Gentamycin Sulfate

Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC50 of 0.57 mM.

Signaling Pathways >> Anti-infection >> Bacterial

Research Areas >> Infection

IC50: 0.57 mM (DNase I)[1]

Gentamicin is a more effective in vitro bacterial inhibitor than combined penicillin-streptomycin, is nontoxic to tissue culture monolayers, and does not inhibit virus replication. It has been used with success as an additive in commercial mycology media to inhibit growth of bacteria and has been shown to be bactericidal for a wider range of organisms (Pseudomonas aeruginosa, Proteus sp., and Streptococcus faecalis) than penicillin and streptomycin. It does not interfere with the production of cytopathic effect by certain echoviruses and polioviruses in tissue culture, is nontoxic to Rhesus monkey kidney, HeLa, and human amnion cells, and is stable at autoclave temperatures[2]. Gentamicin is produced by various species of the genus Micromonospora. Commercial gentamicin consists mainly of different gentamicin C components. Yoshizawa elucidates the 3D-structure of gentamicin C1a bound to an A-site RNA. Gentamicin C1a binds in the major groove of the A-site of the RNA[3].

Gentamicin is currently the first choice aminoglycoside for the treatment of serious infections with alternatives being amikacin, netilmicin, and tobramycin. Gentamicin preparations are commercially available in three forms, namely otic, ophthalmic, and topical based on the respective function to treat infections of ear canal, eye, and skin. Oral and injectable forms of gentamicin are found to exhibit effective antibacterial activity against Yersinia pestis as demonstrated in a mouse infection model[3].Treatment with up to nine doses of methicillin or gentamicin shows a significant reduction of bacteria on the foreign body[4].

Mice: Bacterial challenged mice are treated with methicillin, gentamicin, both methicillin and gentamicin, or no antibiotics. The treatment is given three times a day for up to 3 days. Each dose of methicillin is 75 mg per mouse (3 g/kg of body weight), and the gentamicin dose is 0.75 mg per mouse (0.03 g/kg). The antibiotics are given subcutaneously in 0.1 or 0.5 mL of saline. Mice are sacrificed and serum and aspirate samples are collected[4].

[1]. Xu W, et al. A rapid and sensitive method for kinetic study and activity assay of DNase I in vitro based on a GO-quenched hairpin probe. Anal Bioanal Chem. 2016 May;408(14):3801-9.

[2]. Rudin A, et al. Antibacterial activity of gentamicin sulfate in tissue culture. Appl Microbiol. 1970 Dec;20(6):989-90.

[3]. Kumar CG, et al. Microbial biosynthesis and applications of gentamicin: a critical appraisal.

[4]. Espersen F, et al. Effect of treatment with methicillin and gentamicin in a new experimental mouse model of foreignbody infection. Antimicrob Agents Chemother. 1994 Sep;38(9):2047-53.

Puromycin 2HCl | Geneticin | Tunicamycin | Hygromycin B | Salinomycin | Avibactam sodium | Neomycin sulfate | Vaborbactam | Methicillin SodiuM | Rifampicin | Metronidazole | Carbenicillin disodium | Ceftazidime | Eravacycline dihydrochloride | cefotaxime sodium

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Human - woman

DOSE/DURATION :

45 mg/kg/1W-I

TOXIC EFFECTS :

Nutritional and Gross Metabolic - changes in metals, not otherwise specified

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Human - man

DOSE/DURATION :

21 mg/kg/6D-I

TOXIC EFFECTS :

Nutritional and Gross Metabolic - changes in metals, not otherwise specified

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

>5 gm/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity) Skin and Appendages - hair

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

630 mg/kg

TOXIC EFFECTS :

Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - other changes

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

873 mg(base)/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

96 mg/kg

TOXIC EFFECTS :

Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intramuscular

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

384 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

>11269 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

245 mg/kg

TOXIC EFFECTS :

Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

478 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

47 mg/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intramuscular

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

250 mg/kg

TOXIC EFFECTS :

Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intracerebral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

17300 ug/kg

TOXIC EFFECTS :

Peripheral Nerve and Sensation - sensory change involving peripheral nerve Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - guinea pig

DOSE/DURATION :

600 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

200 mg/kg/5D-I

TOXIC EFFECTS :

Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - changes in calcium Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other Enzymes

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

280 mg(base)/kg/7D-I

TOXIC EFFECTS :

Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - changes in calcium Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - dehydrogenases

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intramuscular

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

240 mg/kg/6D-I

TOXIC EFFECTS :

Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Nutritional and Gross Metabolic - weight loss or decreased weight gain Nutritional and Gross Metabolic - changes in metals, not otherwise specified

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intramuscular

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

3840 mg/kg/4W-I

TOXIC EFFECTS :

Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Related to Chronic Data - death

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intramuscular

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

2 gm/kg/50D-I

TOXIC EFFECTS :

Behavioral - ataxia Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - cat

DOSE/DURATION :

1400 mg/kg/70D-I

TOXIC EFFECTS :

Behavioral - altered sleep time (including change in righting reflex) Behavioral - ataxia Related to Chronic Data - death

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - cat

DOSE/DURATION :

1365 mg/kg/91D-I

TOXIC EFFECTS :

Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - death

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - cat

DOSE/DURATION :

4200 mg/kg/30W-I

TOXIC EFFECTS :

Sense Organs and Special Senses (Ear) - changes in cochlear structure or function Behavioral - altered sleep time (including change in righting reflex) Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - cat

DOSE/DURATION :

2700 mg/kg/27D-I

TOXIC EFFECTS :

Behavioral - ataxia Related to Chronic Data - death

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - guinea pig

DOSE/DURATION :

6557 mg/kg/77D-I

TOXIC EFFECTS :

Sense Organs and Special Senses (Ear) - change in acuity Sense Organs and Special Senses (Ear) - changes in cochlear structure or function Behavioral - muscle contraction or spasticity

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

660 mg/kg

SEX/DURATION :

female 10-15 day(s) after conception

TOXIC EFFECTS :

Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Specific Developmental Abnormalities - urogenital system

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

660 mg/kg

SEX/DURATION :

female 15-20 day(s) after conception

TOXIC EFFECTS :

Reproductive - Effects on Newborn - biochemical and metabolic

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intraperitoneal

DOSE :

375 mg/kg

SEX/DURATION :

female 14-18 day(s) after conception

TOXIC EFFECTS :

Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

TYPE OF TEST :

DNA damage

MUTATION DATA

TEST SYSTEM :

Rodent - rat

DOSE/DURATION :

9600 ug/kg/8D

REFERENCE :

JOURAA Journal of Urology. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1917- Volume(issue)/page/year: 112,348,1974 *** REVIEWS *** TOXICOLOGY REVIEW PMMDAE Panminerva Medica. (Edizioni Minerva Medica, Casella Postale 491, Turin, Italy) V.1- 1959- Volume(issue)/page/year: 16,9,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3126 No. of Facilities: 2125 (estimated) No. of Industries: 7 No. of Occupations: 22 No. of Employees: 46715 (estimated) No. of Female Employees: 34072 (estimated)