INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo THROSYN 150 mg TABLET
SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

THROSYN 150 mg TABLET

COMPOSITION:
Each tablet contains:
Roxithromycin         150 mg

PHARMACOLOGICAL CLASSIFICATION:
A - 20.1.1: Broad and medium spectrum antibiotics

PHARMACOLOGICAL ACTION:
Roxithromycin is a macrolide antibiotic with a broad spectrum of activity. The mode of action is primarily bacteriostatic, with action against many Gram-positive and some Gram-negative bacteria (the antibacterial spectrum is very similar to that of erythromycin). In vitro sensitivity does not necessarily imply in vivo activity.
Gram-positive cocci:
• Streptococcus pneumoniae
• Streptococcus pyogenes
• Staphylococcus aureus (most strains)
• Bacillus anthracis
• Corynebacterium diphtheriae
• Erysipelothrix rhusiopathiae
• Listeria monocytogenes

Anaerobes: • Clostridium spp. (usually susceptible)
  • Propionibacterium acnes (vary in susceptibility)

Gram-negative cocci usually sensitive:
• Neisseria meningitidis
• Neisseria gonorrhoeae
• Moraxella catarrhalis
• Bordatella spp.
• some Brucella strains
• Flavobacterium
• Legionella spp.
• Helicobacter pylori
• Campylobacter jejuni

Other organisms usually sensitive:
• Actinomyces
• Chlamydia
• Rickettsias
• Spirochaetes such as Treponema pallidum and Borrelia burgdorferi
• Mycoplasma pneumoniae
• Mycobacterium scrofulaceum
• Mycobacterium kanssii

Mechanism of action:
Roxithromycin binds reversibly to the 5OS subunit of the ribosome, resulting in blockage of the transpeptidation or translocation reactions, inhibition of protein synthesis, and hence inhibition of cell growth. Its action is predominantly bacteriostatic, but high concentrations are slowly bactericidal against the more sensitive strains. Roxithromycin penetrates rapidly into white blood cells and macrophages.
Pharmacokinetics
Following oral administration, roxithromycin is well absorbed, with a bioavailability of about 50%. Peak plasma concentrations of about 6 to 8 micrograms per 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 per mL. Absorption is reduced when taken after, but not before, a meal. It is widely distributed in tissues and body fluids. It is reported to be about 96% bound to plasma protein (mainly beta1-acid glycoprotein) at trough concentrations, but binding is saturable, and only about 86% 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 unchanged and as metabolites; about 7 to 12% is excreted in urine, and up to 15% via the lungs. The elimination half-life is reported to range between about 8 and 13 hours, but may be more prolonged in patients with impaired hepatic or renal function and in children.

INDICATIONS:
THROSYN is used to treat infections caused by roxithromycin-sensitive bacteria.
These are, in particular:
• ear, nose and throat infections such as tonsillitis, pharyngitis, sinusitis and otitis media, due to Group A beta-haemolytic Streptococci and Streptococcus pneumoniae.
• bronchopulmonary infections such as bronchitis, pneumonia (including mycoplasma or legionella) and pertussis, due to Streptococcus pneumoniae.
• genito-urinary infections such as urethritis, cervicitis, cervico-vaginitis (caused by chlamydia, mycoplasma, and ureaplasma urealyticum but excluding gonococcal infections),
• skin infections such as furunkulosis, pyoderma, impetigo and erysipelas, due to Staphylococcus aureus and Group A beta-haemolytic Streptococci.

CONTRA-INDICATIONS:
Hypersensitivity to roxithromycin or other macrolide antibiotics.
The concomitant administration of THROSYN with vasoconstrictive ergot alkaloid derivatives.
Safety in pregnancy and lactation has not been established. (see pregnancy and lactation).

WARNINGS:
Caution should be observed when using THROSYN in patients with severe impaired hepatic function.

INTERACTIONS:
Concomitant administration with astemizole, terfenadine and cisapride may result in serious adverse effects, including ventricular arrhythmias.
THROSYN may also cause suppression of the gastrointestinal flora responsible for the metabolism of digoxin and possibly oral contraceptives.
Concomitant administration with theophylline may cause theophylline toxicity.

PREGNANCY AND LACTATION:
Safety in pregnancy and lactation has not been established.

DOSAGE AND DIRECTIONS FOR USE:
150 mg (one tablet) orally twice daily, or up to 300 mg (two tablets) once daily, before meals.
To treat beta-haemolytic streptococcal infections, the therapeutic dose must be given for a minimum of 10 days.
The dose should be halved to 150 mg daily in patients with severe impaired hepatic function.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Side-effects:
More frequently
Gastro-intestinal disorders
Nausea, vomiting, diarrhoea and gastric pain.
Less frequently
Hepato-biliary disorders
Increases in AST and ALT and hepatitis have been reported.
Skin and hypersensitivity reactions
Rashes and other hypersensitivity reactions.
Nervous system disorders
Headache and dizziness.
Blood disorders
Changes in blood cell count.
Musculoskeletal disorders
Weakness.

Special Precautions:
Accumulation of THROSYN may occur in renal insufficiency. The half-life is prolonged in elderly patients (>65 years).

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Treatment is symptomatic and supportive.

IDENTIFICATION:
White to off-white, round, convex, film-coated tablets.

PRESENTATION:
Throsyn 150 mg tablets will be packed in packs of 10 tablets in a blister strip of opaque, white PVC foil sealed onto an aluminium foil. Each blister strip is packed in unit cartons of pack sizes 10’s and 100’s.

STORAGE INSTRUCTIONS:
Store below 25°C in airtight containers.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER:
36/20.1.1/0424

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION:
PHARMACARE LIMITED
7 Fairclough Road
Korsten
Port Elizabeth
6020
South Africa

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
To be allocated

New addition to this site: September 2005
Source: Pharmaceutical Industry

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