What are benzodiazepines, and how do they work (mechanism of action)?

Benzodiazepines are man-made medications that cause mild to severe depression of the nerves within the brain (central nervous system) and sedation (drowsiness).

Seizures, anxiety, and other diseases that require benzodiazepine treatment may be caused by excessive activity of nerves in the brain. These drugs may work by enhancing the effects of gamma-aminobutyric acid (GABA) in the brain. Gamma-aminobutyric acid is a neurotransmitter, a chemical that nerves in the brain use to send messages to one another. Gamma-aminobutyric acid reduces the activity of nerves in the brain and increasing the effect of GABA with a benzodiazepine, reduces brain activity.

What are their uses?

Adult men and women use benzodiazepines to treat:

• Anxiety
• Nervousness
• Panic disorders
• Muscle spasms
• Seizures
• Sleeplessness
• Alcohol withdrawal
• Status epilepticus (A life-threatening disorder of the brain.)
• Premenstrual syndrome

Other uses for benzodiazepines

These medications also are used for:

• Sedation during surgery
• The treatment various types of anxiety disorders, for example:
  • Generalized anxiety disorder (GAD)
  • Social anxiety disorder (when antidepressants aren't effective)
  • Panic disorder (when antidepressants aren't effective)

Benzodiazepine drugs (also called benzos) are habit forming and can lead to addiction. Long-term use also can lead to tolerance, which means that lower doses will become ineffective and patients will need higher doses. These drugs are abused to get 'high' due to their effects on the brain.

Benzodiazepine side effects

Benzodiazepine side effects

Common side effects include:

• Lightheadedness
• Drowsiness
• Confusion
• Sedation
• Memory impairment
• Improper body balance
• Increase or decrease in appetite
• Nausea
• Vomiting
• Constipation
• Weight gain
• Dry mouth
• Reduced libido
• Fatigue

Serious side effects include:

• Respiratory depression
• Dependence and abuse
• Withdrawal symptoms
• Jaundice
• Seizures
• Suicide
• Slow heart rate
• Severe low blood pressure
• Fainting
• Akathisia (a movement disorder)
• Increased heart rate

Is it OK to drink alcohol or take similar drugs to benzodiazepines together (drug interactions)?

No. Combining alcohol with a benzodiazepine is very dangerous. People who drink alcohol while taking this medicine will feel the effects of alcohol faster. It's not safe to drink alcohol or take other drugs that have similar effects on the central nervous system (CNS) at the same time because these drugs or substances interact with oral benzodiazepines by causing additional depression of the brain and respiratory depression. Respiratory depression can lead to breathing that's inadequate for supplying oxygen to the body. This can cause death. Examples of these drugs and products that increase sedative side effects or the risk of respiratory depression from benzodiazepines include:

Pain medications called opioids that also cause respiratory depression, for example:

• morphine (MScontin)
• fentanyl (Duragesic)
• oxycodone (Oxycontin)
• hydrocodone (Zohydro ER)
• acetaminophen/hydrocodone (Vicodin, Norco, Lorcet)

Sedatives (for example, insomnia medicine) and other medicine that cause sedation, for example:

• zolpidem (Ambien, ZolpiMist)
• Intermezzo
• zaleplon (Sonata)
• eszopiclone (Lunesta
• phenobarbital
• many other drugs

Can you become addicted to these drugs?

Yes, benzodiazepines or benzos are habit forming and you can become addicted to them - even if you take them as your doctor or health care professional has prescribed. People who have a history of drug or alcohol abuse are more likely to develop an addiction to these drugs. If you use these drugs over a long period of time you can develop a tolerance for them. This means that you will need higher doses of the drug to treat your health condition or disease because you've become tolerant of the weaker formulations of the drug. These drugs may be very effective for the treatment of several conditions, for example, anxiety and insomnia; but be careful because you can become addicted to them.

The street names for benzodiazepine drugs are "Benzos" and "Downers." Drug addicts abuse these drugs to get "high." They can cause addiction similar to opioids (narcotic drugs like oxycodone, morphine, hydrocodone, and fentanyl), cannabinoids (marijuana), and the club drug GHB (gamma-hydroxybutyrate).

They are commonly abused by young adolescents and young adults who crush it up and snort it, or take the tablet to get high. If you abuse this medication you may have adverse effects with symptoms include:

• Disturbing or vivid dreams
• Irritability
• Hostility
• Amnesia

Signs and symptoms that you might be addicted include:

• Problems sleeping
• Diarrhea
• Vomiting
• Nausea
• Goose bumps
• Uncontrollable leg movements
• Bone and muscle pain

It is very difficult to recover from benzodiazepine addiction because these drugs change the chemistry of the brain. Contact a drug addiction treatment center if you or a loved one are suffering from a addiction. Quitting cold turkey is not likely to be successful and can be dangerous because of symptoms of withdrawal. Doctors and other health care professionals that treat addiction will formulate a taper schedule to slowly wean off the medication to reduce the severity of withdrawal symptoms during treatment.

Signs and symptoms of overdose include:

• Clammy skin
• Dilated pupils
• Rapid and weak pulse
• Coma
• Shallow breathing
• Death

Withdrawal symptoms and signs

If you stop taking these medications abruptly you may experience withdrawal symptoms that include:

• Problems concentrating
• Sleep problems
• Irritability
• Increased anxiety and tension
• Panic attacks
• Hand tremors
• Dry heaving and vomiting
• Palpitations
• Headache
• Muscle pain and stiffness
• A host of perceptual changes

The severity of the withdrawal symptoms depends on amount and duration of benzodiazepine use. Withdrawal symptoms can be deadly.

These medications are classified by the Drug Enforcement Administration (DEA) as Schedule IV drugs. This means that they have a lower potential and risk of dependence than other more powerful drugs like codeine, testosterone, anabolic steroids, Vicodin (hydrocodone and acetaminophen), OxyContin (oxycodone), Adderall (amphetamine and dextroamphetamine), and Ritalin (methylphenidate).

List of examples of generic and brand names for benzodiazepines

Examples of oral benzodiazepines are:

• alprazolam (Xanax, Xanax XR)
• clobazam (Onfi)
• clonazepam (Klonopin)
• clorazepate (Tranxene)
• chlordiazepoxide (Librium)
• diazepam (Valium, Diastat Acudial, Diastat)
• estazolam (Prosom is a discontinued brand in the US)
• lorazepam (Ativan)
• oxazepam (Serax is a discontinued brand in the US)
• temazepam (Restoril)
• triazolam (Halcion)

Formulations of benzodiazepines

All oral benzodiazepines are available in tablet forms.

• Alprazolam and clorazepate are available as extended-release tablets.
• Alprazolam, clobazam, diazepam, and lorazepam are available in oral liquid form.
• Alprazolam and clonazepam are available in orally dissolving tablets.
• Chlordiazepoxide, oxazepam, and temazepam are available in capsule form.
• Diazepam also is available as a rectal gel.
• Some benzodiazepines are available for injection.

Is it safe to take benzodiazepines if I'm pregnant or breastfeeding my baby?

• The FDA classifies benzodiazepines as pregnancy category D, which means that benzodiazepines can potentially cause fetal harm if administered to pregnant women. If benzodiazepines have to be used in pregnant women or if the patient may become pregnant while taking benzodiazepines, the patients must be informed of potential risks to the fetus.
• Benzodiazepines enter breast milk and can cause lethargy and weight loss in the newborn. Therefore, they should not be used in nursing mothers.