ATROPINE SULFATE

Atropine Sulfate Injection, USP is a sterile solution of atropine sulfate in Water for Injection. Each mL contains Atropine Sulfate 0.4 mg; Sodium Chloride 9 mg; Benzyl Alcohol 9 mg; Water for Injection qs; pH may be adjusted with Sulfuric Acid if necessary. pH 3.0-6.5. Atropine Sulfate Injection, USP may be given intramuscularly, intravenously or subcutaneously. Atropine is a white crystalline alkaloid which may be extracted from belladonna root or may be produced synthetically. It is used as atropine sulfate because this compound has much greater solubility. Atropine sulfate is an anticholinergic drug. The empirical formula of atropine sulfate is (C 17 H 23 NO 3 ) 2 •H 2 SO 4 •H 2 O. The structural formula is: structural formula

Atropine sulfate is given parenterally as a preanesthetic medication to decrease salivation and bronchial secretions. It is useful in pylorospasm and other spastic conditions of the gastrointestinal tract. For ureteral and biliary colic, atropine sulfate given with morphine may be indicated. Atropine sulfate is indicated for relaxation of the upper gastrointestinal tract and colon during hypotonic radiography. Atropine is used as an antidote for pilocarpine, physostigmine, isoflurophate, choline esters, certain species of aminata and in poisoning by the organic phosphate cholinesterase inhibitors found in certain insecticides and by chemical warfare “nerve gases”. Large doses relieve the muscarine-like symptoms and some of the central nervous system manifestations.

The usual dose of atropine sulfate is 0.4 to 0.6 mg. Suggested dosages for pediatric patients are as follows: 7 - 16 lbs. – 0.1 mg 40 - 65 lbs. – 0.3 mg 17 - 24 lbs. – 0.15 mg 65 - 90 lbs. – 0.4 mg 24 - 40 lbs. – 0.2 mg Over 90 lbs. – 0.4 to 0.6 mg Table of Dosage Equivalents Atropine Sulfate Solution (mL required) mg required 1 mg per mL 0.4 mg per mL 1 1 0.80 0.80 0.60 0.60 0.50 0.50 0.40 0.40 1 0.30 0.30 0.75 0.25 0.25 0.63 0.20 0.20 0.50 0.18 0.18 0.45 0.15 0.15 0.38 0.12 0.12 0.30 0.10 0.10 0.25 These doses may be exceeded in certain cases. For hypotonic radiography of the gastrointestinal tract, the usual adult dose is 1 mg intramuscularly. Adults suspected of contact with organic phosporous insecticides of the parathion type should be given atropine sulfate 0.8 mg intramuscularly. If an atropine effect is not apparent within 30 minutes or if definite symptoms of the poisoning occur (nausea, vomiting, diarrhea, pupillary constriction, pulmonary edema, fasciculations of eyelids and tongue, jerky ocular movements and excessive sweating, salivation and bronchial secretion), atropine sulfate 2 mg should be given intramuscularly at hourly intervals until signs of atropinization are observed. Up to 2 or 3 times of this dose (4 to 6 mg) may be required in severe cases. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

Conditions at which inhibition of postganglionic cholinergic nerves are undesirable, such as glaucoma and tachycardia. Also contraindicated in asthma, because the parenteral dose which might relieve asthma would have an excessive drying effect upon mucous plugs in the bronchi. Prostatic hypertrophy, while not a contraindication, requires special attention to signs of urinary retention.

Individual tolerance varies greatly, but these systemic doses are likely to produce the following effects: 0.5 mg - Slight dryness of nose and mouth, bradycardia. 1 mg - Greater dryness of nose and mouth, with thirst; slowing, then acceleration of heart; slight mydriasis. 2 mg - Very dry mouth, tachycardia, with palpitation, mydriasis, slight blurring of near vision. 5 mg - Increase in the above symptoms plus disturbance of speech, difficulty in swallowing, headache, hot, dry skin, restlessness with asthenia. 10 mg and over - Above symptoms to extreme degree, plus ataxia, excitement, disorentation, hallucinations, delirium and coma. 65 mg - May be fatal. A scarlatiniform rash may occur. Atropine may produce fever, particularly in children, through inhibition of heat loss by evaporation. Although large doses of atropine may cause an alarming condition, recovery is usual.

Atropine, by slowing gastric emptying and gastrointestinal mobility, may interfere with the absorption of other medications. The effect of atropine on dryness of the mouth may be increased if it is given with other drugs that have anticholinergic action.