Benzodiazepines: Complete Guidance From Experts

Benzodiazepines became the world's most commonly prescribed medications in the mid-to-late 1970s for treating anxiety disorders. These are among the most frequently prescribed drugs in the US. i.e., more than 112 million prescriptions in 2007.

Benzodiazepines slow down the central nervous system, which might result in sleepiness and a relaxed mood. They commonly treat brain-related conditions like seizures, anxiety, and other mental health conditions. In addition, benzodiazepines have hypnotic, anxiolytic, anticonvulsant, and muscle-relaxing properties.

Benzodiazepines are controlled substances in many countries, including the US. Hence, to purchase them, you need a prescription. These drugs are often effective and risk-free when taken for a brief period. Prolonged usage might result in tolerance, dependency, and other adverse effects.

What Are Benzodiazepines?

Benzodiazepines are drugs that reduce the activity of your nervous system. These medications are effective for a wide range of symptoms and diseases as they cause a decrease in nervous system activity. The action of benzodiazepines alters the neuronal activity that triggers stress and anxiety.

Uses Of benzodiazepines

The Food and Drug Administration (FDA) has approved BZD for the treatment of:

• Insomnia
• Generalized anxiety disorder
• Social anxiety disorder
• Seizure disorders, such as epilepsy
• Panic disorder

The potential usage will depend on the benzodiazepine type. Other diseases and difficulties for which doctors may give these medications off-label include

• Other sleep disorders
• Tic conditions,
• Alcohol withdrawal,
• Bipolar disorder

They could also employ them to get ready for specific medical procedures.

How Do Benzodiazepines Work?

Benzodiazepines produce CNS depression by activating the major inhibitory neurotransmitter gamma-aminobutyric acid, thus decreasing brain activity.

When BZD attaches to the binding site, there is an increase in the GABA affinity for its binding site. They function as a positive allosteric modulator, increasing the total conduction of chloride ions across the neuronal cell membrane when the BZD binds to the receptor. This increase in chloride ions causes the cell to become hyperpolarized, which lowers neuronal activity.

In the brain, overstimulation takes place when a person is anxious. When you take benzodiazepines, the brain releases signals to reduce this overstimulation, thus reducing anxiety symptoms.

What Are The Effects Of Consuming Benzodiazepine?

Benzodiazepines enhance gamma-aminobutyric acid (GABA), reducing your brain activity. The effects of the slowed activity include:

• Amnestic: BZD temporarily prevents the formation of new memories.
• Anxiolytic: They prevent and treat anxiety linked to various anxiety disorders. Medication having this effect "loosens" your grip on anxiety while it is active.
• Hypnotic: These extend or enhance sleep and decrease wakefulness during sleep.
• Sedative: Drugs with this characteristic decrease brain activity. These medications aid users in feeling more at ease, calming down, and sleeping better.

Types of Benzodiazepines

Benzodiazepines are classified according to their strength and duration of action. What conditions benzodiazepines treat depend on their potency and course of action. More potent, long-acting benzodiazepines are appropriate for usage in the short term or emergencies. Lower-strength, longer-acting benzodiazepines are typically effective in treating chronic, non-emergency illnesses.

BZDs are classified in terms of their elimination half-life into:

• Short-acting: They have a 1-to-12-hour median elimination half-life. This BZD finds use as a hypnotic due to its rapid sleep induction. They have few after-effects and can lead to rebound sleeplessness, amnesia, and dependence issues on disruption. Ex: Midazolam and Triazolam.
• Intermediate-acting: Elimination half-life is 12-40 hours. Typically, they are employed to treat anxiety. Using it as a hypnotic could produce after-residual effects that last the next day. Example, Lorazepam, Alprazolam, and Clonazepam.
• Long-acting: Their average elimination half-life ranges from 40 to 250 hours. They carry a danger of accumulation, particularly in older people or people with metabolic disorders. Ex: Chlordiazepoxide, Diazepam.

What are the Approved Benzodiazepines?

Physicians prescribe Benzodiazepines intravenously or orally. Some are also available as nasal sprays or topical gels. The Food and Drug Administration (FDA) has given the following benzodiazepines its approval to treat the conditions listed below:

What Are The Non-approved Benzodiazepines?

Benzodiazepines are widely helpful in treating various conditions, such as anxiety, sleeplessness, and seizures. Nonetheless, its non-medical/recreational usage has long been linked to abuse, dependence, and overdose deaths.

Many benzodiazepines have been subject to international control since 1984 under United Nations Convention on Psychotropic Substances of 1971, which aims to safeguard access to these necessary medications while reducing their propensity for abuse and dependence.

The use of several benzodiazepines is illegal in the US. Some BZDs have received consent from other nations, while others have received no approval. A few benzodiazepine products have been discontinued over time. Let us take a look.

Are There Differences Between Benzodiazepines?

While the general mechanism of action of benzodiazepines is the same, the specific ways they affect certain GABA-A receptor subtypes vary. Benzodiazepines have different onset times, durations of action, and most often prescribed uses.

Certain benzodiazepines have higher potencies or last longer than others. The table enlists the commonly used BZD based on their duration of action, strength, and elimination half-life.

What Are The Advantages Of Benzodiazepines?

Benzodiazepines have many advantages.

• Well-known history: Benzodiazepines have been extensively studied and understood since the 1960s.
• Safer than their antecedents: Before the advent of benzodiazepines, doctors typically recommended barbiturates to alleviate anxiety. Yet, these medications had a high risk of complications and side effects. While looking for a substitute for barbiturates, Polish-American scientist Leo Sternbach unintentionally found the first Benzodiazepine-chlordiazepoxide.
• Treat different conditions: Treatment with benzodiazepines is effective for many diseases, some of which are likely to occur together. An example is the frequent necessity for pre-anesthesia sedation and pre-surgery anxiety, both of which can be treated with benzodiazepines like Midazolam or Diazepam.
• There is a single antidote for every one of them: There is a chance of overdosing on benzodiazepines. Flumazenil, however, is an antidote that effectively undoes the effects of all benzodiazepines.

What Are the Disadvantages Of Benzodiazepines?

Benzodiazepines are effective, although they have some significant drawbacks.

• There is a potential for abuse: Misuse of benzodiazepines is common. Experts estimate that between 2014 and 2015, at least five million Americans abused benzodiazepines.
• Habit forming:Long-term or improper usage of these drugs may result in benzodiazepine use disorder.
• Overdose is a possibility: Misusing benzodiazepines carries a risk of overdose, which can cause respiratory problems.
• Alcohol and some substances may interact with BZD in a harmful way: Alcohol and drugs like opioid painkillers (like oxycodone or hydrocodone) can also interact with benzodiazepines. These interactions can make the effects of the medications or alcohol more severe, which may have fatal consequences.
• Benzo's Dependence: Even when taken as directed, benzodiazepines can cause dependence. As a result, withdrawal symptoms may appear on abruptly stopping or reducing the drug after becoming physiologically dependent on BZD.
• Potential for use in sexual assault: An example of this is flunitrazepam, sometimes referred to as Rohypnol. Sexual assaulters utilize this substance because it sedates them and hinders the production of new memories. Yet, the criminals involved in these crimes also use Clonazepam and diazepam, among other benzodiazepines.
• Slow down nerve signals: Nerve signal delays might make it difficult or impossible to drive or perform other jobs safely.
• Controlled substances: These medications are frequently under observation and may even be restricted depending on the regulations.

Possible Side Effects Of Benzodiazepine

Side effects are undesirable effects produced after taking the drug. Depending on the medicine, the effects could vary slightly. Also, each person's response to medication varies, so you could or might not have these side effects. Here are some common and severe side effects of BZD:

Precautions Of Benzodiazepines

Precautions are cautionary measures to ensure the safe use of the drug. It is necessary to prevent undesirable events.

• Follow the consumption of these medications as directed.
• Discuss your medication history with your physician before starting BZD.
• Use the lowest effective dose and only take the prescribed medication as directed by your doctor or pharmacist.
• Take the missed dose of this medication as soon as you remember.
• Herbal supplements, grapefruit, and several benzodiazepines can interact significantly.
• Keep away from alcohol when using BZD. Some drugs and alcohol can combine, leading to potentially harmful side effects or issues.
• Benzodiazepines enter the breast milk and can result in lethargy and weight loss in the baby.
• Avoid using them if you are breastfeeding.
• Older people may get drowsy, lightheaded, clumsy, unsteady, or less alert than usual when taking this medication.
• Properly stop using benzodiazepines. If symptoms arise on stopping the medication, speak with your doctor.

Overdosing

Benzodiazepine overdose-related deaths are uncommon. Combining benzodiazepines and other CNS depressants like alcohol and opioids increases the risk of fatal overdose.

An overdose of benzodiazepines may cause:

• Excessive Drowsiness or Sedation
• Incredibly Slow Breathing
• Slurred Speech
• Loss Of Muscle Control,
• Confusion
• Difficulties Thinking
• Coma

Flumazenil reverses the sedative effect of benzodiazepines when used for medical procedures and for treating overdoses.

Misuse And Withdrawal Symptoms Of Benzodiazepine

Misuse of benzodiazepines is a concern. Some individuals use these medicines recreationally without the guidance of a medical practitioner, which can be unsafe. In certain patients, physical dependence on benzodiazepines can develop even after a brief course of treatment or after chronic therapeutic dosage use.

You can have withdrawal symptoms if you suddenly stop using certain medications. These symptoms include-

• Difficulty concentrating
• Trouble sleeping
• Irritability
• Increased tension and anxiety
• Panic attacks
• Hand tremor
• vomiting and dry heaving
• Palpitations
• Headache
• Painful and tight muscles
• Perceptional changes

The quantity and length of benzodiazepine use affect the severity of the withdrawal symptoms. Withdrawal symptoms might be fatal.

Dangers Of Addictions

Even if you take benzodiazepines as directed by your doctor or other healthcare providers, you have the risk of developing an addiction to them since they are habit-forming in nature. People who have previously used drugs or alcohol are more prone to get addicted.

Some medicines can cause tolerance if used repeatedly over an extended period,i.e., you will require higher doses of the medication to treat your disease.

Drug abusers use these substances to feel "high." They have the same potential for addiction as opioids, cannabis, and the club drug GHB (gamma-hydroxybutyrate). Young teenagers and adults who abuse them frequently crush the pills, snort them or consume the tablets to get high.

Some warning signs and symptoms of addiction include:

• Difficulty sleeping
• Diarrhea
• Vomiting
• Nausea
• Goosebumps
• Irregular leg movements
• Muscle and bone pain

Drug Interactions Of Benzodiazepine

A person must inform their doctor of all other medications before beginning benzodiazepines. Some drugs may enhance the effects of benzodiazepines, while others may diminish them.

• The use of benzodiazepines and opioids together might cause fatal respiratory depression, coma, and other serious side effects.
• Antacids can reduce benzodiazepine absorption and concentration in blood.
• Proton pump inhibitors may increase the number of benzodiazepines in your blood by interfering with the liver enzymes that detoxify them from your body.
• Concurrent use of benzodiazepines with alcohol or other medications may impair the central nervous system. Alcohol can intensify adverse effects like sleepiness and raises the possibility of an unintentional overdose.

Bottom Line From Practical Anxiety Solutions

Benzodiazepines, often called benzos, are central nervous system (CNS) depressants often prescribed for mild to moderate anxiety disorders such as panic and sleep disorders. Short-term use of benzos is generally safe and does not have adverse effects when prescribed.

Although all benzodiazepines have a similar effect on the brain, the side effects might vary depending on the type, dose, and duration of treatment. Although these drugs can treat various conditions and benefit millions of people, there are risks.

Do not abruptly cease using benzodiazepines to avoid potentially fatal withdrawal symptoms. If you have any questions on the safe use of benzodiazepines, consult a medical expert.