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Itraconazole Oral Suspension, Custom Concentration

Oral Suspension Vehicle

An itraconazole oral suspension compounded to each prescriber's order, in the concentration and flavor a patient or animal can actually take.

  • USP <795> compliant
  • USP <800> hazardous drug lab
  • PCCA member

Clinical Advantages

  • Custom strength available
  • Weight based dosing
  • Flavored for palatability
  • Alternative to swallowing pills
  • Measured dose applicator

How It Works

What is Itraconazole Oral Suspension?

Itraconazole Oral Suspension is a compounded liquid form of itraconazole, a triazole antifungal sold commercially as capsules and as a 10 mg/mL oral solution. Mixwell prepares it as a suspension in the concentration a prescriber specifies, so the measured dose fits the patient.

How it works

  1. Itraconazole blocks the fungal enzyme that builds ergosterol, a structural part of the fungal cell membrane [1].
  2. Absorption depends heavily on the formulation. Capsules need gastric acid and food, while the commercial oral solution absorbs better on an empty stomach [2].
  3. Barone and colleagues measured 30% to 33% greater bioavailability from the cyclodextrin oral solution than from capsules in 30 volunteers [3].
  4. A suspension lets the prescriber set a concentration that keeps the measured volume practical for a small patient.

When prescribers choose it

  • Veterinarians dosing cats, birds, and reptiles, where commercial concentrations mean impractical volumes
  • Veterinarians who need a flavor an animal will accept
  • Infectious disease and HIV practices whose patients cannot swallow capsules
  • Prescribers who need a strength or vehicle that commercial products do not offer

Clinical Details

What does the evidence show?
  • Barone and colleagues (1998, Antimicrobial Agents and Chemotherapy) compared single 200 mg doses in 30 volunteers. Bioavailability from the cyclodextrin oral solution was 30% to 33% greater than from either capsule formulation [3].
  • The IDSA 2016 candidiasis guideline recommends itraconazole solution 200 mg once daily for fluconazole refractory oropharyngeal candidiasis, a strong recommendation with moderate quality evidence [2].
  • Mawby and colleagues (2014, Journal of Veterinary Internal Medicine) gave 9 healthy dogs itraconazole in a crossover design. A suspension compounded from bulk powder reached about 5.52% of the innovator's AUC and 4.14% of its peak concentration, and the authors concluded compounded itraconazole should not be used in dogs [4].
  • Mawby and colleagues (2018, Journal of the American Veterinary Medical Association) studied 8 healthy cats. Absorption of the reference solution was 3 times that of the reference capsule, while compounded formulations were absorbed poorly and inconsistently, at only 2% to 8% of reference values [5].
  • Renschler and colleagues (2018, Journal of the American Animal Hospital Association) measured serum concentrations in 95 dogs and 20 cats treated for systemic mycosis. Mean concentration was 0.5 micrograms per mL in the compounded group, compared with 8.3 for generic and 6.5 for brand name, and 95.2% of the compounded group fell below the therapeutic threshold. The authors suggested therapeutic drug monitoring may be beneficial in all cases [6].

Findings come from the cited studies and do not promise any individual outcome.

Why is it compounded, and how is it typically used?

Why it is compounded

Itraconazole is sold as 100 mg capsules and as a 10 mg/mL oral solution, and no FDA approved veterinary product exists. A cat or parrot dosed from a 10 mg/mL liquid may need a volume that is impractical to give, and commercial products carry no flavors an animal will accept.

Dosage forms and strengths

  • Concentration set by the prescriber, so the measured volume stays small
  • Flavors selected for the species or the patient
  • Dye free versions on request
  • Starting material specified by the prescriber on the prescription

The studies above tested suspensions compounded from bulk powder. Prescribers ordering this preparation should specify the starting material and consider whether serum concentration monitoring fits the case [4][5][6]. Dosing, monitoring, and duration are the prescriber's decision.

How Mixwell prepares it

Mixwell compounds this suspension in Chino, California under USP 795 standards for non sterile preparations [7]. Prescribers may specify the starting material, and our pharmacist confirms it before compounding. Batch records document each preparation, and finished suspensions ship across California.

Safety information

Itraconazole labeling carries a boxed warning. It should not be given to patients with ventricular dysfunction such as congestive heart failure, except for life threatening or serious infections, and a dose related negative inotropic effect has been documented [1].

Coadministration with several CYP3A4 substrates, including cisapride, pimozide, methadone, and quinidine, is contraindicated, and serious arrhythmias and sudden death have occurred [1]. Serious hepatotoxicity has been reported, including cases with no pre-existing liver disease [1].

Absorption from compounded suspensions can be low and variable, which raises the risk of underexposure [4][5][6]. Patient selection, dosing, monitoring, and duration are the prescriber's responsibility.

References
  1. Itraconazole oral solution, 10 mg/mL. Prescribing information. DailyMed, U.S. National Library of Medicine. DailyMed label
  2. Pappas PG, Kauffman CA, Andes DR, et al. Clinical practice guideline for the management of candidiasis: 2016 update by the Infectious Diseases Society of America. Clin Infect Dis. 2016;62(4):e1 to e50. doi:10.1093/cid/civ933
  3. Barone JA, Moskovitz BL, Guarnieri J, et al. Enhanced bioavailability of itraconazole in hydroxypropyl beta cyclodextrin solution versus capsules in healthy volunteers. Antimicrob Agents Chemother. 1998;42(7):1862 to 1865. doi:10.1128/AAC.42.7.1862
  4. Mawby DI, Whittemore JC, Genger S, Papich MG. Bioequivalence of orally administered generic, compounded, and innovator formulated itraconazole in healthy dogs. J Vet Intern Med. 2014;28(1):72 to 77. doi:10.1111/jvim.12219
  5. Mawby DI, Whittemore JC, Fowler LE, Papich MG. Comparison of absorption characteristics of oral reference and compounded itraconazole formulations in healthy cats. J Am Vet Med Assoc. 2018;252(2):195 to 200. doi:10.2460/javma.252.2.195
  6. Renschler J, Albers A, Sinclair-Mackling H, Wheat LJ. Comparison of compounded, generic, and innovator formulated itraconazole in dogs and cats. J Am Anim Hosp Assoc. 2018;54(4):195 to 200. doi:10.5326/JAAHA-MS-6591
  7. United States Pharmacopeia. General Chapter 795, Pharmaceutical Compounding: Nonsterile Preparations. USP NF. Official November 1, 2023.

What to include on the prescription

  • APIs and strengths
  • Base or vehicle
  • Quantity
  • Directions for use
  • Refills
  • Allergies or dye free needs
Call (909) 378-7301 Fax (909) 378-7071

Compounded in Chino, CA. Delivered across California.

  • Chino
  • Chino Hills
  • Ontario
  • Pomona
  • Diamond Bar
  • Rancho Cucamonga
  • Eastvale
Mixwell Compounding Pharmacy 13788 Roswell Ave, Ste 158, Chino, CA 91710
(909) 378-7301

Compounded medications are not reviewed or approved by the FDA. Dispensed only with a valid prescription. Mixwell is a non sterile pharmacy and does not prepare sterile products or injectables. Compounded preparations are not presented as superior to commercially available products, and nothing here promises a specific result. Mixwell does not accept insurance. Call for pricing.

Want to learn more about Itraconazole Oral Suspension, Custom Concentration

Are you a healthcare provider or patient in Chino, Chino Hills, Ontario, Eastvale, Rancho Cucamonga, or Upland? Mixwell Pharmacy provides specialized pharmaceutical support throughout San Bernardino, Los Angeles, and Orange Counties. Contact our Chino laboratory to learn how we facilitate customized Itraconazole Oral Suspension, Custom Concentrationfor practitioners across Southern California.

(909) 378-7301