Drug Nomenclature
Synonyms: RU-28965; RU-965; Roksitromicinas; Roksitromysiini; Roxithromycin; Roxithromycinum; Roxitromicin; Roxitromicina; Roxitromycin
Pharmacopoeias. In China, Europe, and Japan.
European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Roxithromycin). A white or almost white, crystalline powder. It exhibits polymorphism. Very slightly soluble in water; freely soluble in alcohol, in acetone, and in dichloromethane; slightly soluble in dilute hydrochloric acid. Store in airtight containers.
Adverse Effects and Precautions
Gastrointestinal disturbances are the most frequent adverse effect, but are less frequent than with erythromycin.
The dose of roxithromycin may need to be reduced in patients with hepatic or renal impairment.
Effects on the kidneys
Acute interstitial nephritis has been reported in a patient given roxithromycin; renal function improved over several days after the drug was stopped.
Effects on the lungs
Acute eosinophilic pneumonia was attributed in a patient to the use of roxithromycin. The condition resolved after treatment with methylprednisolone.
Effects on the pancreas
Acute pancreatitis, with duodenal inflammation, pain, pancreatic enlargement, and raised serumamylase developed in a patient within 24 hours of substituting roxithromycin for erythromycin ethyl succinate. Symptoms resolved rapidly once roxithromycin was stopped.
Eosinophilia
For a report of an eosinophilic syndrome in a patient after treatment with azithromycin or roxithromycin, see Azithromycin. See also under Effects on the Lungs, above.
Antimicrobial Action
As for Erythromycin. It is reported to be as active or slightly less active than erythromycin.
Pharmacokinetics
Roxithromycin is absorbed after oral doses with a bio-availability of about 50%. Peak plasma concentrations of about 6 to 8 micrograms/mL occur around 2 hours after a single dose of 150 mg. The mean peak plasma concentration at steady state after a dose of 150 mg twice daily is 9.3 micrograms/mL. Absorption is reduced when taken after a meal. It is widely distributed into tissues and body fluids; high concentrations are taken up into white blood cells. Small amounts of roxithromycin are distributed into breast milk. It is about 96% bound to plasma proteins (mainly aracid glycoprotein) at trough concentrations, but binding is saturable, and only about 87% is bound at usual peak concentrations. Small amounts of roxithromycin are metabolised in the liver, and the majority of a dose is excreted in the faeces as unchanged drug and metabolites; about 7 to 10% is excreted in urine, and up to 15% via the lungs. The elimination half-life is reported to range from about 8 to 13 hours, but may be more prolonged in patients with hepatic or renal impairment and in children. It has been reported that roxithromycin is not substantially removed by peritoneal dialysis.
Uses and Administration
Roxithromycin is a macrolide antibacterial with actions and uses similar to those of erythromycin. It is given orally to adults in a usual dose of 150 mg twice daily or sometimes 300 mg once daily, at least 15 minutes before meals, for 5 to 10 days in the treatment of susceptible infections.
Dosage may need to be modified in patients with hepatic or renal impairment (see below). For doses in infants and children, see below.
Administration in children
In children weighing from 6 up to 40 kg a dose of 5 to 8 mg/kg daily of roxithromycin may be used.
Administration in hepatic impairment
The licensed product information for roxithromycin notes that safety in hepatic impairment has not been established and advises halving the usual daily dose (see above) if used.
Administration in renal impairment
The licensed product information for roxithromycin notes that safety in renal impairment has not been established and dosage adjustment details are not specified.
A pharmacokinetic study in 20 subjects (10 with normal renal function and 10 with severely impaired function) suggested that doubling the dosage interval of roxithromycin would be suitable in those with a creatinine clearance of less than 15 mL/minute.
Hyperplasia
Gingival hyperplasia is a well recognised adverse effect of ciclosporin treatment; a small study indicated that roxithromycin could reduce overgrowth, possibly by an effect on transforming growth factor-β. For the use of another macrolide, azithromycin, for this indication see Hyperplasia.
Ischaemic heart disease
For mention of studies investigating roxithromycin in the prevention of ischaemic heart disease, see under Azithromycin.
Respiratory disorders
For reference to the use of roxithromycin in the management of respiratory disorders, see under Erythromycin.
Roxithromycin: Side Effects
See also Macrolide antibiotics
Roxithromycin is a macrolide antibiotic with actions and uses similar to those of erythromycin.
Observational studies
In 2917 adults, adverse effects of roxithromycin occurred in 4.1% at a dosage of 150 mg/day. Nausea (1.3%), abdominal pain (1.2%), and diarrhea (0.8%) were the most frequently reported events, whereas rash, vomiting, headache, dizziness, pruritus, urticaria, and constipation were reported only rarely. Treatment had to be withdrawn in 0.9% of the patients because of adverse effects.
In an uncontrolled study in 24 HIV-infected patients, roxithromycin (300 mg bd for 4 weeks) was effective against cryptosporidial diarrhea. The most limiting adverse effects were abdominal pain (two patients), raised hepatic enzymes (two patients), and abdominal pain with raised hepatic enzymes (one patient). Minor symptoms occurred in nine patients.
In 304 infants and children under 14 years adverse effects occurred in 6.9%. Treatment was withdrawn in 10 children (two with vomiting, two diarrhea, and six rashes).
In 480 elderly patients (over 65 years), there were adverse events in 3.1% and treatment was withdrawn in 1.9%. The gastrointestinal tract was most often affected, whereas laboratory changes (increases in bilirubin, aspar-tate transaminase, alanine transaminase, and alkaline phosphatase) were seen in under 0.7%.
Organs and Systems
Cardiovascular
Torsade de pointes has been reported in an 83-year-old man who developed severe prolongation of the QT interval after taking roxithromycin 300 mg/day for 4 days.
Respiratory
Eosinophilic pneumonia of acute onset has been attributed to roxithromycin.
A 21-year-old woman developed a fever of 39°C, a generalized pruritic macular rash, odynophagia, and intense weakness, in conjunction with respiratory difficulties 8 days after starting to take roxithromycin 150 mg bd. Her leukocyte count was 15.4 x 109/1 with 9.8% eosinophiis and an erythrocyte sedimentation rate of 32 mm/hour. Peripheral infiltrates were evident on the chest X-ray and CT scan, with multiple areas of consolidation and an air bronchogram, mainly peripherally distributed. Bronchoalveolar lavage showed 50% eosinophiis. She improved with giucocorticoids and 6 months later was free of respiratory symptoms; a chest X-ray was normal.
Hematologic
In one study lymphopenia or eosinophilia were observed in two of 37 patients. However, this finding could not be confirmed in other studies.
Gastrointestinal
During long-term use of roxithromycin 300 mg/day for 2-66 months in nine patients with chronic diffuse scleros-ing osteomyelitis of the mandible, diarrhea and stomach discomfort occurred in one case and liver dysfunction in another.
Liver
- Cholestatic and hepatocellular liver damage occurred in a previously healthy 20-year-old woman after she took roxithromycin 150 mg bd for 4 days.
- Hepatic failure occurred in a previously healthy 5-year-old boy after he was given roxithromycin 50 mg bd for 5 days. He developed a non-pruritic, non-urticarial, erythematous, maculopapular, generalized rash, and occasional vomiting. Three days later he became jaundiced, and after 8 days underwent liver transplantation.
Skin
Allergic dermatitis with characteristic distribution pattern called “baboon syndrome” has been reported.
A 58-year-old man developed a pruritic skin eruption after he had taken roxithromycin 300 mg/day for 3 days. Large erythematous plaques covered his buttocks. Roxithromycin was immediately withdrawn and following treatment with oral antihistamines and topical corticosteroids the rash resolved within a few days.
Urticarial rashes have been attributed to roxithromycin.
Roxithromycin-induced generalized urticaria and tachycardia with a positive prick test and a cross-reaction to erythromycin and clarithromycin has been reported in a 31-year-old woman.
Angioedema and urticaria occurred in a 22-year-old woman a few hours after a second dose of roxithromycin 150 mg for a sore throat. The lesions subsided within 12 hours of drug withdrawal and there was no relapse after 3 months of follow-up. A skin prick test was positive for roxithromycin (1 mg/ml) and negative for erythromycin and clarithromycin in the same concentrations.
Immunologic
Roxithromycin had an immunomodulatory action on peripheral blood mononuclear cells in patients with psoriasis. The anti-inflammatory activity of roxithromycin is due to reduced production of proinflammatory mediators, cytokines, and co-stimulatory molecules, as has been shown in animal studies.
Drug-Drug Interactions
Antacids
Roxithromycin did not interact with antacids containing hydroxides of aluminium and magnesium.
Carbamazepine
Roxithromycin did not alter the pharmacokinetics of carbamazepine or interact with warfarin, ranitidine, or antacids containing hydroxides of aluminium and magnesium.
Oral contraceptives
Plasma concentrations of oral contraceptive steroids were unchanged when roxithromycin was co-administered.
Ranitidine
Roxithromycin did not interact with ranitidine.
Statins
In an open, randomized, crossover study in 12 healthy volunteers, roxithromycin did not alter the pharmacokinetics of lovastatin in such a way that dosage adjustment of lovastatin should be necessary during co-administration.
Myopathy occurred in a 73-year-old woman taking sim-vastatin 80 mg/day and gemfibrozil 600 mg bd 4 days after she started to take roxithromycin 300 mg/day.
Theophylline
Roxithromycin altered the pharmacokinetics of theophylline, mainly increasing the Cmax, prolonging the half-life, and increasing the renal clearance. However, while these changes were statistically significant, they were considered clinically irrelevant. There was no effect of roxithromycin on trough concentrations of theophylline.
Warfarin
Roxithromycin did not interact with warfarin.
Preparations
Proprietary Preparations
- Argentina: Anuar; Delos; Klomicina; Rulid; Sinurit;
- Australia: Biaxsig; Roxar; Roximycin; Rulide;
- Austria: Roxithrostad; Rulide;
- Belgium: Claramid; Docroxithro; Rulid;
- Brazil: Floxid; Rotram; Roxid; Roxina; Roxitran; Roxitricina; Roxitrom; Roxitromin; Rulid;
- Chile: Ramivan;
- Czech Republic: Rovenal; Rulid;
- Denmark: Forilirr; Forimycin; Roximstad; Surlid;
- Finland: Roxibion; Surlicl;
- France: Claramid; Rulid; Subroxine;
- Germany; Infectoroxit; Romyk Roxi; Roxipaed; Roxi-Puren; Roxi-Q; Roxisaar; Roxibeta; Roxidura; Roxigamma; Roxigrun; RoxiHefa; RoxiHexal; Roxiklinge; Roxithro-Lich; Rulid;
- Greece: Acevor; Anti-Bio; Aristom/cin; Asmetic; Azuril; Bazuctril; Bicofen; Delitroxin; Erybros; Macrolid-S; Neo-Suxigal; Nirox; Oxetine; Redotrin; Roxibron; Roxicillin; Roximin; Roxitazon; Roxivinol; Roxy-Due; Roxyspes; Rulid; Seide; Siguon; Thriostaxil; Tirabicin; Toscam/cin-R; Uramilon; Vaselpin; Vomitoran;
- Hong Kong; Roxicin; Rudin; Rulid; Uonin;
- Hungary: Renicin; Rulid;
- India: Biorox; Roxee; Roxem; Roxeptin; Roxibid; Roxid; Roxivista; Roxyrol; Unorox;
- Indonesia: Anbiolid; Biostatik Ixor; Rolexit; Rulid; Ruxcine; Simacron; Sitro; Uplores; Xorin;
- Israel: Roxo; Rulid;
- Italy: Assoral; Overal; Rossitrol; Rulid
- Malaysia: Roxcin; Roxinox; Rulid; Uonin;
- Mexico: Crolix; Kensodic; Rulid Sertrom;
- The Netherlands: Rulide;
- New Zealand: Romicin;
- Philippines: Macrol; Marulide; Rulid Ruthison; Thromyn;
- Poland: Renicin; Rolicyn; Roxiratio; Roxitron; Rulid; Xitrocin;
- Portugal: Inferoxin; Odonticina; Roxitron; Rulide;
- South Africa: Roxulide; Roxxibid; Rulide; Throsyn;
- Singapore; Roxid; Rulid;
- Spain: Macrosil; Rotramin; Rulide;
- Sweden: Surlid;
- Switzerland: Rulid;
- Thailand: Ammirox; Eroxade; Poliroxin; Rothricin; Roxcin; Roxicin; Roxilan; Roximin; Roxithro; Roxithroxyl; Roxitin; Roxitop; Roxlecon; Roxomycin; Roxthomed; Roxthrin; Roxto; Roxtrocin; Roxy; Roxydin; Rucin; Rulid; Uonin; Utolid; Vesthromycin;
- Turkey: Remora; Ritosin; Roksimin; Roksolit; Rulid;
- Venezuela: Rancolid; Roxicure; Roxitrol; Rulid.
Multi-ingredient
- India: Roxeptin-ME
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Therapeutic classes of Roxithromycin:
Anti-Bacterial Agents, Macrolides
Delivery
Australia, Canada, Mexico, New Zealand, USA, Europe [Belgium, France, Norway, Holland, Ireland, Spain, Switzerland, Great Britain (UK), Italy] and etc.