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

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
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Formulary
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