vernakalant

Action and Spectrum

Actions and Spectrum: 

Actions: 

Indicated in patients with recent onset of Atrial Fibrillation on which upon IV administration of vernakalant rapid conversion of AF to sinus rhythm is seen in adults for non-surgery patients where AF lasts for 7 days and for post-cardiac surgery patients where AF is less than 3 days. 

Spectrum: 

vernakalant is a Class III Antiarrhythmic agent that is used in patients with Atrial Fibrillation which is recent to convert this into sinus rhythm after IV administration. Used both in non-surgery patients where AF lasts for 7 days of duration and in post-cardiac surgery patients where AF lasts for 3 days of duration. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Hypotension (13%) 

Dysgeusia (18%) 

Sneezing (13%)  

1-10% 

Atrial Flutter (2 -10%) 

Bradycardia (2 – 8%) 

Ventricular arrhythmia (<6%) 

Hypertension (1 – 2%) 

1st degree AV – Block (1%) 

Ventricular tachycardia (1%) 

Paresthesia (7%) 

Dizziness (4%) 

Fatigue (1 – 3%) 

Feeling hot (2%) 

Infusion site pain (2%) 

Hyperhidrosis (3%) 

Pruritis (3%) 

Nausea (5 – 6%) 

Oral paresthesia (2%) 

Vomiting (1%) 

Diarrhea (1%) 

Cough (4%) 

Nasal discomfort (2%) 

Dyspnea (2%)  

<1% 

Abdominal distress 

Abdominal pain 

Agitation 

Altered sense of smell 

Angina pectoris 

Ansomia 

Anxiety 

Arterial thrombosis 

Arthralgia 

Asphyxia 

Blurred vision 

Increased lacrimation 

Hematuria 

Limb pain 

Malaise 

Orthopnea 

Nodal arrhythmia 

Rhinitis 

Upper respiratory tract infection 

Urinary tract infections 

Ventricular fibrillation 

Skin rash 

Sinus bradycardia 

Black Box Warning

Black Box Warning: 

For IV infusion only. vernakalant should not be used as an IV bolus or push. Vials are for single use only and must be diluted prior to use. Monitor for serious hypotension immediately after IV infusion.

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Severe aortic stenosis 
• Severe bradycardia 
• Sinus node dysfunction 
• 2nd or 3rd degree heart block 

Cautions 

• Hypotension 
• CHF 
• Valvular heart disease 
• Atrial flutter 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the administration of the drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the excretion of drug in breast milk. 

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

Indicated in patients with recent onset of Atrial Fibrillation on which upon IV administration of vernakalant rapid conversion of AF to sinus rhythm is seen in adults for non-surgery patients where AF lasts for 7 days and for post-cardiac surgery patients where AF is less than 3 days. 

Pharmacodynamics: 

vernakalant is an antiarrhythmic Class III drug which is also a multi-ion channel blocker which inhibits several potassium and sodium channel and shows its action in the atria to prolong atrial refractoriness and slow impulse production which combinedly though to inhibit re-entry and are potentiated in the atria during AF. Indicated in patients with recent onset of Atrial Fibrillation on which upon IV administration of vernakalant rapid conversion of AF to sinus rhythm is seen in adults for non-surgery patients where AF lasts for 7 days and for post-cardiac surgery patients where AF is less than 3 days. 

Pharmacokinetics: 

Absorption 

vernakalant shows rapid onset of action following IV administration. Following a single 10-minute infusion of 3mg/kg vernakalant IV average peak plasma concentration were 3.9 mcg/ml and 4.3 mcg/ml is shown following second 10 minutes infusion of vernakalant 2mg/kg where interval between first and second dose is 15 minutes. 

Distribution 

Protein-bound is 37 – 47% 

vernakalant is rapidly and extensively distributed in the body with Vd of approx. 2L/kg where Cmax and AUC were dose proportional between 0.5 mg/kg and 5 mg/kg. total body clearance is 0.41 L/hr/kg. 

Metabolism 

Metabolism takes place in liver via CYP2D6 O-demethylation in CYP2D6 extensive metabolizers to the active metabolite RSD1385 (Finnin 2010) and gluuronidation in CYP2D6 poor metabolizers. 

Elimination and Excretion 

Elimination half-life of vernakalant is 3 hours in CYP2D6 extensive metabolisers and 5.5 hours in poor metabolisers.

Adminstartion

Administration: 

vernakalant is only for Intravenous use only. It should not be administered as an IV push or bolus. These are single use vials only and must be diluted prior to use. Infusions must be via infusion pump or via syringe pump over 10 minutes. If required when conversion sinus rhythm doesn’t occur It should be followed by 2nd infusion where the interval between infusions should be 15 minutes. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: vernakalant 

Pronounced: ver-NAK-uh-lant 

Why do we use vernakalant? 

Indicated in patients with recent onset of Atrial Fibrillation on which upon IV administration of vernakalant rapid conversion of AF to sinus rhythm is seen in adults for non-surgery patients where AF lasts for 7 days and for post-cardiac surgery patients where AF is less than 3 days.