Floctil

Azithromycin dihydrate.

Each capsule contains Azithromycin dihydrate 262.02 mg eq. to Azithromycin 250 mg.
FLOCTIL 100: Each bottle contains 5 mL of suspension contains Azithromycin dihydrate 104.82 mg eq. to azithromycin 100 mg.
FLOCTIL 200: Each bottle contains 5 mL of suspension contains Azithromycin dihydrate 209.64 mg eq. to azithromycin 200 mg.

Pharmacology: Pharmacodynamics: Azithromycin binds to the 23S rRNA of the 50s ribosomal subunit of susceptible microorganisms, thus, interfering with microbial protein synthesis.
Pharmacokinetics: Absorption: Oral: Rapid from the GI tract.
Distribution: Extensive tissue, distributes well into skin, lungs, sputum, tonsils, and cervix; penetration into CSF is poor; V_d: 31 to 33 L/kg.
Protein binding: 7% to 51%.
Metabolism: Hepatic to inactive metabolites.
Bioavailability: 34% to 52%.
Half-life elimination: Adults: 68 to 72 hours.
Time to peak: 2 to 3 hours.
Excretion: Biliary (major route 50%, unchanged) urine (6% to 14% unchanged).

Respiratory tract infection: Lower respiratory tract infections including bronchitis and pneumonia.
Acute otitis media: Treatment of acute otitis media due to susceptible organisms infections.
Sinusitis: Treatment of sinusitis due to susceptible organisms infections.
Pharyngitis/tonsillitis: Treatment of pharyngitis/tonsillitis due to Streptococcus pyogenes as an alternative to first-line therapy.
Skin and skin structure infection: Treatment of skin and skin structure infections.
Sexual transmission disease: Chancroid: Treatment of genital ulcer disease (in men) due to Haemophilus ducreyi (chancroid).
Treatment of uncomplicated genital infections due to Chlamydia trachomatis and non-multiresistant Neisseria gonorrhoeae.
Odontostomatological infections: Odontostomatological infections.

Each dose of the capsules should be taken at least 1 hour before or 2 hours after food.
Azithromycin powder for oral suspension can be taken with or without food.
Dosing: Adult & Geriatric: Mild to moderate respiratory tract, skin, and soft tissue infections: Oral: 500 mg in a single loading dose on day 1 followed by 250 mg daily as a single dose on day 2 to 5.
Acute bacterial sinusitis: 500 mg daily for a total of 3 days.
Pharyngitis/tonsillitis: Oral: 500 mg in a single loading dose on day 1 followed by 250 mg daily as a single dose on day 2 to 5.
Chancroid, Chlamydia trachomatis and non-multiresistant Neisseria gonorrhoeae infections: 1 g as a single dose.
Odontostomatological infections: 500 mg daily for a total of 3 days.
Renal Impairment: Use with caution in patients with GFR <10 mL/minute.
No dosage adjustment is provided.
No supplement dose or dosage adjustment necessary including patients on intermittent hemodialysis, peritoneal dialysis, or continuous renal replacement therapy (eg, CVVHD).
Hepatic Impairment: No dosage adjustment is provided.
Use with caution due to potential for hepatotoxicity (rare); Discontinue immediately for signs or symptoms of hepatitis.
Powder for oral suspension: Children: Acute otitis media: 30 mg/kg as a single dose or 10 mg/kg once daily for 3 days or 10 mg/kg as a single dose on Day 1 followed by 5 mg/kg/day on days 2 to 5.
Pharyngitis/tonsillitis (≥2 years and adolescent): 12 mg/kg once daily for 5 days. (See table.)

Click on icon to see table/diagram/image

Significant toxicity following acute overdose is uncommon. Side effects can occur even within the therapeutic range of dosing. Treatment is symptomatic and supportive.

Hypersensitivity to azithromycin, erythromycin, other macrolide (eg. azalide or ketolide) antibiotics, or any component of the formulation.
History of cholestatic jaundice/hepatic dysfunction associated with prior azithromycin use.

(Based on the Ministry of Public Health Announcement): 1. Do not use in hypersensitive patients.
2. This drug may cause liver damage.

Use with caution in patients with preexisting liver disease; hepatocellular and/or cholestatic hepatitis, with or without jaundice, hepatic necrosis, failure and death have occurred. Discontinue immediately if symptoms of hepatitis occur (malaise, nausea, vomiting, abdominal colic, fever).
Allergic (hypersensitivity) reactions (eg. angioedema, anaphylaxis, Stevens-Johnson syndrome, toxic epidermal necrolysis, and drug reaction with eosinophilia and systemic symptoms (DRESS)) have been reported (rare), including fatalities.
May mask or delay symptoms of incubating gonorrhea or syphilis, so appropriate culture and susceptibility tests should be performed prior to initiating a treatment regimen.
Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD); CDAD has been observed >2 months post-antibiotic treatment.
Use caution with renal dysfunction.
Macrolides (especially erythromycin) have been associated with rare QT_c prolongation and ventricular arrhythmias including torsade de pointes.

Pregnancy risk factor B.
Adverse events were not observed in animal reproduction studies.
Azithromycin is excreted in breast milk. Caution should be exercised when administering azithromycin to breast-feeding women.

Common: Gastrointestinal: Abdominal pain, Diarrhea, Flatulence, Nausea, Vomiting.
Hepatic: Increased Liver enzymes.
Neurologic: Headache.
Ophthalmic: Abnormal vision.
Serious: Cardiovascular: Prolonged QT interval, Torsades de pointes.
Dermatologic: Generalized exanthematous pustulosis, Stevens-Johnson syndrome, Toxic epidermal necrolysis.
Gastrointestinal: Congenital hypertrophic pyloric stenosis.
Hepatic: Hepatic necrosis, Hepatitis, Liver failure.
Immunologic: Drug reaction with eosinophilia and systemic symptoms, Hypersensitivity reaction.
Musculoskeletal: Eaton-Lambert syndrome, Exacerbation of myasthenia gravis, Myasthenic crisis.

Azithromycin is metabolized by enzyme CYP3A4 (minor).
Azithromycin inhibits enzyme CYP1A2 (weak), P-glycoprotein.
Concurrent use of ergot derivative and macrolide antibiotics may result in an increased risk of acute ergotism (nausea, vomiting, vasospastic ischemia).
Concurrent use of azithromycin and warfarin may result in an increased risk of bleeding.
Concurrent use of azithromycin and digoxin may result in digoxin toxicity (vomiting, cardiac arrhythmias).
Concurrent use of azithromycin and simvastatin, lovastatin, or atorvastatin may result in an increased risk of rhabdomyolysis.
Concurrent use of azithromycin and imipramine, lopinavir, apomorphine, nilotinib, vardenafil, citalopram, paliperidone, alfuzosin, lumefantrine, trazodone, granisetron, ranolazine, solifenacin, sunitinib, promethazine, mifepristone, arsenic trioxide, salmeterol, nortriptyline, norfloxacin, clozapine, sorafenib, chloroquine, propafenone, haloperidol, posaconazole, ciprofloxacin, gemifloxacin, ondansetron, pentamidine, ofloxacin, amitriptyline, voriconazole, clomipramine, fluconazole, ketoconazole, quinine, lapatinib, trimipramine, flecainide, octreotide, prochlorperazine, chlorpromazine, pazopanib, mefloquine, domperidone, sodium phosphate may result in an increased risk of QT interval prolongation.
Concurrent use of azithromycin and procainamide may result in an increased risk of QT interval prolongation and serious cardiac events.
Concurrent use of azithromycin and Class III antiarrhythmic agents may result in an increased risk of cardiotoxicity.
Concurrent use of azithromycin and theophylline may result in increase serum theophylline may result in increased serum theophylline.
Concurrent use of azithromycin and phenytoin may result in increased serum phenytoin levels.
Concurrent use of azithromycin and cyclosporine may result in increased serum cyclosporine levels.
Concurrent use of azithromycin and aluminium- or magnesium-containing products may result in decreased azithromycin plasma concentration.
Concurrent use of azithromycin and carbamazepine may result in increased serum carbamazepine levels.

Constituting instructions: Powders for oral suspension 100 mg, 200 mg: 1. Gently shake the bottle to loosen the powder.
2. Open the cap of the bottle, push down and turn.
3. Carefully add 9 ml. of water.
4. Replace the cap of the bottle. Invert the bottle and shake the bottle vigorously.
5. Shake well before each use.
After mixing, 15 ml oral suspension of FLOCTIL 100 contains azithromycin 100 mg/5ml, FLOCTIL 200 contains azithromycin 200 mg/5ml.

Capsule: Store below 30°C and in well closed container.
Powder for oral suspension: Keep below 30°C in well closed container.
After mixing, store suspension at 2-8°C and use within 10 days. Discard after 10 days.

Macrolides

J01FA10 - azithromycin ; Belongs to the class of macrolides. Used in the systemic treatment of infections.

D