Acithromac; uses, contraindication, side effect, toxicity and mechanism of action

Acithromac is an antibiotic used in the treatment of suspectible bacterial infections. It contains a macrolide antibiotic called Erythromycin Stearate as its active pharmaceutical ingredient.

Macrolides, such as erythromycin, stop bacterial growth by inhibiting protein synthesis and translation, treating bacterial infections.

Acithromac Erythromycin does not exert effects on nucleic acid synthesis. This drug has been shown to be active against most strains of the following microorganisms, effectively treating both in vitro and clinical infections.

Despite this, it is important to perform bacterial susceptibility testing before administering this antibiotic, as resistance is a common issue that may affect treatment.

Acithromac comes in different dosage forms which include capsule, tablet, long-acting capsule, long-acting tablet, chewable tablet, suspension, and pediatric drop forms for oral use, topical solution and gel forms and as an ophthalmic ointment. It comes in different dosage strengths.

Acithromac
Acithromac

Mechanism of Action of Acithromac

Acithromac acts by inhibition of protein synthesis by binding 50’S ribosomal subunits of susceptible organisms.

It does not affect nucleic acid synthesis. Antagonism has been demonstrated in vitro between erythromycin and clindamycin, lincomycin, and Chloramphenicol.

Many strains of Haemophilus influenzae are resistant to erythromycin alone but are susceptible to erythromycin and sulfonamides used concomitantly.

Staphylococci resistant to erythromycin may emerge during a course of erythromycin therapy.

Erythromycin is largely bound to plasma proteins. After absorption, erythromycin diffuses readily into most body fluids.

In the absence of meningeal inflammation, low concentrations are normally achieved in the spinal fluid but the passage of the drug across the blood-brain barrier increases in meningitis.

Erythromycin crosses the placental barrier, but fetal plasma levels are low. The drug is excreted in human milk

Indications and Uses of Acithromac

  • Acithromac has been used in the treatment of a wide variety of infections caused by susceptible organisms.
  • It is used to treat bronchitis, severe Campylobacter enteritis, Chancroid, diptheria legionnaire’s disease and other legionella infections, neonatal conjuntivitis, pertussis, pneumonia (mycoplasmal and other atypical pneumonias as well as streptococcal), sinusitis.
  • It has also been used in the treatment of penicillin-allergic patients with syphilis. It is also used as an alternative to tetracyclines in patients with Chlamydial infections (such as epididymitis, lymphogranuloma venereum, non gonococcal urethritis, Chlamydial pneumonia, psittacosis, Q fever and trachoma), in pelvic inflammatory disease (PID) and in tularemia.
  • Upper respiratory tract infections: Tonsillitis, peritonsillar abscess, pharyngitis, laryngitis, sinusitis, and secondary infections in cold and influenza.
  • Skin and soft tissue infections: Boils and carbuncles, paronychia, abscesses, pustular acne, impetigo, cellulitis, furuncolosis, erythrasma.
  • Veneral infections: Non-specific urethritis, syphilis (if the patient is allergic to penicillin).
  • Gastro-intestinal infections: Cholecystitis, Staphylococcal enterocolitis, infectious diarrhoea, & cholera.
  • Ear and oral infections: 0titis media and otitis externa, gingivitis, dental abscesses.
  • Prophylaxis: Pre-operative and post-operative, trauma, burns, rheumatic fever.

Contraindications of Acithromac

Acithromac is contraindicated or shouldn’t be used in patients with known hypersensitivity to this antibiotic.

Precautions

Acithromac is principally excreted by the liver. Caution Should be exercised in administering the antibiotic to patients with impaired hepatic function.

There have been reports of hepatic dysfunction, with or without jaundice, occurring in patients receiving oral erythromycin products, it has been suggested that erythromycin should be used with care in patients with a history of arrhythmia.

Side Effects of Acithromac

Side effects associated with Acithromac use include

  • Abdominal discomfort,
  • diarrhoea,
  • nausea,
  • vomiting,
  • sore mouth or tongue and
  • allergic reactions: Such as rashes, itching, swelling and dizziness.

Drug Interactions with Acithromac

The concomitant administration of theophylline with Acithromac causes potential theophylline toxicity.

In such cases the dose of theophylline should be reduced while the patient is receiving concomitant erythromycin therapy.

Erythromycin administration in children receiving carbamazepine has been reported to cause increased blood levels of carbamazepine with subsequent development of signs of carbamazepine toxicity (ataxia, dizziness, vomiting)

Erythromycin may decrease the clearance of warfarin and thus potentiate the hypoprothrombinemic effect of warfarin.

Erythromycin has been reported to decrease the clearance of triazolam and thus may increase the pharmacologic effect of triazolam.

Erythromycin has been reported to decrease the clearance of cyclosporine causing elevated cyclosporine levels and associated increased serum creatinine.

Renal function as well as serum concentration of cyclosporine should be closely monitored when both drugs are administered concomitantly.

The interaction between erythromycin and ergotamine has been reported to increase the vasospasm associated with ergotamine,

Antagonism in antibacterial activity has been demonstrated between clindamycin and erythromycin in vivo.

Toxicity

LD50

The oral LD50 of erythromycin in rats is 9272 mg/kg.

Overdose information

Symptoms of overdose may include diarrhea, nausea, stomach cramps, and vomiting. Acithromac Erythromycin should immediately be discontinued in cases of overdose.

Rapid elimination of unabsorbed drug should be attempted. Supportive measures should be initiated. Acithromac Erythromycin is not adequately removed by peritoneal dialysis or hemodialysis.

Dosage and Method of Administration of Acithromac

  • General dosing recommendation

Adults dose: 250mg every six hours

500mg every twelve hours

Children: 30-50mg/kg/day in equal divided dose.

  • Adult Dosing Recommendations

Amebiasis

500 mg PO q6hr for 10-14 days

Legionnaires Disease

1-4 g/day PO in divided doses for 21 days

Urethritis caused by C trachomatis or U urealyticum

500 mg PO q6hr for 7 days; alternatively 333 mg PO q8hr for 7 days

Syphilis

30-40 g PO in divided doses for 10-15 days

Children Dosing Recommendations

General Dosing Recommendations

Mild-to-moderate infections: 30-50 mg/kg/day PO divided q6-8hr

Intestinal Amebiasis

30-50 mg/kg/day PO in divided doses for 10-14 days

Pneumonia of Infancy

50 mg/kg/day PO divided q6hr for at least 3 weeks

Dosing terms: PO is per Oral , q6hr is every 6 hours, q8hr is 8 hourly,

  • Over dosage of Acithromac

Allergic reactions associated with acute overdose of Acithromac should be handled in the usual manner that is by the administration of adrenaline, corticosteroids and antihistamine as indicated and the prompt elimination of unabsorbed drug in addition to all needed supportive measures.

How to Store Acithromac

Store in a cool, dry place at a temperature not exceeding 25°C. Protect from light. Keep all medicine away from reach of children.

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