Anxiety Medications, Sleeping Pills, Antihistamines and Over-the-Counter Sleep Aids Drug Information

 

 

 

 

 

The use of sleeping pills, benzodiazepines and antihistamines has soared, even though each class contains warnings against extended use (longer than 7-14 days). Even over-the-counter medication can cause cognitive impairment, delirium and excessive daytime sedation, a particular concern for the elderly.

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.

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

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.








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

Benzodiazepines
- 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)

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                       

    Sleeping Pills (non-benzodiazepines)
    - Zopiclone (Lunesta)
    - Zalepn (Sonata)
    - Zolpidem (Ambien)
    - Alpidem

    Sleeping pills are classified as sedative hypnotics and work on receptors in the brain to slow down the nervous system to induce and maintain sleep.  The newer medications do have a different chemical structure from a benzodiazepine, but they act more specifically in the same area of the brain on the Gamma-aminobutyric acid receptors (GABA). Therefore the hypnotic effects are similar to benzodiazepines even though sleeping pills are molecularly distinct.  The term non-benzodiazepines was given to these new classes of sleeping pills, making many believe they will not experience dependence. But the warnings from the manufactures of zolpidem (Ambien) state, “Complex behaviors such as somnambulism, including driving or eating while not fully awake, with amnesia for the event, as well as abnormal behaviors such as being more outgoing or aggressive than normal, confusion, agitation and hallucinations may occur.” Continuous use is not recommended for more than 7--14 days. Similar warnings appear for all sleeping pills.

    A trial performed by Dr. J.F. Pagel, a sleep physician at the University of Colorado Medical School, indicated that bizarre actions being committed while on sleeping pills are very prevalent.  There have been 4 cases of murder in which the defendant was found not guilty due to a blackout and subsequent amnesia while on sleeping pills. 

    Rebound insomnia is the inability to sleep that occurs following the discontinuation of sleeping pills. Regular use of these substances can cause dependence and when the medication is stopped, the rebound insomnia can be worse than the sleep issues the drug was intended to treat.

    Sleeping pills are considered to have less potential for addiction than benzodiazepines, but evidence is mounting that they share the same side effects and dependence tendency.  

    Side Effects May Include: Memory loss, Behavioral changes including less inhibition or aggressiveness, Abnormal thinking, Night eating or driving with amnesia, Loss of concentration, Depression, Manic reactions, Suicidal thoughts, Loss of identity, Hypertension, Tachycardia, Angina, Sudden falls, Heart attacks, Confusion, Agitation, Sleepiness, Poor coordination, Dizziness, Insomnia, Excessive sleepiness, Anxiety, Gastrointestinal issues, Headaches

    Melatonin Receptor Agonist Hypnotic:
    - Ramelteon (Rozerem)

    Ramelteon mimics the sleep regulation hormone melatonin. It is used for sleep onset problems and is not effective for difficult staying asleep. Ramelteon is a short-acting drug that clears the body within an hour or two and in trials the most common side effects were fatigue, sluggishness and dizziness. Whether it will prove to be safe and effective is still uncertain.

    Because of the insufficient information and trials, Ramelteon is not recommended for pregnant women, nursing mothers or children. Certain medications, including fluvoxamine (antidepressant), compete with Ramelteon to bind the enzymes in the liver that break the drug down. This will slow the clearance and elimination from the body and increase the risk of side effects.  Those with liver disease should not take Ramelteon and alcohol should not be combined or hallucinations, depression, irritability and confusion may occur.


    Antihistamines & Over-the-Counter Sleep Aids:

    The use of sleeping pills, benzodiazepines and antihistamines has soared but none are recommended for extended use (longer than 7-14 days). Even over-the-counter medication can cause cognitive impairment, delirium and excessive daytime sedation, a particular concern for the elderly. The most common type of sleeping medication are those found in almost all over-the-counter sleep aids – Antihistamines.

    Insomnia is a common complaint that affects about 30% of public. Prescription sleeping pills and anxiety medications are often prescribed. However, the FDA also permits over-the-counter sleep aids if they contain one of these three types of antihistamines:
    - diphenhydramine hydrocholorida
    - diphenhydramine citrate
    - doxylamine succinate

    Most common brands include:
    Diphenhydramine (Benedryl, Simply Sleep, SleepGels, Sleepinal, Sominex, Hytol, Advil PM), Doxylamine (Unisom, SleepTabs)

    Antihistamines work against Histamine, the central nervous system chemical. Histamine is the neurotransmitter your body produces when you are having an allergic reaction. Although there is always some histamine in the body, a bee sting or mosquito bite (for example) can cause your body to release more histamine in the area of the bite, making the skin read and itchy. Histamines also have an important role in the immune system, where as a neurotransmitter it helps to defend against viruses, bacteria and other foreign invaders.

    The Pain Connection

    Taking antihistamines is one of the most common causes of dehydration and an indication of too little moisture in the body is pain.

    Our brain, working nonstop, requires more water than any other part of the body. Under normal conditions it contains about 20% of all the blood that circulates through the body, and it is estimated that brain cells consist of 85% water. Antihistamines, diuretics, alcohol, blood pressure medications and some psychiatric drugs cause dehydration. In response to the water shortage, the brain activates and stores the important neurotransmitter histamine, which immediate redirects water to areas where it is needed for basic metabolic activity and survival.  When histamine and the regulators for water intake come across pain-sensing nerves in the body, they cause strong and continual pain. These pain signals are necessary to alert the person to attend to the dehydration.

    During normal movement of a joint, a minimal amount of cartilage cells are destroyed from friction, but are replaced without issue. When the body is dehydrated, cartilage loses the ability to glide smoothly and the additional friction causes an increased number of cartilage cells to be destroyed.  Cartilage cells typically receive water and nutrients from the blood that flows through the end of the underlying bone. However, damage to the cartilage must rely on an increased flow of blood to the joint capsule that causes inflammation and pain. Lack of water not only increases the damage to cartilage, but prevents the healing.

    The spine supports the weight of the upper body and about 75% of the support comes from the water within the spinal discs that sit between each vertebra. When the body is dehydrated, these discs contain less water and shrink in size. This renders them less capable of providing the necessary support that results in an increased risk of nerve impingement. Additional strain on the musculature that supports the spine causes an increased risk of disc herniation.

    Dehydration is a primary cause of insomnia and fatigue. Water is also our internal cooling and temperature balancing system and dehydration can lead to an increase of toxins in the bloodstream. This can cause an imbalance that becomes more noticeable at night. Drinking water throughout the day helps to flush toxins out of the body.

    Side Effects May Include: Blurred Vision, Constipation, Urinary retention, Dizziness, Forgetfulness, Lack of Coordination, Continual dry throat and mouth, Difficulty Sleep, Drowsiness, Urinary retention, Heart rate changes, Low blood pressure, Muscle weakness, Vomiting and nausea, Restlessness, Irritability


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*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...

*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...

Quick Reference


Azapirone - names include (Buspirone, Buspar) More...

Benzodiazepines - common names include (Ativan, Alprazolam, Xanax, Clonazepam, Diazepam, Valium, Lorazepam) More...

  1. Sleeping Pills (Non Benzodiazepines) - common names include (Ambien, Lunesta) More...

  1. Melatonin Receptor Agonist Hypnotic - common names include (Rozeram) More...

Antihistamines - common names include (Benedryl, Unisom, Advil PM) More...

  1. Over-the-Counter Sleep Aids - common names include (Tylenol PM) More...

    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 Bespar Bolvidon
      Bromam Bromazepam Bupropion
      Buspar Buspimen Buspinol
      Buspirone Buspisal Butriptyline

      1. C
      2. Calmday Celexa Centrax
        Centroton Chlordiazepoxide Clobazam
        Clomipramine Clonazepam Clorazepate
        Cloxazolam Cipralex Cipramil
        Cinolazepam Citalopram Citox
        Coaxil Compendium Concerta
        Creosedin Cylert Cymbalta
      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
    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 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 Zopliclone Zyban





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*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...

*Because these drugs can cause severe withdrawal reactions, do not stop taking any medication without first consulting your physician. The decision to quit any medication should be discussed with your doctor and with their consent and support. More...