Macrolide antibiotics action

Eryfhramycin Benzoyl Peroxide (Benzamycin) [Anti-intective/ Macrolide/Keratolytic] Uses Topical for acne vulgaris Action Macrolide antibiotic w/ keratolytic Dose Apply bid (am pm) Caution [C, ] Contra Component sensitivity Disp Gel SE Local irritation, dryness EMS See Erythromycin OD Unlikely... 

Er hromycin Sulfisoxazole (Eryzole, Pediazole) [Anti-infective, Macrolide/Sulfonamide] Uses Upper lower resp tract bacterial Infxns H. influenzae otitis media in children Infxns in PCN-allergic pts Action Macrolide antibiotic w/ sulfonamide Dose Adults. Based on erythromycin content 400 mg erythromycin/1200 mg sulfisoxazole PO q6h Feds > 2 mo. 40-50 mg/kg/d erythromycin 150 mg/kg/d sulfisoxazole PO -s- q6h max 2 g/d erythromycin or 6 g/d sulfisoxazole x 10 d in renal impair Caution [C (D if near term), +] w/ PO anticoagulants, hypoglycemics, phenytoin, cyclosporine Contra Infants <2 mo Disp Susp SE GI upset Additional Interactions T Effects of sulfonamides W/ ASA, diuretics, NSAIDs, probenecid EMS See Erythromycin OD See Erythromycin... 

Erythromycin, Ophthalmic (llotycin Ophthalmic) [Anti infective, Macrolioe, Opthalmic agent] U e Conjunctival/comeal Infxns Action Macrolide antibiotic Dose 1/2 in 2-6 x /d Caution [B, +] Contra Erythromycin hyp sensitivity Disp Oint SE Local irritation EMS See Erythromycin may cause burning, stinging, blurred vision... 

Rapamycin (sirolimus), a macrolide antibiotic, has been used recently in organ transplantation for its potent immunosuppressive actions by inhibiting both cytokine mediated and growth factor mediated proliferation of smooth muscle cells and lymphocytes [55, 56]. In the RAVEL trial of non-acute single vessel lesions, the Sirolimus-eluting stent was compared to bare metal stent (BMS) in a 1 1 fashion [57]. One-year major adverse cardiovascular events and 6 month neointimal proliferation as assessed by late luminal loss (-0.01 0.33 mm in Sirolimus stent versus 0.80 0.53 mm in BMS) were improved. The Sirolimus-eluting stent thus virtually eliminated in-stent restenosis with no evidence of edge effect, dissection, or in-stent thrombosis. 

Although it is not chemically related to cyclosporine, tacrolimus (6.7) has a similar mechanism of action. Tacrolimus is an immunosuppressant macrolide antibiotic derived from Streptomyces tsukubaenis. Like cyclosporine, tacrolimus inhibits the same cytoplasmic phosphatase, calcineurin, which catalyzes the activation of a T-cell-specific transcription factor (NF-AT) involved in the biosyntheses of interleukins such as IL-2. Sirolimus (6.8) is a natural product produced by Streptomyces hydroscopicus, it blocks the ability of T cells to respond to cytokines. 

Tacrolimus (FK 506) is an immunosuppressant macrolide antibiotic produced by Streptomyces tsukubaensis. It is not chemically related to cyclosporine, but their mechanisms of action are similar. Both drugs bind to cytoplasmic peptidyl-prolyl isomerases that are abundant in all tissues. While cyclosporine binds to cyclophilin, tacrolimus binds to the immunophilin FK-binding protein (FKBP). Both complexes inhibit calcineurin, which is necessary for the activation of the T-cell-specific transcription factor NF-AT. 

Sirolimus, a macrolide antibiotic, in one mode of action, binds to FK506-binding protein (FKBP12), inhibiting the activation of mammalian target of rapamycin (mTOR), which, in turn, blocks the cellular transition from G, to the S phase of the cell cycle (35). Sirolimus was approved by the Food and Drug Administration (FDA) in 1999 for the prevention of renal... 

Roxithromycin is a macrolide antibiotic with actions and uses similar to those of erythromycin. 

This class of macrolide antibiotic has mostly antiparasitic activity. Avermectin Bia (45) and ivermectin (46) (O Scheme 18) are used mostly in veterinary medicine, however, some semisynthetic derivatives are also used for treatment of onchocerciasis in humans [59]. The action of avermectin is believed to stimulate specific chloride ion transport systems increasing the membrane permeability to Cl ions via GABA (y-butyrate) receptors and non-GABA receptors [60]. 

The mode of action of macrolide antibiotics involves the inhibition of protein synthesis of specific binding to the 50S ribosomal subunit but without a specific target at the 23S ribosomal subunit and various proteins [66]. Nevertheless, the exact interaction of the macrolide and the ribosome unit is still not fully understood. In principle, the macrolide antibiotic should inhibit also mammalian mitochondrial protein syuithesis but they are unable to penetrate the mitochondrial membrane. 

The macrolide antibiotics include erythromycin, clarithromycin, azithromycin, tylosin, tilmicosin and tiamulin. Clindamycin and lincomycin are related lincosamides. Susceptible bacteria include staphylococci, streptococci, Campylobacter jejunii, Clostridium spp., R. equi, Mycoplasma pneumoniae and Chlamydia spp. Drugs in this group are only effective against a few Gram-negative bacteria in cattle, namely some strains of Pasteurella and Haemophilus spp. Macrolides and lincosamides are associated with causing colitis in horses, so their use is usually restricted to p.o. erythromycin for the treatment of R. equi infections in foals. Subantimicrobial doses of erythromycin are administered i.v. to horses for gastrointestinal prokinetic action. 

Rapamycin (sirolimus) is also a natural product, from a soil organism, which is unrelated to cyclosporin but has similar actions, though binding to a different immunophilins. Tacrolimus is a recently introduced macrolide antibiotic similar to cyclosporin, but appears to have a higher incidence of neurotoxicity and nephrotoxicity. 

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