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Atropine (Ophthalmic)

Generic name: atropine ophthalmic

Brand names: Isopto Atropine, Atropisol, Ocu-Tropine, Atrosulf-1, Atropine-Care

Dosage Forms

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

Ointment, Ophthalmic, as sulfate:

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)

Pharmacology

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.

Pharmacokinetics/Pharmacodynamics

Absorption

Well absorbed from all dosage forms

Metabolism

Hepatic via enzymatic hydrolysis

Excretion

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

Onset of Action

Ophthalmic solution: Within minutes; maximum effect: within hours

Time to Peak

28 ± 27 minutes (range: 3 to 60 minutes)

Duration of Action

Multiple days

Half-Life Elimination

2.5 ± 0.8 hours

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

Terminal respiratory secretionsc

Data from case reports and a retrospective chart review of palliative care patients indicate that sublingual administration of ophthalmic atropine may provide subjective reductions in noisy respiratory tract secretions, commonly referred to as “death rattle” Protus 2013, Shinjo 2013. The results of a randomized controlled trial failed to demonstrate a significant benefit after single-dose administration (2 drops) compared to placebo Heisler 2013. The quick onset of action and ease of sublingual atropine administration compared to alternative anticholinergic agents may make sublingual atropine an acceptable option in end-of-life care.

Contraindications

Hypersensitivity to atropine or any component of the formulation; primary glaucoma or tendency toward narrow anterior chamber angle glaucoma (ointment only).

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.

Dosage and Administration

Dosing: Adult

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

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.

Terminal 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)

Dosing: Pediatric

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:

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

Administration

Ophthalmic: 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.

Storage

Solution: Store at 2°C to 25°C (36°F to 77°F).

Ointment: Store at 15°C to 25°C (59°F to 77°F).

Drug Interactions

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Atropine (Ophthalmic). 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. 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. Monitor therapy

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

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

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

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

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. 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. Consider therapy modification

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

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

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

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

Adverse Reactions

Frequency not defined. Severity and frequency of adverse reactions are dose related.

Cardiovascular: Delirium, flushing, hypotension, increased blood pressure

Central nervous system: Irritability, restlessness

Dermatologic: Contact dermatitis, xeroderma

Gastrointestinal: Xerostomia

Ophthalmic: Blurred vision, decreased lacrimation, eye irritation, eyelid edema, eye pain, papillary conjunctivitis, photophobia, stinging of eyes, superficial keratitis

Respiratory: Dry throat, respiratory depression

Warnings/Precautions

Concerns related to adverse effects:

  • Elevated blood pressure: 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.

Concurrent drug therapy issues:

  • Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Dosage form specific issues:

  • Benzalkonium chloride: Some products may contain benzalkonium chloride which may be absorbed by soft contact lenses.

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.

Pregnancy

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).

Patient Education

What is this drug used for?

  • It is used to widen the pupil before an eye exam or eye surgery.
  • It is used to treat eye swelling.
  • It is used to treat lazy eye (amblyopia).

Frequently reported side effects of this drug

  • Blurred vision
  • Fatigue
  • Stinging

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

  • Severe headache
  • Dizziness
  • Passing out
  • Vision changes
  • Fast heartbeat
  • Abnormal heartbeat
  • Flushing
  • Irritability
  • Agitation
  • Dry mouth
  • Dry skin
  • Severe eye irritation
  • Eye pain
  • Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Source: Wolters Kluwer Health. Last updated January 25, 2020.