Annotation. The article discusses the properties of the most effective tool to date for relieving symptoms of schizophrenia and other mental disorders. The mechanism of action of neuroleptics is explained, side effects are described. The main attention is paid to the correct intake of the drug-strictly according to its intended purpose and with the observance of the dosage.
SEROQUEL-THE DRUG OF CHOICE FOR THE TREATMENT OF PSYCHOSIS
Mental illness is not uncommon today. It is almost impossible to make a correct diagnosis, conduct adequate therapy, and achieve success in treatment without the help of a specialist. The first and most important step for a sick person and their relatives is to find a doctor whose actions can be trusted. Especially when we are talking about the drug therapy of psychoses: schizophrenia, bipolar disorders, age-related behavioral disorders. In such situations, doctors prescribe neuroleptics. They destroy the symptoms of the disease, but in themselves are far from harmless drugs. The choice of psychiatrists is increasingly becoming an atypical neuroleptic with proven effectiveness, whose side effects are less pronounced than those of other antipsychotics. Seroquel is one of The most effective and safe drugs.
Seroquel: What You Need To Know
DESCRIPTION OF THE DRUG
Seroquel is a trademark of the drug, which is produced by the English company AstraZeneca Uk. Ltd. Its main active substance-quetiapine-belongs to the group of atypical neuroleptics. This class of medications is used primarily to relieve symptoms of severe mental illnesses: hallucinations, delusions, manic and depressive disorders, and autism.
How do neuroleptics work?
The action of antipsychotic drugs is based on blocking the receptors of nerve cells (neurons). To transmit a signal, neurons are equipped with receptors that are sensitive to certain mediators – substances released by the brain.
- Dopamine is responsible for motor activity and cognitive (cognitive) activity. When there is an excess of dopamine, excessive receptor sensitivity to it, hallucinations, manic episodes develop; when there is a lack of it, depressive States appear, motor disorders up to Parkinson's disease. D1 and D2 - dopamine receptors in nerve cells receive and transmit information that the brain transmits through dopamine.
- Norepinephrine-regulates the state of internal organs during stress, provides quick decision-making. Under the influence of norepinephrine, blood pressure increases, and the heart rate increases. Excess norepinephrine leads to hyperactivity, aggression, and lack of it leads to apathy and depression. For the perception of norepinephrine are responsible in the neurons 1 and 2-adrenoreceptors.
- Serotonin-reduces the sensitivity of the nervous system to negative emotions, thereby it increases the effect of dopamine and norepinephrine. In essence, this mediator keeps a smooth, good mood in the flow of various events. When one of the types of serotonin receptors - 5-HT2-is activated, the nervous system is excited, and the secretion of hormones such as prolactin and corticosterone increases. An overabundance of serotonin causes hallucinations, and its lack – pumping of negative emotions, depressive syndrome.
- Histamine-causes the immune system to respond to a threat to the body. Excess histamine is the cause of migraines, chronic fatigue syndrome, and many allergic reactions, including nervous allergies. The transmission of impulses from histamine occurs through H-histamine receptors
Neuroleptics are substances that block the work of nerve cell receptors and interfere with the transmission of signals sent by the brain through mediators.
Typical and atypical neuroleptics
Typical neuroleptics (discovered in the 50s of the XX century) belong to the first generation of antipsychotic drugs. They block mainly dopamine receptors, which explains the serious neurological side effects of their use.
Atypical antipsychotics differ from classical neuroblastoma a more gentle effect on the psyche. They have a lower degree of affinity with the d 1 and D 2 – dopamine receptors, which is associated with a reduced risk of developing EPR. The positive effect is achieved by blocking the receptors of other mediators: serotonin, norepinephrine, histamine. For serious diseases, psychiatrists prefer to prescribe atypical neuroleptics: with good performance, they have a high level of security. However, recent research and many years of experience in the use of atypical neuroleptics in Western countries show that they also cause harm to health.
Quetiapine-mechanism of action, clinical effect, indications
Several drugs have been created based on quetiapine, one of the mildest atypical neuroleptics: Seroquel, Catalept, Raquel, Quateron. They practically do not cause EPR and hyperprolactinemia.
Mechanism of action
The therapeutic effect of quetiapine is since it blocks a wide range of receptors:
- H1-histamine receptors, so the drug has a sedative effect;
- 1-adrenoreceptors-their blocking is accompanied by a decrease in blood pressure, a decrease in cholesterol and triglycerides in the blood;
- 5-HT2A-serotonin receptors; suppressing the sensitivity of 5-HT2A-receptors is one of the ways to get rid of depression while improving the quality of sleep, the overexcited nervous system gets to rest. The drug acts as an antidepressant, normothermic (stabilizes mood), relieves anxiety (anxiolytic effect);
- D 1 and D 2-dopamine receptors are less blocked by quetiapine than serotonin ones. The antipsychotic effect of the drug is not accompanied by extrapyramidal disorders: a therapeutic dose of Seroquel can cause only weak convulsive muscle contractions.
A positive clinical result allows patients with Seroquel to overcome undesirable symptoms of the disease, improve the quality of life, and preserve social functions: work, study, and perform family duties.
The neuroleptic effect of Seroquel is manifested in the treatment of a strictly limited range of diseases.
- Acute and chronic psychoses, schizophrenia. The drug suppresses the positive symptoms of the disease: delusions, hallucinations, obsessions, stupor, excitement, confusion of thinking. The drug can smooth out negative manifestations: isolation, lack of will, autism (emotional poverty, lack of communication skills).
- Manic episodes in a bipolar disorder-the drug are used to stabilize mood
- Depression. Quetiapine has shown good results in the treatment of depressive disorders of various etiologies – even where the use of antidepressants has not been successful. In 60% of patients taking the drug, improvements begin with the 2nd week of therapy and increase by 6-8 weeks.
- The borderline States between severe neuroses and psychoses. The use of Seroquel is justified for panic attacks, obsessive-compulsive disorders, phobias, and increasing anxiety. The drug has a sedative effect, relieves aggression, fear, helps to get out of the circle of obsessive actions and neurotic States prevent their transformation into psychosis.
! Please note: the atypical neuroleptic Seroquel is only indicated for severe mental disorders. The use of the drug in the treatment of neuroses, addictions, like a sleeping pill or sedative, is not justified. Seroquel is not sold without a prescription in pharmacies. If your doctor prescribes this drug, be sure to consult with what purpose he does it, what results from he expects.
The therapeutic dose of quetiapine is quickly absorbed, acts within a day (the half-life is 7 hours), and almost all are excreted from the body without accumulating. After receiving the tablet in the gastrointestinal tract, the medicinal substance is absorbed into the blood by 83%, the maximum concentration is reached within an hour and a half. The drug is decomposed in the liver to inactive substances: 73% of the metabolites are excreted through the kidneys with urine, 21% - through the intestines with feces. In the elderly (over 50 years), the rate of absorption and excretion of the drug is reduced by 30-50%. The high digestibility of the medicinal substance ensures the rapid appearance of positive treatment results. Rapid metabolism and lack of accumulation (accumulation of decay products) make it possible to treat this drug for the elderly and people with minor liver and kidney pathologies.
INSTRUCTIONS FOR USE
Seroquel is available in the form of tablets of normal and prolonged action.
The usual preparation contains Quetiapine and auxiliary components: magnesium stearate, lactose monohydrate, microcrystalline cellulose, hypromellose, iron-based dyes, and other substances. Biconvex tablets differ in their active substance content and color:
- Seroquel 25-tablets of 25 g quetiapine; pink color;
- Seroquel 100-100 g; yellow color;
- Seroquel 200-200 g, white.
Seroquel Prolong contains Quetiapine coated with a special coating that allows you to gradually release the active substance and prolong its action in the body. Prolonged tablets are oblong and biconvex, and they are engraved with information about the amount of medicine in the tablets:
Each package contains 60 tablets-the norms for a 2-month treatment. The daily dose is carefully selected by the doctor depending on the type and severity of the disease, the patient's age, and treatment strategy.
! Please note: tablets of prolonged action are not recommended to divide, break, chew; they are used 1 time a day – on an empty stomach, before going to bed.
In some cases, it is necessary to refuse treatment with Seroquel and Seroquel Prolong or use them with extreme caution.
- Intolerance to the components included in the tablets - most often, it is galactose. Patients with lactase deficiency and glucose-galactose malabsorption should look for tablets without galactose in the shell.
- Children's age-up to 18 years. Side effects when taking quetiapine include a violation of metabolism, which provokes obesity, can affect the growth of the body, the formation of reproductive function. In the treatment of panic disorders with quetiapine in children, changes in the thyroid gland were observed, an increase in prolactin in the blood, and EPR symptoms-phenomena not typical of this drug in therapy in adults.
- Presence of severe cardiovascular diseases. The drug reduces blood pressure, increases cholesterol levels in the blood – all this creates a risk of developing acute heart failure, atherosclerosis.
- Low operating pressure. Taking the drug is accompanied by orthostatic hypotension, which provokes dizziness, fainting with a sudden fall and injuries.
- Cerebrovascular dystonia. With a decrease in blood pressure, there is a sharp violation of brain nutrition, hypoxia.
The use of quetiapine in late pregnancy affects the condition of newborns: they suffer from blood pressure disorders, there are extrapyramidal disorders, tremor (trembling) of the limbs, drowsiness. During the period of taking Quetiapine medications, it is recommended to refuse to breastfeed.
Top 11 Questions about Seroquel Withdrawal, Side Effects, and Tapering
Although quetiapine is considered the most "mild" neuroleptic, its use has revealed several serious side effects. The most common of them at the beginning of taking the drug are:
- Rapid heart rate;
- an irresistible desire to sleep-lasts 10-14 days, gradually decreases during taking the medication;
- dry mouth;
- weight gain – at the beginning of quetiapine therapy, the weight of adults increases by about 7%.
Interaction of quetiapine with other medications
Standard in psychiatry is monolecte use a serious drug for the relief of mental disorders. In practice, it is necessary to combine the treatment of the psyche with the therapy of somatic pathologies. In this case, there may be a problem with the combination and interaction of drugs, which should be taken into account by the doctor when selecting the dose of an antipsychotic.
Quetiapine + azoles/ macrolides. Simultaneous use of quetiapine with antifungal agents or antibiotics from the macrolide group increases the concentration of the neuroleptic in the blood. Its daily dose should be reduced. This is especially important for the elderly and people weakened by other diseases.
Seroquel + drugs that affect the enzyme composition of the liver. Carbamazepine, phenytoin, rifampicin, barbiturates-drugs that regulate the enzyme composition of the liver, reduce the concentration of quetiapine in the blood plasma. To achieve a therapeutic effect, the dose of neuroleptics should be increased by about 13%.
Administration of quetiapine with such drugs as lithium, sodium valproate, haloperidol, cimetidine, imipramine/fluoxetine – does not change the picture of biological digestibility of an atypical neuroleptic, does not require correction of its daily dose.
! Please note: the selection and change of the dose of a neuroleptic, taking into account all the circumstances of reception, can only be calculated by a competent doctor. When making a decision, it weighs all the pros and cons and is also legally responsible for the patient's health. Independently changing the amount of medication taken will only prevent the successful treatment of the disease.
Ten years later, in 2009, the US government sued AstraZeneca over side effects suffered by patients who used the neuroleptic Seroquel.
Metabolic syndrome. The drug based on quetiapine causes persistent weight gain, which is accompanied by an excessive appetite and thirst. The blood glucose concentration increases, there is a risk of developing type 2 diabetes.
Drug was accused of provoking patients to suicide: there were examples of suicide during clinical trials of the drug when it was used by veterans who treated PTSD.
The company was accused of advertising the drug to expand the scope of its use as a sleeping pill, a means to treat neuroses (Gender Differences in Neuroticism), and so on. At the same time, the emphasis was placed on the sedative and anxiolytic (relieving the feeling of anxiety) effect of the antipsychotic. The drug was recommended for use by children, the elderly, former soldiers, and prisoners. At that time. as indications for such use were not approved by the FDA: Alzheimer's disease, hyperactivity, insomnia. As a result, AstraZeneca was forced to pay $ 520 million, which was used for independent research of the drug.
In Melbourne in 2011, it was planned to conduct a study of the drug and test whether it can stop the early signs of psychosis in people aged 15-40 years. However, a group of scientists from Australia, the United States, and the United Kingdom said that such tests on humans are unethical.
The FDA has issued an official warning about the use of Seroquel
- An antipsychotic based on quetiapine contraindicated in senile dementia. Symptoms of the disease: memory loss; confusion of thinking; mood changes; loss of personal qualities. The risk of death increases when using neuroleptics by persons with such symptoms.
- Seroquel is associated with a risk of suicide – it is highest at the very beginning of the use of the drug or at times of increasing the dose – especially among people under the age of 24 years. The FDA encourages young people and their relatives to monitor their mood during the period of taking a neuroleptic (the appearance of irritability, anxiety, aggression; panic attacks, spontaneous actions).
- Seroquel has not been proven effective in the treatment of bipolar mania in children under 13 years of age and bipolar depression in children under 8 years of age.
Quetiapine is not officially recognized as a drug, so its use is not controlled at the state level. Meanwhile, people who have served time in American prisons have learned to use it for drug intoxication. Seroquel tablets were given to them as sleeping pills - the prisoners turned them into powder and inhaled the narcotic dust. Seroquel was administered intravenously in combination with cocaine, and its use in conjunction with methadone led prison inmates to a state similar to opium intoxication.
The intake of Seroquel by prisoners revealed the dependence that these neuroleptic forms. Prisoners faked psychosis and threatened suicide if they were deprived of "sleepy berries", although other psychotropic drugs did not cause them a similar reaction. American psychiatrists called Quetiapine the "drug of choice" for people with chemical dependence.
Drug withdrawal syndrome is closely related to the question of addiction. Long-term use of Quetiapine leads to compensatory changes in those receptors that have long been suppressed by the neuroleptic. And there are quite a lot of them: dopamine, serotonin, histamine, adrenergic receptors-a sudden withdrawal of the drug will cause a severe withdrawal syndrome or a new psychosis. The UK prescription guide (UK form) recommends a gradual reduction in the dose of the drug to safely exit their addiction. An effective and painless schedule has not yet been developed, but it has been established that the dose should be reduced by a "ladder" - every 5-7 days, take 25 mg less.
Disadvantages of the drug are associated with side effects, the main of which is a violation of metabolism and the risk of developing diabetes. Do not forget about possible heart problems and the strong sedative effect of Seroquel.
If you take the medication for a long time, it will be difficult to cancel it. The high cost of an English licensed drug makes patients look for much cheaper substitutes. You can only buy Seroquel at a pharmacy with a doctor's prescription.
- The cost of Generic Seroquel - from $0.61 per pill;
- The cost of Brand Seroquel - from $3.5 per pill.
REVIEWS OF THE DRUG
Reviews of the drug are very different, but there is a certain logic in them: someone who takes the drug for other purposes leaves a negative opinion about it.
Patient M: I finally found the drug that relieved me of obsessions, in a word, cured me. Seroquel, first of all, helped me to think normally, my confusion and anxiety disappeared. Returned to normal sleep, fully get enough sleep, and get up rested. There was energy, a taste for life, incentives to work. I don't plan to cancel it – I need to get better. I will take another 2-3 years.
Patient I.: Seroquel affected me like a button the head: I drank, and immediately collapsed to sleep, as if knocked down. I woke up all broken, with fog in my head. I forget everything I planned to do a minute ago. I have been drinking pills for 2 weeks – the doctor prescribed them to get rid of anxiety. But no: the anxiety remains, and I feel much worse-sluggish and stupid. In General, I threw these pills.
Patient C: I Want to describe my wild Seroquel withdrawal syndrome, which I took for only 3 months-100 mg per night. Treated anxiety depression. Descended from the drug ladder, 25 g reduced and sat on this dose for 4-5 days. Today is the second day without pills. The condition is terrible: terrible weakness, dizzy, aching bones. I don't know why my eyes are itching, my nose is stuffy. I can't control my emotions: I throw tantrums – and then I start laughing. I can't sleep at night. In General, I want to shoot myself so that all these stops. How long will this state last?
SEROQUEL-DRUG OF CHOICE FOR PATIENTS AND DOCTORS
Atypical neuroleptic Seroquel is an effective and most safe drug for the treatment of mental illness. In Russia, it is included in the form of preferential medicines – the state assists citizens in the treatment of this drug.
Already with the first episode of the disease, the choice of the drug should be made in favor of Seroquel – It has a reputation as a drug that treats with the least number of relapses, successfully copes with negative symptoms. A break in social ties, isolation – a characteristic feature of people who have experienced the first attack of psychosis. Treatment should last at least 5 years - so that there are no relapses. For this period, you need a drug with the best tolerance, safe for health. Seroquel does not need additional therapy to prevent EPR and other side effects.
The economic benefit of using Seroquel is calculated in the cost of maintaining 1 year of quality life of the patient – 1 QALY. The price of such a year for treatment with this drug is the lowest: the choice of a humane (well-tolerated), although expensive, the drug is generally more profitable than a cheap treatment with a large number of side effects.