* Beta lactam, no other ring attached

* Only active on G- aerobes

* Resists most Beta lactamases of G-

* Binds penicillin protein 3--> filamentouc, lysable bacteria

* IV/IM, unchanged excretion. Adjust dose for renal failure

* not a beta lactam

* IV/IM, oral for local effect in GIT

* For MRSA or Staph with patient allergic to beta lactam

* Local action against C diff

* Prevents removal of D-Ala in muramic acid cell wall and thus prevents cross linking.

* Red Man Syndrome- flushing from vessel dilation

* Hypotension, tachycardia, shock.

*Nothing to do with IgE, just drug on body action-causes histamine release

* Nephrotoxicity (with other nephrotoxic drugs) Ototoxicity

* NOT Beta lactam, inhibits cell wall synthesis

* Cidal vs various G+ cocci and bacilli

* NEPHROTOXIC

* Lipid carrier bactoprenol carries NAG-NAM to outside via dephosphorylation

* Bacitracin complexes w pyrophosphate to prevent dephosphorylation.

* topical for minor cuts and scrapes

* ophthalmic ointment for ulcerative blepharitis and bacterial conjunctivitis

* Often used with other drugs

* Used for short course Tx of uncomplicated UTI in women

* Mechanism:This blocks the addition of phosphoenolpyruvate to UDP-N-acetylglucosamine, the 2nd step in the in the synthesis of Park Nucleotide. Inhibits cell wall synthesis@font-face { font-family: "Times New Roman"; }p.MsoNormal, li.MsoNormal, div.MsoNormal { margin: 0in 0in 0.0001pt; font-size: 12pt; font-family: "Times New Roman"; }p.MsoFooter, li.MsoFooter, div.MsoFooter { margin: 0in 0in 0.0001pt; font-size: 12pt; font-family: "Times New Roman"; }table.MsoNormalTable { font-size: 10pt; font-family: "Times New Roman"; }div.Section1 { page: Section1; }

* Inhibits cell wall synthesis

* Amino sugars attached to glycosidic links to an aminocyclitol ring

* very polar polycations

* IV route, orally cleans out bowel

* Mechanism Enters G- via porin down gradient, enters cell, inhibits protein synthesis

* Cidal

1. Inhibit initiaion of protein synthesis

2. Make faulty proteins misreading mRNA

3. Premature terminations, polyribosome turns to monoribosome. Responsible for postantiobiotic effect

* Attain highest levels in renal cortex> reversible nephrotoxicity

* Endolymph> irreversible ototoxicity

* Degeneration of auditory nerve can lead to permanent hearing loss

      Auditory Sx: tinnitus, high freq hearing loss

      Vestibular: vertigo, ataxia, loss of balance

* Can accumulate in fetus! ototoxicity in neonates

*(generic) topical cream/ointment for burns, wounds

*prevent catheter infections, opthalmic for superficial ocular infection(then called Genoptic)

* IV Aminoglycosides

* Generally intechangeable with gentamicin

* Possibly less ototoxic than gentamicin

* IV Aminoglycosides

* enzyme resistant for nosocomial infections that resist gentamicin and tobramycin

*IV Aminoglycoside

* Neomycin and Paromomycin

* Neomycin prep for bowel surgery, topical antiinfectant

*Paromomycin kills cysts of Entamoeba histolytica which cause amebic dysentery

* CL= (140-Age) x(lean wt in kg)

          ------------------------------

          72 x Serum Creatinine (mg/dL)

For WOMEN multiply 0.85

Only distribute in lean body mass due to polycationic nature do not distribute in total body mass/water.

* MALE=50kg _2.3 kg for each inch over 5ft

* Female- 45.5 kg + 2.3 kg for each inch over 5 ft.

* Aminoglycoside dose: Maximum daily dose x estimated CL/normal CL

* For a 70 kg male, dosing 1x/day monitor trough

* Dose is 2-3x/day, monitor peak and trough levels

* Know the trough and peak are notable different for Amikacin vs. Gent and Tobra

* Neuromuscular Block by

1.Blocking Ca++ uptake into nerve terminal> prevent Ach release

2. Block postsynaptic Ach Receptor

* Broad spectrum static vs G=/G- and some intracellular organisms

* Lipid soluble

* Undergo enterhepatic cycle to have persistant drub levels

* Inihibt binding of aminoacyl tRNA to ribosome. Inhibit translation

*Grouped on duration of activity

* 6-8 hours

* Tetracycline is name of drug.

* For acne

* Act for about 12 hrs

* Demeclocycline

* For chronic dilutional hyponatremia in the syndrome of ADH (too much ADH)

* inhibits protein kinase in gut of renal tubule whee ADH depends to act

* 16-18 hrs

* Doxycycline oral and parental, lipidphilic!

* Minocycline (next card)

* Long lasting tetracycline

*originally for acne

* Associated with pulmonary complications eg pulm lupus, hypersensitivity pneumonitis, pleural effusions

* Immunomodulatory and anti-inflammatory activity

* Neuroprotective?

* pigments nail skin sclera, thyroid, gums>not reversible

* Blocks synthesis of NO

* Activates microglia, decreasing neuronal damage

* Improved stroke outcome given 6-24 hours afer stroke

* Neuroprotecting in Parkinson, Huntington's ALS< MS< Moderately effective RA

* GI Upset- Take w food

* permanent brown teeth

* Slowed growth photosensitivity esp w demeclocycline

* Expired Rx> Fanconi like syndrome from nephrotoxic metabolite epianhydrotetracycline> nausea vomitting, polyuria, polydipsia, glucosuria, aminoaciduria, hyperchloremic metabolic acidosis

* absorption decreased by dairy and antacids

* Parenteral, long acting

* Derivative of minocycline w similar side effects

* Same Mech. as tetracycline, cidal in some species.

* Greater acitvity vs tetracycline sens G+ G- and MRSA from greater hindrance

* Lactone ring + 1 or more deoxy sugars

* All active against MRSA

* inhibit translocation from A to P site

* Release peptidyl tRNA form ribosomes

* Block formation of initiation complex

* Active against Legionella

* Metabolites complex with w cytochrome heme, Fe+2, inhibit CYP3A4

* Prokinetic, can bind and stimulate GI motility via motilin receptors. Stimulates peristalsis, speeds gastric empyting

* Large lactome ring

* Mostly static sometimes Cidal

* Active against methicillin sensitive aureas, Moraxella catarrhalis, H. influenza

* Increase digoxin activity

* Immunomodulatory, esp clarithromycin

*Prolongs repolarization via K+ Channel effect> Torsades de pointes

* Can prolong cardiac repolarization> Torsades de pointes. Increased risk if used w another Rx that inhibits CYP3A4>increases erythromycin

* Binds heme, inhibiting CYP3A4, increasing its and other drugs' levels ie dilitiazem, verapamil

* For some reason increases risk of sudden death

* Now used for Legionellas, community acquired pneumonia, mycobacterium avium complex

* Concentrates intracellularly

* long half life 70 hrs

 Doesn't inhibit P450

* excreted unchanged in bile

* For community acquired pneumonia and mycobacterium avium complex

* Immunomodulatory: inhibit trancription for proinflammatory cytokines

* Inhibits CYP3A:

           Caution using with colchicine (used for      gout)>increase risk of colchicine toxicity.

* Ketolides are macrolide derivatives with better G+ activity

* Same mechanism as macrolides but binds 2 separate domains on ribosomes to recrease risk of resistance and have broader activity.

*

* A ketolide

* Used for community acquired respiratory infections

* Concentrates in pulmonary tissues and WBCs

* Active vs Beta lactam and macrolide resistant organisms

* Inhibits CYP3A4 Prolongs Q-T interval

* Rarely, serious hepatotoxicity

BBW Contraindicated if myasthenia gravis, life threatening respiratory failure

* complicated skin and intraabdominal infections, community acquires bacterial pneumonia

* Side effects: N&V, increased risk of mortality if hopsital acquires pneumonia, esp if ventilator asspciated, complicated intra ab infection or complicated skin and skin structure infection

*Hepatic excretion, decrease dose if hepatic impairment