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Guanfacine: Difference between revisions

From Pharmacopedia
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parser-claude housekeeping, stimulants to psychostimulants per house rule
 
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{{MedTemplate
{{MedTemplate
| generic           = Guanfacine
| generic           = Guanfacine
| brand             = Intuniv
| brand             = Intuniv (extended-release), Tenex (immediate-release)
| structure         =  
| structure         =
| classes           = Alpha-2 agonist, ADHD medicine
| classes           = [[:Category:Alpha-2 adrenergic agonists|Alpha-2 adrenergic agonist]], [[:Category:ADHD medicines|ADHD medicine]], [[:Category:Antihypertensives|Antihypertensive (historical)]]
| mechanism          = Selective alpha-2A adrenergic receptor agonist
| uses              = <vote slug="adhd-use">Attention-deficit/hyperactivity disorder (monotherapy or adjunct to psychostimulants, ages 6-17)</vote>, <vote slug="tic-disorders-use">Tic disorders / Tourette syndrome (off-label)</vote>, <vote slug="opioid-withdrawal-adjunct-use">Opioid withdrawal adjunct (off-label)</vote>, <vote slug="ptsd-nightmares-use">PTSD-associated nightmares and hyperarousal (off-label, selected populations)</vote>, <vote slug="hypertension-historical-use">Hypertension (historical indication, largely supplanted by other classes)</vote>
| uses              =  
| starting_dose    = Intuniv ER 1 mg PO once daily; titrate by 1 mg/week as tolerated to clinical response
| starting_dose     =  
| preparations     = Extended-release tablets 1, 2, 3, 4 mg (Intuniv); immediate-release tablets 1, 2 mg (Tenex)
| preparations      =  
| fda_max          = 7 mg/day in children and adolescents; weight-based ceiling (~0.12 mg/kg/day) applies in smaller patients
| fda_max           =  
| pill_id           =
| routes             =  
| routes           = Oral
| onset             =  
| onset             = Gradual; full clinical effect over 2-4 weeks of titration
| duration           =  
| duration         = ~24 hours (ER formulation supports once-daily dosing)
| halflife           =
| halflife          = ~17-18 hours (Intuniv ER); ~17 hours (immediate-release)<ref name="intuniv-label">FDA Prescribing Information, Intuniv (guanfacine extended-release), Shire/Takeda, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf</ref>
| bioavailability    =
| bioavailability   = ~58% (extended-release); ~80% (immediate-release)<ref name="intuniv-label" />
| pregnancy         =  
| pregnancy        = Limited human data. Animal studies show fetal effects at maternally toxic doses; use only if benefits justify the potential risk.{{citation needed}}
| legal              =  
| legal             = [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, which is a meaningful contrast to the psychostimulant alternatives for ADHD<ref name="intuniv-label" />
| intro              =
| mechanism         = <vote slug="guanfacine-mech-claim">Selective postsynaptic α2A-adrenergic receptor agonist. In the prefrontal cortex, α2A activation on pyramidal-neuron dendritic spines strengthens working-memory and attention-regulation circuits by closing HCN channels and reducing cyclic-AMP-driven "noise" from competing inputs. The peripheral antihypertensive effect (the historical indication) reflects α2 agonism in brainstem sympathetic outflow regions.</vote> Sedation and hypotension are the dose-limiting effects; gradual titration and bedtime or split dosing mitigate both. Abrupt discontinuation can precipitate rebound hypertension, particularly with long-standing use<ref name="intuniv-label" />.
| pharmacokinetics   =  
| pharmacodynamics  =  
| indications        =  
| dosing             =  
| effects            =  
| interactions      = <pharmaInteractions/>
| pregnancy_details  =
| monitoring         =  
| counseling        =  
| anecdotes          =
| seealso            =
| references        =  
}}
}}


 
== References ==
[[Category:Alpha-2 Adrenergic Agonists]]
<references />