Isopto Homatropine: Indications, Dosage, Precautions, Adverse Effects
Россия
  • Россия
  • Украина

Isopto Homatropine - Product Information

Manufacture: Alcon
Country: United States
Condition: Pupillary Dilation
Class: Mydriatics
Form: Eye drops (ophthalmic)
Ingredients: Homatropine hydrobromide, Sodium chloride, Benzalkonium chloride, Polysorbate 80, Hypromellose, Sodium hydroxide/or hydrochloric acid (to adjust pH) and Purified water.

(Homatropine hydrobromide 2%) Eye Drops

Name of the Drug

Isopto Homatropine Eye Drops contain homatropine hydrobromide 2%. The chemical structure of homatropine hydrobromide is:

and enatiomer   ,   HBr 

Chemical Name: (1R,3R,5S)-8-methyl-8-azabicyclo-[3.2.1]oct-3-yl (2RS)-2-hydroxy-2-phenylacetate

CAS Number: 51-56-9

Description

Homatropine hydrobromide is a white, crystalline powder or colourless crystals, freely soluble in water, sparingly soluble in alcohol. It has a molecular weight of 356.3 and a melting point of 215 C (with decomposition).

Isopto Homatropine Eye Drops contain 20 mg/mL (2%) homatropine hydrobromide, together with hypromellose, sodium chloride, polysorbate 80 (in 2% only), sodium hydroxide and/or hydrochloric acid (to adjust pH) and purified water. The 2% strength is preserved with benzalkonium chloride (0.1 mg/mL).

Isopto Homatropine Eye Drops is a clear solution and is presented in a DROP-TAINER bottle.

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 dilatation (mydriasis) and paralysis of accommodation (cycloplegia).

Indications

A moderately long acting mydriatic and cycloplegic for cycloplegic refraction and in the treatment of inflammatory conditions of the uveal tract. For pre- and postoperative states when mydriasis is required.

Contraindications

Isopto Homatropine Eye Drops are contraindicated in persons with primary glaucoma or a tendency toward glaucoma, e.g. narrow anterior chamber angle; and in those persons showing hypersensitivity to any component of this preparation. Children less than 12 years are also contraindicated (see PRECAUTIONS).

Precautions

FOR TOPICAL USE ONLY - NOT FOR INJECTION.

Use with caution in patients, especially children, who have previously had a severe systemic reaction to atropine.

Risk-benefit should be considered when the following medical problems exist: keratoconus (homatropine may produce fixed dilated pupil); Down’s syndrome, children with brain damage and elderly (increased susceptibility). In infants and small children, use with extreme caution.

Isopto Homatropine Eye Drops may cause increased intraocular pressure (See Adverse Reactions). The possibility of undiagnosed glaucoma should be considered in some patients, such as elderly patients. To avoid inducing angle closure glaucoma, determine the intraocular pressure and an estimation of the depth of the angle of the anterior chamber should be made prior to initiation of therapy.

All atropine-like drugs have similar dose-dependent peripheral effects, including dryness of mucous membranes, reduced secretions, constipation, reduced bladder tone, and the risk of urinary retention especially in older men.

Isopto Homatropine Eye Drops-induced psychotic reactions and behavioural disturbances may occur in patients with increased susceptibility to anticholinergic drugs (See Adverse Reactions). Excessive topical use of this drug can potentially lead to systemic anticholinergic toxicity including ataxia and a confusional state characterized by delirium, agitation, and rarely coma. This state is more apt to occur in the paediatric and geriatric age groups.

Patients may experience sensitivity to light and should protect eyes in bright illumination.

Because of risk of provoking hyperthermia, use with caution in patients, especially children, who may be exposed to elevated environmental temperatures or who are febrile.

Nasolacrimal occlusion or gently closing the eyelid after administration is recommended. This may reduce the systemic absorption of medicinal products administered via the ocular route and result in a decrease in systemic adverse reactions.

No contact lenses should be worn under Isopto Homatropine treatment. This product contains benzalkonium chloride which may cause eye irritation and is known to discolour soft contact lenses.

Carcinogenicity/Mutagenicity, Impairment of Fertility

There have been no long-term studies done using homatropine hydrobromide in animals to evaluate carcinogenic potential. Studies have not been performed to evaluate the effects of topical ocular administration of homatropine on fertility.

Use in Pregnancy

CATEGORY B2

There are no or limited amount of data from the use of Isopto Homatropine Eye Drops in pregnant women. Animal reproduction studies have not been conducted with homatropine hydrobromide. Animal studies are insufficient with respect to reproductive toxicity. It is not known whether homatropine hydrobromide can cause foetal harm when administered to a pregnant woman or can affect reproductive capacity.

The Collaborative Perinatal Project (1977) monitored 50,282 mother child pairs, 26 of which used homatropine in the first trimester with no observed increased risk of congenital defects. For use of homatropine anytime during the pregnancy, 86 exposures (dose form not specified) were recorded, from which 3 malformations were recorded compared to 1.94 expected, a standardised relative risk of 1.55 (95% Confidence Interval 0.32-4.38). The association has not been confirmed.

Homatropine hydrobromide should not be given to a pregnant woman unless clearly needed.

Use in Lactation

It is not known if this drug is excreted in human milk. However, homatropine and other antimuscarinic agents have been shown to adversely affect lactation in preclinical and in clinical studies. Therefore, Isopto Homatropine Eye Drops should not be used during breast feeding.

Paediatric Use

Isopto Homatropine Eye Drops is contraindicated in children less than 12 years because of the risk of serious systemic side effects (See Contraindications, Adverse Events and Overdosage). When dosed in older children the lowest strength should be used.

Fair-skinned children with blue eyes may exhibit an increased response and/or increased susceptibility to adverse reactions.

Observe infants closely for at least 30 minutes following instillation.

Parents should be warned not to get this preparation in their children's mouth or cheeks and to wash their hands and the child's hands or cheeks following administration.

Effects on Ability to Drive and Use Machines

Homatropine may cause drowsiness, blurred vision and sensitivity to light. Patients receiving Isopto Homatropine Eye Drops should be advised not to drive or engage in other hazardous activities while pupils are dilated and until vision is clear.

Interactions with Other Medicines

The effects of Isopto Homatropine Eye Drops may be enhanced by concomitant use of other drugs having antimuscarinic properties, such as amantadine, some antihistamines, phenothiazine antipsychotics, and tricyclic antidepressants.

Instructions to Patients

Patient 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.

To avoid excessive systemic absorption, patients should be advised to occlude the nasolacrimal ducts for two to three minutes after instillation.

To prevent contaminating the dropper tip and solution, care should be taken not to touch the eyelids or surrounding areas with the dropper tip of the bottle. The bottle should be tightly closed when not in use.

Adverse Reactions

Ocular Effects

Common (≥ 1% < 10%):Transient stinging or burning upon instillation; increased sensitivity to light
Uncommon (≥ 0.1% < 1%):Eye irritation not present before therapy
Rare (≥ 0.01% < 0.1%):Local irritation with prolonged use characterized by follicular conjunctivitis, vascular congestion, edema, exudates, eczemetoid dermatitis.

Systemic Effects

Rare (≥ 0.01% < 0.1%):Thirst or dryness of mouth

Post Marketing Experience

The following adverse reactions have been described with the use of topical ophthalmic homatropine. Frequencies cannot be estimated from the available data. Within each System Organ Class adverse reactions are presented in order of decreasing seriousness.

Eye disorders

Conjunctivitis, photophobia, mydriasis (drug effect prolonged), eye pain, eye oedema, eye discharge, eye irritation, ocular hyperaemia

Psychiatric disorders

Confusional state

Nervous system disorders

Somnolence

Cardiac disorders

Heart rate increased

Description of selected adverse reactions

Prolonged use may produce local irritation characterized by conjunctivitis (follicular), ocular hyperaemia, eye oedema and eye discharge.

This drug produces reactions similar to those of other anticholinergic drugs. The central nervous system manifestations such as ataxia, incoherent speech, restlessness, hallucinations, hyperactivity, seizures, disorientation as to time and place, and failure to recognize people are possible. Other toxic manifestations of anticholinergic drugs are skin rash, abdominal distention in infants, unusual drowsiness, tachycardia, hyperpyrexia, vasodilation, urinary retention, diminished gastrointestinal motility, and decreased secretion in salivary and sweat glands, pharynx, bronchi and nasal passages. Severe reactions are manifested by hypotension with rapid progressive respiratory depression.

Symptoms of toxicity are usually transient (lasting a few hours), but may last up to 24 hours.

Mydriatics may increase intraocular pressure and provoke glaucoma attacks in patients predisposed to acute angle closure in particular geriatric patients (see Precautions).

Paediatric population

Use of topical ophthalmic anticholinergics has been associated with psychotic disorders and behaviour changes such as agitation and confusional state in paediatric patients. Central nervous system reactions manifest similar to those listed above.

Isopto Homatropine Eye Drops can cause hyperpyrexia in children.

Dosage and Administration

Single patient use only.

For refraction, instill one or two drops topically in the eye(s). May be repeated in five to ten minutes if necessary. For uveitis, instil one or two drops topically up to every three to four hours. Individuals with heavily pigmented irides may require larger doses.

See “Precautions: Instructions to Patients” for important information about avoiding systemic absorption and contamination.

Overdosage

As with other anticholinergics, systemic homatropine toxicity may occur following topical use, particularly in children. It is manifested by flushing and dryness of the skin (a rash may be present in children), blurred vision, a rapid and irregular pulse, hypertension, hyperpyrexia, abdominal distention in infants, convulsions, mental aberration (hallucinations) and loss of neuro-muscular coordination. In severe cases, central nervous system depression, circulatory and respiratory failure, paralytic ileus, confusion, psychoses, agitation, delusions, delirium, and paranoia may be encountered as well as tachycardia, dysrhythmias, hypertension, seizures, coma and death. Homatropine poisoning, although distressing, is rarely fatal even with large doses of homatropine, and is self-limited if the cause is recognised and the homatropine medication is discontinued. Treatment includes symptomatic and supportive measures including maintaining a patent airway and assisting respiration if needed. Treat hyperthemia, coma and seizure if they occur. In infants and children, the body surface must be kept moist. Treatment of severe anticholinergic poisoning should be supervised by physicians with adequate expertise.

In Australia, contact Poisons Information Centre on 13 11 26; in New Zealand call 0800 POISON or 0800 764 766 for advice on management.

Presentation

Eye Drops (clear solution), 20 mg/mL (2%), 15mL DROP-TAINER dispenser.

Storage

Store below 25  C.

Discard container 28 days after opening.

Poison Schedule

Prescription Only Medicine S4

Approved by TGA 28th July 2004

Revised 17th August 2010

Date of most recent amendment: 9 May 2013

Alcon Laboratories (Australia) Pty Ltd

25 Frenchs Forest Road East

FRENCHS FOREST NSW 2086

Registered trademark