SPIRAZOLE film coated tablet -spiramycin from Pharaonia Pharma

SPIRAZOLE tablet compsition

Each tablet contains

Active ingredients

  • Spiramycin …..750,000 IU
  • Metronidazole …..125 mg

Inactive ingredients

maize starch, povidone k30, croscarmellose sodium, magnesium stearate, lactose monohydrate, HPMC, titanium dioxide, talc powder, PEG 6000, PEG 400.

PHARMACOLOGICAL  ACTION

Pharmacotherapeutic class: antibacterial combination

Spirazole is a combination of spiramycin which is a macrolide antibacterial, and metronidazole which is a 5-nitro-imidazole antibacterial.

Spirazole is active against a wide range of pathogenic micro-organisms notably antiparasitic activity.

The complementary combination shows synergism in inhibiting certain sensitive bacteria involved in buccodental infections.

PHARMACOKINETICS

Spiramycin  pharmacokinetics

– Absorption of spiramycin is fast but incomplete and not modified by food intake.

– Plasma half life is approximately 8 hours.

– Plasma protein binding is weak.

– Salivary and tissue diffusion is excellent.

– Spirarmycm is metabolized in the liver resulting in chemically unknown active metabolites.

– Excretion is mainly biliary.

Metronidazole pharmacokinetics

– After oral administration, the absorption of metronidazole is fast, 80% in less than one hour.

– The serum peaks obtained after oral administration is similar to that obtained after intravenous administration

in equivalent doses. The oral bioavailability is 100% and it is not significantly modified by simultaneous food intake. – The plasma half life is 8 to 10 hours.

– The blood proteins binding is not significant: less than 20%.

– Wide distribution into most body tissues and fluid.

– Metronidazole is metabolized by oxidation in the liver to a number of metabolites, one of which (hydroxyl

metabolite) has some antibacterial activity.

– Excretion is mainly in urine as a nitro-containing compounds.

Both constituents of this medication are concentrated in saliva, gingival tissue and alveolar bone.

Spirazole Indications

Treatment of acute and chronic stomatologic infections:

– Dental absecesses, phlegmons, perimaxillary cellulitis, pericoronitis.

– Gingivitis and stomatitis. •

– Parodentitis.

Parotiditis and submaxillaritis.

Prophylactic treatment of local post-operative infection complications in odonstomatologic surgery.

DOSAGE AND ADMINISTRATION

Adult dosage

4 to 6 tablets divided on 2 to 3 times/day during meals.

In severe cases the dose may be increased to 8 tablets/day.

Children 6 – 10  years

 2 tablets/day.

Children 10 – 15 years

3 tablets / day.

CONTRAINDICATIONS

Hypersensitivity to metronidazole , spiramycin or any of the excipients.

Spirazole side effects

Spiramycin side effects

  • gastric pain, nausea, vomiting, diarrhea, very rare cases of pseudomembranous colitis .
  • rash, urticaria, pruritis, very rare cases of Quinke oedema, anaphylaxis, acute generalized exanthematous pustulosis .
  • peripheral and central nervous system: occasional and transient parathesia.
  • Liver : rare cases of abnorrnal liver function tests
  • Haematology : very rare cases of haemolytic anemia.

Metronidazole side effects

  • Gastrointestinal: epigastric pain, nausea, vomiting, diarrhea, dry mouth, stomatitis, metallic taste, anorexia, exceptional and reversible cases of pancreatitis.
  • Hypersensitivity reactions: flushing, pruritis, rash, sometimes fever, urticaria, Quinke oedema, anaphylaxis may occur rarely.
  • Peripheral and central nervous system: headache, peripheral neuropathy, convulsions, vertigo, ataxia, confusion. hallucinations.
  • Haematology: very rare cases of neutropenia, agranulocytosis, thrombocytopenia.
  • Liver: very rare cases of reversible abnormal liver function tests and cholestatic hepatitis. Other: brown reddish colouration of urine may appear due to soluble metabolite products.

DRUG INTERACTIONS

Spiramycin drug interactions

Monitoring the dose of levodopa, as the absorption of carbidopa is inhibited with the decrease in levodopa plasma concentrations.

Metronidazole drug interactins

– Psychotic reactions have been reported In patients who are using metronidazole and disulfuram.

Intake of medications containing alcohol during metronidazole therapy may cause disulfuram like reaction.

– Potentiation of anticoagulant effect and increased haemorrhagic risk of oral anticoagulants. Dosage of the oral anticoagulant may require to be reduced and prothrombin level should be more frequently monitored.

– Increased toxicity of fluorouracil caused by reduction in its clearance.

– Metronidazole may immobilize treponema, thus giving false positive Nelson test.

WARNINGS

– Treatment with spiramycm should be discontinued in case of appearance of generalized febrile erythema associated with pustule. occurrence of ataxia, vertigo, mental confusion.

– Metronidazole should be used with caution in patients with active or chronic severe peripheral and central nervous system diseases due to the risk of neurological aggravation.

PRECAUTIONS

– Administration of spiramycin is not recommended in patients suffering from deficit in glucose-6-phosphate dehydrogenase, as rare cases of haematolytic anemia were reported.

– In case of high doses or prolonged treatment, it is recommended that haematological test, especially

Leuckocyte count should be carried out regularly.

– Proceeding treatment in case of leucopenia depends on the infection severity.

– In case of prolonged treatment, patients should be monitored for adverse reactions such as peripheral or

central neuropathy (parasthesia, ataxia, dizziness, convulsive seizures).

PREGNANCY & LACTATION

The administration of Spirazole can be considered during any stage of pregnancy if needed.

Metronidazole did not show any malformatif or foetotoxic effect in studies on high number of pregnancies.

Studies in animals did not show evidence of metronidazole teratogenic effect.

So far, excessive intake of spiramycin during pregnancy did not show malformatif or foetotoxic effect.

Spirazole should not be used during lactation as metronidazole and spiramycin pass in milk.

EFFECTS ON ABILITY TO DRIVE AND USE MACHINES

Patients should be warned about the potential for confusion, dizziness, hallucinations or convulsions and advised not to drive or operate machinery if these symptoms occur.

OVERDOSE

No specific antidote for spiramycin or metronidazole. In case of overdosage, the treatment is symptomatic.

PACKAGE

A carton box containing 20 tablets in two ( PVC/AI) strips with a pamphlet

STORAGE

Keep at a temperature not exceeding 30°C in dry place.

Keep out of reach of children.

Company

Produced by: Pharaonia pharmaceuticals (Pharo Pharma)

New Burg El Arab city – 3rd Industrial zone – block no. 16 – Alexandria – Egypt.

spirazole patient information leaflet

SPIRAZOLE tablet
SPIRAZOLE tablet