Prozac - a cure for all problems
About 25 years ago, a new drug, Prozac, entered the world market. It was the first antidepressant that eliminated "bad mood". Initially, the drug was intended as a treatment for hypertension. But later, the Swiss company Eli Lilly Vostok, developer of Prozac, decided to change the prescription of the drug, making it one of the most popular antidepressants to date. Depression is characterized by symptoms: a feeling of sadness, a decrease in mood, hopelessness, pessimism, a loss of interest in life, combined with a feeling of reduced emotional comfort. According to the WHO, every 10th person after 40 years suffers from this disease, and after 65 years, these figures are three times more. In adolescence, from 5% to 30% of the younger generation may be depressed. The causes of the onset of the disease are different and the depressive state can have both endogenous origin, when the body lacks the neurotransmitters serotonin and noradrenaline, and exogenous origin. These are external factors - seasonal depression with a lack of sunlight, a reaction to a negative event that has occurred, sometimes mental and emotional exhaustion.
The annual turnover of the American market of medicines that treat "mental" disorders is estimated at $ 49 billion. Of these, means for getting rid of depression occupy about 17 billion. Antidepressants or "happiness pills", as they are called, in recent years, have become very popular not only among the older generation, but also among young people. The number of countries leading in the number of antidepressant prescriptions for many years includes the United States. Permanent "Prozacoman" is every 20th resident of the United States. Prozac has become an indispensable medicine in home first-aid kits. In other countries, the United States society is called the "Prozac nation." What is the secret of antidepressants and why Americans no longer see their daily lives without pills. This popularity of this drug in the US is explained by the fact that it is much easier for a person to take one pill and get rid of their problems for a while than to waste time on “work on yourself” and money on a psychotherapist.
As Dr. Roger Greenberg, a psychologist from the Department of Psychiatry at the Center for Syracuse Health at the State University of New York, said in an interview with The New York Times: “The answer to psychiatric problems is not in the field of medicines. Their effectiveness is actually much less than it seems to a wide range of people. ”
Today, according to the IMS Helth study, with a population of 320 million people in the United States, 250 million prescriptions for antidepressants are prescribed by doctors every year.
Special demand for Prozac appears in the winter - time of the blues and emotional instability. Not only domestic problems and constant bad mood, or misunderstanding in the family, but also such problems as the world crisis, wars, the collapse of the exchange market, etc., also have a strong effect on the development of depression. All this leads a person to the alarm, causing fear, bad mood, questions about the meaning of life and, as a result, dispersion. Our society has been modernized, and the psychological tension of people has increased.
How does Prozac get rid of problems? The active substance in the drug is fluoxetine - a substance selectively inhibiting serotonin reuptake. Fluoxetine practically does not bind to other receptors, in particular, it has no affinity for adrenergic, dopaminergic, histamine and cholinergic receptors. "Prozac" helps to increase serotonin levels in the brain structures, which leads to an increase in the duration of the stimulating effect of serotonin. Fluoxetine has a pronounced anti-depressive effect, reduces anxiety, tension and fear, improves mood, and also helps to reduce dysphoria.
The action of Prozac, developing gradually, reaches a certain level, which remains constant even with a decrease in the dose of the drug and lasts for several days after stopping the treatment. Because of this duration of development of the effect, patients with suicidal tendencies are subject to particular control.
It is also not a secret that Prozac not only relieves depression symptoms, but also improves performance. Depression is the plague of the new time and pharmacological companies offer this problem with the help of antidepressants. However, whether everything is so cloudless, it seems, and whether it is possible to use them on a daily basis? World pharmacological companies claim that modern antidepressants are not addictive and side effects. Is it so? Antidepressants are addictive. The tendency to simply use drugs simply increases, and after discontinuation of antidepressants, 98% of the symptoms of depression recur. The side effects characteristic of prozac are associated with its effect on 5-HT1, and on 5-HT2-serotonin receptors, which can lead to insomnia and sexual disorders, as well as on 5-HT3 receptors. Disorders of the nervous system and sensory organs, cardiovascular system, blood and metabolism, disorders of the gastrointestinal tract and urinary system can occur. There are also a number of undesirable effects, such as headaches, sweating, nausea, rash, reduced visual acuity and many others. And this is not a complete list.
The number of people suffering from depression, unfortunately, is increasing every year. Undoubtedly, antidepressants are an integral part of modern medicine, without which sometimes you really can not do. Therefore, the question arises about a more adequate, selective and responsible approach to solving the problem of treating depression, given the huge number of side effects.
Prozac Discovery History
The story of Prozac begins in 1970, when Brian Molloy and Robert Rasban from the Eli Lily research laboratory in the United States began a research project aimed at obtaining a new antidepressant that does not have the side effects of tricyclic antidepressants. He led a group of researchers Ray Faller, who in 1993 for the discovery of Prozac received the award of the American Association of Pharmaceutical Companies. Unfortunately, in 1996, the scientist died of leukemia, during his scientific career he published over 500 research articles in the field of neuropharmacology and neurochemistry.
Meanwhile, another Eli Lily employee, a native of Hong Kong, pharmacologist David Wong studied reuptake mechanisms using the brain tissue of mice, the purpose of the study was to find a substance that would prevent reuptake. Wong tested some of the molecules synthesized by Brian Molloy. On July 24, 1972, he tested a substance with the coding L110,140, which had a strong inhibitory effect on serotonin reuptake and a weak inhibitory effect on norepinephrine reuptake. Substance L110,140 was fluoxetine, better known today as Prozac. (“Eli Lili” did not immediately start developing Wong’s discovery, because at that time the company was more interested in another drug, desipramine, which blocks the reuptake of norepinephrine.)
Fluoxetine studies on animals have shown its efficacy and safety, and in 1976 it was first tested on volunteers. Fluoxetine proved to be a good medicine and in 1982 was patented, and in 1988 it went on sale under the trade name Prozac. By 1994, the drug has become the world leader in the market for antidepressants.
Prozac counterparts soon appeared, such as Pfizer zoloft (original name sertraline, trade name in the United States lustral), SmithKline Beecham paxil (original name paroxetine, trade name in the United States and Great Britain seroxat), luvox company Solvay (original name fluvoxamine, the trade name in the USA is the favertine) and celex from Forest Laboratories (the original name is citalopram, the trade name in the USA is cipramil). Despite numerous competitors, Prozac retained 35% of the market for anti-depressants, zoloft accounted for 15% of the market, and Paxila accounted for 11%.
SmithKline Beecham stated that Paxil is effective in treating people suffering from social phobia, in other words, overly shy people who shun society. In May 1999, the Food and Drug Administration approved the drug as a treatment for this pathology, after which the manufacturer conducted an active advertising campaign for its drug. As a result, Paxil began to write out with the same frequency as Prozac. Some doctors did not agree with the existence of social phobia as such and therefore criticized the new drug, in their opinion, people who are shy by nature do not need to be attracted, because in certain situations shyness is the norm. Despite this, Paxil turned out to be a good tool for those for whom shyness strongly interferes with living, the drug became so popular that its current sales volume is about three billion dollars a year.
In the meantime, Eli Lily has taken steps to make Prozac an even better treatment for depression. The activity of this drug is associated with only one of its two enantiomers; therefore, it is advisable to use a purified active enantiomer, known as R-fluoxetine, to treat depression. And although the cost of producing such a drug is somewhat higher, it can reduce the dose of the medication and reduce the severity of side effects of treatment.
Mechanism of Prozac
Prozac is prescribed at a dose of 20 mg per day for the treatment of depression and 60 mg per day for the treatment of bulimia nervosa. The most famous consumer of prozac was Diana, Princess of Wales; the drug was prescribed to her in 1994. Prozac is not recommended for children, adults suffering from liver failure, and nursing mothers. Some of the people taking the medicine have side effects like nausea, diarrhea, headache, and a few others, but this is quite rare.
The problem with prozac and other serotonin reuptake inhibitors is that the side effects of therapy develop before the therapeutic effect occurs, so many patients stop taking the drug before they benefit from it. It is not yet clear why these antidepressants take so long to get started, because they take minutes to increase the level of neurotransmitters in the brain. However, it appears that this increase is only the first step in the sequence of events leading to relief of symptoms. Despite the increase in the concentration of messengers in the synaptic network, these molecules do not find targets for their effects due to the fact that the number of active receptors that have not received adequate stimulation for a long time has been reduced, and their reactivation requires a sufficiently long time.
The prozac effect, developing gradually, reaches a certain level, which remains constant even with a decrease in the dose of the drug and will last for several days after stopping the treatment. Prozac is metabolized by the liver, in which it turns into norfluoxetine. The latter is also an inhibitor of serotonin reuptake and acts by the same mechanism as Prozac. And this partly explains the long-lasting effect of Prozac.
Prozac half-elimination period is four days, norfluoxetine nine days. This means that even if Prozac ceases to enter the patient's body, nine more days must pass before the concentration of this drug in the blood decreases by half, even after nine days the activity drops to a quarter of the initial one, and in about a month its effects will completely disappear.
Due to the fact that it takes so much time to develop a prozac effect, it is necessary to control those patients whose depression is so severe that they are able to commit suicide at the beginning of treatment. But when Prozac does begin to act, its effect is truly noticeable. It is believed that this drug is able to make shy confident, impressionable more persistent and turn introverts into extroverts, and pessimists into optimists. Therefore, it is not surprising that Prozac has become one of the most commonly prescribed drugs for treating anxiety disorders, social phobia, panic attacks, agoraphobia, manic-obsessive states, bulimia, chronic pain and tension headaches. Prozac gives confidence to people who previously lacked it; this effect has been proven experimentally on rats. In the rat colonies, there is always one dominant male, the level of serotonin in his brain is twice as high as that of other male males. But if you increase the level of serotonin from outsiders, they cease to be members of an obedient herd and no longer allow the leader to take away the best food.
When Prozac appeared in the United States, doctors discharged him to 60 thousand patients every month, and over five years 5 million Americans tried it on themselves. Not surprisingly, the effects of Prozac began to exaggerate, there were examples when he mistakenly hit the front pages of newspapers. But later on all contradictions were put to an end, and now this drug continues to be extremely useful for many sick people. Prozak has no side effects that have been observed in previous types of antidepressants, in particular, it does not develop dependencies.
Another advantage of Prozac is that even massive overdoses of it, as a rule, do not lead to death. Although some people took from fifty to one hundred Prozac pills in an attempt to commit suicide, those who survived developed convulsive disorders. Some of those who question the use of prozac claim that it causes more side effects than old antidepressants. However, statistics show that because of the side effects of Prozac, a smaller percentage of people refuse from it than other antidepressants, moreover, lately, the registration of side effects has become a more widespread procedure, and therefore more patients report their observations.
The side effects attributed to prozac seem to be related to its effect on 5-HT1, and in some people, on 5-HT2-serotonin receptors, which can lead to insomnia and sexual dysfunction, as well as on 5-HT3 receptors which causes nausea and headaches in patients. Sometimes Prozac can also cause a rash.
The extent to which side effects are associated with the use of the drug, and for other reasons, can be seen from a series of double-blind studies conducted on 1,800 patients who were given Prozac and 800 patients who took placebo. As it should be in such a study, neither those who took the pills, nor those who gave them out, knew where Prozac and where the placebo was. As a result, 20% of patients taking Prozac reported a headache, but 16% of those who took a placebo presented the same complaint. 18% of those taking Prozac experienced nausea, the same symptom occurred in 10% of those taking a placebo. 14% of those taking Prozac complained of insomnia, compared with 7% of those taking placebo. For diarrhea, these figures were 12% and 7%, respectively. Only 5% of people from each group reported symptoms of a cold (such as a runny nose). 1% who took Prozac and 3% who took a placebo experienced suicide, while for patients using old antidepressants, this figure was 4%.
It is not surprising that the success of prozac provoked a reaction from those people who perceive this drug as part of a medicinal culture, where people trust the solution of their problems to medical drugs instead of adjusting their lives by their own efforts. In some books, Prozac is subjected to harsh criticism, in particular in the book by Peter Breggin "Let's talk about Prozac: what the doctors are silent about the most controversial medicine of our time." At the same time, in the book Prozac Nation: Young and Depressive in America, 28-year-old writer Elizabeth Wurzel talks about how, thanks to a proseka, she became a happy and successful journalist and writer from a depressive-suicidal addict.
Peter Kramer in his book, Listen to Prozac, also gives the drug a positive rating. But the Harvard psychiatrist Joseph Glenmullen in his book “The Prozac Strike Back” talks about the side effects of this medicine. According to him, half of those people who take Prozac develop a tic or sexual dysfunction. Moreover, he says that when you stop taking the medication, many patients develop withdrawal symptoms, such as dizziness and anxiety.