Rulid, 150 mg 10 pcs.

Pharmacodynamics

A semisynthetic oral macrolide antibiotic.

The drug is usually sensitive to: Bordetella pertussis. Borrelia burgdorferi. Moraxella (Branhamella) catarrhalis. Campylobacter coli. Campylobacter jejuni. Chlamydia trachomatis, psittaci and pneumoniae. Clostridium perfringens. Corynebacterium diptheriae. Enterococcus. Gardnerella vaginalis. Methi-S-Staphylococcus. Neisseria meningitidis. Helicobacter pylori. Legionella pneumophilia. Lysteria monocytogenes obiluncus. Mycoplasma pneumoniae. Pasteurella multocida. Peptostreptococcus. Porphyromonas. Propionibacterium acnes. Rhodococcus equi. Streptococcus pneumoniae. Streptococcus spp.

Moderately sensitive to the drug: Haemophilus influenzae. Ureaplasma urealyticum. Vibrio cholerae.

The following are resistant to the drug: Acinetobacter spp. Bacteroides fragilis. Enterobacteriaceae. Methi-R Staphylococcus. Pseudomonas spp. Fusobacterium. Mycoplasma hominis. Nocardia.

Pharmacokinetics

Absorption and distribution

Roxytromycin is rapidly absorbed after oral administration. Roxithromycin is more stable than other macrolides in the acidic environment of the stomach. Taking the drug 15 minutes before a meal has no effect on pharmacokinetics. After taking the drug in a dose of 150 mg, maximum blood concentration averages 6.6 mg/l and is reached after 2.2 hours. Administration of the drug at 12-hour intervals ensures maintenance of effective concentrations in the blood for 24 hours.

The elimination half-life after a single dose of 150 mg is 10.5 hours. After a single dose of 300 mg of roxithromycin the average maximum concentration in the blood is 9.7 mg/l and is reached after 1.5 hours. When re-administration of roxithromycin (150 mg twice daily, for 10 days) the equilibrium state in plasma is reached between 2-4 days, making C mah 9.3 mg/l. Administration of 300 mg of roxithromycin every 24 hours for 11 days provided a C mah of 10.9 mg/L.

Roxithromycin penetrates well into many tissues, especially the lungs, palatine tonsils and prostate. The drug also penetrates well into cells, especially into neutrophilic leukocytes and monocytes, stimulating their phagocytic activity. Binding to blood proteins is 96%, has a saturable character and decreases at concentrations of roxithromycin over 4 mg/l.

Metabolism and excretion

Roxytromycin is metabolized only partially, more than half of the active substance is excreted unchanged mainly in the feces and in the urine. In adults with normal renal and hepatic function 65% of roxithromycin is excreted with the feces. Less than 0.05% of the accepted dose of roxithromycin is excreted in breast milk.

Pharmacokinetics in special clinical cases

In renal failure excretion of roxithromycin and its metabolites through the kidneys is approximately 10% of the taken dose. The dose of the drug does not change in renal failure. In severe hepatic insufficiency the elimination half-life is prolonged (25 h) and C mah is increased.

Indications

Active ingredient

Composition

Active ingredient:

Roxithromycin – 150 mg.

Auxiliary substances:

Hydroxypropylcellulose,

poloxamer,

CZO povidone,

colloidal silicon dioxide,

magnesium stearate,

talc,

corn starch.

Composition of the shell:

hypromellose,

glucose anhydrous,

titanium dioxide,

propylene glycol.

How to take, the dosage

Adults are prescribed 150 mg of roxithromycin orally at 12-hour intervals. The daily dose is 300 mg. It is possible to prescribe 300 mg once daily.

Performance in children

In children (body weight over 40 kg) 150 mg of roxithromycin orally administered at 12-hour intervals. The daily dose is 300 mg. This dosage form is not used in children under 4 years of age!

The use in elderly patients

The dosage and daily dose of roxithromycin do not change in elderly patients.

The use in patients with renal failure

In patients with renal failure roxithromycin is prescribed in a dose of 150 mg 2 times a day.

The use in patients with hepatic impairment

In patients with hepatic impairment, 150 mg is prescribed once.

The duration of roxithromycin administration depends on the indication for use, the severity of the infectious process and the activity of the pathogen. Roxithromycin is taken before meals orally once or twice a day. The tablet should be swallowed with enough water.

Interaction

The concomitant administration of terfenadine is not recommended because of the increased concentration of the latter when concomitant administration of macrolide antibiotics, which may lead to the development of severe ventricular arrhythmias.

While this complication has not been noted with roxithromycin, and no pharmacokinetic interactions or ECG changes have been shown in studies on volunteers, the combination of roxithromycin and terfenadine is not recommended.

The administration of drugs such as astemizole, cisapride, and pimozide may lead to prolongation of the QT interval and/or severe cardiac arrhythmias as a result of their increased serum concentrations, due to the competitive effect for CYP3A isozyme between the above mentioned drugs and macrolide antibiotics.

There is no interaction with warfarin, carbamazepine, ranitidine, antacids and oral contraceptives.

When concomitant administration of Roxithromycin with vitamin K antagonists, it is recommended to monitor the prothrombin time or the international normalized ratio (INR).

Roxithromycin may displace protein-bound disopyramide, resulting in increased serum levels of disopyramide.

EKG monitoring and, if possible, determination of serum disopyramide levels are recommended.

Concomitant administration with digoxin may increase the absorption of the latter. It is recommended to monitor the electrocardiogram and serum levels of cardiac glycoside.

This is mandatory if symptoms of cardiac glycoside overdose occur.

Roxithromycin may increase the half-life of midazolam, resulting in an increase and prolongation of its effects.

Special Instructions

Use in patients with hepatic impairment and elderly patients

When prescribing the drug in patients with hepatic impairment, special caution, monitoring of liver function and dose adjustments are required.

There is no need for dose adjustment when prescribing the drug in patients with renal failure and in elderly patients.

Contraindications

Side effects

Anaphylactic reactions: angioedema, bronchospasm, weakness, anaphylactic shock (rare).

Skin reactions: rash, redness, urticaria.

Gastrointestinal reactions: nausea and vomiting, abdominal pain, diarrhea (very rare with blood).

Liver reactions: increased liver enzymes (ALT, ACT, ALP), cholestatic or hepatocellular acute hepatitis.

Possible: minor changes in taste and smell.

In isolated cases: symptoms of pancreatitis, dizziness, headache, paresthesias have been observed.

Possible: development of superinfection due to growth of insensitive microorganisms.

Overdose

In case of overdose, gastric lavage and symptomatic therapy are necessary.

There is no specific antidote.

Pregnancy use

Roxithromycin is contraindicated in pregnancy.

Small amounts of Roxithromycin penetrate into breast milk, so it is necessary to stop breastfeeding or taking the drug.

Similarities