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Itraconazole CAS 84625-61-6

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CAS No.:

84625-61-6

Port:

shanghai

Packaging:

bag

Price valid (until):

2024-01-04

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SHANDONG LOOK CHEMICAL CO.,LTD

Company Type:

Manufactory

Location:

China

Qualification:

Main Products:

Agrochemicals,Daily Chemicals,Catalysts & Chemical Auxiliary Agents,Extract,Inorganic Chemicals,Organic Intermediate

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Product Description
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Inquiry History

Description

Product Detail

Broad - spectrum antifungal agents	Itraconazole is an artificially synthetic clotrimazole, being a broad-spectrum synthetic antifungal agent. Its antimicrobial spectrum and antimicrobial mechanism is similar to clotrimazole, but has strong antibacterial activity against Aspergillus. It exerts its anti-fungal effect through changing the fungal cell membrane permeability with antibacterial activity against superficial and deep fungal pathogens. Its antibacterial spectrum is broader and stronger than ketoconazole, being able to inhibit the ergosterol synthesis of fungal cell membrane, thus playing the antifungal effect. This product is suitable for the treatment of Dermatophytes (Trichophyton, Microsporum, Flocculent Epidermophyton), Yeast [Cryptococcus neoformans, Pityrosporum, Candida (including Candida albicans, Candida glabrata and candida krusei)], Aspergillus, Histoplasma, Paracoccidioides brasiliensis, Sporothrix schenckii, Hormodendrum, Cladosporium, Blastomyces dermatitidis and various kinds of other types of yeasts and fungi. Itraconazole is not able to inhibit the growth of Rhizopus and Mucor. One nitrogen atom contained in the itraconazole molecule can bind to the ferrous ion on the heme of the P450 molecule in the fungal cell, thereby inhibiting the P450 hydroxylase-catalyzed de-methylation of lanosterol, Sterol to ergosterol conversion blocked, lanosterol and other precursors accumulation, membrane chemical composition changes, membrane associated enzyme dysfunction, increased permeability, intracellular fluid spill, so as to achieve the inhibition and sterilization. The combination of this product with the fungus P450 system is quite strong while its combination with the mammalian P450 system is weak, so that the toxicity of drugs on human is greatly reduced. Clinical Itraconazole is mainly used for the treatment of systemic deep fungal infections caused by systems such as blastomycosis, histoplasmosis, coccidioidomycosis, chromoblastomycosis, sporotrichosis and coccidioidomycosis. It can also be used for the treatment of candidiasis and aspergillosis. The above information is compiled and edited by Tongtong from Chemicalbook.
Pharmacokinetics	Itraconazole, when taken immediately after the meal, can give the highest bioavailability. After (4.6 ± 1.3) hours of oral administration of 200 mg of itraconazole, the plasma concentration can reach peak with the plasma concentration being (0.32 ± 0.16) mg/mL. The product has a plasma protein binding rate of 99.8% with the whole blood concentration being about 60% of the plasma concentration. The drug concentration in the lung, kidney, liver, bone, stomach, spleen and muscle was found to be 2 to 3 times as high as that in the corresponding plasma concentration. In keratin-rich tissues, especially in the skin, the concentration is four times as high as that in the plasma concentration while the drug clearance is associated with the process of epidermal regeneration. If withdraw the drug after continuous medication of 4 weeks, the plasma concentration become undetectable after 7 days while drug contained in the skin can be still maintained in the drug treatment concentration for 2 to 4 weeks. After a week of starting the treatment, it can be measured of itraconazole in the keratin. At the end of the 3-month treatment course, the drug concentration can be maintained for at least 6 months. This product is present in sebum with a small amount also existing in sweat. Itraconazole is also concentrated in areas susceptible to fungal infection. The duration of the treatment concentration in the vaginal tissue is: 200mg once per day for 3 days, last for 2 days; 200mg 2 times a day for 1 day, can last 3 days. Itraconazole is mainly metabolized in the liver, producing large amounts of metabolites. One of them is hydroxylated itraconazole; in vitro study has found that it has a similar antifungal activity with this product. The level of antifungal drug measured by bioanalytical method is three times as high as the level measured by high-pressure liquid chromatography analysis. This product was biphasic in plasma clearance with the terminal half-life of (23.8 ± 4.7) hours. The dosage of the prototype drug through fecal excretion accounts for about 3 to 18% of the total dose. The prototype drug via renal excretion is less than 0.03% of the dose with about 35% being subject to urine excretion in the form of metabolites within a week.
Clinical application and indications	Itraconazole is applicable for the treatment of the following diseases: 1, it can be used for the treatment of systemic fungal infections, such as aspergillosis, candidiasis, cryptococcosis (including cryptococcal meningitis), histoplasmosis, sporotrichosis, Paracoccidioides brasiliensis disease, blastomycosis and many other kinds of rare systemic or tropical fungal diseases. 2, it can be used for the treatment of the candidiasis infection occurred in the mouth, throat (foreign data), esophageal (foreign data) and vulvovagina, and fungal conjunctivitis, fungal keratitis. 3, it can be used for the treatment of superficial fungal infections, such as hand, foot and ringworm, tinea corporis, tinea corporis, tinea versicolor and so on. 4, it can be used for the treatment of dermatophytes and (or) yeast-induced onychomycosis.
Dosage and Usage	Capsules: In order to achieve optimal absorption, itraconazole capsules should be administered immediately after a meal and the capsule must be swallowed. 1. Candida vaginitis: 200mg each time, twice a day, a course of treatment for 1 day or 200mg, once the course of treatment of 3 days; 2. Tinea versicolor: 200mg each time, once a day with the course of treatment of 7 days ; 3. Dermatomycosis: 100 mg each time, once a day with the course of treatment of 15 days; high-degree keratinized area (such as foot bottom ringworm, hand tinea) need: extended treatment of 15 days; 4 Oral candidiasis: 100mg each time, once a day with the course of treatment of 15 days; 5. Fungal keratitis: 200 mg each time, once a day with the course of treatment of 21 days; 6. For some immunodeficiency patients, such as leukemia (such as leukemia), AIDs and organ transplanted patients, application of itraconazole capsules for the treatment of fungal infections can get reduced oral bioavailability; in this case, the dose can be doubled. 7. Onychomycosis: 1) shock treatment: 200 mg each time, twice per day with continuous one week as a shock treatment. For the treatment of nail infections, it is recommended to adopt two shock treatment courses with each course having a gap of 3 weeks; for the treatment of toenail infection, it is recommended to adopt three shock treatment courses. Each treatment course has a gap of 3 weeks. 2) Or adopt continuous treatment: 200 mg each time, once a day, continue for three months. This product is removed more slowly in the skin and keratin tissue than removed in the plasma. Therefore, for skin infections, 2 to 4 weeks after stopping the drug can achieve the most ideal clinical and mycological efficacy. For the treatment of onychomycosis, people can achieve the best clinical and mycological efficacy after 6~9 months of stopping the drugs. Injection: during the first two days, give itraconazole injection 2 times a day, later change to once per day. Treatment protocol in Day 1 and 2: 2 times per day; adopt intravenous infusion of 200 mg itraconazole 1 hour each time. From day 3: perform once per day with intravenously infusion of 200 mg of itraconazole for 1 hour each time. The safety for intravenous administration of more than 14 days is not clear.

Basic Info

Product Name:

Itraconazole

Other Name:

3H-1,2,4-Triazol-3-one,4-[4-[4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl)-,rel-;rel-4-[4-[4-[4-[[(2R,4S)-2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl)-3H-1,2,4-triazol-3-one;Itraconazole;R 51211;Oriconazole;Sporanox;Orungal;Itrizole;Triasporin;Sempera;Canditral;Traconal;Sporamelt;Spherazole CR;Spherazole IR;Sporonox;Sporal;Itrac;Cladosal 100;Itralek;Sporanox IV;Candistat;cis-Itraconazole;SUBA Itraconazole;Orungamin;PUR 1900;Fungitraxx

CAS No.:

84625-61-6

Molecular Formula:

C35H38Cl2N8O4

InChIKeys:

InChIKey=VHVPQPYKVGDNFY-WGEGMAFPNA-N

Molecular Weight:

705.63300

Exact Mass:

705.63

EC Number:

617-596-9

NSC Number:

759239

DSSTox ID:

DTXSID3023180

Color/Form:

Solid|Crystals from toluene

ATC Code:

QJ02AC02|J02AC02|J - Antiinfectives for systemic use

HScode:

2934999090

Categories:

Synthetic Anti-infective Drugs

Characteristics

PSA:

104.70000

XLogP3:

5.66 (LogP)

Appearance:

off-White crystalline solid

Density:

1.27 g/cm³

Melting Point:

166.2 °C

Boiling Point:

850ºC at 760 mmHg

Flash Point:

467.9ºC

Refractive Index:

1.678

Water Solubility:

chloroform: 50 mg/mL, clear, colorless

Storage Conditions:

2-8ºC

Vapor Pressure:

2.6X10-20 mm Hg at 25 °C (est)

Toxicity:

LD50 (14 day) in mice, rats, dogs (mg/kg): >320, >320, >200 orally (Van Cauteren)

Dissociation Constants:

3.70|pKa = 3.7

See More Itraconazole Properties 

Hazard Identification

Classification of the substance or mixture

Acute toxicity - Category 4, Oral

Skin irritation, Category 2

Eye irritation, Category 2

Specific target organ toxicity â single exposure, Category 3

GHS label elements, including precautionary statements

Precautionary statement(s)
Pictogram(s)
Signal word	Warning
Hazard statement(s)	H302 Harmful if swallowed H315 Causes skin irritation H319 Causes serious eye irritation H335 May cause respiratory irritation
Prevention	P264 Wash ... thoroughly after handling. P270 Do not eat, drink or smoke when using this product. P280 Wear protective gloves/protective clothing/eye protection/face protection/hearing protection/... P261 Avoid breathing dust/fume/gas/mist/vapours/spray. P271 Use only outdoors or in a well-ventilated area.
Response	P301+P317 IF SWALLOWED: Get medical help. P330 Rinse mouth. P302+P352 IF ON SKIN: Wash with plenty of water/... P321 Specific treatment (see ... on this label). P332+P317 If skin irritation occurs: Get medical help. P362+P364 Take off contaminated clothing and wash it before reuse. P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P304+P340 IF INHALED: Remove person to fresh air and keep comfortable for breathing. P319 Get medical help if you feel unwell.
Storage	P403+P233 Store in a well-ventilated place. Keep container tightly closed. P405 Store locked up.
Disposal	P501 Dispose of contents/container to an appropriate treatment and disposal facility in accordance with applicable laws and regulations, and product characteristics at time of disposal.

Other hazards which do not result in classification

no data available

Handling and Storage

Precautions for safe handling

Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.

Conditions for safe storage, including any incompatibilities

Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.

See More Itraconazole Safety Data Sheet 

Seller Information

Business Type:
Manufactory

Main Products:
Agrochemicals,Daily Chemicals,Catalysts & Chemical Auxiliary Agents,Extract,Inorganic Chemicals,Organic Intermediate

Location:
hisense intelligence valley,no 2116,of phoenix road

Payment Terms:
TT against copy of documents,D/P,L/C

Average lead Time:
7

Total Annual Revenue:
Less than $1 million

Total Employees:
11-50

Year of Establishment:
2017

SHANDONG LOOK CHEMICAL CO.LTD, a new chemical enterprise in researching, manufacturing and supplying of chemicals located in beautiful “Spring City”-Jinan.Our company mainly working on the researching new-born APIs, intermediate ( especially Carbohydrate derivatives series). Meanwhile, we made huge breakthrough in industries of food, feed additives, cosmetics ,dye and industrial chemicals. Our company enjoyed great reputation both domestic and abroad under the belief of “Integrity management,Quality controlling and Customer orientation”. Web : www.chinalookchemical.com

We had been cooperated with NingXia University and Shandong University on more than ten projects for years and which had been in mass production on the market. We now have more than 80 people in our team and built research center in Jinan and Ningxia. Our manufacturing site allocated in chemical industry parks of Zhangqiu, Heze, Dezhou and Ningxia Fine Chemical Park. We strictly complying with ISO9001 and ISO 2000 standard in manufacturing process, our lab and workshop tightly in accordance with GMP standard.Our products best selling in Europe, South and North America,Asia pacific area and Africa. We sincerely welcome new and regular customers around the world visit us for business negotiation.

Inquiry History

13 Inquiries

Country	Product	Purchase Quantity	Date Posted
United States	Itraconazole 99% powder API CAS 84625-61-6	10 MT	Dec 2, 2023
Brazil	Itraconazole	500 G	Apr 24, 2026
Bangladesh	Itraconazole	1 KG	Mar 4, 2026
Bangladesh	Itraconazole	100 KG	Mar 4, 2026
United States	Itraconazole	1 KG	Dec 23, 2024
Colombia	Itraconazole Powder API Raw Material Itraconazole 99% White Color Powder SAA632177777000 SAA	5000 G	Nov 5, 2023
Brazil	Itraconazole Powder API Raw Material Itraconazole 99% White Color Powder SAA632177777000 SAA	1 KG	Jul 7, 2023
Morocco	Itraconazole	50 G	Jun 9, 2026
United States	Itraconazole	10 MG	Mar 6, 2026
United States	Itraconazole	1 KG	Oct 6, 2025
Brazil	Itraconazole	1	Nov 18, 2023
Brazil	Itraconazole Powder API Raw Material Itraconazole 99% White Color Powder SAA632177777000 SAA	1 KG	Nov 10, 2023
India	Itraconazole	1.00 KG	Mar 12, 2026

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Itraconazole Powder API Raw Material Itraconazole 99% White Color Powder SAA632177777000 SAA	Pharmaceutical Grade/99	M A M M TRANDING ENTERPRISE	Inquiry
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Itraconazole CAS 84625-61-6

Product Description

Seller Information