used for ENT strep infections

1) 2 drugs, administration

2) half life

3) what increases half life?

1st generation PCNs:

Pen V (po), Pen G (IV/IM)

t1/2=30-60 min

Pen G Procaine/Benathine (DEPO) released slowly over time

beta-lactam antibiotics

1) name 4

2) MOA

PCN

Cephalosporins

Carbapenems

Monobactams

MOA: inhibit PCP (penicilin binding proteins) and block stage 3 of bacterial cell wall synthesis (no peptidoglycan cross linking), causing bacterial lysis.

1) syn of NAG and NAM in cytoplasm

2) syn of peptidoglycan chain (NAG-NAM...)

3) PBPs cross link peptidoglycans

1) Benzyl-

2) Amino-

3) carboxyl-

4) Ureide-

tx of:

strep viridans/pyogenes/viridans

syphilis

nonres gonorrhea

Lyme disease

Pen G (IM/IV)

Pen G Procaine OR benzathine (IM) for longer/slower release.

Pen G benzathine

effective against:

-gram + strep

-gram neg rods (E. coli, P. mirabelis, H. influenzae, Salmonella/Shingella, anaerobes)

NOT effective against P. aeruginosa, Proteus vulgaris

2nd gen PCNs:

Ampicillin (po/IV/IM), Amox (PO)

3rd/4th generation:

Geocillin

ticarcillin

pipercillin

mezlocillin

geocillin (po)

3rd gen PCN

main indication is serious gram negatives: P. vulgaris, P. aeruginosa

Used in combo w/ aminoglycoside (gentamicin)

disodium salt drugs

3rd gen PCN:

ticarcillin (IM/IV)

(geocillin (PO) only for UTIs)

4th gen PCN + aminoglycoside:

broad spectrum, parenterel admin

pipercillin, mezlocillin

main indications:

proteus vulgaris

enterobacteria

pseudomonas aeruginosa

4th gen PCNs, parenteral admin

Pipercillin, Mezlocillin

+ aminoglycoside for endocarditis

cephalosporin/ PCN cross-allergies:

1) %

2) RULE of administration of cephalosporins

5-10%

RULE: don't administer cephalosporins to individuals who have previously had immediate-type rxn to PCNs.

1st gen cephalosporins

cefazolin (IM/IV)

cephalexin (PO)

tx of Resistant gonorrhea infections.

increased gram neg activity including H. influenzae (lactamase-producing), resisitant N. gonorrhea, N. meningitis, Bacteroides fragilis

effective against most anaerobes.

NO P. aeruginosa.

Name 4

2nd gen cephalosporins:

cefoxitin - most anaerobes, resistant gonorrhea,

cefotetan - most anaerobes

cefuroxime - lactamase + H influenzae

cefaclor - lactamase + H influenzae

3rd gen cephalosporins:

cefoperazone (IM/IV)

ceftriaxone (IM/IV)

cefixime (PO)

3rd gen cephalosporins

good lipid solubility

Ceftriaxone (half life: 6-8 hours)

3rd gen cephalosporin

-this cephalosporin has longest half life (6-8hrs).

-high levels achieved in blood and CSF.

-effective in tx of resistant pharyngeal/genital N gonorrhea.

-good bone penetration.

-GOOD FOR RENAL INSUFF pts b/c excreted in bile.

ceftriaxone (IV/IM)

3rd gen cephalosporin.

Cefepime (IV/IM)

4th gen cephalosporin.

Carbapenems

1) class

2) 2 drugs

3) administration

4) MOA

5) spectrum

1) beta lactam ABX

2) Imipenem-clastin*, Meropenem (both IV)

3) parenterel

4) similar to PCN

5) broad spectrum, beta lactamases, NO MRSA.

*clastin counteracts kidney damage of impenem metabolite.

Aztreonam

a Monobactam

adv rxns of this drug include:

ototixicity

nephrotoxicity

red man syndrome (w/ rapid IV admin)

pseudomembranous colitis

serious rash

bullous dermatosis

tx of C. difficile pseudomembranous colitis (admin) (alt to what?)

Vancomycin (PO)

(alt to metronidazole)

non-beta lactam ABX

interferes with stg 2 bacterial cell wall syn

bacteriocidal

res gm +, MRSA, res strep/enterococci, C. difficile (pseudomembranous colitis)

tx of otitis media:

-most common etiologies (4)

-primary & for allergies to PCN

tx of pharyngitis:

-most common etiologies (3)

-primary & alt

tx sinusitis:

-most common etiologies (3)

-kids & adults

MOA of this ABX class:

-reversibly inhibit 30S bacterial ribosome,block protein synthesis

-passive diffusion through outer cell wall

-active diffusion through bacterial cytoplasmic membrane

-bacteriostatic

tetracylcines (ABX):

short acting: tetracycline, oxytetracycline

long acting: demeclocycline, doxycycline, minocycline

tetracyclines (and tigecycline)

*neurotoxicity: minocyclines*

tx of complicated skin infections and abdominal infections, esp MRSA, E. faecalis, E. coli

administration directions.

tigecycline

IV x 5-14days

this ABX class is bacteriocidal

-irreversible binding to 30S (and some 50S) to inhibit protein synthesis.

-passive diffusion through porin channels.

-active transport by anionic transporter through cytoplasmic reticulum, requires O2 (NOT EFFECTIVE AGAINST ANAEROBES).

administration (2)?

Aminoglycosides (IV b/c polarized):

Streptomycin

gentamicin

tobramycin

netilmicin

amikacin

*Neomycin

*kanamycin

...*administered PO for nonsystemic bowel cleansing.

Neomycin & Kanamycin

(Aminoglycosides)

Neo also used topically (otitis externa)

1)What is the most widely used systemic aminoglycoside for aerobic, serious gram negative infections?

2) what is 2-4x more potent than #1 in treating Pseudomonas?

3)What is used is bacterial is resistant to #1?

4) What drug exhibits the greatest resistance, used in #1 and #2 resistant bacteria?

1) Gentamicin - most widely used in combo with 3/4 PCN and cephalosporins.

2) Tobramycin 2-4x more potent than gentamicin

3) Netilmicin - used in gent resistance

4) Amikacin  - used in gent and tobra resistance

what drug class?

-binds to 50S bacterial ribosome.

-bacteriostatic

-Indications: grm + strep, chlamydia, myco pneumonia, legionella, syphilis

-usually administered orally

bacteriostatic

50 S binder

decomposed by HCl to irritant

PO with enteric coating, qid

-gm+ alt to PCN/ceph for strep/pneumococcal ENTs

-gm- legionella, mycoplasma, genitial (chlamydia, syph, gonorr), C. diptheria (carrier state)

-NO GM- enteric organisms

Adv: GI, rash, allergy

bacteriostatic

50 S binder

t 1/2=2-3days, qid PO

wide distribution

-gm+ strep alt to b-lactams for pharyngitis, sinusitis, CAP.

-gm- H. influenzae, mycoplasma, chlamydia, gonorrhea, MAC

bacteriostatic

50 S binder

gm- L. pneumo, C. trachomatis, MAC, H. pylori

semisynthetic macrolie: ketolide

Indications: sinusitis, pneumonia, bronchitis

ADV: N/V/D, vision, headache/dizzy, cardia QT interval

bacteriostatic

binds 50S

main clin use: anaerobic infections, gm+ strep/staph

AVD: pseudomembranous colitis due to overgrowth of resistant C. difficile in GI tract.

bacteriostatic

binds to 50S

good PO, wide distribution

reserved for life-threatening infections

broad spectrum, esp H. infl, meningitis, Salmonella, RMSF

NO PSEUDOMONAS

-gray baby syndrome: metabolised by glucuronidation which is deficient in babies

-drug interactions b/c inhibition of CYP450 enzymes

this drug has dose related bone marrow supression & anemia due to inhibitory effect on prot syn & Fe incorporation into heme.

also idiosyncratic nondose related response of aplastic anemia...risk of leukemia later.

Quinupristine/Dalfopristin:

streptogramin, inhibits 2 sites on 50S ribosome.

(IV)

ADV: N/D, pain @ injection, arthralgia/myalgia, hyperbilirubinemia

bacteriostatic for MRSA, VREF, VRE faecium, VR staph.

cidal for PCN/CEPHALO-resistant strep.

Sulfanomides: Sulfisoxisole, Sulfamethoxazole

(folic acid antagonists)

Sulfanomides (FOlic acid antagnists):

sulfisoxisole, sulfamethoxazole

Sulfanomides (Folic acid antagnists):

sulfisoxisole, sulfamethoxazole

main indication: gm - enterobacteria: UTI, prostatits, vaginitis, GI, otitis media, respiratory infections

DOC: pneumocystitis jeroveci (but can cause fever, rash, decr blood cells, folate def...macrocrytic anemia in AIDS pts)

Trimethoprim/ Sulfamethoxazole

folic acid antagonist, 20x more potent than others.

tpoical tx of gm(+) minor skin/ocular infections

1) name & MOA

2) used in combo with what 2 drugs?

bacitracin: inhibits cell wall peptidoglycan syn

often combo with polymyxin B or neomycin

topical tx of minor skin infections: gm+ staph (MRSA) and strep (b-hemolytic), impetigo

1) name and MOA

topical ABXs:

1) gram + minor skin/ocular infections, inhibit peptidoglycan syn, combined with polymycin B/neomycin

2) minor skin infections: grm+ staph (MRSA) & strep (B-hemolytic), impetigo.  Inhibit bacterial protein synthesis.

1) bacitracin

2) mupirocin

What ABX class?

-bacteriocidal

-inhibit DNA gyrase, bind subunit A

-resistance developed from altered A, decr bacterial uptake, & effluc pump.

this ABX class has

-good po (antacid interference)

-mixed excretion:urine/GI unchanged and metabolized; accumulate in renal failure

TB/ Mycobacteria tx

1) length

2) # of drugs

1) 6-18ms

2) 2-4 drugs because of resistance

tx of Mycobacteria tuberculosis:

1) cavitary (lung): high O2, neutral/alkaline pH ,rapid multiplication.  (3)

2) caseous (granulomas): lower O2, acidic, slow multiplacation. (3)

3) macrophages: low O2, acidic, slow mult, intracellular reservoir for bacilli (3)

1) cavitary (lung): high O2, neutral/alkaline pH ,rapid multiplication.  INH, rifampin, streptomycin

2) caseous (granulomas): lower O2, acidic, slow multiplacation. INH, rifampin, PZA

3) macrophages: low O2, acidic, slow mult, intracellular reservoir for bacilli.  INH, rifampin, PZA

UTIs

1) main etiology

2) tx (*in pregnancy?) and # of days for UTI, pregnancy, and kidney involvement

1) E. coli (80%)

2) PO: FQ (CIPRO), TMP/SMX, AM/CL, CEPH x 3days (preg x 7days, no FQ or sulfanomides), kidney x 14 days

most potent bronchodilators: class?

Dx of this class

1) administered sub cut for acute asthmatic emergencies (2)

2) selective B2 agonist, racemic mixture

3) R enantiomer binding to B2 100x greater than S enatiomers.  Causes less cardiac stimulation than #2.

4) longest duration=12-18hrs. slow onset, prophylactic control

sympathomimetic amines:

1) Epinephrine & Terbutalin: administered sub cut for acute asthmatic emergencies

2) Albuterol: selective B2 agonist, racemic mixture

3) Levoalbuterol: R enantiomer binding to B2 100x greater than S enatiomers.  Causes less cardiac stimulation than #2.

4) Salmeterol: longest duration=12-18hrs. slow onset, prophylactic control

blocks cholinergic receptor (anticholinergic) causing bronchodilation.  Reduces sputum volume without incr viscosity and doesn't inhibit mucociliary clearance.

1) dx

2) onset

3) duration

4) 1st line dx in....

5) absportion

1) ipratroprium (ATROVENT)

2) 1-2 hr

3) 4-6hr

4) COPD (combined with albuterol for asthma: COMBIVENT)

5) charged, no systemic absorption...only effective when inhaled.

Asthma:

1) reliever drugs are...

2) Controller drugs are...

1) reliever.  Tx of early sx.  BRONCHODILATORS

2) controllers.  Tx of late sx.  ANTI-INFLAMMATORIES.

these drugs only effective in acute asthmatic attacks as rescues.

1) class

drugs in this class:

2) short duration, B1 incr HR, not recommended (2)

3) administered sub cut for acute asthmatic emergencies (2)

4) selective b2 agonists (3)

5) longest acting b2 (duration?)

1) sympathomimetic amines:

2) epinephrine, isoproterenol: short duration, B1 incr HR

3) epinephrine, terbutalin: administered sub cut for acute asthmatic emergencies

4)b2 agonists: albuterol, levoalbuterol (more potent), salmeterol (longest acting, lipophilic)

5) salmeterol dur=12-16hrs

long acting anticholinergic bronchodilator indicated for COPD, inhalation as dry powder, slow onset, duration 24 hrs.

tiotropium (SPIRIVA) (dry powder inhalation)

slow onset

dur=24 hrs

COPD

1) tx for acute exacerbations

2) tx mainstay

1) systemic corticosteroids x 2wks (prednisone)

2) bronchodilators are mainstay

Drugs used to reduce/control chronic inflammation of asthma and allow reduction of reliever/steroid drug dosages, also indicated for aspirin induced asthma

class and 3 drugs

Antileukotrienes:

-Zileuton: removed from use

-Zafirlukast: 20mg PO on empty stomach for prophylactic/chronic asthma control. P450 inhibitor (interactions with phnytoin, warfarin)

-Montelukast (SINGULAR): LTD4 blocker.  PO 10mg & 5mg tablets qid @ pm.

adm sub cut q 2-4 weeks based on body wt.  prevents IgE binding on mast cells (anti-inflammatory).  Indicated for moderate to severe persistant asthma uncontrolled by inhaled steroids.

Cost 10-12k/yr

active metabolite of terfenadine; doesn’t accumulate with drugs that inhibit P-450s, usu adm BID

Fexofenadine (ALLEGRA)

non sedating H1 antagonist

once/day, low sedation, also does not accumulate with P- 450 inhibitors, exc urine unchanged; claimed to also inhibit mast cell mediator release

Cetirizine (ZYRTEX)

non sedating H1 antagonist

forms long-acting metabolite (desloratadine), now OTC

Loratadine (CLARITIN)

non sedating H1 antagonist

Azelastine (ASTELIN)

non sedating H1 antagonist

1) acetylcysteine

2) human DNase

promote discharge of mucus from respiratory tract by stimulating gastric vagal nerves that increase respiratory secretions.

Class and name 2.

Expectorants:

Ammonium chloride  and guaifenesin(MUCINEX)

3 antitussive drugs.

Indication for what type of cough?

codeine, hydrocodein, dextromethorphan

for NON productive coughs