New Release: Alpha testing version has been released.

Spectinomycin

J01X - Other antibacterials ATC J01XX04 Small molecule approved 1971 Parenteral Natural product

🧬 Cross-allergy: Aminoglycosides

JFDA label: TOGAMYCIN INJ 2GM/A

Indications

Approved

  • Bacterial Infections — bacterial disease

Antimicrobial Spectrum

Expected / intrinsic spectrum (EUCAST breakpoints & labels) — not local resistance. Source: EUCAST v16.

Bacteria

OrganismActivityMIC
Neisseria gonorrhoeae Susceptible 64.0 mg/L

Class profile

gramStatusGram-
spectrumBreadthNarrow
atypicalCoverageNo
isBactericidal0
moaCategoryProtein synthesis inhibitor (30S ribosomal, 16S rRNA)
pdIndexTime-dependent
postAntibioticEffectNone
mrsaCoverage0
resistanceMechanismsRibosomal mutation (spectinomycin resistance),Methylation

Monitoring

EfficacyCulture and susceptibility testing; clinical resolution (temperature, WBC, CRP, procalcitonin)
ToxicityRenal function (dose adjustment in renal impairment); hepatic function for hepatically cleared agents; signs of C. difficile infection (diarrhoea)
Clinical pearlCulture results guide de-escalation to narrower-spectrum therapy. Review antibiotic appropriateness at 48–72 h (antimicrobial stewardship).
CounselingComplete the full course. Report persistent diarrhoea, rash, or lack of improvement after 48–72 h.

Chemistry & Properties

2D structure
FormulaC14H24N2O7
Molecular weight332.35 g/mol
IUPAC name(1R,3S,5R,8R,10R,11S,12S,13R,14S)-8,12,14-trihydroxy-5-methyl-11,13-bis(methylamino)-2,4,9-trioxatricyclo[8.4.0.03,8]tetradecan-7-one
CAS1695-77-8
PubChem CID15541
InChIKeyUNFWWIHTNXNPBV-WXKVUWSESA-N
logP-2.93 (XLogP -3.1)
Polar surface area129.51 Ų
H-bond acceptors / donors9 / 5
Drug-likeness (QED)0.36
Lipinski violations0
SMILESCN[C@@H]1[C@H](O)[C@H](NC)[C@H]2O[C@@]3(O)C(=O)C[C@@H](C)O[C@H]3O[C@@H]2[C@H]1O

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability70.0%
Half-life3.124 h
Volume of distribution0.144 L/kg
Protein binding9.3%
BBB penetrantNo

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (1, DDInter)

Interacting drugSeverityManagement
Picosulfuric acid moderate

Registered Products (1)

BrandForm / strengthPackAgentCitizen (JOD)
TOGAMYCIN INJ 2GM/A Powder for Injection 2 g VIAL+SOLVENT Khoury Drug Store 3.800