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Macrolides

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Macrolides

Background:  "The macrolides are a group of drugs (typically antibiotics) whose activity stems from the presence of a macrolide ring, a large macrocyclic lactone ring to which one or more deoxy sugars, usually cladinose and desosamine, may be attached. The lactone rings are usually 14-, 15-, or 16-membered. Macrolides belong to the polyketide class of natural products."

Uses:  "Antibiotic macrolides are used to treat infections caused by Gram-positive bacteria (e.g., Streptococcus pneumoniae) and Haemophilus influenzae infections such as respiratory tract and soft-tissue infections. The antimicrobial spectrum of macrolides is slightly wider than that of penicillin, and, therefore, macrolides are a common substitute for patients with a penicillin allergy. Beta-hemolytic streptococci, pneumococci, staphylococci, and enterococci are usually susceptible to macrolides. Unlike penicillin, macrolides have been shown to be effective against Legionella pneumophila, mycoplasma, mycobacteria, some rickettsia, and chlamydia." 
[Source: http://en.wikipedia.org/wiki/Macrolides]
Azithromycin (Zithromax ®) Clarithromycin (Biaxin ® ) Erythromycin
  Infectious Disease -ALL Agents (INDEX)  

Ketolides

Background:    "Ketolides are antibiotics belonging to the macrolide group. Ketolides are derived from erythromycin by substituting the cladinose sugar with a keto-group and attaching a cyclic carbamate group in the lactone ring."   [Source: http://en.wikipedia.org/wiki/Ketolide]
  Telithromycin (Ketek®)  
     

Antimicrobials - Infectious Disease

Aminoglycosides Ansamycins/Rifamycins Antibiotics (Other)
Anti- Fungals Anti-Herpetic Agents Anti-Influenza Agents
Anti-Malarials Carbapenems Cephalosporins
Fluoroquinolones Glycopeptides HIV (anti) Agents
Lincosamides Lipopeptides Macrolides
Monobactams Oxazolidones Penicillins
Sulfonamide antibiotics Tetracyclines Tuberculosis (anti) agents
     

Azithromycin  (Zithromax ®)   top of page

Dosing (Adults)
Usual oral dose
: 500mg x 1, then 250mg po qd x 4 days.
Chlamydia: 1 gram po x 1.
MAC prevention: 1200mg once a week.
Uncomplicated gonococcal infection: 2 grams po x 1.
CAP: 500mg IV qd x 2 days or more then 500mg po qd.
PID: 500mg IV x 1-2days, then 250mg (IV/PO) for total of 7 days.
Note: Extended release suspension (Zmax™) is not interchangeable with immediate release formulations. Use should be limited to approved indications. All doses are expressed as immediate release azithromycin unless otherwise specified.

Mild to moderate respiratory tract, skin, and soft tissue infections: 500 mg orally in a single loading dose on day 1 followed by 250 mg/day as a single dose on days 2-5. Alternative regimen: Bacterial exacerbation of COPD: 500 mg/day for a total of 3 days

Bacterial sinusitis: 500 mg orally once daily x 3 days.
Extended release suspension (Zmax): 2 grams x 1.

Community-acquired pneumonia:
Oral (Zmax™): 2 g as a single dose.
I.V.: 500 mg IV qd at least 2 days, then 500 mg orally ( to complete a 7 to 10 day course of therapy).

Urethritis/cervicitis:
Due to C. trachomatis: 1 gram orally x 1.
Due to N. gonorrhoeae: 2 grams orally x 1.

Chancroid due to H. ducreyi: 1 gram orally x 1.

Pelvic inflammatory disease (PID): 500 mg IV qd x 1-2 days, then 250 mg orally once daily to complete a 7 day course of therapy.

Disseminated MAC disease in patient with advanced HIV infection: Prophylaxis: 1200 mg orally once weekly (may be combined with rifabutin). Treatment: 600 mg orally once daily in combination with ethambutol 15 mg/kg.

Endocarditis, prophylaxis (unlabeled use): Oral: 500 mg 1 hour prior to the procedure

Pertussis (CDC guidelines): Oral: 500 mg on day 1 followed by 250 mg/day on days 2-5 (maximum: 500 mg/day)

Renal Dosing: No adjustments required in renal failure. Hemodialysis: No adjustments required in renal failure.

Supplied:
Tablet: 250 mg, 500 mg, 600 mg.
Zithromax® TRI-PAK - 500 mg (Unit dose package: 3 tabs)
Zithromax® Z-PAK - 250 mg (Unit dose package: 6 tabs)
Oral Suspension: 100 mg/5 ml (15 ml); 200 mg/5 ml (15 ml, 22.5 ml, 30 ml) ; 1 gram - single dose packet. Zmax: 2 gram single-dose bottle (extended release formulation).
Injection (powder for reconstitution): 500mg vial.

Clarithromycin  (Biaxin ® )  top of page

Dosing (Adults)
Usual dosage range
: Oral: 250-500 mg every 12 hours or 1000 mg (two 500 mg extended release tablets) once daily for 7-14 days.
Acute exacerbation of chronic bronchitis:
Oral:
M. catarrhalis and S. pneumoniae: 250 mg every 12 hours for 7-14 days or 1000 mg (two 500 mg extended release tablets) once daily for 7 days.
H. influenzae: 500 mg every 12 hours for 7-14 days or 1000 mg (two 500 mg extended release tablets) for 7 days.
H. parainfluenzae: 500 mg every 12 hours for 7 days or 1000 mg (two 500 mg extended release tablets) for 7 days.

Acute maxillary sinusitis: Oral: 500 mg every 12 hours or 1000 mg (two 500 mg extended release tablets) once daily for 14 days.

Endocarditis, prophylaxis: Oral: 500 mg 1 hour prior to procedure

Mycobacterial infection (prevention and treatment): Oral: 500 mg twice daily (use with other antimycobacterial drugs, eg, ethambutol or rifampin)

Peptic ulcer disease: Eradication of Helicobacter pylori: Oral: Dual or triple combination regimen with bismuth subsalicylate, tetracycline, clarithromycin, and an H2-receptor; or combination of omeprazole and clarithromycin; 500 mg every 8-12 hours for 10-14 days.

Pertussis (CDC guidelines): Oral: 500 mg twice daily for 7 days

Pharyngitis, tonsillitis: Oral: 250 mg every 12 hours for 10 days.

Pneumonia:
Oral:
C. pneumoniae, M. pneumoniae, and S. pneumoniae: 250 mg every 12 hours for 7-14 days or 1000 mg (two 500 mg extended release tablets) once daily for 7 days.
H. influenzae: 250 mg every 12 hours for 7 days or 1000 mg (two 500 mg extended release tablets) once daily for 7 days.

Skin and skin structure infection, uncomplicated: Oral: 250 mg every 12 hours for 7-14 days.

Renal Dosing:
[CRCL >30 ]: No changes.
[<30 ]: Half the normal dose or double the dosing interval.
Hemodialysis: 250 mg q12-24 hours. Schedule dose after HD on dialysis days.

Supplied:
Granules for oral suspension:
Biaxin®: 125 mg/5 mL, 250 mg/5 mL

Tablet: 250 mg, 500 mg
Biaxin®: 250 mg, 500 mg

Tablet, extended release:
Biaxin® XL: 500 mg

ADMINISTRATION — Clarithromycin may be given with or without meals. Give every 12 hours rather than twice daily to avoid peak and trough variation.

Biaxin® XL: Should be given with food. Do not crush or chew extended release tablet.

Erythromycin   top of page

Dosing (Adults)
(Oral): 500mg to 1g po q12h or 250mg to 1gm q6h.
(IV ): 250mg to 1 gm q6h. Max 4 grams/day.

Children and Adults:
Ophthalmic: Instill 1 /2" (1.25 cm) 2-6 times/day depending on the severity of the infection
Topical: Apply over the affected area twice daily after the skin has been thoroughly washed and patted dry

Adults:
Treatment of susceptible infections:
Oral:
Base: 250-500 mg every 6-12 hours
Ethylsuccinate: 400-800 mg every 6-12 hours

 I.V. (lactobionate): 15-20 mg/kg/day divided every 6 hours or 500 mg to 1 g every 6 hours, or given as a continuous infusion over 24 hours (maximum: 4 g/24 hours)

Preop bowel preparation: Oral: 1 g erythromycin base at 1, 2, and 11 PM on the day before surgery combined with mechanical cleansing of the large intestine and oral neomycin

Gastrointestinal prokinetic (unlabeled use): Erythromycin has been used as a prokinetic agent to improve gastric emptying time and intestinal motility. In adults, 200 mg was infused I.V. initially followed by 250 mg orally 3 times/day 30 minutes before meals. Lower dosages have been used in some trials.

Renal Dosing:
[>10 ml/min]: No change.
[<10 ] 50-75% of usual dose at same interval. Max 2 grams/day. [Hemo]: 50-75% of usual dose at same interval. Max 2 grams/day. No supplement.

Supplied
Capsule, delayed release, enteric-coated pellets, as base (Eryc®): 250 mg
Granules for oral suspension, as ethylsuccinate (E.E.S.®): 200 mg/5 mL (100 mL, 200 mL)
Injection, powder for reconstitution, as lactobionate (Erythrocin®): 500 mg, 1 g
Tablet, chewable, as ethylsuccinate (EryPed®): 200 mg [fruit flavor] [DSC]
Tablet, delayed release, enteric coated, as base (Ery-Tab®): 250 mg, 333 mg, 500 mg
Tablet [film coated], as base: 250 mg, 500 mg
Tablet [film coated], as ethylsuccinate (E.E.S.®): 400 mg
Tablet [film coated], as stearate: 250 mg
Erythrocin®: 250 mg, 500 mg
Tablet [polymer-coated particles], as base (PCE®): 333 mg, 500 mg

Telithromycin - Ketek ®: top of page

Ketolide antibiotic.  
INDICATIONS AND USAGE
KETEK tablets are indicated for the treatment of community-acquired pneumonia (of mild to moderate severity) due to Streptococcus pneumoniae, (including multi-drug resistant isolates [MDRSP3]), Haemophilus influenzae, Moraxella catarrhalis, Chlamydophila pneumoniae, or Mycoplasma pneumoniae, for patients 18 years old and above.

To reduce the development of drug-resistant bacteria and maintain the effectiveness of KETEK and other antibacterial drugs, KETEK should be used only to treat infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.

3. MDRSP, Multi-drug resistant Streptococcus pneumoniae includes isolates known as PRSP (penicillin-resistant Streptococcus pneumoniae), and are isolates resistant to two or more of the following antibiotics: penicillin, 2nd generation cephalosporins, e.g., cefuroxime, macrolides, tetracyclines and trimethoprim/sulfamethoxazole.

CONTRAINDICATIONS
KETEK is contraindicated in patients with myasthenia gravis. Exacerbations of myasthenia gravis have been reported in patients and sometimes occurred within a few hours of the first dose of telithromycin. Reports have included fatal and life-threatening acute respiratory failure with a rapid onset and progression.

KETEK is contraindicated in patients with previous history of hepatitis and/or jaundice associated with the use of KETEK tablets, or any macrolide antibiotic.

KETEK is contraindicated in patients with a history of hypersensitivity to telithromycin and/or any components of KETEK tablets, or any macrolide antibiotic.

Concomitant administration of KETEK with cisapride or pimozide is contraindicated.

Concomitant administration of KETEK and colchicine is contraindicated in patients with renal or hepatic impairment.

DOSAGE AND ADMINISTRATION
Dosing (Adults): 
The dose of KETEK tablets is 800 mg (2 tablets of 400 mg) taken orally once every 24 hours, for 7–10 days. KETEK tablets can be administered with or without food.

KETEK may be administered without dosage adjustment in the presence of hepatic impairment.


Renal Dosing
In the presence of severe renal impairment (CLCR < 30 mL/min), including patients who need dialysis, the dose should be reduced to KETEK 600 mg once daily. In patients undergoing hemodialysis, KETEK should be given after the dialysis session on dialysis days.

In the presence of severe renal impairment (CLCR < 30 mL/min), with coexisting hepatic impairment, the dose should be reduced to KETEK 400 mg once daily.
 
Hemodialysis
: Administer dose following dialysis.

Supplied:  300 mg, 400mg tab.

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.
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