Diazepam

Chemical name

7-Хлор-1,3-дигидро-1-мети л-5-фенил-2H-1,4-бензодиа��епин-2-он

Gross

C16-H13-Cl-N2-O

Characteristics

Anksiolitik, derivative Benzodiazepina.bely or white with weak yellowish white crystalline powder and odourless with a molecular mass of 284.74. Virtually nerastvorim water, it is difficult soluble in alcohol, soluble in chloroform.

Of drugs

Drugs, the anxiolytic, protivosudorozhnoe, miorelaksirutee (central), sedative, sleeping. Interacts with specific receptors benzodiazepinovmi located in postsinapticescom Gamk_a-retseptornom compound in the limbic system of the brain, talamuse, Hypothalamus, upstream activating retikuliarna formations barrel brain and neuron inserted horns lateral spinal cord. Increases sensitivity to Gamk-retseptorov mediatoru (GABA), which leads to an increase in the frequency of opening zitoplazmaticescoy neuronal membrane channels for incoming currents chlorine ions. As a result, increasing braking power GABA and braking межнейронной reference to the divisions ЦНС.Анксиолитическая activity is the ability of pain domestic anxiety, fear, anxiety, stress. Provides антипаническое and амнестическое (mostly in Injecting application) действие.При treatment of sleep disturbance of diazepam, as a means to correct it where a welcome anxiolytic effect throughout дня.Центральный миорелаксирующий effect linked to the braking полисинаптических spinal рефлексов.Обладает expressed противосудорожным effect used in medicines for the treatment of convulsions paroxizmov, mental equivalents, for cupping epileptic Statusa.pri acute alcohol withdrawal made from symptoms such as agitation nervous tension, anxiety, anxiety, tremor, as well as reduces the risk of developing or signs of acute crisis deliria, incl. галлюцинации.Эффекти��ен in the liver in adults with acute conditions involving motor excitation, convulsions and Dr.sedativei effect observed in a few minutes after the on / in the introduction and in 30-40 minutes after the / m. After acute withdrawal symptoms diazepam appoint Vnutri.v anesthesiological practice used to reduce fear, anxiety, tension and reduce acute stress reactions in predoperatinom period and the complex, including diagnostic, intervention in therapy and surgery. The latter may weaken patient memories of the procedure (elektroimpoulsnaya therapy, O heart endoscopic procedures vpravljenie bruising and repozice bone fragments, biopsies, tubal burn wounds, etc.). Diazepam enhances the effectiveness of induction narcosis (premedikation using diazepam may reduce fentanyl dose required for the to be effective with the opening anaesthesia, and to reduce the time before your consciousness through induction doses). Increases pain threshold sensitivity to antiaritmicescoe act lowers AD (with the rapid on / in the introduction). Decreases night secretion of digestive juice. Has the ability to make capital vnutriglazna liquid or increase its secretion, and thereby increase the inner Davljenie.v experimental studies showed that ELD_50 diazepam when administered at 720 mg / kg (mouse), and 1240 mg / kg (rats). Reproduction study in rats to the reception of diazepam in doses 1, 10, 80 and 100 mg / kg inside for 60-228 days prior to the crossing showed that at doses of 100 mg / kg has been a decline in the number of pregnancies and offspring survival (possibly at the expense of sedative action leading to a decline in interest in the cross and vcarmlivaniu progeny). Doses of less than 100 mg / kg not affected by mental выживаемость.Исследо��ание in rabbits to the reception of diazepam in doses of 1, 2, 5 and 8 mg / kg from the 6th to the 18th day of pregnancy revealed no adverse effects on reproduction and tertogennogo Actia.posle intake of fast and well (about 75% of dose) of the skin glands. After the / m of fully absorbed, but at a slower pace than in ingestion (speed intake depends on the place, the largest, with the introduction of the deltoid muscle). In a Rectal diazepam solution

Indications

As a sedative, and anksioliticski believed Sredstwa.neurologia and psychiatry. All disturbing disorders, including neuroses, Psychopathy, and неврозоподобные психопатоподобные state accompanied by anxiety, fear, increased hadst, emotional stress; disturbing syndrome in endogenous mental illnesses, including with schizophrenia (adjuvant treatment in a comprehensive therapy), with organic lesion in the brain, including with cerebrovascular diseases (in a combination therapy as a further means); senesto-ipohondricescie, obsessions and fobicakie disorders, параноидально-галлюц��наторные status; somatovegetativee violations dwigatelnoe bring different etiology in neurology and psychiatry; headache voltage; sleep disturbance; vertebrogenic syndrome; withdrawal syndrome (alcohol, drugs), including : deliri alcohol (composed of combination therapy). In paediatric practice : repentance and the neurozopodobne accompanied by emotional stress, anxiety, fear, increased hadst, headaches, human sleep disorder, mood disorders and behavior, etc. Cardiology. Angina, myocardial infarction arterial hypertension, etc. Anaesthesiology and surgery. Premedikation before and immediately prior to the operational interventions and endoscopic procedures anaesthesia induction, as a component of the combined narcosis (with ataralgesia combined with analgetikami). OBGYN. Eclampsia, facilitating delivery (for injecting), premature birth, premature detachment of the placenta (for injecting); Changing pains and psychosomatic disorders. Asian practice. Dermatitis and other diseases associated with everything, hadst (complex therapy). As protivosudorozhnogo Sredstwa.epilepcia (auxiliary means of combination therapy), a nervous status or heavy repeated epileptic seizures (for injecting, adjunct); Stolbnjak.v a miorelaksirutego средства.Спастически�� of the central genesis of the brain injury or spinal cord (cerebral palsy, atetoz); causes skeletal muscles in the local trauma (aid); spasticskie state of other diseases of the bones, myofasciitis, bursitis, arthritis, rheumatoid spondilit, progressive chronic polyarthritis; arthrosis, with a voltage of skeletal muscles.

Restrictions on the use of

Chronic respiratory distress, the syndrome patients during sleep expressed by the human kidney otkratougolnaya glaucoma (in the face of adequate therapy), up to 6 months (only for health reasons in a hospital), pregnancy (II and III Plus).

Pregnancy and lactation

Contraindicated in the first trimester of pregnancy (increases the risk of congenital malformations). In II and III trimester of pregnancy is possible if the expected effect therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, acute liver disease and kidney expressed liver failure, severe male, suicidal tendencies, drug or alcohol dependence (except for the treatment of acute withdrawal syndrome) expressed respiratory distress expressed gipercapnia, cerebral and spinalnaya ataxy, acute glaucoma attack, zakratougolnaya glaucoma, pregnancy (I term), breast-feeding, age up to 30 days.

Side-Effects

From the nervous system and sensory organs : weakness, drowsiness, increased fatigue; Ataxy, diminished emotions, the ambiguity, diplopia, movement, tremor, reduced reaction speed and concentration, impaired short-term memory, dizartria, smazannaya it; Sputannosti consciousness, depression, fear, headache, dizziness; Strange reaction (acute arousal, anxiety, hallucinations, nightmares, fits of rage, misconduct); anterogradnaya Amnesia.so the circulatory system and blood (blood, gemostaz) : aetiology, Neitropenia.so part of the stomach : the slunootdelenia (dry mouth or gipersalivacia), nausea, Zapor.prochie : allergic reactions (urticaria, rash), urinary whose influence, changing face, the increase in the liver transaminaz and alkaline phosphatase, Jeltuha.pri Injecting introduction : reaction at the site of (X, flebit, the formation of skeletal); with the rapid on / in the introduction-gipotenzia, serdern-sosudisty collapse, the effects of external breathing apparatus Icota.vozmozhno development addiction, drug dependency syndrome lifting aftereffect syndrome (muscle weakness, reduced efficiency), rebound-sindroma (see "Precautions").

Specific guidance

It should be borne in mind that anxiety or stress in the day-to-day stress, usually do not require treatment Anxiolitikami.ne be mixed in one sprite diazepam with other drugs (possibly surface preparation on the walls). The on / in the introduction should be inserted into the large blood slowly, controlling respiratory function. There is a need to avoid falling solution into the artery and ekstrawazalnoe space.

Patient interaction

Потенцирует effects of alcohol, and противосудорожных гипотензивных funds doses, tricyclic antidepressants, analgesics (including narcotic analgesics), PP pills, general anaesthetics миорелаксантов, антигистаминных PP with sedative effect. Analeptiki, psihostimulatora-reducing activity. Антациды can reduce speed, but not the intake диазепама.Изониазид slows down diazepam (and increasing its concentration in the blood). Inhibitors mikrosomalnogo oxidation (including zimetidin, ketokonazol, fluvoksamin, fluoxetin, omeprazol) farmakokinetiku change and increase the effect diazepam. Rifampicin reduces the concentration of diazepam in blood. Erythromycin slows diazepam metabolism in the liver. Diazepam can modify plasma concentrations fenitoina.

Overdosing

Symptoms : oppression CNS varying degrees of symptoms (from itching to coma) : expressed drowsiness, lethargy, weakness, reduced muscle strength, ataxy, long sputannosti consciousness, oppression reflexes, coma; It is also possible to gipotenzia, oppression Dahania.lechenie : induction vomiting and the appointment of activated charcoal (if the patient is in the minds of) washed through the stomach probe (if the patient is unconscious), symptomatic therapy, monitoring vital functions, / with the introduction of liquids (for enhanced diureza), as appropriate IVL. In the case should not be used barbiturates. As a specific antidote used BZ antagonist flumazenil receptors (in the hospital). Haemodialysis weak.

Precautions

Not recommended for Aciclovir benzodiazepines, the combination of anxiety depression (possible traumas). In connection with the possibility of paradoxical reactions, including aggressive behaviour with caution appoint patients with personal and behavioural disorders. The paradox reaction can be observed in children and the sick senile age. In the event of a paradoxical reaction diazepam should Otmeniti.v treatment period diazepam not use alcoholic Napitkov.ne should be applied in conjunction with the drivers of vehicles and people, which requires a quick mental and physical reactions, and was linked to elevated concentrations Vnimania.primenenie diazepam in children under the age of 14 allowed only in clearly defined circumstances, the duration of treatment should be Minimalna.pri admission diazepam (even in therapeutic doses), there is a growing addiction, the physical and psychological dependence. The risk of dependence increases in the use of high doses and with the increase in the length of admission, as well as in patients with drug and alcohol problems in the disorder. Lifting diazepam should be undertaken gradually by reducing dose to reduce the risk of the syndrome and rebound-sindroma. In an abrupt cancellation after a long reception or receive high doses of the syndrome of the (headache, muscle pain, anxiety, anxiety sputannosti consciousness, tremor, convulsions), in the most severe cases, depersonalization, hallucinations, epileptic seizures (sudden elimination with epilepsy). Tranzitornyi syndrome, in which the symptoms provoked the appointment of diazepam, renewed in a more pronounced form (rebound-sindrom), could also be accompanied by changes in mood, concern and Dr.pri long-term use should be periodically monitored picture peripheral blood and the Pecheni.primenenie in doses above 30 mg (especially / m or / c), within 15 hours before giving birth can be the cause of the newborn patients, hypotension, hypothermia, the rejection of the breast and Dr.opisana of benzodiazepine addiction.

Dosing and Administration

Inside, in / in, in / m rektalno. The dispensing establish a case-by-case basis, depending on the evidence, of course, endurance, etc. Treatment to start with the lowest effective dose for a particular form Patologii.obychne dose for adults with the ingestion : primary-5-10 mg daily, 5-20 mg, the maximum lump-20 mg, maximum daily Mg.pri 60 in / in and / m average a single dose for adults-10 mg, the average daily-30 mg, the maximum one-time 30-mg maximum daily 70 mg. The duration of treatment with a Injecting should not take more than 3-5 days (after which, if necessary, are in the process of ingesting), the total duration of treatment should be as short as possible and should not exceed 2-3 months (including gradually reducing dosage). The duration of treatment over two to three months is possible only after a thorough re-evaluation of the patient. Before reconnecting rate break should be at least three Ned.dozu and duration of treatment for children picked individually, depending on the nature of the disease, age, body mass index Rebenka.patientam elderly and senile patients, as well as patients with impaired liver treatment to start with lower doses.

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