Erythromycin stearate

1018.4

1003.717102

211-396-1

LXW024X05M

756747

DTXSID0020571

C47989

CRYSTALS|WHITE OR SLIGHTLY YELLOW CRYSTALS OR POWDER

29415000

231.21000

8.11810

white to off-white

1.112g/cm3

77-79°C

523.101ºC

1.518

ethanol: soluble50mg/mL, clear to very slightly hazy, colorless

2-8°C

PRACTICALLY ODORLESS

SLIGHTLY BITTER

SOLN IS ALKALINE TO LITMUS

258.5 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Insoluble in water.

Alcohols and Polyols

A base. Readily forms salts with acids. (NTP, 1992)

NONH for all modes of transport

2

42/43-36/37/38

36-26

KF5785000

Xn,Xi

Stable. Combustible. Incompatible with acids, strong oxidizing agents.

P261-P280-P284-P304 + P340-P342 + P311

H317-H334

A REVIEW, WITH APPROX 20 REFERENCES, OF THE BIOAVAILABILITY FROM VARIOUS FORMULATIONS OF ERYTHROMYCIN STEARATE.[KNOTHE H, DETTE GA; PHARMACOKINETICS OF ERYTHROMYCIN; SCOTT MED J 22(5) 397 (1977)]|DHHS/NTP; Toxicology & Carcinogenesis Studies of Erythromycin sulfate in F344/N Rats and B6C3F1 Mice (Feed Studies) Technical Report Series No. 338 (1988) NIH Publication No. 89-2594

Flash point data for this chemical are not available; however, it is probably combustible. (NTP, 1992)

|Danger|H317 (59.62%): May cause an allergic skin reaction [Warning Sensitization, Skin]|P261, P264, P272, P280, P285, P302+P352, P304+P341, P305+P351+P338, P321, P333+P313, P337+P313, P342+P311, P363, and P501|Aggregated GHS information provided by 105 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Fires involving this material can be controlled with a dry chemical, carbon dioxide or Halon extinguisher. (NTP, 1992)

SMALL SPILLS AND LEAKAGE: Should a spill occur while you are handling this chemical, FIRST REMOVE ALL SOURCES OF IGNITION, then you should dampen the solid spill material with 60-70% ethanol and transfer the dampened material to a suitable container. Use absorbent paper dampened with 60-70% ethanol to pick up any remaining material. Seal the absorbent paper, and any of your clothes, which may be contaminated, in a vapor-tight plastic bag for eventual disposal. Solvent wash all contaminated surfaces with 60-70% ethanol followed by washing with a soap and water solution. Do not reenter the contaminated area until the Safety Officer (or other responsible person) has verified that the area has been properly cleaned. STORAGE PRECAUTIONS: You should store this material under ambient temperatures. (NTP, 1992)

RECOMMENDED RESPIRATOR: Where the neat test chemical is weighed and diluted, wear a NIOSH-approved half face respirator equipped with a combination filter cartridge, i.e. organic vapor/acid gas/HEPA (specific for organic vapors, HCl, acid gas, SO2 and a high efficiency particulate filter). (NTP, 1992)

A 77-YR-OLD WOMAN IS REPORTEDLY MAINTAINED ON 7.5 MG OF WARFARIN DAILY IN WHOM THE ADMIN OF ORAL ERYTHROMYCIN STEARATE, 500 MG 4 TIMES A DAY, RESULTED IN A PROTHROMBIN TIME OF 64 SECONDS (CONTROL, 11 SECONDS).

Toxicology and carcinogenesis studies of erythromycin stearate (USP grade, greater than 96% pure) were conducted by admin ... in feed to groups of F344/N rats and B6C3F1 mice for ... 2 yr studies of erythromycin stearate were conducted by feeding diets containing 0, 5,000 or 10,000 ppm erythromycin stearate to groups of 50 rats of each sex for 103 wk. Diets containing 0, 2,5000 or 5000 ppm were fed to groups of 50 mice of each sex for 103 wk. Conclusions: Under the conditions of these 2 yr studies, there was no evidence of carcinogenic activity of erythromycin stearate for male or female F344/N rats administered erythromycin stearate in the diet at 5,000 or 10,000 ppm. There was no evidence of carcinogenic activity of erythromycin stearate for male or female B6C3F1 mice administered erythromycin stearate in the diet at 2,500 or 5,000 ppm. ... /Erythromycin stearate/

ITS ACTIONS & USES ARE IDENTICAL TO THOSE OF ERYTHROMYCIN.|ERYTHROMYCIN MAY BE USEFUL FOR DISSEMINATED GONOCOCCAL DISEASE IN PREGNANT PT WHO IS ALLERGIC TO PENICILLIN... 13 PT...TREATED WITH 500 MG OF ERYTHROMYCIN... STEARATE, GIVEN ORALLY EVERY 6 HR FOR 5 DAYS, SHOWED RAPID CLINICAL & BACTERIOLOGICAL RESPONSES.|ANTIBACTERIAL AGENT|MEDICATION (VET): ANTIBACTERIAL AGENT

...ERYTHROMYCIN & ITS DERIV SELDOM CAUSE SERIOUS ADVERSE REACTIONS.

Substances that inhibit the growth or reproduction of BACTERIA. (See all compounds classified as Anti-Bacterial Agents.)|Drugs used for their effects on the gastrointestinal system, as to control gastric acidity, regulate gastrointestinal motility and water flow, and improve digestion. (See all compounds classified as Gastrointestinal Agents.)

PEAK CONCN IN PLASMA...0.3-0.5 UG/ML 4 HR AFTER ORAL ADMIN OF 250 MG OF BASE & ARE 0.3-1.9 UG/ML AFTER...500-MG TABLET. VARIOUS ESTERS OF ERYTHROMYCIN HAVE BEEN PREPARED TO...IMPROVE STABILITY & FACILITATE ABSORPTION. ...CONCN OF ERYTHROMYCIN IN PLASMA ARE LITTLE DIFFERENT IF STEARATE IS GIVEN ORALLY.|...DIFFUSES READILY INTO INTRACELLULAR FLUIDS, & ANTIBACTERIAL ACTIVITY... ACHIEVED AT...ALL SITES EXCEPT BRAIN & CSF. ...ONE OF FEW ANTIBIOTICS THAT PENETRATES INTO PROSTATIC FLUID, CONCN ARE APPROX 40% OF...PLASMA. EXTENT OF BINDING...TO PLASMA PROTEINS VARIES...PROBABLY EXCEEDS 70% IN ALL.../FORMS OF DRUG/. /ERYTHROMYCIN/|ERYTHROMYCIN BASE IS ADEQUATELY ABSORBED FROM UPPER PART OF SMALL INTESTINE; IT IS INACTIVATED BY GASTRIC JUICE... FOOD IN STOMACH DELAYS ITS ULTIMATE ABSORPTION. /ERYTHROMYCIN/|ERYTHROMYCIN TRAVERSES PLACENTAL BARRIER; & CONCN OF DRUG IN FETAL PLASMA ARE ABOUT 5-20% OF THOSE IN MATERNAL CIRCULATION. /ERYTHROMYCIN/|For more Absorption, Distribution and Excretion (Complete) data for ERYTHROMYCIN STEARATE (11 total), please visit the HSDB record page.

IT IS HYDROLYZED IN SMALL INTESTINE & IN TISSUES TO YIELD ERYTHROMYCIN.

...INHIBIT PROTEIN SYNTH BY BINDING TO 50 S RIBOSOMAL SUBUNITS OF SENSITIVE MICROORGANISMS. ... ASSOC BETWEEN ERYTHROMYCIN & RIBOSOME IS REVERSIBLE BUT TAKES PLACE ONLY WHEN 50 S SUBUNIT IS FREE FROM TRNA MOLECULES BEARING NASCENT PEPTIDE CHAINS. PRODN...OF HIGHLY POLYMERIZED HOMOPEPTIDES IS SUPPRESSED. /ERYTHROMYCIN/|THE NONIONIZED FORM OF THE DRUG IS CONSIDERABLY MORE PERMEABLE TO CELLS, & THIS PROBABLY EXPLAINS INCREASED ANTIMICROBIAL ACTIVITY THAT IS OBSERVED AT ALKALINE PH. /ERYTHROMYCIN/

SYMPTOMS: Symptoms of exposure to this compound include nausea, vomiting, diarrhea and abdominal cramps. Chronic overexposure may cause jaundice. This may be accompanied by fever, leukocytosis, eosinophilia and elevated activities of transaminases in plasma. Allergic reactions to this compound may include fever, eosinophilia, skin eruptions, urticaria and anaphylaxis. Cholestatic hepatitis occurs rarely. Epigastric distress, possibly severe may also occur. Intramuscular injections of large quantities of this compound may cause extremely severe pain that persists for hours. Intravenous infusions of 1 gram doses have reportedly been followed by thrombophlebitis. Prolonged use may result in an overgrowth of nonsusceptible bacteria or fungi. There have been isolated reports of reversible hearing loss occurring after exposure to this chemical, chiefly in persons with renal insufficiency. ACUTE/CHRONIC HAZARDS: When heated to decomposition, this compound may emit toxic fumes of NOx. (NTP, 1992)

EYES: First check the victim for contact lenses and remove if present. Flush victim's eyes with water or normal saline solution for 20 to 30 minutes while simultaneously calling a hospital or poison control center. Do not put any ointments, oils, or medication in the victim's eyes without specific instructions from a physician. IMMEDIATELY transport the victim after flushing eyes to a hospital even if no symptoms (such as redness or irritation) develop. SKIN: IMMEDIATELY flood affected skin with water while removing and isolating all contaminated clothing. Gently wash all affected skin areas thoroughly with soap and water. If symptoms such as redness or irritation develop, IMMEDIATELY call a physician and be prepared to transport the victim to a hospital for treatment. INHALATION: IMMEDIATELY leave the contaminated area; take deep breaths of fresh air. IMMEDIATELY call a physician and be prepared to transport the victim to a hospital even if no symptoms (such as wheezing, coughing, shortness of breath, or burning in the mouth, throat, or chest) develop. Provide proper respiratory protection to rescuers entering an unknown atmosphere. Whenever possible, Self-Contained Breathing Apparatus (SCBA) should be used; if not available, use a level of protection greater than or equal to that advised under Protective Clothing. INGESTION: If the victim is conscious and not convulsing, give 1 or 2 glasses of water to dilute the chemical and IMMEDIATELY call a hospital or poison control center. Generally, the induction of vomiting is NOT recommended outside of a physician's care due to the risk of aspirating the chemical into the victim's lungs. However, if the victim is conscious and not convulsing and if medical help is not readily available, consider the risk of inducing vomiting because of the high toxicity of the chemical ingested. Ipecac syrup or salt water may be used in such an emergency. IMMEDIATELY transport the victim to a hospital. If the victim is convulsing or unconscious, do not give anything by mouth, ensure that the victim's airway is open and lay the victim on his/her side with the head lower than the body. DO NOT INDUCE VOMITING. IMMEDIATELY transport the victim to a hospital. (NTP, 1992)

AMONG ALLERGIC REACTIONS ARE FEVER, EOSINOPHILIA, & SKIN ERUPTIONS, WHICH MAY OCCUR ALONE OR IN COMBINATION; EACH DISAPPEARS SHORTLY AFTER THERAPY IS STOPPED. ...OFTEN PRODUCES IRRITATIVE EFFECTS. ORAL ADMIN...FREQUENTLY ACCOMPANIED BY EPIGASTRIC DISTRESS, WHICH MAY BE QUITE SEVERE. /ERYTHROMCYIN/|IM INJECTION OF QUANTITIES LARGER THAN 100 MG PRODUCES EXTREMELY SEVERE PAIN THAT PERSISTS FOR HOURS. IV INFUSION OF 1-G DOSES...ALMOST REGULARLY IS FOLLOWED BY THROMBOPHLEBITIS. /ERYTHROMYCIN/|...MILD ELEVATIONS OF THE SGOT /SERUM GLUTAMIC-OXALOACETIC TRANSAMINASE/ WERE ALSO NOTED IN...3 OF 97 PT TREATED WITH ERYTHROMYCIN STEARATE...|SEVERE RESP DISTRESS DEVELOPED IN A 60-YR-OLD MAN AFTER INGESTION OF 2 TABLETS OF ERYTHROMYCIN STEARATE. AUTHORS SUGGEST AN ALLERGIC REACTION OF TYPE 1 & TYPE 3 PARTICIPATED IN COURSE OF CLINICAL PICTURE.|OTOTOXICITY DUE TO ORAL ERYTHROMYCIN STEARATE DEVELOPED IN 2 PT (17 & 50-YR-OLD) RECEIVING AT LEAST 4 G DAILY. UPON WITHDRAWAL OF THE DRUG, HEARING RETURNED IN BOTH PT.

erythromycin stearate

ERYTHROMYCIN STEARATE TABLETS, USP (BRISTAMYCIN, ERYTHROCIN STEARATE, ETHRIL), CONTAIN 125, 250, OR 500 MG EACH.|ERYTHROMYCIN STEARATE: ...STEARIC ACID SALT OF ERYTHROMYCIN, WITH EXCESS OF STEARIC ACID. IT CONTAINS NOT LESS THAN 55% OF ERYTHROMYCIN.

TLC ANALYSIS OF MACROLIDE ANTIBIOTICS. FOR THE SEPARATION OF ERYTHROMYCIN ESTERS, CHLOROFORM-ETHANOL-15% AMMONIUM ACETATE PH 7.0 (OR 3.5% AMMONIA) (85:15:1) GAVE BEST RESULTS.|FLUOROPHOTOMETRIC DETERMINATION OF ERYTHROMYCIN & ITS DERIVATIVES BY ION PAIR EXTRACTION WITH TETRABROMOSULFONEFLUORESCEIN.|MICROBIOLOGICAL METHOD FOR ESTIMATING ERYTHROMYCIN & ITS DERIV WAS VALIDATED. THERE WAS A GRADUAL DECREASE IN ANTIMICROBIAL ACTIVITY AS INCUBATION TEMP INCREASED. THE DATA OBEYED ARRHENIUS EQUATION REQUIREMENTS, ASSURING THE VALIDITY OF THE METHOD.|DIFFERENTIAL PULSE POLAROGRAPHY WAS USED IN THE DETECTION & QUANTITATION OF ANTIBIOTICS.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients