Atropine is a m-cholinergic receptor blocker.
The pharmacological preparation is in the form of eye drops, as well as in the form of solutions for injection. It contains the main active element - atropine sulfate. In the form of eye drops, the drug is available in 10 and 5 ml in bottles equipped with polyethylene droppers. They are packed in cardboard boxes in one bottle.
Consider the contraindications to the use of Atropine.
Pharmacological properties of the drug
Atropine in the form of eye instillation solutions is a m-cholinergic receptor blocker and a tertiary natural amine. It is believed that atropine is equally capable of binding to the M1, M2, and M3 types of muscarinic receptors and affect central m-cholinergic receptors.
This substance lowers the secretion of sweat, stomach, salivary and bronchial glands. Reduces the tone of smooth muscles of the organs (digestive, genitourinary, respiratory), reduces the motility of the digestive tract. Virtually no effect on the secretion of the pancreas and bile. Causes accommodation paralysis, mydriasis, reduces the secretion of lacrimal fluid.
At moderate therapeutic dosages, atropine has a stimulating effect on the central nervous system and a delayed but prolonged sedative effect. The main anticholinergic effect explains the ability of this substance to eliminate tremor in Parkinson's disease. At higher dosages, atropine causes agitation, agitation, coma, hallucinations.
This can be especially pronounced if contraindications to the use of Atropine are not taken into account.
The medication reduces the vagus nerve excitation, which contributes to an increase in heart rate (with an insignificant change in blood pressure), an increase in conductivity in the bundle of His.
In recommended therapeutic doses, this active element does not significantly affect the work of peripheral vessels, however, with an overdose, vasodilation is noted.
When used locally in ophthalmology, pupil expansion occurs after about 40 minutes and disappears after 8-10 days. Mydriasis caused by atropine cannot be eliminated during the instillation of cholinomimetic drugs.
Indications and contraindications "Atropine" are described in detail in the instructions.
Pharmacokinetics
The medicine is well absorbed from the digestive tract and through the conjunctival membrane. With regular administration, the drug is distributed over the tissues of the body and penetrates the placental barrier. The maximum concentration in the central nervous system is achieved within 30-60 minutes. Slightly bound to plasma proteins. The half-life of the active element from the body is two hours. A medication is excreted, mainly with urine. Unchanged - about 60%, the rest - in the form of conjugation products.
Before considering the contraindications of Atropine, we’ll talk about when it is prescribed.
Indications for use
For systemic use, Atropine is prescribed in such cases:
- Spasms of the smooth muscle organs of the digestive system, bronchi and bile ducts.
- Peptic ulcer of the stomach and duodenum, acute pancreatitis.
- Hypersalivation (heavy metal poisoning, parkinsonism, after dental interventions).
- Colon irritation syndrome, intestinal colic.
- Renal colic.
- Premedication before surgical procedures.
- Bronchitis with hypersecretion, laryngospasm, bronchospasm.
- AV block, slow heart rate.
- Poisoning with anticholinesterase and m-cholinomimetics substances (irreversible and reversible effects).
- X-ray examination of the digestive tract of the digestive tract (if necessary, reduce their tone).
Local use of this pharmacological agent in ophthalmology:
- In studies of the fundus and achievement of paralysis of accommodation in order to establish true eye refraction.
- In the treatment of iritis, choroiditis, iridocyclitis, embolism, keratitis and spasm of the retinal arteries and eye injuries.
Atropine drops are contraindicated in large quantities.
Dosage and administration
This medication is used subcutaneously or intramuscularly 300-600 mcg one hour before the induction of anesthesia or intravenously in the same dosage immediately before induction.
For relief of bradycardia, intravenously 0.5-1 mg, if necessary, after a few minutes, the drug can be repeated.
With local use in ophthalmology, the drug is instilled in the eyes for 1-2 drops - up to 3 times a day with an interval of 6 hours.
In some cases, the drug solution can be administered parabulbally - 0.3-0.5 ml or subconjunctival 0.2-0.5 ml. Through electrophoresis, a 0.5% solution from the anode is injected through the eyelids or eye baths.
The contraindications of Atropine and side effects are listed below.
Side effects
Digestive tract: thirst, dry mouth, change in taste, decreased bowel motility, atony, dysphagia, decreased gall bladder tone.
Urinary system: delay and difficulty urinating.
Cardiovascular system: arrhythmia, tachycardia, extrasystole, facial flushing, myocardial ischemia, hot flashes.
Nervous system: cephalgia, dizziness, insomnia, nervousness.
Organs of vision: dilated pupils, photophobia, increased intraocular pressure, change in vision. Because of these phenomena, “Atropine” contraindications are available not only with systemic treatment, but also with local treatment.
Respiratory and mediastinal organs: decreased secretory tone and activity of the bronchi, which leads to the formation of viscous sputum, difficulty in expectoration.
Subcutaneous tissue and skin: skin rashes, exfoliative dermatitis, urticaria.
Immune system: hypersensitivity reaction, anaphylactic shock, anaphylactic reactions.
Other phenomena: decreased sweating, dysarthria, dry skin, soreness at the injection site.
Contraindications "Atropine"
You can not use this medication for hypersensitivity, pathologies of the cardiovascular system, characterized by an increase in the frequency of heart contractions: tachycardia, coronary artery disease, atrial fibrillation, mitral stenosis. In addition, the list of contraindications includes hypertension, bleeding, thyrotoxicosis, intestinal atony in the elderly and weak patients, paralytic obstruction in the intestine, open-angle or angle-closure glaucoma, renal failure (risk of side effects due to decreased excretion), prostate hypertrophy without obstruction of the urinary tract predisposition to urinary retention and diseases that are accompanied by obstruction, depletion of the body.
Atropina contraindications should be strictly observed.
With some caution, this medication is used at elevated body temperature, reflux esophagitis, hiatal hernias in the diaphragm, diseases of the digestive system, accompanied by obstruction - achalasia of the esophagus. With caution, a medicine is also prescribed for diseases with high intraocular pressure, ulcerative colitis, dry oral mucosa, chronic lung pathologies, myasthenia gravis, gestosis, brain damage in children, cerebral palsy, and Down's disease.
It is important to familiarize yourself with the contraindications and instructions for “Atropine” in advance.
Use during pregnancy and lactation
The drug penetrates the placental barrier. Strictly controlled and adequate clinical studies on the safety of this substance during pregnancy have not been conducted. Therefore, it is not prescribed to women during the period of bearing a child. With intravenous use during pregnancy or before childbirth, the fetus may develop tachycardia. Atropine in trace concentrations can be found in breast milk.
With special care, this medication is used in children with chronic lung pathologies, brain damage, Down's disease and cerebral palsy.
special instructions
With caution, the medication is used in patients with diseases of the heart and blood vessels, in which an increase in heart rate may be undesirable: tachycardia, atrial fibrillation, mitral stenosis, coronary heart disease, etc.
Between receptions of this drug and antacid medicines containing calcium carbonate or aluminum, the interval should be at least one hour.
With parabulbar or subconjunctival administration of Atropine, the patient should take a validol tablet under the tongue in order to reduce the severity of tachycardia.
During therapy, the patient is advised to exercise some caution when driving and engaging in other potentially dangerous activities that require a high concentration of attention, speed of mental and motor reactions, and normal vision.
Not only contraindications for atropine sulfate must be considered, but also its interaction with other substances.
Interaction with other medicines
With concomitant oral administration with antacids that contain calcium carbonate or aluminum, the absorption of atropine from the digestive tract is reduced.
With simultaneous use with anticholinergics and drugs that have anticholinergic activity, the anticholinergic effect increases.
With atropine therapy, inhibition of the absorption of mexiletine, zopiclone, nitrofurantoin and the excretion of these substances by the kidneys is possible. A slight increase in the side and therapeutic effects of nitrofurantoin is also possible.
With the concomitant use of the drug with phenylephrine, an increase in pressure can be observed. Under the influence of guanethidine, a decrease in the hyposecretory activity of atropine is likely. Nitrates increase the likelihood of increased intraocular pressure. The medicine lowers the concentration in the blood plasma of levodopa.
This is confirmed by the instructions for use.
Contraindications for Atropine and its analogues are the same.
Analogs
Similar means are:
- Midriacil is a mydriatic blocking the m-cholinergic receptors of the ciliary muscle and sphincter of the iris, causing accommodation paralysis and mydriasis. It acts quickly, but not for long. The likelihood of an increase in intraocular pressure is less pronounced than with Atropine. It is used for diagnostic purposes, if necessary, cycloplegia and mydriasis in studies of the fundus.
- "Tropicamide" is a medication that is absolutely identical to the above.
- "Cycloptic" - a pharmacological agent, which is an M-anticholinergic. Cyclopentolate, as the main element of this medication, blocks m-cholinergic receptors, inhibiting the effects of mediators of cholinergic synapses. As a result of this effect, the expansion of the eye pupil occurs due to the fact that muscle tone, the dilating pupil begins to prevail, as well as the relaxation of those muscles that constrict it. At the same time, cycloplegia (accommodation paralysis) occurs.
Reviews
There are very few reviews about this medication, since it is a specific drug that is not often used by patients during self-treatment, but is used, as a rule, in hospitals for specific purposes specified in the instructions.
Patients who used it, as well as medical specialists indicate its high efficiency and full compliance with the goals for which it is prescribed and used. Patients say that the medicine is well tolerated, almost never provokes unwanted reactions.
We reviewed the instructions and contraindications of Atropine.