logo

Ophthalmic Ocular Decongestants,  Anti-allergy Products

Ophthalmic agents - Home Page
alcaftadine - LASTACAFT ® azelastine (Optivar ®)
bepotastine besilate -BEPREVE™ Cromolyn sodium (Crolom ®)
emedastine (Emadine ®) Epinastine (Elestat ®)
Ketotifen Fumarate (Zaditor ®) Levocabastine (Livostin ®)
Lodoxamide tromethamine (Alomide ®) Naphazoline (Naphcon, Vasocon ®)
Naphcon-A ® (naphazoline + pheniramine) nedocromil (Alocril ®)
Olopatadine (Patanol ®) pemirolast (Alamast ®)

alcaftadine - LASTACAFT ®  top of page

CLINICAL PHARMACOLOGY
Mechanism of Action
Alcaftadine is an H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.

INDICATIONS AND USAGE
LASTACAFT® is an H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis.
------------------------------------
Contamination of Tip and Solution
To minimize 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. Keep bottle tightly closed when not in use.

Contact Lens Use
Patients should be advised not to wear a contact lens if their eye is red. LASTACAFT® should not be used to treat contact lens-related irritation.

LASTACAFT® should not be instilled while wearing contact lenses. Remove contact lenses prior to instillation of LASTACAFT®. The preservative in LASTACAFT®, benzalkonium chloride, may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of LASTACAFT®.

Topical Ophthalmic Use Only
LASTACAFT® is for topical ophthalmic use only.

DOSAGE AND ADMINISTRATION
Instill one drop in each eye once daily.

DOSAGE FORMS AND STRENGTHS
Topical ophthalmic solution containing alcaftadine, 0.25% (2.5 mg/mL).

azelastine (Optivar ®)  top of page

CLINICAL PHARMACOLOGY:
Azelastine hydrochloride is a relatively selective histamine H1 antagonist and an inhibitor of the release of histamine and other mediators from cells (e.g. mast cells) involved in the allergic response. Based on in-vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (e.g. leukotrienes and PAF) has been demonstrated with azelastine hydrochloride. Decreased chemotaxis and activation of eosinophils has also been demonstrated.

INDICATIONS AND USAGE:
OPTIVAR® is indicated for the treatment of itching of the eye associated with allergic conjunctivitis.


CONTRAINDICATIONS:
OPTIVAR® is contraindicated in persons with known or suspected hypersensitivity to any of its components.

ADMINISTRATION
: one drop instilled into each affected eye twice a day.

[Supplied: 0.05% ophthalmic solution]

bepotastine besilate -BEPREVE™ top of page

DESCRIPTION
BEPREVE™ (bepotastine besilate ophthalmic solution) 1.5% is a sterile, topically administered drug for ophthalmic use. Each mL of BEPREVE™ contains 15 mg bepotastine besilate.

Bepotastine besilate is designated chemically as (+) -4-[[(S)-p-chloro-alpha -2-pyridylbenzyl]oxy]-1-piperidine butyric acid monobenzenesulfonate.

INDICATIONS AND USAGE
BEPREVE™ is a histamine H1 receptor antagonist indicated for the treatment of itching associated with allergic conjunctivitis.

DOSAGE AND ADMINISTRATION
Instill one drop into the affected eye(s) twice a day (BID).

HOW SUPPLIED
Solution containing bepotastine besilate, 1.5%.

Cromolyn sodium (Crolom ®) top of page

Clinical Pharmacology
In vitro and in vivo animal studies have shown that cromolyn sodium inhibits the degranulation of sensitized mast cells which occurs after exposure to specific antigens. Cromolyn sodium acts by inhibiting the release of histamine and SRS-A (slow-reacting substance of anaphylaxis) from the mast cell.
Another activity demonstrated in vitro is the capacity of cromolyn sodium to inhibit the degranulation of nonsensitized rat mast cells by phospholipase A and the subsequent release of chemical mediators. Another study showed that cromolyn sodium did not inhibit the enzymatic activity of released phospholipase A on its specific substrate.

Cromolyn sodium has no intrinsic vasoconstrictor, antihistamine, or anti-inflammatory activity.

Cromolyn sodium is poorly absorbed. When multiple doses of cromolyn sodium ophthalmic solution are instilled into normal rabbit eyes, less than 0.07% of the administered dose of cromolyn sodium is absorbed into the systemic circulation (presumably by way of the eye, nasal passages, buccal cavity and gastrointestinal tract). Trace amounts (less than 0.01%) of the cromolyn sodium dose penetrate into the aqueous humor and clearance from this chamber is virtually complete within 24 hours after treatment is stopped.

In normal volunteers, analysis of drug excretion indicates that approximately 0.03% of cromolyn sodium is absorbed following administration to the eye.

Indications and Usage
Cromolyn sodium ophthalmic solution is indicated in the treatment of vernal keratoconjunctivitis, vernal conjunctivitis, and vernal keratitis.

Contraindications
Cromolyn sodium ophthalmic solution is contraindicated in those patients who have shown hypersensitivity to cromolyn sodium or to any of the other ingredients.

Dosing:
The dose for adults and children is 1 or 2 drops in each eye 4 to 6 times a day at regular intervals. One drop contains approximately 1.6 mg cromolyn sodium.
Patients should be advised that the effect of cromolyn sodium ophthalmic solution therapy is dependent upon its administration at regular intervals, as directed.

Supplied:  CrolomTM (Cromolyn Sodium Ophthalmic Solution USP, 4%)

emedastine (Emadine ®) top of page

Emedastine is a selective H1-receptor antagonist with antiallergic and antiasthmatic properties.
 Dosing:  Allergic conjunctivitis: 1 drop 0.05% ophthalmic solution in affected EYE(s) up to four times daily.
 [Supplied: 0.05% solution] .

Epinastine  (Elestat ®)  top of page

H1 Blocker. Allergic conjunctivitis: Instill 1 drop into each eye twice daily. Continue throughout period of exposure, even in the absence of symptoms.

Supplied: Oph solution: 0.05% (5 ml).

Ketotifen Fumarate Ophthalmic Solution 0.025% (Zaditor ®) top of page

Indications: Temporary prevention of itching of the eye caused by allergic conjunctivitis. Noncompetitive histamine antagonist (H-1 receptor) and mast cell stabilizer.

Dosing
The recommended dose is one drop in the affected eye(s) every 8 to 12 hours.

Supplied: Oph solution: 0.025% (5 ml).

Levocabastine (Livostin ®)  top of page

Indications: temporary relief of the signs and symptoms of seasonal allergic conjunctivitis.

Dosing
: The usual dose is one drop instilled in affected eyes four times per day.  SHAKE WELL BEFORE USING.

Supplied:
[suspension: 0.05%]

Lodoxamide tromethamine (Alomide ®)  top of page

Indications: treatment of the ocular disorders referred to by the terms vernal keratoconjunctivitis, vernal conjunctivitis, and vernal keratitis.

Dosing: The dose for adults and children greater than two years of age is one to two drops in each affected eye four times daily for up to 3 months.

Supplied: [soln: 0.1%]

Naphazoline (Naphcon, Vasocon ®)  top of page

Dosing: 1 drop every 3 to 4 hours as needed up to 4 times daily.

Naphcon-A ® (naphazoline + pheniramine): top of page

 Dosing: 1-2 drops 2 to 4 times daily as needed.

nedocromil (Alocril ®)  top of page

Mast cell stabilizer. Indication: allergic conjunctivitis.
Dosing: Instill one or two drops in each eye twice a day.

[Supplied: 2% ophthalmic soln]

Olopatadine (Patanol ®) top of page

Indications: treatment of the signs and symptoms of allergic conjunctivitis.

Dosing: The recommended dose is one drop in each affected eye two times per day at an interval of 6 to 8 hours.

Supplied: [0.1% soln]

pemirolast (Alamast ®)  top of page

Mast cell stabilizer. Indication: allergic conjunctivitis.
Dosing: Instill one to two drops in each affected eye four times daily. Symptomatic response to therapy (decreased itching) may be evident within a few days, but frequently requires longer treatment (up to four weeks).

Supplied: ophthalmic solution 0.1%
top of page

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.
more Career Center image description
Medical Calculators - A thru Z
Lab Values - A thru Z