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Loxat Plus

Al-Tinez Visions Limited
9, Olowogbowo Str off Obokun Str by Coker Rd, Ilupeju, Lagos
Email: altinezvisions@gmail.com
Tel: 01-7418609, 08296588658, 0708900917

Brand Name

Loxat Plus

Manufacturer

HANLIM PHARM. CO., LTD. 1007, YUBANG-DONG, CHEOIN-GU, YONGIN-SI, GYEONGGI-DO, KOREA http://www.hanlim.com.

Therapeutic Class

Antiglaucoma preparations and Miotics

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Drop (NRN:   ): Each mL contains: Active: Latanoprost 50 µg (0.005%), Timolol maleate 6.83 mg (0.5%), Preservative: 10% Benzalkonium chloride solution 2.0 mg (as benzalkonium chloride 0.2 mg).

Pack size: In a bottle containing 2.5 mL.

Pharmacology

[Appearance] Colorless and transparent solution in white plastic bottle.

Indications

LAXAT PLUS is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma, chronic closed-angle glaucoma or ocular hypertension.

Contra-indications

Known hypersensitivity to lantanoprost, benzalkonium chloride or any other ingredients in this product.

Precautions/Warnings

Systemic effects
Like other topically applied ophthalmic agents. LAXAT PLUS may be absorbed systemically. Due to the beta-adrenergic component timol, the same types of cardiovascular and pulmonary adverse reactions as seen with systemic beta-blockers may also mask the signs of hyperthyroidism.

Anaphylactic reactions
While taking beta-blockers, patients with a history of atopy or a history of severe anaphylactic reaction to a variety of allergens may be unresponsive to the usual doses of adrenaline used to treat anaphylactic reactions.

Concomitant therapy
Timolol may interact with other drugs; see “Interaction with other medicine products and other forms of interaction”.
The effect on intraocular pressure or the known effects of systemic beta-blockade may be potentiated when LAXAT PLUS is given to patients already receiving an oral beta-blocking agent. The use of two local beta-blockers or two local prostaglandins is not recommended.

Ocular effects
Latanoprost may gradually change the eye colour by increasing the amount of brown pigment in the iris. Similar to experience with latanoprost eye drops, increased iris pigmentation was seen in 16 – 20% 0f all patients treated with LAXAT PLUS for up to one year (based on photographs). This effect has predominantly been seen in patients with mixed coloured irides, i.e., green-brown or blue/ grey-brown, and is due to increased melanin content in the stromal melanocytes of the iris.

Typically the brown pigmentation around the pupil spreads concentrically towards the periphery in affected eyes, but the entire iris or parts of it may become more brownish. In patients with homogeneously blue, grey, green or brown eyes, the changes has only rarely been seen during two years of treatments in clinical trials with latanoprost.

The change in iris colour occurs slowly and may not be noticeable for several months to years and it has not been associated with any symptom or pathological changes.

No further increase in brown iris pigment has been observed after discontinuation of treatment, but the resultant colour change may be permanent.

Neither naevi nor freckles of the iris have been affected by treatment.

Accumulation of pigment in the trabecular meshwork or elsewhere in the anterior chamber has been observed but patients should be examined regularly and depending on the clinical situation, treatment may be stopped if increased iris pigmentation ensues.

Before treatment is instituted, patient should be informed of the possibility of a change in eye colour. Unilateral treatment can result in permanent heterochromia.

There is no documented experience with latanoprost in inflammatory, neovascular, chronic angle closure or congenital glaucoma, in open angle glaucoma of pseudophakic patients and in pigmentary glaucoma.

Latanoprost has no or little effect on the pupil but there is no documented experience in acute attacks of closed angle glaucoma. It is recommended, therefore, that LAXAT PLUS should be used with caution in these conditions until more experience is obtained.

Macular oedema, including cystoid macular oedema has been reported during treatment with latanoprost. These reports have mainly occurred in aphakic patients, in pseudophakic patients with a torn posterior lens capsule, or in patients with known risk factors for macular oedema. LAXAT PLUS should be used with caution in these patients.

Choroidal detachment has been reported with administration of aqueous suppressant therapy (e.g. timolol, acetazolamide) after filtration procedures.

Use of contact lenses
LAXAT PLUS contains benzalkonium chloride which is commonly used as a preservative in ophthalmic products.

Benzalkonium chloride has been reported to cause punctate keratopathy and/or toxic ulcerative keratopathy may cause eye irritation and is known to discolour soft contact lenses.

Close monitoring is required with frequent or prolonged use of LAXAT PLUS in dry eye patients or in conditions where the cornea is compromised.

Contact lenses may absorb benzalkonium chloride and these should be removed before applying LAXAT PLUS but may be reinserted after 15 minutes.

[Preclinical Safety Data]
The ocular and systemic safety profile of the individual components is well established. No adverse ocular or systemic effects were seen in rabbits treated topically with fixed combination or with concomitantly administered latanoprost and timolol ophthalmic solutions.

Safety pharmacology, genotoxicity and carcinogenicity studies with each of the components revealed no special hazards for humans.

Latanoprost did not affect corneal wound healing in the rabbit eye, whereas timolol inhibited the process in the rabbit and the monkey eye when administered more frequently than once a day.

For latanoprost, no effects on male and female fertility in rats and no teratogenic potential in rats and rabbits have been established. No embryotoxicity was observed in rats after intravenous doses of up to 250 micrograms/kg/day. 

Latanoprost, however, caused embryofetal toxicity, characterized by increased incidence of late resorption and abortion and by reduced foetal weight in rabbits at intravenous doses of 5 micrograms/kg/day (approximately 100 times the clinical dose) and above.

Timolol showed no effects on male and female fertility in rats or teratogenic potential in mice, rats and rabbits.

Interactions

[Interaction with other Medicinal Products and Other forms of Interaction]

Special medicinal product interaction studies have not been performed with LAXAT PLUS.

There have been reports of paradoxical elevations in intraocular pressure following the concomitant ophthalmic administration of two prostaglandin analogues. Therefore, the use of two or more prostaglandins, prostaglandin analogues or prostaglandin derivatives is not recommended.

Mydriasis has occasionally been reported when timolol was given with epinephrine.

There are a potential for additive effects resulting in hypotension and/or marked bradycardia when eye drops with timolol are administered concomitantly with oral calcium channel blockers, guanethidine or beta-blocking agents, antiarrhythmics, digitalis glycosides or parasympathomimetics.

The hypertensive reaction to sudden withdrawal of clonidine can be potentiated when taking beta- blockers.

Beta-blockers may increase the hypoglycaemic effect of antidiabetic agents. Beta-blockers can mask the signs and symptoms of hypoglycaemia.

Adverse Effects

For latanoprost, the majority of adverse events relate to the ocular system. In data from the extension phase of the pivotal trials, 16 – 20% of patients developed increased iris pigmentation which may be permanent. In an open 5 year latanoprost safety study, 33% of patients developed pigmentation. Other ocular adverse events are generally transient and occur on dose administration.

For timolol, the most serious adverse events are systemic in nature including bradycardia, arrhythmia, congestive heart failure, bronchospasm and allergic reactions. Treatment related adverse events seen in clinical trials are listed below.

Adverse events are categorized by frequency as follows: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10, 0000, <1/ 1000) and very rare (<1/10,000).

Nervous System Disorders:
Uncommon: Headache

Eye Disorders:
Very common: Increased iris pigmentation.
Uncommon: Eye hyperaemia, conjunctivitis, Vision blurred, Lacrimation increased, Blepharitis, corneal disorders.

Skin and Subcutaneous Tissue Disorders:
Uncommon: Skin rash, Pruritus.
Additional adverse events have been reported specific to the use of the individual components of LAXAT PLUS Eye Drops in either in clinical studies, spontaneous reports or in the available literature.

For latanoprost, these are:

Nervous System Disorders: Dizziness.

Eye Disorders:
Eyelash and vellus hair changes (increased length, thickness, pigmentation and number), punctate epithelial erosions, periorbital oedema, iritis/ Uveitis, macular oedema (in aphakic, pseudophakic patients with torn posterior lens capsules or in patients with known risk factors for macular oedema), dry eye, keratitis, corneal oedema and erosions, misdirected eyelashes sometimes resulting in eye irritation and iris cyst.

Cardiac Disorders:
Aggrevation of angina in patients with pre-existing disease palpitations.
Respiratory, Thoracic and Mediastinal Disorders.
Asthma, Asthma aggrevation, Dysponea.

Skin and Subcutaneous Tissue Disorders:
Darkening of palpebral skin.
Musculoskeletal, Connective Tissue and Bone Disorders:
Joint pain, Muscle pain.

General disorders and administration Site Conditions:
Chest pain

For timolol, these are:

Immune System Disorders:
Signs and symptoms of systemic allergic reactions including angioedema, urticarial and localized and generalized rash.

Psychiatric Disorders:
Depression, Memory loss, Decreased libido, Insomnia, Nightmares.

Nervous System Disorders:
Dizziness, Paraethesia, Cerebral ischemia, Cerebravascular accident, Increase in signs and symptoms of myasthenia gravis, Syncope.

Eye Disorders:
Signs and symptoms of ocular irritation including keratitis decreased corneal sensitivity and dry eyes. Visual disturbances including refractive changes (due to withdrawal of miotic therapy in some cases). Diplopia, Ptosis, Choroidal detachment (following filtration surgery).

Ear and Labyrinth Disorders:
Tinnitus

Cardiac Disorders:
Palpitation, Arrhythmia, Bradycardia, Cardiac arrest, Heart block, Congestive heart failure.

Vascular Disorders:
Hypotension, Raynaud’s phenomenon, cold hands and feet.

Respiratory, Thoracic and Mediastinal Disorders: bronchospasm (predominantly in patients with pre-existing bronchospastic disease). Dyspnoea, Cough.

Gastrointestinal Disorders:
Nausea, Diarrhoea, Dyspepsia, Dry mouth.

Skin and Subcutaneous Tissue Disorders:
Alopecia, Psoriasiform rash or exacerbation of psoriasis.

General Disorders and administration site conditions:
Asthenia/fatigue, Chest pain, Oedema.

Dosage & Administration

The recommended dosage is one drop (1.5 µg) in the affected eye(s) once in the evening.

The dosage of LAXAT PLUS should not exceed once daily since it has been shown that more frequent administration may decrease the intraocular pressure starts approximately 3 to 4 hours after administration and the maximum effect is reached after 8 to 12 hours.

LAXAT PLUS may be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure. If more than one topical ophthalmic drug is being used, the drugs should be administered at least five (5) minutes apart.

[Overdosage]

No data are available in humans with regards to overdose with this drug.

Symptoms of systemic timolol overdose are: bradycardia, hypotension, bronchospasm and cardiac arrest. If such symptoms occur the treatment should be symptomatic and supportive. Studies have shown that timolol does not dialyse readily.

Apart from ocular irritation and conjunctival hyperaemia no other ocular or systemic side effects are known if latanoprost is overdosed.

If latanoprost is accidentally ingested orally the following information may be useful: Treatment: Gastric lavage if needed.

Symptomatic treatment. Latanoprost is extensively metabolized during the first pass through the liver. Intravenous infusion of 3 micrograms/kg in healthy volunteers induced no symptoms but a dose of 5.5 -10 micrograms/kg caused nausea, abdominal pain, dizziness, fatigue, hot flushes and sweating. These events were mild to moderate in severity and resolved without treatment within 4 hours after terminating the infusion.

[Pregnancy and Lactation]

PREGNANCY

Latanoprost:
There are no adequate data from the use of latanoprost in pregnant women. Studies in animals have shown reproductive toxicity. The potential risk for humans is unknown.

Timolol:
Well controlled epidemiological studies with systemic use of beta-blockers did not indicate malformative effects, but some pharmacological effects such as bradycardia have already been observed in fetuses or neonates.
Consequently LAXAT PLUS should not be used during pregnancy.

LACTATION

Timolol is excreted into breast milk. Latanoprost and its metabolites may pass into breast milk. LAXAT PLUS should therefore not be used in women who are breast-feeding.

[Use in Children and Adolescents]
Safety and effectiveness in children and adolescents has not been established.

Storage/Handling Recommendations

Store in a refrigerator (2oC – 8oC).

Opened bottle: Do not store above 25oC. Keep the bottle in the outer Carton. After Opening of container: 4 weeks.

Review Date

2016-05-10 10:04:10