DURANEST
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DURANEST (DURANEST).
Etonidate is an ultrashort-acting nonbarbiturate hypnotic agent that produces anesthesia by enhancing GABA-mediated chloride conductance at GABA-A receptors, leading to central nervous system depression.
| Metabolism | Primarily hepatic via hydrolysis by esterases (plasma and hepatic) to inactive metabolites. Less than 5% excreted unchanged in urine. |
| Excretion | Primarily hepatic metabolism; renal excretion of metabolites accounts for <10% unchanged drug. Biliary/fecal elimination is minimal. |
| Half-life | Terminal elimination half-life is 4.5 hours (range 3-6 hours). Clinical context: Prolonged in severe hepatic impairment but not significantly in renal impairment. |
| Protein binding | 85-90% bound primarily to alpha-1-acid glycoprotein; minor binding to albumin. |
| Volume of Distribution | Vd is 2.5-3.5 L/kg, indicating extensive extravascular distribution and tissue binding. |
| Bioavailability | Oral: 60-70% (first-pass metabolism); Intramuscular: ~90%; Intravenous: 100%. |
| Onset of Action | Intravenous: within 1-2 minutes; Intramuscular: 5-10 minutes; Oral: 30-60 minutes. |
| Duration of Action | Intravenous: 30-60 minutes; Intramuscular: 1-2 hours; Oral: 4-6 hours. Clinical note: Duration may be extended in hepatic disease. |
| Molecular Weight | 288.38 |
2-10 mL of a 1-2% solution, subarachnoid injection, single dose only.
| Dosage form | INJECTABLE |
| Renal impairment | No specific guidelines; contraindicated in severe renal impairment due to potential for accumulation of preservatives. |
| Liver impairment | Use with caution; no specific Child-Pugh adjustments available. Contraindicated in severe hepatic disease due to impaired metabolism. |
| Pediatric use | Not recommended for pediatric use due to limited data and high risk of neurotoxicity. |
| Geriatric use | Reduce dose and volume; monitor for prolonged motor block and hypotension. Use lowest effective dose. |
| 1st trimester | Avoid; animal studies show teratogenic effects; no adequate human studies. |
| 2nd trimester | Avoid; may cause fetal bradycardia and acidosis; use only if clearly needed. |
| 3rd trimester | Avoid; may cause fetal bradycardia and acidosis; use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for DURANEST (DURANEST).
| Placental transfer | Rapidly crosses placenta; fetal/maternal ratio approximately 0.5–0.7. |
| Breastfeeding | Excreted into breast milk in small amounts; avoid breastfeeding due to potential cardiovascular effects in infant. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to amide anestheticsSevere hypotensionThird-degree atrioventricular blockMyasthenia gravis
| Precautions | Adrenocortical suppression: Etonidate inhibits 11β-hydroxylase, reducing cortisol and aldosterone synthesis; may last up to 24 hours after single dose., Myoclonus: Involuntary muscle movements occur in up to 70% of patients, especially with rapid injection., Hypotension: Less pronounced than with other induction agents, but may occur, particularly in hypovolemic patients., Injection site pain: Common with peripheral administration., Use in intensive care: Prolonged infusion associated with increased mortality; not recommended for sedation in ICU., Pregnancy category C: Use only if clearly needed. |
| Food/Dietary | No known direct food interactions. However, avoid hot beverages and foods until numbness resolves to prevent oral burns. No specific dietary restrictions. |
Loading safety data…
| L5 |
| Teratogenic Risk | Duranest (etidocaine) is a local anesthetic of the amide type. Limited human data; animal studies show no teratogenicity at clinically relevant doses. Use in first trimester only if clearly needed. Second and third trimesters: no known teratogenic risk; may cause fetal bradycardia if high systemic levels occur. Avoid in near-term unless necessary due to neonatal effects. |
| Fetal Monitoring | Continuous maternal ECG, blood pressure, and oxygen saturation during administration. Fetal heart rate monitoring for bradycardia or signs of distress after epidural or high-dose use. Assess for signs of systemic toxicity (perioral numbness, metallic taste, seizures) in mother. Postoperative assessment of neonatal neurobehavioral status if high doses used near delivery. |
| Fertility Effects | No known effect on fertility in humans. Animal studies show no impairment of fertility at doses up to 2-3 times the maximum recommended human dose. |
| Clinical Pearls | DURANEST (articaine HCl 4% with epinephrine 1:100,000 or 1:200,000) is an amide local anesthetic commonly used in dentistry. Not effective for topical anesthesia; must be injected. Onset is rapid (1-3 min) with duration of pulpal anesthesia ~60-75 min and soft tissue anesthesia ~2-4 h. Maximum dose: 7 mg/kg (epinephrine 1:100,000) or 5 mg/kg (epinephrine 1:200,000). Avoid in patients with sulfite allergy (epinephrine component) or para-aminobenzoic acid (PABA) hypersensitivity. Caution in patients with methemoglobinemia (can cause methemoglobin formation at high doses). |
| Patient Advice | Avoid eating or drinking until numbness in mouth and throat has fully resolved (usually 2-4 hours) to prevent accidental biting or burns. · Do not chew gum or eat hard foods while numb. · Report any signs of allergic reaction (rash, hives, swelling, difficulty breathing) or prolonged numbness (>8 hours) to your dentist immediately. · Inform your dentist of all medications you are taking, especially MAO inhibitors, tricyclic antidepressants, beta-blockers, and anticoagulants. · If you have a history of sulfite sensitivity, tell your dentist before the procedure. |