CITANEST PLAIN DENTAL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CITANEST PLAIN DENTAL (CITANEST PLAIN DENTAL).
Propylocaine, an amide-type local anesthetic, stabilizes the neuronal membrane by binding to voltage-gated sodium channels, thereby inhibiting sodium influx and blocking conduction of nerve impulses.
| Metabolism | Primarily metabolized by ester hydrolysis in plasma and liver via pseudocholinesterase and carboxylesterases. |
| Excretion | Renal excretion of metabolites (primarily 4-hydroxyprilocaine and N-propylalanine) accounts for >95% of elimination; <5% excreted unchanged in urine. Less than 1% eliminated via feces. |
| Half-life | Terminal elimination half-life is approximately 1.6 hours (range 1–2 hours). This short half-life allows for rapid clearance, minimizing systemic accumulation during repeated dosing in dental procedures. |
| Protein binding | Approximately 55% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.8–1.0 L/kg, indicating moderate distribution to total body water. This reflects its lipid solubility and moderate tissue binding. |
| Bioavailability | Due to extensive first-pass hepatic metabolism, oral bioavailability is negligible (≈5%). For dental use, administered by injection, thus systemic bioavailability is 100% for the injected dose. |
| Onset of Action | Following submucosal injection (dental infiltration or nerve block), onset of anesthesia occurs within 1–3 minutes. |
| Duration of Action | Duration of pulpal anesthesia is 10–20 minutes for infiltration and 30–60 minutes for nerve block; soft tissue anesthesia persists longer, up to 90 minutes. Clinical note: the shorter duration compared to lidocaine makes prilocaine useful for brief procedures. |
Adult dose for dental anesthesia: 20-50 mg (0.5-1.25 mL of 4% solution) by infiltration; up to 200 mg (5 mL) by nerve block. Maximum dose: 6 mg/kg, not exceeding 300 mg per appointment.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment for GFR. Use with caution in severe renal impairment (GFR <30 mL/min) due to potential accumulation of metabolites; consider lower doses and extended intervals. |
| Liver impairment | Child-Pugh Class A: No adjustment. Class B: Reduce dose by 50%; maximum single dose 150 mg. Class C: Avoid use or reduce dose by 75%; maximum single dose 75 mg. |
| Pediatric use | Children: 0.5-2.5 mg/kg by infiltration; maximum dose: 4 mg/kg. Weight-based: <20 kg: 0.5-1.0 mg/kg; 20-40 kg: 1.0-1.5 mg/kg; >40 kg: up to 2.5 mg/kg. Not recommended for children under 6 months. |
| Geriatric use | Elderly: Reduce doses by 50% due to decreased tissue perfusion and increased sensitivity; maximum single dose 150 mg. Use with caution in patients with cardiovascular disease or on antiarrhythmics. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CITANEST PLAIN DENTAL (CITANEST PLAIN DENTAL).
| Breastfeeding | Prilocaine is excreted into breast milk in small amounts. The milk-to-plasma (M/P) ratio is approximately 0.5 to 0.6. Breastfeeding is generally considered safe at therapeutic doses, but caution is advised due to the theoretical risk of methemoglobinemia in the infant, especially if the mother receives multiple doses or high doses. |
| Teratogenic Risk | Citanest Plain Dental (prilocaine) is classified as FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, but there are no adequate and well-controlled studies in pregnant women. Prilocaine crosses the placenta. First trimester: risks are minimal based on animal data. Second and third trimesters: potential for methemoglobinemia in the newborn if high doses are used or if the mother has a history of methemoglobinemia. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to amide-type local anesthetics; severe hepatic disease; patients with congenital or idiopathic methemoglobinemia.
| Precautions | Avoid intravascular injection; risk of methemoglobinemia; caution in patients with hepatic impairment, methemoglobin reductase deficiency, or conditions predisposing to methemoglobinemia. |
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| Fetal Monitoring | Monitor maternal vital signs (blood pressure, heart rate, respiratory rate) and ECG during administration. Assess for signs of local anesthetic toxicity (e.g., perioral numbness, tinnitus, metallic taste, seizures). Fetal heart rate monitoring is recommended during labor and delivery if used for obstetric anesthesia. Monitor newborn for signs of methemoglobinemia (cyanosis, hypoxia, altered mental status) if high doses were administered. |
| Fertility Effects | No specific studies have assessed fertility effects in humans. Animal studies have not shown impaired fertility at doses relevant to clinical use. Prilocaine is not known to adversely affect reproductive organs or gametogenesis. |