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PubChem
| Name: | Guanfacine |
|---|---|
| PubChem Compound ID: | 3519 |
| Description: | A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. |
| Molecular formula: | C9H9Cl2N3O |
| Molecular weight: | 246.093 g/mol |
| Synonyms: |
NCGC00024950-01; EINECS 249-442-8; Tocris-1030; Guanfacine; Guanfacina [INN-Spanish]; Benzeneacetamide, N-(aminoiminomethyl)-2,6-dichloro-; NCGC00015469-01; CAS-29110-48-3; NCGC00015469-02; 29110-48-3.
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DrugBank
Identification
| Name: | Guanfacine |
|---|---|
| Name (isomeric): | DB01018 |
| Drug Type: | small molecule |
| Description: | A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. |
| Synonyms: |
Guanfacine HCl; SPD 503; Guanfacinum [INN-Latin]; Guanfacine Hydrochloride; Guanfacina [INN-Spanish]
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| Brand: | Intuniv, Estulic, Tenex |
| Category: | Sympatholytics, Adrenergic alpha-Agonists, Antihypertensive Agents |
| CAS number: | 29110-47-2 |
Pharmacology
| Indication: | For use alone or in combination with other classes of antihypertensive agents in the management of hypertension. Has also been used for the treatment of attention deficit hyperactivity disorder (ADHD) in pediatric patients. |
|---|---|
| Pharmacology: | Guanfacine is a phenylacetyl-guanidine derivative hypotensive and a centrally-acting, alpha(2)-adrenergic receptor agonist used alone or in combination with other drugs for the treatment of hypertension. |
| Mechanism of Action: |
Guanfacine selectively stimulates central alpha(2)-adrenergic receptors, resulting in inhibition of sympathetic vasomotor centers, which contributes predominantly to the hypotensive effects of the drug. Central effects of guanfacine lead to reduced peripheral sympathetic nerve impulses from the vasomotor center to the heart and blood vessels. This ...
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| Absorption: | Rapid and complete, with an oral bioavailability of approximately 80%. |
| Protein binding: | Approximately 70% bound to plasma proteins, independent of drug concentration. |
| Biotransformation: | Hepatic |
| Route of elimination: | In individuals with normal renal function, guanfacine and its metabolites are excreted primarily in the urine. |
| Half Life: | 17 hours (range 10-30 hours) |
| Toxicity: | Symptoms of overdose include drowsiness, lethargy, bradycardia and hypotension. LD50=165mg/kg (orally in mice) |
| Affected organisms: | Humans and other mammals |
Interactions
| Drug interaction: |
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Targets
Enzymes
