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Guanfacine | CAS No: 29110-47-2 | GMP-certified suppliers
A medication that treats attention deficit hyperactivity disorder (ADHD) alone or with stimulants, providing central nervous system effects and cardiovascular regulation benefits.
Therapeutic categories
Primary indications
- Guanfacine is indicated alone or as an adjunct with stimulants to treat ADHD
Product Snapshot
- Guanfacine is available primarily as an extended-release oral tablet formulation
- It is indicated for the treatment of attention deficit hyperactivity disorder (ADHD), either as monotherapy or combined with stimulants
- Guanfacine holds approved status in key regulatory markets including the US, Canada, and the EU
Clinical Overview
Pharmacodynamically, guanfacine exerts its effects primarily through stimulation of central alpha-2A adrenergic receptors. This receptor selectivity reduces sympathetic outflow, resulting in decreased heart rate and blood pressure. While the precise mechanism linking guanfacine’s receptor activity to its efficacy in ADHD remains undetermined, its central nervous system depressant properties contribute to symptom management. The drug demonstrates a long duration of action with once-daily dosing and a wide therapeutic window, as fatal overdoses have not been documented.
The mechanism of action involves attenuation of sympathetic nervous system effects on cardiovascular tissues, leading to hypotensive and bradycardic effects. Due to these pharmacologic actions, patients should be closely monitored for adverse events such as hypotension, bradycardia, and syncope during therapy.
Guanfacine is metabolized partly by cytochrome P450 enzymes, including CYP3A4 and CYP2C19. It is also a substrate and inhibitor of various transporters such as OCT1, OCT2, and MATE1, which may influence its pharmacokinetic profile. Renal excretion is a significant elimination pathway. Attention to possible drug-drug interactions mediated by these enzymes and transporters is advised.
From a safety and toxicity perspective, guanfacine’s bradycardia and hypotension risks necessitate careful dose titration and vigilance in populations sensitive to cardiovascular effects. It falls within multiple drug categories including central alpha-2 adrenergic agonists and antihypertensive agents.
Notable usage contexts include its branded extended-release formulations for ADHD, which are used globally as part of comprehensive treatment regimens.
For API procurement, quality considerations should prioritize compliance with pharmacopeial standards relevant to guanfacine, confirmation of polymorphic form and stability profiles, and assurance of appropriate impurity controls. Given the involvement of CYP enzymes in metabolism, API batches should be evaluated for consistency to ensure predictable pharmacokinetic behavior. Reliable sourcing should also address regulatory compliance with global good manufacturing practices (GMP).
Identification & chemistry
| Generic name | Guanfacine |
|---|---|
| Molecule type | Small molecule |
| CAS | 29110-47-2 |
| UNII | 30OMY4G3MK |
| DrugBank ID | DB01018 |
Pharmacology
| Summary | Guanfacine is a selective agonist of alpha-2A adrenergic receptors, modulating sympathetic nervous system activity on cardiovascular function. Its therapeutic effect in attention-deficit/hyperactivity disorder (ADHD) is observed clinically, though the precise mechanistic link remains unclear. The drug exhibits a long duration of action and primarily targets alpha-2A and alpha-2B adrenergic receptors. |
|---|---|
| Mechanism of action | Guanfacine is a selective alpha-2A adrenergic receptor agonist, which reduces the effects of the sympathetic nervous system on the heart and circulatory system. The link between guanfacine’s molecular mechanism and it’s effect on the treatment of ADHD has not been determined. |
| Pharmacodynamics | Guanfacine is a selective alpha-2A adrenergic receptor agonist but it is unclear how this translates to the treatment of ADHD. It has a long duration of action as it is given once daily and a wide therapeutic window as fatal overdoses have not been described in literature. Patients should be counselled regarding the risk of hypotension, bradycardia, and syncope. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alpha-2A adrenergic receptor | Humans | agonist |
| Alpha-2B adrenergic receptor | Humans | binder |
ADME / PK
| Absorption | Guanfacine is 80% orally bioavailable. 1mg immediate release oral guanfacine reaches a C<sub>max</sub> of 2.5±0.6ng/mL with a T<sub>max</sub> of 3.0h and an AUC of 56±15ng\*h/mL. 1mg extended release oral guanfacine reaches a C<sub>max</sub> of 1.0±0.3ng/mL with a T<sub>max</sub> of 6.0h and an AUC of 32±9ng\*h/mL. In adults, a 4mg oral extended release dose reaches a C<sub>max</sub> of 3.58±1.39ng/mL with a T<sub>max</sub> of 5.5h; in children, a 2mg oral extended relsease dose reaches a C<sub>max</sub> of 2.6±1.03ng/mL with a T<sub>max</sub> of 4.98h; in adolescents, a 2mg oral extended release dose reaches a C<sub>max</sub> of 1.7±0.43ng/mL with a T<sub>max</sub> of 4.96h. |
|---|---|
| Half-life | Guanfacine has a half life of 17 hours, but this may range from 10-30 hours. The half life is largely independant of renal function. |
| Protein binding | Guanfacine is approximately 70% protein bound in serum. |
| Metabolism | Guanfacine is oxidized by CYP3A4 to it's main metabolite, 3-hydroxyguanfacine. 3-hydroxyguanfacine is then either glucuronidated or sulphated. |
| Route of elimination | Guanfacine is 57.0±32.0% eliminated in the urine in patients with normal renal function. Patients with a glomerular filtration rate (GFR) of 10-30mL/min eliminate 14.0±9.0% of a dose in the urine, while patients with a GFR of <1mL/min eliminate 7.5±2.4% of a dose in the urine. |
| Volume of distribution | Guanfacine has a volume of distribution of 6.3L/kg. |
| Clearance | Guanfacine has a total body cleraance of 360±262mL/min and a renal clearance of 233±245mL/min in patients with normal renal function. Patients with a glomerular filtration rate (GFR) of 10-30mL/min had a total body clearance of 308±274mL/min and a renal clearance of 34±22mL/min. Patients with a GFR of <1mL/min had a total body clearance of 257±187mL/min and a renal clearance of 18±15mL/min. |
Formulation & handling
- Guanfacine is a small molecule API formulated primarily for oral extended-release tablet administration.
- It exhibits limited water solubility, requiring consideration in formulation to ensure adequate bioavailability.
- Handling and administration should avoid co-administration with high-fat meals due to increased systemic exposure.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's key patents in the United States expired between 2016 and 2023, indicating a transition toward market maturity with availability of generic versions. The product is currently marketed in Canada, the US, and the EU. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Guanfacine is produced by multiple manufacturers including several with generic capabilities, supported by a broad network of packagers. Branded extended-release guanfacine products are available in the US, EU, and Canadian markets. Patent expirations between 2016 and 2023 indicate that generic competition is currently present or imminent, contributing to a competitive supply landscape. |
|---|
Safety
| Toxicity | The oral LD<sub>50</sub> in rats is 142mg/kg and 15.3mg/kg in mice. The subcutaneous LD<sub>50</sub> in rats is 114mg/kg and 46mg/kg in mice. Patients experiencing and overdose may present with hypotension, drowsiness, lethargy, and bradycardia. Overdose should be managed by first calling local poison control. Patients may require intravenous saline to maintain blood pressure. |
|---|
- Handle with appropriate personal protective equipment due to moderate acute toxicity (oral LD50: 142 mg/kg in rats
- 15
- 3 mg/kg in mice)
Guanfacine is a type of Alpha-2 adrenergic agonist
Alpha-2 adrenergic agonists are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) commonly used in the field of medicine. These compounds specifically target and activate alpha-2 adrenergic receptors in the body, which are found primarily in the central nervous system.
Alpha-2 adrenergic agonists exhibit a wide range of pharmacological effects due to their interaction with these receptors. One of their main applications is in the management of hypertension (high blood pressure). By stimulating the alpha-2 adrenergic receptors in the brain, these agonists inhibit the release of norepinephrine, a neurotransmitter that constricts blood vessels. This action leads to vasodilation, resulting in a decrease in blood pressure.
Furthermore, alpha-2 adrenergic agonists are also utilized in ophthalmology to treat conditions such as glaucoma. By reducing the production of aqueous humor, the fluid responsible for intraocular pressure, these compounds help alleviate the symptoms of this eye disorder.
In addition to their cardiovascular and ophthalmological applications, alpha-2 adrenergic agonists have been investigated for their potential role in pain management, sedation, and even in the treatment of attention deficit hyperactivity disorder (ADHD). Research into these areas is ongoing, highlighting the versatility and potential of this API subcategory.
Overall, alpha-2 adrenergic agonists are valuable pharmaceutical compounds that play a crucial role in the treatment of hypertension, glaucoma, and other related disorders. Through their selective interaction with alpha-2 adrenergic receptors, these APIs offer a targeted approach to achieving desired therapeutic outcomes.
Guanfacine (Alpha-2 adrenergic agonist), 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.
Guanfacine API manufacturers & distributors
Compare qualified Guanfacine API suppliers worldwide. We currently have 4 companies offering Guanfacine 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 |
|---|---|---|---|---|---|
| Medichem | Producer | Spain | Unknown | CoA, USDMF | 39 products |
| Procos | Producer | Italy | Italy | CoA, USDMF | 22 products |
| Quimica Sintetica | Producer | Spain | Unknown | CoA, JDMF, USDMF | 51 products |
| Torrent Pharma | Producer | India | India | CoA, USDMF | 34 products |
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