Optivar

Keep all appointments with your doctor.

Do not let anyone else use your medication. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

Azelastine is an antihistamine that reduces the natural chemical histamine in the body. Histamine can produce symptoms of itching or watery eyes.

Azelastine ophthalmic (for the eyes) is used to treat itchy eyes caused by allergies (hay fever).

Azelastine ophthalmic may also be used for purposes not listed in this medication guide.

You should not use this medication if you are allergic to azelastine.

Do not allow the dropper tip to touch any surface, including the eyes or hands. If the dropper becomes contaminated it could cause an infection in your eye, which can lead to vision loss or serious damage to the eye.

Do not use this medication while wearing contact lenses. Azelastine ophthalmic may contain a preservative that can discolor soft contact lenses. Wait at least 15 minutes after using azelastine before putting your contact lenses in.

Do not wear contact lenses while your eyes are red or irritated. Azelastine ophthalmic should not be used to treat minor contact lens irritation.

Stop using azelastine ophthalmic and call your doctor if you have severe eye pain, trouble breathing, or severe burning, stinging, itching, or redness in your eyes.

You should not use this medication if you are allergic to azelastine.

Do not wear contact lenses while your eyes are red or irritated. Azelastine ophthalmic should not be used to treat minor contact lens irritation.

FDA pregnancy category C. It is not known whether azelastine ophthalmic will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

It is not known whether azelastine ophthalmic passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

Do not give this medication to a child younger than 3 years old.

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.

Pharmacokinetics And Metabolism

Absorption of azelastine following ocular administration was relatively low. A study in symptomatic patients receiving one drop of OPTIVAR® in each eye two to four times a day (0.06 to 0.12 mg azelastine hydrochloride) demonstrated plasma concentrations of azelastine hydrochloride to generally be between 0.02 and 0.25 ng/mL after 56 days of treatment. Three of nineteen patients had quantifiable amounts of N-desmethylazelastine that ranged from 0.25–0.87 ng/mL at Day 56.

Based on intravenous and oral administration, the elimination half-life, steady-state volume of distribution and plasma clearance were 22 hours, 14.5 L/kg and 0.5 L/h/kg, respectively. Approximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system. In-vitro studies in human plasma indicate that the plasma protein binding of azelastine and N-desmethylazelastine are approximately 88% and 97%, respectively.

Clinical Trials

In a conjunctival antigen challenge study, OPTIVAR® was more effective than its vehicle in preventing itching associated with allergic conjunctivitis. OPTIVAR® had a rapid (within 3 minutes) onset of effect and a duration of effect of approximately 8 hours for the prevention of itching.

In environmental studies, adult and pediatric patients with seasonal allergic conjunctivitis were treated with OPTIVAR® for two to eight weeks. In these studies, OPTIVAR® was more effective than its vehicle in relieving itching associated with allergic conjunctivitis.

Optivar is a prescription medication used to treat allergy symptoms of the eyes. This medication belongs to a group of drugs called antihistamines. It works by preventing histamine release and by blocking histamine at receptors. Histamine is a chemical of the immune system that causes allergy symptoms.

Optivar also comes in eye drop form to be applied into the affected eye(s) twice a day.

Common side effects of Optivar include burning, irritation, and stinging of the eyes. Optivar can cause temporary blurring of vision. Do not operate machinery or drive until you know Optivar will affect you. 

Optivar is a prescription medication used to treat allergy symptoms of the eyes.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

• Meda Pharmaceuticals, Inc.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Studies on this medicine have been done only in adult patients, and there is no specific information comparing use of azelastine in children under the age of 3 years with use in other age groups.

Geriatric

This medicine has been tested and has not been shown to cause different side effects or problems in older people than it does in younger adults.

Pregnancy

Breast Feeding

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.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Bupropion
• Donepezil

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Cimetidine

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

• It is used to ease allergy signs in the eye.

• If you have an allergy to azelastine or any other part of Optivar (azelastine (ophthalmic)).
• If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Change in eyesight, eye pain, or very bad eye irritation.

Optivar® is indicated for the treatment of itching of the eye associated with allergic conjunctivitis.

Information for Patients:

To prevent contaminating the dropper tip and solution, care should be taken not to touch any surface, the eyelids, or surrounding areas with the dropper tip of the bottle. Keep bottle tightly closed when not in use. This product is sterile when packaged.

Patients should be advised not to wear a contact lens if their eye is red. Optivar® should not be used to treat contact lens related irritation. The preservative in Optivar®, benzalkonium chloride, may be absorbed by soft contact lenses. Patients who wear soft contact lenses and whose eyes are not red, should be instructed to wait at least ten minutes after instilling Optivar® before they insert their contact lenses.

Carcinogenesis, Mutagenesis, Impairment of Fertility:

Azelastine hydrochloride administered orally for 24 months was not carcinogenic in rats and mice at doses up to 30 mg/kg/day and 25 mg/kg/day, respectively. Based on a 30 µL drop size, these doses were approximately 25,000 and 21,000 times higher than the maximum recommended ocular human use level of 0.001 mg/kg/day for a 50 kg adult.

Azelastine hydrochloride showed no genotoxic effects in the Ames test, DNA repair test, mouse lymphoma forward mutation assay, mouse micronucleus test, or chromosomal aberration test in rat bone marrow. Reproduction and fertility studies in rats showed no effects on male or female fertility at oral doses of up to 25,000 times the maximum recommended ocular human use level. At 68.6 mg/kg/day (57,000 times the maximum recommended ocular human use level), the duration of the estrous cycle was prolonged and copulatory activity and the number of pregnancies were decreased. The numbers of corpora lutea and implantations were decreased; however, the implantation ratio was not affected.

Pregnancy:

Teratogenic Effects: Pregnancy Category C. Azelastine hydrochloride has been shown to be embryotoxic, fetotoxic, and teratogenic (external and skeletal abnormalities) in mice at an oral dose of 68.6 mg/kg/day (57,000 times the recommended ocular human use level). At an oral dose of 30 mg/kg/day (25,000 times the recommended ocular human use level), delayed ossification (undeveloped metacarpus) and the incidence of 14th rib were increased in rats. At 68.6 mg/kg/day (57,000 times the maximum recommended ocular human use level) azelastine hydrochloride caused resorption and fetotoxic effects in rats. The relevance to humans of these skeletal findings noted at only high drug exposure levels is unknown.

There are no adequate and well-controlled studies in pregnant women. Optivar® should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers:

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

Pediatric Use:

Safety and effectiveness in pediatric patients below the age of 3 have not been established.

Geriatric Use:

No overall differences in safety or effectiveness have been observed between elderly and younger adult patients.

Applies to azelastine ophthalmic: ophthalmic solution

Along with its needed effects, azelastine ophthalmic (the active ingredient contained in Optivar) may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking azelastine ophthalmic:

• Cough
• difficulty breathing
• noisy breathing
• shortness of breath
• tightness in chest
• wheezing

Some side effects of azelastine ophthalmic may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Bitter taste in mouth
• headaches
• temporary eye burning or stinging

• Burning, dry or itching eyes
• blurred vision, temporary
• chills
• diarrhea
• eye discharge or excessive tearing
• fever
• general feeling of discomfort or illness
• hoarseness or other voice changes
• itching skin
• joint pain
• loss of appetite
• muscle aches and pains
• nausea
• redness, pain, swelling of eye, eyelid, or inner lining of eyelid
• runny nose
• shivering
• sneezing
• sore throat
• stuffy nose
• sweating
• tender, swollen glands in neck
• trouble in swallowing
• trouble sleeping
• unusual tiredness or weakness
• vomiting