Version May 2024
Note: The effective anesthetic dose varies with procedure, intensity of anesthesia needed, duration of anesthesia required, and physical condition of the patient. Always use the lowest effective dose along with careful aspiration prior to administration.
Dental anesthesia:
Initial: 40 to 80 mg (1 to 2 mL) of prilocaine hydrochloride as a 4% solution with epinephrine 1:200,000
Maximum dose (weight-based) within a 2-hour period: Prilocaine hydrochloride (Ref):
<70 kg: 6 mg/kg (400 mg)
≥70 kg: 400 mg or 5 to 6 cartridges
There are no dosage adjustments provided in manufacturer's labeling; use with caution (renally metabolized).
There are no dosage adjustments provided in manufacturer's labeling; use with caution (hepatically metabolized).
Refer to adult dosing.
Dental anesthesia:
Children <10 years: Doses >40 mg (1 mL) of prilocaine hydrochloride as a 4% solution with epinephrine 1:200,000 are rarely needed for procedures involving a single tooth, in a maxillary infiltration for 2 to 3 teeth, or for an entire quadrant with a mandibular block.
Children >10 years: Refer to adult dosing.
There are no dosage adjustments provided in manufacturer’s labeling; use with caution (renally metabolized).
There are no dosage adjustments provided in manufacturer’s labeling; use with caution (hepatically metabolized).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Degree of adverse effects in the CNS and cardiovascular system are directly related to the blood levels of prilocaine. The effects below are more likely to occur after systemic administration rather than infiltration.
Frequency not defined:
Cardiovascular: Bradycardia, circulatory shock, edema, hypotension, vasodepressor syncope
Central nervous system: Apprehension, confusion, dizziness, drowsiness, euphoria, flushing sensation, loss of consciousness, nervousness, numbness, seizure, sensation of cold, twitching
Dermatologic: Skin lesion, urticaria
Gastrointestinal: Vomiting
Hypersensitivity: Anaphylactoid shock, hypersensitivity reaction (rare)
Ophthalmic: Blurred vision, diplopia
Otic: Tinnitus
Neuromuscular & skeletal: Tremor
Respiratory: Respiratory depression, hypoxia
Hypersensitivity to local anesthetics of the amide-type or any component of the formulation; congenital or idiopathic methemoglobinemia
Concerns related to adverse effects:
• CNS toxicity: Careful and constant monitoring of the patient's state of consciousness should be done following each local anesthetic injection; at such times, restlessness, anxiety, tinnitus, dizziness, blurred vision, tremors, depression, or drowsiness may be early warning signs of CNS toxicity. Treatment is primarily symptomatic and supportive.
• Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue). Use is contraindicated in patients with congenital or idiopathic methemoglobinemia.
• Respiratory arrest: Local anesthetics have been associated with rare occurrences of sudden respiratory arrest.
• Seizures: Convulsions due to systemic toxicity leading to cardiac arrest have also been reported, presumably following unintentional intravascular injection.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with cardiovascular disease; should be used in minimal amounts in patients with significant cardiovascular disease (because of epinephrine component).
• Familial malignant hyperthermia: Prilocaine may potentially trigger malignant hyperthermia; follow standard protocol for identification and treatment.
• Hepatic impairment: Use with caution in patients with hepatic impairment; amide-type anesthetics are hepatically metabolized.
• Hyperthyroidism: Should be avoided in patients with uncontrolled hyperthyroidism.
• Vascular disease: Local anesthetic solutions containing a vasoconstrictor should be used cautiously. Patients with peripheral vascular disease or hypertensive vascular disease may exhibit exaggerated vasoconstrictor response, possibly resulting in ischemic injury or necrosis.
Special populations:
• Acutely ill patients: Use with caution in acutely ill patients; reduce dose consistent with age and physical status.
• Debilitated patients: Use with caution in debilitated patients; reduce dose consistent with age and physical status.
• Older adult: Use with caution in older adults; reduce dose consistent with age and physical status.
• Pediatric: Use with caution in children; reduce dose consistent with age and physical status.
Dosage form specific issues:
• Sodium metabisulfite: May contain sodium metabisulfite; use caution in patients with asthma or a sulfite allergy.
Other warnings/precautions:
• Administration: Intravascular injections should be avoided; aspiration should be performed prior to administration; the needle must be repositioned until no return of blood can be elicited by aspiration; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided.
• Appropriate dosing: To avoid serious adverse effects and high plasma concentrations, the lowest dosage resulting in effective anesthesia should be administered. Repeated doses may significantly increase blood concentrations of both the drug or its metabolites; tolerance to elevated blood concentrations varies with patient status. Reduced dosages, commensurate with age and physical condition, should be given to patients who are debilitated or acutely ill, and in older adults or the pediatric population.
• Trained personnel: Dental practitioners using local anesthetic agents should be well trained in diagnosis and management of emergencies that may arise from the use of these agents. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution [for dental use]:
Citanest Forte Dental: Prilocaine hydrochloride 4% and epinephrine 1:200,000 (1.7 mL [DSC]) [contains sodium metabisulfite]
No
Solution (Citanest Forte Dental Injection)
4%-1:200000 (per mL): $0.56
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution [for dental use]:
Citanest Forte Dental: Prilocaine hydrochloride 4% and epinephrine 1:200,000 (1.8 mL) [contains sodium metabisulfite]
Generic: Prilocaine hydrochloride 4% and epinephrine 1:200,000 (1.8 mL)
Dental anesthesia: Local, infiltrative, or nerve block anesthesia in dental procedures
Refer to individual components.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Similarly, Alpha-/Beta-Agonists may antagonize Alpha1-Blocker vasodilation. Risk C: Monitor therapy
Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Risk C: Monitor therapy
Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Azosemide: May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk C: Monitor therapy
Benperidol: May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Alpha-/Beta-Agonists may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Consider use of a histamine skin test as a positive control to assess a patient's ability to mount a wheal and flare response. Risk D: Consider therapy modification
Beta-Blockers (Beta1 Selective): May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk C: Monitor therapy
Beta-Blockers (Nonselective): May enhance the hypertensive effect of EPINEPHrine (Systemic). Risk C: Monitor therapy
Beta-Blockers (with Alpha-Blocking Properties): May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk C: Monitor therapy
Blonanserin: May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk X: Avoid combination
Bretylium: May enhance the therapeutic effect of Alpha-/Beta-Agonists (Direct-Acting). Risk C: Monitor therapy
Bromocriptine: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Management: Consider alternatives to this combination when possible. If combined, monitor for hypertension and tachycardia, and do not coadminister these agents for more than 10 days. Risk D: Consider therapy modification
Bromperidol: May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk X: Avoid combination
BUPivacaine: Local Anesthetics may enhance the adverse/toxic effect of BUPivacaine. Management: Avoid using any additional local anesthetics within 96 hours after insertion of the bupivacaine implant (Xaracoll) or bupivacaine and meloxicam periarticular solution (Zynrelef) or within 168 hours after subacromial infiltration (Posimir brand). Risk C: Monitor therapy
BUPivacaine (Liposomal): Local Anesthetics may enhance the adverse/toxic effect of BUPivacaine (Liposomal). Management: Liposomal bupivacaine should not be administered with local anesthetics, but may be administered 20 minutes or more after lidocaine. Avoid all local anesthetics within 96 hours after administration of liposomal bupivacaine. Risk X: Avoid combination
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Chloroprocaine (Systemic): May enhance the hypertensive effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
CloZAPine: May diminish the therapeutic effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Risk D: Consider therapy modification
COMT Inhibitors: May increase the serum concentration of COMT Substrates. Risk C: Monitor therapy
Dapsone (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Risk C: Monitor therapy
Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Risk C: Monitor therapy
Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): May enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Risk X: Avoid combination
Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy
Haloperidol: May diminish the vasoconstricting effect of EPINEPHrine (Systemic). Management: Consider alternatives to this combination and monitor for reduced epinephrine efficacy, and possible paradoxical effects (ie, hypotension), when combined. Use of alternative vasopressor agents (eg, phenylephrine, metaraminol, norepinephrine) is preferred. Risk D: Consider therapy modification
Hyaluronidase: May enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Management: Do not use hyaluronidase to enhance the dispersion or absorption of alpha-/beta-agonists. Use of hyaluronidase for other purposes in patients receiving alpha-/beta-agonists may be considered as clinically indicated. Risk D: Consider therapy modification
Inhalational Anesthetics: May enhance the arrhythmogenic effect of EPINEPHrine (Systemic). Management: Administer epinephrine with added caution in patients receiving, or who have recently received, inhalational anesthetics. Use lower than normal doses of epinephrine and monitor for the development of cardiac arrhythmias. Risk D: Consider therapy modification
Isoproterenol: May enhance the therapeutic effect of EPINEPHrine (Systemic). Risk X: Avoid combination
Kratom: May enhance the adverse/toxic effect of Sympathomimetics. Risk X: Avoid combination
Levothyroxine: May enhance the adverse/toxic effect of Sympathomimetics. Specifically, the risk of coronary insufficiency may be increased in patients with coronary artery disease. Levothyroxine may enhance the therapeutic effect of Sympathomimetics. Sympathomimetics may enhance the therapeutic effect of Levothyroxine. Risk C: Monitor therapy
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Consider initial dose reductions of sympathomimetic agents, and closely monitor for enhanced blood pressure elevations, in patients receiving linezolid. Risk D: Consider therapy modification
Lisuride: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Risk X: Avoid combination
Local Anesthetics: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor therapy
Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Prilocaine. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when prilocaine is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine in infants receiving such agents. Risk C: Monitor therapy
Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of EPINEPHrine (Systemic). Risk C: Monitor therapy
Neuromuscular-Blocking Agents: Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Risk C: Monitor therapy
Nitric Oxide: May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Risk C: Monitor therapy
Ozanimod: May enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy
Pergolide: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
Promethazine: May diminish the vasoconstricting effect of EPINEPHrine (Systemic). Management: Avoid epinephrine and consider norepinephrine or phenylephrine when treating hypotension due to promethazine overdose. Consider alternative vasocontrictors in patients treated with promethazine. This combination may be indicated in anaphylaxis treatment. Risk D: Consider therapy modification
Serotonin/Norepinephrine Reuptake Inhibitors: May enhance the tachycardic effect of Alpha-/Beta-Agonists. Serotonin/Norepinephrine Reuptake Inhibitors may enhance the vasopressor effect of Alpha-/Beta-Agonists. Management: If possible, avoid coadministration of direct-acting alpha-/beta-agonists and serotonin/norepinephrine reuptake inhibitors. If coadministered, monitor for increased sympathomimetic effects (eg, increased blood pressure, chest pain, headache). Risk D: Consider therapy modification
Sodium Nitrite: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Sodium Nitrite. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Risk C: Monitor therapy
Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Sympathomimetics may enhance the tachycardic effect of Solriamfetol. Risk C: Monitor therapy
Spironolactone: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy
Technetium Tc 99m Tilmanocept: Local Anesthetics may diminish the diagnostic effect of Technetium Tc 99m Tilmanocept. Management: Avoid mixing and simultaneously co-injecting technetium Tc 99m tilmanocept with local anesthetics. This interaction does not appear to apply to other uses of these agents in combination. Risk C: Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Tricyclic Antidepressants: May enhance the vasopressor effect of Alpha-/Beta-Agonists. Management: Avoid, if possible, the use of alpha-/beta-agonists in patients receiving tricyclic antidepressants. If combined, monitor for evidence of increased pressor effects and consider reductions in initial dosages of the alpha-/beta-agonist. Risk D: Consider therapy modification
Vasopressin: Alpha-/Beta-Agonists (Direct-Acting) may enhance the hypertensive effect of Vasopressin. The effect of other hemodynamic parameters may also be enhanced. Risk C: Monitor therapy
Adverse events were not observed in animal reproduction studies.
Usual infiltration doses of prilocaine with epinephrine given to nursing mothers has not been shown to affect the health of the nursing infant.
Cardiovascular and respiratory vital signs; state of consciousness after each injection; CNS toxicity
Local anesthetics bind selectively to the intracellular surface of sodium channels to block influx of sodium into the axon. As a result, depolarization necessary for action potential propagation and subsequent nerve function is prevented. The block at the sodium channel is reversible. When drug diffuses away from the axon, sodium channel function is restored and nerve propagation returns.
Epinephrine prolongs the duration of the anesthetic actions of prilocaine by causing vasoconstriction (alpha-adrenergic receptor agonist) of the vasculature surrounding the nerve axons. This prevents the diffusion of prilocaine away from the nerves resulting in a longer retention in the axon.
Onset of action: Infiltration: <2 minutes; Inferior alveolar nerve block: <3 minutes
Duration: Infiltration: ~2.25 hours; Inferior alveolar nerve block: ~3 hours
آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟
