PSY 245 (drugs and behavior) Chapter 10 final

opium

(a) petals fall after the poppy blooms, leaving a round seedpod the size of an egg. (b) if the seedpod is scored lightly with a knife, it secretes a milky white sap. (c) after drying, this sap forms a thick, gummy, brown substance that is called __________. (i.e., dried sap from poppy pods)

1914 Harrison Narcotic Act

- growing awareness of the danger and pervasiveness of opiate dependence led to many legal changes, all culminated in this act in the United States -marked the beginning of drug crime in the U.S. -placed control of opiate drugs in the hands of physicians; determination of whether an addict had a valid medical need for opiates was exclusively the physician's decision

metabolism of opiate drugs

- most opiate drugs are rapidly metabolized by the liver and excreted by the kidneys

administration of opiate drusg

- most readily absorbed from gastrointestinal tract, although a given dose has a greater effect if its injected intravenously - most opiates are also absorbed through the nasal mucosa (heroin frequently taken intransally) and lungs (opium and pure forms of heroin are smoked) -opiates are also absorbed after intramuscular or subcutaneous administration (e.g., on the street heroin may be injected intravenously - "mainlining" - or subcutaneously

medical uses of opiates

-have constipating effect, so good for treatment of diarrhea -cough suppressant (e.g., dextromethorpan synthetic opiate with no analgesic or addictive properties) -treatment of heroin addicts in withdrawal and in maintenance programs designed to help addicts stay off heroin (e.g., methadone)

$634 million

By the mid-2000s the death rate due to prescription opiate overdose was exploding all over the country -a number of state took the matter to court and in September 2007, Purdue Pharma was forced to pay __________ in fines for misrepresenting the abuse liability of OxyContin

Mexican heroin (Mexican brown heroin/ black tar heroin)

Even though the number of overdose deaths due to prescription opiates stopped rising in 2011, Quionones (2015) noted that at the same time crack-down in diversion of prescription opiates, a supply line was bringing cheap, _______________ into the United States

morphine

Excretion of opiates is fairly rapid, with 90% excretion within a day after taking the drug. However, traces of ________ may stay in urine for 2-4 days.

legislative interpretations

Harrison act placed control of opiate drugs in physicians' hands; determination of whether an addict had a valid medical need for opiates was exclusively the physician's decision. However, ____________ ruled that: 1915: A physician must not prescribe opiate unless doses can be shown to be decreasing over time. 1917: Opiates must not be prescribed to addicts 1924: Heroin must not be prescribed AT ALL.

Chinese tea

In spite of the ban on importing opium into China, British ships continued to trade opium grown in India for ______________, and this activity was the basis for the Opium Wars between China and Great Britain in the middle of the 19th century.

Joint Commission on Accreditation of Health Care Organizations

Ironically, in 2001, _________________________ made treatment of pain a FOCUS of the medical profession and encouraged prescription of opiates with teaching materials (some developed by Purdue Pharma) by suggesting that these drugs were not very dangerous such as "Some clinicians have inaccurate and exaggerated concerns about addiction, tolerance and risk of death." -in light of this physicians increasingly began to feel obligated to prescribe opiate drugs when patients complained of pain and old guidelines imposing struct limits on dosage and frequency of use were often discarded ---> So prescriptions for OxyContin and other opiate painkillers (e.g., Vicodin) continued to rise

Papver somniferum

One of the many poppy species. However this is the only poppy species that produces opium.

June 2017

Opana abuse continued, so in __________ the FDA took the unprecedented step of requesting Endo Pharmaceutical to remove extended-release Opana from the market

Role of Oxycontin in Opiate Addiction Epidemic

Purdue Pharma released OxyContin in 1996 with an EXTENSIVE advertising campaign. -generic drug in OxyContin was not new, it was oxycodone -oxycodone is synthetic opiate that was found in Percodan and other prescription painkillers that had been on the market for DECADES -Difference is that OxyContin was designed to treat severe and chronic pain, so it contained A HIGHER DOSE of oxycodone (e.g., Percodan - with oxycodone - contained 5 mg and was short duration of action but OxyContin - with oxycodone - contained 20 - 160 mg of oxycodone in time-release form so that a single pill has a duration of action up to 12 HOURS) -New formulation within oxycontin mad eit highly effective pain reliever, and PURDUE'S promotional campaigns suggested that ABUSE LIABILITY WAS LOW in this form -HOWEVER, illicit (illegal) users figured out they could crush the pill form of OxyContin tablet to produce a powder they could then inject or snort and thus releasing all of the oxycodone ONCE delivering a LARGE dose of opiate IMMEDIATELY to users *OxyContin abuse, addiction, and lethal overdose all began to go up in the early 2000s -DEA announced national strategy to stop Oxycontin abuse --> under pressure, Purdue Pharma which made more than $4 billion on OxyContin sales between 2001 and 2003 discontinued the high dose (160mg) OxyContin pill in 2001, but widespread diversion and abuse of the drug continued

History of opium

Sumerian and Assyrian civilizations: evidence that they cultivated and used opium 6,000 years ago. Ancient Egyptians: discovered medical uses for opiates 3,500 years ago. Greek & Roman civilizations: used opium for variety of medical purposes. Great Greek physician Galen (A.D. 130-201, ~2,000 year ago) noted uses for opium. Islamic people of Middle East: medical and recreational purposes; to this day opium is less sensored than alcohol among muslims (Koran). Arab Traders: in the 9th century these traders spread opium use to India and China; this is when smoking Opium developed.

heroin

____ is frequently taken intra-nasally (since most opiates are absorbed through nasal mucosa)

Opium and pure forms of heroin

________ are often smoked (since most opiates are also absorbed through the lungs )

fentanyl

__________ is the latest opiate threat -has many chemical analogs some of which are even stronger (e.g., carfentanyl is approximately 100x more potent than fentanyl :O) -sometimes sold on their own -sometimes laced with heroin

illegal opiate use

_______________ meant that opium and heroin were smuggled into the country. This resulted in escalation of prices and a change in the type of person who became or remained addicted to opiates.

cross-dependence and cross-tolerance

________________ between all opiate drugs

cut drug

a cutting agent is chemical used to "cut" (dilute or adulterate) recreational drugs with something less expensive than the drug itself

endorphins

all of the opiate drugs are unique in that they activate one receptor in the brain, at first called opiate receptors, we now know the natural neurotransmitters that bind to those receptors and chemicals generally called _______ -opiates mimic these

stopped rising

although prescription opiate use remains high today, it is noteworthy that the number of overdose deaths due to prescription opiates _________ in 2011

endogenous morphine

although several morphine-like substances are found in the brain, these complex peptide molecules are referred to collectively as endorphins, a contraction of _________

psychological effects of opiates

analgesia/euphoria known for producing a loss of interest in sexual activity (males: impotence, or inability to achieve erection or orgasm) - Famous for feeling of users complete satisfication and meeting all of the users needs -impair social interactions -smoking opium or take other piate drugs often report vivid dreamlike experiences; theses are the basis for the expression "pipe dreams" -interference with cogntiive function: impariments in learning and memory

increase

deaths due to ALL types of opiates combined shows an ________ in every year since 1999

China

dependence on opium was first recognized as a problem in ________, with the first edict (ban) against opium issued in 1729. However, this country already had so many opium addicts that the demand remained very high.

synergy

depressant drugs/alcohol do not show cross-dependence or cross-tolerance with opiate drugs, but they do show __________ (many overdoses due to combos of opiates with depressant drugs)

8-12 hours, flu-like

early indications of withdrawal begin _________ after last dose and include __________ symptoms

injected intravenously

even though most opiate drugs are readily asborbed from the GI tract, a given dose has a greater effect if it's _______________

Prince

fentanyl has become such an important issue today due to the potency of the drug as well as the even more potency of its chemical analogs (e.g., carfentanyl) -in APRIL 2016 famous rock musician ________ died from a fentanyl overdose which increased awareness of this drug

100 (thats 1000x more potent than crude opium)

fentanyl is not a new drug -began available in 1960, at which time it was recognized as the most powerful opiate drug ever developed -fentanyl is about ______x(times) more potent than morphine but has a shorter duration of action than most other opiate drugs

surgical anesthesia

fentanyl's main medical use was for __________, but in more recent years formulations have been used in pain treatment

Morpheus

greek god of dreams that German pharmacist, F.W. Serturner, named the chemical morphine after due to the blissful dreamlike state that it produced.

legal changes

growing awareness of the danger and pervasiveness of opiate dependence led to a number of __________.

Mexico

has become an important opium producer and MOST heroin entering the U.S. today comes from poppies grown here

gluey

in 2010 oxycontin was reformulated to prevent injection: if crushed it becomes ________ and cannot be dissolved

U-47700, pink

in April famous rock, musician died from a fentanyl overdose which increased awareness of the drug, but it was later revealed that another synthetic opiate (opioid) ________ or _________ was found at the scene of his death

heroin overdose deaths

increase in Heroin use was accompanied by an abrupt increase in _____________ starting about 2012

how did the opiate epidemic begin in the US?

it began in the clinic (not on the street) -after Harrison Act, due to awareness of addictive properties opiates were generally used quite sparingly (use generally reserved to severe and acute pain (e.g., post-surgery, trauma) -treatment of persistent or chronic pain with opiates was seen as inappropriate because of the risk of addiction -in 1970s synthetic opiate drugs (i.e., such as hydrocodone (Vicodin) and oxycodone (Percodan) began to be widely used. -physicians continued to be cautious in prescribing these synthetic drugs (opioids) understanding their effects and potential for addiction to be similar to the naturally occurring compounds (e.g., Heroin, opium, morphine, codeine) Late 1990s things changed: between 1999-2011 prescriptions for opiate pain-killers quadrupled, factors for this seem to be: -change in philosophy of pain treatment such that physicians began to treat pain, even chronic pain, with opiate drugs; this philosophical change was driven by the belief that pain patients were unlikely to become addicted to opiates (this belief was based off of a SMALL study with FEW subjects) -Promotion of "newly" developed opiates by the pharmaceutical industry fueled the increase in opiate prescriptions (poster child = OxyContin); Purdue Pharma

analgesic or pain-relieving effects

major medical use for opiate drugs

cross-dependence

medical detox uses __________ giving opiate addict suitable opiate drug, usually/historically methadone (pill form or liquid form - don't need to inject); relieve withdrawal symptoms and long-acting

soldiers disease

morphine dependence so common on both sides of Civil War in America that it was often called _____________

hypodermic syringe

morphine widely available with the concomitant development of ________________, causing injectable morphine to become major problem of dependence in Europe and United States

nasal mucosa and lungs

most opiate drugs are also absorbed through the __________ and ________.

liver

most opiate drugs are rapidly metabolized by the __________ and excreted by the kidneys. Excretion of opiates is fairly rapid, with 90% excretion within a day after taking the drug. However, traces of morphine may stay in urine for 2-4 days.

gastrointestinal tract (esophagus, mouth, stomach, SI, LI, and anus)

most opiate drugs are readily absorbed from the ____________

opiates

most potent and selective pain relievers known to medicine today

heroin

new opiate drug formed in slight weak of morphine molecule -2x more powerful than morphine -discovered first by C.R. Alder Wright then unnoticed -rediscovered by the great German pharmacologist Heinrich Dreser (also discovered Advil) -Dreser noted this new chemical as twice as potent as morphine -due to the fact that this new compound was so powerful, it was viewed as a new treatment with "heroic" possibilities and thus was christened ____________ -used immediately as cough suppressant and pain reliever -more likely than morphine to produce dependence

suboxone

new treatment drug -combination of two drugs: buprenorphine and naloxone -buprenorphine is an opiate drug that is an agonist - this drug reduces abuse risk because if suboxone is crushed up or chewed or snorted- since the naloxone is bypassed by the liver when this drug is taken subliminally so it doesn't antagonize UNLESS the user tries to crush it up and snort it because then it has to go through the liver and the naloxone will completely antagonize the buprenorphine (opiate agonist) making suboxone a less abusable form of substitution treatment

19th century

not until this time was the active drug(s) within the opium was discovered -German psychologist first to isolate principle active drug from opium

distribution of opiate drugs

once in the bloodstream, opiates are distributed throughout the body and accumulate in the kidneys, lungs, liver, spleen, digestive tract, and muscles, as well as the brain. - with some opiates, such as morphine, only a small amount penetrates the blood-brain barrier - heroin more lipid soluble, more penetrates BBB - once in brain heroin converted to morphine

morphine

once in the brain, heroin is converted to _________. So heroin is essentially a more effective package for delivering ________ (same term) to the brain than is ________ (same term) itself.

what do endorphins do

ongoing research started with premise: since opiate drugs apparently mimic endorphin activity by stimulating the opiate or endorphin receptor sites in the brain, endorphins might share many properties with opiate drugs, such as pain relief and production of pleasure One idea: is that endorphins are part of a natural pain-relief system. It's been argued that endorphins are released and produce analgesia (pain relief without loss of consciousness) or pain relief after certain kinds of pain or stress

naloxone

opiate receptor antagonist -can easily prevent death from overdose -higher affinity for opiate receptor site; outcompetes opiate

relation between opium, morphine, heroin, and codeine

opium is the dark, dried, gummy sap from the poppy seedpod. Within opium are two naturally occurring opium drugs, found in their basic form within the poppy,: morphine and codeine. Morphine is the principle active drug from opium (named after greek god of dreams, Morpheus); morphine 10x more potent than crude opium. Later in the late 1800s, a new opiate drug is introduced by being created by slightly tweaking the morphine molecule: diacetylmorphine. Due to this chemicals potency (being twice as potent as morphine, which is already 10x more potent than opium) being viewed with "heroic" possibilities, this new compound was named heroin. Heroin used immediately as cough suppressant and pain reliever. Not until many years later, was it discovered that heroin was even more likely than morphine to produce dependence.

placebo

pain relief induced by ______ can activate endorphin recptrs in several brain regions -this suggests an endorphinergic basis for at least some cases in which simply "expecting" that you have taken a pain-relieving drug is sufficient to relieve pain

analgesia

pain relief produced WITHOUT a loss of consciousness

acupuncture

pain relief produced by acupuncture may be related to endorphin release because naloxone can reverse acupuncture-induced analgesia. -Since major action o f naloxone is to block the endorphin receptors, naloxone-reversible analgesia is strong evidence that the acupuncture needles are triggering the release of endorphins and relieving pain through this system

Opana

reformulation of OxxyContin so that if crushed it becomes gluey and can't be dissolved REDUCED OxyContin Injection but illicit use quickly shifted to another prescription opiate called _______ (oxymorphone) -similar to OxyContin, treatment of severe pain and use timed release of relatively high doses of the painkiller -by 2011 this prescription opiate abuse overtook Oxycontin and it too was reformulated

major physical effects of opiates

similar to depressants in: Depression of heart rate, depression of blood pressure, depression of respiratory rate (decrease in HR, BP, and respiratory rate), decrease body temperature unique to opiates: effect the pupils instead of dilating as most other drugs we have talked about do, opiates constrict pupils (pinpoint pupils) AND constipation

fentanyl

since heroin is frequently laced with _______, some researchers estimate that as many as 40% of deaths attributed to heroin may actually involve a ________(same term)-heroin combination

opiods

synthetic pain-killers (e.g., hydrocodone, oxycodone) are often called "_________" to contrast with the naturally-occurring opaites (e.g., opium, morphine, codeine, and heroin included)

lipid-soluble

the main difference between morphine and the more potent drug heroin is that heroin is more ___________ and thus more readily penetrates the blood-brain barrier

morphine

the major active chemical in opium -10x more potent than crude opium

doubled

the number of fatal overdoses on fentanyl _________ between 2012 and 2014

middle east

the opium poppy is native to the _____________, in the areas that border the Mediterranean Sea, but is now cultivated extensively throughout Asia and the Middle East.

India and China

the practice of smoking opium began in ________ and ________ when opium use spread to these places from Arab traders in the 9th century .

automobile accidents

then, in 2008, drug overdose deaths, largely due to opiates, passed _________________ as the leading cause of death in the United States

today

there is still considerable public concern that opiate drugs are being overprescribed and the changed medical approach to pain treatment has come under scrutiny and criticism

morphine and codeine

these are referred to as the naturally occurring opium drugs because they are found in their basic form in the seedpod of the Papver somniferum poppy.

afghanistan

today _________ (of south asia) produces most of the world's opium

injectable heroin

user who got hooked on prescription opiate drugs began to switch away from the reformulated compounds to __________________.

black market

with the doors closing for addicts to obtain drugs from legitimate sources through the Harrison Act (1914) and from legislative interpretations that followed the Act in 1915, 1917, and 1924, addicts turned to a growing ________ to maintain their addiction