CITANEST FORTE DENTAL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CITANEST FORTE DENTAL (CITANEST FORTE DENTAL).
Citanest Forte Dental (prilocaine and epinephrine) acts by blocking sodium channels in nerve cell membranes, inhibiting nerve impulse propagation and producing local anesthesia. Epinephrine is a vasoconstrictor that prolongs the anesthetic effect by reducing vascular uptake.
| Metabolism | Prilocaine is primarily metabolized in the liver by amidases to o-toluidine and other metabolites; epinephrine is metabolized by catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO). |
| Excretion | Renal excretion of unchanged drug and metabolites (primarily glucuronide conjugates) accounts for approximately 95% of elimination, with less than 2% excreted in bile/feces. |
| Half-life | Terminal elimination half-life is 1.6–2.0 hours in adults, prolonged in hepatic impairment or neonates. |
| Protein binding | Approximately 55% bound to plasma proteins, mainly to alpha-1-acid glycoprotein and albumin. |
| Volume of Distribution | Volume of distribution is 1.0–1.5 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Bioavailability is essentially 100% after local administration due to direct injection at the site. |
| Onset of Action | Onset of action after dental infiltration: 2–4 minutes; after nerve block: 5–10 minutes. |
| Duration of Action | Duration of pulpal anesthesia: 30–60 minutes; soft tissue anesthesia: 2–3 hours. Longer in inflamed tissues due to lower pH. |
| Molecular Weight | 220.31 |
1.7 mL (30 mg) of 4% solution for infiltration; 0.5-1.5 mg/kg for nerve block, not to exceed 2.5 mg/kg (maximum 150 mg). Administered submucosally or perineurally.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment required for mild-to-moderate renal impairment (GFR >30 mL/min). For severe renal impairment (GFR <30 mL/min), reduce dose by 50% due to potential accumulation of metabolites. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose by 50% and avoid repeat administration. Child-Pugh C: Not recommended. |
| Pediatric use | Infiltration: 0.5-1.0 mL of 4% solution per dose, not to exceed 0.5 mg/kg. Nerve block: 0.25-0.5 mg/kg, max 1.5 mg/kg. Use 2% solution in children <6 years. |
| Geriatric use | Reduce dose by 50% due to decreased clearance and increased risk of CNS toxicity. Maximum single dose: 1.5 mg/kg. |
| 1st trimester | Limited human data; animal studies show adverse effects at high doses. Use only if benefit outweighs risk. |
| 2nd trimester | Similar to t1; consider use after careful risk-benefit assessment. |
| 3rd trimester | May cause methemoglobinemia in newborn if used near term; avoid use during delivery. |
Clinical note
Comprehensive clinical and safety monograph for CITANEST FORTE DENTAL (CITANEST FORTE DENTAL).
| Placental transfer | Prilocaine crosses the placenta; fetal-to-maternal ratio approximately 0.7-0.9. |
| Breastfeeding | Prilocaine is excreted into breast milk in small amounts; however, due to potential for methemoglobinemia in infants, caution is advised. Monitor infant for signs of methemoglobinemia. |
| Lactation Rating |
■ FDA Black Box Warning
Use caution to avoid intravascular injection; epinephrine may cause severe hypertension, cardiac arrhythmias, or cerebrovascular accidents in patients with cardiovascular disease.
| Serious Effects |
Hypersensitivity to prilocaine or any componentSevere hepatic diseaseMethemoglobinemia (congenital or idiopathic)Severe hypotensionMyasthenia gravis (relative, but often absolute)
| Precautions | Methemoglobinemia: prilocaine doses >600 mg may cause methemoglobinemia, especially in patients with glucose-6-phosphate dehydrogenase deficiency, Cardiovascular: epinephrine may cause increased heart rate and blood pressure; use with caution in patients with cardiac disease, hypertension, or hyperthyroidism, Allergic reactions: cross-sensitivity with other amide-type local anesthetics |
| Food/Dietary | No specific food interactions. Avoid hot foods and beverages until local anesthesia wears off to prevent oral burns. Limit caffeine intake as epinephrine may potentiate stimulant effects. |
Loading safety data…
| L2 - Limited safety data |
| Teratogenic Risk | Citanest Forte Dental (prilocaine 4% with epinephrine 1:200,000) is classified as FDA Pregnancy Category B. Animal studies have not demonstrated teratogenic effects, but adequate human studies in pregnant women are lacking. Prilocaine crosses the placenta. Methemoglobinemia risk exists for the fetus if high doses are used, especially in the third trimester. Use only if clearly needed, with caution. |
| Fetal Monitoring | Monitor mother for signs of local anesthetic systemic toxicity (LAST): perioral numbness, dizziness, tinnitus, seizures, cardiovascular collapse. Monitor fetal heart rate during prolonged procedures. In late pregnancy, avoid excessive dosing to minimize fetal methemoglobinemia; consider pulse oximetry for fetal/maternal oxygen saturation if high doses are used. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies with prilocaine have not shown impaired fertility. Epinephrine at low concentrations does not affect fertility. Theoretical concerns with high-dose local anesthetics on sperm motility if administered paracervically; not applicable for dental use. |
| Clinical Pearls | Citanest Forte Dental (prilocaine 4% with epinephrine 1:200,000) provides rapid onset (1-2 min) and moderate duration (60-90 min) for dental procedures. Maximum dose: 600 mg prilocaine (10 mg/kg) and 0.09 mg epinephrine. Contraindicated in patients with history of methemoglobinemia, severe hepatic impairment, or hypersensitivity to amide anesthetics. Caution in cardiac disease, hypertension, and thyroid disorders due to epinephrine content. Avoid intravascular injection; aspirate before administration. |
| Patient Advice | Notify your dentist if you have a history of methemoglobinemia, liver disease, or allergy to local anesthetics. · Inform your dentist of all medications you take, especially MAO inhibitors, tricyclic antidepressants, and beta-blockers. · Temporary numbness of lips, tongue, or face is normal; avoid chewing gum or hot foods until sensation returns. · If you experience difficulty breathing, dizziness, or bluish skin, seek emergency care immediately. · Do not exceed recommended dose; use the smallest effective amount. |