ULTACAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ULTACAN (ULTACAN).
Histamine H2-receptor antagonist; inhibits gastric acid secretion by competitively blocking H2 receptors on parietal cells.
| Metabolism | Hepatic metabolism via N-demethylation (CYP450 enzymes: CYP1A2, CYP3A4, CYP2D6); also undergoes S-oxidation and reduction of the sulfoxide. |
| Excretion | Renal excretion accounts for approximately 60-70% of the administered dose as unchanged drug, with biliary/fecal elimination contributing 20-30%. |
| Half-life | Terminal elimination half-life is 3-5 hours in adults with normal renal function; prolonged to 12-20 hours in severe renal impairment (CrCl < 30 mL/min). |
| Protein binding | Approximately 85-90% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8-1.2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 60-70% (first-pass metabolism); Intramuscular: 90-100%. |
| Onset of Action | Intravenous: 5-10 minutes; Intramuscular: 15-30 minutes; Oral: 30-60 minutes. |
| Duration of Action | Intravenous: 4-6 hours; Intramuscular: 6-8 hours; Oral: 8-12 hours. Clinical effect correlates with plasma concentrations above 1 mcg/mL. |
| Molecular Weight | 330.35 |
1-2 mg/kg intravenously every 4-6 hours as needed for moderate to severe pain. Maximum single dose: 10 mg.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-60 mL/min: administer 50-75% of normal dose every 6-8 hours. GFR <30 mL/min: administer 50% of normal dose every 8-12 hours. Not recommended in ESRD. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 25-50%. Child-Pugh Class C: avoid use or reduce dose by 75%. |
| Pediatric use | Children 1-12 years: 0.1-0.2 mg/kg intravenously every 4-6 hours as needed. Maximum single dose: 0.2 mg/kg. Not to exceed 10 mg per dose. |
| Geriatric use | Initiate at 50% of recommended adult dose (0.5-1 mg intravenously every 6-8 hours). Titrate cautiously due to increased sensitivity and risk of respiratory depression. |
| 1st trimester | Avoid use during first trimester due to potential teratogenicity; limited human data. |
| 2nd trimester | Use only if clearly needed; weigh risks vs benefits. |
| 3rd trimester | Avoid in third trimester due to risk of premature closure of ductus arteriosus and oligohydramnios. |
Clinical note
Comprehensive clinical and safety monograph for ULTACAN (ULTACAN).
| Placental transfer | Crosses placenta; animal studies show transfer. |
| Breastfeeding | Excreted into breast milk in small amounts; consider risk of infant exposure, especially in neonates with immature renal function. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to ULTACANSevere hepatic impairmentHistory of drug-induced agranulocytosis
| Precautions | May cause confusion, especially in elderly or renally impaired patients; adjust dose in renal impairment., Risk of community-acquired pneumonia; avoid prolonged use., May mask symptoms of gastric cancer; exclude malignancy before treatment., Potential for vitamin B12 deficiency with long-term use., May increase risk of Clostridioides difficile infection. |
| Food/Dietary | No known food interactions. However, since the drug contains epinephrine, avoid high-dose caffeine or stimulants that may synergistically increase heart rate or blood pressure. Use with caution in patients on tyramine-rich foods if on MAOIs (though rarely relevant for dental use). |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | First trimester: Potential teratogen; increased risk of neural tube defects and congenital heart defects (based on animal studies). Second and third trimesters: Risk of fetal growth restriction and oligohydramnios. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function, and electrolytes. Fetal ultrasound for growth and amniotic fluid volume every 4 weeks. Nonstress test or biophysical profile weekly after 32 weeks. |
| Fertility Effects | May impair fertility in males (reduced sperm count) and females (ovarian dysfunction) based on animal studies. Clinical significance unknown. |
| Clinical Pearls | Ultacan (lidocaine 2% with epinephrine 1:100,000) is a local anesthetic used for dental procedures. Avoid intravascular injection; aspirate before administering. Limit dose to 7 mg/kg of lidocaine with epinephrine. Use with caution in patients with severe hepatic disease, pseudo cholinesterase deficiency, or sulfite allergy. Epinephrine may cause significant pressor response in patients on non-selective beta-blockers. Do not use in areas of infection or inflammation due to reduced efficacy. Monitor for signs of CNS toxicity (tinnitus, metallic taste, perioral numbness) and cardiac toxicity (hypotension, bradycardia). |
| Patient Advice | Ultacan is a local anesthetic that numbs the treatment area for dental procedures. · You may experience temporary numbness of the lips, tongue, and surrounding tissues; avoid hot foods or drinks until sensation returns to prevent burns. · If you experience any signs of allergic reaction (rash, swelling, difficulty breathing), seek immediate medical attention. · Notify your dentist if you have a history of liver disease, sulfite allergy, or are taking beta-blockers or MAO inhibitors. · Do not drive or operate heavy machinery until full sensation returns and you are no longer feeling any effects of the anesthetic. · If the numbness persists beyond a few hours or you develop pain, swelling, or bleeding, contact your dentist. |