Opiates 1 Flashcards
What are opiates?
Opiates are naturally-occuring alkaloids found in the
sap of the opium poppy. Dozens of opiates -
the most important
psychoactive ones are
morphine and codeine. Raw opium contains 10% morphine and 0.5% codeine. Also have thebaine.
Why are these compounds produced in nature?
Opiate (alkaloid) synthesis is metabolically ‘expensive’. Takes lots of nutrition to create these compounds. May have similar functions as cocaine and nicotine in serving as insecticides.
What is the history for use and abuse for opium?
One of the oldest recorded psychoactive substances. Score the sides of the poppy and after a while collect it dried = opium. Contains different alkaloids e.g. morphine and codeine. One of the main medicinal uses of opioid related procedures is being used as an analgesic.
How is raw opium taken?
Raw opium is usually spoked. The Opium/Anglo-Chinese wars - British tried to take control of the opium market. China was the main place where opium was cultivated. Massive problem of opium use in China, partly what led to opium wars (as the government banned it). You can either eat or smoke raw opium. The main effect opioids have is it produces a ‘dream-like’ state. The Dutch involved in opium
trade from 1613 to 1942, and during the 19th century even under a state-sponsored monopoly.
In 1928, use of opium and other narcotic drugs was banned in the Netherlands, but opium trade in Dutch East Indies (i.e., Indonesia) remained outside of these regulations.
Where is opium mainly produced?
Modern day production is mostly in Afghanistan. Metric tons of opium being produced - see a dip in 2001 during the Taliban rule. When U.S. NATO groups invaded, see a steady increase. Past 2018 there has been a massive increase in production in Afghanistan. There is the Golden crescent of production (Iran, Afghanistan, and Pakistan), and the golden triangle of production (Burma, Vietnam, Thailand, and Laos). Some production in Colombia and Mexico, but not much - more distribution.
What is the history of abuse?
Morphine named after Morpheus, Greek god of dreams. Opiates don’t induce sleep - they induce a sleepy, dream-like sensations: feeling of enhanced imagination and well-being, also lethargy.
Why did the US consumption of opiates expand in the late 1800s?
3 reasons: it was difficult to ship raw opioid sap. In Western Europe and US it wasn’t common until realised that you can extract morphine from raw opium (can dissolve into solution). Also the invention of the hypodermic needle - now have a vessel for administering, in a way to produce an optimal effect. The third factor is the Civil War - can be injected in any location, large amount of people getting injured (analgesic effects).
What are medicinal opiates?
Poppy extracts have been used as medicine throughout recorded history. A lot of drugs were marketed for kids. Primarily for pain, also for diarrhoea, coughing. Also used as poison (e.g. fentanyl used in terrorist attacks). Laudanum - a paregoric (weaker form of opium). In the US it was available over the counter until 1914.
What is heroin?
A semi-synthetic opioid. Marketed as a safe replacement for opium. Illegal since 1924. Different forms you can get in terms of purity - the problem is varied types of preparation is spiked with different things, e.g. fentanyl. Heroin is morphine with two acetyl groups to it, which means it goes to your brain faster (increases lipid solubility, and means its 5x more potent than morphine). Heroin is converted to morphine in the brain (but this is not the whole story).
What is the development of a rational scale to assess the harm of drugs of potential misuse?
Nutt former chief advisor to the UK government for drug advisory committee. Compared physical harm to the likelihood that it produces dependency. Physical harm and dependency measured on a scale of 0-3. Heroin marked as one of the most harmful drug for physical harm to the person (in particular in relation to overdose) and dependency. Category A in the UK, Schedule I in the US (morphine is Schedule II). In the UK, heroin is a legal prescription drug (diamorphine).
What is fentanyl?
Fentanyl – synthesised 60/70 years ago, some abuse and presence on the street, but become much more common to find. Full synthetic – only need a lab and some basic ingredients. The heroin that people buy is often laced with fentanyl. If heroin is a more potent version of morphine, then fentanyl is a much more potent version of heroin. Very small mistakes in dose can be lethal. 80 x more potent than morphine in most of its effects.
What are different types of opiates and opioids?
Natural narcotics - morphine, codeine, thebaine.
Semisynthetic narcotics - heroin, hydromorphine, oxycontin, etorphine.
Totally synthetic narcotics - fentanyl, LAAM.
Also have competitive agonists - naloxone and naltrexone (longer-lasting version). Used to treat overdoses. In presence as opioid acts as a competitive antagonist – fighting for the same receptor.
How do opioids differ in terms of their analgesic properties?
For mild to moderate pain use codeine of propoxyphene (Darvon). For moderate to severe pain use meperidine/pethidine (Demerol). For severe pain use heroin or hydromorphone (Dilauded). Heroin or fentanyl. Often used in patches because of risk of overdose. Give different opioids depending on what you’re trying to do (e.g. what type of pain you’re trying to treat).
What are medications containing opiates?
Medications contain morphine, codeine or heroin (diamorphine). e.g. take codeine tablets to treat a really bad cough.
Why are abuse of prescription opioids a big problem?
OxyContin famously abused. Marijuana is the most commonly used illict drugs. Vicadin (cough medicine i.e. codeine) high on use of illicit drugs. People then convert into other opioids e.g. heroin or fentanyl when their prescription is stopped. Death due to opioids overdose – prescriptions are contributing in a major way to overdoses, to a much greater extent than heroin. Its fuelling a spike in heroin abuse and other type of opioids seen on the streets. The amount of overdoses have increased since 2014.
