by stephanie rouse robby gill. depressants – aka downers drugs that calm and relax the central...
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DepressantsBy Stephanie Rouse
Robby Gill
Depressants – aka DownersDrugs that calm and relax the central nervous system by
interfering with nerve impulse transmission
slow the function of the brain, heart, and other organs, reduce the rate of breathing, and dull emotional responses
action strongly based upon dosage of druglow dose – little or no impact
moderate dose – sedationhigh dose – induce sleep
extremely high dose – death
GABA is the main inhibitory neurotransmitter in the central nervous system (CNS). GABAergic inhibition is seen at all levels of the CNS, including the hypothalamus, hippocampus, cerebral cortex and cerebellar cortex. As well as the large well-established GABA pathways, GABA interneurones are abundant in the brain, with 50% of the inhibitory synapses in the brain being GABA mediated.
Calmness, relaxation, reduction of anxiety, sleepiness, slow breathing, slurred speech, staggering gait, poor judgment, slow, uncertain reflexesIf abused result in unconsciousness and death
TranquilizersReduce nervous tension/anxiety without inducing
sleep
Examples include:AlcoholDenzodiazepines (safer than barbituates)
Valium (diasepam) Librium
Barbiturates and benzodiazepines are the two major categories of sedative-hypnoticssimilar in chemical structure Benzodiazepine
Fusion of benzene and diazepine ring systems
Barbiturate
Barbituric Acid Ultrashort, short, intermediate, and long acting
depending upon type used to keep patient from waking before surgery is complete
Short acting are abused Similar to alcohol Thiopental ultra-short acting marketed as
Sodium Pentothal when dissolved in water in large does becomes one of the3 drugs used in the US to execute prisoners on death row, low dose used as truth serum, decreased inhibitions
Oldest depressant, 35 prescribable 5,5-disubstituted derivatives of barbituric acid (vary by R group from carbon to alkyl, saturation, bromo groups, phenyl group)
Not highly potent methaquolene
Other depressantsSedatives HypnoticsCertain barbiturates
Soothing of distress without effects of sleep i
tranquilizers are milder than sedatives
Class of drugs that produce sleep
Ex: Chloral hydrateEx: Phenobarbital
(barbiturate) behaves as either a sedative or hypnotic dependent upon dose
Continuum of Sedation Behavior
DeathComaGeneral AnesthesiaHypnosisSedationDisinhibitionRelief of AnxietyNormal
Increasing Dose
Ethanol – a common depressantCapable of
hydrogen bonding, but also
Fat soluble (small size)
Readily penetrates cell and tissue membranes
Easily and completely absorbed from the entire gastrointestinal tract.
Ethanol – a common depressant30-50 mg / 100 mL
blood
100 mg / 100 mL blood
200 mg / 100 mL blood
400 mg / 100 mL blood
mild intoxication; Silly behavior
slurred speech; staggering; aggression
vision and movement difficult
Coma, death
Ethanol – a common depressant
Alcoholism – a diseaseProgressiveFrequently fatalMay run in families? genetic component
Other uses• Antiseptic
• Tincture of iodine
• mouthwashes
Discuss the social and physiological effect of the use and abuse of ethanol.
Include effects on the family, cost to society and the short-and long-term health effects.
Social Effects of the Abuse of Ethanol
Major social costs due to alcohol use and abuse.
In the U.S., Australia, Europe, Japan, and other countries, over 80% of all alcohol-induced costs are borne by society.
Connected to many different degrees of crime.
MADD
Physiological Effects of EthanolShort-term effects:
DepressantImpairs CNS function proportional to intake of
alcoholImpacts Pregnancy - Miscarriage, low birth
mass and fetal abnormalities.
Long-term effects:Cirrhosis and cancer of the livercoronary heart diseasehigh blood pressureStrokesDigestive issues - gastritis, peptic ulcers.Poor eating habits.
Other Physical EffectsDriving
impairmentAlcoholism is a
diseaseIncludes
physical and psychological addiction as well as genetic factors
Enhances the effects of other drugs.
Describe the synergistic effect of ethanol with other drugs.
Reactions with other Drugs
Synergistic Effects - combination of two drugs is more harmful than either drug taken aloneAlcohol + aspiring – increase risk of stomach
bleedingAlcohol + sedatives - increases risk of heavy
sedation leading to coma and deathAlcohol + cocaine – cocaethylene forms…
extends high… but is very toxic… causes severe constriction of blood vessels (high blood pressure)… and irregular heart beat.
Alcohol + bezodiapenes (mogadon, valium) – suppresses CNS leading to death
Describe and explain the techniques used for the detection of ethanol in the breath and in the blood or urine.
Include potassium dichromate (VI) in the breathalyzeranalysis of blood or urine by chromatographyabsorption of infra-red radiation in intoximeter.
Detecting BAC (Question 12)Breathalyzer test
(potassium dichromate [K2Cr2O7] used as oxidizing agent).
Gas Liquid Chromatography
Takes breath sample and detects presence of gases at a quantitative level.
Blood and urine can be used in the machine as well.
Detecting BAC (continued)Infra-Red Spectroscopy (“intoximeter”)IR absorption at 2950 cm-1 is used to detect
presence of the C-H group.Very accurate (% C-H absorbed acts as a
marker for BAC).
Other Commonly Used DepressantsNitrazepam (mogadon)Hypnotic, induces sleep, control seizures and infantile spasms
Prozac (Fluoxetine hydrochloride)Anti-depressant used for mental depression, increases activity of the neurotransmitter serotonin
Depressants are often described as anti-depressants because they relieve depression
Valium (diazepam)relief of anxiety and tension
Carbon skeleton structures of diazepam and nitrazepam are the same, the two differing in side groups.The structure of Prozac differs from the other two