Dosing & Uses
Dosage Forms & Strengths
injectable solution (cartridge for dental use)
- 4%
- 4% with epinephrine 1:200,000
Local Anesthesia
Dental infiltration: 40-80 mg (1-2 mL) of 4% solution prilocaine or prilocaine with epinephrine
Dosage Forms & Strengths
injectable solution (cartridge for dental use)
- 4%
- 4% with epinephrine 1:200,000
Local Anesthesia
< 10 years
> 10 years
- Dental infiltration: 40-80 mg (1-2 mL) of 4% solution prilocaine or prilocaine with epinephrine; not to exceed 600 mg (8 mg/kg) within 2 hr
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (1)
- bupivacaine implant
prilocaine, 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.
Monitor Closely (5)
- nadolol
nadolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents.
- phenazopyridine
phenazopyridine increases toxicity of prilocaine by Other (see comment). Modify Therapy/Monitor Closely. Comment: Phenazopyridine may significantly increase risk of methemoglobinemia when coadministered with prilocaine. Monitor patients closely.
- pindolol
pindolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents.
- propranolol
propranolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents.
- timolol
timolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents.
Minor (1)
- hyaluronidase
hyaluronidase, prilocaine. Other (see comment). Minor/Significance Unknown. Comment: Hyaluronidase hastens the onset of local analgesia and reduces swelling, but increases systemic absorption of anesthetic. This decreases the duration of action and increases incidence of systemic reaction.
Adverse Effects
Frequency Not Defined
CNS depression manifested by drowsiness, unconsciousness, respiratory arrest, nausea, vomiting, chills, miosis, tinnitus; myocardial depression, bradycardia, cardiac arrhythmias, hypotension, cardiovascular collapse, cardiac arrest; palpitation, headache, tremors, tachycardia, anginal pain, hypertension (epinephrine-containing solutions)
Anxiety
Apprehension
Restlessness
Nervousness
Disorientation
Confusion
Dizziness
Blurred vision
Tremors
Twitching
Shivering
Seizures
Edema
Status asthmaticus
Anaphylactoid reactions (sometimes fatal)
Warnings
Contraindications
Hypersensitivity to prilocaine, amide-type local anesthetics, sulfites, parabens
Idiopathic or congenital methemoglobinemia
Cautions
Administration of >600 mg to adults causes non-acute 15% methemoglobinemia via formation of o-toluidine metabolite
Use preservative-free preparations for spinal or epidural anesthesia
DO NOT use solutions with epinephrine in distal areas of body (e.g. digit, nose, ear, etc)
History of malignant hyperthermia
Respiratory arrest reported with local anesthetics
Seizures reported with systemic toxicity
Addition of vasoconstrictor, epinephrine, will promote local hemostasis, decrease systemic absorption, and increase duration of action
Methemoglobinemia
- Use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly; patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition
- Advise patients or caregivers to seek immediate medical attention if patient experiences the following signs or symptoms: pale, gray, or blue colored skin (cyanosis); headache; rapid heart rate; shortness of breath; lightheadedness; or fatigue; discontinue Bicillin C-R and any other oxidizing agents; depending on severity of signs and symptoms, patients may respond to supportive care, including oxygen therapy and hydration; a more severe clinical presentation may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen
Pregnancy & Lactation
Pregnancy Category: C
Lactation: not known if excreted in breast milk
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 anesthetics prevent generation/conduction of nerve impulses by reducing sodium permeability and increasing action potential threshold
Absorption
Duration: the greater the degree of vasodilation produced by the local anesthetic, the faster the rate of absorption & shorter the duration of action (bupivacaine has a long duration of action)
Distribution
Protein bound: 55%
Vd: 0.6-4.4 L/kg
Onset: 2 min (infiltration); 3 min (inferior alveolar nerve block)
Metabolism
Metabolism: Liver and kidney
Metabolites: Ester- & amide-type local anesthetics
Elimination
Excretion: Urine (principally)
Half-life: 10-150 min
Images
Patient Handout
prilocaine injection
NO MONOGRAPH AVAILABLE AT THIS TIME
USES: Consult your pharmacist.
HOW TO USE: Consult your pharmacist.
SIDE EFFECTS: Consult your pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Consult your pharmacist.
DRUG INTERACTIONS: Consult your pharmacist.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: No monograph available at this time.
MISSED DOSE: Consult your pharmacist.
STORAGE: Consult your pharmacist.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.
Information last revised July 2016. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
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