November 25, 2010 – 7:00 pm
Prescription name: Diapam
International name: Diazepam (Diazepam)
Group affiliation: anxiolytic tool
Description active substance (INN): Diazepam
Dosage form: tablet, solution for intravenous and intramuscular injection, injection, tablets, coated tablets, coated tablets [for children]
Pharmacological action: anxiolytic drug (anxiolytic) benzodiazepine. has a sedative-hypnotic, anticonvulsant and central miorelaksiruyuschee action. the mechanism of action of diazepam is due to stimulation of benzodiazepine receptor supramolecular GABA-benzodiazepine-hlorionofor receptor complex, leading to increased inhibitory action 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 of sleeping pills is the oppression of the cells of the reticular formation of the brain. Anticonvulsant action is realized by increasing presynaptic inhibition. Reduces spread of epileptogenic activity, but not removed the excited state of the hearth. Central miorelaksiruyuschee 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. With moderate sympatholytic activity, may decrease blood pressure and increased coronary blood vessels. Increases the threshold of pain sensitivity. Suppresses sympathadrenalic and parasympathetic (including vestibular) paroxysms. Reduces nocturnal secretion of gastric juice. the action of the drug is observed in 2-7 day of treatment. On the productive psychotic symptoms genesis (acute delusional, hallucinatory, affective disorders) has practically no effect, is rarely observed decrease in affective intensity, delusional disorders. When abstinent syndrome in chronic alcoholism causes a weakening of agitation, tremor, negativism, as well as alcoholic delirium and hallucinations. the therapeutic effect in patients with false angina, arrhythmias, and paresthesia observed by the end of 1 week.
Indications: Anxiety disorders. Dysphoria (consisting of combination therapy as an additional LAN). Insomnia (difficulty falling asleep). Spasm of skeletal muscle under local injury, spastic conditions associated with damage to the brain or spinal cord (cerebral palsy, athetosis, tetanus), myositis, bursitis, arthritis, rheumatoid pelvispondiloartrit, progressive chronic polyarthritis, arthrosis, accompanied by a voltage of skeletal muscles, vertebral syndrome, angina , tension headache. Abstinent alcohol syndrome: anxiety, tension, agitation, tremor, transient reactive states. In the combined therapy: hypertension, peptic ulcer and 12 duodenal ulcer; psychosomatic disorders in obstetrics and gynecology: menopausal and menstrual disorders, preeclampsia, status epilepticus, eczema and other diseases accompanied by itching, irritability. Meniere’s disease. Poisoning drugs. Premedication before surgical interventions, and endoscopic manipulation, general anesthesia. For parenteral administration: premedication before general anesthesia, as a component of combined general anesthesia, myocardial infarction (in the complex therapy); motor stimulation of different etiologies in neurology and psychiatry paranoid-hallucinatory state, epileptic seizures (docking); relief in labor, premature genera (only at the end of III trimester of pregnancy); premature exfoliation of the placenta.
Contraindications: Hypersensitivity, coma, shock, acute alcohol intoxication with the weakening of 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 (risk of progression of the degree of respiratory failure), acute respiratory failure, absans syndrome or Lennox-Gastaut (with a / in the introduction contributes to the tonic status epilepticus), pregnancy (especially the I trimester), lactation, children younger than 6 months (ingestion), and 30 days inclusive (with the / m and / in the introduction). C carefully. Epilepsy or seizures in history (start of treatment with diazepam or abrupt withdrawal may accelerate the development of seizures or status epilepticus), liver and / or renal failure, cerebral and spinal ataxia, hyperkinesis, drug dependency history, the propensity to abuse drugs, organic diseases brain, hypoproteinemia, sleep apnea (or suspected), advanced age.
Side effects: of the nervous system: at the beginning of treatment (particularly in elderly patients) – drowsiness dizziness, fatigue, reduced ability to concentrate, ataxia, disorientation, unsteady gait and poor coordination of movements, apathy, blunting of emotions, mental retardation and motor reactions, anterograde amnesia (in more often than when taking other benzodiazepines), rarely – headache, euphoria, depression, tremor, depressed mood, catalepsy, confusion, dysautonomic extrapyramidal reactions (uncontrolled movements of body, including eyes), weakness, myasthenia gravis during the day, hyporeflexia, dysarthria, very rarely – paradoxical reactions (aggressive outbursts, psychomotor anxiety, fear, suicidal tendencies, muscle spasms, confusion, hallucinations, severe agitation, irritability, anxiety, insomnia). From the side of hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, pyrexia, sore throat, extreme tiredness or weakness), anemia, and thrombocytopenia. On the part of the digestive system: dry mouth or hyperptyalism, heartburn, hiccups, stomachalgia, nausea, vomiting, decreased appetite, constipation, liver problems, increased activity of “liver” transaminases and alkaline phosphatase, jaundice. From the CCC: palpitations, tachycardia, blood pressure reduction (with parenteral administration). On the part of the genitourinary system: urinary incontinence, urinary retention, renal failure, increased or decreased libido, dysmenorrhea. Allergic reactions: skin rash, itching. Effect on the fetus: teratogenicity (especially the I trimester), CNS depression, respiratory failure and the suppression of sucking reflex in infants whose mothers used the drug. Local reactions: at the injection site – phlebitis or venous thrombosis (redness, swelling or pain at the injection site). other: addiction, drug dependency, rarely – inhibition of the respiratory center, respiratory dysfunction, impaired vision (diplopia), bulimia, body weight loss. 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). When used in obstetrics – in term and preterm children – muscular hypotension, hypothermia, dyspnoea. Overdose. Symptoms: drowsiness, confusion, paradoxical excitement, reduced reflexes, arefleksiya, stupor, decreased response to pain stimuli, deep sleep, dysarthria, ataxia, visual disturbances (nystagmus), tremor, bradycardia, dyspnea or labored breathing, apnea, marked weakness, lowering blood pressure, collapse, depression of cardiac and respiratory activity, coma. Treatment: gastric lavage, forced diuresis, receiving activated charcoal. Symptomatic therapy (maintenance of respiration and blood pressure), mechanical ventilation. as a specific antagonist flumazenil use (in a hospital). Hemodialysis is ineffective. the antagonist of benzodiazepines flyumazenil not shown in patients with epilepsy who were treated with benzodiazepines. In such patients antagonistic action with respect to benzodiazepines can provoke the development of epileptic seizures.
Dosage and administration: inside, in / m / v, rectally. the dose is calculated individually depending on the patient, the clinical picture of disease, sensitivity to the drug. as an anxiolytic drugs appointed interior, 2. 5-10 mg 2-4 times a day. Psychiatry: in neurosis, hysterical or hypochondriacal reactions, states of dysphoria different genesis, phobias – of 5-10 mg 2-3 times a day. if necessary, the dose may be increased to 60 mg / day. When alcohol withdrawal syndrome – 10 mg 3-4 times a day during the first 24 h, with a subsequent decrease to 5 mg 3-4 times a day. Elderly, debilitated patients and patients with atherosclerosis in the beginning of treatment – by mouth, 2 mg 2 times a day, if necessary, be increased to optimum effect. A working patient is recommended to take 2. 5 mg 1-2 times daily or 5 mg (base dose) in the evening. Neurology: spastic states of central origin in degenerative neurological diseases – mouth, 5-10 mg 2-3 times a day. Cardiology and Rheumatology: Angina – at 2-5 mg 2-3 times a day, hypertension – at 2-5 mg 2-3 times a day, vertebral syndrome with bedrest – 10 mg 4 times a day, and as additional drugs in Physical Therapy in Rheumatoid pelvispondiloartrite, progressive chronic polyarthritis, arthrosis – 5 mg 1-4 times a day. In the combined therapy of myocardial infarction: initial dose – 10 mg / m, then the inside of 5-10 mg 1-3 times a day, and premedication in the case of defibrillation – 10-30 mg / in slowly (single dose), spastic state rheumatic origin, vertebral syndrome – an initial dose of 10 mg / m, then inside, 5 mg 1-4 times a day. Obstetrics and Gynecology: psychosomatic disorders, menopausal and menstrual disorders, preeclampsia – at 2-5 mg 2-3 times a day. Pre-eclampsia – initial dose – 10-20 mg / in, followed by 5-10 mg by mouth 3 times daily; eclampsia – during a crisis – in / at 10-20 mg, followed if necessary in / jet or drip, does not more than 100 mg / day. to facilitate labor when cervix dilated 2-3 toe – i / m 20 mg, with premature delivery and premature placental abruption – a / m in the initial dose of 20 mg over 1 hour introduction of the same dose is repeated; maintenance doses – of 10 mg 4 times up to 20 mg 3 times a day. In preterm placental abruption treatment is carried out without interruption – to the ripening fruit. Anesthesiology, Surgery: premedication – on the eve of the operation, in the evening – 10-20 mg orally, preparation for surgery – for 1 h prior to anesthesia / m adults – 10-20 mg, children – 2. 5-10 mg; introduction to anesthesia – in / in 0. 2-0. 5 mg / kg for short-term narcotic sleep with sophisticated diagnostic and therapeutic interventions in therapy and surgery – in / in adults – 10-30 mg, for children – 0. 1-0. 2 mg / kg. Pediatrics: psychosomatic and reactive disorders, spastic states of central origin – appoint a gradual increase in dose (starting with low doses and slowly increasing them until the optimal dose is well tolerated sick), daily intake (can be divided into 2-3 reception, with the bulk, the largest dose, taken at night): Inside, up to 6 months is not recommended, 6 months and older – 1-2. 5 mg, or 40-200 mg / kg, or 1. 6.17 mg / sq. m, 3-4 times a day. Inside, from 1 to 3 years – 1 mg, from 3 to 7 years – 2 mg, from 7 years and older – 5.3 mg. Daily dose – 2, 6 and 8-10 mg, respectively. Parenteral, status epilepticus and severe recurrent epileptic seizures: children from 30 days to 5 years – in / in (slowly) 0. 2-0. 5 mg every 2-5 minutes up to a maximum dose of 5 mg of 5 years and over – 1 mg every 2-5 minutes up to a maximum dose of 10 mg, if necessary, treatment can be repeated after 2-4 h. Muscle relaxation, tetanus: the children of 30 days to 5 years – i / m or i / v 1-2 mg of 5 years and over – 5-10 mg, if necessary, the dose may be repeated every 3-4 h. Patients in elderly care should begin with half the usual dose for adults, gradually increasing it, depending on the achieved effect and tolerability. Parenteral with anxiety is introduced into / in the initial dose of 0. 1-0. 2 mg / kg, repeated injections every 8 h until symptoms disappear, then move on to oral. When the motor excitation is introduced into the / m or / 10-20 mg 3 times a day. In traumatic spinal cord lesions, accompanied by paraplegia or hemiplegia, chorea – a / m in adults an initial dose of 10-20 mg, for children – 2-10 mg. When status epilepticus – in / at the initial dose of 10-20 mg, subsequently, if necessary – 20 mg / m or i / v drip. if you need / to drip (no more than 4 ml) diluted in 5-10% dextrose or 0. 9% solution of NaCl. to avoid loss of product in the sediment should be used not less than 250 ml infusion solution, quickly and thoroughly mix the resulting solution. For relief of muscle spasm expressed – in / at once, or twice 10 mg. Tetanus: an initial dose – 0. 1-0. 3 mg / kg at intervals of 1-4 hours or as a / v infusion 4-10 mg / kg / day. Rectal, as antiepileptic drugs (status epilepticus and severe recurrent seizures) – 0. 15-0. 5 mg / kg to maximum dose – 20 mg. Children – 0. 2-0. 5 mg / kg, elderly patients – 0. 2-0. 3 mg / kg.
Special instructions: In / diazepam in solution must be injected slowly, into a large vein at least 1 min for every 5 mg (1 ml) of the drug. not recommended for continuous i / v infusion – perhaps precipitation and adsorption of the drug polyvinylchloride materials infusion bottles and tubes. In the treatment of patients is strictly prohibited the use of ethanol. In renal / hepatic failure and prolonged treatment is necessary to monitor patterns of peripheral blood and “liver” enzymes. 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. it is unacceptable 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, tactile hypersensitivity, paresthesias in the extremities, hallucinations and epileptic seizures), but due to a slow T1 / 2 of diazepam expressed its manifestation is much weaker than that of other benzodiazepines. if you have any patients with such unusual reactions, as increased aggressiveness, acute state of excitement, anxiety, fear, suicidal thoughts, hallucinations, increased muscle cramps, difficult to fall asleep, shallow sleep, treatment should be discontinued. start of treatment with diazepam or its abrupt withdrawal in patients with epilepsy or seizures in history can accelerate the development of seizures or status epilepticus. During pregnancy, only in exceptional cases and only for “real life” testimony. 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 lead to physical dependence – can syndrome “cancellation” of the newborn. Children, especially at a younger age, are very sensitive to central depressant drug action of benzodiazepines. Babies are not encouraged to nominate drugs containing benzyl alcohol – may develop a fatal toxic syndrome, manifested metabolic acidosis, CNS depression, difficulty breathing, kidney failure, lower blood pressure, and possibly seizures and intracranial hemorrhages. Using (especially in the / m or i / v) at doses above 30 mg for 15 hours before birth or during labor may cause newborn respiratory depression (up to apnea), decreased muscle tone, lower blood pressure, hypothermia, poor suckling act ( syndrome flaccid child “) and violation of metabolism in response to cold stress. During the period of treatment must be careful when driving and other lesson potentially dangerous activities which require high concentration and speed of psychomotor reactions.
Interaction: strengthens the inhibitory effect on CNS ethanol, sedative and antipsychotic drugs (neuroleptics), antidepressants, narcotic analgesics, drugs for general anesthesia, muscle relaxants. Inhibitors of microsomal oxidation (including cimetidine, oral contraceptives, erythromycin, disulfiram, fluoxetine, isoniazid, ketoconazole, metoprolol, propranolol, propoxyphene, valproic acid) extend T1 / 2 and increase the effect. Inductors microsomal liver enzymes decrease the efficiency. Narcotic analgesics increase the euphoria, leading to the rise of psychological dependence. Antacids drugs reduce the rate of absorption of diazepam from the gastrointestinal tract, but not its fullness. Antihypertensive drugs may increase the severity of BP reduction. Against the background of the simultaneous appointment of clozapine may be increased respiratory depression. At simultaneous application with nizkopolyarnymi cardiac glycosides may increase the concentration of recent serum and the development of digitalis intoxication (as a result of competition for association with plasma proteins). Reduces the effectiveness of levodopa in patients with Parkinson’s disease. Omeprazole prolongs the elimination of diazepam. MAO inhibitors, analeptics, psychostimulants – reduce activity. Premedication with diazepam reduces the dose of fentanyl required for the induction of general anesthesia, and reduce the time needed to “switch off” of consciousness with induction doses. May increase the toxicity of zidovudine. Treating may increase the excretion of diazepam and decrease its concentration in plasma. Theophylline (used in low doses) may reduce or even distort the sedative effect. Pharmaceutical incompatible in the same syringe with other drugs.