Probenecid Tablets

Probenecid Tablets, USP

500 mg


Rx only

Probenecid Tablets Description

Probenecid is a uricosuric and renal tubular transport blocking agent.

The chemical name for probenecid is 4-[(dipropylamino) sulfonyl] benzoic acid. It has the following structural formula:

Probenecid, USP is a white or nearly white, fine, crystalline powder. Probenecid is soluble in dilute alkali, in alcohol, in chloroform, and in acetone; it is practically insoluble in water and in dilute acids.

Each tablet for oral administration contains 500 mg of probenecid and the following inactive ingredients: microcrystalline cellulose, sodium lauryl sulfate, sodium starch glycolate, starch (corn), povidone, colloidal silicon dioxide, magnesium stearate, polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, D&C Yellow #10 Aluminum Lake, FD&C Yellow #6 Aluminum Lake, and FD&C Blue #2 Aluminum Lake.

Probenecid Tablets - Clinical Pharmacology

Probenecid is a uricosuric and renal tubular blocking agent. It inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Effective uricosuria reduces the miscible urate pool, retards urate deposition, and promotes resorption of urate deposits.

Probenecid inhibits the tubular secretion of penicillin and usually increases penicillin plasma levels by any route the antibiotic is given. A 2-fold to 4-fold elevation has been demonstrated for various penicillins.

Probenecid also has been reported to inhibit the renal transport of many other compounds including aminohippuric acid (PAH), aminosalicylic acid (PAS), indomethacin, sodium iodomethamate and related iodinated organic acids, 17-ketosteroids, pantothenic acid, phenolsulfonphthalein (PSP), sulfonamides, and sulfonylureas. See also Drug Interactions.

Probenecid decreases both hepatic and renal excretion of sulfobromophtalein (BSP). The tubular reabsorption of phosphorus is inhibited in hypoparathyroid but not in euparathyroid individuals.

Probenecid does not influence plasma concentrations of salicylates, nor the excretion of streptomycin, chloramphenicol, chlortetracycline, oxytetracycline, or neomycin.

Indications and Usage for Probenecid Tablets

Probenecid Tablets are indicated for the treatment of the hyperuricemia associated with gout and gouty arthritis.

As an adjuvant to therapy with penicillin or with ampicillin, methicillin, oxacillin, cloxacillin, or nafcillin, for elevation and prolongation of plasma levels by whatever route the antibiotic is given.

Contraindications

Hypersensitivity to probenecid.

Children under 2 years of age.

Not recommended in persons with known blood dyscrasias or uric acid kidney stones.

Therapy with probenecid should not be started until an acute gouty attack has subsided.

Warnings

Exacerbation of gout following therapy with probenecid may occur; in such cases colchicine or other appropriate therapy is advisable.

Probenecid increases plasma concentrations of methotrexate in both animals and humans. In animal studies, increased methotrexate toxicity has been reported. If probenecid is given with methotrexate, the dosage of methotrexate should be reduced and serum levels may need to be monitored.

In patients on probenecid the use of salicylates in either small or large doses is contraindicated because it antagonizes the uricosuric action of probenecid. The biphasic action of salicylates in the renal tubules accounts for the so-called "paradoxical effect" of uricosuric agents. In patients on probenecid who require a mild analgesic agent the use of acetaminophen rather than small doses of salicylates would be preferred.

Rarely, severe allergic reactions and anaphylaxis have been reported with the use of probenecid. Most of these have been reported to occur within several hours after readministration following prior usage of the drug.

The appearance of hypersensitivity reactions requires cessation of therapy with probenecid.

Use in Pregnancy

Probenecid crosses the placental barrier and appears in cord blood. The use of any drug in women of childbearing potential requires that the anticipated benefit be weighed against the possible hazards.

Precautions

General

Hematuria, renal colic, costovertebral pain, and formation of uric acid stones associated with the use of probenecid in gouty patients may be prevented by alkalization of the urine and a liberal fluid intake (see DOSAGE AND ADMINISTRATION). In these cases when alkali is administered, the acid-base balance of the patient should be watched.

Use with caution in patients with a history of peptic ulcer.

Probenecid has been used in patients with some renal impairment, but dosage requirements may be increased. Probenecid may not be effective in chronic renal insufficiency particularly when the glomerular filtration rate is 30 mL/minute or less. Because of its mechanism of action, probenecid is not recommended in conjunction with a penicillin in the presence of known renal impairment.

A reducing substance may appear in the urine of patients receiving probenecid. This disappears with discontinuance of therapy. Suspected glycosuria should be confirmed by using a test specific for glucose.

Drug Interactions

When probenecid is used to elevate plasma concentrations of penicillin or other beta-lactams, or when such drugs are given to patients taking probenecid therapeutically, high plasma concentrations of the other drug may increase the incidence of adverse reactions associated with that drug. In the case of penicillin or other beta-lactams, psychic disturbances have been reported.

The use of salicylates antagonizes the uricosuric action of probenecid (see WARNINGS). The uricosuric action of probenecid is also antagonized by pyrazinamide.

Probenecid produces an insignificant increase in free sulfonamide plasma concentrations, but a significant increase in total sulfonamide plasma levels. Since probenecid decreases the renal excretion of conjugated sulfonamides, plasma concentrations of the latter should be determined from time to time when a sulfonamide and probenecid are coadministered for prolonged periods. Probenecid may prolong or enhance the action of oral sulfonylureas and thereby increase the risk of hypoglycemia.

It has been reported that patients receiving probenecid require significantly less thiopental for induction of anesthesia. In addition, ketamine and thiopental anesthesia were significantly prolonged in rats receiving probenecid.

The concomitant administration of probenecid increases the mean plasma elimination half-life of a number of drugs which can lead to increased plasma concentrations. These include agents such as indomethacin, acetaminophen, naproxen, ketoprofen, meclofenamate, lorazepam, and rifampin. Although the clinical significance of this observation has not been established, a lower dosage of the drug may be required to produce a therapeutic effect, and increases in dosage of the drug in question should be made cautiously and in small increments when probenecid is being coadministered. Although specific instances of toxicity due to this potential interaction have not been observed to date, physicians should be alert to this possibility.

Probenecid given concomitantly with sulindac had only a slight effect on plasma sulfide levels, while plasma levels of sulindac and sulfone were increased. Sulindac was shown to produce a modest reduction in the uricosuric action of probenecid, which probably is not significant under most circumstances.

In animals and in humans, probenecid has been reported to increase plasma concentrations of methotrexate (see WARNINGS).

Falsely high readings for theophylline have been reported in an in vitro study, using the Schack and Waxler technique, when therapeutic concentrations of theophylline and probenecid were added to human plasma.

Adverse Reactions

The following adverse reactions have been observed and within each category are listed in order of decreasing severity.

Central Nervous System: headache, dizziness.

Metabolic: precipitation of acute gouty arthritis.

Gastrointestinal: hepatic necrosis, vomiting, nausea, anorexia, sore gums.

Genitourinary: nephrotic syndrome, uric acid stones with or without hematuria, renal colic, costovertebral pain, urinary frequency.

Hypersensitivity: anaphylaxis, fever, urticaria, pruritus.

Hematologic: aplastic anemia, leukopenia, hemolytic anemia which in some patients could be related to genetic deficiency of glucose -6- phosphate dehydrogenase in red blood cells, anemia.

Integumentary: dermatitis, alopecia, flushing.

Probenecid Tablets Dosage and Administration

Gout

Therapy with probenecid should not be started until an acute gouty attack has subsided. However, if an acute attack is precipitated during therapy, probenecid may be continued without changing the dosage, and full therapeutic dosage of colchicine, or other appropriate therapy, should be given to control the acute attack.

The recommended adult dosage is 250 mg (½ probenecid tablet), twice a day for one week, followed by 500 mg (1 tablet) twice a day thereafter.

Some degree of renal impairment may be present in patients with gout. A daily dosage of 1000 mg may be adequate. However, if necessary, the daily dosage may be increased by 500 mg increments every 4 weeks within tolerance (and usually not above 2000 mg per day) if symptoms of gouty arthritis are not controlled or the 24 hour uric acid excretion is not above 700 mg. As noted, probenecid may not be effective in chronic renal insufficiency particularly when the glomerular filtration rate is 30 mL/minute or less.

Gastric intolerance may be indicative of overdosage, and may be corrected by decreasing the dosage.

As uric acid tends to crystallize out of an acid urine, a liberal fluid intake is recommended, as well as sufficient sodium bicarbonate (3 to 7.5 g daily), or potassium citrate (7.5 g daily) to maintain an alkaline urine (see PRECAUTIONS).

Alkalization of the urine is recommended until the serum urate level returns to normal limits and tophaceous deposits disappear, i.e., during the period when urinary excretion of uric acid is at a high level. Thereafter, alkalization of the urine and the usual restriction of purine-producing foods may be somewhat relaxed.

Probenecid should be continued at the dosage that will maintain normal serum urate levels. When acute attacks have been absent for 6 months or more and serum urate levels remain within normal limits, the daily dosage may be decreased by 500 mg every 6 months. The maintenance dosage should not be reduced to the point where serum urate levels tend to rise.

Probenecid and Penicillin Therapy (General)

Adults

The recommended dosage is 2000 mg (4 tablets of probenecid) daily in divided doses. This dosage should be reduced in older patients in whom renal impairment may be present.

Children: 2-14 years of age:

Initial dose: 25 mg/kg body weight (or 0.7 g/square meter body surface).

Maintenance Dose: 40 mg/kg body weight (or 1.2 g/square meter body surface) per day, divided into 4 doses.

For children weighing more than 50 kg (110 lb) the adult dosage is recommended.

Probenecid is contraindicated in children under 2 years of age.

The PSP excretion test may be used to determine the effectiveness of probenecid in retarding penicillin excretion and maintaining therapeutic levels. The renal clearance of PSP is reduced to about one-fifth the normal rate when dosage of probenecid is adequate.

Penicillin Therapy (Gonorrhea)1

In uncomplicated gonococcal infections in men and women (urethral, cervical, rectal), 1 g of probenecid should be given orally with 4.8 million units of aqueous procaine penicillin G2 (given IM), or 3 g of amoxicillin2 (given orally), or 3.5 g of ampicillin2 (given orally).

For further guidance, see CDC recommendations for definition of regimens of choice, alternative regimens, treatment of hypersensitive patients, and other aspects of therapy.

1

Recommended by the Center for Disease Control, U.S. Department of Health and Human Services, Public Health Service (Morbidity and Mortality Weekly Report Supplement, Volume 34, Number 4S, October 18, 1985).

2

See package circulars of manufacturers for detailed information about CONTRAINDICATIONS, WARNINGS, PRECAUTIONS, and ADVERSE REACTIONS.

How is Probenecid Tablets Supplied

Probenecid Tablets, USP are available containing 500 mg of Probenecid, USP.

The tablets are capsule shaped, film-coated yellow, debossed LCI on one side and 1367 on the other side. They are available as follows:

NDC 0527-1367-01     bottles of 100 tablets

NDC 0527-1367-10     bottles of 1000 tablets

STORE AT 20°-25°C (68°-77°F) [See USP Controlled Room Temperature]

PROTECT FROM LIGHT.

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

MANUFACTURED BY

LANNETT COMPANY, INC.

PHILADELPHIA, PA 19136

0527

1367

Revised 10/06

PRINCIPAL DISPLAY PANEL

NDC 0527-1367-10

Lannett

PROBENECID

TABLETS, USP

500 mg

Rx Only

1000 TABLETS

PROBENECID  probenecid  tablet, film coated

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0527-1367 Route of Administration ORAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength PROBENECID (PROBENECID) PROBENECID 500 mg

Inactive Ingredients Ingredient Name Strength CELLULOSE, MICROCRYSTALLINE   SODIUM LAURYL SULFATE   SODIUM STARCH GLYCOLATE TYPE A POTATO   STARCH, CORN   POVIDONE K29/32   COLLOIDAL SILICON DIOXIDE   MAGNESIUM STEARATE   POLYVINYL ALCOHOL   TITANIUM DIOXIDE   POLYETHYLENE GLYCOL   TALC   D&C YELLOW NO. 10   FD&C YELLOW NO. 6   FD&C BLUE NO. 2   ALUMINUM OXIDE

Product Characteristics Color YELLOW (Yellow) Score no score Shape OVAL Size 18mm Flavor Imprint Code LCI;1367 Contains

Packaging # NDC Package Description Multilevel Packaging 1 0527-1367-01 100 TABLET In 1 BOTTLE None 2 0527-1367-10 1000 TABLET In 1 BOTTLE None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA080966	07/29/1976

Labeler - Lannett Company, Inc. (002277481)

Establishment
Name	Address	ID/FEI	Operations
Lannett Company, Inc.		002277481	MANUFACTURE

Establishment
Name	Address	ID/FEI	Operations
Lannett Company, Inc.		829757603	ANALYSIS, LABEL, MANUFACTURE, PACK

Establishment
Name	Address	ID/FEI	Operations
Lannett Company, Inc.		683520909	ANALYSIS

Revised: 11/2010Lannett Company, Inc.

More Probenecid Tablets resources

• Probenecid Tablets Side Effects (in more detail)
• Probenecid Tablets Dosage
• Probenecid Tablets Use in Pregnancy & Breastfeeding
• Drug Images
• Probenecid Tablets Drug Interactions
• Probenecid Tablets Support Group
• 1 Review for Probenecids - Add your own review/rating

Compare Probenecid Tablets with other medications

• Adjunct to Antibiotic Therapy
• Gout

Pneumococcal vaccine polyvalent Intramuscular

NOO-moe-KOK-al VAX-een pol-ee-VAY-lent

Commonly used brand name(s)

In the U.S.

• Pneumovax 23


• Pnu-Imune 23

In Canada

• Prevnar

Available Dosage Forms:

• Solution

Therapeutic Class: Vaccine

Uses For pneumococcal vaccine polyvalent

Pneumococcal polyvalent vaccine is an active immunizing agent used to prevent infection by pneumococcal bacteria. It works by causing your body to produce its own protection (antibodies) against the disease.

The following information applies only to the polyvalent 23 pneumococcal vaccine. Other polyvalent pneumococcal vaccines may be available in countries other than the U.S.

Pneumococcal infection can cause serious problems, such as pneumonia, which affects the lungs; meningitis, which affects the brain; bacteremia, which is a severe infection in the blood; and possibly death. These problems are more likely to occur in older adults and persons with certain diseases or conditions that make them more susceptible to a pneumococcal infection or more apt to develop serious problems from a pneumococcal infection.

Unless otherwise contraindicated, immunization (vaccination) against pneumococcal disease is recommended for all adults and children 2 years of age and older, especially:

• Older adults, especially those 65 years of age and older.


• Adults and children 2 to 64 years of age with chronic illnesses.


• Adults and children 2 to 64 years of age with sickle cell disease, those with spleen problems or without spleens, and those who are to have their spleens removed.


• Adults and children 2 to 64 years of age who are at increased risk for pneumococcal disease because of another illness (e.g., heart disease, lung disease, asthma, diabetes, alcoholism, liver disease, or kidney disease). People who smoke cigarettes should also receive the vaccine.


• Adults and children 2 to 64 years of age who are living in special environments or social settings (e.g., Alaskan Natives and certain American Indian populations), and residents of nursing homes and other long-term-care facilities.


• Adults and children 2 to 64 years of age with decreased disease-fighting ability (e.g., those with human immunodeficiency virus (HIV) infection, organ or bone marrow transplantations, and cancer).

Immunization (vaccination) against pneumococcal infection is not recommended for infants and children younger than 2 years of age, because these persons cannot produce enough antibodies to the vaccine to protect them against a pneumococcal infection.

This vaccine is to be administered only by or under the supervision of your doctor or other health care professional.

Before Using pneumococcal vaccine polyvalent

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

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to pneumococcal vaccine polyvalent 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

Use of pneumococcal polyvalent vaccine is not recommended in infants and children younger than 2 years of age.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of pneumococcal polyvalent vaccine in the elderly. However, elderly patients are more likely to have unwanted effects which may require caution in patients receiving this vaccine.

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 receiving this vaccine, 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.

Receiving this vaccine 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.

• Varicella Virus Vaccine

Receiving this vaccine 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.

• Rituximab

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 this vaccine. Make sure you tell your doctor if you have any other medical problems, especially:

• Brain disease or


• Immune system problems (e.g., cancer, HIV)—This vaccine may not work as well in patients with these conditions.

• Heart or blood vessel disease or


• Lung disease—Use with caution. May increase risk for more serious side effects.

• Moderate to severe acute illness—Patients with this condition should receive the vaccine at a delayed time.

• Thrombocytopenic purpura (blood disorder)—Use with caution. May make this condition worse.

Proper Use of pneumococcal vaccine polyvalent

A nurse or other trained health professional will give you or your child this vaccine. This vaccine is given as a shot into one of the muscles or under the skin, usually in the thigh or upper arm.

Pneumococcal vaccine is usually given only once to each person. Additional injections are only given for special cases, because of the possibility of more frequent and more severe side effects.

Precautions While Using pneumococcal vaccine polyvalent

If you have more than one doctor, be sure they all know that you have received pneumococcal vaccine polyvalent 23 so that they can put the information into your medical records. This vaccine is usually given only once to each person, except in special cases.

This vaccine may cause a serious type of allergic reaction called anaphylaxis. Anaphylaxis can be life-threatening and requires immediate medical attention. Tell your doctor right away if you or your child has a rash, itching, swelling of the tongue and throat, or trouble breathing after receiving the vaccine.

The pneumococcal polyvalent vaccine will not protect you or your child against all types of pneumococcal infections. It will also not treat an active infection.

pneumococcal vaccine polyvalent 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 or nurse immediately if any of the following side effects occur:

More common

• Chills

Less common

• Body aches or pain


• cough


• difficulty with breathing


• ear congestion


• fever


• headache


• loss of voice


• nasal congestion


• runny nose


• sneezing


• sore throat


• unusual tiredness or weakness

Rare

• Fever over 102.2 °F (39 °C)

Incidence not known

• Black, tarry stools


• bleeding gums


• bloating or swelling of the face, arms, hands, lower legs, or feet blood in the urine or stools


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


• decreased movement of the legs


• difficulty with breathing or swallowing


• dizziness


• eye pain


• fast heartbeat


• feeling of discomfort


• general feeling of discomfort or illness


• headache


• hives


• inflammation of the joints


• itching, especially of the feet or hands


• itching, pain, redness, swelling, tenderness, or warmth on the skin


• large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs


• muscle aches


• pinpoint red spots on the skin


• puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue


• rapid weight gain


• rash


• shortness of breath


• swollen lymph glands


• swollen, painful, or tender lymph glands in the neck, armpit, or groin


• tightness in the chest


• tingling of the hands or feet


• reddening of the skin, especially around the ears


• swelling of the eyes, face, or inside of the nose


• unusual bleeding or bruising


• unusual tiredness or weakness (sudden and severe)


• unusual weight gain or loss


• wheezing

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

• Difficulty with moving


• lack or loss of strength


• muscle aching or cramping


• muscle pains or stiffness


• redness, soreness, hard lump, swelling, tenderness, or pain at the injection site


• swollen joints

Less common or rare

• Aches or pain in the joints or muscles


• fever of 101 °F (38.3 °C) or less


• swollen glands


• vague feeling of bodily discomfort

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

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

The information contained in the Thomson Reuters 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 Reuters 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 Reuters 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 REUTERS 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 REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More pneumococcal vaccine polyvalent Intramuscular resources

• Pneumococcal vaccine polyvalent Intramuscular Use in Pregnancy & Breastfeeding
• Pneumococcal vaccine polyvalent Intramuscular Drug Interactions
• Pneumococcal vaccine polyvalent Intramuscular Support Group
• 0 Reviews for Pneumococcal vaccine polyvalent Intramuscular - Add your own review/rating

Compare pneumococcal vaccine polyvalent Intramuscular with other medications

• Pneumococcal Disease Prophylaxis

Fesoterodine

fes-oh-TER-oh-deen

Commonly used brand name(s)

In the U.S.

• Toviaz

Available Dosage Forms:

• Tablet, Extended Release

Pharmacologic Class: Antimuscarinic

Uses For fesoterodine

Fesoterodine is used to treat symptoms of an overactive bladder, such as incontinence (loss of bladder control) or a frequent need to urinate.

fesoterodine is available only with your doctor's prescription.

Before Using fesoterodine

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 fesoterodine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to fesoterodine 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 have not been performed on the relationship of age to the effects of fesoterodine in the pediatric population. 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 fesoterodine in the elderly. However, elderly patients are more likely to have unwanted side effects (e.g., constipation, dizziness, dry mouth, upset stomach, or urinary tract infection), or age-related liver or kidney problems, which may require caution in patients receiving fesoterodine.

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

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 fesoterodine, 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 fesoterodine 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.

• Clarithromycin


• Erythromycin


• Itraconazole


• Ketoconazole


• Rifampin

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 fesoterodine. Make sure you tell your doctor if you have any other medical problems, especially:

• Glaucoma, narrow-angle or


• Intestinal or stomach problems (e.g., severe constipation) or


• Myasthenia gravis (severe muscle weakness) or


• Urinary problems (e.g., blockage)—Use with caution. May make these conditions worse.

• Glaucoma, narrow-angle, uncontrolled or


• Liver disease, severe or


• Stomach problems (e.g., gastric retention) or


• Urinary retention—Should not be used in patients with these conditions.

• Kidney disease or


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

Proper Use of fesoterodine

Take fesoterodine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

fesoterodine comes with a patient information insert. Read and follow the instructions in the insert carefully. Ask your doctor if you have any questions.

fesoterodine may be taken with or without food.

Swallow the extended-release tablet whole with a full glass of water. Do not split, crush, or chew it.

Dosing

The dose of fesoterodine 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 fesoterodine. 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.

• For oral dosage form (extended-release tablets):
  
  • For bladder problems:
    
    • Adults—At first, 4 milligrams (mg) once a day. Your doctor may increase your dose if needed. However, the dose is usually not more than 8 mg once a day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

If you miss a dose of fesoterodine, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

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.

Precautions While Using fesoterodine

It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to take it.

fesoterodine may make you sweat less, causing your body temperature to increase. Use extra care not to become overheated during exercise or hot weather while you are taking fesoterodine, since overheating may result in heat stroke.

Avoid drinking alcohol while you are taking fesoterodine.

fesoterodine may cause some people to become dizzy, drowsy, or have blurred vision. Make sure you know how you react to fesoterodine before you drive, use machines, or do anything else that could be dangerous if you are dizzy, not alert, or not able to see well.

fesoterodine may cause dryness of the mouth, nose, and throat. For temporary relief of mouth dryness, use sugarless candy or gum, melt bits of ice in your mouth, or use a saliva substitute. However, if your mouth continues to feel dry for more than 2 weeks, check with your medical doctor or dentist. Continuing dryness of the mouth may increase the chance of dental disease, including tooth decay, gum disease, and fungus infections.

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.

fesoterodine 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

• Difficulty having a bowel movement (stool)


• dry mouth

Less common

• Bladder pain


• bloating or swelling of the face, arms, hands, lower legs, or feet


• bloody or cloudy urine


• body aches or pain


• burning while urinating


• chills


• cough


• decrease in frequency of urination


• decrease in urine volume


• difficult, burning, or painful urination


• difficulty in breathing


• difficulty in passing urine (dribbling)


• dry eyes


• ear congestion


• fever


• frequent urge to urinate


• headache


• loss of voice


• lower back or side pain


• nasal congestion


• rapid weight gain


• runny nose


• sneezing


• sore throat


• tingling of the hands or feet


• unusual tiredness or weakness


• unusual weight gain or loss

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:

Less common

• Acid or sour stomach


• back pain


• belching


• dry throat


• heartburn


• indigestion


• nausea


• rash


• sleeplessness


• stomach discomfort, upset, or pain


• trouble sleeping


• unable to sleep


• upper abdominal pain

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

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: fesoterodine side effects (in more detail)

The information contained in the Thomson Reuters 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 Reuters 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 Reuters 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 REUTERS 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 REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More fesoterodine resources

• Fesoterodine Side Effects (in more detail)
• Fesoterodine Use in Pregnancy & Breastfeeding
• Fesoterodine Drug Interactions
• Fesoterodine Support Group
• 18 Reviews for Fesoterodine - Add your own review/rating

• Fesoterodine MedFacts Consumer Leaflet (Wolters Kluwer)


• Fesoterodine Fumarate Monograph (AHFS DI)


• Toviaz Prescribing Information (FDA)


• Toviaz Consumer Overview

Compare fesoterodine with other medications

• Overactive Bladder
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Penlac

ciclopirox

Dosage Form: Nail Lacquer

For use on fingernails and toenails and immediately adjacent skin only

Not for use in eyes

Penlac Description

Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, contains a synthetic antifungal agent, ciclopirox. It is intended for topical use on fingernails and toenails and immediately adjacent skin.

Each gram of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, contains 80 mg ciclopirox in a solution base consisting of ethyl acetate, NF; isopropyl alcohol, USP; and butyl monoester of poly[methylvinyl ether/maleic acid] in isopropyl alcohol. Ethyl acetate and isopropyl alcohol are solvents that vaporize after application.

Penlac ®NAIL LACQUER (ciclopirox) Topical Solution, 8%, is a clear, colorless to slightly yellowish solution.

The chemical name for ciclopirox is 6-cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone, with the empirical formula C12H17NO2 and a molecular weight of 207.27. The CAS Registry Number is [29342-05-0]. The chemical structure is:

Penlac - Clinical Pharmacology

Microbiology

Mechanism of Action

The mechanism of action of ciclopirox has been investigated using various in vitro and in vivo infection models. One in vitro study suggested that ciclopirox acts by chelation of polyvalent cations (Fe+3 or Al+3) resulting in the inhibition of the metal-dependent enzymes that are responsible for the degradation of peroxides within the fungal cell. The clinical significance of this observation is not known.

Activity in vitro and ex vivo

In vitro methodologies employing various broth or solid media with and without additional nutrients have been utilized to determine ciclopirox minimum inhibitory concentration (MIC) values for the dermatophytic molds.(1–2) As a consequence, a broad range of MIC values, 1–20 ug/mL, were obtained for Trichophyton rubrum and Trichophyton mentagrophytes species. Correlation between in vitro MIC results and clinical outcome has yet to be established for ciclopirox.

One ex vivo study was conducted evaluating 8% ciclopirox against new and established Trichophyton rubrum and Trichophyton mentagrophytes infections in ovine hoof material.(3) After 10 days of treatment the growth of T. rubrum and T. mentagrophytes in the established infection model was very minimally affected. Elimination of the molds from hoof material was not achieved in either the new or established infection models.

Susceptibility testing for Trichophyton rubrum species

In vitro susceptibility testing methods for determining ciclopirox MIC values against the dermatophytic molds, including Trichophyton rubrum species, have not been standardized or validated. Ciclopirox MIC values will vary depending on the susceptibility testing method employed, composition and pH of media and the utilization of nutritional supplements. Breakpoints to determine whether clinical isolates of Trichophyton rubrum are susceptible or resistant to ciclopirox have not been established.

Resistance

Studies have not been conducted to evaluate drug resistance development in T. rubrum species exposed to 8% ciclopirox topical solution. Studies assessing cross-resistance to ciclopirox and other known antifungal agents have not been performed.

Antifungal Drug Interactions

No studies have been conducted to determine whether ciclopirox might reduce the effectiveness of systemic antifungal agents for onychomycosis. Therefore, the concomitant use of 8% ciclopirox topical solution and systemic antifungal agents for onychomycosis is not recommended.

Pharmacokinetics

As demonstrated in pharmacokinetic studies in animals and man, ciclopirox olamine is rapidly absorbed after oral administration and completely eliminated in all species via feces and urine. Most of the compound is excreted either unchanged or as glucuronide. After oral administration of 10 mg of radiolabeled drug (14C-ciclopirox) to healthy volunteers, approximately 96% of the radioactivity was excreted renally within 12 hours of administration. Ninety-four percent of the renally excreted radioactivity was in the form of glucuronides. Thus, glucuronidation is the main metabolic pathway of this compound.

Systemic absorption of ciclopirox was determined in 5 patients with dermatophytic onychomycoses, after application of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, to all 20 digits and adjacent 5 mm of skin once daily for six months. Random serum concentrations and 24 hour urinary excretion of ciclopirox were determined at two weeks and at 1, 2, 4 and 6 months after initiation of treatment and 4 weeks post-treatment. In this study, ciclopirox serum levels ranged from 12–80 ng/mL. Based on urinary data, mean absorption of ciclopirox from the dosage form was <5% of the applied dose. One month after cessation of treatment, serum and urine levels of ciclopirox were below the limit of detection.

In two vehicle-controlled trials, patients applied Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, to all toenails and affected fingernails. Out of a total of 66 randomly selected patients on active treatment, 24 had detectable serum ciclopirox concentrations at some point during the dosing interval (range 10.0–24.6 ng/mL). It should be noted that eleven of these 24 patients took concomitant medication containing ciclopirox as ciclopirox olamine (Loprox® Cream, 0.77%).

The penetration of the Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, was evaluated in an in vitro investigation. Radiolabeled ciclopirox applied once to onychomycotic toenails that were avulsed demonstrated penetration up to a depth of approximately 0.4 mm. As expected, nail plate concentrations decreased as a function of nail depth. The clinical significance of these findings in nail plates is unknown. Nail bed concentrations were not determined.

Indications and Usage for Penlac

(To understand fully the indication for this product, please read the entire INDICATIONS AND USAGE section of the labeling.)

Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, as a component of a comprehensive management program, is indicated as topical treatment in immunocompetent patients with mild to moderate onychomycosis of fingernails and toenails without lunula involvement, due to Trichophyton rubrum. The comprehensive management program includes removal of the unattached, infected nails as frequently as monthly, by a health care professional who has special competence in the diagnosis and treatment of nail disorders, including minor nail procedures.

• No studies have been conducted to determine whether ciclopirox might reduce the effectiveness of systemic antifungal agents for onychomycosis. Therefore, the concomitant use of 8% ciclopirox topical solution and systemic antifungal agents for onychomycosis, is not recommended.


• Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be used only under medical supervision as described above.


• The effectiveness and safety of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, in the following populations has not been studied. The clinical trials with use of Penlac®NAIL LACQUER (ciclopirox) Topical Solution, 8%, excluded patients who: were pregnant or nursing, planned to become pregnant, had a history of immunosuppression (e.g., extensive, persistent, or unusual distribution of dermatomycoses, extensive seborrheic dermatitis, recent or recurring herpes zoster, or persistent herpes simplex), were HIV seropositive, received organ transplant, required medication to control epilepsy, were insulin dependent diabetics or had diabetic neuropathy. Patients with severe plantar (moccasin) tinea pedis were also excluded.


• The safety and efficacy of using Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, daily for greater than 48 weeks have not been established.

Clinical Trials Data

The results of use of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, in treatment of onychomycosis of the toenail without lunula involvement were obtained from two double-blind, placebo-controlled studies conducted in the US. In these studies, patients with onychomycosis of the great toenails without lunula involvement were treated with ciclopirox topical solution, 8% in conjunction with monthly removal of the unattached, infected toenail by the investigator. Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, was applied for 48 weeks. At baseline, patients had 20–65% involvement of the target great toenail plate. Statistical significance was demonstrated in one of two studies for the endpoint "complete cure" (clear nail and negative mycology), and in two studies for the endpoint "almost clear" (≤10% nail involvement and negative mycology) at the end of study. These results are presented below.

At Week 48 (plus Last Observation Carried Forward) for the Intent-to-Treat (ITT) Population

	Study 312		Study 313
	Active	Vehicle	Active	Vehicle
* Clear nail and negative mycology † ≤10% nail involvement and negative mycology ‡ Negative KOH and negative culture
Complete Cure*	6/110 (5.5%)	1/109 (0.9%)	10/118 (8.5%)	0/117 (0%)
Almost Clear†	7/107 (6.5%)	1/108 (0.9%)	14/116 (12%)	1/115 (0.9%)
Negative Mycology Alone‡	30/105 (29%)	12/106 (11%)	41/115 (36%)	10/114 (9%)

The summary of reported patient outcomes for the ITT population at 12 weeks following the end of treatment are presented below. Note that post-treatment efficacy assessments were scheduled only for patients who achieved a complete cure.

Post-treatment Week 12 Data for Patients Who Achieved Complete Cure at Week 48

	Study 312		Study 313
	Active	Vehicle	Active	Vehicle
* Four patients (from studies 312 and 313) who were completely cured did not have post-treatment Week 12 planimetry data.
Number of Treated Patients	112	111	119	118
Complete Cure at Week 48	6	1	10	0
Post-treatment Week 12 Outcomes:
Patients Missing All Week 12 Assessments	2	0	2	0
Patients with Week 12 Assessments	4	1	8	0
Complete Cure	3	1	4	0
Almost Clear	2*	1	1*	0
Negative Mycology	3	1	5	0

Contraindications

Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, is contraindicated in individuals who have shown hypersensitivity to any of its components.

Warnings

Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, is not for ophthalmic, oral, or intravaginal use. For use on nails and immediately adjacent skin only.

Precautions

If a reaction suggesting sensitivity or chemical irritation should occur with the use of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, treatment should be discontinued and appropriate therapy instituted.

So far there is no relevant clinical experience with patients with insulin dependent diabetes or who have diabetic neuropathy. The risk of removal of the unattached, infected nail, by the health care professional and trimming by the patient should be carefully considered before prescribing to patients with a history of insulin dependent diabetes mellitus or diabetic neuropathy.

Information for Patients

Patients should have detailed instructions regarding the use of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, as a component of a comprehensive management program for onychomycosis in order to achieve maximum benefit with the use of this product.

The patient should be told to:

1. Use Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, as directed by a health care professional. Avoid contact with the eyes and mucous membranes. Contact with skin other than skin immediately surrounding the treated nail(s) should be avoided. Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, is for external use only.


2. Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be applied evenly over the entire nail plate and 5 mm of surrounding skin. If possible, Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be applied to the nail bed, hyponychium, and the under surface of the nail plate when it is free of the nail bed (e.g., onycholysis). Contact with the surrounding skin may produce mild, transient irritation (redness).


3. Removal of the unattached, infected nail, as frequently as monthly, by a health care professional is needed with use of this medication. Inform a health care professional if they have diabetes or problems with numbness in your toes or fingers for consideration of the appropriate nail management program.


4. Inform a health care professional if the area of application shows signs of increased irritation (redness, itching, burning, blistering, swelling, oozing).


5. Up to 48 weeks of daily applications with Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, and professional removal of the unattached, infected nail, as frequently as monthly, are considered the full treatment needed to achieve a clear or almost clear nail (defined as 10% or less residual nail involvement).


6. Six months of therapy with professional removal of the unattached, infected nail may be required before initial improvement of symptoms is noticed.


7. A completely clear nail may not be achieved with use of this medication. In clinical studies less than 12% of patients were able to achieve either a completely clear or almost clear toenail.


8. Do not use the medication for any disorder other than that for which it is prescribed.


9. Do not use nail polish or other nail cosmetic products on the treated nails.


10. Avoid use near heat or open flame, because product is flammable.

Carcinogenesis, Mutagenesis, Impairment of Fertility

No carcinogenicity study was conducted with Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, formulation. A carcinogenicity study of ciclopirox (1% and 5% solutions in polyethylene glycol 400) in female mice dosed topically twice per week for 50 weeks followed by a 6-month drug-free observation period prior to necropsy revealed no evidence of tumors at the application sites.

In human systemic tolerability studies following daily application (~340 mg of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%) in subjects with distal subungual onychomycosis, the average maximal serum level of ciclopirox was 31±28 ng/mL after two months of once daily applications. This level was 159 times lower than the lowest toxic dose and 115 times lower than the highest nontoxic dose in rats and dogs fed 7.7 and 23.1 mg ciclopirox (as ciclopirox olamine)/kg/day.

The following in vitro genotoxicity tests have been conducted with ciclopirox: evaluation of gene mutation in Ames Salmonella and E. coli assays (negative); chromosome aberration assays in V79 Chinese hamster lung fibroblasts, with and without metabolic activation (positive); gene mutation assay in the HGPRT-test with V79 Chinese hamster lung fibroblasts (negative); unscheduled DNA synthesis in human A549 cells (negative); and BALB/c3T3 cell transformation assay (negative). In an in vivo Chinese hamster bone marrow cytogenetic assay, ciclopirox was negative for chromosome aberrations at 5,000 mg/kg.

The following in vitro genotoxicity tests were conducted with Penlac ®NAIL LACQUER (ciclopirox) Topical Solution, 8%: Ames Salmonella test (negative); unscheduled DNA synthesis in the rat hepatocytes (negative); cell transformation assay in BALB/c3T3 cell assay (positive). The positive response of the lacquer formulation in the BALB/c3T3 test was attributed to its butyl monoester of poly[methylvinyl ether/maleic acid] resin component (Gantrez® ES-435), which also tested positive in this test. The cell transformation assay may have been confounded because of the film-forming nature of the resin. Gantrez® ES-435 tested nonmutagenic in both the in vitro mouse lymphoma forward mutation assay with or without activation and unscheduled DNA synthesis assay in rat hepatocytes.

Oral reproduction studies in rats at doses up to 3.85 mg ciclopirox (as ciclopirox olamine)/kg/day [equivalent to approximately 1.4 times the potential exposure at the maximum recommended human topical dose (MRHTD)] did not reveal any specific effects on fertility or other reproductive parameters. MRHTD (mg/m2) is based on the assumption of 100% systemic absorption of 27.12 mg ciclopirox (~340 mg Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%) that will cover all the fingernails and toenails including 5 mm proximal and lateral fold area plus onycholysis to a maximal extent of 50%.

Pregnancy

Teratogenic effects: Pregnancy Category B

Teratology studies in mice, rats, rabbits, and monkeys at oral doses of up to 77, 23, 23, or 38.5 mg, respectively, of ciclopirox as ciclopirox olamine/kg/day (14, 8, 17, and 28 times MRHTD), or in rats and rabbits receiving topical doses of up to 92.4 and 77 mg/kg/day, respectively (33 and 55 times MRHTD), did not indicate any significant fetal malformations.

There are no adequate or well-controlled studies of topically applied ciclopirox in pregnant women. Penlac ®NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Since many drugs are excreted in human milk, caution should be exercised when Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, is administered to a nursing woman.

Pediatric Use

Based on the safety profile in adults, Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8% is considered safe for use in children twelve years and older. No clinical trials have been conducted in the pediatric population.

Geriatric Use

Clinical studies of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between elderly and younger patients.

Adverse Reactions

In the vehicle-controlled clinical trials conducted in the US, 9% (30/327) of patients treated with Penlac ®NAIL LACQUER (ciclopirox) Topical Solution, 8%, and 7% (23/328) of patients treated with vehicle reported treatment-emergent adverse events (TEAE) considered by the investigator to be causally related to the test material.

The incidence of these adverse events, within each body system, was similar between the treatment groups except for Skin and Appendages: 8% (27/327) and 4% (14/328) of subjects in the ciclopirox and vehicle groups reported at least one adverse event, respectively. The most common were rash-related adverse events: periungual erythema and erythema of the proximal nail fold were reported more frequently in patients treated with Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, (5% [16/327]) than in patients treated with vehicle (1% [3/328]). Other TEAEs thought to be causally related included nail disorders such as shape change, irritation, ingrown toenail, and discoloration.

The incidence of nail disorders was similar between the treatment groups (2% [6/327] in the Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, group and 2% [7/328] in the vehicle group). Moreover, application site reactions and/or burning of the skin occurred in 1% of patients treated with Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, (3/327) and vehicle (4/328).

A 21-Day Cumulative Irritancy study was conducted under conditions of semi-occlusion. Mild reactions were seen in 46% of patients with the Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, 32% with the vehicle and 2% with the negative control, but all were reactions of mild transient erythema. There was no evidence of allergic contact sensitization for either the Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, or the vehicle base. In a separate study of the photosensitization potential of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8% in a maximized test design that included the occluded application of sodium lauryl sulfate, no photoallergic reactions were noted. In four subjects localized allergic contact reactions were observed. In the vehicle-controlled studies, one patient treated with Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, discontinued treatment due to a rash, localized to the palm (causal relation to test material undetermined).

Use of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, for 48 additional weeks was evaluated in an open-label extension study conducted in patients previously treated in the vehicle-controlled studies. Three percent (9/281) of subjects treated with Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, experienced at least one TEAE that the investigator thought was causally related to the test material. Mild rash in the form of periungual erythema (1% [2/281]) and nail disorders (1% [4/281]) were the most frequently reported. Four patients discontinued because of TEAEs. Two of the four had events considered to be related to test material: one patient's great toenail "broke away" and another had an elevated creatine phosphokinase level on Day 1 (after 48 weeks of treatment with vehicle in the previous vehicle-controlled study).

Penlac Dosage and Administration

Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be used as a component of a comprehensive management program for onychomycosis. Removal of the unattached, infected nail, as frequently as monthly, by a health care professional, weekly trimming by the patient, and daily application of the medication are all integral parts of this therapy. Careful consideration of the appropriate nail management program should be given to patients with diabetes (see PRECAUTIONS).

Nail Care By Health Care Professionals

Removal of the unattached, infected nail, as frequently as monthly, trimming of onycholytic nail, and filing of excess horny material should be performed by professionals trained in treatment of nail disorders.

Nail Care By Patient

Patients should file away (with emery board) loose nail material and trim nails, as required, or as directed by the health care professional, every seven days after Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, is removed with alcohol.

Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be applied once daily (preferably at bedtime or eight hours before washing) to all affected nails with the applicator brush provided. The Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be applied evenly over the entire nail plate.

If possible, Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be applied to the nail bed, hyponychium, and the under surface of the nail plate when it is free of the nail bed (e.g., onycholysis).

The Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, should not be removed on a daily basis. Daily applications should be made over the previous coat and removed with alcohol every seven days. This cycle should be repeated throughout the duration of therapy.

How is Penlac Supplied

Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, is supplied in 3.3 mL (NDC 0066-8008-01) and 6.6 mL (NDC 0066-8008-02) glass bottles with screw caps which are fitted with brushes.

Protect from light (e.g., store the bottle in the carton after every use).

Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, should be stored at room temperature between 59° and 86° F (15° and 30° C).

CAUTION: Flammable. Keep away from heat and flame.

Prescribing Information as of July 2006.

Dermik Laboratories

a business of sanofi-aventis U.S. LLC

Bridgewater, NJ 08807

Country of Origin: Germany

References

1. Dittmar W., Lohaus G. 1973. HOE296, A new antimycotic compound with a broad antimicrobial spectrum. Arzneim-Forsch./Drug Res. 23:670–674.


2. Niewerth et. al., 1998. Antimicrobial susceptibility testing of dermatophytes: Comparison of the agar macrodilution and broth micro dilution tests. Chemotherapy. 44:31–35.


3. Yang et. al. 1997. A new simulation model for studying in vitro topical penetration of antifungal drugs into hard keratin. J. Mycol. Med. 7:195–98.

Gantrez is a registered trademark of GAF Corporation

©2006 sanofi-aventis U.S. LLC

Penlac® NAIL LACQUER

(ciclopirox)

Topical Solution, 8%

Patient Information and Instructions

Patients should have detailed instructions regarding the use of Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, as a component of a comprehensive management program for onychomycosis in order to achieve maximum benefit with the use of this product. Discuss your treatment plan with your health care professional for regular removal of the unattached, infected nail.

Before using this medication, tell your doctor if you:

• Are pregnant or nursing


• Are an insulin dependent diabetic or have diabetic neuropathy


• Have a history of immunosuppression


• Are immunocompromised (e.g., received an organ transplant, etc.)


• Require medication to control epilepsy


• Use or require topical corticosteroids on a repeated monthly basis


• Use steroid inhalers on a regular basis

Patient Information:

• Use Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, as directed by your health care professional.


• Penlac ®NAIL LACQUER (ciclopirox) Topical Solution, 8%, is for external use only.


• Contact with skin other than skin immediately surrounding the treated nail(s) should be avoided.


• Avoid contact with the eyes and mucous membranes.


• Removal of the unattached, infected nail, as frequently as monthly, by your health care professional is needed with use of this medication to obtain maximal benefit with use of this product. If you have diabetes or problems with numbness in your toes or fingers, talk to your health care provider before trimming your nails or removing any nail material.


• Inform your health care professional if the area of application shows signs of increased irritation (redness, itching, burning, blistering, swelling, oozing).


• Up to 48 weeks of daily applications with Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, and professional removal, as frequently as monthly, of the unattached, infected nail are considered the full treatment time to achieve a clear or almost clear nail (defined as 10% or less residual nail involvement). Six months of therapy with professional removal of the unattached, infected nail may be required before initial improvement of symptoms is noticed.


• A completely clear nail may not be achieved with use of this medication. In clinical studies less than 12% of patients were able to achieve either a clear or almost clear toenail.


• Do not use nail polish or other nail cosmetic products on the treated nails.


• Avoid use near heat or open flame, because product is flammable.

Patient Instructions

1. Before starting treatment, remove any loose nail or nail material using nail clippers or nail files. If you have diabetes or problems with numbness in your toes or fingers, talk to your health care provider before trimming your nails or removing any nail material.

2.

Apply Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, once daily (preferably at bedtime) to all affected nails with the applicator brush provided. Apply the lacquer evenly over the entire nail. Where possible, nail lacquer should also be applied to the underside of the nail and to the skin beneath it. Allow lacquer to dry (approximately 30 seconds) before putting on socks or stockings. After applying medication, wait 8 hours before taking a bath or shower.

3.

Apply Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, daily over the previous coat.

	4. Once a week, remove the Penlac® NAIL LACQUER (ciclopirox) Topical Solution, 8%, with alcohol. Remove as much as possible of the damaged nail using scissors, nail clippers, or nail files. 5. Repeat process (steps 2 through 4).

	Please Note: 1. To prevent screw cap from sticking to the bottle, do not allow solution to get into the bottle threads. 2. To prevent the solution from drying out, bottle should be closed tightly after every use. 3. To protect from light, replace bottle into carton after each use.

Prescribing Information as of July 2006.

Dermik Laboratories

a division of sanofi-aventis U.S. LLC

Bridgewater, NJ 08807

Country of Origin: Germany

©2006 sanofi-aventis U.S. LLC

Penlac  ciclopirox  solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0066-8008 Route of Administration TOPICAL DEA Schedule

INGREDIENTS Name (Active Moiety) Type Strength ciclopirox (ciclopirox) Active 80 MILLIGRAM  In 1 MILLILITER ethyl acetate Inactive   isopropyl alcohol Inactive   butyl monoester of polymethylvinyl ether/maleic acid Inactive

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0066-8008-01 3.3 mL (MILLILITER) In 1 BOTTLE, WITH APPLICATOR None 2 0066-8008-02 6.6 mL (MILLILITER) In 1 BOTTLE, WITH APPLICATOR None

Revised: 02/2009Dermik Laboratories

More Penlac resources

• Penlac Side Effects (in more detail)
• Penlac Use in Pregnancy & Breastfeeding
• Penlac Support Group
• 1 Review for Penlac - Add your own review/rating

Compare Penlac with other medications

• Onychomycosis, Fingernail
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Phenchlor Tannate Pediatric

Generic Name: chlorpheniramine and phenylephrine (KLOR fen IR a meen and FEN il EFF rin)

Brand Names: Actifed Cold & Allergy, Allan Tannate Pediatric, Allerest PE, AlleRx, BP Allergy JR, C Phen, Cardec, Ceron, Chlor-Mes Jr, ChlorTan D, Cold & Allergy Relief, CP Dec, Dallergy Drops, Dallergy-JR, Dec-Chlorphen, Ed A-Hist, Ed ChlorPed D, Histadec, Nasohist Pediatric, NoHist, Ny-Tannic, PD-Hist D, PD-Hist D Drops, PediaTan D, Phenchlor Tannate Pediatric, R-Tanna, Relera, Rinate Pediatric, Rondec, Rondex, Rynatan, Rynatan Pediatric, Sildec-PE, Sinus & Allergy Maximum Strength, Sinus & Allergy PE, Sonahist, Sudafed PE Sinus & Allergy, Tanahist-D, Triaminic Cold & Allergy

What is Phenchlor Tannate Pediatric (chlorpheniramine and phenylephrine)?

Chlorpheniramine is an antihistamine that reduces the natural chemical histamine in the body. Histamine can produce symptoms of sneezing, itching, watery eyes, and runny nose.

Phenylephrine is a decongestant that shrinks blood vessels in the nasal passages. Dilated blood vessels can cause nasal congestion (stuffy nose).

The combination of chlorpheniramine and phenylephrine is used to treat symptoms of the common cold or seasonal allergies, including sneezing, runny or stuffy nose, and itchy, watery eyes.

Chlorpheniramine and phenylephrine may also be used for purposes not listed in this medication guide.

What is the most important information I should know about Phenchlor Tannate Pediatric (chlorpheniramine and phenylephrine)?

There are many brands and forms of this medication available and not all brands are listed on this leaflet.

Do not use chlorpheniramine and phenylephrine if you have used an MAO inhibitor such as furazolidone (Furoxone), isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam, Zelapar), or tranylcypromine (Parnate) in the last 14 days. A dangerous drug interaction could occur, leading to serious side effects. You should not use this medication if you are allergic to chlorpheniramine or phenylephrine, or if you have severe high blood pressure or coronary artery disease, narrow-angle glaucoma, a stomach ulcer, or if you are unable to urinate.

Do not use this medication during an asthma attack.

This medication may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert. Drinking alcohol can increase certain side effects of chlorpheniramine and phenylephrine. Older adults may be more likely to have side effects from this medicine. Do not give this medication to a child younger than 4 years old. Always ask a doctor before giving a cough or cold medicine to a child. Death can occur from the misuse of cough and cold medicines in very young children.

Talk with your doctor if your symptoms do not improve after 7 days of treatment, or if you have a fever with a headache, cough, or skin rash.

What should I discuss with my healthcare provider before taking Phenchlor Tannate Pediatric (chlorpheniramine and phenylephrine)?

Do not use chlorpheniramine and phenylephrine if you have used an MAO inhibitor such as furazolidone (Furoxone), isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam, Zelapar), or tranylcypromine (Parnate) in the last 14 days. A dangerous drug interaction could occur, leading to serious side effects. You should not use this medication if you are allergic to chlorpheniramine or phenylephrine, or if you have:

• 
  

  severe or uncontrolled high blood pressure;

  
  


• 
  

  severe coronary artery disease;

  
  


• 
  

  narrow angle glaucoma;

  
  


• 
  

  a stomach ulcer;

  
  


• 
  

  if you are unable to urinate; or

  
  


• 
  

  if you are having an asthma attack.

  
  

Ask a doctor or pharmacist if it is safe for you to take this medication if you have:

• kidney disease;


• liver disease;


• 
  

  diabetes;

  
  


• 
  

  glaucoma;

  
  


• 
  

  circulation problems;

  
  


• 
  

  heart disease or high blood pressure;

  
  


• 
  

  overactive thyroid;

  
  


• 
  

  a seizure disorder such as epilepsy;

  
  


• 
  

  asthma, emphysema or chronic bronchitis; or

  
  


• 
  

  urination problems or an enlarged prostate.

  
  

It is not known whether chlorpheniramine and phenylephrine is harmful to an unborn baby. Do not take this medication with a doctor's advice if you are pregnant. It is not known whether chlorpheniramine and phenylephrine 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. Older adults may be more likely to have side effects from this medicine.

Artificially sweetened liquid cold medicine may contain phenylalanine. If you have phenylketonuria (PKU), check the medication label to see if the product contains phenylalanine.

How should I take Phenchlor Tannate Pediatric (chlorpheniramine and phenylephrine)?

Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Cold medicine is usually taken only for a short time until your symptoms clear up.

Do not give this medication to a child younger than 4 years old. Always ask a doctor before giving a cough or cold medicine to a child. Death can occur from the misuse of cough and cold medicines in very young children. Do not crush, chew, break, or open an extended-release tablet or capsule. Swallow it whole. Breaking or opening the pill may cause too much of the drug to be released at one time.

The chewable tablet must be chewed before swallowing.

Measure liquid medicine with a special dose-measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

Talk with your doctor if your symptoms do not improve after 7 days of treatment, or if you have a fever with a headache, cough, or skin rash.

This medication can cause unusual results with allergy skin tests. Tell any doctor who treats you that you are taking an antihistamine.

If you need surgery, tell the surgeon ahead of time if you have taken a cold medicine within the past few days.

Store at room temperature away from moisture and heat.

What happens if I miss a dose?

Since cold medicine is taken as needed, you may not be on a dosing schedule. If you are taking the medication regularly, take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

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

Overdose symptoms may include some of the serious side effects listed in this medication guide.

What should I avoid while taking Phenchlor Tannate Pediatric (chlorpheniramine and phenylephrine)?

This medication may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert. Drinking alcohol can increase certain side effects of chlorpheniramine and phenylephrine. Ask a doctor or pharmacist before using any other cold, allergy, or sleep medicine. Chlorpheniramine and phenylephrine are contained in many combination medicines. Taking certain products together can cause you to get too much of a certain drug. Check the label to see if a medicine contains an antihistamine or decongestant.

Avoid taking this medication if you also take diet pills, caffeine pills, or other stimulants (such as ADHD medications). Taking a stimulant together with a decongestant can increase your risk of unpleasant side effects.

Phenchlor Tannate Pediatric (chlorpheniramine and phenylephrine) side effects

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

• 
  

  fast or pounding heartbeats;

  
  


• 
  

  confusion, hallucinations, unusual thoughts or behavior;

  
  


• 
  

  severe dizziness, anxiety, restless feeling, nervousness;

  
  


• 
  

  urinating less than usual or not at all;

  
  


• 
  

  easy bruising or bleeding, unusual weakness; or

  
  


• 
  

  seizure (black-out or convulsions).

  
  

Less serious side effects may include:

• 
  

  blurred vision;

  
  


• 
  

  dry nose or mouth;

  
  


• 
  

  nausea, stomach pain, constipation, loss of appetite;

  
  


• 
  

  dizziness, drowsiness;

  
  


• 
  

  problems with memory or concentration;

  
  


• 
  

  ringing in your ears; or

  
  


• 
  

  feeling restless or excited (especially in children).

  
  

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.

What other drugs will affect Phenchlor Tannate Pediatric (chlorpheniramine and phenylephrine)?

Before using this medication, tell your doctor if you regularly use other medicines that make you sleepy (such as other cold or allergy medicine, sedatives, narcotic pain medicine, sleeping pills, muscle relaxers, and medicine for seizures, depression, or anxiety). They can add to sleepiness caused by chlorpheniramine.

Tell your doctor about all other medications you use, especially:

• 
  

  mecamylamine (Inversine);

  
  


• 
  

  methyldopa (Aldomet);

  
  


• 
  

  reserpine;

  
  


• 
  

  a beta-blocker such as atenolol (Tenormin, Tenoretic), carvedilol (Coreg), labetalol (Normodyne, Trandate), metoprolol (Lopressor, Toprol), nadolol (Corgard), propranolol (Inderal, InnoPran), sotalol (Betapace), and others;

  
  


• 
  

  a barbiturate such as butabarbital (Butisol), secobarbital (Seconal), pentobarbital (Nembutal), or phenobarbital (Solfoton); or

  
  


• 
  

  an antidepressant such as amitriptyline (Elavil, Vanatrip), doxepin (Sinequan), nortriptyline (Pamelor), and others.

  
  

This list is not complete and other drugs may interact with chlorpheniramine and phenylephrine. 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 Phenchlor Tannate Pediatric resources

• Phenchlor Tannate Pediatric Side Effects (in more detail)
• Phenchlor Tannate Pediatric Use in Pregnancy & Breastfeeding
• Phenchlor Tannate Pediatric Drug Interactions
• 0 Reviews for Phenchlor Tannate Pediatric - Add your own review/rating

• AlleRx Suspension MedFacts Consumer Leaflet (Wolters Kluwer)


• Cardec Drops MedFacts Consumer Leaflet (Wolters Kluwer)


• Dallergy-JR Sustained-Release Capsules MedFacts Consumer Leaflet (Wolters Kluwer)


• Ny-Tannic MedFacts Consumer Leaflet (Wolters Kluwer)


• Relera Controlled-Release Tablets MedFacts Consumer Leaflet (Wolters Kluwer)


• Rondec MedFacts Consumer Leaflet (Wolters Kluwer)


• Rynatan Prescribing Information (FDA)


• Sonahist Prescribing Information (FDA)

Compare Phenchlor Tannate Pediatric with other medications

• Cold Symptoms
• Hay Fever

Where can I get more information?

• Your pharmacist can provide more information about chlorpheniramine and phenylephrine.

See also: Phenchlor Tannate Pediatric side effects (in more detail)