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What-is-clindamycin

What are common side effects of clindamicina?

Posted on  February 2, 2021, Edited by Jason, Category  

What is clindamycin?

1. Definition

Clindamicina, also called cleocin, is a white crystalline powder chemical with a chemical formula of C18H33ClN2O5S and a molecular weight of 424.98. Clindamycin is an antibiotic. It is mainly used clinically for abdominal cavity and gynecological infections caused by anaerobic bacteria. It is the first choice for treatment of Staphylococcus aureus osteomyelitis.

2. Pharmacology

Pharmacological effects: Clindamycin phosphate is a chemically synthesized derivative of clindamycin, which has no antibacterial activity in vitro. After entering the body, it is quickly hydrolyzed to clindamycin to exert antibacterial activity.

In vitro tests have shown that clindamycin is active against the following microorganisms; aerobic gram-positive cocci: Staphylococcus aureus and Staphylococcus epidermidis (both including penicillinase-producing and non-penicillinase-producing strains), streptococcus (fecal Except enterococcus), pneumococcus. Anaerobic Gram-negative Bacteria: Bacteroides (including Bacteroides fragilis group and Bacteroides niger group) and Fusobacterium. Anaerobic Gram-positive non-producing Bacillus: Propionibacterium, Eubacteria and Actinomycetes. Anaerobic and microaerobic gram-positive bacilli genera: Peptococcus, Microaerophilic Streptococcus, and Peptostreptococcus.

Toxicological research: Ames Salmonella reverse mutation test and rat micronucleus test results were negative. Reproductive toxicity: Clindamycin dosage is 0.3g/kg orally administered to rats, which has no effect on the mating and fertility of animals. Rats and mice were given oral clindamycin at a dose of 0.6 g/kg or subcutaneous injection at a dose of 0.25 mg/kg, respectively. The result was no teratogenic effect. However, adequate and rigorous clinical studies have not been conducted on pregnant women, and animal reproduction studies cannot fully predict human responses. Carcinogenicity: Long-term carcinogenic potential studies have not been conducted in animals.

3. Pharmacokinetics

Clindamycin phosphate enters the body and is quickly hydrolyzed to clindamycin under the action of alkaline phosphatase in the blood. The pharmacokinetics of normal people showed that: a single intravenous infusion of 0.6g clindamycin phosphate, the clindamycin in the blood immediately reached a peak, the concentration was 11.09±2.02mg/L, and the 8-hour blood concentration was 1.69± 0.35mg/L; single intramuscular injection of 0.6g, clindamycin in the blood reaches its peak within 1~2 hours, the concentration is 5.92±1.45mg/L, the 8-hour blood concentration is 2.51±0.91mg/L, effective blood drug concentration can be maintained for more than 8 hours. After administration of clindamycin phosphate, it is mainly metabolized in the liver and excreted in bile and feces.

For most adults once every 8-12 hours, pediatric patients once every 6-8 hours using clindamycin, or continuous intravenous infusion of clindamycin, the serum drug concentration can be maintained at the lowest antibacterial in vitro test. After three consecutive use, the blood concentration can reach a steady state.

What is clindamycin used for?

What-is-clindamycin-used-for
What-is-clindamycin-used-for

1. Indications

A. Clindamicina is applicable to the following infectious diseases caused by the positive bacterium:

  • Tonsillitis, suppurative otitis media, sinusitis, etc.
  • Acute bronchitis, acute exacerbation of chronic bronchitis, pneumonia, lung abscess, and bronchiectasis combined with infection.
  • Skin and soft tissue infections: furuncle, carbuncle, abscess, cellulitis, trauma and post-operative infection, etc.
  • Urinary system infection: acute urethritis, acute pyelonephritis, prostatitis, etc.
  • Others: osteomyelitis, sepsis, peritonitis and oral infections.

B. Clindamicina is applicable to all kinds of infectious diseases caused by anaerobic bacteria:

  • Pulmonary infections caused by empyema, lung abscess, anaerobic bacteria.
  • Skin and soft tissue infections, sepsis.
  • Intra-abdominal infection: peritonitis, intra-abdominal abscess.
  • Female pelvic and genital infections: endometritis, non-gonococcal fallopian tube and ovarian abscess, pelvic cellulitis and infection after gynecological surgery.

2. Uses

Clindamycin belongs to the lincomycin class of drugs. It is an artificial semi-synthetic antibiotic that mainly acts by inhibiting the synthesis of bacterial protein. Clindamycin has a stronger effect than lincomycin and has fewer side effects than lincomycin. It can be taken orally, intramuscularly, or intravenously. There are many commonly used clindamycin preparations, such as dalacin.

The main feature of clindamycin is its strong antibacterial effect on various anaerobic bacteria. It is clinically used to treat abdominal, gynecological and dental infections caused by anaerobic bacteria; and sensitive aerobic bacteria, mainly Gram Respiratory tract infections, bone and soft tissue infections, biliary tract infections, endocarditis, sepsis and so on caused by stain-positive cocci.

3. Dosage

  • Oral: hydrochloride, adult severe infection, oral 150-300 mg once, 450 mg if necessary, once every 6 hours. Children with severe illness 8-16 mg/kg per day, 20 mg/kg if necessary, divided into 3~ 4 times use. Palmitate hydrochloride, for children, 8-12 mg/kg a day for severe infections, and can be increased to 20-25 mg/kg a day for severe infections, divided into 3 to 4 doses.
  • Injection: Phosphate injection, intravenous or intramuscular injection, for adult Gram-positive aerobic bacteria infection, 0.6~1.2g per day, anaerobic bacteria infection 1.2~2.7g per day, very severe infection can use up to 4.8g per day, divided into 2 to 4 times. Children over 1-month-old, 15-25 mg/kg a day for severe infections, 25-40 mg/kg for very severe infections, divided into 3 to 4 times. Intramuscular injection does not exceed 0.6g once.
  • Preparation: Clindamycin Hydrochloride Capsules: 75 mg (active) per capsule; 150 mg (active). Clindamycin Phosphate Injection: 150 mg (2ml) each. Clindamycin Phosphate Injection: 2ml: 0.3g (calculated according to C18H33ClN2O5S).

Clindamycin side effects

Clindamycin-side-effects
Clindamycin-side-effects

It is a derivative of lincomycin and has been on the market in China since 1970. Its purpose is mainly used to fight various infectious diseases. The most common adverse reactions: allergic reactions, injection local irritation and abnormal liver function, the most serious is pseudomembranous enteritis.

Clindamycin is a derivative of lincomycin. It has been used for more than 40 years. It is generally used for infectious diseases caused by gram-positive bacteria. Clindamycin has a broad antibacterial spectrum and strong antibacterial efficacy, and it can be used without skin test. In order to save trouble, many doctors prefer to use this. But clindamycin is not very safe.

The most common adverse reactions: allergic reactions, local injection irritation and abnormal liver function, the most serious is pseudomembranous enteritis. The adverse reactions of clindamycin have attracted increasing attention.

In the database of the National Adverse Drug Reaction Monitoring Center, the adverse reactions of clindamycin injection are serious, mainly systemic damage, respiratory system damage, and urinary system damage. Among them, acute renal function damage and hematuria are prominent.

1. Adverse reactions

It can cause gastrointestinal reactions: nausea, vomiting, loss of appetite, abdominal distension, diarrhea, skin rash, leukopenia, elevated transaminase, double infection, pseudomembranous colitis. It can also cause difficulty in breathing, swelling of the lips, swelling of the nose, tearing and allergic reactions. It has been reported that the incidence of pseudomembranous enteritis caused by this product is the highest, which may exceed 2%. Approximately 10% of people treated with clindamycin have skin rashes.

A. Anaphylactic shock

In anaphylactic shock, the allergic reaction that causes the greatest damage to the body usually occurs within 3 to 5 minutes after intravenous administration, and is mainly manifested as profuse sweating, chest tightness, palpitation, dyspnea, and cyanosis. If the rescue is not in time, it will be life-threatening, so patients, especially those with a history of allergies, should pay attention to the medication.

B. Acute laryngeal edema

Acute laryngeal edema is a rare manifestation of allergic reactions. It leads to acute throat obstruction, causing breathing difficulties, inspiratory throat, mild cyanosis of the lips, irritability, rapid onset, rapid development of the disease, and suffocation will happen if rescue is not timely.

C. Gastrointestinal reactions

Gastrointestinal reactions are the most common reaction of clindamycin, which can occur both by oral administration and intramuscular injection. It manifests as nausea, vomiting, anorexia, abdominal distension, diarrhea, abdominal pain and other symptoms. Pseudomembranous enteritis can cause the most serious complications.

D. Abnormal liver function

Some patients will experience elevated serum transaminases and jaundice after applying clindamycin. Most of them are transient and disappear after stopping the drug. Early information often describes that "it may have liver damage." Recent data show that the increase in transaminase is mainly related to the damage of local muscles during intramuscular injection, and is also related to the colorimetric results when clindamycin phosphate and its metabolites interfere with the determination of transaminase. It is not caused by liver cell damage, but clindamycin is mainly metabolized in the liver, so it should be used with caution with severe liver insufficiency.

E. Impairment of renal function

Clindamycin can lead to acute renal failure caused by related acute interstitial nephritis. The acute renal damage may be caused by the decrease of the plasma protein binding rate in the body, the increase of free active ingredients and renal excretion. Therefore, it is suggested that the clinicians should pay close attention to the changes in the patient's renal function and the dosage and concentration, and deal with abnormalities in time to reduce or avoid the harm of adverse reactions to the patients.

F. Skin damage

Skin damages are mainly manifested as multi-line erythema, rash, dermatitis, pustules, lip ulceration, eyelid congestion, itching, allergic purpura and other skin damages. These are common clinical vascular allergic diseases of clindamycin. Allergic reactions of these sensitizers lead to increased permeability and fragility of small arteries, veins and capillaries, blood oozing, and bleeding of the skin, mucous membranes and certain organs, which may be accompanied by angioedema and urticaria.

G. Local reactions

After intramuscular injection, slight pain may occur at the injection site. Long-term intravenous drip may cause thrombophlebitis.

H. Blood system

Oral administration or intramuscular injection can cause neutropenia, leukopenia, thrombocytopenia, and thrombocytopenic purpura, which are generally mild and can return to normal after stopping the drug.

I. Nervous System

Clindamycin has a poor ability to penetrate the normal blood-brain barrier, and it is not easy to reach an effective concentration in brain tissue. However, excessive doses of the drug can also cause central nervous system damage. Therefore, if patients using clindamycin have mental illness, the dosage should be adjusted or stopped. Clindamycin has a blocking effect on presynaptic terminal, receptors and neuromuscular, and can enhance the neuromuscular blocking effect, leading to skeletal muscle weakness and respiratory muscle depression or paralysis.

J. Cardiovascular system

Large-dose intravenous drip can cause cardiovascular system abnormalities such as blood pressure drop and electrocardiogram changes, so it should be slowly dripped after dilution.

2. Clindamycin Warnings

  • There is no cross-allergic reaction with penicillin and cephalosporin antibiotics, and it can be used for people allergic to penicillin.
  • It is compatible with ampicillin, phenytoin sodium, barbiturate hydrochloride, aminophylline, calcium gluconate and magnesium sulfate. And it has an antagonistic effect with erythromycin, so it is not suitable for combined use.
  • Patients with liver and kidney damage, gastrointestinal diseases such as ulcerative colitis, localized enteritis, and antibiotic-related enteritis should use it with caution.
  • When using clindamicina, pay attention to the possibility of pseudomembranous enteritis. If pseudomembranous enteritis occurs, first supplement water, electrolytes, and protein; then give metronidazole orally, 250-500 mg, 3 times a day, if it is invalid, then choose vancomycin orally 0.125~0.5g, 4 times a day for treatment.

3. Clindamycin interactions

  • Clindamycin has neuromuscular blocking effects and may increase the effects of other neuromuscular blockers. Therefore, patients who use these drugs should use clindamycin with caution.
  • It has been confirmed that the antagonism between clindamycin, erythromycin and chloramphenicol exists, so the two drugs should not be used with clindamicina.
  • Clindamicina is compatible with novobiocin, kanamycin, ampicillin, phenytoin, barbiturate hydrochloride, aminophylline, calcium gluconate and magnesium sulfate.
  • The combination of clindamicina and opioid analgesics may aggravate the depression of the respiratory center.

Conclusion

Clindamicina and lincomycin belong to the lincomycin antibiotics, but clindamycin is more effective than lincomycin and has fewer side effects. Clindamycin has a very good effect on osteomyelitis caused by Staphylococcus aureus.

BALLYA provides a ballya-clindamycin-test to tell you if there are clindamycin residues in feed and food.

References

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