Heroin nick Atencio



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HEROIN

  • Nick Atencio

  • &

  • Gabrielle Sanchez


Introduction

  • Heroin is a narcotic analgesic derived from morphine. It is believed to be one of the most addictive drugs in the world today. For our group this topic was selected due to interest sparked by friends and family who have used and died from heroin as well as coming from a city and state that leads the nation in heroin related deaths per capita.

  • This presentation will cover topics such as the history, routes of administration, mechanism of action, treatments, effects on babies and laws attributed to heroin.



“Need Something New”

  • In the late 1800’s morphine and codeine were the most popular prescribed and addictive drugs. The Bayer company in Germany was looking for alternate medications that were capable of treating the same diseases as codeine and morphine (which is derived from the opium poppy) but yet less potent and less addictive (Hodgson).



Diacetlymorphine

  • In 1874, English chemist C.R. Wright ventured out into making a non-addictive form of codeine and morphine. In doing so he combined anhydrous morphine alkoid and acetic andhydride (Hodgson). This produced what is known as diacetylmorhpine (Hodgson). In short diacetylmorphine is an acetylated version of morphine.



“Heroic”

  • In 1898, Heinrich Dreser of Germany saw the commercial value in Wright’s invention and began testing on rabbits, himself and fellow co-workers at the drug company he worked at in Germany, Bayer (Hodgson). Dreser later then termed Wright’s invention as “Heroin.” This was due to the results from testing his co-workers which said they had a “heroic” like feeling while using the drug (Hodgson).



“It’s not hypnotic and theirs no danger in acquiring a habit!” –Boston Medical and Surgical Journal 1900

  • In 1898, Dreser advertised Heroin to the Congress of German Naturalists and Physicians (Hodgson). Claiming it was 10x more effective then codeine as a cough medicine with only 1/10 of it’s effects (Hodgson). Also that it was more effective then morphine as a pain killer (Hodgson). In 1899, the Bayer company began advertising heroin to doctors and practitioners in Europe and the U.S. (Hodgson).





Routes of Administration

  • Intravenously a.k.a. Shooting up!

  • The most common route of administration. Requires user to dissolve the heroin powder in an acid such as citric acid or lemon juice in order to break down the heroin (Hart). Sometimes water. Then heated into fine liquid and injected intravenously. This route requires smaller doses yet achieves faster effects then other routes of administration. Most injections occur on majors veins (aka mainling) such as those in the arm (Hart). If veins collapse then injections typically will occur in groin, neck and legs (Hart). Intravenous avoids first pass metabolism and therefore readily able to cross the blood brain barrier and effects felt immediately after injection (Meyer).



Routes of Administration

  • The second most common route is smoking. Smoking heroin requires the user to heat the drug in order to inhale the vapors. Typically heated on tin foil or lacing the drug with marijuana or tobacco and smoking it in a pipe or cigarette (Meyer). When heated it turns into a thick liquid. Smoking heroin is also termed as “chasing the dragon,” since the user chases the globs of heroin that are in the tube with the intention of inhaling as much smoke as possible (Meyer).



Routes of Administration

  • Snorting heroin is one of the least common routes. When snorted, users will use a glass tube or tin foil to make a tube Meyer. Any residue left in the tin foil tube allows for further usage. By snorting users bypasses first pass metabolism in the liver (Meyer).



Routes of Administration

  • The less common route of administration is oral intake. When taken orally, heroin merely serves as a pro-drug for morphine (Hart). Heroin must first pass metabolism in the liver when taken orally. It is in the liver that heroin is converted into morphine (Meyer).



Distribution

  • The acetyl groups in heroin make it more lipid soluble and able to penetrate the BBB (Meyer). It is in the brain where heroin is able to have its overall effects.

  • Heroin primarily modifies the action of dopamine in the nucleus accumbens and ventral tegemental area (VTA) of the brain (Meyer).



Metabolism of Heroin



Mechanism of Action

  • 6-MAM and Morphine then act as agonists and bind to mu, kappa (both play a role in pain reception) and delta opioid receptors in the brain (Hart).

  • It is important to note that the mu receptor has the highest affinity of the three for morphine and opiate related drugs (Meyer).

  • This binding then prevents the release of GABA, therefore reducing the inhibitory effects of GABA on dopamine neurons (Meyer).

  • The increase in activation of the dopamine neurons further results in activation of the post-synaptic membrane (Meyer). Which then results in the activation of the dopaminergic reward pathway. Leading to heroin’s desired effects (Meyer).





This is all made possible due to the three opioid receptors being linked to G proteins. First G protein activation opens K+ channels which increase K+ exiting the cell (Meyer). This leads to hyperpolarization of the cell. When the receptors are on the cell, the hyperpolarization decreases the cell’s firing rate of GABA (Meyer).

  • This is all made possible due to the three opioid receptors being linked to G proteins. First G protein activation opens K+ channels which increase K+ exiting the cell (Meyer). This leads to hyperpolarization of the cell. When the receptors are on the cell, the hyperpolarization decreases the cell’s firing rate of GABA (Meyer).

  • Second opiates such as heroin can have inhibitory effects by closing Ca2+ channels, when G protein receptors are on the presynaptic terminal (Meyer). Reducing Ca2+ intake during an action potential proportionately decreases the amount of inhibitory neurotransmitter released (i.e. GABA) (Meyer). Therefore increasing the amount of dopamine production and pleasure felt (Meyer).



Mechanism of Action for Pain Inhibition

  • Once heroin crosses the BBB and becomes morphine, morphine is then able to bind to the opiate receptors that trigger inhibitory spinal neurons to release endorphins (Meyer). It is these endorphins that then inhibit the spinal projection neurons from being activated. There are three ways of inhibiting spinal cord pain transmission (Meyer):

  • Directly inhibiting the projection neuron.

  • 2) Inhibiting the excitatory neuron

  • 3) Exciting the inhibitory opioid neuron, which sends out a neuron of its own when activated to inhibit the activation of the projection neuron.





It’s just not worth it!

  • Desired Effects

  • Euphoria rush

  • Decrease in anxiety

  • Reduction in pain



Excretion

  • The excretion of heroin occurs a majority of the time through the kidneys and out as urine (Hart).

  • Depending on the amount administered/frequency heroin levels in the body vary, therefore complete excretion from the body varies from days, to weeks to months.



Overdosing

  • In the events of a heroin overdose, medical professionals and in some cases law enforcement administer naloxone, commonly reffered to as Narcan.

  • Narcan acts as an antagonist and reverses the traumatic effects of a heroin overdose by competing with morphine for the opiate receptors (mostly the mu receptors) and binding to them therefore reversing the effects of heroin overdosing such as respiratory depression and sedation (Meyer).

  • It is administered via I.V., I.M. or S.C. (sub cutaneously) and is excreted through the urine within 72 hours (A.P.A) .

  • One down fall to the usage of Narcan is the onset of withdrawal symptoms for the heroin user.



Withdrawal

  • The onset of withdrawal symptoms vary among users. Typically those who use heroin once a day experience peak withdrawal effects within 36-48 hours of there last administered dose (A.P.A). Symptoms such as pain, restlessness and vomiting go away within in 7-10 days (Meyer).

  • There are several treatments for withdrawal, methadone is one of them.



Methadone

  • Methadone helps alleviate withdrawal symptoms. When taken orally it occupies opiate receptors (like heroin) (Meyer). In a sense it acts like heroin by reducing the need for more heroin, therefore causing a reduction in withdrawal side effects (Meyer).

  • It is important to note that Methadone does not provide any of the euphoric effects that heroin does when administered.



Narcan vs Methadone

  • When coming off of heroin it is best to quit “cold turkey” and seek prescribed methadone treatment. When Narcan is used opiate receptors are more rapidly deprived of opiate compared to quitting “cold turkey” (Hart).

  • However, one complication with methadone is that some individuals will begin to become addicted to methadone if it is not prescribed in adequate amounts (Meyer).



Heroin Use During Pregnancy

  • Heroin is easily made available to the unborn baby because it can cross the placenta and enter the blood stream of the baby. Most of the blood supplied to babies does not experience the first pass effect, it does not pass through the mother’s liver, and thus is more potent (Blackburn).

  • Heroin once broken into its metabolites becomes less lipid soluble and stays trapped on the fetal side of the placenta (Blackburn). There it begins to accumulate in the fetus and the amniotic fluid. (Blackburn)





The affects of Heroin on Babies

  • Heroin can cause serious complications during pregnancy including miscarriage, premature birth, decreased weight, birth defects, withdrawal symptoms (or Neonatal Abstinence Syndrome), behavioral or learning disabilities, and are at a larger risk for sudden infant death syndrome (SIDS). (March of Dimes)



Treatment for Mothers

  • Mothers who are using are encouraged to seek treatment from professional medical staff. Treatments such as methadone or minimal amounts of opiates for the baby in order to prevent withdrawal symptoms at birth (Edwards). Where as completely quitting heroin, A sudden decrease of heroin may have serious negative affects on the baby ranging from breathing complications to seizures (Edwards).



Heroin by the Numbers

  • The average heroin addict will spend $150 to $200 dollars a day to support their habit (G.D.C.A.D.A).

  • It is estimated that there were 149,000 new heroin users in 1998 with nearly 80% under the age of 26. (G.D.C.A.D.A).

  • Current estimates suggest that nearly 600,000 people in America need treatment for heroin addiction. (Heroin Addiction)

  • In the 25 to 49 age group, illicit drug overdose is the fourth leading cause of death, about the same number as motor vehicle crashes. (Heroin Addiction)



Heroin Studies and Classification

  • One study recently conducted found that addicts will find themselves overdosing on there normal dose of heroin if administered in a new environment. For more information on this study visit: http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=1196296

  • Heroin is a Schedule I drug, labeling it as one of the most easily addictive drugs (A.P.A.).

  • Animals can also become just as addicted as humans, 3 elephants were rescued from smugglers who were lacing their bananas with the drug heroin. The elephants are easily irritated and cannot return to the wild. (Telegraph.co)



Heroin Laws

  • Due to the increase in heroin use in the early 1900’s, congress passed the Harrison Act of 1924. Which made it illegal to produce, import or distribute opiates of any kind. Doctors however were allowed to prescribe them for medical issues and not addictive issues (Hodgson).

  • In New Mexico if heroin is in your possession it is considered a 4th degree felony. If found selling the drug it is considered a 2nd degree felony. However, if the selling of the drug is near a drug free school zone or is a subsequent offense it is then a 1st degree felony (JRank)

  • Most national laws include a felony offense with some jail time included. Punishments depend on the severity of heroin as a problem in the state.

  • Monetary values are placed as high as 1 million dollars and jail time up to life in prison with no parole (JRank).



Not All Exposure is Great

  • In 1999, Rio Arriba County in New Mexico led the nation in heroin related deaths per capita (NDIC).

  • To combat the amount of overdoses/deaths, the Espanola Police Department required its officers to start caring Narcan with them at all times (NDIC).

  • In addition the New Mexico Health Department began the free needle exchange and Narcan distribution for heroin users (NDIC).

  • Recently in April 2008, the New York Times featured an article/documentry regarding Rio Arriba County and its small towns struggling with heroin abuse. To read the article and view the video documentary visit:

  • http://www.nytimes.com/2008/04/02/us/02overdose.html?ref=us&pagewanted=all



Summary

  • The take home message from this presentation for the audience is three things.

  • Heroin is highly addictive which can lead to serious health issues that may even result in death.

  • The overdosing and withdrawal side effects/issues presented are the hardest part for heroin addicts and that treatment for addiction is a slow and long process that must be monitored by professionals in the medical field.

  • Although laws are continually made and enforced, Heroin continues to be one of the major pandemics of crime and drug abuse not only across the world and in America but right here in New Mexico, which is unfortunate for a state that is known as “The Land of Enchantment.”

  • If you know someone that is struggling with heroin addiction or would like more information visit Heroin Help at http://heroinhelp.com/ or call at 1.866.925.4033.



References

  • American Pharmacists Association. The Pharmacy Technician. p.40-43 Englewood. 2007.

  • Blackburn, Susan. Maternal, Fetal, and Neonatal Physiology: A Clinical Perspective. p.204-206

  • Philadelphia, 2007.

  • "Drug Addiction and Your Baby." Suite101.com: Online Magazine and Writers'

  • Network. 2007. 22 Apr. 2009 .

  • Foley, Michael. “Drug Use During Pregnancy.” Merck. May 2007. 14 Apr. 2009.

  • http://www.merck.com/mmhe/sec22/ch259/ch259a.html

  • Hart, Carl. “Drugs, Society and Human Behavior 12th Edition” p.309-328

  • Boston, MA. McGraw Hill 2008.

  • “Heroin Elephant Can Never be Freed.” Telegraph.co. 2006. 26 Apr. 2009

  • “Heroin-Facts and Statistics.” Greater Dallas Council on Alcohol and Drug Abuse.2004. 22

  • Apr. 2009

  • “Heroin Laws- Information on the law about Heroin.” JRank. 2007. 26 Apr. 2009

  • “Heroin Statistics.” Heroin Addiction 2. 2005. 22 Apr. 2009

  • www.heroinaddiction2.com.heroin-statistics.htm

  • Hodgson, Barbar. “How Aspirin Turned Hero.” 1999

  • http://www.heroin-addiction.info/history.htm

  • “Illicit Drug Use During Pregnancy.” March of Dimes Foundation. 22 Apr. 2009

  • http://www.marchofdimes.com/professionals/14332-1169.asp.

  • Meyer, Jarold. “Psychopharmacology: Drugs, The Brain and Behavior.” p.247-269

  • Sunderland, MA. Sinauer Assoc. Inc. 2005.

  • “New Mexico Drug Threat Assessment.” NDIC. April 2002. 27 Mar. 2009.

  • http://www.usdoj.gov/ndic/pubs07/803/heroin.htm

  • “The mechanism of action of heroin at the mu (m) opiate receptors.” CNSForum. 2005. 14 Apr. 2009

  • http://www.cnsforum.com/imagebank/item/moa_heroin_mu/default.aspx




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