Presentation and Status in Health Basket
100 X 1 mg/ml
5, 25, 100 X 20 mg / 10 ml
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Recommended dosage is 0.4-0.6 mg by I.M. or I.V. injection. The complete atropinizing dose in man is believed to be in the order of 2 mg I.V.
Relaxation of spastic GI tract (e.g. pylorospasm), biliary and GU tracts; reduction of salivation and bronchial secretion, combat CNS and peripheral toxic effects; suppression of vagally-mediated bradyarrhythmias.
Known hypersensitivity to atropine and other anticholinergic drugs.
Ocular: Closed angle glaucoma, adhesions (synechiae) between the iris and lens.
Cardiovascular: Tachycardia secondary to cardiac insufficiency or thyrotoxicosis, unstable cardiovascular status in acute hemorrhage,
Gastrointestinal: Obstructive disease (e.g. achalasia, pyloroduodenal stenosis or pyloric obstruction, cardiospasm); paralytic ileus, intestinal atony of the elderly or debilitated, severe ulcerative colitis, toxic megacolon complicating ulcerative colitis, hepatic disease; reflux esophagitis.
Genitourinary: Obstructive uropathy (e.g., bladder neck obstruction due to prostatic
hypertrophy), renal disease. Prostatic enlargment.
Musculoskeletal: Myasthenia gravis (unless used to treat the adverse effects of an anticholinesterase agent) .
Atropine is contraindicated in asthma patients. Due to risk of provoking hyperpyrexia due to reduced sweating, Atropine should not be given to febrile patients, or when the ambient temperature is high.
Toxemia of pregnancy.
Hypersensitivity to atropine and other anticholinergic drugs. Narrow-angle glaucoma, adhesions (synechiae) between the iris and lens. Tachycardia, unstable cardiovascular status in acute hemorrhage, myocardial ischemia. Obstructive disease (e.g. pyloric obstruction), paralytic ileus, toxic megacolon complicating ulcerative colitis. Obstructive uropathy (e.g. bladder neck obstruction due to prostatic hypertrophy). Myasthenia gravis.
For full details see prescribing information.
Atropine should be used with caution in the presence of the following:
Ocular: Light irides. If there is mydriasis and photophobia, dark glasses should be worn. Caution should be exercised in the elderly because of increased incidence of glaucoma.
Gastrointestinal: Early evidence of ileus as in peritonitis, ulcerative colitis (large doses may suppress intestinal motility and precipitate or aggravate toxic megacolon), hiatal hernia associated with reflux esophagitis (anticholinergics may aggravate this condition).
Genitourinary: Renal disease, prostatic hypertrophy. Patients with prostatism can have dysuria and may require catheterization.
Cardiovascular: Coronary artery disease, congestive heart failure, cardiac arrhythmias, tachycardia, hypertension.
Pulmonary: Debilitated patients with chronic lung disease, reduction in bronchial secretions can lead to inspissation and formation of bronchial plugs. Caution should be exercised in patients with allergies.
Miscellaneous: Hepatic disease, autonomic neuropathy, hyperthyroidism. The risk of hyperpyrexia is increased in patients with fever. In elderly patients, confusional states are more common.
Special Risk Patients: Caution should be exercised in infants, small children, blondes, persons with Down’s syndrome, brain damage, or spastic paralysis.
Hazardous Tasks: Drowsiness, dizziness, or blurred vision may be produced. Caution should therefore be exercised when driving or performing other tasks requiring alertness.
Tachycardia may result from vagal inhibition and induce angina pectoris in patients with coronary heart disease. With respect to the central nervous system doses of 0.5-1 mg of atropine are mildly stimulating.
After larger doses, there may be mental disturbances; still larger doses may cause depression.
Tolerance may occur to a limited extent, particularly in patients with parkinsonism. Patients should be cautioned not to exceed the prescribed dose, to decrease the dose if dry mouth occurs and to discontinue use if rapid pulse, blurred vision or dizziness occur.
Most side effects are directly related to the antimuscarinic actions of atropine. Adverse effects following single or repeated doses are most often the result of excessive dosage.
Cardiovascular: Transient bradycardia followed by tachycardia with palpitations and arrhythmia. Atropine blocks vagal impulses with consequent increase in heart rate with possible atrial arrhythmias, atrioventricular dissociation, multiple ventricular ectopics and angina. The development of angina in patients with known cardiac problems has been reported. Hypertensive crises and atrioventricular block have also been reported.
Central Nervous System : Dryness of the mouth, with difficulty in swallowing or talking, thirst. These are due to the reduction of salivary, bronchial and sweat secretions and are dose related. Active and passive functions of the Eustachian tube may be affected. Tremor, fatigue, drowsiness, ataxia, mental confusion, and/or excitement, dizziness, loss of taste, headache, nervousness, weakness, nausea, vomiting, insomnia, psychotic reactions, sedation and seizures. Anhidrosis also may occur and produce heat intolerance in patients living in a hot environment. The inhibition of sweat secretions may also result in hyperthermia.
Gastrointestinal: Constipation; due to inhibition of parasympathetic control of the GI tract Paralytic ileus. Nausea, vomiting, retrosternal pain due to increased gastric reflux, bloated feeling.
Genitourinary: Urinary difficulty and retention due to inhibition of parasympathetic control of the bladder.
Ocular: Visual changes, including blurred vision. Dilatation of the pupils (mydriasis) with loss of accommodation (cycloplegia) and photophobia can occur with increasing doses of atropine. Increased ocular tension.
Dermatological: Flushing, and dryness of the skin. Hypersensitivity reactions may manifest as conjuncitivitis or skin rash which, in some instances, progresses to exfoliation and various dermal manifestations.
Other: More common: Redness or other signs of irritation at the injection site.
Antimuscarinic Effects: The effect of atropine may be enhanced by concomitant administration of other drugs with antimuscarinic properties, such as:
– some antihistamines, including cyproheptadine, promethazine
– butyrophenones e.g. haloperidol
– phenothiazines e.g.. chlorpromazine, fluphenazine, perphenazine, prochlorperazine,
promazine, thioridazine, trifluoperazine.
– tricyclic antidepressants e.g. amitriptilyne, desipramine, doxepin, imipramine, nortriptyline
– antiparkinsonian drugs
– antiarrhythmics with anticholinergic activity (eg. disopyramide, quinidine)
Patients should be advised to report occurrence of gastrointestinal problems promptly since paralytic ileus may occur with concurrent therapy.
MAOIs: Inhibition of drug metabolizing enzymes by MAOIs may possibly enhance the effects of atropine.
Opioid (narcotic) analgesics Concurrent use with anticholinergics may result in increased risk of severe constipation, which may lead to paralytic ileus and/or urinary retention.
Urinary Alkalizers: Urinary excretion of atropine may be delayed by alkalization of the urine, thus potentiating its effects.
The absorption of other medicines may be affected by the reduction in gastric motility caused by atrooine.
Ketoconazole : Anticholinergics may increase gastrointestinal pH, possibly resulting in a marked reduction in ketoconazole absorption during concurrent use. If concomitant therapy is necessary, atropine atropine should be given at least two hours after oral ketoconazole.
Atropine antagonizes the actions of a number of compounds, including:
– synthetic choline esters e.g. bethanecol, carbachol
– anticholinesterase drugs e.g. physostigmine, neostigmine, pyridostigmine
– cholinomimetic alkaloids e.g. pilocarpine.
Parasympathomimetics (each may counteract the effect of the other)
Cisapride and Metoclopramide : Concurrent use with anticholinergics may antagonize the effects of cisapride and metoclopramide on gastrointestinal motility
Haloperidol : Antipsychotic effectiveness of haloperidol may be decreased in schizophrenic patients.
Cholinesterase inhibitors : In view of the pharmacodynamic effects of atropine, it may interfere with the activity of cholinesterase inhibitors such as rivastigmine, donepezil.
Effect on the ability to drive or operate machinery : Systemic administration of antimuscarinics may cause drowsiness, blurred vision, dizziness and other effects that may impair a patients ability to perform tasks requiring mental alertness and/or visual acuity (such as driving or operating machinery).
Pregnancy and Lactation
Pregnancy: Safety of use in pregnancy has not been established. Although atropine has been taken by a large number of pregnant women and women of child-bearing age without an increase in the frequency of malformations or other direct or indirect harmful effects on the fetus being observed, the safety of atropine in pregnancy has not been positively established. As with all other drugs, caution must be exercised in the use of atropoine in pregnant women and women of child-bearing age. Atropine crosses the placental barrier and may cause tachycardia in the fetus.
Lactation: Atropine may be excreted in milk causing infant toxicity and may reduce milk production. Documentation is lacking or conflicting. Generally, this drug should not be used in nursing mothers.
Manifestations: Acute overdose of atropine produces both peripheral and central signs and symptoms characterized by dilated pupils, difficultly swallowing, hot dry skin, vasodilation and urinary retention. A rash may appear on the face or upper trunk. Tachycardia and hypertension with arrhythmias, anxiety, delirium, hallucinations, hyperactivity convulsions, marked dryness of the mouth, photophobia, raised body temperature, leucocytosis, nausea, vomiting and restlessness also occur. In severe overdose, CNS depression, circulatory collapse and hypotension may be followed by coma, skeletal muscle paralysis and death from respiratory and circulatory failure.
In addition to tachycardia, cardiac manifestations may include ECG abnormalities (e.g., ventricular arrhythmias, extrasystoles resulting from enhanced re-entrant excitation secondary to reduced conduction velocity). Widening of the QRS complex, prolongation of the QT interval and ST segment depression may also be seen. There is considerable variation in susceptibility to atropine; recovery has occurred even after 1 g, whereas deaths have been reported from doses of 100 mg or less for adults and 10 mg in children.
Treatment: Symptomatic treatment should be instigated to ensure an adequate airway in maintained, fluids are replaced and body temperature is lowered using cold packs and tepid sponging. Artificial respiration with oxygen may be necessary and urinary catheterization may be required. Hypoxia and acidosis should be corrected and sodium bicarbonate may be given even if acidosis is not present. If photophobia occurs, the patient may be kept in a dark room. risk of central depression occurring late in the course of atropine poisoning contraindicates large doses of sedative; phenothiazines should not be given since they may exacerbate antimuscarinic effects. Antiarrhythmics are not recommended if arrhythmias develop. The use of physostigmine as an antidote for atropine poisoning is controversial due to the potential for physostigmine to produce severe adverse effects, eg. seizures, asystole. The use of physostigmine should be reserved for treatment of patients with extreme delirium of agitation, patients with repetitive seizures, patients with severe sinus tachycardia or supraventricular tachycardia or unresponsive extreme hyperthermia in patients who fail to respond to alternative therapy. Physostigmine should not be used to treat cardiac conduction defects or ventricular tachyarrhythmias. IV propranolol may be useful for treatment of supraventricular tachyarrhythmias unresponsive to physostigmine or where phystostigmine is contraindicated. Physostigmine should be used with caution in the presence of asthma, gangrene, cardiovascular disease or mechanical obstruction of the gastrointestinal or genitourinary tract. Physostigmine should be used in these circumstances only if a life-threatening emergency occurs. Dialysis is not effective in atropine overdose.