The active substance amoxicillin: use, contraindications, analogues

Amoxicillin is an active ingredient in many popular drugs, including the drug called “Amoxicillin” presented in the pharmacy. This compound belongs to the category of antibiotics. Bactericidal qualities and antibacterial properties are inherent in it. The drug has been used for a long time and has found application in medical practice in different countries.

Pharmacology

Finding out how amoxicillin works, scientists have found that this, belonging to the penicillin class, is a drug product. It is semi-synthetic, has a wide range of performance. A positive effect is observed in the treatment of infection with a variety of gram-positive life forms. Amoxicillin can be used if necessary to eliminate staphylococci and streptococci. The compound is recommended in the fight against several anaerobic infections, including Klebsiella, Shigella, Salmonella. Amoxicillin is used for invasion of escheria, neisseria.

A medication is ineffective if a microscopic life form is capable of generating penicillinase. You can combine the drug with metronidazole. Such a two-component composition allows you to treat Helicobacter pylori infection. Scientists believe that amoxicillin inhibits the appearance of resistance of this microbe to metronidazole.

How fast is Amoxicillin

Performance Features

There is no antibiotic on sale without an active substance. Amoxicillin is one of the active compounds that ensure the effectiveness of taking antibacterial drugs. Studies have shown that if ampicillin is ineffective during infection, it is possible that agents containing amoxicillin will also not give a result. This is due to cross-resistance.

You can expand the number of cases in which amoxicillin is effective by combining it with clavulanic acid. It inhibits beta-lactamases produced by dangerous microorganisms. It is through these compounds that the active ingredient of many popular tablets loses its therapeutic effect. The combined composition is used if the analyzes showed pseudomonas, legionella, nocardia, bacteroid. Some varieties of pseudomonads, as well as various gram-negative life forms, are resistant to combination.

Kinetics

If the doctor has prescribed a course of antibiotics based on this substance, the patient is interested in how quickly amoxicillin acts. To understand this, you should turn to the pharmacological kinetics of the drug.

The ability of the compound to be rapidly absorbed during the passage of the gastrointestinal tract was clarified. The process proceeds with an increased degree of efficiency. The substance is not afraid of the acidic gastric environment, the destruction of molecules does not occur in it. The maximum concentration in serum is observed an hour or two after administration. If you double the dose relative to the standard, the concentration will also double. Eating food does not reduce absorption.

There are forms for insertion into a vein, muscle tissue. The concentrations obtained in this case in blood serum are comparable to those achieved by oral use. Instructions explaining when amoxicillin injected begins to act, pay attention to the rapid achievement of maximum concentration in the circulatory system, which means that the primary effect on microscopic organisms will be recorded faster.

Kinetics: what happens inside?

Amoxicillin, which is present in many antibacterial medicines as the main compound (active), is able to enter into strong bonds with whey proteins. The level of binding is estimated at 20%. The compound easily penetrates into liquid organic media and is well distributed in them. Achieve a high level of concentration in the liver cells.

Amoxicillin active ingredient antibiotic

Elimination

The half-life of the circulatory system takes an hour and a half. About 60% of the substance received in the body is eliminated in the initial state with urine. The main ways: glomerular filtration, secretion by tubules. When using a quarter of a gram of the drug in urine, amoxicillin is detected in an amount of 300 μg / ml. A small percentage is determined in the discharge during bowel movements.

In infants, the elderly, the half-life may increase. With kidney failure, it reaches 20 hours.

Kinetics Features

Amoxicillin is an active substance of antibacterial drugs that can penetrate the blood-brain barrier. This is observed if the focus of inflammation is localized in the soft membrane of the brain. Only a small amount of the dose received passes through the biological barrier.

It is possible to remove the compound with dialysis blood.

"Amoxicillin" active

About doses

Used in many antibacterial medicines as an active substance, amoxicillin is prescribed based on the diagnosis. Dosage is selected individually. A one-time volume for people over 10 years of age and weighing more than 40 kg varies from a quarter to half a gram. If the disease develops in severe form, you can increase the one-time volume to a gram. For children over five years of age, it is shown to use a quarter of a gram, for people over two years of age - half. If the baby is younger than two years old, the dose depends on body weight: 20 mg of the substance are taken for each kilogram.

As you can learn from the instructions for the preparations, whose active substance is amoxicillin, medicines should be used with eight-hour pauses between doses. If gonorrhea is established in acute form without complications, it is enough to use the drug once. Dose - three grams. Additionally, probenecid is prescribed.

Features

If a violation of renal functionality is detected, the treatment program is formed based on the performance of the organ. With creatinine clearance within 10-40 units between doses, 12-hour pauses are needed. If the parameter is even less, amoxicillin is used once a day.

Introduction to the muscle for adults is recommended twice a day. One-time volume - one gram. It is allowed to enter 2-12 g per day into a vein. For children, the dose is calculated based on weight: 50 mg / kg per muscle, 100-200 mg / kg per vein.

In case of renal failure, the dosage and pause between the procedures is determined based on the creatinine clearance.

"Amoxicillin" active substance

It's curious

In veterinary medicine, amoxicillin for animals is allowed. The active substance is the main component of the popular Armavir product. There are different options for release: 10%, 15%. Prescribing and administering the drug is the responsibility of the veterinarian. It is impossible to independently use amoxicillin in the treatment of a pet, since side effects and negative consequences are possible.

Is there an alternative?

In pharmacies there is a wide variety of drugs in which the active substance is amoxicillin. Other antibiotics, effective in similar infections, are analogues of such drugs. They differ not only in the main and auxiliary ingredients, but also in the form of release. There are tablets, solutions for injection, drops and syrups, powders, on the basis of which liquid for injection is prepared.

Perhaps the most popular antibiotics in modern medicine are those containing amoxicillin as the active ingredient. The analogues are ampicillin, penicillin, combined formulations ("Augmentin" and "Flemoxin Solutab"). In some cases, the doctor recommends using medicines containing sulbactam or cefazolin. The final decision is based on the sensitivity of the strain identified in the patient's body.

"Amoxicillin" how it works

Combination treatment

Preparations containing amoxicillin as the active substance (Flemoxin Solutab, Augmentin, Amosin) can be used in combination with some medicinal formulations, but only with a preliminary safety assessment. The instructions for each specific pharmaceutical product describe the limitations. Amoxicillin is known to reduce the effectiveness of birth control pills. If combined with bactericidal formulations, synergism is observed. When combined with antibiotics such as bacteriostats, antagonism occurs.

Amoxicillin increases the effectiveness of blood thinners due to indirect action. It inhibits the activity of intestinal microflora, as a result, the production of vitamin K and the time of prothrombin are weakened. The effectiveness of drugs, the transformation of which is accompanied by the generation of PABA, is reduced.

Combination: minimum risks!

When choosing a comprehensive treatment, it is taken into account that amoxicillin is combined with clavulanic acid. The kinetic parameters of these compounds are not adjusted due to each other.

If the patient is shown laxatives, glucosamine, then the antibiotic absorption efficiency decreases. This is observed if the patient takes antacids and aminoglycosides. The opposite effect is recorded with vitamin C.

Some drugs weaken the secretion of amoxicillin by the tubules of the kidneys. This can trigger an increase in the concentration of the antibiotic in the blood serum. This was fixed when combined with non-hormonal anti-inflammatory, diuretic, probenecid, allopurinol, phenylbutazone.

"Flemoxin": active substance amoxicillin

Pregnancy

Tests have shown the ability of amoxicillin to cross the placenta. A study of breast milk showed a low concentration of antibiotic in the secretion of glands. If during the period of bearing a child there is a need to use antibacterial drugs, first you need to weigh the risks and obvious benefits. Only when the second is exceeded, amoxicillin is prescribed, and the patient is previously informed of possible negative consequences. When lactating, they use the drug, but very carefully.

Unwanted effects

Like any other substance common in medical practice, amoxicillin can cause side effects. There is a likelihood of a sensitization reaction. This is manifested by angioedema, skin rashes and spots, joint pain, runny nose and inflammation of the conjunctiva. There is a danger of anaphylactic shock. The concentration of eosinophils in the blood increases. Possible erythema.

Amoxicillin intake is accompanied by the danger of superinfection. With a long course, there is a risk of a depressed state, neuropathy, convulsive state, ataxia. Some have headaches and dizzy.

When combined with clavulanic acid, the likelihood of hepatitis, jaundice, erythema, necrolysis increases. In combination with metronidazole, the risk of the formation of inflammatory foci in the tongue and mucous membranes of the mouth, as well as stool and abdominal pain, is increased.

"Amoxicillin": active substance, analogues

When not

Amoxicillin is prohibited if mononucleosis is established due to infection, a severe infectious process in the gastrointestinal tract, in which the patient vomits or is disturbed by persistent loose stools. It can not be used for lymphocytic leukemia, diathesis due to allergies, hay fever. Contraindications are hypersensitivity to amoxicillin, drugs from the class of cephalosporins, penicillins.


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