ELROKS
Active material: Roksitromitsin
When ATH: J01FA06
CCF: Macrolide antibiotics
When CSF: 06.07.01
Manufacturer: M.J.BIOPHARM Pvt.Ltd. (India)
Pharmaceutical form, composition and packaging
Pills, Film-coated blue, round, lenticular; color on a break – white or almost white.
| 1 tab. | |
| roksitromitsin | 100 mg |
Excipients: colloidal silicon dioxide, magnesium stearate, Croscarmellose sodium, microcrystalline cellulose, methylparaben, propyl.
The composition of the shell: methacrylic acid, triэtiltsitrat, talc, hydroxypropyl, ethyl cellulose, polyethylene glycol 6000, propylene glycol, sodium lauryl, Titanium dioxide, Brilliant Blue FCF varnish.
10 PC. – packings Valium planimetric (1) – packs cardboard.
10 PC. – packings Valium planimetric (2) – packs cardboard.
10 PC. – packings Valium planimetric (3) – packs cardboard.
Pills, Film-coated blue, round, lenticular; color on a break – white or almost white.
| 1 tab. | |
| roksitromitsin | 150 mg |
Excipients: colloidal silicon dioxide, magnesium stearate, Croscarmellose sodium, microcrystalline cellulose, methylparaben, propyl.
The composition of the shell: methacrylic acid, triэtiltsitrat, talc, hydroxypropyl, ethyl cellulose, polyethylene glycol 6000, propylene glycol, sodium lauryl, Titanium dioxide, Brilliant Blue FCF varnish.
10 PC. – packings Valium planimetric (1) – packs cardboard.
10 PC. – packings Valium planimetric (2) – packs cardboard.
10 PC. – packings Valium planimetric (3) – packs cardboard.
Pills, Film-coated blue, round, lenticular; color on a break – white or almost white.
| 1 tab. | |
| roksitromitsin | 50 mg |
Excipients: colloidal silicon dioxide, magnesium stearate, Croscarmellose sodium, microcrystalline cellulose, methylparaben, propyl.
The composition of the shell: methacrylic acid, triэtiltsitrat, talc, hydroxypropyl, ethyl cellulose, polyethylene glycol 6000, propylene glycol, sodium lauryl, Titanium dioxide, Brilliant Blue FCF varnish.
10 PC. – packings Valium planimetric (1) – packs cardboard.
10 PC. – packings Valium planimetric (2) – packs cardboard.
10 PC. – packings Valium planimetric (3) – packs cardboard.
DESCRIPTION OF ACTIVE SUBSTANCES
Pharmacological action
Semisynthetic macrolide antibiotics. The mechanism of action due to a violation of the intracellular protein synthesis of microorganisms. At low concentrations, it has a bacteriostatic effect, high – bactericide.
Active against gram-positive bacteria: Streptococcus pneumoniae, Streptococcus pyogenes, methicillin-susceptible strains of Staphylococcus aureus; against gram-negative bacteria: Moraxella catarrhalis.
Roxithromycin is also active against Mycoplasma pneumoniae, Ureaplasma urealyticum, Chlamidia spp.
Activity roxithromycin against Haemophilus influenzae is less pronounced, than erythromycin.
Maloaktiven against Mycoplasma hominis.
By roksitromitsin resistant Pseudomonas spp., Enterobacter spp., Acinetobacter spp.
Pharmacokinetics
After ingestion is rapidly absorbed from the gastrointestinal tract. Defined serum after 15 m. Is more stable in the acidic environment of the stomach, than other macrolides. Food intake has no effect on absorption. Cmax plasma levels achieved after 1.5-2 no. Css in blood plasma when receiving 150 mg 2 times / day achieved through 2-4 and d is 9.3 mg / l, when receiving 300 mg 1 time / day – 10.9 mg / l.
Roxithromycin penetrates well into tissues, especially in light, tonsils and prostate, as well as inside of neutrophils and monocytes, stimulating their phagocytic activity. Plasma protein binding is 96%, decreases with increasing concentration over roxithromycin 4 mg / l. Since breast milk is derived less 0.05% the dose.
Partially metabolized in the liver, more than half of the active substance is excreted in the feces as unchanged, about 12% excreted by the kidneys and about 15% light. T1/2 in adults with normal renal function is 10.5 h at a multiplicity of reception 1-2 times / day.
Testimony
Infectious-inflammatory diseases, caused by microorganisms sensitive to roxithromycin, incl. infections of the upper and lower respiratory tract, infections of skin and soft tissue, NGU.
Dosage regimen
Inside adults – by 150 mg 2 times / day (every 12 no) or 300 mg 1 time / day for 15 minutes before meals or on an empty stomach.
Patients with liver failure, the dose is 150 mg every 24 no.
For patients with severe renal insufficiency, the recommended dose is 150 mg every 24 no.
For children, the daily dose is 5-8 mg / kg, depending on the type of pathogen and severity of infection, razdelennaya of 2 admission.
Side effect
From the digestive system: nausea, vomiting, epigastric pain, diarrhea, anorexia, flatulence, transient increase in liver transaminases and alkaline phosphatase in the blood (more frequently in patients older 65 years); rarely – abnormal liver function, cholestatic hepatitis, pancreatitis.
Allergic reactions: hives, rash, itch, angioedema, bronchospasm, anaphylactoid reactions, swelling of the tongue, general edema, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome.
From the central and peripheral nervous system: headache, dizziness, paresthesia.
Effects, caused by chemotherapeutic action: rarely – candidiasis.
Other: rarely – general malaise, tynnyt, disorders of taste and / or smell.
Contraindications
Serious liver, concurrent use of ergot alkaloids with vasoconstrictor effect, Hypersensitivity to roxithromycin and other macrolides (including erythromycin).
Pregnancy and lactation
There are no adequate and well-controlled studies on the safety of roxithromycin in pregnancy and lactation is not held.
Roxithromycin in small amounts excreted in breast milk.
IN experimental studies in animals revealed no mutagenic and embryotoxic action, negative effect on fertility.
Cautions
To use caution in patients with impaired liver and kidney function.
With the development of superinfection or pseudomembranous colitis roxithromycin should be lifted immediately and appoint appropriate therapy.
With caution used in conjunction with terfenadine and astemizole.
IN experimental studies revealed no carcinogenic effect.
Drug Interactions
In an application with indirect anticoagulants may increase the anticoagulant action.
In an application with drugs ergot, ergotaminopodobnymi vasoconstrictor ergotism may develop up to tissue necrosis limbs.
In an application with digoxin increases absorption of digoxin.
In an application may be a small increase in the concentration of midazolam and triazolam plasma.
While the use of theophylline may increase the concentration of theophylline in the blood plasma.
We can not exclude the possibility of increasing plasma concentrations of cisapride, astemizola, terfenadine when an application with roxithromycin.
At simultaneous application with cyclosporine may be some increase in blood concentration and toxic effects of cyclosporine.
While the use of ethambutol marked synergy against Mycobacterium avium.
