Rokitamycin

Antibiotic Class:

Macrolide

Antimicrobial Activity:

Gram-positive bacteria, Enterococcus faecalis, Enterococcus faecius, H. influenzae, Neisseria gonorrhoeae, Moraxella catarrhalis, Bacteroides fragilis

Mechanism of Action:

Macrolides are inhibitors of protein synthesis.  They impair the elongation cycle of the peptidyl chain by specifically binding to the 50 S subunit of the ribosome.  Specificity towards prokaryotes relies upon the absence of 50S ribosomes in eukaryotes.

Pharmacodynamics:

Macrolides are considered time-dependent antibiotics.

Pharmacokinetics:

Tmax (h): 0.5-1,  T (h): 2-3,  AUC (mg *h/L): 2.05

Adverse Effects:

Gastrointestinal: stomach discomfort, nausea, vomiting, epigastric pain

Hepatic: liver function abnormalities

Hematologic: eosinophilia

Dermatologic: skin rashes, exanthema, urticaria

Ocular: blurred vision

Dosage:

Oral granules: 10g

Oral tablet: 400mg

Susceptible infections: 400mg every 12 hours for 7-14 days

Disease state based dosing:

None necessary

Contraindications/Warnings/Precautions:

Contraindications: hypersensitivity to rokitamycin.

Precautions: biliary occlusion, liver disease, concurrent use of ergotamine or carbamazepine.

Drug Interactions:

Ergot Derivatives: (major severity):

MOA: inhibition of cytochrome P450 3A4-mediated ergot derivative metabolism by a macrolide antibiotic

Management: The concurrent use of an ergot derivative and a macrolide antibiotic, such as rokitamycin, is contraindicated.

Pregnancy:

The manufacturer suggests that rokitamycin not be administered during pregnancy and lactation unless extreme circumstances require its use.

Monitoring Requirements:

Therapeutic:Periodic WBC, chest X-ray if pneumonia, cultures, vital signs

Brand names/Manufacturer:

Paidocin/Promedica (Italy), and Rokital/Formenti (Italy)