ROXISARA  AM
Composition : Each tablet of Roxisara AM contains roxithromycin 150 mg and ambroxol hydrochloride 30mg.
Description :
Roxithromycin is a semisynthetic, long-acting, acid-stable macrolide antibiotic. As compared to erythromycin, it has a very similar antibacterial spectrum of action, better bioavailability by the oral route, better tissue penetration, and much longer duration of action. Chemically it is designated as Erythromycin 9-{0-[(2-methoxyethoxyl) methyl]oxime} (C41H76N2O15 = 837.0).
Ambroxol is an active metabolite of bromhexine and has similar but somewhat longer-lasting mucolytic action. Chemically ambroxol (as hydrochloride salt) is designated as trans-4-(2-Amino-3,5 dibromobenzylamino) cyclohexanol hydrochloride (C13H18Br2N2O1HCl=414.6). It has been incorporated in tablet Roxisara AM to facilitate better penetration of roxithromycin into respiratory tract fluids for superior antibacterial action.
Pharmacological Actions and Their Mechanisms :
Roxithromycin is highly active against Streptococcus pyogenes and S. pneumoniae, Staphylococcus aureus (methicillin-sensitive)*, Clostridia, Corynebacterium diphtheriae, Bacillus anthracis, Erysipelothrix rhusiopathy, Listeria monocytogenes, Propionibacterium acnes, and also against Neisseria gonorrhoeae, Moraxella catarrhalis, Campylobacter, Gardnerella vaginalis, Legionella pneumophilia, and Mycoplasma pneumoniae. Organisms moderately sensitive to the drug include S. viridans, N. meningitides, Haemophilus ducrei, H. Influenzae, Helicobacter pylori, Bordetella pertussis, Campylobacter jejuni, Actinomyces, Chlamydia trachomatis, Rickettsias, Treponema pallidum, Borrelia burgdorferi, and mycobacterium scrofulaceum and M. kansasi.  (* Some strains may develop resistance during the course of therapy with
roxithromycin).
Roxithromycin binds to the 50S ribosomal subunit of susceptible bacteria and inhibits their growth and multiplication by disrupting bacterial protein synthesis.
Ambroxol liquefies tenacious respiratory tract secretions by depolymerising mucopolysaccharide fibres directly as well as by liberating lysosomal enzymes. It also increases the secretion of thin bronchial fluids. Such mucolytic and mucokinetic actions facilitate penetration of antimicrobial agents into the respiratory tract fluids and ensure a better and faster clinical response.
Clinical Pharmacokinetics
There is no significant pharmacokinetic interaction between roxithromycin and ambroxol present in tablet Roxisara AM. Therefore, the pharmacokinetics of the preparation may be regarded as equivalent to that of the individual active components summed up. About 50% of an oral dose of roxithromycin is absorbed from the gastro-intestinal tract. A single 150mg oral dose produces peak plasma concentrations of about 6 to 8 mcg/ml after 2 hours. Absorption may be reduced when taken after, but not before, a meal. It is widely distributed in tissues and body fluids. High concentrations are achieved in the lung, prostate, tonsils, skin, and epididymis. It is also concentrated in neutrophils, macrophages, and monocytes. The drug is about 86 to 91% serum protein bound (mainly to alpha1-acid glycoprotein). It is metabolized to a limited extent in the liver. About 54% of an administered dose is excreted in the feces, about 10% in the urine, and 10 to 20% in the expired air. The elimination plasma half-life ranges from 8 to 13 hours, but may be longer in patients with severe kidney or liver function impairment, and children.
Following oral administration ambroxol is rapidly and completely absorbed. After intravenous administration, the apparent volume of distribution, the terminal elimination half-life and the total plasma clearance were
tablet英文
determined to be 1.52 L/kg, 3.72 h, and 565 ml/min, respectively. The drug is metabolized extensively to dibromoanthranilic acid and almost completely excreted in the urine.
Indications :
Tablet Roxisara AM is indicated for the treatment of the following conditions caused by susceptible microorganisms : Acute bronchitis (bacterial), acute exacerbations of chronic bronchitis, bronchopneumonia, pneumonia due to a typical pathogens, bacterial infections complicating bronchial asthma or bronchiectasis, sinusitis and otitis media.  Contraindications :
Tablet Roxisara AM should not be given to patients with known hypersensitivity to either macrolide antibiotics, ambroxol, or bromhexine. It also should not be given to patients receiving vasoconstrictive ergot alkaloids.
Precautions :
In severe hepatic insufficiency (e.g. hepatic cirrhosis with jaundice and/or ascites) the dose should be reduced by half.
In pregnancy the safety of roxithromycin and ambroxol to the foetus has not been established. Howeve
r, roxithromycin has not been found to be teratogenic or foetotoxic at 40 times the human therapeutic doses in several species of laboratory animals. Thus, the preparation should not be used in pregnancy unless clearly indicated.
Small quantities of roxithromycin are excreted in the breast milk. Breast-feeding by the mother or treatment of the mother with tablet Roxisara AM should be discontinued if required.
Since mucolytics may disrupt the gastric mucosal barrier tablet Roxisara AM containing ambroxol should be used with caution in patients with a history of peptic ulceration.
Drug Interactions :
Concurrent administration of a macrolide antibiotic and ergotamine or its
derivatives may provoke vasospasm and cause serious ischaemia. Hence, tablet Roxisara AM should not be given along with these drugs.
No clinically significant drug interaction of roxithromycin occurs with concurrent administered antacids, carbamazepine, ciclosporine, oral contraceptives, theophylline, triazolam, and warlarin (prothrombin time increased in patients receiving vitamin Kantagonists). Serum levels of free disopyramide can be i
ncreased due to displacement from serum protein binding sites. Like other macrolides roxithromycin may prolong the half-life of midazolam. Macrolides may increase serum levels of terfenadine which may result in ventricular arrhythmias. This has not been documented with roxithromycin but caution is warranted in case of co-administration.
No clinically significant drug interaction has been described for ambroxol.
Adverse Effects :
Tablet Roxisara AM is generally well tolerated by most patients.  However, roxithromycin present in the preparation may occasionally produce gastro-intestinal disturbances such as nausea, vomiting, epigastric pain, and diarrhoea. These adverse effects are less frequent (<4% of treated patients) than with erythromycin. Increases in liver enzyme values and hepatitis have been reported. Rashes, urticaria, angioedema, and exceptionally bronchospasm and anaphylactic shock are hypersensitivity reactions reported. Other adverse effects reported occasionally include headache, dizziness, weakness, and changes in blood cell count.
Hypersensitivity reactions and mild gastro-intestinal side-effect such as constipation and dry mouth may be occasionally produced by ambroxol.  Dosage and Administration :
Adults with normal hepatic function mild to moderate renal impairment : One tablet to be taken twice a day (morning and evening) before meals for
at least upto 2 days after resolution of the symptoms. The usual duration of therapy is between 5 and 10 days.
Adults with severe liver disease :One tablet to be taken once a day.  Elderly persons : Usual dosage.
Children :Dose is calculated on the basis of roxithromycin content; 2.5 to 4mg of roxithromycin/kg body-weight to be given before meals twice daily for a maximum of 10 days.
Storage :
Store in a cool, dry and dark place.
Presentation :
In strips of 10’s.

版权声明：本站内容均来自互联网，仅供演示用，请勿用于商业和其他非法用途。如果侵犯了您的权益请与我们联系QQ:729038198，我们将在24小时内删除。