Thursday, January 2, 2020

What's the Deal With: Fioricet?

Image result for fioricet history

This post is about the somewhat rare pharmaceutical butalbital; a barbiturate.  If you're unfamiliar with barbiturates, they include drugs like secobarbital (Seconal), amobarbital (Amytal), pentobarbital (Nembutal) & phenobarbital (Luminal).  Barbiturates are, by and large, obsolete in today's pharmacopoeia.  Benzos have replaced them due to the lower risk of overdose, though the withdrawal & addiction risks are quite similar.  Sometimes other old tranquilizers like Quaaludes & Miltown are lumped in with the barbs, though they aren't technically in the same family.  Common uses for these meds included treatment of anxiety, insomnia, seizures & muscle pain. 

There is one exception, however:  butalbital.  Known by its brand names Fioricet, Esgic & Margesic, butalbital is now prescribed mainly for migraine & tension headache treatment.  I happened to have a liberal doctor in my previous area who prescribed it as a FIRST LINE treatment for my migraines, which is apparently rare.  Now my current doctor continues to fill the script even though he "doesn't really like the med" lol.  Fioricet contains a combo of acetaminophen (300 mg), caffeine (40 mg) & butalbital (50 mg), making it something of an upper/downer combo.  Neato!  Butalbital has apparently been banned in some European nations due to its addictive nature.

History & Pharmacology

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Barbiturates of yore

Barbs act more like alcohol than benzos do.  Unlike benzos, which bind to a subunit on the GABA-a site & increase firing of the neuron, barbs are simple GABA agonists that induce their effects by triggering the brain to convert GABA to glutamate.  Now barbiturates are mostly reserved for assisted suicide & executions due to their reliability as euthanasia both in humans & animals.  Yeah, scary.  This is why you must take care not to overdose or combine with other downers.  Fioricet was approved by the FDA in 1984 for treating migraine & related headaches.  It does work quickly for migraines but that's not why I'm writing about it.  My interest is mostly in its uniqueness & rarity as a barbiturate. 

I have no idea why butalbital survived the barbiturate culling & is still prescribed today, nor why it's a Schedule IV drug (in many states; Schedule III in others) rather than a more heavily controlled substance.  Its effects are definitely heavy; more potent than equal doses of Valium or Klonopin & longer-lasting than Xanax.  It potentiates codeine & other opioids powerfully, but beware:  butalbital by itself can cause respiratory depression in high doses, let alone when combined with other depressants like opioids.  Don't ever combine high doses of the two or drive under its influence.  I guess I would compare its effects most closely to Soma (carisoprodol) if I had to pick. 

Recreational Effects

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Scary 1950's ad for a benzo (Mogadon).

As for the effects, they're somewhere between those of alcohol & benzos.  Your body feels more loose & floaty while your mind is deeply relaxed like with a benzo.  There's a bit of a physical numbness that feels like what I imagine Quaaludes must've felt like.  On the downside, I get all the same miserable after-effects with butalbital that I get from benzos--maybe a little worse.  Low mood, irritability, anxiety & worsening OCD symptoms the next day.  But in the moment you haven't a care in the world.  Butalbital is an intermediate-acting barbiturate that stays in your system for days & induces the P450 enzyme.  This makes it somewhat liver toxic on its own--with the combined acetaminophen it could be dangerous in high doses or if you have liver troubles.  But it's fine for a one-off good time if you don't drink. 

So what's the verdict?  Fioricet can be a somewhat fun & interesting substance if used in moderation.  I probably would give it a 3.5 out of 5 on the 'recreational potential meter'.  I like it best when combined with LOW doses of codeine to spice things up; the combo makes both drugs more interesting than either is alone.  (But again, be careful).  It makes me curious what other barbs were like, as they were highly popular in my parents' day. 

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