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guanabenz (Wytensin)
Tradename: Wytensin.
Dosage: start 4 mg PO BID; max 32 mg/day
Tabs: 4 & 8 mg.
Mechanism of action:
1) a centrally acting antihypertensive agent
2) a centrally acting agent like clonidine
3) unlike clonidine, no rebound hypertension associated with discontinuation
4) binds to a regulatory subunit of protein phosphatase 1, PPP1R15A/GADD34, selectively disrupting stress-induced dephosphorylation of eIF2-alpha & stress-induced protein synthesis, adjusting protein synthesis rates to levels manageable by chaperones, favoring protein folding & rescuing cells from protein misfolding stress [2]
5) no effect on related PPP1R15B-phosphatase complex & constitutive protein synthesis [2]
Interactions
drug interactions
drug adverse effects (more general classes)
General
centrally-active alpha-adrenergic receptor agonist
Properties
AGONIST-FOR: adrenergic receptor
MISC-INFO: elimination route LIVER
KIDNEY
pregnancy-category C
safety in lactation -
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996 pg 781
- Tsaytler P et al.
Selective inhibition of a regulatory subunit of protein
phosphatase 1 restores proteostasis.
Science 2011 Apr 1; 332:91.
PMID: 21385720