Dipotassium clorazepate

Chemical name

Complex 7-Хлор-2,3-дигидро-2-оксо -5-фенил-1Н-1,4-бензодиаз епин-3-карбоновой acid with potassium hydroxide (1:1)

Gross

C16-H11-Cl-K2-N2-O4

Characteristics

Anksiolitik from the benzodiazepines. Powder white or light colors, virtually odourless. Very good soluble in water, very poorly soluble in ethanol, practically nerastvorim in the organic solvent. Hydrogen-transparent, light-yellow with alkaline reaction unstable.

Of drugs

Drugs, the anxiolytic, protivosudorozhnoe. Associated with specific receptors benzodiazepinovmi (bark brain mindalevidne kernel gippocamp, podbugorie, Wikipedia, polostoe body and the spinal cord), and increases the sensitivity to Gamk-retseptorov mediatoru, increasing the braking effect of GABA Zns.posle intake of becoming nordiazepam (desmetildiazepam), and in this form quickly and adequately absorbed in the digestive tract and circulates in the blood system. C_max nordiazepama plasma achieved through 120 min. Equilibrium concentration in the blood normally achieved in 5 days to 2 weeks. Nordiazepam characterized by a high level of bonding with plasma proteins (97-98%), T_1/2 of plasma is 40-50 hrs, enters the breast milk. Nordiazepam further metabolized in the liver by gidrauxilirovania. Mainly excreted with the urine, mostly in the form of conjugated oxazepamum (3-гидроксинордиазепа��а) and small quantities of conjugated p -гидроксинордиазепам��. The reappointment of the accumulation of active metabolites значительное.Относит��я to the long-term benzodiazepine actions. It has long depressing influence on the central nervous system. Has strong anxiolytic effect. Miorelaksiruty and sedative effects are poorly. Reduces levels of anxiety, agitation. Ease the symptoms of acute alcohol абстиненции.Эксперим��нтальные studies in animals (rats, monkeys) showed a significant difference in rates of anxioliticeski, sedative and toxic effects. Thus, in rats lifting a reflex warned when administered 10 mg / kg, the sedative effect dispensed with the dose of 32 mg / kg, ELD_50 - 1320 mg / kg The monkeys aggressive behaviour back at doses 0.25 mg / kg, the sedative effect (ataxy) dispensed with the 7.5 mg / kg ELD_50 than 1,600 mg / kg, but is not defined as in high doses is emeticeski Effect.v toxicity studies in dogs (21 animals), receiving dikalia klorazepat inwards in doses up to 75 mg / kg for 22 months were associated with hosting drugs changes in the liver (decrease in the mass holetaz with minimal damage gepatotellularian). In toxicity studies in monkeys (18 animals), receiving dikalia klorazepat inwards in doses 36 mg / kg / day for 52 weeks, the female monkeys with a high dose was considered related to drugs admission trend for a decrease in the number of cells, with the total number of cells remained within the normal level. Not function or structure of the liver (as well as others), identified Balo.issledovania fertility, reproduction, teratogenicity in rodents (rats, rabbits) showed that the admission dikalia klorazepata inwards in doses up to 150 mg / kg (rats) and up to 15 mg / kg (rabbits) is the development of the fetus, no effect on fertility and reproductive capacity in adults Zivotnykh.v experiments on animals (dogs and rabbits), a dependence manifested in the development of convulsing Quick lifting or lowering doses PP; this syndrome in dogs kupirovalsa introduction dikalia klorazepata.

Indications

All disturbing disorders (treatment alarming conditions, or for the short-term withdrawal symptoms of anxiety), the withdrawal syndrome in patients with alcoholism (symptomatic treatment), stiffness epileptic seizures, texture (children).

Restrictions on the use of

Depressive state, psychotic reactions, infants, children up to 9 years (safety and efficacy of the application of non-identified).

Pregnancy and lactation

Contraindicated in pregnancy (especially in the first trimester). At the time of treatment must stop breastfeeding.

Contraindications

Hypersensitivity, respiratory distress, zakratougolnaya glaucoma, pregnancy (especially I trimester), breast-feeding.

Side-Effects

From the nervous system and sensory organs : drowsiness, dizziness, irritability, lack of, headache, sputannosti consciousness, insomnia, fatigue, ataxy, diplopia, depression, tremor, smazannaya Reci.so part of the intestine : gastrointestinale complaints, including nausea, vomiting, dry mouth, changes in the functional kidney and liver Testov.prochie : passing skin rashes, urogenital disorders, demotion Sad, reducing Gematokrita.pri long-term use or receive large doses physical and psychological dependence, the syndrome (convulsions, deliri, tremor, abdominal and muscle cramps, vomiting, increased sweating, nervousness, insomnia, irritability, diarrhoea, worsening memory).

Specific guidance

Anxiety or tension associated with the day-to-day stress, usually do not require treatment anxiolitikami.

Patient interaction

Effects increase (each) alcohol, neiroleptiki, barbiturates and other drugs, depressing central nervous system and peripheral and central muscle.

Overdosing

Symptoms : oppression CNS varying degrees of symptoms (from itching to coma), the oppression of the respiratory and cardiac Deatelnosti.lechenie : washing stomach, vomiting induction, monitoring vital functions of the respiratory and cardiovascular analeptikov. As an antidote can be used specific antagonist benzodiazapine receptors flumazenil (in the hospital).

Precautions

Be wary of liver and kidney diseases, children, the elderly and immunocompromised patients. In patients with drug and alcohol problems apply under the close supervision Vracha.dl prevent the syndrome dose to be reduced gradually. Not recommended admission of oppressive central nervous system. It should not be combined with the admission of alcohol. The treatment is not recommended vehicle fleet management and the work that requires increased attention and quick reactions. In the long admission shows periodic monitoring picture blood and the liver.

Dosing and Administration

Inside. The dosage and duration of treatment determine on a case-by-case (under medical supervision), depending on the evidence, clinical picture, endurance, etc. The average dose for adults-30 mg / day (60 mg / day) with a maximum dose of 90 mg / sut. Initial dose for the elderly and handicapped patients 3.75 mg per Noci.dozu for children and the duration of treatment picked individually, depending on the age and the nature of the disease.

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