Buspar (Buspirone)

Pharmacological action - anxiolytic, antidepressant. Selectively blocks presynaptic dopamine receptor and raises speed of excitation dopamine neurons average brain, selectively activate (partial agonist) serotonin receptors subtype 1А (5-НТ1А).
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I will tell about the operational experience with Buspar. As anxiolytic Buspar it is not justified both because of side effects, and because of ignorance of many doctors about specificity of work with this preparation: action develops in a current of month, and at patients preliminary treated benzodiazepines can be stretched and on much longer. It is good for combining at the beginning with a day lung benzodiazepine and especially with Phenibut - it strengthens action Buspar and eliminating many side effects, shortens approach term anxiolytic effect. The reason of underestimation Buspirone is non-observance of the scheme of reception as the doctor, and the patient: in the beginning it is given 10-15mg in the day, broken into three receptions, sometimes it is effective in second half of day to give during the lunchtime and a supper on 5mg, and for the night - 10mg. Side effects especially in the first days it is weariness, nervousness, a nausea, vomiting, pains in right hypochondrium etc. (From outside G.I. tract); Nasal bleedings, instability of arterial pressure, change of hepatic parametres - all it meets. It is often observed tachypnea and tachycardia (perhaps, in 100 % of cases) - but it is all passes quickly enough. The preparation is heavy enough - can be used even as soporific. It is transferred approximately as well as SSRI, but it is easier and with the specificity... The Main highlight of a preparation - analgetic activity! Expectancy effect - the big obstacle, but a preparation it is capable to kill the most different pains, and even muscle relaxantions!
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Has forgotten to mention the most important side effect! This special dizziness which develops at the first receptions and especially in the big dose, it can cause a faint in some. Terrible in this dizziness anything especially is not present - it soon passes, and in the course of treatment disappears, but can strongly frighten. Therefore I would recommend to those who will use this preparation as anxiolytic, the first receptions to spend in a quiet place as at head assignment this very unpleasant phenomenon though lasts not for long aside is observed.

Serenal (Oxazepam, Tazepam)

Serenal On a structure and pharmacological properties it is similar with Elenium and Valium, less sharp an effect, than Valium however has. Oxazepam is a little less toxic, it miorelaxant the effect is less expressed, anticonvulsive properties weak. It is in certain cases transferred better, than Valium and Elenium. Apply at neurosises, psychopathys, neurosis-like and psychopathy-like conditions, and also at infringements of a dream and convulsive conditions.

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On what would be desirable to pay attention. Often a preparation underestimate, as "not expressed, greased effect" is sometimes observed false is нетак. Serenal - powerful enough the BD, but action after intake comes gradually it it is important to consider, since it is possible and to overdose to reach (!) At intake 10-20 mg a preparation, its initial action starts to be felt within 20-30 minutes - many wrongly believe that it and is "action Oxazepam", no, completely action Serenal reaches peak after an hour-two (!). At monotherapy, or in a complex about the antidepressants, it is necessary to consider that to a preparation tolerance (not dependence) quickly enough develops, and at application of it a BD it is necessary to distribute carefully dosages on a course. In the first days "starting" doses - 10-20 mg are appointed, and the next days the daily dose of a preparation should be increased, however thus it is necessary to consider a condition of a liver of the patient - if there not everything is all right it is better to use more high-speed and strong, demanding small doses, the BD as Serenal the liver strongly enough can strain and GI tract as a whole - can be observed a pain in the field of a liver, discomfort, anausea, vomiting - consider that it already metabolite, and its action in an organism specific rather. I met glue sniffers who accepted on 20 tablets on time, and were dissatisfied with action, however after some hours many of them appeared either in resuscitation, or in SSRI (because of a coma, or inadequate behaviour after effect "disclosing" Oxazepam after some hours). At combinations with analgetics it is necessary to consider some tardive effect approaches - Serenal it is perfectly combined with psychoactive drug which reach the maximum concentration in blood after an hour-two: tablets Oxazepam can be drunk successfully in common with many SSRI (which not ingibit the enzymes of a liver responsible for a metabolism Tazepam - I such the antidepressants do not know even among SSRI - basically they are successfully combined with Oxazepam, but
nevertheless effect of a DB less we will feel - I write off it on activity the antidepressant).
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So, after intake, preparation action develops in a current of hour-two, and lasts long enough, but it is less expressed than at Valium that, on the one hand does not promote abusing this BD, however in a current of course of treatment the effect quickly enough dies away, and escalating of doses is required is, clearly, badly, therefore it is necessary to calculate very carefully preparation dosages smoothly to begin, finish to an admissible maximum, and then smoothly to lower these dosages. At the beginning the preparation is perfectly combined with many SSRI at people in whom SSRI cause agitation and insomnia in the first days; on a hand plays smoothness of action Serenal, and a course of a preparation it is quite enough for achievement of effect of many the antidepressants.

Xanax (Alprazolam)

Xanax concerns a subgroup triazolobenzodiazepines and enters into number 7 of the most popular preparations made in USA. Effects xanax have been in detail studied in laboratory of psychopharmacology of Institute of pharmacology. It is established that the given preparation possesses all basic displays of action which are peculiar benzodiazepines tranquillizers: anxiolytic, anticonvulsive, sedative, hypnotic, relaxante. However it possesses also a number of features which allocate it from the general group tranquillizers. The range of average doses xanax makes 0,25-4,5 mg/day, is thus observed accurate dosedependence effects. On anxiolytic it is essential activity Xanax, almost in 3 times, surpasses Valium, Rudotel, Buspirone. It does not concede In an average therapeutic dose (1 mg) powerful tranquillizers Rivotril and Ativan, but at application
of higher doses (to 5 and even 10 mg) have smaller activity, than these preparations.

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The important feature anxiolytic effect Xanax is that it is not accompanied, as at others ataractics (Klonopin, Valium, Buspirone) sedative. The preparation has much bigger therapeutic width in comparison with others tranquillizers and большее stratification sedative, relaxante and anxiolytic action that defines its smaller side effects.

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Alprazolam possesses moderated hypnotic effect, practically without breaking dream structure, causing only some reduction of 3 and 4 stages and a paradoxical phase of a dream. The basic hypnotic effect is expressed in period reduction dropping-off to sleep, increase in duration of a dream and decrease in quantity of night awakenings. Unlike traditional benzodiazepines, xanax possesses to straight lines independent antidepressant effect. Besides, it possesses expressed antistress and antipanic action. Primary mechanisms antidepressant effect a preparation remain incomprehensible, however is established that the preparation can exasperate noradrenergic transfer.

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Essential interest is represented by experimental data that Xanax possesses positive cardioprotector action. The basic application in clinic Xanax has found in quality anxiolytic, antidepressant and antipanic means. It shows efficiency at neurosises, secondary neurotic frustration at somatic patients. At patients with functional and organic diseases of nervous system, a gastroenteric path and a skin, and also at abstinent syndrome at alcoholics.

Tranquillizers (anxiolytics, ataractics): all of them!(Part2)

Anxiolytic action tranquillizers appears to reduce the emotional lability, withdrawal of mental stress, anxiety, fear, and their corresponding autonomic and endocrine changes. Man takes life more calmly, critically, able to make correct and deliberate actions, without too much emotion in stressful situations. These properties are manifested only when tranquillizers neurotic disorders. When psychosis (schizophrenia, manic-depressive psychosis, epilepsy, Organic lesions of the brain) tranquillizers are not effective. They fundamentally do not change picture of the disease, although they may reduce its flow. This is an important feature tranquillizers.

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Sedative effect is to remove the excessive excitation and motor activity in improving the process of sleep and increased sleep duration without significant changes in its structure, to enhance the action on the central nervous system of general anesthetics, ethanol. Sedative effect of weakly expressed in "daily" tranquillizers (Mezapam, Rudotel, Anxitol, Mebicar, Adaptol, Trioxazin, Sedoxazin). This type of activity should be taken into account in the appointment of persons working with moving machinery drivers, operators, as tranquillizers decrease the concentration of attention and precision performance.

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Activating effect observed while taking small doses of drugs with low sedative effect. There has been a recovery initiative, communication, courage to make responsible decisions. This effect is a consequence of the higher functions unbraking central nervous system.

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Soporific effect is typical for all benzodiazepines. Manifested in the acceleration of falling asleep, increasing the total duration of sleep, decrease in deep sleep. In neurotic disorders of sleep is also due to the normalization of anxiolytic action. Typically, soporific effect proportionally sedative effect. If sleeping problems preferred drugs with a long (Phenazepam, Nitrazepam, Radedorm, Dormicum, Eunoctin) or short (Temazepam, Signopam, Oxazepam, Aplakil, Seresta) type of action.

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Muscle relaxation effect evident decrease tone and force cuts in skeletal muscle. In the reinforcement function based on the segmental inhibitory control of excitability of motoneurons. The chemical nature of this phenomenon is also GABA-ergic, because benzodiazepines potentiation work intercalated GABA-ergic neurons, regulating motor reflex reaction. Through this mechanism, benzodiazepines are heterospecific antagonists poisoning convulsive poisons, which block the receptors GABA, such bicucullin and picrotocsin.

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Anticonvulsant action inherent in all benzodiazepines and fairly universally in respect of different genesis convulsions (epilepsy, poisoning convulsive poisons, neuroinfection etc). The most effective means of anticonvulsant Phenazepam, Valium, Serensin, Eridan, Nitrazepam, Neozepam, Lorazepam, Ativan, Duralozam. The mechanism of action is linked to the ability of drugs to suppress paroxysmal discharge in hippocamp via the GABA-receptors.

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Amnestic action tranquillizers seen with long-term use, is to reduce operational and short-term memory. The phenomenon of reversible, takes place after the abolition of tranquilizers, although not immediately.

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Indications for the use of tranquillizers extremely broad. However, it should be remembered that the appointment of uncontrolled drugs can lead to drug dependence.

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1) The border of the state in the form of neurotic reactions, neuroses, psychopathic. Funds under specified conditions of choice, since such expressions as fear, anxiety, tension is included in the "core" structure of these diseases.

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2) Psihosomatics disease (angina, myocardial infarction transferred, cardialgia, aggravation of hypertension, peptic ulcer, bronchial asthma, etc.), the genesis of which is important psychogenic factor.

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3) Epileptic status, epilepsy, muscular gipertonus as a result of the central nervous system injury, stroke. Used as a means of urgent (emergency) treatment.

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4) In surgery, consisting of premedication in connection with a high patient's emotional reaction to the forthcoming operation. In pediatrics, comprising ataralgesia to conduct transactions with preserved consciousness (similar to neuroleptanalgesia).

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5) For the prevention of stress in healthy people in extreme situations, including during the conduct of hostilities, after the disasters etc. It is important to remember that tranquillizers diminish attention and accuracy of performance, so they can not be applied to drivers, pilots, vysotnikam et al. The most preferred "daily" tranquilizers.

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Most of tranquilizers to soak slowly from the gastrointestinal tract and slowly metabolize in the body. The main way to metabolism - glucuronidation. Tranquilizers well enter all organs and tissues, it is easy to penetrate through biological barriers.

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For the duration of action drugs are divided into three groups:

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-Short duration (half-life period is less than 10 hours):

Oxazepam, Seresta, Grandaxin, Tofizopam, Temazepam, Signopam.

Drugs of choice for the treatment of sleep disorders;
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-Long-acting (half-life period 15 - 20 hours):

Valium, Diazepam, Relanium, Chlordiazepoxide, Elenium, Benzodiapin, Phenazepam, Radedorm,
Sereneh, Epinelbon, Nitrodiazepam.

The drugs of choice for the anxiolytic, sedative and anticonvulsant therapy;
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-Overlong action (half-life period of up to 100 hours): Flurazepam, Dalmadorm, Catazalam. Practical applications are not yet clearly defined.

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Tranquilizers are powerful psychotropic agents with a relatively large breadth of therapeutic action. Toxicities observed with the 5-10 fold increase in therapeutic doses. Typically, using an average therapeutic dose, slowly increasing up to their anxiolytic effect. High doses (up to multiples of 5-10 and above) used in a psychiatric clinic. Duration of treatment tranquilizers should not exceed 6-12 weeks, usually 4 - 6 weeks, as well as developing tolerance to the drug, requiring a dose increase to achieve the same therapeutic effect as well as possible medication. Type of Drug Dependence - more physical than mental. We recommend the appointment of tranquilizers for 7-10 days with short breaks.

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Widely known specific antagonist benzodiazepines is Flumazenil (Anexate), which has its antagonism against receptors benzodiazepines on transmembrane receptor complex GABAa/Cl-
channel. Flumazenil is used to remove residual effects of benzodiazepines, as well as their overdosage or acute poisoning.

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In appointing the tranquilizers may razvivatsya various side effects. There are several groups of side-effects:

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Mental. There are declining efficiency, mood, drowsiness, muscle weakness, slower psychomotor
action. These effects are due to sedative, soporific, and muscle relaxation properties of tranquilizers.

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Physical. There are unstable blood pressure, tachycardia, muscle weakness, antispasmodic effect on internal hollow organs.

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Dependence. There at the beginning of adaptation, the need to increase the dose, then the development of the typical rebound syndrome, accompanied by sleep disturbance, anxiety, irritability, weakness, headaches, muscle jumps, tremor, palpitation, increased sweating, dizziness, a violation of concentration, nausea, loss of appetite. Developed objective signs of depression, Depersonalization, derealizatsii, increasing sensitivity to the incentives sensory (olfactory, tactile, visual), perceptual disorder, or kinaesthetic illusions.

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Safety of the use of benzodiazepines ataraxics linked to the relatively large therapeutic breadth, ie the ratio between therapeutic and lethal doses substances, the lack of adverse effects on mbolshinstvo functional systems, as well as minimal unwanted interactions with other drugs. Evidence of the possibility of fatal complications in the treatment of derivatives benzodiazepine in therapeutic doses so far, no. Benzodiazepines do not have a clinically significant effect on liver function, endocrine and urinary system. However, it is necessary to bear in mind that benzodiazepines may interact with certain medications and general therapeutics, in some cases, such interaction should rassmatrivatsya as negative.

Tranquillizers (anxiolytics, ataractics): all of them! (Part1)

Tranquilizers - substances selectively eliminate emotional instability, tension, anxiety, fear, with neurotic disorders. The name comes from the Latin word tranquillium - quiet, anxius - anxious, smitten with fear. The term emerged in 1955.

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Divided tranquilizers to "strong" and "daily". Strong tranquilizers (Valium, Diazepam, Alprazolam, Xanax, Clonazepam, Oxazepam, Seresta, Phenazepam, Nitrazepam ... and others) have the most pronounced anxiolytic and sedative effects, a large breadth of therapeutic action, in general, much oppressed by the central nervous system. Daily (Hydazepam, Tofizopam, Mezapam) have a selective effect of stress-tread, do not cause significant sedation, have a minimal negative effect on the mental and physical performance. They concede the effectiveness of drugs for the first group and apply priemuschestvenno on an outpatient basis.

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Currently benzodiazepine derivatives occupy a key position among the tranquilizers. Benzodiazepines have a specific mechanism of action, interacting with benzodiazepines sites of GABA-ergic neurons. Since GABA-ergic synapses morphologically homogeneous and distributed in different departments of central nervous system, benzodiazepines can influence most of the functional entities of the brain. It is believed that the effect of tranquilizers on benzodiazepines receptors leads to increased activity in close association with GABA-ergic systems of oppression, followed by adrenergic and cholinergic systems, changing the activity of noradrenaline and serotonin, play an important role in the regulation of sleep, stress reactions, paroxysmal states.

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Tranquilizers have a set of specific features unique to this group of substances. The spectrum of pharmacological activity of tranquilizers include:

-anxiolytic action;

-sedative effect;

-lack of effectiveness in psychosis;

-activating effect;

-soporific effect;

-muscle relaxation;

-anticonvulsant action;

-amnestic action;

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Some used tranquilizers: (name) \ (average daily dose) \ (half-life period)

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Alprazolam, Xanax \ 1-2 mg per os \ 10-12 h

Bromazepam \ 4-6 mg per os \ 8-20 h

Chlordiazepoxide \ 30-50 mg per os \ 5-30 h

Clonazepam \ 4-6 mg per os \ 20-60 h

Diazepam, Valium \ 14-45 mg per os \ 15-48 h

Oxazepam, Seresta \ 30-50 mg per os \ 8-10 h

Phenazepam \ 2-3 mg per os \ 20-30 h

Nitrazepam \ 5-10 mg per os \ 18-25 h

Temazepam \ 40-50 mg per os \ 5-15 h

Flunitrazepam, Rohipnol \ 1-2 mg per os \ 20-30 h

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...to be continued

Sonapax (Thioridazine)

Weak universality neuroleptics are mainly used in chronic schizophrenia, intrusive state, endogenous depression, states of psychomotor excitation of different genesis; neuroses accompanied by tension, excitation, intrusive state and a sense of fear, ticks, withdrawal symptoms when substance abuse and chronic alcoholism.

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Sonapax also has anxiolytic and antidepressive activity, reduces feelings of tension and anxiety. It has a moderate antipsychotic, antiemetic, antihistamines, adrenoblocking, holinoblocking action.

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The main feature of this drug is a broad spectrum of its actions in the various manifestations of affective disorders. Sonapax reliably eliminates the anxiety, fear, aggressive tension, the state of manic exaltation. In fact, this drug should be considered as unique for its diversity of effects, speaking as a tranquilizer, as neuroleptics, as antidepressant. Sonapax appointed for the treatment of psychotic disorders, anxiety, behavioral disturbances and for the treatment of depressive symptoms. The effectiveness of its so obvious, the more pronounced affective components in the structure of psychopathological syndrome.

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In sonapax generally well tolerated, serious side effects are almost not observed in the application of medium and especially small doses. However, in the appointment of high doses and prolonged admission is possible, though extremely rare, manifestation of arterial hypotension, particularly orthostatic, kardiotoksic effects, sometimes in violation of rhythm, which have a functional and reversible. Neuroendocrine violations may occur in the form of increases in weight, dysmenorhea, lactorhea. Of the neurological side effects very rarely, and probably in the latter stages of therapy may occur akathisia, violation of muscle tone and dyskinesia.

Atarax (Hydroxyzine)

Atarax - not benzodiazepin tranquilizer, but only in exchange for the use of individually tailored doses. This is a drug structurally similar to cinnarizinе and dimedrol, and also has an intermediate effect: it has a sedative effect thanks to central holinolitic effects and can be used in sleeping problems. At the outset of the preparation is expressed sedative component, but soon he has a better anxiolytic effect has analgetics effect, and may be useful in the treatment of neurotic states.

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Characterized expressed sedative effect and moderate anxiolytic activity. Has a positive effect on cognitive ability, improves memory and attention. With no long-term admission syndrome cancel. Has also antiholinergic, spasmolytic, antihistaminic effect. Relaxes smooth muscle, has bronhodilatirytic and analgetics effect, and provides anti miorelaksant effect and a moderate inhibitory effect on gastrointestinal secretion. Reduces itching with hives, eczema, dermatitis et al.

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Sedative effect is usually observed after 10-45 min after ingestion (depending on dosage form), antihistamines - over 1 h after ingestion. In patients with liver diseases antihistamines effect can last up to 96 hours. Use to couping anxiety, psychomotor excitation, internal tension, irritability, with neurological, psychiatric (generalized anxiety and a violation of adaptation) and somatic diseases; abstinence alcohol syndrome; premedication and post-operative period (in a combination therapy), pruritus (symptomatic treatment).

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Atarax - this is an excellent tool in drug abuse, it is well to appoint, with neuroses with the agitation and insomnia. It is well combined with nootropic. This is a drug for certain cases, but it anxiolitic, though, and has sedative effect.

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Atarax in connection with the sedative effect is contraindicated in persons who drive a car, works requiring great concentration of attention or to complex mechanisms (like other tranquilizers!) Now in the course of many atypical, selective anxiolytics-allosteric modulators of receptors of GABA etc - afobazol, etifoksin, mexidol and others. And you need to consult a doctor, describe the problem.

Afobazol

Mild tranquilizer afobazol is a selective anxiolytic, not related to the class of receptor agonists benzodiazepin. Prevents the development of membranozavisimyh changes in GABA-receptor.

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Has anxiolytic effect of activating a component, not accompanied by gipnosedative effect. A lack of preparation neuromuscular relaxant properties, negative impact on the performance of memory and attention. If its application is not a medication and does not develop syndrome cancel.

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Effects of the drug is sold mainly in the form of a combination of anxiolytic and light activation effect. Reducing or eliminating anxiety, tension, inability to relax, insomnia, fear, somatics (muscle, sensory, cardiovascular, respiratory, gastrointestinal symptoms), vegetals (dry mouth, sweating, dizziness), cognitives (difficulty concentrating, weak memory) violations observed at 5-7 days of treatment afobazol. The maximum effect is achieved by the end of 4 weeks of treatment and remains in the posttherapeutic period, an average of 1-2 weeks. Especially shows the use of the drug in patients with predominantly asthenic personality traits as a disturbing valetudinarianism, insecurity, increased vulnerability and emotional lability, tendency to emotional and stress reactions.

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Afobazol there was a positive influence on brain activity (often subjectively perceived the drug as a "light version phenibut"). To sum up - a few days (course afobazola since four weeks!) Is the effect, if afobazol - a lightweight, unobtrusive, no side effects, with some improvement in the subjective sensations in the head and body - not a placebo because the help and those in anyone with circulatory problems of the brain, they say, that occur soon after taking edakie "goose" pleasing to the head. Soft drug to his patient ... and cheap!

Risperdal (Risperidone)

Strong medicine, especially good in the treatment of paranoia. In bipolar affektiv disorder drug well removes the viscosity of thoughts, hinders education delusionals ideas, and, strangely enough, leads to better dropping-off to sleep. But the main problem - it is his impact on the improvement of prolactin...

About Risperidone is better to say that there are no "bad" drugs ..
Good help for chronic delusional symptoms, defective conditions. But a effect on the acute
positive symptoms- unsatisfactory (so I could experience a negative) - treating a young patient with syndrome Kandinsky, Risperidone 6-8 mg / day automatismes and ideas the impact removes, but verbal psevdohallucinosis remains...

Seroquel (Quetiapine)

On the whole, quite good atypical neuroleptic. At the level of prolactin Seroquel almost no influence. Extrapyramidal complications are also rare. This product is a good portability, perhaps one of the best drugs affecting negative symptoms.

It should be noted that unfortunately Seroquel strongly reduces blood pressure and hypotensive patients (blood pressure 90/60), he at least is not recommended when applying with antidepressants (threecycles, SSRIs) is expressed tachycardia.

Sexual dysfunction is not a cause, or they ill-defined. Sometimes it is a set of weights caused by antihistaminic and antiserotoninic actions and improve appetite.

Sulpiride (eglonyl, dogmatil)

As for my patients - the product is good, especially in the treatment of endogenous depression. And given its somatic effect is not fear of serious complications from the gastro intestinal tract. Another point is that the drug induce and prolactinemia and parkinsonism. Long-term treatment, must have for the treatment of mental illness has. Therefore have to appoint a short course of medication.

The drug has a very broad spectrum of activity. In his depressions have different combinations of antidepressants, according to the clinical picture of depression. Given that the majority of AD did not show his timoleptic actions eglonil well as tactical medicine (AD effect fairly soon), and combined well at the doses of 100-200 mg / day with melipramin, amitriptilin, pirazidol, serotoninergic AD fine. Unfortunately, the duration of treatment is limited hyperprolactinemia, but only some.

Sulpirid most (compared to others) raises the level of prolactin. This may be linked such things as ginekomasty and "impotence". Although impotence in the full sense of the word is hardly can be described as following the lifting of the drug after some time, everything should be back to normal. That if these side effects will be celebrated.