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Tuesday, October 25, 2016

Amorolfine Hydrochloride

Amorolfine Hydrochloride may be available in the countries listed below.

Ingredient matches for Amorolfine Hydrochloride

Amorolfine

Amorolfine Hydrochloride (BANM) is also known as Amorolfine (Rec.INN)

International Drug Name Search

Glossary

BANM	British Approved Name (Modified)
Rec.INN	Recommended International Nonproprietary Name (World Health Organization)

Click for further information on drug naming conventions and International Nonproprietary Names.

Generic Name: Leflunomide
Class: Disease-modifying Antirheumatic Agents
Chemical Name: 5-Methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide
Molecular Formula: C₁₂H₉F₃N₂O₂
CAS Number: 75706-12-6

Pregnancy

Contraindicated in pregnant women and women of childbearing potential who are not using a reliable form of contraception.¹ (See Fetal/Neonatal Morbidity and Mortality and also see Contraindications under Cautions.)

Pregnancy must be excluded prior to initiation of therapy.¹

Pregnancy must be avoided while the woman is receiving leflunomide and prior to completion of the drug elimination procedure following discontinuance of the drug.¹ (See Drug Elimination Procedures Following Leflunomide Discontinuance under Dosage and Administration.)

Hepatotoxicity

Severe liver injury, including fatal liver failure, reported.¹

Do not use in patients with preexisting liver disease or baseline ALT >2 times ULN; use with caution in patients receiving other potentially hepatotoxic drugs.¹ (See Hepatic Effects under Cautions.)

Regular monitoring of ALT during therapy required; ALT >3 times ULN warrants interruption of therapy while cause is investigated.¹ (See Hepatic Effects under Cautions.)

Introduction

Immunomodulating agent and disease-modifying antirheumatic drug (DMARD).¹ ² ³ ⁴ ⁵ ⁶ ⁷ ⁸ ¹² ¹³ ¹⁴ ¹⁵ ¹⁷ Considered a prodrug since it is rapidly and almost completed metabolized to an active metabolite (A77 1726).² ³ ⁴ ⁸ ¹² ¹³ ¹⁴ ¹⁵

Uses for Arava

Rheumatoid Arthritis in Adults

Used to manage the signs and symptoms of rheumatoid arthritis, to improve physical function, and to retard structural damage associated with the disease.¹ ² ³ ⁴ ⁵ ⁶ ⁷ ⁸ ¹² ¹³ ¹⁴ ¹⁵ ¹⁶ ⁴⁶ ⁴⁷ ⁵⁶ ⁵⁷ Efficacy comparable to that of methotrexate or sulfasalazine.² ⁵ ⁶ ¹⁶ ⁵⁶ ⁵⁷ ⁵⁸ ⁵⁹ ⁶⁴

Has been used with methotrexate in a limited number of adults.¹ ³ ⁴⁸ ⁷⁰ Used concomitantly with aspirin, NSAIAs, or low dosages of oral corticosteroids (e.g., prednisone 10 mg daily) in clinical studies.¹ ⁵ ⁶

Solid Organ Transplantation

Has been used for the prevention of acute and chronic rejection† in recipients of solid organ transplants (designated an orphan drug by FDA for this use).⁵⁴ Evaluated in a limited number of renal or hepatic transplant recipients.⁶⁰

Arava Dosage and Administration

General

Drug Elimination Procedures Following Leflunomide Discontinuance

Plasma concentration of the active metabolite of leflunomide (A77 1726) may be detectable in plasma for up to 2 years following discontinuance of the drug.⁴⁴ ⁴⁵ Manufacturer recommends use of a drug elimination procedure whenever more rapid elimination is indicated or desirable.¹

An 11-day cholestyramine regimen is recommended whenever leflunomide is discontinued in women of childbearing potential and should be considered in men who wish to father a child after discontinuing the drug; this regimen reduces plasma concentrations of A77 1726 to undetectable levels.¹

A shorter regimen of cholestyramine or activated charcoal (≥1 day) can be used to hasten elimination of A77 1726 in other patients (see Prolonged Leflunomide Exposure following Discontinuance under Cautions).¹ In patients who discontinued leflunomide because of hypersensitivity reaction, a more prolonged regimen may be necessary to achieve rapid and sufficient clearance of A77 1726.¹

11-Day Cholestyramine Drug-Elimination Procedure

Cholestyramine 8 g orally 3 times daily for 11 days; the 11 days do not need to be consecutive unless plasma concentrations need to be reduced rapidly.¹

Following completion of regimen, determine plasma concentrations of A77 1726 twice (≥14 days apart) to verify that concentrations are undetectable.¹ If plasma concentrations exceed 0.02 mcg/mL, administer additional cholestyramine.¹

Shorter Cholestyramine or Activated Charcoal Regimen

Cholestyramine (8 g 3 times daily) given orally for 24 hours reduces plasma concentrations of A77 1726 by approximately 40% in 24 hours and 49–65% in 48 hours.¹

Alternatively, suspension of activated charcoal (50 g every 6 hours) given for 24 hours either orally or via nasogastric tube reduces plasma concentrations of A77 1726 by approximately 37% in 24 hours and 48% in 48 hours.¹

Repeat the elimination procedure if clinically necessary.¹

Concomitant Therapy for Rheumatoid Arthritis

Aspirin, NSAIAs, and low-dose corticosteroids may be continued.¹ ⁵ ⁶

Used concomitantly with methotrexate in a limited number of patients.³ ⁴⁸ ⁷⁰ Manufacturer states that concomitant use with antimalarials, azathioprine, methotrexate, penicillamine, or oral or injectable gold has not been adequately studied.¹

Administration

Oral Administration

Usually administered orally as a single daily dose, without regard to meals.¹

Dosage

Adults

Rheumatoid Arthritis in Adults

Oral

100 mg once daily for 3 days, then 20 mg once daily.¹ ² ⁵ ⁶ If this dosage is not tolerated, decrease to 10 mg once daily.¹ Discontinuance may be required in patients who experience hepatotoxicity.¹ (See Hepatic Effects under Cautions.)

Eliminating the 3-day loading dose may decrease the risk of adverse effects (see Plasma Concentrations under Pharmacokinetics).¹ Elimination of loading dose may be especially important for patients at increased risk of hematologic or hepatic toxicity.¹

Solid Organ Transplantation

Renal or Hepatic Transplant Recipients†

Oral

Initial loading dosage of 1.2–1.4 g (administered in divided doses over 5–7 days), then 10–120 mg daily.⁶⁰

Prescribing Limits

Adults

Rheumatoid Arthritis in Adults

Oral

Maintenance therapy: Maximum 20 mg daily.¹ Dosage of 25 mg daily associated with higher incidence of alopecia, weight loss, and increases in serum liver enzyme concentrations.¹

Special Populations

Hepatic Impairment

Not recommended in patients with preexisting acute or chronic liver disease (including those who are seropositive for hepatitis B or C) or in patients with baseline ALT >2 times the ULN.¹ ² ⁶⁸ (See Hepatic Impairment and also Hepatic Effects, under Cautions.)

Geriatric Patients

Routine dosage adjustment based on age is not necessary in patients >65 years of age.¹

Cautions for Arava

Contraindications

Known hypersensitivity to leflunomide or any ingredient in the formulation.¹

Do not initiate leflunomide in pregnant women or women of childbearing potential unless the possibility of pregnancy has been excluded and an effective method of contraception has been started.¹ (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Warnings/Precautions

Warnings

Hepatic Effects

Possible hepatic reactions (e.g., hepatitis, jaundice/cholestasis); severe liver injury (e.g., liver failure, acute hepatic necrosis), sometimes fatal, reported rarely.¹ ⁵⁵ ⁶⁴ ⁶⁸ Reactions generally occur within first 6–12 months of initiating therapy.⁵⁵ ⁶⁸

Increased risk of liver injury in patients with preexisting liver disease and those receiving other hepatotoxic agents concomitantly.⁶⁸ Do not use in patients with preexisting liver disease or baseline ALT >2 times ULN; use with caution in patients receiving other potentially hepatotoxic drugs.¹ ⁶⁸

Monitor closely for hepatotoxicity.¹ Determine serum ALT concentrations prior to initiation of therapy, at least once monthly during the first 6 months, and (if ALT concentrations remain stable) every 6–8 weeks thereafter.¹ If leflunomide is used concomitantly with methotrexate, also follow American College of Rheumatology (ACR) guidelines for monitoring for methotrexate liver toxicity.¹

Increases in serum concentrations of ALT and/or AST ¹ ² ⁵ ⁶ ⁷ ⁸ generally are mild (≤2 times the ULN) and resolve despite continued administration.¹ ⁵ ⁶ ⁸

If ALT concentrations are >3 times the ULN, interrupt leflunomide therapy and investigate cause of ALT elevation.¹ If leflunomide is the probable cause, administer cholestyramine to hasten drug elimination and monitor serum ALT concentration weekly until value is normal.¹ If leflunomide is considered an unlikely cause of ALT elevation because another probable cause is found, may consider resuming leflunomide therapy.¹

Infectious Complications

Opportunistic infections (e.g., Pneumocystis jiroveci pneumonia, tuberculosis [including extrapulmonary disease], aspergillosis) and serious infection, including sepsis and death, reported rarely.¹ Most serious infections occurred in patients receiving concomitant therapy with immunosuppressive agents and/or with comorbid illness that, in addition to rheumatoid arthritis, could have predisposed them to infections.¹

Interrupt leflunomide therapy and administer cholestyramine or charcoal if serious infection develops.¹

Not recommended in patients with severe immunodeficiency or severe uncontrolled infections.¹

Not evaluated in patients with latent tuberculosis infection; safety in such patients is not known.¹ Evaluate all patients for latent tuberculosis prior to initiation of therapy.¹ When indicated, initiate appropriate antimycobacterial regimen for treatment of latent tuberculosis infection prior to leflunomide therapy.¹

Hematologic Effects

Pancytopenia,¹ ² ⁵³ ⁶¹ agranulocytosis,¹ and thrombocytopenia¹ ⁷ reported; these effects reported most frequently when leflunomide was given with or immediately after methotrexate or another immunosuppressive agent.¹ Some patients had a history of clinically important hematologic abnormality.¹

Anemia (including iron deficiency anemia), ¹ ecchymosis,¹ eosinophilia,¹ leukopenia,¹ ² ⁸ neutropenia¹ reported.

Monitor for hematologic toxicity.¹ Determine platelet count, leukocyte count, and hemoglobin concentration or hematocrit prior to initiating therapy, once monthly during the first 6 months, then every 6–8 weeks.¹ If used in conjunction with methotrexate or another immunosuppressive agent, determine platelet count, leukocyte count, and hemoglobin concentration or hematocrit once monthly throughout therapy.¹ Consider continued monitoring in patients who discontinue leflunomide and receive subsequent therapy with a drug with known potential for hematological suppression.¹

Discontinue leflunomide if evidence of bone marrow suppression occurs; consider use of a drug elimination procedure.¹

Not recommended in patients with bone marrow dysplasia.¹

Fetal/Neonatal Morbidity and Mortality

Can cause fetal toxicity.¹ Because the risks clearly outweigh any possible benefits, leflunomide is contraindicated in pregnant women.¹ ¹⁰

Do not initiate in a woman of childbearing potential until pregnancy is excluded and use of a reliable form of contraception is confirmed.¹ ¹¹

Pregnancy must be avoided during leflunomide therapy and prior to completion of the drug-elimination procedure following discontinuance of the drug.¹

Discontinue leflunomide if the drug is administered inadvertently during pregnancy or if the patient becomes pregnant while receiving the drug.¹ Use of a drug-elimination procedure to rapidly lower plasma concentrations of A77 1726 to undetectable concentrations early in pregnancy (i.e., at the first delay in menses) may decrease risk to fetus.¹

Although available information does not indicate that leflunomide therapy is associated with an increased risk of male-mediated fetal toxicity, animal studies to evaluate this specific risk have not been conducted.¹ ¹¹ To minimize risk, men wishing to father a child should consider discontinuing leflunomide therapy and undergoing an 11-day cholestyramine drug-elimination procedure.¹

Malignancy

Increased risk of malignancy, particularly lymphoproliferative disorders, in patients receiving some immunosuppressant drugs.¹ While an increased incidence of malignancies or lymphoproliferative disorders has not been observed in patients receiving leflunomide in clinical trials, long-term studies are needed to establish the precise risk.¹ ²

Sensitivity Reactions

Dermatologic Reactions

Stevens-Johnson syndrome,¹ ⁵³ toxic epidermal necrolysis,¹ ⁵³ and erythema multiforme¹ ⁵³ reported rarely.

If severe skin reaction occurs, discontinue immediately; use of a drug-elimination procedure recommended.¹

General Precautions

Prolonged Leflunomide Exposure following Discontinuance

Up to 2 years may be required for plasma concentrations of the active metabolite (A77 1726) to decrease to undetectable concentrations (<0.02 mcg/mL) following discontinuance of leflunomide.⁴⁴ ⁴⁵ Manufacturer recommends a drug-elimination procedure when more rapid elimination of A77 1726 is indicated or desirable (see Drug Elimination Procedures Following Leflunomide Discontinuance under Dosage and Administration).¹

Adverse effects or drug interactions associated with leflunomide may continue to occur after the patient is no longer receiving the drug.⁴⁴ ⁴⁵

Manufacturer recommends a drug-elimination procedure following discontinuance in women of childbearing potential; procedure should be considered in men who wish to father a child after discontinuing the drug.¹

A drug-elimination procedure also recommended in patients with potentially serious drug-related adverse effects (e.g., persistently increased liver function test results, severe dermatologic or sensitivity reactions, bone marrow suppression, pancytopenia, serious infection).¹

A drug-elimination procedure may be appropriate in patients who will receive a drug with known potential for hematologic suppression following discontinuance of leflunomide.¹

Pulmonary Effects

Intersitial lung disease (e.g., pneumonitis, pulmonary fibrosis) reported, including fatalities.¹ In patients experiencing new or worsening pulmonary symptoms (e.g., cough, dyspnea) with or without fever, consider discontinuing leflunomide.¹ If discontinuance is warranted, consider use of a drug elimination procedure.¹

Cardiovascular Effects

Hypertension reported; evaluate BP at baseline and periodically during therapy.¹

Specific Populations

Pregnancy

Category X.¹

Pregnancy registry at 877-311-8972.¹ (See Fetal/Neonatal Morbidity and Mortality and also see Contraindications under Cautions.)

Lactation

Do not use in nursing women; either proceed with nursing or initiate therapy with leflunomide, taking into account the importance of the drug to the woman.¹

Pediatric Use

Safety and efficacy in pediatric patients not fully evaluated.¹ Leflunomide has been used for treatment of polyarticular course juvenile rheumatoid arthritis† in a limited number of children and adolescents 3–17 years of age;¹ ⁶⁶ however, appropriate dosing in pediatric patients is not clear.⁶⁶ ⁶⁷ Adverse effects observed in children were similar to those in adults.¹ ⁶⁶

Geriatric Use

No overall differences in efficacy or safety relative to younger adults, but increased sensitivity cannot be ruled out.¹

No difference in pharmacokinetics based on adult age; routine dosage adjustment is not needed.¹

Hepatic Impairment

Use not recommended in patients with preexisting acute or chronic liver disease or baseline serum ALT concentrations >2 times the ULN because of possible increased risk of hepatotoxicity and liver’s role in formation of active metabolite and in recirculation and elimination of the drug.¹ ² Not recommended in patients who are seropositive for hepatitis B or C.² ⁶⁸ (See Hepatic Effects under Cautions.)

Renal Impairment

Use with caution; not evaluated in this population.¹

Common Adverse Effects

Diarrhea, increased serum AST/ALT concentrations, alopecia, rash.¹ ⁵ ⁶ ⁷ ⁸

Interactions for Arava

A77 1726 inhibits CYP2C9.¹

Drug interactions may continue to occur after patient no longer is receiving the drug.⁴⁴ ⁴⁵

Drugs Affecting Hepatic Microsomal Enzymes

CYP2C9 substrates: Potential pharmacokinetic interaction (increased plasma concentrations of CYP2C9 substrate).¹

Vaccines

Data not available regarding administration of vaccines in patients receiving leflunomide.¹

Do not administer live vaccines to patients receiving leflunomide.¹ ⁴⁹ Consider the long half-life of A77 1726 when administration of a live vaccine is being considered.¹

Hepatotoxic Agents

Increase in adverse hepatic effects expected.¹ ⁶⁸ Use with caution.¹ ⁶⁸

DMARDs

Used concomitantly with methotrexate in a limited number of patients with rheumatoid arthritis (see Specific Drugs under Interactions).³ ⁴⁸ ⁷⁰ Manufacturer states that concomitant administration with antimalarials, azathioprine, methotrexate, penicillamine, or oral or injectable gold not adequately studied.¹

Specific Drugs

Drug	Interaction	Comments
Anticoagulants	Increases in INR reported rarely in patients receiving warfarin;¹ possible increases in plasma warfarin concentrations¹	Monitor carefully¹
Cimetidine	Interaction unlikely¹
Charcoal, activated	Decreased plasma concentrations and hastened elimination of A77 1726¹	Used for drug elimination¹
Cholestyramine	Decreased plasma concentrations and hastened elimination of A77 1726¹	Used for drug elimination¹
Contraceptives, oral triphasic	Interaction unlikely¹
Methotrexate	Pharmacokinetic interaction unlikely;¹ increased incidence of adverse effects and increases in serum ALT¹ ³ ⁷⁰	Caution advised; monitor closely for hepatotoxicity (see Hepatic Effects under Cautions)¹
NSAIAs	Used without any evidence of any change in effect;¹ increased free fraction of diclofenac and ibuprofen¹	Clinical importance of pharmacokinetic changes unknown¹
Phenytoin	Possible increased plasma phenytoin concentration¹	Clinical importance unknown¹
Rifampin	Increased peak plasma concentrations of A77 1726¹	Caution advised¹
Tolbutamide	Increased free fraction of tolbutamide¹	Clinical importance unknown¹

Arava Pharmacokinetics

Absorption

Bioavailability

Following oral administration, leflunomide is rapidly converted to the active metabolite A77 1726 in the GI mucosa and liver; peak plasma concentrations of A77 1726 usually occur within 6–12 hours.¹ ² ⁸ ¹² ¹⁵ ⁴⁴

Food

High-fat meal does not appear to affect absorption of A77 1726.¹

Plasma Concentrations

Therapy usually initiated with a loading dosage so that steady-state plasma concentrations are achieved relatively rapidly.¹ Steady-state plasma concentrations of A77 1726 likely would not be attained for at least 2 months in the absence of the initial loading dosage used for rheumatoid arthritis.¹

Distribution

Extent

Not fully characterized.¹

Plasma Protein Binding

A77 1726: >99% (albumin).¹ ² ⁴ ¹² The percentage of unbound A77 1726 is slightly higher in those with rheumatoid arthritis.¹ ²

Special Populations

In patients undergoing CAPD or hemodialysis, percentage of unbound A77 1726 is twice that in healthy adults (1.51 versus 0.62%).¹

Elimination

Metabolism

Specific enzyme(s) involved in the principal metabolism of leflunomide have not been determined; however, hepatic cytosolic and microsomal cellular fractions are sites of metabolism.¹ ² ⁸

Elimination Route

Excreted in urine principally as glucuronides and an oxanilic acid derivative of A77 1726 and by direct biliary excretion as A77 1726.¹

Half-life

A77 1726: 14–18 days.¹ ² ⁴ ¹²

Special Populations

Clearance decreased in children weighing ≤40 kg compared with adults and children weighing >40 kg.¹ ⁶⁷

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).¹ Protect from light.¹

ActionsActions

A pharmacologically active metabolite (A77 1726) is responsible for essentially all of the drug’s activity in vivo.¹ ² ³ ⁴ ⁸ ¹² ¹³ ¹⁴ ¹⁵

Mechanism of action in rheumatoid arthritis appears to principally involve regulation of autoimmune lymphocytes.² ⁵ ⁸ ¹² ¹⁴ ¹⁵ ¹⁸

Reversibly inhibits the mitochondrial enzyme dihydroorotate dehydrogenase.¹ ² ³ ⁴ ⁵ ⁶ ⁷ ⁸ ¹² ¹³ ¹⁴ ¹⁵ ¹⁷ ¹⁸ Inhibition of dihydroorotate dehydrogenase prevents production of ribonucleotide uridine monophosphate (rUMP) by the de novo pathway, which leads to decreased rUMP levels, decreased DNA and RNA synthesis, inhibition of cell proliferation, and G₁ cell cycle arrest.² ¹² ¹⁵ Thus, leflunomide inhibits autoimmune T-cell proliferation and production of autoantibodies by B cells.¹² ¹⁸

Advice to Patients

Risk of birth defects.¹ Importance of clinicians informing women of childbearing potential that they may be at increased risk of having a child with birth defects if they are pregnant, become pregnant while receiving leflunomide, or do not wait to become pregnant until they have completed a drug-elimination procedure following discontinuance of the drug.¹ Women of childbearing potential should be advised to notify their clinician immediately if they experience a delay in menses or believe they may be pregnant.¹

Risk of rare, serious skin reactions.¹ Importance of promptly reporting rash or mucous membrane lesions to their clinician.¹

Potential for hepatotoxic effects; need for monitoring of liver enzymes.¹ Importance of reporting symptoms such as unusual tiredness, abdominal pain, or jaundice to their clinician.¹

Potential for hematologic toxicity; need for frequent hematologic monitoring.¹ Importance of promptly reporting symptoms such as easy bruising or bleeding, recurrent infections, fever, paleness, or unusual tiredness to their clinician.¹

Risk of interstitial lung disease.¹ Importance of reporting any new or worsening respiratory symptoms.¹

Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs.¹

Importance of women informing clinicians if they are breast-feeding or plan to breast-feed.¹

Importance of informing patients of other important precautionary information.¹ (See Cautions.)

Preparations

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

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Leflunomide
Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets, film-coated	10 mg*	Arava	Sanofi-Aventis
			Leflunomide Tablets
		20 mg*	Arava	Sanofi-Aventis
			Leflunomide Tablets
		100 mg	Arava	Sanofi-Aventis

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 04/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Arava 10MG Tablets (SANOFI-AVENTIS U.S.): 30/$642.98 or 60/$1274.89

Arava 20MG Tablets (SANOFI-AVENTIS U.S.): 30/$671.02 or 60/$1324.41

Leflunomide 10MG Tablets (TEVA PHARMACEUTICALS USA): 30/$64 or 90/$188.91

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 February 01, 2011. 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

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33. Weinblatt ME, Kremer JM, Bankhurst AD et al. A trial of etanercept, a recombinant tumor necrosis factor receptor:Fc fusion protein, in patients with rheumatoid arthritis receiving methotrexate. N Engl J Med. 1999; 340:253-9. [IDIS 417654] [PubMed 9920948]

34. Sharp JT, Strand V, Leung H et al. Treatment with leflunomide slows radiographic progression of rheumatoid arthritis: results from three randomized controlled trials of leflunomide in patients with active rheumatoid arthritis. Leflunomide rheumatoid arthritis investigators group. Arthritis Rheum. 2000; 43:495-505. [IDIS 444429] [PubMed 10728741]

35. Bruyn GAW, Griep EN, Korff KJ. Leflunomide for active rheumatoid arthritis. Lancet. 1999; 353:1883. [IDIS 427088] [PubMed 10359439]

36. Smolen JS, Scott DL, Kalden JT et al. Leflunomide for active rheumatoid arthritis. Lancet. 1999; 353:1883-4.

37. Strand V. Approaches to the management of systemic lupus erythematosus. Curr Opin Rheumatol. 1997; 9:410-20. [PubMed 9309196]

38. Eckhardt SG, Rizzo J, Sweeney KR et al. Phase I and pharmacologic study of the tyrosine kinase inhibitor SU101 in patients with advanced solid tumors. J Clin Oncol. 1999; 17:1095-104. [IDIS 425769] [PubMed 10561166]

39. Hausen B, Boeke K, Berry GJ et al. Potentiation of immunosuppresive efficacy by combining the novel leflunomide analog, HMR 279, with microemulsion cyclosporine in a rat lung transplant model. Transplantation. 1999; 67:354-9. [PubMed 10030278]

40. Xu X, Shen J, Mall JW et al. In vitro and in vivo antitumor activity of a novel immunomodulatory drug, leflunomide: mechanism of action. Biochem Pharmacol. 1999; 58:1405-13. [PubMed 10513984]

41. VanUmmersen L, Ness E, Goldstein DJ et al. A phase I trial of SU101 in patients with solid tumors. Proceedings of ASCO Denver 1997. Abstract No. 740.

42. Rosen L, Lopez AM, Mulay M et al. A phase I/II study of SU101 in patients with ovarian, prostate, and non-small cell lung cancers. Proceedings of ASCO Denver 1997. Abstract No. 739.

43. Antoniou EA, Deroover A, Howie AJ et al. Immunosuppressive effect of combination schedules of brequinar with leflunomide or tacrolimus on rat cardiac allotransplantation. Microsurgery. 1999; 19:98-102. [PubMed 10188834]

44. Aventis Pharmaceuticals, Kansas City, MO. Personal communication.

45. Reviewers’ comments (personal observations).

Monday, October 24, 2016

Starlix

Pronunciation: NA-te-GLYE-nide
Generic Name: Nateglinide
Brand Name: Starlix

Starlix is used for:

Lowering blood sugar levels in patients with type 2 diabetes. It used along with diet and exercise. It may also be used for other conditions as determined by your doctor.

Starlix is an antidiabetic agent. It works by causing insulin to be released from the pancreas. This helps to lower blood glucose levels.

Do NOT use Starlix if:

you are allergic to any ingredient in Starlix

you have type 1 diabetes

you have a certain problem associated with diabetes (diabetic ketoacidosis)

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

Before using Starlix:

Some medical conditions may interact with Starlix. 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 adrenocortical, pituitary, liver, or kidney problems

if you have a high fever, or poor health or nutrition

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

Amiodarone, beta-adrenergic blockers (eg, metoprolol), gemfibrozil, guanethidine, imidazoles (eg, ketoconazole), monoamine oxidase inhibitors (MAOIs) (eg, phenelzine), nonsteroidal anti-inflammatory drugs (NSAIDs) (eg, ibuprofen), oxandrolone, or salicylates (eg, aspirin) because the risk of low blood sugar may be increased

Corticosteroids (eg, prednisone), phenytoin, rifamycins (eg, rifampin), somatropin, St. John's wort, sympathomimetics (eg, pseudoephedrine), thiazides (eg, hydrochlorothiazide), or thyroid hormones (eg, levothyroxine) because they may decrease Starlix's effectiveness

Somatostatin analogs (eg, octreotide) because they may decrease Starlix's effectiveness or increase the risk of low blood sugar

This may not be a complete list of all interactions that may occur. Ask your health care provider if Starlix 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 Starlix:

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

Take Starlix by mouth 1 to 30 minutes before meals.

If you skip a meal, you must also skip your scheduled dose to avoid the risk of low blood sugar levels (hypoglycemia).

Talk to your doctor or other health care provider about what to do if you miss a dose of Starlix.

Ask your health care provider any questions you may have about how to use Starlix.

Important safety information:

Starlix may cause dizziness. This effect may be worse if you take it with alcohol or certain medicines. Use Starlix with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.

Follow the diet and exercise program given to you by your health care provider.

Strenuous exercise, drinking alcohol, fever, infection, surgery, trauma, dieting, and skipping meals can affect your blood sugar levels.

Carry an ID card at all times that says you have diabetes.

Check your blood sugar levels as directed by your doctor. If they are often higher or lower than they should be and you take Starlix exactly as prescribed, tell your doctor.

Starlix may cause low blood sugar. Low blood sugar may make you anxious, sweaty, weak, dizzy, drowsy, or faint. It may also make your heart beat faster; make your vision change; give you a headache, chills, or tremors; or make you more hungry. It is a good idea to carry a reliable source of glucose (eg, tablets or gel) to treat low blood sugar. If this is not available, you should eat or drink a quick source of sugar like table sugar, honey, candy, orange juice, or non-diet soda. This will raise your blood sugar level quickly. Tell your doctor right away if this happens. To prevent low blood sugar, eat meals at the same time each day and do not skip meals.

Tell your doctor or dentist that you take Starlix before you receive any medical or dental care, emergency care, or surgery.

Lab tests, including fasting blood sugar levels and hemoglobin A_1c levels, may be performed while you use Starlix. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.

Use Starlix with caution in the ELDERLY; they may be more sensitive to its effects.

Starlix should be used with extreme caution in CHILDREN; safety and effectiveness in children have not been confirmed.

PREGNANCY and BREAST-FEEDING: Do not use Starlix if you are pregnant. If you think you may be pregnant, contact your doctor right away. It is not known if Starlix is found in breast milk. Do not breast-feed while taking Starlix.

Possible side effects of Starlix:

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:

Dizziness; flu-like symptoms (fever, chills, sore throat); joint pain; upper respiratory tract infection.

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); symptoms of liver problems (eg, dark urine, loss of appetite, pale stools, stomach pain, unusual nausea or tiredness, yellowing of the skin or eyes); symptoms of low blood sugar (eg, anxiety, chills, fast heartbeat, headache, increased hunger, severe or persistent dizziness or drowsiness, tremors, unusual sweating, vision changes, weakness).

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: Starlix 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. Symptoms may include changes in vision; headache; increased hunger; loss of consciousness; nervousness; seizures; shakiness; sweating; tiredness.

Proper storage of Starlix:

Store Starlix at 77 degrees F (25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store in a tightly closed container. Store away from heat, light, and moisture. Do not store in the bathroom. Keep Starlix out of the reach of children and away from pets.

General information:

If you have any questions about Starlix, please talk with your doctor, pharmacist, or other health care provider.

Starlix 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 Starlix. 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

More Starlix resources

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

Starlix Prescribing Information (FDA)

Starlix Consumer Overview

Starlix Monograph (AHFS DI)

Starlix Advanced Consumer (Micromedex) - Includes Dosage Information

Nateglinide Prescribing Information (FDA)

Nateglinide Professional Patient Advice (Wolters Kluwer)

Compare Starlix with other medications

Diabetes, Type 2

ethotoin

ETH-oh-toin

Commonly used brand name(s)

In the U.S.

Peganone

Available Dosage Forms:

Tablet

Therapeutic Class: Anticonvulsant

Chemical Class: Hydantoin (class)

Uses For ethotoin

Ethotoin is used to control tonic-clonic (grand mal) and complex partial seizures. ethotoin is an anticonvulsant that works in the brain tissue to stop seizures.

ethotoin is available only with your doctor's prescription.

Before Using ethotoin

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 ethotoin, the following should be considered:

Allergies

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

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of ethotoin in children. However, safety and efficacy have not been established in children younger than 1 year of age.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of ethotoin in the elderly. However, elderly patients are more likely to have age-related liver, kidney, or heart problems, which may require caution and an adjustment in the dose for patients receiving ethotoin.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	D	Studies in pregnant women have demonstrated a risk to the fetus. However, the benefits of therapy in a life threatening situation or a serious disease, may outweigh the potential risk.

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 ethotoin, 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 ethotoin 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.

Ketorolac

Naproxen

Using ethotoin 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.

Ginkgo

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.

Proper Use of ethotoin

Take ethotoin 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.

ethotoin should come with a Medication Guide. Read and follow these instructions carefully. Ask your doctor if you have any questions.

It is best to take ethotoin after meals.

It is best to plan your doses so they are evenly spaced during the day. Talk with your doctor if you have questions about when to take ethotoin.

Dosing

The dose of ethotoin 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 ethotoin. 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 (tablets):
- For seizures:
  - Adults—At first, 1000 milligrams (mg) per day, divided and given in 4 to 6 doses per day. Your doctor may increase your dose as needed. The usual dose is 2000 to 3000 mg per day.
  - Children 1 year of age and older—Dose is based on age and body weight and must be determined by your doctor. The usual dose is 500 to 1000 milligrams (mg) per day, divided and given in 4 to 6 doses per day.
  - Infants younger than 1 year of age—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of ethotoin, take it as soon as possible. However, if it is almost time for your next dose, 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 ethotoin

It is very important that your doctor check the progress of you or your child at regular visits while you or your child are using ethotoin to see if it is working properly and to allow for a change in the dose. Blood and urine tests may be needed to check for any unwanted effects.

Using ethotoin while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant. If you think you have become pregnant while using the medicine, tell your doctor right away. Your doctor may want you to join a pregnancy registry for patients taking seizure medicines.

Do not stop taking ethotoin without first checking with your doctor. Your doctor may want you or your child to gradually reduce the amount you are using before stopping it completely.

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

Call your doctor right away if you or your child have a fever; nosebleeds; skin rash; small red or purple spots on the skin; a sore throat; unusual bruising or bleeding; unusual tiredness or weakness; or generally feel ill. These may be signs that you have an infection or a bleeding problem.

Lymph node problems may occur while using ethotoin. Check with your doctor right away if you or your child have swollen, painful, or tender lymph glands in your neck, armpit, or groin.

ethotoin 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:

Rare

Enlarged gums

shakiness and unsteady walk

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

Incidence not known

Blistering, peeling, or loosening of the skin

chest pain

cough

diarrhea

fever and chills

general feeling of discomfort or illness

hair loss

headaches

hives or itching

joint or muscle pain

numbness

red, irritated eyes

red skin lesions, often with a purple center

shortness of breath or troubled breathing

skin rash

sore throat

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

swollen glands

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

unusual tiredness or weakness

Get emergency help immediately if any of the following symptoms of overdose occur:

Symptoms of overdose

Blurred or loss of vision

change in consciousness

disturbed color perception

double vision

drowsiness

halos around lights

loss of consciousness

nausea

night blindness

overbright appearance of lights

tunnel vision

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:

Incidence not known

Dizziness

sleeplessness

trouble sleeping

unable to sleep

uncontrolled eye movements

vomiting

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: ethotoin 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 ethotoin resources

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

ethotoin Concise Consumer Information (Cerner Multum)

Ethotoin MedFacts Consumer Leaflet (Wolters Kluwer)

Ethotoin Professional Patient Advice (Wolters Kluwer)

Peganone Prescribing Information (FDA)

Compare ethotoin with other medications

Epilepsy
Seizure Prevention
Seizures

Friday, October 21, 2016

Golaseptine

Golaseptine may be available in the countries listed below.

Ingredient matches for Golaseptine

Chlorhexidine

Chlorhexidine dihydrochloride (a derivative of Chlorhexidine) is reported as an ingredient of Golaseptine in the following countries:

Belgium

Luxembourg

International Drug Name Search

Beatizem

Beatizem may be available in the countries listed below.

Ingredient matches for Beatizem

Diltiazem

Diltiazem hydrochloride (a derivative of Diltiazem) is reported as an ingredient of Beatizem in the following countries:

Singapore

International Drug Name Search

Micronase

Generic Name: glyburide (Oral route)

GLYE-bure-ide

Commonly used brand name(s)

In the U.S.

Diabeta

Glycron

Glynase Pres-Tab

Micronase

In Canada

Euglucon

Available Dosage Forms:

Tablet

Therapeutic Class: Hypoglycemic

Chemical Class: 2nd Generation Sulfonylurea

Uses For Micronase

Glyburide is used to treat high blood sugar levels caused by a type of diabetes mellitus (sugar diabetes) called type 2 diabetes. In type 2 diabetes, your body does not work properly to store excess sugar and the sugar remains in your bloodstream. Chronic high blood sugar can lead to serious health problems in the future.

Proper diet is the first step in managing type 2 diabetes, but often medicines are needed to help your body. Glyburide belongs to a class of medicines called sulfonylureas. It causes your pancreas to release more insulin into the blood stream. This medicine may be used alone or with another oral medicine such as metformin.

This medicine is available only with your doctor's prescription.

Before Using Micronase

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

Allergies

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

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of glyburide 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 glyburide in the elderly. However, elderly patients are more likely to have age-related liver or kidney problems, which may require an adjustment in the dose for patients receiving glyburide.

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

Interactions with Medicines

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

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

Bosentan

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

Acarbose

Alatrofloxacin

Balofloxacin

Ciprofloxacin

Clinafloxacin

Disopyramide

Enoxacin

Fleroxacin

Flumequine

Gatifloxacin

Gemifloxacin

Grepafloxacin

Levofloxacin

Lomefloxacin

Moxifloxacin

Norfloxacin

Ofloxacin

Pefloxacin

Prulifloxacin

Rufloxacin

Sparfloxacin

Temafloxacin

Tosufloxacin

Trovafloxacin Mesylate

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

Acebutolol

Aceclofenac

Acemetacin

Alclofenac

Alprenolol

Apazone

Aspirin

Atenolol

Benoxaprofen

Betaxolol

Bevantolol

Bisoprolol

Bitter Melon

Bromfenac

Bucindolol

Bufexamac

Carprofen

Carteolol

Carvedilol

Celiprolol

Clarithromycin

Clometacin

Clonixin

Clorgyline

Colesevelam

Cyclosporine

Dexketoprofen

Diclofenac

Diflunisal

Dilevalol

Dipyrone

Droxicam

Esmolol

Etodolac

Etofenamate

Felbinac

Fenbufen

Fenoprofen

Fentiazac

Fenugreek

Floctafenine

Flufenamic Acid

Flurbiprofen

Gemfibrozil

Glucomannan

Ibuprofen

Indomethacin

Indoprofen

Iproniazid

Isocarboxazid

Isoxicam

Ketoprofen

Ketorolac

Labetalol

Levobunolol

Lornoxicam

Meclofenamate

Mefenamic Acid

Meloxicam

Mepindolol

Metipranolol

Metoprolol

Moclobemide

Nabumetone

Nadolol

Naproxen

Nebivolol

Nialamide

Niflumic Acid

Nimesulide

Oxaprozin

Oxprenolol

Oxyphenbutazone

Pargyline

Penbutolol

Phenelzine

Phenylbutazone

Pindolol

Pirazolac

Piroxicam

Pirprofen

Procarbazine

Propranolol

Propyphenazone

Proquazone

Psyllium

Rifampin

Rifapentine

Selegiline

Sotalol

Sulfamethoxazole

Sulindac

Suprofen

Talinolol

Tenidap

Tenoxicam

Tertatolol

Tiaprofenic Acid

Timolol

Tolmetin

Toloxatone

Tranylcypromine

Voriconazole

Warfarin

Zomepirac

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. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

Ethanol

Proper Use of glyburide

This section provides information on the proper use of a number of products that contain glyburide. It may not be specific to Micronase. Please read with care.

Follow carefully the special meal plan your doctor gave you. This is the most important part of controlling your condition, and is necessary if the medicine is to work properly. Also, exercise regularly and test for sugar in your blood or urine as directed.

Use only the brand of this medicine that your doctor prescribed. Different brands may not work the same way.

Dosing

The dose of this medicine 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 this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

For type 2 diabetes:
- For oral dosage form (tablets):
  - Adults—At first, 2.5 to 5 milligrams (mg) once a day taken with breakfast or the first main meal. Your doctor may adjust your dose if needed. However, the dose is usually not more than 20 mg per day.
  - Children—Use and dose must be determined by your doctor.
- For oral dosage form (micronized tablets):
  - Adults—At first, 1.5 to 3 milligrams (mg) once a day taken with breakfast or the first main meal. Your doctor may adjust your dose if needed. The dose is usually not more than 12 mg per day.
  - Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, 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 Micronase

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly. Blood tests may be needed to check for unwanted effects.

It is very important to follow carefully any instructions from your health care team about:

Alcohol—Drinking alcohol may cause severe low blood sugar. Discuss this with your health care team.

Counseling—Other family members need to learn how to prevent side effects or help with side effects if they occur. Also, patients with diabetes may need special counseling about diabetes medicine dosing changes that might occur because of lifestyle changes, such as changes in exercise and diet. Furthermore, counseling on contraception and pregnancy may be needed because of the problems that can occur in patients with diabetes during pregnancy.

Travel—Keep your recent prescription and your medical history with you. Be prepared for an emergency as you would normally. Make allowances for changing time zones and keep your meal times as close as possible to your usual meal times.

In case of emergency—There may be a time when you need emergency help for a problem caused by your diabetes. You need to be prepared for these emergencies. It is a good idea to wear a medical identification (ID) bracelet or neck chain at all times. Also, carry an ID card in your wallet or purse that says you have diabetes and a list of all of your medicines.

Check with your doctor right away if you start having chest pain or discomfort; nausea; pain or discomfort in arms, jaw, back, or neck; shortness of breath; sweating; or vomiting while you are using this medicine. These may be symptoms of a serious heart problem, including a heart attack.

Too much glyburide can cause low blood sugar (hypoglycemia) when it is used under certain conditions. Symptoms of low blood sugar must be treated before they lead to unconsciousness (passing out). Different people may feel different symptoms of low blood sugar. It is important that you learn which symptoms of low blood sugar you usually have so that you can treat it quickly and call someone on your health care team right away when you need advice.

Symptoms of hypoglycemia (low blood sugar) include anxiety; behavior change similar to being drunk; blurred vision; cold sweats; confusion; cool, pale skin; difficulty in thinking; drowsiness; excessive hunger; fast heartbeat; headache (continuing); nausea; nervousness; nightmares; restless sleep; shakiness; slurred speech; or unusual tiredness or weakness.

If symptoms of low blood sugar occur, eat glucose tablets or gel, corn syrup, honey, or sugar cubes; or drink fruit juice, non-diet soft drink, or sugar dissolved in water. Also, check your blood for low blood sugar. Glucagon is used in emergency situations when severe symptoms such as seizures (convulsions) or unconsciousness occur. Have a glucagon kit available, along with a syringe or needle, and know how to use it. Members of your household also should know how to use it.

Do not take this medicine if you are also using bosentan (Tracleer®). Also, make sure your doctor knows about all other medicines you are using for diabetes, including insulin.

Micronase 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:

Less common

Difficulty with swallowing

dizziness

fast heartbeat

hives

itching

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

shortness of breath

skin rash

tightness in the chest

unusual tiredness or weakness

wheezing

Rare

Abdominal or stomach pain

chills

clay-colored stools

dark urine

diarrhea

fever

headache

light-colored stools

loss of appetite

nausea and vomiting

rash

unpleasant breath odor

upper right abdominal pain

vomiting of blood

yellow eyes and skin

Incidence not known

Agitation

back, leg, or stomach pains

bleeding gums

blood in the urine or stools

bloody, black, or tarry stools

blurred vision

change in near or distance vision

chest pain

coma

confusion

convulsions

cough or hoarseness

decreased urine output

depression

difficulty in focusing eyes

difficulty with breathing

fast or irregular heartbeat

fluid-filled skin blisters

general body swelling

high fever

hostility

increased thirst

irritability

itching of the skin

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

lethargy

lower back or side pain

muscle pain or cramps

muscle twitching

nosebleeds

painful or difficult urination

pale skin

pinpoint red spots on the skin

rapid weight gain

seizures

sensitivity to the sun

skin thinness

sore throat

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

stupor

swelling of the face, ankles, or hands

swollen or painful glands

unusual bleeding or bruising

Get emergency help immediately if any of the following symptoms of overdose occur:

Symptoms of overdose

Anxiety

cold sweats

cool, pale skin

increased hunger

nervousness

nightmares

shakiness

slurred speech

Less common

Indigestion

passing of gas

Incidence not known

Difficulty with moving

itching

joint pain

redness or other discoloration of the skin

severe sunburn

swollen joints

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: Micronase side effects (in more detail)

More Micronase resources

Micronase Side Effects (in more detail)
Micronase Dosage
Micronase Use in Pregnancy & Breastfeeding
Drug Images
Micronase Drug Interactions
Micronase Support Group
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Micronase Prescribing Information (FDA)

Micronase MedFacts Consumer Leaflet (Wolters Kluwer)

Micronase Concise Consumer Information (Cerner Multum)

DiaBeta Prescribing Information (FDA)

Glyburide Monograph (AHFS DI)

Glyburide Professional Patient Advice (Wolters Kluwer)

Compare Micronase with other medications

Diabetes, Type 2