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MACROLIDES - Coggle Diagram
MACROLIDES
- Characterized by a Macrocyclic Lactone ring to which deoxy sugars are attached
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NEWER MACROLIDES
CLARITHROMYCIN SPECTRUM :check:
- ~Erythromycin
- In addition:
○ MAC, other atypical mycobacteria, Myco. leprae& some anaerobes
- More active against H.pylori, Moraxella, Legionella, Mycoplasma pneumoniae & sensitive G+
- Erythromycin resistant bacteria→ resistant to Clarithromycin also
PHARMACOKINETICS
- More acid stable, rapidly absorbed
- Oral BA: 50% d/t FPM
- Food delays abs.
- Larger tissue distribution
- Metabolised by saturation kinetics: T½ prolonged at higher dose
- Active metabolite is produced.
- Twice daily dosing possible
- ⅓ oral dose excr. unchanged in urine
○ No dose modification in kidney/liver failure
USES :check:
- URTI/ LRTI
- Sinusitis/ otitis media
- Pertussis, atypical pneumonia
- Skin & skin str. inf. d/t Strep. pyogenes & some Staph. aureus
- Component of triple drug regimen→H. pylori eradication in 1-2wks
- 1st Line in combi. regimens for MAC inf. in AIDS patients
- 2nd line for other atypical mycobacterial diseases & leprosy
Dose: 250mgBD x7days
ADVERSE EFFECTS :warning:
- High doses→ reversible hearing loss
- Pseudomembranous colitis, hepatic dysfn., rhabdomyolysis-few
- Safety in pregnancy & lactation unknown
- Inhibits CYP3A4→ similar drug interaction potential
AZITHROMYCIN
- Azalide congener of erythromycin
- Expanded spectrum, improved PK, better tolerability, & drug interaction profiles
SPECTRUM :check:
- More active against H.influenzae than others
- Less active against G+ cocci
- High action on resp. pathogens
○ Mycoplasma, Chlamydia pneumoniae, Legionella, Moraxella, Campylobacter, Ch. trachomatis, H. ducreyi, Calymm. granulomatis, N. gonorrheae
- Not active against erythromycin resistant bacteria
- Penicillinase producing Staph. inhibited, not MRSA
- Good activity against MAC
PHARMACOKINETICS
Absorption :check:
- Acid stability
- Rapid oral abs. from empty stomach
Distribution :check:
- Larger tissue distribution & intracellular penetration
- Conc. in most tissues >> plasma
- High conc. in macrophages & fibroblasts
- Vd~ 30L/kg
- Slow release from intracellular sites→ long terminal T½ >50hr
Metabolism & Excretion :check:
- Largely excreted unchanged in bile, renal excrn. 10%
USES :check:
D/t higher efficacy, better gastric tolerance & convenient OD dosing, preferred as:First choice Drug for
- Legionnaire's pneumonia:
○ 500mg OD oral/IV for 2 wks
- Chlamydia trachomatis
○ Non specific urethritis/ genital inf. : 1g single dose curative
○ Lymphogranuloma venereum→ 3 wkly doses
○ DOC for chlamydial pneumonia
- Donovanosis by Calymm. granulomatis
○ 500mg OD x7days or 1g weeklyx 4wks
- Chancroid & PPNG Urethritis
○ Single dose 1g curative/ combined with ceftriaxone
Other indications
- Pharyngitis, tonsillitis, sinusitis, otitis media, CAP, A/c exacerbatons of C/c bronchitis
- Combi with one other drug→ prophylaxis & trt. of MAC in AIDS patients
- MDR typhoid in CS allergic patients
- Toxoplasmosis
ADVERSE EFFECTS :warning:
- Mild gastric upset, abdominal pain, headache & dizziness
- Does not affect hepatic CYP3A4. But caution exercised
ROXITHROMYCIN
- Semisynthetic, longer acting acid-stable macrolide
- Good enteral abs.
- Avg plasma T½ of 12 hrs= twice daily dosing
- Alt. to erythromycin for ENT, skin, soft tissue & genital tract inf.
TELITHROMYCIN
- Ketolide congener of erythro
- Active against many penicillin & erythromycin resistant Strep. pneumoniae, B. fragilis & nonTB mycobatceria
- Oral~60% BA
- Good tissue penetration
- Inhibits CYP3A4 & has potential for QTc prolongation
- S/E: abd. pain, nausea, diarrhea, taste disturbance
- Adverse Effect: :warning: serious hepatitis
USE :check:
- Restricted use
- CAP, sinusitis & exacerbations of C/c bronchitis by resistant strep. pneumoniae
SPIRAMYCIN
- Employed only sporadically
- Limit risk of transplacental transmission of Toxoplasma gondii
- S/E: gastric irritation, nausea, diarhea, rashes
USE :check:
- Toxoplasmosis & recurrent abortion in pregnant women