Benzodiazepine Drug Information

 

Benzodiazepines are widely used for a variety of conditions including anxiety and insomnia, but also for muscle tightness, pre-surgical sedation, detoxification from alcohol and the anxiety experienced with cardiovascular or gastrointestinal conditions.

Benzodiazepines primary mode of action is on GABA (gamma-aminobutryic acid), the most common receptor in the nervous system. GABA is a neurotransmitter that is the cornerstone of the inhibitory (calming) system of the body, and controls the action of epinephrine, norepinephrine and dopamine.  The main function of GABA is to prevent anxiety and stress-related messages from reaching the motor centers of the brain. They regulate excitability, including the seizure threshold. The brain must balance the excitatory and calming influences. Excessive excitation can lead to seizures, insomnia, anxiety and other clinical conditions; whereas excessive inhibition results in incoordination, sedation and anesthesia.

Benzodiazepines, barbiturates and alcohol all act on GABA, and chronic use down-regulates and modify the GABA receptors, which in turn causes dependence. With continued use of Benzodiazepines, the calming effect of GABA is diminished while the excitatory neurotransmitter Glutamate, is increased. Glutamate is always an excitatory neurotransmitter, and GABA is what counters this action. As GABA is initially enhanced by Benzodiazepines, the brain’s output of excitatory neurotransmitters, including Norepinephrine (noradrenalin), Serotonin, Acetyl Choline and Dopamine are reduced. These neurotransmitters are necessary for alertness, muscle tone, coordination, memory, emotional responses, endocrine gland hormones, heart rate, blood pressure control and other functions. As a result, all these may be impaired by Benzodiazepines.

Additional receptors for Benzodiazepines (non-GABA) are located in the colon, kidney, blood cells and adrenal cortex, and therefore may also be affected by Benzodiazepines.  These actions are responsible for the well-known side effects and adverse reactions.

As the primary inhibitory neurotransmitter, GABA filters out irrelevant messages by terminating the excitatory glutamate, epinephrine and norepinephrine. GABA is viewed as the ‘braking system’ among neurotransmitters and it is estimated that about 40% of the synapses in the human brain work with GABA. GABA also enhances alpha wave production to promote relaxation and moderate occasional stress and supports immune health. It has been shown that T-cells (white blood cells critical to the immune system), are inhibited by GABA, and GABA has been shown to inhibit the response to foreign antigens. This suggests that the immune system needs GABA to function properly. This may explain why it is common to have frequent infections and a compromised immune system after long-term use of Benzodiazepines, or in the withdrawal process.

In situations of high stress or excitement, the brain responds with an increase in GABA production. Under normal situations, our levels of GABA are sufficient to maintain control of the excitatory stimuli. GABA’s high concentration in the hypothalamus suggests it plays a critical role in both hypothalamus and pituitary function. The hypothalamus is a region of the brain that is the regulating center for instinctive functions such as sleep cycles, body temperature, and the pituitary gland is the master endocrine gland affecting all hormone functions of the body.

The GABA receptor allows more chloride ions to enter the brain cell, thus working to maintain the electrical charge within the cells. Benzodiazepines work by increasing the effectiveness of GABA in the chloride opening so the chloride ion cells to allow more chloride to enter the nerves. Caffeine does the opposite and inhibits the property of GABA.   Therefore Benzodiazepines work as a tranquilizer and caffeine as a stimulant. Benzodiazepines act as a booster to the actions of GABA, and allow more chloride ions to enter the neuron. This in turn makes the nerve more resistant to excitation.

The Calcium-Channel activity is also increased by Benzodiazepines. Calcium-channels are located in the central nervous system, but also are located in excitable cells including in the muscle, nerve cells and in the Glial cells that form myelin to protect the nerve endings, and provide support and protection for the brain’s nerve cells. There is roughly one Glial for every neuron in the gray matter of the brain. Prolonged use of benzodiazepines result in adaptation of the receptors that may increase in number and/or their sensitivity to GABA. A larger dose of the Benzodiazepine may be needed to produce the same calming effect. This phenomenon is known as ‘tolerance’. Additionally, upregulated Calcium Channels are linked to an increase in neuropathy pain. Withdrawal of the drug can result in the receptor becoming hypoactive, producing symptoms worse than what the patient originally sought treatment for. If Benzodiazepines are suddenly stopped or reduced too rapidly, the calcium floods into the cell. This can cause intense withdrawal symptoms and be life-threatening due to the seizure risk.

Additionally, prolonged exposure to Benzodiazepines measurably increase accumulation of intracellular calcium that over-excites the neurons and increases anxiety, muscle tension, insomnia and many other symptoms associated with tolerance and withdrawal.

When the GABA is no longer capable of opening the chloride ion channels, the cells become overly excited. This cellular hyper-excitability is responsible for the insomnia, irritability, tachycardia, hypertension, hallucinations and seizures from the abrupt cessation of long-term alcohol use and also benzodiazepines. 

Alcohol has a similar effect to benzodiazepines, increasing the release of chloride back into the neurons. This is the major way in which alcohol affects the brain. Tolerance to alcohol and benzodiazepines is the receptor adapting to the drug by increasing the number of receptors so more of the drug is needed to have the effect. The receptors become hypoactive by the drug being withdrawn, which enhances the symptoms that the drug was intended to treat.

Benzodiazepine withdrawal is far more involved than alcohol, heroin, methamphetamine or even opiates. Yet 112.8 million prescriptions were filled in 2008, with the majority prescribed by primary care physicians. They remain among the most frequently recommended medication.

Benzodiazepines can be extremely habit-forming and long-term use is not recommended (longer than 14 consecutive days).

    Side Effects May Include: Confusion, Depression, Headache, Slurred Speech, Tremor, Vertigo, Blurred or Double Vision, Dizziness, Stimulation, Restlessness, Anxiety, Agitation, Aggressiveness, Irritability, Rage, Akathasia, Tiredness / Sleepiness, Increased Salivation, Rigidity, Nasal Congestion, Weight loss or Weight Gain, Nausea, Stomach Upset, Constipation or Diarrhea, Insomnia, Tachycardia / Palpitations, Hypertension, Memory Impairment, Abnormal Involuntary Movement, Muscular Twitching, Change in Libido, Weakness, Talkativeness, Muscle Tone Disorders, Upper Respiratory Infections, Sweating, Menstrual Disorders, Edema, Infection, Fear

    Benzodiazepine Drug Names Include
    - Alprazolam (Xanax, Xanor, Kalma, Tafil, Alprox, Frontal)
    - Bromazepam (Bromam, Compendium, Creosedin, Calmepam, Durazanil, Lectopam, Lexaurin, Lexilium, Lexomil, Lexotan, Lexotanil, Normoc, Novepam, Somalium)
    - Chlordiazepoxide (Librium, Tropium, Risolid, Klopoxid)
    - Cinolazepam (Gerodorm)
    - Clobazam (Frisium)
    - Clonazepam (Klonopin, Klonapin, Rivotril, Rivatril)
    - Clorazepate (Tranxene)
    - Cloxazolam (Olcadil, Sepazon)
    - Diazepam (Valium, Apzepam, Stesolid, Vival, Apozepam, Hexalid, Valaxona, Ducene, Antenex)
    - Estazolam (ProSom)
    - Flurazepam (Dalmane, Dalmadorm)
    - Flunitrazepam (Rohypnol, Fluscand, Flunipam, Hynodorm, Ronal, Rohydorm)
    - Halazepam (Paxipam)
    - Ketazolam (Anseren, Ansieten, Ansietil, Marcen, Sedatival, Sedotime, Solatran, Unakalm)
    - Loprazolam (Dormonoct)
    - Lorazepam (Ativan, Temesta, Lorabenz)
    - Lormetazepam (Loramet, Nictamid, Pronoctan, Ergocalm, Dilamet, Sedaben, Stilaze, Nocton, Noctamid, Noctamide, Loretam, Minias, Methyllorazepam)
    - Meprobamate (Meprospan , Miltown, Equanil)
    - Midazolam (Versed, Hypnovel, Dormicum)
    - Nitrazepam (Mogadon, Alodorm Pacisyn, Dumolid)
    - Nordazepam (Calmday, Stilny, Madar, Vegesan, Desoxydemoxepam, Nordiazepam, Desmethyldiazepam)
    - Oxazepam (Serax, Seresta, Serenid, Sobril, Oxascand, Alopam, Oxabenz, Oxapax, Murelax, Alepam)
    - Quazepam (Doral)
    - Temazepam (Restoril, Normison, Euhypnos, Temaze, Temtabs, Remestan, Tenox, Norkotral)
    - Triazolam (Halcion, Rilamir)

    Anxiolytic Drug Information:Anxiolytics are medications used for the treatment of anxiety. Currently the two main categories are Azapirone, which only includes Buspirone; and Benzodiazepines, which are among the top 100 most commonly prescribed medications. Often Anxiety Medications are prescribed for insomnia.

    There is mixed evidence on using Azapirones for the treatment of anxiety disorders. They are commonly employed as an augment to antidepressant therapy and are occasionally used as an antipsychotic agent. Its anti-anxiety action is believed to work through its action on Serotonin.  Buspirone is often used to enhance the activity of SSRIs but is not used as an antidepressant alone. But there are warnings against combining multiple Serotonin-inducing agents due to the risk of Serotonin Syndrome, a potentially life-threatening condition. Symptoms of the Serotonin Syndrome may include mental changes such as irritability, altered consciousness, confusion, hallucinations, and coma; shivering, heart irregularities, tremor, rigidity and gastrointestinal symptoms such as cramping, nausea, vomiting or diarrhea.

    Azapirone Drug Names:
    - Buspirone (BuSpar, Ansiced, Ansial, Anxiron, Bespar, Buspimen, Buspirone, Buspinol, Buspisal, Narol, Spitomin, Sorbon)

    Side Effects May Include: dizziness, nervousness, nausea, numbness, headache, weakness, lightheadedness, excitement                    


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Disclaimer: *While great care has been taken in organizing and presenting the material throughout this website, please note that it is provided for informational purposes only and should not be taken as Medical Advice. More...
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*Because these drugs can cause severe withdrawal reactions, do not stop taking any medication without first consulting your physician. The decision to quit any mediction should be discussed with your doctor and with their consent and support .More...

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    Side Effects / Withdrawal Information by Drug Name

      A
      Adapin Adderall Adeprim
      Agedal Alodorm Alepam
      Aldosomnil Alpidem Alprazolam
      Ambien Amineptine Amphetamine
      Amitriptyline Amitriptylinoxide Amoxapine
      Anafranil Anxiron Aponal
      Aropax Asendin Ativan
      Atomoxetine Avanza Aventyl
      B
      Benmoxin Belsomra Bespar
      Bolvidon Bromam Bromazepam
      Bupropion Buspar Buspimen
      Buspinol Buspirone Buspisal
      1. Butriptyline  

      1. C
      2. Calmday Celexa Centrax
        Centroton Chantix Chlordiazepoxide
        Clobazam Clomipramine Clonazepam
        Clorazepate Cloxazolam Cipralex
        Cipramil Cinolazepam Citalopram
        Citox Coaxil Compendium
        Concerta Creosedin Cymbalta
        Cylert
      D
      Dalcipran Dalmadorm Dalmane
      Dapoxetine Davedax Daytrana
      Demexiptiline Deptran Desipramine
      Desyrel Desoxyn Desvenlafaxine
      Dexedrine Dimetacrine Dexmethylphenidate
      Diazepam Dibenzepin Difemetorex
      Doral Dormicum Dormonoct
      Doxepin Dosulepin Duloxetine
    E
    Edronax Effexor Elavil
    Emovit Enact Escitalopram
    Esertia Estazolam Eszopiclone
    Etrafon Euhypnos  
    F
    Fecamfamine Fevarin Fluctan
    Fluoxetine Flunitrazepam Flurazepam
    Fluvoxamine Focalin Fontex
    Frisium Frontal  

    G

    Gabapentin Gamanil Gerodorm
    H
    Halazepam Halcion Havlane
      Hypnovel  
    I
    Imipramine Imipraminoxide Imovane
    Iproclozide Iproniazid Isocarboxazid
    K
    Kalma Klonopin  
    L
    Lamictal Leftamine Lexapro
    Lexaprin Lexomil Lexotan
    Lexotanil Librium Lisdexamfetamine
    Lofepramine Lorabenz Loramet
    Loprazolam Lorazepam Lormetazepam
    Ludiomil Lunesta Lustral
    Luvox    
    M
    Maneon Maprotiline Mazindol
    Mebanazine Meprobamate Meprospan
    Metadate Metapramine Methamphetamine
    Methyphenidate Melitracen Mianserin
    Midazolam Milnacipran Mirtabene
    Mirtaz Mirtazapine Mirtazon
    Moclobemide Mogadon  
    N
    Neurontin Nialamide Nitrazepam
    Nordazepam Nortriptyline Nitroxazepine
    Norebox Norpramin Normison
    Norval Noxibel Noxiptiline
         
    O
    Octamoxin Oxazepam  
    P
    Pamelor Paroxetine Paxil
    Paxipam Pemoline Pertofrane
    Pexeva Pertofraneis Phenelzine
    Prazepam Pristiq Propizepine
    Pipofezine Pipradrol Prolift
    Prolintane Promotil Promyrtil
    Pronoctan ProSom Prothiaden
    Protriptyline Prozac Pyrovalerone
    Q
    Quazepam Quinupramine  
    R
    Ramelteon Reboxetine Remergil
    Remergon Remeron Restoril
    Rexer Ritalin Rivotril
    Rohypnol Rozerem  
    S
    Safrazine Savella Selegiline
    Serafem Serax Seromex
    Seronil Seropram Seroxat
    Sertraline Setiptiline Sobril
    Silenor Sinequan Sinquan
    Sintamil Sipralexa Solvex
    Sonata Sonin Stablon
    Stesolid Strattera Surmontil
    Saphris
    T
    Tafil Temazepam Temesta
    Thombran Tofranil Tianeptine
    Tranylcpromine Tranxene Trazodone
    Trialodine Triavil Triazolam
    Trimipramine Trittico Tryptizol
       
    V
    Valaxona Valium Venlafaxine
    Vestra Versed Viloxazine
    Vivactil Vival Vyvanse
    Viibryd    
    W
    Wellbutrin
    X
    Xanax Xanor Xeristar
    Y
    Yentreve
    Z
    Zalepn Zispin Zoloft
    Zolpidem Zopiclone Zyban





 

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