Guanfacine

Patent 2,928,829 March 15, 1960 assigned to Ciba Pharmaceutical Products, Inc. 

Patent 3,055,882 September 25, 1962 assigned to Ciba Corporation 

Chemical Name N-(Aminoiminomethyl)-2,6 lichlorobenzeneacetamide Common Name — 

Trade Name Manufacturer Country Year Introduced 

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Guanfacine. Guanfaciae, used ia patients having mild to moderate hypertension, can lower blood pressure 50/25 mm Hg (systoHc/diastoHc) ia hypertensive patients. Side effects such as sedation, dry mouth, and asthenia are less as compared to those of guanaben2 and clonidine. Guanfaciae reduces blood cholesterol and triglyceride and does not cause glucose iatolerance. 

Antiadrenergic drags (centrally acting)—for example, guanabenz (Wytensin) and guanfacine (Tenex)... 

C11H14CI3NO2) see Lofexidine ethyl 2,6-dichIorophenylacetate (C10H10CI2O2 90793-64-9) see Guanfacine ethyl 2,2-diethylacetoacetate... 

CH5N3 113-00-8) see Abacavir Amiloride Folic acid Guanfacine Pemoline Pyrimethamine Sulfamerazine Tetroxoprim... 

Central a2-Agonists Methyl dopa Clonidine (Catapres) Guanabenz Guanfacine (Tenex) Guanadrel No recommendations at this time Transient sedation initially First-line in pregnancy (methyldopa)... 

The proposed mechanism of ADHD pharmacotherapy is to modulate neurotransmitters in order to improve academic and social functioning. Pharmacologic therapy can be divided into two categories stimulants and non-stimulants. Stimulant medications include methylphenidate, dexmethylphenidate, amphetamine salts, and dextroamphetamine, whereas non-stimulant medications include atomoxetine, tricyclic antidepressants (e.g., imipramine), clonidine, guanfacine, and bupropion. 

T Blood pressure and stimulant Give clonidine or guanfacine 4- Dose or change to another medication Same as above but with baseline and... 

Clonidine, guanabenz, guanfacine, and methyldopa lower BP primarily by stimulating a2-adrenergic receptors in the brain, which reduces sympathetic outflow from the vasomotor center and increases vagal tone. Stimulation of presynaptic oq-receptors peripherally may contribute to the reduction in sympathetic tone. Consequently, there may be decreases in heart rate, cardiac output, total peripheral resistance, plasma renin activity, and baroreceptor reflexes. 

Other agents, clonidine and guanfacine, reduce norepinephrine activity by reducing its release. Open label studies suggest these agents might be helpful for the impulsivity that often accompanies PTSD, but the lone controlled study did not find guanfacine to be effective. 

Because it has not been used extensively to treat ADHD, not as much is known about its safety in children. It appears to cause less sedation than clonidine and fewer untoward effects on blood pressure as well. Because of its similarity to clonidine, the same precautions should be taken when prescribing guanfacine. EKGs should be performed periodically, and blood pressure and pulse should be checked at each office visit. 

Antidepressants and clonidine are the most commonly used augmentation strategies for ADHD. If the patient has tics or is troubled by insomnia, clonidine is a reasonable choice. After collecting a baseline EKG, clonidine should be started at 0.05 mg at bedtime for children and adolescents and 0.1 mg at bedtime for adults. The dose can be increased every 2 weeks or so while monitoring the patient s blood pressure and pulse. Although it has not been studied as well, guanfacine may work in much the same manner as clonidine. 

Guanfacine Stimulates NE alpha-2 receptor None ADHD... 

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