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تعداد آیتم قابل مشاهده باقیمانده : 3 مورد

Landiolol: Drug information

Landiolol: Drug information
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For additional information see "Landiolol: Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: US
  • Rapiblyk
Brand Names: Canada
  • Sibboran
Pharmacologic Category
  • Antiarrhythmic Agent, Class II;
  • Beta-Blocker, Beta-1 Selective
Dosing: Adult

Dosage guidance:

Dosing: Landiolol is for short-term use only; limited experience with infusion durations >24 hours.

Dosage form information: Landiolol 280 mg base is equivalent to landiolol hydrochloride 300 mg.

Supraventricular tachycardia

Supraventricular tachycardia:

Rapiblyk:

Note: Doses are expressed as landiolol base.

IV continuous infusion: Initial: 9 mcg/kg/minute; titrate dose every 10 minutes based on response and tolerability by 9 mcg/kg/minute up to a maximum dose of 36 mcg/kg/minute.

Patients with impaired cardiac function: IV continuous infusion: Initial: 1 mcg/kg/minute; titrate dose every 15 minutes based on response and tolerability by 1 mcg/kg/minute up to a maximum dose of 36 mcg/kg/minute.

Sibboran [Canadian product]:

Note: Doses are expressed as landiolol hydrochloride.

Loading dose (optional): IV: 100 mcg/kg/minute for 1 minute (to achieve heart rate lowering in 1 to 4 minutes) followed by IV continuous infusion dosing below.

IV continuous infusion: Initial: 10 to 40 mcg/kg/minute to achieve heart rate lowering in ≤16 minutes; dose may be increased to a maximum of 80 mcg/kg/minute for a short period of time if necessary and if maximum daily dose has not been met; maximum total daily dose: 57.6 mg/kg/day (eg, infusion of 40 mcg/kg/minute for 24 hours).

Patients with left ventricular function impairment (left ventricular ejection fraction <40%, CI <2.5 L/minute/m2, New York Heart Association functional class 3 or 4): IV continuous infusion: Initial: 1 mcg/kg/minute; may increase stepwise to 10 mcg/kg/minute; further dose increases may be considered under close hemodynamic monitoring.

Transitioning to an alternative medication: After achieving heart rate control and stable clinical status, transition to alternative medication while considering pharmacokinetics and pharmacodynamics of that medication. If switching to an oral beta-blocker (or a different rate control medication), reduce landiolol dose by 50% over the next ~60 minutes using heart rate and clinical status as guide. If heart rate remains controlled for at least 1 hour, further reduction and discontinuation of landiolol should be considered.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Liver Impairment: Adult

Mild impairment (Child-Turcotte-Pugh class A): There are no specific dosage adjustments provided in the manufacturer's labeling (has not been studied). More conservative dose titration is recommended.

Moderate or severe impairment (Child-Turcotte-Pugh class B or C): Avoid use.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%: Cardiovascular: Hypotension (10%)

Frequency not defined: Local: Infusion-site reaction (including erythema at injection site, infusion-site pain, swelling at injection site)

Contraindications

Hypersensitivity to landiolol or any component of the formulation; severe sinus bradycardia; sick sinus syndrome; decompensated heart failure; cardiogenic shock; second- or third- degree AV block (without pacemaker); pulmonary hypertension.

Canadian labeling: Additional contraindications (not in the US labeling): Untreated pheochromocytoma; acute asthma attack; severe metabolic acidosis (uncorrectable); severe bradycardia (<50 beats per minute); severe hypotension.

Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Warnings/Precautions

Concerns related to adverse effects:

• Anaphylactic reactions: Use caution with history of severe anaphylaxis to allergens; patients taking beta-blockers may become more sensitive to repeated allergen challenges. Treatment of anaphylaxis (eg, epinephrine) in patients taking beta-blockers may be ineffective or promote undesirable effects.

• Hyperkalemia: May increase serum potassium; risk is increased in patients with kidney impairment.

• Hypotension: Can commonly occur; patients need close BP monitoring. Patients with hemodynamic compromise, hypovolemia, or on interacting medications are at increased risk. If an unacceptable drop in BP occurs, reduction in dose or discontinuation may reverse hypotension.

• Infusion site reactions: Can commonly occur including pain, swelling, and erythema; avoid infusion into small veins or through a butterfly catheter. If infusion site reaction occurs, use an alternative infusion site. Avoid extravasation.

• Metabolic acidosis: May cause hyperkalemic renal tubular acidosis which may be associated with reduced cardiac contractility.

Disease-related concerns:

• Bronchospastic disease: In general, patients with bronchospastic disease should not receive beta-blockers; however, landiolol with beta1 selectivity may be used cautiously with close monitoring; dose reduction may be necessary.

• Cardiac failure: Beta blockers can cause reduced myocardial contractility and may precipitate heart failure or cardiogenic shock. If signs or symptoms of cardiac failure occur, discontinue therapy and begin supportive care.

• Conduction abnormality: Can cause bradycardia; consider preexisting conditions such as first-degree AV block before initiating. Do not use in patients with pre-excited atrial fibrillation or suspected wide complex tachycardia associated with an accessory pathway as this can lead to ventricular arrhythmias.

• Diabetes: Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms.

• Liver impairment: Use with caution in patients with mild liver impairment; avoid use in patients with moderate to severe liver impairment.

• Peripheral vascular disease and Raynaud disease: May precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease and Raynaud disease; use with caution.

• Pheochromocytoma (untreated): Adequate alpha-blockade is required prior to use of any beta-blocker.

• Thyroid disease: May mask signs of hyperthyroidism (eg, tachycardia). If hyperthyroidism is suspected, carefully manage and monitor; abrupt withdrawal may exacerbate symptoms of hyperthyroidism or precipitate thyroid storm.

• Vasospastic angina: Beta-blockers without alpha1-adrenergic receptor blocking activity should be avoided in patients with vasospastic angina since unopposed alpha1-adrenergic receptors mediate coronary vasoconstriction and can worsen anginal symptoms (Mayer 1998).

Other warnings/precautions:

• Abrupt discontinuation: Severe exacerbations of angina, myocardial infarction, and ventricular arrhythmia may occur upon abrupt discontinuation in patients with coronary artery disease.

Product Availability

Rapiblyk: FDA approved November 2024; anticipated availability is currently unknown.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous [preservative free]:

Rapiblyk: 280 mg (1 ea)

Generic Equivalent Available: US

No

Pricing: US

Solution (reconstituted) (Rapiblyk Intravenous)

280 mg (per each): $1,020.00

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous:

Sibboran: 300 mg (1 ea)

Administration: Adult

IV: Administer as a continuous IV infusion. May be administered via central or peripheral catheter.

Use: Labeled Indications

Supraventricular tachycardia: Short-term reduction of ventricular rate in patients with supraventricular tachycardia, including atrial fibrillation and atrial flutter.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Acetylcholinesterase Inhibitors: May increase bradycardic effects of Beta-Blockers. Risk C: Monitor

Alfuzosin: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Alpha2-Agonists: Beta-Blockers may increase rebound hypertensive effects of Alpha2-Agonists. This effect can occur when the Alpha2-Agonist is abruptly withdrawn. Alpha2-Agonists may increase AV-blocking effects of Beta-Blockers. Sinus node dysfunction may also be enhanced. Management: Closely monitor heart rate during treatment with a beta blocker and clonidine. Withdraw beta blockers several days before clonidine withdrawal when possible, and monitor blood pressure closely. Recommendations for other alpha2-agonists are unavailable. Risk D: Consider Therapy Modification

Amifostine: Blood Pressure Lowering Agents may increase hypotensive effects of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider Therapy Modification

Amisulpride (Oral): May increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor

Antidiabetic Agents: Beta-Blockers (Beta1 Selective) may increase adverse/toxic effects of Antidiabetic Agents. Specifically, beta-blockers may mask the hypoglycemic symptoms of antidiabetic agents. Risk C: Monitor

Antipsychotic Agents (Phenothiazines): May increase hypotensive effects of Beta-Blockers. Beta-Blockers may decrease metabolism of Antipsychotic Agents (Phenothiazines). Antipsychotic Agents (Phenothiazines) may decrease metabolism of Beta-Blockers. Risk C: Monitor

Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may increase hypotensive effects of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor

Arginine: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Barbiturates: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Benperidol: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Beta2-Agonists: Beta-Blockers (Beta1 Selective) may decrease bronchodilatory effects of Beta2-Agonists. Of particular concern with nonselective beta-blockers or higher doses of the beta1 selective beta-blockers. Risk C: Monitor

Blood Pressure Lowering Agents: May increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor

Bradycardia-Causing Agents: May increase bradycardic effects of Landiolol. Risk X: Avoid

Brimonidine (Topical): May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Bromperidol: May decrease hypotensive effects of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may increase hypotensive effects of Bromperidol. Risk X: Avoid

Cafedrine: May increase bradycardic effects of Beta-Blockers. Beta-Blockers may decrease therapeutic effects of Cafedrine. Risk C: Monitor

Cannabis: Beta-Blockers may increase adverse/toxic effects of Cannabis. Specifically, the risk of hypoglycemia may be increased. Risk C: Monitor

Cholinergic Agonists: Beta-Blockers may increase adverse/toxic effects of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction. Risk C: Monitor

Diazoxide: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Dipyridamole: May increase bradycardic effects of Beta-Blockers. Risk C: Monitor

Disopyramide: May increase bradycardic effects of Beta-Blockers. Beta-Blockers may increase negative inotropic effects of Disopyramide. Risk C: Monitor

DOBUTamine: Beta-Blockers may decrease therapeutic effects of DOBUTamine. Risk C: Monitor

DULoxetine: Blood Pressure Lowering Agents may increase hypotensive effects of DULoxetine. Risk C: Monitor

EPHEDrine (Systemic): Beta-Blockers may decrease therapeutic effects of EPHEDrine (Systemic). Risk C: Monitor

EPINEPHrine (Nasal): Beta-Blockers (Beta1 Selective) may decrease therapeutic effects of EPINEPHrine (Nasal). Risk C: Monitor

EPINEPHrine (Oral Inhalation): Beta-Blockers (Beta1 Selective) may decrease therapeutic effects of EPINEPHrine (Oral Inhalation). Risk C: Monitor

EPINEPHrine (Systemic): Beta-Blockers (Beta1 Selective) may decrease therapeutic effects of EPINEPHrine (Systemic). Risk C: Monitor

Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): Beta-Blockers may increase vasoconstricting effects of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor

Etilefrine: Beta-Blockers may decrease therapeutic effects of Etilefrine. Etilefrine may increase bradycardic effects of Beta-Blockers. Risk C: Monitor

Etofylline: Beta-Blockers may decrease therapeutic effects of Etofylline. Risk X: Avoid

Fexinidazole: Bradycardia-Causing Agents may increase arrhythmogenic effects of Fexinidazole. Risk X: Avoid

Grass Pollen Allergen Extract (5 Grass Extract): Beta-Blockers may increase adverse/toxic effects of Grass Pollen Allergen Extract (5 Grass Extract). More specifically, Beta-Blockers may inhibit the ability to effectively treat severe allergic reactions to Grass Pollen Allergen Extract (5 Grass Extract) with epinephrine. Some other effects of epinephrine may be unaffected or even enhanced (e.g., vasoconstriction) during treatment with Beta-Blockers. Management: Consider alternatives to either grass pollen allergen extract (5 grass extract) or beta-blockers in patients with indications for both agents. Canadian product labeling specifically lists this combination as contraindicated. Risk D: Consider Therapy Modification

Herbal Products with Blood Pressure Lowering Effects: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Hypotension-Associated Agents: Blood Pressure Lowering Agents may increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor

Iloperidone: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Isoproterenol: Beta-Blockers may decrease therapeutic effects of Isoproterenol. Risk C: Monitor

Lacosamide: Bradycardia-Causing Agents may increase AV-blocking effects of Lacosamide. Risk C: Monitor

Levodopa-Foslevodopa: Blood Pressure Lowering Agents may increase hypotensive effects of Levodopa-Foslevodopa. Risk C: Monitor

Lormetazepam: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Mavacamten: Beta-Blockers may increase adverse/toxic effects of Mavacamten. Specifically, negative inotropic effects may be increased. Risk C: Monitor

Metergoline: May decrease antihypertensive effects of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may increase orthostatic hypotensive effects of Metergoline. Risk C: Monitor

Methacholine: Beta-Blockers may increase adverse/toxic effects of Methacholine. Risk C: Monitor

Midodrine: May increase bradycardic effects of Bradycardia-Causing Agents. Risk C: Monitor

Mivacurium: Beta-Blockers may increase therapeutic effects of Mivacurium. Risk C: Monitor

Molsidomine: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Naftopidil: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Nicergoline: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Nicorandil: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

NIFEdipine (Topical): May increase adverse/toxic effects of Beta-Blockers. Risk C: Monitor

NIFEdipine: May increase hypotensive effects of Beta-Blockers. NIFEdipine may increase negative inotropic effects of Beta-Blockers. Risk C: Monitor

Nitrendipine: May increase therapeutic effects of Beta-Blockers. Risk C: Monitor

Nitroprusside: Blood Pressure Lowering Agents may increase hypotensive effects of Nitroprusside. Risk C: Monitor

Nonsteroidal Anti-Inflammatory Agents (Topical): May decrease therapeutic effects of Beta-Blockers. Risk C: Monitor

Nonsteroidal Anti-Inflammatory Agents: May decrease antihypertensive effects of Beta-Blockers. Risk C: Monitor

Obinutuzumab: May increase hypotensive effects of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Risk D: Consider Therapy Modification

Opipramol: Beta-Blockers may increase serum concentration of Opipramol. Opipramol may increase serum concentration of Beta-Blockers. Risk C: Monitor

Pentoxifylline: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Pholcodine: Blood Pressure Lowering Agents may increase hypotensive effects of Pholcodine. Risk C: Monitor

Phosphodiesterase 5 Inhibitors: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Prostacyclin Analogues: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Quinagolide: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Reserpine: May increase hypotensive effects of Beta-Blockers. Reserpine may increase bradycardic effects of Beta-Blockers. Risk C: Monitor

Rivastigmine: May increase bradycardic effects of Beta-Blockers. Risk X: Avoid

Silodosin: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor

Succinylcholine: Beta-Blockers may increase neuromuscular-blocking effects of Succinylcholine. Risk C: Monitor

Sympathomimetics: May decrease therapeutic effects of Landiolol. Risk C: Monitor

Tasimelteon: Beta-Blockers may decrease therapeutic effects of Tasimelteon. Management: Consider avoiding nighttime administration of beta-blockers during tasimelteon therapy due to the potential for reduced tasimelteon efficacy. Risk D: Consider Therapy Modification

Theodrenaline: May increase bradycardic effects of Beta-Blockers. Beta-Blockers may decrease therapeutic effects of Theodrenaline. Risk C: Monitor

Theophylline Derivatives: Beta-Blockers (Beta1 Selective) may decrease bronchodilatory effects of Theophylline Derivatives. Risk C: Monitor

White Birch Allergen Extract: Beta-Blockers may increase adverse/toxic effects of White Birch Allergen Extract. Specifically, beta-blockers may reduce the effectiveness of beta-agonists that may be required to treat systemic reactions to white birch allergen extract. Risk X: Avoid

Pregnancy Considerations

Outcome data following use of landiolol during delivery are limited (Abe 2010; Ishizaki 2021; Kubo 2005; Saeki 2010). In a small study, a single dose of landiolol prior to intubation in patients undergoing cesarean delivery was found to prevent intraoperative and postoperative tachycardia and/or hypertension without adversely effecting uterine contractions or Apgar scores (Suehiro 2012).

Breastfeeding Considerations

It is not known if landiolol is present in breast milk.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.

Monitoring Parameters

BP, heart rate, continuous ECG; serum glucose (in patients with diabetes); signs/symptoms of bronchospasm in patients with existing bronchospastic disease, serum potassium (especially with kidney impairment), IV site; consult institutional policies and procedures.

Mechanism of Action

Ultra-short-acting selective beta1-adrenergic receptor site blocker that reduces heart rate, slows conduction, and increases refractory period of the AV node. It does not have any membrane-stabilizing activity or any intrinsic sympathomimetic activity.

Pharmacokinetics (Adult Data Unless Noted)

Distribution: 0.3 to 0.4 L/kg.

Protein binding: <10%.

Metabolism: Metabolized via hydrolysis of the ester moiety in the plasma by pseudocholinesterases and carboxylesterases. Active metabolite, M1, has <1/40th of the pharmacological activity of landiolol.

Half-life elimination: Bolus: 3.2 minutes; Infusion: 4.5 minutes.

Excretion: Urine (~50% to 75% within 4 hours [54.4% and 11.5% as M1 and M2 metabolites]; 89% to 99% within 24 hours [landiolol and M1 and M2 metabolites]).

Clearance: Bolus: 66.1 mL/kg/minute; Infusion: 57 mL/kg/minute.

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Liver impairment: Patients with mild liver impairment have shown an increased landiolol plasma concentration by ~40% to 44%.

  1. Abe T, Yamamoto S, Yasuda N, et al. Effective control of paroxysmal tachycardia with landiolol hydrochloride during cesarean section in a patient with hypertrophic obstructive cardiomyopathy. J Anesth. 2010;24(5):765-767. doi:10.1007/s00540-010-1000-8 [PubMed 20711617]
  2. Ishizaki H, Murata H, Maekawa T, Ichinomiya T, Hara T. Successful vaginal delivery in a parturient with long QT syndrome type 2 using double-catheter epidural analgesia: a CARE-compliant case report. Medicine (Baltimore). 2021;100(47):e27790. doi:10.1097/MD.0000000000027790 [PubMed 34964742]
  3. Kubo K, Murao K, Nakao S, Kanoda T, Yamada M, Shingu K. Successful management of cesarean section in a patient with Romano-Ward syndrome using landiolol, a selective and short-acting beta1 receptor antagonist. J Anesth. 2005;19(2):174-176. doi:10.1007/s00540-005-0302-8 [PubMed 15875139]
  4. Mayer S, Hillis LD. Prinzmetal's variant angina. Clin Cardiol. 1998;21(4):243-246. doi:10.1002/clc.4960210403 [PubMed 9562933]
  5. Rapiblyk (landiolol) [prescribing information]. Vienna, Austria: AOP Orphan Pharmaceuticals GmbH; November 2024.
  6. Saeki N, Taguchi S, Kawamoto M. Successful management of a patient with Marfan syndrome complicated with acute aortic dissection using landiolol during Cesarean section. J Anesth. 2010;24(2):277-279. doi:10.1007/s00540-009-0859-8 [PubMed 20101513]
  7. Sibboran (landiolol) [product monograph]. Concord, Ontario, Canada: Trimedic Therapeutics Inc; November 2023.
  8. Suehiro K, Okutani R. Landiolol attenuates cardiovascular response at induction of general anesthesia for cesarean delivery. J Anesth. 2012;26(2):200-205. doi:10.1007/s00540-011-1305-2 [PubMed 22179601]
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