Meticillin

1.22

1.22

FINE, WHITE, CRYSTALLINE POWDER; FREELY SOL IN METHANOL, PYRIDINE; SLIGHTLY SOL IN PROPYL AND AMYL ALCOHOL, ETHYLENE CHLORIDE; INSOL IN BENZENE; ODORLESS OR HAVING SLIGHT ODOR /METHICILLIN SODIUM/

3.10e-01 g/L

SALT IS STABLE IN DRY FORM; UNSTABLE IN ACIDIC MEDIA & LOSES POTENCY DISSOLVED IN 0.85% SODIUM CHLORIDE OR IN DEXTROSE SOLN. /METHICILLIN SODIUM/

Reconstituted solutions of methicillin sodium may gradually darken to a deep orange and acquire a distinctive hydrogen sulfide odor upon standing at room temperature for several days. Following reconstitution with sterile water for injection or 0.9% sodium chloride, methicillin sodium solutions containing 500 mg/ml are stable for 24 hours at room temperature, 4 days when refrigerated at 2-8 °C, or 4 weeks when frozen at -20 °C. Longer periods of stability have been reported. In one study following reconstitution with sterile water for injection, solutions containing 500 mg/ml were stable for 71 days when frozen at -16 °C. Once thawed, stabilities of these solutions are the same as those of the unfrozen solutions. /Methicillin sodium/

Reconstituted solutions of methicillin sodium further diluted to a concentration of 2-20 mg/ml lose less than 10% of their activity at room temperature within 8 hours in the following IV solutions: 5% dextrose or 5% dextrose and 0.9% sodium chloride; 0.9% sodium chloride; 10% fructose or 10% fructose and 0.9% sodium chloride; 10% invert sugar or 0.3% potassium chloride in 10% invert sugar; 10% invert sugar with electrolytes (Travert with Electrolytes No. 1, 2, or 3); 1/6 M sodium lactate; or lactated Ringer's injection. When diluted with 10% invert sugar and 0.9% sodium chloride injection, solutions containing 2 mg/ml are stable for only 4 hours at room temperature, but solutions containing 10-30 mg/ml are stable for 8 hours at room temperature. Pharmacy bulk packages containing 10 g of methicillin sodium that have been reconstituted with sterile water for injection or O.45 or O.9% sodium chloride to a concentration of 100 mg/ml are stable for 24 hours at room temperature. /Methicillin sodium/

Warning

H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]

P264, P270, P301+P317, P330, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 40 reports by companies from 1 notifications to the ECHA C&L Inventory.；Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown. For more detailed information, please visit ECHA C&L website.

IMAP assessments - 4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 6-[(2,6-dimethoxybenzoyl)amino]-3,3-dimethyl-7-oxo-, [2S-(2.alpha.,5.alpha.,6.beta.)]-: Environment tier I assessment；IMAP assessments - 4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 6-[(2,6-dimethoxybenzoyl)amino]-3,3-dimethyl-7-oxo-, [2S-(2.alpha.,5.alpha.,6.beta.)]-: Human health tier I assessment

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

J - Antiinfectives for systemic use；J01 - Antibacterials for systemic use；J01C - Beta-lactam antibacterials, penicillins；J01CF - Beta-lactamase resistant penicillins；J01CF03 - Meticillin

QJ - Antiinfectives for systemic use；QJ01 - Antibacterials for systemic use；QJ01C - Beta-lactam antibacterials, penicillins；QJ01CF - Beta-lactamase resistant penicillins；QJ01CF03 - Meticillin

QJ - Antiinfectives for systemic use；QJ51 - Antibacterials for intramammary use；QJ51C - Beta-lactam antibacterials, penicillins, for intramammary use；QJ51CF - Beta-lactamase resistant penicillins；QJ51CF03 - Meticillin

Meticillin (INN, BAN) or methicillin (USAN) is a narrow spectrum beta-lactam antibiotic of the penicillin class. It is no longer clinically used. Its role in therapy has been largely replaced by flucloxacillin and dicloxacillin, however the term methicillin-resistant <i>Staphylococcus aureus</i> (MRSA) continues to be used to describe <i>Staphylococcus aureus</i> strains resistant to all penicillins.

Similar to other beta-lactam antimicrobials, meticillin blocks synthesis of the bacterial cell wall. Meticillin stops cross-linkage between the peptidoglycan polymer chains, which make up a large portion of gram-positive bacterial cell walls. It does this by binding to and competitively inhibiting the transpeptidase enzyme used by bacteria to cross-link the peptide (D-alanyl-alanine) used in peptidogylcan synthesis.

The penicillins and their metabolites are potent immunogens because of their ability to combine with proteins and act as haptens for acute antibody-mediated reactions. The most frequent (about 95 percent) or "major" determinant of penicillin allergy is the penicilloyl determinant produced by opening the beta-lactam ring of the penicillin. This allows linkage of the penicillin to protein at the amide group. "Minor" determinants (less frequent) are the other metabolites formed, including native penicillin and penicilloic acids. /Penicillins/

Bactericidal; inhibit bacterial cell wall synthesis. Action is dependent on the ability of penicillins to reach and bind penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Penicillin-binding proteins (which include transpeptidases, carboxypeptidases, and endopeptidases) are enzymes that are involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Penicillins bind to, and inactivate, penicillin-binding proteins, resulting in the weakening of the bacterial cell wall and lysis. /Penicillins/