Filters
Custom request?
Type
Production region
Qualifications
Country of origin
Naphazoline API Manufacturers & Suppliers
3 verified results
All Naphazoline data. Full access. Full negotiation power
Commercial-scale Suppliers
Employees: 50+
All certificates
Employees: 25
All certificates
All certificates
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Naphazoline | CAS No: 835-31-4 | GMP-certified suppliers
A medication that provides symptomatic relief of nasal congestion and ocular redness through topical vasoconstriction in over-the-counter nasal and ophthalmic formulations.
Therapeutic categories
Primary indications
- Naphazoline is indicated for use as OTC eyedrops for ocular vasoconstriction or as a nasal preparation for nasal congestion
Product Snapshot
- Naphazoline is primarily available in solution and spray formulations for ophthalmic (eyedrops) and nasal administration
- It is used mainly for ocular vasoconstriction and nasal congestion relief
- The product is approved and marketed in the US and Canada
Clinical Overview
Clinically, naphazoline is indicated as a topical vasoconstrictor for symptomatic relief of nasal congestion and ocular redness. It achieves these effects through stimulation of alpha-adrenergic receptors located on the smooth muscle of arterioles in the nasal mucosa and conjunctiva. This alpha-adrenergic agonism causes vasoconstriction, reducing blood flow and thereby decreasing swelling and fluid leakage that contribute to congestion.
Pharmacodynamically, naphazoline acts as an alpha-1 and alpha-2 adrenergic receptor agonist, with additional mild beta-adrenergic activity. It induces the release of endogenous norepinephrine from sympathetic nerves, which further binds alpha receptors to sustain vasoconstriction. This release also initiates a negative feedback mechanism that suppresses endogenous norepinephrine production, which is implicated in rebound congestion or rhinitis medicamentosa after prolonged use and abrupt withdrawal.
Absorption of naphazoline following topical administration is minimal, limiting systemic exposure; however, systemic effects such as hypertension or tachycardia can occur if overused or absorbed in significant amounts. Safety considerations include avoiding extended or excessive use to prevent rebound congestion, and caution is advised in patients with cardiovascular diseases or increased intraocular pressure.
Naphazoline-containing products are widely available as generic and branded formulations, commonly combined with other agents in nasal sprays or eye drops for symptomatic relief.
For API procurement, sourcing naphazoline requires confirmation of compliance with relevant pharmacopeial standards and impurity profiles, given the sensitivity of alpha-adrenergic agents to synthesis impurities. Reliable suppliers should provide comprehensive documentation on synthesis, purity, and stability to ensure consistent quality suitable for pharmaceutical formulation.
Identification & chemistry
| Generic name | Naphazoline |
|---|---|
| Molecule type | Small molecule |
| CAS | 835-31-4 |
| UNII | H231GF11BV |
| DrugBank ID | DB06711 |
Pharmacology
| Summary | Naphazoline is a sympathomimetic agent that primarily targets alpha-1A and alpha-2A adrenergic receptors to induce vasoconstriction in nasal or ocular arterioles, reducing local congestion. It also promotes norepinephrine release, which mediates its vasoconstrictive effects and contributes to a feedback mechanism affecting norepinephrine synthesis. Additionally, mild beta adrenergic agonism by naphazoline can lead to rebound vasodilation following alpha receptor stimulation. |
|---|---|
| Mechanism of action | Naphazoline is a vasoconstrictor that functions by stimulating alpha adrenergic receptors in arterioles leading to decreased congestion at the site of administration. Naphazoline causes the release of norepinephrine in sympathetic nerves. Norepinephrine binds to alpha adrenergic receptors and causes vasoconstriction. Naphazoline is also a mild beta adrenergic receptor agonist, which can cause rebound vasodilation after the alpha adrenergic stimulation has ended. Naphazoline's release of norepinephrine also triggers a negative feedback loop which decreases production of norepinephrine, which can lead to rhinitis medicamentosa after long term use when naphazoline is stopped. |
| Pharmacodynamics | Naphazoline is a sympathomimetic alpha adrenergic agonist that acts to vasoconstrict nasal or ocular arterioles, resulting in reduced congestion at the site of administration. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alpha-2A adrenergic receptor | Humans | agonist |
| Alpha-1A adrenergic receptor | Humans | agonist |
ADME / PK
| Absorption | Absorption data for naphazoline are scarce but imidazoline compounds in general are weakly basic and lipophilic, with high bioavailability from the gastrointestinal tract. |
|---|---|
| Half-life | Half life has not been determined but effects last for 4 to 8 hours. Other imidazoline compounds have half lives varying from 2 to 12 hours. |
| Protein binding | Protein binding data for naphazoline is unavailable. |
| Metabolism | Metabolism data for naphazoline are scarce. Imidazoline compounds undergo some hepatic metabolism but a large fraction of the dose may be excreted unchanged in the urine. |
| Route of elimination | Imidazoline compounds undergo some hepatic metabolism but a large fraction of the dose may be excreted unchanged in the urine. Urinary excretion is higher with more acidic urine. |
| Volume of distribution | Distribution data for naphazoline are scarce but imidazoline compounds are distributed throughout the body, and can cross the blood-brain barrier. |
| Clearance | Clearance data for naphazoline is unavailable. |
Formulation & handling
- Naphazoline is a small molecule primarily formulated for topical ocular and nasal delivery as solutions or sprays.
- Low water solubility and moderate logP indicate careful formulation is needed for optimal bioavailability in aqueous-based dosage forms.
- No known peptide or biologic nature or significant food sensitivity influences its handling or formulation considerations.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is nearing patent expiry in the US and Canada, leading to increased availability of generic versions and a transition towards a mature market phase in both regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Naphazoline includes multiple originator companies producing branded products predominantly in the US and Canadian markets. The presence of several branded formulations suggests an established supply network, while the absence of noted patent details indicates potential existing generic competition in these regions. |
|---|
Safety
| Toxicity | In high doses or when ingested, naphazoline can lead to central nervous system depression (which can progress to coma and death), hypothermia, bradycardia, and death. This effect is especially pronounced in children under 6 years. Long term use of naphazoline can lead to rhinitis medicamentosa once naphazoline is stopped. This condition is a result of norepinephrine release by naphazoline triggering a negative feedback loop. Safety and effectiveness in children under 12 has not been established. Studies in elderly patients have yet to be performed. Risk in pregnancy, breast feeding, and on overall fertility have not been established, though pregnant and breast feeding patients should consider the risk and benefit before starting naphazoline treatment. |
|---|
- Naphazoline poses a risk of central nervous system depression, hypothermia, and bradycardia in cases of overdose, with increased severity in children under 6 years
- Prolonged use may induce rhinitis medicamentosa due to norepinephrine-mediated feedback mechanisms
- Safety and efficacy data are insufficient for pediatric patients under 12, elderly populations, and during pregnancy or lactation
Naphazoline is a type of Alpha blockers
Alpha blockers are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are widely used in the medical field. These medications are primarily utilized for their ability to block the alpha-adrenergic receptors, which are present in various parts of the body, including blood vessels and smooth muscle tissues. Alpha blockers work by preventing the receptor activation by the neurotransmitter norepinephrine, resulting in relaxation of the smooth muscles and dilation of the blood vessels.
These drugs find extensive applications in the treatment of several medical conditions. One of the most common applications of alpha blockers is in managing hypertension (high blood pressure) by promoting vasodilation, thereby reducing the resistance to blood flow. Additionally, they are employed in the treatment of benign prostatic hyperplasia (BPH) to relieve urinary symptoms by relaxing the smooth muscles in the prostate and bladder neck.
Some examples of popular alpha blockers include doxazosin, prazosin, and tamsulosin. Each of these medications may have specific indications and variations in their mechanism of action.
It is important to note that alpha blockers may cause certain side effects, such as dizziness, low blood pressure, and nasal congestion. Hence, it is crucial for healthcare professionals to carefully monitor patients receiving these medications and adjust the dosage accordingly.
In summary, alpha blockers are a vital subcategory of pharmaceutical APIs, playing a significant role in the management of conditions like hypertension and benign prostatic hyperplasia. Their mechanism of action involves blocking alpha-adrenergic receptors, leading to vasodilation and relaxation of smooth muscles. However, it is crucial to exercise caution while using these medications due to potential side effects.
Naphazoline (Alpha 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.
Naphazoline API manufacturers & distributors
Compare qualified Naphazoline API suppliers worldwide. We currently have 3 companies offering Naphazoline API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Micro Labs | Producer | India | India | CoA, USDMF | 38 products |
| Pharm Rx Chemical Corp | Distributor | United States | India | BSE/TSE, CoA, GMP, MSDS, USDMF | 166 products |
When sending a request, specify which Naphazoline 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 Naphazoline 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.
