Neoral

— THERAPEUTIC CATEGORIES —
  • Arthritis/rheumatic disorders
  • Organ rejection prophylaxis
  • Psoriasis
PAGE CONTENTS
  • Jump to Section
  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Neoral Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Cyclosporine (modified) 25mg, 100mg; caps; contains alcohol.

    Pharmacological Class

    DMARD (immunosuppressant).

    See Also

    How Supplied

    Caps—30; Soln—50mL

    Manufacturer

    Novartis Pharmaceuticals Corp

    Generic Availability

    YES

    Mechanism of Action

    Cyclosporine specifically and reversibly inhibits immunocompetent lymphocytes in the G0- and G1-phase of the cell cycle. Cyclosporine also inhibits lymphokine production and release including interleukin-2.

    Neoral Indications

    Indications

    Severe, active rheumatoid arthritis unresponsive to methotrexate alone.

    Neoral Dosage and Administration

    Adult

    Give consistently with regard to meals and time of day. ≥18yrs: 1.25mg/kg twice daily; may increase by 0.5–0.75mg/kg per day after 8 weeks and again after 12 weeks; max 4mg/kg per day (many patients on concomitant methotrexate can be treated with doses of 3mg/kg per day or less). Dilute soln in a glass of room temp orange or apple juice. Reduce dose by 25–50% if adverse events (eg, hypertension or serum creatinine increases ≥30% above baseline) occur. Renal or severe hepatic impairment: consider reducing dose. Discontinue if adverse events are severe or persistent, or if no benefit by week 16.

    Children

    <18yrs: not established.

    Administration

    Take consistently with regard to time of day and meals.

    Nursing Considerations

    Take consistently with regard to time of day and meals.

    Neoral Contraindications

    Contraindications

    Renal impairment. Uncontrolled hypertension. Malignancies.

    Neoral Boxed Warnings

    Boxed Warning

    Be fully aware with immunosuppresive therapy before prescribing. Increased bioavailability compared to Sandimmune; do not use interchangeably. Increased risk of infection, lymphomas and other malignancies.

    Neoral Warnings/Precautions

    Warnings/Precautions

    Be fully familiar with immunosuppressive therapy before prescribing. Not bioequivalent to all other forms of cyclosporine; do not interchange without physician supervision. Increased risk of infections, lymphomas and other malignancies (eg, skin). Avoid sun or UV light exposure. Monitor renal and hepatic function, BP, CBC, serum magnesium, potassium, uric acid, lipids (see full labeling for monitoring frequency). Reduce dose if hypertension occurs; do not attempt to manage medically. Elderly. Pregnancy. Nursing mothers.

    Neoral Pharmacokinetics

    Absorption

    Time to peak blood concentrations (Tmax): ranged from 1.5–2.0 hours. The administration of food decreased AUC and Cmax.

    Distribution

    Distributed largely outside the blood volume. Steady state volume of distribution (IV dosing): 3–5 L/kg in solid organ transplant recipients. Plasma protein bound: ~90% (primarily lipoproteins).

    Metabolism

    Hepatic (CYP3A).

    Elimination

    Biliary (primarily), renal (6%). Half-life: ~8.4 hours (range: 5–18 hours).

    Neoral Interactions

    Interactions

    Avoid other nephrotoxic drugs (eg, ciprofloxacin, gentamicin, tobramycin, vancomycin, SMX/TMP, melphalan, amphotericin B, ketoconazole, cimetidine, ranitidine, tacrolimus, NSAIDs, colchicine), fibric acid derivatives. Cyclosporine levels increased by CYP3A inhibitors (eg, calcium channel blockers, amiodarone, azithromycin, azole antifungals, erythromycin, clarithromycin, quinupristin/dalfopristin, boceprevir, telaprevir, methylprednisolone, allopurinol, colchicine, bromocriptine, danazol, metoclopramide; probably indinavir, saquinavir, nelfinavir, ritonavir, imatinib, nefazodone, oral contraceptives). Avoid alcohol, grapefruit juice. Cyclosporine levels decreased by CYP3A inducers (eg, nafcillin, rifampin, carbamazepine, oxcarbazepine, bosentan, phenobarbital, phenytoin, octreotide, ticlopidine, St. John's wort), orlistat. Avoid potassium-sparing diuretics. Concomitant repaglinide: monitor blood glucose. Concomitant aliskiren: not recommended. Concomitant sirolimus: separate by 4 hours. May antagonize mycophenolic acid; monitor efficacy. May decrease effectiveness of vaccines; avoid live attenuated vaccines. May increase levels of digoxin (monitor), colchicine, prednisolone, statins (reduce dose), ambrisentan, and anthracycline antibiotics. Gingival hyperplasia with nifedipine (avoid). Convulsions with high-dose methylprednisolone.

    Neoral Adverse Reactions

    Adverse Reactions

    Renal dysfunction, hypertension, headache, GI disturbances, hirsutism, hypertrichosis, leg cramps, pain, tremor, paresthesia, edema, dizziness, gum hyperplasia, liver dysfunction; increased risk of infections or malignancies, progressive multifocal leukoencephalopathy, hyperkalemia, thrombotic microangiopathy, possible encephalopathy.

    Neoral Clinical Trials

    See Literature

    Neoral Note

    Not Applicable

    Neoral Patient Counseling

    See Literature

    Neoral Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Cyclosporine (modified) 25mg, 100mg; caps; contains alcohol.

    Pharmacological Class

    Immunosuppressant.

    See Also

    How Supplied

    Caps—30; Soln—50mL

    Manufacturer

    Novartis Pharmaceuticals Corp

    Generic Availability

    YES

    Mechanism of Action

    Cyclosporine specifically and reversibly inhibits immunocompetent lymphocytes in the G0- and G1-phase of the cell cycle. Cyclosporine also inhibits lymphokine production and release including interleukin-2.

    Neoral Indications

    Indications

    Organ rejection prophylaxis in allogeneic kidney, liver, and heart transplant patients, in combination with azathioprine and corticosteroids.

    Neoral Dosage and Administration

    Adult

    See full labeling. Give consistently with regard to meals and time of day. ≥18yrs: Give daily dose in two divided doses. Individualize. Give initial dose 4–12 hours prior to transplantation or post-op with corticosteroids. Adjust Neoral dose to achieve a pre-defined cyclosporine blood concentration. Dilute soln in glass of room temp orange or apple juice. Conversion from Sandimmune: initially 1:1 dose conversion, then adjust to attain pre-conversion cyclosporine blood trough concentration; monitor every 4–7 days until pre-conversion value attained. Monitor serum creatinine and BP every 2 weeks during first two months after conversion. If initial dose >10mg/kg/day, monitor concentration daily until stabilized in desired range. Renal or severe hepatic impairment: consider reducing dose.

    Children

    Not studied.

    Administration

    Take consistently with regard to time of day and meals.

    Nursing Considerations

    Take consistently with regard to time of day and meals.

    Neoral Contraindications

    Not Applicable

    Neoral Boxed Warnings

    Boxed Warning

    Be fully aware with immunosuppresive therapy before prescribing. Increased bioavailability compared to Sandimmune; do not use interchangeably. Increased risk of infection, lymphomas and other malignancies.

    Neoral Warnings/Precautions

    Warnings/Precautions

    Be fully familiar with immunosuppressive therapy before prescribing. Not bioequivalent to all other forms of cyclosporine; do not interchange without physician supervision. Increased risk of infections, lymphomas and other malignancies (eg, skin). Avoid sun or UV light exposure. Monitor renal and hepatic function, BP, CBC, serum magnesium, potassium, uric acid, lipids (see full labeling for monitoring frequency). Reduce dose if hypertension occurs; do not attempt to manage medically. Elderly. Pregnancy. Nursing mothers.

    Neoral Pharmacokinetics

    Absorption

    Time to peak blood concentrations (Tmax): ranged from 1.5–2.0 hours. The administration of food decreased AUC and Cmax.

    Distribution

    Distributed largely outside the blood volume. Steady state volume of distribution (IV dosing): 3–5 L/kg in solid organ transplant recipients. Plasma protein bound: ~90% (primarily lipoproteins).

    Metabolism

    Hepatic (CYP3A).

    Elimination

    Biliary (primarily), renal (6%). Half-life: ~8.4 hours (range: 5–18 hours).

    Neoral Interactions

    Interactions

    Avoid other nephrotoxic drugs (eg, ciprofloxacin, gentamicin, tobramycin, vancomycin, SMX/TMP, melphalan, amphotericin B, ketoconazole, cimetidine, ranitidine, tacrolimus, NSAIDs, colchicine), fibric acid derivatives. Cyclosporine levels increased by CYP3A inhibitors (eg, calcium channel blockers, amiodarone, azithromycin, azole antifungals, erythromycin, clarithromycin, quinupristin/dalfopristin, boceprevir, telaprevir, methylprednisolone, allopurinol, colchicine, bromocriptine, danazol, metoclopramide; probably indinavir, saquinavir, nelfinavir, ritonavir, imatinib, nefazodone, oral contraceptives). Avoid alcohol, grapefruit juice. Cyclosporine levels decreased by CYP3A inducers (eg, nafcillin, rifampin, carbamazepine, oxcarbazepine, bosentan, phenobarbital, phenytoin, octreotide, ticlopidine, St. John's wort), orlistat. Avoid potassium-sparing diuretics. Concomitant repaglinide: monitor blood glucose. Concomitant aliskiren: not recommended. Concomitant sirolimus: separate by 4 hours. May antagonize mycophenolic acid; monitor efficacy. May decrease effectiveness of vaccines; avoid live attenuated vaccines. May increase levels of digoxin (monitor), colchicine, prednisolone, statins (reduce dose), ambrisentan, and anthracycline antibiotics. Gingival hyperplasia with nifedipine (avoid). Convulsions with high-dose methylprednisolone.

    Neoral Adverse Reactions

    Adverse Reactions

    Renal dysfunction, hypertension, headache, GI disturbances, hirsutism, hypertrichosis, leg cramps, pain, tremor, paresthesia, edema, dizziness, gum hyperplasia, liver dysfunction; increased risk of infections or malignancies, progressive multifocal leukoencephalopathy, hyperkalemia, thrombotic microangiopathy, possible encephalopathy.

    Neoral Clinical Trials

    See Literature

    Neoral Note

    Not Applicable

    Neoral Patient Counseling

    See Literature

    Neoral Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Cyclosporine (modified) 25mg, 100mg; caps; contains alcohol.

    Pharmacological Class

    Immunosuppressant.

    See Also

    How Supplied

    Caps—30; Soln—50mL

    Manufacturer

    Novartis Pharmaceuticals Corp

    Generic Availability

    YES

    Mechanism of Action

    Cyclosporine specifically and reversibly inhibits immunocompetent lymphocytes in the G0- and G1-phase of the cell cycle. Cyclosporine also inhibits lymphokine production and release including interleukin-2.

    Neoral Indications

    Indications

    Treatment of adult, non-immunocompromised patients with severe, recalcitrant, plaque psoriasis who have failed to respond to at least one systemic therapy or in patients for whom other systemic therapies are contraindicated or intolerable.

    Neoral Dosage and Administration

    Adult

    Give consistently with regard to meals and time of day. ≥18yrs: 1.25mg/kg twice daily; may increase after 4 weeks by 0.5mg/kg per day, then adjust at 2-week intervals; max 4mg/kg per day. Dilute soln in glass of room temp orange or apple juice. Reduce by 25–50% if adverse events (eg, hypertension or serum creatinine increases ≥25% above baseline) occur. Renal or severe hepatic impairment: consider reducing dose. Discontinue if adverse events are severe or persistent.

    Children

    <18yrs: not established.

    Administration

    Take consistently with regard to time of day and meals.

    Nursing Considerations

    Take consistently with regard to time of day and meals.

    Neoral Contraindications

    Contraindications

    Concomitant PUVA or UVB therapy; methotrexate, other immunosuppressants, coal tar, or radiation therapy.

    Neoral Boxed Warnings

    Boxed Warning

    Prescribe only by physicians experienced in immunosuppressive therapy. May increase risk of infection, lymphomas and other malignancies. Increased bioavailability compared to Sandimmune; do not use interchangeably. Psoriasis patients: previously treated with PUVA, methotrexate or other immunosuppressants, UVB, coal tar, or radiation, are at an increased risk of developing skin malignancies.

    Neoral Warnings/Precautions

    Warnings/Precautions

    Be fully familiar with immunosuppressive therapy before prescribing. Not bioequivalent to all other forms of cyclosporine; do not interchange without physician supervision. Increased risk of infections, lymphomas and other malignancies (eg, skin). Avoid sun or UV light exposure. Monitor renal and hepatic function, BP, CBC, serum magnesium, potassium, uric acid, lipids (see full labeling for monitoring frequency). Reduce dose if hypertension occurs; do not attempt to manage medically. Elderly. Pregnancy. Nursing mothers.

    Neoral Pharmacokinetics

    Absorption

    Time to peak blood concentrations (Tmax): ranged from 1.5–2.0 hours. The administration of food decreased AUC and Cmax.

    Distribution

    Distributed largely outside the blood volume. Steady state volume of distribution (IV dosing): 3–5 L/kg in solid organ transplant recipients. Plasma protein bound: ~90% (primarily lipoproteins).

    Metabolism

    Hepatic (CYP3A).

    Elimination

    Biliary (primarily), renal (6%). Half-life: ~8.4 hours (range: 5–18 hours).

    Neoral Interactions

    Interactions

    Avoid other nephrotoxic drugs (eg, ciprofloxacin, gentamicin, tobramycin, vancomycin, SMX/TMP, melphalan, amphotericin B, ketoconazole, cimetidine, ranitidine, tacrolimus, NSAIDs, colchicine), fibric acid derivatives. Cyclosporine levels increased by CYP3A inhibitors (eg, calcium channel blockers, amiodarone, azithromycin, azole antifungals, erythromycin, clarithromycin, quinupristin/dalfopristin, boceprevir, telaprevir, methylprednisolone, allopurinol, colchicine, bromocriptine, danazol, metoclopramide; probably indinavir, saquinavir, nelfinavir, ritonavir, imatinib, nefazodone, oral contraceptives). Avoid alcohol, grapefruit juice. Cyclosporine levels decreased by CYP3A inducers (eg, nafcillin, rifampin, carbamazepine, oxcarbazepine, bosentan, phenobarbital, phenytoin, octreotide, ticlopidine, St. John's wort), orlistat. Avoid potassium-sparing diuretics. Concomitant repaglinide: monitor blood glucose. Concomitant aliskiren: not recommended. Concomitant sirolimus: separate by 4 hours. May antagonize mycophenolic acid; monitor efficacy. May decrease effectiveness of vaccines; avoid live attenuated vaccines. May increase levels of digoxin (monitor), colchicine, prednisolone, statins (reduce dose), ambrisentan, and anthracycline antibiotics. Gingival hyperplasia with nifedipine (avoid). Convulsions with high-dose methylprednisolone.

    Neoral Adverse Reactions

    Adverse Reactions

    Renal dysfunction, hypertension, headache, GI disturbances, hirsutism, hypertrichosis, leg cramps, pain, tremor, paresthesia, edema, dizziness, gum hyperplasia, liver dysfunction; increased risk of infections or malignancies, progressive multifocal leukoencephalopathy, hyperkalemia, thrombotic microangiopathy, possible encephalopathy.

    Neoral Clinical Trials

    See Literature

    Neoral Note

    Not Applicable

    Neoral Patient Counseling

    See Literature

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