What is Zolpidem Tartrate?

Zolpidem (Zolpidem tartrate) is a sedative; a hypnotic that works on the chemicals in the brain that causes insomnia or the inability to sleep. There are immediate-release Zolpidem preparations and extended-release preparations. The former will help a person fall asleep. The latter is made up of two layers. The first layer dissolves quickly to help a person fall asleep and the second layer dissolves more slowly to help a person stay asleep.

Zolpidem is available through prescription. The prescribing physician will be the one to determine which type (immediate or extended release) is more appropriate for any particular patient.

Brief History of Zolpidem

Zolpidem tartrate was originally discovered in the early 1980s in France by Laboratoires d’Etudes et de Recherches Synthélabo, today’s Sanofi-Aventis. They were looking to develop a hypnotic agent with potential benefits over benzodiazepines. These desired benefits include:

  • Fast but short duration of action
  • No active metabolites

Their scientists worked with a group of imidazopyridines that demonstrated hypnotic activity when used on laboratory animals. From this group of chemicals, zolpidem was the one to combine the beneficial properties the scientists were looking for. Further research showed that zolpidem caused the number of awakenings and total wake time to be reduced, without any significant modification to REMs and slow wave sleep. They introduced the drug in France as a treatment for insomnia. It made its way into the USA as Ambien® the original brand approved by the U.S. FDA in 1992. Generic Ambien became available in 2007.

Brand Names for Zolpidem

  • Ambien®
  • Ambien CR®
  • Edluar®
  • Zolpimist®
  • Intermezzo®

Street Names for Zolpidem

  • A-minus
  • No-Go pills
  • Sleep-Easy
  • Tic-Tacs
  • Zombie Pills

Zolpidem Drug Type

Zolpidem is a sedative, aka central nervous system depressant, downer or tranquilizer. It slows down brain activity, effectively inducing sleep or a deep state of relaxation. Depressants, in general, are prescribed for anxiety and sleep disorders. Other substances of the same type include:

DEA Drug Class

Zolpidem is listed in the Controlled Substances Act under Schedule IV. Drugs, substances or chemicals under Schedule IV:2

  • have current medical application in the U.S.;
  • have a low potential for abuse;
  • may cause limited physical or psychological dependence.

Other Schedule IV drugs include:3

  • Acetaminophen
  • Alprazolam (Xanax)
  • Chlordiazepoxide (Librium)
  • Diazepam (Valium)
  • Lorazepam (Ativan)
  • Naloxone/Pentazocine
  • Oxazepam
  • Phentermine (Ionamin)
  • Tramadol

Forms and Routes of Administration4

  • Tablets – Zolpidem 5mg tablets are to be taken orally once a day right before bedtime. The maximum dose is 10mg/day.
  • Sublingual tablets – These 5mg tablets are to be dissolved under the tongue once a day right before bedtime, with at least 7-8 hours remaining before one needs to wake up in the morning. If the initial 5mg is insufficient, the dose can be increased up to 10mg. This form is NOT to be swallowed or taken with water.
  • Spray – One oral spray of Zolpidem delivers 5mg of the drug and is used once daily right before bedtime.

Uses for Zolpidem

Zolpidem was FDA approved for the short-term management of insomnia cases but it has also found therapeutic uses for the following:

  • Restless Leg Syndrome
  • Catatonia
  • Parkinson’s Disease (for improvement of motor symptoms)

Zolpidem and Pregnancy5

This drug can harm an unborn fetus. Most doctors discourage using Zolpidem during pregnancy. If you are pregnant or planning on becoming pregnant it is best to inform your doctor before taking a prescription for Zolpidem.

The same is true for nursing moms. Zolpidem can be passed into breast milk so your doctor should be aware of this fact. Zolpidem has also not been proven safe or effective in children under 18.

Zolpidem and Alcohol

Zolpidem and alcohol do not mix. Alcohol only worsens the drug’s side effects like drowsiness and abnormal behaviors/thoughts. Zolpidem is supposed to be taken just prior to bedtime, so people who have taken Zolpidem are advised not to engage in activities that require coordination or mental alertness, like driving or operating machinery.

Short & Long Term Effects of Zolpidem4

Some people may be allergic to Zolpidem. Allergic reactions can sometimes be severe and should be reported to a doctor immediately. These include:

  • Difficulty breathing (shortness of breath)
  • Chest pain
  • Fast or irregular heartbeat
  • Hives
  • Swelling of face, throat, lips and tongue

Other common side effects after taking Zolpidem include:

  • Constipation/diarrhea, upset stomach
  • Dizziness
  • Drowsiness during the day
  • Dry mouth
  • Headache
  • Lightheadedness (like you might pass out)
  • Loss of coordination
  • muscle pain
  • Nausea
  • Stuffy nose/nose and throat irritation
  • Weakness/feeling tired

Other serious long-term effects include:

  • Aggression
  • Agitation
  • Anxiety
  • Changes in personality
  • Confusion
  • Decreased inhibitions
  • Depression
  • Hallucination
  • Memory problems
  • No fear of danger
  • Risk-taking behavior
  • Self-harm or Suicidal thoughts
  • Unusual thoughts

Zolpidem Abuse & Addiction6

This drug can be habit forming and addictive so it is generally prescribed only for a short period, like a few weeks. When misused or abused by taking more than the prescribed dose, Zolpidem can result in a high, giving the user hallucinations. Symptoms of Zolpidem addiction include:

  • Bloodshot eyes
  • Changes in appetite
  • Diarrhea
  • Headaches
  • Heartburn
  • Loss of coordination
  • Muscle and joint pains
  • Shakiness/unsteadiness
  • stomach pain

Zolpidem Withdrawal

People who have been taking Zolpidem for extended periods can develop a dependence on the drug. They are advised not to quit cold-turkey without medical supervision. Withdrawal symptoms include:

  • Agitation/Irritability
  • Cravings
  • Delirium
  • Nervousness
  • Rebound insomnia
  • Seizures

Zolpidem Overdose

Taking too much of this drug can lead to:

  • Extreme drowsiness
  • Weakened breathing
  • Weakened heart function
  • Coma
  • Death

If you think you may have taken too much, or believe a family member may have overdosed on Zolpidem, seek emergency medical help.

Types of Testing for Zolpidem Use

Several factors affect how long Zolpidem stays in the system, namely age, body mass, recent food and fluid intake, organ function, metabolic rate, dosage and frequency of use. While it is not likely to be detected in a routine drug screening, testing for Zolpidem can be done by any of 4 methods:

Urine Testing

Urine drug tests are commonly used to test for Zolpidem. Zolpidem phenyl-4-carboxylic acid (ZPCA) is the most common metabolite of Ambien®. It may remain detectable in urine for up to 72 hours from the time of use.

Blood Testing

This method is rarely used because of the short window of time that the drug stays in the bloodstream, but the test is available if/when necessary like for cases when Ambien-use is suspected of a hospitalized patient/accident victim.

Hair Testing

Hair follicle drug tests can be useful for those seeking to establish long-term Zolpidem use. Typically, 1.5inches of hair sample will be required to do this test.

Saliva Testing

The quickest way to test for Ambien® is to perform a saliva drug test because it can be detected in oral fluids in as little as 15 minutes after intake, and may remain traceable up to 8 hours after use. Saliva testing is favored in some cases because sample collection is easy and non-invasive.

Screening Cut-off and Detection Time for Zolpidem

In drug testing, the cut-off level marks the point at which a drug metabolite is detected without a doubt that it might be a false positive. A negative result does not mean the sample is drug-free, only that the concentration level may be too low that it falls below the established cut-off.

Specimen

Concentration Cut-off Level

Detection Time

Urine

300 ng/ml  

 Up to 72 hours


Sources:

1 http://www.emedexpert.com/facts/zolpidem-facts.shtml

2 https://www.dea.gov/druginfo/ds.shtml

 3https://www.pharmacy.umaryland.edu/media/SOP/medmanagementumarylandedu/ControlledSubstanceList.pdf

4 https://www.drugs.com/zolpidem.html

5 https://www.everydayhealth.com/drugs/zolpidem

6 https://www.therecoveryvillage.com/ambien-addiction/faq/how-long-does-ambien-stay-in-system/#gref

For Further Reading:

https://casapalmera.com/top-8-drug-categories/

http://www.treatment4addiction.com/drugs/society/csa/



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