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prilocaine (Citanest)

 

Classes: Local Anesthetics, Amides; Local Anesthetics, Dental

Dosing and uses of Citanest (prilocaine)

 

Adult dosage forms and 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

Not to exceed 600 mg (8 mg/kg) within 2 hr

See also combo with lidocaine

 

Other Indications & Uses

Infiltrative or nerve block anesthesia for dental procedures

 

Pediatric dosage forms and strengths

injectable solution (cartridge for dental use)

  • 4%
  • 4% with epinephrine 1:200,000

 

Local Anesthesia

Dental infiltration: 40 mg of (1 mL) 4% solution

Not to exceed 8 mg/kg within 2 hr

 

Citanest (prilocaine) adverse (side) effects

Frequency not defined

Anxiety

Apprehension

Restlessness

Nervousness

Disorientation

Confusion

Dizziness

Blurred vision

Tremors

Twitching

Shivering

Seizures

CNS depression manifested by drowsiness, unconsciousness, respiratory arrest, nausea, vomiting, chills, miosis, tinnitus; myocardial depression, bradycardia, cardiac arrhythmias, hypotension, cardiovascular collapse, cardiac arrest; anxiety, palpitation, dizziness, headache, restlessness, tremors, tachycardia, anginal pain, hypertension (epinephrine-containing solutions)

Edema

Status asthmaticus

Anaphylactoid reactions (sometimes fatal)

 

Warnings

Contraindications

Hypersensitivity to prilocaine, amide-type local anesthetics, sulfites, parabens

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

Addition of vasoconstrictor, epinephrine, will promote local hemostasis, decrease systemic absorption, and increase duration of action

 

Pregnancy and 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 of Citanest (prilocaine)

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: highly

 

Metabolism

Metabolism: liver

Metabolites: ester- & amide-type local anesthetics

 

Elimination

Excretion: urine (principally)