Saturday, 18 August 2012

Asparaginase


Class: Antineoplastic Agents
VA Class: AN900
CAS Number: 9015-68-3
Brands: Elspar

Introduction

Antineoplastic agent; enzyme derived from Escherichia coli.108 a


Uses for Asparaginase


Acute Lymphocytic Leukemia (ALL)


Component of combination chemotherapeutic regimens for the treatment of ALL.107 108 109 110 111 112 114 122 123 124 Used in induction and/or intensification (consolidation) regimens.109 110 122 123 124


In non-high-risk childhood ALL, combination therapy with asparaginase (or pegaspargase), a corticosteroid (dexamethasone or prednisone), and vincristine is used as an induction regimen.109 Intensive induction regimens with ≥4 drugs, including asparaginase (or pegaspargase), an anthracycline (e.g., daunorubicin), a corticosteroid, and vincristine, with or without cyclophosphamide, may improve event-free survival but cause greater toxicity.107 109 111 Some clinicians reserve 4-drug regimens for patients with high-risk childhood ALL;107 109 111 others elect to use such regimens for all patients with childhood ALL regardless of presenting features.109


In adults, induction regimens typically include an anthracycline, vincristine, and prednisone; some regimens also add other drugs (e.g., asparaginase, cyclophosphamide).110 122 123


Acute Myeloid Leukemia (AML)


Used in conjunction with high-dose cytarabine as post-induction intensification therapy for AML in patients without a suitable donor for allogeneic bone marrow transplant.117 118


Non-Hodgkin’s Lymphoma


Used in combination with other antineoplastic agents for treatment of non-Hodgkin’s lymphoma† (e.g., lymphoblastic lymphoma).107 110 120


Asparaginase Dosage and Administration


General


Hypersensitivity Reactions



  • Monitor patients for hypersensitivity reactions for 1 hour after administration of asparaginase; be prepared to provide immediate treatment.108 (See Sensitivity Reactions under Cautions.)



Administration


Administer by IM injection, IV infusion, or sub-Q injection†.108 123 126 130


Discard solutions that appear cloudy, discolored, or contain precipitates.108


Vials are for single use only; discard any unused portion.108


Avoid vigorous shaking; may cause foaming and difficulty removing entire contents of vial.121


IM Administration


Administer by IM injection.108


Do not give >2 mL at one injection site.108


Reconstitution

For IM injection, add 2 mL of 0.9% sodium chloride injection to a vial containing 10,000 units of asparaginase to provide a solution containing 5000 units/mL.108


IV Administration


For solution compatibility information, see Compatibility under Stability.


Administer by IV infusion.108


Filter gelatinous fiber-like particles that develop in standing solutions through a 5-mcm filter during administration.108


Reconstitution

Add 5 mL of 0.9% sodium chloride injection or sterile water to a vial containing 10,000 units of asparaginase to provide a solution containing 2000 units/mL.108


Dilution

For IV infusion, dilute dose in either 0.9% sodium chloride or 5% dextrose injection.121


Rate of Administration

Administer dose slowly (over ≥30 minutes) into the tubing of a freely flowing IV solution.108


Dosage


Dosage expressed in terms of international units (IU, units).108


Consult published protocols for optimum dosage and administration sequence of drugs in combination regimens.a


Pediatric Patients


ALL

Discontinue if pancreatitis, serious allergic reaction, or serious thrombotic reaction occurs.108


Induction Therapy

IM or IV

Manufacturer recommends 6000 units/m2 3 times a week.108


Adults


ALL

Discontinue if pancreatitis, serious allergic reaction, or serious thrombotic reaction occurs.108


Induction Therapy

IM

Manufacturer recommends 6000 units/m2 3 times a week.108


Linker regimen: 6000 units/m2 daily on days 17–28 (total of 12 doses) during 4-week induction phase.122


IV

Manufacturer recommends 6000 units/m2 3 times a week.108


Sub-Q†

Larson regimen: 6000 units/m2 for 6 doses (days 5, 8, 11, 15, 18, and 22) during 4-week induction phase.123


Intensification (Consolidation) Phase

IM

Linker regimen: 12,000 units/m2 for 6 doses (days 2, 4, 7, 9, 11, and 14) during cycles 1, 3, 5, and 7 (of a total of 9 cycles administered approximately monthly).122


Sub-Q†

Larson regimen: 6000 units/m2 for 4 doses (days 15, 18, 22, and 25) during each of two 4-week early intensification periods.123


Special Populations


No special population dosage recommendations at this time.108


Cautions for Asparaginase


Contraindications



  • History of serious thrombosis associated with prior asparaginase therapy.108




  • History of pancreatitis with prior asparaginase therapy.108 (See Pancreatitis under Cautions.)




  • History of serious hemorrhagic events associated with prior asparaginase therapy.108




  • History of serious allergic reactions to asparaginase derived from E. coli.108



Warnings/Precautions


Sensitivity Reactions


Hypersensitivity

Potential for severe sensitivity reactions (e.g., anaphylaxis).108 116 117 126 129 Risk of hypersensitivity reactions increases upon reexposure to the drug;108 a more common with IV than with IM administration.116 125 126


If severe hypersensitivity reaction occurs, discontinue immediately and institute appropriate therapy as indicated (e.g., antihistamine, epinephrine, corticosteroids, maintenance of an adequate airway and oxygen).108


Intradermal sensitivity testing has limited value in predicting hypersensitivity; false-positive and false-negative results occur.126


Thrombotic Effects


Thrombotic events (e.g., sagittal sinus thrombosis,101 108 cerebral infarction,101 thrombosis associated with a central venous catheter,122 superficial and deep-vein thrombosis,101 123 130 132 pulmonary embolism123 130 ) have been reported;108 discontinue the drug in patients with serious thrombotic events.108


Coagulopathy


Coagulopathy (e.g., prolonged PT and PTT; decreased fibrinogen, protein C, protein S, and antithrombin III), sometimes severe,108 a and CNS hemorrhage reported.100 101 102 108 121 Alterations in coagulation factors may predispose individuals to bleeding and/or thrombosis.100 101 102 103 108


Perform coagulation tests (e.g., PT, PTT, fibrinogen) at baseline and periodically during and following therapy.108 In patients with severe or symptomatic coagulopathy, initiate treatment with fresh frozen plasma to replace coagulation factors.108


Pancreatitis


Pancreatitis (sometimes fulminant and fatal) reported.108 a


Evaluate patients with abdominal pain for pancreatitis; discontinue the drug in patients with pancreatitis.108


Hyperglycemia


Glucose intolerance, sometimes irreversible, reported.108


Possible hyperglycemia;108 133 monitor blood glucose concentrations.108


Hepatic Effects


Hepatotoxicity (including hepatic failure), liver disorder, and various liver function abnormalities (e.g., elevated AST, ALT, alkaline phosphatase, and bilirubin [direct and indirect]; decreased albumin and fibrinogen) reported;108 a may be fatal in some patients.a Fatty changes in liver documented on biopsy or autopsy.108 a


Hyperbilirubinemia and elevated ALT and AST occur frequently.108 Marked hypoalbuminemia with peripheral edema may occur.108 a


Hepatic abnormalities usually reversible on discontinuance of therapy;108 some reversal may occur with continued therapy.108


Adequate Patient Monitoring


Perform coagulation tests (e.g., fibrinogen concentrations, PT, PTT) at baseline and periodically during and following therapy.108


Monitor serum glucose concentrations.108


Renal Effects


Azotemia, usually prerenal, occurs frequently.108 a


Discontinue at first sign of renal failure.a


Immunologic Effects


Antibodies to asparaginase may develop.108 Antibody-positive patients more likely to experience a hypersensitivity reaction.108 Hypersensitivity reactions associated with increased clearance of asparaginase.108 (See Sensitivity Reactions under Cautions.)


Clinical implications of antibody formation not fully established, but higher levels of antibody associated with decreased asparaginase activity.108 129 In several studies, development of a hypersensitivity reaction did not appear to alter outcome of treatment for ALL; most patients who required discontinuance of the drug were switched to another formulation (Erwinia-derived asparaginase) to complete treatment.129 130


Specific Populations


Pregnancy

Category C.108


Lactation

Not known whether asparaginase is distributed into milk; discontinue nursing or the drug.108


Pediatric Use

Efficacy of combination chemotherapeutic regimens containing asparaginase established in pediatric patients with ALL.108 109


Adult Use

Toxicity of asparaginase generally is greater in adults than in children.116 117 122 a


Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger patients.108


Common Adverse Effects


Allergic reactions,108 116 117 126 129 azotemia,108 a pancreatitis,105 106 108 116 a coagulopathy,108 a hyperglycemia,108 133 CNS thrombosis,101 108 liver function abnormalities (e.g., hyperbilirubinemia, elevated transaminases).108 a


Interactions for Asparaginase


No formal drug interaction studies to date.108


Specific Drugs and Laboratory Tests


















Drug or Test



Interaction



Comments



Methotrexate



Possible decreased effectiveness of methotrexate during period of asparagine suppressiona



Prednisone



Possible increased hyperglycemia133 a



Tests for thyroid function



Decreased serum concentration of thyroxine-binding globulin104



Values return to pretreatment levels within 4 weeks of asparaginase discontinuance104



Vincristine



Possible reduction in hepatic clearance of vincristine135 a


Cumulative neuropathy136 a and disturbances of erythropoiesis if asparaginase and vincristine administered concomitantlya



Manufacturer of vincristine recommends administration of asparaginase 12–24 hours after vincristine135


Consult published protocols for sequence of administration of chemotherapeutic agents in combination regimensa


Asparaginase Pharmacokinetics


Absorption


Bioavailability


Not absorbed from GI tract after oral administration; must be given parenterally.a


Peak plasma concentration attained 14–24 hours after IM administration.108


Distribution


Extent


Following IV administration, apparent volume of distribution is slightly higher than plasma volume.108


Not known whether asparaginase is distributed into milk.108


Crosses blood-brain barrier to a minimal extent.108


Elimination


Half-life


8–30 hours after IV administration.108 a


34–49 hours after IM administration.108


Stability


Storage


Parenteral


Powder for Injection

2–8°C.108


Store reconstituted solutions and solutions diluted for IV infusion at 2–8°C; discard after 8 hours or sooner if solution becomes cloudy.108 121


Compatibility


For information on systemic interactions resulting from concomitant use, see Interactions.


Parenteral


Solution CompatibilityHID






Compatible



Ringer, injection, lactated



Dextrose lcx2 5% in water



Sodium chloride 0.9%


Drug Compatibility





Y-Site CompatibilityHID

Compatible



Methotrexate sodium



Sodium bicarbonate


ActionsActions



  • Inactivates the amino acid asparagine, which is required by tumor cells to synthesize DNA and essential proteins.108 a




  • Resistance to cytotoxic effects of asparaginase develops rapidly.a




  • No apparent cross-resistance between asparaginase and other available antineoplastic agents.a




  • Large foreign protein; therefore, is antigenic and may cause antibody production and varying degrees of hypersensitivity.108 a



Advice to Patients



  • Risk of hypersensitivity reactions, including the possibility of anaphylaxis; importance of patients being monitored for 1 hour after asparaginase administration.108




  • Importance of immediately notifying a clinician if facial swelling, seizures, severe headache, arm or leg swelling, acute shortness of breath, chest pain, or severe abdominal pain occurs.108




  • Importance of immediately notifying a clinician of signs of glucose intolerance (e.g., increased volume or frequency of urination, excessive thirst).108




  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.108




  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.108




  • Importance of informing patients of other important precautionary information.108 (See Cautions.)



Preparations


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.













Asparaginase

Routes



Dosage Forms



Strengths



Brand Names



Manufacturer



Parenteral



For injection



10,000 units



Elspar



Lundbeck



Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.


The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions December 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.


† Use is not currently included in the labeling approved by the US Food and Drug Administration.




References



100. Cairo MS, Lazarus K, Gilmore RL et al. Intracranial hemorrhage and focal seizures secondary to use of l-asparaginase during induction therapy of acute lymphocytic leukemia. J Pediatr. 1980; 97:829-33. [IDIS 127909] [PubMed 6933231]



101. Priest JR, Ramsay NKC, Steinherz PG et al. A syndrome of thrombosis and hemorrhage complicating l-asparaginase therapy for childhood acute lymphoblastic leukemia. J Pediatr. 1982; 100:984-9. [IDIS 157208] [PubMed 6953221]



102. Lederman GS. Stroke due to treatment with l-asparaginase in an adult. N Engl J Med. 1982; 307:1643. [IDIS 161589] [PubMed 7144855]



103. Priest JR, Ramsay NKC, Bennett AJ et al. The effect of l-asparaginase on antithrombin, plasminogen, and plasma coagulation during therapy for acute lymphoblastic leukemia. J Pediatr. 1982; 100:990-5. [IDIS 157209] [PubMed 6953222]



104. Garnick MB, Larsen PR. Acute deficiency of thyroxine-binding globulin during l-asparaginase therapy. N Engl J Med. 1979; 301:252-3. [PubMed 109764]



105. Underwood TW, Frye CB. Drug-induced pancreatitis. Clin Pharm. 1993; 12:440-8. [IDIS 314327] [PubMed 8403815]



106. Mclean R, Martin S, Lan-Po-Tang PRL. Fatal case of l-asparaginase induced pancreatitis. Lancet. 1982; 2:1401-2.



107. Anon. Drugs of choice for cancer. Treat Guidel Med Lett. 2003; 1:41-52.



108. Lundbeck Inc. Elspar (asparaginase) prescribing information. Deerfield, IL; 2010 Feb.



109. Childhood acute lymphoblastic leukemia. From: PDQ. Physician data query (database). Bethesda, MD: National Cancer Institute; 2010 Feb 12.



110. Adult acute lymphoblastic leukemia. From: PDQ. Physician data query (database). Bethesda, MD: National Cancer Institute; 2009 Sep 10.



111. Poplack DG, Magrath IT, Kun LE et al. Leukemias and lymphomas of childhood. In: DeVita VT Jr, Hellman S, Rosenberg SA, eds. Cancer: principles and practice of oncology. 4th ed. Philadelphia: JB Lippincott; 1993:1792-1818.



112. Preti A, Kantarjian HM. Management of adult acute lymphocytic leukemia: present issues and key challenges. J Clin Oncol. 1994; 12:1312-22. [IDIS 331854] [PubMed 8201394]



113. Enzon. Oncaspar (pegaspargase) intravenous or intramuscular injection prescribing information. Bridgewater, NJ; 2006 Sep.



114. Keating MJ, Estey E, Kantarjian H. Acute leukemia. In: DeVita VT Jr, Hellman S, Rosenberg SA, eds. Cancer: principles and practice of oncology. 4th ed. Philadelphia: JB Lippincott; 1993:1938-64.



115. Kurtzberg J. A new look at PEG-L-asparaginase and other asparaginases in hematological malignancies. Cancer Invest. 1994; 12(Suppl 1):59.



116. Capizzi RL, Holcenberg JS. Asparaginase. In: Holland JF, Frei E, Bast RC Jr et al, eds. Cancer medicine. 3rd ed. Philadelphia: Lea & Febiger; 1993:796-805.



117. Childhood acute myeloid leukemia/other myeloid malignancies. From: PDQ. Physician data query (database). Bethesda, MD: National Cancer Institute; 2008 Aug 18.



118. Wells RJ, Woods WG, Lampkin BC et al. Impact of high-dose cytarabine and asparaginase intensification on childhood acute myeloid leukemia: a report from the Childrens Cancer Group. J Clin Oncol. 1993; 11:538-45. [PubMed 8445429]



119. Fragasso G, Pastore MR, Vicari A et al. Myocardial infarction in a patient with acute lymphoblastic leukemia during L-asparaginase therapy. Am J Hematol. 1995; 48:136-7. [PubMed 7847336]



120. Childhood non-Hodgkin lymphoma. From: PDQ. Physician data query (database). Bethesda, MD: National Cancer Institute; 2008 Sep 9.



121. Ovation Pharmaceuticals. Elspar (asparaginase) prescribing information. Deerfield, IL; 2005 Dec.



122. Linker CA, Levitt LJ, O'Donnell M et al. Treatment of adult acute lymphoblastic leukemia with intensive cyclical chemotherapy: a follow-up report. Blood. 1991; 78:2814-22. [PubMed 1835410]



123. Larson RA, Dodge RK, Burns CP et al. A five-drug remission induction regimen with intensive consolidation for adults with acute lymphoblastic leukemia: cancer and leukemia group B study 8811. Blood. 1995; 85:2025-37. [PubMed 7718875]



124. Pui CH, Evans WE. Treatment of acute lymphoblastic leukemia. N Engl J Med. 2006; 354:166-78. [PubMed 16407512]



125. Nesbit M, Chard R, Evans A et al. Evaluation of intramuscular versus intravenous administration of L-asparaginase in childhood leukemia. Am J Pediatr Hematol Oncol. 1979; 1:9-13. [PubMed 295576]



126. Lee C, Gianos M, Klaustermeyer WB. Diagnosis and management of hypersensitivity reactions related to common cancer chemotherapy agents. Ann Allergy Asthma Immunol. 2009; 102:179-87. [PubMed 19354063]



127. Ohnuma T, Holland JF, Freeman A et al. Biochemical and pharmacological studies with asparaginase in man. Cancer Res. 1970; 30:2297-305. [PubMed 4920133]



128. Evans WE, Tsiatis A, Rivera G et al. Anaphylactoid reactions to Escherichia coli and Erwinia asparaginase in children with leukemia and lymphoma. Cancer. 1982; 49:1378-83. [PubMed 7037164]



129. Woo MH, Hak LJ, Storm MC et al. Hypersensitivity or development of antibodies to asparaginase does not impact treatment outcome of childhood acute lymphoblastic leukemia. J Clin Oncol. 2000; 18:1525-32. [PubMed 10735901]



130. Larson RA, Fretzin MH, Dodge RK et al. Hypersensitivity reactions to L-asparaginase do not impact on the remission duration of adults with acute lymphoblastic leukemia. Leukemia. 1998; 12:660-5. [PubMed 9593262]



131. Caruso V, Iacoviello L, Di Castelnuovo A et al. Thrombotic complications in childhood acute lymphoblastic leukemia: a meta-analysis of 17 prospective studies comprising 1752 pediatric patients. Blood. 2006; 108:2216-22. [PubMed 16804111]



132. Caruso V, Iacoviello L, Di Castelnuovo A et al. Venous thrombotic complications in adults undergoing induction treatment for acute lymphoblastic leukemia: results from a meta-analysis. J Thromb Haemost. 2007; 5:621-3. [PubMed 17229043]



133. Lowas SR, Marks D, Malempati S. Prevalence of transient hyperglycemia during induction chemotherapy for pediatric acute lymphoblastic leukemia. Pediatr Blood Cancer. 2009; 52:814-8. [PubMed 19260096]



134. Sarris A, Cortes J, Kantarjian H et al. Disseminated intravascular coagulation in adult acute lymphoblastic leukemia: frequent complications with fibrinogen levels less than 100 mg/dl. Leuk Lymphoma. 1996; 21:85-92. [PubMed 8907274]



135. Hospira Inc. Vincristine sulfate (for injection) prescribing information. Lake Forest, IL; 2007 Dec.



136. Hildebrand J, Kenis Y, Mubashir BA et al. Vincristine neurotoxicity. N Engl J Med. 1972; 287:517.



137. EUSA Pharma (Europe). Products: Erwinase. Available from website. Accessed 2010 May 5.



a. AHFS drug information 2009. McEvoy GK, ed. Asparaginase. Bethesda, MD: American Society of Health-System Pharmacists; 2009: 935–8.



HID. Trissel LA. Handbook on injectable drugs. 14th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2007:176-7.



More Asparaginase resources


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


Compare Asparaginase with other medications


  • Acute Lymphocytic Leukemia

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Thursday, 16 August 2012

Co-Q10



Generic Name: ubiquinone (ue BIK wi none)

Brand Names: Co-Q10, Coenzyme Q10, LiQsorb, Liquid Co-Q10, NutraDrops, QuinZyme


What is Co-Q10 (ubiquinone)?

Ubiquinone, also called Coenzyme Q-10, is a coenzyme that is made naturally in the body.


Ubiquinone has been used in congestive heart failure, gum disease, and type 2 diabetes. It has also been used to replace low levels of ubiquinone caused by taking certain cholesterol medications.


Ubiquinone has not been approved by the FDA to treat any disease, and it should not be substituted for prescription medications.

Ubiquinone may also have uses other than those listed in this product guide.


What is the most important information I should know about Co-Q10 (ubiquinone)?


Ubiquinone has not been approved by the FDA to treat any disease, and it should not be substituted for prescription medications.

Ubiquinone has not been evaluated by the FDA for safety, effectiveness, or purity. All potential risks and/or advantages of this product may not be known. Additionally, there are no regulated manufacturing standards in place for these compounds. Some marketed herbal supplements have been found to be contaminated with toxic metals or other drugs. Herbal/health supplements should be purchased from a reliable source to minimize the risk of contamination.


What should I discuss with my healthcare provider before taking Co-Q10 (ubiquinone)?


Before taking ubiquinone, talk to your doctor, pharmacist, herbalist, or other healthcare provider. You may not be able to use this product if you have:



  • allergies (especially to plants);




  • diabetes; or




  • a blood (platelet) disorder.




Do not take ubiquinone without telling your doctor if you are pregnant or could become pregnant. It is not known whether ubiquinone will be harmful to an unborn baby. Do not take ubiquinone without telling your doctor if you are breast-feeding a baby. It is not known whether ubiquinone will be harmful to a nursing infant. Do not give any herbal/health supplement to a child without a doctor's advice.

How should I take Co-Q10 (ubiquinone)?


Ubiquinone has not been evaluated by the FDA for safety, effectiveness, or purity. All potential risks and/or advantages of this product may not be known. Additionally, there are no regulated manufacturing standards in place for these compounds. Some marketed herbal supplements have been found to be contaminated with toxic metals or other drugs. Herbal/health supplements should be purchased from a reliable source to minimize the risk of contamination.


If you choose to take ubiquinone, use it exactly as directed on the label, or as prescribed by your doctor, pharmacist, or other health care provider.


Take the ubiquinone capsule or tablet with a full glass of water.

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


To take disintegrating tablet, use dry hands to remove the tablet from the package, and place it in your mouth. It will begin to dissolve right away. Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing.


Do not take more of this product than is recommended. Too much medicine could be dangerous.

Store ubiquinone at room temperature, away from light, heat, and moisture. Keep the medicine bottle closed when not in use.


What happens if I miss a dose?


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


What happens if I overdose?


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

What should I avoid while taking Co-Q10 (ubiquinone)?


Follow your healthcare provider's instructions about any restrictions on food, beverages, or activity.


Co-Q10 (ubiquinone) 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.

Less serious side effects are more likely to occur, and you may have none at all.


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 Co-Q10 (ubiquinone)?


The following drugs can interact with ubiquinone. Tell your doctor if you are using any of these:



  • a beta blocker blood pressure medication such as atenolol (Tenormin), carvedilol (Coreg), labetalol (Normodyne, Trandate), metoprolol (Lopressor, Toprol), propranolol (Inderal, InnoPran), sotalol (Betapace), and others;




  • a blood thinner such as warfarin (Coumadin);




  • doxorubicin (Adriamycin); or




  • diabetes medication.



This list is not complete and other drugs may interact with ubiquinone. 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 Co-Q10 resources


  • Co-Q10 Use in Pregnancy & Breastfeeding
  • Co-Q10 Drug Interactions
  • Co-Q10 Support Group
  • 3 Reviews for Co-Q10 - Add your own review/rating


  • Ubiquinone Natural MedFacts for Professionals (Wolters Kluwer)

  • Ubiquinone Natural MedFacts for Consumers (Wolters Kluwer)

  • Coenzyme Q10 Chewable Tablets MedFacts Consumer Leaflet (Wolters Kluwer)

  • Quinzyme MedFacts Consumer Leaflet (Wolters Kluwer)



Compare Co-Q10 with other medications


  • Dietary Supplementation


Where can I get more information?


  • Consult with a licensed healthcare professional before using any herbal/health supplement. Whether you are treated by a medical doctor or a practitioner trained in the use of natural medicines/supplements, make sure all your healthcare providers know about all of your medical conditions and treatments.


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Floxuridine




Floxuridine FOR INJECTION USP

FOR INTRA-ARTERIAL INFUSION ONLY


Rx ONLY.




WARNING


It is recommended that Floxuridine be given only by or under the supervision of a qualified physician who is experienced in cancer chemotherapy and intra-arterial drug therapy and is well versed in the use of potent antimetabolites.


Because of the possibility of severe toxic reactions, all patients should be hospitalized for initiation of the first course of therapy.



Floxuridine Description

Floxuridine for Injection USP, an antineoplastic antimetabolite, is available as a sterile, nonpyrogenic, lyophilized powder for reconstitution. Each vial contains 500 mg of Floxuridine which is to be reconstituted with 5 mL of sterile water for injection. An appropriate amount of reconstituted solution is then diluted with a parenteral solution for intra-arterial infusion (see DOSAGE AND ADMINISTRATION section).


Floxuridine is a fluorinated pyrimidine. Chemically, Floxuridine is 2'-Deoxy-5-fluorouridine, with a molecular formula of C9H11FN2O5. It is a white to off-white odorless solid which is freely soluble in water.


The 2% aqueous solution has a pH of between 4.0 and 5.5. The molecular weight of Floxuridine is 246.20 and the structural formula is:




Floxuridine - Clinical Pharmacology


When Floxuridine is given by rapid intra-arterial injection it is apparently rapidly catabolized to 5-fluorouracil. Thus, rapid injection of Floxuridine produces the same toxic and antimetabolic effects as does 5-fluorouracil. The primary effect is to interfere with the synthesis of deoxyribonucleic acid (DNA) and to a lesser extent inhibit the formation of ribonucleic acid (RNA). However, when Floxuridine is given by continuous intra-arterial infusion its direct anabolism to Floxuridine-monophosphate is enhanced, thus increasing the inhibition of DNA.


Floxuridine is metabolized in the liver. The drug is excreted intact and as urea, fluorouracil, a-fluoro-b-ureidopropionic acid, dihydrofluorouracil, a-fluoro-b-guanidopropionic acid and a-fluoro-b-alanine in the urine; it is also expired as respiratory carbon dioxide. Pharmacokinetic data on intra-arterial infusion of Floxuridine are not available.



Indications and Usage for Floxuridine


Floxuridine is effective in the palliative management of gastrointestinal adenocarcinoma metastatic to the liver, when given by continuous regional intra-arterial infusion in carefully selected patients who are considered incurable by surgery or other means. Patients with known disease extending beyond an area capable of infusion via a single artery should, except in unusual circumstances, be considered for systemic therapy with other chemotherapeutic agents.



Contraindications


Floxuridine therapy is contraindicated for patients in a poor nutritional state, those with depressed bone marrow function or those with potentially serious infections.



Warnings


BECAUSE OF THE POSSIBILITY OF SEVERE TOXIC REACTIONS, ALL PATIENTS SHOULD BE HOSPITALIZED FOR THE FIRST COURSE OF THERAPY.


Floxuridine should be used with extreme caution in poor risk patients with impaired hepatic or renal function or a history of high-dose pelvic irradiation or previous use of alkylating agents. The drug is not intended as an adjuvant to surgery.


Floxuridine may cause fetal harm when administered to a pregnant woman. It has been shown to be teratogenic in the chick embryo, mouse (at doses of 2.5 to 100 mg/kg) and rat (at doses of 75 to 150 mg/kg). Malformations included cleft palates; skeletal defects; and deformed appendages, paws and tails. The dosages which were teratogenic in animals are 4.2 to 125 times the recommended human therapeutic dose.


There are no adequate and well-controlled studies with Floxuridine in pregnant women. If this drug is used during pregnancy or if the patient becomes pregnant while taking (receiving) this drug, the patient should be apprised of the potential hazard to the fetus. Women of childbearing potential should be advised to avoid becoming pregnant.



Combination Therapy


Any form of therapy which adds to the stress of the patient, interferes with nutrition or depresses bone marrow function will increase the toxicity of Floxuridine.



Precautions



General


Floxuridine is a highly toxic drug with a narrow margin of safety. Therefore, patients should be carefully supervised since therapeutic response is unlikely to occur without some evidence of toxicity. Severe hematological toxicity, gastrointestinal hemorrhage and even death may result from the use of Floxuridine despite meticulous selection of patients and careful adjustment of dosage. Although severe toxicity is more likely in poor risk patients, fatalities may be encountered occasionally even in patients in relatively good condition.


Therapy is to be discontinued promptly whenever one of the following signs of toxicity appears:


 

Myocardial ischemia

 

Stomatitis or esophagopharyngitis, at the first visible sign

 

Leukopenia (WBC under 3500) or a rapidly falling white blood count

 

Vomiting, intractable

 

Diarrhea, frequent bowel movements or watery stools

 

Gastrointestinal ulceration and bleeding

 

Thrombocytopenia (platelets under 100,000)

 

Hemorrhage from any site


Information for Patients


Patients should be informed of expected toxic effects, particularly oral manifestations. Patients should be alerted to the possibility of alopecia as a result of therapy and should be informed that it is usually a transient effect.



Laboratory Tests


Careful monitoring of the white blood count and platelet count is recommended.



Drug Interactions


See WARNINGS section.



Carcinogenesis, Mutagenesis, Impairment of Fertility


Carcinogenesis

Long-term studies in animals to evaluate the carcinogenic potential of Floxuridine have not been conducted. On the basis of the available data, no evaluation can be made of the carcinogenic risk of Floxuridine to humans.


Mutagenesis

Oncogenic transformation of fibroblasts from mouse embryo has been induced in vitro by Floxuridine, but the relationship between oncogenicity and mutagenicity is not clear. Floxuridine has also been shown to be mutagenic in human leukocytes in vitro and in the Drosophila test system. In addition, 5-fluorouracil, to which Floxuridine is catabolized when given by intra-arterial injection, has been shown to be mutagenic in in vitro tests.


Impairment of Fertility

The effects of Floxuridine on fertility and general reproductive performance have not been studied in animals. However, because Floxuridine is catabolized to 5-fluorouracil, it should be noted the 5-fluorouracil has been shown to induce chromosomal aberrations and changes in chromosome organization of spermatogonia in rats at doses of 125 or 250 mg/kg, administered intraperitoneally.


Spermatogonial differentiation was also inhibited by fluorouracil, resulting in transient infertility. In female rats, fluorouracil, administered intraperitoneally at doses of 25 or 50 mg/kg during the preovulatory phase of oogenesis, significantly reduced the incidence of fertile matings, delayed the development of pre- and post-implantation embryos, increased the incidence of preimplantation lethality and induced chromosomal anomalies in these embryos. Compounds such as Floxuridine, which interfere with DNA, RNA and protein synthesis, might be expected to have adverse effects on gametogenesis.



Pregnancy


Teratogenic Effects: Pregnancy Category D

See WARNINGS section. Floxuridine has been shown to be teratogenic in the chick embryo, mouse (at doses of 2.5 to 100 mg/kg) and rat (at doses of 75 to 150 mg/kg). Malformations included cleft palates, skeletal defects and deformed appendages, paws and tails. The dosages which were teratogenic in animals were 4.2 to 125 times the recommended human therapeutic dose.


There are no adequate and well-controlled studies with Floxuridine in pregnant women. While there is no evidence of teratogenicity in humans due to Floxuridine, it should be kept in mind that other drugs which inhibit DNA synthesis (e.g., methotrexate and aminopterin) have been reported to be teratogenic in humans. Floxuridine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.


Nonteratogenic Effects

Floxuridine has not been studied in animals for its effects on peri- and postnatal development. However, compounds which inhibit DNA, RNA and protein synthesis might be expected to have adverse effects on peri- and postnatal development.



Nursing Mothers


It is not known whether Floxuridine is excreted in human milk. Because Floxuridine inhibits DNA and RNA synthesis, mothers should not nurse while receiving this drug.



Pediatric Use


Safety and effectiveness in pediatric patients have not been established.



Adverse Reactions


Adverse reactions to the arterial infusion of Floxuridine are generally related to the procedural complications of regional arterial infusion.


The more common adverse reactions to the drug are nausea, vomiting, diarrhea, enteritis, stomatitis and localized erythema. The more common laboratory abnormalities are anemia, leukopenia, thrombo-cytopenia and elevations of alkaline phosphatase, serum transaminase, serum bilirubin and lactic dehydrogenase.


Other adverse reactions are:


Gastrointestinal: duodenal ulcer, duodenitis, gastritis, bleeding, gastroenteritis, glossitis, pharyngitis, anorexia, cramps, abdominal pain; possible intra- and extrahepatic biliary sclerosis, as well as acalculous cholecystitis.


Dermatologic: alopecia, dermatitis, nonspecific skin toxicity, rash.


Cardiovascular: myocardial ischemia.


Miscellaneous Clinical Reactions: fever, lethargy, malaise, weakness.


Laboratory Abnormalities: BSP, prothrombin, total proteins, sedimentation rate and thrombopenia.


Procedural Complications of Regional Arterial Infusion: arterial aneurysm; arterial ischemia; arterial thrombosis; embolism; fibromyositis; thrombophlebitis; hepatic necrosis; abscesses; infection at catheter site; bleeding at catheter site; catheter blocked, displaced or leaking.


The following adverse reactions have not been reported with Floxuridine but have been noted following the administration of 5-fluorouracil. While the possibility of these occurring following Floxuridine therapy is remote because of its regional administration, one should be alert for these reactions following the administration of Floxuridine because of the pharmacological similarity of these two drugs: pancytopenia, agranulocytosis, myocardial ischemia, angina, anaphylaxis, generalized allergic reactions, acute cerebellar syndrome, nystagmus, headache, dry skin, fissuring, photosensitivity, pruritic maculopapular rash, increased pigmentation of the skin, vein pigmentation, lacrimal duct stenosis, visual changes, lacrimation, photophobia, disorientation, confusion, euphoria, epistaxis and nail changes, including loss of nails.



Overdosage


The possibility of overdosage with Floxuridine is unlikely in view of the mode of administration. Nevertheless, the anticipated manifestations would be nausea, vomiting, diarrhea, gastrointestinal ulceration and bleeding, bone marrow depression (including thrombocytopenia, leukopenia and agranulocytosis). No specific antidotal therapy exists. Patients who have been exposed to an overdosage of Floxuridine should be monitored hematologically for at least 4 weeks. Should abnormalities appear, appropriate therapy should be utilized.


The acute intravenous toxicity of Floxuridine is as follows:















 LD50  
Species(mg/kg ± S.E.)
Mouse880 ± 51
Rat670 ± 73
Rabbit94 ± 19.6
Dog157 ± 46

Floxuridine Dosage and Administration


Each vial must be reconstituted with 5 mL of sterile water for injection to yield a solution containing approximately 100 mg of Floxuridine/mL. The calculated daily dose(s) of the drug is then diluted with 5% dextrose or 0.9% sodium chloride injection to a volume appropriate for the infusion apparatus to be used. The administration of Floxuridine is best achieved with the use of an appropriate pump to overcome pressure in large arteries and to ensure a uniform rate of infusion.


Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.


The recommended therapeutic dosage schedule of Floxuridine by continuous arterial infusion is 0.1 to 0.6 mg/kg/day. The higher dosage ranges (0.4 to 0.6 mg) are usually employed for hepatic artery infusion because the liver metabolizes the drug, thus reducing the potential for systemic toxicity.


Therapy can be given until adverse reactions appear. (See PRECAUTIONS section.) When these side effects have subsided, therapy may be resumed. The patient should be maintained on therapy as long as response to Floxuridine continues.


Procedures for proper handling and disposal of anticancer drugs should be considered. Several guidelines on this subject have been published.1-7 There is no general agreement that all of the procedures recommended in the guidelines are necessary or appropriate.



How is Floxuridine Supplied


Floxuridine for Injection USP, 500 mg, lyophilized, in a 5 mL vial, is supplied in individual cartons.


NDC 55390-135-01. This is to be reconstituted with 5 mL sterile water for injection. The sterile powder should be stored at 15° to 30°C (59° to 86°F). Reconstituted vials should be stored under refrigeration 2° to 8°C (36° to 46°F) for not more than 2 weeks.



REFERENCES


  1. Recommendations for the safe handling of parenteral antineoplastic drugs. Washington, DC, US Government Printing Office, NIH publication 83-2621.

  2. AMA Council Report. Guidelines for handling parenteral antineoplastics. JAMA. Mar 15, 1985, 253:1590-1592.

  3. National Study Commission on Cytotoxic Exposure: Recommendation for handling cytotoxic agents. Available from Louis P. Jeffrey, ScD, Director of Pharmacy Services, Rhode Island Hospital, 593 Eddy Street, Providence, Rhode Island 02902.

  4. Clinical Oncological Society of Australia: Guidelines and recommendations for safe handling of antineoplastic agents. Med J Aust. Apr 30, 1983, 1:426-428.

  5. Jones, RB, Frank R, Mass T: Safe handling of chemotherapeutic agents: a report from the Mount Sinai Medical Center. CA. Sept - Oct, 1983, 33:258-263.

  6. American Society of Hospital Pharmacists Technical Assistance Bulletin on Handling Cytotoxic and Hazardous Drugs. AM J Hosp Pharm 1990:47:1033-1049.

  7. Controlling Occupational Exposure to Hazardous Drugs. (OSHA WORK-PRACTICE GUIDELINES). AM J Health-Syst Pharm. 1996:523:1669-1685


Manufactured by:                                                       Manufactured for:


Ben Venue Laboratories Inc.                                       Bedford laboratories™


Bedford, OH 44146                                                    Bedford, OH 44146


February 2000                                                            FLX - P00



VIAL LABEL


Vial Label 500 mg




CARTON


Unit Carton 500 mg










Floxuridine 
Floxuridine  injection, powder, lyophilized, for solution










Product Information
Product TypeHUMAN PRESCRIPTION DRUGNDC Product Code (Source)55390-135
Route of AdministrationINTRA-ARTERIALDEA Schedule    








Active Ingredient/Active Moiety
Ingredient NameBasis of StrengthStrength
Floxuridine (Floxuridine)Floxuridine500 mg  in 5 mL






Inactive Ingredients
Ingredient NameStrength
WATER 


















Product Characteristics
Color    Score    
ShapeSize
FlavorImprint Code
Contains      














Packaging
#NDCPackage DescriptionMultilevel Packaging
155390-135-011 VIAL In 1 BOX, UNIT-DOSEcontains a VIAL
15 mL In 1 VIALThis package is contained within the BOX, UNIT-DOSE (55390-135-01)










Marketing Information
Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
ANDAANDA07538710/16/2000


Labeler - Bedford Laboratories (884528407)









Establishment
NameAddressID/FEIOperations
Ben Venue Laboratories Inc.004327953MANUFACTURE
Revised: 04/2010Bedford Laboratories

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Tuesday, 14 August 2012

clioquinol topical


Generic Name: clioquinol topical (klye oh KWIN all)

Brand Names: Iodo Plain


What is clioquinol topical?

Clioquinol topical is an antifungal and antibacterial medication. Clioquinol topical prevents fungus from growing on your skin.


Clioquinol topical is used to treat skin infections such as eczema, athlete's foot, and other fungal infections.


Clioquinol topical may also be used for purposes other than those listed in this medication guide.


What is the most important information I should know about clioquinol topical?


Use this medication for the full amount of time prescribed by your doctor or as recommended in the package even if you begin to feel better. Your symptoms may improve before the infection is completely healed.

Do not use bandages or dressings that do not allow air to circulate to the affected area (occlusive dressings) unless otherwise directed by your doctor. Wear loose-fitting clothing (preferably cotton).


Avoid getting this medication in your eyes, nose, or mouth.

Who should not use clioquinol topical?


Do not use clioquinol topical if you have had an allergic reaction to it in the past.


It is not known whether clioquinol topical will harm an unborn baby. Do not use clioquinol topical without first talking to your doctor if you are pregnant. It is not known whether clioquinol passes into breast milk. Do not take clioquinol topical without first talking to your doctor if you are breast-feeding a baby.

How should I use clioquinol topical?


Use clioquinol topical exactly as directed by your doctor or follow the directions that accompany the package. If you do not understand these instructions, ask your pharmacist, nurse, or doctor to explain them to you.

Wash your hands before and after using this medication.


Clean and dry the affected area. Apply a small amount of the cream two or three times daily as directed for up to 1 week.


Use this medication for the full amount of time prescribed by your doctor or recommended in the package even if you begin to feel better. Your symptoms may improve before the infection is completely healed.

Do not use clioquinol topical for longer than 1 week without consulting your doctor.


Do not use bandages or dressings that do not allow air circulation over the affected area (occlusive dressings) unless otherwise directed by your doctor. A light cotton-gauze dressing may be used to protect clothing.


Avoid getting this medication in your eyes, nose, or mouth. Store clioquinol topical at room temperature away from moisture and heat.

What happens if I miss a dose?


Apply the missed dose as soon as you remember. However, if it is almost time for your next regularly scheduled dose, skip the dose you missed and apply only the regular amount of clioquinol topical. Do not use a double dose unless otherwise directed by your doctor.


What happens if I overdose?


An overdose of clioquinol topical is unlikely to occur. If you do suspect that a much larger than normal dose has been used or that clioquinol topical has been ingested, contact an emergency room or a poison control center.


What should I avoid while using clioquinol topical?


Avoid wearing tight-fitting, synthetic clothing that doesn't allow air circulation. Wear clothing made of loose cotton and other natural fibers until the infection is healed.


Clioquinol topical side effects


Serious side effects of clioquinol topical use are unexpected. Stop using clioquinol topical and see your doctor if you experience unusual or severe blistering, itching, redness, peeling, dryness, swelling, or irritation of the skin.


Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side effects to FDA at 1-800-FDA-1088.


Clioquinol topical Dosing Information


Usual Adult Dose for Tinea Cruris:

Apply to the affected area 2 to 4 times daily. Do not use for longer than 7 days.

Usual Adult Dose for Tinea Pedis:

Apply to the affected area 2 to 4 times daily. Do not use for longer than 7 days.

Usual Pediatric Dose for Tinea Cruris:

>= 2 years: Apply to the affected area 2 to 4 times daily. Do not use for longer than 7 days.

Usual Pediatric Dose for Tinea Pedis:

>= 2 years: Apply to the affected area 2 to 4 times daily. Do not use for longer than 7 days.


What other drugs will affect clioquinol topical?


Avoid using other topicals at the same time unless your doctor approves. Other skin medications may affect the absorption or effectiveness of clioquinol topical.



More clioquinol topical resources


  • Clioquinol topical Side Effects (in more detail)
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  • Tinea Cruris
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Where can I get more information?


  • Your pharmacist has additional information about clioquinol topical written for health professionals that you may read.

See also: clioquinol side effects (in more detail)


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Monday, 13 August 2012

lidocaine and prilocaine topical


Generic Name: lidocaine and prilocaine topical (LY doh kayn and PRIL oh kayn TOP ik al)

Brand names: Emla, Emla Anesthetic Disc


What is lidocaine and prilocaine topical?

Lidocaine and prilocaine topical is a local anesthetic (numbing medication). It works by blocking nerve signals in your body.


Lidocaine and prilocaine topical is used to numb the skin, or surfaces of the penis or vagina, in preparation for a medical procedure or to lessen the pain of inserting a medical instrument such as a tube or speculum.


Lidocaine and prilocaine topical may also be used for other purposes not listed in this medication guide.


What is the most important information I should know about lidocaine and prilocaine?


An overdose of numbing medications can cause fatal side effects if too much of the medicine is absorbed through your skin and into your blood. This is more likely to occur when using a numbing medicine without the advice of a medical doctor (such as during a cosmetic procedure like laser hair removal). However, overdose has also occurred in women treated with a numbing medicine before having a mammography. Overdose symptoms may include uneven heartbeats, seizure (convulsions), coma, slowed breathing, or respiratory failure (breathing stops). Your body may absorb more of this medication if you use too much, if you apply it over large skin areas, or if you apply heat, bandages, or plastic wrap to treated skin areas. Skin that is cut or irritated may also absorb more topical medication than healthy skin.

Use the smallest amount of this medication needed to numb the skin or relieve pain. Do not use large amounts of lidocaine and prilocaine topical, or cover treated skin areas with a bandage or plastic wrap without medical advice. Be aware that many cosmetic procedures are performed without a medical doctor present.


Do not use lidocaine and prilocaine topical if you have had an allergic reaction to a numbing medicine in the past.

Before lidocaine and prilocaine topical is applied, tell your doctor if you have liver disease, a history of allergic reaction to lidocaine or prilocaine, or a personal or family history of methemoglobinemia, or any genetic enzyme deficiency.


Lidocaine and prilocaine topical is for use only on the surface of your body. Avoid getting this medication in your eyes.

Avoid accidentally injuring treated skin areas while they are numb. Avoid coming into contact with very hot or very cold surfaces.


What should I discuss with my health care provider before using lidocaine and prilocaine topical?


An overdose of numbing medications can cause fatal side effects if too much of the medicine is absorbed through your skin and into your blood.

Overdose is more likely to occur when using a numbing medicine without the advice of a medical doctor (such as during a cosmetic procedure like laser hair removal). However, overdose has also occurred in women treated with a numbing medicine before having a mammography. Symptoms may include uneven heartbeats, seizure (convulsions), coma, slowed breathing, or respiratory failure (breathing stops).


Do not use lidocaine and prilocaine topical if you have a blood cell disorder called methemoglobinemia.

Before lidocaine and prilocaine topical is applied, tell your doctor if you have:



  • liver disease;




  • a history of allergic reaction to lidocaine or prilocaine; or




  • a personal or family history of methemoglobinemia, or any genetic enzyme deficiency.



If you have any of these conditions, you may need a dose adjustment or special tests to safely use lidocaine and prilocaine topical.


FDA pregnancy category B. This medication is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Lidocaine and prilocaine topical can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I use lidocaine and prilocaine topical?


Use this medication exactly as directed on the label, or as it has been prescribed by your doctor. Do not use the medication in larger amounts, or use it for longer than recommended.


Your body may absorb more of this medication if you use too much, if you apply it over large skin areas, or if you apply heat, bandages, or plastic wrap to treated skin areas. Skin that is cut or irritated may also absorb more topical medication than healthy skin.

Use the smallest amount of medicine needed to numb the skin or relieve pain. Do not use large amounts of lidocaine and prilocaine topical, or cover treated skin areas with a bandage or plastic wrap without medical advice. Be aware that many cosmetic procedures are performed without a medical doctor present.


This medication comes with instructions for safe and effective application. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.


You should be lying down when lidocaine and prilocaine topical cream is applied.


Your medicine may have been supplied with bandages to cover the cream when it is applied to a small area on your skin. If using a bandage dressing, first apply a thick layer of the cream to the skin, taking care not to spread the cream out. Place the bandage over the cream and smooth down the edges until it is completely sealed around the cream.


Lidocaine and prilocaine topical is usually applied 1 to 2 hours before the start of a procedure that requires the treated area to be numb. Follow your doctor's instructions about the length of time the cream should be left on the skin.


Store lidocaine and prilocaine topical at room temperature away from moisture and heat. Do not allow the cream to freeze.

What happens if I miss a dose?


Since lidocaine and prilocaine topical is used as needed, it is not likely that you will be on a dosing schedule.


What happens if I overdose?


Seek emergency medical attention if you think you have used too much of this medicine. An overdose of lidocaine and prilocaine topical applied to the skin can cause life-threatening side effects such as uneven heartbeats, seizure (convulsions), coma, slowed breathing, or respiratory failure (breathing stops).

What should I avoid while taking lidocaine and prilocaine topical?


Lidocaine and prilocaine topical is for use only on the surface of your body. Avoid getting this medication in your eyes.

Avoid accidentally injuring treated skin areas while they are numb. Avoid coming into contact with very hot or very cold surfaces.


Lidocaine and prilocaine topical 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 lidocaine and prilocaine topical and call your doctor at once if you have any of these serious side effects:

  • severe burning, stinging, or sensitivity where the medicine is applied;




  • swelling or redness;




  • sudden dizziness or sleepiness after medicine is applied;




  • bruising or purple appearance of the skin; or




  • unusual sensations of temperature.



Less serious side effects may include:



  • mild burning where the medicine is applied;




  • skin redness; or




  • changes in skin color where the medicine was applied.



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.


Lidocaine and prilocaine topical Dosing Information


Usual Adult Dose for Anesthesia:

Venipuncture and intravenous cannulation: 2.5 g (one-half of 5 g tube) over 20 to 25 cm² of skin surface for at least 1 hour.

Painful dermatologic procedure on a large skin area such as split thickness skin graft harvesting: 2 g per 10 cm² of skin surface for at least 2 hours.

Genital skin (male): adjunct prior to local anesthetic infiltration, 1 g per 10 cm² of skin surface for 15 minutes. Local anesthetic infiltration should be performed immediately after the removal of the cream. Dermal analgesia can be expected to increase for up to 3 hours under occlusive dressing and persist for 1 to 2 hours after removal of the cream.

Genital mucous membranes (female): 5 to 10 g for 5 to 10 minutes. Occlusion is not necessary for absorption. The procedure or the local anesthetic infiltration should be performed immediately after the removal of the cream.

Applied directly into periodontal pockets to provide localized anesthesia: Apply lidocaine-prilocaine liquid on the gingival margin around the selected teeth using the blunt tipped applicator included in the package. Wait 30 seconds, then fill the periodontal pockets with lidocaine-prilocaine liquid using the blunt tipped applicator until the gel becomes visible at the gingival margin. Wait another 30 seconds before starting treatment. A longer waiting time does not enhance the anesthesia. Anesthetic effect, as assessed by probing of pocket depths, has a duration of approximately 20 minutes. If the anesthesia starts to wear off, lidocaine-prilocaine liquid may be reapplied if needed. The maximum recommended dose of lidocaine-prilocaine liquid at one treatment session is 5 cartridges.

Usual Pediatric Dose for Anesthesia:

Neonatal:
Topical:
Gestational Age (GA): Less than 37 weeks: 0.5 g/dose has been most frequently reported. One study of 30 preterm neonates (GA: greater than or equal to 30 weeks) showed application to the heel for 1 hour resulted in no measurable changes in methemoglobin levels; others have reported similar findings
GA: greater than or equal to 37 weeks:
Painful procedures (i.e.,, intramuscular injections): Apply 1 g/site for at least 60 minutes
Circumcision: Apply 1 to 2 g to prepuce and occlude for 60 to 90 minutes prior to procedure
Manufacturer recommended maximum dose and application area (based on application to intact skin): Weight less than 5 kg:
Maximum total dose of 1 g
Maximum application area: 10 cm2
Maximum application time: 1 hour

Dosage based on age, weight, application area, and application times - maximum recommended:
Less than or equal to 3 months (or less than 5 kg): 1 g, 10 cm2, 1 hour
Greater than 3 to less than or equal to 12 months: (and greater than 5 kg): 2 g, 20 cm2, 4 hours
1 to 6 years (and greater than 10 kg): 10 g, 100 cm2, 4 hours
7 to 12 years (and greater than 20 kg): 20 g, 200 cm2, 4 hours


What other drugs will affect lidocaine and prilocaine topical?


Before this medication is applied, tell your doctor if you are using any of the following drugs:



  • heart rhythm medication such as mexiletine (Mexitil);




  • acetaminophen (Tylenol);




  • chloroquine (Aralen);




  • dapsone;




  • nitrates or nitrites such as Imdur, Isordil, Monoket;




  • nitrofurantoin (Furadantin, Macrodantin, Macro-Bid);




  • phenobarbital (Luminal, Solfoton);




  • primaquine;




  • quinine; or




  • a sulfa drug (Bactrim, Gantanol, Gantrisin, Septra, SMX-TMP, and others).



This list is not complete and there may be other drugs that can interact with lidocaine and prilocaine topical. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.



More lidocaine and prilocaine topical resources


  • Lidocaine and prilocaine topical Side Effects (in more detail)
  • Lidocaine and prilocaine topical Use in Pregnancy & Breastfeeding
  • Lidocaine and prilocaine topical Support Group
  • 2 Reviews for Lidocaine and prilocaine - Add your own review/rating


Compare lidocaine and prilocaine topical with other medications


  • Anesthesia


Where can I get more information?


  • Your pharmacist can provide more information about lidocaine and prilocaine topical.

See also: lidocaine and prilocaine side effects (in more detail)


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Saturday, 11 August 2012

Capsaicin in Lidocaine Cream


Pronunciation: kap-SAY-uh-sin
Generic Name: Capsaicin in Lidocaine
Brand Name: Axsain


Capsaicin in Lidocaine Cream is used for:

Temporary relief of nerve pain when used as directed by your doctor. It may also be used for other conditions as determined by your doctor.


Capsaicin in Lidocaine Cream is a topical analgesic. Exactly how it works is unknown, but it is thought to decrease the amount of a certain substance (substance P) that transmits pain in the body.


Do NOT use Capsaicin in Lidocaine Cream if:


  • you are allergic to any ingredient in Capsaicin in Lidocaine Cream or to other local anesthetics (eg, benzocaine)

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



Before using Capsaicin in Lidocaine Cream:


Some medical conditions may interact with Capsaicin in Lidocaine Cream. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:


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

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

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

  • if you have an open wound or damaged, broken, or irritated skin

Some MEDICINES MAY INTERACT with Capsaicin in Lidocaine Cream. Tell your health care provider if you are taking any other medicines, especially any of the following:


  • Antiarrhythmics (eg, mexiletine, tocainide) because it may increase the risk of Capsaicin in Lidocaine Cream's side effects

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


How to use Capsaicin in Lidocaine Cream:


Use Capsaicin in Lidocaine Cream as directed by your doctor. Check the label on the medicine for exact dosing instructions.


  • An extra patient leaflet is available with Capsaicin in Lidocaine Cream. Talk to your pharmacist if you have questions about this information.

  • It is recommended that you wear disposable gloves when applying Capsaicin in Lidocaine Cream to decrease the chance that you will accidentally get Capsaicin in Lidocaine Cream on your eyes, nose, or mouth.

  • Apply just enough medicine to cover the affected area. Gently rub the medicine into skin until it disappears.

  • Wash your hands with soap and water immediately after using Capsaicin in Lidocaine Cream unless your hands are part of the treated area.

  • Do not apply to wounds or damaged, broken (open), or irritated skin.

  • Do not bandage or wrap the affected area.

  • Do not use Capsaicin in Lidocaine Cream with a heating pad.

  • Do not expose the treated area to heat or direct sunlight. Warm or hot water or sunlight may increase the likelihood of burning or itching. Do not use Capsaicin in Lidocaine Cream immediately after bathing, swimming, using a hot tub, sunbathing, or exposure to heat.

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

Ask your health care provider any questions you may have about how to use Capsaicin in Lidocaine Cream.



Important safety information:


  • For external use only. Avoid contact with the eyes, nose, and mouth. If Capsaicin in Lidocaine Cream gets into your eyes, rinse immediately with cool water.

  • Do NOT take more than the recommended dose or use large amounts of Capsaicin in Lidocaine Cream without checking with your doctor.

  • If you use topical products too often, your condition may become worse.

  • Do not inhale any residue from Capsaicin in Lidocaine Cream after it has dried. Coughing, sneezing, or throat or respiratory irritation may occur.

  • Capsaicin in Lidocaine Cream may cause harm if it is swallowed. If you may have taken it by mouth, contact your poison control center or emergency room right away.

  • If redness is present or if irritation develops, check with your doctor before using any more of Capsaicin in Lidocaine Cream.

  • If severe burning or itching occurs, remove product by thoroughly washing the area with soap and cold water. If regular soap and water does not completely wash away Capsaicin in Lidocaine Cream, try using dishwashing liquid or cooking oil at room temperature.

  • Capsaicin in Lidocaine Cream should not be used in CHILDREN younger than 10 years old; safety and effectiveness in these children have not been confirmed.

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


Possible side effects of Capsaicin in Lidocaine Cream:


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



Temporary burning or stinging at the application site that usually disappears in a few days.



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

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); difficulty breathing or swallowing; irritation, redness, blistering, or severe or persistent burning at the application site.



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


See also: Capsaicin in Lidocaine side effects (in more detail)


If OVERDOSE is suspected:


Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Capsaicin in Lidocaine Cream may be harmful if swallowed.


Proper storage of Capsaicin in Lidocaine Cream:

Store Capsaicin in Lidocaine Cream at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Close cap tightly after use. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Capsaicin in Lidocaine Cream out of the reach of children and away from pets.


General information:


  • If you have any questions about Capsaicin in Lidocaine Cream, please talk with your doctor, pharmacist, or other health care provider.

  • Capsaicin in Lidocaine Cream is to be used only by the patient for whom it is prescribed. Do not share it with other people.

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

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

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



Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Capsaicin in Lidocaine resources


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


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