Guanfacine is an agonist type drug, belonging to a subtype of norepinephrine receptors. These receptors are heavily concentrated in the locus ceruleus and the prefrontal cortex. The main mode of action of the guanfacine drug is to lower both systolic and diastolic blood pressure, by activating norepinephrine receptors in the central nervous system that results in reduced peripheral sympathetic outflow and tone.
Although guanfacine’s effect is to lower blood pressure, it does not affect the patient’s heart rate. Studies have also shown that apart from its short-term effects of reducing hypertension, it also normalizes blood pressure over the long run.
Guanfacine, marketed under the brand name Tenex, is indicated for the treatment of patients with conditions such as hypertension, and may also be used as a part of adjunctive therapy in the treatment of Attention Deficit Hyperactivity Disorder (ADHD).
The recommended initial dosage of guanfacine hydrochloride either when given alone or concomitantly with other anti-hypertensive drugs, is 1 mg daily to be taken at bedtime in order to reduce somnolence. By 3 to 4 weeks, if the 1 mg dose seems insufficient, 2 mg may be given. Higher doses may be sued, but the occurrence of the side effects increase with the dosages taken (above 3 mg/day).
The most common side effects of guanfacine use include dizziness, drowsiness, constipation, gastrointestinal pains, headaches, appetite loss, nasal congestion and appetite loss. Allergic reactions such as hives, itching, swelling of the face, mouth and lips, have also been reported as some side effects of the drug.
Highly unlikely and rare side effects of the drug include chest pains, difficulty in breathing, blurred vision, jaundice and shortness of breath. The use of guanfacine may also result in side effects affecting sexual desire, behavioral changes such as mood and decision making changes, numbness and tingling of extremities, leg cramps, changes in taste and even impotence.
The use of the drug may also result in orthostatic hypotension, palpitations, tachycardia, and even bradycardia. A rather positive side effect found in patients is the increase in the performance of the spatial working memory.
Guanfacine hydrochloride is contraindicated in patients with a known hypersensitivity to the drug or its known components. It is also contraindicated in patients with severe liver, lung and heart failure.
Caution is to be exercised if patients have reported to have been diagnosed with cardiovascular conditions such as myocardial infarctions, fibrillations, and other heart problems.
Guanfacine may also cause sedation, dizziness or drowsiness, and hence, the use of the drug must be given caution when used during the execution of activities utilizing mental focus, alertness and attention. Caution should also be exercised if guanfacines is to be co-administered with other sedative drugs.
It is not known whether guanfacine has adverse effects to the fetus. However, the use of the drug in pregnant women should always be consulted with the doctor. Nursing mothers, or women planning to breastfeed must first consult their doctor prior to the usage of the drug. The potential benefits of the drug must always be weighed against its risks to the nursing mother and infant.
Guanfacine has the following structural formula:
• Molecular formula of guanfacine is C9H9Cl2N3O
• Chemical IUPAC Name is N-(diaminomethylidene)-2-(2,6-dichlorophenyl)acetamide
• Molecular weight is 246.093 g/mol
• Guanfacine available : 1mg tablets and 2mg tablets
Brand name(s): Estulic, Guanfacina, Guanfacinum, Tenex
Review published on: 19 August 2009
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