Clindamycin: MedlinePlus Drug Information

pronounced as (klin” da mye’ sin)

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Many antibiotics, including clindamycin, may cause overgrowth of dangerous bacteria in the large intestine. This may cause mild diarrhea or may cause a life-threatening condition called colitis (inflammation of the large intestine). Clindamycin is more likely to cause this type of infection than many other antibiotics, so it should only be used to treat serious infections that cannot be treated by other antibiotics. Tell your doctor if you have or have ever had colitis or other conditions that affect your stomach or intestines.

You may develop these problems during your treatment or up to several months after your treatment has ended. Call your doctor if you experience any of the following symptoms during your treatment with clindamycin or during the first several months after your treatment has finished: watery or bloody stools, diarrhea, stomach cramps, or fever.

Talk to your doctor about the risks of taking clindamycin.

Clindamycin is used to treat certain types of bacterial infections, including infections of the lungs, skin, blood, female reproductive organs, and internal organs. Clindamycin is in a class of medications called lincomycin antibiotics. It works by slowing or stopping the growth of bacteria.

Antibiotics such as clindamycin will not work for colds, flu, or other viral infections. Using antibiotics when they are not needed increases your risk of getting an infection later that resists antibiotic treatment.

Clindamycin comes as a capsule and a solution (liquid) to take by mouth. It is usually taken three to four times a day. The length of your treatment depends on the type of infection you have and how well you respond to the medication. Take clindamycin at around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take clindamycin exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Shake the liquid well before each use to mix the medication evenly.

Take the capsules with a full glass of water so that the medication will not irritate your throat.

You should begin to feel better during the first few days of treatment with clindamycin. If your symptoms do not improve or if they get worse, call your doctor.

Take clindamycin until you finish the prescription, even if you feel better. If you stop taking clindamycin too soon or skip doses, your infection may not be completely treated and the bacteria may become resistant to antibiotics.

Clindamycin is also sometimes used to treat acne and is used along with other medications to treat anthrax (a serious infection that may be deliberately spread as part of a terror attack) and malaria (a serious infection that is spread by mosquitoes in certain parts of the world). Clindamycin is also sometimes used to treat ear infections, tonsillitis (infection that causes swelling of the tonsils), pharyngitis (infection that causes swelling in the back of the throat), and toxoplasmosis (an infection that may cause serious problems in people who do not have healthy immune systems or in unborn babies whose mothers are infected) when these conditions cannot be treated with other medications. Clindamycin is also sometimes used to treat bacterial vaginosis (an infection caused from too much of certain bacteria in the vagina). Clindamycin is also sometimes used to prevent endocarditis (infection of the heart valves) in certain people who are at risk of developing this infection as a result of a dental procedure. Talk to your doctor about the risks of using this medication for your condition.

This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

Before taking clindamycin,

• tell your doctor and pharmacist if you are allergic to clindamycin, lincomycin (Lincocin), any other medications, or any of the ingredients in clindamycin capsules or solution. Ask your pharmacist for a list of the ingredients. If you will be taking clindamycin capsules, tell your doctor if you are allergic to aspirin or tartrazine (a yellow dye found in some medications).
• tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention clarithromycin (Biaxin, in PrevPac), erythromycin (E.E.S, E-Mycin, Erythrocin, others), indinavir (Crixivan), itraconazole (Sporanox), ketoconazole (Nizoral), nefazodone, nelfinavir (Viracept), rifampin (Rifadin, in Rifamate, in Rifater, Rimactane), and ritonavir (Norvir, in Kaletra). Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Many other medications may also interact with clindamycin, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
• tell your doctor if you have or have ever had asthma, allergies, eczema (sensitive skin that often becomes itchy or irritated) or kidney or liver disease.
• tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking clindamycin, call your doctor.
• if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking clindamycin.

Unless your doctor tells you otherwise, continue your normal diet.

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Clindamycin may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

• nausea
• vomiting
• unpleasant or metallic taste in the mouth
• joint pain
• pain when swallowing
• heartburn
• white patches in the mouth
• thick, white vaginal discharge
• burning, itching, and swelling of the vagina

Some side effects can be serious. If you experience any of these symptoms or those listed in the IMPORTANT WARNING section, call your doctor immediately or get emergency medical treatment:

• peeling or blistering skin
• rash
• hives
• itching
• difficulty breathing or swallowing
• hoarseness
• swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
• yellowing of the skin or eyes
• decreased urination

Clindamycin may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Do not refrigerate clindamycin liquid because it may thicken and become hard to pour. Dispose of any unused clindamycin liquid after 2 weeks.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.

• Cleocin^®

Last Revised – 05/15/2018

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Clindamycin Uses, Dosage & Side Effects

Generic name: clindamycin (oral/injection) [ klin-da-MYE-sin ]
Brand names: Cleocin HCl, Cleocin Pediatric, Cleocin Phosphate, Cleocin Phosphate ADD-Vantage, Clindesse, ClindaMax Vaginal
Drug class: Lincomycin derivatives

Medically reviewed by Carmen Pope, BPharm. Last updated on May 3, 2023.

What is clindamycin?

Clindamycin is an antibiotic that fights bacteria in the body.

Clindamycin is used to treat serious infections caused by bacteria.

Clindamycin is usually available as one of three salts: clindamycin phosphate, clindamycin hydrochloride, or clindamycin nicotinamide. These salt forms are all prodrugs of clindamycin but once inside the body or applied to the skin, they are rapidly converted to active clindamycin by hydrolysis. All three salt forms of clindamycin: clindamycin phosphate, clindamycin hydrochloride, and clindamycin nicotinamide have the same antimicrobial spectrum and effectiveness.

Clindamycin phosphate salts are usually used for intravenous, intramuscular, and topical formulations of clindamycin. Clindamycin hydrochloride salts are usually used for oral forms of clindamycin, and clindamycin nicotinamide is another topical form of clindamycin.

Clindamycin may also be used for purposes not listed in this medication guide.

Warnings

Clindamycin can cause diarrhea, which may be severe or lead to serious, life-threatening intestinal problems. If you have diarrhea that is watery or bloody, stop using this medicine and call your doctor.

Before using clindamycin, tell your doctor if you have kidney disease, liver disease, an intestinal disorder such as colitis or Crohn’s disease, or a history of asthma, eczema, or allergic skin reaction.

Take clindamycin for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Clindamycin will not treat a viral infection such as the common cold or flu.

Before taking this medicine

You should not use this medicine if you are allergic to clindamycin or lincomycin.

To make sure clindamycin is safe for you, tell your doctor if you have ever had:

• colitis, Crohn’s disease, or other intestinal disorder;

• eczema, or allergic skin reaction;

• liver disease;

• asthma or a severe allergic reaction to aspirin;

• an allergy to yellow food dye.

Animal studies have not shown any harm during pregnancy, but in humans, it is not known whether clindamycin will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

Clindamycin does pass into breast milk and may cause side effects in the nursing baby. If you are breastfeeding while taking this medicine, call your doctor if your baby has diaper rash, redness or white patches in the mouth or throat, stomach discomfort, or diarrhea that is watery or bloody. Let your doctor know if you are breastfeeding before taking clindamycin.

Clindamycin injection may contain an ingredient that can cause serious side effects or death in very young or premature babies. Do not give this medicine to a child without medical advice.

How should I use clindamycin?

Take clindamycin exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.

Clindamycin oral is taken by mouth. Clindamycin injection is injected into a muscle, or as an infusion into a vein. A healthcare provider will give your first dose and may teach you how to properly use the medication by yourself.

Take the capsule with a full glass of water to keep it from irritating your throat.

Measure liquid medicine carefully. Use the dosing syringe provided, or use a medicine dose-measuring device (not a kitchen spoon).

You may need frequent medical tests during treatment.

If you need surgery, let your surgeon know you use clindamycin as it may interact with certain drugs used for anesthesia.

Use this medicine for the full prescribed length of time, even if your symptoms quickly improve. Skipping doses can increase your risk of infection that is resistant to medication. Clindamycin will not treat a viral infection such as the flu or a common cold.

Store at room temperature away from moisture and heat. Protect the injectable medicine from high heat.

Do not store the oral liquid in the refrigerator. Throw away any unused oral liquid after 2 weeks.

What happens if I miss a dose?

Use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while using clindamycin?

Do not use clindamycin at the same time as the antibiotic, erythromycin.

Clindamycin side effects

Antibiotic medicines can cause diarrhea, which may be a sign of a new infection. If you have diarrhea that is watery or bloody, stop using clindamycin and call your doctor. Do not use anti-diarrhea medicine unless your doctor tells you to.

Get emergency medical help if you have any signs of an allergic reaction to clindamycin: (hives, difficult breathing, swelling in your face or throat) or a severe skin reaction (fever, sore throat, burning in your eyes, skin pain, red or purple skin rash that spreads and causes blistering and peeling).

Seek medical treatment if you have symptoms of a serious drug reaction that can affect many parts of your body. Symptoms may include: skin rash, fever, swollen glands, flu-like symptoms, muscle aches, severe weakness, unusual bruising, or yellowing of your skin or eyes. This reaction may occur several weeks after you began using clindamycin.

Clindamycin can cause diarrhea, which may be severe or lead to serious, life-threatening intestinal problems. If you have diarrhea that is watery or bloody, stop using clindamycin and call your doctor.

Call your doctor at once if you have:

• any change in bowel habits;

• severe stomach pain, diarrhea that is watery or bloody;

• little or no urination; or

• a metallic taste in your mouth (after clindamycin injection).

Common clindamycin side effects may include:

• nausea, vomiting, stomach pain;

• mild skin rash; or

• vaginal itching or discharge;

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect clindamycin?

Other drugs may interact with clindamycin, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Popular FAQ

There are several antibiotics that kill the common mouth bacteria that cause tooth infections. The best (first-line) antibiotics for tooth infection include: Amoxicillin, Penicillin, Cephalexin, Clindamycin, Azithromycin. Amoxicillin is often the first choice because it is widely effective and has the fewest gastrointestinal side effects. Continue reading

Penicillin or amoxicillin are considered the best first-line treatments for Strep throat. According to the CDC (Centers for Disease Control and Prevention) “ There has never been a report of a clinical isolate of group A strep that is resistant to penicillin”. For people with a penicillin allergy, treat Strep throat with either a narrow-spectrum cephalosporin (such as cephalexin or cefadroxil), clindamycin, azithromycin, or clarithromycin. Note that resistance to azithromycin and clarithromycin has been reported. Continue reading

Clindamycin is a strong broad-spectrum antibiotic, typically prescribed for serious infections, such as life-threatening methicillin-resistant Staphylococcus aureus (MRSA) skin infections. Continue reading

Yes, you can. It is recommended that the use of the antibiotic clindamycin be reserved for patients who are allergic to penicillin or for those patients a healthcare provider determines penicillin to be an inappropriate treatment. Continue reading

No, clindamycin is not a penicillin antibiotic. Instead, it belongs to a class of medications known as lincomycin antibiotics, or lincosamides. Clindamycin is a broad-spectrum antibiotic, with the ability to impact many types of bacteria in the body. Continue reading

More FAQ

• Why can’t you lay down after taking clindamycin?
• Can clindamycin be used to treat chlamydia?

View more FAQ

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• Advanced Reading
• Clindamycin (Oral) (Advanced Reading)
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Other brands

Cleocin, Cleocin Pediatric, Cleocin Phosphate, Cleocin HCl

Professional resources

• Prescribing Information

Related treatment guides

• Aspiration Pneumonia
• Babesiosis
• Bacteremia
• Bacterial Endocarditis Prevention

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medicine only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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Azithromycin: instruction, price, analogues | Compendium – drug guide

The year is 1980. Dr. Slobodan Rokeach and his research team at Pliva (a pharmaceutical company in Croatia) have discovered Azithromycin. A patent for it was obtained a year later. And then, using the Pliva license, Pfizer brings the drug to the pharmaceutical markets and already under a completely different trade name. And this happens in 10 years. A few more years passed. And they approved a new formulation of azithromycin for the treatment of eye infections.

Azithromycin is practically insoluble in water and freely soluble in anhydrous ethanol and methylene chloride. Azithromycin is a macrolide antibiotic. It is a semi-synthetic derivative of erythromycin. Azithromycin differs from erythromycin by the addition of a methyl-substituted nitrogen atom to the lactone ring. This structural modification increased the acid resistance of the compound and improved the penetration of the drug molecule into tissues, expanding its spectrum of action. Macrolides are generally distinguished by their activity, covering a wide range of Gram-positive and Gram-negative bacterial species, including intracellular pathogens such as Chlamydia and Legionella. They exhibit their antibiotic activity by binding to the 50S ribosome (its subunit) and inhibiting protein synthesis. Modern antibacterial drugs are intended not only for inpatient treatment, but also for outpatient use. But at the same time, patients often do not comply with the drug regimen or the total duration of the course of treatment. In turn, this can lead to chronic bacterial inflammation or to the development of antibiotic resistance in bacteria. That is why preference is given to drugs with a simple regimen (1 r / day) with a long T _½ , which reduces the duration of the course of treatment. Such drugs make it possible to achieve the complete elimination of the bacterial pathogen and are even able to prevent the exacerbation of chronic diseases. Azithromycin meets all these requirements.

Compared with other macrolide drugs, azithromycin has a number of advantages in terms of pharmacokinetics, pharmacodynamics, as well as safety and tolerability in both adult and pediatric practice. It demonstrates time-dependent bacteriostatic or bactericidal activity, and at the same time shows concentration-dependent bactericidal activity and a pronounced post-antibacterial effect (Matzneller P., 2013). After oral administration, the drug is distributed throughout the body, with C _max is achieved in 2–3 hours, and the tissue concentration exceeds the serum concentration by 50 times (instruction of the Ministry of Health of Ukraine). At the same time, azithromycin accumulates mainly in the extracellular space of muscle tissue and subcutaneous adipose tissue, as well as in fibroblasts and tissue phagocytes. The concentration of azithromycin in the lung tissue can be characterized as high or very high, which ensures the effectiveness of the drug against most respiratory bacterial infections (Leophonte P. , 1995). The post-antibacterial effect of azithromycin lies in the fact that its molecules strongly bind to tissue proteins and T _½ is 5 days after the completion of the course of treatment, and in some patients it reached 10 days (Matzneller P., 2013).

The spectrum of antibacterial activity of azithromycin covers methicillin-susceptible strains of staphylococcus, penicillin-susceptible strains of streptococcus, hemophilic infection, moraxella and pasteurella, as well as intracellular pathogens such as chlamydia and legionella (Neu H.C., 1991). In addition, azithromycin is active against anaerobic bacteria such as clostridia and fusobacteria.

The group of bacteria resistant to azithromycin is represented by penicillin-resistant streptococci, methicillin-resistant Staphylococcus aureus, bacteroids and the overwhelming majority of gram-negative bacteria. Cross-resistance to azithromycin is observed in pathogens resistant to erythromycin, other macrolides and lincosamides (instruction of the Ministry of Health of Ukraine).

Azithromycin pharmacology and therapy

Azithromycin has been found to be less active than erythromycin against Gram-positive bacteria, but more effective against some Gram-negative organisms such as Haemophilus influenzae, Moraxella catarrhalis, and also has activity against some enterobacteria such as Escherichia coli and Salmonella and Shigella species, as well as against Legionella pneumophila, B. burgdorferi, Mycoplasma pneumoniae. He (azithromycin) has increased activity against Mycobacterium avium-intracellulare, as well as some protozoa (eg Cryptosporidium and Plasmodium species), excellent action against Toxoplasma gondii, kills cysts. It is more active than erythromycin against Chlamydia trachomatis and Ureaplasma urealyticum.

Mechanism of action. It is a bacteriostatic agent that inhibits protein synthesis by reversibly binding to the 50S ribosomal subunits of susceptible microorganisms. The cells of the body are much more permeable to the dosage form of the drug, which is likely to exhibit increased antimicrobial activity at an alkaline pH.

Macrolide resistance. Generally, resistance to macrolides is mediated by the following mechanisms:

• ribosomal protection through inducible or constitutive production of methylase enzymes mediated by the expression of (ermA), (ermB), and (ermC), which modify the ribosomal target and reduce drug binding;
• hydrolysis by esterases produced by Enterobacteriaceae;
• chromosomal mutations that alter the 50S ribosome subunit protein (noted in B. subtilis, Campylobacter species, mycobacteria, and Gram-positive cocci).

Action other than antimicrobial effects. Studies have indicated the activity of Azithromycin as a promising drug for the treatment of gastroparesis and gastrointestinal motility disorders.

• One study showed that azithromycin may be effective against asthma (late onset).
• Information has been obtained on the effectiveness of azithromycin against malaria when used in combination with artemisinin or quinine sulfate. Azithromycin-artemisinin, even if taken only once a day (3 days), and azithromycin-quinine sulfate – 3 times a day. These drug combinations have been relatively safe and effective in uncomplicated malaria and deserve further study in specific patient populations.
• Ischemic heart disease: macrolide antibacterial agents, including Azithromycin.

Clarithromycin, roxithromycin, azithromycin have been investigated for the prevention of coronary artery disease based on the proposed association between atherosclerosis and Chlamydophila pneumoniae (Chlamydia) infection. Although the preliminary results of some experimental studies have been promising, long-term studies in a large number of patients have been disappointing, and none of the three macrolides reduced ischemic outcomes or provided a clinical benefit. In one study, an unexpected increase in cardiovascular mortality was observed with clarithromycin.

• Gingival hyperplasia: azithromycin has a positive effect on the treatment of gingival hyperplasia, which was caused by the use of cyclosporine, especially when it (azithromycin) is introduced early in the inflammation process.
• Cystic fibrosis: Azithromycin is widely used in cystic fibrosis, with evidence demonstrating decreased lung function and exacerbation rates. This immunomodulatory therapy likely interferes with Pseudomonas aeruginosa biofilm growth.

ADME (absorption, distribution, metabolism, and excretion) profile. Orally administered azithromycin is rapidly absorbed and widely distributed throughout the body except the brain and cerebrospinal fluid. Peak plasma concentrations are reached 2-3 hours after oral administration. A loading dose of 500 mg will give a peak plasma drug concentration of 0.4 g/mL. When the loading dose is 250 mg 1 time per day for 4 days, then in a stationary state, the peak concentration of the drug is 0.24 g / ml. Azithromycin can also be administered intravenously, producing plasma concentrations of 3–4 g/mL following a 1-hour infusion of 500 mg. Absorption from capsules decreases with food. The unique pharmacokinetic properties of the drug are extensive redistribution in tissues and high concentrations of the drug in cells (including phagocytes). This leads to an increase in the concentration of the drug in the tissues, when compared with simultaneous concentrations in the blood serum. Tissue fibroblasts act as a natural drug reservoir in vivo.

Animal data show that azithromycin crosses the placenta. At very low plasma concentrations, this represents 50% of the amount of protein. Azithromycin undergoes demethylation in the liver to an inactive metabolite, but excretion is carried out by the biliary tract – the main route. Only 12% of the drug is excreted unchanged in the urine. Half-life (T _½ ) – 40-68 hours

Adverse reactions. Anorexia, dyspepsia, flatulence, dizziness, headache, drowsiness, convulsions, arthralgia and taste and smell disorders; rarely – constipation, hepatitis, liver failure, syncope, insomnia, agitation, restlessness, asthenia, paresthesia, hyperactivity, thrombocytopenia, hemolytic anemia, interstitial nephritis, acute renal failure, photosensitivity, discoloration of the lips and tongue.

Drug interactions. It is not recommended to use Azithromycin in combination with antacids containing aluminum or magnesium. Salts can reduce the rate, but not the extent of its absorption;

Azithromycin should be given at least 1 hour before or 2 hours after an antacid.

• Serum concentrations of azithromycin are markedly increased when given with nelfinavir.
• Azithromycin capsules should not be administered with food because this reduces the availability of the drug itself.
• Azithromycin possibly enhances the anticoagulant effect of coumarins.
• Azithromycin possibly increases the concentration of theophylline in blood plasma (Bakheit A.H., 2014).

Clinical experience with azithromycin

Clinical use and dosing (see instructions of the Ministry of Health of Ukraine).

1. respiratory infections;

2. skin and soft tissue infections;

3. chlamydial infections;

4. mild or moderate non-gonococcal urethritis;

5. otitis media;

6. typhoid fever due to multiple antibacterial resistant organisms;

7. prophylaxis of group A streptococcal infection;

8. as a prophylactic treatment for bacterial endocarditis in patients undergoing dental procedures at high risk of developing endocarditis;

whooping cough;

10. mycobacterial infections.

• Treatment or prophylaxis of Mycobacterium avium intracellular infection in AIDS patients requiring higher doses: 600 mg per day in combination with one or more other drugs for treatment or 1200 mg once a week for primary prevention.
• Azithromycin is prescribed for the treatment of sexually transmitted diseases, especially during pregnancy, when tetracyclines are contraindicated. Treatment for uncomplicated nongonococcal urethritis suspected to be C. trachomatis is a single dose (1 g) of azithromycin. This dose is also effective in chancroid.
• Azithromycin (1 g/week for 3 weeks) is an alternative regimen for the treatment of inguinal or venous lymphogranuloma.
• Uncomplicated genital chlamydial infections and non-gonococcal urethritis, 1 g as a single dose.
• Typhoid fever, 500 mg once a day (total number of days of taking the drug – 7).

Systematic reviews contain a wealth of information on the use and safety of Azithromycin in various therapeutic areas.

Here is information on several studies that, in our opinion, may be of interest.

Long-term therapy with azithromycin has been shown to reduce exacerbations of chronic obstructive pulmonary disease (COPD) and is indicated according to the latest recommendations for patients with COPD who are at risk of recurrent exacerbations. However, concerns about adverse effects limit its widespread use. Physicians deciding whether to use long-term azithromycin therapy should evaluate each patient’s individual risk of cardiovascular events and the individual and population impact of macrolide resistance versus expected benefit. This review will summarize data on the efficacy and safety of chronic azithromycin for the prevention of COPD exacerbations (Taylor S. P., 2015).

The FDA updated the package labeling of azithromycin to include the risk of prolonged cardiac repolarization and prolongation of the QT interval, which increases the risk of cardiac dysrhythmias, especially in the elderly. The update was initiated by a study that found an increased risk of death in patients taking azithromycin compared to patients taking amoxicillin. However, the cardiovascular results of other studies of azithromycin have been inconsistent, so more research is needed. At the same time, specialists should recognize that azithromycin plays a role in the treatment of bacterial infections, and should prescribe an antibiotic if necessary (Sutton S.S., 2017).

Azithromycin is widely used as a first-line drug for the treatment of children with mycoplasmal pneumonia, although children often vomit in the pediatric ward as a result of oral administration. It is believed that drugs that are administered rectally enter the circulatory system without first passing through the liver. Therefore, 5 healthy volunteers were included in the study. All participants gave written informed consent to participate in the study. Either oral administration of a 500 mg Azithromycin tablet or rectal administration of a suppository of the same preparation 125 was randomly assigned; 250 or 500 mg. Blood samples for serum preparation were taken before and after 1; 2; 3; 4; 6; 12 and 24 hours after the first rectal dose. Serum azithromycin concentrations were determined by high performance liquid chromatography (HPLC) with electrochemical detection.

Thus, the bioavailability of the suppository when administered rectally was 20.3% compared to oral administration. It is assumed that the surface area where the active substance is absorbed also affects the absorption when administered rectally. Although further research is needed to improve rectal absorption and child safety, azithromycin suppositories may already be effective in cases where oral administration is not allowed (Maeda M. et al., 2016).

Antibacterial therapy with azithromycin is widely used in modern medical practice: the drug is effective for middle ear infections, tonsillitis, pneumonia, typhoid, bronchitis and sinusitis. In addition, it is effective against some STDs – it is included in the treatment regimens for non-gonococcal urethritis, cervicitis and chlamydia (Bakheit A., 2014). Azithromycin is successfully used for the treatment of chlamydial cervicitis and urethritis, and its single dose is comparable in its effectiveness to a 7-day course of doxycycline treatment (Katanani M.S., 1994).

According to a prospective study, it was found that a 5-day course of azithromycin can be considered quite sufficient for the treatment of erythema migrans in tick-borne borreliosis (Arnez M., 2015).

Interestingly, azithromycin has been shown to be effective against typhus in 5 clinical trials, with activity comparable to that of other anti-rickettsial drugs. Azithromycin is an effective alternative to doxycycline, which is contraindicated, for example, in pregnant women or young children (Lee S. C., 2017).

Azithromycin is recommended for the treatment of obstructive bronchiolitis, obstructive airway injury associated with lung or allogeneic stem cell transplantation. Meta-analysis data suggest that when it is included in the treatment regimen, there is a small but statistically significant increase in such an indicator as forced expiratory volume in the first second. The therapeutic effect is associated with the fact that under the influence of azithromycin, the secretion of interleukin-8 by alveolar macrophages decreases, the activity of fibroblast matrix metalloproteases decreases, the survival of neutrophils and the general microbial contamination of the lungs decrease (Yadav H., 2016). In addition, studies of in vitro and in animals it was found that azithromycin acts like an inhibitor of nuclear factor κβ and inhibits the maturation of dendritic cells, thereby reducing the severity of the graft versus host reaction (Iwamoto S., 2013).

In a randomized, double-blind, placebo-controlled trial (3 years), it was found that the use of azithromycin as an antibiotic prophylaxis helps to reduce the number of chronic lung infections in patients with primary antibody deficiency (Milito C. , 2019).

Azithromycin is also recommended for the prevention of exacerbations in patients with fibrous bronchiectasis – its systematic use improves the quality of life in patients who have experienced at least one exacerbation per year without therapy (Wong C., 2012).

The effectiveness of azithromycin for the treatment and prevention of whooping cough has been proven (Devasia R., 2009) – it is recommended as an alternative first-line drug. The high efficacy of azithromycin in the treatment of legionella pneumonia has also been established – it has been proven not only in animal models, but also in clinical studies (Plouffe J.F., 2003).

According to a systematic review, it was found that azithromycin can be prescribed to premature babies – the antibiotic significantly reduces the risk of developing bronchopulmonary dysplasia in them (Smith C., 2015). The ability of azithromycin to prevent the development of chronic pulmonary pathology during intrauterine infection with ureaplasma has been proven (Turner M. A., 2012). Azithromycin is also used in pediatric practice for the treatment of mycoplasmal pneumonia (Wang J., 2018). It is very important that azithromycin therapy is well combined with probiotic preparations based on Saccharomyces boulardii – with this combination, the cure for mycoplasmal pneumonia is accelerated and the frequency of intestinal dysbacteriosis is reduced (Chen Q.F., 2018).

Azithromycin has proven itself in dermatological practice. For the treatment of chronic furunculosis – recurrent staphylococcal abscesses of hair follicles – it is recommended to use the drug for a 12-week course at a dosage of 500 mg / week. This treatment regimen makes it possible to achieve stable remission after 3 months in 79 patients..2% of patients (Amynzadeh A., 2007).

The literature describes the successful treatment of cutaneous leishmaniasis with azithromycin. At the same time, the drug was prescribed in the regimen of 500 mg/day for 10 days (Minodier P. , 2008).

Data from a meta-analysis suggest the possibility of including azithromycin in a triple therapy regimen for peptic ulcer disease. Azithromycin after a single dose accumulates in the gastric mucosa, is secreted with gastric juice and reaches a sufficient concentration for eradication Helicobacter pylori (Dong J., 2009).

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Lincomycin: instruction, price, analogues | capsules Kievmedpreparat

• Pharmacological properties
• Indications Lincomycin
• Application Lincomycin
• Contraindications
• Side effects
• Special instructions
• Interactions
• Overdose
• Storage conditions
• Diagnosis
• Recommended alternatives
• Trade names

pharmacodynamics

Sensitivity. Depending on the sensitivity of the pathogen and the concentration of the antibiotic, lincomycin can have both bactericidal and bacteriostatic effects.

The table below shows the MIC values ​​obtained from the literature. The spread of resistance may change over time and by region.

*Lincomycin is inactive against H. influenzae , enterococci and species of the genus Neisseria (see INDICATIONS).

In vitro observed the phenomenon of cross-resistance in a dissociated type between clindamycin and lincomycin on the one hand and antibiotics of the macrolide group (erythromycin, clarithromycin, azithromycin) on the other. There is absolute cross-resistance between lincomycin and clindamycin. In studies in vitro and in vivo did not show rapid development of resistance. In staphylococci, resistance to lincomycin or clindamycin in vitro develops gradually. Studies indicate the absence of common antigenic properties of lincomycin and penicillins.

Pharmacokinetics

Suction . When taken orally on an empty stomach, 20-30% of the drug is absorbed. With oral administration of 500 mg of lincomycin, C _max in serum is about 3 μg / ml and is reached 2-4 hours after application. If lincomycin is taken with food, this figure is reduced by about 50%. After oral administration, the therapeutic concentration of the drug in the blood is maintained for 6-8 hours for the most sensitive gram-positive pathogens.

Distribution . Based on published studies, it has been established that the binding of the drug to plasma proteins has a saturation pattern, that is, the percentage of bound drug decreases with increasing serum concentration of the drug.

The concentration of the drug in the blood of the fetus, in the peritoneal and pleural fluid can reach 25-50% of the concentration in the blood, in breast milk – 50-100%, in bone tissue – about 40%, and in soft tissues – 75% of the concentration in blood.

However, lincomycin slowly penetrates into the cerebrospinal fluid (1-18% of the concentration in the blood). With meningitis, an increase in the level of the drug to about 40% of the concentration in the blood was observed.

Removal. Much of the drug’s metabolism occurs predominantly in the liver. Normally, T _½ from blood serum is 5.4 ± 1 hour. In case of impaired liver and / or kidney function, this time may increase, so patients with impaired liver and / or kidney function should consider the possibility of reducing the frequency of lincomycin.

After a single oral dose of 500 mg of the drug, the excretion of the microbiologically active form in the urine is 1-31% (mean – 4%), and in the feces – up to 33%.

Given that the concentration of the drug in the bile can be 10 times the level of the drug in the blood, excretion in the bile is undoubtedly an important route of excretion of the drug from the body when taken orally.

Residues of the drug are excreted as microbiologically inactive metabolites. Hemodialysis and peritoneal dialysis procedures do not affect the elimination of lincomycin from the blood.

Lincomycin is indicated for the treatment of infections caused by strains of gram-positive aerobic microorganisms susceptible to lincomycin, such as streptococci, pneumococci and staphylococci, or by susceptible anaerobic bacteria:

1. Upper respiratory tract infections: chronic sinusitis caused by anaerobic strains. Lincomycin can be used in selected cases of suppurative otitis media or as adjunctive therapy along with an antibiotic that is effective against aerobic gram-negative pathogens. Infections caused by H.influenzae are not an indication for the use of the drug (see pharmacodynamics ).

2. Infections of the lower respiratory tract, including infectious exacerbations of chronic bronchitis and infectious pneumonia.

3. Infections of the skin and soft tissues caused by susceptible microorganisms, in cases where the administration of antibiotics of the penicillin group is not indicated.

4. Bone and joint infections, including osteomyelitis and septic arthritis.

5. Septicemia and endocarditis. In some cases of septicemia and / or endocarditis due to the sensitivity of pathogens to lincomycin, a pronounced response to treatment with lincomycin was observed. However, in the treatment of such infections, the use of bactericidal drugs has an advantage.

dose and route of administration should be determined taking into account the severity of the infection, the condition of the patient and the sensitivity of the bacterial pathogen. The duration of treatment is determined individually by the doctor.

The drug is preferably taken 1-2 hours before or 1-2 hours after a meal. Hard capsules should be taken with plenty of water.

Adults. 500 mg 3-4 times daily.

Children (age 6+) . 30-60 mg / kg / day, which are divided into 3-4 equal doses.

Patients with impaired renal and/or hepatic function . If necessary, the use of lincomycin for the treatment of patients with severely impaired renal and / or liver function, the appropriate dose is 25-30% of the dose recommended for patients with unchanged kidney / liver function.

Children . Do not prescribe the drug in this dosage form (capsules) to children under the age of 6 years.

hypersensitivity to the active substance or to any other component of the preparation, or to clindamycin. Meningitis.

from the gastrointestinal tract : abdominal pain, nausea, vomiting and antibiotic-associated diarrhea (see SPECIAL INSTRUCTIONS), esophagitis, glossitis, stomatitis, anal itching. Almost all antibiotics, including penicillins, cephalosporins and lincosamides, can lead to the development of severe diarrhea (sometimes the onset of diarrhea is preceded by a latent period), colitis, including pseudomembranous, caused by the action of toxins C.difficile . If diarrhea occurs during treatment, the drug should be discontinued gradually. Colitis may also develop 2-3 weeks after completion of therapy. The use of drugs that inhibit intestinal motility should be avoided.

From the side of the hematopoietic system : Cases of neutropenia, leukopenia, agranulocytosis and thrombocytopenic purpura have been reported. Rare cases of aplastic anemia and pancytopenia have also been described in which the role of lincomycin as a causative factor cannot be ruled out.

From the side of the immune system : hypersensitivity reactions, including angioedema, serum sickness, anaphylaxis; some of these reactions were observed in patients with hypersensitivity to penicillin. Rare cases of erythema multiforme, sometimes similar to Stevens-Johnson syndrome, have been associated with the use of lincomycin.

Serious anaphylactoid reactions require urgent intensive treatment with epinephrine, oxygen therapy and intravenous corticosteroids. If indicated, the airway should also be restored, if necessary by intubation.

Skin and mucosal disorders : Cases of pruritus, skin rash, urticaria, vaginitis and rare cases of exfoliative and vesicular bullous dermatitis have been reported.

From the side of the liver : during therapy with lincomycin, the occurrence of jaundice and changes in liver function parameters (in particular, an increase in serum transaminase levels) were observed.

From the side of the kidneys : although a direct relationship between lincomycin and kidney damage has not been established, in some cases, impaired renal function was observed, as evidenced by azotemia, oliguria and / or proteinuria.

From the side of the organ of hearing and balance : in some cases, tinnitus and vertigo have been reported.

The use of lincomycin may cause overgrowth of non-susceptible organisms, in particular yeasts.

it is necessary to conduct microbiological studies in order to determine pathogens and their sensitivity to lincomycin.

Lincomycin has been shown to be effective in the treatment of staphylococcal infections resistant to other antibiotics and susceptible to lincomycin. Strains of staphylococci resistant to lincomycin have been identified, therefore, during therapy with Lincomycin, it is necessary to carry out bacteriological cultures and sensitivity studies of pathogens. In the case of the use of macrolides, partial, but not complete, cross-resistance is possible. If indicated, the drug can be used simultaneously with other antibacterial drugs.

To reduce the rate of emergence of drug-resistant bacteria and maintain the efficacy of lincomycin and other antibacterial drugs, Lincomycin should only be used to treat or prevent infections that are proven or very likely to be caused by susceptible bacteria. Where culture and susceptibility information is available, it should be taken into account when selecting or changing antibiotic therapy. In the absence of such data, local epidemiological data and susceptibility characteristics may influence the empirical choice of treatment.

Lincomycin is not indicated for the treatment of minor bacterial infections and viral infections. The administration of Lincomycin in the absence of a confirmed or highly suspected bacterial infection is unlikely to be of benefit to the patient and increases the risk of developing drug-resistant bacteria.

Because of the risk of developing pseudomembranous colitis, the physician should evaluate the nature of the infection and evaluate the suitability of less toxic alternatives (eg, erythromycin) before deciding to use lincomycin.

Diarrhea associated with Clostridium difficile has been reported with almost all antibacterial agents, including lincomycin.

The severity of the manifestation can be from mild diarrhea to fatal colitis. C. difficile , which produce toxins A and B. C. difficile associated diarrhea may be mild with watery, liquid stools, but may also progress to severe persistent diarrhea, leukocytosis, fever, severe abdominal cramps, mucus or blood in stools.

For mild pseudomembranous colitis, discontinuation of the drug is usually sufficient. Moderate to severe cases should be treated with fluids, electrolytes, proteins, and antibacterial agents effective against C. difficile in colitis.

As soon as the initial diagnosis of pseudomembranous colitis is established, treatment should be started. Diagnosis is usually based on clinical symptoms, but endoscopy or definitions can also be used to confirm the diagnosis C.difficile and its toxins in the stool of a patient.

If left untreated, the patient may develop potentially fatal peritonitis, shock, and toxic megacolon.

C.difficile associated diarrhea is more common and more severe in debilitated and elderly patients. The cause of increased morbidity and mortality can also be strains C. difficile , which are capable of increased production of toxins.

The possibility of diarrhea associated with C. difficile should be considered in patients with diarrhea associated with antibiotic use. It is necessary to conduct a thorough analysis of the anamnesis, since the development of diarrhea associated with C. difficile was described even 2 months after the completion of antibiotic therapy.

Lincomycin should be used with caution in patients with a history of gastrointestinal disease, especially colitis.

Lincomycin should not be used to treat patients with meningitis because levels of the drug in the cerebrospinal fluid are insufficient.

During long-term treatment, liver and kidney function should be monitored and blood tests performed.

The use of lincomycin may lead to overgrowth of non-susceptible organisms, in particular yeasts. In the event of superinfection, appropriate measures should be taken according to the clinical situation. If patients with pre-existing fungal infections need treatment with Lincomycin, antifungal therapy should be carried out simultaneously.

Lincomycin should be used with caution in patients with a history of asthma burden or severe allergy.

Assigned surgical procedures should be carried out in conjunction with antibiotic therapy.

Lincomycin has been shown to be able to block neuromuscular impulse transmission, and therefore may potentiate the effects of other neuromuscular blockers. Thus, lincomycin should be used with caution in patients taking drugs of this class.

Lincomycin should be used with caution in atopic patients.

Lincomycin should be used with caution in patients with severe renal and/or hepatic impairment associated with severe metabolic disorders. For such patients, the dose of the drug should be changed (see APPLICATION). During treatment with high doses in such patients, it is necessary to control the level of lincomycin in the blood serum, since T _½ of the drug in these categories of patients can be extended by 2-3 times.

Use during pregnancy or lactation . In humans, lincomycin is able to cross the hematoplacental barrier. At the same time, the levels of the drug in the cord blood serum reach 25% of the levels of the drug in the mother’s blood serum. Significant accumulation of the drug in the amniotic fluid does not occur. Controlled studies on the use of the drug in pregnant women have not been conducted. In 302 children of patients treated with lincomycin in different trimesters of pregnancy, there was no increase in the frequency of congenital anomalies or developmental delay compared with the control group during the first 7 years of life.

Lincomycin should not be used during pregnancy unless there is a clearly defined need for treatment. Lincomycin has been detected in breast milk at a concentration of 0.5–2.4 µg/mL. Due to the possibility of severe reactions to lincomycin in breastfed infants, a decision should be made to stop breastfeeding or stop treatment with the drug, depending on the need for the drug for the mother.

Ability to influence the reaction rate when driving vehicles or operating other mechanisms . There was no particular effect on the reaction rate when driving vehicles or working with other mechanisms, but isolated cases of dizziness were reported.

may increase the effect of drugs of the neuromuscular blocker class (see SPECIAL INSTRUCTIONS).

Simultaneous oral administration of kaolin-pectin mixtures slows down the absorption of lincomycin by 90%. Therefore, in order to avoid such an interaction, these mixtures should be taken at least 2 hours before or 3-4 hours after taking lincomycin.

In vitro antagonistic interactions have been observed between lincomycin and erythromycin, as well as macrolide compounds that have a chemical structure similar to erythromycin. Because of the possible clinical significance of the described interaction, these two drugs should not be administered simultaneously.

Lincomycin may interfere with blood ALP levels.