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fluorouracil
Overview
What is Carac?
Carac (fluorouracil cream) Cream, 0.5%, contains fluorouracil for topical dermatologic use. Chemically, fluorouracil is 5-fluoro-2,4(1H, 3H)-pyrimidinedione. The molecular formula is CHFNO. Fluorouracil has a molecular weight of 130.08.
Carac Cream contains 0.5% fluorouracil, with 0.35% being incorporated into a patented porous microsphere (Microsponge) composed of methyl methacrylate/glycol dimethacrylate crosspolymer and dimethicone. The cream formulation contains the following other inactive ingredients: Carbomer Homopolymer Type C, glycerin, methyl gluceth-20, methylparaben, octyl hydroxy stearate, polyethylene glycol 400, polysorbate 80, propylene glycol, propylparaben, purified water, sorbitan monooleate, stearic acid, and trolamine.
What does Carac look like?
What are the available doses of Carac?
Sorry No records found.
What should I talk to my health care provider before I take Carac?
Sorry No records found
How should I use Carac?
Carac is indicated for the topical treatment of multiple actinic or solar keratoses of the face and anterior scalp.
Carac Cream should be applied once a day to the skin where actinic keratosis lesions appear, using enough to cover the entire area with a thin film. Carac Cream should not be applied near the eyes, nostrils, or mouth. Carac Cream should be applied 10 minutes after thoroughly washing, rinsing, and drying the entire area. Carac Cream may be applied using the fingertips. Immediately after application, the hands should be thoroughly washed. Carac Cream should be applied up to 4 weeks as tolerated. Continued treatment up to 4 weeks results in greater lesion reduction. Local irritation is not markedly increased by extending treatment from 2 to 4 weeks, and is generally resolved within 2 weeks of cessation of treatment.
What interacts with Carac?
Fluorouracil may cause fetal harm when administered to a pregnant woman. Fluorouracil is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.
No adequate and well-controlled studies have been conducted in pregnant women with either topical or parenteral forms of fluorouracil. One birth defect (ventricular septal defect) and cases of miscarriage have been reported when fluorouracil was applied to mucous membrane areas. Multiple birth defects have been reported in the fetus of a patient treated with intravenous fluorouracil.
Animal reproduction studies have not been conducted with Carac. Fluorouracil, the active ingredient, has been shown to be teratogenic in mice, rats, and hamsters when administered parenterally at doses greater than or equal to 10, 15, and 33 mg/kg/day, respectively, [4X, 11X and 20X, respectively, the Maximum Recommended Human Dose (MRHD) based on body surface area (BSA)]. Fluorouracil was administered during the period of organogenesis for each species. Embryolethal effects occurred in monkeys at parenteral doses greater than 40 mg/kg/day (65X the MRHD based on BSA) administered during the period of organogenesis.
Carac should not be used in patients with dihydropyrimidine dehydrogenase (DPD) enzyme deficiency. A large percentage of fluorouracil is catabolized by the DPD enzyme. DPD enzyme deficiency can result in shunting of fluorouracil to the anabolic pathway, leading to cytotoxic activity and potential toxicities.
Carac is contraindicated in patients with known hypersensitivity to any of its components.
What are the warnings of Carac?
Flucytosine Capsules must be given with extreme caution to patients with bone marrow depression. Patients may be more prone to depression of bone marrow function if they: 1) have a hematologic disease, 2) are being treated with radiation or drugs which depress bone marrow, or 3) have a history of treatment with such drugs or radiation. Bone marrow toxicity can be irreversible and may lead to death in immunosuppressed patients. Frequent monitoring of hepatic function and of the hematopoietic system is indicated during therapy.
The potential for a delayed hypersensitivity reaction to fluorouracil exists. Patch testing to prove hypersensitivity may be inconclusive.
Patients should discontinue therapy with Carac if symptoms of DPD enzyme deficiency develop.
Rarely, unexpected systemic toxicity (e.g., stomatitis, diarrhea, neutropenia, neurotoxicity) associated with parenteral administration of fluorouracil has been attributed to deficiency of dihydropyrimidine dehydrogenase "DPD" activity. One case of life-threatening systemic toxicity has been reported with the topical use of 5% fluorouracil in a patient with a complete absence of DPD enzyme activity. Symptoms included severe abdominal pain, bloody diarrhea, vomiting, fever, and chills. Physical examination revealed stomatitis, erythematous skin rash, neutropenia, thrombocytopenia, inflammation of the esophagus, stomach, and small bowel. Although this case was observed with 5% fluorouracil cream, it is unknown whether patients with profound DPD enzyme deficiency would develop systemic toxicity with lower concentrations of topically applied fluorouracil.
Applications to mucous membranes should be avoided due to the possibility of local inflammation and ulceration.
What are the precautions of Carac?
General:
There is a possibility of increased absorption through ulcerated or inflamed skin.
Information for the Patient:
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Patients using Carac should receive the following information and instructions:
Laboratory Tests:
To rule out the presence of a frank neoplasm, a biopsy may be considered for those areas failing to respond to treatment or recurring after treatment.
Carcinogenesis, Mutagenesis, and Impairment of Fertility:
Adequate long-term studies in animals to evaluate carcinogenic potential have not been conducted with fluorouracil. Studies with the active ingredient of Carac, fluorouracil, have shown positive effects in and tests for mutagenicity and on impairment of fertility in animal studies.
Fluorouracil produced morphological transformation of cells in cell transformation assays. Morphological transformation was also produced in an assay by a metabolite of fluorouracil, and the transformed cells produced malignant tumors when injected into immunosuppressed syngeneic mice. Fluorouracil has been shown to exert mutagenic activity in yeast cells, , and assays. In addition, fluorouracil has produced chromosome damage at concentrations of 1.0 and 2.0 mcg/mL in an hamster fibroblast assay, was positive in a microwell mouse lymphoma assay, and was positive in micronucleus assays in rats and mice following intraperitoneal administration. Some patients receiving cumulative doses of 0.24 to 1.0 g of fluorouracil parenterally have shown an increase in numerical and structural chromosome aberrations in peripheral blood lymphocytes.
Fluorouracil has been shown to impair fertility after parenteral administration in rats. Fluorouracil administered at intraperitoneal doses of 125 and 250 mg/kg has been shown to induce chromosomal aberrations and changes in chromosome organization of spermatogonia in rats. In mice, single-dose intravenous and intraperitoneal injections of fluorouracil have been reported to kill differentiated spermatogonia and spermatocytes at a dose of 500 mg/kg and produce abnormalities in spermatids at 50 mg/kg.
Pediatric Use:
Actinic keratosis is not a condition seen within the pediatric population, except in association with rare genetic diseases. Carac should not be used in children. The safety and effectiveness of Carac have not been established in patients less than 18 years old.
Geriatric Use:
No significant differences in safety and efficacy measures were demonstrated in patients age 65 and older compared to all other patients.
Pregnancy:
See .
Nursing Women:
It is not known whether fluorouracil is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from fluorouracil, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
What are the side effects of Carac?
The following were adverse events considered to be drug related and occurring with a frequency of ≥1% with Carac: application site reaction (94.6%), and eye irritation (5.4%). The signs and symptoms of facial irritation (i.e., application site reaction) are presented below.
During clinical trials, irritation generally began on Day 4 and persisted for the remainder of treatment. Severity of facial irritation at the last treatment visit was slightly below baseline for the vehicle group, mild to moderate for the 1-week active treatment group, and moderate for the 2- and 4-week active treatment groups. Mean severity declined rapidly for each active group after completion of treatment and was below baseline for each group at the Week 2 post-treatment follow-up visit.
Thirty-one patients (12% of those treated with Carac in the Phase 3 clinical studies) discontinued study treatment early due to facial irritation. Except for three patients, discontinuation of treatment occurred on or after Day 11 of treatment.
Eye irritation adverse events, described as mild to moderate in intensity, were characterized as burning, watering, sensitivity, stinging, and itching. These adverse events occurred across all treatment arms in one of the two Phase 3 studies.
| Clinical Sign or Symptom | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| n | (%) | n | (%) | n | (%) | n | (%) | n | (%) | |
| Erythema | 76 | (89.4) | 82 | (94.3) | 82 | (96.5) | 240 | (93.4) | 76 | (59.8) |
| Dryness | 59 | (69.4) | 76 | (87.4) | 79 | (92.9) | 214 | (83.3) | 60 | (47.2) |
| Burning | 51 | (60.0) | 70 | (80.5) | 71 | (83.5) | 192 | (74.7) | 28 | (22.0) |
| Erosion | 21 | (24.7) | 38 | (43.7) | 54 | (63.5) | 113 | (44.0) | 17 | (13.4) |
| Pain | 26 | (30.6) | 34 | (39.1) | 52 | (61.2) | 112 | (43.6) | 7 | (5.5) |
| Edema | 12 | (14.1) | 28 | (32.2) | 51 | (60.0) | 91 | (35.4) | 6 | (4.7) |
| n (%) | n (%) | n (%) | n (%) | n (%) | ||||||
| BODY AS A WHOLE | 7 | (8.2) | 6 | (6.9) | 12 | (14.1) | 25 | (9.7) | 15 | (11.8) |
| Headache | 3 | (3.5) | 2 | (2.3) | 3 | (3.5) | 8 | (3.1) | 3 | (2.4) |
| Common Cold | 4 | (4.7) | 0 | 2 | (2.4) | 6 | (2.3) | 3 | (2.4) | |
| Allergy | 0 | 2 | (2.3) | 1 | (1.2) | 3 | (1.2) | 2 | (1.6) | |
| Infection UpperRespiratory | 0 | 0 | 0 | 0 | 2 | (1.6) | ||||
| MUSCULOSKELETAL | 1 | (1.2) | 1 | (1.1) | 1 | (1.2) | 3 | (1.2) | 5 | (3.9) |
| Muscle Soreness | 0 | 0 | 0 | 0 | 2 | (1.6) | ||||
| RESPIRATORY | 5 | (5.9) | 0 | 1 | (1.2) | 6 | (2.3) | 6 | (4.7) | |
| Sinusitis | 4 | (4.7) | 0 | 0 | 4 | (1.6) | 2 | (1.6) | ||
| SKIN & APPENDAGES | 78 | (91.8) | 83 | (95.4) | 82 | (96.5) | 243 | (94.6) | 85 | (66.9) |
| Application SiteReaction | 78 | (91.8) | 83 | (95.4) | 82 | (96.5) | 243 | (94.6) | 83 | (65.4) |
| Irritation Skin | 1 | (1.2) | 0 | 2 | (2.4) | 3 | (1.2) | 0 | ||
| SPECIAL SENSES | 6 | (7.1) | 4 | (4.6) | 6 | (7.1) | 16 | (6.2) | 6 | (4.7) |
| Eye Irritation | 5 | (5.9) | 3 | (3.4) | 6 | (7.1) | 14 | (5.4) | 3 | (2.4) |
Adverse Experiences Reported by Body System:
In the Phase 3 studies, no serious adverse event was considered related to study drug. A total of five patients, three in the active treatment groups and two in the vehicle group, experienced at least one serious adverse event. Three patients died as a result of adverse event(s) considered unrelated to study drug (stomach cancer, myocardial infarction, and cardiac failure).
Post-treatment clinical laboratory tests other than pregnancy tests were not performed during the Phase 3 clinical studies. Clinical laboratory tests were performed during conduct of a Phase 2 study of 104 patients and 21 patients in a Phase 1 study. No abnormal serum chemistry, hematology, or urinalysis results in these studies were considered clinically significant.
To report SUSPECTED ADVERSE REACTIONS, contact Valeant Pharmaceuticals North America LLC at 1-800-321-4576 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
What should I look out for while using Carac?
Fluorouracil may cause fetal harm when administered to a pregnant woman. Fluorouracil is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.
No adequate and well-controlled studies have been conducted in pregnant women with either topical or parenteral forms of fluorouracil. One birth defect (ventricular septal defect) and cases of miscarriage have been reported when fluorouracil was applied to mucous membrane areas. Multiple birth defects have been reported in the fetus of a patient treated with intravenous fluorouracil.
Animal reproduction studies have not been conducted with Carac. Fluorouracil, the active ingredient, has been shown to be teratogenic in mice, rats, and hamsters when administered parenterally at doses greater than or equal to 10, 15, and 33 mg/kg/day, respectively, [4X, 11X and 20X, respectively, the Maximum Recommended Human Dose (MRHD) based on body surface area (BSA)]. Fluorouracil was administered during the period of organogenesis for each species. Embryolethal effects occurred in monkeys at parenteral doses greater than 40 mg/kg/day (65X the MRHD based on BSA) administered during the period of organogenesis.
Carac should not be used in patients with dihydropyrimidine dehydrogenase (DPD) enzyme deficiency. A large percentage of fluorouracil is catabolized by the DPD enzyme. DPD enzyme deficiency can result in shunting of fluorouracil to the anabolic pathway, leading to cytotoxic activity and potential toxicities.
Carac is contraindicated in patients with known hypersensitivity to any of its components.
The potential for a delayed hypersensitivity reaction to fluorouracil exists. Patch testing to prove hypersensitivity may be inconclusive.
Patients should discontinue therapy with Carac if symptoms of DPD enzyme deficiency develop.
Rarely, unexpected systemic toxicity (e.g., stomatitis, diarrhea, neutropenia, neurotoxicity) associated with parenteral administration of fluorouracil has been attributed to deficiency of dihydropyrimidine dehydrogenase "DPD" activity. One case of life-threatening systemic toxicity has been reported with the topical use of 5% fluorouracil in a patient with a complete absence of DPD enzyme activity. Symptoms included severe abdominal pain, bloody diarrhea, vomiting, fever, and chills. Physical examination revealed stomatitis, erythematous skin rash, neutropenia, thrombocytopenia, inflammation of the esophagus, stomach, and small bowel. Although this case was observed with 5% fluorouracil cream, it is unknown whether patients with profound DPD enzyme deficiency would develop systemic toxicity with lower concentrations of topically applied fluorouracil.
Applications to mucous membranes should be avoided due to the possibility of local inflammation and ulceration.
What might happen if I take too much Carac?
Ordinarily, topical overdosage will not cause acute problems. If Carac is accidentally ingested, induce emesis and gastric lavage. Administer symptomatic and supportive care as needed. If contact is made with the eye, flush with copious amounts of water.
How should I store and handle Carac?
NDC 0187-5200-30 30 g tube
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
A multiple-dose, randomized, open-label, parallel study was performed in 21 patients with actinic keratoses. Twenty patients had pharmacokinetic samples collected: 10 patients treated with Carac and 10 treated with Efudex 5% Cream. Patients were treated for a maximum of 28 days with Carac, 1 g once daily in the morning; or Efudex 5% Cream, 1 g twice daily, in the morning and evening. Steady-state plasma concentrations and the amounts of fluorouracil in urine resulting from the topical application of either product were measured.
Three patients who received Carac and nine patients who received Efudex 5% Cream had measurable plasma fluorouracil levels; however, only one patient receiving Carac and six patients receiving Efudex 5% Cream had a sufficient number of data points to calculate mean pharmacokinetic parameters.
Five of 10 patients receiving Carac and nine of 10 patients receiving Efudex 5% Cream had measurable urine fuorouracieves.
Both Carac and Efudex 5% Cream demonstrated low measurable plasma concentrations for fluorouracil when administered under steady-state conditions. Cumulative urinary excretion of fluorouracil was low for Carac and for Efudex, corresponding to 0.055% and 0.24% of the applied doses, respectively.
Non-Clinical Toxicology
Fluorouracil may cause fetal harm when administered to a pregnant woman. Fluorouracil is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.No adequate and well-controlled studies have been conducted in pregnant women with either topical or parenteral forms of fluorouracil. One birth defect (ventricular septal defect) and cases of miscarriage have been reported when fluorouracil was applied to mucous membrane areas. Multiple birth defects have been reported in the fetus of a patient treated with intravenous fluorouracil.
Animal reproduction studies have not been conducted with Carac. Fluorouracil, the active ingredient, has been shown to be teratogenic in mice, rats, and hamsters when administered parenterally at doses greater than or equal to 10, 15, and 33 mg/kg/day, respectively, [4X, 11X and 20X, respectively, the Maximum Recommended Human Dose (MRHD) based on body surface area (BSA)]. Fluorouracil was administered during the period of organogenesis for each species. Embryolethal effects occurred in monkeys at parenteral doses greater than 40 mg/kg/day (65X the MRHD based on BSA) administered during the period of organogenesis.
Carac should not be used in patients with dihydropyrimidine dehydrogenase (DPD) enzyme deficiency. A large percentage of fluorouracil is catabolized by the DPD enzyme. DPD enzyme deficiency can result in shunting of fluorouracil to the anabolic pathway, leading to cytotoxic activity and potential toxicities.
Carac is contraindicated in patients with known hypersensitivity to any of its components.
The potential for a delayed hypersensitivity reaction to fluorouracil exists. Patch testing to prove hypersensitivity may be inconclusive.
Patients should discontinue therapy with Carac if symptoms of DPD enzyme deficiency develop.
Rarely, unexpected systemic toxicity (e.g., stomatitis, diarrhea, neutropenia, neurotoxicity) associated with parenteral administration of fluorouracil has been attributed to deficiency of dihydropyrimidine dehydrogenase "DPD" activity. One case of life-threatening systemic toxicity has been reported with the topical use of 5% fluorouracil in a patient with a complete absence of DPD enzyme activity. Symptoms included severe abdominal pain, bloody diarrhea, vomiting, fever, and chills. Physical examination revealed stomatitis, erythematous skin rash, neutropenia, thrombocytopenia, inflammation of the esophagus, stomach, and small bowel. Although this case was observed with 5% fluorouracil cream, it is unknown whether patients with profound DPD enzyme deficiency would develop systemic toxicity with lower concentrations of topically applied fluorouracil.
Applications to mucous membranes should be avoided due to the possibility of local inflammation and ulceration.
Administration of reserpine during therapy with a tricyclic antidepressant has been shown to produce a "stimulating" effect in some depressed patients.
Close supervision and careful adjustment of the dosage are required when nortriptyline hydrochloride is used with other anticholinergic drugs and sympathomimetic drugs.
Concurrent administration of cimetidine and tricyclic antidepressants can produce clinically significant increases in the plasma concentrations of the tricyclic antidepressant. The patient should be informed that the response to alcohol may be exaggerated.
A case of significant hypoglycemia has been reported in a type II diabetic patient maintained on chlorpropamide (250 mg/day), after the addition of nortriptyline (125 mg/day).
There is a possibility of increased absorption through ulcerated or inflamed skin.
The following were adverse events considered to be drug related and occurring with a frequency of ≥1% with Carac: application site reaction (94.6%), and eye irritation (5.4%). The signs and symptoms of facial irritation (i.e., application site reaction) are presented below.
During clinical trials, irritation generally began on Day 4 and persisted for the remainder of treatment. Severity of facial irritation at the last treatment visit was slightly below baseline for the vehicle group, mild to moderate for the 1-week active treatment group, and moderate for the 2- and 4-week active treatment groups. Mean severity declined rapidly for each active group after completion of treatment and was below baseline for each group at the Week 2 post-treatment follow-up visit.
Thirty-one patients (12% of those treated with Carac in the Phase 3 clinical studies) discontinued study treatment early due to facial irritation. Except for three patients, discontinuation of treatment occurred on or after Day 11 of treatment.
Eye irritation adverse events, described as mild to moderate in intensity, were characterized as burning, watering, sensitivity, stinging, and itching. These adverse events occurred across all treatment arms in one of the two Phase 3 studies.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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