Atropine Sulfate eent

Pronunciation

Class: Mydriatics
ATC Class: S01FA01
VA Class: OP600
Chemical Name: Benzeneacetic acid, α-(hydroxymethyl)-, 8-methyl-8- azabicyclo-[3.2.1]oct-3-yl ester, endo-(±)-, sulfate (2:1) (salt), monohydrate
CAS Number: 5908-99-6
Brands: Atropine Care, Isopto Atropine

Introduction

Mydriatic and cycloplegic; naturally occurring tertiary amine antimuscarinic.104 a b

Uses for Atropine Sulfate

Ophthalmologic Examination

Used to produce mydriasis and cycloplegia for refraction (e.g., retina and optic disc examination, measurement of refractive error).104 a b However, because of long duration of action relative to that of other anticholinergic agents, atropine is seldom, if ever, used for cycloplegic refraction in adults.101

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In rare cases, ophthalmic atropine use may be necessary to achieve maximal cycloplegia in pediatric patients, but cyclopentolate is more frequently used.102 103

Ophthalmic Inflammation

Management of acute inflammatory conditions (e.g., iridocyclitis) of the iris and uveal tract (e.g., uveitis).104 a b

Amblyopia

Used for cycloplegic effects in the treatment of suppression amblyopia (lazy eye) to reduce the visual acuity of the unaffected eye below that of the amblyopic one and force fixation with the amblyopic eye.a 101

Excess Accommodation and Convergence

Used to treat patients with a functional excess of accommodation and convergence.a

Atropine Sulfate Dosage and Administration

General

  • Prior to initiation of therapy, estimate the depth of the angle of the anterior chamber to avoid induction of angle-closure glaucoma in susceptible patients.104 a b

Administration

Ophthalmic Administration

Apply topically to eye(s) as an ophthalmic ointment or solution.104 a

For topical ophthalmic use only.104 Not for injection.104

Following topical application, apply finger pressure on the lacrimal sac for 2–3 minutes to avoid excessive systemic absorption.104 a b

Avoid contamination of the solution or ointment container.104 a

Dosage

Available as atropine sulfate; dosage expressed in terms of the salt.104 b

In patients with heavily pigmented irides, higher dosages may be required.104

Pediatric Patients

Cycloplegic Refraction
Ophthalmic

1–2 drops of a 0.5% solution in the eye(s) twice daily has been used for 1–3 days before the procedure, but this preparation no longer is commercially available in the US.a No specific pediatric dosage recommendations for 1% ophthalmic solution.104 (See Pediatric Use under Cautions.)

Alternatively, apply 0.3 cm of a 1% ointment into the conjunctival sac 3 times daily for 1–3 days before the procedure.a (See Pediatric Use under Cautions.)

Inflammatory Conditions
Uveitis
Ophthalmic

1–2 drops of a 0.5% solution into the affected eye(s) up to 3 times daily has been used, but this preparation no longer is commercially available in the US.a No specific pediatric dosage recommendations for 1% ophthalmic solution.104

Alternatively, apply 0.3–0.5 cm of a 1% ointment into the conjunctival sac of the affected eye(s) 1–3 times daily.a

Adults

Mydriasis and Cycloplegia for Refraction
Ophthalmic

1 drop of a 1% solution in the eye(s) 1 hour before the procedure.a

Alternatively, apply 0.3–0.5 cm of a 1% ointment into the conjunctival sac 1–3 times daily.a b If ointment is used for refraction, apply several hours before procedure.a

Inflammatory Conditions
Uveitis
Ophthalmic

1–2 drops of a 1% solution into the affected eye(s) up to 4 times daily, or as directed by a clinician.104 Alternatively, apply 0.3–0.5 cm of a 1% ointment into the conjunctival sac of the affected eye(s) 1–3 times daily.a b

Special Populations

No special population dosage recommendations at this time.104 a b

Cautions for Atropine Sulfate

Contraindications

  • Known hypersensitivity to atropine or any ingredient in the formulation.104 a b

  • Pediatric patients who have previously had a severe systemic reaction to atropine.b

  • Known or suspected angle-closure (narrow-angle) glaucoma or tendency toward angle-closure glaucoma.104 a b

Warnings/Precautions

Warnings

Overdosage

Excessive use in children and patients with a history of susceptibility to belladonna alkaloids may produce systemic manifestations of atropine poisoning (e.g., flushing, skin dryness, rash in children, rapid and irregular pulse, fever, abdominal distention in infants, mental aberration, loss of neuromuscular coordination).104 b If systemic symptoms occur, discontinue the drug and initiate appropriate therapy.a b

Specific Populations

Pregnancy

Category C.104 b

Lactation

Not known whether atropine is distributed into milk.104 Caution when used in nursing women.104

Pediatric Use

Safety and efficacy of atropine sulfate 1% ophthalmic solution have not been established in pediatric patients.104

Use with extreme caution, if at all, in infants and small children, and in children with spastic paralysis or brain damage because of increased susceptibility to the systemic effects of the drug in these patients.104 a b

Coma and death have been reported in very young patients.104 b

Geriatric Use

No substantial differences in safety or efficacy relative to younger adults.104

Common Adverse Effects

Elevated IOP.a With prolonged administration, local irritation,104 a b hyperemia,104 a b edema,104 a b exudate,104 b follicular conjunctivitis,104 a b dermatitis.104 a b

Atropine Sulfate Pharmacokinetics

Absorption

Bioavailability

Following topical application to the eye, readily absorbed transconjunctivally.a

Onset

Following topical application to the eye, maximum mydriasis occurs in about 30–40 minutes, and maximum cycloplegia occurs after several hours.a

Duration

Mydriasis generally lasts about 7–12 days, and cycloplegia persists for up to 14 days or longer.a

Special Populations

Onset of effects may be slower and duration more prolonged in individuals with heavily pigmented irides.a (See Dosage under Dosage and Administration.)

Distribution

Extent

Not known whether atropine is distributed into milk after topical application to the eye.104

Stability

Storage

Ophthalmic

Ointment

Tightly closed containers at 15–30°C.b Protect from heat; do not freeze.a

Solution

Tight containers at 8–27°C,104 or as specified by manufacturer. Do not freeze.a

Actions

  • After topical application to the eye, blocks responses of the sphincter muscle of the iris and the accommodative ciliary muscle of the ciliary body to cholinergic stimulation.101 102 104 a b

  • Produces pupillary dilation (mydriasis) and paralysis of accommodation (cycloplegia).101 102 104 a b

  • Slower onset of mydriatic and cycloplegic action and more prolonged ocular effects than most other anticholinergic drugs.101 102 a

Advice to Patients

  • Advise patients not to drive or engage in hazardous activities while pupils are dilated.104 b

  • Advise patients that they may experience sensitivity to light and should protect eyes in bright illumination during dilation.104 b

  • Advise parents to prevent the child from getting the solution or ointment into his or her mouth and to wash their own hands and the child’s hands following administration.104 b

  • Importance of learning and adhering to proper administration techniques to avoid contamination of the product.104 a

  • Importance of applying finger pressure on the lacrimal sac of the eye for 2–3 minutes following topical administration.104 a b

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.104 a b

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.104 b

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Atropine Sulfate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Ointment

1%*

Atropine Sulfate Ophthalmic Ointment

Bausch & Lomb, Fougera

Solution

1%*

Atropine Care (with benzalkonium chloride)

Akorn

Atropine Sulfate Ophthalmic Solution (with benzalkonium chloride)

Bausch & Lomb, Falcon, Fougera

Isopto Atropine (with benzalkonium chloride)

Alcon

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Atropine Sulfate 1% Ointment (BAUSCH & LOMB): 4/$24.99 or 11/$55.97

Atropine Sulfate 1% Solution (BAUSCH & LOMB): 5/$23.99 or 15/$69.97

Atropine Sulfate 1% Solution (BAUSCH & LOMB): 15/$101.27 or 30/$168.75

Isopto Atropine 1% Solution (ALCON VISION): 5/$39.19 or 15/$93.62

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions July 1, 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

100. Merli GJ, Weitz H, Martin JH et al. Cardiac dysrhythmias associated with ophthalmic atropine. Arch Intern Med. 1986; 146:45-7. [IDIS 212286] [PubMed 3942464]

101. Zimmerman CF, Hogan RN, Le TD. Mydriatic and cycloplegic drugs. In: Zimmerman TJ, Kooner KS, Sharir M et al, eds. Textbook of ocular pharmacology. Philadelphia: Lippincott-Raven; 1997:787-9.

102. Ellis FD. Cycloplegic agents. In: Zimmerman TJ, Kooner KS, Sharir M et al, eds. Textbook of ocular pharmacology. Philadelphia: Lippincott-Raven; 1997:807-26.

103. American Academy of Ophthalmology Pediatric Ophthalmology/Strabismus Panel. Preferred practic pattern guidelines. Pediatric eye evaluations. San Francisco, CA: American Academy of Ophthalmology; 2007. Available from website. Accessed 2008 Apr 24.

104. Alcon Pharmaceuticals. Isopto Atropine (atropine sulfate) ophthalmic solution prescribing information. Fort Worth, TX; 2003 Aug.

a. AHFS Drug Information 2008. McEvoy GK, ed. Atropine sulfate. Bethesda, MD: American Society of Health-System Pharmacists; 2008: 2903–4 .

b. Bausch & Lomb Inc. Atropine Sulfate ophthalmic ointment prescribing information. Tampa, FL; Undated.

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