PHRM 211 Lecture Notes - Lecture 5: Primidone, Zopiclone, Phenobarbital
Document Summary
Med chem of neuromodulator drugs (part 2) 19 possible subunits: 1-6 , 1-3 , 1-3 , , , , , 1-3 in a 2:2:1 ratio. Tautomerization is driven by acidity at position 2. Lacks pharmacological activity, but its 5,5-disubstituted derivatives yield potent & lipophilic weak acids (pka between 7. 5 & 9. 3) the more lipophilic, the more potent. & faster onset of action (10 min vs 60 min), but shorter duration of action. All three compounds possess anti-seizure activity (pema is weaker, more toxic metabolite). Similar to other gaba a receptor activators, barbiturates enhance gaba activity . However, higher barbiturate concentrations can lead to direct opening of the cl- channel & possible overdose due to cns-mediated respiratory and cardiovascular depression. Tricyclic compound chemically related to tricyclic antidepressants. Stabilizes the inactivated state of voltage-dependent na+ channels. Primarily metabolized by cyp3a4 (autoinduction) to a 10,11-epoxide (active but possibly toxic), which is subsequently hydrolyzed by epoxide hydrolase to.
