In the conditions of modern city life and increased mental work, a person often experiences unbearable stress. And stress, physical inactivity, and the use of stimulants such as coffee, tobacco, and alcohol contribute to sleep disturbances. Most often for symptomatic therapy For insomnia disorders (this is what insomnia is called), a mild hypnotic is used, for example, plant origin.
A good sleeping pill must be effective and safe
But medical science does not stand still, and such drugs as, for example, peony tincture, Corvalol and Phytosedan are being replaced by new generation drugs that improve sleep. In addition, they do not cause side effects typical of “classical” drugs. These drugs belong to the so-called Z - hypnotics. What is it and how to choose the most suitable sedative or sleeping pill?
What are Z - hypnotic (sleeping pills) drugs?
As you know, sleeping pills are called “hypnotics”, from the word “hypnosis”. By modern standards, it is necessary to begin treatment of insomnia disorders (that is, insomnia and difficulty falling asleep) with non-medicinal methods: changing the work and rest schedule, walking, going to bed on time, treating diseases that can provoke insomnia, for example, thyrotoxicosis or neurasthenia.
If these measures are not enough, then sedatives of herbal origin are prescribed. They are available freely, without prescriptions, and almost all are mildly sedative and hypnotic effect. IN in this case the weak effect is an advantage since the degree of sleep disturbance is small. In addition, they are not addictive, and these drugs have a low price.
Perhaps Valocordin has the most effective effect due to its phenobarbital content. It is the only barbiturate that can be purchased without a prescription as part of Valocordin (Corvalol).
Valocordin has a sedative effect
In the event that sleep disorders become so pronounced that they interfere with work and leading a normal lifestyle, then the appointment of “real” sleep aids is required. sleeping pills, which cannot be purchased without appropriate prescriptions.
Such drugs previously included barbiturates (“Etaminal sodium”, “Barbamil”, “Veronal”), then they were replaced by benzodiazepine drugs, which were very actively used throughout the world in the 70s - 80s of the twentieth century. In the USA, for example, there was even a “benzodiazepine epidemic”: it was believed that such drugs not only improve sleep and bring harmony with oneself and the world around us, but are also an excellent stress preventative.
Time has shown that this is not so: benzodiazepine drugs, for example, nitrazepam (Radedorm) or Phenazepam, plunge a person into deep dream, but the next morning they leave you feeling exhausted. They also relax muscles (muscle relaxation), which can be dangerous when driving. Also, these drugs cause withdrawal syndrome: the patient becomes “addicted” to such drugs.
Therefore, the persistent search for such means that satisfied a very “capricious” list of requirements continued. For example, it is known that a good sleeping pill of the new generation should be as close to the ideal as possible. It should immediately induce sleep, cease its effect no later than an hour after waking up, maintain daytime alertness and performance, and not cause addiction or side effects. However, the drug should not be used as sedative medicine, do not affect memory and thinking.
And finally, at the end of the twentieth century, such drugs appeared, they were called Z - hypnotics. They are capable of very selectively influencing the structures of inhibitory GABAergic (inhibitory) receptors. Scientifically, these drugs are called “non-benzodiazepine benzodiazepine receptor agonists.” Representatives of this family began entering the global pharmaceutical market in 1993.
The most prominent representatives of the family
By tradition, all Z-drugs have international generic name, which in Russian transcription begins with the letter “z”. Let's look at typical representatives of this class.
Zopiclone
Modern hypnotic drug of non-benzodiazepine structure
In the Russian Federation it is better known under the trade name “Imovan”. This is an easy and convenient sleeping pill that can be taken for 2 to 3 weeks without much fear. Falling asleep usually occurs (as with other drugs of this family) within 1 to 2 hours after administration. The sleep is even and calm, the morning awakening is quick, the daytime well-being is good. Single daily dose – 7.5 mg. In old age, it is recommended to reduce the dosage by half. In this case, the time to fall asleep may be extended by 1–2 hours, but the drug will have less effect on the liver, since Imovan is contraindicated in pronounced violations liver and kidney functions.
The cost of one package of “Imovan” (according to 2016 data) is, on average, 250 rubles for 20 tablets, for 3 weeks of use.
Zolpidem
Another of the Z-hypnotics is Zolpidem
The second drug of this family is better known as Hypnogen or Ivadal. This remedy (as well as other Z-hypnotics) should be taken within an hour immediately before bedtime, or even while lying in bed. It has a good therapeutic range: the initial dose is 5 mg, the maximum is 10 mg.
Has a significant drawback - high price. So, a similar number of tablets for 3 weeks of use will already cost over 2,500 rubles, that is, ten times higher than that of Imovan.
Zaleplon
This drug has beautiful musical trade names: "Andante" or "Sonata". This drug can be considered a really strong sleeping pill, but with its long-term use, a sharp withdrawal syndrome may develop, which will manifest itself in the form of persistent insomnia disorders. Therefore, this drug should be taken in short courses and in a minimal dosage.
However, an indisputable “plus” is the fact that after taking it, it is completely eliminated from the body within 1 – 2 hours, so daytime drowsiness never occurs while taking zaleplon.
Its recommended dose is the same as the maximum - 10 mg. It is recommended to take it a couple of hours after eating, but no later than an hour before bedtime. The ideal option is to go to bed two hours after dinner and take this medicine at night.
The active ingredient in Andante is zaleplon.
The cost of zaleplon preparations is on average 460 rubles, but only for 7 tablets.
Therefore, in terms of a weekly course we get:
- zopiclone 12.5 rubles;
- andante 460 rubles;
- I gave 850 rubles.
It should be recalled that these drugs are sold by prescription only. Perhaps this is an unnecessary precaution (after all, these drugs are relatively safe), but this is how it should be done in relation to all sleeping pills. After all, before, when barbiturates were sold without prescriptions, their overdose often caused death, and they were used to commit suicide attempts and various crimes.
All Z-hypnotics are released strictly according to a doctor’s prescription
In conclusion, we note that in case of severe sleep disorders, these drugs should become the basis drug treatment, and zopiclone and zolpidem have an average effect over time, and zaleplon is a drug with an ultra-short, “spot” effect on insomnia.
The positive aspects of these remedies are the absence of breathing disturbances during sleep and the minimal risk of developing sleep apnea, as well as vigorous awakening and wellness during the day.
But still, the ideal treatment option for insomnia disorders should be considered modification of the patient’s lifestyle, and joint efforts should be made by both the patient and the doctor to normalize sleep physiological methods, leaving medications “in reserve”.
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Nonbenzodiazepines (sometimes colloquially called "Z-drugs") are a class of psychoactive substances, similar in nature to benzodiazepines. The pharmacodynamics of non-benzodiazepines are almost identical to the pharmacodynamics of benzodiazepine drugs, and, therefore, the drugs have similar benefits, side effects and risks. Non-benzodiazepines, however, have different or completely different chemical structures from benzodiazepines and, therefore, are not related to benzodiazepines at the molecular level.
Classes
Currently, the main chemical classes of non-benzodiazepines are:
Imidazopyridines
Zolpidem (Ambien) Necopidem Saripidem
Pyrazolopyrimidines
Zaleplon (Sonata) Divaplon Fasiplon Indiplon Lorediplon Ocinaplon Panadiplon Taniplon
Cyclopyrrolones
Eszopiclone (Lunesta) Zopiclone (Imovane) Pagoclone Pazinaclone Suproclone Suriclone
β-carbolines
Abecarnil Gedocarnil ZK-93423
CGS-9896 CGS -20625 CL-218, 872 ELB-139 GBLD-345 L- 838, 417 NS- 2664 NS- 2710 Pipequaline RWJ - 51204 SB- 205, 384 SL- 651, 498 SX- 3228 TP- 003 TP- 13 TPA- 023 Y- 23684
Pharmacology
Nonbenzodiazepines are positive allosteric modulators of the GABA-A receptor. Like benzodiazepines, they exert their effects by binding and activating the benzodiazepine receptor site.
Story
Nonbenzodiazepines have demonstrated effectiveness in the treatment of sleep disorders. There is limited data to suggest that tolerance develops more slowly to nonbenzodiazepines than to benzodiazepines. However, the data is limited and no conclusions can be drawn. Data are also limited regarding the long-term effects of nonbenzodiazepines. There are some differences between the Z drugs, for example zaleplon does not cause tolerance or relapse effects.
Pharmaceuticals
The first three non-benzodiazepines on the market were the so-called "Z-drugs" Zopiclone, Zolpidem and . All three drugs are sedatives, and are used exclusively for mild treatment insomnia. They are safer than older barbiturates, especially in overdose, and, compared with benzodiazepines, have less tendency to induce physical dependence and addiction. Z-drugs have gained widespread popularity as a treatment for insomnia, especially in older patients. Long-term use of such drugs is not recommended, since the patient may develop tolerance and addiction. Survey of patients using non-benzodiazepine Z-drugs and benzodiazepines sedatives, showed no difference in reports regarding side effects, reported by 41% of users. Z-drug users were more likely to report attempts to quit taking sleeping pills than benzodiazepine users. The effectiveness of the drugs also did not differ.
Side effects
Z-drugs are not without their drawbacks, and all three compounds produce side effects such as severe amnesia and, less commonly, hallucinations, especially when used in high doses. In rare cases, taking such drugs can lead to a fugue state in which the patient can perform relatively complex actions, including cooking or driving a car while unconscious and subsequently having no memory of the events that occurred after awakening. Although this effect is quite rare (and has also been observed with certain sedatives previous generation, such as temazepam and secobarbital), it can be potentially dangerous, so the search for new compounds with an improved side effect profile continues. Daytime withdrawal anxiety may also occur with chronic nighttime use of nonbenzodiazepines such as zopiclone. Side effects of drugs in this class may vary due to differences in metabolism and pharmacology. For example, long-acting benzodiazepines can accumulate in the body, especially in older adults or those with liver disease. Benzodiazepines short acting associated with more high risk more serious symptoms cancellations. In the case of non-benzodiazepines, zaleplon may be safest in terms of sedation the day after dosing, and, unlike and, zaleplon does not increase the risk of motor vehicle accidents, even when administered in the middle of the night, due to its ultra-short half-life.
Increased risk of depression
It has been stated that insomnia can cause depression, which suggests that insomnia medications may help treat depression. However, data analysis clinical trials, submitted to the FDA regarding , and , showed that these sedative-hypnotics more than doubled the risk of developing depression compared with placebo. Hypnotics may therefore be contraindicated in patients suffering from or at risk depression. Sleeping pills are more likely to lead to depression than to relieve it. Studies have shown that long-term users of sedative-hypnotics have noticeable increased risk suicides, as well as an overall increase in the risk of mortality. On the other hand, cognitive behavioral therapy (CBT) for insomnia has been found to improve sleep quality and overall mental well-being.
Addiction and discontinuation
Nonbenzodiazepines should not be stopped abruptly if the drugs are taken for more than a few weeks because of the risk of relapse and acute withdrawal reactions, which may resemble those seen during benzodiazepine withdrawal. Treatment usually involves a gradual dose reduction over weeks or months, depending on the patient, dosage, and length of time of treatment. If this approach does not work, you can try switching to an equivalent dose of a long-acting benzodiazepine (eg, chlordiazepoxide or chlordiazepoxide) followed by a gradual dose reduction. IN extreme cases and, in particular, in the presence of severe addiction and/or abuse, inpatient detoxification with .
Carcinogenicity
In the journal Clinical Medicine A systematic review of sleep has been published medical literature on anti-insomnia drugs and concerns were raised about benzodiazepine receptor agonists, benzodiazepines and Z-drugs, which are used as sleep aids. The review found that almost all sleep disorder and drug trials were sponsored by pharmaceutical industry giants. It was found that the relationship positive results, favorable to industry in industry-sponsored trials was 3.6 times higher than in non-industry-sponsored trials and that 24% of authors did not disclose funding for their published work pharmaceutical companies. The paper noted that there are few studies of sleep aids independent of drug manufacturers. The author expressed concern about the lack of discussion of the side effects of benzodiazepine agonists, such as the significantly increased risk of infection, cancer and increased mortality in hypnotic trials and the overemphasis on positive effects. No sleep aid manufacturer has attempted to refute epidemiological data showing that use of their product is associated with increased mortality. The author stated that "major trials of hypnotics need to examine in more detail possible adverse effects of hypnotics, such as weakness in daytime days, infections, cancer and death, and weigh the resulting balance of benefits and risks.” In clinical trials of these nonbenzodiazepine hypnotics, a significant increase in the risk of skin cancer and tumor development was found compared with placebo. Development of other types of cancer has also been observed, such as brain, lung, colon, breast and Bladder. Users of non-benzodiazepines also experienced an increased risk of infections, possibly due to decreased immune function. It is believed that the cause of the increased risk of cancer was either suppression of immune function or the viral infections themselves. The FDA was initially hesitant to approve some nonbenzodiazepines due to concerns about increased cancer risk. The author reported that because the FDA requires reporting of favorable and unfavorable results from clinical trials, data from the FDA's New Drug Application are more reliable than data from the peer-reviewed literature. In 2008, the FDA again reviewed its data and confirmed the increased risk of cancer in randomized trials of the drugs compared with placebo, but concluded that the cancer risk was not associated with the need for regulatory action.
Elderly patients
Nonbenzodiazepine hypnotics, which are related to benzodiazepines, cause disturbances in body balance and standing stability in individuals who awaken during the night or the next morning; Falls and hip fractures are frequently reported. Concomitant use with alcohol increases these disorders. In relation to these violations, partial, but incomplete, tolerance develops. In general, nonbenzodiazepines are not recommended for older patients due to the increased risk of falls and fractures. Detailed review medical literature regarding the management of insomnia, including in older people, has shown that there is sufficient evidence of effectiveness and long-term benefits non-drug treatment insomnia in all adults age groups. Compared with benzodiazepines, nonbenzodiazepine hypnotics and sedatives show little advantage in efficacy or tolerability in older adults. It has been found that new drugs such as melatonin agonists may be more suitable and effective means for the treatment of chronic insomnia in the elderly. Long-term use of sedative hypnotics for insomnia has no evidence base and is not recommended for reasons possible development side effects such as cognitive impairment (anterograde amnesia), daytime sedation, impaired motor coordination and an increased risk of motor vehicle accidents and falls. In addition, the effectiveness and safety of long-term use of these agents is still to be determined. It was concluded that further research is needed to evaluate the long-term effects of treatment and the most appropriate treatment strategy for older adults suffering from chronic insomnia.
Controversy
A review of the literature regarding hypnotics, including non-benzodiazepine Z-drugs, concludes that these drugs pose unnecessary risks to human health and lack evidence of long-term effectiveness due to the development of tolerance. Risks include addiction, accidents and other adverse consequences. Gradual cessation of taking sleeping pills leads to improved health without worsening sleep. It is advisable to prescribe sleeping pills only for a few days at low effective dose, and in older people, if possible, avoid taking sleeping pills altogether.
New connections
More recently, a number of non-sedating anxiolytic drugs derived from the same structural families as the Z-drugs, such as pagoclone, have been developed and approved for clinical use. Nonbenzodiazepine drugs act much more selectively than the older benzodiazepine anxiolytics, producing effective relaxation for anxiety/panic with little or no sedation, anterograde amnesia, or anticonvulsant effects, and thus potentially more effective than the older ones sedatives. However, anxiolytic nonbenzodiazepines are not widely used and many have failed after initial clinical trials, stopping many projects, including alpidem, indiplon and suriclone.
This instruction is provided only for informational purposes and in no way encourages or encourages you to perform an abortion with pills yourself!
Please note Special attention! Before taking medications, consultation with a gynecologist is required!!!
Dosages of Mifepristone and Misoprostol
All dosages in our complex for MA are selected according to latest recommendations WHO (link to official World Health Organization recommendations for safe abortion).
For: Mifepristone – 200 mg
Our complex uses Ginestril (the brand name of the drug containing Mifepristone): 4 tablets of 50 mg.
For: Misoprostol – 400 mcg
Our kit uses Cytotec (the brand name of the drug containing Misoprostol): 2 tablets of 200 mcg.
Please note that the dosages indicated are current. only for our drugs from the world's leading manufacturers, the quality of which we guarantee!
For other manufacturers (China, Vietnam), the doses may increase significantly; we cannot in any way guarantee the success of the procedure with drugs not purchased from us, and we also do not comment on the numerous side effects and complications that arise after taking untested drugs.
IN Lately cases of attempts to use only one drug - Cytotec - in large doses to terminate a pregnancy have become more frequent.
Urgently NOT recommended do this!
Firstly, this is fraught with very serious complications.
Secondly, efficiency this method does not exceed 30-40% (in other words, in most cases it is Lost time and wasted money).
There is an official and very effective technique medical abortion. Don't ruin your own health!
Procedure for taking medications for Medical abortion
The drug administration procedure consists of two stages.
First stage. Taking Mifepristone
Before the procedure it is necessary be sure to do an ultrasound of the pelvic organs to determine the duration of pregnancy and the location of the fertilized egg (exclude ectopic pregnancy).
To begin the medical abortion procedure, the patient must take 200 mg of Mifepristone orally with water (at least 150 ml).
Most often, after taking the first drug (Mifepristone), a woman subjectively feels nothing. THIS IS THE NORM! The main effect begins in the second stage - after taking Misoprostol.
And only in in some cases minor problems may begin bloody issues And aching pain lower abdomen. This is also normal, but much rarer.
Action of Mifepristone
Mifepristone is a progesterone blocker (this is the main hormone that maintains pregnancy). The main effect of the drug during medical abortion is to stop the development of pregnancy. Mifepristone also significantly increases the sensitivity of uterine cells to prostaglandins (in particular, Misoprostol).
Second phase. Taking Misoprostol
36-48 hours after taking Mifepristone, you must take the second drug from the complex - Misoprostol (Cytotec) in the following dose: 2 tablets of 200 mcg.
There are three ways to take Misoprostol:
- place under the tongue (sublingual);
- vaginally (deep in posterior arch vagina) and
- buccally (place the tablet in the space between the cheek and gum).
The strength of the effect is the same for all methods, but we strongly recommend dissolving one tablet under the tongue first, and then a second one after 40-60 minutes. At the same time, the likelihood of vomiting is significantly reduced, and the duration of the effect increases.
Action of Misoprostol (Cytotec)
Misoprostol against the background of the action of Mifepristone stimulates the contractile activity of the uterus, which leads to cramping pain in the lower abdomen, as well as the appearance (much more often) or intensification (if it appeared at the first stage) of bloody discharge. Against the background of these processes, the fertilized egg is separated from the walls of the uterus and released through the genital tract.
After taking medications
Usually, over the next 3-5 days, spotting is observed (usually a little heavier than menstruation). Possible duration bleeding (with decreasing intensity) is 12-14 days.
After 10-14 days from the onset of bleeding, it is necessary to carry out a control ultrasonography pelvic organs. If bleeding continues, ultrasound should be delayed.
Briefly about the possible complications of medical abortion. Remedies
General symptoms
The following symptoms may occur during the use of Mifepristone and Misoprostol:
- Dizziness;
- Headache;
- Nausea;
- Vomit;
- Feeling of discomfort;
- Weakness;
- Increase in body temperature to 37.5 degrees
- Diarrhea.
Typically, these symptoms are mild and disappear without medical intervention.
If vomiting occurs within one hour after taking Mifepristone or Misoprostol, then you must take the corresponding drug in the same dose.
If the patient has severe early toxicosis pregnancy (vomiting of pregnant women), then before using the complex for medical abortion, it is necessary to administer Cerucal intramuscularly, 2.0 ml, after 30 minutes, take food (in a small volume), and then apply the drug.
Pain
Pain during medical abortion can be of varying intensity and depends on the duration of pregnancy (pain intensifies with increasing gestational age), as well as on the individual sensitivity threshold. Usually the pain is tolerable and does not require additional interventions. According to women, the pain is somewhat stronger than during menstruation.
The pain usually goes away within 1-3 days after the fertilized egg is released. To eliminate severe pain, it is possible to use antispasmodics, for example, No-shpu.
Please note that the use of non-steroidal anti-inflammatory drugs (NSAIDs) (most analgesics, for example Analgin, Paracetamol, Ketanov, Nimesulide, etc.) for pain relief is contraindicated, since they block the action of Misoprostol (!), thereby reducing the abortive effect of the complex. Read more about Pain with MA.
Bloody issues
Incomplete abortion
If detected this complication, then vacuum aspiration is necessary to evacuate the remaining fertilized egg. .
Rehabilitation after medical abortion
Abortion by medication completely eliminates mechanical damage uterus, but does not exclude the development of possible functional disorders as a result of hormonal stress. To prevent the development of such a pathology, all patients who have undergone medical termination of pregnancy are recommended to menstrual cycles take monophasic combination oral contraceptives(for example, Regulon). You need to start taking contraceptives from the fifth day from the start of menstrual-like discharge during a medical abortion.
This page describes how to use Mifepristone and Misoprostol (Cytotec) for medication interruption early pregnancy.
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