Estreptomicina Labesfal

Estreptomicina Labesfal Uses, Dosage, Side Effects, Food Interaction and all others data.

Aminoglycosides like Estreptomicina Labesfal "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically Estreptomicina Labesfal 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.

Although streptomycin originally had broad gram-negative and gram-positive coverage, its spectrum of activity has been significantly narrowed due to antibiotic resistance. Estreptomicina Labesfals current spectrum of activity includes susceptible strains of Yersinia pestis, Francisella tularensis, Brucella, Calymmatobacterium granulomatis, H. ducreyi, H. influenza, K. pneumoniae pneumonia, E.coli, Proteus, A. aerogenes, K. pneumoniae, Enterococcus faecalis, Streptococcus viridans, Enterococcus faecalis, and Gram-negative bacillary bacteremia. Estreptomicina Labesfal is not reliably active against pseudomonas aeruginosa.

Similar to other aminoglycosides, streptomycin is considered to have a narrow therapeutic index. Characteristic toxicities of streptomycin include nephrotoxicity and ototoxicity. Patients should be carefully monitored for early signs of hearing loss and vestibular dysfunction in order to prevent permanent damage to sensorineural cells. Neuromuscular blockade has also been rarely reported.

Trade Name Estreptomicina Labesfal
Availability Prescription only
Generic Streptomycin
Streptomycin Other Names Estreptomicina, Streptomicina, Streptomycin, Streptomyzin
Related Drugs doxycycline, ciprofloxacin, metronidazole, azithromycin, ceftriaxone, levofloxacin, vancomycin, gentamicin, Zithromax, Levaquin
Type
Formula C21H39N7O12
Weight Average: 581.5741
Monoisotopic: 581.265669747
Groups Approved, Vet approved
Therapeutic Class Aminoglycosides, Anti-Tubercular Antibiotics
Manufacturer
Available Country Portugal
Last Updated: September 19, 2023 at 7:00 am
Estreptomicina Labesfal
Estreptomicina Labesfal

Uses

Estreptomicina Labesfal is used for the treatment of individuals with moderate to severe infections caused by susceptible 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. Estreptomicina Labesfal is also used for therapy of tuberculosis when one or more of the above drugs is contraused 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

Estreptomicina Labesfal is also used to associated treatment for these conditions: Bacteremia, Bacterial Infections caused by susceptible bacteria, Chancroid, Disseminated mycobacterium avium complex infection, Flu caused by Influenza, Granuloma Inguinale, Menière's Disease, Mycobacterium avium complex infection, Mycobacterium kansasii infection, Mycobacterium marinum infection, Plague, Pneumonia, Tuberculosis (TB), Tularemia, Urinary Tract Infection

How Estreptomicina Labesfal works

There are 3 key phases of aminoglycoside entry into cells. The first “ionic binding phase” occurs when polycationic aminoglycosides bind electrostatically to negatively charged components of bacterial cell membranes including with lipopolysaccharides and phospholipids within the outer membrane of Gram-negative bacteria and to teichoic acids and phospholipids within the cell membrane of Gram-positive bacteria. This binding results in displacement of divalent cations and increased membrane permeability, allowing for aminoglycoside entry.

The second “energy-dependent phase I” of aminoglycoside entry into the cytoplasm relies on the proton-motive force and allows a limited amount of aminoglycoside access to its primary intracellular target - the bacterial 30S ribosome. This ultimately results in the mistranslation of proteins and disruption of the cytoplasmic membrane. Finally, in the “energy-dependent phase II” stage, concentration-dependent bacterial killing is observed. Aminoglycoside rapidly accumulates in the cell due to the damaged cytoplasmic membrane, and protein mistranslation and synthesis inhibition is amplified.

Hence, aminoglycosides have both immediate bactericidal effects through membrane disruption and delayed bactericidal effects through impaired protein synthesis; observed experimental data and mathematical modeling support this two-mechanism model.

Inhibition of protein synthesis is a key component of aminoglycoside efficacy. Structural and cell biological studies suggest that aminoglycosides bind to the 16S rRNA in helix 44 (h44), near the A site of the 30S ribosomal subunit, altering interactions between h44 and h45. This binding also displaces two important residues, A1492 and A1493, from h44, mimicking normal conformational changes that occur with successful codon-anticodon pairing in the A site. Overall, aminoglycoside binding has several negative effects including inhibition of translation, initiation, elongation, and ribosome recycling. Recent evidence suggests that the latter effect is due to a cryptic second binding site situated in h69 of the 23S rRNA of the 50S ribosomal subunit. Also, by stabilizing a conformation that mimics correct codon-anticodon pairing, aminoglycosides promote error-prone translation. Mistranslated proteins can incorporate into the cell membrane, inducing the damage discussed above.

Dosage

Estreptomicina Labesfal dosage

Tularaemia:

  • Adult: 1-2 g daily in divided doses for 7-14 days until the patient is afebrile for 5-7 days.
  • Child: 15 mg/kg bid for at least 10-14 days. Max: 2 g daily

Bacterial endocarditis:

  • Adult: Streptococcal endocarditis: 1 g bid for 1 wk, then 500 mg bid for the 2nd wk. Enterococcal endocarditis: 1 g bid for 2 wk then 500 mg bid for an additional 4 wk. Doses are given in combination with penicillin.
  • Child: Enterococcal endocarditis: 20-30 mg/kg daily in 2 divided doses, in combination w/ penicillin.
  • Elderly: Streptococcal endocarditis: >60 yr 500 mg bid for the entire 2 wk period.

Tuberculosis:

  • Adult: 15 mg/kg as a single dose daily. Max: 1 g daily. As part of intermittent regimen: 25-30 mg/kg 2-3 times wkly. Max: 1.5 g/dose.
  • Child: 20-40 mg/kg as a single dose daily. Max: 1 g daily. As part of intermittent regimen: 25-30 mg/kg 2-3 times wkly. Max: 1.5 g/dose.
  • Elderly: >40 yr Max: 500-750 mg daily.

Plague:

  • Adult: 2 g daily in 2 divided doses for a minimum of 10 days.
  • Child: 30 mg/kg daily in 2-3 divided doses. Max: 2 g daily.

Bacteraemia, Brucellosis, Meningitis, Pneumonia, Urinary tract infections:

  • Adult: For concomitant use with other agents and as 2nd line agent: 1-2 g daily in divided doses 6-12 hrly. Max: 2 g daily.
  • Child: 20-40 mg/kg daily in divided doses 6-12 hrly.

Add 4.2 mL, 3.2 mL, or 1.8 mL of sterile water for inj to prepare a soln containing approx 200 mg, 250 mg, or 400 mg, respectively, of streptomycin per mL.

Side Effects

Neurotoxic reactions (e.g. vestibular and cochlear function disturbance, optic nerve dysfunction, peripheral neuritis, arachnoiditis, encephalopathy); paraesthesia of face, rash, fever, angioneurotic oedema, eosinophilia; exfoliative dermatitis, azotemia, leucopenia, thrombocytopenia, pancytopenia, haemolytic anaemia, muscular weakness, amblyopia.

Toxicity

The most common symptoms of streptomycin overdose are ototoxicity and vestibular impairment. Estreptomicina Labesfal is also associated with nephrotoxicity which presents as mild elevations in blood urea, mild proteinuria, and excess cellular excretion. While in severe cases, streptomycin may lead to permanent hearing loss and vestibular dysfunction, any associated nephrotoxicity is typically transient. In cases of toxicity, streptomycin serum concentrations may be lowered with dialysis.

Precaution

Patient with neuromuscular disorders (e.g. myasthenia gravis), pre-existing vertigo, or hearing loss. Renal impairment. Elderly, childn. Pregnancy and lactation.

Interaction

Additive neurotoxic and nephrotoxic effect with neomycin, kanamycin, gentamicin, cefaloridine, paronomycin, viomycin, polymyxin B, colistin, tobramycin, and ciclosporin. Enhanced ototoxic and nephrotoxic effect with ethacrynic acid, mannitol, furosemide and possibly other diuretics. May enhance the resp depressant effect of neuromuscular blockers. Increased risk of nephrotoxicity with cephalosporins. Reduced excretion with NSAIDs.

Food Interaction

No interactions found.

Estreptomicina Labesfal Disease Interaction

Major: dehydration, neuromuscular blockade, ototoxicity, renal dysfunction

Elimination Route

Due to poor oral absorption, aminoglycosides including streptomycin are administered parenterally. Estreptomicina Labesfal is available as an intramuscular injection, and in some cases may be administered intravenously. A peak serum concentration of 25-50 mcg/mL is achieved within 1 hour after intramuscular administration of 1 gram of streptomycin.

Half Life

Estreptomicina Labesfals serum half-life is estimated to be 2.5 hours.

Elimination Route

Approximately 50% of streptomycin is eliminated in the urine within 24 hours after intravenous or intramuscular administration.

Pregnancy & Breastfeeding use

Estreptomicina Labesfal can cause fetal harm when administered to a pregnant woman. Because streptomycin readily crosses the placental barrier, caution in use of the drug is important to prevent ototoxicity in the fetus. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.

Contraindication

Hypersensitivity to streptomycin and other aminoglycosides.

Special Warning

Renal Impairment: Dosage adjustment needed.

Storage Condition

Store between 15-30°C. Protect from light.

Innovators Monograph

You find simplified version here Estreptomicina Labesfal

Estreptomicina Labesfal contains Streptomycin see full prescribing information from innovator Estreptomicina Labesfal Monograph, Estreptomicina Labesfal MSDS, Estreptomicina Labesfal FDA label

FAQ

What is Estreptomicina Labesfal used for?

Estreptomicina Labesfal belongs to a class of drugs known as aminoglycoside antibiotics.Estreptomicina Labesfal works by killing the organisms that cause the infection. This drug may also be used to treat other serious infections along with other medications.

How to use Estreptomicina Labesfal?

This medication is given by injection, usually into a muscle as directed by your doctor. When you start treatment for TB, it is usually given once a day or as directed by your doctor. It is important to change the location of the injection site daily to avoid problem areas under the skin.

What are the common side effects of Estreptomicina Labesfal?

Common side effects of Estreptomicina Labesfal are include:

  • nausea,
  • vomiting,
  • stomach upset,
  • loss of appetite,
  • spinning sensation (vertigo),
  • injection site reactions (pain, irritation, and redness),
  • tingling or prickling sensation in the face,
  • rash,
  • fever,
  • hives, and
  • swelling (edema).

Is Estreptomicina Labesfal safe during pregnancy?

Estreptomicina Labesfal should not be used in pregnancy.

Is Estreptomicina Labesfal safe during breastfeeding?

Estreptomicina Labesfal is poorly excreted into breastmilk.

Can Estreptomicina Labesfal cause deafness?

They found that Estreptomicina Labesfal caused less ototoxicity than the other two drugs but that the size or frequency of dosage did not affect toxicity. Older age and cumulative dose were associated with an increased risk and median onset of hearing loss was 9 weeks in both patients treated daily and three times a week.

Why is Estreptomicina Labesfal so effective?

Estreptomicina Labesfal is an effective antibiotic because its structure is similar to that of the anticodons that would usually bind to the ribosome.Estreptomicina Labesfal is significant because it was the first antibiotic that could treat tuberculosis.

What causes Estreptomicina Labesfal resistance?

Chromosomally acquired Estreptomicina Labesfal resistance is frequently due to mutations in the gene encoding the ribosomal protein S12, rpsL.

Can Estreptomicina Labesfal cure staphylococcus?

Aminoglycosides like Estreptomicina Labesfal were once effective against Staphylococcal infections. They have developed resistance by modifying enzymes, changing the ribosomal attachment sites and by actively pushing out the drug from the bacteria.

Is Estreptomicina Labesfal a strong antibiotic?

Estreptomicina Labesfal is an antibiotic that inhibits both Gram-positive and Gram-negative bacteria, and is therefore a useful broad-spectrum antibiotic.

How many days can Estreptomicina Labesfal be taken?

Two grams of Estreptomicina Labesfal daily in two divided doses should be administered intramuscularly. A minimum of 10 days of therapy is recommended.

When should I take Estreptomicina Labesfal?

Estreptomicina Labesfal is an antibiotic that is used to treat moderate to severe tuberculosis, pneumonia, E. coli, influenza, plague and other infections caused by certain bacteria.Estreptomicina Labesfal may also be used for purposes not listed in this medication guid.

How do I take Estreptomicina Labesfal?

Estreptomicina Labesfal may be used in combination with Aureofungin sol for the control of bacterial and fungal diseases.

Who should not take Estreptomicina Labesfal?

The risk is higher if you have kidney disease, if you are receiving high doses of this medication, if you use this drug for a long time, if you are an older adult (older than 60 years), or if you develop a severe loss of body water (become dehydrated).

Can Estreptomicina Labesfal cause blindness?

Estreptomicina Labesfal may causes blindness.A case of transient blindness occurring during long-term therapy with Estreptomicina Labesfal and chloramphenicol is described.

Can Estreptomicina Labesfal cause seizures?

Estreptomicina Labesfal may cause seizures also with other side effects.

Can Estreptomicina Labesfal cause hearing loss?

Estreptomicina Labesfal may cause nerve damage or hearing loss, especially if you have kidney disease or use certain other medicines.

Why is Estreptomicina Labesfal so effective?

Estreptomicina Labesfal is an effective antibiotic because its structure is similar to that of the anticodons that would usually bind to the ribosome.

Can Estreptomicina Labesfal cause hearing loss?

Estreptomicina Labesfal may cause nerve damage or hearing loss, especially if you have kidney disease or use certain other medicines.

Can Estreptomicina Labesfal cause deafness to unborn baby?

The risk of deafness developing in the unborn child following the use of Estreptomicina Labesfal during pregnancy remains uncertain.

When do you give Estreptomicina Labesfal?

Estreptomicina Labesfal is administered via injection daily or 5 days a week during the intensive phase, in the first two months of treatment.

Why is Estreptomicina Labesfal not given orally?

Estreptomicina Labesfal is not absorbed by the gastrointestinal track, and except for the treatment gastrointestinal infections, has to be administered by regular intramuscular injections, the usual dose being 1 g daily.

Is Estreptomicina Labesfal an ototoxic?

Estreptomicina Labesfal and gentamicin are primarily vestibulotoxic,

Why Estreptomicina Labesfal is no longer used?

Estreptomicina Labesfal was the first effective antituberculosis drug but is no longer a first-line drug as it has the disadvantage that it is not absorbed from the intestine and must therefore be given by intramuscular injection.

*** Taking medicines without doctor's advice can cause long-term problems.
Share