Universal reference book for medicines
Name of the drug: Ditilin-Darnitsa (DITHYLIN-DARNITSA)

Active substance: suxamethonium iodide

Type: Muscle relaxant of peripheral action of depolarizing type

Manufacturer: DARNITSA PHARMACEUTICAL FIRM (Ukraine)
Composition, form of production and packaging
Solution for intravenous and / m administration
1 ml 1 amp.

suxamethonium iodide 20 mg 100 mg

5 ml - ampoules (10) - packs of cardboard.

5 ml - ampoules (5) - contoured packages (1) - cardboard packs.

5 ml - ampoules (5) - packings contour (2) - packs cardboard.

5 ml - ampoules (5) - contoured packages (5) - cardboard packs.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Depolarizing short-acting muscle relaxant.
It causes a blockade of the neuromuscular transmission. Interacting with H-holinoretseptorami, causes depolarization of the terminal plate. The process extends to adjacent membranes, there is a generalized contraction of myofibrils (i.e., the development of blockade is preceded by muscle twitching - the result of a short-term relief of neuromuscular transmission). Membranes, remaining depolarized, do not respond to additional impulses, since the maintenance of muscle tone requires the arrival of repeated pulses, associated with repolarization of the terminal plate, spastic paralysis occurs.
After intravenous administration, muscle relaxation occurs in the following sequence: eyelids, chewing muscles, muscles of the fingers, eyes, limbs, neck, back and abdomen, vocal cords;
then intercostal muscles and diaphragm.
Causes an increase in cerebral blood flow and increased intracranial pressure.

After the / m introduction, the effect develops in 2-4 minutes;
after intravenous administration - after 54-60 sec, after 2-3 min the muscle relaxation reaches a maximum and remains in full 3 min. The duration of action is 5-10 minutes.
The severity of the action depends on the amount of the administered dose: 0.1 Ој / kg - relaxation of the skeletal muscle without significant effect on the respiratory system, 0.2-1 mg / kg - complete relaxation of the musculature of the abdominal wall and respiratory muscles (there is significant restriction or complete stopping of spontaneous breathing).
For a long relaxation of the muscles, a second injection is necessary. The rapid onset of the effect and the subsequent rapid restoration of muscle tone allow the creation of a controlled and controlled relaxation of the muscles.
PHARMACOKINETICS

After intravenous administration is distributed in plasma and extracellular fluid.
More than 90% is hydrolyzed by cholinesterase of blood to succinic acid and choline.The half-life period is 90 sec with a normal level of pseudocholinesterase. It is excreted by the kidneys. Does not penetrate the intact blood-brain barrier. Do not cumulate.
INDICATIONS

- disabling of spontaneous breathing (intratracheal intubation, bronchoscopy);

- complete miorelaxation (endoscopy, correction of dislocations, repositioning of fractures, gynecological, thoracic, abdominal operations);

- prevention of seizures in electropulse therapy;

- Strychnine poisoning;

- tetanus (symptomatic therapy).

DOSING MODE

In / in (struyno, drip), in / m.

Adults: iv, slow, jet or drip (for long-term drop infusion use 0.1 solution).
Depending on the clinical situation, with iv introduction, a single dose varies from 100 Ојg / kg to 1.5-2 mg / kg.
In / m is used only in children in doses up to 2.5 mg / kg, but not more than 150 mg, in / in - 1-2 mg / kg.

To carry out intiubation of the trachea - 0.2-0.8 mg / kg;
for miorelaxation and disabling of spontaneous breathing - 0.2-1 mg / kg; for the relaxation of skeletal muscles when sprains are dislocated and reposition of bone fragments at fractures is 0.1-0.2 mg / kg, for endoscopy - 0.2 mg / kg; for the prevention of complications during electropulse therapy (convulsions, muscle and tendon rupture) - 0.1-1 mg / kg IV and up to 2.5 mg / kg IM, but not more than 150 mg.
For a long relaxation of the musculature during the whole operation, it can be injected fractionally, after 5-7 minutes, at 0.5-1 mg / kg.
Repeated doses last longer.
SIDE EFFECT

Allergic reactions (anaphylactic shock, bronchospasm);
hyperkalaemia, decreased blood pressure, arrhythmias, bradycardia (more often in children, with repeated administration - in children and adults), conduction disorders, cardiogenic shock, increased intraocular pressure, hypersalivation, fever; myalgia (in the postoperative period); long paralysis of the respiratory muscles (associated with a genetically determined violation of the formation of serum cholinesterase); rarely - rhabdomyolysis with the development of myoglobinemia and myoglobinuria.
CONTRAINDICATIONS

hypersensitivity;

- malignant hyperthermia (including in the anamnesis);

myasthenia gravis;

- congenital and dystrophic myotonia;

- Duchenne muscular dystrophy;

- an angle-closure glaucoma;

acute liver failure;

- pulmonary edema;

penetrating eye trauma;

- bronchial asthma;

- Hyperkalemia;

- Infant age (up to 1 year);

- Pregnancy.

Caution: decreased serum pseudocholinesterase activity (terminal stage of hepatic insufficiency, anemia, cachexia, prolonged fasting, chronic infections, common burns, traumas), postpartum period, tetanus, tuberculosis, malignant neoplasms, chronic renal failure, myxedema, systemic connective tissue diseases, after plasma transfusion, plasmapheresis, artificial circulation, acute or chronic intoxication with insecticides - cholinester inhibitors
(if ingested) or with anticholinesterase agents (neostigmine, physostigmine, distigmine, phospholin), simultaneous use of drugs competing with succinylcholine for cholinesterase (procaine intravenous), emergency surgery in patients with a "full stomach".
PREGNANCY AND LACTATION

Contraindicated in pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution: chronic renal failure.
Patients with renal insufficiency (without signs of hyperkalemia and neuropathy) are given a single dose of the drug in moderate doses, but do not apply for multiple injections or at elevated doses because of the risk of developing hyperkalemia.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in acute liver failure.
With caution: decreased serum pseudocholinesterase activity (terminal stage of hepatic impairment


APPLICATION FOR CHILDREN

Prohibited intake of the drug in infancy (up to 1 year).

SPECIAL INSTRUCTIONS

Applied only in the conditions of a specialized department with the availability of equipment for artificial ventilation and personnel who own this technique and against a background of general anesthesia.

Pre-introduction 1 minute prior to infusion of suxamethonium chloride with a drug of 3-4 mg d-tubocurarin or 10-15 mg of diplatin prevent fibrillar muscle twitching and the subsequent appearance of muscle pain.

With the appropriate dose and repeated administration can be used for longer operations, however, for long-term relaxation of the muscles, nondepolarizing muscle relaxants are usually used, which are administered after a pre-intubation of the trachea against a background of suxamethonium iodide.

Slow introduction of the drug, as well as preliminary intravenous injection of atropine at a dose of 1-1.5 mg significantly prevents bradycardia and increased bronchial secretion.

Patients with renal insufficiency (without signs of hyperkalemia and neuropathy) are given a single dose of the drug in moderate doses, but do not apply for multiple injections or at elevated doses because of the risk of developing hyperkalemia.

Prolonged muscle relaxation with possible apnea can be caused by several reasons: "atypical" cholinesterase of blood serum, hereditary insufficiency of serum cholinesterase, or a temporary decrease in its level.

If the drug is injected repeatedly and 25-30 minutes after the last injection, the patient does not restore muscle tone, there is superficial breathing, one can think of the transition of the depolarizing unit to an antidepolarizing one (the occurrence of a "double block").
To remove this effect, you should use proserine according to the usual method: pre-atropine is administered to the vein at a dose of 0.5-0.7 mg (0.5-0.7 ml of 0.1% solution), pulse arrivals are waiting and after 1-2 minutes IV injected prozerin at a dose of 1.5 mg (3 ml of a 0.05% solution).
In children, young patients and women (mainly in the vagotonics), a short-term bradycardia may occur, and in some cases, an asystole.

After 10-12 hours after application of the drug, muscle pain may occur.
With repeated administration of the drug, excessively prolonged muscle relaxation and prolonged apnea can sometimes develop.
OVERDOSE

Symptoms: stop breathing.

Treatment: IVL, in case of a decrease in the content of cholinesterase in the blood serum - a transfusion of fresh blood.

DRUG INTERACTION

Pharmaceutically incompatible with donor blood and blood products (hydrolysis occurs), blood and serum preservatives;
with solutions of barbiturates and alkaline solutions (a precipitate is formed). Compatible with isotonic solutions of sodium chloride, Ringer's solution, 5% fructose solution and 6% dextran solution.
Anticholinesterase drugs, procaine, procainomide, lidocaine, verapamil, beta-adrenoblockers, aminoglycoside antibiotics, amphotericin B, clindamycin, cycloprane, propanidide, organophosphate insecticides, Mg2 + and Li + salts, quinidine, quinine, chloroquine, pancuronium strengthen and prolong the muscle relaxant effect.Compatible with other muscle relaxants, narcotic analgesics.

Strengthens the cardiac effects of cardiac glycosides (bradycardia).

Reduces the effectiveness of antimiasthenic drugs.

Halogen-containing agents for general anesthesia are enhanced, and thiopental sodium and atropine reduce the unwanted effects on the cardiovascular system.

Drugs that have the potential to reduce cholinesterase activity (aprotinin, diphenhydramine, promethazine, estrogens, oxytocin, high-dose glucocorticosteroids, oral contraceptives) increase and prolong the muscle relaxant effect of suxamethonium.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List A.

The drug should be stored at a temperature no higher than 5 В° C (freezing is not allowed), protected from light, out of reach of children.

Shelf life 2 years.

Do not use after the expiry date printed on the package.

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