Gentamicin

Gentamicin is an aminoglycoside antibiotic with an extensive range of efficacy.

[1], [2], [3], [4], [5], [6]

Indications Gentamicin

It is used in cases of infectious and inflammatory genesis of diseases, the development of which provokes the activity of bacteria that are susceptible 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 for sepsis and purulent infections of the epidermis with the subcutaneous layer, pleural empyema, infections affecting the bones with joints or developing due to burns with wounds, as well as with ventriculitis.

Injections are performed in case of severe stages of gynecological inflammations.

The ointment is used for furunculosis, sycosis, superficial folliculitis, paronychia and pyoderma, and also for acne or seborrheic form of infected dermatitis, with wounds of different etiology (burns, bites, ulcers, etc.) and infected varicose type ulcers. In addition, it may be prescribed for the secondary infection of a bacterial nature due to fungal or viral lesions of the epidermis.

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

[7]

Release form

The release of a therapeutic agent is implemented in several different forms:

• lyophilisate for injection fluid in bottles;
• 4% solution inside ampoules capacity 1 or 2 ml;
• 0.3% eye drops inside the dropper tubes;
• spray and ointment for external processing.

[8], [9], [10], [11], [12], [13], [14], [15], [16]

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 complex informational and transport RNA. Erroneous RNA reading is observed, and inactive proteins are also formed. At the same time, a bactericidal effect is noted - high drug indicators weaken the barrier activity of the cytoplasmic walls, which is why bacteria die.

Separate gram-negative microbes, and in addition, a number of positive bacteria have a strong sensitivity to gentamicin.

Resistant to the effect of the drug, such microorganisms as: Providence Rettgera, streptococci, gonococci, pale treponema, clostridia and bacteroids.

The combination of medication and penicillins develops an effect on fecal streptococci and enterococci, enterococci and streptococci fecium, and in addition to this bird enterococci, Enterococcus durans and Streptococcus durans.

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

[17], [18], [19], [20], [21], [22], [23], [24]

Pharmacokinetics

When i / m injections drug fully and at high speed absorbed. Values of Cmax inside the body when the / m use observed after 30-90 minutes. If a half-hour intravenous infusion is used, this figure is achieved in 0.5 hours, and with a similar, but hourly infusion, after 15 minutes.

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

Low values of the drug are recorded inside fatty tissues, bones with muscles, bile, bronchial secretions, sputum, breast milk, and besides eye moisture and CSF. In adults, the substance almost never passes through the BBB, unlike the placenta through which it can penetrate.

Inside the cerebrospinal fluid in newborns, the drug has higher rates than in an adult.

The drug does not pass metabolic processes inside the body. Half-life is 2-4 hours (adult) or 3-3.5 hours (babies under half a year).

The excretion of most of the unchanged drug occurs through the kidneys, a small amount of drugs excreted in the bile. With a stable work of the kidneys for the period of the first 24 hours, 70-95% of the drug is excreted. Inside the urine is detected in a concentration of more than 100 µg / ml. In the case of a re-injection, cumulation is observed.

[25], [26], [27], [28], [29], [30], [31], [32], [33], [34]

Dosing and administration

Hetamicin sulphate is required to be used taking into account the location of the infectious lesion, the sensitivity of the pathogen microbe and the severity of the disease.

The use of medicinal injections.

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

V / m or / in the introduction of medication from ampoules for an adult is required in a dose of 1.7 mg / kg. During the day, you must enter 3-5 mg / kg. The drug is used 2-4 times per day. The whole therapeutic 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.

Taking into account the type of the disease, Gentamicin can be administered in portions of 0.12-0.16 g 1 times per day in a period of 7-10 days or in a single dose of 0.24-0.28 g. Intravenous injections are carried out throughout 60-120 minutes

For children, medication is used exclusively for severe forms of infections. Premature and newborn babies require 2–5 mg / kg, 2 times a day. Children under 2 years of age use the same dosage, but with a 3-fold administration per day. Children over this age should receive 3-5 mg / kg, administered 3 times a day.

Persons with renal dysfunction need dosage adjustment.

During the day, you can not enter more than 5 mg / kg of the drug (both children and adults).

Schemes of use of ointment.

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

Methods of applying eye drops.

Instilled drug is required in the region of the lower conjunctival sac, in the amount of 1-2 drops, with 1-4 hour intervals.

People with conjunctivitis, keratitis and other eye diseases that have infectious and inflammatory genesis require 3 times a day to dig in a 0.3% solution of the drug.

[43], [44], [45], [46], [47]

Use Gentamicin during pregnancy

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

Contraindications

Main contraindications:

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

While using Gentamicin, it is necessary to periodically monitor the performance of the kidneys.

[35], [36]

Side effects Gentamicin

Performing injections may cause some side effects:

• digestive disorders: vomiting, increased liver transaminase activity, as well as nausea and hyperbilirubinemia;
• violation of hematopoietic processes: anemia, leuko-, thrombocyto- or granulocytopenia;
• lesions affecting NS: headaches, epileptic seizures, paresthesias, numbness or drowsiness, and muscle twitching. Children may show signs of psychosis;
• problems with the work of the senses: hearing loss, deafness, ear noise, vestibular and labyrinth disorders;
• disorders of urinary processes: nephrotoxicity, against which the violation of renal activity. Occasionally, renal necrosis of tubular nature occurs;
• allergy signs: fever, angioedema, rash, eosinophilia and itching;
• change in laboratory indications: children may develop hypocalcemia, and in addition, kalemia or magnemia;
• other disorders: the emergence of superinfection.

[37], [38], [39], [40], [41], [42]

Overdose

Intoxication with a drug can lead to a weakening of the neuronal-muscular conductivity, which sometimes comes to a stop in the respiratory process.

To eliminate the disorder, anticholinesterase substances (for example, prozerin) or calcium drugs are administered to adults. Before using prozerin, it is required to inject atropine (0.5-0.7 mg) to the patient, wait for an increase in pulse rate, and then inject 1.5 mg of proserin. In the absence of a result after using this dosage, a similar portion of prozerin is used again. If bradycardia develops, additional atropine is added.

Poisoning in children requires the use of potassium funds. Gentamicin sulfate can be excreted through peritoneal dialysis or hemodialysis procedures.

[48], [49], [50], [51], [52], [53], [54], [55], [56], [57]

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, a decrease in the level of drug clearance and an increase in its blood values, due to which its toxic properties increase.

Drug administration in combination with opioids or inhalation anesthesia agents increases the risk of developing neuromuscular blockade; apnea may also occur.

Blood indicators of gentamicin increase when it is combined with loop-type diuretic drugs.

[58], [59], [60], [61], [62], [63], [64]

Storage conditions

Gentamicin must be kept in a dark place with a temperature not higher than 25 ° C.

[65], [66], [67]

Shelf life

Gentamicin can be used within 4 years from the time a therapeutic drug is released.

[68], [69], [70], [71], [72], [73]

Application for children

Infants are prescribed medication only if they are strictly indicated. It is required to comply with the prescribed medical scheme prescribed by the doctor, and in addition to provide medical monitoring of the patient's condition.

[74], [75], [76], [77], [78], [79], [80], [81], [82]

Analogs

Analogues of the drug are such drugs as Gentacicol, Garamycin with Asgent, and in addition Gentamicin Akos, Gentamicin K and Gentamicin-Teva, as well as Septop.

[83], [84], [85], [86], [87], [88], [89], [90], [91], [92], [93], [94], [95]

Reviews

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

Of the shortcomings in some comments, the appearance of negative symptoms is mentioned (mainly headaches, hearing loss, nausea and drowsiness). In addition, often quite a painful sting produced injections.

Of the positive aspects, the low cost of the therapeutic agent is noted.