Interferon alfa-2a Subcutaneous

in-ter-FEER-on AL-fa-2a

Subcutaneous routeKit

Alpha-interferons, including interferon alfa-2a, cause or aggravate fatal or life-threatening neuropsychiatric, autoimmune, ischemic, and infectious disorders. Patients should be monitored closely with periodic clinical and laboratory evaluations. Patients with persistently severe or worsening signs or symptoms of these conditions should be withdrawn from therapy. In many, but not all cases, these disorders resolve after stopping interferon alfa-2a therapy .

May cause or aggravate fatal or life-threatening neuropsychiatric, autoimmune, ischemic, and infectious disorders. Monitor closely with periodic clinical and laboratory evaluations. Discontinue therapy with persistently severe or worsening signs or symptoms of these conditions .

Commonly used brand name(s):

In the U.S.

• Roferon-A

Available Dosage Forms:

• Solution

Therapeutic Class: Immunological Agent

Pharmacologic Class: Interferon, Alfa (class)

Uses For interferon alfa-2a

Interferon alfa-2a is used to treat chronic hepatitis C and certain types of leukemia (such as hairy cell leukemia and Philadelphia chromosome positive chronic myelogenous leukemia [CML]). Interferons are substances naturally produced by cells in the body to help fight infections and tumors. Interferon alfa-2a is a synthetic (man-made) version of these substances.

interferon alfa-2a was available only with your doctor's prescription.

This product was withdrawn from the U.S. market by Roche on October 1, 2007. This action was not due to safety or efficacy concerns .

Before Using interferon alfa-2a

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 interferon alfa-2a, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to interferon alfa-2a 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

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of interferon alfa-2a in children with chronic myelogenous leukemia.

Appropriate studies have not been performed on the relationship of age to the effects of interferon alfa-2a in children with chronic hepatitis C and hairy cell leukemia. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of interferon alfa-2a in the elderly. However, elderly patients are more likely to have age-related kidney problems, which may require caution in patients receiving interferon alfa-2a.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

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

Using interferon alfa-2a 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.

• Autumn Crocus


• Captopril


• Colchicine


• Enalaprilat


• Enalapril Maleate

Using interferon alfa-2a 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.

• Theophylline

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.

Other Medical Problems

The presence of other medical problems may affect the use of interferon alfa-2a. Make sure you tell your doctor if you have any other medical problems, especially:

• Autoimmune disorders (e.g., systemic lupus erythematosus, psoriasis, Raynaud's phenomenon, rheumatoid arthritis, or vasculitis) or


• Bleeding problems or


• Bone marrow problems (e.g., aplastic anemia) or


• Breathing problems or other lung diseases or


• Depression, history of or


• Diabetes or


• Diabetic retinopathy (eye problem caused by diabetes) or


• Eye or vision problems or


• Heart attack, history of or


• Heart disease, or history of or


• Heart or blood vessel disease or


• Hyperglycemia (high blood sugar level) or


• Hypertriglyceridemia (high triglyceride levels in the blood) or


• Seizures, history of or


• Thyroid disease or


• Weakened immune system—Use with caution. May make these conditions worse.

• Autoimmune hepatitis (liver inflammation) or


• Liver disease, severe—Should not be used in patients with these conditions.

• Colitis (inflammation of the bowel) or


• Pancreatitis (inflammation of the pancreas)—Interferon alfa-2a should be stopped in patients with these conditions.

• Human immunodeficiency virus (HIV) infection or


• Liver or other organ transplant—It is not known if interferon alfa-2a will work in patients with these conditions.

• Kidney disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

Proper Use of interferon alfa-2a

A nurse or other trained health professional may give you interferon alfa-2a. interferon alfa-2a is given as a shot under your skin. You may be taught how to give interferon alfa-2a at home. Make sure you understand all of the instructions before giving yourself an injection. Do not use more medicine or use it more often than your doctor tells you to.

You will be shown the body areas where this shot can be given. Use a different body area each time you give yourself a shot. Keep track of where you give each shot to make sure you rotate body areas.

Each package of interferon alfa-2a contains a Medication Guide. Read the guide carefully and make sure you understand:

• How to prepare the injection.


• Proper use of disposable syringes.


• How to give the injection.


• How long the injection is stable.

If you have any questions about any of this, check with your doctor.

Use only the brand of interferon alfa-2a that your doctor prescribed. Different brands may not work the same way.

Use a new needle and syringe each time you inject your medicine.

Drink extra fluids so you will pass more urine while you are using interferon alfa-2a. This will keep your kidneys working well and help prevent kidney problems.

Dosing

The dose of interferon alfa-2a will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of interferon alfa-2a. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

Missed Dose

interferon alfa-2a needs to be given on a fixed schedule. If you miss a dose or forget to use your medicine, call your doctor or pharmacist for instructions.

Storage

Store in the refrigerator. Do not freeze.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Throw away used needles in a hard, closed container that the needles cannot poke through. Keep this container away from children and pets.

Precautions While Using interferon alfa-2a

It is very important that your doctor check your progress at regular visits to make sure that interferon alfa-2a is working properly. Blood tests may be needed to check for unwanted effects.

interferon alfa-2a contains benzyl alcohol which may cause serious reactions to newborn or premature infants. Discuss this with your doctor if you are concerned.

Interferon alfa-2a may cause some people to be agitated, irritable, or display other abnormal behaviors. It may also cause some people to have suicidal thoughts and tendencies or to become more depressed. If you, your child, or your caregiver notice any of these side effects, tell your doctor or your child's doctor right away.

Serious allergic reactions can occur with interferon alfa-2a. Check with your doctor right away if you have blistering, peeling, or loosening of the skin; fever or chills; hives or welts; red skin lesions; severe acne or skin rash; or sores or ulcers on the skin while you are using interferon alfa-2a.

Interferon alfa-2a can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. It can also lower the number of platelets, which are necessary for proper blood clotting. If this occurs, there are certain precautions you can take, especially when your blood count is low, to reduce the risk of infection or bleeding:

• If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.


• Check with your doctor immediately if you notice any unusual bleeding or bruising; black, tarry stools; blood in the urine or stools; or pinpoint red spots on your skin.


• Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.


• Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.


• Be careful not to cut yourself when you are using sharp objects such as a safety razor or fingernail or toenail cutters.


• Avoid contact sports or other situations where bruising or injury could occur.

Check with your doctor immediately if blurred vision, difficulty in reading, or any other change in vision occurs during or after treatment. Your doctor may want you to have your eyes checked by an ophthalmologist (eye doctor).

interferon alfa-2a may cause some people to become dizzy, drowsy, or less alert than they are normally. Make sure you know how you react to interferon alfa-2a before you drive, use machines, or do anything else that could be dangerous if you are dizzy or are not alert and not able to see well.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

interferon alfa-2a Side Effects

Along with its needed effects, a medicine 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:

More common

• Blurred vision


• burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings


• chest pain


• chills


• cough


• depression


• diarrhea


• discouragement


• dizziness


• dry skin


• fainting


• fast, slow, or irregular heartbeat


• feeling sad or empty


• fever or chills


• general feeling of discomfort or illness


• headache


• irritability


• itching


• joint pain


• lack of appetite


• loss of interest or pleasure


• muscle aches and pains


• nausea


• nervousness


• pounding in the ears


• rash


• runny nose


• shivering


• shortness of breath


• sneezing


• sore throat


• sweating


• thickening of bronchial secretions


• tightness in the chest


• tiredness


• trouble with concentrating


• trouble with sleeping


• troubled breathing


• unusual tiredness or weakness


• vomiting


• weight loss


• wheezing

Less common

• Back, leg, or stomach pains


• black, tarry stools


• bladder pain


• bleeding gums


• bloating


• bloody nose


• bloody or cloudy urine


• changes in skin color


• chest discomfort


• cold feeling


• collection of blood under the skin


• confusion


• constipation


• convulsions


• darkened urine


• deep, dark purple bruise


• difficult or labored breathing


• difficult, burning, or painful urination


• difficulty with breathing


• difficulty with moving


• dizziness, faintness, or lightheadedness when getting up from a lying or sitting position suddenly


• eye pain


• fear


• feeling cold


• feeling of constant movement of self or surroundings


• frequent urge to urinate


• general body swelling


• hair loss


• hoarseness or husky voice


• increased sweating


• indigestion


• itching, pain, redness, or swelling


• loss of bladder control


• lower back or side pain


• muscle cramps and stiffness


• muscle spasm or jerking of all extremities


• noisy breathing


• nosebleeds


• pain


• pain, swelling, or redness in the joints


• pain, tenderness, or swelling of the foot or leg


• pains in the stomach, side, or abdomen, possibly radiating to the back


• pale skin


• poor concentration


• redness, soreness, or itching skin


• sensation of spinning


• shaking


• sores, ulcers, or white spots on the lips or in the mouth


• sores, welting, or blisters


• stomach cramps


• stuffy nose


• sudden loss of consciousness


• swelling or inflammation of the mouth


• swollen or painful glands


• tenderness


• unusual drowsiness, dullness, tiredness, weakness, or feeling of sluggishness


• vomiting of blood or material that looks like coffee grounds


• watery or bloody diarrhea


• weakness in the arms or legs


• weight gain


• yellow eyes or skin

Rare

• Agitation


• bluish color of the fingernails, lips, skin, palms, or nail beds


• change in consciousness


• changes in the patterns and rhythms of speech


• coma


• dandruff


• decreased vision


• double vision


• drowsiness


• earache


• feeling of warmth


• generalized slowing of mental and physical activity


• inability to move the arms, legs, or facial muscles


• inability to speak


• lack of feeling or emotion


• light-colored stools


• loss of ability to use or understand speech or language


• loss of consciousness


• loss of memory


• oily skin


• pain or discomfort in the arms, jaw, back, or neck


• pain or tenderness around the eyes and cheekbones


• paleness or cold feeling in the fingertips and toes


• problems with memory


• problems with speech or speaking


• rapid, shallow breathing


• red, scaling, or crusted skin


• red, sore eyes


• redness of the face, neck, arms, and occasionally, upper chest


• restlessness


• seeing, hearing, or feeling things that are not there


• sensation of pins and needles


• shakiness and unsteady walk


• skin rash, encrusted, scaly, and oozing


• slow speech


• slurred speech


• stabbing pain


• stiff neck


• sudden sweating


• tingling or pain in the fingers or toes when exposed to cold


• trouble sitting still


• uncaring


• unsteadiness, trembling, or other problems with muscle control or coordination


• upper right abdominal pain

Incidence not known

• Blindness


• change in ability to see colors, especially blue or yellow


• coughing that sometimes produces a pink frothy sputum


• difficult, fast, or noisy breathing, sometimes with wheezing


• heavier menstrual periods


• migraine headache

Some side effects 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:

More common

• Bleeding, blistering, burning, coldness, discoloration of the skin, feeling of pressure, hives, infection, inflammation, itching, lumps, numbness, pain, rash, redness, scarring, soreness, stinging, swelling, tenderness, tingling, ulceration, or warmth at the injection site


• hair loss or thinning of the hair


• lack or loss of strength


• sleeplessness


• unable to sleep

Less common

• Abnormal ejaculation


• change in taste or bad unusual or unpleasant (after) taste


• decreased interest in sexual intercourse


• decreased sexual performance or desire


• excess air or gas in the stomach or intestines


• full feeling


• inability to have or keep an erection


• irregular menstrual period


• loss in sexual ability, desire, drive, or performance


• passing gas

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

The information contained in the Thomson Healthcare (Micromedex) products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Healthcare does not assume any responsibility or risk for your use of the Thomson Healthcare products.

More interferon alfa-2a Subcutaneous resources

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• Chronic Myelogenous Leukemia
• Hairy Cell Leukemia
• Hepatitis C
• Kaposi's Sarcoma
• Lymphoma
• Renal Cell Carcinoma

Indium Oxyquinoline

Dosage Form: Solution

For the Radiolabeling of Autologous Leukocytes

Rx ONLY

Diagnostic—For intravenous use

For single dose, single use only

Indium Oxyquinoline Description

Indium In 111 oxyquinoline (oxine) is a diagnostic radiopharmaceutical intended for radiolabeling autologous leukocytes. It is supplied as a sterile, non-pyrogenic, isotonic aqueous solution with a pH range of 6.5 to 7.5. Each mL of the solution contains 37 MBq, 1 mCi of indium In 111 [no carrier added, >1.85 GBq/µg indium (>50 mCi/µg indium)] at calibration time, 50 µg oxyquinoline, 100 µg polysorbate 80, and 6 mg of HEPES (N-2-hydroxyethylpiperazine-N'-2-ethane sulfonic acid) buffer in 0.75% sodium chloride solution. The drug is intended for single use only and contains no bacteriostatic agent. The radionuclidic impurity limit for indium 114m is not greater than 37 kBq, 1 µCi of indium 114m per 37 MBq, 1 mCi of indium In 111 at the time of calibration. The radionuclidic composition at expiration time is not less than 99.75% of indium In 111 and not more than 0.25% of indium In 114m/114.

Chemical name: Indium In 111 Oxyquinoline.

The precise structure of the indium In 111 oxyquinoline complex is unknown at this time. The empirical formula is (C9H6NO)3 In 111.

PHYSICAL CHARACTERISTICS

Indium In 111 decays by electron capture with a physical half-life of 67.2 hours (2.8 days). The energies of the photons that are useful for detection and imaging studies are listed in Table 1.

Table 1. Principal Radiation Emission Data*

Radiation	Mean %/ Disintegration	Mean Energy (keV)
* Kocher, David C., "Radioactive Decay Data Tables", DOE/TIC-11026, 115 (1981).
Gamma 2	90.2	171.3
Gamma 3	94	245.4

EXTERNAL RADIATION

The exposure rate constant for 37 MBq, 1 mCi indium In 111 is 8.3 × 10-4 C/kg/h (3.21 R/h) at 1 cm. The first half value thickness of lead (Pb) for indium In 111 is 0.023 cm. A range of values for the relative attenuation of the radiation emitted by this radionuclide that results from the interposition of various thicknesses of Pb is shown in Table 2. For example, the use of 0.834 cm of lead will decrease the external radiation exposure by a factor of about 1,000.

Table 2. Radiation Attenuation by Lead Shielding*

Shield Thickness (Pb) cm	Coefficient of Attenuation
* Data supplied by Oak Ridge Associated Universities, Radiopharmaceutical Internal Dose Information Center, 1984.
0.023	0.5
0.203	10-1
0.513	10-2
0.834	10-3
1.12	10-4

These estimates of attenuation do not take into consideration the presence of longer-lived contaminants with higher energy photons, namely indium In 114m/114.

To allow correction for physical decay of indium In 111, the fractions that remain at selected intervals before and after the time of calibration are shown in Table 3.

Table 3. Physical Decay Chart for Indium In 111, Half-life 67.2 hours

Day	Fraction Remaining	Day	Fraction Remaining
* Calibration Time
-2	1.641	2	0.610
-1	1.281	3	0.476
0*	1.000	4	0.372
1	0.781	5	0.290

Indium Oxyquinoline - Clinical Pharmacology

Indium forms a saturated (1:3) complex with oxyquinoline. The complex is neutral and lipid-soluble, which enables it to penetrate the cell membrane. Within the cell, indium becomes firmly attached to cytoplasmic components; the liberated oxyquinoline is released by the cell. It is thought likely that the mechanism of labeling cells with indium In 111 oxyquinoline involves an exchange reaction between the oxyquinoline carrier and subcellular components which chelate indium more strongly than oxyquinoline. The low stability constant of the oxyquinoline complex, estimated at approximately 10, supports this theory.

Following the recommended leukocyte cell labeling procedure, approximately 77% of the added indium In 111 oxyquinoline is incorporated in the resulting cell pellet (which represents approximately 3-4 × 108 WBC).

Cell clumping can occur and was found in about one fifth of the leukocyte preparations examined. The presence of red blood cells or plasma will lead to reduced leukocyte labeling efficiency. Transferrin in plasma competes for indium In 111 oxyquinoline.

After injection of labeled leukocytes into normal volunteers, about 30% of the dose is taken up by spleen and 30% by liver, reaching a plateau at 2-48 hours after injection. No significant clearance of radioactivity is observed at 72 hours in these two organs. Pulmonary uptake is 4-7.5% at 10 minutes but is lost rapidly; pulmonary radioactivity is usually visible in scans only up to about 4 hours after injection.

The human biodistribution studies in three normal subjects injected with indium In 111 oxyquinoline labeled leukocytes indicate a biexponential disappearance of indium In 111 from the blood when monitored for up to 72 hours. Between 9.5 to 24.4% of the injected dose remains in whole blood and clears with a biological half-time of 2.8 to 5.5 hours. The remainder (13-18%) clears from blood with a biological half-time of 64 to 116 hours.

Elimination from the body of injected indium In 111 oxyquinoline is probably mainly through decay to stable cadmium since only a negligible amount (less than 1%) of the dose is excreted in feces and urine in 24 hours.

Clearance from whole blood and biological distribution can vary considerably with the individual recipient, the condition of the injected cells and labeling techniques used.

Release of radioactivity from the labeled cells is about 3% at 1 hour and 24% at 24 hours.

Clearance from liver and spleen, for the purpose of calculating the radiation dose, is assumed to be equal to the physical half-life of indium In 111 (67.2 hours).

Indications and Usage for Indium Oxyquinoline

Indium In 111 oxyquinoline is indicated for radiolabeling autologous leukocytes.

Indium In 111 oxyquinoline labeled leukocytes may be used as an adjunct in the detection of inflammatory processes to which leukocytes migrate, such as those associated with abscesses or other infection, following reinjection and detection by appropriate imaging procedures. The degree of accuracy may vary with labeling techniques and with the size, location and nature of the inflammatory process.

Indium In 111 oxyquinoline labeled leukocyte imaging is not the preferred technique for the initial evaluation of patients with a high clinical probability of an abscess in a known location. Ultrasound or computed tomography may provide a better anatomical delineation of the infectious process and information may be obtained more quickly than with labeled leukocytes. If localization by these techniques is successful, labeled leukocytes should not be used as a confirmatory procedure. If localization or diagnosis by these methods fails or is ambiguous, indium In 111 oxyquinoline labeled leukocyte imaging may be appropriate.

Contraindications

None known.

Warnings

The content of the vial of indium In 111 oxyquinoline solution is intended only for use in the preparation of indium In 111 oxyquinoline labeled autologous leukocytes, and is not to be administered directly. Autologous leukocyte labeling is not recommended in leukopenic patients because of the small number of available leukocytes.

Due to radiation exposure, indium In 111 oxyquinoline labeled leukocytes could cause fetal harm when administered to pregnant women. If this radiopharmaceutical is used during pregnancy, the patient should be informed of the potential hazard to the fetus.

Indium In 111 oxyquinoline labeled autologous leukocytes should be used only when the benefit to be obtained exceeds the risks involved in children under eighteen years of age owing to the high radiation burden and the potential for delayed manifestation of long-term adverse effects.

Precautions

Clumping of cells may produce focal accumulations of radioactivity in lungs which do not wash out in 24 hours and thus may lead to false positive results. This phenomenon can be detected by imaging the chest immediately after injection.

The normally high uptake of indium In 111 oxyquinoline labeled leukocytes by spleen and liver may mask inflammatory lesions in these organs. Labeled leukocytes have been observed to accumulate in the colon and accessory spleens of patients with or without disease.

Chemotaxis of granulocytes deteriorates during storage and loss of chemotaxis may cause false negative scans. The spontaneous release of indium In 111 has been reported to range from about 3% at one hour to 24% at 24 hours [ten Berge, R.J.M., Natarajan, A.T., Hardeman, M.R., et al, Labeling with indium In 111 has detrimental effects on human lymphocytes, Journal of Nuclear Medicine, 24, 615-620 (1983)]. The maximum amount of time recommended between drawing the blood and reinjection should not exceed 5 hours. It is recommended that the labeled cells be used within one hour of preparation, if possible and in no case more than three hours after preparation.

Plasma and red cell contamination impairs labeling efficiency of leukocytes. Hemolyzed blood in labeled leukocytes may produce heart pool activity and should be avoided.

Cell aggregates of various degrees have been reported. Cell labeling techniques and standing of cell preparation may be contributing factors.

Nuclear medicine procedures involving withdrawal and reinjection of blood have the potential for transmission of blood borne pathogens. Procedures should be implemented to avoid administration errors and viral contamination of personnel during blood product labeling. A system of checks similar to the ones used for administering blood transfusions should be routine.

General

Strict aseptic techniques should be used to maintain sterility throughout the procedures for using this product.

Do not use after the expiration time and date (5 days after calibration time) stated on the label.

The contents of the vial are radioactive. Adequate shielding of the preparation must be maintained at all times.

Indium In 111 oxyquinoline, like other radioactive drugs, must be handled with care and appropriate safety measures should be used to minimize radiation exposure to clinical personnel. Care should also be taken to minimize radiation exposure to the patient consistent with proper patient management.

Radiopharmaceuticals should be used only by physicians who are qualified by training and experience in the safe use and handling of radionuclides and whose experience and training have been approved by the appropriate governmental agency authorized to license the use of radio-nuclides.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Although earlier studies suggested that oxyquinoline (oxine) might have carcinogenic potential, recent studies have found no evidence of carcinogenicity in either rats or mice given oxyquinoline in feed at concentrations of 1,500 or 3,000 ppm for 103 weeks.

It has been reported [ten Berge, R.J.M., Natarajan, A.T., Hardeman, M.R., et al, Labeling with indium In 111 has detrimental effects on human lymphocytes, Journal of Nuclear Medicine, 24, 615-620 (1983)] that human lymphocytes labeled with recommended concentrations of indium In 111 oxyquinoline showed chromosome aberrations consisting of gaps, breaks and exchanges that appear to be radiation induced. At 555 kBq/107, 15 µCi/107 lymphocytes 93% of the cells were reported to be abnormal. The oncogenic potential of such lymphocytes has not been studied. It has been reported that the radiation dose to 108 leukocytes is 9 × 104 mGy (0.9 × 104 rads) from 18.5 MBq, 500 µCi [Goodwin, David A., Cell labeling with oxine chelates of radioactive metal ions: Techniques and clinical implications, Journal of Nuclear Medicine, 19, 557-559 (1978)].

Studies have not been performed to evaluate whether indium In 111 oxyquinoline affects fertility in male or female laboratory animals or humans.

Pregnancy Category C

Animal reproduction studies have not been conducted with Indium In 111 Oxyquinoline labeled leukocytes. It is also not known whether Indium In 111 Oxyquinoline labeled leukocytes can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity.

However, Indium Nitrate, a closely related compound, was teratogenic and embryopathic in hamsters. Indium In 111 Oxyquinoline labeled leukocytes should be given to a pregnant woman only if clearly needed.

Ideally, examinations using radiopharmaceuticals, especially those elective in nature, in women of childbearing capability should be performed during the first few (approximately ten) days following the onset of menses.

Nursing Mothers

It is reported that indium 111 is secreted in human milk following administration of indium In 111 labeled leukocytes. Therefore, formula feedings should be substituted for breast feedings.

Pediatric Use

Safety and effectiveness in pediatric patients below age 18 have not been established (See Warnings).

Adverse Reactions

Sensitivity reactions (urticaria) have been reported. The presence of fever may mask pyrogenic reactions from indium In 111 oxyquinoline labeled leukocytes. The possibility of delayed adverse reactions has not been studied.

Indium Oxyquinoline Dosage and Administration

The recommended adult (70 kg) dose of indium In 111 oxyquinoline labeled autologous leukocytes is 7.4 to 18.5 MBq, 200-500 µCi. Indium In 111 oxyquinoline solution is intended for the radiolabeling of autologous leukocytes. The indium In 111 oxyquinoline labeled autologous leukocytes are administered intravenously.

Imaging is recommended at approximately 24 hours post injection. Typically, anterior and posterior views of the chest, abdomen and pelvis should be obtained with other views as required.

Aseptic procedures and a shielded syringe should be employed in the withdrawal of indium In 111 oxyquinoline from the vial. Similar procedures should be employed during the labeling procedure and the administration of the labeled leukocytes to the patient. The user should wear waterproof gloves during the entire procedure. The patient's dose should be measured by a suitable radioactivity calibration system immediately before administration. At this time, the leukocyte preparation should be checked for gross clumping and red blood cell contamination.

RADIATION DOSIMETRY

The estimated absorbed radiation doses to an adult patient weighing 70 kg from an intravenous dose of 18.5 MBq, 500 µCi of indium In 111 oxyquinoline labeled leukocytes including contributions from indium In 114m/114 as a radionuclidic impurity are shown in Table 4.

Table 4. Radiation Dose Estimate in a 70 kg Human for 18.5 MBq, 500 µCi at Expiry of Indium In 111 (99.75%) Oxyquinoline labeled leukocytes with Indium In 114m/114 (0.25%)

Assumptions: 30% to spleen, 30% to liver, 34% to red marrow, 6% to remainder of body, with no excretion.
Organ	mGy/18.5 MBq In 111	Rads/500 µCi In 111
Spleen	130	13
Liver	19	1.9
Red Marrow	13	1.3
Skeleton	3.64	0.364
Testes	0.1	0.01
Ovaries	1.9	0.19
Total Body	3.1	0.31
Organ	mGy/46.25 kBq In 114m/114	Rads/1.25 µCi In 114m/114
Spleen	70	7
Liver	7.1	0.71
Red Marrow	6.9	0.69
Skeleton	0.85	0.085
Testes	0.04	0.004
Ovaries	0.06	0.006
Total Body	0.6	0.06
Organ	Total Dose in mGy	Total Dose in Rads
Spleen	200	20
Liver	26.6	2.66
Red Marrow	19.9	1.99
Skeleton	4.5	0.45
Testes	0.14	0.014
Ovaries	2.0	0.2
Total Body	3.7	0.37

The dose of radiation absorbed by the organs will vary with the distribution of the blood cells in the organs, which in turn will depend on the predominance of the cell types labeled and their condition.

LABELING PROCEDURE

Sterile technique must be used throughout. It is important that all equipment used for the preparation of reagents be thoroughly cleaned to assure the absence of trace metal impurities. The user should wear waterproof gloves during the handling and administration procedure.

1. The following equipment is recommended:
   
   One (1) 60 mL or two (2) 30 mL sterile disposable plastic syringes with a 19 or 20 gauge needle (NOTE: Do not use a smaller gauge needle).
   
   Ring stand and clamp(s).
   
   Three (3) 50 mL sterile conical plastic centrifuge tubes with screw caps. Label each set with patient ID and "WBC", "LPP" and "Wash" respectively (NOTE: 3 centrifuge tubes per patient).
   
   Clinical Centrifuge with horizontal, 4 place rotor or equivalent.
   
   Sodium Chloride 0.9% Injection, USP.
   
   Three (3) disposable 5 or 10 mL syringes and 19 gauge needles.
   
   Syringe shield to dispense indium In 111 oxyquinoline.
   
   A dose calibrator.
   
   Butterfly catheter infusion set.
   
   Test tube rack.
   
   Lab timer.
   
   10 mL syringe with a 19 gauge or 20 gauge needle.
   
   19 gauge needle with filter (optional).


2. Withdraw from the patient 30-50 mL blood [preferably fifty (50) mL] using aseptic venipuncture technique using the 60 mL syringe fitted with a 19 gauge or 20 gauge needle and containing approximately 1000-1500 units heparin in 1-2 mL. Blood withdrawal should be smooth and slow so as not to produce bubbles or foaming.


3. Remove and dispose of the needle and replace with a syringe cap. Gently mix the contents of the syringe and label with the patient's ID, date and time.


4. Upon receipt of the full syringe for processing, the contents should again be gently mixed.


5. Clamp the syringe barrel to the ring stand in an upright (needle side up) position and tilt the syringe 10-20 degrees from its position perpendicular to the bench.


6. Allow the red cells to sediment 30-60 minutes, depending upon when the supernatant [leukocyte rich plasma (LRP)] looks clear of red blood cells.


7. Replace the syringe cap with an infusion set.


8. Collect the plasma (LRP) in the centrifuge tube marked "WBC" by expressing the LRP through the catheter tubing making sure not to get any red cells into the WBC tube.


9. Immediately centrifuge the capped WBC tube at 400-450 g for 5 minutes.


10. Transfer the supernatant to the leukocyte poor plasma (LPP) tube leaving behind 0.5-1.0 mL supernatant to cover the white cell button (NOTE: the button often contains a small number of red cells and may appear red).


11. Wash the white cell button with 4-6 mL Sodium Chloride (0.9%) Injection, USP. Resuspend the button by gentle swirling.


12. Centrifuge the capped WBC tube at 400-450 g for 5 minutes (alternatively, 150 g for 8 minutes) and discard all but 0.5-1.0 mL of the supernate to cover the cells.


13. Add 5.0 mL Sodium Chloride (0.9%) Injection, USP. Resuspend the cells by gentle swirling.


14. With the shielded syringe, draw up approximately 22.2 MBq, 600 µCi indium In 111 oxyquinoline. Check the amount of radioactivity in a dose calibrator set for indium In 111 and record for labeling efficiency calculations.
    
    Parenteral drug products should be inspected visually for particulate matter and discoloration before administration.


15. In several additions, add the indium In 111 oxyquinoline to the WBC tube, gently swirling after each addition.


16. Set the lab timer for 15 minutes and allow the capped WBC tube to incubate. Swirl the cell preparation several times during the incubation.


17. With a sterile plastic syringe, add half of the saved LPP (or about 8 mL) from the LPP tube. Cap and gently swirl the contents of WBC tube to resuspend the cells.


18. Centrifuge the WBC tube at 450 g for 5 minutes (or 150 g for 8 minutes). Decant supernatant into the wash tube leaving behind about 0.5 mL of the supernate to cover the cells.


19. Assay the activity in the WBC tube and in the wash tube in a dose calibrator and record.


20. With a sterile plastic syringe add the remaining LPP to the cell button and gently resuspend by swirling. With a sterile syringe fitted with a 19 gauge needle, resuspend the cells by drawing the cells up into the syringe and expressing the suspension against the tube gently once or twice. Alternatively, draw up the cells into a syringe fitted with the filtered 19 gauge needle, and replace the needle with an unfiltered 19 or 20 gauge needle.


21. Reserve in the WBC tube a minimum amount of white cell suspension for a WBC count. A microscopic examination should also be completed to observe for clumping. Draw up the patient's dose (7.4 to 18.5 MBq, 200-500 µCi) and check the syringe in the dose calibrator. Record the measurement.

QUALITY CONTROL

It is generally advantageous to record any observations on cell abnormalities (e.g., cell clumping). A trypan blue exclusion test may also be performed.

It is recommended that the preparation be used within one hour of labeling (See Precautions).

How is Indium Oxyquinoline Supplied

Indium In 111 oxyquinoline solution is supplied in a vial as a single use only product containing 37 MBq, 1.0 mCi in 1.0 mL aqueous solution at the calibration date stated on the label. Vials are packaged in individual lead shields.

(NDC 17156-021-01)

The contents of the vial are radioactive and adequate shielding and handling precautions must be maintained.

This radiopharmaceutical is licensed by Illinois Department of Nuclear Safety for distribution to persons licensed pursuant to 32 Ill. Adm. Code 330.260 (a) and Part 335, Subpart E, 335.4010, or under equivalent licenses of an Agreement State or a Licensing State.

SPECIAL HANDLING AND STORAGE

Indium In 111 oxyquinoline solution should be stored at room temperature (15-25 °C, 59-77 °F).

Indium In 111 oxyquinoline labeled autologous leukocytes should preferably be reinjected within one hour of labeling. The labeled cells may be stored at room temperature (15-25 °C, 59-77 °F) for up to three hours following completion of the cell labeling procedure. Reinjection of indium In 111 oxyquinoline labeled autologous leukocytes more than 5 hours after initial blood drawing is not recommended.

Sterile technique must be used throughout the collection, labeling and re-injection procedures.

Amersham Health

Medi-Physics, Inc.

Arlington Heights, IL 60004

1-800-654-0118

Printed in U.S.A.

Manufactured by:

Amersham plc,

Amersham, England

43-2015J

CODE IN.15PA

INDIUM IN 111 OXYQUINOLINE  indium in-111 oxyquinoline  solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 17156-021 Route of Administration INTRAVENOUS DEA Schedule

INGREDIENTS Name (Active Moiety) Type Strength Indium In-111 Oxyquinoline (Indium In-111 Oxyquinoline) Active 1 MICROGRAM  In 1 MILLILITER Polysorbate 80 Inactive 100 MICROGRAM  In 1 MILLILITER

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 17156-021-01 1 VIAL In 1 BOX contains a VIAL 1 1 mL (MILLILITER) In 1 VIAL This package is contained within the BOX (17156-021-01)

Revised: 05/2006Amersham Health Medi Physics, Inc.

More Indium Oxyquinoline resources

• Indium Oxyquinoline Side Effects (in more detail)
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• Indium Oxyquinoline Support Group
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Happinose Nasal Decongestant Balm

1. Name Of The Medicinal Product

HAPPINOSE™ NASAL DECONGESTANT BALM

2. Qualitative And Quantitative Composition

Levomenthol 0.3% w/w.

3. Pharmaceutical Form

Ointment.

4. Clinical Particulars

4.1 Therapeutic Indications

By topical administration to the nasal passages for the symptomatic relief of nasal congestion associated with the common cold, catarrh, head colds and hay fever. If desired, Happinose may also be rubbed onto the lips, nose, throat and chest and between the shoulders.

4.2 Posology And Method Of Administration

For adults and the elderly. Blow the nose before application. Carefully apply half an inch of Happinose inside each nostril using the little finger and inhale. If desired, Happinose can also be rubbed on the bridge of the nose, throat and chest and between the shoulders. Re-apply four hourly as required. If symptoms persist after 10-14 days, consult your doctor.

Children over 10 years. As above, but one half the adult dose.

Children 5-9 years. As above, but one quarter the adult dose.

Children under 5 years. Not recommended.

4.3 Contraindications

Known sensitivity to the preparation or any of its ingredients. Children under 5 years of age.

4.4 Special Warnings And Precautions For Use

For external use only. Keep away from the eyes and keep out of reach of children. Hands should be washed after use.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

None reported.

4.6 Pregnancy And Lactation

There have been no reports of abnormalities or adverse effects associated with the use of Happinose in pregnant women or nursing mothers.

4.7 Effects On Ability To Drive And Use Machines

None reported.

4.8 Undesirable Effects

None reported.

4.9 Overdose

There is no specific antidote to Happinose. Symptomatic methods should be instituted.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

When inhaled, menthol produces a sensation of cooling in the nasal passages thus providing symptomatic relief.

5.2 Pharmacokinetic Properties

Not applicable.

5.3 Preclinical Safety Data

No special information.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Cineole (Eucalyptol); Geranium Oil; White Soft Paraffin; Light Liquid Paraffin.

6.2 Incompatibilities

None stated.

6.3 Shelf Life

36 months.

6.4 Special Precautions For Storage

Do not store above 25°C. Keep the container tightly closed.

6.5 Nature And Contents Of Container

Collapsible aluminium tube with plastic screw cap, containing 14 g.

6.6 Special Precautions For Disposal And Other Handling

Not applicable.

7. Marketing Authorisation Holder

Diomed Developments Limited

Tatmore Place, Gosmore

Hitchin, Herts SG4 7QR, UK

8. Marketing Authorisation Number(S)

00173/0177.

9. Date Of First Authorisation/Renewal Of The Authorisation

12 January 2009.

10. Date Of Revision Of The Text

June 2002.

Nicotinell fruit 4mg medicated chewing gum

1. Name Of The Medicinal Product

Nicotinell^® Fruit 4mg Medicated Chewing Gum

2. Qualitative And Quantitative Composition

One piece of medicated chewing gum contains 4 mg nicotine (as 20 mg nicotine – polacrilin (1:4)).

For excipients, see section 6.1.

3. Pharmaceutical Form

Medicated chewing gum.

Each piece of coated chewing gum is off-white in colour and rectangular in shape.

4. Clinical Particulars

4.1 Therapeutic Indications

Nicotinell gum is indicated for the relief of nicotine withdrawal symptoms, as an aid to smoking cessation. Nicotinell Fruit 4mg gum is for use when severe withdrawal symptoms are experienced.

Concurrent counselling/behavioural support is recommended as it is likely to increase the chances of a successful quit.

4.2 Posology And Method Of Administration

Adults and elderly

Users should stop smoking completely during treatment with Nicotinell gum.

One piece of Nicotinell gum to be chewed when the user feels the urge to smoke. Normally, 8-12 pieces per day can be used, up to a maximum of 15 pieces per day.

The 4 mg chewing gum is intended to be used by smokers with a strong or very strong nicotine dependency and those who have previously failed to stop smoking with the aid of nicotine replacement therapy.

The optimal dosage form is selected according to the following table:

If an adverse event is noted when high dose forms are initiated, this should be replaced by the lower dosage form.

The characteristics of chewing-gum as a pharmaceutical form are such that individually different nicotine levels can result in the blood. Therefore, dosage frequency should be adjusted according to individual requirements within the stated maximum limit.

Directions for use:

1. One piece of gum should be chewed until the taste becomes strong.

2. The chewing gum should be rested between the gum and cheek.

3. When the taste fades, chewing should commence again.

4. The chewing routine should be repeated for 30 minutes.

The treatment time is individual. Normally, treatment should continue for at least 3 months.

After three months, the user should gradually cut down the number of pieces chewed each day until they have stopped using the product.

Treatment should be discontinued when the dose has been reduced to 1-2 pieces of gum per day. Use of nicotine products like Nicotinell gum beyond 6 months is generally not recommended. Some ex-smokers may need treatment with the gum for longer to avoid returning to smoking. Patients who have been using oral nicotine replacement therapy beyond 9 months are advised to seek additional help and information from health care professionals.

Nicotinell gum is sugar free.

Adolescents (aged 12-18 years of age)

The above recommendation can be used for adolescents aged between 12 and 18 years of age. As data are limited in this age group, medical advice should be obtained should it be found necessary to use the gum beyond 12 weeks.

Concomitant use of acidic beverages such as coffee or soda may decrease the buccal absorption of nicotine. Acidic beverages should be avoided for 15 minutes prior to chewing the gum.

4.3 Contraindications

Hypersensitivity to nicotine or any components of the gum.

Nicotinell gum should not be used by non-smokers.

4.4 Special Warnings And Precautions For Use

Any risks that may be associated with nicotine replacement therapy are substantially outweighed by the well established dangers of continued smoking.

Precautions: Users should stop smoking completely during therapy with Nicotinell gum. They should be informed that if they continue to smoke while using the gums they may experience increased adverse effects due to the hazards of smoking, including cardiovascular effects.

Cardiovascular disease

In stable cardiovascular disease Nicotinell gum presents a lesser hazard than continuing to smoke. However dependant smokers currently hospitalised as a result of a recent myocardial infarction, severe disrythmia, or recent cerebrovascular accident who are considered to be haemodynamically unstable should be encouraged to stop smoking with non-pharmacological interventions. If this fails, Nicotinell gum may be considered but as data on safety in this patient group are limited, initiation should only be under medical supervision.

Diabetes mellitus

Patients with diabetes mellitus should be advised to monitor their blood sugar levels more closely than usual when nicotine replacement therapy is initiated as catecholamines released by nicotine can affect carbohydrate metabolism.

Allergic reactions

Angioedema and urticaria have been reported.

Gastro-intestinal disease

Swallowed nicotine may exacerbate symptoms in patients suffering from oesophagitis, gastritis, or peptic ulcers and oral nicotine replacement therapy preparations should be used with caution in these conditions. Ulcerative stomatitis have been reported.

Renal and or hepatic impairment

Should be used with caution in patients with moderate to severe hepatic impairment and/or severe renal impairment as the clearance of nicotine or its metabolites may be decreased with the potential for increased adverse effects.

Danger in small children

Doses of nicotine tolerated by adult and adolescent smokers can produce severe toxicity in small children that may be fatal. Products containing nicotine should not be left where they may be misused, handled or ingested by children. Nicotinell gum should be disposed of with care.

Pheochromocytoma and uncontrolled hyperthyroidism

Nicotinell gum should be used with caution in patients with uncontrolled hyperthyroidism or pheochromocytoma as nicotine causes the release of catecholamines.

Transferred dependence

Transferred dependence is rare and is both less harmful and easier to break than smoking dependence.

Stopping smoking

Polycyclic aromatic hydrocarbons in tobacco smoke induce the metabolism of drugs catalysed by CYP 1A2 (and possibly CYP 1A1). When a smoker stops, this may result in slower metabolism and a consequential rise in blood levels of drugs such as theophylline, tacrine, olanzaprine and clozaprine.

Other warnings

If denture wearers experience difficulty in chewing the gum, it is recommended that they use a different pharmaceutical form of nicotine replacement therapy.

Patients with rare hereditary problems of fructose intolerance should not take this medicine.

Nicotinell 4mg gum contains sorbital (E420) 0.2g per gum, a source of 0.04g fructose. Calorific value 0.9 kcal/piece of gum.

Nicotinell 4mg gum contains sodium 11.52 mg per piece of gum.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

No information is available on interactions between Nicotinell gum and other drugs. No clinically relevant interactions between nicotine replacement therapy and other drugs has definitely been established, however nicotine may possibly enhance the haemodynamic effects of adenosine.

4.6 Pregnancy And Lactation

Pregnancy

Smoking during pregnancy is associated with risks such as intra-uterine growth retardation, premature birth or still birth. Stopping smoking is the single most effective intervention for improving the health of the pregnant smoker and her baby. The earlier abstinence is achieved the better.

Ideally smoking cessation during pregnancy should be achieved without nicotine replacement therapy. For women unable to quit on their own nicotine replacement therapy may be recommended to assist a quit attempt. The risk of using nicotine replacement therapy to the foetus is lower than that expected with tobacco smoking, due to lower maximal plasma concentrations and no additional exposure to polycyclic hydrocarbons and carbon monoxide.

However as nicotine passes to the foetus affecting breathing movements and has a dose-dependant effect on placental/foetal circulation, the decision to use nicotine replacement therapy should be made on a risk-benefit assessment as early on in pregnancy as possible with the aim of discontinuing use after 2-3 months.

Intermittent dose products may be preferable as these usually provide a lower daily dose of nicotine than patches. However, patches may be preferred if the woman is suffering from nausea during pregnancy. If patches are used they should be removed before going to bed to avoid exposure overnight when the foetus would not normally be subjected to smoke derived nicotine.

Lactation

Nicotine from smoking and nicotine replacement therapy is found in breast milk. However the amounts of nicotine the infant is exposed to is relatively small and less hazardous than the second-hand smoke they would otherwise be exposed to.

Using intermittent dose products, compared to patches, may minimize the amount of nicotine in the breast milk as the time between administrations of nicotine replacement therapy and feeding can be more easily prolonged.

4.7 Effects On Ability To Drive And Use Machines

Not applicable.

4.8 Undesirable Effects

Some symptoms such as dizziness, headache and sleep disturbances may be related to the withdrawal of nicotine associated with stopping smoking.

In principle, Nicotinell gums can cause adverse reactions similar to those associated with nicotine administered by other means (including smoking) and these are mainly dose dependant. At recommended doses Nicotinell gum has not been found to cause any serious adverse effects. Excessive consumption of Nicotinell gum by those who have not been in the habit of inhaling tobacco smoke could possibly lead to nausea, faintness or headaches.

Most of the side effects which are reported by patients occur generally during the first 3-4 weeks after initiation of therapy.

Nicotine from gums may sometimes cause a slight irritation of the throat and increase salivation at the start of the treatment.

The gum may stick to and in rare cases damage dentures and dental appliances.

Common (> 1/100).

Nervous system disorders: headache, dizziness

Gastrointestinal disorders: hiccups, gastric symptoms e.g. nausea, vomiting, indigestion, heartburn, increased salivation, irritation or sore mouth or throat

Musculoskeletal, connective and bone disorders: jaw muscle ache.

Uncommon (>1/1,000, <1/100)

Cardiac disorders: palpitations

Skin and subcutaneous tissue disorders: erythema, urticaria

Rare (<1/1,000)

Cardiac disorders: cardiac arrhythmias (e.g. atrial fibrillation)

Immune system disorders: hypersensitivity, angioneurotic oedema and anaphylactic reactions.

4.9 Overdose

In overdose, symptoms corresponding to heavy smoking may be seen, however the toxicity of nicotine cannot be directly compared with that of smoking, because tobacco smoke contains additional toxic substances (eg. carbon monoxide and tar).

Overdose with Nicotinell gum may only occur if many pieces are chewed simultaneously. Nicotine toxicity after ingestion will most likely be minimized as a result of early nausea and vomiting that occur following excessive nicotine exposure. Risk of poisoning by swallowing the gum is small. Since the release of nicotine from the gum is slow, very little nicotine is absorbed from the stomach and intestine, and if any is, it will be inactivated in the liver.

Chronic smokers can tolerate doses of nicotine that, in a non-smoker, would be more toxic, because of the development of tolerance.

Symptoms

The minimum lethal dose of nicotine in a non-tolerant man has been estimated to be 40-60mg. Symptoms of acute nicotine poisoning include nausea, salivation, abdominal pain, diarrhoea, sweating, headache, dizziness, disturbed hearing and marked weakness. In extreme cases, these symptoms may be followed by hypotension, rapid or weak or irregular pulse, breathing difficulties, prostration, circulatory collapse and terminal convulsions.

Management of overdose

Following overdose, symptoms may be rapid particularly in children. All nicotine intake should stop immediately and the patient should be treated symptomatically. Artificial respiration with oxygen should be instituted if necessary. Activated charcoal reduces the gastro-intestinal absorption of nicotine.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

ATC Code: N07B A01

Pharmacotherapeutic group: Drugs used in nicotine dependence

Nicotine, the primary alkaloid in tobacco products and a naturally occurring autonomous substance, is a nicotine receptor agonist in the peripheral and central nervous systems and has pronounced CNS and cardiovascular effects. On consumption of tobacco products, nicotine has proven to be addictive, resulting in craving and other withdrawal symptoms when administration is stopped. This craving and these withdrawal symptoms include a strong urge to smoke, dysphoria, insomnia, irritability, frustration or anger, anxiety, concentration difficulties agitation and increased appetite or weight gain. The gum replaces part of the nicotine that would have been administrated via tobacco and reduces the intensity of the withdrawal symptoms and smoking urge.

5.2 Pharmacokinetic Properties

When the gum is chewed, nicotine is steadily released into the mouth and is rapidly absorbed through the buccal mucosa. A proportion, by the swallowing of nicotine containing saliva, reaches the stomach and intestine where it is inactivated.

The nicotine peak plasma mean concentration after a single dose of the 4 mg coated gum is approximately 9.3 nanograms per ml (after approximately 60 minutes) (average plasma concentration of nicotine when smoking a cigarette is 15-30 nanograms per ml).

Nicotine is eliminated mainly via hepatic metabolism; small amounts of nicotine are eliminated in unchanged form via the kidneys. The plasma half-life is approximately three hours. Nicotine crosses the blood-brain barrier, the placenta and is detectable in breast milk.

5.3 Preclinical Safety Data

No definite conclusion can be drawn on the genotoxic activity of nicotine in vitro. Nicotine was negative in in-vivo tests.

Animal experiments have shown that nicotine induces post-implantation loss and reduces the growth of foetuses.

The results of carcinogenicity assays did not provide any clear evidence of a tumorigenic effect of nicotine.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Gum base (containing butylhydroxytoluene)

Calcium carbonate

Sorbitol (E420)

Sodium carbonate anhydrous

Sodium hydrogen carbonate

Polacrilin

Glycerol

Purified water

Levomenthol

Tutti flavour

Saccharin

Sodium saccharin

Acesulfame potassium

Xylitol

Mannitol (E421)

Gelatin

Titanium dioxide (E171)

Carnauba wax

Talc.

6.2 Incompatibilities

Not applicable.

6.3 Shelf Life

2 years.

6.4 Special Precautions For Storage

Do not store above 25^oC.

6.5 Nature And Contents Of Container

The chewing-gum is packed in PVC/PVdC/aluminium blisters each containing either 2 or 12 pieces of gum. The blisters are packed in boxes containing 2, 12, 24, 36, 48, 60, 72, 96 108, 120 and 204 pieces of gum.

Not all pack sizes may be marketed.

6.6 Special Precautions For Disposal And Other Handling

No special requirements.

7. Marketing Authorisation Holder

Novartis Consumer Health UK Ltd

Trading as Novartis Consumer Health

Wimblehurst Road,

Horsham,

West Sussex RH12 5AB

8. Marketing Authorisation Number(S)

PL 00030/0430

9. Date Of First Authorisation/Renewal Of The Authorisation

08 December 2006

10. Date Of Revision Of The Text

12 June 2008

Legal category: GSL

Ganciclovir ophthalmic

Generic Name: ganciclovir ophthalmic (gan SYE klo veer off THAL mik)

Brand Names: Vitrasert, Zirgan

What is ganciclovir?

Ganciclovir is an antiviral drug. It slows the growth and spread of the cytomegalovirus.

Ganciclovir ophthalmic (for the eyes) is used to treat certain viral infections affecting the eyes.

Ganciclovir implant (Vitrasert) is used to treat cytomegalovirus (CMV) infection of the eye. This infection usually occurs in patients who have suppressed immune systems such as patients with AIDS and organ transplant patients.

Ganciclovir gel (Zirgan) is used to treat eye ulcers caused by the herpes simplex virus.

Ganciclovir is not a cure for CMV or herpes. This medication will not treat symptoms of these infections in any other part of the body.

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

What is the most important information I should know about ganciclovir?

You should not use this medication if you are allergic to ganciclovir or acyclovir (Zovirax).

Ganciclovir implant (Vitrasert) is used to treat cytomegalovirus (CMV) infection of the eye. Ganciclovir gel (Zirgan) is used to treat eye ulcers caused by the herpes simplex virus.

Ganciclovir is not a cure for cytomegalovirus or herpes. This medication will not treat symptoms of these infections in any other part of the body.

To make sure you can safely use ganciclovir, tell your doctor if you have low levels of platelets in your blood (easy bruising or bleeding), or an infection in any part of your body (other than your eyes).

Do not wear contact lenses while you are using this medication. You should not wear contact lenses at any time you have an active eye ulcer or infection.

What should I discuss with my health care provider before using ganciclovir?

You should not use this medication if you are allergic to ganciclovir or acyclovir (Zovirax).

To make sure you can safely use ganciclovir, tell your doctor if you have any of these other conditions:

• 
  

  an infection in any part of your body (other than your eyes); or

  
  


• 
  

  low levels of platelets in your blood (easy bruising or bleeding).

  
  

Do not wear contact lenses while you are using this medication. You should not wear contact lenses at any time you have an active eye ulcer or infection. FDA pregnancy category C. It is not known whether ganciclovir will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication. This medication can decrease sperm count and may affect a man's fertility (ability to have children). It is not known whether ganciclovir passes into breast milk or if it could harm a nursing baby. Do not use Zirgan without telling your doctor if you are breast-feeding a baby. You should not breast-feed after you have received a Vitrasert implant. Ganciclovir gel (Zirgan) should not be given to a child younger than 2 years old.

How should I use ganciclovir?

The Vitrasert implant is surgically placed into the eye. The implant will slowly release ganciclovir into the affected eye over a period of 5 to 8 months.

Use Zirgan gel exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Zirgan is usually applied 5 times each day until your eye ulcer heals. Then the gel is applied 3 times per day for 7 days. Follow your doctor's instructions.

Wash your hands before using the eye drops.

To apply Zirgan:

• 
  

  Tilt your head back slightly and pull down your lower eyelid to create a small pocket. Hold the dropper above the eye with the tip down. Look up and away from the dropper as you squeeze out a drop, then close your eye.

  
  


• 
  

  Use only the number of drops your doctor has prescribed.

  
  


• 
  

  Gently press your finger to the inside corner of the eye (near your nose) for about 1 minute to keep the liquid from draining into your tear duct. If you use more than one drop in the same eye, wait about 5 minutes before putting in the next drop.

  
  

Do not allow the tip of the dropper to touch any surface, including your 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.

Ganciclovir does not cure herpes or CMV. Your disease may continue to progress even after you are treated with this medication. Your doctor will need to check your progress on a regular basis, and you will need routine eye exams.

Store Zirgan at room temperature away from moisture and heat. Do not freeze. Keep the bottle tightly closed when not in use.

What happens if I miss a dose?

Use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.

Since the Vitrasert implant is surgically put into place, you will not be on a dosing schedule for this medication. The implant may be removed and replaced after 5 to 8 months.

What happens if I overdose?

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

What should I avoid while taking ganciclovir?

Do not use any eye medications that your doctor has not prescribed.

Ganciclovir may cause blurred vision, which may last up to 4 weeks after Vitrasert implant surgery. Be careful if you drive or do anything that requires you to be able to see clearly.

Ganciclovir side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have a serious side effect such as:

• 
  

  eye pain, swelling, redness, or watering;

  
  


• 
  

  severe burning or itching of your eyes;

  
  


• 
  

  vision changes, increased sensitivity to light;

  
  


• 
  

  tunnel vision, problems with peripheral (side) vision;

  
  


• 
  

  seeing flashes of light, halos around lights, or "floaters" in your vision;

  
  


• 
  

  white patches on your eyes;

  
  


• 
  

  cloudiness in the pupils or iris of your eyes;

  
  


• 
  

  bleeding, oozing, or crusting of your eyes; or

  
  


• 
  

  sudden vision loss.

  
  

Less serious side effects may include:

• 
  

  blurred vision (may last up to 4 weeks after Vitrasert implant surgery);

  
  


• 
  

  mild eye irritation; or

  
  


• 
  

  increased tearing.

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Ganciclovir ophthalmic Dosing Information

Usual Adult Dose for CMV Retinitis:

1 surgical implant in the posterior segment of the affected eye(s) every 5 to 8 months. Following depletion of ganciclovir from the implant, as evidenced by progression of retinitis, the implant may be removed and replaced.

Usual Adult Dose for Herpes Simplex Dendritic Keratitis:

1 drop in the affected eye 5 times per day (approximately every 3 hours while awake) until the corneal ulcer heals, and then 1 drop 3 times per day for 7 days.

Usual Pediatric Dose for CMV Retinitis:

Less than 9 years: Safety and efficacy have not been established.
9 years or older: 1 surgical implant in the posterior segment of the affected eye(s) every 5 to 8 months. Following depletion of ganciclovir from the implant, as evidenced by progression of retinitis, the implant may be removed and replaced.

Usual Pediatric Dose for Herpes Simplex Dendritic Keratitis:

2 years or older:
1 drop in the affected eye 5 times per day (approximately every 3 hours while awake) until the corneal ulcer heals, and then 1 drop 3 times per day for 7 days.

What other drugs will affect ganciclovir?

It is not likely that other drugs you take orally or inject will have an effect on ganciclovir used in the eyes. But many drugs can interact with each other. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

More ganciclovir ophthalmic resources

• Ganciclovir ophthalmic Use in Pregnancy & Breastfeeding
• Ganciclovir ophthalmic Support Group
• 1 Review for Ganciclovir - Add your own review/rating

• Vitrasert Prescribing Information (FDA)


• Vitrasert Advanced Consumer (Micromedex) - Includes Dosage Information


• Vitrasert Implant MedFacts Consumer Leaflet (Wolters Kluwer)


• Zirgan Prescribing Information (FDA)


• Zirgan Advanced Consumer (Micromedex) - Includes Dosage Information


• Zirgan Consumer Overview


• Zirgan Gel MedFacts Consumer Leaflet (Wolters Kluwer)

Compare ganciclovir ophthalmic with other medications

• CMV Retinitis
• Herpes Simplex Dendritic Keratitis

Where can I get more information?

• Your pharmacist can provide more information about ganciclovir.

Zilactin L Liquid

Pronunciation: LIE-doe-cane
Generic Name: Lidocaine
Brand Name: Examples include Bactine and Zilactin L

Zilactin L Liquid is used for:

Temporarily relieving pain caused by cold sores/fever blisters. It may also be used at the first sign of tingling, itching, or burning to treat cold sores before they develop.

Zilactin L Liquid is an anesthetic. It works by preventing nerves from transmitting painful impulses to the brain.

Do NOT use Zilactin L Liquid if:

• you are allergic to any ingredient in Zilactin L Liquid or other similar medicines (eg, amide-type medicines)

Contact your doctor or health care provider right away if any of these apply to you.

Before using Zilactin L Liquid:

Some medical conditions may interact with Zilactin L Liquid. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have a blood infection or severe injury of the mouth or throat


• if you have heart, liver, or kidney problems


• if you have had a severe allergic reaction (eg, severe rash, hives, difficulty breathing, dizziness) to any anesthetic medicine

Some MEDICINES MAY INTERACT with Zilactin L Liquid. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Amiodarone, beta-adrenergic blockers (eg, metoprolol), cimetidine, or mexiletine because side effects, such as confusion, dizziness, lightheadedness or tiredness, may occur

This may not be a complete list of all interactions that may occur. Ask your health care provider if Zilactin L Liquid may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Zilactin L Liquid:

Use Zilactin L Liquid as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Moisten a cotton swab with several drops of Zilactin L Liquid. Apply to affected area and allow to dry for 15 seconds.


• Do not get Zilactin L Liquid in your eyes.


• If you miss a dose of Zilactin L Liquid, use it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not use 2 doses at once.

Ask your health care provider any questions you may have about how to use Zilactin L Liquid.

Important safety information:

• Zilactin L Liquid may cause drowsiness, dizziness, or blurred vision. These effects may be worse if you take it with alcohol or certain medicines. Use Zilactin L Liquid with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Tell your doctor or dentist that you take Zilactin L Liquid before you receive any medical or dental care, emergency care, or surgery.


• Zilactin L Liquid may make it difficult for you to swallow. Do not eat anything for at least 1 hour after Zilactin L Liquid has been applied in the mouth or throat area.


• Numbness of the tongue may cause you to bite the inside of your mouth accidentally. Do not eat any food or chew gum while your mouth or throat area is numb.


• Zilactin L Liquid may cause a numbing effect at the application site. Do not scratch, rub, or expose the area to extreme hot or cold temperature until the numbness is gone.


• Do not use more medicine, apply it more often, or use it for longer than prescribed. Your condition will not improve faster, but the risk of side effects may be increased.


• If your symptoms do not get better within 7 days or if they get worse, check with your doctor.


• Zilactin L Liquid should not be used in CHILDREN younger than 2 years old; safety and effectiveness in these children have not been confirmed.


• PREGNANCY and BREAST-FEEDING: It is not known if Zilactin L Liquid can cause harm to the fetus. If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Zilactin L Liquid while you are pregnant. It is not known if Zilactin L Liquid is found in breast milk after topical use. If you are or will be breast-feeding while you use Zilactin L Liquid, check with your doctor. Discuss any possible risks to your baby.

Possible side effects of Zilactin L Liquid:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Redness or swelling at the application site.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); choking; confusion; dizziness or lightheadedness; fast breathing; fast, slow, or irregular heartbeat; fever; mood or mental changes; ringing in the ears or hearing changes; seizures; shortness of breath; swelling of the throat; vision changes.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include apprehension; blurred vision; confusion; difficulty breathing; nervousness; ringing in the ears; seizures; sensations of heat, cold, or numbness; severe dizziness, drowsiness, or lightheadedness; slow or irregular heartbeat; tremor; twitching; unconsciousness; vomiting.

Proper storage of Zilactin L Liquid:

Store Zilactin L Liquid at room temperature, between 59 and 86 degrees F (15 and 30 degrees C), in a tightly closed container. Store away from heat, moisture, and light. Keep Zilactin L Liquid out of the reach of children and away from pets.

General information:

• If you have any questions about Zilactin L Liquid, please talk with your doctor, pharmacist, or other health care provider.


• Zilactin L Liquid is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Zilactin L Liquid. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Zilactin L resources

• Zilactin L Use in Pregnancy & Breastfeeding
• Zilactin L Support Group
• 22 Reviews for Zilactin L - Add your own review/rating

Compare Zilactin L with other medications

• Anal Itching
• Anesthesia
• Burns, External
• Hemorrhoids
• Pain
• Persisting Pain, Shingles
• Pruritus
• Sunburn