Alomide - Scientific Information
|Condition:||Conjunctivitis, Keratitis, Keratoconjunctivitis|
|Class:||Ophthalmic antihistamines and decongestants|
|Form:||Liquid solution, Eye drops (ophthalmic)|
|Ingredients:||lodoxamide, benzalkonium chloride 0.007% w/v as preservative, as well as mannitol, hydroxypropyl methylcellulose, sodium citrate, tyloxapol,citric acid, edetate disodium, purified water|
|Proper Name:||lodoxamide tromethamine|
|Chemical Name:||N, N'-(2-chloro-5-cyano-m-phenylene) dioxamic acid tromethamine salt.|
|Physical Form:||White to off white powder or crystals|
ALOMIDE is a sterile isotonic solution containing lodoxamide 0.1% w/v (as 0.178% w/v lodoxamide tromethamine), benzalkonium chloride 0.007% w/v as preservative, as well as mannitol, hydroxypropyl methylcellulose, sodium citrate, tyloxapol,citric acid, edetate disodium, and purified water.
ALOMIDE is supplied in natural plastic ophthalmic DROPTAINER* dispensers containing 10 mL or in natural plastic unit dose containers each containing 0.4 mL.
Store at room temperature (15°C – 25°C).
Information to patient
Your doctor has prescribed ALOMIDE solution for you to treat the symptoms of allergy (itching, discomfort, tearing etc) in your eyes. Regular use of this product is essential to obtain relief from your allergic symptoms.
- Remove your contact lenses before using ALOMIDE solution.
- Wait at least 15 minutes after using ALOMIDE solution before inserting your lenses.
- Do not touch the dropper tip to any surface to avoid contamination.
Put one drop into each eye, four times per day at regular intervals (about every 4 hours) while awake. It is necessary to use ALOMIDE solution regularly to obtain relief from your allergic eyes.
Lodoxamide, a mast cell stabilizer, inhibits the in vivo type I immediate hypersensitivity reaction in animals and man. Allergen-induced bronchospasms and reduced pulmonary function in monkeys are prevented with lodoxamide treatment. A cutaneous vascular permeability increase associated with reagin or IgE and antigen mediated reactions in rats, monkeys and humans are inhibited with lodoxamide therapy. A similar vascular reaction in the palpebral conjunctiva of rats has been inhibited with topical ocular administration of lodoxamide. Therefore, it is anticipated that lodoxamide will be useful in the treatment of ocular diseases where type I immediate hypersensitivity plays a major role in the pathogenesis.
In vitro studies have demonstrated the ability of lodoxamide to stabilize mast cells and prevent the antigen specific induced release of histamine. In addition, lodoxamide prevents the release of other mast cell inflammatory mediators (i.e. SRS-A, slow reacting substances of anaphylaxis, also known as the peptido-leukotrienes) and appears to inhibit eosinophil chemotaxis. Lodoxamide inhibits histamine release in vitro by preventing the movement of calcium into the mast cell after stimulation.
In a multi-centre double-masked study (9 centres), 0.1% lodoxamide was more effective than 2% sodium cromoglycate in the treatment of the signs and symptoms of conjunctivitides of an allergic nature (vernal, giant papillary, atopic/allergic types). ocular signs and symptoms were generally controlled in fourteen to twenty-one days of therapy (q.i.d. dosing), and improvement continued with further therapy. Based upon physician and patient judgements, a therapeutic effect was observed within seven days of the initiation of treatment. In a similar single centre study, 0.1% lodoxamide was judged more effective than 2% sodium cromoglycate, but the difference was not statistically significant.
Lodoxamide has no intrinsic vasoconstrictor, antihistaminic, cyclooxygenase inhibition or other anti-inflammatory activity.
The disposition of 14C-lodoxamide was studied in six healthy adult volunteers receiving a 3 mg (50 μCi) oral dose of lodoxamide. Urinary excretion was the major route of elimination. The elimination half-life of 14C-lodoxamide was 8.5 hours in urine. In a study conducted in twelve healthy adult volunteers, topical administration of ALOMIDE, one drop in each eye four times per day for ten days, did not result in any measurable lodoxamide plasma levels at a detection limit of 2.5 ng/ml.
|Species/Route||LD50 (mg/kg)||Signs of Toxicity|
|Mouse, i.p closed eyes.||4,000 - 5,000||Depression, laboured breathing, partially|
|Mouse, i .p||3634||Depression, prostration, coma.|
|Rat, i.p||5.019||Altered gait, thirstiness, prostration, coma.|
|Rat, i.p.||>5,000||Slight amount of blood tinged abdominal fluid.|
|Species/Route||Daily Dosage (mg/kg)||Signs of Toxicity|
|0, 500, 1600, 5,000||None|
|10, 30, 100||None|
|0, 500, 1600, 5,000||None|
1, 3 months
|10, 30, 100||Decreases in erythrocyte
parameters in females
|10, 30, 100||Dose related decrease in body
weights in males. Small renal
calculi (relationship questionable).
|10, 30, 100||No overt effects|
|10, 30, 100||Comparable to controls.|
|Ames (Salmonella) (3 strains)
with and without activation
|Negative up to
|Ames (Salmonella) (2 additional strains)
with and without metabolic activation
Reproduction and Teratology
|Rat, p.o Segment l||30 - Male
10, 30 - Female
|No adverse effects.|
|Rat, p.o Segment l||10, 30, 100||Possible decrease in proportion of
|Rat, p.o Segment 2||10, 30||No adverse effects.|
|Rat, p.o Segment 2||10, 30, 100||Not teratogenic.|
|Rat, p.o Segment 3||10, 30||No adverse effects.|
|Rat, p.o Segment 3||10, 30, 100||No adverse effects.|
|Rabbit, p.o Segment 2||10, 30, 100||No adverse effects.|
|Rabbit, p.o Segment 2||10, 30||No adverse effects.|
|Species||Dosage (mg/kg)||Signs of Toxicity|
both eyes BID
|Reddening of eyelids-
comparable to control
Every 30 mins.
for 12 doses
В В В
and discharge; minimal
Comparable to controls.
1, 3 months
right eye; QID
congestion and discharge.
Sporadic and transient instances of
superficial corneal epithelium,
irregularities (not dose related) in product
and vehicle with HPMC.
|0.25, 0.5, 1%None
right eye; QID