guanabenz (Wytensin)
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Introduction
Tradename: Wytensin.
Dosage
start 4 mg PO BID; max 32 mg/day
Tabs: 4 & 8 mg.
Mechanism of action
- a centrally acting antihypertensive agent
- a centrally acting agent like clonidine
- unlike clonidine, no rebound hypertension associated with discontinuation
- 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]
- no effect on related PPP1R15B-phosphatase complex & constitutive protein synthesis[2]
More general terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996 pg 781
- ↑ 2.0 2.1 2.2 Tsaytler P et al. Selective inhibition of a regulatory subunit of protein phosphatase 1 restores proteostasis. Science 2011 Apr 1; 332:91. PMID: https://www.ncbi.nlm.nih.gov/pubmed/21385720