Levosimendan
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| Image:Levosimendan.png | |
| Levosimendan
| |
| Systematic (IUPAC) name | |
| (-)-(R)-(4-(4-methyl-6-oxo- 1,4,5,6-tetrahydropyridazin-3-yl)phenyl) carbonohydrazonoyl dicyanide | |
| Identifiers | |
| CAS number | 141505-33-1 |
| ATC code | C01CX08 |
| PubChem | 3033825 |
| DrugBank | APRD01296 |
| Chemical data | |
| Formula | C14H12N6O |
| Mol. weight | 280.28 |
| Pharmacokinetic data | |
| Bioavailability | 85% (oral) |
| Metabolism | hepatic |
| Half life | 1 hour |
| Excretion | renal |
| Therapeutic considerations | |
| Pregnancy cat. |
no data |
| Legal status |
Prescription only |
| Routes | IV |
Levosimendan (INN) (IPA: [ˌlivosaɪˈmɛmdən]) is a calcium sensitiser used in the management of severe congestive heart failure and is considered an agent of last resort. It is marketed under the trade name Simdax (Abbott).
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[edit] Mode of action
Levosimendan is a calcium sensitiser – it increases the sensitivity of the heart to calcium, thus increasing cardiac contractility. Levosimendan exerts its positive inotropic effect by increasing calcium sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner. It also has a vasodilatory effect, by opening adenosine triphosphate (ATP)-sensitive potassium channels in vascular smooth muscle to cause smooth muscle relaxation. The combined inotropic and vasodilatory actions result in an increased force of contraction, decreased preload and decreased afterload.
[edit] Clinical use
[edit] Indications
Levosimendan is indicated for inotropic support in acutely-decompensated severe congestive heart failure. Owing to its cost, it is usually reserved for last-line therapy when other inotropes (e.g. dobutamine) have failed.
[edit] Contraindications
The use of levosimendan is contraindicated in patients with: moderate-to-severe renal impairment, severe hepatic impairment, severe ventricular filling or outflow obstruction, severe hypotension and tachycardia, and/or history of torsades de pointes (Rossi, 2006).
[edit] Adverse effects
Common adverse drug reactions (≥1% of patients) associated with levosimendan therapy include: headache, hypotension, arrhythmias (atrial fibrillation, extrasystoles, atrial tachycardia, ventricular tachycardia), myocardial ischaemia, hypokalaemia and/or nausea (Rossi, 2006).
[edit] Formulations
Levosimendan is marketed as a 2.5 mg/mL concentrated solution for IV infusion. The concentrate is diluted with glucose 5% solution before infusion.
[edit] References
- Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006.
