ARESTOCAINE HYDROCHLORIDE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ARESTOCAINE HYDROCHLORIDE (ARESTOCAINE HYDROCHLORIDE).
Arestocaine hydrochloride is a local anesthetic of the amide type. It stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthesia.
| Metabolism | Primarily metabolized by the liver via hydrolysis by esterases (though it is an amide, it may be partially hydrolyzed) and conjugation. The major metabolic pathways involve CYP1A2 and CYP3A4. |
| Excretion | Renal excretion of unchanged drug and metabolites; approximately 90% excreted in urine as parent compound and metabolites (60% as unchanged drug, 30% as metabolites), with less than 10% fecal elimination. |
| Half-life | Terminal elimination half-life is approximately 1.5–2 hours in adults with normal hepatic and renal function; prolonged in hepatic impairment or congestive heart failure. |
| Protein binding | Approximately 70% bound primarily to alpha-1-acid glycoprotein (AAG) and to a lesser extent albumin. |
| Volume of Distribution | Volume of distribution is 0.8–1.5 L/kg, reflecting extensive tissue distribution; higher in neonates and infants. |
| Bioavailability | Topical: variable, approximately 30–50% absorbed through intact skin; Oral: negligible due to extensive first-pass metabolism (bioavailability <10%); Intravenous: 100%. |
| Onset of Action | Infiltration: <2 minutes; Nerve block: 5–15 minutes; Epidural: 10–20 minutes; Topical: 2–5 minutes. |
| Duration of Action | Infiltration: 30–60 minutes (with epinephrine: 60–90 minutes); Nerve block: 60–90 minutes (with epinephrine: 2–3 hours); Epidural: 30–60 minutes. |
2-5 mg/kg intramuscularly every 60-90 minutes, not to exceed 500 mg total dose in a 12-hour period.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-50 mL/min: reduce dose by 25%; GFR 15-29 mL/min: reduce dose by 50%; GFR <15 mL/min: avoid use. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use. |
| Pediatric use | 1-3 mg/kg intramuscularly every 60-90 minutes, max 200 mg per dose; maximum cumulative dose 400 mg/12 hours. |
| Geriatric use | Initiate at lowest effective dose (2 mg/kg) due to increased sensitivity and potential for prolonged duration; monitor for adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ARESTOCAINE HYDROCHLORIDE (ARESTOCAINE HYDROCHLORIDE).
| Breastfeeding | No data on excretion in human milk. M/P ratio unknown. Caution advised; discontinue breastfeeding or drug based on importance of drug to mother. |
| Teratogenic Risk | Pregnancy Category C. Animal reproduction studies have not been conducted. In first trimester, limited data; potential for adverse effects on fetal development cannot be excluded. In second and third trimesters, risk of placental transfer and fetal bradycardia; use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
There is no FDA black box warning for Arestocaine hydrochloride.
| Serious Effects |
["Hypersensitivity to amide-type local anesthetics","Severe hypotension","Myasthenia gravis (relative contraindication)","Bradycardia"]
| Precautions | ["Risk of systemic toxicity if injected intravascularly","Use with caution in patients with hepatic impairment","Use with caution in patients with cardiovascular disease","Risk of methemoglobinemia in patients with glucose-6-phosphate dehydrogenase deficiency"] |
| Food/Dietary | No specific food interactions; avoid hot foods until numbness resolves to prevent burns. |
| Clinical Pearls |
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| Monitor maternal heart rate, blood pressure, and signs of CNS toxicity. Fetal heart rate monitoring recommended during labor and delivery. |
| Fertility Effects | No studies on fertility effects. Animal studies not available; potential for transient reduction in fertility due to systemic toxicity at high doses. |
| ARESTOCAINE HYDROCHLORIDE (presumed anesthetic) is not a recognized drug; likely a misspelling of articaine or similar. If referring to articaine, clinical pearls: 1) Onset within 1-3 minutes, duration 1-3 hours; 2) Metabolized by plasma esterases, caution in pseudocholinesterase deficiency; 3) Maximum dose 7 mg/kg (adults) to avoid CNS/cardiac toxicity; 4) Contains sulfites, avoid in allergic patients. |
| Patient Advice | Avoid chewing or biting lips/cheeks while numb to prevent injury. · Report any signs of allergic reaction (rash, swelling, difficulty breathing) immediately. · Do not consume hot foods or beverages until sensation returns. · Inform dentist of all medications, especially MAOIs or anticoagulants. |