Benzodiazepines: The Need-to-Know Series

I was a junior in college, and the anxiety was so intense I couldn’t peel myself from the ceiling. I had no clue as to what was going on, much less what to do about it. So I headed to the E.R. for help!?

I may have been clueless, but it seems my doc wasn’t. In very short order a syringe-full of Valium hit me like a ton of bricks. I sure as heck didn’t know what it was. But I walked away with a prescription for the stuff.

The benzodiazepines are a huge player in the treatment of the anxiety disorders.

In fact, alprazolam (Xanax) was the 12th most prescribed med in the US in 2010.

(Care to take a shot at #1? The answer’s at the bottom…)

Just as we did with the antidepressants, it’s time to get started on a benzodiazepine need-to-know series.

“What’s a benzodiazepine?”

Benzodiazepines (benzos) are actually anticonvulsants. They possess hypnotic, anxiolytic (anxiety-relieving), sedative, anticonvulsant, muscle relaxant, and amnesic actions.

Benzos are typically used to treat anxiety, panic, agitation, seizures, insomnia, and substance withdrawal. They’re also used for sedation.

Two tidbits of interesting history…

  • The first benzodiazepine, chlordiazepoxide (Librium), hit the market in 1960. Any idea what #2 was? diazepam (Valium).
  • The predecessors of the benzos were the barbiturates – e.g.: phenobarbital (Luminal).

The benzos are Schedule IV substances, according to the USs Controlled Substances Act (CSA).

“Short, intermediate, and long-acting?”

In very broad terms, let’s categorize the benzos…

  • Short-acting: Median half-life of 1–12 hours. They have few residual effects if taken before bedtime, rebound insomnia may occur upon discontinuation, and they might cause day time withdrawal symptoms such as next day rebound anxiety with prolonged usage. Examples: brotizolam (Lendormin), midazolam (Versed), and triazolam (Halcion).
  • Intermediate-acting: Median half-life of 12–40 hours. They may have some residual effects in the first half of the day if used as a hypnotic. Rebound insomnia, however, is more common upon discontinuation of intermediate-acting benzos than longer-acting. Examples: alprazolam (Xanax), estazolam (ProSom), flunitrazepam (Rohypnol), clonazepam (Klonopin), lormetazepam (Noctamid), lorazepam (Ativan), nitrazepam (Mogadon), and temazepam (Restoril).
  • Long-acting: Median half-life of 40–250 hours. They have a risk of accumulation in the elderly and in individuals with severely impaired liver function, but they have a reduced severity of rebound effects and withdrawal. Examples: diazepam (Valium), chlorazepate (Tranxene), chlordiazepoxide (Librium), and flurazepam (Dalmane).

A couple of “by-the-ways”…

  • A drug’s “half-life” is the time it takes for its plasma concentration to reach half of its original level. This is accomplished by our metabolic and elimination systems.
  • Benzos are not approved by the US Food and Drug Administration (FDA) for long-term use. You’ll find out why in a short.

“How do benzos work?”

Gamma-amino butyric acid (GABA) is by far the most abundant inhibitory (slows things down) neurotransmitter in the brain.

Located all over the brain, GABA has the ability to unlock and actually bring to life anxiety-inhibiting receptors on nerve cells. It also has sleep-inducing characteristics.

Sounds like the perfect target in the midst of a nasty case of anxiety. Well, it is – and the benzos enhance the action of GABA. And that’s why they can make you feel so (too?) good.

“Do benzos carry any baggage?”

Benzos can pose some very serious problems in the immediate and down the road. The reason benzos aren’t approved for long-term use by the US FDA is because of the huge risk for tolerance, dependence, and withdrawal symptoms upon cessation.

Other potential problems stemming from long-term use are psychomotor, cognitive, and/or memory impairments. Depression and anxiety may also present.

Potential risks that come with short-term benzo use include – cognitive impairments, aggression, and other behavioral disinhibition. The last two are known as paradoxical effects – presentation of the exact opposite of the intended effects. Other paradoxical effects include increased seizures in epileptics, irritability, impulsivity, and suicidal ideation/behavior.

Paradoxical effects occur in much greater frequency in benzo abusers, those with borderline personality disorder, children, and those using high-dosage regimens.


The most common side-effects of the benzos are – drowsiness, dizziness, decreased alertness and concentration, lack of coordination (particularly in the elderly), impairment of driving skills, decreased libido, erectile dysfunction, depression, and disinhibition.

With intravenous benzo use, hypotension and suppressed breathing may occur.

Side-effects not as likely to present are – nausea, appetite change, blurred vision, confusion, euphoria, depersonalization, and nightmares. Cases of liver toxicity have been noted, but are very rare.

If you endure depressive symptoms or are a recent substance abuser, benzos aren’t for you! The same applies to pregnancy.

Be sure to discuss use, potential use, and cessation with your physician.

Let’s Wrap Part 1

Did we get off to a great start, or what? Benzos are serious business!

Be sure to come back tomorrow, as we’ll wrap the series by talking about how to stop taking a benzo – and what to expect.

I’ll also offer-up my professional opinion on benzo use.

Oh, almost forgot! The answer I promised you earlier. Did you make a guess?

The most prescribed med in the US for 2010 was hydrocodone/acetaminophen (Vicodin).