Guanfacine – Product Information

The prescription drug Guanfacine is used for the potential treatment of several modalities including anxiety, high blood pressure, and attention deficit hyperactivity disorder (ADHD). It is a member of the pharmacological class known as alpha-2 agonists, which reduces the activity of specific nerves in the body and brain. [R]

The guanfacine hydrochloride-modified release tablets are made to release the medication gradually, allowing it to be absorbed over a longer period of time and lowering peak plasma levels; as a result, the tablets shouldn’t be crushed or otherwise changed.  [R]

• CAS Number is stated as 29110-47-2.
• Molar Mass is 246.72 g/mol.
• It has a Chemical Formula of C9H9Cl2N3O
• IUPAC Name: N-(diaminomethylidene)-2-(2,6-dichlorophenyl)acetamide.
• Also known by Synonyms as the brand name Intuniv, as well as by other trade names such as Tenex, Afken, and Estulic.

What is Guanfacine?

On October 27, 1986, the FDA approved guanfacine. [R] This is a white to off-white crystalline powder sporadically soluble in water, approximately 1 mg/mL. The 2-octanol/water partition coefficient (logP) of guanfacine hydrochloride is 0.10; when dissolved in water, a pH of 4 and a dissociation constant of 7.69. The only organic solvent with relatively high solubility is methanol. [R] 

It belongs to a class of medications known as alpha-2 agonists, which function by reducing the activity of specific nerves in the body and brain. [R]

80% of guanfacine is bioavailable when taken orally. No distinct proof of any first-pass metabolism exists. With a 17-hour elimination half-life, renal excretion is the primary mode of elimination. The major intermediate is an epoxide, and the main metabolite is the 3-hydroxy-derivative, with evidence of modest biotransformation. Impairment of renal function has no effect on elimination. As a result, the liver is assumed to be responsible for metabolism with compromised renal function. [R] [R]

How Does Guanfacine Work?

Guanfacine works by making more norepinephrine, a neurotransmitter that is involved in controlling attention, available in the brain.  Being an agonist of the 2-adrenergic receptor, guanfacine affects the 2-adrenergic receptors’ ability to function. These receptors, which are dispersed throughout the central nervous system, control the sympathetic nervous system, which plays a role in the stress response. Guanfacine can decrease dopamine release, which is linked to hyperactivity and other ADHD symptoms, by activating these receptors. [R]

Guanfacine has been demonstrated to lower heart rate and blood pressure in people with high blood pressure in addition to its effects on catecholamines and the sympathetic nervous system. The central nervous system’s direct suppression of sympathetic nerve activation, which can lower blood pressure and reduce cardiac output, mediates this action. [R]

Independent of drug concentration, guanfacine is moderately (around 70% bound) bound to plasma proteins. [R]

Guanfacine Research

Guanfacine is a prescription medication commonly used to treat ADHD, anxiety, and high blood pressure. Research efforts aimed at providing insights into the efficacy and safety of guanfacine have been ongoing.

Guanfacine and Attention Deficit Hyperactivity Disorder (ADHD)

In young and adolescents test subjects with ADHD aged 6 to 17 years old, the effectiveness of guanfacine extended-release (GXR) was examined in a randomized, double-blind, placebo-controlled experiment. The study discovered that GXR lessen ADHD symptoms and enhanced social and familial functioning more effectively than a placebo. The negative effects, which often ranged from mild to moderate, included fatigue, headaches, and stomachaches. [R]

Guanfacine is successful in lowering ADHD symptoms and enhancing cognitive performance in young and adolescents test subjects, according to a thorough assessment of the drug’s clinical efficacy, safety, and pharmacology for the treatment of ADHD. Guanfacine has a good safety record, according to the study, with drowsiness, vertigo, and headache being the most frequent side effects. [R]

Guanfacine and Anxiety / Post-Traumatic Stress Disorder (PTSD)

An evaluation of the effectiveness of guanfacine in lowering anxiety symptoms in test subjects with a generalized anxiety disorder (GAD) used randomized, double-blind, placebo-controlled research. According to the study, guanfacine considerably outperformed a placebo in terms of easing anxiety symptoms. Dry mouth and severe dizziness were the most frequent side effects. [R]

Guanfacine was found to be beneficial in lowering anxiety symptoms in the majority of test subjects in a case series of 12 test subjects with treatment-resistant anxiety disorders. The study also found that guanfacine was typically well tolerated, with somnolence and dizziness being the most frequent side effects. [R]

In a randomized, double-blind, placebo-controlled research, the effectiveness of guanfacine in easing PTSD symptoms in test subjects was assessed. According to the study, guanfacine reduced PTSD symptoms like hyperarousal, re-experiencing, and avoidance better than a placebo. Sleepiness and lightheadedness were the most frequent side effects. [R]

Guanfacine and High Blood Pressure

1,614 adult test subjects with hypertension randomized, double-blind, placebo-controlled research demonstrated that guanfacine extended release significantly reduced systolic and diastolic blood pressure compared to placebo. Constipation, headaches, lethargy, and dizziness were the most frequent side effects. [R]

Another systematic review and network meta-analysis of placebo-controlled studies involving 3,988 hypertensive adult test subjects revealed that guanfacine extended release was as effective as other widely prescribed antihypertensive drugs at lowering both systolic and diastolic blood pressure. Constipation, sleepiness, and dizziness were the most frequent adverse reactions. [R]

Guanfacine extended release was found to be helpful in lowering both systolic and diastolic blood pressure, with a significant reduction seen within two weeks of starting therapy, according to this double-blind, randomized, placebo-controlled research that involved 99 test subjects with hypertension. Sleepiness, sleeplessness, and dry mouth were the most frequent adverse reactions. [R]

Guanfacine and Tourette Syndrome

Before the age of 18, Tourette syndrome manifests as a hyperkinetic movement condition with a variety of motor and phonic tics that can fluctuate in severity. An individual’s tics may change in intensity and manifestation throughout time. Tourette syndrome has been linked to depression and has the potential to harm social interactions and academic performance. Obsessive-compulsive disorder and attention-deficit/hyperactivity disorder are the most prevalent comorbidities. The goal of this study is to provide practitioners with the knowledge they need to provide pediatric patients with this illness with the best possible care by focusing on the symptoms, potential causes, and current non-pharmacologic and pharmacologic treatment options for Tourette syndrome. Overall, both non-pharmacologic and pharmaceutical therapies must be individually chosen depending on the severity of the symptoms, the test subject’s lifestyle, the side effects, and the effectiveness of past therapies. Future research may help define consistent strategies for treating tics associated with Tourette syndrome. [R]

Guanfacine and Withdrawal Treatments

Guanfacine has been researched as a treatment for opioid, ethanol, and nicotine withdrawal. It has been demonstrated that using guanfacine can lessen stress-induced nicotine cravings in smokers trying to stop, which may include enhancing prefrontal cortex-mediated self-control. [R] [R]

One study used a validated laboratory analog of stress-precipitated smoking, fMRI, and a proof-of-concept treatment period to evaluate the effects of guanfacine on stress-precipitated smoking in the laboratory, cortico-striatal activation during a cognitive-control task, and smoking following a quit attempt. The study found that stress-induced smoking was reduced in nicotine-deprived test subjects who were treated with guanfacine compared to those who received a placebo. Guanfacine also altered prefrontal activity during a cognitive control task and reduced cigarette use, although it did not increase complete abstinence during treatment.

Interestingly, following stress, guanfacine-treated subjects demonstrated increased cortisol levels, whereas placebo-treated subjects demonstrated decreased levels. These findings suggest that guanfacine may be a promising treatment option for smoking cessation, particularly in test subjects who experience stress-induced smoking. The study also highlights the potential importance of the noradrenergic system in stress-induced smoking and prefrontal cognitive control. Overall, while these findings are preliminary, they suggest that guanfacine may be a promising treatment for smoking cessation and further studies are warranted to evaluate its efficacy and safety in this population. [R]

Guanfacine Side Effects

Drowsiness, dry mouth, vertigo, headaches, nausea, stomach pain, and orthostatic hypotension (low blood pressure upon standing) are typical adverse effects. [R]

Angioedema (facial swelling), depression, breathing difficulties, irregular heartbeats, mental status changes, and seizures are rare but potentially significant adverse effects. [R]

Certain medications, may interact with guanfacine and increase the risk of side effects or possible drug interactions. It is uncommon for Guanfacine to cause a very serious allergic reaction. If an overdose has occurred, contact a poison control center immediately. In the United States, you can contact either the provincial poison control center or the local poison control center.

Frequently Asked Questions (FAQs)

What is the half-life of Guanfacine?

According to statistics released by the U.S., the half-life of guanfacine, or the period of time it takes for half of the initial dose to be removed from the body, is roughly 7-8 hours in adults. Drug Enforcement Agency (DEA). [R]

Is Guanfacine legal?

The United States has approved guanfacine. FDA has approved these indications for use in specific age groups.

Guanfacine is FDA-approved for the treatment of ADHD in children and adolescents aged 6 and older. Additionally, it is permitted to treat anxiety in kids six years old and older. Finally, adults who are 18 years of age and older can use it to treat high blood pressure. [R]

It is not recommended to purchase Guanfacine from an online pharmacy unless with a valid prescription from a health care professional. It is essential to ensure the safety and efficacy of the medication you are purchasing.

Is it safe during pregnancy?

Studies on animals failed to find any proof of prenatal damage. Considering that it is unknown if this medication passes to human breast milk, caution is suggested when breastfeeding. [R]

Handling and Storage

Guanfacine should be kept in its original container to prevent cross-contamination of the drug. Keep minors and other unauthorized individuals away from the medication. Drugs may be hazardous, so never share them or give them to someone else. Do not store the drug in the bathroom, close to a range, or in direct sunlight. Keep it away from heat and moisture. The drug should be discarded if it has expired, been accidentally contaminated, or has been dumped on a floor or other surface. Always abide by the expiration date printed on the medication label. [R]

Summary

Guanfacine or guanfacine hydrochloride, works by making more norepinephrine, a neurotransmitter that is involved in controlling attention, available in the brain. The symptoms of attention deficit hyperactivity disorder (ADHD) in children, adults, and teenagers may be lessened by this impact. Also, Guanfacine has been demonstrated to lower heart rate and blood pressure in people with high blood pressure. However, due to its potential typical adverse side effects, the use of Guanfacine needs further research and consultation.

 BehemothLabz Disclaimer

Please make sure you go through the Terms and Conditions, and please familiarize yourself with it as it is important. Please research the scientific uses of this product before making any purchases. Make note that the packaging and labels of the product may differ from those shown on the website.
Buying the product means you agree with our Terms and Conditions. You can contact our awesome customer service team at [email protected] if you are not fully satisfied with the product. Customer satisfaction is our number one priority!

 ATTENTION: All BehemothLabz products are strictly for LABORATORY AND RESEARCH PURPOSES ONLY. They are not to be used for any human or veterinary purposes.