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level: DRUGS

Questions and Answers List

level questions: DRUGS

Question	Answer
First macrolides in 1950 and 1952	1950: Picromycin 1952: Erythromycin and Carbomycin
Macrolides which display the best activity against GRAM POSITIVE AEROBES against Staphylococcus aureus, Streptococcus pneumoniae, Bacillus pneumoniae	Erythromycin & Clarithromycin
Macrolides which display the best activity against GRAM NEGATIVE AEROBES against H.influenzae, Neisseria spp., Bordetella pertussis	Azithromycin Newer macrolides
Drug Of Choice for Legionnaire's disease For patients allergic to pens Use: Upper respiratory tract infections cause by gram +. Inhibitor of CYP-450 Oral and topical administration Very bitter> enteric coated, delayed release from Streptomyces erythraeus	Erythromycin BN: E-Mycin, Erythrocin, Ilotycin
Erythromycin Modification 1 __ for parenteral dosage forms 2 __ for improved oral absorption 3 Acid salts of the dimethylamino group of desosamine moiety 4 Esters of the 2'- hydroxyl group of the desosamine	. 1 increase either its water or lipid solubility 2 increase its acid stability 3 glucoheptonate, lactobionate, stearate 4 ethylsuccinate, propionate, available as the lauryl sulfate, known as estolate
Stearic acid salt of erythromycin Acid labile Film coated to protect it from acid degradation of stomach given as oral dosage form	Erythromycin stearate
2' hydroxyl group of desosamine is esterified Somewhat acid labile Absorption is absorbed in the presence of food parenteral preparation	Erythromycin ethylsuccinate
Erythromycin propionate lauryl sulfate (Ilosone) Incidence of CHOLESTATIC HEPATITIS Lauryl sulfate salt of the 2' propionate ester of erythromycin Acid stable prepared as suspension	Erythromycin estolate
6-methyl ether of erythromycin. Methylation of 6-hydroxyl group. Better acid stability > Oral administration Reduced GI side effects and superior activity than erythromycin Enzyme inhibitor Methylated form of Erythromycin	Clarithromycin (Biaxin)
It is more potent than erythromycin against STAPH and STREP Food does not affect absorption Extended release form typically given once daily as 1 g DOSE	Clarithromycin (Biaxin)
Clarithromycin extended release form typically given daily as __ dose	1 g
Nitrogen containing, 15 membered ring called azalides. Act against H. influenza, M. catarrhalis, M. pneumoniae> 5 day dosing for respiratory tract infections Stability to acid catalyzed degradation Increase lipid solubility Taken 1 hr before or 2 hrs after meal Food ↓ absorption PROLONGED HALF-LIFE UP TO 5 DAYS. MORE ACTIVE AGAINST GRAM NEGATIVE. ONCE DAILY DOSING.	Azithromycin( Zithromax)
SINGLE DOSE TREATMENT for urogenital and STD caused by C. trachomatis, N. gonorrhea, H. ducreyi, Ureaplasma urealyticum	Azithromycin( Zithromax)
MOST POTENT CYP450 inhibitor Oleandomycin, triacetyl derivative troleandomycin, triacetyloleandomycin (TAO) TREATMENT of Upper Respiratory Tract infections caused by S. pyogenes and S. pneumoniae Alternative to erythromycin of an oral dosage forms	Troleandomycin