Darenthin

Darenthin Uses, Dosage, Side Effects, Food Interaction and all others data.

Darenthin blocks the release of noradrenaline from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. The primary mode of action for bretylium is thought to be inhibition of voltage-gated K(+) channels. Recent evidence has shown that bretylium may also inhibit the Na,K-ATPase by binding to the extracellular K-site.

Darenthin is a bromobenzyl quaternary ammonium compound which selectively accumulates in sympathetic ganglia and their postganglionic adrenergic neurons where it inhibits norepinephrine release by depressing adrenergic nerve terminal excitability. Darenthin also suppresses ventricular fibrillation and ventricular arrhythmias.

Trade Name Darenthin
Availability Discontinued
Generic Bretylium
Bretylium Other Names Bretylium
Related Drugs propranolol, atenolol, amiodarone, lidocaine, flecainide, Tenormin, Pacerone, vasopressin, Cordarone, Pitressin
Type
Formula C11H17BrN
Weight Average: 243.163
Monoisotopic: 242.054437196
Groups Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Darenthin
Darenthin

Uses

Darenthin is a norepinephrine release inhibitor used for the prophylaxis and therapy of ventricular fibrillation, as well as the treatment of life-threatening ventricular arrhythmias.

For use in the prophylaxis and therapy of ventricular fibrillation. Also used in the treatment of life-threatening ventricular arrhythmias, such as ventricular tachycardia, that have failed to respond to adequate doses of a first-line antiarrhythmic agent, such as lidocaine.

Darenthin is also used to associated treatment for these conditions: Ventricular Fibrillation, Ventricular Tachycardia (VT)

How Darenthin works

Darenthin inhibits norepinephrine release by depressing adrenergic nerve terminal excitability. The mechanisms of the antifibrillatory and antiarrhythmic actions of bretylium are not established. In efforts to define these mechanisms, the following electrophysiologic actions of bretylium have been demonstrated in animal experiments: increase in ventricular fibrillation threshold, increase in action potential duration and effective refractory period without changes in heart rate, little effect on the rate of rise or amplitude of the cardiac action potential (Phase 0) or in resting membrane potential (Phase 4) in normal myocardium, decrease in the disparity in action potential duration between normal and infarcted regions, and increase in impulse formation and spontaneous firing rate of pacemaker tissue as well as increase ventricular conduction velocity.

Toxicity

Oral, mouse: LD50 = 400 mg/kg. In the presence of life-threatening arrhythmias, underdosing with bretylium probably presents a greater risk to the patient than potential overdosage. However, one case of accidental overdose has been reported in which a rapidly injected intravenous bolus of 30 mg/kg was given instead of an intended 10 mg/kg dose during an episode of ventricular tachycardia. Marked hypertension resulted, followed by protracted refractory hypotension. The patient expired 18 hours later in asystole, complicated by renal failure and aspiration pneumonitis. Darenthin serum levels were 8000 ng/mL.

Food Interaction

No interactions found.

Half Life

The terminal half-life in four normal volunteers averaged 7.8±0.6 hours (range 6.9-8.1). During hemodialysis, this patient's arterial and venous bretylium concentrations declined rapidly, resulting in a half-life of 13 hours.

Innovators Monograph

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https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3172
http://www.hmdb.ca/metabolites/HMDB0015289
http://www.genome.jp/dbget-bin/www_bget?drug:D00645
http://www.genome.jp/dbget-bin/www_bget?cpd:C06855
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2431
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505320
https://www.chemspider.com/Chemical-Structure.2337.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50239966
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=19685
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=3172
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1199080
https://zinc.docking.org/substances/ZINC000000001041
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000939
http://www.pharmgkb.org/drug/PA448662
http://www.rxlist.com/cgi/generic3/bretosy.htm
https://en.wikipedia.org/wiki/Bretylium
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