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Procainamide | CAS No: 51-06-9 | GMP-certified suppliers
A medication that treats life-threatening ventricular arrhythmias by stabilizing cardiac rhythm and increasing ventricular excitability thresholds.
Therapeutic categories
Primary indications
- For the treatment of life-threatening ventricular arrhythmias
Product Snapshot
- Procainamide is available in multiple oral small molecule formulations including capsules and extended-release tablets, as well as injectable solutions for intravenous and intramuscular administration
- It is primarily indicated for the treatment of life-threatening ventricular arrhythmias
- The product is approved for use in key regulatory markets including the United States and Canada
Clinical Overview
Pharmacodynamically, procainamide functions as a Class Ia antiarrhythmic agent. It depresses ventricular excitability and raises the stimulation threshold during diastole without affecting the sinoatrial node. Its antiarrhythmic effect resembles that of procaine and quinidine. Mechanistically, procainamide acts as a sodium channel blocker, stabilizing neuronal membranes by inhibiting the ionic fluxes necessary for impulse initiation and conduction. This blocking of voltage-gated sodium channels underlies both its antiarrhythmic properties and local anesthetic activity.
In terms of absorption, distribution, metabolism, and excretion (ADME), procainamide is metabolized hepatically with involvement of cytochrome P-450 CYP2D6 isoenzymes and exhibits a narrow therapeutic index. It is primarily eliminated via renal excretion. The drug is recognized as a substrate and inhibitor of multiple transporters, including OCT1, OCT2, and MATE 1 and 2, contributing to its complex pharmacokinetics and potential for drug interactions. Procainamide is known to prolong the QT interval and carries a risk of cardiac toxicity, including proarrhythmic effects, particularly torsades de pointes. It also acts as a negative inotrope, which is clinically relevant in patients with compromised cardiac function.
Due to its narrow therapeutic index and propensity for serious adverse effects, careful dose titration and monitoring of plasma levels are essential during clinical use. Procainamide has established approval in various regions for antiarrhythmic therapy, with usage primarily confined to hospital or specialized settings.
From an API sourcing perspective, procainamide must meet stringent purity criteria and stability profiles due to its narrow safety margin and regulatory scrutiny. Manufacturers and sourcing managers should ensure compliance with pharmacopeial standards, control of impurities, and robust supply chain traceability to support consistent pharmaceutical quality and patient safety.
Identification & chemistry
| Generic name | Procainamide |
|---|---|
| Molecule type | Small molecule |
| CAS | 51-06-9 |
| UNII | L39WTC366D |
| DrugBank ID | DB01035 |
Pharmacology
| Summary | Procainamide functions as a sodium channel blocker that stabilizes neuronal and cardiac membranes by inhibiting ionic fluxes essential for impulse initiation and conduction. It primarily targets voltage-gated sodium channels to decrease ventricular excitability and increase stimulation thresholds, contributing to its antiarrhythmic effects. Procainamide is indicated for managing life-threatening ventricular arrhythmias, particularly during cardiac events such as myocardial infarction or surgery. |
|---|---|
| Mechanism of action | Procainamide is sodium channel blocker. It stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action. |
| Pharmacodynamics | Procainamide is an agent indicated for production of local or regional anesthesia and in the treatment of ventricular tachycardia occurring during cardiac manipulation, such as surgery or catheterization, or which may occur during acute myocardial infarction, digitalis toxicity, or other cardiac diseases. The mode of action of the antiarrhythmic effect of Procainamide appears to be similar to that of procaine and quinidine. Ventricular excitability is depressed and the stimulation threshold of the ventricle is increased during diastole. The sinoatrial node is, however, unaffected. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Potassium voltage-gated channel subfamily H member 2 | Humans | inhibitor |
| Sodium channel protein type 5 subunit alpha | Humans | inhibitor |
| DNA (cytosine-5)-methyltransferase 1 | Humans | other |
ADME / PK
| Absorption | 75 to 95% |
|---|---|
| Half-life | ~2.5-4.5 hours |
| Protein binding | 15 to 20% |
| Metabolism | Hepatic |
| Route of elimination | Trace amounts may be excreted in the urine as free and conjugated p-aminobenzoic acid, 30 to 60 percent as unchanged PA, and 6 to 52 percent as the NAPA derivative. |
| Volume of distribution | * 2 L/kg |
Formulation & handling
- Procainamide is a small molecule API available for oral and parenteral (intramuscular/intravenous) administration requiring formulation adjustments for each route. It exhibits moderate water solubility and a low logP, suggesting suitable aqueous formulations for injection and typical oral dosage forms like capsules and tablets. Food intake reduces gastrointestinal irritation, indicating formulation strategies to mitigate local irritation in oral dosage forms should be considered.
Regulatory status
| Lifecycle | The API's primary patent expired in the United States in August 2014, resulting in mature market conditions in both the US and Canada with established generic competition. Market activity is characterized by multiple available products and stable demand. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Procainamide is supplied by multiple packaging companies primarily serving the US and Canadian markets. Branded products are available in varying doses, indicating an established presence in these regions. The noted patent expiration in 2014 suggests that generic competition is currently present or likely established. |
|---|
Safety
| Toxicity | LD<sub>50</sub>=95 mg/kg (rat, IV); LD<sub>50</sub>=312 mg/kg (mouse, oral); LD<sub>50</sub>=103 mg/kg (mouse, IV); LD<sub>50</sub>=250 mg/kg (rabbit, IV) |
|---|
- Handle with appropriate personal protective equipment due to moderate acute toxicity via intravenous and oral routes
- Avoid inhalation, ingestion, and skin contact to minimize exposure risk
- Ensure proper containment and ventilation during manufacturing and processing to prevent accidental release
Procainamide is a type of Anti-arrhythmics
Anti-arrhythmics belong to the pharmaceutical API category designed to treat irregular heart rhythms, also known as arrhythmias. These medications work by targeting the electrical signals in the heart, helping to regulate the heart's rhythm and restore it to a normal, steady beat.
Anti-arrhythmics are crucial in managing various types of arrhythmias, such as atrial fibrillation, ventricular tachycardia, and supraventricular tachycardia. These conditions can pose serious risks, including an increased likelihood of stroke or heart failure. Hence, anti-arrhythmics play a vital role in improving patient outcomes and reducing these associated risks.
Pharmaceutical companies develop anti-arrhythmic APIs, which are the active ingredients used to formulate the final medications. These APIs undergo rigorous testing and quality control measures to ensure their safety, efficacy, and consistent performance. They are manufactured in accordance with Good Manufacturing Practices (GMP) guidelines to meet the highest quality standards.
Healthcare professionals prescribe anti-arrhythmics based on the specific arrhythmia type, severity, and individual patient factors. These APIs can be formulated into different dosage forms, including tablets, capsules, or intravenous solutions, depending on the desired route of administration and patient requirements.
It is important to note that anti-arrhythmics are prescription-only medications and should only be used under medical supervision. Patients using these medications must follow their healthcare provider's instructions and regularly monitor their heart rhythm to ensure optimal treatment effectiveness and minimize potential side effects.
In conclusion, anti-arrhythmics are a crucial category of pharmaceutical APIs used to treat various types of irregular heart rhythms. They are formulated into medications that help regulate the heart's electrical signals, reduce associated risks, and improve patient outcomes.
Procainamide API manufacturers & distributors
Compare qualified Procainamide API suppliers worldwide. We currently have 5 companies offering Procainamide API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Albemarle | Producer | United States | United States | CoA, USDMF | 17 products |
| Biophore India | Producer | India | India | CoA, USDMF | 46 products |
| Cheng Fong Chemical | Producer | Taiwan | Taiwan | CoA, USDMF | 6 products |
| Duchefa Farma B.V. | Distributor | Netherlands | Taiwan | CoA, GMP, ISO9001, MSDS | 170 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
When sending a request, specify which Procainamide API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Procainamide API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
