Guanfacine
- Atc Codes:C02AC02
- CAS Codes:29110-48-3#29110-47-2
- PHARMGKB ID:29110-48-3#29110-47-2
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Belgium: Estulic; Hungary: Estulic.
North America
USA: Guanfacine, Intuniv, Tenex.
Asia
Japan: Tenex.
Drug combinations
Chemistry
Guanfacine Hydrochloride: C~9~H~9~Cl~2~N~3~O HCl. Mw: 282.55. (1) Benzeneacetamide, N-(aminoiminomethyl)-2,6-dichloro-, monohydrochloride; (2) N-Amidino-2-(2,6-dichlorophenyl)acetamide monohydrochloride. CAS-29110-48-3; CAS-29110-47-2 (guanfacine)(1979).
Pharmacologic Category
Hypotensive Agents; Central α-Agonists; α~2~-Adrenergic Agonist. Central Nervous System Agents, Miscellaneous. (ATC-Code: C02AC02).
Mechanism of action
The drug is a derivative hypotensive agent; selective α~2~-adrenergic agonist. Stimulates α~2~-adrenoreceptors in brain stem, thus activating an inhibitory neuron, resulting in reduced sympathetic outflow, producing a decrease in vasomotor tone and heart rate.
Therapeutic use
Used alone or in combination with other classes of antihypertensive agents in management of hypertension.
Pregnancy and lactiation implications
Not recommended for treatment of acute hypertension associated with toxemia of pregnancy. Unknown whether drug is distributed into human milk (use caution).
Unlabeled use
Has been used for treatment of attention-deficit hyperactivity disorder (ADHD) in pediatric patients.
Contraindications
Hypersensitivity to guanfacine or any component of the formulation.
Warnings and precautions
Skin rash with exfoliation reported. Avoid abrupt withdrawal (risk of symptoms of nervousness and anxiety and, less commonly, rebound hypertension). Use with caution in severe coronary insufficiency, recent acute MI, or cerebrovascular disease. Use not recommended in children under 12 years of age. Mania and aggressive behavior reported in pediatric patients with ADHD who received guanfacine. Use with caution in chronic hepatic or renal failure. Sedation and drowsiness possible (avoid use in CNS disease). May cause orthostasis. Use with caution in severe coronary insufficiency or recent MI. Use with caution in cerebrovascular disease. Use with caution in diabetes mellitus (may mask signs of hypoglycemia). Avoid use with other CNS depressants (effects might be potentiated). Avoid use in the elderly.