Clacid SR, 500 mg 7 pcs

Clacid SR is an antibiotic of macrolide group. Clarithromycin inhibits protein synthesis in microbial cell by interacting with 50S ribosomal subunit of bacteria. Highly active against a wide range of aerobic, anaerobic, Gram-positive and Gram-negative bacteria.

Clarithromycin has demonstrated high in vitro activity against standard and isolated cultures of bacteria. Highly effective against many aerobic and anaerobic gram-positive and gram-negative microorganisms. In vitro studies confirm high effectiveness of clarithromycin against Legionella pneumophila and Mycoplasma pneumoniae.

The drug is also active against aerobic gram-positive microorganisms: Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Listeria monocytogenes; aerobic gram-negative microorganisms: Haemophilus influenzae, Haemophilus parainftuenzae, Moraxella catarrhalis, Neisseria gonorrhoeae; other microorganisms: Mycoplasma pneumoniae, Chlamydia pneumoniae (TWAR), Chlamydia trachomatis, Mycobacterium leprae, Mycobacterium kansasii, Mycobacterium chelonae, Mycobacterium fortuitum, Mycobacterium avium complex (MAC): Mycobacterium avium, Mycobacferium intracellulare.

The Enterobacteriaceae, Pseudomonas spp. and other non-lactose degrading Gram-negative bacteria are not sensitive to clarithromycin.
B-lactamase production has no effect on clarithromycin activity. Most staphylococcal strains that are resistant to methicillin and oxacillin are also resistant to clarithromycin.

Clarithromycin is also effective in vitro against most strains of the following microorganisms (but the safety and effectiveness of clarithromycin in clinical practice has not been confirmed by clinical studies, and the practical significance remains unclear): Aerobic Gram-positive microorganisms: Streptococcus agalactiae, Streptococci (groups C,F,G), Viridans group streptococci; aerobic gram-negative microorganisms: Bordeteila pertussis, Pasteurella multocida; anaerobic gram-positive microorganisms: Clostridium perfringens, Peptococcus niger, Propionibacterium acnes; anaerobic gram-negative microorganisms: Bacteroides melaninogenicus; Borrelia burgdorferi, Treponema pallidum, Campylobacter jejuni.

The microbiological activity of the metabolite is the same as that of the parent substance, or 1-2 times weaker against most microorganisms. The exception is Haemophilus influenzae against which the effectiveness of the metabolite is 2 times higher. The starting substance and its main metabolite have either additive or synergistic effect against Naemophilus influenzae under in vitro and in vivo conditions depending on the bacterial culture.

The sustained release tablets are a homogeneous crystalline base that allows prolonged release of the active ingredient as it travels through the gastrointestinal tract.

Indications

Active ingredient

Composition

How to take, the dosage

In adults, Clacid SR is prescribed at 500 mg (1 tablet) 1 time per day. In severe infections the dose is increased to 1 g (2 tablets) once a day.

The tablets should be taken with food, swallowed whole without breaking or chewing.

Interaction

Concomitant administration of clarithromycin with drugs metabolized with the participation of CYP3A cytochrome P450 isoenzyme may lead to increased plasma concentrations of such drugs as alprazolam, astemizole, carbamazepine, cilostazol, cisapride, cyclosporine, disopyramide, ergot alkaloids, lovastatin, methylprednisolone, midazolam, omeprazole, oral anticoagulants (e.g., warfarin), pimozide, quinidine, rifabutin, sildenafil, simvastatin, tacrolimus, terfenadine, triazolam, vinblastine.

A similar mechanism of interaction is observed with the use of drugs metabolized by another isoenzyme of cytochrome P450 system – phenytoin, theophylline and valproate. When concomitant use of theophylline and carbamazepine with clarithromycin, a moderate but significant (p)-significant incidence of rhabdomyolysis has been reported with clarithromycin and HMG-CoA reductase inhibitors (such as lovastatin and simvastatin).

Concomitant use of clarithromycin with cisapride has resulted in increased concentrations of cisapride. This may cause QT interval prolongation, arrhythmias, ventricular tachycardia, ventricular fibrillation and torsade de pointes. Similar effects have been observed in patients taking clarithromycin concomitantly with pimozide.

Drugs of macrolide group affect metabolism of terfenadine. Terfenadine blood levels increase, which may be accompanied by an increased QT interval, the development of arrhythmias, ventricular tachycardia, ventricular fibrillation and torsade de pointes. The content of acid metabolites of terfenadine increases by 2-3 times, the QT interval increases, but it does not cause any clinical manifestations. The same pattern was observed with concomitant administration of astemizole with drugs of macrolide group.

There have been reports of ventricular torsade de pointes with clarithromycin and quinidine and disopyramide. Blood concentrations should be monitored when these drugs are used concomitantly.

Concomitant use of clarithromycin with digoxin has resulted in increased serum digoxin levels. Serum digoxin levels should be monitored in these patients.

Concomitant oral administration of clarithromycin and zidovudine decreased equilibrium levels of zidovudine in HIV-infected patients. Because clarithromycin affects the absorption of zidovudine, the two drugs should be separated in time.

Ritonavir significantly slows down the metabolism of clarithromycin when taken concomitantly. In this case the Cmax value of clarithromycin increases by 31%, Cmin by 182% and AUC by 77%. There is a significant delay in the formation of 14-hydroxyclarithromycin. In this case in patients without renal impairment there is no need to adjust clarithromycin dose. In patients with a CK of 60-30 ml/min, the dose of clarithromycin should be reduced by 50% to a maximum dose of 500 mg (1 sustained release tablet) once daily. If ritonavir is taken, no dose of clarithromycin greater than 1 g/day should be administered concomitantly.

Cross-resistance may develop between clarithromycin and other macrolide drugs such as lincomycin and clindamycin.

Special Instructions

With caution prescribe the drug in patients with liver dysfunction. In the presence of chronic liver disease, regular monitoring of serum enzymes should be carried out.

Patients with mild to moderate renal dysfunction should also be treated with caution. In patients with significant renal impairment (CKR less than 30 ml/min), rapid-release clarithromycin (tablets 250 mg or 500 mg) should be prescribed.

In case of co-administration with warfarin or other indirect anticoagulants, prothrombin time should be monitored.

Synopsis

Contraindications

Side effects

Cardiovascular system disorders: rarely – ventricular arrhythmia, including ventricular tachycardia (with prolongation of the QT interval).

Digestive system disorders: nausea, abdominal pain, vomiting, diarrhea, gastralgia, pancreatitis, glossitis, stomatitis, oral candidiasis, discolored tongue and teeth; rarely – pseudomembranous enterocolitis. Discoloration of teeth is reversible and is usually restored by professional dental cleaning. Rarely, liver dysfunction has been reported, including increased liver enzyme activity, hepatic cellular and/or cholestatic hepatitis with or without jaundice. These liver dysfunctions can be severe, but are usually reversible. Very rare cases of hepatic failure and death have been observed mainly against the background of severe comorbidities and/or concomitant drug therapy.

CNS disorders: transient headaches, dizziness, anxiety, insomnia, nightmares, tinnitus, depersonalization, hallucinations, seizures, feelings of fear; rarely – psychosis, confusion; in some cases – hearing loss (when stopping clarithromycin hearing restored), change of smell (usually accompanied by distortion of taste).

Allergic reactions: urticaria, skin hyperemia, pruritus, anaphylaxis, Stevens-Johnson syndrome.

Hematopoietic system disorders: leukopenia, thrombocytopenia.

Laboratory disorders: increase in blood creatinine; hypoglycemia is rare (with simultaneous use of hypoglycemic agents).

Others: development of microbial resistance.

Overdose

Symptoms: Taking a large dose of clarithromycin may cause gastrointestinal symptoms. One patient with a history of bipolar disorder has described mental changes, paranoid behavior, hypokalemia and hypoxemia after taking 8 g of clarithromycin.

Treatment: unabsorbed drug should be removed from the gastrointestinal tract and symptomatic therapy should be carried out. Hemodialysis and peritoneal dialysis have no significant effect on serum levels of clarithromycin.

Pregnancy use

The safety of clarithromycin use during pregnancy and breastfeeding has not been established.

The use of clarithromycin in pregnancy (especially in the first trimester) is possible only if there is no alternative therapy and the potential benefit to the mother exceeds the potential risk to the fetus.

If administration during lactation is necessary, breastfeeding must be discontinued.

Similarities