- May 9, 2022
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Brand Name :
Ajimalin
Synonyms :
ajmaline, ajmalin
Class :
Antiarrhythmic agent Alkaloids
Dosage forms and strengths
Concentrate, solution, injection
(5 mg/ml)
Not indicated
Refer adult dosing
when both drugs are combined, there may be increase in the bradycardic effect of ceritinib
when both drugs are combined, there may be increase in the bradycardic effect of ceritinib cerit
may increase the QTc prolonging effect of QT-prolonging Class III Antiarrhythmics
may increase the QTc-prolonging effect of each other when combined
may enhance the arrhythmogenic activities of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
may enhance the serum concentration
may enhance the serum concentration
may enhance the serum concentration
may enhance the serum concentration
may enhance the serum concentration
may increase the adverse effect of sulfonamides
may increase the adverse effect of sulfonamides
choline magnesium trisalicylate
may have an increasingly adverse effect when combined with ajmaline
ajmaline: they may increase the toxic effect of sulfonamides
ajmaline: they may increase the toxic effect of sulfonamides
relugolix/estradiol/norethindrone
androgens increase the toxic or adverse effect of ajmaline
relugolix/estradiol/norethindrone
androgens increase the toxic or adverse effect of ajmaline
androgens increase the toxic or adverse effect of ajmaline
androgens increase the toxic or adverse effect of ajmaline
androgens increase the toxic or adverse effect of ajmaline
it may enhance the risk of QTc prolongation when combined with amifampridine
The combination of estrogen derivatives with ajmaline could potentially amplify its harmful and toxic effects
The combination of estrogen derivatives with ajmaline could potentially amplify its harmful and toxic effects
bazedoxifene/conjugated estrogens
The combination of estrogen derivatives with ajmaline could potentially amplify its harmful and toxic effects
synthetic conjugated estrogens, a
The combination of estrogen derivatives with ajmaline could potentially amplify its harmful and toxic effects
synthetic conjugated estrogens, b
The combination of estrogen derivatives with ajmaline could potentially amplify its harmful and toxic effects
estrogen derivatives could potentially increase the toxicity of ajmaline
estrogen derivatives could potentially increase the toxicity of ajmaline
androgens increase the toxic or adverse effect of ajmaline
may increase the serum concentration of CYP2D6 substrates
may decrease the serum concentration of tamoxifen by increasing CYP2D6 substrates
salicylates increase the adverse effect of ajmaline
sulfonamides increase the toxic or adverse effects of ajmaline
QT-prolonging Miscellaneous Agents may enhance the QTc-prolonging effect of anti-arrhythmics
QT-prolonging Miscellaneous Agents may enhance the QTc-prolonging effect of anti-arrhythmics
QT-prolonging Miscellaneous Agents may enhance the QTc-prolonging effect of anti-arrhythmics
QT-prolonging Miscellaneous Agents may enhance the QTc-prolonging effect of anti-arrhythmics
QT-prolonging Miscellaneous Agents may enhance the QTc-prolonging effect of anti-arrhythmics
may enhance the adverse/toxic effect of lacosamide
hydrocodone/chlorpheniramine/pseudoephedrine
may increase the CNS depressant activity of CNS depressants
may enhance the antiarrhythmic effect
may increase the risk or severity of QTc prolongation when combined
may increase the toxic effect of sulfonamides
may increase the adverse effect of Antiarrhythmic Agents
may have an increasingly adverse effect when combined with antiarrhythmic agents (class Ib)
may increase the QTc-prolonging effect of QT-Prolonging Inhalational Anesthetics
The arrhythmogenic effects of ajmaline might be intensified by acebutolol
ajmaline enhances the risk of QTc prolongation when combined with amisulpride
ajmaline enhances the risk of QTc prolongation when combined with amifampridine
ajmaline enhances the risk of QTc prolongation when combined with amantadine
ajmaline enhances the risk of QTc prolongation when combined with alimemazine
ajmaline enhances the risk of QTc prolongation when combined with alfuzosin
ajmaline enhances the risk of QTc prolongation when combined with acrivastine
may enhance the QTc-prolonging effect of each other when combined
when ajmaline is used together with artemether, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with asenapine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with atomoxetine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with azithromycin, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with bilastine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with brompheniramine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with carbinoxamine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with ceritinib, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with cetirizine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with chloroquine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with chlorpheniramine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with chlorpromazine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with ciprofloxacin, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with cisapride, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with citalopram, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with clarithromycin, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with clozapine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with cyclizine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with desipramine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with dexbrompheniramine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with disulfiram, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with domperidone, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with doxepin, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with doxylamine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with droperidol, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with entrectinib, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with famotidine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with fluconazole, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with fluorouracil, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with fluoxetine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with haloperidol, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with imipramine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with isoflurane, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with itraconazole, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with ketoconazole, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with levocetirizine, the risk or seriousness of QTc prolongation is enhanced
when ajmaline is used together with lopinavir, the risk or seriousness of QTc prolongation is enhanced
pilsicainide hydrochloride increases the risk of arrhythmia when co-administered with other anti-arrhythmic agents
Actions and Spectrum:
Action:
Antiarrhythmic Action: ajmaline is primarily known for its antiarrhythmic effects. It belongs to Class Ia antiarrhythmics based on the Vaughan Williams classification system. Class Ia antiarrhythmics act by blocking sodium channels in cardiac cells, which affects the conduction of electrical impulses and helps stabilize abnormal heart rhythms.
Sodium Channel Blockade: ajmaline selectively blocks the fast sodium channels in cardiac cells, The rapid influx of sodium ions during the depolarization phase of the cardiac action potential is attributed to its responsible mechanism. By doing so, ajmaline prolongs the refractory period of cardiac cells and reduces the conduction velocity in some heart regions.
Spectrum: ajmaline is primarily utilized to diagnose and assess Brugada syndrome, an inherited condition impacting the heart’s electrical behavior and potentially causing severe ventricular arrhythmias that can be life-threatening. The administration of ajmaline during an electrocardiogram (ECG) can help unmask specific characteristic patterns in the ECG that indicate Brugada syndrome.
Frequency not defined
Agranulocytosis
Hepatotoxicity
Convulsions
eye twitching
cardiac arrhythmias
Heart block
Black Box Warning:
None
Contraindication/Caution:
Known hypersensitivity: Individuals with a known hypersensitivity or allergic reaction to ajmaline or any other ingredients in the medication should not take it.
Severe heart block: ajmaline can worsen heart block, which is a condition where the electrical impulses responsible for regulating the heartbeat experience delays or interruptions. It should not be used in individuals with severe heart block.
Sick sinus syndrome: This medical condition involves malfunctioning the heart’s natural pacemaker, also known as the sinus node. ajmaline can further suppress the heart’s electrical activity, making it unsuitable for people with sick sinus syndrome.
Bradycardia: ajmaline can cause a slowing of the heart rate (bradycardia). It is not recommended for individuals with pre-existing bradycardia.
Atrioventricular (AV) block: ajmaline may worsen AV block, which is a condition where the electrical signals between the atria and ventricles are delayed or blocked. It should be used with caution or avoided in individuals with AV block.
Cardiogenic shock: ajmaline is not suitable for individuals with cardiogenic shock.
Ventricular tachycardia: Although ajmaline is used to diagnose certain rhythm disorders, it should not be used in individuals with known ventricular tachycardia or other life-threatening ventricular arrhythmias.
Long QT syndrome: ajmaline can prolong the QT interval on an electrocardiogram (ECG), and it should be used with caution or avoided in individuals with long QT syndrome.
Pregnancy warnings:
Pregnancy category: N/A
Lactation: Excreted into human milk is unknown
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.
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: There is no data available for the drug under this category
Pharmacology:
ajmaline belongs to the category of class 1A antiarrhythmic agents, exerting its effects by modulating sodium channels. This medication has been shown to effectively ameliorate irregular heart rhythms.
Pharmacodynamics:
ajmaline works primarily by blocking sodium channels in cardiac cells, specifically the fast inward sodium current (INa). This reduces the depolarization and conduction velocity rate in cardiac tissue, particularly in the His-Purkinje system and the right ventricular outflow tract.
Pharmacokinetics:
Absorption
ajmaline is typically administered intravenously or orally. When given orally, its absorption from the gastrointestinal tract is relatively slow. The absorption rate may vary among individuals and can be influenced by factors such as the formulation of the drug and the presence of food in the stomach.
Distribution
Once absorbed into the bloodstream, ajmaline is distributed throughout the body. It is likely to bind to plasma proteins, such as albumin, which affects its distribution in the body.
Metabolism
ajmaline undergoes extensive hepatic (liver) metabolism. The major metabolic pathway involves the liver enzymes, resulting in the formation of various metabolites. One of the primary metabolites is known as “deacetylajmaline.”
Excretion and Elimination
After metabolism, the metabolites of ajmaline are excreted mainly through the kidneys in the form of urine. The elimination half-life of ajmaline can be around 13 to 19 hours, depending on the individual and other factors.
Administration:
Medical Supervision: ajmaline administration should be performed by qualified healthcare professionals, preferably in a hospital setting or under close medical supervision, as it may lead to significant changes in heart rhythm and blood pressure.
Dosage: The dosage of ajmaline will depend on the specific medical condition being evaluated and the patient’s individual characteristics. The physician will determine the appropriate dose based on the patient’s weight, age, and medical history.
Slow Infusion: ajmaline is typically administered as a slow intravenous infusion to reduce the risk of adverse reactions. The infusion rate should be adjusted based on the patient’s response and tolerability.
Patient information leaflet
Generic Name: ajmaline
Why do we use ajmaline?
Antiarrhythmic agent: ajmaline is primarily used as an antiarrhythmic medication. It is administered to diagnose and treat abnormal heart rhythms, such as ventricular arrhythmias, by altering the heart’s electrical activity. It is significant in diagnosing Brugada syndrome, a rare genetic condition predisposing individuals to life-threatening arrhythmias.
Diagnostic tool: ajmaline is used in combination with other medications during an electrophysiological test called the ajmaline test. This test helps identify the presence of Brugada syndrome and other cardiac arrhythmias by inducing characteristic changes in the ECG (electrocardiogram) patterns.