Guanfacine Hcl Er (guanfacine HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Guanfacine is a phenylacetyl-guanidine derivative hypotensive agent; the drug is a selective alpha2-adrenergic agonist.
Guanfacine appears to stimulate alpha2-adrenergic receptors in the CNS, causing inhibition of sympathetic vasomotor centers; this contributes predominantly to the hypotensive effects of the drug. Central effects of the drug result in reduced peripheral sympathetic nerve impulses from the vasomotor center to the heart and blood vessels, resulting in a decrease in peripheral vascular resistance and a reduction in heart rate. Under conditions of rest or exercise, cardiac output is not altered.
Guanfacine reduces blood pressure in both supine and standing positions; hypotensive effects may be somewhat greater in the standing position. Peripheral effects (stimulation of peripheral alpha2-adrenergic receptors) also may contribute to the drug's hypotensive effects.
Guanfacine lowers elevated plasma renin activity and plasma catecholamine concentrations in patients with hypertension, although these effects do not correlate with individual hypotensive responses.
Acute administration of guanfacine stimulates release of growth hormone, but the drug does not produce sustained elevation of growth hormone during chronic administration. Guanfacine does not affect plasma aldosterone, mean body weight, or electrolytes; a slight but insignificant increase in plasma volume is observed after 1 month of therapy. The drug reduces serum prolactin concentrations in hypertensive patients with elevated serum prolactin concentrations.
Guanfacine enhances neurologic activity in the prefrontal cortex, an area of the brain involved in planning, impulse control, and organization. The drug has been shown in nonhuman primates to improve prefrontal cortical function through direct action on postsynaptic alpha2A-adrenergic receptors located in the prefrontal cortex. Sedative effects, which are less severe than those seen with clonidine, are the result of inhibitory effects on noradrenergic locus ceruleus neurons and direct effects on the thalamus.
USES: This medication is used to treat attention deficit hyperactivity disorder (ADHD), as part of a total treatment plan including psychological, educational, and social measures. Unlike other drugs used to treat ADHD, guanfacine is not a stimulant. The exact way that guanfacine works to treat ADHD is unknown.
Guanfacine is thought to affect receptors in the parts of the brain that lead to strengthening working memory, reducing distraction, and improving attention and impulse control. Guanfacine may help lessen ADHD symptoms such as being disruptive, inattentive, hyperactive, impulsive, and arguing with adults or losing one's temper.
Generic name: guanfacine HCl
Pronunciation: (GWAN-fuh-seen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Guanfacine Hcl Er
Indications
The following indications are listed for Guanfacine Hcl Er:
- Attention-Deficit Hyperactivity Disorder
Also known as: Add With Hyperactivity.
Dosing
Dosage of guanfacine hydrochloride is expressed in terms of guanfacine.
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Guanfacine is contraindicated in patients with known hypersensitivity to the drug.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Common adverse effects in patients receiving guanfacine include dry mouth, somnolence, dizziness, constipation, fatigue, asthenia, impotence, and headache.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of guanfacine for the management of hypertension have not been established in children younger than 12 years of age; use in these pediatric patients is not recommended.
Mania and aggressive behavioral changes have been reported in pediatric patients with ADHD receiving guanfacine (as conventional tablets)+; all patients had medical or family risk factors for bipolar disorder. All patients recovered following discontinuance of the drug.
Category B. (See Users Guide.)
Guanfacine is not recommended for the treatment of acute hypertension associated with toxemia of pregnancy.
Guanfacine is distributed into milk in rats; it is not known whether the drug is distributed into human milk. Caution is advised if guanfacine is used in nursing women.
Guanfacine dosage should be selected with caution (usually starting at the low end of the dosing range) because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.
Clinical trial data for patients 65 years of age or older are insufficient to determine whether geriatric patients respond differently than younger adults. Other experience suggests that response is similar to that in younger adults.
Dosage of guanfacine should be selected with caution because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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