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Atropine (ophthalmic): Drug information

Atropine (ophthalmic): Drug information
(For additional information see "Atropine (ophthalmic): Patient drug information" and see "Atropine (ophthalmic): Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Isopto Atropine
Brand Names: Canada
  • Alcon Atropine;
  • Minims Atropine Sulfate
Pharmacologic Category
  • Anticholinergic Agent, Ophthalmic;
  • Ophthalmic Agent, Mydriatic
Dosing: Adult
Amblyopia, healthy eye penalization

Amblyopia, healthy eye penalization: Ophthalmic: Solution: Instill 1 drop in the conjunctiva of the sound eye (nonamblyopic eye) once daily on weekends or daily (Repka 2004).

Mydriasis/cycloplegia

Mydriasis/cycloplegia: Ophthalmic:

Solution: Instill 1 drop in the conjunctiva 40 minutes prior to intended maximal dilation time; may repeat up to twice daily as needed.

Ointment: Apply a small amount in the conjunctival sac 1 to 2 times daily.

Palliative care of respiratory secretions

Palliative care of respiratory secretions (off-label use): Sublingual (using 1% ophthalmic solution): Initial: 1 to 2 drops every 2 to 4 hours; usual dose range: 2 to 4 drops every 2 to 4 hours (Protus 2013).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Use caution; dosage adjustment may be required.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Pediatric

(For additional information see "Atropine (ophthalmic): Pediatric drug information")

Amblyopia, healthy eye penalization

Amblyopia, healthy eye penalization: Solution (1%):

Infants ≥3 months and Children <3 years: Ophthalmic: Instill 1 drop once daily to healthy eye

Children ≥3 years and Adolescents: Ophthalmic: Solution (1%): Instill 1 drop once daily to healthy eye; dose may be repeated up to twice daily if needed

Mydriasis, cycloplegia

Mydriasis, cycloplegia:

Solution (1%):

Infants ≥3 months and Children <3 years: Ophthalmic: Instill 1 drop 40 minutes prior to intended maximal dilation time; maximum dose: 1 drop per eye per day

Children ≥3 years and Adolescents: Ophthalmic: Instill 1 drop 40 minutes prior to intended maximal dilation time; may repeat up to twice daily as needed

Ointment: Infants, Children, and Adolescents: Ophthalmic: Apply a small amount in the conjunctival sac 1 to 2 times daily

Inflammatory conditions of iris and uveal tract

Infla mmatory conditions of iris and uveal tract: Infants, Children, and Adolescents: Ophthalmic: Ointment: Apply a small amount in the conjunctival sac 1 to 2 times daily

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Ointment, Ophthalmic, as sulfate:

Generic: 1% (3.5 g)

Ointment, Ophthalmic, as sulfate [preservative free]:

Generic: 1% (3.5 g)

Solution, Ophthalmic, as sulfate:

Isopto Atropine: 1% (5 mL) [contains benzalkonium chloride]

Generic: 1% (2 mL, 5 mL, 15 mL)

Generic Equivalent Available: US

Yes

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic:

Generic: 1% (0.3 mL, 0.5 mL)

Solution, Ophthalmic, as sulfate:

Alcon Atropine: 1% (5 mL) [contains benzalkonium chloride]

Generic: 1% (5 mL)

Administration: Adult

Ophthalmic: For topical ophthalmic use only. Wash hands before and after use. Avoid touching tip of applicator to eye or other surfaces. Finger pressure should be applied to lacrimal sac for 1 to 3 minutes after instillation to decrease risk of absorption and systemic reactions.

Administration: Pediatric

Ophthalmic: Wash hands prior to use.

Solution: Instill solution into conjunctival sac of affected eye(s); Avoid contact of bottle tip with eye or skin; apply gentle pressure to lacrimal sac during and immediately following instillation (1 minute) or instruct patient to gently close eyelid after administration, to decrease systemic absorption of ophthalmic drops (Urtti 1993; Zimmerman 1984)

Ointment: Place a small amount of ointment into the conjunctival sac of the affected eye(s)

Use: Labeled Indications

Amblyopia, healthy eye penalization (solution only): Penalization of the healthy eye in the treatment of amblyopia.

Mydriasis, Cycloplegia: Produce mydriasis and/or cycloplegia.

Use: Off-Label: Adult

Terminal respiratory secretions

Medication Safety Issues
International issues:

Atropt [Australia and New Zealand] may be confused with Azopt brand name for brinzolamide [US, Canada, and multiple international markets]

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Severity and frequency of adverse reactions are dose related.

Frequency not defined:

Cardiovascular: Flushing, hypotension, increased blood pressure, tachycardia

Dermatologic: Contact dermatitis, xeroderma

Gastrointestinal: Xerostomia

Nervous system: Delirium, irritability, restlessness

Ophthalmic: Blurred vision, decreased lacrimation, decreased visual acuity (reversible, healthy eye) (Scheiman 2008), eye irritation, eye pain, eyelid edema, papillary conjunctivitis, photophobia, stinging of eyes, superficial keratitis

Respiratory: Dry throat, respiratory depression

Miscellaneous: Fever

Contraindications

Hypersensitivity to atropine or any component of the formulation; primary glaucoma or tendency toward angle-closure glaucoma (narrowing or closure of the anterior chamber angle).

Documentation of allergenic cross-reactivity for anticholinergic agents is limited; however, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Warnings/Precautions

Concerns related to adverse effects:

• Elevated BP: May occur due to systemic absorption following conjunctival instillation.

• Photophobia/blurred vision: May last up to 2 weeks due to pupil unresponsiveness and cycloplegia.

Disease-related concerns:

• Brain damage: Use with caution in patients with brain damage; these patients are particularly susceptible to CNS disturbances and cardiopulmonary and GI toxicity from systemic absorption of atropine.

• Down syndrome: Use with caution in patients with Down syndrome; these patients are particularly susceptible to CNS disturbances and cardiopulmonary and GI toxicity from systemic absorption of atropine.

• Spastic paralysis: Use with caution in patients with spastic paralysis; these patients are particularly susceptible to CNS disturbances and cardiopulmonary and GI toxicity from systemic absorption of atropine.

Dosage form specific issues:

• Benzalkonium chloride: Some products may contain benzalkonium chloride which may be absorbed by soft contact lenses; avoid contact use during treatment.

Other warnings/precautions:

• Appropriate use: To avoid precipitating angle closure glaucoma, an estimation of the depth of the anterior chamber angle should be made prior to use.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy

Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination

CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider therapy modification

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination

Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy

Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Atropine (Ophthalmic). Risk X: Avoid combination

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy

Opioid Agonists: Anticholinergic Agents may enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Risk C: Monitor therapy

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Risk X: Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Pregnancy Considerations

Atropine crosses the placenta following systemic maternal use (Shutt 1979). Atropine is systemically available following ophthalmic administration. If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Samples 1988).

Breastfeeding Considerations

It is not known if atropine is excreted in breast milk following ophthalmic administration; however, systemic absorption occurs. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Monitoring Parameters

Reduction in visual acuity; local and systemic toxicity. Gonioscopy exam to assess ocular drainage angle.

Mechanism of Action

Blocks the action of acetylcholine that induces mydriasis and allows the radial pupillary dilator muscle to contract resulting in dilation of the pupil; induces cycloplegia by paralysis of the ciliary muscle. In amblyopia, use temporarily blurs sight in the healthy eye and encourages the use of the amblyopic eye.

Pharmacokinetics

Onset of action: Ophthalmic solution: Within minutes; maximum effect: within hours (3 hours [Matta 2013]).

Duration: Multiple days; visual acuity near normal at 4 days postadministration (Matta 2013).

Absorption: Well absorbed from all dosage forms.

Metabolism: Hepatic via enzymatic hydrolysis.

Bioavailability: Ophthalmic solution: 64% ± 29% (range: 19% to 95%).

Half-life elimination: 2.5 ± 0.8 hours.

Time to peak: 28 ± 27 minutes (range: 3 to 60 minutes).

Excretion: Urine (13% to 50% as unchanged drug and metabolites).

Pricing: US

Ointment (Atropine Sulfate Ophthalmic)

1% (per gram): $6.00 - $10.67

Solution (Atropine Sulfate Ophthalmic)

1% (per mL): $10.51 - $11.68

Solution (Isopto Atropine Ophthalmic)

1% (per mL): $12.18

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Antol (TW);
  • Apitropin (AE, BH, JO, KW);
  • Atoren-P (TH);
  • Atro Grin (MX);
  • Atro Ofteno Al (MX);
  • Atropin (SE);
  • Atropin Vision (BG);
  • Atropin-POS (CZ);
  • Atropine Alcon (FR);
  • Atropisol (EG);
  • Atropocil (PT);
  • Atropt (AU, NZ);
  • Atroptal (PH);
  • Atrosol (SG, TR);
  • Atrospan (IL);
  • Colircusi Atropina (ES);
  • Colircusi Atropine (PT, SA);
  • Di Shan (CN);
  • Isopto Atropin (SE);
  • Isopto Atropina (CO, PE, PY, UY);
  • Isopto Atropine (BE, EG, KR, LK, MY, PH, PK, TH);
  • Isopto-Atropine (ET, ZA, ZW);
  • Isotic Cycloma (ID);
  • Itropin (BD);
  • Klonatropina (AR);
  • Minims Atropine (GB);
  • Minims Atropine Sulfate (MT);
  • Mydripine (BD);
  • Ocutropine (KR);
  • Riatropine (AE, QA)


For country code abbreviations (show table)
  1. Atropine ointment [prescribing information]. Tampa, FL Bausch & Lomb; June 2017.
  2. Atropine solution [prescribing information]. Lake Forest, IL: Akorn; July 2014.
  3. Heisler M, Hamilton G, Abbott A, Chengalaram A, Koceja T, Gerkin R. Randomized double-blind trial of sublingual atropine vs. placebo for the management of death rattle. J Pain Symptom Manage. 2013;45(1):14-22. [PubMed 22795904]
  4. Isopto (atropine) [prescribing information]. Fort Worth, TX: Alcon; December 2016.
  5. Matta N, Silbert DI. Effects of atropine on the accommodative system: parameters to consider in its use for penalization treatment of amblyopia. Binocul Vis Strabolog Q Simms Romano. 2013;28(1):39-44. [PubMed 23521035]
  6. Nelson WE, Behrman RE, Kliegman RM, et al, eds. Nelson Textbook of Pediatrics. 15th ed. Philadelphia, PA: WB Saunders Company; 1996.
  7. Protus BM, Grauer PA, Kimbrel JM. Evaluation of atropine 1% ophthalmic solution administered sublingually for the management of terminal respiratory secretions. Am J Hosp Palliat Care. 2013;30(4):388-392. doi: 10.1177/1049909112453641. [PubMed 22833553]
  8. Repka MX, Cotter SA, Beck RW, et al; Pediatric Eye Disease Investigator Group. A randomized trial of atropine regimens for treatment of moderate amblyopia in children. Ophthalmology. 2004;111(11):2076-85. doi:10.1016/j.ophtha.2004.04.032 [PubMed 15522375]
  9. Repka MX, Kraker RT, Holmes JM, et al; Pediatric Eye Disease Investigator Group. Atropine vs patching for treatment of moderate amblyopia: follow-up at 15 years of age of a randomized clinical trial. JAMA Ophthalmol. 2014;132(7):799-805. [PubMed 24789375]
  10. Samples JR, Meyer SM. Use of ophthalmic medications in pregnant and nursing women. Am J Ophthalmol. 1988;106(5):616-623. [PubMed 2903673]
  11. Scheiman MM, Hertle RW, Kraker RT, et al; Pediatric Eye Disease Investigator Group. Patching vs atropine to treat amblyopia in children aged 7 to 12 years: a randomized trial. Arch Ophthalmol. 2008;126(12):1634-1642. [PubMed 19064841]
  12. Shinjo T, Okada M. Atropine eyedrops for death rattle in a terminal cancer patient. J Palliat Med. 2013;16(2):212-213. [PubMed 22747099]
  13. Shutt LE, Bowes JB. Atropine and hyoscine. Anaesthesia. 1979;34(5):476-490. Review. [PubMed 382907]
  14. Urtti A, Salminen L. Minimizing systemic absorption of topically administered ophthalmic drugs. Surv Ophthalmol. 1993;37(6):435-456. [PubMed 8100087]
  15. Zimmerman TJ, Kooner KS, Kandarakis AS, Ziegler LP. Improving the therapeutic index of topically applied ocular drugs. Arch Ophthalmol. 1984;102(4):551-553. [PubMed 6704011]
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