol
- taurine
- telmisartan
- terazosin
- terbutaline
- teriflunomide
- testosterone
- thalidomide
- theophylline
- thiothixene
- thyroid
- ticagrelor
- timolol ophthalmic
- tirzepatide
- tivozanib
- tizanidine
- tolcapone
- tolmetin
- topiramate
- torsemide
- tramadol
- trametinib
- trandolapril
- trastuzumab
- trazodone
- treprostinil
- triamcinolone
- triamterene
- valsartan
- vamorolone
- vandetanib
- vardenafil
- vasopressin
- vecuronium
- venlafaxine
- verapamil
- vilanterol inhaled
- viloxazine
- voclosporin
- vosoritide
- ziprasidone
- ziv-aflibercept
- zolmitriptan
- zonisamide
Caution Advised
- acetaminophen
- benzocaine topical
- butamben
- chloroquine
- chlorpheniramine
- cyclophosphamide
- dapsone
- dapsone topical
- diphenhydramine
- hydroxyurea
- ifosfamide
- nitrofurantoin
- phenazopyridine
- primaquine
- procaine
- rasburicase
- resorcinol topical
- sulfadiazine
- sulfamethoxazole
- sulfasalazine
- tafenoquine
- tetracaine
Adverse Reactions .
Serious Reactions
- CNS toxicity
- seizures
- respiratory arrest
- cardiac arrest
- heart block
- bradycardia
- ventricular arrhythmia
- HTN
- hypotension, severe
- local anesthetic systemic toxicity (LAST), rapid or delayed onset
- anaphylactoid rxn
- methemoglobinemia
Common Reactions
- hypotension
- nausea
- vomiting
- constipation
- taste disturbance
- paresthesia
- pain
- bradycardia
- headache
- fever
- rigors
- dizziness
- injection site burning
- pruritus
- drowsiness
- restlessness
- anxiety
- blurred vision
- tinnitus
- tremor
Safety/Monitoring .
Monitoring Parameters
ECG; pulse oximetry; vital signs; neurological status
Pregnancy/Lactation .
Pregnancy
Clinical Summary
bupivacaine: contraindicated for obstetrical paracervical block; avoid 0.75% conc. (except hyperbaric form), otherwise weigh risk/benefit during pregnancy; inadequate human data available, though risk of fetal harm not expected based on limited human data w/ other amide local anesthetics; risk of embryo-fetal death based on conflicting animal data at MRHD
epinephrine: weigh risk/benefit during pregnancy, esp. during labor and delivery; possible risk of teratogenicity based on limited or conflicting human data; risk of teratogenicity and embryo-fetal death based on animal data at 3-15x MRHD; risk of decr. uterine perfusion and interference w/ uterine contractility based on drug's mechanism of action
Lactation
Clinical Summary
bupivacaine: may use while breastfeeding; no known risk of infant harm based on limited human data and drug properties; no known adverse effects on milk production based on limited human data
epinephrine: weigh risk/benefit while breastfeeding; no human data available, though risk of infant harm not expected based on drug properties; no human data available, though theoretical decr. milk production w/ high-dose IV use based on decr. prolactin levels
Pharmacology .
Metabolism: for bupivacaine: liver primarily; CYP450: 3A4 (minor) substrate; for epinephrine: liver, other tissues; CYP450: unknown
Excretion: for bupivacaine: urine (6% unchanged); Half-life: 2.7h; for epinephrine: urine (minimally unchanged); Half-life: <5min (IV)
Subclass: Anesthetics, Local
Mechanism of Action
bupivacaine inhibits Na ion channels, stabilizing neuronal cell membranes and inhibiting nerve impulse initiation and conduction (amide local anesthetic); epinephrine stimulates alpha and beta adrenergic receptors (sympathomimetic)
Formulary .
No Formulary Selected
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