AK-Pentolate

Name: AK-Pentolate

AK-Pentolate Drug Class

AK-Pentolate is part of the drug class:

  • Opthalmic anticholinergics

AK-Pentolate™ Cyclopentolate Hydrochloride Ophthalmic Solution, USP -Sterile

Rx only

AK-Pentolate - Clinical Pharmacology

This anticholinergic preparation blocks the responses of the sphincter muscle of the iris and the accommodative muscle of the ciliary body to cholinergic stimulation, producing pupillary dilation (mydriasis) and paralysis of accommodation (cycloplegia). It acts rapidly, but has a shorter duration than atropine. Maximal cycloplegia occurs within 25 to 75 minutes after instillation. Complete recovery of accommodation usually takes 6 to 24 hours. Complete recovery from mydriasis in some individuals may require several days. Heavily pigmented irides may require more doses than lightly pigmented irides.

Contraindications

AK-Pentolate™ (Cyclopentolate Hydrochloride Ophthalmic Solution) should not be used when untreated narrow-angle glaucoma, or untreated anatomically narrow angles are present, or if the patient is hypersensitive to any component of this preparation.

Warnings

For topical ophthalmic use only. Not for injection. This preparation may cause CNS disturbances. This is especially true in younger age groups, but may occur at any age, especially with the stronger solutions. Infants are especially prone to CNS and cardiopulmonary side effects from cyclopentolate. To minimize absorption, use only 1 drop of 0.5% cyclopentolate hydrochloride ophthalmic solution per eye, followed by pressure applied over the nasolacrimal sac for two to three minutes. Observe infants closely for at least 30 minutes.

Mydriatics may produce a transient elevation of intraocular pressure.

Precautions

General

The lacrimal sac should be compressed by digital pressure for two to three minutes after instillation to reduce excessive systemic absorption. Caution should be observed when considering use of this medication in the presence of Down's syndrome and in those predisposed to angle-closure glaucoma.

Information for Patients

Do not touch dropper tip to any surface, as this may contaminate the solution. A transient burning sensation may occur upon instillation. Patients should be advised not to drive or engage in other hazardous activities while pupils are dilated. Patients may experience sensitivity to light and should protect eyes in bright illumination during dilation. Parents should be warned not to get this preparation in their child's mouth and to wash their own hands and the child's hands following administration. Feeding intolerance may follow ophthalmic use of this product in infants. It is recommended that feeding be withheld for four (4) hours after examination.

Drug Interactions

Cyclopentolate may interfere with the ocular anti-hypertensive action of carbachol, pilocarpine, or ophthalmic cholinesterase inhibitors.

Carcinogenesis, Mutagenesis, and Impairment of Fertility

Studies in animals or humans have not been conducted to evaluate the carcinogenic potential of cyclopentolate.

Pregnancy

Pregnancy Category C

Animal reproduction studies have not been conducted with cyclopentolate. It is also not known whether cyclopentolate can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Cyclopentolate should be administered to a pregnant woman only if clearly needed.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when cyclopentolate hydrochloride is administered to a nursing woman.

Pediatric Use

Use of cyclopentolate has been associated with psychotic reactions and behavioral disturbances in pediatric patients. Increased susceptibility to cyclopentolate has been reported in infants, young children, and in children with spastic paralysis or brain damage. These disturbances include ataxia, incoherent speech, restlessness, hallucinations, hyperactivity, seizures, disorientation as to time and place, and failure to recognize people. Feeding intolerance may follow ophthalmic use of this product in infants. It is recommended that feeding be withheld for four (4) hours after examination. Observe infants closely for at least 30 minutes (see WARNINGS).

AK-Pentolate Dosage and Administration

Adults: Instill one or two drops of 1% or 2% solution in the eye which may be repeated in five to ten minutes if necessary. Complete recovery usually occurs in 24 hours. Complete recovery from mydriasis in some individuals may require several days. Children: Instill one or two drops of 1% or 2% solution in the eye which may be repeated five to ten minutes later by a second application of 1% solution if necessary.

Pregnancy & Lactation

Pregnancy Category: C

Lactation: Excretion in milk unknown; use with caution

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

Pharmacology

Onset: rapid; max effect not for 30 min

Excretion: urine

Mechanism of Action

Blocks action of acetylcholine resulting in relaxation of the cholinergically innervated iris sphincter muscle

Cholinergic stimulation of accommodative ciliary muscle of lens is also blocked

Anticholinergic effects of cyclopentolate in eye produce dilation of the pupil (mydriasis) and paralysis of accommodation (cycloplegia)

Pharmacokinetics

Onset of action: 25-75 min (cycloplegia); 30-60 min (mydriasis)

Duration: < 24hr

Absorption: Minimal systemic

Breastfeeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

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