Download Benzodiazepines

Benzodiazepines
Rachel Anderson
Introduction
Benzodiazepines (BZD, BZs) "benzos”
 Psychoactive drugs
 Chemical structure is the fusion of
a benzene ring and a diazepine
ring
 Central nervous system
depressants that are commonly
known as tranquilizers, sedatives,
or anxiolytics
 Due to the sedative effects they
produce, they are often used as
“date rape” drugs
 Approximately 2,000
benzodiazepines have been
produced but only 15 are
marketed in the U.S
 Schedule IV
 Twice as many women as men
taking them
CNS depressants
• They are the most commonly
prescribed medications in the
U.S. and are mainly used to treat
anxiety and insomnia
• Second most frequently abused
prescription
• Combination with other CNS
depressants can cause
dangerous drug interactions,
and contribute to death via
overdose
History
 As we learned in class:
 1800’s looking for something other than alcohol
to be used as CNSD
 Bromides 1800s helpful but toxic
 Barbiturates 1900s initially safe/effective; eventual
problems with tolerance, safety and dependence
 Benzodiazepines 1950s safe for short periods of
time; long term use cause dependence and
withdrawal
 However, they are less toxic than their predecessors,
(the barbiturates) and death rarely results when a
benzodiazepine is the only drug taken.
Benzodiazepines History
 1955 – Synthesis of the first benzodiazepine,
Chlordiazepoxide (Librium) 1960 – Librium
(Chlordiazepoxide) made available
 1963 – Valium (Diazepam) made available
 1970s – Benzodiazepines had replaced barbiturates
 1973 - 100 million prescriptions written
 1977- Benzodiazepines were globally the most
prescribed medications
 1978 – 2.3 billion tablets of Valium sold
 1980 – Researchers issued one of the earliest warnings
against long term use
Reason for Use
• Benzodiazepines possess sedative,
hypnotic, anxiolytic, anticonvulsant,
muscle relaxant, and amnesia
actions, which are useful in a variety
of indications:
 Generalized anxiety disorder (GAD)/ Panic Attacks
/ Acute Anxiety,
 Insomnia
 Psychiatric Emergencies
 Muscle Spasms
 Epileptic seizures
 Alcohol Dependence
 Sedate patients
Mechanism of Action
 Most are administered orally; however, they can also be given
intravenously, or intramuscularly
 Mechanism of Action:
 Affect neurons that have receptors for neurotransmitter gammaaminobutyric acid (GABA)
 GABA is the most common inhibitory transmitter in brain regions
Limbic System (alter mood)
RAS (cause Drowsiness)
Motor Cortex (relax muscles)
 Distinguished primarily by duration of action: (short acting) hypnotics,
(long acting) sedatives
 Benzos are categorized as either short-, intermediate-, or long-acting:
longer-acting benzodiazepines are recommended for the treatment of anxiety
Short- and intermediate-acting benzodiazepines are preferred for the treatment
of insomnia
 High doses of many shorter-acting benzodiazepines may also cause
anterograde amnesia and dissociation
Contraindications
 Respiratory depression - myasthenia gravis, sleep
apnea, bronchitis, and COPD.
 Increase suicidal tendencies – major depression
 Life Threatening interactions – history or current
drug comorbidity
 Not safe – Pregnancy
Side Effects
 The most common side-effects of benzodiazepines are related
to their sedating and muscle-relaxing action:
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Drowsiness
Dizziness
Decreased alertness
Decreased concentration
Lack of coordination
Driving impairment
Decreased libido
Depression
 Less common side effects:
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Nausea
Blurred vision
Confusion
Euphoria
Nightmares
ADDICTION/ DEPENDENCE
/TOLERANCE AND WITHDRAWALS
 Main Sign of Physical
Dependence
 Rebound Symptoms
 Withdrawal
Symptoms
 Most Frequent
Symptoms of
Withdrawal
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Insomnia
Gastric problems
Tremors
Agitation
Anxiety
Difficulty breathing
Headaches
Fear
Muscle spasms
 Less Frequent Symptoms of
Withdrawal
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Irritability
Sweating
Depersonalization
Hypersensitivity
Depression
Suicidal behavior
Psychosis
Seizures
Abrupt Withdrawal
can be dangerous
– gradual reduction
regimen/ tapering
is recommended
Some Benzos to Know
 Of the 15 FDA-approved
benzodiazepines in the U.S., the
most commonly known include:
 Versed (midazolam)
& Halcion (triazolam), which
are ultra-short acting
[These are often prescribed
to help a person sleep or to
calm a person down
before surgery]
 Xanax (alprazolam), Klonopin
(clonazepam), & Ativan (loraz
epam), which are short-acting
 Librium (chlordiazepoxide)
& Valium (diazepam), which
are long-actin
Prescribing rates per 100 persons (in
quartiles), by state and drug type — IMS
Health, United States, 2012
Wide variation exists from
one state to another in
prescribing rates for these
drugs. High rates of
prescribing these
controlled substances are
important determinants of
rates of fatal overdose
and drug abuse,
especially when
prescribed with opioids
Alabama, Tennessee, and
West Virginia were the
three highest-prescribing
states
https://www.cdc.gov/mmwr/preview/m
mwrhtml/mm6326a2.htm
Charts/ Graphs
National Overdose Deaths—
Number of Deaths from
Benzodiazepines. The figure
is a bar chart showing the
total number of U.S.
overdose deaths involving
benzodiazepines from 2002
to 2015. The chart is
overlayed by a line graph
showing the number of
deaths of females and
males. From 2002 to 2015
there was a 4.3-fold increase
in the total number of
deaths.
https://www.drugabuse.gov
/related-topics/trendsstatistics/overdose-deathrates
Other/Interesting
 Toxicology screen - A toxicology screen refers to
various tests that determine the type and approximate
amount of legal and illegal drugs a person has taken.
 Benzodiazepines: up to 6 weeks with high level use
 1966 hit “Mothers Little Helper” by Rolling Stones is a
song written about Valium
 “What a drag it is getting old ‘kids are different today’ I
hear every mother say. Mother needs something to calm
her down. And though shes not really ill. Theres a little
yellow pill. She goes running for the shelter of a mothers
little helper
Current Awareness
 https://www.madinamerica.com/2016/06/new-videofor-world-benzodiazepine-day/
 in a new video for World Benzodiazepine Awareness
Day (W-BAD) people from all over the world share
about the iatrogenic harm they sustained from taking
benzodiazepines as prescribed.
Summary
 Benzodiazepines are psychoactive
drugs
 They are classified as depressants
and act on the Central Nervous
System
 Benzodiazepines possess sedative,
hypnotic, anxiolytic, anticonvulsant,
muscle relaxant, and amnesia
actions
 They are the most commonly
prescribed medications in the U.S.
and are mainly used to treat
anxiety and insomnia.
 Combination with other CNS
depressants can cause dangerous
drug interactions, and contribute to
death via overdose
Resources

http://wickedsober.com/benzodiazepines/

https://vsearch.nlm.nih.gov/vivisimo/cgi-bin/querymeta?query=benzodiazepine&v%3Aproject=nlm-main-website

http://www.pdr.net/drug-summary/Xanax-alprazolam-1873

http://www.pdr.net/search-results?q=clonazepam

https://www.drugabuse.gov/related-topics/trends-statistics/overdosedeath-rates

https://medlineplus.gov/ency/article/003578.htm

http://genpsych.com/2015/08/11/quick-facts-aboutbendodiazepines/

https://stacks.cdc.gov/view/cdc/40352

https://en.wikipedia.org/wiki/Benzodiazepine

http://www.narconon.org/drug-information/benzodiazepines.html