prilocaine (Rx)

Brand and Other Names:Citanest
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Dosing & Uses

AdultPediatric

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

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

Dosage Forms & Strengths

injectable solution (cartridge for dental use)

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

Local Anesthesia

< 10 years

  • Dental infiltration: 40 mg of (1 mL) 4% solution; not to exceed 8 mg/kg within 2 hr  

> 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
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Interactions

Interaction Checker

and prilocaine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (1)

              • bupivacaine implant

                prilocaine, bupivacaine implant. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid additional local anesthetic administration within 96 hr following bupivacaine implantation. If use of additional local anesthetics is unavoidable based on clinical need, monitor for neurologic and cardiovascular effects related to local anesthetic systemic toxicity.

              Monitor Closely (5)

              • nadolol

                nadolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents.

              • phenazopyridine

                phenazopyridine increases toxicity of prilocaine by Other (see comment). Modify Therapy/Monitor Closely. Comment: Phenazopyridine may significantly increase risk of methemoglobinemia when coadministered with prilocaine. Monitor patients closely.

              • pindolol

                pindolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents.

              • propranolol

                propranolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents.

              • timolol

                timolol, prilocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Use extreme caution during concomitant use of bupivacaine and antihypertensive agents.

              Minor (1)

              • hyaluronidase

                hyaluronidase, prilocaine. Other (see comment). Minor/Significance Unknown. Comment: Hyaluronidase hastens the onset of local analgesia and reduces swelling, but increases systemic absorption of anesthetic. This decreases the duration of action and increases incidence of systemic reaction.

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              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)

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              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
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              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.

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              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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              Images

              No images available for this drug.
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              Patient Handout

              Patient Education
              prilocaine injection

              NO MONOGRAPH AVAILABLE AT THIS TIME

              USES: Consult your pharmacist.

              HOW TO USE: Consult your pharmacist.

              SIDE EFFECTS: Consult your pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Consult your pharmacist.

              DRUG INTERACTIONS: Consult your pharmacist.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

              NOTES: No monograph available at this time.

              MISSED DOSE: Consult your pharmacist.

              STORAGE: Consult your pharmacist.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

              Information last revised July 2016. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Formulary

              FormularyPatient Discounts

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              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.