The unlikely route from inflammation to antipsychotics
The drug development journey leading to olanzapine (Zyprexa) reaching the market did not always follow the steps of rational drug design. Inspired by the first antipsychotic drugs, it took a while from the first discovery of antipsychotic drugs until Zyprexa was developed. The first antipsychotics were come across largely by chance. They were not specifically tailored to a relevant biological effector as rational drug design promotes. Even now as most drugs, Zyprexa is not quite perfect, it is accused of side effects such as weight gain and diabetes. But it has proven to be a potent medication for the treatment of schizophrenia, bipolar disorder and today is also widely used for the treatment of depression (Perlmultter. 2014).
The story of this drug begins in the streets of Paris (and Lyon) in the 1930s, where the pharma-company Laboratoires Rhône-Poulenc (today Sanofi) noticed that the drugs they were developing as antihistamines also demonstrated relaxant and sedative effects (Shen ,1999; Healy, 2004). Their observations and research eventually lead to the synthesis of chlorpromazine in 1950, the first drug with specific antipsychotic action (Yuhas, 2013).
Chlorpromazine was the first so called typical/first generation antipsychotic drug, introduced to the market in 1952. The discovery of chlorpromazine is still considered one of the greatest breakthroughs in psychiatric care, and was the first drug in its class
4. What type of drug is chlorpromazine, and where was it first tested on patients? Antipsychotic, A new phenothiazine drug, chlorpromazine, was synthesized in France in 1950 and was tested on such patients. In 1952, two French psychiatrists, Delay and Deniker, announced that the drug exerted a specific effect in diminishing the symptoms and signs of psychosis in patients with severe mental illnesses. (Hart & Ksir, p. 171)
The modern world’s first glimpse into the world of psychedelics was through d-lysergic acid diethylamide, or LSD. LSD was first synthesized in 1938 by two Swiss chemists from the alkaloid lysergic acid found in ergot, a parasitic fungus that grows on rye and other grains. Five years later, on April 19, 1943 Albert Hoffman, one of LSD’s co-discoverers
Phencyclidine, or PCP, was synthesized in 1926 and used in the 1950s to act as a surgical anesthetic. However, it was retired in 1960s due to significant side effects including delusion, emotional trauma and acutely irrational behavior. It now sees illegal use as an extremely potent and dangerous hallucinogenic drug. It is generally ingested either orally or through the nose and its sedative effects take hold extremely quickly. PCP takes the form of a white, readily soluble powder crystalline in nature. It has It has been classified as being a hallucinogen, dissociative anesthetic, psychotomimetic, and sedative-hypnotic.
Zoloft was first introduced to the United States in 1980’s. Another name for Zoloft is sertraline and is in a group of antidepressants called selective serotonin reuptake inhibitors. At first Zoloft was made to treat major depressive disorder, but as the drug progressed over time it can now treat panic disorder, social anxiety disorder, posttraumatic stress disorder, and premenstrual dysphoric disorder. Zoloft is the most commonly used antidepressant because it works extremely well, it is safe, and its side effects are not as serious as other antidepressants.
Ecstasy, or 3, 4 methylenedioxymethamphetamine, was first synthesized and patented in 1914, by the German drug company Merck. The original purpose of the drug was to be an appetite suppressant, however in 1970 it was given to clinical depressed patients to open them up and talk about their feelings. Then in 1986, Ecstasy was determined to cause brain damage (http://faculity.washington.edu/chudler/mdma.html).
In Part Three, which covers 1950-1990’s, Whitaker describes the propensity in the U.S.A. to diagnose patients with schizophrenia. This fed into the rise in popularity of the drug chlorpromazine, originally used for the treatment of psychosis, was lauded as an antischizophrenic medication. Chlorpromazine and other neuroleptics
The 1950s saw several developments in medications such as antipsychotics. The term antipsychotic refers to medicines or drugs that are primarily needed to manage psychosis. They are usually used to treat schizophrenia and bipolar disorder, though they can be helpful for other mental health problems such as severe depression. In One Flew Over the Cuckoo’s Nest, a patient called Chief Bromden, describes his surroundings after taking medication. He said, “The words come to me like water, it’s so thick. In fact it’s so much like water it floats me right up out of my chair and I don’t know which end is up for a while. Floating makes me a little sick to the stomach at first. I can’t see a thing. I never had it so thick it floated me like this.” (Kesey 133) The quote gives an accuate picure of how an antipsychotic would work. Chlorpromazine, the first anitpsychotic, was synthesized in 1950 by the French pharmacuetical company Rhône-Poulenc. It was followed by the creation of many other drugs with diverse chemical structures. In 1954, another
In 1955, antipsychotic medications were introduced to help mental disorders. These medications are usually taken orally in which help relieve symptoms for periods of days. The misuse or abuse of the medications are low. There are three generations of antipsychotic medications. The first generation is known for reducing hallucinations and delusions, but not affecting problems like disorientation or depression. An example would be chlorpromazine, brand name being Thorazine. Some negative side effects of taking the first generation drugs are Parkinson’s-like symptoms, tardive dyskinesia, and weight gain. Next, the second generation drugs minimized the outcome of the individual getting Parkinson’s-like symptoms. An example of this generation would be Clozaril. “A unique feature of Clozaril is the 1 to 2 percent chance of developing a potentially lethal blood disease called agranulocytosis” (Levinthal 282). This disease decreases white blood cells and affects the immune system. If early signs of this disease start to appear the patient will stop taking Clozaril and recover. Lastly, the third generation has shown to be the most effective on schizophrenia. Abilify is an example of this generation drug. It does not have a risk of Parkinson’s, tardive dyskinesia, or diabetes. Abilify blocks specific serotonin receptors in which prevents negative side effects from happening. These different
In the early 1990s new antipsychotic medications were developed and used to help those dealing with bipolar and schizophrenia which have symptoms like psychosis and hallucinations. These medications are called second-generation or atypical antipsychotics and they are the first line
At first it was the cure all people were looking for. Then it became the drug they were afraid to take. Somewhere between these two extremes lies the truth about the drug Flouxetine, better known as Prozac, the most widely prescribed drug on the globe. It is mainly prescribed to patients suffering from clinical depression. It was first brought to the market in 1988 by the pharmaceutical giant Eli Lilly co. Even though it was originally prescribed for depression, it has been prescribed for everything from eating disorders to insomnia. It was first considered the wonder drug of the new decade because of the way it helped depression patients when no other anti-depressant could
Covers, C. (2009). Second-generation versus first-generation antipsychotic drugs for Schizophrenia. Retrieved March 16, 2011 from
Antipsychotics are classified as major tranquilizers that are used to treat mental health illnesses such as schizophrenia, bipolar disorder, and other mental illnesses. They can also treat severe depression and severe anxiety. These antipsychotics drugs reduce or increase the effect of neurotransmitters in the brain to regulate levels that help transfer information throughout the brain. The neurotransmitters that are affected are the serotonin, dopamine, and noradrenaline.
A Swiss chemist named Dr. Albert Hoffman first produced lysergic acid Diethylmide –or best known as LSD in 1938 (Dye, 1992, p. 2). Hoffman discovered the drug while trying to synthesize a new drug for the treatment of headaches. He obtained the lysergic acid from the parasitic fungus that grows on rye plants known as ergot. From the lysergic acid, he synthesized the compound LSD. He used the compound to test for its pain killing properties on laboratory animals. Being that appeared totally ineffective, the bottle of LSD was placed on a shelf and remained untouched for five years.
The first compounds of the triazolobenzodiazepine structure were synthesized at the end of the 1960s by a team of specialists from the USA, but it was 10 years before the tranquilizers appeared in the triadolobenzodiazepine group. Alprazolam (Xanax), which has been on sale since 1981, is
Throazine, other major tranquilizers developed 1952 - The French psychiatrists Jean Delay and Pierre Deniker report that Thorazine ® calms hospitalized chronic schizophrenic patients without causing clinically significant depression. The drug is called 'hibernotherapie' because patients became quiet, like