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Details

Stereochemistry ABSOLUTE
Molecular Formula C21H39N7O12.C9H17NO5
Molecular Weight 800.809
Optical Activity UNSPECIFIED
Defined Stereocenters 16 / 16
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of STREPTOMYCIN PANTOTHENATE

SMILES

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

InChI

InChIKey=YXIORFGPXSLCOT-FGZKHVCBSA-N
InChI=1S/C21H39N7O12.C9H17NO5/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;1-9(2,5-11)7(14)8(15)10-4-3-6(12)13/h4-18,26,29,31-36H,3H2,1-2H3,(H4,22,23,27)(H4,24,25,28);7,11,14H,3-5H2,1-2H3,(H,10,15)(H,12,13)/t5-,6-,7+,8-,9-,10-,11+,12-,13-,14+,15+,16-,17-,18-,21+;7-/m00/s1

HIDE SMILES / InChI

Description
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).

Originator

Curator's Comment: Selman Waksman, who was awarded the Nobel Prize for the discovery, has since generally been credited as streptomycin's sole discoverer. However, one of Waksman's graduate students, Albert Schatz, was legally recognized as streptomycin's co-discoverer.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
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
Curative
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
Curative
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
Curative
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
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
42.6 μg/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
264 μg × h/mL
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2.67 h
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

Doses

DosePopulationAdverse 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: Page: p.2066
unhealthy, 12–70
n = 94
Health Status: unhealthy
Condition: Brucellosis
Age Group: 12–70
Sex: M+F
Population Size: 94
Sources: Page: p.2066
Disc. AE: Heartburn, Fatigue...
AEs leading to
discontinuation/dose reduction:
Heartburn (1.06%)
Fatigue (1.06%)
Sources: 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: 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: Page: p.47
Disc. AE: Hypersensitivity, Disorder vestibular...
AEs leading to
discontinuation/dose reduction:
Hypersensitivity (1.7%)
Disorder vestibular (0.84%)
Sources: 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: 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: Page: p.1539
Other AEs: Ototoxicity, Nephrotoxicity...
Other AEs:
Ototoxicity
Nephrotoxicity
Vestibular toxicity
Sources: 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: 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: Page: p.1539
Other AEs: Ototoxicity, Nephrotoxicity...
Other AEs:
Ototoxicity
Nephrotoxicity
Vestibular toxicity
Sources: 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: 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: Page: p.1539
Other AEs: Ototoxicity, Nephrotoxicity...
Other AEs:
Ototoxicity
Nephrotoxicity
Sources: 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: 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: Page: p.1539
Other AEs: Ototoxicity, Nephrotoxicity...
Other AEs:
Ototoxicity
Nephrotoxicity
Sources: Page: p.1539
AEs

AEs

AESignificanceDosePopulation
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: Page: p.2066
unhealthy, 12–70
n = 94
Health Status: unhealthy
Condition: Brucellosis
Age Group: 12–70
Sex: M+F
Population Size: 94
Sources: 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: Page: p.2066
unhealthy, 12–70
n = 94
Health Status: unhealthy
Condition: Brucellosis
Age Group: 12–70
Sex: M+F
Population Size: 94
Sources: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: Page: p.1539
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer



Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
not determined
not determined
yes [IC50 33.2 uM]
PubMed

PubMed

TitleDatePubMed
Chemotherapy of experimental tuberculosis. V. Isonicotinic acid hydrazide (nydrazid) and related compounds.
1952 Apr
[The pathogenesis of tuberculous infection and the prognosis in tuberculous meningitis in children after streptomycin therapy].
1952 Mar 15
[Pathological anatomical changes in tuberculous meningitis in children after streptomycin therapy].
1953 Jul
Antituberculosis agents. VI. Streptidine-oxyethyl beta-D-glucopyranoside.
1960 Apr
Therapeutic efficacy of tobramycin--a clinical and laboratory evaluation.
1975 Dec
Complete respiratory paralysis caused by a large dose of streptomycin and its treatment with calcium chloride.
1975 Feb
["Typical" and "atypical" damages of the organ of hearing from the administration of streptomycin].
1975 Jan
Ototoxicity with children caused by streptomycin.
1975 Mar-Apr
[The intratympanic treatment of Menière's disease with ototoxic antibiotics. A follow-up study of 55 cases (author's transl)].
1977 May
Bacteriostatic and bactericidal activity of antituberculosis drugs against Mycobacterium tuberculosis, Mycobacterium avium-Mycobacterium intracellulare complex and Mycobacterium kansasii in different growth phases.
1992
Chlorpromazine: a drug potentially useful for treating mycobacterial infections.
1992
Spectrum of drugs against atypical mycobacteria: how valid is the current practice of drug susceptibility testing and the choice of drugs?
1992 Dec
Capability of serum to convert streptomycin to cytotoxin in patients with aminoglycoside-induced hearing loss.
1999 Nov
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
1999 Oct 18
A new class of antituberculosis agents.
2000 Aug 24
Use of genomics and combinatorial chemistry in the development of new antimycobacterial drugs.
2000 Feb 1
Activity of poloxamer CRL-1072 against drug-sensitive and resistant strains of Mycobacterium tuberculosis in macrophages and in mice.
2000 Jun
Intrinsic resistance of Mycobacterium tuberculosis to clarithromycin is effectively reversed by subinhibitory concentrations of cell wall inhibitors.
2000 Sep
Retrospective analysis of drug-induced urticaria and angioedema: a survey of 2287 patients.
2001 Nov
Antimycobacterial plant terpenoids.
2001 Nov
Bactericidal activities of commonly used antiseptics against multidrug-resistant mycobacterium tuberculosis.
2002
Aminoglycoside-induced hearing loss in a patient with the 961 mutation in mitochondrial DNA.
2002 May-Jun
Cryptolepine hydrochloride: a potent antimycobacterial alkaloid derived from Cryptolepis sanguinolenta.
2003 Apr
Protective effect of edaravone against streptomycin-induced vestibulotoxicity in the guinea pig.
2003 Mar 7
Synthesis, antimicrobial activity and molecular modeling studies of halogenated 4-[1H-imidazol-1-yl(phenyl)methyl]-1,5-diphenyl-1H-pyrazoles.
2004 Oct 15
Neogenin expression may be inversely correlated to the tumorigenicity of human breast cancer.
2005 Dec 3
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
Differential antibiotic susceptibilities of starved Mycobacterium tuberculosis isolates.
2005 Nov
Signaling of the Human P2Y(1) Receptor Measured by a Yeast Growth Assay with Comparisons to Assays of Phospholipase C and Calcium Mobilization in 1321N1 Human Astrocytoma Cells.
2005 Sep
Fluoroquinolones: an important class of antibiotics against tuberculosis.
2006
Enhanced susceptibility of multidrug resistant strains of Mycobacterium tuberculosis to granulysin peptides correlates with a reduced fitness phenotype.
2006 Jul
Activity of 7-methyljuglone in combination with antituberculous drugs against Mycobacterium tuberculosis.
2006 Nov
Inhibition of NF-kappaB activation in vivo impairs establishment of gammaherpesvirus latency.
2007 Jan
Streptomycin action to the mammalian inner ear vestibular organs: comparison between pigmented guinea pigs and rats.
2007 Jul-Aug
Prevention of SIV rectal transmission and priming of T cell responses in macaques after local pre-exposure application of tenofovir gel.
2008 Aug 5
Patents

Sample Use Guides

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.
Name Type Language
STREPTOMYCIN PANTOTHENATE
WHO-DD  
Common Name English
PANTOTHENIC ACID, COMPD. WITH STREPTOMYCIN
Common Name English
PANTOTHENIC ACID, D-, COMPD. WITH STREPTOMYCIN (1:1)
Common Name English
Streptomycin pantothenate [WHO-DD]
Common Name English
D-STREPTAMINE, O-2-DEOXY-2-(METHYLAMINO)-.ALPHA.-L-GLUCOPYRANOSYL-(1->2)-O-5-DEOXY-3-C-FORMYL-.ALPHA.-L-LYXOFURANOSYL-(1->4)-N,N'-BIS(AMINOIMINOMETHYL)-, COMPD. WITH (R)-N-(2,4-DIHYDROXY-3,3-DIMETHYL-1-OXOBUTYL)-.BETA.-ALANINE (1:1)
Systematic Name English
PANTOTHENIC ACID, COMPD. WITH STREPTOMYCIN (1:1)
Common Name English
Code System Code Type Description
EPA CompTox
DTXSID50977839
Created by admin on Fri Dec 15 18:44:24 GMT 2023 , Edited by admin on Fri Dec 15 18:44:24 GMT 2023
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FDA UNII
XOQ162YYFV
Created by admin on Fri Dec 15 18:44:24 GMT 2023 , Edited by admin on Fri Dec 15 18:44:24 GMT 2023
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PUBCHEM
197845
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CAS
6227-52-7
Created by admin on Fri Dec 15 18:44:24 GMT 2023 , Edited by admin on Fri Dec 15 18:44:24 GMT 2023
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SMS_ID
100000084979
Created by admin on Fri Dec 15 18:44:24 GMT 2023 , Edited by admin on Fri Dec 15 18:44:24 GMT 2023
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EVMPD
SUB04592MIG
Created by admin on Fri Dec 15 18:44:24 GMT 2023 , Edited by admin on Fri Dec 15 18:44:24 GMT 2023
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