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Isradipine | CAS No: 75695-93-1 | GMP-certified suppliers
A medication that manages mild to moderate essential hypertension by lowering blood pressure, suitable for monotherapy or combination with thiazide diuretics.
Therapeutic categories
Primary indications
- For the management of mild to moderate essential hypertension
- It may be used alone or concurrently with thiazide-type diuretics
Product Snapshot
- Isradipine is available as oral small molecule formulations including tablets and capsules with extended release and film-coated options
- It is primarily indicated for the management of mild to moderate essential hypertension, either as monotherapy or in combination with thiazide diuretics
- The product is approved in the US market and also has investigational status
Clinical Overview
Pharmacodynamically, isradipine exerts its antihypertensive effect by selectively inhibiting the influx of calcium ions through L-type voltage-gated calcium channels located in arterial smooth muscle cells. This inhibition reduces intracellular calcium availability, preventing calmodulin activation and subsequent myosin light chain kinase (MLCK) phosphorylation required for smooth muscle contraction. The decreased contractility results in vasodilation and a reduction in systemic vascular resistance, thereby lowering blood pressure. Notably, isradipine shows greater selectivity for arterial over cardiac smooth muscle due to alternative splicing variants of the alpha-1 subunit of L-type channels and a higher proportion of inactive channels in arterial smooth muscle. Consequently, at therapeutic concentrations, cardiac conduction and contractility are minimally affected.
Mechanistically, isradipine binds with high affinity to the inactive conformation of L-type calcium channels, stabilizing this non-conductive state. Since arterial smooth muscle cells exhibit prolonged depolarization phases compared to cardiac myocytes, the prevalence of inactive channels enhances isradipine’s vascular selectivity.
Key ADME characteristics include metabolism predominantly by cytochrome P450 enzymes, particularly CYP3A4, establishing the potential for drug-drug interactions with CYP3A substrates and inhibitors. Isradipine is mainly eliminated renally, indicating consideration in patients with impaired renal function.
Safety and toxicity considerations involve its classification as a potential QTc-prolonging agent and its association with bradycardia in some cases. Monitoring for hyperkalemia is advised due to its categorization among agents causing elevated potassium levels.
Isradipine is marketed under various brand names globally and is recognized within cardiovascular therapeutic categories. For API procurement, sourcing should prioritize compliance with pharmacopeial standards, stringent impurity profiles, and stability under recommended conditions. Due diligence in vendor qualification is essential to ensure batch-to-batch consistency and regulatory conformity.
Identification & chemistry
| Generic name | Isradipine |
|---|---|
| Molecule type | Small molecule |
| CAS | 75695-93-1 |
| UNII | YO1UK1S598 |
| DrugBank ID | DB00270 |
Pharmacology
| Summary | Isradipine is a dihydropyridine calcium channel blocker that selectively inhibits L-type voltage-dependent calcium channels in arterial smooth muscle, reducing calcium influx and subsequent muscle contraction. This action decreases vascular smooth muscle contractility and induces vasodilation, leading to lowered blood pressure. Its arterial selectivity stems from differential channel subunit expression and prolonged depolarization states in smooth muscle compared to cardiac tissue. |
|---|---|
| Mechanism of action | Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. There are at least five different types of calcium channels in <i>Homo sapiens</i>: L-, N-, P/Q-, R- and T-type. CCBs target L-type calcium channels, the major channel in muscle cells that mediates contraction. Similar to other DHP CCBs, isradipine binds directly to inactive calcium channels stabilizing their inactive conformation. Since arterial smooth muscle depolarizations are longer in duration than cardiac muscle depolarizations, inactive channels are more prevalent in smooth muscle cells. Alternative splicing of the alpha-1 subunit of the channel gives isradipine additional arterial selectivity. At therapeutic sub-toxic concentrations, isradipine has little effect on cardiac myocytes and conduction cells. |
| Pharmacodynamics | Isradipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through L-type calcium channels. Calcium ions entering the cell through these channels bind to calmodulin. Calcium-bound calmodulin then binds to and activates myosin light chain kinase (MLCK). Activated MLCK catalyzes the phosphorylation of the regulatory light chain subunit of myosin, a key step in muscle contraction. Signal amplification is achieved by calcium-induced calcium release from the sarcoplasmic reticulum through ryanodine receptors. Inhibition of the initial influx of calcium decreases the contractile activity of arterial smooth muscle cells and results in vasodilation. The vasodilatory effects of isradipine result in an overall decrease in blood pressure. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Voltage-dependent L-type calcium channel subunit alpha-1C | Humans | inhibitor |
| Voltage-dependent calcium channel subunit alpha-2/delta-1 | Humans | inhibitor |
| Voltage-dependent L-type calcium channel subunit beta-2 | Humans | inhibitor |
ADME / PK
| Absorption | Isradipine is 90%-95% absorbed and is subject to extensive first-pass metabolism, resulting in a bioavailability of about 15%-24%. |
|---|---|
| Half-life | 8 hours |
| Protein binding | 95% |
| Metabolism | Hepatic. Completely metabolized prior to excretion and no unchanged drug is detected in the urine. |
| Route of elimination | Approximately 60% to 65% of an administered dose is excreted in the urine and 25% to 30% in the feces. |
Formulation & handling
- Isradipine is a small molecule oral API commonly formulated as immediate or extended-release tablets and capsules.
- It exhibits moderate lipophilicity (LogP ~2) and low water solubility, requiring consideration in formulation design to ensure adequate bioavailability.
- No specific food interaction restrictions are necessary; it can be administered with or without food.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is currently available in the US market following patent expiry, leading to increased generic competition and market maturity. Ongoing availability is supported by multiple manufacturers. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Isradipine's manufacturing landscape includes multiple players, with original branded products mainly produced by GlaxoSmithKline and associated entities. The drug is marketed primarily in the US, with the brand name DynaCirc appearing consistently across samples. Patent expiry has allowed for existing generic competition, as evidenced by several manufacturers and packagers involved in supply. |
|---|
Safety
| Toxicity | Symptoms of overdose include lethargy, sinus tachycardia, and transient hypotension. Significant lethality was observed in mice given oral doses of over 200 mg/kg and rabbits given about 50 mg/kg of isradipine. Rats tolerated doses of over 2000 mg/kg without effects on survival. |
|---|
- Overdose may result in lethargy, sinus tachycardia, and transient hypotension
- Acute oral lethality observed in mice at doses ›200 mg/kg and rabbits at ~50 mg/kg
- Rats tolerate ›2000 mg/kg without mortality
Isradipine is a type of Calcium Channel Blockers
Calcium channel blockers (CCBs) are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the treatment of various cardiovascular conditions. CCBs work by blocking the influx of calcium ions into smooth muscle cells and cardiac muscle cells, leading to vasodilation and reduced cardiac contractility.
CCBs are commonly prescribed to manage hypertension (high blood pressure), angina (chest pain), and certain arrhythmias (irregular heart rhythms). They are also effective in treating Raynaud's disease and migraine headaches. These medications exert their therapeutic effects by selectively inhibiting L-type calcium channels in the heart and blood vessels.
By blocking calcium channels, CCBs help relax and widen blood vessels, reducing peripheral resistance and improving blood flow. This mechanism of action lowers blood pressure, relieves angina symptoms, and helps prevent certain types of abnormal heart rhythms.
Some well-known CCBs include amlodipine, nifedipine, diltiazem, and verapamil. These medications are available in various formulations, including immediate-release and extended-release tablets, as well as injectable solutions.
It's important to note that CCBs may cause certain side effects, such as dizziness, headache, flushing, and ankle swelling. They may also interact with other medications, so it's crucial to consult a healthcare professional before starting or changing any CCB therapy.
In summary, Calcium channel blockers are a subcategory of cardiovascular medications that inhibit calcium channels, resulting in vasodilation, decreased cardiac contractility, and overall therapeutic effects in conditions such as hypertension, angina, and arrhythmias. Proper medical supervision and individualized treatment plans are essential for optimizing the use of CCBs.
Isradipine (Calcium Channel Blockers), 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.
Isradipine API manufacturers & distributors
Compare qualified Isradipine API suppliers worldwide. We currently have 5 companies offering Isradipine 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 |
|---|---|---|---|---|---|
| Chemo Iberica | Producer | Spain | Spain | CoA, USDMF | 12 products |
| Chemoswed | Producer | Sweden | Sweden | CEP, CoA, FDA, GMP | 3 products |
| Magle Chemoswed | Producer | Sweden | Sweden | CoA, GMP | 1 products |
| Quimica Sintetica | Producer | Spain | Spain | CoA, GMP | 51 products |
| Sun Pharma | Producer | India | India | CoA, GMP, WC | 219 products |
When sending a request, specify which Isradipine 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.).
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