Pharmacokinetics and Pharmacodynamics of Immediate-Release Versus Extended-Release Guanfacine in Adult Daily Smokers.
J Clin Psychopharmacol
; 39(2): 124-128, 2019.
Article
in En
| MEDLINE
| ID: mdl-30707118
ABSTRACT
BACKGROUND:
Guanfacine is Food and Drug Administration approved for hypertension and attention-deficit hyperactivity disorder and has been used off-label for migraine prophylaxis, heroin withdrawal, and more recently smoking cessation. Previous studies have shown positive effects of 3 mg/d of immediate-release (IR) guanfacine on smoking outcomes, but the dose equivalency of the IR and extended-release (ER) formulations is unknown. PROCEDURES A within-subject design was used to compare the pharmacokinetics and pharmacodynamics of 3 mg/d of IR, 4 mg/d of ER, and 6 mg/d of ER guanfacine in adult daily smokers (n = 5). Plasma medication levels, vital signs, cigarettes per day, tobacco craving, and adverse events were assessed. Medication was titrated to stable dosing after each laboratory day (3 mg/d IR, then 4 mg/d ER, then 6 mg/d ER).RESULTS:
Plasma medication levels did not differ between the 3 mg/d of IR and 4 mg/d of ER doses after 24 hours from last dose and were highest at the 6 mg/d of ER dose (3 mg/d IR M = 3.40 ng/mL, SE = 0.34 vs 4 mg/d ER M = 3.46 ng/mL, SE = 0.67 vs 6 mg/d ER M = 5.92 ng/mL, SE = 1.02). All doses of guanfacine decreased heart rate and blood pressure from baseline. Absolute values of cigarettes per day (6 mg/d ER) and tobacco craving (4 and 6 mg/d ER) were lowest with the ER formulations. Treatment-emergent adverse events were subject rated as minimal to mild, except dry mouth.CONCLUSIONS:
We demonstrated similar pharmacokinetic profiles between 3 mg/d of IR guanfacine and 4 mg/d of ER guanfacine, as hypothesized. All doses of guanfacine were well tolerated.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Guanfacine
/
Smoking Cessation
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Adrenergic alpha-2 Receptor Agonists
Limits:
Adult
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Female
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Humans
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Male
/
Middle aged
Language:
En
Journal:
J Clin Psychopharmacol
Year:
2019
Document type:
Article