Alpha 2 Agonist
Clonidine
Methydopa
Guanabenz
Guanfacine
Alpha 2 Agonist
Pharmacodynamics
inhibit cardiac acceleration and vasoconstriction centers in the brain-> decrease in
peripheral resistance, renal vascular resistance, HR, and BP
May lead to Na+ retention (increase blood volume-> increase BP) give with a diuretic if
this occurs
Clonidine
adverse reactions
DRY MOUTH, REBOUND HTN, GYNECOMASTIA, bradycardia, AV block, palpitations,
tachycardia, hallucinations, sleep disorders, contact dermatitis, OH, constipation,
nausea, urinary retention, decreased sexual activity, wt gain, leg cramps,
thrombocytopenia
Guanabenz and Guanfacine
adverse reactions
OH with standing, somnolence, fatigue, nausea, lethargy, hypotension, insomnia,
dizziness, abdominal pain
Methydopa
adverse reactions
Hemolytic anemia, positive coombs after 6 months of therapy
Clonidine
Metabolism & Excretion
Easily absorbed in GI tract and skin
Lipid-Soluble- enter Brain (CNS) from circulation rapidly
Crosses the placenta and found in breast milk
, 50% hepatically metabolized
50% excreted in urine
Guanabenz & Guanfacine
Metabolism and Excretion
Metabolized by CYP3A4 in liver and excreted by the kidneys- 50% eliminated in urine
Guanabenz- <1% unchanged in urine
Methydopa
Metabolism and Excretion
Not completely absorbed in the gut
Absorbed via aromatic amino acid transport system
Crosses placenta and found in breast milk
20% of drug in plasma
70% excreted in urine
Clonidine
Contraindications and Precautions
Caution with cerebrovascular disease, depression, Hx of bradycardia
Pregnancy Category Class C
Methydopa
Contraindications and Precautions
Caution with cerebrovascular disease
Pregnancy Category B- pass to breast milk
REBOUND HTN if given with Beta-Blocker
Coombs
Hemolytic anemia
Guanabenz & Guanfacine
Contraindications and Precautions
Guanabenz- Pregnancy Category C may cause gynecomastia
Guanfacine- Pregnancy Category B
Clonidine
Drug Interactions