Itraconazole

Class: Azoles
VA Class: AM700
Chemical Name: 4 - [4 - [4 - [4 - [[2 - (2,4 - dichlorophenyl) - 2 - (1H - 1,2,4 - triazol - 1 - ylmethyl) - 1,3 - dioxolan - 4 - l]methoxy]phenyl] - 1 - piperazinyl]phenyl] - 2,4 - dihydro - 2 - (1 - methylpropyl) - 3H - 1,2,4 - triazol - 3 - one
CAS Number: 84625-61-6
Brands: Sporanox

• 
  

  Itraconazole capsules should not be used for treatment of onychomycosis in patients with evidence of ventricular dysfunction, including CHF or history of CHF.¹

  
  


• 
  

  Discontinue itraconazole if signs or symptoms of CHF occur.¹ IV itraconazole (no longer commercially available in the US) caused negative inotropic effects in healthy individuals and in dogs.^{1 48}

  
  


• 
  

  Concomitant use with cisapride (currently commercially available in the US only under a limited-access protocol), pimozide, quinidine, dofetilide, or levomethadyl (no longer commercially available in the US) is contraindicated.^{1 48} Itraconazole is a potent inhibitor of CYP3A4 isoenzymes and may increase plasma concentrations of drugs metabolized by CYP3A4.^{1 48} Serious cardiovascular events, including QT prolongation, torsades de pointes, ventricular tachycardia, cardiac arrest, and/or sudden death have occurred in patients using cisapride, pimozide, levomethadyl, or quinidine concomitantly with itraconazole and/or other CYP3A4 inhibitors.^{1 48} (See Interactions.)

  
  

Introduction

Antifungal; azole (triazole derivative).^{1 3 37 48}

Uses for Itraconazole

Aspergillosis

Treatment of invasive aspergillosis.^{1 66 423} Considered an alternative, not a drug of choice.^{1 423 436}

Treatment of pulmonary and extrapulmonary aspergillosis in patients intolerant of, or whose disease is refractory to, IV amphotericin B.^{1 66}

IDSA considers voriconazole the drug of choice for primary treatment of invasive aspergillosis in most patients and IV amphotericin B the preferred alternative.⁴²³ For salvage therapy in patients refractory to or intolerant of primary antifungal therapy, IDSA recommends amphotericin B, caspofungin, micafungin, posaconazole, or itraconazole.⁴²³ For empiric or preemptive therapy of presumed aspergillosis, IDSA recommends amphotericin B, caspofungin, itraconazole, or voriconazole.⁴²³

Not considered a drug of choice or preferred alternative for treatment of invasive aspergillosis in HIV-infected individuals.^{440 441} For treatment of invasive aspergillosis in HIV-infected adults and adolescents, CDC, NIH, and IDSA recommend voriconazole as the drug of choice;⁴⁴⁰ voriconazole also considered the drug of choice for treatment of invasive aspergillosis in HIV-infected children.⁴⁴¹ Because the drugs have similar mechanisms of action and cross-resistance may occur, itraconazole not recommended for treatment of aspergillosis refractory to voriconazole.⁴⁴¹

For primary prophylaxis of aspergillosis in immunocompromised individuals at high risk of invasive disease (i.e., neutropenic patients with acute myelogenous leukemia [AML] or myelodysplastic syndrome [MDS], hematopoietic stem cell transplant [HSCT] recipients with graft-versus-host disease [GVHD]), IDSA considers posaconazole the drug of choice;⁴²³ alternatives are itraconazole or micafungin.⁴²³

Blastomycosis

Treatment of pulmonary and extrapulmonary blastomycosis caused by Blastomyces dermatitidis.^{1 36 49 50 51 52 53 54 59 62 63 424 436}

Drugs of choice are oral itraconazole or IV amphotericin B.^{36 49 50 51 52 436}

IV amphotericin B is preferred for initial treatment of severe blastomycosis, especially infections involving the CNS^{51 52 55 56 50 51 52 53 54 61 424 436} and for initial treatment of presumptive blastomycosis in immunocompromised patients, including HIV-infected individuals.^{50 55 61 424}

Itraconazole is the drug of choice for treatment of nonmeningeal, non-life-threatening blastomycosis, including mild to moderate pulmonary blastomycosis or mild to moderate disseminated blastomycosis (without CNS involvement), and also is recommended for follow-up therapy in patients with more severe infections after an initial response has been obtained with IV amphotericin B.^{36 61 62 63 424 436}

Azole antifungals should not be relied on for initial treatment of CNS blastomycosis.⁴²⁴ Treatment failures have been reported when an oral antifungal (e.g., ketoconazole) was used in the treatment of cutaneous or pulmonary blastomycosis in patients who had asymptomatic or subclinical CNS involvement at the time of the initial diagnosis.^{57 58}

IDSA states that long-term suppressive or maintenance therapy (secondary prophylaxis)† with itraconazole may be required to prevent relapse or recurrence of blastomycosis in immunocompromised patients and in other patients who experience relapse despite appropriate therapy.⁴²⁴ Such prophylaxis is not addressed in current CDC, NIH, and IDSA guidelines for prevention of opportunistic infections in individuals infected with HIV.^{440 441}

Candidemia and Other Invasive Candida Infections

Not a drug of choice or preferred alternative for treatment of candidemia† or other invasive Candida infections†.^{425 436} Fluconazole or voriconazole usually are recommended when an azole antifungal is used for treatment of candidemia.^{425 436}

Has been used and is recommended as an alternative for initial empiric treatment of suspected invasive candidiasis in neutropenic patients†.⁴²⁵ IV amphotericin B, caspofungin, or voriconazole are drugs of choice in these patients;⁴²⁵ alternatives are fluconazole or itraconazole.⁴²⁵ Do not use an azole antifungal for empiric treatment in patients who previously received an azole for prophylaxis.⁴²⁵

Oropharyngeal Candidiasis

Treatment of oropharyngeal candidiasis.^{48 425}

IDSA recommends topical treatment with clotrimazole lozenges or nystatin oral suspension for mild oropharyngeal candidiasis;⁴²⁵ oral fluconazole is recommended for moderate to severe disease.⁴²⁵ For refractory oropharyngeal candidiasis, including fluconazole-refractory infections, itraconazole oral solution, oral posaconazole, or oral voriconazole is recommended.⁴²⁵ An IV echinocandin (caspofungin, micafungin, anidulafungin) or IV amphotericin B also are recommended as alternatives for refractory infections.⁴²⁵

For treatment of oropharyngeal candidiasis in HIV-infected adults and adolescents, CDC, NIH, and IDSA recommend oral fluconazole as the preferred drug of choice for initial episodes;⁴⁴⁰ other drugs of choice are clotrimazole lozenges or nystatin oral suspension.⁴⁴⁰ Alternatives for initial episodes are itraconazole oral solution or oral posaconazole.⁴⁴⁰ For fluconazole-refractory infections in HIV-infected adults and adolescents, itraconazole oral solution or oral posaconazole is preferred;⁴⁴⁰ alternatives include IV amphotericin B, an IV echinocandin (caspofungin, micafungin, anidulafungin), or oral or IV voriconazole.⁴⁴⁰

Although routine long-term suppressive or maintenance therapy (secondary prophylaxis)† to prevent relapse or recurrence is not usually recommended in patients adequately treated for oropharyngeal candidiasis, patients with frequent or severe recurrences, including HIV-infected adults, adolescents, or children, may benefit from secondary prophylaxis with oral fluconazole or itraconazole oral solution; however, consider the potential for azole resistance.^{425 440 441} Patients with fluconazole-refractory oropharyngeal candidiasis who responded to treatment with an echinocandin should receive voriconazole or posaconazole for secondary prophylaxis until antiretroviral therapy produces immune reconstitution.⁴⁴⁰

Esophageal Candidiasis

Treatment of esophageal candidiasis.^{48 425}

Esophageal candidiasis requires treatment with a systemic antifungal (not a topical antifungal).^{425 440}

IDSA recommends oral fluconazole as the preferred drug of choice for treatment of esophageal candidiasis;⁴²⁵ if oral therapy is not tolerated, IV fluconazole, IV amphotericin B, or an IV echinocandin (caspofungin, micafungin, anidulafungin) is recommended.⁴²⁵ For fluconazole-refractory infections, preferred alternatives are itraconazole oral solution, oral posaconazole, or oral or IV voriconazole;⁴²⁵ other alternatives are an IV echinocandin (caspofungin, micafungin, anidulafungin) or IV amphotericin B.⁴²⁵

For treatment of esophageal candidiasis in HIV-infected adults and adolescents, CDC, NIH, and IDSA recommend oral or IV fluconazole as the preferred drug of choice and itraconazole oral solution as the preferred alternative.⁴⁴⁰ Other alternatives include an IV echinocandin (caspofungin, micafungin, anidulafungin), oral or IV voriconazole, oral posaconazole, or IV amphotericin B.⁴⁴⁰ For refractory esophageal candidiasis, including fluconazole-refractory infections, in HIV-infected adults and adolescents, itraconazole oral solution or oral posaconazole is preferred;⁴⁴⁰ alternatives include IV amphotericin B, an IV echinocandin (caspofungin, micafungin, anidulafungin), or oral or IV voriconazole.⁴⁴⁰

Although routine long-term suppressive or maintenance therapy (secondary prophylaxis)† to prevent relapse or recurrence is not usually recommended in patients adequately treated for esophageal candidiasis, patients with frequent or severe recurrences, including HIV-infected adults, adolescents, or children, may benefit from secondary prophylaxis with oral fluconazole or oral posaconazole; however, consider the potential for azole resistance.^{425 440 441} Patients with fluconazole-refractory esophageal candidiasis who responded to treatment with an echinocandin should receive voriconazole or posaconazole for secondary prophylaxis until antiretroviral therapy produces immune reconstitution.⁴⁴⁰ Itraconazole is not included in current recommendations for secondary prophylaxis of esophageal candidiasis.^{425 440}

Vulvovaginal Candidiasis

Has been used for treatment of uncomplicated vulvovaginal candidiasis†.⁴³⁶

Vulvovaginal candidiasis is usually treated with an intravaginal azole antifungal (e.g., butoconazole, clotrimazole, miconazole, terconazole, tioconazole) or a single-dose oral fluconazole regimen.^{425 436 443 444} Although some clinicians suggest that oral itraconazole or oral ketoconazole can be used as alternatives for treatment of vulvovaginal candidiasis,⁴³⁶ fluconazole is the only oral antifungal included in CDC recommendations for treatment of uncomplicated or complicated vulvovaginal candidiasis.⁴⁴³

Chromomycosis

Has been used for treatment of chromomycosis† (chromoblastomycosis) caused by various dematiaceous fungi (e.g., Cladosporium, Exophiala, Fonsecaea, Phialophora).^{43 60 71 72 73}

Coccidioidomycosis

Treatment and prevention of coccidioidomycosis† caused by Coccidioides immitis or C. posadasii.^{36 56 60 426 436 440 441} A drug of choice.^{426 436 440}

Antifungal treatment may not be necessary for mild, uncomplicated coccidioidal pneumonia since such infections may resolve spontaneously;⁴²⁶ treatment is recommended for patients with more severe or rapidly progressing infections, those with chronic pulmonary or disseminated infections, and immunocompromised or debilitated individuals (e.g., HIV-infected individuals, organ transplant recipients, those receiving immunosuppressive therapy, those with diabetes or cardiopulmonary disease).^{426 440 441}

For initial treatment of symptomatic pulmonary coccidioidomycosis and chronic fibrocavitary or disseminated (extrapulmonary) coccidioidomycosis, IDSA states than an oral azole (fluconazole or itraconazole) usually is recommended.⁴²⁶ IV amphotericin B is recommended as an alternative and is preferred for initial treatment of severely ill patients who have hypoxia or rapidly progressing disease, for immunocompromised individuals, or when azole antifungals cannot be used (e.g., pregnant women).⁴²⁶

For treatment of clinically mild coccidioidomycosis (e.g., focal pneumonia or a positive coccidioidal serologic test alone) in HIV-infected adults or adolescents, CDC, NIH, and IDSA recommend oral fluconazole or oral itraconazole.⁴⁴⁰ For treatment of diffuse pulmonary coccidioidomycosis or extrathoracic disseminated (nonmeningeal) coccidioidomycosis in HIV-infected adults and adolescents, CDC, NIH, and IDSA recommend initial therapy with IV amphotericin B followed by oral azole therapy.⁴⁴⁰ Alternatively, some experts recommend initial therapy with IV amphotericin B used in conjunction with an oral azole (e.g., fluconazole) followed by an oral azole alone.⁴⁴⁰

For treatment of diffuse pulmonary or disseminated coccidioidomycosis in HIV-infected infants and children, CDC, NIH, and IDSA recommend initial treatment with IV amphotericin B followed by oral fluconazole or oral itraconazole.⁴⁴¹ In those with severe disseminated disease, some experts recommend initial therapy with IV amphotericin B used in conjunction with an oral azole (e.g., fluconazole) followed by an oral azole alone.⁴⁴¹ Use of fluconazole or itraconazole alone may be sufficient for treatment of mild coccidioidomycosis in HIV-infected infants and children with only mild disease (e.g., focal pneumonia) and also can be considered an alternative for those with stable pulmonary or disseminated (nonmeningeal) coccidioidomycosis.⁴⁴¹

For treatment of coccidioidal meningitis in HIV-infected adults, adolescents, or children or for other individuals, fluconazole (with or without intrathecal amphotericin B) is the regimen of choice.^{426 440 441} Itraconazole may be an alternative to fluconazole in adults and adolescents.⁴⁴⁰ Consultation with an expert is recommended.^{440 441}

In HIV-infected adults and adolescents who live in areas where coccidioidomycosis is endemic, CDC, NIH, and IDSA recommend primary prophylaxis against coccidioidomycosis† in those who have positive IgM or IgG serologic tests and CD4⁺ T-cell counts <250/mm³ since these individuals may be at increased risk for development of active infections.⁴⁴⁰ Oral fluconazole or oral itraconazole should be used for primary prophylaxis against coccidioidomycosis in these HIV-infected adults and adolescents. ⁴⁴⁰ Primary prophylaxis against coccidioidomycosis is not recommended in HIV-infected children.⁴⁴¹

HIV-infected adults, adolescents, or children who have been adequately treated for coccidioidomycosis should receive long-term suppressive or maintenance therapy (secondary prophylaxis)† to prevent recurrence or relapse.^{440 441} CDC, NIH, and IDSA recommend oral fluconazole or oral itraconazole for secondary prophylaxis of coccidioidomycosis in HIV-infected individuals.^{440 441}

Long-term (life-long) suppressive or maintenance therapy (secondary prophylaxis)† with oral fluconazole or oral itraconazole also is necessary in any individual treated for coccidioidal meningitis.⁴²⁶

Cryptococcosis

Has been used for treatment of cryptococcosis†.^{36 49 68 427 436 440 441} Not a drug of choice or preferred alternative.^{427 440 441}

For treatment of cryptococcal meningitis in HIV-infected adults, adolescents, and children, CDC, NIH, and IDSA state that the preferred regimen is initial (induction) therapy with IV amphotericin B given in conjunction with oral flucytosine, then follow-up (consolidation) therapy with oral fluconazole.^{427 440 441} Although data are limited and use of the drug is discouraged, IDSA and others state that itraconazole can be considered an alternative for induction and consolidation therapy if all other alternative regimens have failed or are not available.^{427 440 441}

For treatment of mild to moderate pulmonary cryptococcosis in immunocompetent individuals, the regimen of choice is oral fluconazole.⁴²⁷ Although data are limited, IDSA states that itraconazole, voriconazole, and posaconazole are acceptable alternatives in immunocompetent individuals if fluconazole is unavailable or contraindicated.⁴²⁷

Severe pulmonary infections, cryptococcemia, and disseminated infections in immunocompetent or immunosuppressed individuals should be treated using regimens recommended for cryptococcal meningitis.⁴²⁷

HIV-infected adults, adolescents, and children who have been adequately treated for cryptococcus should receive long-term suppressive or maintenance therapy (secondary prophylaxis)† to prevent recurrence or relapse.^{427 440 441} CDC, NIH, and IDSA recommend oral fluconazole as the drug of choice for secondary prophylaxis of cryptococcosis in HIV-infected individuals;^{427 440 441} oral itraconazole is considered an alternative in those who cannot tolerate fluconazole, but may be less effective than fluconazole.^{427 440 441}

Although data are limited, IDSA states that recommendations for treatment of CNS or disseminated infections caused by Cryptococcus gattii and recommendations for secondary prophylaxis of C. gattii infections are the same as recommendations for C. neoformans infections.⁴²⁷

Histoplasmosis

Treatment of histoplasmosis caused by Histoplasma capsulatum, including chronic cavitary pulmonary disease and disseminated nonmeningeal disease.^{48 428 436 440 441}

Drugs of choice for treatment of histoplasmosis are IV amphotericin B and oral itraconazole.^{36 49 55 59 60 61 65 428 436 440 441} IV amphotericin B is preferred for initial treatment of severe, life-threatening histoplasmosis, especially in immunocompromised patients such as those with HIV infection.^{36 42 44 45 49 55 56 60 61 64 65 428 436 440 441} Oral itraconazole generally is used for initial treatment of less severe disease (e.g., mild to moderate acute pulmonary histoplasmosis, chronic cavitary pulmonary histoplasmosis) and as follow-up treatment of severe infections after a response has been obtained with IV amphotericin B.^{36 49 56 59 61 65 428 436 440 441}

For treatment of moderately severe to severe acute pulmonary histoplasmosis or progressive disseminated histoplasmosis in HIV-infected adults and adolescents and other adults, CDC, NIH, and IDSA recommend initial treatment with IV amphotericin B and follow-up treatment with oral itraconazole.^{428 440}

For treatment of progressive disseminated histoplasmosis in children, IDSA states that IV amphotericin B or an initial regimen of IV amphotericin B and follow-up treatment with oral itraconazole can be used.⁴²⁸ For treatment of moderately severe to severe disseminated histoplasmosis in HIV-infected infants and children, CDC, NIH, and IDSA recommend initial treatment with IV amphotericin B and follow-up treatment with oral itraconazole.⁴⁴¹ Although oral itraconazole may be used alone for treatment of mild to moderate disseminated histoplasmosis in children, including HIV-infected infants and children, it is not recommended for more severe infections.^{428 441}

HIV-infected adults or adolescents with CD4⁺ T-cell counts <150/mm³ who are at high risk because they reside in areas where histoplasmosis is highly endemic should receive primary prophylaxis† against initial episodes of histoplasmosis.^{428 436 440} Itraconazole is the drug of choice for primary prophylaxis against histoplasmosis in these HIV-infected adults and adolescents.^{428 436 440} Primary prophylaxis against histoplasmosis is not recommended in HIV-infected children.⁴⁴¹

HIV-infected adults, adolescents, or children and other immunosuppressed individuals who have been adequately treated for histoplasmosis should receive long-term suppressive or maintenance therapy (secondary prophylaxis)† to prevent recurrence or relapse.^{428 440 441} Itraconazole is the drug of choice for secondary prophylaxis against histoplasmosis†.^{428 440}

Microsporidiosis

Treatment of microsporidiosis†.^{135 136 440 442}

Has been effective in a few cases of keratoconjunctivitis or sinusitis caused by Encephalitozoon.^{135 136} Regimen of choice for ocular microsporidiosis is fumagillin (not commercially available in the US) used in conjunction with albendazole.^{440 441 442}

Alternative for disseminated microsporidiosis, especially infections caused by Trachipleistophora or Anncaliia;^{440 442} used in conjunction with albendazole.^{440 442} Albendazole usually is the drug of choice for intestinal or disseminated microsporidiosis (except infections caused by Enterocytozoon bienuesi or Vittaforma corneae).^{440 441 442}

Onychomycosis

Treatment of onychomycosis of the toenails (with or without fingernail involvement) and onychomycosis of the fingernails caused by dermatophytes (tinea unguium).^{1 132 133 436}

Paracoccidioidomycosis

Treatment of paracoccidioidomycosis† (South American blastomycosis) caused by Paracoccidioides brasiliensis.^{36 43 56 436}

IV amphotericin B is the drug of choice for initial treatment of severe paracoccidioidomycosis.⁴³⁶ Oral itraconazole is the drug of choice for treatment of less severe or localized paracoccidioidomycosis and for follow-up in more severe infections after initial treatment with IV amphotericin B.^{56 60}

Penicilliosis

Treatment of penicilliosis† caused by Penicillium marneffei.^{115 116 117 119 440}

For treatment of severe or disseminated P. marneffei infections, including in HIV-infected adults or adolescents, an initial regimen of IV amphotericin B followed by oral itraconazole is recommended.^{115 116 119 440} Oral itraconazole can be used alone for treatment of mild infections.⁴⁴⁰

Chronic suppressive or maintenance therapy (secondary prophylaxis) with oral itraconazole is recommended to prevent relapse of penicilliosis† in HIV-infected adults or adolescents who respond to an initial treatment regimen of IV amphoterin B and/or oral itraconazole.^{116 117 440}

Sporotrichosis

Treatment of sporotrichosis† caused by Sporothrix schenckii.^{43 49 55 56 61 67 429 436}

IV amphotericin B is the drug of choice for initial treatment of severe, life-threatening sporotrichosis and sporotrichosis that is disseminated or has CNS involvement.^{56 60 61 67 429 436} Oral itraconazole is the drug of choice for treatment of cutaneous, lymphocutaneous, or mild pulmonary or osteoarticular sporotrichosis and for follow-up treatment of severe infections after a response has been obtained with IV amphotericin B.^{43 56 60 61 67 429 436}

Zygomycosis

Treatment of GI basidiobolomycosis†, a zygomycosis caused by Basidiobolus ranarum.^{38 104 105 106 107}

Has been effective in a few patients for the treatment of subcutaneous basidiobolomycosis.^{124 125}

GI basidiobolomycosis has been successfully treated with oral itraconazole after partial surgical resection of the GI tract; unclear whether a clinical response would have been obtained if itraconazole had been used alone without surgical intervention.^{38 105}

Empiric Therapy in Febrile Neutropenic Patients

Has been used for empiric therapy of presumed fungal infections in febrile neutropenic patients.^{48 93 425}

Itraconazole Dosage and Administration

Administration

Administer orally.^{1 3 30 36 37 38 48}

Has been administered by IV infusion,⁷⁶ but an IV preparation is no longer commercially available in the US.

Oral Administration

Oral bioavailability varies depending on whether the drug is administered as capsules or the oral solution; these preparations should not be used interchangeably.^{1 48}

The possibility that GI absorption may be decreased in patients with hypochlorhydria (e.g., HIV-infected individuals) should be considered.^{1 10} (See Absorption under Pharmacokinetics.)

Capsules

The capsules should be administered with a full meal to ensure maximal absorption of the drug.¹

Capsules should not be used for treatment of oropharyngeal or esophageal candidiasis;^{425 440 441} efficacy not established,¹ may be less effective than oral solution for these infections.^{425 440 441}

If capsules are given in a dosage >200 mg daily, daily dosage should be divided into 2 doses.¹

Oral Solution

The oral solution should be administered without food to ensure maximal absorption of the drug.⁴⁸

For treatment of oropharyngeal or esophageal candidiasis, the recommended dosage of itraconazole oral solution should be vigorously swished in the mouth (10 mL at a time) for several seconds and then swallowed.⁴⁸

Manufacturer states that data are limited to date regarding the safety of long-term use of itraconazole oral solution (i.e., >6 months).⁴⁸

Dosage

Because of differences in oral bioavailability, itraconazole capsules and oral solution should not be used interchangeably.^{1 48}

Only the oral solution (not capsules) is indicated for treatment of oropharyngeal or esophageal candidiasis.⁴⁸

To ensure adequate plasma concentrations of itraconazole (especially in patients with life-threatening fungal infections), IDSA and others recommend that itraconazole plasma concentrations be determined, usually after 2 weeks of therapy.^{423 424 425 428 429}

Pediatric Patients

Blastomycosis†

Treatment of Blastomycosis†

Oral

Mild to moderate blastomycosis: IDSA recommends 10 mg/kg daily (up to 400 mg daily) for 6–12 months.⁴²⁴

Moderately severe to severe blastomycosis: IDSA recommends an initial regimen of IV amphotericin B given for 1–2 weeks, followed by itraconazole 10 mg/kg daily (up to 400 mg daily) for a total treatment duration of 12 months.⁴²⁴

Candida Infections†

Treatment of Oropharyngeal Candidiasis†

Oral

HIV-infected infants and children (oral solution): 2.5 mg/kg twice daily (up to 200 mg daily) for 7–14 days.⁴⁴¹

HIV-infected infants and children with fluconazole-refractory infections (oral solution): 2.5 mg/kg twice daily (up to 200–400 mg daily) for 7–14 days.⁴⁴¹

HIV-infected adolescents (oral solution): 200 mg daily for 7–14 days.⁴⁴⁰ Same dosage can be used for fluconazole-refractory infections.⁴⁴⁰

Prevention of Recurrence (Secondary Prophylaxis) of Oropharyngeal Candidiasis†

Oral

HIV-infected adolescents (oral solution): 200 mg daily.⁴⁴⁰

Secondary prophylaxis not usually recommended; use only if patient has frequent or severe recurrences.⁴⁴⁰ Consider discontinuing secondary prophylaxis if CD4⁺ T-cell count increases to ≥200/mm³ in response to antiretroviral therapy.⁴⁴⁰

Treatment of Esophageal Candidiasis†

Oral

HIV-infected infants and children (oral solution): 2.5 mg/kg twice daily or 5 mg/kg once daily for 14–21 days.⁴⁴¹

HIV-infected adolescents (oral solution): 200 mg daily for 14–21 days.⁴⁴⁰

Treatment of Vulvovaginal Candidiasis†

Oral

HIV-infected adolescents (oral solution): 200 mg daily for 3–7 days.⁴⁴⁰

Coccidioidomycosis†

Treatment of Coccidioidomycosis (Nonmeningeal)†

Oral

HIV-infected infants and children with mild coccidioidomycosis (e.g., focal pneumonia): 5–10 mg/kg twice daily for 3 days, then 2–5 mg/kg twice daily.⁴⁴¹

HIV-infected infants and children with diffuse pulmonary or disseminated coccidioidomycosis: Initial regimen of IV amphotericin B given until a response is obtained, followed by itraconazole 5–10 mg/kg twice daily for 3 days, then 2–5 mg/kg twice daily (up to 400 mg daily).⁴⁴¹

HIV-infected adolescents with mild coccidioidomycosis (e.g., focal pneumonia or positive coccidioidal serologic test alone): 200 mg 3 times daily for 3 days, then 200 mg twice daily.⁴⁴⁰

Treatment of Coccidioidal Meningitis†

Oral

HIV-infected adolescents with meningeal coccidioidomycosis: 200 mg 3 times daily for 3 days, then 200 mg twice daily.⁴⁴⁰

Consultation with an expert experienced in treating coccidioidal meningitis is recommended.⁴⁴¹

Primary Prophylaxis to Prevent First Episode of Coccidioidomycosis†

Oral

HIV-infected adolescents living in areas endemic for coccidioidomycosis who have positive IgM or IgG serologic test and CD4⁺ T-cell count <250/mm³: 200 mg twice daily.⁴⁴⁰

Consider discontinuing primary prophylaxis if CD4⁺ T-cell count is >250/mm³ for 6 months.⁴⁴⁰ Reinitiate primary prophylaxis against coccidioidomycosis if CD4⁺ T-cell count decreases to <250/mm³.⁴⁴⁰

Prevention of Recurrence (Secondary Prophylaxis) of Coccidioidomycosis†

Oral

HIV-infected infants and children: 2–5 mg/kg (up to 200 mg) twice daily.⁴⁴¹

HIV-infected adolescents: 200 mg twice daily.⁴⁴⁰

Initiate secondary prophylaxis after primary infection has been adequately treated.^{440 441}

HIV-infected infants and children: Continue life-long, secondary prophylaxis against coccidioidomycosis, regardless of antiretroviral therapy or immune reconstitution.⁴⁴¹

HIV-infected adolescents with history of focal coccidioidal pneumonia who responded to antifungal treatment, are receiving antiretroviral therapy, and have CD4⁺ T-cell counts >250/mm³: Consider discontinuing secondary prophylaxis against coccidioidomycosis after 12 months, but continue monitoring for recurrence (e.g., serial chest radiographs, coccidioidal serology).⁴⁴⁰

HIV-infected adolescents with history of diffuse pulmonary or disseminated coccidioidomycosis or history of coccidioidal meningitis: Continue life-long secondary prophylaxis against coccidioidomycosis, regardless of antiretroviral therapy or immune reconstitution.⁴⁴⁰

Cryptococcosis†

Treatment of Cryptococcosis†

Oral

HIV-infected infants and children with CNS cryptococcosis: Initial (induction) regimen of IV amphotericin B given for at least 2 weeks, then follow-up (consolidation) regimen of itraconazole 200 mg 3 times daily for 3 days, then 5–10 mg/kg (maximum 200 mg) once or twice daily for at least 8 weeks.⁴⁴¹

HIV-infected adolescents with CNS cryptococcosis: Initial (induction) regimen of IV amphotericin B given for at least 2 weeks, then follow-up (consolidation) regimen of itraconazole 200 mg twice daily for 8 weeks or until CD4⁺ T-cell count is ≥200/mm³ for at least 6 months as the result of antiretroviral therapy.⁴⁴⁰

Some clinicians suggest the oral solution may be preferred (instead of capsules) for treatment of cryptococcosis.⁴²⁷

Prevention of Recurrence (Secondary Prophylaxis) of Cryptococcosis†

Oral

HIV-infected infants and children (oral solution): 5 mg/kg (up to 200 mg) daily.⁴⁴¹

HIV-infected adolescents: 200 mg daily.⁴⁴⁰

Initiate secondary prophylaxis after primary infection has been adequately treated.^{440 441}

HIV-infected infants and children with a history of cryptococcosis usually should receive life-long suppressive therapy to prevent recurrence.⁴⁴¹ Consideration can be given to discontinuing secondary prophylaxis in HIV-infected children ≥6 years of age who are asymptomatic for cryptococcosis, have received secondary prophylaxis for ≥6 months, have been receiving antiretroviral therapy for ≥6 months, and have CD4⁺ T-cell counts ≥200/mm³ for ≥6 months.⁴⁴¹ Reinitiate secondary prophylaxis against cryptococcosis if CD4⁺ T-cell count decreases to <200/mm³.⁴⁴¹

HIV-infected adolescents with a history of cryptococcosis usually should receive life-long secondary prophylaxis to prevent recurrence.⁴⁴⁰ Some experts state that consideration can be given to discontinuing secondary prophylaxis in HIV-infected adolescents who are asymptomatic for cryptococcosis, are receiving antiretroviral therapy, and have CD4⁺ T-cell counts ≥200/mm³ for >6 months.⁴⁴⁰ Reinitiate secondary prophylaxis against cryptococcosis if CD4⁺ T-cell count decreases to <200/mm³.⁴⁴⁰

Histoplasmosis†

Treatment of Histoplasmosis†

Oral

Acute pulmonary histoplasmosis: IDSA recommends 5–10 mg/kg daily (up to 400 mg daily) given in 2 divided doses.⁴²⁸

Progressive disseminated histoplasmosis: IDSA recommends initial regimen of IV amphotericin B given for 2–4 weeks, followed by itraconazole 5–10 mg/kg daily (up to 400 mg daily) given in 2 divided doses for a total duration of 3 months.⁴²⁸ A longer duration may be necessary in children with severe disease or with immunosuppression or primary immunodeficiency syndromes.⁴²⁸

HIV-infected infants and children with mild disseminated histoplasmosis (oral solution): 2–5 mg/kg (up to 200 mg) 3 times daily for 3 days, then 2–5 mg/kg (up to 200 mg) twice daily for 12 months.⁴⁴¹

HIV-infected infants and children with moderately severe to severe disseminated histoplasmosis: Initial regimen of IV amphotericin B given for at least 1–2 weeks, followed by itraconazole (oral solution) 2–5 mg/kg (up to 200 mg) 3 times daily for 3 days, then 2–5 mg/kg (up to 200 mg) twice daily for 12 months.⁴⁴¹

HIV-infected infants and children with CNS histoplasmosis: Initial regimen of IV amphotericin B given for 4–6 weeks, followed by itraconazole (oral solution) 2–5 mg/kg (up to 200 mg) 3 times daily for 3 days, then 2–5 mg/kg (up to 200 mg) twice daily for at least 12 months and until CSF abnormalities resolve and histoplasmal antigen is undetectable.⁴⁴¹

HIV-infected adolescents with less severe disseminated histoplasmosis: 200 mg 3 times daily for 3 days, then 200 mg twice daily for at least 12 months.⁴⁴⁰

HIV-infected adolescents with moderately severe to severe disseminated histoplasmosis: Initial regimen of IV amphotericin B given for at least 2 weeks or until a response is obtained, followed by itraconazole 200 mg 3 times daily for 3 days, then 200 mg twice daily for a total duration of at least 12 months and until histoplasmal antigen is undetectable.⁴⁴¹

HIV-infected adolescents with CNS histoplasmosis: Initial regimen of IV amphotericin B given for 4–6 weeks or until a response is obtained, followed by itraconazole 200 mg 2 or 3 times daily for at least 12 months and until CSF abnormalities resolve and histoplasmal antigen is undetectable.⁴⁴¹

Some clinicians suggest the oral solution may be preferred (instead of capsules) f

influenza a virus vaccine, h1n1, live Nasal

in-floo-EN-za AY VYE-rus VAX-een, H1N1, lyve

Available Dosage Forms:

• Spray

Therapeutic Class: Vaccine

Uses For influenza a virus vaccine, h1n1, live

Influenza virus vaccine, H1N1 is used to prevent an infection caused by the influenza A (H1N1) 2009 virus. The vaccine works by causing your body to produce its own protection (antibodies) against the disease.

Influenza is a virus infection of the throat, bronchial tubes, and lungs. Influenza infection causes fever, chills, cough, headache, muscle aches, and pains in your back, arms, and legs. In addition, adults and children weakened by other diseases or medical conditions, and persons 50 years of age and over, even if they are healthy, may get a much more serious illness that may have to be treated in a hospital. Each year thousands of people die as a result of an influenza infection.

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

Before Using influenza a virus vaccine, h1n1, live

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

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to influenza a virus vaccine, h1n1, live 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 nasal influenza virus vaccine, H1N1 in children up to 2 years of age. Safety and efficacy have not been established.

Children under 5 years of age with one or more episodes of wheezing in the past year should not receive this vaccine.

Geriatric

Appropriate studies have not been performed on the relationship of age to the effects of nasal influenza virus vaccine, H1N1 in adults 50 years of age and older. Safety and efficacy have not been established.

Pregnancy

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

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this vaccine. Make sure you tell your doctor if you have any other medical problems, especially:

• Allergy to eggs, egg products, or gelatin, history of—Should not be used in patients with these conditions.

• Asthma, severe or


• Wheezing—Use with caution. May make these conditions worse.

• Guillain-Barré syndrome, history of—May cause the symptoms of this condition to return.

• Immune system problems (e.g., cancer, HIV)—This vaccine may not work as well if you have weak immune system.

Proper Use of influenza a virus vaccine, h1n1, live

A nurse or other trained health professional will give you or your child this vaccine. This vaccine is given as a nasal spray.

Use the nasal spray only in the nose. Do not get any of it in your eyes or on your skin. If it does get on these areas, rinse it off right away.

Before using the nasal spray, gently blow your nose to clear the nostrils.

Children 2 to 9 years of age who have not received the nasal vaccine before should receive 2 doses at least 1 month apart.

Precautions While Using influenza a virus vaccine, h1n1, live

It is very important that your child return to your doctor's office at the right time for the second dose. Be sure to notify your doctor of any side effects that occur after your child receives this vaccine.

This vaccine should not be given to children and teenagers (2 to 17 years of age) who are also using aspirin or any medicine that contains aspirin (e.g., Aggrenox®, Soma® Compound, Norgesic®, and many cold medicines).

Children under 2 years of age are usually not given the flu vaccine nasal spray. Young children who need the flu vaccine are usually given the flu vaccine injection (a shot).

This vaccine should not be given to pregnant women.

The nasal influenza virus vaccine, H1N1 contains a live virus. Avoid contact with people who are sick or at increased risk of getting the infection after you receive this vaccine. Talk to your doctor about this if you have concerns.

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

This vaccine will not treat flu symptoms if you already have the virus. Also, this vaccine may not protect all persons given the vaccine.

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

influenza a virus vaccine, h1n1, live Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

• Chills


• cough


• fever


• runny nose


• sore throat


• stuffy nose


• wheezing

Less common

• Headache


• pain or tenderness around the eyes and cheekbones


• shortness of breath or troubled breathing


• tightness of the chest

Incidence not known

• Bloody nose


• difficulty with swallowing


• dizziness


• fast heartbeat


• hives


• inability to move the arms and legs


• itching


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


• skin rash


• sudden numbness and weakness in the arms and legs


• unusual tiredness or weakness


• weakness of the muscles in your face

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Abdominal or stomach pain


• decreased appetite


• irritability


• muscle aches


• tiredness or weakness


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

Less common

• Earache


• redness or swelling in the ear

Incidence not known

• Diarrhea


• nausea


• 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.

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.

Imodium Multi-Symptom Relief

Pronunciation: loe-PER-a-mide/sye-METH-i-kone
Generic Name: Loperamide/Simethicone
Brand Name: Imodium Multi-Symptom Relief

Imodium Multi-Symptom Relief is used for:

Treating the symptoms of diarrhea plus bloating, pressure, and cramps from gas.

Imodium Multi-Symptom Relief is an antidiarrheal and antiflatulent combination. It works by slowing the movement of bowel contents. It also breaks up gas bubbles to make gas easier to eliminate.

Do NOT use Imodium Multi-Symptom Relief if:

• you are allergic to any ingredient in Imodium Multi-Symptom Relief


• you have stomach pain without diarrhea


• you have constipation; stomach bloating; bloody stools; or dark, tarry stools.

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

Before using Imodium Multi-Symptom Relief:

Some medical conditions may interact with Imodium Multi-Symptom Relief. 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 bloody diarrhea; mucus in your stool; fever; bowel problems (eg, inflammation, blockage, enlarged colon); or diarrhea caused by food poisoning, antibiotic use, or bacterial infection.


• if you have AIDS or liver problems


• if you are taking an antibiotic

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

• Quinidine or ritonavir because they may increase the risk of Imodium Multi-Symptom Relief's side effects


• Saquinavir because its effectiveness may be decreased by Imodium Multi-Symptom Relief

This may not be a complete list of all interactions that may occur. Ask your health care provider if Imodium Multi-Symptom Relief 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 Imodium Multi-Symptom Relief:

Use Imodium Multi-Symptom Relief as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Imodium Multi-Symptom Relief by mouth with or without food.


• Drinking extra fluids is recommended while you have diarrhea. Check with your doctor if you have questions.


• If you miss a dose of Imodium Multi-Symptom Relief, take it as soon as you remember. Continue to take it as directed by your doctor or on the package label.

Ask your health care provider any questions you may have about how to use Imodium Multi-Symptom Relief.

Important safety information:

• Imodium Multi-Symptom Relief may cause drowsiness, dizziness, or tiredness. These effects may be worse if you take it with alcohol or certain medicines. Use Imodium Multi-Symptom Relief with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Do not take more than the recommended dose or use for longer than 48 hours without checking with your doctor.


• If your diarrhea does not get better within 48 hours or if it gets worse, contact your doctor.


• If you develop a fever, stomach bloating or swelling, or blood in your stools, contact your doctor.


• Imodium Multi-Symptom Relief is used to treat the symptoms of diarrhea, but will not treat the condition causing the diarrhea. Check with your doctor if you have any questions or concerns about the cause of your diarrhea.


• Caution is advised when using Imodium Multi-Symptom Relief in CHILDREN; they may be more sensitive to its effects, especially dehydration.


• Do not use Imodium Multi-Symptom Relief in CHILDREN younger than 6 years old without checking with the child's doctor.


• PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Imodium Multi-Symptom Relief while you are pregnant. Imodium Multi-Symptom Relief is found in breast milk. Do not breast-feed while taking Imodium Multi-Symptom Relief.

Possible side effects of Imodium Multi-Symptom Relief:

All medicines may cause side effects, but many people have no, or minor, side effects. No COMMON side effects have been reported with this product. 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); constipation; decreased urination; red, swollen, blistered, or peeling skin; stomach bloating, swelling, or pain.

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: Imodium Multi-Symptom Relief 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 decreased urination; nausea; severe constipation or drowsiness; vomiting.

Proper storage of Imodium Multi-Symptom Relief:

Store at room temperature, between 59 and 77 degrees F (15 and 25 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Imodium Multi-Symptom Relief out of the reach of children and away from pets.

General information:

• If you have any questions about Imodium Multi-Symptom Relief, please talk with your doctor, pharmacist, or other health care provider.


• Imodium Multi-Symptom Relief 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 Imodium Multi-Symptom Relief. 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 Imodium Multi-Symptom Relief resources

• Imodium Multi-Symptom Relief Side Effects (in more detail)
• Imodium Multi-Symptom Relief Use in Pregnancy & Breastfeeding
• Imodium Multi-Symptom Relief Drug Interactions
• 0 Reviews for Imodium Multi-Symptom Relief - Add your own review/rating

Compare Imodium Multi-Symptom Relief with other medications

• Diarrhea, Acute

Instacort-10

Generic Name: hydrocortisone (Topical application route)

hye-droe-KOR-ti-sone

Commonly used brand name(s)

In the U.S.

• Ala-Cort


• Ala-Scalp HP


• Anusol HC


• Aquanil HC


• Beta HC


• Caldecort


• Cetacort


• Corta-Cap


• Cortagel Extra Strength


• Cortaid


• CortAlo With Aloe


• Corticaine


• Corticool Maximum Strength


• Cortizone-10


• Cortizone-5


• Cotacort


• Delacort


• Dermarest


• Dermtex-HC


• Foille Cort


• Gly-Cort


• Hydrozone Plus


• Hytone


• Instacort-10


• Ivy Soothe


• IvyStat


• Keratol HC


• Kericort 10


• Lacticare-HC


• Locoid


• Locoid Lipocream


• Medi-Cortisone Maximum Strength


• Microcort


• Mycin Scalp


• Neutrogena T/Scalp


• NuCort


• Nupercainal HC


• Nutracort


• Pandel


• Pediaderm HC Kit


• Preparation H Hydrocortisone


• Proctocream-HC


• Recort Plus


• Sarnol-HC Maximum Strength


• Scalacort


• Scalpcort


• Summer's Eve Specialcare


• Texacort


• Therasoft Anti-Itch & Dermatitis


• U-Cort


• Westcort

In Canada

• Barriere-Hc


• Cortate


• Cort-Eze


• Cortoderm Mild Ointment


• Cortoderm Regular Ointment


• Emo-Cort


• Emo-Cort Scalp Solution


• Hydrocortisone Cream


• Novo-Hydrocort


• Novo-Hydrocort Cream


• Prevex Hc


• Sarna Hc

Available Dosage Forms:

• Solution


• Cream


• Spray


• Lotion


• Ointment


• Pad


• Liquid


• Gel/Jelly


• Kit


• Foam


• Stick


• Paste

Therapeutic Class: Corticosteroid, Weak

Pharmacologic Class: Adrenal Glucocorticoid

Uses For Instacort-10

Hydrocortisone topical is used to help relieve redness, itching, swelling, or other discomfort caused by skin conditions. This medicine is a corticosteroid (cortisone-like medicine or steroid).

This medicine is available both over-the-counter (OTC) and with your doctor's prescription.

Before Using Instacort-10

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 performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of hydrocortisone topical in the pediatric population. However, because of this medicine's toxicity, it should be used with caution. Children may absorb large amounts through the skin, which can cause serious side effects. If your child is using this medicine, follow your doctor's instructions very carefully.

Geriatric

No information is available on the relationship of age to the effects of hydrocortisone topical in geriatric patients.

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. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Cushing's syndrome (adrenal gland disorder) or


• Diabetes or


• Hyperglycemia (high blood sugar) or


• Intracranial hypertension (increased pressure in the head)—Use with caution. May make these conditions worse.

• Infection of the skin at or near the place of application or


• Large sores, broken skin, or severe skin injury at the place of application—The chance of side effects may be increased.

Proper Use of hydrocortisone

This section provides information on the proper use of a number of products that contain hydrocortisone. It may not be specific to Instacort-10. Please read with care.

It is very important that you use this medicine only as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may cause unwanted side effects or skin irritation.

This medicine is for use on the skin only. Do not get it in your eyes. Do not use it on skin areas that have cuts, scrapes, or burns. If it does get on these areas, rinse it off right away with water.

This medicine should only be used for skin conditions that your doctor is treating. Check with your doctor before using it for other conditions, especially if you think that a skin infection may be present. This medicine should not be used to treat certain kinds of skin infections or conditions, such as severe burns.

To use:

• Wash your hands with soap and water before and after using this medicine.


• Apply a thin layer of this medicine to the affected area of the skin. Rub it in gently.


• With the lotion, shake it well before using.


• Do not bandage or otherwise wrap the skin being treated unless directed to do so by your doctor.


• If the medicine is applied to the diaper area of an infant, do not use tight-fitting diapers or plastic pants unless directed to do so by your doctor.


• If your doctor ordered an occlusive dressing or airtight covering to be applied over the medicine, make sure you know how to apply it. Occlusive dressings increase the amount of medicine absorbed through your skin, so use them only as directed. If you have any questions about this, check with your doctor.

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.

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 redness, itching, and swelling of the skin:
  
  • For topical dosage form (cream):
    
    • Adults—Apply to the affected area of the skin two or three times per day.
    
    
    • Children—Apply to the affected area of the skin two or three times per day.
    
    
  
  
  • For topical dosage form (lotion):
    
    • Adults—Apply to the affected area of the skin two to four times per day.
    
    
    • Children—Apply to the affected area of the skin two to four times per day.
    
    
  
  
  • For topical dosage form (ointment):
    
    • Adults—Apply to the affected area of the skin three or four times per day.
    
    
    • Children—Apply to the affected area of the skin three or four times per day.
    
    
  
  
  • For topical dosage form (solution):
    
    • Adults—Apply to the affected area of the skin three or four times per day.
    
    
    • Children—Apply to the affected area of the skin three or four times per day.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, apply 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.

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 Instacort-10

It is very important that your doctor check your or your child's progress at regular visits for any unwanted effects that may be caused by this medicine.

If your or your child's symptoms do not improve within a few days, or if they become worse, check with your doctor.

Using too much of this medicine or using it for a long time may increase your risk of having adrenal gland problems. The risk is greater for children and patients who use large amounts for a long time. Talk to your doctor right away if you or your child have more than one of these symptoms while you are using this medicine: blurred vision; dizziness or fainting; a fast, irregular, or pounding heartbeat; increased thirst or urination; irritability; or unusual tiredness or weakness.

Stop using this medicine and check with your doctor right away if you or your child have a skin rash, burning, stinging, swelling, or irritation on the skin.

Do not use cosmetics or other skin care products on the treated areas.

Instacort-10 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:

Incidence not known

• Blistering, burning, crusting, dryness, or flaking of the skin


• irritation


• itching, scaling, severe redness, soreness, or swelling of the skin


• redness and scaling around the mouth


• thinning of the skin with easy bruising, especially when used on the face or where the skin folds together (e.g. between the fingers)


• thinning, weakness, or wasting away of the skin

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

• Acne or pimples


• burning and itching of the skin with pinhead-sized red blisters


• burning, itching, and pain in hairy areas, or pus at the root of the hair


• increased hair growth on the forehead, back, arms, and legs


• lightening of normal skin color


• lightening of treated areas of dark skin


• reddish purple lines on the arms, face, legs, trunk, or groin


• softening of the skin

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

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

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

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

More Instacort-10 resources

• Instacort-10 Use in Pregnancy & Breastfeeding
• Instacort-10 Drug Interactions
• Instacort-10 Support Group
• 15 Reviews for Instacort-10 - Add your own review/rating

Compare Instacort-10 with other medications

• Anal Itching
• Aphthous Stomatitis, Recurrent
• Atopic Dermatitis
• Dermatitis
• Eczema
• Gingivitis
• Hemorrhoids
• Proctitis
• Pruritus
• Psoriasis
• Seborrheic Dermatitis
• Skin Rash
• Ulcerative Colitis, Active

Isocaine

mepivacaine hydrochloride

Dosage Form: injection, solution
Mepivacaine HCl 3%

(Mepivacaine Hydrochloride Injection, USP)


Mepivacaine HCl 2%

(with Levonordefrin 1:20,000)

(Mepivacaine Hydrochloride and Levonordefrin Injection, USP)

Rx Only

THESE SOLUTIONS ARE INTENDED FOR DENTAL USE ONLY.

Isocaine Description

Mepivacaine Hydrochloride, a tertiary amine used as a local anesthetic, is 1-methyl-2', 6' - pipecoloxylidide monohydrochloride with the following structural formula:

It is a white, crystalline, odorless powder soluble in water, but very resistant to both acid and alkaline hydrolysis.

Levonordefrin, a sympathomimetic amine used as a vasoconstrictor in local anesthetic solution, is (-)-

It is a white or buff-colored crystalline solid, freely soluble in aqueous solutions of mineral acids, but practically insoluble in water;

DENTAL CARTRIDGES MAY NOT BE AUTOCLAVED.

Mepivacaine hydrochloride injection 3% and Mepivacaine hydrochloride 2% with levonordefrin 1:20,000 injection are sterile solutions for injection.

COMPOSITION

	CARTRIDGE
Each mL contains:	2%	3%
Mepivacaine Hydrochloride	20 mg	30 mg
Levonordefrin	0.05 mg	-
Sodium Chloride	4 mg	6 mg
Potassium metabisulfite	1.2 mg	-
Edetate disodium	0.25 mg	-
Sodium Hydroxide q.s. ad pH; Hydrochloric Acid	0.5 mg	-
Water For Injection, qs. ad.	1 mL	1 mL
The pH of the 2% cartridge solution is adjusted between 3.3 and 5.5 with NaOH.
The pH of the 3% cartridge solution is adjusted between 4.5 and 6.8 with NaOH.

Isocaine - Clinical Pharmacology

Mepivacaine stabilizes the neuronal membrane and prevents the initiation and transmission of nerve impulses, thereby effecting local anesthesia.

Mepivacaine is rapidly metabolized, with only a small percentage of the anesthetic (5 to 10 percent) being excreted unchanged in the urine. Mepivacaine because of its amide structure, is not detoxified by the circulating plasma esterases. The liver is the principal site of metabolism, with over 50 percent of the administered dose being excreted into the bile as metabolites. Most of the metabolized Mepivacaine is probably resorbed in the intestine and then excreted into the urine since only a small percentage is found in the feces. The principal route of excretion is via the kidney. Most of the anesthetic and its metabolites are eliminated within 30 hours. It has been shown that hydroxylation and N-demethylation, which are detoxification reactions, play important roles in the metabolism of the anesthetic. Three metabolites of Mepivacaine have been identified from adult humans: two phenols, which are excreted almost exclusively as their glucuronide conjugates, and the N-demethylated compound (2', 6' - pipecoloxylidide).

The onset of action is rapid (30 to 120 seconds in the upper jaw; 1 to 4 minutes in the lower jaw) and Mepivacaine HCl 3% will ordinarily provide operating anesthesia of 20 minutes in the upper jaw and 40 minutes in the lower jaw.

Mepivacaine HCl 2% with Levonordefrin 1:20,000 provides anesthesia of longer duration for more prolonged procedures, 1 hour to 2.5 hours in the upper jaw and 2.5 hours to 5.5 hours in the lower jaw.

Mepivacaine does not ordinarily produce irritation or tissue damage.

Levonordefrin is a sympathomimetic amine used as a vasoconstrictor in local anesthetic solutions. It has pharmacologic activity similar to that of Epinephrine but it is more stable than Epinephrine. In equal concentrations, Levonordefrin is less potent than Epinephrine in raising blood pressure, and as a vasoconstrictor.

Indications and Usage for Isocaine

Mepivacaine is indicated for production of local anesthesia for dental procedures by infiltration or nerve block in adults and pediatric patients.

Contraindications

Mepivacaine is contraindicated in patients with a known hypersensitivity to amide-type local anesthetics.

Warnings

RESUSCITATIVE EQUIPMENT AND DRUGS SHOULD BE IMMEDIATELY AVAILABLE. (See ADVERSE REACTIONS).

Reactions resulting in fatality have occurred on rare occasions with the use of local anesthetics, even in the absence of a history of hypersensitivity.

Fatalities may occur with use of local anesthetics in the head and neck region as the result of retrograde arterial flow to vital CNS areas even when maximum recommended doses are observed. The practitioner should be alert to early evidence of alteration in sensorium or vital signs.

The solution which contains a vasoconstrictor (Mepivacaine HCl 2%) should be used with extreme caution for patients whose medical history and physical evaluation suggest the existence of hypertension, arteriosclerotic heart disease, cerebral vascular insufficiency, heart block, thyrotoxicosis and diabetes, etc.

The solution which contains a vasoconstrictor (Mepivacaine HCl 2%) also contains potassium metabisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in non-asthmatic people. Mepivacaine HCl 3% is SULFITE FREE.

Mepivacaine, along with other local anesthetics, is capable of producing methemoglobinemia. The clinical signs of methemoglobinemia are cyanosis of the nail beds and lips, fatigue and weakness. If methemoglobinemia does not respond to administration of oxygen, administration of methylene blue intravenously 1-2 mg/kg body weight over a 5 minute period is recommended.

The American Heart Association has made the following recommendations regarding the use of local anesthetics with vasoconstrictors in patients with ischemic heart disease: "Vasoconstrictor agents should be used in local anesthesia solutions during dental practice only when it is clear that the procedure will be shortened or the analgesia rendered more profound. When a vasoconstrictor is indicated, extreme care should be taken to avoid intravascular injection. The minimum possible amount of vasoconstrictor should be used." (Kaplan, EL, editor: Cardiovascular disease in dental practice, Dallas 1986, American Heart Association.)

Precautions

The safety and effectiveness of Mepivacaine depend upon proper dosage, correct technique, adequate precautions, and readiness for emergencies.

The lowest dose that results in effective anesthesia should be used to avoid high plasma levels and possible adverse effects. Injection of repeated doses of Mepivacaine may cause significant increases in blood levels with each repeated dose due to slow accumulation of the drug or its metabolites, or due to slower metabolic degradation than normal.

Tolerance varies with the status of the patient. Debilitated, elderly patients, acutely ill patients, and children should be given reduced doses commensurate with their weight and physical status.

Mepivacaine should be used with caution in patients with a history of severe disturbances of cardiac rhythm or heart block.

INJECTIONS SHOULD ALWAYS BE MADE SLOWLY WITH ASPIRATION TO AVOID INTRAVASCULAR INJECTION AND THEREFORE SYSTEMIC REACTION TO BOTH LOCAL ANESTHETIC AND VASOCONSTRICTOR.

If sedatives are employed to reduce patient apprehension, use reduced doses, since local anesthetic agents, like sedatives, are central nervous system depressants which in combination may have an additive effect. Young children should be given minimal doses of each agent.

Changes in sensorium such as excitation, disorientation or drowsiness may be early indications of a high blood level of the drug and may occur following inadvertent intravascular administration or rapid absorption of Mepivacaine.

Local anesthetic procedures should be used with caution when there is inflammation and/or sepsis in the region of the proposed injection.

Information for Patients

The patient should be cautioned against loss of sensation and possibility of biting trauma should the patient attempt to eat or chew gum prior to return of sensation.

Clinically Significant Drug Interactions

The administration of local anesthetic solutions containing vasopressors, such as Levonordefrin, Epinephrine or Norepinephrine, to patients receiving tricyclic antidepressants or monoamine oxidase inhibitors may produce severe, prolonged hypertension. Concurrent use of these agents should generally be avoided. In situations when concurrent therapy is necessary, careful patient monitoring is essential. Concurrent administration of vasopressor drugs and of ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents.

Phenothiazines and butyrophenones may reduce or reverse the pressor effect of Epinephrine.

Solutions containing a vasoconstrictor should be used cautiously in the presence of disease which may adversely affect the patient's cardiovascular system. Serious cardiac arrhythmias may occur if preparations containing a vasoconstrictor are employed in patients during or following the administration of potent inhalation anesthetics.

MEPIVACAINE SHOULD BE USED WITH CAUTION IN PATIENTS WITH KNOWN DRUG ALLERGIES AND SENSITIVITIES. A thorough history of the patient's prior experience with Mepivacaine or other local anesthetics as well as concomitant or recent drug use should be taken (see CONTRAINDICATIONS). Patients allergic to methylparaben or para-aminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross-sensitivity to agents of the amide type such as Mepivacaine. Since Mepivacaine is metabolized in the liver and excreted by the kidneys, it should be used cautiously in patients with liver and renal disease.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Studies of Mepivacaine HCl in animals to evaluate the carcinogenic and mutagenic potential or the effect on fertility have not been conducted.

Pregnancy

Teratogenic Effects

Pregnancy Category C

Animal reproduction studies have not been conducted with this solution. It is also not known whether this solution can cause fetal harm when administered to a pregnant woman or can effect reproductive capacity. This solution should be given to a pregnant woman only if clearly needed.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when this solution is administered to a nursing woman.

Pediatric Use

Great care must be exercised in adhering to safe concentrations and dosages for pedodontic administration (see DOSAGE AND ADMINISTRATION).

Adverse Reactions

Reactions to MEPIVACAINE are characteristic of those associated with other amide-type local anesthetics. Systemic adverse reactions involving the central nervous system and the cardiovascular system usually result from high plasma levels (which may be due to excessive dosage, rapid absorption, inadvertent intravascular injection, or slow metabolic degradation), injection technique, or volume of injection.

A small number of reactions may result from hypersensitivity, idiosyncrasy or diminished tolerance to normal dosage on the part of the patient.

Persistent paresthesias of the lips, tongue, and oral tissues have been reported with the use of mepivacaine, with slow, incomplete, or no recovery. These post-marketing events have been reported chiefly following nerve blocks in the mandible and have involved the trigeminal nerve and its branches.

Reactions involving the central nervous system are characterized by excitation and/or depression. Nervousness, dizziness, blurred vision, or tremors may occur followed by drowsiness, convulsions, unconsciousness, and possible respiratory arrest. Since excitement may be transient or absent, the first manifestations may be drowsiness merging into unconsciousness and respiratory arrest.

Cardiovascular reactions are depressant. They may be the result of direct drug effect or more commonly in dental practice, the result of vasovagal reaction, particularly if the patient is in the sitting position. Failure to recognize premonitory signs such as sweating, feeling of faintness, changes in pulse or sensorium may result in progressive cerebral hypoxia and seizure or serious cardiovascular catastrophe. Management consists of placing the patient in the recumbent position and administration of oxygen. Vasoactive drugs such as Ephedrine or Methoxamine may be administered intravenously.

Allergic reactions are rare and may occur as a result of sensitivity to the local anesthetic and are characterized by cutaneous lesions of delayed onset or urticaria, edema and other manifestations of allergy. The detection of sensitivity by skin testing is of limited value. As with other local anesthetics, anaphylactoid reactions to Mepivacaine have occurred rarely. The reaction may be abrupt and severe and is not usually dose related. Localized puffiness and swelling may occur.

Overdosage

Treatment of a patient with toxic manifestations consists of assuring and maintaining a patient airway and supporting ventilation (respiration) as required. This usually will be sufficient in the management of most reactions. Should a convulsion persist despite ventilatory therapy, small increments of anticonvulsive agents may be given intravenously, such as benzodiazephine (e.g., diazepam) or ultrashort-acting barbiturates (e.g., thiopental or thiamylal) or short-acting barbiturates (e.g., pentobarbital or secobarbital). Cardiovascular depression may require circulatory assistance with intravenous fluids and/or vasopressor (e.g., Ephedrine) as dictated by the clinical situation. Allergic reactions should be managed by conventional means.

IV and SC LD50's in mice for Mepivacaine Hydrochloride 3% are 33 and 258 mg/kg, respectively. The acute IV and SC LD50's in mice for Mepivacaine Hydrochloride 2% with Levonordefrin 1:20,000 are 30 and 184 mg/kg, respectively.

Isocaine Dosage and Administration

As with all local anesthetics, the dose varies and depends upon the area to be anesthetized, the vascularity of the tissues, individual tolerance and the technique of anesthesia. The lowest dose needed to provide effective anesthesia should be administered. For specific techniques and procedures refer to standard dental manuals and textbooks.

For infiltration and block injections in the upper or lower jaw, the average dose of 1 cartridge will usually suffice.

Each cartridge contains 1.7 mL (34 mg of 2% or 51 mg of 3%).

5.3 cartridges (180 mg of the 2% solution or 270 mg of the 3% solution) are usually adequate to effect anesthesia of the entire oral cavity. Whenever a larger dose seems to be necessary for an extensive procedure, the maximum dose should be calculated according to the patient's weight. A dose of up to 3 mg per pound of body weight may be administered. At any single dental sitting the total dose for all injected sites should not exceed 400 mg in adults.

The maximum pediatric dose should be carefully calculated.

Maximum dose for pediatric population =

Child's Weight (lbs.) 150

×

Maximum Recommended Dose for Adults (400 mg)

The following table, approximating these calculations, may also be used as a guide. This table is based upon a recommended maximum for larger pediatric population of 5.3 cartridges (the maximum recommended adult dose) during any single dental sitting, regardless of the pediatric patient's weight or (for 2% mepivacaine) calulated maximum amount of drug:

Maximum Allowable Dosage*
	3% Mepivacaine		2% Mepivacaine
			1:20,000 Levonordefrin
	3 mg/lb		3mg/lb
	(270 mg max.)		(180 mg max.)
Weight (lb.)	mg	Number of Cartridges	mg	Number of Cartridges
* Adapted from Malamed, Stanley F: Handbook of medical emergencies in the dental office, ed. 2, St. Louis, 1982. The C.V. Mosby Co.
20	60	1.2	60	1.8
30	90	1.8	90	2.6
40	120	2.3	120	3.5
50	150	2.9	150	4.4
60	180	3.5	180	5.3
80	240	4.7	180	5.3
100	270	5.3	180	5.3
120	270	5.3	180	5.3

When using Mepivacaine HCl injection USP for infiltration or regional block anesthesia, injection should always be made slowly and with frequent aspiration.

Any unused portion of a cartridge should be discarded.

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

DISINFECTION OF CARTRIDGES

As in the case of any cartridge, the diaphragm should be disinfected before needle puncture. The diaphragm should be thoroughly swabbed with either pure 91% isopropyl alcohol or 70% ethyl alcohol, USP, just prior to use. Many commercially available alcohol solutions contain ingredients which are injurious to container components, and therefore, should not be used. Cartridges should not be immersed in any solution.

How is Isocaine Supplied

Mepivacaine HCl 3%; (Mepivacaine Hydrocholoride Injection USP) is available in cardboard boxes containing 5 blisters of 10 × 1.7 mL dental cartridges, 50 per carton. Mepivacaine HCl 2% (Mepivacaine Hydrochloride and Levonordefrin Injection; USP) is available in cardboard boxes containing 5 blisters of 10 × 1.7 mL dental cartridges, 50 per carton.

Both solutions should be stored at controlled room temperature, below 25° C (77° F). Protect from light. Do not permit to freeze. BOXES: For protection from light, retain in box until time of use. Once opened, the box should be reclosed by closing the top flap. The Mepivacaine 2% solution should not be used if its color is pinkish or darker than slightly yellow or it contains a precipitate. Cartridge warmers should not be used with Mepivacaine HCl injection USP products.

Manufactured and Distributed by

Novocol Pharmaceutical of Canada, Inc.

Cambridge Ontario Canada N1R 5S9

Rev 07/07 (2780-1)

PRINCIPAL DISPLAY PANEL - 1.7 mL Cartridge Carton

NRG

Distributed by IQ Dental

NDC 51004-2020-5

MEPIVACAINE HCl 3%

INJECTION

without VASOCONSTRICTOR

(MEPIVACAINE HCl INJECTION, USP)

50 Cartridges • 1.7 mL Minimum

Rx Only

iQDental™

Isocaine  mepivacaine hydrochloride  injection, solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 51004-2020 Route of Administration SUBCUTANEOUS DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength Mepivacaine Hydrochloride (Mepivacaine) Mepivacaine Hydrochloride 30 mg  in 1 mL

Inactive Ingredients Ingredient Name Strength Sodium Chloride 6 mg  in 1 mL Water

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 51004-2020-5 50 CARTRIDGE In 1 CARTON contains a CARTRIDGE 1 1.7 mL In 1 CARTRIDGE This package is contained within the CARTON (51004-2020-5)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA088387	08/20/2010

Labeler - Novocol Pharmaceutical of Canada, Inc. (201719960)

Registrant - IQ Dental (800349763)

Establishment
Name	Address	ID/FEI	Operations
Novocol		201719960	MANUFACTURE

Revised: 07/2010Novocol Pharmaceutical of Canada, Inc.

More Isocaine resources

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

Compare Isocaine with other medications

• Local Anesthesia