pharmacopeia
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Mechanism of action

Sourced from openFDA

Prilocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.

Indications

Sourced from openFDA
  • 4% Citanest Plain Dental Injection, Prilocaine Hydrochloride Injection, USP, 4% (72 mg/1.8 mL) (40 mg/mL), is indicated for the production of local anesthesia in dentistry by nerve block or infiltration techniques. Only accepted procedures for these techniques as described in standard textbooks are recommended.

Contraindications

Sourced from openFDA
  • Prilocaine is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the amide type and in those rare patients with congenital or idiopathic methemoglobinemia.contraindicated

Dosage & administration

Sourced from openFDA

The dosage of 4% Citanest Plain Dental Injection, Prilocaine Hydrochloride Injection, USP, 4% (72 mg/1.8 mL) (40 mg/mL), varies and depends on the physical status of the patient, the area of the oral cavity to be anesthetized, the vascularity of the oral tissues, and the technique of anesthesia. The least volume of injection that results in effective local anesthesia should be administered. For specific techniques and procedures of local anesthesia in the oral cavity, refer to standard textbooks. Inferior Alveolar Block There are no practical clinical differences between prilocaine with and without epinephrine when used for inferior alveolar blocks. Maxillary Infiltration 4% Citanest Plain Dental, Prilocaine Hydrochloride Injection, USP, 4% (72 mg/1.8 mL) (40 mg/mL), is recommended for use in maxillary infiltration anesthesia for procedures in which the painful aspects can be completed within 15 minutes after the injection. 4% Citanest Plain Dental, Prilocaine Hydrochloride Injection, USP, 4% (72 mg/1.8 mL) (40 mg/mL), is therefore especially suited to short procedures in the maxillary anterior teeth. For long procedures, or those involving maxillary posterior teeth where soft tissue numbness is not troublesome to the patient, Prilocaine HCl 4% with epinephrine 1:200,000 is recommended. For most routine procedures, initial dosages of 1 to 2 mL of 4% Citanest Plain Dental Injection, Prilocaine Hydrochloride Injection, USP, 4% (72 mg/1.8 mL) (40 mg/mL), will usually provide adequate infiltration or major nerve block anesthesia.

Warnings & precautions

Sourced from openFDA

DENTAL PRACTITIONERS WHO EMPLOY LOCAL ANESTHETIC AGENTS SHOULD BE WELL VERSED IN DIAGNOSIS AND MANAGEMENT OF EMERGENCIES THAT MAY ARISE FROM THEIR USE. RESUSCITATIVE EQUIPMENT, OXYGEN AND OTHER RESUSCITATIVE DRUGS SHOULD BE AVAILABLE FOR IMMEDIATE USE. Methemoglobinemia Cases of methemoglobinemia have been reported in association with local anesthetic use. Although all patients are at risk for methemoglobinemia, 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. If local anesthetics must be used in these patients, close monitoring for symptoms and signs of methemoglobinemia is recommended. Signs of methemoglobinemia may occur immediately or may be delayed some hours after exposure, and are characterized by a cyanotic skin discoloration and/ or abnormal coloration of the blood. Methemoglobin levels may continue to rise; therefore, immediate treatment is required to avert more serious central nervous system and cardiovascular adverse effects, including seizures, coma, arrhythmias, and death. Discontinue CITANEST and any other oxidizing agents. Depending on the severity of the signs and symptoms, patients may respond to supportive care, i.e., oxygen therapy, hydration. A more severe clinical presentation may require treatment with methylene blue exchange transfusion, or hyperbaric oxygen.

Adverse reactions

Sourced from openFDA

Swelling and persistent paresthesia of the lips and oral tissues may occur. Persistent paresthesias lasting weeks to months, and in rare instances paresthesia lasting greater than one year, have been reported. Adverse experiences following the administration of prilocaine are similar in nature to those observed with other amide local anesthetic agents. These adverse experiences are, in general, dose-related and may result from high plasma levels caused by excessive dosage, rapid absorption or unintentional intravascular injection, or may result from a hypersensitivity, idiosyncrasy or diminished tolerance on the part of the patient. Serious adverse experiences are generally systemic in nature. The following types are those most commonly reported: Central Nervous System CNS manifestations are excitatory and/or depressant and may be characterized by lightheadedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, sensations of heat, cold or numbness, twitching, tremors, convulsions, unconsciousness, respiratory depression, and arrest. The excitatory manifestations may be very brief or may not occur at all, in which case the first manifestation of toxicity may be drowsiness merging into unconsciousness and respiratory arrest. Drowsiness following the administration of prilocaine is usually an early sign of a high blood level of the drug and may occur as a consequence of rapid absorption.

Use in specific populations

Sourced from openFDA

Use in Pregnancy Teratogenic Effects Pregnancy Category B Reproduction studies have been performed in rats at doses up to 30 times the human dose and revealed no evidence of impaired fertility or harm to the fetus due to prilocaine. There are, however, no adequate and well-controlled studies in pregnant women. Animal reproduction studies are not always predictive of human response. General consideration should be given to this fact before administering prilocaine to women of childbearing potential, especially during early pregnancy when maximum organogenesis takes place.

Pharmacokinetics

Sourced from openFDA
Metabolism
and Metabolism Information derived from diverse formulations, concentrations and usages reveals that prilocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon such factors as the site of administration and the presence or absence of a vasoconstrictor agent. Prilocaine is metabolized in both the liver and the kidney and excreted via the kidney.

Overdosage

Sourced from openFDA

Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics (see ADVERSE REACTIONS , WARNINGS , and PRECAUTIONS ). Management of Local Anesthetic Emergencies The first consideration is prevention, best accomplished by careful and constant monitoring of cardiovascular and respiratory vital signs and the patient’s state of consciousness after each local anesthetic injection. At the first sign of change, oxygen should be administered. The first step in the management of convulsions consists of immediate attention to the maintenance of a patent airway and assisted or controlled ventilation with oxygen and a delivery system capable of permitting immediate positive airway pressure by mask. Immediately after the institution of these ventilatory measures, the adequacy of the circulation should be evaluated, keeping in mind that drugs used to treat convulsions sometimes depress the circulation when administered intravenously.

Approval history

Sourced from openFDA
  • Aug 18, 2003ANDAANDA076453Fougera Pharms
  • Aug 27, 2003ANDAANDA076320Encube
  • Dec 19, 2003NDANDA021451Dentsply Pharm
  • Sep 29, 2010ANDAANDA079235Septodont Inc
  • Aug 30, 2011ANDAANDA078959Septodont Inc
  • Jun 29, 2018ANDAANDA205887Pai Holdings Pharm
  • Jul 27, 2021ANDAANDA212482Padagis Us
  • Apr 8, 2022ANDAANDA213923Alembic

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
1,759 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue18110%
  2. 2Nausea1528.6%
  3. 3Diarrhoea1186.7%
  4. 4Off Label Use965.5%
  5. 5Vomiting935.3%
  6. 6Drug Ineffective895.1%
  7. 7Dyspnoea885.0%
  8. 8Headache854.8%
  9. 9Pyrexia844.8%
  10. 10Pain754.3%
  11. 11Death744.2%
  12. 12Dizziness724.1%
  13. 13Pneumonia714.0%
  14. 14Product Dose Omission Issue683.9%
  15. 15Sinusitis633.6%

Literature

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Recent PubMed references pinned to Prilocaine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 252 ClinicalTrials.gov registrations naming Prilocaine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Prilocaine work?
Prilocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.
What is Prilocaine used for?
According to FDA labeling, Prilocaine carries indications including: 4% Citanest Plain Dental Injection, Prilocaine Hydrochloride Injection, USP, 4% (72 mg/1.8 mL) (40 mg/mL), is indicated for the production of local anesthesia in dentistry by nerve block or infiltration techniques. Only accepted procedures for these techniques as described in standard textbooks are recommended.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Prilocaine?
Prilocaine is classified as Amides, Amide Local Anesthetic, Sodium Channel Interactions, Decreased Organized Electrical Activity, Local Anesthesia.
What are the brand names for Prilocaine?
Prilocaine is marketed under brand names including Citanest, Citanest Forte, Oraqix, Relador.
What are the contraindications for Prilocaine?
Prilocaine labeling lists contraindications including: Prilocaine is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the amide type and in those rare patients with congenital or idiopathic methemoglobinemia.. Always consult the full prescribing information and a clinician.
Note. Data for prilocaine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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