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.

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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 Impairment

Pharmacokinetics may be altered.

Hepatic Function Impairment

Pharmacokinetics 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

Adults

Infiltration 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 age

Infiltration 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

Monitor

Monitor 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.

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