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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ULTACAN FORTE (ULTACAN FORTE).
| Breastfeeding | Excreted in human milk; M/P ratio not established. Potential for adverse effects in nursing infant (e.g., renal dysfunction, photosensitivity). Discontinue breastfeeding or drug, considering importance to mother. |
| 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. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to cimetidine or any component of the formulation.
| 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. |
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| 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. |