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Category Archives: Pharmacology of Addiction
Marijuana – Understanding Addiction
Hallucinogens – Understanding Addiction
Opioids and Opiates – Understanding Addiction
- Opioids are naturally occurring substances derived from the opium poppy. They have a long history of medicinal use.
- Opium delivers pleasure and relieves pain and anxiety. This is what makes it so popular in medical and recreational use.
- Papaver somniferum produces opium for only 7 to 10 days a year. All opioids are derived from this.
- As far back as 1500BC the medical use of opium is on record. Galen, a Greek physician, emphasized caution in the use of opium but felt it was a cure all.
- Because of the dark ages the Arabic world is credited for bringing opioids to the world. The Arabian world started to trade with India and China.
- Arabic civilization prospered and made grand contributions to medicine and history of opium.
- Biruni, an Arabic physician, wrote about opioid dependence in 1000AD. At the same time Avicenna, an Arabic physician as well, used opium extensively in medical practice. His work, along with Galen’s work set the base for medical education in Europe.
- By the 10th century opium was integrated into Chinese medicine.
- In Europe a phenomenon named Paracelsus was a successful doctor who praised what he labeled the “stone of immortality”.
- Dr. Thomas Sydenham, who was called the English Hippocrates, believed that without opium medicine would not be.
- In 1805 writer Tomas De Quincey had a toothache and was given laudanum. From that point he continued to take it and did not try to hide his opium use. He wrote “The Confessions of an English Opium-Eater,” and gave insight into opium. He enjoyed it so much he continued to use opium until his dependence on it made him unable to write.
- China was introduced to opium before 1000 AD but it did not come into favor except for the elite.
- When there was a ban on tobacco, opium use went up in China.
- The first law against opium smoking, called for opium shop owners to be strangled.
- Once opium was outlawed it was smuggled in from India. This started the road to the Opium wars.
- Many countries wanted to trade with China but China did not want to. Under pressure, the port of Canton was opened but with very strict rules for foreigners. While tea was the major export opium, thou illegal, was the primary import. In 1839, the emperor of China sent a representative to deal with the opium problem. He did and destroyed 20,000 British chests of opium, about $6 million worth, and sent the British merchants free. Then drunken American and British sailors killed a Chinese citizen starting the Opium Wars in 1839.
- The British army arrived 10 months later and won within two years. China lost Hong Kong to Great Britain and had to reimburse the merchants the $6 million whose opium was destroyed as well as give the British broader trading rights.
- In 1805, Frederich Serturner isolated the primary active ingredient in opium. He named it morphium.
- Use of this new opioid, that is 10 times stronger then opium, did not happen until 1831 when the medical use of morphine had become so powerful.
- In 1832 another alkaloid was isolated named codeine.
- The hypodermic syringe and war helped morphine. With the hypodermic syringe, morphine was delivered into the blood stream or tissue getting a faster reaction from the drug. Military medicine is about fast reactions. The American Civil War, the Prussian-American War and the Franco-Prussian War put morphine into many soldiers.
- Many came back dependent on morphine and the illness was called “soldier’s disease” or the “army disease”.
- In 1874, heroin was developed by adding two acetyl groups to morphine.
- This chemical change made heroin easier to pass through the brain barrier, making it three times stronger then morphine.
- Heroin and morphine effects are the same except that the reaction comes faster with heroin and it is more potent.
- Heroin was marketed as a non-habit-forming substitute for codeine. Heroin was later found to be habit forming
- There were three types of opioid dependence developing at the end of the 19th century: oral intake of opium, opium smoking and injection morphine.
- By the start of the 20th century, more Americans were dependent on one or more of the opioids. No real statistics are available but it is thought that 1% of the population was dependent.
- In 1880 the typical opioid user was a white woman between 30-50 years old. She would buy opium or morphine at the local store.
- After the 1914 Harrison Act, many laws were passed that effecedt people dependent on opioids.
- In 1915 possession of smuggled opioids became a crime. Users could still get their supply from their doctor until 1919 when that was outlawed.
- Even when a new law opened the avenue back up in 1925, most doctors chose not to prescribe opioids.
- For this and other reasons opioids became expensive on the black market.
- More and more people chose to injected morphine so they could get the most for their money.
- After World War II fewer stay-at-home moms were using, as were more entertainers and musicians, thieves and pickpockets, and pimps.
- In the 1960’s the use of heroin increased as did the use of other drugs.
- Heroin was very cheep and easy to get in Vietnam. Some estimates are that 10 to 15 % of American troops in Vietnam were dependent on heroin.
- Operation Golden Flow was used to test solders for use. What they found was that when the solders got back to the US few went back to using. This exemplified the belief that if drugs were cheap and readily available and people were bored, then the chance that a person will use is high.
- The US spent $35 million in 1972 on Turkey to make up for destroyed crops and helped develop new cash crops. This and a cooperative effort with France helped take a large percentage of heroin off the streets.
- By 1975 the shortage of heroin was over because Mexican black tar was plentiful and cheap.
- Currently it is estimated that the majority of illicit heroin comes from South America. The purity of the street product is better from South America (46%) then from Mexico (27%) and there is not much of a price difference.
- Opioids have long been used for there pain killing effects.
- Opioid antagonists were being developed to help block the action of morphine, heroin and other drugs. In the early 1970’s, opioid receptors (that were long believed to be there) were found in the synapses of the brain.
- Enkephalins are naturally found in the brain. They act like morphine but are more potent. Endorphins were also detected to have opioid-like effects.
- Pain relief is the most common medical use of opioids.
- Morphine reduces the emotional response to pain and diminishes the patient’s awareness of and response to the aversive stimulus.
- Opioids also help with intestinal disorders. They counteract diarrhea and help with colic.
- As a cough suppressants codeine is very helpful. In the form of Dextromethorphan it is available over the counter. At high doses hallucinogenic effects are seen.
- Opioids have a large dependence potential.
- Tolerance comes on relatively quick so an increased amount of the drug is needed for both medical and recreational results once tolerance is reached.
- There is a high-cross tolerance potential within all opioids.
- Physical dependence is also seen with opioids.
- The time needed to become dependent on opioids depends on the amount used and for how long.
- Psychological Dependence is easy to see through opioids positive reinforcement interaction.
- Once physical dependence is set negative reinforcement is seen in not using; thus making it had to stop using.
- There is a high toxicity potential of opioids.
- Acute toxicity leads to depressed respiratory action. This is a very deadly reaction.
- Chronic toxicity was believed to make the user weak but there has been no scientific evidence of harm to the organ systems. The largest chronic effect is that it takes more and more drug to get the effect and with that, overdose becomes more common.
- Due to the short-lived reaction of the drug, many people dependant on opioids must take the drug many times a day. For this, the sheer time needed to find and take the drug is great.
- Not to mention the cost on the addiction. Not only to you have to consider the cost of the drug but also the cost of the paraphernalia needed to use the drug.
- There are many misconceptions and preconceptions in opioid use. Many believe that each time a person mainlines they get a feeling of a whole body orgasm. This is not the case for most. While they might have that feeling the first time they use, all subsequent uses are not as intense. Others only feel nausea and discomfort the first time.
- Another misconception is that if you try heroin once, you are hooked for life. No drug fits that mold. All dependence takes time to develop.
- Remember: No drug can have an effect until it enters the body. Don’t take that first step.
Tobacco – Understanding Addiction
- Tobacco was one of the main things that Europe got from the New World, along with chocolate, sweet potatoes and corn.
- Tobacco was used in two forms: snuff and smoked.
- Tobacco had many early medical uses: from treating headaches to the common cold and other ailments of the time.
- There are two main different types of Nicotiana: Nicotiana tobacum and Nicotiana rustica. In Virginia, tobacum was found to grow well and became the colony’s main product in 1612.
- Tobacco played a large role in the war. From money to trade, tobacco was the turning point.
- The method for administering nicotine also changed. It went from snuff to smoking and chewing.
- The regulation of tobacco happened as early as 1604 by King James of England. While he published anti-tobacco information, he supported the growth of tobacco in Virginia.
- In 1908 New York made it illegal for women to smoke in public.
- In the 1930’s and 40’s reports of health risks came out. A 1952 Readers Digest printed “Cancer by the Carton”.
- Filtered cigarettes were starting to be looked at as alternatives and marketed to make sure that everyone knew original cigarettes were “safe”.
- “Safer” cigarettes were filtered and lower in tar. They were looked at as safer but not safe cigarettes.
- Cigarettes makers looked at delivery devices that were even safer. The problem became that if they went in a particular direction cigarettes were no longer a food and then would be regulated as a drug. The companies stopped looking at the devices and looked toward less-smoke or smokeless cigarettes.
- Smokeless tobacco became a popular alternative in the 1970’s due to the rising risks of lung cancer.
- Once thought of as something just cowboys did, chewing tobacco grew until it became a public concern. There are two different types of chew: loose-leaf and moist snuff.
- Though chewing tobacco was not as unhealthy as smoking it, chewing tobacco still had risks. An increased risk of cancer of the mouth, pharynx, and esophagus as well as leukoplakia and other dental problems came with chewing tobacco.
- There are a lot of causes for concern with the adverse health effects of tobacco. There are effects of tobacco without smoking the tobacco itself such as environmental tobacco smoke, sidestream smoke, passive smoke and even mainstream smoke.
- There are effects on children of people who smoke. They include low birth weight and Sudden Infant Death syndrome.
- Nicotine is a liquid alkaloid that is colorless and volatile. Tolerance develops quickly as dose-dependence on nicotine.
- When smoked, 90% of inhaled nicotine is absorbed.
- A lethal dose of nicotine is 60mg; death would follow quickly.
- Enzymes in the liver help with the deactivation of nicotine in the body.
- The elimination of deactivated nicotine is slowed by nicotine itself because of its affects on thehypothalamus.
- Effects on the central nervous system by nicotine mimics acetylcholine.
- With the continued occupation of receptors, nicotine blocks the transmission of information at the synapse while stimulating it.
- Some of these receptors are found in the skin, tongue and large arteries. Nausea, dizziness and feeling of illness are all the feeling of a person’s first smoke. These are also the symptoms of low-level nicotine poisoning.
- With acute poisoning, the cause of death is suffocation from paralysis of the respiratory muscles. Another negative effect of nicotine is that it increases the tendency of the blood to clot.
- Monotonous of the taste buds and a slight increase in blood sugar might be the basis for a decrease in hunger after smoking.
- Regular smokers will have high levels of carboxyhemoglobin in their blood decreasing the oxygen-carrying ability of blood.
- Nicotine is the driving force in tobacco that reinforces behavior. Nicotine dependence was reinforced by the 1988 surgeon general’s report that stated that:
- Cigarettes and other forms of tobacco are addicting.
- Nicotine is the drug in tobacco that causes the addiction.
- The pharmacological and behavioral processes that determine tobacco addiction are similar to those that determine addiction to drugs such as heroin and cocaine.
- Most new research is focused on the fact that nicotine affects dopamine.
- There is a large reduction in one type of MAO in the brains of chronic nicotine smokers. This slows the breakdown of dopamine henceforth enhancing the effect of the dopamine released by each nicotine dose.
- Smoking is extremely hard to quit. One reason might be the pure number of hits a pack-a-day smoker gets;annually hits total over 50,000.
- Most can quit smoking for a few days but 70 to 80 percent will be smoking again in six months.
- There are also drugs to help people quit. Gum, and skin patches as well as pills are now available to help someone quit smoking.
Medications for Mental Disorders – Understanding Addiction
- The look and treatment of mental illness has changed over the years. Currently the main method of therapy is drug therapy.
- Using this approach: the patient shows symptoms, they are diagnosed, and then treated with drugs. Others believe that this just covers the problem.
- The Diagnostic and Statistical Manual of Mental Disorders provides criteria for classifying mental disorders to hundreds of specific diagnostics. The DSM V is expected in 2013.
- Many insurance companies use these definitions. DSM sets the standards for health
- Anxiety disorders include:
- panic disorders
- specific phobias
- generalized anxiety disorder
- They are commonly treated with benzodiazepines and otherdepressants.
- Psychosis is a major loss of contact with reality. People suffering from a long-term psychotic condition with no known cause are diagnosed with Schizophrenia.
- “Malaria therapy” was used to treat general paresis when they say that the fever produced helped. The introduction of antibiotics eliminated this treatment.
- Thiopental sodium, “truth serum”, was used to help patients express repressed thoughts.
- Insulin was used to shock schizophrenics but was seen to be not effective.
- Electronvulsive therapy, ECT, was also used on schizophrenics but was found to only work in half the people and there was a high relapse rate.
- Phenothiazines have special properties that did not by itself induce drowsiness or loss of consciousness. First used to calm patients before surgery, it was then used to help calm mentally ill patients.Chlorpromazine was the first tranquilizer.
- Phenothiazines are still used to treat acute schizophrenics. It is understood that this is not a cure but it is better then the placebo treatments.
- Pseudoparkinsonism is sometimes a side effect of those treated with Phenothiazines.
- Antipsychotic drugs block D2 dopamine receptors.
- Clozapine blocks D2 dopamine and 5HT2A serotonin receptors.
- Clozapine produces less Pseudoparkinsonism then other antipsychotics. Another advantage is that some patients show improvement that did not on the other drugs. The major negative side effect is that in some it suppresses white blood cell production.
- With antipsychotic drugs, few are addictive.
- Monoamine Oxidase Inhibitors (MAO) are limited due to side effects.
- Tricyclic antidepressant had little effect on psychotic symptoms but improved the mood of depressed patients.
- Selective Serotonin Reuptake Inhibitors changed how the class of drug was looked at and marketed. Prozac, and other SSRIs drugs, are safer than tricyclic antidepressants because they are less likely to lead to overdose deaths.
- Most antidepressants work by increasing the availability of norepinephrine or serotonin at the respective synapses.
- Electroconvulsive therapy is the most effective treatment for depression.
- If there is possibility of suicide then ECT is the best choice due to the fast results as compared to drug therapy.
- Mood Stabilizers like Lithium show good results with manic individuals while showing little to no improvement in depressed individuals.
- Valproic, Carbamazepine and lamotrigine are not as effective on bipolar disorder but do help with patients that are susceptible to epileptic seizures.
- One consequence of these drugs is the number of people in mental hospitals went down greatly.
- The number of outpatient programs has increased dramatically as has the number of people onantidepressant drugs.
- Psychiatrists are more likely to prescribe drug than do psychotherapy.
Depressants and Inhalants (Downers) – Understanding Addiction
- Most widely used and abused drugs in the U.S.
- Popular for its stress and anxiety relieving properties as well as acceptably.
- Chloral Hydrate was first synthesized in 1832 but not used clinically until 1870.
- Chloral Hydrate has a short onset (30 minutes) and 1g can induce sleep.
- Chloral Hydrate abuse causes massive stomach pain.
- Paraldehyde was first synthesized in 1829 but not used clinically until 1882.
- Paraldehyde has a very large margin of safety and is a very effective CNS depressant.
- Its negative point is that it has an awful taste and a bad smell that permeates the breath of the user.
- Bromides salts were used to induce sleep in the 19th century and used until the 1960’s in OTC meds.
- Bromides have serious toxic effects.
- Barbiturates were first used clinically in 1903.
- Barbiturates are very dangerous when combined with alcohol, however, they are still used for sleep.
- Barbiturates are grouped into time of onset and duration of action.
- Meprobamate was the first antianxiety agent, known as The Happy Pill of 1953.
- Meprobamate can cause physical dependence with as little as twice the normal daily dose.
- Methaqualone was mass marketed as a safe downer.
- Physicians over prescribed Methaqualone and many problems, from suicides to overdoses, were seen.
- Methaqualone is now listed as a schedule I drug.
- Librium was the first benzodiazepines marketed as an anxiety reducer with a large safety margin. Others followed as did reports of psychological dependence.
- Rohypnol is one version. It is legal in places other then the US. Here it is known as the “date rape” drug.
- Benzodiazepines work by bonding with receptors. They enhance the normally inhibitory effects of GABA.
Sedatives and Hypnotics (Nonbenzodiazepines)
- Nonbenzodiazepine hypnotics are the newest additions to the depressant drug class.
- Nonbenzodiazepine are more selective for the GABA-A type of receptor
- Sedatives cause mild depression of the CNS and are used to treat extreme anxiety referred to as anxiolytic.
- Four top selling prescribed medications in the US are anxiolytic. They are the most widely prescribed drug class.
- Many types of anxieties are treated with these antianxiety drugs.
- Hypnotics are used to encourage sleep because of their amnesiac effects. They have, in the past, been liked to very harsh side effects.
- Anticonvulsants are given at very low doses, chronically. For this reason a tolerance tends to develop. This lowers or stopping the desired effects.
- Short-acting barbiturates are the benzodiazepines that are most likely to cause psychological dependence.
- Chronic use of large doses can lead to withdraw syndromes from barbiturates that are similar to alcohol but longer lasting and more unpleasant.
- Barbiturates can produce alcohol-like intoxication with impaired judgment and coordination. This can make it easier to cause harm to oneself while under the influence.
- Depressed rate of respiration is the largest physiological concern. Especially when mixed with alcohol.
- Gaseous anesthetics have been used for many years, with people misusing them for just as long. Nitrous oxide, laughing gas, is still used today as a light anesthesia.
- Butyl nitrites cause rapid delegation of the arteries and can cause faintness or unconsciousness. It can help with high blood pressure. Sold as “Poppers” , they usual have a very unpleasant stench.
- There are many types of volatile solvents. Most “huffers” are children that use household items to get high. Aerosols, toluene, gasoline, freon, butane and propane can all be used.
- GHB – gamma hydroxybutyric acid is a CNS depressant that occurs natural in the body.
- It has been taken as a dietary supplement to stimulate muscle growth.
- It is listed as a schedule I drug except in one form that is used to help with cataplexy. In the form of Xyrem it is a schedule II.
Stimulants (Uppers) – Understanding Addiction
- Stimulants are substances that cause the user to feel pleasant effects such as an increase in energy, due to the ability of the drug’s release of dopamine.
- Stimulants increase alertness, excitation, and euphoria, and are referred to as uppers.
- Cocaine can be traced back to coca, which has been used as a stimulant for thousands of years.
- Natives of the Andes mountains chewed coca leafs into balls and held them in their mouths. This gave them energy to run and carry large weights long istances over hard terrain.
- The coca leaf is an important part of the culture and civilization in 16th Century Peru. Coca was treated as money even by invaders of the country.
- Angelo Mariani was a French chemist who used extracts from coca in multiple products. It was wine that made him rich.
- Then Dr. W.S. Halsted experimented with cocaine as a local anesthesia. He became known as “the father of modern surgery”.
- Sigmund Freud saw cocaine’s potential for treatment of a variety of complaints. For many years he sang the praises of cocaine. He helped one of his friends through a cocaine psychosis that Freud had prescribed him into.
- Even with so much positive force behind cocaine from 1887 to 1914, 46 states passed laws to regulate cocaine.
- With unverified facts, articles were written stating that cocaine was used at very high rates by blacks in the south, and that they had “homicidal” tendency because of this. It explained that cocaine made black men unaffected by .32 caliber guns. Many of these articles in the press and in medical journals were a major influence on the passage of the Harrison Act.
- Coca paste is coca leaves that have been mixed with an organic solvent, soaked, mixed, mashed and had all the excess liquid filtered out. The paste is made into cocaine hydrochloride that is snorted or injected.
- Freebase is cocaine that is converted into a volatile organic solvent, heated and then the vapors inhaled. This is very dangerous and flammable.
- Crack is cocaine mixed with baking soda and water, then dried.
- At the end of the 1960’s cocaine use began to increase again due to the cost of amphetamines.
- Psychiatrist Peter Bourne sounded like Sigmund Freud when he made a case for legalizing cocaine. Many plugged the benefits of cocaine, from doctors to celebrities. It was these doctors and celebrities, along with others with auxiliary income, who could afford the drug due to its high cost.
- Then an inexpensive ($5 to $10 a hit) form of cocaine that could be smoked became available. Again, history repeated itself with the media and politicians going after a certain race of urbanites who used the drug.
- The Anti-drug Abuse act of 1986 targeted high-level crack dealers.
- It lowered the amount of drug you need to be caught due to the potency of crack.
- The Anti-drug abuse act of 1988 added tougher penalties for first time users. After these two laws passed, there was an increase in the number of black Americans in jail and thus concerns about racial profiling was raised.
- The chemical structure of cocaine does not tell us how or why it works.
- Cocaine blocks reuptake many neurotransmitters at one time.
- Chewing or sucking on the leaves allows small amounts to slowly enter the system.
- With snorting the absorption is fast as is the effect on the body.
- Intravenous offers a fast, but short, lasting effect.
- Smoking crack is becoming the preferred way to use cocaine due to the fact that no needles are needed and the high happens fast as well.
- In 1860 the anesthetic properties of cocaine were developed but not used medically until 1884.
- It is stilled used in surgery in the nasal and laryngeal regions.
- Acute toxicity of cocaine or the lethal dose is hard to estimate.
- The route of admission can change the LD as can the form of the drug.
- Chronic toxicity of cocaine is found in problems with the nasal septum and the heart.
- Dependence of cocaine is most likely in those who inject or smoke the drug.
- Lab animals, when given the chance, will administer the drug to themselves until the die. This shows that even without deadly withdraw symptoms, cocaine is additive.
- Cocaine is easy to obtain in most major cities and is around 75% pure. Most of it comes in from South America countries; the majority of that from Peru.
- Due to pressure on the water/land routes, more then half of cocaine is smuggled in at the US- Mexico border.
- Amphetamines, patented in 1932, are potent synthetic stimulant capable of causing dependence.
- They were first used as replacement for ephedrine to treat asthma.
- Then it was used as a treatment for narcolepsy due to it being a stimulant.
- American soldiers in WWII used amphetamines to fight fatigue.
- Truck drivers and students use amphetamines to help them stay awake for long periods of time.
- One of several side effects was that people taking amphetamines were not hungry. This became a major use for amphetamines.
- Speed, which is an illegal methamphetamine, is a common and highly used amphetamine.
- Until the 1960 the problems with amphetamines were with legally manufactured and prescribed ones.
- Amphetamines are often used with other combinations of drugs called speedballs.
- An approach to using amphetamines is smoking ice or crystal meth, which induces a rush, followed by a 4-16 hour high.
- Synthesized drugs that mimic the psychoactive effects of amphetamines are called “designer” amphetamines. MDMA (Ecstacy) is the most popular designer amphetamine.
- Amphetamines are consumed in a verity of ways including orally, intranasally, intravenously and smoked.
- When taking amphetamines orally, effects are felt about 1.5 hours after ingesting them. This differs from intranasal peak effects that come 15 to 30 minutes after taking the drug.
- During intoxication, behavioral toxicity can cause the user harm. With large doses over long periods of time paranoia and panic can be problems, as can violence and aggression.
- Compulsive and repetitive actions are yet another development of chronic toxicity of amphetamines.
- Withdraw effects are small and more annoying then dangerous.
- Psychological dependence is a concern with amphetamines.