Note: This document contains side effect information about itraconazole. Some dosage forms listed on this page may not apply to the brand name Tolsura.
Applies to itraconazole: oral capsule, oral solution.
Warning
Oral route (Capsule)
Itraconazole capsules should not be administered for the treatment of onychomycosis in patients with evidence of ventricular dysfunction such as congestive heart failure (CHF) or a history of CHF. If signs or symptoms of congestive heart failure occur during administration of itraconazole capsules, discontinue administration. When itraconazole was administered intravenously to dogs and healthy human volunteers, negative inotropic effects were seen.Drug Interactions: Coadministration of the following drugs are contraindicated with itraconazole capsules: methadone, disopyramide, dofetilide, dronedarone, quinidine, isavuconazole, ergot alkaloids (such as dihydroergotamine, ergometrine (ergonovine), ergotamine, methylergometrine (methylergonovine)), irinotecan, lurasidone, oral midazolam, pimozide, triazolam, felodipine, nisoldipine, ivabradine, ranolazine, eplerenone, cisapride, naloxegol, lomitapide, lovastatin, simvastatin, avanafil, ticagrelor. In addition, coadministration with colchicine, fesoterodine, and solifenacin is contraindicated in subjects with varying degrees of renal or hepatic impairment, and coadministration with eliglustat is contraindicated in subjects that are poor or intermediate metabolizers of CYP2D6 and in subjects taking strong or moderate CYP2D6 inhibitors. Coadministration with venetoclax is contraindicated in patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) during the dose initiation and ramp-up phase of venetoclax. Coadministration with itraconazole can cause elevated plasma concentrations of these drugs and may increase or prolong both the pharmacologic effects and/or adverse reactions to these drugs. For example, increased plasma concentrations of some of these drugs can lead to QT prolongation and ventricular tachyarrhythmias including occurrences of torsades de pointes, a potentially fatal arrhythmia.
Oral route (Capsule)
Warning: Congestive Heart Failure and Drug InteractionsTolsura(TM)Congestive Heart Failure:Itraconazole can cause or exacerbate congestive heart failure (CHF). When itraconazole was administered intravenously to healthy human volunteers and dogs, negative inotropic effects were seen. If signs or symptoms of congestive heart failure occur or worsen during administration of itraconazole, reassess the benefit and risk of continuing treatment.Drug Interactions:Coadministration of certain drugs that are metabolized by human CYP3A4 enzymes are contraindicated with itraconazole because plasma concentrations of such drugs are increased, which may also increase or prolong both the pharmacologic effects and/or adverse reactions to these drugs.Coadministration with colchicine, fesoterodine, and solifenacin is contraindicated in subjects with varying degrees of renal or hepatic impairment, and coadministration with eliglustat is contraindicated in subjects that are poor or intermediate metabolizers of CYP2D6 and in subjects taking strong or moderate CYP2D6 inhibitors.Increased plasma concentrations of some of these drugs can lead to QT prolongation and/or ventricular tachyarrhythmias, including occurrences of torsades de pointes, a potentially fatal arrhythmia.
Oral route (Solution)
Congestive Heart Failure, Cardiac Effects and Drug Interactions: If signs or symptoms of congestive heart failure occur during administration of itraconazole oral solution, continued itraconazole use should be reassessed. When itraconazole was administered intravenously to dogs and healthy human volunteers, negative inotropic effects were seen.Drug Interactions: Coadministration of the following drugs are contraindicated with itraconazole oral solution: methadone, disopyramide, dofetilide, dronedarone, quinidine, isavuconazole, ergot alkaloids (such as dihydroergotamine, ergometrine (ergonovine), ergotamine, methylergometrine (methylergonovine)), irinotecan, lurasidone, oral midazolam, pimozide, triazolam, felodipine, nisoldipine, ivabradine, ranolazine, eplerenone, cisapride, naloxegol, lomitapide, lovastatin, simvastatin, avanafil, ticagrelor. In addition, coadministration with colchicine, fesoterodine, and solifenacin is contraindicated in subjects with varying degrees of renal or hepatic impairment, and coadministration with eliglustat is contraindicated in subjects that are poor or intermediate metabolizers of CYP2D6 and in subjects taking strong or moderate CYP2D6 inhibitors. Coadministration with itraconazole can cause elevated plasma concentrations of these drugs and may increase or prolong both the pharmacologic effects and/or adverse reactions to these drugs. For example, increased plasma concentrations of some of these drugs can lead to QT prolongation and ventricular tachyarrhythmias including occurrences of torsades de pointes, a potentially fatal arrhythmia.
Oral route (Tablet)
Do not use itraconazole to treat onychomycosis in patients with ventricular dysfunction (eg, congestive heart failure). If signs or symptoms of congestive heart failure occur, continued use should be reassessed. Itraconazole is contraindicated in patients concomitantly taking cisapride, pimozide, quinidine, dofetilide, levacetylmethadol (levomethadyl), felodipine, oral midazolam, nisoldipine, triazolam, lovastatin, simvastatin, ergot alkaloids such as dihydroergotamine, ergometrine (ergonovine), ergotamine and methylergometrine (methylergonovine), or methadone. Concomitant administration can cause the plasma levels of the concomitant drug to increase. Serious cardiovascular events have been reported in patients taking cisapride, pimozide, levacetylmethadol (levomethadyl), methadone, or quinidine concomitantly with itraconazole or other CYP3A4 inhibitors.
Serious side effects of Tolsura
Along with its needed effects, itraconazole (the active ingredient contained in Tolsura) 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 while taking itraconazole:
More common
- Decreased urine output
- dry mouth
- fever
- increased thirst
- irregular heartbeat
- loss of appetite
- mood changes
- muscle pain or cramps
- nausea
- numbness or tingling in the hands, feet, or lips
- seizures
- trouble breathing
- unusual tiredness or weakness
- vomiting
Less common
- Blurred vision
- chest pain
- chills
- clay-colored stools
- cloudy urine
- cold sweats
- confusion
- cough
- dark urine
- decrease in urine-concentrating ability
- diarrhea
- dizziness
- dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
- drowsiness
- feeling unusually cold
- headache
- itching, skin rash
- light-colored stools
- mental changes
- muscle cramps in the hands, arms, feet, legs, or face
- muscle spasms (tetany) or twitching
- nervousness
- noisy, rattling breathing
- numbness and tingling around the mouth or fingertips
- pounding in the ears
- shivering
- slow, fast, or pounding heartbeat or pulse
- sneezing
- sore throat
- stomach cramps or pain
- sweating
- swelling of the fingers, hands, feet, or lower legs
- tightness in the chest
- trembling
- trouble breathing at rest
- unpleasant breath odor
- vomiting of blood
- weight gain
- yellow eyes or skin
Rare
- Black, tarry stools
- bleeding gums
- blistering, peeling, or loosening of the skin
- bloating or swelling of the face, arms, hands, lower legs, or feet
- blood in the urine or stools
- blue lips and fingernails
- burning, crawling, itching, numbness, painful, prickling, "pins and needles", or tingling feelings
- continuing ringing or buzzing or other unexplained noise in the ears
- coughing that sometimes produces a pink frothy sputum
- cracks in the skin
- decreased appetite
- difficulty with swallowing
- dilated neck veins
- disturbed color perception
- double vision
- extreme tiredness or weakness
- fast or irregular breathing
- feeling of discomfort
- general feeling of tiredness or weakness
- halos around lights
- hearing loss
- hives or welts
- inflammation of the joints
- joint pain
- large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or genitals
- loss of heat from the body
- loss of vision
- lower back or side pain
- night blindness
- overbright appearance of lights
- painful or difficult urination
- pale skin
- pinpoint red spots on the skin
- puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
- rapid weight gain
- red skin lesions, often with a purple center
- red, irritated eyes
- red, swollen skin
- scaly skin
- sores, ulcers, or white spots on the lips or in the mouth
- stomach pain, continuing
- stomach tenderness
- swollen lymph glands
- tunnel vision
- unsteadiness or awkwardness
- unusual bleeding or bruising
- unusual weight gain or loss
- upper right abdominal or stomach pain
- weakness in the arms, hands, legs, or feet
Incidence not known
- Bloating
- constipation
- difficult, fast, noisy breathing
- indigestion
- loss of bladder control
- pains in the stomach, side, or abdomen, possibly radiating to the back
Other side effects of Tolsura
Some side effects of itraconazole 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:
Less common
- Decreased interest in sexual intercourse
- difficulty having a bowel movement
- difficulty with moving
- discouragement
- feeling of constant movement of self or surroundings
- feeling sad or empty
- inability to have or keep an erection
- irritability
- loss in sexual ability, desire, drive, or performance
- loss of interest or pleasure
- muscle aching or stiffness
- pain or tenderness around the eyes and cheekbones
- passing of gas
- sensation of spinning
- sleepiness or unusual drowsiness
- soreness of the skin
- stomach fullness or discomfort
- stuffy or runny nose
- trouble concentrating
- trouble sleeping
Rare
- Belching
- change in taste
- hair loss or thinning of the hair
- heartburn
- increased need to urinate
- increased sensitivity of the eyes or skin to sunlight
- loss of taste
- menstrual changes
- passing urine more often
- redness or other discoloration of the skin
- severe sunburn
For Healthcare Professionals
Applies to itraconazole: compounding powder, intravenous kit, oral capsule, oral solution, oral tablet.
General
In clinical trials, side effects were reported in about 7% of patients receiving short-term therapy and about 15% of patients receiving prolonged (about 1 month) continuous therapy. The side effects reported most often with the 100-mg capsule formulation were headache, abdominal pain, and nausea; the side effects reported most often with the oral solution were dizziness, headache, dysgeusia, dyspnea, cough, abdominal pain, diarrhea, vomiting, nausea, dyspepsia, rash, and pyrexia. The most serious side effects reported with this drug were serious allergic reactions, cardiac failure/congestive heart failure/pulmonary edema, pancreatitis, serious hepatotoxicity (including some cases of fatal acute liver failure), and serious skin reactions.[Ref]
Gastrointestinal
Very common (10% or more): Nausea (up to 11%), diarrhea (up to 11%)
Common (1% to 10%): Vomiting, abdominal pain/discomfort, dyspepsia, flatulence, gingivitis, constipation, ulcerative stomatitis, gastritis, gastroenteritis
Rare (0.01% to 0.1%): Pancreatitis
Frequency not reported: Dysphagia, hemorrhoids, gastrointestinal disorder[Ref]
Pancreatitis, abdominal pain, vomiting, dyspepsia, nausea, diarrhea, and constipation have also been reported during postmarketing experience.[Ref]
Metabolic
Very common (10% or more): Hypertriglyceridemia (up to 11%)
Common (1% to 10%): Hypokalemia, hypomagnesemia, hypophosphatemia, increased appetite
Uncommon (0.1% to 1%): Fluid overload, hypocalcemia, anorexia, hyperglycemia
Frequency not reported: Dehydration, decreased weight, hyperkalemia[Ref]
Hypertriglyceridemia and hypokalemia have also been reported during postmarketing experience.[Ref]
Nervous system
Common (1% to 10%): Headache, dizziness, hypoacusis, tremor, dysgeusia
Uncommon (0.1% to 1%): Vertigo, somnolence, hypoesthesia, transient/permanent hearing loss, peripheral neuropathy, paresthesia, tinnitus[Ref]
Peripheral neuropathy, paresthesia, hypoesthesia, headache, dizziness, tinnitus, transient/permanent hearing loss, dysgeusia, and tremor have also been reported during postmarketing experience.[Ref]
Respiratory
Common (1% to 10%): Rhinitis, upper respiratory tract infection, sinusitis, cough, pneumonia, increased sputum, dyspnea, pharyngitis, pulmonary infiltration
Uncommon (0.1% to 1%): Pulmonary edema, pharyngolaryngeal pain
Frequency not reported: Dysphonia[Ref]
Pulmonary edema and dyspnea have also been reported during postmarketing experience.[Ref]
Other
Edema and pyrexia have also been reported during postmarketing experience.[Ref]
Common (1% to 10%): Pyrexia, injury, edema, chest pain, fatigue, malaise, pain, asthenia, increased blood alkaline phosphatase, increased blood lactate dehydrogenase, Pneumocystis carinii infection, herpes zoster
Frequency not reported: Unspecified infection, rigors, back pain, hot flushes, implantation complication, face edema, chills, generalized edema, mucosal inflammation
Postmarketing reports: Peripheral edema[Ref]
Dermatologic
Common (1% to 10%): Rash, pruritus, hyperhidrosis, unspecified skin disorder, erythematous rash
Uncommon (0.1% to 1%): Urticaria
Rare (0.01% to 0.1%): Toxic epidermal necrolysis, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis, exfoliative dermatitis, leukocytoclastic vasculitis, erythema multiforme, photosensitivity, alopecia[Ref]
Toxic epidermal necrolysis, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis, erythema multiforme, exfoliative dermatitis, leukocytoclastic vasculitis, alopecia, photosensitivity, rash, pruritus, and urticaria have also been reported during postmarketing experience.[Ref]
Hepatic
Mild, transient elevations in liver function tests have occurred in up to 7% of patients receiving continuous therapy.
Serious hepatotoxicity (including some cases of fatal acute liver failure), hepatitis, and reversible increases in hepatic enzymes have also been reported during postmarketing experience.[Ref]
Common (1% to 10%): Increased hepatic enzymes (including reversible increases), bilirubinemia, abnormal liver function, increased ALT, jaundice, increased AST, increased GGT, hepatitis, hyperbilirubinemia
Uncommon (0.1% to 1%): Hepatic failure
Rare (0.01% to 0.1%): Serious hepatotoxicity (including some cases of fatal acute liver failure)
Frequency not reported: Cholestasis, cholestatic jaundice[Ref]
Cardiovascular
Common (1% to 10%): Hypertension, vein disorder, abnormal electrocardiogram
Uncommon (0.1% to 1%): Hypotension, orthostatic hypotension, vasculitis, sinus bradycardia, tachycardia, cardiac failure
Frequency not reported: Premature ventricular contractions, left ventricular failure
Postmarketing reports: Congestive heart failure[Ref]
Renal
Common (1% to 10%): Increased serum creatinine
Uncommon (0.1% to 1%): Abnormal renal function, increased blood urea
Frequency not reported: Renal impairment[Ref]
Psychiatric
Common (1% to 10%): Depression, anxiety, abnormal dreaming
Frequency not reported: Insomnia, decreased libido, visual hallucinations, confusional state[Ref]
An elderly patient experienced visual hallucinations, confusion, and weakness after receiving this drug. The symptoms reappeared following accidental doses of this drug 7 and 10 days later.[Ref]
Musculoskeletal
Common (1% to 10%): Myalgia, bursitis, back pain
Uncommon (0.1% to 1%): Arthralgia
Rare (0.01% to 0.1%): Increased blood creatine phosphokinase[Ref]
Increased blood creatine phosphokinase, myalgia, and arthralgia have also been reported during postmarketing experience.[Ref]
Genitourinary
Pollakiuria, menstrual disorders, and erectile dysfunction have also been reported during postmarketing experience.[Ref]
Common (1% to 10%): Cystitis, urinary tract infection
Uncommon (0.1% to 1%): Impotence, menstrual disorders, abnormal urine analysis, pollakiuria, erectile dysfunction
Frequency not reported: Albuminuria, hematuria, gynecomastia, male breast pain, bacteriuria
Postmarketing reports: Urinary incontinence[Ref]
Hypersensitivity
Anaphylactic reactions, allergic reactions, serum sickness, and angioneurotic edema have also been reported during postmarketing experience.[Ref]
Uncommon (0.1% to 1%): Hypersensitivity
Rare (0.01% to 0.1%): Allergic reactions (e.g., pruritus, rash, urticaria, angioedema), serum sickness, angioneurotic edema, anaphylactic reaction
Frequency not reported: Anaphylactic shock
Postmarketing reports: Anaphylaxis, anaphylactoid reaction[Ref]
Hematologic
Leukopenia and thrombocytopenia have also been reported during postmarketing experience.[Ref]
Uncommon (0.1% to 1%): Leukopenia, thrombocytopenia
Frequency not reported: Granulocytopenia
Postmarketing reports: Neutropenia[Ref]
Ocular
Uncommon (0.1% to 1%): Visual disturbances (including blurred vision, diplopia)
Frequency not reported: Abnormal vision[Ref]
Visual disturbances (including blurred vision, diplopia) have also been reported during postmarketing experience.[Ref]
Endocrine
Frequency not reported: Adrenal insufficiency[Ref]
Local
IV:
-Frequency not reported: Injection site inflammation[Ref]
