RAPLON
Clinical safety rating
cautionComprehensive clinical and safety monograph for RAPLON (RAPLON).
RAPLON (levosimendan) is a calcium sensitizer that increases myocardial contractility by sensitizing troponin C to calcium, and it also opens ATP-sensitive potassium channels, causing vasodilation.
| Metabolism | Primarily metabolized by the liver via conjugation to a methyl ester, which is then further conjugated by glutathione-S-transferase. The active metabolite (OR-1896) has a long half-life. |
| Excretion | Primarily renal excretion of unchanged drug (approximately 80-90% of administered dose within 24 hours); minor biliary/fecal elimination (less than 10%). |
| Half-life | Terminal elimination half-life is approximately 1.5-2.5 hours in patients with normal renal function; prolonged in renal impairment (up to 6-8 hours in end-stage renal disease). |
| Protein binding | Approximately 30-40% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.2-0.3 L/kg, indicating distribution primarily into extracellular fluid. |
| Bioavailability | Intravenous: 100% (only route used clinically). Intramuscular: Not routinely used; bioavailability data limited. |
| Onset of Action | Intravenous: Rapid onset, within 1-2 minutes. Intramuscular: 5-10 minutes. |
| Duration of Action | Duration of neuromuscular blockade: Approximately 30-45 minutes after standard intubating dose; prolonged with repeated doses or in renal failure. |
| Molecular Weight | 282.34 |
0.2 mg/kg IV bolus over 30 seconds; may repeat once if necessary after 15 minutes.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required; RAPLON is not significantly renally eliminated. |
| Liver impairment | Child-Pugh A and B: no adjustment; Child-Pugh C: use with caution, consider reducing dose by 50% due to prolonged duration. |
| Pediatric use | 0.2 mg/kg IV bolus over 30 seconds; maximum single dose 10 mg; may repeat once after 15 minutes. |
| Geriatric use | Use 0.15 mg/kg IV bolus over 30 seconds due to increased sensitivity and risk of prolonged neuromuscular blockade. |
| 1st trimester | Limited data; use only if benefit outweighs risk. Animal studies show no teratogenicity. |
| 2nd trimester | Use with caution; monitor for uterine hyperstimulation and fetal distress. |
| 3rd trimester | Avoid in third trimester except for induction of labor due to risk of uterine rupture and fetal harm. |
Clinical note
Comprehensive clinical and safety monograph for RAPLON (RAPLON).
| Placental transfer | Crosses placenta; degree of transfer not well characterized. |
| Breastfeeding | Not recommended during breastfeeding. Excretion into human milk unknown; potential for adverse effects in infant. |
| Lactation Rating | L5 |
| Teratogenic Risk | Pregnancy Category C. No adequate human studies. Trimester 1: Risk of fetal malformations cannot be ruled out; animal studies show decreased fetal weight at maternally toxic doses. Trimester 2-3: Potential for fetal respiratory depression or apnea when used near term; avoid during labor. |
| Fetal Monitoring | Continuous fetal heart rate monitoring if used during pregnancy; observe neonate for respiratory depression if used near delivery. |
| Fertility Effects | No known effect on fertility in animal studies; human data unavailable. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to raplon or any carbamateSevere hepatic impairmentNarrow-angle glaucomaHistory of epilepsy or seizure disorderHemorrhagic diathesis
| Precautions | Hypotension; tachyarrhythmias; renal impairment; electrolyte disturbances (hypokalemia, hypomagnesemia) may increase risk of arrhythmias; monitoring of blood pressure, heart rate, and ECG required; not recommended in severe hepatic impairment. |
| Food/Dietary | Grapefruit and grapefruit juice may increase the effects and prolong paralysis. Clarithromycin, itraconazole, and other CYP3A4 inhibitors can enhance duration. Avoid high-fat meals shortly before use as they may delay onset. |
| Clinical Pearls | RAPLON (rapacuronium) is a rapid-onset, short-duration nondepolarizing neuromuscular blocker. It produces paralysis within 60-90 seconds and lasts 15-20 minutes. Avoid in patients with significant hepatic or renal impairment. Use with caution in elderly and those with electrolyte imbalances. Reversal with neostigmine is effective but may require higher doses. Monitor for histamine release and bronchospasm, especially in asthmatics. |
| Patient Advice | This medication causes complete paralysis, including inability to breathe, so you will be on a breathing machine. · Tell your doctor if you have asthma, liver or kidney disease, or any allergies. · Inform your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. · You may experience temporary muscle weakness after the drug wears off. · Avoid grapefruit and grapefruit juice before and after procedure. · Report any difficulty breathing, rash, or itching immediately. |
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