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Fluconazole injection 100ml is an antifungal drug administered intravenously, belonging to the triazole class of compounds. Its core mechanism is to inhibit the 14 α - lanosterol demethylase dependent on fungal cytochrome P450, block ergosterol synthesis, and increase fungal cell membrane permeability and cell lysis. This preparation is provided in the form of a sterile isotonic solution with a concentration of 2mg/mL. The packaging specifications include 100mL (containing 200mg fluconazole) and 200mL (containing 400mg fluconazole), and is suitable for patients who cannot take it orally or need to quickly reach therapeutic concentrations.
Indications for treatment: including oral and pharyngeal candidiasis, esophageal candidiasis, cryptococcal meningitis, invasive candidemia, and disseminated candidiasis, especially suitable for severe infections in immunosuppressed patients (such as HIV infected individuals and bone marrow transplant recipients).
Preventive medication: Used to prevent fungal infections in high-risk populations such as cancer patients and organ transplant recipients receiving chemotherapy or radiation therapy.
This preparation has significant advantages: intravenous administration can bypass gastrointestinal absorption, ensuring a bioavailability of nearly 100%; Low plasma protein binding rate (11% -12%), strong tissue penetration, cerebrospinal fluid concentration can reach up to 80% of plasma, especially suitable for central nervous system infections. However, attention should be paid to its interaction with CYP3A4/2C9 substrates (such as warfarin and phenytoin), which may cause QT interval prolongation or bleeding risk, and should be closely monitored during medication.
Additional information of chemical compound:
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Fluconazole +. COA
Fluconazole injection 100ml, as a representative of fluorotriazole antifungal drugs, has become an important choice for the cure of skin fungal diseases due to its broad-spectrum antibacterial activity, good tissue penetration, and convenient administration method. Its mechanism of action is to selectively inhibit the biosynthesis of ergosterol in fungal cell membranes, disrupt membrane integrity, and thus exert bactericidal or bacteriostatic effects.
1. Superficial skin fungal disease
It has a strong inhibitory effect on common pathogenic bacteria such as Trichophyton rubrum, Trichophyton beard, and Trichophyton flocs, as well as Malassezia and Candida genera. It is suitable for the following diseases:
Tinea corporis and tinea crus: circular erythema and scaly skin lesions caused by dermatophytes. Flunazol can quickly penetrate the stratum corneum through oral or local administration, inhibiting fungal metabolism.
Tinea pedis: For erosive or vesicular types of tinea pedis between the toes, the course of flunazol cure is usually 2-6 weeks, which can significantly reduce the recurrence rate. Research has shown that the weekly 150mg oral regimen has a cure rate of 70% -85% for onychomycosis, especially for nail infections.
Tinea capitis: In the cure of tinea capitis in children, flunazol is taken continuously at a daily dose of 50-100mg for 4-8 weeks, which can replace traditional gibberellin and reduce the risk of liver function damage.Tinea versicolor (Malassezia folliculitis): Flunazol inhibits the lipase activity of Malassezia, blocking its pathway of utilizing sebum for reproduction. A single oral dose of 150-300mg can achieve clinical cure.
2. Deep skin fungal diseases
For deep fungal infections in immunocompromised patients (such as HIV infected individuals and organ transplant recipients), flunazol can penetrate the blood-brain barrier and skin appendages, exerting a systemic therapeutic effect:
Chronic cutaneous candidiasis: Long term use of flunazol 50-100mg/day can maintain stable condition and reduce recurrence.
Chromogenic blastomycosis: As a combination therapy drug, flunazol combined with amphotericin B or itraconazole can enhance efficacy and shorten cure duration.
Sporothrix disease: Although not the preferred medication, flunazol 200-400mg/day orally can control the progression of the disease in patients who are intolerant to potassium iodide.
3. Pathogen coverage
Flunazol is effective against dermatophytes such as Trichophyton rubrum and Trichophyton rubrum (the main pathogens of onychomycosis) and Candida genus, but ineffective against some non dermatophytes such as Aspergillus genus. Research has shown that its clinical cure rate for nail fungal diseases is 76% -90%, the cure rate for toenails is about 28% -36%, the mycological conversion rate is 47% -62%, but the recurrence rate is less than 4%.
Comparison of therapeutic effects
Compared with terbinafine/itraconazole, flunazol has a lower cure rate than terbinafine (85% -95% for nails) and itraconazole (70% -80% for pulse therapy), but a lower incidence of adverse reactions (about 10% vs. terbinafine 15%, itraconazole 20%).
Advantage scenario: Suitable for patients with mild to moderate onychomycosis, those who cannot tolerate other drugs, or those who require long-term maintenance cure (such as immunosuppressants).
Accurate regulation of dosage and treatment course
The dosing regimen of fluconazole injection 100ml should be formulated based on the type, severity, and immune status of the patient, with the core principles of "sufficient amount, sufficient cure duration, and individualization".
Tinea corporis/tinea pedis:
Oral administration: 150mg single dose (shock therapy) or 50mg/day, with a course of 2-4 weeks;
Localized: Combining topical azole cream (such as clotrimazole) can enhance efficacy and shorten cure duration.
Onychomycosis:
Nail infection: 150mg/week for 8 consecutive weeks;
Nail infection: 150mg/week for 12 consecutive weeks;
The combination of topical application of 5% Amorofen ointment can increase the cure rate to over 90%.
Tinea capitis:
Children: Adjust the dosage according to body weight (<20kg: 62.5mg/day; 20-40kg: 125mg/day; >40kg: 250mg/day), cure course 4-8 weeks;
Adults: 200-400mg/day, combined with topical application of sulfur ointment or ketoconazole detergent.
Immunosuppressed patients:
Preventive medication: Oral administration of 50-200mg per day after organ transplantation can reduce the risk of invasive candidiasis by up to 60%;
Therapeutic medication: For HIV infected individuals with oral candidiasis, the first dose is 200mg, followed by 100mg per day, for a course of 7-14 days.
Individuals with liver and kidney dysfunction:
Mild liver injury (Child Pugh A): No dose adjustment required;
Moderate to severe liver injury (Child Pugh B/C grade): dose halved to 50mg/day or extended dosing interval;
Renal insufficiency (CrCl<50mL/min): The oral dose remains unchanged, but blood drug concentration needs to be monitored.
For Candida albicans or Candida albicans with decreased sensitivity to flunazol, the following combination therapy can be used:
Flunazol+Amphotericin B: When treating chromoblastomycosis, intravenous infusion of Amphotericin B 0.5-1mg/kg/day is given for 1-2 weeks, followed by oral flunazol 200mg/day to maintain cure.
Flunazol+Terbinafine: For onychomycosis, flunazol 150mg/week combined with Terbinafine 250mg/day for 12 weeks can improve the clinical cure rate to 85%.
Therapeutic advantages:
Flunazol has dual characteristics of high water solubility and lipid solubility, with an oral absorption rate of over 90%, and its bioavailability is not affected by food. Its protein binding rate is low (11% -12%), and it can be widely distributed in the skin, nails, cerebrospinal fluid, and prostate tissue. It maintains a stable blood drug concentration for a long time (half-life of 30 hours) and supports a weekly dosing regimen.
Onychomycosis: A meta-analysis involving 1200 patients showed that after 12 weeks of flunazol cure, the clinical cure rate reached 78%, fungal clearance rate was 82%, and the 1-year recurrence rate was only 15%, significantly lower than that of oxytetracycline (35%) and itraconazole pulse therapy (25%).
Recurrent vaginal candidiasis: Flunazol 150mg once a week for 6 consecutive months of maintenance cure can reduce the one-year recurrence rate from 60% to 10%.
Compared to topical medications that require multiple daily doses or intravenous infusion of amphotericin B, oral flunazol formulations (tablets/capsules) and single pulse therapy significantly improve patient compliance. Research shows that patients who use a weekly flunazol dosing regimen have a cure completion rate of 92%, while the daily dosing regimen is only 65%.
Adverse Reaction Management: Safety Assessment and Monitoring Strategies
Although fluconazole injection 100ml has good overall safety, the following potential risks still need to be considered:
Liver toxicity monitoring
Risk population: patients with long-term medication (>3 months), concomitant use of statins or anti tuberculosis drugs, and pre-existing liver disease.
Monitoring indicators: ALT, AST, ALP, and bilirubin should be tested before cure and monthly. If ALT increases to more than three times the upper limit of normal, medication should be suspended and liver protection cure should be given.
rug interaction management
Anticoagulants: Flunazol can inhibit CYP2C9 enzyme, causing a 20% -50% increase in warfarin blood concentration. INR values need to be monitored and dosage adjusted.
Immunosuppressants: When used in combination with cyclosporine, flunazol can increase the blood concentration of cyclosporine by 50% -100%, and the dose of cyclosporine needs to be reduced to 50% -70% of the original dose.
Antiepileptic drugs: Flunazol can inhibit the metabolism of phenytoin sodium, leading to neurotoxicity (such as ataxia and tremor). It is necessary to halve the dose of phenytoin sodium and monitor blood drug concentration.
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