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The two main groups of sedative-hypnotics are
benzodiazepines and the barbiturates
sedative-hypnotic drugs are prescribed to
to control neurotic reactions in unstable patients, to
control anxiety, hypertension (high blood pressure), reduce seizure activity, and to
induce sleep.
sedative-hypnotic drugs effects
similar to those of alcohol
sedatives
produce a calming effect on mood, and behavior and are often perscribed for anxiety
hypnotics
are short acting drugs that are used to induce sleep their name comes from
a sleep like state
sedatives hypnotics drugs bind
to the receptors on the neurotransmitter GABA and enhance the receptors response to GABA. GABA is sometimes called
the brains natural or endogenous, sedative. they play an important role in the brain to prevent regions from becoming over excited
ancient civilations
used alcohol and opiums to calm and control the mind
Bromides
introduced in the 1850s but slow metabolism meant that toxins could build up in the body
choral hydrate
1969 could give a sailor a mickey finn
peraldehyde
used to control alcohol withdrawls but has offensive odor
barbiturates first developed at the end of the 19th century medical use
peaked in the 1940s and 1950s, during the 1960s and 70s they
were abused but their low margin of safety and high addiction potential
examples of barbiturates
phenobarbital, seconal, meprobamate (milton), chlordiazepoxide (librium),
diazepam (valium)
phenobarbital- a slow acting drug whose effects can last for 12-24 hours used to reduce seizure activity in patients with epilepsy
Seconal-short acting compounds (3-6) hours a favorite party drug for those who liked downer
Meprobamate-mothers little helper, replaced by the benzodiazepines
chlordiazepoxide and diazepam-first widely manufactured benzodiazepines were considered miracle drugs due to safety and lack of addicting qualities, by 1975 100 million perscriptions were written per year
medically, benzodiazepines are used to treat
1. symptoms of anxiety and panic disorders
2. anxiety in surgical patients
3. sleep disorders
4. spasms ans seizures
5. acute alcohol withdrawl symptoms
most widely perscribed benzodiazepines
1. alprazolam (xanax)
2. lorazipam (activan)
3. clonazepam (klonopin)
4. diazepam (valium)
5. temazepam (restoril)
nonmedical use of benzodiazepines
used because effects are similar to alcohol so can be abused for same reasons as alcohol. Often abused with
alcohol or stimulant users use them to comedown from excess stimulation
tolerance of benzodiazepines
develops as the liver becomes more efficient at processing them, elderly patients the liver does not process the drug as quickly and can lead to over stimulation
tissue of benzodiazepines
can develop if a patient takes 10-20 times the normal dosage daily for a couple of months, or if taken normal dosage for a year or more, to avoid withdrawls
a physician will slowly reduce the patients dosage over a period of time
downers (depressents)
depress functioning of the Central nervous system
physical and mental effects of downers
physical-sedation, muscle relaxation, drowsiness, coma if dose is high enough
mental effects of downers- disinhibition of of impulses and emotions, europhia due to reduction of anxiety, and emotional distress
three major classes of downers
opiats/opioids, sedatives-hypnotics, alcohol
opiats and opium
are drugs refined from raw opium which is the milky fluid of the unripe seed pod,
the opium poppy
(papavear somniferum) and the major opiates are, morphine and codeine
semi- synthetic opiates
are chemical variations of morphine and codeine they include
diacetylmorphine (Heroin)
hydrocodone (vicodin)
oxycodone (oxycontin)
hydromorphone (dilaudid)
opiods
are fully synthetic drugs and include
methadone (dolophine)
meperidine (demoral)
propoxyphine (darvon)
fentanyl (sublimaze)
the opium poppy was first cultivated in
ancient mesopotamia, egypt, and greece around around 3400 B.C. plant was used as a
cureall medicine, a source of pleasure, and a poison
oral ingestion of opium
opium was originally chewed, eaten, or mixed with a drink and swallowed to induce drowsiness and cure illness
smoking opium
in the 16th century explorers and traders introduced the pipe to europe and asia and use became widespred most in china. this led to
china blockading its ports from english trading ships selling opium. this period of time was known as the opium wars (1939-1842 and 1856-1860) railroads brought it to the us
refinement of morphine, codeine, and heroin
in 1805 morphine was isolated from opium, and in 1874 chemists altered the morphine molecule to make heroin
diactetylomorphine is more fat soluble than morphine which causes it to move across the blood brain barrier faster
injection of morphine, codeine, and heroin
the development of the hypodermic needle in 1853 made morphines even more potent and more addicting
patent medicines of morphine, codeine, and heroin
in the 1800's hundreds of opium laced tonics were available. the overmedication by doctors and the popularity of the drug
raised addiction rates dramatically
snorting
if heroin is sufficiently pure, users can get high by snorting it. today over half of all heroin addicts get started their habits by this method
20th century and government regulation of heroin
became illegal in the 1900s by which acts
food and drug act-1906
harrison narcotics act- 1914
when laws increased for heroin
prison population boomed and supplies dwindled to take place
criminal organizations stepped in to take control of growing, processing and distributing
how many use heroin in the world
5-10 million heroin users
how much does the us consume
3 percent, how much did afghanistan produce
grew 92% or world opium which is produced into heroin
other significant growers of opium
the golden triangle
myanmar, thailand, and laos
most of u.s supply comes from
columbia and mexico
reasons doctors perscibe opioid drugs
to deaden pain, contol coughing, and to stop diarrhea
substance p
is the neurotransmitter released by neuronsin spinal cord pathways to signal tissue damage.during a intense pain
specific neurons release endorphines and enkephalins, that block the release of substance p and dampen pain sensation.
endorphines and enkephalins are sometimes called
our brains natural painkiller
opiate and opioids are able to bind to
and activate endorphin receptors, and thus mimics our brains natural pain reaction
in fact these drugs can completely block severe pain such as a burn or major abdomial surgrey
endorphines also dampen another pain
mental pain such as fear and anxiety, and to produce a calm, detached mood.
opioid drugs can produce a feeling of being completely dissattached from emotions
opioid druga increase the activity in the brains
reward/pleasure pathway which can produce a state of euphoria this can be detrimental to people at risk of addiction
cough suppression of opioids
bind the receptors in the brain whose function is to control the cough reflex
control of diarrhea
opioid drugs reduce gastric secretions and slow contractions of smooth muscles lining the intestines so that life threatening fluids is reduced
side effects of opioids drugs
physical side effects include constipation, pupil constriction, drooping eyelids, relaxed muscle tone, dry itchy skin, vomiting
tolerance of opioids
people seeking mental effectssuch as euphoria may need 10 times their original useage after a month of use
withdrawl
occurs when someone stops taking drugs. and they suffer from mental and physical side effects.
opioid withdrawl symptoms
fever chills and goosebumps
intestinal cramping and diarrhea
bone and joint pain
muscle cramps
insomnia
and intense craving
they are produced quickly and around 8-10 hours after last dose and peek within 48 hours
neonatal effects of heroin
it easily crosses the plecenta barrier so the fetus is exposed to the same level as the mom
pregnant addicts have a higher risk of miscarraige, plecental seperation, premature labor and still births.
overdose on heroin
each year 4000 to 5000 people die from opioids or combination of depressents
severe respiratory depression is the major cause of overdose death with opioids.
symptoms of an opioid overdose
blue lips and pale or blueish skin
Slow shallow breaths with fluid rattles or gasps
Very constricted pupils that look like pin pricks
Skin feels cold and clammy
to combat an opioid overdose
Immediate CPR is needed, and, if possible, an injection of an opioid receptor
antagonist such as naloxon (Narcan).
what are risks of injecting opioids
Dirty and shared needles. Heroin users can unknowingly inject adulterants, bacteria, and
viruses, including those that cause hepatitis B or C, endocarditus, flesh-eating bacteria,
and HIV, virus that causes AIDS.
what percentage of needle sharing opioid users have hep. c and aids
50-90% carry hep. c and over half of IV drug users carry HIV which can spread to their sexual partners.
dilution of street opioid
Street drugs can vary from 0 to 99% pure. Heroin is always cut or stepped on
with adulterates (cheap substitutes used to replace the drug).
what is the cost of opioids and how do users pay for it
A majority (79%) of heroin users has full-time jobs but a habit can grow from $20 to
$200 dollars a day. t is estimated that 60% of the cost is covered by prostitution and drug
dealing and 40% by shoplifting and burglary.
heroin
diacetylmorphine
Largest sources of illegal opium and heroin are Afghanistan and the Golden Triangle
(Burma, Northern Thailand and Laos). India is the largest grower of opium for legal
medical purposes.
Types of heroin include "China White" and “Persian brown". Since the 40's, Mexico has been largest supplier to U.S. of “black tar" heroin which is often smoked.
Codeine
is not as strong as morphine, and generally used for relief of moderate pain or to
control coughs.
Morphine
refined from opium and is the standard for pain relief measurement
Methadone
(Dolophine)-A long-lasting opioid which is taken orally to reduce
heroin craving and reduce withdrawal symptoms
Hydromorphone
(Dilaudid) A semi-synthetic opioid refined from morphine. It
is 8 times more potent than morphine
Oxycodone
(Oxycontin) A time release form of oxycodone.
Hydrocodone (Vicodin)
Today it is the most abused oral pain reliever
Meperidine
(Demerol) A short-acting opioid, usually injected
Propoxyphene
(Darvon) An opioid prescribed for mild to moderate pain, especially
by dentists
Fentanyl
(Sublimaze) The most powerful pain killer available (50 to 100 times
stronger than morphine)
Designer heroin
Street versions of fentanyl, known as "China white," are made
without controls and can be very dangerous.
LAAM
An opioid being tested for heroin replacement therapy
Naloxone and Naltrexone
Opioid receptor antagonists which block the effects of
opioids and can be used to reverse a heroin overdose or discourage relapse.