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So in pharm we learned that the free base form of a local anesthetic (amides or esters) is the form that penetrates membranes better, and the cationic form is the active form that blocks VGNaC's.
But they've been extremely unclear on what kind of environment they're more "potent" in. In an acidic area, more ionized and less free base would exist. In a more basic pH, the free base would predominate.
Yet we've essentially had both situations presented as "less than ideal", it seems. Obviously the free base has to penetrate and the ionized form has to do the job. But since you really can't change the body's pH very well (although you could mix in some NaHCO3 I guess), I'm not really sure I understand which is more "ideal."
For instance, we're told that in an inflammed area, it would have a lower pH, and thus you'd have to inject more of the anesthetic (or inject it more peripherally with regards to the wound) because less free base would exist. Then we're told that an area with a very basic pH (and thus a higher amount of free base) would cause a reversal of a nerve block because of the lower amount of ionized active form.
I guess I'm just confused about how to actually apply the information.
But they've been extremely unclear on what kind of environment they're more "potent" in. In an acidic area, more ionized and less free base would exist. In a more basic pH, the free base would predominate.
Yet we've essentially had both situations presented as "less than ideal", it seems. Obviously the free base has to penetrate and the ionized form has to do the job. But since you really can't change the body's pH very well (although you could mix in some NaHCO3 I guess), I'm not really sure I understand which is more "ideal."
For instance, we're told that in an inflammed area, it would have a lower pH, and thus you'd have to inject more of the anesthetic (or inject it more peripherally with regards to the wound) because less free base would exist. Then we're told that an area with a very basic pH (and thus a higher amount of free base) would cause a reversal of a nerve block because of the lower amount of ionized active form.
I guess I'm just confused about how to actually apply the information.