Drug

D1411 | Gentamicin

Molecular Formula C21H43N5O7
Molecular Weight 477.6
Structure
State solid
Protein binding Low (between 0 and 30%)
Half life 3-3½ hours in infants one week to six months of age; this increases to 5½ hours in full-term and large premature infants less than one week old.
Absorption Injections lead to peak serum concentrations in 30-60 minutes. Topical gentamicin is readily absorbed from large burned, denuded, or granulating areas but not through intact skin. Absorption of gentamicin is faster and greater with the cream compared to the ointment. Gentamicin is absorbed in small quantities following topical application to the eye. Gentamicin is also absorbed in small amounts following topical application to the ear (especially if the eardrum is perforated or if tissue damage is present). Gentamicin is very poorly absorbed orally.
Trade names Cidomycin, Genticyn, Garamycin
Description a complex of three different closely related aminoglycoside sulfates; broad-spectrum antibiotics

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D

S03AA06 Gentamicin


[S03AA] Antiinfectives


[S03A] ANTIINFECTIVES


[S03] OPHTHALMOLOGICAL AND OTOLOGICAL PREPARATIONS


[S] Sensory organs


S02AA14 Gentamicin


[S02AA] Antiinfectives


[S02A] ANTIINFECTIVES


[S02] OTOLOGICALS


[S] Sensory organs


S01AA11 Gentamicin


[S01AA] Antibiotics


[S01A] ANTIINFECTIVES


[S01] OPHTHALMOLOGICALS


[S] Sensory organs


J01GB03 Gentamicin


[J01GB] Other aminoglycosides


[J01G] AMINOGLYCOSIDE ANTIBACTERIALS


[J01] ANTIBACTERIALS FOR SYSTEMIC USE


[J] Antiinfectives for systemic use


D06AX07 Gentamicin


[D06AX] Other antibiotics for topical use


[D06A] ANTIBIOTICS FOR TOPICAL USE


[D06] ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE


[D] Dermatological drugs


Toxicity Dose Time Species Model Method Action Positive criterion Reference
TRANSMEMBRANE POTENTIAL 2.5 mM rat isolated rat liver (and kidney) mitochondria MtMP was investigated with the use of safranin, a biological stain with an excitation wavelength of 495 nm and an emission wavelength of 587 nm. reduce 316
TRANSMEMBRANE POTENTIAL mouse Mouse Cochlear Culture Sensory Hair Cells Rhodamine-123 reduce 316
REDOX CYCLING 278
STATE 2 RESPIRATION 5mM 10min rat isolated rat liver (and kidney) mitochondria Oroboros O2K Oxygraph, complex II-based state 4 respiration increase 316
STATE 2 RESPIRATION 5mM 10min rat isolated rat liver mitochondria Oroboros O2K Oxygraph, complex I-based state 4 respiration increase 316
STATE 3U RESPIRATION 5mM 10min rat isolated rat liver (and kidney) mitochondria Oroboros O2K Oxygraph, complex II-based state 3u respiration decrease 316
STATE 3U RESPIRATION 5mM 10min rat isolated rat liver mitochondria Oroboros O2K Oxygraph, complex I-based state 3u respiration decrease 316
RESPIRATORY CONTROL RATIO (RCR) 5mM 10min rat isolated rat liver (and kidney) mitochondria Oroboros O2K Oxygraph reduce 316
NADH LEVEL 300 μg/ml 1hr postnatal day 6 (P6±1d) FVB mice apical turn outer hair cells ( low-frequency processing OHCs) from intact cochlear (organ of Corti) explants scanning confocal microscope (NADH autofluorescence); T1 imaging buffer contained 5 mM glucose. T2 imaging buffer contained 10 mM glucose, 3 mM glutamate and 2 mM pyruvate. Negative 312
NADH LEVEL 300 μg/ml 1hr postnatal day 6 (P6±1d) FVB mice apical turn inner hair cells ( low-frequency processing IHCs) from intact cochlear (organ of Corti) explants scanning confocal microscope (NADH autofluorescence); T1 imaging buffer contained 5 mM glucose. T2 imaging buffer contained 10 mM glucose, 3 mM glutamate and 2 mM pyruvate. Negative 312
NADH LEVEL 300 μg/ml 1hr postnatal day 6 (P6±1d) FVB mice basal turn outer hair cells ( low-frequency processing OHCs) from intact cochlear (organ of Corti) explants scanning confocal microscope (NADH autofluorescence); T1 imaging buffer contained 5 mM glucose. T2 imaging buffer contained 10 mM glucose, 3 mM glutamate and 2 mM pyruvate. decrease 312
NADH LEVEL 300 μg/ml 1hr postnatal day 6 (P6±1d) FVB mice basal turn inner hair cells ( high-frequency processing IHCs) from intact cochlear (organ of Corti) explants scanning confocal microscope (autofluorescence); T1 imaging buffer contained 5 mM glucose. T2 imaging buffer contained 10 mM glucose, 3 mM glutamate and 2 mM pyruvate. Negative 312
H2O2 PRODUCTION 5mM 10min rat isolated rat liver (and kidney) mitochondria Mitochondrial ROS production can be measured using Amplex Red, a dye that fluoresces dependent on hydrogen peroxide (H2O2) levels. reduce 316

Target Dose Time Species Model Method Action Positive criterion Reference
Succinate dehydrogenase 300 μg/ml 1hr postnatal day 6 (P6±1d) FVB mice apical turn ( low-frequency processing) outer hair cells (OHCs) from intact cochlear (organ of Corti) explants Succinate dehydrogenase (SDH) histochemistry (tetranitro-blue accumulation) inhibit 312
Succinate dehydrogenase 300 μg/ml 1hr postnatal day 6 (P6±1d) FVB mice apical turn ( low-frequency processing) outer hair cells (OHCs) from intact cochlear (organ of Corti) explants Succinate dehydrogenase (SDH) histochemistry (tetranitro-blue accumulation) Negative 312
Succinate dehydrogenase 300 μg/ml 1hr postnatal day 6 (P6±1d) FVB mice basal turn(high-frequency regions of the cochlea) outer hair cells from intact cochlear (organ of Corti) explants Succinate dehydrogenase (SDH) histochemistry (tetranitro-blue accumulation) inhibit 312
Succinate dehydrogenase 300 μg/ml 1hr postnatal day 6 (P6±1d) FVB mice basal turn(high-frequency regions of the cochlea) outer hair cells from intact cochlear (organ of Corti) explants Succinate dehydrogenase (SDH) histochemistry (tetranitro-blue accumulation) Negative 312
Succinate dehydrogenase 17 mM rat isolated rat liver mitochondria Complex II activity was determined by following the reduction of DCPIP at 600 nm in the presence of 2 μM Antimycin A and 50 μM ubiquinone-2 inhibit IC50 316
coenzyme Q10 1.94 mM rat isolated rat liver mitochondria The activity of complex III was measured by following the rate of reduction of cytochrome C at 550 nm using 50 μM ubiquinol 2 in the presence of 1 mM cyanide (KCN) to prevent electron transfer to complex IV. inhibit IC50 316

Pictogram Signal Statements Precautionary Statement Codes
Danger

Aggregated GHS information provided by 84 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


H317 (55.95%): May cause an allergic skin reaction [Warning Sensitization, Skin]


H334 (55.95%): May cause allergy or asthma symptoms or breathing difficulties if inhaled [Danger Sensitization, respiratory]


H360 (44.05%): May damage fertility or the unborn child [Danger Reproductive toxicity]


H372 (44.05%): Causes damage to organs through prolonged or repeated exposure [Danger Specific target organ toxicity, repeated exposure]


H400 (44.05%): Very toxic to aquatic life [Warning Hazardous to the aquatic environment, acute hazard]


H410 (44.05%): Very toxic to aquatic life with long lasting effects [Warning Hazardous to the aquatic environment, long-term hazard]


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.


P201, P202, P260, P261, P264, P270, P272, P273, P280, P281, P285, P302+P352, P304+P341, P308+P313, P314, P321, P333+P313, P342+P311, P363, P391, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Organism Test type Route Dose (normalized dose) Effect Source
mouse LD50 intravenous 88mg/kg (88mg/kg) Journal of Antibiotics. Vol. 27, Pg. 677, 1974.


  • DrugBank DB00798
    CAS Number 1403-66-3, 1405-41-0, 25876-10-2, 26689-70-3
    PubChem Compound 3467