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APMLE PART 1 – PHARM(SCIENCE,MEDICINE,INFECTIOUS DISEASE)WITH WELL EXPLAINED UNDERSTANDABLE ANSWERS.

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Amoxicillin - ANSWER Amino-Penicillin: wider spectrum than pen G with activity similar to ampicillin but greater oral bioavailability; less adverse effects on GI tract than ampicillin. *Susceptible to penicillinases unless used with clavulanic acid.* Tox: penicillin allergy *block the enzyme envolved in transpeptidation* Ampicillin - ANSWER *Penicillin: wider−spectrum than pen G, susceptible to penicillinases unless used with sulbactam.* Activity similar to pen G, plus E coli, H influenzae, P mirabilis, Shigella. Synergy with aminoglycosides versus enterococci and *listeria -- especially e coli UTI. Tox: penicillin allergy; more adverse effects on GI tract than other penicillins; maculopapular skin rash Azithromycin Dirithromycin Clarithromycin Troleandomycin - ANSWER *Antibiotic: similar to erythromycin (50S protein synthesis inhibitor)*, but greater activity versus chlamydia and streptococci; long half−life due to tissue accumulation.

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Amoxicillin - ANSWER Amino-Penicillin: wider spectrum than pen G with activity
similar to ampicillin but greater oral bioavailability; less adverse effects on GI tract
than ampicillin. *Susceptible to penicillinases unless used with clavulanic acid.*

Tox: penicillin allergy

*block the enzyme envolved in transpeptidation*

Ampicillin - ANSWER *Penicillin: wider−spectrum than pen G, susceptible to
penicillinases unless used with sulbactam.* Activity similar to pen G, plus E coli, H
influenzae, P mirabilis, Shigella.

Synergy with aminoglycosides versus enterococci and *listeria -- especially e coli
UTI. Tox: penicillin allergy; more adverse effects on GI tract than other penicillins;
maculopapular skin rash

Azithromycin
Dirithromycin
Clarithromycin
Troleandomycin - ANSWER *Antibiotic: similar to erythromycin (50S protein
synthesis inhibitor)*, but greater activity versus chlamydia and streptococci; long
half−life due to tissue accumulation.

Used for: "Leginnaires camp on my border": Legionella, Camplyobacter,
Mycoplasma, Bordetella.

Cefazolin
Cephalexin - ANSWER *First−generation* cephalosporin prototype: *bactericidal
betalactam inhibitor of cell wall synthesis.* Inhibit transpeptidases known as
penicillin-binding proteins (PBPs). *PBPs bind to the D-Ala-D-Ala* at the end of
muropeptides (peptidoglycan precursors) to crosslink the peptidoglycan.

Active against gram−positive cocci, E coli, K pneumoniae, but does not enter CSF.
(1st gen Narrow spectrum, destroyed by lactamse)

Tox: potential allergy; partial cross−reactivity with penicillins

, Cefoxitin - ANSWER Second−generation cephalosporin: *bactericidal betalactam
inhibitor of cell wall synthesis.* Inhibit transpeptidases known as penicillin-binding
proteins (PBPs). PBPs bind to the D-Ala-D-Ala at the end of muropeptides
(peptidoglycan precursors) to crosslink the peptidoglycan.

active against a wide spectrum of gram−negative bacteria including anaerobes (B
fragilis).

Does not enter the CNS (slight penetration)

Ceftriaxone - ANSWER Third−generation cephalosporin: *bactericidal betalactam
inhibitor of cell wall synthesis.* Inhibit transpeptidases known as penicillin-binding
proteins (PBPs). PBPs bind to the D-Ala-D-Ala at the end of muropeptides
(peptidoglycan precursors) to crosslink the peptidoglycan.

active against resistant bacteria including gonococci, H influenzae, and other
gram−negative organisms.

Crosses the blood−brain barrier, can be used for bacterial meningitis. *Used for
prophylaxisis in hospital.*

Chloramphenicol - ANSWER Antibiotic: broad spectrum agent; *inhibits protein
synthesis (50S);* uses restricted to back−up drug for bacterial meningitis, infections
due to anaerobes, Salmonella (except pseudomonas).

*Tox: reversible myelosuppression, aplastic anemia, gray baby syndrome*

Gray Baby = babies lack phase II metabolism in liver (which is the route of this drug),
which causes drug to accumulate to toxic levels in children (Vasomotor collapse).

Cipro*floxacin*...... En*oxacin*
Levofloxacin...... Ofloxacin
Sparfloxacin...... Trovafloxacin
Gatifloxacin...... Gemifloxacin
Lomefloxacin...... Moxifloxacin - ANSWER *Fluoroquinolone antibiotic:* bactericidal
inhibitor of topoisomerases (DNA Gyrase) - thus inhibit DNA synthesis. *The only
drug class that inhibits DNA synthesis. *(GTQ)

,*Active against many gram−negative rods* including E coli, H influenzae,
Campylobacter, Enterobacter, Pseudomonas, Shigella.

Uses: Lower Resp infec, Bone and Joint infections, Prostatisis.

Tox: CNS dysfunction, GI distress, superinfection, *collagen damage (avoid in
children and pregnant women).*

Clindamycin
Lincomycin - ANSWER Lincosamide antibiotic: *bacteriostatic inhibitor of protein
synthesis (50S)*; active against gram−positive cocci, B fragilis. (anaerobes).

Drug can *penetrates bone*, Drug of choice for GI Infection.

*Tox: Clostridium Difficile is resistant to Clindamycin, so patient can develope
pseudomembranous colitis (HUGE GTQ)*

Doxy*cycline* - ANSWER *Tetracycline antibiotic: protein synthesis inhibitor (30S)*
more effective than other tetracyclines against bacillary dysentery.

Unlike other tetracyclines, it is *eliminated mainly in the feces.* Tox: see tetracycline
(DOX SHIT)

Erythromycin - ANSWER Macrolide antibiotic: *inhibitor of protein synthesis (50S)*;
activity includes gram− positive cocci and bacilli:

*Used for odd ball diseases*: Mycoplasma Infections, Legionnaires disease,
Chalamydial infections, Diptheria, Pertussis)

Tox: cholestatic jaundice, inhibits liver drug−metabolizing enzymes, interactions with
astemizole, theophylline, terfenadine, warfarin

Foscarnet - ANSWER *Antiviral*: structural mimic of the anion *pyrophosphate* that
selectively inhibits the pyrophosphate binding site on *viral DNA polymerases* at
concentrations that do not affect human DNA polymerases.

*effective against CMV and HSV* (including TK− strains); PP analog.

, Tox: electrolyte imbalance (chelates and increases Ca and Mg wasting),
nephrotoxicity

Ganciclovir - ANSWER Antiviral: effective against CMV; *requires bioactivation via
thymidine kinase.* Ganciclovir triphosphate is a competitive *inhibitor of
deoxyguanosine triphosphate (dGTP) incorporation into DNA* and preferentially
inhibits viral DNA polymerases more than cellular DNA polymerases.

Tox: myelosuppression, nephrotoxicity

Gentamicin
Tobramycin
Amikacin
neomycin
netilmicin
Streptomycin - ANSWER Aminoglycoside prototype: *bactericidal inhibitor of protein
synthesis (30S)*; Active against many aerobic gram−negative bacteria. Anaerobes
are resistant, do not have O2 pumps, to get drug into bug.

*Penicillin is used to open pores in cell wall which promote entry of aminoglycosides
into to cell to bind to ribosomes. (GTQ)*

Narrow Therapeutic of index, peak and trough. = *Tox: Ototoxicity (cochlear) out hair
cell destruction in the organ of corti, Vestibular toxicity (balance)*: Think ringing/
tennitus, deafness, vertigo, high fq hearing loss.

Imipenem
Meropenem - ANSWER Antibiotic: carbapenem *(all have "penem" in name)* - all
given IV. Betalactam active against many aerobic and anaerobic bacteria including
penicillinase−producing organisms; a bactericidal inhibitor of cell wall synthesis.

*Used with cilastatin* (which inhibits metabolism by renal dehydropeptidases).
Otherwise toxic metabolite in kidney.

Tox: allergy (partial cross−reactivity with penicillins), seizures (overdose)

*Meropenum* more stable, less toxic, no need to use w/ cilastatin.

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