Name | flucytosine |
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Synonyms |
4-amino-5-fluoro-1,2-dihydropyrimidin-2-one
4-Amino-5-fluoro-2(1H)-pyrimidinone 5-Fluorocytosine Fluocytosine 6-amino-5-fluoro-1H-pyrimidin-2-one Flucytosin Ancotil 4-amino-5-fluoro-2(1H)-pyrimidinone,5-Fluorocytosine,Flucytosine 5-Fluorocytosin 4-amino-5-fluoro-2(1H)-pyrimidinone,Flucytosine MFCD00006035 4-Amino-5-fluoro-2-hydroxypyrimidine EINECS 217-968-7 Fluorcytosine Flucytosine Ancobon 5-Fluorocystosine 4-amino-5-fluoro-2-pyrimidone Fluorocytosine |
Description | Flucytosine (5-Fluorocytosine, 5-FC, Ancobon), a fluorinated pyrimidine analogue, is an antifungal drug.Target: antifungalFlucytosine, or 5-fluorocytosine, a fluorinated pyrimidine analogue, is a synthetic antimycotic drug. It is structurally related to the cytostatic fluorouracil and to floxuridine. It is available in oral and in some countries also in injectable form. A common brand name is Ancobon. Flucytosine was first synthesized in 1957 but its antifungal properties were discovered in 1964. The drug is dispensed in capsules of 250 mg and 500 mg strength. The injectable form is diluted in 250 mL saline solution to contain 2.5 g total (10 mg/mL). The solution is physically incompatible with other drugs including amphotericin B.Flucytosine is well absorbed (75 to 90%) from the gastrointestinal tract. Intake with meals slows the absorption, but does not decrease the amount absorbed. Following an oral dose of 2 grams peak serum levels are reached after approximately 6 hours. The time to peak level decreases with continued therapy. After 4 days peak levels are measured after 2 hours. The drug is eliminated renally. In normal patients flucytosine has reportedly a half-life of 2.5 to 6 hours. In patients with impaired renal function higher serum levels are seen and the drug tends to cumulate in these patients. The drug is mainly excreted unchanged in the urine (90% of an oral dose) and only traces are metabolized and excreted in the feces. Therapeutic serum levels range from 25 to 100 ?g/ml. Serum levels in excess of 100 ug are associated with a higher incidence of side effects. Periodic measurements of serum levels are recommended for all patients and are a must in patients with renal damage. |
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Related Catalog | |
References |
Density | 1.7±0.1 g/cm3 |
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Boiling Point | 298ºC |
Melting Point | 298-300 °C (dec.)(lit.) |
Molecular Formula | C4H4FN3O |
Molecular Weight | 129.092 |
Exact Mass | 129.033844 |
PSA | 71.77000 |
LogP | -2.36 |
Vapour Pressure | 0.0492mmHg at 25°C |
Index of Refraction | 1.649 |
Storage condition | 2-8°C |
Stability | Light Sensitive |
Water Solubility | 1.5g/100mL (25 ºC) |
Synonym: Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS
Risk Phrases: 40 Section 3 - HAZARDS IDENTIFICATION EMERGENCY OVERVIEW
Limited evidence of a carcinogenic effect.Light sensitive. Potential Health Effects Eye: May cause eye irritation. Skin: May cause skin irritation. Ingestion: No hazard expected in normal industrial use. Inhalation: May cause respiratory tract irritation. The toxicological properties of this substance have not been fully investigated. Chronic: Prolonged or repeated exposure may cause adverse reproductive effects. Section 4 - FIRST AID MEASURES Eyes: Flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid. Skin: Get medical aid. Flush skin with plenty of water for at least 15 minutes while removing contaminated clothing and shoes. Ingestion: Get medical aid. Wash mouth out with water. Inhalation: Remove from exposure and move to fresh air immediately. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical aid. Notes to Physician: Section 5 - FIRE FIGHTING MEASURES General Information: As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. Extinguishing Media: Use water spray, dry chemical, carbon dioxide, or chemical foam. Section 6 - ACCIDENTAL RELEASE MEASURES General Information: Use proper personal protective equipment as indicated in Section 8. Spills/Leaks: Vacuum or sweep up material and place into a suitable disposal container. Section 7 - HANDLING and STORAGE Handling: Avoid breathing dust, vapor, mist, or gas. Avoid contact with skin and eyes. Store protected from light. Storage: Store in a cool, dry place. Store in a tightly closed container. Keep refrigerated. (Store below 4C/39F.) Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION Engineering Controls: Use adequate ventilation to keep airborne concentrations low. Exposure Limits CAS# 2022-85-7: Personal Protective Equipment Eyes: Not available. Skin: Wear appropriate protective gloves to prevent skin exposure. Clothing: Wear appropriate protective clothing to prevent skin exposure. Respirators: Follow the OSHA respirator regulations found in 29 CFR 1910.134 or European Standard EN 149. Use a NIOSH/MSHA or European Standard EN 149 approved respirator if exposure limits are exceeded or if irritation or other symptoms are experienced. Section 9 - PHYSICAL AND CHEMICAL PROPERTIES Physical State: Solid Color: white Odor: odorless pH: Not available. Vapor Pressure: Not available. Viscosity: Not available. Boiling Point: Not available. Freezing/Melting Point: 296 deg C dec Autoignition Temperature: Not available. Flash Point: 296 deg C ( 564.80 deg F) Explosion Limits, lower: Not available. Explosion Limits, upper: Not available. Decomposition Temperature: 296 deg C Solubility in water: IN WATER: 1.5 G/100 ML (25C) Specific Gravity/Density: Molecular Formula: Molecular Weight: 129.09 Section 10 - STABILITY AND REACTIVITY Chemical Stability: Not available. Conditions to Avoid: Incompatible materials, light, excess heat, exposure to flame. Incompatibilities with Other Materials: Oxidizing agents. Hazardous Decomposition Products: Hydrogen cyanide, carbon monoxide, oxides of nitrogen, carbon dioxide, hydrogen fluoride gas. Hazardous Polymerization: Has not been reported Section 11 - TOXICOLOGICAL INFORMATION RTECS#: CAS# 2022-85-7: HA6040000 LD50/LC50: CAS# 2022-85-7: Oral, rat: LD50 = >15 gm/kg. Carcinogenicity: 5-Fluorocytosine - Not listed by ACGIH, IARC, or NTP. Other: See actual entry in RTECS for complete information. Section 12 - ECOLOGICAL INFORMATION Section 13 - DISPOSAL CONSIDERATIONS Dispose of in a manner consistent with federal, state, and local regulations. Section 14 - TRANSPORT INFORMATION IATA No information available. IMO No information available. RID/ADR No information available. Section 15 - REGULATORY INFORMATION European/International Regulations European Labeling in Accordance with EC Directives Hazard Symbols: XN Risk Phrases: R 40 Limited evidence of a carcinogenic effect. Safety Phrases: S 36/37 Wear suitable protective clothing and gloves. S 45 In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible). WGK (Water Danger/Protection) CAS# 2022-85-7: No information available. Canada None of the chemicals in this product are listed on the DSL/NDSL list. CAS# 2022-85-7 is not listed on Canada's Ingredient Disclosure List. US FEDERAL TSCA CAS# 2022-85-7 is not listed on the TSCA inventory. It is for research and development use only. SECTION 16 - ADDITIONAL INFORMATION N/A |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
MUTATION DATA
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Symbol |
GHS08 |
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Signal Word | Warning |
Hazard Statements | H361 |
Precautionary Statements | P280 |
Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
Hazard Codes | Xn:Harmful |
Risk Phrases | R40 |
Safety Phrases | S22-S24/25-S45-S36/37 |
RIDADR | NONH for all modes of transport |
WGK Germany | 2 |
RTECS | HA6040000 |
HS Code | 2933599090 |
Precursor 3 | |
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DownStream 5 | |
HS Code | 2933599090 |
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Summary | 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |