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Transcript of Ambien
Use and Abuse
Drug History and Regulation
Brand name Ambien has been available to consumers in the U.S. since 1991 when clinical trials were completed
1971 it was officially characterized by WHO as a Schedule IV drug that can produce dependence
Absorbed quickly from the GI tract and expelled rapidly via the kidneys
Peak concentration occurs after 1.6 hours
5mg = 59ng/mL
10mg = 121ng/ml
Mean elimination time:
5mg = 2.6 hrs
10mg = 2.5 hrs
Normal therapeutic dose is 5-10mg (5 recommended for elderly patients)
Binds to the - GABA-A benzodiazepine receptor complex and binds with high affinity to the alpha 1 & 5 subunits.
Potential trigger for dependence
Does not interfere with deep (slow wave) sleep
92.5% protein binding
Does not accumulate
Young adults 20mg nightly for two weeks
Prescribed for treatment of insomnia
Also used as a anticonvulsant and anxiolytic
Typical dosage prescribed is 5-10 mg
Usually not prescribed for more than 2 weeks of use
9.1% of individuals 18 and older have abused sedatives
Abuse in elevated dosages
Larger doses cause euphoria and exaltation
Abusers rely on its anxiolytic and stimulating action to cope with everyday activities
Often abused in concurrence with alcohol
Likelihood of abuse ranked as 35 out of 100.
Half a million people in the U.S. are currently using Ambien or other hypnotics
Ambien is most commonly prescribed
Quickly becoming the most commonly used date-rape drug
Generic forms (13 forms) have been available since 2007
Tapering off dosage gradually
Should NOT quite medication all at once
Withdrawal seizures caused by over excitation
Withdrawal Side Effects
Withdrawal symptoms are worse if the drug is stopped suddenly
Shares pharmokinetic properties with benzodiazepines
Average users: 64 years old, female
Classified as a non-benzodiazepine hypnotic of the imidazopyridine class
6 male, 5 female (11 total) aged 21-35
DSM-IV non-drug dependent individuals
No family history of alcoholism, neurological disorder, and not on any current medications
Had to show they could handle an acute high (20mg) dose of Zolpidem w/o vomiting or nausea
Subjects given either 0, 5, 10, or 20 mg Zolpidem
• Assessed (via questionaire) feelings similar to: stimulants, sedatives, amphetamine, euphoric, or psychotomimetic (LSD).
• Assessed “willingness to take again” and “willingness to pay for”
• Anxious, dizzy, restless, sleepy, whether they liked how they were feeling or not
• Preference for drug over : $0.35, $0.50, $0.85, $0.95, $2.00, $3.25, $4.75, $6.50, $9.00, $10.00
60 min. MRI scanning session
• Rated at the end, “drug liking”, “drug strength”, “good effects”, “bad effects”
• Monitored HR, O2 saturation, body temp etc.
Zolpidem may have aversive-like effects in absence of drug experience
Study designed to document drug-induced effects of multiple doses of zolpidem in drug-naïve volunteers
Supra-therapeutic dose (20 mg) would increase self-reported ratings of abuse-reported subjective effects, while lower therapeutic doses (5 and 10 mg) would not
Zolpidem increases sedative and intoxicating effects while decreasing stimulant-like effects
Zolpidem increased self-reported ratings of “high”, “like”, “sleepy” and “confused” in 20 mg relative to all other doses
All doses of zolpidem have more “drug-strength” than placebo. Increased feeling of both “good” and “bad” effects, “take again”, and “drug liking” in 20 mg
Zolpidem increased self-reported measures of sedation
Abuse-related feelings reported at highest dose
No impact on hypothetical choices between drug and money
Drug seeking behavior unlikely
Modest potential for abuse and/or dependence
Victorri-Vgigneau C, Feuillet F, Wainstein L, Grall-Bronnec M, Pivette J, Chaslerie A, Sebille V, Jolliet P. (2013). Pharmacoepidemiological characterization of zolpidem and zopiclose usage. Eur J Clin Pharamacol 69:1965-1972.
Clinical Pharmacology. RxList. Ambien. (2013). http://www.rxlist.com/ambien-drug/clinicalpharmacology.htm
Cubala W, Landowski J. (2007). Seizure following sudden zolpidem withdrawal. Prog. In Neuropharmoc. 31: 539-540.
Occurs in younger individuals
Behavioral Side Effects
Unexplained sleep walking
Binge eating while asleep
No memory of these actions
Performing other daily tasks while asleep
Most often prescribed by GPs
Liappas IA, Malitas PN, Dimopoulos NP, Gitsa OE, Liappas AI, Nikolaou ChK, Christodoulou (2003). Zolpidem dependence case series: possible neurobiological mechanisms and clinical management. J Psychopharm. 17: 131-135
Sakkas P, Psarros C, Masdrakis V, Liappas J, Christodoulou GN (1999). Dependence on zolpidem: a case report. Eur Psychiatry. 14: 358-59.
Ford JA, McCutcheon J (2012). The misuse of Ambien among adolescents: Prevalence and correlates in a national sample. Addictive Behaviors. 37: 1389-1394.
Wilkinson CJ (1998). The abuse potential of zolpidem administered alone and with alcohol. Pharmacology Biochemistry and Behavior. 60: 193-202.
Licata S, Mashhoon Y, MacLean R, Lukas S.(2011). Modest abuse-related subjective effects of zolpidem in drug-naïve volunteers. Behav Pharmacol. 22:160-166.
100mm scale: “extremely” and “not at all”
administered every 15 minutes during scan,
30 minutes until 6 hours post-administration of drug.
Modest abuse-related subjective effects of zolpidem in drug-naïve volunteers
Initial trials indicated that there was no dependence potential
New studies are finding it can have addictive potential
50-70 million people in the U.S. have sleep disorders
38 million people using this drug
FDA approved so lets get the facts right
Wolfson, E. (2013, May 8). The rise of ambien: why more americans are taking the sleeping pill and why the numbers matter. The Huffington Post. http://www.huffingtonpost.com/elijah-wolfson-/ambien_b_3223347.html