In the conditions of modern urban life and increased mental work, a person often experiences unbearable stress. And stress, physical inactivity, the use of stimulants such as coffee, tobacco, alcohol contribute to sleep disturbance. Most often, for the symptomatic treatment of insomnia disorders (this is what insomnia is called), a mild hypnotic, for example, of plant origin, is used.
Good sleeping pills must be effective and safe.
But medical science does not stand still, and such drugs as, for example, peony tincture, "Corvalol" and "Fitosedan" are being replaced by new generation drugs that improve sleep. In addition, they do not cause the side effects of the "classic" remedies. These drugs are referred to as 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, "hypnotics", from the word "hypnosis" are called sleeping pills. According to modern standards, it is necessary to start the treatment of insomnia disorders (that is, insomnia and sleep disorders) with non-drug methods: changing the work and rest routine, walking, going to bed on time, treating diseases that can provoke insomnia, for example, thyrotoxicosis or neurasthenia.
In the event that these measures are not enough, then sedatives of herbal origin are prescribed. They are available over the counter, and nearly all have mild sedative and hypnotic effects. In this case, a weak effect is an advantage, since the degree of sleep disturbance is small. In addition, they are not addictive and have a low price tag.
Perhaps the most effective effect is "Valocordin", due to the content of phenobarbital. It is the only barbiturate available without a prescription as part of Valocordin (Corvalola).
Valocordin has a sedative effect
In the event that sleep disorders become so pronounced that they interfere with work and lead a normal life, then the appointment of "real" sleeping pills is required, which cannot be purchased without appropriate prescriptions.
These drugs previously included barbiturates (Etaminal-sodium, Barbamil, Veronal), then they were replaced by benzodiazepine drugs, which were very actively used all over the world in the 70s - 80s of the XX century. In the USA, for example, there was even a "benzodiazepine epidemic": it was believed that such drugs not only improve sleep and bring in harmony with themselves and the world around them, but also are an excellent prevention of stress.
Time has shown that this is not so: benzodiazepine drugs, for example, nitrazepam ("Radedorm") or "Phenazepam" plunge a person into a deep sleep, but in the morning they cause a feeling of weakness. They also relax muscles (muscle relaxation), which can be dangerous when driving. Also, these drugs cause withdrawal syndrome: the patient is "addicted" to such drugs.
Therefore, the persistent search for such funds continued, which satisfied a very "capricious" list of requirements. So, for example, it is known that a good sleeping pill of the new generation should approach the ideal as much as possible. It should immediately induce sleep, cease its effect no later than an hour after waking up, maintain daytime vigor and efficiency, and not cause addiction and side effects. In this case, the drug should not be used as a sedative medicine, should not affect memory and thinking.
And finally, at the end of the twentieth century, such drugs appeared, they were called Z - hypnotics. They are able to very selectively affect the structures of inhibitory GABAergic (inhibitory) receptors. Scientifically, these drugs are called "non-benzodiazepine agonists of benzodiazepine receptors." Representatives of this family began to enter the world pharmaceutical market in 1993.
The brightest representatives of the family
By tradition, all Z - drugs have an international non-proprietary name, which in Russian transcription begins with the letter "z". Consider the 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". It is an easy and convenient sleeping aid that can be taken for 2 to 3 weeks without much fear. Falling asleep usually occurs (however, as with other drugs of this family) within 1 - 2 hours after administration. Sleep is even and calm, morning awakening is quick, 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 of falling asleep may be lengthened by 1 - 2 hours, but the drug will have less effect on the liver, since Imovan is contraindicated in severe liver and kidney dysfunction.
The cost of one package of "Imovan" (according to 2016) is, on average, 250 rubles for 20 tablets, for 3 weeks of admission.
Zolpidem
Another of the Z-hypnotics - Zolpidem
The second drug in this family is better known as "Hypnogen" or "Ivadal". You need to take this remedy (as well as other Z-hypnotics) within an hour just before bedtime, or even while lying in bed. Has a good therapeutic breadth: the initial dose is 5 mg, the maximum dose is 10 mg.
It has a significant drawback - high cost. So, a similar number of pills for 3 weeks of administration will 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 remedy can be considered a really strong hypnotic, but with prolonged use, a sharp withdrawal syndrome can develop, which will manifest itself in the form of persistent insomnic disorders. Therefore, this drug should be taken in short courses and in the lowest dosage.
However, an indisputable "plus" is the fact that after taking it, it is completely excreted from the body within 1 - 2 hours, therefore, against the background of taking zaleplon, daytime drowsiness never occurs.
Its recommended dose is the same as the maximum dose - 10 mg. It is recommended to take it a couple of hours after a meal, 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 of Andante is zaleplon
The cost of zaleplon drugs is on average 460 rubles, but only for 7 tablets.
Therefore, in terms of the weekly rate, we get:
- zopiclone 12.5 rubles;
- andante 460 rubles;
- ivadal 850 rub.
It should be recalled that these drugs are only sold by prescription. Maybe this is an unnecessary precaution (after all, these drugs are relatively safe), but this is the way to be done in relation to all sleeping pills. After all, earlier, when barbiturates were sold without a prescription, their overdose was often fatal, and they were used to commit suicide attempts and various crimes.
All Z-hypnotics are dispensed strictly according to the doctor's prescription.
In conclusion, we note that in case of severe sleep disorders, these drugs should become the basis of drug treatment, with zopiclone and zolpidem having a medium-term effect, and zaleplon being an ultra-short, "point" drug for insomnia.
The positive aspects of these remedies are the absence of disturbed breathing during sleep and the minimum risk of sleep apnea, as well as a vigorous awakening and well-being during the day.
But nevertheless, modification of the patient's lifestyle should be considered the ideal option for the treatment of insomnic disorders, and joint efforts should be made, both by the patient and the doctor, to normalize sleep by physiological methods, leaving medications "in reserve".
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Non-benzodiazepines (sometimes colloquially called "Z-drugs") are a class of psychoactive substances similar to benzodiazepines in nature. The pharmacodynamics of non-benzodiazepines are almost identical to those of benzodiazepines, 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 act by binding and activating the benzodiazepine site of the receptor complex.
History
Non-benzodiazepines have been shown to be effective in the treatment of sleep disorders. There is limited evidence to suggest that tolerance to non-benzodiazepines develops more slowly than to benzodiazepines. However, data are limited, so no conclusions can be drawn. There is also limited data on the long-term effects of non-benzodiazepines. There are some differences between the Z-drugs, for example, zaleplon does not induce tolerance and 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 to treat mild insomnia. They are safer than older generation barbiturates, especially in overdose, and, compared to benzodiazepines, have a lower tendency to induce physical dependence and addiction. Z-drugs have gained widespread popularity as a treatment for insomnia, especially in elderly patients. Long-term use of such drugs is not recommended, as the patient may develop tolerance and addiction. A survey of patients using non-benzodiazepine Z-drugs and benzodiazepine sedatives showed no difference in the reports of side effects reported by 41% of users. Z-drug users were more likely to report trying to quit taking sleeping pills than benzodiazepine users. The effectiveness of the drugs did not differ either.
Side effects
Z-Drugs are not without 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 activities, including cooking or driving, while unconscious and subsequently having no recollection of the events that occurred upon awakening. Although this effect is quite rare (and is also seen with some older sedatives such as temazepam and secobarbital), it can be potentially dangerous, so the search continues for new compounds with improved side effect profiles. Daytime anxiety associated with discontinuation can also occur as a result of persistent nocturnal use of non-benzodiazepines such as zopiclone. Side effects of drugs in this class may differ due to differences in metabolism and pharmacology. For example, long-acting benzodiazepines can accumulate in the body, especially in the elderly or those with liver disease. Short-acting benzodiazepines are associated with a higher risk of more severe withdrawal symptoms. In the case of non-benzodiazepines, zaleplon may be the safest in terms of sedation the day after administration, and unlike and, zaleplon does not increase the risk of road accidents, even when used in the middle of the night, due to its ultra-short half-life.
Increased risk of depression
It has been claimed that insomnia can cause depression, which suggests that insomnia medications may help treat depression. However, an analysis of the data from clinical trials submitted by the FDA in relation to, and, showed that these sedative-hypnotics more than double the risk of developing depression compared to placebo. Sleeping pills, therefore, may be contraindicated in patients suffering from or at risk of depression. Sleeping pills lead to depression rather than relieve it. Studies have shown that long-term users of sedative sleeping pills have a markedly increased risk of suicide, as well as an overall increased risk of death. 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
Non-benzodiazepine use should not be discontinued abruptly if the drug is taken for more than a few weeks, because of the risk of relapse and acute withdrawal reactions, which may resemble those seen with benzodiazepine withdrawal. Treatment usually involves a gradual dose reduction over weeks or several months, depending on the patient, dosage, and length of treatment time. If this approach does not work, you can try switching to an equivalent dose of long-acting benzodiazepines (eg, chlordiazepoxide or), followed by a gradual dose reduction. In extreme cases, and in particular in the presence of severe dependence and / or abuse, an inpatient detoxification may be required c.
Carcinogenicity
The Journal of Clinical Sleep Medicine published a systematic review of the medical literature on anti-insomnia drugs and raised concerns about benzodiazepine receptor agonists, benzodiazepines, and Z-drugs used as hypnotics. The review found that nearly all trials of sleep disorders and drugs were sponsored by the pharmaceutical industry giants. It found that the ratio of positive results favorable to the industry in industry-sponsored trials was 3.6 times higher than in studies not sponsored by the industry, and that 24% of authors did not disclose that their published work was funded by pharmaceutical companies. The document pointed out that there is little research into hypnotics that is independent of drug manufacturers. The author expressed concern about the lack of discussion of the side effects of benzodiazepine agonists, for example, a significant increase in the risk of infection, cancer and increased mortality in hypnotic trials and an over-emphasis on positive effects. No hypnotic manufacturer has attempted to disprove the epidemiological data showing that the use of their product is correlated with increased mortality. The author stated that "in the main trials of hypnotics, the potential adverse effects of hypnotics, such as daytime weakness, infections, cancer and death, need to be examined in more detail, and the balance between benefits and risks should be weighed." In clinical trials of these non-benzodiazepine hypnotics, a significant increase in the risk of skin cancer and tumor development was found compared with placebo. Other cancers such as brain, lung, bowel, breast and bladder cancers have also been observed. Users of non-benzodiazepines also showed an increased risk of infections, possibly due to weakened immune function. It is assumed that the reason for the increased risk of developing cancer was either suppression of immune function or the viral infections themselves. Initially, the FDA was hesitant about approving some non-benzodiazepines due to concerns about an increased risk of cancer. The author advised that because the FDA requires the reporting of favorable and unfavorable results from clinical trials, the FDA's New Medicinal Supplement data is more reliable than the peer-reviewed literature. In 2008, the FDA reviewed its data again and confirmed the increased risk of cancer in randomized trials of drugs compared to placebo, but concluded that the risk of cancer was not related to the need for regulatory action.
Elderly patients
Non-benzodiazepine hypnotics, similar to benzodiazepines, cause disturbances in body balance and stability when standing in individuals who wake up during the night or the next morning; falls and hip fractures are frequently reported. Combined use with alcohol enhances these disorders. In relation to these violations, a partial, but incomplete, tolerance develops. In general, non-benzodiazepines are not recommended for older patients due to the increased risk of falls and fractures. A detailed review of the medical literature regarding the management of insomnia, including in the elderly, has shown that there is sufficient evidence for the efficacy and long-term benefits of non-drug treatment of insomnia in adults of all age groups. Compared to benzodiazepines, non-benzodiazepine hypnotics and sedatives show little benefit in efficacy or tolerability in the elderly. It has been found that new drugs, such as melatonin agonists, may be more suitable and effective treatments for chronic insomnia in the elderly. Long-term use of sedative sleeping pills for insomnia has no evidence base and is not recommended due to possible side effects such as cognitive impairment (anterograde amnesia), daytime sedation, impaired motor coordination, and an increased risk of road traffic accidents and falls. In addition, the efficacy and safety of long-term use of these agents remains to be determined. It concluded that further research is needed to assess the long-term effects of treatment and the most appropriate treatment strategy for older people with chronic insomnia.
Controversy
A literature review of hypnotic drugs, including non-benzodiazepine Z-drugs, concludes that the use of such drugs is associated with an unjustified risk to human health and there is no evidence of long-term efficacy due to the development of tolerance. Risks include addiction, accidents and other adverse effects. The gradual cessation of sleeping pills leads to better health without worsening sleep. It is advisable to prescribe sleeping pills for only a few days at a low effective dose, and in older people, if possible, avoid taking sleeping pills altogether.
New connections
More recently, a number of non-sedating anxiolytics have been developed, derived from the same structural families as the Z-drugs, for example, and pagoclone, and these drugs have been approved for clinical use. Non-benzodiazepine drugs work much more selectively than older benzodiazepine anxiolytics, inducing effective relaxation in anxiety / panic attacks with little or no sedation, anterograde amnesia, or anticonvulsant effects, and are thus potentially more effective than older anti-anxiety drugs. However, anxiolytic non-benzodiazepines are not widely used and many have failed after initial clinical trials, halting many projects including alpidem, indiplon, and suriclone.
This instruction is provided only for informational purposes and in no way encourages or encourages abortion with pills on your own!
We pay special attention! Before taking medications, a consultation with a gynecologist is required !!!
Dosages of Mifepristone and Misoprostol
All dosages in our complex for MA are selected according to the latest WHO recommendations (link to official recommendations of the World Health Organization for safe termination of pregnancy).
For: Mifepristone - 200 mg
Our complex uses Ginestril (brand name of the drug containing Mifepristone): 4 tabs of 50 mg each.
For: Misoprostol 400 mcg
Our kit uses Cytotec (brand name of the drug containing Misoprostol): 2 tabs, 200 mcg each.
Please note that the indicated dosages are relevant. only for our preparations from the world's leading manufacturers, the quality of which we guarantee!
For other manufacturers (China, Vietnam), the doses can be increased several times, we cannot guarantee the success of the procedure from drugs purchased not from us, and we also do not comment on the numerous side effects and complications that arise after taking unverified drugs.
Recently, there have been more cases of attempts to use only one drug - Saitoteka - in large doses in order to terminate pregnancy.
Strongly DO NOT RECOMMEND do it!
First, it is fraught with very serious complications.
Secondly, the effectiveness of this method does not exceed 30-40% (in other words, in most cases this is wasted time and money wasted).
There is an official and very effective method of medical abortion, tested on millions of cases. Don't ruin your own health!
Procedure for Taking Medication for Medical Abortion
The medication procedure consists of two stages.
First step. Taking Mifepristone
Before the procedure, you must be sure to do an ultrasound of the pelvic organs to determine the duration of pregnancy and the location of the ovum (exclude ectopic pregnancy).
To start 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 at the second stage - after taking Misoprostol.
And only in some cases minor spotting and aching pains in the lower abdomen may begin. This is also a normal course, but much more rare.
Action of Mifepristone
Mifepristone is a progesterone blocker (this is the main hormone that keeps pregnancy). The main effect of the drug in medical abortion is to stop the development of pregnancy. Also, Mifepristone significantly increases the sensitivity of uterine cells to prostaglandins (in particular, to Misoprostol).
Second phase. Taking Misoprostol
After 36-48 hours from the moment of taking Mifepristone, it is necessary to take the second drug from the complex - Misoprostol (Cytotec) in the following dose: 2 tablets of 200 mcg each.
There are three ways to take Misoprostol:
- place under the tongue (sublingually);
- vaginally (deep into the posterior fornix of the vagina) and
- buccal (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 that first dissolve one tablet under the tongue, and after 40-60 minutes the second. This significantly reduces the likelihood of vomiting, 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 pains in the lower abdomen, as well as the appearance (much more often) or intensification (if appeared at the first stage) of bloody discharge. Against the background of these processes, the ovum is separated from the walls of the uterus and excreted through the genital tract.
After taking medications
Bloody discharge is usually observed over the next 3-5 days (usually a little more profuse than menstruation). The possible duration of spotting (with decreasing intensity) is 12-14 days.
After 10-14 days from the onset of bloody discharge, it is necessary to conduct a control ultrasound examination of the pelvic organs. If the bleeding continues, the ultrasound should be delayed.
Briefly about the possible complications of medical abortion. Remedies
Common Symptoms
With the use of Mifepristone and Misoprostol, the following symptoms may occur:
- Dizziness;
- Headache;
- Nausea;
- Vomit;
- Feeling uncomfortable
- Weakness;
- Increase in body temperature to 37.5 degrees
- Diarrhea.
Usually, these symptoms appear slightly 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 a pronounced early toxicosis of pregnancy (vomiting of pregnant women), then before using the complex for medical abortion, it is necessary to inject intramuscularly Cerucal, 2.0 ml, after 30 minutes take food (in a small amount), and then apply the drug.
Pain
Pain during medical abortion can be of varying intensity and depends on the duration of pregnancy (with an increase in gestational age, the pain increases), as well as on the individual threshold of sensitivity. Usually the pain is tolerable and does not require additional intervention. As women say, the pain is somewhat stronger than during menstruation.
Painful sensations usually disappear within 1-3 days, after the release of the ovum. To eliminate severe pain, it is possible to use antispasmodics, for example, No-shpu.
It should be noted that the use of non-steroidal anti-inflammatory drugs (NSAIDs) is contraindicated for pain relief (most analgesics, for example, Analgin, Paracetamol, Ketanov, Nimesulide, etc.), 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 this complication is detected, then vacuum aspiration is necessary to evacuate the remnants of the ovum. ...
Rehabilitation after medical abortion
Termination of pregnancy with medication completely eliminates mechanical damage to the 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 take monophasic combined oral contraceptives (for example, Regulon) for two menstrual cycles. You need to start taking contraceptives from the fifth day after the onset of menstrual discharge during medical abortion.
This page describes how to use Mifepristone and Misoprostol (Cytotec) for early medical abortion.
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