STREPTOMYCIN

First approved in 1946

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H39N7O12
Molecular Weight	581.5741
Optical Activity	UNSPECIFIED
Defined Stereocenters	15 / 15
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@]2(O[C@@H]1O[C@@H](CO)[C@H](O)[C@@H](O)[C@@H]1NC)[C@H](O[C@@]3([H])[C@H](O)[C@@H](O)[C@H](NC(N)=N)[C@@H](O)[C@@H]3NC(N)=N)O[C@@H](C)[C@]2(O)C=O

InChI

InChIKey=UCSJYZPVAKXKNQ-HZYVHMACSA-N

InChI=1S/C21H39N7O12/c1-5-21(36,4-30)16(40-17-9(26-2)13(34)10(31)6(3-29)38-17)18(37-5)39-15-8(28-20(24)25)11(32)7(27-19(22)23)12(33)14(15)35/h4-18,26,29,31-36H,3H2,1-2H3,(H4,22,23,27)(H4,24,25,28)/t5-,6-,7+,8-,9-,10-,11+,12-,13-,14+,15+,16-,17-,18-,21+/m0/s1

HIDE SMILES / InChI

Molecular Formula	C21H39N7O12
Molecular Weight	581.5741
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	15 / 15
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.drugbank.ca/drugs/DB01082
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/064210s009lbl.pdf

Streptomycin is a water-soluble aminoglycoside derived from Streptomyces griseus. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses. Aminoglycosides like Streptomycin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically Streptomycin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes. Streptomycin is indicated for the treatment of tuberculosis. May also be used in combination with other drugs to treat tularemia (Francisella tularensis), plague (Yersia pestis), severe M. avium complex, brucellosis, and enterococcal endocarditis (e.g. E. faecalis, E. faecium).

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Ribosome 11 Target ID: map03010 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17967466 \| http://www.genome.jp/dbget-bin/www_bget?dr:D01350	Inhibitor 8297
Mycobacterium tuberculosis 21 Target ID: CHEMBL360 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27135906	Inhibitor 8297	5.36 µM [IC50]
Francisella tularensis subsp. tularensis SCHU S4 5 Target ID: CHEMBL612748 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23065699	Inhibitor 8297

Conditions

Condition	Modality	Highest Phase	Product
Tuberculosis 83 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/064210s009lbl.pdf	Curative	Approved 8429	STREPTOMYCIN SULFATE Approved Use Streptomycin is indicated for the treatment of individuals with moderate to severe infections caused by susceptibile strains of microorganisms in the specific conditions listed below: Mycobacterium tuberculosis: The Advisory Council for the Elimination of Tuberculosis, the American Thoracic Society, and the Center for Disease Control recommend that either streptomycin or ethambutol be added as a fourth drug in a regimen containing isoniazid (INH), rifampin and pyrazinamide for initial treatment of tuberculosis unless the likelihood of INH or rifampin resistance is very low. The need for a fourth drug should be reassessed when the results of susceptibility testing are known. In the past when the national rate of primary drug resistance to isoniazid was known to be less than 4% and was either stable or declining, therapy with two and three drug regimens was considered adequate. If community rates of INH resistance are currently less than 4%, an initial treatment regimen with less than four drugs may be considered. Streptomycin is also indicated for therapy of tuberculosis when one or more of the above drugs is contraindicated because of toxicity or intolerance. The management of tuberculosis has become more complex as a consequence of increasing rates of drug resistance and concomitant HIV infection. Additional consultation from experts in the treatment of tuberculosis may be desirable in those settings. Non-tuberculosis infections: The use of streptomycin should be limited to the treatment of infections caused by bacteria which have been shown to be susceptible to the antibacterial effects of streptomycin and which are not amenable to therapy with less potentially toxic agents. Pasteurella pestis (plague), Francisella tularensis (tularemia), Brucella, Calymmatobacterium granulomatis (donovanosis, granuloma inguinale), H. ducreyi (chancroid), H. influenzae (in respiratory, endocardial, and meningeal infections-concomitantly with another antibacterial agent), K. pneumoniae pneumonia (concomitantly with another antibacterial agent), E.coli, Proteus, A. aerogenes, K. pneumoniae, and Enterococcus faecalis in urinary tract infections, Streptococcus viridans, Enterococcus faecalis (in endocardial infections -concomitantly with penicillin), Gram-negative bacillary bacteremia (concomitantly with another antibacterial agent). To reduce the development of drug-resistant bacteria and maintain the effectiveness of streptomycin and other antibacterial drugs, streptomycin should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. Launch Date 1946
Plague 14 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/064210s009lbl.pdf	Curative	Approved 8429	STREPTOMYCIN SULFATE Approved Use Streptomycin is indicated for the treatment of individuals with moderate to severe infections caused by susceptibile strains of microorganisms in the specific conditions listed below: Mycobacterium tuberculosis: The Advisory Council for the Elimination of Tuberculosis, the American Thoracic Society, and the Center for Disease Control recommend that either streptomycin or ethambutol be added as a fourth drug in a regimen containing isoniazid (INH), rifampin and pyrazinamide for initial treatment of tuberculosis unless the likelihood of INH or rifampin resistance is very low. The need for a fourth drug should be reassessed when the results of susceptibility testing are known. In the past when the national rate of primary drug resistance to isoniazid was known to be less than 4% and was either stable or declining, therapy with two and three drug regimens was considered adequate. If community rates of INH resistance are currently less than 4%, an initial treatment regimen with less than four drugs may be considered. Streptomycin is also indicated for therapy of tuberculosis when one or more of the above drugs is contraindicated because of toxicity or intolerance. The management of tuberculosis has become more complex as a consequence of increasing rates of drug resistance and concomitant HIV infection. Additional consultation from experts in the treatment of tuberculosis may be desirable in those settings. Non-tuberculosis infections: The use of streptomycin should be limited to the treatment of infections caused by bacteria which have been shown to be susceptible to the antibacterial effects of streptomycin and which are not amenable to therapy with less potentially toxic agents. Pasteurella pestis (plague), Francisella tularensis (tularemia), Brucella, Calymmatobacterium granulomatis (donovanosis, granuloma inguinale), H. ducreyi (chancroid), H. influenzae (in respiratory, endocardial, and meningeal infections-concomitantly with another antibacterial agent), K. pneumoniae pneumonia (concomitantly with another antibacterial agent), E.coli, Proteus, A. aerogenes, K. pneumoniae, and Enterococcus faecalis in urinary tract infections, Streptococcus viridans, Enterococcus faecalis (in endocardial infections -concomitantly with penicillin), Gram-negative bacillary bacteremia (concomitantly with another antibacterial agent). To reduce the development of drug-resistant bacteria and maintain the effectiveness of streptomycin and other antibacterial drugs, streptomycin should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. Launch Date 1946
Tularemia 5 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/064210s009lbl.pdf	Curative	Approved 8429	STREPTOMYCIN SULFATE Approved Use Streptomycin is indicated for the treatment of individuals with moderate to severe infections caused by susceptibile strains of microorganisms in the specific conditions listed below: Mycobacterium tuberculosis: The Advisory Council for the Elimination of Tuberculosis, the American Thoracic Society, and the Center for Disease Control recommend that either streptomycin or ethambutol be added as a fourth drug in a regimen containing isoniazid (INH), rifampin and pyrazinamide for initial treatment of tuberculosis unless the likelihood of INH or rifampin resistance is very low. The need for a fourth drug should be reassessed when the results of susceptibility testing are known. In the past when the national rate of primary drug resistance to isoniazid was known to be less than 4% and was either stable or declining, therapy with two and three drug regimens was considered adequate. If community rates of INH resistance are currently less than 4%, an initial treatment regimen with less than four drugs may be considered. Streptomycin is also indicated for therapy of tuberculosis when one or more of the above drugs is contraindicated because of toxicity or intolerance. The management of tuberculosis has become more complex as a consequence of increasing rates of drug resistance and concomitant HIV infection. Additional consultation from experts in the treatment of tuberculosis may be desirable in those settings. Non-tuberculosis infections: The use of streptomycin should be limited to the treatment of infections caused by bacteria which have been shown to be susceptible to the antibacterial effects of streptomycin and which are not amenable to therapy with less potentially toxic agents. Pasteurella pestis (plague), Francisella tularensis (tularemia), Brucella, Calymmatobacterium granulomatis (donovanosis, granuloma inguinale), H. ducreyi (chancroid), H. influenzae (in respiratory, endocardial, and meningeal infections-concomitantly with another antibacterial agent), K. pneumoniae pneumonia (concomitantly with another antibacterial agent), E.coli, Proteus, A. aerogenes, K. pneumoniae, and Enterococcus faecalis in urinary tract infections, Streptococcus viridans, Enterococcus faecalis (in endocardial infections -concomitantly with penicillin), Gram-negative bacillary bacteremia (concomitantly with another antibacterial agent). To reduce the development of drug-resistant bacteria and maintain the effectiveness of streptomycin and other antibacterial drugs, streptomycin should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. Launch Date 1946
Chancroid 5 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/064210s009lbl.pdf	Curative	Approved 8429	STREPTOMYCIN SULFATE Approved Use Streptomycin is indicated for the treatment of individuals with moderate to severe infections caused by susceptibile strains of microorganisms in the specific conditions listed below: Mycobacterium tuberculosis: The Advisory Council for the Elimination of Tuberculosis, the American Thoracic Society, and the Center for Disease Control recommend that either streptomycin or ethambutol be added as a fourth drug in a regimen containing isoniazid (INH), rifampin and pyrazinamide for initial treatment of tuberculosis unless the likelihood of INH or rifampin resistance is very low. The need for a fourth drug should be reassessed when the results of susceptibility testing are known. In the past when the national rate of primary drug resistance to isoniazid was known to be less than 4% and was either stable or declining, therapy with two and three drug regimens was considered adequate. If community rates of INH resistance are currently less than 4%, an initial treatment regimen with less than four drugs may be considered. Streptomycin is also indicated for therapy of tuberculosis when one or more of the above drugs is contraindicated because of toxicity or intolerance. The management of tuberculosis has become more complex as a consequence of increasing rates of drug resistance and concomitant HIV infection. Additional consultation from experts in the treatment of tuberculosis may be desirable in those settings. Non-tuberculosis infections: The use of streptomycin should be limited to the treatment of infections caused by bacteria which have been shown to be susceptible to the antibacterial effects of streptomycin and which are not amenable to therapy with less potentially toxic agents. Pasteurella pestis (plague), Francisella tularensis (tularemia), Brucella, Calymmatobacterium granulomatis (donovanosis, granuloma inguinale), H. ducreyi (chancroid), H. influenzae (in respiratory, endocardial, and meningeal infections-concomitantly with another antibacterial agent), K. pneumoniae pneumonia (concomitantly with another antibacterial agent), E.coli, Proteus, A. aerogenes, K. pneumoniae, and Enterococcus faecalis in urinary tract infections, Streptococcus viridans, Enterococcus faecalis (in endocardial infections -concomitantly with penicillin), Gram-negative bacillary bacteremia (concomitantly with another antibacterial agent). To reduce the development of drug-resistant bacteria and maintain the effectiveness of streptomycin and other antibacterial drugs, streptomycin should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. Launch Date 1946

C_max

Value	Dose	Co-administered	Analyte	Population
42.6 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11560193/	18 mg/kg single, intramuscular dose: 18 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered:		STREPTOMYCIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
264 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11560193/	18 mg/kg single, intramuscular dose: 18 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered:		STREPTOMYCIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
2.67 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11560193/	18 mg/kg single, intramuscular dose: 18 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered:		STREPTOMYCIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
1 g 1 times / day multiple, intramuscular Recommended Dose: 1 g, 1 times / day Route: intramuscular Route: multiple Dose: 1 g, 1 times / day Co-administed with:: Doxycycline(100 mg oral; 2/day) Sources: https://pubmed.ncbi.nlm.nih.gov/8540716 Page: p.2066	unhealthy, 12–70 n = 94 Health Status: unhealthy Condition: Brucellosis Age Group: 12–70 Sex: M+F Population Size: 94 Sources: https://pubmed.ncbi.nlm.nih.gov/8540716 Page: p.2066	Disc. AE: Heartburn, Fatigue... AEs leading to discontinuation/dose reduction: Heartburn (1.06%) Fatigue (1.06%) Sources: https://pubmed.ncbi.nlm.nih.gov/8540716 Page: p.2066
1 g 1 times / day steady, intravenous Recommended Dose: 1 g, 1 times / day Route: intravenous Route: steady Dose: 1 g, 1 times / day Co-administed with:: lsoniazid(300 mg iv; 1/day) rifampicin(600 mg iv; 1/day) pyrazinamide(2 g iv; 1/day) Sources: https://pubmed.ncbi.nlm.nih.gov/6989067 Page: p.47	unhealthy, 15-70 n = 119 Health Status: unhealthy Condition: Pulmonary tuberculosis Age Group: 15-70 Sex: M+F Population Size: 119 Sources: https://pubmed.ncbi.nlm.nih.gov/6989067 Page: p.47	Disc. AE: Hypersensitivity, Disorder vestibular... AEs leading to discontinuation/dose reduction: Hypersensitivity (1.7%) Disorder vestibular (0.84%) Sources: https://pubmed.ncbi.nlm.nih.gov/6989067 Page: p.47
1225 mg 3 times / week steady, intravenous Recommended Dose: 1225 mg, 3 times / week Route: intravenous Route: steady Dose: 1225 mg, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 25–76 n = 13 Health Status: unhealthy Condition: Mycobacterium avium complex Age Group: 25–76 Sex: M+F Population Size: 13 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	Other AEs: Ototoxicity, Nephrotoxicity... Other AEs: Ototoxicity Nephrotoxicity Vestibular toxicity Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
1225 mg 3 times / week steady, intravenous Recommended Dose: 1225 mg, 3 times / week Route: intravenous Route: steady Dose: 1225 mg, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 25–76 n = 3 Health Status: unhealthy Condition: Mycobacterium tuberculosis Age Group: 25–76 Sex: M+F Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	Other AEs: Ototoxicity, Nephrotoxicity... Other AEs: Ototoxicity Nephrotoxicity Vestibular toxicity Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
800 mg 1 times / day steady, intravenous Recommended Dose: 800 mg, 1 times / day Route: intravenous Route: steady Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 26–73 n = 10 Health Status: unhealthy Condition: Mycobacterium avium complex Age Group: 26–73 Sex: M+F Population Size: 10 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	Other AEs: Ototoxicity, Nephrotoxicity... Other AEs: Ototoxicity Nephrotoxicity Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
800 mg 1 times / day steady, intravenous Recommended Dose: 800 mg, 1 times / day Route: intravenous Route: steady Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 26–73 n = 6 Health Status: unhealthy Condition: Mycobacterium tuberculosis Age Group: 26–73 Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	Other AEs: Ototoxicity, Nephrotoxicity... Other AEs: Ototoxicity Nephrotoxicity Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539

AEs

AE	Significance	Dose	Population
Fatigue	1.06% Disc. AE	1 g 1 times / day multiple, intramuscular Recommended Dose: 1 g, 1 times / day Route: intramuscular Route: multiple Dose: 1 g, 1 times / day Co-administed with:: Doxycycline(100 mg oral; 2/day) Sources: https://pubmed.ncbi.nlm.nih.gov/8540716 Page: p.2066	unhealthy, 12–70 n = 94 Health Status: unhealthy Condition: Brucellosis Age Group: 12–70 Sex: M+F Population Size: 94 Sources: https://pubmed.ncbi.nlm.nih.gov/8540716 Page: p.2066
Heartburn	1.06% Disc. AE	1 g 1 times / day multiple, intramuscular Recommended Dose: 1 g, 1 times / day Route: intramuscular Route: multiple Dose: 1 g, 1 times / day Co-administed with:: Doxycycline(100 mg oral; 2/day) Sources: https://pubmed.ncbi.nlm.nih.gov/8540716 Page: p.2066	unhealthy, 12–70 n = 94 Health Status: unhealthy Condition: Brucellosis Age Group: 12–70 Sex: M+F Population Size: 94 Sources: https://pubmed.ncbi.nlm.nih.gov/8540716 Page: p.2066
Disorder vestibular	0.84% Disc. AE	1 g 1 times / day steady, intravenous Recommended Dose: 1 g, 1 times / day Route: intravenous Route: steady Dose: 1 g, 1 times / day Co-administed with:: lsoniazid(300 mg iv; 1/day) rifampicin(600 mg iv; 1/day) pyrazinamide(2 g iv; 1/day) Sources: https://pubmed.ncbi.nlm.nih.gov/6989067 Page: p.47	unhealthy, 15-70 n = 119 Health Status: unhealthy Condition: Pulmonary tuberculosis Age Group: 15-70 Sex: M+F Population Size: 119 Sources: https://pubmed.ncbi.nlm.nih.gov/6989067 Page: p.47
Hypersensitivity	1.7% Disc. AE	1 g 1 times / day steady, intravenous Recommended Dose: 1 g, 1 times / day Route: intravenous Route: steady Dose: 1 g, 1 times / day Co-administed with:: lsoniazid(300 mg iv; 1/day) rifampicin(600 mg iv; 1/day) pyrazinamide(2 g iv; 1/day) Sources: https://pubmed.ncbi.nlm.nih.gov/6989067 Page: p.47	unhealthy, 15-70 n = 119 Health Status: unhealthy Condition: Pulmonary tuberculosis Age Group: 15-70 Sex: M+F Population Size: 119 Sources: https://pubmed.ncbi.nlm.nih.gov/6989067 Page: p.47
Nephrotoxicity		1225 mg 3 times / week steady, intravenous Recommended Dose: 1225 mg, 3 times / week Route: intravenous Route: steady Dose: 1225 mg, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 25–76 n = 13 Health Status: unhealthy Condition: Mycobacterium avium complex Age Group: 25–76 Sex: M+F Population Size: 13 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
Ototoxicity		1225 mg 3 times / week steady, intravenous Recommended Dose: 1225 mg, 3 times / week Route: intravenous Route: steady Dose: 1225 mg, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 25–76 n = 13 Health Status: unhealthy Condition: Mycobacterium avium complex Age Group: 25–76 Sex: M+F Population Size: 13 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
Vestibular toxicity		1225 mg 3 times / week steady, intravenous Recommended Dose: 1225 mg, 3 times / week Route: intravenous Route: steady Dose: 1225 mg, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 25–76 n = 13 Health Status: unhealthy Condition: Mycobacterium avium complex Age Group: 25–76 Sex: M+F Population Size: 13 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
Nephrotoxicity		1225 mg 3 times / week steady, intravenous Recommended Dose: 1225 mg, 3 times / week Route: intravenous Route: steady Dose: 1225 mg, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 25–76 n = 3 Health Status: unhealthy Condition: Mycobacterium tuberculosis Age Group: 25–76 Sex: M+F Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
Ototoxicity		1225 mg 3 times / week steady, intravenous Recommended Dose: 1225 mg, 3 times / week Route: intravenous Route: steady Dose: 1225 mg, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 25–76 n = 3 Health Status: unhealthy Condition: Mycobacterium tuberculosis Age Group: 25–76 Sex: M+F Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
Vestibular toxicity		1225 mg 3 times / week steady, intravenous Recommended Dose: 1225 mg, 3 times / week Route: intravenous Route: steady Dose: 1225 mg, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 25–76 n = 3 Health Status: unhealthy Condition: Mycobacterium tuberculosis Age Group: 25–76 Sex: M+F Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
Nephrotoxicity		800 mg 1 times / day steady, intravenous Recommended Dose: 800 mg, 1 times / day Route: intravenous Route: steady Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 26–73 n = 10 Health Status: unhealthy Condition: Mycobacterium avium complex Age Group: 26–73 Sex: M+F Population Size: 10 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
Ototoxicity		800 mg 1 times / day steady, intravenous Recommended Dose: 800 mg, 1 times / day Route: intravenous Route: steady Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 26–73 n = 10 Health Status: unhealthy Condition: Mycobacterium avium complex Age Group: 26–73 Sex: M+F Population Size: 10 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
Nephrotoxicity		800 mg 1 times / day steady, intravenous Recommended Dose: 800 mg, 1 times / day Route: intravenous Route: steady Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 26–73 n = 6 Health Status: unhealthy Condition: Mycobacterium tuberculosis Age Group: 26–73 Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539
Ototoxicity		800 mg 1 times / day steady, intravenous Recommended Dose: 800 mg, 1 times / day Route: intravenous Route: steady Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539	unhealthy, 26–73 n = 6 Health Status: unhealthy Condition: Mycobacterium tuberculosis Age Group: 26–73 Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/15156439 Page: p.1539

Overview

CYP3A4	CYP2C9	CYP2D6	hERG

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OATP1B1 788 OATP2B1 123 OATP1B3 706

Drug as perpetrator

Target	Modality	Activity
OATP1B1 803	inhibitor 3277 Sources: https://aac.asm.org/content/aac/60/5/3096.full.pdf#page=6 Page: 6.0	not determined
OATP1B3 715	inhibitor 3277 Sources: https://aac.asm.org/content/aac/60/5/3096.full.pdf#page=6 Page: 6.0	not determined
OATP2B1 126	inhibitor 3277 Sources: https://aac.asm.org/content/aac/60/5/3096.full.pdf#page=6 Page: 6.0	yes [IC50 33.2 uM]

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:17076	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:17076
ChemicalBook	CB3462887	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB3462887
MolPort	MolPort-002-525-998	https://www.molport.com/shop/molecule-link/MolPort-002-525-998
ZINC	ZINC000008214681	http://zinc15.docking.org/substances/ZINC000008214681

PubMed

Title	Date	PubMed
A method for evaluating antitubercular activity in mice.	1949 Dec 14	15408463
The evaluation of neomycin and other antimicrobial agents of bacterial and fungal origin, and substances from higher plants.	1949 Dec 14	15398785
Chemotherapy of experimental tuberculosis. V. Isonicotinic acid hydrazide (nydrazid) and related compounds.	1952 Apr	14903503
Therapeutic efficacy of tobramycin--a clinical and laboratory evaluation.	1975 Dec	1107297
Bacteriostatic and bactericidal activity of antituberculosis drugs against Mycobacterium tuberculosis, Mycobacterium avium-Mycobacterium intracellulare complex and Mycobacterium kansasii in different growth phases.	1992	1406364
[A case of pulmonary tuberculosis associated with severe skin eruption, prominent eosinophilia, and liver dysfunction induced by streptomycin].	1992 May	1534589
New pyrrole derivatives as antimycobacterial agents analogs of BM212.	1999 Oct 18	10571160
Use of genomics and combinatorial chemistry in the development of new antimycobacterial drugs.	2000 Feb 1	10609550
Intrinsic resistance of Mycobacterium tuberculosis to clarithromycin is effectively reversed by subinhibitory concentrations of cell wall inhibitors.	2000 Sep	10980165
Connexin-mimetic peptide Gap 27 decreases osteoclastic activity.	2001	11747476
Postantibiotic effects of antituberculosis agents alone and in combination.	2001 Dec	11709357
Enhancement of antibiotic activity against poly-drug resistant Mycobacterium tuberculosis by phenothiazines.	2001 Mar	11282269
Retrospective analysis of drug-induced urticaria and angioedema: a survey of 2287 patients.	2001 Nov	11792017
Antimycobacterial plant terpenoids.	2001 Nov	11731906
Synthesis and biological evaluation of azole derivatives, analogues of bifonazole, with a phenylisoxazolyl or phenylpyrimidinyl moiety.	2001 Sep	11680806
Bactericidal activities of commonly used antiseptics against multidrug-resistant mycobacterium tuberculosis.	2002	12011515
Reversible anosmia after amikacin therapy.	2003 Dec	14676161
Fluoxetine attenuates thermal hyperalgesia through 5-HT1/2 receptors in streptozotocin-induced diabetic mice.	2004 Aug 30	15336946
Antimycobacterial agents differ with respect to their bacteriostatic versus bactericidal activities in relation to time of exposure, mycobacterial growth phase, and their use in combination.	2005 Jun	15917538
Endostatin inhibits VEGF-A induced osteoclastic bone resorption in vitro.	2006 Jul 13	16839420
Hearing impairment in patients with tuberculosis from Northeast Brazil.	2006 Mar-Apr	16699632
Activity of 7-methyljuglone in combination with antituberculous drugs against Mycobacterium tuberculosis.	2006 Nov	16987644
Time- and concentration-dependent changes in gene expression induced by benzo(a)pyrene in two human cell lines, MCF-7 and HepG2.	2006 Oct 16	17042939
Resistance of Leishmania (Leishmania) amazonensis and Leishmania (Viannia) braziliensis to nitric oxide correlates with disease severity in Tegumentary Leishmaniasis.	2007 Feb 22	17316450
Streptomycin action to the mammalian inner ear vestibular organs: comparison between pigmented guinea pigs and rats.	2007 Jul-Aug	17011831
Effect and mechanism of lipopolysaccharide on allergen-induced interleukin-5 and eotaxins production by whole blood cultures of atopic asthmatics.	2007 Mar	17302892
Regulation of glycogen synthase kinase 3beta functions by modification of the small ubiquitin-like modifier.	2008	18949077
Curcumin inhibits glyoxalase 1: a possible link to its anti-inflammatory and anti-tumor activity.	2008	18946510
Prevention of SIV rectal transmission and priming of T cell responses in macaques after local pre-exposure application of tenofovir gel.	2008 Aug 5	18684007
Genomic organization, sequence divergence, and recombination of feline immunodeficiency virus from lions in the wild.	2008 Feb 5	18251995

Patents

Sample Use Guides

In Vivo Use Guide

Intramuscular Route Only Adults: The preferred site is the upper outer quadrant of the buttock, (i.e., gluteus maximus), or themid-lateral thigh. Children: It is recommended that intramuscular injections be given preferably in the mid-lateral muscles of the thigh. In infants and small children the periphery of the upper outer quadrant of the gluteal region should be used only when necessary, such as in burn patients, in order to minimize the possibility of damage to the sciatic nerve. 1. TUBERCULOSIS: Children daily - 20-40 mg/kg Adults daily - 15 mg/kg Streptomycin is usually administered daily as a single intramuscular injection. A total dose of not more than 120 g over the course of therapy should be given unless there are no other therapeutic options. 2. TULAREMIA: One to 2 g daily in divided doses for 7 to 14 days until the patient is afebrile for 5 to 7 days. 3. PLAGUE: Two grams of Streptomycin daily in two divided doses should be administered intramuscularly. A minimum of 10 days of therapy is recommended. 4. BACTERIAL ENDOCARDITIS: a. Streptococcal endocarditis; in penicillin-sensitive alpha and non-hemolytic streptococcal endocarditis (penicillin MIC<0.1 mcg/mL), Streptomycin may be used for 2-week treatment concomitantly with penicillin. The Streptomycin regimen is 1 g b.i.d. for the first week, and 500 mg b.i.d. for the second week. If the patient is over 60 years of age, the dosage should be 500 mg b.i.d. for the entire 2- week period. b. Enterococcal endocarditis: Streptomycin in doses of 1 g b.i.d. for 2 weeks and 500 mg b.i.d. for an additional 4 weeks is given in combination with penicillin. Ototoxicity may require termination of the Streptomycin prior to completion of the 6-week course of treatment. 5. CONCOMITANT USE WITH OTHER AGENTS: For concomitant use with other agents to which the infecting organism is also sensitive: Streptomycin is considered a secondline agent for the treatment of gram-negative bacillary bactermia, meningitis, and pneumonia; brucellosis; granuloma inguinale; chancroid, and urinary tract infection. For adults: 1 to 2 grams in divided doses every six to twelve hours for moderate to severe infections. Doses should generally not exceed 2 grams per day. For children: 20 to 40 mg/kg/day (8 to 20 mg/lb/day) in divided doses every 6 to 12 hours. (Particular care should be taken to avoid excessive dosage in children).

Route of Administration: Intramuscular

In Vitro Use Guide

At 5 and 50 ug/ml, streptomycin inhibited the tubercle bacilli strongly and killed some; at the lowest tested concentration of 0.5 ug/ml, it inhibited them weakly.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:20:51 GMT 2023` Edited by `admin` on `Fri Dec 15 15:20:51 GMT 2023`
Record UNII	Y45QSO73OB
Record Status	`Validated (UNII)`
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Name

Type

Language

STREPTOMYCIN

Official Name

English

STREPTOMYCIN [VANDF]

Common Name

English

STREPTOMYCIN [MART.]

Common Name

English

STREPTOMYCIN [HSDB]

Common Name

English

streptomycin [INN]

Common Name

English

Streptomycin [WHO-DD]

Common Name

English

NSC-14083

Code

English

STREPTOMYCIN [GREEN BOOK]

Common Name

English

STREPTOMYCIN [MI]

Common Name

English

Classification Tree Code System Code

WHO-ESSENTIAL MEDICINES LIST

6.2.4