What Is Novobiocin?

An antibiotic, which belongs to aminoglycoside antibiotics together with streptomycin, kanamycin and gentamicin. It is produced by Streptomyces freundii; it is effective against both Gram-positive and negative bacteria, and the product is mainly a mixture of neomycin B and C. Neomycin and kanamycin have complete cross-resistance and streptomycin have partial cross-resistance. Similar to similar antibiotics, they have nephrotoxicity and inner ear toxicity. The damage to the inner ear is often irreversible. This antibiotic is no longer actually used.

Drug Name: Neomycin
Foreign name: neomycin

Main indications: Prepared before colon surgery, as an adjuvant treatment in liver coma.
Dosage: Adults take orally, 0.25-0.5g at a time, 1-2g a day.
Athletes use with caution: Inadvertent use

Neomycin drug name

Chinese name: neomycin

English name: neomycin

English alias: Neomycin; CCRIS 5462; Caswell No. 595; EPA Pesticide Chemical Code 006303; Fradiomycin; Fradiomycinum; HSDB 3242; Myacyne; sulfate (salt)

CAS: 1404-04-2

EINECS: 215-766-3

Molecular formula: C23H48N6O17S

Molecular weight: 712.7222

Pharmacological effects of neomycin

See streptomycin sulfate. Pharmacokinetics are rarely absorbed after oral administration. Intact intestinal mucosa can only be absorbed by about 3%, but a considerable amount can be absorbed through mucous membranes with ulcers or exfoliation or inflammation. Most are excreted unchanged. Neomycin has a strong antibacterial effect on Mycobacterium tuberculosis, and its minimum inhibitory concentration is generally 0.5 mg / ml. Most non-tuberculous mycobacteria are resistant to this product. Neomycin also works against many Gram-negative bacteria such as Escherichia coli, Klebsiella, Proteus, Enterobacter, Salmonella, Shigella, Brucella, Pasteurella, etc. Antibacterial effect; Neisseria meningitidis and Neisseria gonorrhoeae are also sensitive to this product. Neomycin has a poor effect on Staphylococcus and other Gram-positive cocci. Streptococcus, Pseudomonas aeruginosa and anaerobic bacteria in each group are resistant to this product. Neomycin mainly binds to the bacterial ribosome 30S subunit and inhibits bacterial protein synthesis. Bacteria are prone to drug resistance after contact with neomycin. The combination of neomycin with other antibacterial or antituberculosis drugs can reduce or delay the development of resistance. The product is white or off-white powder.

Neomycin indications

Prepared before colon surgery, as an adjuvant treatment in liver coma. Neomycin should not be used for the treatment of systemic infections. This product is not effective against Pseudomonas aeruginosa.

Neomycin kinetics

Poor oral absorption requires intravenous administration. Quickly distributed to whole body tissues after intravenous injection. The highest concentration of liver and kidney, concentrated in nucleated cells, higher in white blood cells, the product does not easily penetrate its brain barrier, so it does not enter the cerebrospinal fluid: the product has very little metabolism, 12% to 25 within 24 hours % Is excreted by the kidney, and 50% ~ 90% is excreted by the bile. Due to the slow release of the product from the storage tissue, the plasma elimination half-life is long, about 36 hours.

Neomycin adverse reactions

1. Hearing loss, tinnitus or ear fullness (ototoxicity) are less common; staggering, dizzy, or unstable footsteps (ototoxicity, affecting the vestibule); significantly reduced urine output or frequency of urination, or extreme mouth Thirsty (renal toxicity).

2. The following conditions need to be paid attention to: the mouth or perianal irritation or pain, nausea or vomiting are more frequent; diarrhea or pale odorous fatty stools are caused in a small amount, or a large amount of air is released (absorption) Syndrome), rash. Can cause kidney and hearing damage, gastrointestinal reactions, loss of appetite, nausea, and vomiting. Delayed allergic reactions can occur. Large doses may have symptoms of neurotoxicity, respiratory depression, etc. Among aminoglycosides, the neuromuscular junction of this product has the strongest inhibitory effect, and many patients have experienced severe respiratory depression or even death. The ototoxic effect of this product may be accompanied by or without nephrotoxicity, and the two often occur simultaneously. Inner ear damage began as high-pitched hearing loss and later progressed to deafness. Vestibular dysfunction is only seen when hearing is impaired at the same time. Inner ear damage is permanent. The nephrotoxic effect of the product may be related to the combination of the drug with the protein of renal tubular cells. The clinical manifestations were mild proteinuria, necrosis of renal tubular epithelial cells, cast, decreased muscle drunk clearance, and oliguria. This damage can develop into extensive tubular epithelial cell necrosis. May cause malabsorption syndrome and steatorrhea when taken orally. Applying neomycin topically, 6 to 8% of patients develop allergies (mainly various rashes). Patients who are allergic to this drug may cross-react when other aminoglycosides are used. Hearing loss often occurs during neomycin treatment. Even in people with normal renal function, hearing loss has occurred with topical application or washing of wounds with 0.5% neomycin solution. In patients treated with neomycin, abnormal urine sediments and azotemia are common. After the neomycin solution flushed the wound or serosal cavity, there was also a block of neuromuscular contacts with respiratory paralysis. Applying neomycin to a large area of skin or trauma may cause a whole body reaction.

Neomycin usage and dosage

1. Oral doses for adults are 0.25-0.5g (based on neomycin, the same below), 1-12g a day. Adjuvant treatment of hepatic encephalopathy, 0.5-1.0g at a time, once every 6 hours, the course of treatment is 5-6 days. Before colon surgery, 0.5g per hour, medication for 4 hours, followed by 0.5g every 4 hours for a total of 24 hours.

2. The usual dose for children is 25-50mg / kg daily, divided into 4 doses. Follow-up examinations: audiograms, renal function tests, patients with pre-existing renal impairment or 8th pair of neurological damage or long-term treatment need to be checked before and during the medication. Those who have not improved for several days after taking the drug should be checked. Neomycin can be taken on an empty stomach or after a meal; Renal function or the 8th pair of patients with reduced cerebral nerve function should be reduced; If patients with liver coma can not take neomycin orally, use sterile neomycin powder Formulated as a 1% solution for retention enema; neomycin sulfate is too toxic and is no longer for injection. It is not advisable to indwell in a large amount in the body cavity, which can cause ear, kidney toxicity and inhibit breathing due to absorption.

Neomycin contraindications

1. Cross-allergies, those who cannot tolerate one aminoglycoside antibiotic may not tolerate other aminoglycosides.

2. The following conditions should be used with caution: No. 8 pairs of cerebral nerve damage, intestinal obstruction, myasthenia gravis, patients with Parkinson's disease, impaired renal function, and colonic ulcerative lesions.

Precautions

Neomycin interaction

1. When used systemically with other aminoglycosides or capreomycin, it may increase ototoxicity, nephrotoxicity and neuromuscular blockade; hearing loss may occur, and even after stopping the drug, it can continue to progress to deafness, which is often permanent .

2. Simultaneous application with neuromuscular blocking drugs may increase neuromuscular blocking effects, resulting in skeletal muscle weakness and respiratory depression or paralysis (apnea).

3. Simultaneous systemic application with cisplatin, itanilic acid injection, furosemide injection or vancomycin may cause hearing impairment and may continue to progress to deafness after discontinuation, often permanent.

4. Long-term combination of oral contraceptives (including estrogen) and oral neomycin may cause contraceptive failure and increase the incidence of bleeding.

5. Oral neomycin can affect the absorption of digitalis glycosides, vitamin A or vitamin Bl2, and reduce the efficacy; therefore, patients should be closely observed whether the efficacy of digitalis has changed. Patients who take neomycin orally, especially when combined with colchicine and vitamin A, may require increased vitamin B12.

6. Simultaneous systemic application with polymyxins may increase renal toxicity and neuromuscular blockade.

The formulation is based on neomycin. Neomycin sulfate tablets (1) 0.1g (100,000 units) (2) 0.25g (250,000 units) orally, 1g at a time, 3-4 times a day. Children, 5-10mg / kg once, 4 times a day.

Neomycin sulfate tablets

English name NeomycinSulfateTablets

Category: Western medicine

Pharmacological action

Neomycin sulfate is an aminoglycoside antibiotic. This product has good antibacterial effect on Enterobacteriaceae bacteria such as Staphylococcus (methicillin-sensitive strain), Corynebacterium, Escherichia coli, Klebsiella, Proteus, etc. Cocci and Enterococcus are poor in activity. Pseudomonas aeruginosa and anaerobic bacteria are resistant to this product. Bacteria have partial or complete cross-resistance to streptomycin, neomycin, kanamycin, and gentamicin. Neomycin systemic administration has significant nephrotoxicity and ototoxicity, so it is limited to oral or topical application. The product is a white tablet.

dynamics

Neomycin is rarely absorbed orally (approximately 3%), but large doses are taken orally for a long period of time, and a considerable amount can be absorbed even when there is ulcer or inflammation in the intestinal mucosa, especially when the renal function is reduced, the blood concentration can be significantly increased. Most of them are excreted without change after oral administration.

Indication

Can be used orally:

1. Intestinal infection.

2. It can also be used as an adjuvant treatment during bowel preparation or liver coma before colon surgery. Neomycin should not be used for the treatment of systemic infections.

Dosage

1. Oral, 0.25 0.5g for adults (based on neomycin), 4 times a day. Adjuvant treatment of hepatic encephalopathy, 0.5 to 1 g once, once every 6 hours, the course of treatment is 5 to 6 days. Prepare before colon surgery, 0.5g per hour, 4 times in a row, followed by 0.5g every 4 hours for a total of 24 hours.

2. For children, take 25 to 50 mg / kg a day in 4 divided doses.

Adverse reactions

1, can cause loss of appetite, nausea, diarrhea, etc., but long-term application (more than 10 weeks) does not affect the synthesis of vitamin K.

2. Hearing loss, tinnitus or ear fullness are rarely found; dizziness or instability; significantly reduced urine output or frequent urination or extreme thirst.

3, even can cause intestinal mucosal atrophy leading to malabsorption syndrome and fatty diarrhea, and even pseudomembranous enteritis.

Taboo This product is contraindicated in patients who are allergic to neomycin or other aminoglycoside antibiotics.

Precautions

1. Cross-allergy Patients who are allergic to an aminoglycoside antibiotic such as streptomycin, gentamicin, amikacin may also be allergic to this product.

2. Urine routine and renal function tests should be performed regularly during medication to prevent renal toxicity and audiometry or electrocardiogram measurements.

3. This product should be used with caution in the following cases: dehydration, 8th pair of cerebral nerve damage, myasthenia gravis, Parkinson's disease, renal impairment, ulcerative colitis and patients with oral dental disease (neomycin can cause oral irritation Or pain).

4. Patients with chronic intestinal infections who take the product orally for a long time, especially those with renal dysfunction or taking other ototoxic or nephrotoxic drugs, should still pay attention to the possibility of symptoms of nephrotoxicity or ototoxicity. There is no information on the safe use of this product in preterm infants and newborns, so it should not be used. Pregnant women should use this product with caution. Breastfeeding women should suspend breastfeeding during medication. This product should be used with caution in elderly patients.

Overdose treatment of this product has no specific antagonist. When the drug is overdose, it is mainly symptomatic therapy and supportive therapy, such as gastric lavage, emetic and fluid replacement.

interaction

1. Long-term combination with oral contraceptives (including estrogen) may cause contraceptive failure and increase the incidence of bleeding.

2. Oral neomycin can affect the absorption of digitalis, fluorouracil, methotrexate, penicillin V, vitamin A or vitamin B12. When patients taking neomycin orally take colchicine and vitamin A, their vitamin B12 requirements may increase.

Enteritis used with caution 3. This product should not be used in combination with other nephrotoxic drugs and ototoxic drugs.

4. When combined with neuromuscular blocking drugs, it may increase the neuromuscular blocking effect, resulting in skeletal muscle weakness.

Preparation (1) 0.1g (100,000 units) (2) 0.25g (250,000 units)

Neomycin eye drops

English name NeomycinSulfateEyeDrops

Category: Western medicine

Pharmacological action

Neomycin is an aminoglycoside antibiotic. This product has a good effect on Staphylococcus (methicillin-sensitive strains) and Corynebacterium, and it also has a good effect on Enterobacteriaceae bacteria such as Escherichia coli, Klebsiella, Proteus, etc. Cocci, Streptococcus pneumoniae, Enterococcus are poor in activity, and Pseudomonas aeruginosa and anaerobic bacteria are resistant to this product. Bacteria have partial or complete cross-resistance to streptomycin, neomycin, kanamycin, and gentamicin. This product is colorless or slightly yellow clear liquid.

dynamics

Neomycin sulfate eye drops are rarely absorbed into the eye tissue or systemic blood circulation after eye drops.

Indication

This product is suitable for conjunctivitis, tears caused by sensitive staphylococci (methicillin-sensitive Staphylococcus aureus and coagulase-negative staphylococci), Haemophilus influenzae, Escherichia coli, and Proteus Bursitis, keratitis, blepharitis, meibomitis, etc.

Dosage 1 to 2 drops at a time, 3 to 5 times a day.

Adverse reactions Occasionally mild eye irritation and discomfort, no systemic adverse reactions.

Contraindications Patients who are allergic to neomycin or other aminoglycoside antibiotics are contraindicated.

Precautions

1. This product should not be injected directly under the bulbous conjunctiva or into the anterior chamber of the eye.

2. Lacrimal sac infection (dacryocystitis) often occurs in children with lacrimal duct occlusion. In addition to using the product for eye drops, it can be supplemented with local hot compresses.

3. Do not touch the mouth of the bottle during eye drops. Tighten the bottle cap after use to avoid contaminating the liquid medicine.

Neomycin compound ointment

English name CompoundNeomycinOintment

Category: Western medicine

Pharmacological action

1. The main ingredients in the pharmacological compound neomycin ointment are neomycin and bacitracin. Neomycin is an aminoglycoside antibiotic that has good antibacterial effect on Enterobacteriaceae bacteria such as Staphylococcus (methicillin-sensitive strains), Corynebacterium, Escherichia coli, Klebsiella, Proteus , Poor activity against Streptococcus, Streptococcus pneumoniae, Enterococcus, etc. in each group. Pseudomonas aeruginosa and anaerobic bacteria are resistant to this product. Bacitracin is a polypeptide antibiotic that has a strong antibacterial effect on Gram-positive bacteria such as Staphylococcus and Streptococcus. It also has a certain effect on Neisseria gonorrhoeae, Neisseria meningitidis, and certain Borrelia, Actinomyces. Gram-negative bacteria are all resistant.

2. Systemic administration of toxic neomycin can cause severe nephrotoxicity and ototoxicity. Systemic administration of bacitracin can cause severe renal toxicity, so both are limited to local application. The product is light yellow or yellow ointment.

dynamics

The product is rarely absorbed topically for external use, but it should be noted that it can still absorb a considerable amount when used on a large area of ulcer surface, especially when the patient's renal function is reduced or combined with other nephrotoxic or ototoxic drugs, it may still cause toxic reactions.

Indications are used for purulent skin diseases such as impetigo caused by sensitive bacteria and bacterial infections on burns and ulcers.

Dosage Apply to the affected area 2 to 3 times a day.

Adverse reactions Individual patients may cause skin irritation and may cause allergic reactions in the future when oral or topical neomycin is applied.

It is contraindicated in patients who are allergic to neomycin or other aminoglycoside antibiotics or allergic to bacitracin.

Precautions

Burned surface, granulation tissue, or huge wound with exfoliated skin can be easily absorbed when using this product, especially when the patient has renal dysfunction or other renal toxicity or ototoxic drugs are applied throughout the body, should pay attention to the possibility of toxicity, such as hematuria, urination Symptoms of nephrotoxicity such as decreased frequency, decreased or increased urine output, or symptoms of ototoxicity such as tinnitus and hearing loss.