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| - | =======Opioid Powerpoint======= | + | =======Opioids Powerpoint======= |
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| ====== Opioids ====== | ====== Opioids ====== | ||
| - | Opioids can be traced back to the Sumerian people who occupied what is modern day Iraq (Brownstein 1993). They were able to cultivate the therapeutic properties of poppy seeds, and called the drug “gil” which means joy, and the poppy plant “hul gil” which translates to plant of joy (Brownstein 1993). The drug was used for multiple purposes, including: preventing children from excessive crying, providing people who were suffering a quick and painless death and as a euphoric agent in religious ceremony, whether it was inhaled or ingested (Brownstein 1993). Historical documents show that as early as the 10th century, opium was being brought over to Europe from the middle east, and by the 16th century drug abuse and addiction was rampant in countries such as England, Germany, and Turkey (Brownstein 1993). By the early 1800s, a chemist named Serturner was able to isolate the active ingredient in opium, which was called Morphine after the God of dreams, Morpheus. Since this time, scientists have been constantly trying to find new, stronger forms of the drug. The one that has been most commonly talked about as of late is known as Fentanyl. | + | Opioids can be traced back to the Sumerian people who occupied what is modern day Iraq (Brownstein, 1993). They were able to cultivate the therapeutic properties of poppy seeds, and called the drug “gil” which means joy, and the poppy plant “hul gil” which translates to plant of joy (Brownstein, 1993). The drug was used for multiple purposes, including: preventing children from excessive crying, providing people who were suffering a quick and painless death and as a euphoric agent in religious ceremony, whether it was inhaled or ingested (Brownstein, 1993). Historical documents show that as early as the 10th century, opium was being brought over to Europe from the middle east, and by the 16th century drug abuse and addiction was rampant in countries such as England, Germany, and Turkey (Brownstein, 1993). By the early 1800s, a chemist named Serturner was able to isolate the active ingredient in opium, which was called Morphine after the God of dreams, Morpheus. Since this time, scientists have been constantly trying to find new, stronger forms of the drug. The one that has been most commonly talked about as of late is known as Fentanyl (Brownstein, 1993). |
| ===== Fentanyl ===== | ===== Fentanyl ===== | ||
| - | Fentanyl is a drug that sits within the opioid group. It is considered to be anywhere from 40-100 times more potent than heroin, and subsequently requires a much smaller amount to cause adverse effects to an individual. In New York alone in 2016, 44% of drug related deaths were a due to fentanyl overdose. The worst part is, most of these people did not even know they were taking the drug. | + | Fentanyl is a synthetic opioid that is 50-100 times more potent than morphine (Fentanyl, 2016). It is an analgesic, meaning that it works to relieve pain. It was invented in the 1960’s to treat chronic pain, particularly in patients with terminal cancer. It was also used as an anaesthetic for individuals going through intense surgery such as cardiac bypass surgery. Fentanyl was a better alternative to morphine which as used at the time, because it provided greater relief from pain and reduced the risk for respiratory depression, which is a leading cause of death from opioid use. The effects include: euphoria, drowsiness, nausea, confusion, sedation and warmth (Fentanyl, 2016). |
| - | + | ||
| - | Fentanyl was a breakthrough drug invented in the 1960s to treat patients with chronic pain, (specifically with terminal cancer) as well as an anesthetic for individuals going through intense survey (like heart bypass surgery, for example) (Stanley 1992). Fentanyl was a better alternative to morphine because unlike morphine, it did not bind to oxygen. Scientists were struggling with this, as the binding of oxygen to the opioid in the body would lead to only partial anesthesia and occasionally respiratory depression (Stanley 1992). Fentanyl does cause respiratory depression if taken in large enough doses as the leading cause of death from overdose is asphyxiation (Stanley 1992). Although fentanyl is an extremely potent and dangerous substance, if used under the right supervision and care it can be very beneficial to those who need it. | + | |
| <box 40% round | > {{ :screen_shot_2018-03-01_at_5.32.09_pm.png?200 |}} </box| Figure 1: | <box 40% round | > {{ :screen_shot_2018-03-01_at_5.32.09_pm.png?200 |}} </box| Figure 1: | ||
| Chemical structure of fentanyl. Visibly different then morphine, but will act on the same receptors in the brain. http://www.chemspider.com/Chemical-Structure.3228.html > | Chemical structure of fentanyl. Visibly different then morphine, but will act on the same receptors in the brain. http://www.chemspider.com/Chemical-Structure.3228.html > | ||
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| ==== Pain ==== | ==== Pain ==== | ||
| - | Pain is subjective and is perceived through a combination of both sensory information and psychological (emotional) experiences (Chahl, 1996). Pain is experienced when mechanical or thermal stimuli causes an increased activity in the primary sensory neurons (Chahl, 1996). These neurons result in the release of excitatory neurotransmitters in the dorsal horn of the spinal cord, which sends a signal to the central nervous system (Chahl, 1996). Opioids main action is to inhibit the release of the neurotransmitters at the dorsal horn, in order to reduce the perception of pain (Chahl, 1996). | + | Pain is subjective, however it is generally defined as an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage (Chahl, 1996). It is perceived through a combination of sensory and psychological experiences. Pain is experienced when mechanical or thermal stimuli cause increased activity in the primary sensory neurons. This is accompanied by the release of excitatory neurotransmitters in the dorsal horn of the spinal cord, which sends a signal to the central nervous system to indicate pain. The main action of opioids is to inhibit the release of the neurotransmitters at the dorsal horn of the spinal cord to reduce the perception of pain (Chahl, 1996). |
| ==== Opioid Receptors ==== | ==== Opioid Receptors ==== | ||
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| ====== Adverse Effects of Opioid Use ====== | ====== Adverse Effects of Opioid Use ====== | ||
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| - | <box 25% round right | > {{ :screen_shot_2018-03-02_at_8.00.49_pm.png?200|}} </box| Figure 3: Opioid receptors in GI tract. http://slideplayer.com/slide/11681545/ > | ||
| There are various adverse effects associated with long term use of opioids (Voon, Karamouzian & Kerr, 2017). These effects have been shown to target the gastrointestinal, cardiovascular, respiratory and central nervous systems (Voon, Karamouzian & Kerr, 2017). With regards to the gastrointestinal system, constipation is a prevalent effect of chronic opiate therapy (Khansari, Sohrabi & Zamani, 2013). This process depends on the stimulation of μ and κ opioid receptors in the gastrointestinal tract. Studies show that 40-45% of patients on opiate therapy experience constipation. Treatment involves the use of stool softeners and laxatives, which is not always effective. In some cases, constipation can be so severe that patients reduce their medication dosage or discontinue opiate use altogether (Khansari, Sohrabi & Zamani, 2013). | There are various adverse effects associated with long term use of opioids (Voon, Karamouzian & Kerr, 2017). These effects have been shown to target the gastrointestinal, cardiovascular, respiratory and central nervous systems (Voon, Karamouzian & Kerr, 2017). With regards to the gastrointestinal system, constipation is a prevalent effect of chronic opiate therapy (Khansari, Sohrabi & Zamani, 2013). This process depends on the stimulation of μ and κ opioid receptors in the gastrointestinal tract. Studies show that 40-45% of patients on opiate therapy experience constipation. Treatment involves the use of stool softeners and laxatives, which is not always effective. In some cases, constipation can be so severe that patients reduce their medication dosage or discontinue opiate use altogether (Khansari, Sohrabi & Zamani, 2013). | ||
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| + | <box 35% round right | > {{ :screen_shot_2018-03-02_at_8.00.49_pm.png?350|}} </box| Figure 3: Opioid receptors in GI tract. http://slideplayer.com/slide/11681545/ > | ||
| Long term use of opioid therapy has been shown to have deleterious effects on the cardiovascular system (Chen & Ashburn, 2015). When the use of opioid therapy was compared to Nonsteroidal anti-inflammatory drugs (NSAIDs) and selective cyclooxygenase-2 (COX-2) inhibitors, opioid therapy was associated with a 77% increased risk of cardiovascular effects such as heart failure and myocardial infarction (MI) (Voon, Karamouzian & Kerr, 2017). After 30 days, the risk of cardiovascular events was similar across different opioid medications. However, after 180 days of therapy, codeine was associated with a 62% increase in adverse events when compared to hydrocodone (Voon, Karamouzian & Kerr, 2017). Furthermore, studies have shown an increased risk of MI among patients on chronic opioid therapy relative to the general population (Chen & Ashburn, 2015). | Long term use of opioid therapy has been shown to have deleterious effects on the cardiovascular system (Chen & Ashburn, 2015). When the use of opioid therapy was compared to Nonsteroidal anti-inflammatory drugs (NSAIDs) and selective cyclooxygenase-2 (COX-2) inhibitors, opioid therapy was associated with a 77% increased risk of cardiovascular effects such as heart failure and myocardial infarction (MI) (Voon, Karamouzian & Kerr, 2017). After 30 days, the risk of cardiovascular events was similar across different opioid medications. However, after 180 days of therapy, codeine was associated with a 62% increase in adverse events when compared to hydrocodone (Voon, Karamouzian & Kerr, 2017). Furthermore, studies have shown an increased risk of MI among patients on chronic opioid therapy relative to the general population (Chen & Ashburn, 2015). | ||
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| ==== Pain Management ==== | ==== Pain Management ==== | ||
| - | Pain is often inadequately addressed and managed in patients, which can in part be attributed to hesitation to employ the use of opioids, including fentanyl, stemming from fear that they will be abused. Fentanyl is utilized for the relief of severe chronic pain (such as pain associated with cancer). This drug operates in the brain to modulate how the body feels and responds to pain (Joranson et al., 2000). This can be achieved through the forms of transdermal patch and intravenously. The patch form of fentanyl should only be used when absolutely required, and not used in cases of mild pain or pain that is short-term. Fentanyl is not suited for occasional or “as needed” use. It may take up to 24 hours before a patient experiences pain relief from fentanyl patches. The patch is usually changed every 72 hours (Joranson et al., 2000) (“Fentanyl Transdermal”, 2018). | + | Pain is often inadequately addressed and managed in patients, which can in part be attributed to hesitation to employ the use of opioids, including fentanyl, stemming from fear that they will be abused (Joranson et al., 2000). Fentanyl is utilized for the relief of severe chronic pain (such as pain associated with cancer). This drug operates in the brain to modulate how the body feels and responds to pain (Joranson et al., 2000). This can be achieved through the forms of transdermal patch and intravenously (Joranson et al., 2000). The patch form of fentanyl should only be used when absolutely required, and not used in cases of mild pain or pain that is short-term (“Fentanyl Transdermal”, 2018; Joranson et al., 2000). Fentanyl is not suited for occasional or “as needed” use. It may take up to 24 hours before a patient experiences pain relief from fentanyl patches. The patch is usually changed every 72 hours (“Fentanyl Transdermal”, 2018; Joranson et al., 2000). |
| - | Intravenously, fentanyl is distributed under the name Sublimaze. It is mainly used for pain management prior to surgery and pain relief after medical procedures. This is always administered by health care professional. The usual dosage is 50 to 100 micrograms (1 to 2 mL) and is given intramuscularly. In elderly and poor-risk patients, a lesser dose of 25 to 50 micrograms (0.5 to 1mL) is recommended. The dose may be re-administered every one to two hours if required (Janssen, 2014). Dosage should of course be adjusted based on each patient’s individual needs, and some of the factors that are used to determine dose are: age, body weight, physical status, underlying pathological condition, use of other drugs, type of anaesthesia, and type of surgical procedure. Due to the many potential side effects, health care professionals monitor patients closely and regularly evaluate vital signs after administering this drug. | + | Intravenously, fentanyl is distributed under the name Sublimaze (Janssen, 2014). It is mainly used for pain management prior to surgery and pain relief after medical procedures. This is always administered by health care professional. The usual dosage is 50 to 100 micrograms (1 to 2 mL) and is given intramuscularly. In elderly and poor-risk patients, a lesser dose of 25 to 50 micrograms (0.5 to 1mL) is recommended. The dose may be re-administered every one to two hours if required. Dosage should of course be adjusted based on each patient’s individual needs, and some of the factors that are used to determine dose are: age, body weight, physical status, underlying pathological condition, use of other drugs, type of anaesthesia, and type of surgical procedure. Due to the many potential side effects, health care professionals monitor patients closely and regularly evaluate vital signs after administering this drug (Janssen, 2014). |
| ==== Emergence Delirium and Relaxation ==== | ==== Emergence Delirium and Relaxation ==== | ||
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| ====== Recreational Use of Opioids ====== | ====== Recreational Use of Opioids ====== | ||
| - | Fentanyl is a drug that has a massive abuse potential. Any individual who uses fentanyl that does not have a previous tolerance to opioids is largely at risk. Many first-time recreational users of fentanyl are in drastic danger of overdose. Fentanyl is highly addictive and addictions often develop quickly, which is why prescription fentanyl is so closely monitored by physicians (Lautieri, 2016). Fentanyl has an extreme potency, and is much stronger than other opioids including morphine and oxycodone. On the street, fentanyl often replaces the selling of high-grade heroin (also known as as "China White), and mixed into heroin to magnify the high (Lautieri, 2016). Fentanyl is now frequently being incorporated into other street drugs to elevate potency and addictiveness. Recreational users often consume fentanyl seeking the short-term effects of pain relief, euphoria, and relaxation. Shockingly, over the last decade, the access to recreational drugs, including fentanyl, over the internet has significantly grown and only become easier (Cunningham et al., 2015). According to Cunningham et al. (2015), in a toxicological analysis of a deceased individual by the cause of fentanyl overdose revealed fentanyl concentrations in blood, liver, vitreous fluid, and urine of respectively 235 ng/mL, 2400 ng/g, 131 ng/mL, and 234 ng/mL, which is colossally greater than medical dosing. | + | Fentanyl is a drug that has a massive abuse potential. Any individual who uses fentanyl that does not have a previous tolerance to opioids is largely at risk. Many first-time recreational users of fentanyl are in drastic danger of overdose. Fentanyl is highly addictive and addictions often develop quickly, which is why prescription fentanyl is so closely monitored by physicians (Lautieri, 2016). Fentanyl has an extreme potency, and is much stronger than other opioids including morphine and oxycodone. On the street, fentanyl often replaces the selling of high-grade heroin (also known as as "China White), and mixed into heroin to magnify the high (Lautieri, 2016). Fentanyl is now frequently being incorporated into other street drugs to elevate potency and addictiveness. Recreational users often consume fentanyl seeking the short-term effects of pain relief, euphoria, and relaxation. Shockingly, over the last decade, the access to recreational drugs, including fentanyl, over the internet has significantly grown and only become easier (Cunningham et al., 2015). According to Cunningham et al. (2015), in a toxicological analysis of a deceased individual by the cause of fentanyl overdose revealed fentanyl concentrations in blood, liver, vitreous fluid, and urine of respectively 235 ng/mL, 2400 ng/g, 131 ng/mL, and 234 ng/mL, which is significantly greater than medical dosing. |
| ====== Drug Cutting ====== | ====== Drug Cutting ====== | ||
| - | Drug cutting refers to the addition of different solvents to a pure drug product in order to either reduce the cost of drug production or increase the potency of the drug. The materials added to the drug include baking soda, rat poison as well as other drugs such as fentanyl. Additives such as baking soda and rat poison are used to dilute the product which increases profit for the drug seller. The addition of other drugs such as fentanyl is used to increase the potency of the drug, which increases consumer appeal. | + | Drug cutting refers to the addition of different solvents to a pure drug product in order to either reduce the cost of drug production or increase the potency of the drug (Fentanyl, 2016). The materials added to the drug include baking soda, rat poison as well as other drugs such as fentanyl. Additives such as baking soda and rat poison are used to dilute the product which increases profit for the drug seller. The addition of other drugs such as fentanyl is used to increase the potency of the drug, which increases consumer appeal (Fentanyl, 2016). |
| ==== Drug Trade and Trafficking of Opioids ==== | ==== Drug Trade and Trafficking of Opioids ==== | ||
| - | The “Beekeeper” was considered one of the Canada's most dangerous chemists for many years. He was well known for creating many synthetic opioids such as fentanyl. | + | The “Beekeeper” was considered one of the Canada's most dangerous chemists for many years (CBC, 2017). He was well known for creating many synthetic opioids such as fentanyl (CBC, 2017). |
| <box 50% round | > {{youtube>2NCofLChqU8?medium}} </box| Video: One of Canada’s most prolific chemists, The Beekeeper. > | <box 50% round | > {{youtube>2NCofLChqU8?medium}} </box| Video: One of Canada’s most prolific chemists, The Beekeeper. > | ||
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| Naloxone is a lipophilic compound that acts as a non-selective, competitive opioid receptor antagonist. The pharmacologically active isomer in naloxone is (-) naloxone, its binding affinity is highest for mu-opioid receptors. Naloxone has a higher binding affinity for the opioid receptor compared to opioids like fentanyl which is what makes it such an effective treatment (Dowling et al., 2008). | Naloxone is a lipophilic compound that acts as a non-selective, competitive opioid receptor antagonist. The pharmacologically active isomer in naloxone is (-) naloxone, its binding affinity is highest for mu-opioid receptors. Naloxone has a higher binding affinity for the opioid receptor compared to opioids like fentanyl which is what makes it such an effective treatment (Dowling et al., 2008). | ||
| - | <box 30% round | > {{ :screen_shot_2018-03-02_at_9.15.46_pm.png?300|}} </box| Figure 9: Naloxone mode of action (Dowling et al., 2008) > | + | <box 40% round | > {{ :screen_shot_2018-03-02_at_9.15.46_pm.png?400|}} </box| Figure 9: Naloxone mode of action (Dowling et al., 2008) > |
| Naloxone only acts on opioid receptors, so it will not help with drug overdoses that are not opioids since they do not use the same receptors within the body. If naloxone is administered by itself, it will not cause an effect on the individual due to it being an antagonist (Filizola & Devi, 2012). It will, however, cause the body to not be able to combat pain naturally. The mechanism is not completely understood but researchers believe it is a competitive antagonist because it prevents the action of both endogenous and xenobiotic opiates on the opioid receptors while not producing any effects itself (Sauro & Greenberg, 2018). | Naloxone only acts on opioid receptors, so it will not help with drug overdoses that are not opioids since they do not use the same receptors within the body. If naloxone is administered by itself, it will not cause an effect on the individual due to it being an antagonist (Filizola & Devi, 2012). It will, however, cause the body to not be able to combat pain naturally. The mechanism is not completely understood but researchers believe it is a competitive antagonist because it prevents the action of both endogenous and xenobiotic opiates on the opioid receptors while not producing any effects itself (Sauro & Greenberg, 2018). | ||
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| Naloxone has no effect on the body if no opioids are present because it binds to the body’s natural opioid receptors. It has been shown to have common side effects with individuals who have opioids in their body which include flushing, dizziness, tiredness, weakness, nervousness, restlessness, fever, nausea, chills, shortness of breath seizures and death. Naloxone has also been shown to block the body’s natural pain lowering endorphins. It is thought that naloxone acts on the same receptors that these endorphins operate on (Cunha, 2016). | Naloxone has no effect on the body if no opioids are present because it binds to the body’s natural opioid receptors. It has been shown to have common side effects with individuals who have opioids in their body which include flushing, dizziness, tiredness, weakness, nervousness, restlessness, fever, nausea, chills, shortness of breath seizures and death. Naloxone has also been shown to block the body’s natural pain lowering endorphins. It is thought that naloxone acts on the same receptors that these endorphins operate on (Cunha, 2016). | ||
| - | + | ====== Conclusion ====== | |
| + | |||
| + | Opioids are substances which act on opioid receptors in the body to relieve pain (Voon, Karamouzian & Kerr, 2017). While these drugs have beneficial uses for the relief of chronic pain they have massive abuse potential (Voon, Karamouzian & Kerr, 2017). The abuse of these drugs has lead to an increase in opioid overdosing, particularly in Canada (Fentanyl, 2016). In Ontario there were 336 opioid related deaths from May to July 2017 and 2449 emergency room visits due to overdosing from July to September 2017. Any individual that is using prescribed or street opioids is at risk of having an overdose, however most individuals overdose because they are using street drugs which are laced with potent substances. Street drugs laced with opioids such as fentanyl and carfentanil can be particularly dangerous because they can be fatal even in very small amounts. Individuals using opioids can reduce their risk of overdose by not using the drugs alone and having a naloxone kit available (Fentanyl, 2016). | ||
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| + | Moving forward, there is a need for more research on problematic substance use in order to identify ways to mitigate the problem (Fentanyl, 2016). Furthermore, the public needs to be educated on the use of opioids and other legal and illegal drugs (Fentanyl, 2016). | ||
| - | ===== References ===== | + | ====== References ====== |
