Dithilinum (solution for injections 2%)
Solutio Dithilini 2% pro injectionibus
International not patented name
Suxamethonium iodide
Pharmacotheraupic group
Myorelaxation drug of peripheral action
Preparation composition
1 ml of solution contains 20 mg of dithilinum.
Pharmaceutical action
Pharmacodynamics
Dithilinum is a depolarizing myorelaxation drug. It violates the neuromuscular stimulation conduct and causes the skeletal muscles relaxation. The preparation is destructed quickly by the blood pseudocholinesterase. Repeated injections of the preparation are necessary for the muscles long time relaxation. A quick preparation effect and a quick restoration of the muscular tonus after that allow to make the muscular relaxation controlled and regulated.
After in intravenous injection a complete muscular relaxation is observed for 40 – 60 seconds. The muscular tonus and function restore in full as a rule within 5 – 10 minutes.
Pharmacokinetics
The preparation is hydrolyzed under pseudocholinesterase action in blood and tissues. It is excreted by the kidneys. The period of half elimination from the blood plasma (T1/2) is 2 – 4 minutes. Under a severe hepatic failure or genetic pseudocholinesterase lack T1/2 increases to several hours.
Indications
Trachea intubation, endoscopic procedures (broncho- and esophagoscopy, cytoscopy, etc.), short time operations (making sutures on the abdominal wall, setting bones, reposition of osseous pieces in case of fractures and other interferences). In case the dose is adequate and for re-injections dithilinum may be used for more long time operations as well. In addition the preparation may be used for convulsions stopping in case of tetanus and strychnine intoxication.
Mode of appliance and dosing regime
Dithilinum may be applied only in specialized hospitals having adequate apparata and specific antidotes. The dosing regime is determined individually.
For intubation and for a complete relaxation of skeletal and respiratory muscles during the operation dithilinum is injected in doses 1.5 – 2 mg/kg. For providing a prolonged muscular relaxation during the operation the preparation is injected by fractions in 5 – 7 minutes the dose being 0.5 – 1 mg/kg. For the skeletal muscles relaxation when the bone should be set or the osseous pieces reposition should be performed the preparation is injected in a dose 100 – 200 μg/kg. For performing endoscopy or electroencephalography the dithilinum dose is 200 μg/kg.. For complications prevention under electric impulse therapy the preparation is injected in a dose 100 μg/kg – 1 mg/kg.
Special warnings
Nervous and muscular blockade intensity and duration increase caused by dithilinum may be observed under the following diseases and states: pregnancy and postpartum period; tetanus, tuberculosis and other severe or chronic infections; states after severe burns; chronic diseases accompanied by nervous and physical breakdown; malignant neoplasms, chronic anemia and malnutrition, hepatic and/or renal failure, myxedema, collagenous diseases, states after plasma transfusion, plasmapheresis, artificial blood circulation.
Side effects
In case of dithilinum appliance the following complications are possible: the myocardium conductivity and stimulation changes, bradycardia, arterial hypertension or hypotensiom; prolonged apnea; hyperthermia; hepatic function changes; intraocular pressure increase; muscular pain especially in the thorax and abdominal area; hyperkalemia; hypersalivation; hypotension; bronchospasm; rhabdomyolisis accompanied by myoglobulinemia and myoglobinuria; fever; allergic reactions.
Contraindications
The preparation hypersensitivity, acute renal and hepatic failure, myasthenia, glaucoma, penetrating trauma of the eye, pronounced anemia, extended burns and traumas, bronchial asthma, respiratory failure, pseudocholinesterase low activity, malignant hyperthermia in the anamnesis, hyperkalemia. The preparation is not recommended for infants, for children over 1 year in case of out-of-plan operations. It is not recommended for pregnant women except for cases of an extreme necessity.
The preparation should be prescribed with care in case of severe diseases of the liver, anemia, cachexia, diseases of the respiratory organs, neuromuscular diseases, in case of an increased intraocular pressure, for persons manifesting hypokalemia. The preparation is not recommended for multiple injections or for injections of increased doses to persons with renal failure (hyperkalemia and neuropathy absent). Dithilinum ijections should be avoided in case of congenital and dystrophic myotonia, Duchenne’s muscular dystrophy.
Interaction with other medicines
Proserin and other anti-cholinesterase drugs may prolong and enhance the dithilinum effect. Dithilinum cannot be injected with the blood preparations (the preparation activity reduces). It is prohibited to be mixed with alkaline solutions in the same syringe including the barbituric acid derivatives with a short action (a precipitation is formed).
The neuromuscular blockade duration caused by dithilinum is observed to increase in case of a simultaneous introduction of preparations reducing the pseudocholinesterase activity (phosphor organic insecticides and metrifonate, trimetafan, neostigmin, piridostigmin, edrofonium, cyclophosphamide, thiotepa, promasine and chlorpromazine, ketamin, morphine and its antagonists, pancuronium, propanidid, etc.). The neuromuscular blockade intensity and duration are caused by the magnesium salts, lithium carbonate, quinine, chloroquinine, antibiotics from the aminoglicosides group, clyndamycin and polymixins, anti-arrhythmic drugs – quinidine, procaine amide, verapamil, beta-adrenoblockers, lidocain and procain, drugs for inhalation narcosis – halothane, enflurane, isoflurane, diethyl esther and metoxyflurane.
Overdosing
Symptoms: difficult breathing may occur, in some cases a short time spontaneous respiratory standstill is possible.
Treatment: the lungs artificial ventilation. In case of a necessity fresh blood should be transfused for introducing the pseudocholonesterase it contains. The electrolyte changes should be corrected.
Dosage form
2% solution for injections in 10 ml vials. Five or ten vials are packed into a cartoon or a contour cellular pack. One or two contour cellular packs are put into a cartoon.
