ULTACAN FORTE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ULTACAN FORTE (ULTACAN FORTE).
Cimetidine is a histamine H2-receptor antagonist that inhibits gastric acid secretion by competitively blocking histamine at H2 receptors on parietal cells.
| Metabolism | Hepatic via CYP1A2, CYP2C19, CYP2D6, and CYP3A4; also undergoes sulfoxidation and N-demethylation. |
| Excretion | Renal (90% as unchanged drug), biliary/fecal (10%) |
| Half-life | Terminal elimination half-life: 3–5 hours (prolonged to 12–24 hours in severe renal impairment; dose adjustment required if CrCl < 30 mL/min). |
| Protein binding | 98% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | 0.15–0.3 L/kg (suggests low tissue distribution, mainly confined to vascular space). |
| Bioavailability | Oral: 80–90%; Intramuscular: 100%. |
| Onset of Action | Oral: 30–60 minutes; Intramuscular: 5–10 minutes; Intravenous: 1–3 minutes. |
| Duration of Action | Oral: 4–6 hours; Intramuscular: 3–4 hours; Intravenous: 2–4 hours. Duration extended in hepatic or renal impairment. |
| Molecular Weight | 312.4 |
1 tablet (5 mg bisoprolol) orally once daily; maximum 10 mg once daily.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-50 mL/min: reduce initial dose to 2.5 mg once daily; increase cautiously. GFR < 30 mL/min: use 2.5 mg once daily with careful titration. |
| Liver impairment | Child-Pugh A or B: dose reduction recommended; start at 2.5 mg once daily. Child-Pugh C: contraindicated. |
| Pediatric use | Not recommended for use in pediatric patients due to lack of safety and efficacy data. |
| Geriatric use | Initiate at 2.5 mg once daily with gradual titration; monitor heart rate and blood pressure closely. |
| 1st trimester | Avoid; potential teratogenic effects (animal data, no adequate human studies). |
| 2nd trimester | Use only if benefit outweighs risk; may cause fetal harm (oligohydramnios, renal dysfunction). |
| 3rd trimester | Contraindicated; risk of premature closure of ductus arteriosus, oligohydramnios, neonatal renal impairment. |
Clinical note
Comprehensive clinical and safety monograph for ULTACAN FORTE (ULTACAN FORTE).
| Placental transfer | Crosses placenta; animal studies show transfer, human data limited but documented transfer occurs. |
| Breastfeeding | Excreted in breast milk; due to potential adverse effects on infant (e.g., CNS effects, renal impairment), breastfeeding is not recommended during therapy. Consider discontinuing drug or breastfeeding. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to active substance or excipientsThird trimester of pregnancySevere hepatic impairment (Child-Pugh C)Severe renal impairment (eGFR < 30 mL/min/1.73 m²)History of gastrointestinal bleeding or perforation related to previous NSAIDsActive peptic ulcer / gastrointestinal bleedingSevere uncontrolled heart failure
| Precautions | Cimetidine is a potent inhibitor of CYP enzymes and can increase serum levels of many drugs (e.g., warfarin, theophylline, phenytoin). Avoid abrupt discontinuation in long-term therapy (risk of acid rebound). Use with caution in elderly and renally impaired patients, as decreased clearance may require dose adjustment. CNS effects (confusion, hallucinations) more common in elderly or severely ill patients; reversible upon discontinuation. May cause gynecomastia and sexual dysfunction with prolonged use. |
| Food/Dietary | There are no known food interactions with ULTRACAN FORTE. No dietary restrictions are required. However, caffeine-containing beverages should be limited as they may exacerbate epinephrine-induced tachycardia. |
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| Lactation Rating |
| L5 - Contraindicated |
| Teratogenic Risk | ULTACAN FORTE is contraindicated in pregnancy. First trimester: Crosses placenta; associated with major congenital malformations (neural tube defects, cardiovascular anomalies). Second/third trimester: Risk of fetal renal impairment, oligohydramnios, premature ductus arteriosus closure, and neonatal pulmonary hypertension. |
| Fetal Monitoring | Monitor maternal renal function (serum creatinine, BUN), hepatic enzymes, and blood pressure. Fetal ultrasound to assess amniotic fluid volume, renal anatomy, and ductus arteriosus patency. Neonatal monitoring for hypotension, renal impairment, and hyperbilirubinemia after delivery. |
| Fertility Effects | Reversible impairment of spermatogenesis in males; decreased sperm count and motility. In females, possible disruption of ovarian function and menstrual irregularities. Long-term effects on fertility not fully characterized. |
| Clinical Pearls | ULTRACAN FORTE (bupivacaine HCl 0.5% with epinephrine 1:200,000) is a long-acting amide local anesthetic used for surgical anesthesia and postoperative pain management. Onset of action is 5–10 minutes, duration 3–6 hours with epinephrine. Maximum dose: 2 mg/kg (without epinephrine) or 3 mg/kg (with epinephrine). Do not exceed 400 mg in 24 hours. Avoid in patients with hypersensitivity to amide anesthetics, severe hepatic disease, or myasthenia gravis. Epinephrine component may cause tachycardia or hypertension; use cautiously in cardiovascular disease, hyperthyroidism, or patients on MAOIs or tricyclic antidepressants. Always aspirate before injection to prevent intravascular administration. For epidural use, test dose (3 mL with epinephrine) should be given to rule out intrathecal or intravascular placement. Do not use in paracervical block in obstetrics due to risk of fetal bradycardia. Store at 20–25°C; do not freeze. |
| Patient Advice | You will receive this medication as an injection near the area where surgery or a procedure will be performed. It numbs the area so you do not feel pain. · The numbing effect starts within a few minutes and can last up to 6 hours. Do not touch or scratch the numb area as you could injure it without feeling it. · Avoid driving or operating machinery until the numbness has completely worn off and you are no longer feeling dizzy or drowsy. · Tell your doctor if you have liver disease, heart problems, thyroid disorders, or if you take medications for depression or high blood pressure. · If you experience any of the following after the injection, seek emergency medical help: difficulty breathing, swelling of the face or lips, fast or irregular heartbeat, severe headache, or seizures. · Do not eat or drink anything until the numbness in your mouth or throat (if applicable) has resolved to prevent choking or biting your tongue. |