Levosimendan


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Acutely decompensated heart failure
Adult: In situations where conventional therapy is insufficient and inotropic support is considered appropriate: Loading dose: 6-12 mcg/kg via infusion over 10 minutes. Maintenance: 0.1 mcg/kg/min via continuous infusion; may decrease to 0.05 mcg/kg/min if significant hypotension or tachycardia occur or may increase to 0.2 mcg/kg/min if the initial dose is tolerated and an increased haemodynamic effect is required. Dose and duration of treatment are individualised according to the patient’s clinical condition and response. Patients on concomitant IV vasodilators and/or inotropes: Reduce loading dose to 6 mcg/kg over 10 minutes.
Suy thận
CrCl (mL/min) Dosage
<30 Contraindicated.

Suy gan
Severe: Contraindicated.
Hướng dẫn pha thuốc
To prepare the 0.025 mg/mL infusion, mix 5 mL of the 2.5 mg/mL inj concentrate with 500 mL of dextrose 5% solution. To prepare the 0.05 mg/mL infusion, mix 10 mL of 2.5 mg/mL inj concentrate with 500 mL of dextrose 5% solution.
Chống chỉ định
Severe hypotension and tachycardia, history of torsades de pointes, significant mechanical obstructions affecting ventricular filling and/or outflow. Severe hepatic and renal (CrCl <30 mL/min) impairment. Lactation.
Thận trọng
Patient with low baseline systolic or diastolic blood pressure or those at risk for a hypotensive episode, concurrent ischaemic CV disease and anaemia, tachycardia, atrial fibrillation with rapid ventricular response or potentially life-threatening arrhythmia, ongoing coronary ischaemia, long QTc interval regardless of aetiology. Patients taking QTc prolonging agents or concomitant IV vasodilators or inotropes. Severe hypovolaemia and hypokalaemia should be corrected prior to the administration. Mild to moderate hepatic and renal impairment. Pregnancy.
Tác dụng không mong muốn
Significant: Hypokalaemia, decreased Hb and haematocrit, ventricular tachycardia, atrial fibrillation, ventricular extrasystoles, hypotension.
Cardiac disorders: Myocardial ischaemia, cardiac failure.
Gastrointestinal disorders: Diarrhoea, constipation, nausea, vomiting.
Nervous system disorders: Headache, dizziness.
Psychiatric disorders: Insomnia.
Chỉ số theo dõi
Monitor ECG, blood pressure and heart rate during treatment and at least 3 days (5 days in patients with mild to moderate renal and hepatic impairment) after the end of infusion or until the patient is clinically stable; serum K during treatment; urine output. Assess haemodynamic response immediately after loading dose and within 30-60 minutes of any dosage adjustment.
Quá liều
Symptoms: Hypotension, tachycardia. Management: Hypotension may be treated with vasopressors (e.g. dopamine in patients with CHF and epinephrine in patients following cardiac surgery). Parenteral fluids may be administered for excessive decreases in cardiac filling pressures. Continuous ECG, invasive haemodynamic monitoring, and repeated determinations of serum electrolytes must be performed.
Tương tác
Increased risk of hypotension with other IV vasoactive agents. May increase the exposure of drugs that are primarily metabolised by CYP2C8 (e.g. loperamide, pioglitazone, repaglinide, enzalutamide). Concomitant use with isosorbide mononitrate may potentiate orthostatic hypotensive response.
Tương tác với thức ăn
May reduce the effects of alcohol.
Tác dụng
Description: Levosimendan is a cardiac inotrope and vasodilator with Ca-sensitising properties. It sensitises Ca-dependent troponin C in cardiac tissue, thus increasing contractility. It also opens ATP-sensitive K channels on vascular smooth muscle thereby inducing vasodilation. The combined inotropic and vasodilator activity leads to an increased force of contraction with decreased preload and afterload in the myocardium.
Duration: Haemodynamic effects: Up to 7-9 days after discontinuation of a 24-hour infusion.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: Approx 2 days after infusion is stopped (OR-1855 and OR-1896).
Distribution: Plasma protein binding: 97-98% (levosimendan), mainly to albumin; 39% (OR-1855); 42% (OR-1896).
Metabolism: Extensively metabolised via conjugation to cyclic or N-acetylated cysteinylglycine and cysteine conjugates; approx 5% is metabolised in the intestine via reduction to aminophenylpyridazinone (OR-1855), which after reabsorption to the systemic circulation is metabolised in the plasma by N-acetyltransferase to the active metabolite OR-1896.
Excretion: Via urine (54%, as metabolites) and faeces (44%). Elimination half-life: Approx 1 hour (levosimendan); approx 75-80 hours (OR-1855 and OR-1896).
Đặc tính

Chemical Structure Image
Levosimendan

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3033825, Levosimendan. https://pubchem.ncbi.nlm.nih.gov/compound/Levosimendan. Accessed Sept. 27, 2022.

Bảo quản
Intact vials: Store between 2-8°C. Diluted solutions are stable for up to 24 hours when stored between 2-8°C. Do not freeze.
Phân loại MIMS
Các loại thuốc tim mạch khác
Phân loại ATC
C01CX08 - levosimendan ; Belongs to the class of other cardiac stimulants excluding glycosides. Used in the treatment of hypotension.
Tài liệu tham khảo
Anon. Levosimendan. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 18/08/2022.

Buckingham R (ed). Levosimendan. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 18/08/2022.

Orion Pharma (NZ) Limited. Simdax 2.5 mg/mL Injection Concentrate data sheet 16 May 2022. Medsafe. http://www.medsafe.govt.nz. Accessed 18/08/2022.

Simdax 2.5 mg/mL Concentrate for Solution for Infusion (Orion Corporation). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 18/08/2022.

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