Last Updated on March 16, 2024
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What is clarithromycin?
Clarithromycin refers to antibiotics from the macrolide group. Macrolides are one of the most advanced and effective groups of antibiotics. And clarithromycin is one of the newest drugs in this group.
The active ingredient Clarithromycin belongs to a group of macrolide antibiotics and is used primarily for treatment of bacterial respiratory infections, ear and skin used. It is usually inserted into tablet form or taken twice a day. Possible Clarithromycin side effects are about digestive problems, insomnia and headaches. Here you can read all you need to know about effects and side effects of Clarithromycin, Dosage and administration.
Indications for use:
- Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation;
- Infections of the upper respiratory tract, infections of the LOP-organs (pharyngitis, sinusitis);
- Infections of the lower respiratory tract (pneumonia, bronchitis);
- Infections of the skin and soft tissues (folliculitis, phlegmon, erysipelas);
- Odontogenic infections;
- Mycobacterial infections caused by Mycobacterium avium, Mycobacterium intracellular, localized infections caused by Mycobacterium kansasii, Mycobacterium chelonae, Mycobacterium fortuitum.
- Prevention of the spread of infection caused by the complex of Mycobacterium avium (MAC), HIV-infected patients with a CD4 T-cell (T-helper lymphocyte) content of no more than 100 in 1 mm3.
To eradicate Helicobacter pylori and reduce the recurrence of duodenal ulcer.
Contraindications:
- Hypersensitivity to clarithromycin or other components of the drug;
- The first trimester of pregnancy;
- Lactation period;
- Porphyria;
- Simultaneous reception of clarithromycin with the following drugs: astemizole, cisapride, pimozide, terfenadine, ergotamine, dihydroergotamine (see Interaction with other drugs);
- Children under 12 years of age or with a body weight of less than 40 kg (for this dosage form).
With caution appoint to patients with impaired liver and kidney function.
Pregnancy and lactation
Clarithromycin is contraindicated in the first trimester of pregnancy. In the second and third trimester of pregnancy, the drug is prescribed only if there is clear evidence if the intended benefit to the mother exceeds the potential risk to the fetus. If necessary, the appointment in the lactation period should resolve the issue of stopping breastfeeding.
Mechanism of action
Clarithromycin prevents the growth of bacteria, preventing their protein synthesis. It binds to the 50S subunit of the bacterial ribosome and thereby inhibits transcription peptides.
The active ingredient Clarithromycin penetrates into the bacteria cells and prevent them from producing proteins (proteins). The bacteria are therefore not killed by the antibiotic, but only inhibited in growth – the drug is bacteriostatic. This growth inhibition of bacteria to the immune system is given the opportunity to contain the infection.
In comparison to Erythromycin, another well-known macrolide antibiotic Clarithromycin is effective against even more bacteria. Moreover, it is in contrast to Erythromycin gastric acid stable, ie does not disintegrate in the stomach. In addition, it is better tissue penetration, thus achieved the target in the body much better.
Clarithromycin is absorbed into the blood in the intestines quickly and completely. A portion of the antibiotic is metabolized in the liver. Approximately four hours after ingestion of the drug half is excreted again, namely to about three-quarters over the chair and one quarter in the urine.
Clarithromycin uses
The active substance Clarithromycin is used to treat bacterial infections with Clarithromycin-susceptible organisms, ie organisms that can be inhibited by the antibiotic in the growth. These infections often include respiratory tract infections (such as pneumonia and bronchitis), infections in the ear, nose and ears (such as almond, paranasal sinus and throat infections) and skin infections (such as wound infections, Haarbalg- / Haarfollikelentzündungen and erysipelas).
Pharmacological properties
Pharmacodynamics
Clarithromycin is a semisynthetic antibiotic of the macrolide group and has an antibacterial effect by interacting with the 50S ribosomal subunit of sensitive bacteria and suppressing protein synthesis.
It has been shown that clarithromycin exerts antibacterial action against the following pathogens:
Aerobic Gram-positive microorganisms: Staphylococcus aureus, Streptococcus pneumonia, Streptococcus pyogenes, Listeria monocytogenes.
Aerobic Gram-negative microorganisms: Haemophilus influenzae, Haemophilus parainfluenzae, Branhamella (Moraxella) catarrhalis, Neiserria gonorrhoeae, Legionella pneumophila. Other microorganisms: Mycoplasma pneumoniae, Chlamydia pneumoniae. Mycobacterium: Mycobacterium leprae, Mycobacterium kansasii, Mycobacterium chelonae, Mycobacterium fortuitum, Mycobacterium avium complex (MAC): Mycobacterium avium, Mycobacterium intracellulare.
The production of beta-lactamase does not affect the activity of clarithromycin. Most strains of staphylococcus aureus resistant to methicillin and oxacillin are resistant to clarithromycin.
Clarithromycin has an effect in vitro and against most strains of the following microorganisms: aerobic gram-positive microorganisms Streptococcus agalactiae, Streptococci (groups C, F, G), Viridans group streptococci; aerobic gram-negative microorganisms – Bordetella pertussis, Pasteurella multocida; anaerobic Gram-positive microorganisms Clostridium perfringens, Peptococcus niger, Propionibacterium acnes; anaerobic gram-negative microorganisms – Bacteroides melaninogenicus; spirochetes – Borrelia burgdorferi, Treponema pallidum; Campylobacter jejuni, Helicobacter pylori.
Pharmacokinetics
Quickly absorbed from the gastrointestinal tract after oral administration.
Absolute bioavailability is about 50%. With repeated intake of a dose of cumulation is not found, and the nature of metabolism in the human body has not changed. The intake of food immediately before taking the drug increased the bioavailability of the drug by an average of 25%. Clarithromycin can be used before meals or during meals. The connection with plasma proteins is more than 90%. After a single dose, 2 peaks of maximum concentration are recorded. The second peak is due to the ability of the drug to concentrate in the gallbladder, followed by a gradual or rapid intake into the intestine and absorption. Time to reach the maximum concentration with oral intake of 250 m g – 1-3 hours.
After oral administration, 20% of the dose is rapidly hydroxylated in the liver by cytochrome CYP3A4, CYP3A5, CYP3A7 enzymes to form the main metabolite, 14-hydroxyclarithromycin, which has a pronounced antimicrobial activity against Haemophilus influenzae. With a regular intake of 250 mg / day, the concentration of unchanged drug and its main metabolite is 1 and 0.6 μg / ml, respectively; the elimination half-life is 3-4 and 5-6 hours, respectively. When the dose is increased to 500 mg / day, the concentration of unchanged drug and its metabolite in plasma is 2.7-2.9 and 0.83-0.88 μg / ml, respectively; the half-life is 4.8-5 and 6.9-8.7 hours, respectively. In therapeutic concentrations, it accumulates in the lungs, skin and soft tissues (concentrations 10 times higher than serum levels).
It is excreted by the kidneys and through the gastrointestinal tract (GIT) (20-30% – in unchanged form, the rest – in the form of metabolites). With a single admission of 250 and 1200 mg kidneys are allocated 37.9 and 46%, through the GIT-40.2 and 29.1%, respectively.
The application must be performed exactly as your doctor or pharmacist has told you. Too short or too long application threatens the development of resistance, which means that the bacteria are resistant to Clarithromycin. In case of premature discontinuation of treatment, it may also lead to a relapse.
Dosing and How to Take Clarithromycin
Inside, regardless of food intake.
Adults and children over 12 years of age (with a body weight of more than 40 kg): the standard dose is 250 mg 2 times a day, with an interval of 12 hours. With sinusitis, severe infections, including those caused by Haemophilus influenzae, the dose can be increased to 500 mg twice a day, with an interval of 12 hours.
The average duration of treatment is 7-14 days.
For patients with hepatic impairment, the recommended dose is 250 mg every 24 hours.
For patients with renal insufficiency (creatinine clearance less than 30 ml / min.), The recommended dose is 250 mg every 24 hours or, for more severe infections, 250 mg 2 times a day, with an interval of 12 hours.
With mycobacterial infections, 500 mg of the drug is prescribed 2 times a day, with an interval of 12 hours.
With common infections caused by MAC, in AIDS patients:
The recommended dose of clarithromycin for adults and children over 12 years of age (with a body weight of more than 40 kg) is 500 mg twice a day, with an interval of 12 hours.
Treatment should continue as long as there are clinical and microbiological evidence of its usefulness. Clarithromycin should be administered in combination with other antimicrobial agents.
For the prevention of infections caused by MAC:
The recommended dose of clarithromycin for adults and children over 12 years of age (with a body weight of more than 40 kg) is 500 mg twice a day, with an interval of 12 hours.
In odontogenic infections, the dose of clarithromycin is 250 mg twice a day for 5 days.
For eradication of H. pylori
Combined treatment with three drugs:
Clarithromycin, 500 mg twice a day, in combination with lansoprazole, 30 mg twice a day, and amoxicillin, 1000 mg twice a day for 10 days.
Clarithromycin, 500 mg twice a day, in combination with amoxicillin, 1000 mg twice a day, and omeprazole, 20 mg / day, for 7-10 days.
Combination treatment with two drugs
Clarithromycin, 500 mg 3 times a day, in combination with omeprazole at a dose of 40 mg / day, for 14 days, with the appointment within the next 14 days of omeprazole at a dose of 20-40 mg / day.
Clarithromycin, 500 mg 3 times daily, in combination with lansoprazole at a dose of 60 mg / day, for 14 days. To fully heal the ulcer, an additional decrease in the acidity of the gastric juice may be required.
Typically, the drug Clarithromycin in the form of tablets is applied. For patients who have difficulty swallowing or are fed by gavage, there is also a Clarithromycin juice and granules for oral suspension. Also available are tablet with a sustained-release (prolonged-release tablets). They need to be taken once a day, in contrast to normal tablets.
The usual duration of use is six to 14 days, depending on the severity of the infection. The Clarithromycin dose is 250 milligrams twice daily Clarithromycin. In severe infections, however, the doctor can also double this dosage.
Clarithromycin should be applied over the entire duration of treatment prescribed by the doctor. Even if symptoms improve earlier, the patient may not settle by hand (risk of development of resistance and relapse!).
For the treatment of Helicobacter pylori infection (a bacterium that can cause stomach ulcers) is Clarithromycin in combination with another antibiotic and a proton pump inhibitor used (for inhibiting gastric acid production). This triple therapy is provided only for that particular infection.
Clarithromycin side effects
On the part of the digestive system: decreased appetite, nausea, vomiting, diarrhea, abdominal pain, stomatitis, glossitis, pancreatitis, discoloration of the tongue and teeth; extremely rarely pseudomembranous enterocolitis. The discoloration of the teeth is reversible and is usually restored by a special treatment in the dental clinic. As with the administration of other antibiotics from the macrolide group, liver function abnormalities are possible, including an increase in hepatic enzyme activity, hepatic cell and / or cholestatic hepatitis with or without jaundice. These violations of the liver can be severe, but usually they are reversible. Very few cases of hepatic insufficiency and death were observed, mainly on the background of severe co-morbidities and / or concomitant drug therapy.
From the side of the nervous system: dizziness, headache, paresthesia, smell disorders, change in taste, excitement, insomnia, nightmares, feelings of fear, ringing in the ears; rarely – disorientation, hallucinations, psychosis, depersonalization, confusion.
From the side of the cardiovascular system: as with the reception of other macrolides, prolongation of the QT interval, ventricular tachycardia; polymorphic ventricular tachyarrhythmia (torsade de pointe).
On the part of the organs of hematopoiesis and hemostasis system: rarely – leukopenia and thrombocytopenia (unusual bleeding, hemorrhage). From the musculoskeletal system: arthralgia, myalgia.
From the side of the urinary system: individual cases of increased plasma creatinine, interstitial nephritis, kidney failure.
Allergic reactions: skin hyperemia, urticaria, skin rash, angioedema, bronchospasm, eosinophilia; rarely anaphylactic shock, Stevens-Johnson syndrome.
Other: increased body temperature, possible development of superinfection, candidiasis, development of resistance of microorganisms.
The side effects in the digestive tract caused by the fact that the antibiotic against the beneficial intestinal bacteria acts. This affects the digestive system.
Cautions
What should I assess when taking Clarithromycin?
The active ingredient Clarithromycin has similar interactions with other macrolide antibiotics, such as Erythromycin. Because it is metabolized in the liver by an enzyme which degrades other drugs can lead to mutual interference. Thus, with concurrent use – even at different times of the day – too low or too high arise drug levels in the body. The drugs affected then either do not work or accumulate so much in the body, toxic effects. Concomitant administration of Clarithromycin and these drugs should be discussed in advance with the doctor or pharmacist.
Examples of such agents are:
- Oral diabetes medications (hypoglycemic agents) such as pioglitazone, repaglinide, rosiglitazone
- anticoagulant like warfarin, warfarin
- statins (cholesterol-lowering drug) such as lovastatin, Simvastatin
- allergy agents (antihistamines) as terfenadine
- migraine such as ergotamine
- remedy (antiepileptic drugs) such as Phenytoin, Carbamazepine
- antifungal (antifungal), like Fluconazole, ketoconazole
- HIV medications such as ritonavir, efavirenz, nevirapine
- heart medicines like Digoxin, Verapamil, Nifedipine
- gout agents such as colchicine
- remedy for erectile dysfunction such as sildenafil, tadalafil, vardenafil, Avanafil
Simvastatin: updated advice on drug interactions.
Clarithromycin may already be used in neonates (in accordance with low dosage). Older people may also take the antibiotic, unless there is evidence hepatic impairment.
If the doctor considers it necessary to reflect, the antibiotic can be applied during pregnancy and lactation.
Some new information:
Antibiotic taken by millions is linked to heart deaths: Treatment.
How to get Clarithromycin online?
Clarithromycin requires a prescription in each dose and to apply only in pharmacies, but you can buy Clarithromycin citrate online from UK.
Since when Clarithromycin is known?
Clarithromycin was developed along the lines of the antibiotic Erythromycin in the ’70s by the Japanese pharmaceutical company Taisho Pharmaceutical. In 1980, the drug was patented and marketed since 1991 in Japan. Later that year, the antibiotic has been approved by cooperation with the US pharmaceutical company Abbott Laboratories first in the USA and later worldwide. In Europe in 2004 ran out of patent protection in the United States in 2005. Subsequently, brought many manufacturers with the generic active ingredient Clarithromycin on the market.
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