2010/06/13

Flurazepam

Trade name:
Dalmadorm

The international name:
Flurazepam (Flurazepam)

Group Affiliation:
Soporific

Description of the active substance (INN):
Flurazepam

Mode of action:
Hypnotic benzodiazepine. Also has anxiolytic, anticonvulsant and central miorelaksiruyuschee action. Assign usually as a sedative-hypnotics drugs. Strengthens the inhibitory effect of GABA (neurotransmitter pre-and postsynaptic inhibition in all parts of the CNS) to the transmission of nerve impulses. Stimulates benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors of the ascending activating brain stem reticular formation and lateral horn neurons of the spinal cord, reduces the excitability of the subcortical brain structures (limbic system, thalamus, hypothalamus), inhibits the polysynaptic spinal reflexes. Anxiolytic effects due to the influence on the amygdaloid complex of the limbic system and appears to reduce the emotional stress, reducing anxiety, fear, anxiety. Sedation due to the influence on the reticular formation of the brain stem and nonspecific thalamic nucleus and manifests a decrease in symptoms of neurotic origin (anxiety, fear). The main mechanism of action is soporific in the inhibition of cells of the reticular formation of the brain. Reduces the impact of emotional, autonomic and motor stimuli that violate the mechanism of sleep. Reduces the duration of the period of sleep, reduces the number of awakenings, increase sleep. Therapeutically significant effect occurs at 2-3 overnight after starting treatment. Anticonvulsant action is realized by increasing presynaptic inhibition. Reduces spread of epileptogenic activity, but not removed the excited state of the hearth. Miorelaksiruyuschee central action is caused by inhibition of spinal polysynaptic afferent inhibitory ways (to a lesser extent and monosynaptic). It is possible, and direct inhibition of motor nerve and muscle function. The productive psychotic symptoms genesis (acute delusional, hallucinatory, affective disorders) has practically no effect, is rarely observed decrease in affective intensity, delusional disorders.

Indications:
Sleep disorders: a violation of falling asleep, nocturnal awakening, early awakening.

Contraindications:
Hypersensitivity, coma, shock, acute alcohol intoxication with a weakening of the vital functions, acute intoxication of drugs, have a depressing effect on the central nervous system (including narcotic analgesics and hypnotics drugs), myasthenia gravis, angle-closure glaucoma (acute onset or predisposition), severe COPD (degree of progression of respiratory failure), acute respiratory failure, paradoxical reactions to ethanol and / or sedative drugs, severe depression (suicidal tendencies may be observed), pregnancy (especially the I trimester), lactation, age 15 (safety and efficacy have not identified ). C care. Depression, liver and / or renal failure, cerebral and spinal ataxia, hyperkinesis, drug dependency history, the propensity to abuse drugs, organic brain disease, psychosis (possible paradoxical reactions), hypoproteinemia, respiratory disorders due to depression of the respiratory center (in including sleep apnea, established or suspected), advanced age.

Adverse effects:
Of the nervous system: at the beginning of treatment (particularly in older patients) - drowsiness, fatigue, dizziness, reduced ability to concentrate, ataxia, unsteady gait and poor coordination of movements, apathy, blunting of emotions, mental retardation and motor responses, seldom - headache, euphoria, depression, tremor, depressed mood, catalepsy, anterograde amnesia, confusion, dysautonomic extrapyramidal reactions (uncontrolled movements of body, including eyes), asthenia, myasthenia gravis during the day, dysarthria, very rarely - paradoxical reactions (aggressive outbursts, fear, suicidal tendencies, muscle cramps, confusion, hallucinations, severe agitation, irritability, anxiety, insomnia). From the side of the SSA: false angina, heart rate, blood pressure reduction. From the side of hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, pyrexia, pain in the throat, excessive fatigue or weakness), anemia, and thrombocytopenia. On the part of the digestive system: dry mouth or salivation, heartburn, abdominal pain, nausea, vomiting, diarrhea or constipation, decreased appetite, liver problems, increased activity of "liver" transaminases and alkaline phosphatase, jaundice. On the part of the genitourinary system: urinary incontinence, urinary retention, renal failure, increased or decreased libido, dysmenorrhea. Allergic reactions: skin rash, itching. Impact on fruit: teratogenicity (especially the I term), CNS depression, respiratory failure and suppression of the sucking reflex in infants whose mothers used the drug. Other: addiction, drug dependency, rarely - inhibition of the respiratory center, blurred vision (diplopia), bulimia, weight loss, tachycardia. With a sharp decrease in dose or cessation of reception - syndrome "cancel" (irritability, headache, anxiety, agitation, excitement, fear, nervousness, sleep disturbances, dysphoria, a spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremors, disorders of perception, including giperakuziya, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rare - acute psychosis). overdosage. Symptoms: drowsiness, confusion, paradoxical excitement, reduced reflexes, stupor, decreased response to pain stimuli, deep sleep, dysarthria, ataxia, visual disturbances (nystagmus), tremor, bradycardia, dyspnea or shortness of breath, marked weakness, reduced blood pressure, collapse , inhibition of cardiac and respiratory activity, coma. Treatment: gastric lavage, forced diuresis, receiving activated charcoal. Symptomatic therapy (maintenance of respiration and blood pressure, excited by the introduction of barbiturates is not recommended). As a specific antagonist flumazenil use (in a hospital). Hemodialysis is ineffective.

Dosage and administration:
Inside, the smallest effective dose, before bedtime. Adult: 15-30 mg, debilitated patients and in old age - 15 mg, if necessary, taking into account the tolerance dose increases. Treatment duration - 7-10 days.

Cautions:
In the treatment of patients is strictly prohibited the use of ethanol. In renal and / or hepatic insufficiency and prolonged treatment is necessary to monitor the pattern of peripheral blood and liver "enzymes. On the second or third night of consecutive use increased efficiency flurazepama, after stopping for 1 - 2 days, may continue its operation. In the absence of therapeutic effect after 7-10 days of treatment necessary to verify the diagnosis. The risk of drug dependence increases when using large doses, a considerable length of treatment, patients who previously abused drugs or ethanol. Without specific instructions, should not be used for a long time. Do not abrupt discontinuation of treatment because of the risk of the syndrome of "lifting" (headache, myalgia, anxiety, tension, confusion, irritability, and in severe cases - derealization, depersonalization, giperakuziya, photophobia, paresthesia in extremities, hallucinations and seizures). Remove the drug should be gradual. If you have any patients with such unusual reactions, as increased aggressiveness, acute state of excitement, anxiety, suicidal thoughts, hallucinations, increased muscle cramps, difficult to fall asleep, shallow sleep, treatment should be discontinued. During pregnancy, use only in exceptional cases and only emergencies. Toxic effect on the fetus and increase the risk of birth defects when used in the I trimester of pregnancy. Therapeutic dose in the later stages of pregnancy can cause depression of the central nervous system of the newborn. The constant use during pregnancy can cause physical dependence with the development of the syndrome of "cancellation" of the newborn. Children, especially at a younger age, are very sensitive to the depressant drug action of benzodiazepines. Using just before birth or during labor may cause newborn respiratory depression, reduced muscle tone, hypotension, hypothermia and a weak act of sucking (syndrome flaccid child. ") During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and quickness of psychomotor reactions.

Interaction:
Antihistamines, psychoactive drugs, ethanol and etanolsoderzhaschie drugs increase the depressant effect on CNS. Microsomal oxidation inhibitors increase the sedative effect, extend T1 / 2, increase the risk of toxic effects. Inductors of microsomal liver enzymes less efficient. Opioid analgesics enhance the euphoria, leading to the rise of psychological dependence . Antihypertensive drugs - the risk of significant decrease of BP. Against the background of the simultaneous appointment of clozapine may be increased respiratory depression. reduces the effectiveness of levodopa in patients with Parkinson's disease. may increase the toxicity of zidovudine.