PharmGIAaron1.txt

Penicillinase resistant penicillins

Active against penicillinase producing Staph. Drug of choice for Staphylococcal dz.

Worthless for garm neg bac, and MRSA

Stable in acid: absorbed in GI tract

Severe infection requires injection

Natural Penicillin

Good oral abosrption. Treats group AB hemolytic Strep gram pos and neg cocci.

Anaerobes are susceptible

Watch renal fxn in neonates/infants

Natural Penicillins

• Used for: Group AB hemolytic strep.
• Gram neg and gram pos cocci

Anaerobes are susceptible

Unstable in gastric acid: poor oral absorption

Special considerations: neonates/infants: renal fxn

• Aminopenicillins
• Broad spectrum
• used for URI, L. monocytogenes in immunocompromised. Gram negh

Resisitant: H. influenzae, N. Gonorrhoeae, enterobacteriaceae

Interferes w/ oral contraceptives

• Antipseudomonal PUN
• Up activity against pseudomonal, enterobacter and proteus. Activfe against Klebsiella
• Up gram neg coverage

Resistance to PCNG impries resistance to these drugs

Serious, pseudomonal require additional aminoglycoside.

Reserved for severe, hospital acquired gam neg bacteria

Adverse rxn: maculopapular rash

Uticarial rash, stevens-johnson syndrome

Serum sickness, bronchospasm angioedema

Toxicity: rare. Watch for bone

Marrow depression granupocytopenia, hepatitis, impaired pt fxn, lethargy, confusion, seizures superinfections

1st gen cephalosporin

Gram pos coverage w/ gram pos cocci, less gram neg coverage; oral anaerobes are covered

Not active against enterococcus, MRSA, MRSA or VRE

Cefadroxil- better PO absorption, BID

• 2nd gen cephalosporin
• low gram pos coverage
• hih gram neg coveragers (e. coli, klebsiella)

• Resistant to Beta lactamases
• useful for H. influenzae, N. meningitidis and pneumococcal meningitis

Injection

2nd gen cephalosporin/ bacteroides

Better anaerobic coverage including B. fragilis

Injectable

2nd gen cephalosporins

More active against H. Influenzae and M. Catarrhalis

are given PO

3rd gen cephalosporin

Decreased gram pos, much better gam neg, esp Beta lactamase

Penetrates CSF

Enterobacteriaceae

Not for: Listeria mono, MRsA, VRE, injected, once daily, good for penicillinase- gonococcus also empiric for meningitis in noncompromised due to H. influenza, S. pneum, N. meningitis, gram neg bacilli

Injectable 3rd gen cephalosporin

more active against pseudomonas

Penetrates CSF

DOC w/ aminoglycoside for meningitidis by pseudomonas

oral 3rd gen cephalosporin

More active against enterobacteriaceae and B-lactamase producing H. influ and N. gonorrhea

oral 3rd gen cephalosporin

BID dose

Enterobacteriaceae, B-lactamase, H. influenzae, and N. gon

4th gen injected cephalosporin

Enterobacteriaceae resistant to other cephalos

Good antipseudomonal

Excellent CSF

4th gen injected cephalosporin

Designed for MRSA penicillin binding protein, active against MRSA

IV or IM

Carbapenems


Cilastin inhgibits renal tubular dipeptidase (degrades imipenem)

Imipenem: ery broad gram pos cocci-not MRSA

Enterobacteriaseae, pseudomonas, B. fragilis, acinetobacter

For severe UTI, lower RTI, intraabol, gynecologic, skin, bone, joint, severe mixed nosocomial

N/V, hypersensitive- cross w/ pen and up LFT

Similar to imipenem- not sensitive to renal tubular dipeptidase

Less active against gram pos cocci

Limited use

Same as Meropenem

Less gram pos cocci than imipenem

Limited use

Same as meropenem and entapenem but w/ resistance by pseudomonas

Limited use

IV/IM

Monobactams- similar to aminoglycosides

Mostly gram neg- aerobic

gram pos/anerbobes resist

Great for enterobacteriaceae, also pseudomonas, H. flu, N. gon

OK in Penicillin allergy, phlebitis, eosinophilia

Like vanc

T1/2 is 100hrs

Van A enterococci resist

Hypersensitivity, ototoxicity

Ototoxicity, nephrotox-caution w/ aminoglycosides: anaphylaxis, red neck flush w/ rapid....

Glycopeptide

Binds d-alanyl-d-dlanine terminus of peptidoglycan precursors

Inhibits earlier strep than B-lactams

Rapid bactericidal in growing cells

Bacteriostatin for enterococci

Resist: modified enzyme modifies peotidoglycan-plasmid

For gram pos, MRSA, 2nd line C. Dif,

Most enterobacci, bas S. pyogenesw, S. pneumo (?)

Binds 5OS ribo

Gram pos= 100x etter acumulate

inhibits peptide bond formation by inhibiding translocation from A to P site

Bacteriostatic

Resist: plasmid-down permeability, efflux pump, methylate enzymes 50S, esterase hydroxyzes drug

For: gram pos cocci, not staph, enterococcus gram pos bacillus, mycoplasma=DOC

Gram neg bacilli= H. influ, H. Ducreyi, C. jejuni, J. pylori

DOC= legionella, B. pertussis

Macrolide

Poorly absorbed, worse w/ food, destroyed by acid

No Bb cross, and metab by liver

DOC: M. pneumo, C. diptheriae, C. pneumo, B. pertussis, H. ducreyi

Also- clamydiae, C. Trachomatis for strep, C. tetani, T. pallidum preggo w/ PCN allergy

GI:

Prolong QT, transient auditory

Inhibit P455, CYP 3A4= Up benzao, cyclosporine, carbametepine, steroids

Macrolide

rapid absorb, big first pass

DOC Myco avium intracellular complex

Macrolide

rapid absorb, stable in acid

Take on empty stomach

T1/2= 68rh

Single lg dose for C. trachomatis

Also best macrolide for H. influ URI

Ketolide

Slight better spectrum, no food interfere, Major 3A4 metabolizer

No in kids less than 12

GI, NV, Diarrhea, Up LFT, prolong QT

Oral lincosamide

Binds 50S, bacteriostatin similar to macrolides

Gram pos cocci Strep and non-MRSA Staph

Better anerobe coverage than macrolides

• C. Perfingen, peptostrepto, peptococcus, propionbac, Bacteroides
• Also-protozoal

For: anaerobic infect fecal spill, pelvic abscess topical acne, bact vaginosis perotinitis gram pos cocci

GI, superinfection, rash common, STI's

binds 50S prevents amino-acid containing end of aminoacyl tRNA binding to A site

Bacteriostatic

resist: chloramphenicol acetyltransferase, Down perm, mutate 50S

• For: gastroenteritis- Salmonella and syph
• Meningitidis- H. influ, N. men, S. pneumoRickettsial dz if TCN sensitive, Brucellosis 2nd to TCN

Heme tox- anemia, leukopenia, thrombo, N/V common, inhibits P450 and Pheny, anaplastic anemia, gray baby syndrome, inhibit mitochondrial respiration

• Synercid
• Streptogamins

• Quinupristin: conformational change=Up quin effect
• Bacteriostatic= E. faecium, others killed
• For: gram pos cocci, MRSA, VRE, E. faecium, MDR Pneumococci

Atypicals- M. pneumo, C. pneumo, Legionella

CYP3A4 metab- inhibits


Infusion site pain, arthralgias, myalgias,, and up LFT

Oxalidinone- bind 50S

• Bacteriostatic- Staph and Enterococci
• Kills-Strep

• For: gram pos staph, strep, MRsa, VRE, E. faecium, S. pyogenes, bind skin infect.
• Oral
• Not CYP metab,=-MAO

• GI, HA, N/V, diarrhea, myelosuppress thrombocytopenia, anemia
• Interacts w/ MAO inhibitors and adrenergic agonists

Bactroban

From pseudomonas fluorescens

Binds bac Bolencyl-tRNA synth

Highly active aghainst Staph, MRSA, most strep.

Usually topically for MRsa carrier in Strep

Ant. Nares(?)

Better activity against MRSA and VRE

Used empirically for complicatd skin infxns caused by MRSA and intrabol(?) infxns

propionibacterium acnes

Metabolized by liver

vestibular tox

Tetracycline

DOC: borrelia, mycoplasma, ureaplasma, urealyticum, chlamydiae, rickettsiae

Metabolism induced by barbituates/phenytoin

photosensitivity, Not preggo, not less than 8yrs

Tetracycline binds 30S

DOC: rickettsiae, chlamydiae, borellia, mycoplasma, ureaplasma

Gi UPSET, PHOTOSENSITIVITY, NEPHROTOX, TEETH AND BONE

Not- preggo, less than 8yo

Better than gent for pseudomonas

Aminoglycoside

Nosocomial pneumonia- empiric for hospital acquired mulit-resist gram neg aerobes, some kleb and pseudomonas are resistant

• Pseudomonal sepsis
• enterococcal infections
• topical-ocular

• Nephrotox-renal prox tubule
• Ototox: cochlear=25% Starts high then goes low. Tinnitus, vestibular tox=HA leading to vertigo

Diffused through aq pore in outer membrane grm neg acive transport across cytoplasmic membrane

Binds 30S ribo of polysomes

Interfere w/ initiation and synth, block furtyher translation, premature term, misread RNA and destruction of cytoplasmic memb and death

Resist: fail permeation, low affinity for ribo, enzyme inactivation

For: gram neg aerobic bacilli, very little gram pos

w/ b lactam or vanc for sneitive strep

6 months

300 mg adults

900 my 2X week

10mg/kg for kids

Isoniazid, rifampin, pyrazinamide, ethambutol

9-12 months or more

At least 2 drugs continue once done susceptibility testing

Isoniazid and rifampin 6 months and pyrazinamide first 2 months

Or, Iso, rifam, streptomycin for 9 months

Alt. to sulfones if dapsone resistant strains or pt is intolerant

M. Leprae

Similar to sulfonamides most likely inhibits folate synth

Static

For: M. leprae, several years w/ rifampin, must monitor and much support

Bad, hemolysis, methemeglobinemia, GI, allergic

Binds to DNA dependent RNA poly and inhibits RNA synth in Mycobacteria

Cidal

Also: M. leprae w/ dapsone

Urine and body fluids= orange rash, thrombocytopenia, nephritis, down liver fxn w/ isoniazid

• Mostly for extracellular tubercle forms.
• poor cell penetration, crosses BBB

For: iv DRUG W/ LIFE THREATENING meningitis tuberculosis and disseminating Dz

Ototox, nephrotox, CAUTION

Inactive at neutral pH

Bactericidal at slightly acidic pH

Resist alone but not w/ isoniazid

Impair liver fxn

Used only in combos

• Good oral, good CSf
• Fast resistane if alone

Fen adverse

Good for TB, Kansasii, and many atypicals

W/ isoniazid

primary for TB

Inhibits synth of mycolic acid

Hits cell wall

Cidal for active growers, static at low dose

Not for atypical Mycos

Good for tuberculosis and Kansasii

Fast and slow acetylator in liver

CNS/PNS- pyridoxal phos deficiency inhibits metab of diphenylhydantoin

Allergic

Sulfadoxine= long acting

Pyrimethamine= parasite dihydrofolate reductase inhibition

For: P. falciparum

Gram pos/neg

• Sulfamethoxazole- PABA anolog
• Inhibits dihydropteric acid synth. prevents folic acid

Trimethorprim- inhibits dihydrofolate reductase

Bacteriocidal

For: AIDS pneumocystis, jirovecii in up dose UTI

Parasitic if the combo abose is given

Anemias

• 3rd gen
• Once daily

For: low RTI only

May prolong QT, less photo, no inhibit theophylline

3rd gen once daily

For: community acquired pneumo and bronchitis, PCN-resist Strep pneumo

Rash, inhibits theophylline

3rd gen

Levo or ofloxacin- once daily

For: low RTI, skin, bone, joint, gastroenteritis, GUTI, pen resist strep pneum

Less CNS, no theophylline inhibit

2nd gen

For: low RTI, skin, bone, joint, gastroenteritis, GUTI

Photosensitivity, NOT inhibit theophylline, CNS, NSAIDS

Racemic 2nd gen

for: low RTI, skin, bonde, joint, gastroenteritis, GUTI

CNS stim- anxiety hallucinate,

Theophylline, NSAIDS, insomnia

2nd gen fluoroquinolone

More potent gram neg

Better gram pos strep faecalis, staph aureus MRSA

Intracellular

For: low RTI, skin, bone, joint, gastroenteritis, GUTI

Interact w/ theophylline and NSAIDS

oral 1st gen

• For: GUTI, UTI, STD, gonococcus, prostatic-ecoli
• Pseudomonas=resist

inhibits theophylline metab CYP1A2

Crystalluria

inhibits DNA gyrase- Topoiso IV and II

Resist: mutate gyrase, down perm,

Quinolones: gram neg only

Flouroquinolones: great gram neg, gram pos, strep paecalis, staph w/ MRSA, intracellular-chlamydia, mycoplasmin, legionella, brucella, mycobacterium

Poor against anaerobes and S. pneumo

Good oral but not w/ Ca2+ and MG2+

GI, photo, CNS, seizure, Connective tiss, endocrine

Not- preggo or young child: Not-antacids, NSAIDS, inhibit theophylline metab

Synth. analog of PGE,

PG down acid secreation and Up mucus and up bicarb

ASA down PG synth= ulcer

For: NSAID ulcers

Not: preggo= uterine contract

H. pylori w. resistance

PPI + clarith and amox

or

PPI + bismuth and tetraycline and metronidazole (for resistance)

10-14 days, ulcer cure

up mucosal secreation

Coats ulcer

Causes H. pylori detachment and lysis

No antacid effect

Storage issues

Up mucus secreation

Phosphate epletion

bad: binds to tetracycline and constipate

Potent, good for women (Tums)

CA2+ may produce intense and long HCl rebound