CYCLOPENTOLATE HCL (Generic for CYCLOGYL)

General Administration Information
For storage information, see the specific product information within the How Supplied section.

Route-Specific Administration

Ophthalmic Administration
-Wash hands before and after use. Tilt the head back slightly and pull the lower eyelid down with the index finger to form a pouch. Instill a single drop at a time. Wipe excess fluid off the cheek immediately. To limit systemic absorption, apply finger pressure on the lacrimal sac for 2-3 minutes after administration.
-Do not touch dropper tip to any surface to prevent contamination.
-If more than one topical ophthalmic drug product is being used, the drugs should be administered at least 5 minutes apart.
-To avoid contamination or the spread of infection, do not use dropper for more than one person.
-In neonates and infants, hold feeds for 4 hours because feeding intolerance may occur after administration.

Ocular adverse reactions associated with cyclopentolate include ocular pain (burning, stinging), transient increases in intraocular pressure (ocular hypertension), ocular irritation, punctate keratitis, blurred vision, hyperemia, synechiae, conjunctivitis, and photophobia.

Anticholinergic effects of cyclopentolate include skin rash (unspecified), sinus tachycardia, vasodilation (hypotension), flushing, urinary retention, drowsiness, hyperpyrexia (fever), xerostomia, and decreased secretion in sweat glands, pharynx, bronchi, and nasal passages. Severe toxicity includes coma, medullary paralysis, and death.. After topical application to the eye, applying pressure to the nasolacrimal sac for 2 to 4 minutes will help minimize absorption. This can reduce systemic absorption by up to 40%.

Gastrointestinal and digestive adverse reactions have developed in pediatric patients receiving ophthalmic cyclopentolate. Abdominal distention has been reported in neonates and infants. Neonates receiving cyclopentolate may experience feeding difficulties on the day they receive the mydriatic due to inhibition of duodenal motor activity and a delay in gastric emptying. Feeds should be held for 4 hours after examination. In 2 black neonates with heavily pigmented irises, atropine-like GI toxicity occurred after the ocular administration of cyclopentolate 1%. The neonates each received one drop in each eye repeated twice at 5 minute intervals for a total of 6 drops. Additionally, they received phenylephrine 10% eye drops. Gastrointestinal symptoms included vomiting, abdominal distension, and ileus. In both neonates, the systemic concentrations of cyclopentolate supported the clinical impression of cyclopentolate intoxication.

Cyclopentolate 2% may cause behavioral and CNS disturbances, including dysarthria (incoherent speech), impaired cognition (disorientation), ataxia, hallucinations, hyperkinesis, psychosis, and seizures. CNS effects occur more frequently in children and infants than in adults. These reactions are more common than the anticholinergic effects of cyclopentolate. A 4.5 year old boy was given one drop of 2% cyclopentolate in each eye at 15 minute intervals for a total dose of 6 drops. After the last dose, he experienced several CNS adverse events including hallucination, incoherent babbling, hyperactivity alternating with somnolence, confusion, and inability to recognize family members. The acute psychosis resolved over 7 hours; however, tachycardia persisted for approximately 36 hours.

Contact urticaria has been reported after cyclopentolate administration.

Cyclopentolate is contraindicated for use in patients who have experienced a hypersensitivity reaction to the drug or any component of the formulation.

Cyclopentolate is contraindicated for use in patients with closed-angle glaucoma and in patients with anatomical narrow angles.

Neonates, infants, and children are at higher risk for experiencing systemic adverse events after ophthalmic cyclopentolate administration compared to older patients. Neonates and infants are especially susceptible to CNS and cardiopulmonary effects of cyclopentolate. Feeding intolerance may also occur; hold feeds for 4 hours after administration. Observe infants closely for at least 30 minutes after ophthalmic instillation of cyclopentolate. In addition, there is a risk of precipitating psychotic reactions in children; this risk is greatest with the 2% solution. To minimize systemic absorption, apply pressure to the lacrimal sac during and for 2-4 minutes after administration.

Use cautiously in those with Down syndrome, brain-damage (neurological disease), and lightly pigmented patients because they are more susceptible to the toxic effects of cyclopentolate.

Use cautiously in patients with seizures or a seizure disorder; grand mal seizures have occurred after topical application of cyclopentolate in children.

Cyclopentolate contains benzalkonium chloride, which may be absorbed by contact lenses. Users of soft contact lenses should not use cyclopentolate while wearing these lenses.

Description: Cyclopentolate is a cycloplegic, mydriatic ophthalmic agent with anticholinergic effects on the eye that are similar to atropine. It is used for cycloplegic refraction and for dilating the pupil for diagnostic purposes; it is particularly useful to enhance pupillary dilation for retinopathy of prematurity screening examination. Cyclopentolate is the most commonly used cycloplegic agent in children. Systemic adverse effects have been reported after ophthalmic administration, especially in infants and young children. The lowest strength and the lowest dose should be used in these patients. Cyclopentolate is approved in pediatric patients as young as infants.

For mydriasis induction and cycloplegia induction for ophthalmic diagnostic procedures:
NOTE: Maximal cycloplegia typically occurs 25 to 75 minutes after administration.
Ophthalmic dosage:
Neonates and Infants: 1 drop of the 0.5% solution into the eye(s). To minimize systemic absorption, apply pressure over the nasolacrimal sac during and for 2 to 4 minutes after administration. Observe infant closely for at least 30 minutes after administration. Hold feedings for 4 hours.
Children and Adolescents: Instill 1 or 2 drops of 0.5%, 1%, or 2% solution into the eye(s). Repeat in 5 to 10 minutes, if necessary, using the 0.5% or 1% solution. Individuals with heavily pigmented irises may require higher dosage strengths.

Maximum Dosage Limits:
-Neonates
1 drop/eye/day 0.5% solution.
-Infants
1 drop/eye/day 0.5% solution.
-Children
4 drops/eye/day 0.5% or 1% solution; 2 of the 4 drops may be with a 2% solution.
-Adolescents
4 drops/eye/day 0.5% or 1% solution; 2 of the 4 drops may be with a 2% solution.

Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

*non-FDA-approved indication

Monograph content under development

Mechanism of Action: Cyclopentolate blocks the action of acetylcholine to produce relaxation of the sphincter muscle of the iris resulting in dilation of the pupil (mydriasis). This agent has an anticholinergic effect similar to atropine. Paralysis of accommodation (cycloplegia) is produced by blocking cholinergic stimulation of the ciliary muscle of the lens.

Pharmacokinetics: Cyclopentolate is administered as a topical ophthalmic solution. It acts rapidly, and has a shorter duration than atropine. Maximal cycloplegia occurs within 25-75 minutes; complete recovery of accommodation takes approximately 6-24 hours.


-Special Populations
Pediatrics
Neonates, Infants, and Children
Approximately 80% of each drop passes through the nasolacrimal system and is available for rapid systemic absorption by the nasal mucosa; systemic absorption can be minimized by applying pressure to the lacrimal sac during and immediately after administration. To a much lesser extent, systemic absorption may also occur through the conjunctiva, the nasolacrimal duct, the oropharynx, the digestive system, and the skin (due to overflow from the conjunctival sac), especially in infants. Absorbed medications are much more concentrated in neonates and infants because their average blood volume is one twentieth that of an adult. Additionally, immaturity of metabolic enzymes during the neonatal period may prolong the half-life of the drug.