Gentamicin

Gentamicin is an aminoglycoside antibiotic with a broad spectrum of effectiveness.

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Indications Gentamicin

It is used for diseases of infectious and inflammatory genesis, the development of which is provoked by the activity of bacteria that are sensitive to gentamicin.

Parenteral administration of 4% liquid is carried out in the acute stage of cholecystitis, pyelonephritis, cystitis with cholangitis, peritonitis and pneumonia. In addition, it is used in sepsis and purulent infections of the epidermis with the subcutaneous layer, pleural empyema, infections affecting bones with joints or developing due to burns with wounds, as well as in ventriculitis.

Injections are performed in cases of severe stages of gynecological inflammation.

The ointment is used for furunculosis, sycosis, superficial folliculitis, paronychia and pyoderma, as well as acne or seborrheic dermatitis of an infected nature, wounds of various etiologies (burns, bites, ulcers, etc.) and infected varicose ulcers. In addition, it can be prescribed for secondary bacterial infections due to fungal or viral lesions of the epidermis.

Eye drops are prescribed for keratitis, blepharitis or blepharoconjunctivitis, keratoconjunctivitis with conjunctivitis, and also for dacryocystitis or meibomitis.

Release form

The release of the therapeutic agent is realized in several different forms:

• lyophilisate for injection liquid in vials;
• 4% solution inside ampoules with a capacity of 1 or 2 ml;
• 0.3% eye drops in dropper tubes;
• aerosol and ointment for external treatment.

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Pharmacodynamics

Inside the body, the drug is synthesized with the 30S ribosomal subunit, which leads to the destruction of protein binding and the suspension of the production of the complex of information and transport RNA. Erroneous RNA reading is observed, and inactive proteins are formed. At the same time, a bactericidal effect is noted - high levels of the drug weaken the barrier activity of the cytoplasm walls, causing bacteria to die.

Some gram-negative microbes, as well as a number of gram-positive bacteria, have strong sensitivity to Gentamicin.

The following microorganisms are resistant to the effect of the drug: Providence Rettger, streptococci, gonococci, pale treponema, clostridia and bacteroides.

When combined with penicillins, the drug has an effect on fecal streptococci and enterococci, enterococci and Streptococcus faecium, and also avian enterococci, Enterococcus durans and Streptococcus durans.

Bacterial resistance to this drug develops rather slowly, but strains that are resistant to kanamycin and neomycin may also demonstrate resistance to the effects of gentamicin. The drug does not affect the activity of viruses, fungi, and protozoa.

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Pharmacokinetics

With intramuscular injections, the medication is fully and rapidly absorbed. The Cmax values inside the body with intramuscular administration are observed after 30-90 minutes. If a half-hour intravenous infusion is used, this indicator is achieved in 0.5 hours, and with a similar, but hourly infusion - after 15 minutes.

Intraplasmic synthesis with protein is quite low - maximum 10%. In medicinal values, the substance is registered in the lungs, kidneys with the liver and fluids (synovium, lymphatic, peritoneal, pleural with ascitic and pericardial). In addition, it is found in urine, pus from wounds and granulations.

Low values of the drug are registered in fatty tissues, bones with muscles, bile, bronchial secretions, sputum, breast milk, and in addition to this, eye fluid and cerebrospinal fluid. In adults, the substance almost does not pass through the BBB, unlike the placenta, through which it can penetrate.

In the cerebrospinal fluid of newborns, the drug has higher levels than in adults.

The drug does not undergo metabolic processes inside the body. The half-life is 2-4 hours (adult) or 3-3.5 hours (infants under six months).

Excretion of the majority of unchanged drug occurs through the kidneys, a small amount of the drug is excreted with bile. With stable renal function, 70-95% of the drug is excreted during the first 24 hours. In urine, it is found in concentrations of more than 100 mcg / ml. In the case of repeated injection, cumulation is observed.

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Dosing and administration

Getamicin sulfate should be used taking into account the location of the infectious lesion, the sensitivity of the causative microbe and the severity of the disease.

Use of medicinal injections.

Before starting therapy, it is necessary to determine the level of sensitivity of microflora to gentamicin.

Intramuscular or intravenous administration of the drug from ampoules for an adult is required in a dose of 1.7 mg/kg. It is necessary to administer 3-5 mg/kg per day. The drug is used 2-4 times per day. The entire treatment cycle lasts 7-10 days. For intramuscular injections, the lyophilisate must first be dissolved in distilled liquid (2 ml), which is added directly to the ampoule.

Depending on the type of disease, Gentamicin can be prescribed in a dose of 0.12-0.16 g once a day for a period of 7-10 days or in a single dose of 0.24-0.28 g. Intravenous injections are administered over 60-120 minutes.

The drug is used in children only for severe forms of infections. Premature and newborn infants require 2-5 mg/kg, 2 times a day. Children under 2 years of age are given a similar dosage, but with 3-times administration per day. Children over this age should receive 3-5 mg/kg, administered 3 times a day.

Individuals with renal impairment require dosage adjustment.

It is not recommended to administer more than 5 mg/kg of the drug per day (for both children and adults).

Schemes for using the ointment.

The ointment should be used 3-4 times a day. Before applying it, it is necessary to completely remove pus and dead tissue from the affected area. For very large lesions, the daily dosage of the ointment should be a maximum of 200 g. The duration of the therapeutic cycle is selected by a medical specialist.

Methods of using eye drops.

The drug should be instilled into the area of the lower conjunctival sac, in the amount of 1-2 drops, at 1-4 hour intervals.

People with conjunctivitis, keratitis and other eye diseases of infectious and inflammatory origin are required to instill a 0.3% solution of the drug 3 times a day.

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Use Gentamicin during pregnancy

Pregnant women, and also lactating women, should not be prescribed Gentamicin. It is known that small amounts of aminoglycosides can penetrate into breast milk. But this substance is poorly absorbed from the gastrointestinal tract, so no complications were noted in infants.

Contraindications

Main contraindications:

• the presence of severe hypersensitivity to the drug and other aminoglycosides;
• neuritis affecting the auditory nerve;
• severe renal impairment;
• uremia.

During the use of Gentamicin, it is necessary to periodically monitor kidney function.

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Side effects Gentamicin

Injections may cause some side effects:

• digestive disorders: vomiting, increased activity of liver transaminases, as well as nausea and hyperbilirubinemia;
• violation of hematopoietic processes: anemia, leukopenia, thrombocyto- or granulocytopenia;
• Lesions affecting the nervous system: headaches, epileptic seizures, paresthesia, numbness or drowsiness, and muscle twitching. In children, signs of psychosis may be observed;
• problems with the functioning of the sense organs: hearing loss, deafness, tinnitus, vestibular and labyrinthine disorders;
• urinary disorders: nephrotoxicity, which causes renal dysfunction. Tubular renal necrosis occasionally occurs;
• signs of allergy: fever, Quincke's edema, rash, eosinophilia and itching;
• changes in laboratory readings: children may develop hypocalcemia, as well as kalemia or magnesiumemia;
• other disorders: occurrence of superinfection.

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Overdose

Intoxication with a drug can lead to a weakening of neuromuscular conduction, which sometimes leads to the cessation of the respiratory process.

To eliminate the disorder, adults are given anticholinesterase agents (for example, proserin) or calcium medications. Before using proserin, the patient must be given atropine intravenously (0.5-0.7 mg), wait for the pulse to quicken, and then administer 1.5 mg of proserin. If there is no result after using this dosage, a similar portion of proserin is used again. If bradycardia develops, additional atropine is administered.

Poisoning in children requires the use of potassium agents. Excretion of gentamicin sulfate can be achieved through peritoneal dialysis or hemodialysis procedures.

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Interactions with other drugs

The use of the drug in combination with aminoglycosides, vancomycin, and also ethacrynic acid or cephalosporins can lead to potentiation of nephro- and ototoxic activity.

When using the drug together with indomethacin, the drug clearance level decreases and its blood values increase, which also increases its toxic properties.

Administration of the drug in combination with opioids or inhalational anesthetics increases the risk of developing neuromuscular blockade; apnea may also occur.

Blood levels of gentamicin increase when combined with loop diuretics.

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Storage conditions

Gentamicin should be kept in a dark place with a temperature no higher than 25°C.

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Shelf life

Gentamicin can be used within a 4-year period from the date of release of the therapeutic drug.

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Application for children

The medication is prescribed to infants only if there are strict indications. It is necessary to follow the treatment regimen prescribed by the doctor, and also to ensure medical supervision of the patient's condition.

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Analogues

Analogues of the drug are such drugs as Gentacycol, Garamicin with Asgent, as well as Gentamicin Akos, Gentamicin K and Gentamicin-Teva, as well as Septopa.

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Reviews

Gentamicin generally receives good reviews - it is considered to be a fairly effective drug that treats various types of diseases.

Among the disadvantages, some comments mention the appearance of negative symptoms (mainly headaches, hearing loss, nausea and a feeling of drowsiness). In addition, the injections are often quite painful.

One of the positive aspects is the low cost of the therapeutic agent.