Atropin-Darnitsa

General characteristics. Structure:

Pharmacological properties:

Pharmacodynamics. Atropine – the alkaloid which is contained in plants of family of a nightshade family, blocker M-holinoretseptorov equally contacts M1-, Sq.m-and of M3 subtypes of muskarinovy receptors. Influences both on central, and on peripheral M-holinoretseptory. Affects also (though is much weaker) N-holinoretseptory. Interferes with a promoting effect of acetylcholine, reduces secretion salivary, gastric, bronchial, the lacrimal and sweat glands. Reduces a tone of muscles of internals (bronchial tubes, digestive tract, a pancreas, bilious channels and a gall bladder, an urethra, bladder); causes tachycardia, improves AV conductivity. Reduces motility of digestive tract, also the pancreas practically does not influence biliary secretion. Expands pupils, complicates outflow of intraocular liquid, increases intraocular pressure, causes accommodation paralysis. In average therapeutic doses influences the central nervous system and causes delayed, but long sedation, excites breath. In high doses causes breath paralysis. Excites a cerebral cortex (in high doses), in toxic doses causes excitement, agitation, hallucinations, coma. Reduces a tone of a vagus nerve that leads to increase in heart rate (at minor change of arterial pressure) and some increase in conductivity in a ventriculonector. Action is expressed stronger at initially raised tone of a vagus nerve. After intravenous administration the maximum effect is shown in 2-4 min.

Pharmacokinetics. Atropine sulfate is quickly soaked up in a blood stream from an injection site. It is quickly distributed in an organism, gets through a blood-brain, placental barrier and into breast milk. Bioavailability – 25%. 50% are metabolized in a liver by enzymic hydrolysis to tropine and tropane acid. Communication with proteins of a blood plasma makes 18%. In significant concentration it appears in the central nervous system in 0,5-1 h. The elimination half-life makes 2 hours. Drug is removed by kidneys: in not changed look – 50%, the rest – in the form of hydrolysates and conjugation.

Pharmaceutical characteristics.

Main physical and chemical properties: transparent colourless liquid.

Incompatibility. Not to mix with other medicines. To use only the recommended solvent.

Indications to use:

As symptomatic means at a peptic ulcer of a stomach and duodenum, a pylorospasm, acute pancreatitis, cholelithiasis, cholecystitis, enterospasms, uric ways, bronchial asthma, bradycardia, as a result of increase in a tone of a vagus nerve, for reduction of secretion salivary, gastric, bronchial, sometimes – sweat glands, for carrying out X-ray inspection of a digestive tract (reduction of a tone and physical activity of bodies).
Drug is used also before an anesthesia and operation and during surgery as the means preventing bronkho-and a laryngospasm, reduces the secretion of glands, reflex reactions and side effects caused by excitement of a vagus nerve. As a specific antidote at poisonings with cholinomimetic connections and antikholinesterazny (including organophosphorous) substances.

Route of administration and doses:

Atropini sulfas is entered subcutaneously, intramusculary, intravenously. At an introduction anesthesia for the purpose of reduction of risk of oppression vagusy heart rate and reduction of secretion of salivary and bronchial glands – 0,3-0,6 mg under skin or intramusculary in 30-60 min. prior to anesthesia; in a combination with morphine (10 mg of morphine of sulfate) – for an hour to anesthesia. At poisoning with antikholinesterazny drugs Atropini sulfas is entered on 2 mg intramusculary by each 20-30 min. before emergence of reddening and a xeroderma, expansion of pupils and emergence of tachycardia, breath normalization. At a moderate and serious poisoning atropine can be entered within two days (before emergence of signs of "reatropinization").

For children the highest single dose depending on age makes:

– up to 6 months – 0,02 mg;

– from 6 months to 1 year – 0,05 mg;

– from 1 to 2 years – 0,2 mg;

– from 3 to 4 years – 0,25 mg;

– from 5 to 6 years – 0,3 mg;

– from 7 to 9 years – 0,4 mg;

– from 10 to 14 years – 0,5 mg.

The highest doses for adults subcutaneously: one-time – 1 mg, daily – 3 mg.

With care appoint Atropini sulfas to people of advanced age.

Features of use:

With care to apply to patients with a prostatauxe without obstruction of urinary tract, with a Down syndrome, at cerebral palsy, a reflux esophagitis, hernia of an esophageal opening of the diaphragm which is combined about a reflux esophagitis, nonspecific ulcer colitis, megacolon, to patients with a xerostomia, patients of advanced age or the weakened patient at chronic diseases of lungs without reversible obstruction, at chronic diseases of the lungs proceeding with insignificant products of the dense difficult separated phlegm, especially at children of younger age and the weakened patients; at vegetative (autonomous) neuropathy.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

Considering a possibility of emergence of such side reactions as dizziness, hallucinations, accommodation disturbance, during use of drug it is necessary to abstain from control of motor transport or work with other mechanisms.

Side effects:

Gastrointestinal frustration: dryness in a mouth, thirst, disturbance of flavoring feelings, a dysphagy, reduction of motility of intestines up to an atony, reduction of a tone of biliary tract and a gall bladder.

From kidneys and urinary tract: difficulty and delay of an urination.
Cordial frustration: tachycardia, arrhythmia, including premature ventricular contraction, myocardium ischemia.
Vascular frustration: face reddening, feeling of inflows.

Neurologic frustration: headache, dizziness, nervousness, sleeplessness.
From organs of sight: expansion of pupils, photophobia, accommodation paralysis, increase in intraocular pressure.

From respiratory system and bodies of a mediastinum: reduction of secretory activity and a tone of bronchial tubes that leads to formation of a viscous phlegm that hard clears the throat.
Changes from skin and hypodermic cellulose: skin rash, small tortoiseshell, exfoliative dermatitis.

From immune system: anaphylactic reactions, acute anaphylaxis.

Others: sweating reduction, xeroderma, dysarthtia.

Interaction with other medicines:

At use of Atropini sulfas with MAO inhibitors there are heart arrhythmias, with quinidine, novokainamidy – summation cholinolytic effect is observed.

At intake together with drugs of a lily of the valley, with a tannin physical and chemical interaction is observed that leads to mutual easing of effects.
Atropini sulfas reduces duration and depth of effect of drugs, weakens analgetic effect of opiates.

At simultaneous use with Dimedrol or isopromethazine effect of atropine amplifies, with nitrates, a haloperidol, corticosteroids for system use – the probability of increase in intraocular pressure increases, with sertraline – the depressive effect of drugs, about Spironolactonum amplifies, minoksidaly – the effect of Spironolactonum and minoksidal decreases, with penicillin – the effect of both drugs amplifies, with nizatidiny – action of a nizatidin amplifies, with ketokonazoly – absorption of a ketokonazol decreases, with ascorbic acid and attapulgite – effect of atropine decreases, with Pilocarpinum – the effect of Pilocarpinum at treatment of glaucoma decreases, with oksprenolony – the anti-hypertensive effect of drug decreases. Under the influence of Octadinum reduction of hyposecretory effect of atropine which weakens action of M-cholinomimetics and antikholinesterazny means is possible. At simultaneous use with sulfanamide drugs the risk of damage of kidneys increases, with potassium drugs – formation of ulcers in intestines is possible, with non-steroidal anti-inflammatory drugs – the risk of formation of stomach ulcers and bleedings increases.

Action of Atropini sulfas can be strengthened at simultaneous use of other drugs with antimuskarinovy effect: M-holinoblokatorov, protivoparkinsonichesky drugs (амантадин), spasmolysants, some antihistamines, drugs of group of phenyl propyl ketone, fenotiazin, dispiramid, quinidine and tricyclic antidepressants, non-selective inhibitors of the return neyronalny capture of monoamines.

Oppression of a vermicular movement under the influence of atropine can lead to change of absorption of other medicines.

Contraindications:

Hypersensitivity to drug components. Diseases of cardiovascular system at which increase in heart rate can be undesirable: ciliary arrhythmia, tachycardia, chronic heart failure, coronary heart disease, mitral stenosis, heavy arterial hypertension. Acute bleeding. Thyrotoxicosis. Hyper thermal syndrome. The digestive tract diseases which are followed by impassability (a gullet achalasia, a pyloric stenosis, an intestines atony). Glaucoma. Liver and renal failure. gravis myasthenia. Ischuria or predisposition to it. Injury of a brain.

Use during pregnancy or feeding by a breast.

Systematic use of drug during pregnancy and in the period of a kromleniye is not recommended by a breast. At the time of delivery at rigidity of a neck of uterus perhaps single use.

Children.
Children of the first 3 months of life are especially sensitive to atropine.
Use drug to children in the doses specified in the section "Route of Administration and Doses".

Overdose:

Symptoms: strengthening of manifestations of side reactions, nausea, vomiting, lowering of arterial pressure, excitement, tremor, spasms, sleeplessness, drowsiness, hallucinations, irritability, hyperthermia, oppression of the central nervous system, suppression of activity of the respiratory and vasomotor centers.
Treatment. Gastric lavage, parenteral administration of cholinomimetics and antikholinesterazny means. At a hyperthermia wet rubdowns and antipyretics are shown, at excitement – intravenous administration of thiopental of sodium or hydroxybutyrate of sodium; at a mydriasis – locally in the form of eye drops Phosphacolum, physostigmine, Pilocarpinum. In case of development of an attack of glaucoma immediately in a conjunctival sac dig in 1% Pilocarpinum solution each hour on 2 drops and subcutaneously 3-4 times a day enter 1 ml of 0,05% of solution of a prozerin.

Storage conditions:

Period of validity. 3 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C. Not to freeze.

Issue conditions:

According to the recipe

Packaging:

On 1 ml in an ampoule; on 10 ampoules in a box; on 5 ampoules in a blister strip packaging, on the 2nd blister strip packagings in a pack.