Chlordiazepoxide

Chemical name

7-Хлор-N-метил-5-фенил-3H- 1,4-бензодиазепин-2-ами��о-4-оксид (and as hydrochloride)

Gross

C16-H14-Cl-N3-O

Characteristics

Anksiolitik, product or Benzodiazepina.bely melkochristalliceski brown powder. Virtually nerastvorim water, it is difficult soluble in alcohol; As hydrochloride-soluble in water.

Of drugs

Drugs, the anxiolytic, sedative, sleeping, miorelaksirutee (central). Interacts with specific receptors benzodiazepinovmi located in postsinapticescom Gamk_a-retseptornom compound in the cortex, mindalevidne kernel gippocampe, podbugorie, cerebellum, polostom body and the spinal cord. Increases sensitivity neironalnah Gamk-retseptorov to GABA increases Gamcneirotransmissiu, blocking polisinapticalkie Reflexa.posle intake of a well-absorbed from the gastrointestinal (food slows absorption); C_max when administered a single dose is a 0.5 hour equilibrium concentration in the blood is achieved through 12 days after the start of the reception. Linking plasma protein is 96%. T_1/2 hlordiazepoksida plasma from the 7-28 hour C_max the metabolita (дезметилхлордиазепо��сида) - 8-24 am The liver is intense metabolizmu (N-demetilirovanie, dezaminirovanie, gidrauxilirovnie) with the formation of active derivatives (desmetilhlordiazepoksid, demoxepam, desmetildiazepam, oxazepam). Passes through GEB, placenta, enters the breast milk; Slowly absorbed from the muscle tissue. After the end of the treatment metabolites detected in the plasma in a few days or even weeks. T_1/2 - 5-30 hrs (hlordiazepoksid), 18 hrs (desmetilhlordiazepoksid), 95 hrs (demoksepam), 30-100 hrs (desmetildiazepam), 5-15 hrs (oxazepam). Report mostly kidneys (1-2% in unmodified form). Accumulation hlordiazepoksida and its active metabolites at the time of Znachitelnoe.u elderly intake and metabolism hlordiazepoksida slower, metabolic transformation has slowed to defeat Pecheni.okazavaet expressed a calming effect on the central nervous system. Suppress alarm initiation, the emotional strain. Ters obsessive thoughts and fears, increases susceptibility to gipnosuggestevna therapy. Provides antipanicescoe act eliminates tremor, the weak protivosudorojnam effect. Decreases pronounced anxiety and fear associated with the upcoming operational Vmechatelstwom.v high doses may reduce agitation. Is moderate hypnotic effects, which are usually expressed in the first three days of therapy, in the future a positive effect on sleep is the removal of psychogenic nuisances. It is a moderate muscle Relaksaciu.oblegchaet symptoms of acute alcohol withdrawal, such as initiation, nervous tension, anxiety anxiety, tremor, etc. increases appetite has weak analgesic действие.Исследовани�� reproduction in animals showed that the introduction of hlordiazepoksida rats in doses of 10, 20 and 80 mg / kg / day is not a cause of birth defects and the growth of infants, as well as violations of weight with the females. Another study with a dose of 100 mg / kg / day showed a significant reduction in the rate of fertilization, a marked decline in the survival rate and body weight in newborns krasat.

Indications

Outwardly state accompanied by anxiety, either, hadst high, emotional stress, insomnia; Neurotical ataxy, headache voltage cardialgia, ezofagospazm, kauzalgia face gemispazm, hysterical state (hysterical fit, ambliopia, mutism, paralysis), psihogenny stalemate, ikota. Neurozo- and psihopatopodobne disorders in patients with atherosclerosis cerebrovascular, organic brain impairment; Deliri infection, withdrawal syndrome in patients with alcohol and drug abuse; increased tone skeletal muscles giperkinez and rheumatoid neuroticeski; climax, pre syndrome, wegeto-sosudistaya distonia. premedikation (preparing patients for operations and lengthy diagnostic procedures), posleoperazionny period; Integrated therapy for schizophrenia with neurozopodobna symptoms, as well as a host of diseases involving everything, hadst, insomnia, including ackzeme.

Restrictions on the use of

Glaucoma, the liver and / or kidney syndrome patients in a dream, severe cardiac and respiratory distress, ataxy (except neuroticescoy), psychoses (perhaps paradoxically increased exposure), drug or alcohol dependence (except for the treatment of acute withdrawal syndrome), pregnancy (II and III Plus), old age.

Pregnancy and lactation

Contraindicated in the first trimester of pregnancy (increases the risk of birth defects in the appointment during this period). 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, severe gravis, respiratory depression, zakratougolnaya glaucoma, acute liver disease and / or kidney pregnancy (I term), breast-feeding, age up to 4 years.

Side-Effects

From the nervous system and sensory organs : drowsiness, weakness, impaired memory and concentration, slow mental and motor reactions, muscle weakness, the walking, ataxy, sputannosti consciousness, disorientation, dizziness, headache, changes Eeg.so the circulatory system and blood (blood, gemostaz) : tachycardia, a sense of heart, arterial gipotenzia (to high doses), thrombocytopenia, Agranulozitoz.so part of the intestine : dry mouth, nausea, constipation or diarrhoea, intestinal kolica violation of the liver, skin jeltushnosti �окровов.Аллергически е reactions : skin rash, itching, peeling Koji.prochie : difficulty in breathing, the delay urination, the menstrual cycle, changing face (increases or decreases). There addiction, drug dependency, the syndrome and others (see "Precautions").

Specific guidance

The alarming condition and the stress of daily life stress, usually do not require treatment anxiolitikami.

Patient interaction

Do the alcohol and means oppressive central nervous system (narcotic analgesics, anaesthetic, hypnotics, neiroleptiki with the expressed sedative effect), miorelaksantov etc. Antacids means stripping down (but not reduce the intake) hlordiazepoksida. Chlordiazepoxide may weaken the effect of levodopa. Zimetidin, estrogensoderjaschie oral contraceptives, disulfiram and erythromycin down hlordiazepoksida metabolism in the liver, increasing its concentration in the blood and delay the withdrawal. Smoking can weaken hlordiazepoksida.

Overdosing

Symptoms : oppression CNS varying degrees of symptoms (from itching to coma), expressed drowsiness, lethargy, weakness, reduced muscle strength, long sputannosti consciousness, disorientation, indiscriminate speech oppression reflexes, coma; It is also possible to respiratory depression, Gipotenzia.lechenie : induction vomiting, immediately wash stomach, monitoring vital functions, symptomatic therapy, in / in cefuroxim solutions (to enhance diureza) ensuring adequate ventilation light; in the case of hypotension, a norepinephrine. In the case should not be used barbiturates. As a specific antidote used BZ antagonist flumazenil receptors (in the hospital). Haemodialysis weak.

Precautions

It should be borne in mind that, when combined with anxiety depression possible suicidal Popatki.s caution applied simultaneously with other psychotropic substances. There should be appointed at the same time as MAO inhibitors and Fenotiazinami.pri long-term use (over several months), especially at high doses, may be addictive, drug dependency. Hlordiazepoksida lifting should be undertaken gradually by reducing dose to reduce the risk of the syndrome, which is characterized by tremorom, convulsions, or abdominalnami muscle spasm, vomiting, isparina. In an abrupt cancellation, it is also possible to agitation, fear, lunch Violations Bessonnica.ne should hlordiazepoksid more than four weeks without a re-evaluation of the patient to take a decision on the need to continue Terapii.veroatnosti of side effects than older Ludei.pri long-term use should be periodically monitored picture peripheral blood and the Pecheni.imeutza reported to be that, in treating hlordiazepoksidom mentally ill patients and children with aggressive behaviour characteristics were paradoxical reaction (agitation deep anger, etc.). In the case of paradoxical reactions treatment should immediately Prekratiti.sleduet bear in mind that hlordiazepoksid may reduce the liveliness of mind Detei.neobhodimo bear in mind that there are reports on the effects on blood coagulation in patients receiving both oral anticoagulants and hlordiazepoksid (in the clinical studies cause and the effect of the interaction are not installed). There were isolated reports of worsening porfirii due to hlordiazepoksida. Gipoproteinemia may predispose to increased frequency sedative side Effectov.vo treatment and within three days after the lifting should be deleted reception alcohol; Drivers of vehicles and people whose work requires quick mental and physical reactions, as well as linked to the high concentration of attention, during this period should not engage in professional activities.

Dosing and Administration

Inside. Doses (time and daily), and duration of treatment picked a case-by-case basis, depending on the nature and course of the disease, endurance, etc. Treatment to start with the lowest effective dose for a particular form Patologii.obychnaya single dose for adults, 5-10 mg, the normal daily-60 mg (reception 2-4). When the voltage in conjunction with the violation of sleep 10 to 20 mg once a day for 1-2 hours before sleep. In psychiatry is 50-100 mg / day in Puerto withdrawal syndrome, and 300 mg / day in the 3-4 Priema.patientam elderly and senile patients weakened by AIDS, patients with diseases of the liver and / or kidney to appoint smaller doses (single-2.5-5 mg). The treatment should not exceed 2.5 months. Again course (if necessary), not less than 3 Ned.detam from the age of 4 years dose (and the duration of treatment) picked individually, depending on the age, body mass index, etc.

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