Atropine sulfate (Solution, Drops) Instructions for Use

ATC Code

A03BA01 (Atropine)

Active Substance

Atropine (BAN)

Clinical-Pharmacological Group

M-Cholinoreceptor blocker

Pharmacotherapeutic Group

M-cholinoblocker

Pharmacological Action

Atropine is an m-cholinoreceptor blocker, a natural tertiary amine. It is believed that Atropine binds equally to M1-, M2-, and M3- subtypes of muscarinic receptors. It affects both central and peripheral m-cholinoreceptors.

It reduces the secretion of salivary, gastric, bronchial, and sweat glands. It lowers the tone of smooth muscles of internal organs (including the bronchi, digestive system organs, urethra, urinary bladder), and reduces gastrointestinal motility. It has almost no effect on bile and pancreatic secretion.

In average therapeutic doses, Atropine has a moderate stimulating effect on the central nervous system and a delayed but prolonged sedative effect. The central anticholinergic action explains atropine’s ability to relieve tremor in Parkinson’s disease.

In toxic doses, Atropine causes excitation, agitation, hallucinations, and a comatose state. Atropine reduces the tone of the vagus nerve, which leads to an increase in heart rate with little change in blood pressure, and increased conduction in the bundle of His.

In therapeutic doses, Atropine does not have a significant effect on peripheral vessels, but vasodilation is observed in case of overdose.

Pharmacokinetics

After systemic administration, it is widely distributed in the body. It penetrates the blood-brain barrier. A significant concentration in the central nervous system is reached within 0.5-1 hour. Plasma protein binding is moderate.

The elimination half-life (T_1/2) is 2 hours. It is excreted in the urine; about 60% unchanged, the remainder as hydrolysis and conjugation products.

Indications

Spasm of smooth muscle organs of the gastrointestinal tract; gastric ulcer (in the acute phase) and duodenal ulcer (in the acute phase), acute pancreatitis, hypersalivation (parkinsonism, poisoning by heavy metal salts, during dental procedures), renal colic, hepatic colic, bronchospasm, laryngospasm (prevention); AV block, bradycardia; premedication before surgical operations; poisoning by m-cholinomimetics and anticholinesterase substances (reversible and irreversible action).

ICD codes

Dosage Regimen

Solution

To relieve acute pain in gastric and duodenal ulcers and pancreatitis, in renal and hepatic colic, administer subcutaneously or intramuscularly at 0.25-1 mg.

To eliminate bradycardia – intravenously at 0.5-1 mg, if necessary, the administration can be repeated after 5 minutes.

For premedication – intramuscularly 0.4-0.6 mg 45-60 minutes before anesthesia.

For children, administer at a dose of 0.01 mg/kg.

In case of poisoning with m-cholinomimetics and anticholinesterase agents – administer intravenously, preferably in combination with cholinesterase reactivators.

Drops

Apply topically as instillations into the conjunctival sac up to 3 times with an interval of 5-6 hours.

Adverse Reactions

From the digestive system dry mouth, constipation, intestinal atony.

From the central nervous system headache, dizziness.

From the cardiovascular system sinus tachycardia, exacerbation of myocardial ischemia due to excessive tachycardia, ventricular tachycardia and ventricular fibrillation.

From the urinary system difficulty urinating, bladder atony.

From the sensory organs photophobia, mydriasis, paralysis of accommodation, impaired tactile perception, increased intraocular pressure.

Contraindications

Hypersensitivity to atropine, angle-closure glaucoma (mydriasis leading to increased intraocular pressure may cause an acute attack), tachyarrhythmias, severe chronic heart failure, ischemic heart disease, mitral stenosis, reflux esophagitis, hiatal hernia, pyloric stenosis, hepatic and/or renal failure, intestinal atony, obstructive bowel diseases, paralytic ileus, toxic megacolon, ulcerative colitis, xerostomia, myasthenia gravis, urinary retention or predisposition to it, diseases accompanied by obstruction of the urinary tract (including bladder neck due to prostatic hypertrophy), Down’s syndrome, cerebral palsy, pregnancy toxemia, lactation period.

With caution

Hyperthermia, open-angle glaucoma, chronic heart failure, arterial hypertension, chronic lung diseases, acute blood loss, hyperthyroidism, age over 40 years, pregnancy.

Use in Pregnancy and Lactation

Atropine crosses the placental barrier. Adequate and well-controlled clinical studies on the safety of atropine use during pregnancy have not been conducted. Intravenous administration during pregnancy or shortly before delivery may cause fetal tachycardia. Use during pregnancy is only possible if the potential benefit outweighs the potential risk to the fetus.

Atropine is detected in breast milk in trace concentrations. If use during lactation is necessary, breastfeeding should be discontinued.

Use in Hepatic Impairment

Use with caution in hepatic failure.

Use in Renal Impairment

Use with caution in renal failure.

Pediatric Use

Contraindicated in cerebral palsy.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

During treatment, it is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use with anticholinergic agents and agents with anticholinergic activity, the anticholinergic effect is enhanced.

With simultaneous use with atropine, a slowdown in the absorption of zopiclone, mexiletine, and a decrease in the absorption of nitrofurantoin and its renal excretion is possible. The therapeutic and side effects of nitrofurantoin are likely to be enhanced.

With simultaneous use with phenylephrine, an increase in blood pressure is possible.

Under the influence of guanethidine, a decrease in the hyposecretory effect of atropine is possible.

Nitrates increase the likelihood of increased intraocular pressure.

Procainamide enhances the anticholinergic effect of atropine.

Atropine reduces the plasma concentration of levodopa.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.