The drug belongs to the list of potent agents according to the protocol of the meeting PKKN.
Hypnotic of benzodiazepine has a depressant effect on the nervous system (CNS), realized winstrol reviews mainly in the thalamus, hypothalamus and limbiche-tion system. It enhances the inhibitory action of gamma-aminobutyric acid (GABA), which is one of the major mediators of the pre- and post-synaptic inhibition of impulse transmission in the central nervous system.
The drug also has anxiolytic, sedative, muscle relaxant, and protivosudo-goad action. Hypnotic effect occurs within 20-40 minutes after ingestion and lasts 6-8 hours. Under the influence of the drug increases the depth and duration of sleep. Sleep and waking occur physiologically.
The drug was well pass through the blood-brain barrier, the placenta, enters the breast milk, which should be considered when administering the drug to pregnant and lactating women.
Absorption from the gastrointestinal tract – rapid and complete. Bioavailability – from 54% to 98% (depending on the dosage form). When taken together with food intake and slows down the maximum plasma concentration is reduced by about 30%. In a single oral dose of 10 mg nitrazepama average value of the maximum concentration of 0. 08-0.1 g / ml and is achieved within 1-4 hours. Relationship to plasma proteins – about 85-90%. The phase distribution of the active substance in the body varies greatly, ranging from 3.5 to 1. 7 h. The volume of distribution increases with age of patients 1 and 3-2. 6 L / kg. It penetrates through the blood-tissue barriers, including GEB and placental barrier, it is found in mother’s milk.
It is metabolized in the liver by reducing the nitro group and subsequent acetylated-tion with the formation of active acetyl derivatives. The half – 16-48 hours (depending on age and body weight of patients) of cerebrospinal fluid – 68 h main metabolites -. 7-amino-nitrazepam, 7-acetamino-nitrazepam, 2-amino-5-nitrobenzophenone and hydroxy-2- amino-5-nitrobenzophenone, the kidneys (65-71%) and feces (14-20%). Approximately 1-5% is excreted unchanged by the kidneys.
The accumulation during the second appointment – min (refers to benzodiazepines with short or medium half-life), excretion after cessation of treatment – fast.
- sleep disorders winstrol reviews of various origins (difficulty falling asleep, frequent night and / or early morning awakening);
- some forms of seizures (especially in children), in Vol. h. West syndrome.Contraindications
- Hypersensitivity to benzodiazepines;
- coma, shock;
- angle-closure glaucoma (acute onset or predisposition);
- acute alcohol intoxication with the weakening of vital functions;
- acute intoxication of drugs, have a depressing effect on the central nervous system;
- severe depression (suicidal tendencies may occur);
- myasthenia gravis;
- drug or alcohol addiction;
- pregnancy, breast-feeding;
- acute respiratory failure;
- swallowing disorder in children;
- temporal lobe epilepsy;
- severe chronic obstructive pulmonary disease (risk of progression of the degree of respiratory failure)Carefully
- liver and / or kidney failure, respiratory failure, cerebral and spinal ataxia, hyperkinesis, drug dependency history, the propensity to abuse drugs, organic diseases of the brain, psychosis (possible paradoxical reactions), hypoproteinemia, sleep apnea (or suspected) , elderly age.Dosing and Administration
Inside. As a sedative 30 minutes before sleep:
– adult 2.5-5 mg nitrazepama, the maximum daily dose – 10 mg
– elderly patients and debilitated patients – 2.5 mg, the maximum daily dose – 5 mg.
For treatment West syndrome daily dose for children 1-2 years of age and infants – 2. 5-5 mg. Taken once daily dose, for administration to infants, a suitable amount of the drug is crushed and dissolved (suspended) in a convenient volume for receiving water.Side effect
On the part of the nervous system: at the beginning of treatment (particularly in elderly patients) – drowsiness, fatigue, dizziness, decreased concentration, ataxia, lethargy, blunting of emotions, mental retardation and motor responses; rarely – headache, euphoria, depression, tremors, catalepsy, anterograde amnesia, confusion, dystonic extrapyramidal reactions (uncontrolled movements of the body, including the eyes), muscle weakness, dysarthria, blurred speech; rarely -paradoksalnye reaction (aggressive outbursts, fear, suicidal tendencies, muscle spasms, hallucinations, agitation, irritability, anxiety, insomnia).
From the side of hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, pyrexia, sore throat, unusual tiredness or weakness), anemia, thrombocytopenia. From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, decreased or increased appetite, constipation or diarrhea; abnormal liver function, increased activity of “liver” transaminases and alkaline phosphatase, jaundice. From the urogenital system: urinary incontinence, urinary retention, renal dysfunction, increased or decreased libido, dysmenorrhea. Allergic reactions: skin rash, pruritus. Effect on the fetus: central nervous system depression, respiratory failure and suppression of sucking reflex in infants whose mothers used the drug during pregnancy.
Other: addiction, drug dependency; lowering blood pressure; rarely – depression of the respiratory center, blurred vision (diplopia), bulimia, weight loss, tachycardia. With winstrol reviews a sharp decrease in dose or cessation of reception – syndrome “cancel” (irritability, headache, anxiety, agitation, anxiety, sleep disturbances, dysphoria, a spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting , tremors, disorders of perception, incl hyperacusis, hyperesthesia, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rare -… acute psychosis).
Symptoms: drowsiness, depression of consciousness of varying severity (up to coma), paradoxical excitement, reduced reflexes, decreased response to pain stimuli, deep sleep, dysarthria, ataxia, blurred vision (nystagmus), tremor, bradycardia, dyspnea or shortness of breath, severe weakness, decreased blood pressure, collapse, depression of cardiac and respiratory activity. Treatment: gastric lavage, forced diuresis, administration of activated charcoal. Symptomatic therapy (maintenance of respiration and blood pressure). As a specific antagonist flumazenil is used (in a hospital). Hemodialysis – is ineffective.