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Hydralazine | CAS No: 86-54-4 | GMP-certified suppliers
A medication that manages essential hypertension and supports adjunct treatment of heart failure through arteriolar vasodilation and reduction of peripheral vascular resistance.
Therapeutic categories
Primary indications
- Hydralazine is indicated alone or adjunct to standard therapy to treat essential hypertension
- A combination product with isosorbide dinitrate is indicated as an adjunct therapy in the treatment of heart failure
Product Snapshot
- Hydralazine is available as oral tablets and parenteral injectable formulations
- It is primarily used for the treatment of essential hypertension and as adjunct therapy in heart failure in combination with isosorbide dinitrate
- Hydralazine is approved for use in key regulatory markets including the United States and Canada
Clinical Overview
Clinically, hydralazine is approved for use as monotherapy or adjunctive therapy in the management of essential hypertension. Additionally, it is utilized in combination with isosorbide dinitrate as an adjunct treatment for heart failure. Its use as a first-line agent has diminished with the availability of newer antihypertensive drugs.
Pharmacodynamically, hydralazine induces arterial vasodilation predominantly by relaxing arteriolar smooth muscle. Its mechanism of action involves interference with calcium transport mechanisms in vascular smooth muscle cells, although the precise pathways remain incompletely elucidated. Proposed actions include inhibition of calcium influx, prevention of calcium release from intracellular stores, and direct effects on actin-myosin interactions. The resultant decrease in peripheral vascular resistance leads to compensatory increases in heart rate, stroke volume, and cardiac output. Additionally, hydralazine competitively inhibits protocollagen prolyl hydroxylase activity by chelating free iron, preventing HIF-1α hydroxylation and degradation, thereby promoting endothelial proliferation and angiogenesis.
Hydralazine exhibits a short duration of action, approximately 2 to 6 hours, and displays a wide therapeutic window, with doses up to 300 mg generally tolerated. It is metabolized hepatically and primarily excreted via the kidneys. Notable safety considerations include the risk of drug-induced systemic lupus erythematosus-like syndrome, which requires monitoring during therapy.
From a regulatory perspective, hydralazine hydrochloride received FDA approval on January 15, 1953, and remains listed among cardiovascular agents with vasodilatory activity.
For API sourcing, attention should be paid to the purity profile, regulatory compliance with pharmacopeial monographs, and stability under recommended storage conditions, given hydralazine’s known susceptibility to oxidative degradation. Ensuring consistent quality and batch-to-batch uniformity is critical to support formulation development and clinical use.
Identification & chemistry
| Generic name | Hydralazine |
|---|---|
| Molecule type | Small molecule |
| CAS | 86-54-4 |
| UNII | 26NAK24LS8 |
| DrugBank ID | DB01275 |
Pharmacology
| Summary | Hydralazine acts primarily as an arteriolar vasodilator by interfering with calcium transport in vascular smooth muscle, resulting in decreased vascular resistance and lowered blood pressure. It also inhibits prolyl hydroxylase activity, stabilizing hypoxia-inducible factor-1α (HIF-1α) and promoting endothelial cell proliferation and angiogenesis. These combined effects underlie its use in managing hypertension and as adjunct therapy in heart failure. |
|---|---|
| Mechanism of action | Hydralazine may interfere with calcium transport in vascular smooth muscle by an unknown mechanism to relax arteriolar smooth muscle and lower blood pressure. The interference with calcium transport may be by preventing influx of calcium into cells, preventing calcium release from intracellular compartments, directly acting on actin and myosin, or a combination of these actions. This decrease in vascular resistance leads to increased heart rate, stroke volume, and cardiac output. Hydralazine also competes with protocollagen prolyl hydroxylase (CPH) for free iron. This competition inhibits CPH mediated hydroxylation of HIF-1α, preventing the degradation of HIF-1α. Induction of HIF-1α and VEGF promote proliferation of endothelial cells and angiogenesis. |
| Pharmacodynamics | Hydralazine interferes with calcium transport to relax arteriolar smooth muscle and lower blood pressure. Hydralazine has a short duration of action of 2-6h. This drug has a wide therapeutic window, as patients can tolerate doses of up to 300mg. Patients should be cautioned regarding the risk of developing systemic lupus erythematosus syndrome. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Membrane primary amine oxidase | Humans | inhibitor |
| Hypoxia-inducible factor 1-alpha | Humans | inducer |
| Prolyl 4-hydroxylase subunit alpha-1 | Humans | inhibitor |
ADME / PK
| Absorption | Taking oral hydralazine with food improves the bioavailability of the drug. An intravenous dose of 0.3mg/kg leads to an AUC of 17.5-29.4µM\*min and a 1mg/kg oral dose leads to an AUC of 4.0-30.4µM\*min. The C<sub>max</sub> of oral hydralazine is 0.12-1.31µM depending on the acetylator status of patients. |
|---|---|
| Half-life | Hydralazine has a half life of 2.2-7.8h in rapid acetylators and 2.0-5.8h in slow acetylators. The half life in heart failure patients is 57-241 minutes with an average of 105 minutes and in hypertensive patients is 200 minutes for rapid acetylators and 297 minutes for slow acetylators. Hydralazine is subject to polymorphic acetylation; slow acetylators generally have higher plasma levels of hydralazine and require lower doses to maintain control of pressure. However, other factors, such as acetylation being a minor metabolic pathway for hydralazine, will contribute to differences in elimination rates. |
| Protein binding | Hydralazine is 87% protein bound in serum likely to human serum albumin. |
| Metabolism | Acetylation is a minor metabolic pathway for hydralazine; the major pathway is hydroxylation followed by glucuronidation. There are 5 identified metabolic pathways for hydralazine. Hydralazine can be metabolized to phthalazine or α-ketoglutarate hydrazone. These metabolites can be further converted to phthalazinone or hydralazine can be metabolized directly to phthalazinone. Hydralazine can undergo a reversible converstion to the active hydralazine acetone hydrazone. Hydralazine is spontaneously converted to the active pyruvic acid hydrazone or the pyruvic acid hydrazone tricyclic dehydration product, and these metabolites can convert back and forth between these 2 forms. Hydralazine can be converted to hydrazinophthalazinone, which is further converted to the active acetylhydrazinophthalazinone. The final metabolic process hydralazine can undergo is the conversion to an unnamed hydralazine metabolite, which is further metabolized to 3-methyl-s-triazolophthalazine (MTP). MTP can be metabolized to 9-hydroxy-methyltriazolophthalazine or 3-hydroxy-methyltriazolophthalazine; the latter is converted to triazolophthalazine. |
| Route of elimination | <10% of hydralazine is recovered in the feces; 65-90% is recovered in the urine. |
| Volume of distribution | The volume of distribution is 1.34±0.79L/kg in congestive heart failure patients and 1.98±0.22L/kg in hypertensive patients. |
| Clearance | The majority of hydralazine clearance is extrahepatic- 55% for rapid acetylators and 70% for slow acetylators. The average clearance in congestive heart failure patients is 1.77±0.48L/kg/h, while hypertensive patients have an average clearance of 42.7±8.9mL/min/kg. |
Formulation & handling
- Hydralazine is a small molecule available in both oral (tablet, capsule) and parenteral (intravenous, intramuscular) dosage forms requiring versatile formulation approaches.
- Formulations should consider hydralazine’s moderate water solubility (2.64 g/L) and low LogP (0.75) to optimize bioavailability and stability in aqueous solutions.
- No significant food sensitivity observed; however, food intake increases systemic exposure, which should be noted in clinical settings but does not impact formulation design.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's key patents in the United States expired in September 2020, marking its transition into a mature market phase. It is currently marketed in both the United States and Canada. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Hydralazine is manufactured and supplied by numerous companies, including both originator and generic manufacturers, indicating a diverse supplier landscape. Branded versions such as Apresoline are present primarily in the US and Canadian markets. The listed patents have expiration dates in 2020, suggesting that generic competition is currently established. |
|---|
Safety
| Toxicity | The oral LD<sub>50</sub> in rats is 173-187mg/kg and the highest known dose an adult human has survived is 10g orally. Patients experiencing an overdose may present with hypotension, tachycardia, headache, flushing, myocardial ischemia, myocardial infarction, cardiac arrhythmia, and shock. Overdose can be treated through emptying the gastric contents and administering activated charcoal, though these treatments may cause further arrhythmias and shock. Supportive and symptomatic treatment should be administered. |
|---|
- Handle with care as the oral LD50 in rats is 173-187 mg/kg, indicating moderate acute toxicity
- Exposure to high doses may induce cardiovascular and neurological adverse effects including hypotension and arrhythmias
- Use appropriate protective measures to minimize exposure
Hydralazine is a type of Vasodilators
Vasodilators are a crucial subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) that play a significant role in the management of various cardiovascular conditions. These medications work by widening the blood vessels, promoting increased blood flow and reducing peripheral resistance.
Vasodilators are commonly prescribed to treat hypertension (high blood pressure), angina (chest pain), and heart failure. They are designed to relax and dilate the smooth muscle cells in the walls of blood vessels, leading to improved circulation and reduced strain on the heart.
One widely used class of vasodilators is calcium channel blockers, which prevent calcium from entering the muscle cells of blood vessels. This action inhibits muscle contraction, resulting in widened arteries and enhanced blood flow. Another class is nitric oxide (NO) donors, which release NO, a potent vasodilator, to promote relaxation of vascular smooth muscles.
The therapeutic benefits of vasodilators extend beyond cardiovascular disorders. Some vasodilators, such as minoxidil, have been repurposed for treating male pattern baldness. These medications stimulate hair growth by dilating blood vessels around hair follicles, enhancing nutrient and oxygen delivery.
As with any pharmaceutical API, vasodilators must meet strict quality standards and regulatory guidelines to ensure safety and efficacy. Manufacturers employ sophisticated production processes and stringent quality control measures to guarantee the purity, potency, and stability of these APIs.
In conclusion, vasodilators are a vital subcategory of pharmaceutical APIs used to manage cardiovascular conditions. By expanding blood vessels and enhancing blood flow, vasodilators contribute to improved patient outcomes and play a critical role in the treatment of hypertension, angina, heart failure, and even hair loss.
Hydralazine (Vasodilators), classified under Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Hydralazine API manufacturers & distributors
Compare qualified Hydralazine API suppliers worldwide. We currently have 8 companies offering Hydralazine API, with manufacturing taking place in 5 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 |
|---|---|---|---|---|---|
| Euticals | Producer | Italy | Unknown | CoA, USDMF | 48 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Hetero Labs | Producer | India | India | CoA, GMP, USDMF, WC | 90 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| NAVINTA | Producer | United States | Unknown | CoA, USDMF | 15 products |
| Sumitomo Chemical | Producer | Japan | Japan | CoA, JDMF | 28 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 140 products |
| Wanbury | Producer | India | India | CoA, USDMF | 15 products |
When sending a request, specify which Hydralazine 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 Hydralazine 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.
