Overview
| Generic Names: | Guanfacina [INN-Spanish]; Guanfacine HCl; Guanfacine Hydrochloride; Guanfacinum [INN-Latin]; SPD 503; guanfacine |
|---|---|
| Trade Names: | Estulic; Intuniv; Tenex |
| PharmGKB Accession Id: | PA449825 |
Description
A centrally acting antihypertensive agent. The drug lowers both systolic and diastolic blood pressure by activating the central nervous system alpha-2 adrenoreceptors, which results in reduced sympathetic outflow leading to reduced vascular tone. Its adverse reactions include dry mouth, sedation, and constipation. PubChem (source: Drug Bank)
Indication
For use in the management of hypertension. (source: Drug Bank)
ATC Therapeutic Category
- C02AC:Imidazoline receptor agonists
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Guanfacine selectively stimulates central alpha(2)-adrenergic receptors, resulting in inhibition of sympathetic nervous system outflow, reduction of peripheral and renal vascular resistance, and lowering of blood pressure and heart rate. (source: Drug Bank)
Pharmacology
Similar to clonidine, guanfacine is a centrally-acting, alpha(2)-adrenergic receptor agonist used alone or in combination with other drugs for the treatment of hypertension. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
Approximately 70% bound to plasma proteins, independent of drug concentration. (source: Drug Bank)
Absorption
Rapid and complete, with an oral bioavailability of approximately 80%. (source: Drug Bank)
Toxicity
Symptoms of overdose include drowsiness, lethargy, bradycardia and hypotension. LD<sub>50</sub>=165mg/kg (orally in mice) (source: Drug Bank)
Isomeric SMILES Code:
c1cc(c(c(c1)Cl)CC(=O)NC(=N)N)Cl (source: Drug Bank)
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ADRA1B |
|
(source: Drug Bank) |
| ADRA2A |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.