COMPOSITION

Simpli-3™ Tablet: Each tablet contains Azithromycin BP 500 mg.

PHARMACOLOGICAL INFORMATION

Pharmacological action

Simpli-3™ (Azithromycin) is a broad spectrum azalide, a subclass of macrolide antibiotics active against many Gram-positive and Gram-negative organisms. It prevents bacteria from growing by interfering with their protein synthesis.

Mechanism of action

Simpli-3™ (Azithromycin) binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA. Simpli-3 TM (Azithromycin) has similar antimicrobial spectrum as erythromycin, Azithromycin demonstrates activity in vitro against a wide range of Gram-positive and Gram-negative bacteria including: Staphylococcus aureus; Streptococcus pneumoniae, Streptococcus pyogenes and other Streptococcus species; Haemophilus influenzae; Moraxella catarrhalis; Legionella pneumophila, Bordetella pertussis; Borrelia burgdorferi; Haemophilus ducreyi and Chlamydia trachomatis. Azithromycin also demonstrates in vitro activity against Mycoplasma pneumoniae and Treponema pallidum.

PHARMACOKINETIC PROPERTIES

Simpli-3™ (Azithromycin) is relatively rapidly absorbed from the small intestine, with peak plasma concentrations being attained 2-3 hours after a single oral dose of 500 mg. Simpli-3 (Azithromycin) is widely distributed throughout the body; bioavailability is approximately 37% after a single oral dose of 500 mg.

Kinetic studies of variable times ranging from hours to days after oral intake have shown markedly higher Azithromycin levels in tissue than in plasma (up to 50 times the maximum observed concentration in plasma) indicating that the drug is highly tissue bound. Concentrations in target tissues such as lung, tonsil and prostate exceed the MIC90 for likely pathogens after a single dose of 500 mg.

CLINICAL INFORMATION

Therapeutic Indications

Simpli-3™ (Azithromycin) is indicated for infections (caused by susceptible organisms)

Upper respiratory tract infections including sinusitis, pharyngitis, tonsillitis and otitis media

lower respiratory tract infections including bronchitis due to Haemophilus influenzae, Moraxella catarrhalis, Streptococcus pneumoniae or Staphylococcus aureus and pneumonia due to Streptococcus pneumoniae or Haemophilus influenzae

Skin and soft tissue infections

Sexually transmitted diseases in men and women especially in the treatment of non-gonococcal urethritis and cervicitis due to Chlamydia trachomatis

Mycobacterium avium-intracellulare complex infections in AIDS

Other sensitive infections like odontogenic infections

As antimalarial in prophylaxis treatment

Dosage & Administration

Simpli-3™ tablet should be administered as a single daily dose with or without food.

Adults: For all indications other than sexually transmitted diseases, the total dose is 1.5 g which should be given as 500 mg daily for 3 days

For sexually transmitted diseases caused by Chlamydia trachomatis the dose is 1 g given as a single dose.

Use in the elderly: Normal adult dosage is recommended.

Use in hepatic impairment:

As the liver is the principal route of excretion of Azithromycin, it should not be prescribed in patients with hepatic disease.

Use in pregnancy & lactation

Pregnant women: FDA pregnancy category B. In the animal studies, no evidence of harm to the fetus due to Azithromycin was found. Because animal reproduction studies are not always predictive of human response, Azithromycin should be used during pregnancy only if clearly needed.

Lactating mother: It is not known whether Azithromycin is excreted in human milk. As many drugs are excreted in human milk, caution should be exercised when administering to a nursing woman.

Side effect

Simpli-3™ (Azithromycin) is well tolerated with a low incidence of side-effects. The side-effects include nausea, vomiting, abdominal discomfort (pain/cramps), flatulence, diarrhea, headache, dizziness and skin rashes which are reversible upon discontinuation of therapy.

Contraindications

Azithromycin is contra-indicated in patients with a known hypersensitivity to Azithromycin, erythromycin or any of the macrolide antibiotics.

Because of the theoretical possibility of ergotism, Azithromycin and ergot derivatives should not be co-administered.

Precaution

Precaution should be taken in patients with more severe renal impairment.

The drug is not recommended for use in children below 3 years or less than 15 kg body weight.

Drug Interactions

Ergot derivatives: Because of the theoretical possibility of ergotism, Simpli-3 and ergot derivatives should not be co-administered.

Antacids: Peak serum levels but not the total extent of absorption are reduced by magnesium and aluminium containing antacids in stomach.Simpli-3 tablets should be taken at least 1 hour before or 2 hours after the antacid.

Digoxin : Macrolides increases the plasma concentrations of digoxin.

Cimetidine: A single dose of Cimetidine administered 2 hours before Simpli-3 had no effect on the pharmacokinetics of Azithromycin.

Warfarin: Azithromycin and warfarin may be co-administered, but monitoring of the prothrombin time should be continued as routinely performed.

Drugs metabolized by the Cytocrome P450 System: Elevations of serum carbmazepine, terfenadine, cyclosporine, hexobarbital and phenytoin levels.

Over Dosage & Treatment

Typical symptoms of overdosage with macrolide antibiotics include hearing loss, severe nausea, vomiting and diarrhoea. Gastric lavage and general supportive measures are indicated.

PHARMACEUTICAL INFORMATION

Storage conditions

Store in a cool and dry place away from light. Keep out of reach of children.

Presentation

Simpli-3™ tablet: Each commercial box containing 1X6's tablets in Alu-Alu blister pack.