Prilocaine Hydrochloride
Pronunciation: PRIL-oh-kane HYE-droe-KLOR-ide
Class: Local anesthetic
Trade Names
Citanest Forte
- Injection, solution 4%
Citanest Plain
- Injection, solution 4%
Pharmacology
Stabilizes the neuronal membrane by inhibiting the ionic fluxes needed for the initiation and conduction of impulses, thereby affecting local anesthetic action.
Pharmacokinetics
Metabolism
Metabolized by both the liver and kidney.
Elimination
Excreted by the kidney.
Onset
Less than 2 min when used for infiltration injection in dental patients. When used for inferior alveolar nerve block, the onset averages less than 3 min.
Duration
Average duration of soft tissue anesthesia is approximately 2 h when used for infiltration injection in dental patients. Citanest Plain provides a duration of complete palpal anesthesia for procedures lasting 20 min. When used for inferior alveolar nerve block, the duration of soft tissue anesthesia with Citanest Plain and Citanest Forte is 2.5 and 3 h, respectively.
Special Populations
Renal Function ImpairmentPharmacokinetics may be altered.
Hepatic Function ImpairmentPharmacokinetics may be altered.
Indications and Usage
Production of local anesthesia in dentistry by nerve block or infiltration techniques.
Contraindications
Hypersensitivity to amide-type local anesthetics; patients with congenital or idiopathic methemoglobinemia.
Dosage and Administration
AdultsInfiltration For most routine procedures, initial doses of 1 to 2 mL will provide adequate infiltration or major nerve block anesthesia. Maximum recommended dose is 8 mg/kg (4 mg/lb) in patients weighing less than 70 kg (150 lb) and 600 mg in patients weighing 70 kg (150 lb) or more.
Children younger than 10 yr of ageInfiltration Seldom necessary to administer doses greater than 40 mg for a procedure involving a single tooth.
Storage/Stability
Store at 77°F. Protect from light.
Drug Interactions
Drugs associated with methemoglobinemia (eg, acetaminophen, benzocaine, chloroquine, dapsone, nitrates, nitrofurantoin, nitroglycerine, nitroprusside, phenobarbital, phenytoin, primaquine, quinine, sulfonamides)Risk of methemoglobinemia may be increased.
Ergot derivatives (eg, ergotamine)Severe, persistent hypertension or cerebrovascular accidents may occur.
MAOIs (eg, phenelzine), phenothiazines (eg, chlorpromazine), tricyclic antidepressants (amitriptyline)Severe, prolonged hypertension or hypotension may occur. If possible, avoid coadministration.
Laboratory Test Interactions
IM injection may increase CPK levels.
Adverse Reactions
Cardiovascular
Bradycardia, cardiac arrest, CV collapse, hypotension, serious CV catastrophe, vasovagal reaction.
CNS
Apprehension; cerebral hypoxia; confusion; convulsion; depression; dizziness; drowsiness; euphoria; excitation; faintness; light-headedness; nervousness; persistent neurologic deficit; sensations of cold, heat, or numbness; seizures; tremors; twitching; unconsciousness.
EENT
Blurred or double vision, tinnitus.
GI
Swelling and persistent paresthesia of the lips and oral tissue, vomiting.
Hypersensitivity
Allergic reactions characterized by anaphylactic reactions, cutaneous lesions, edema, or urticaria.
Respiratory
Respiratory arrest or depression.
Miscellaneous
Feeling of tightness, sweating.
Precautions
MonitorMonitor CV and respiratory vital signs and the state of consciousness. |
Pregnancy
Category B.
Lactation
Undetermined.
Children
Dosage should be based on age, weight, and physical condition.
Hepatic Function
Use with caution.
Special Risk Patients
Administer reduced doses in debilitated elderly patients, acutely ill patients, and children. Use with caution in patients with impaired CV function, heart block or severe shock.
Sulfite Sensitivity
Prilocaine injection contains a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in susceptible individuals.
Methemoglobinemia
May occur.
Repeated administration
Increases in blood levels may occur.
Use in head and neck area
May cause adverse reactions similar to systemic toxicity.
Overdosage
Symptoms
Cardiovascular arrest, cardiovascular depression, and convulsions can lead to hypoxia, acidosis, bradycardia, arrhythmias, and cardiac arrest; respiratory depression.
Patient Information
- Caution patients about the possibility of temporary loss of sensation and muscle function.
- Caution patients to avoid inadvertent trauma to the cheek mucosa, lips, soft palate, or tongue.
- Advise patients to consult their health care provider if anesthesia persists or a rash develops.
Copyright © 2009 Wolters Kluwer Health.


