Term
| What two components of the Beta Lactam chemical structure are required for action? |
|
Definition
| Thiazolidine Ring and Beta Lactam Ring with secondary amino group |
|
|
Term
| What reaction is inhibited by Beta Lactams? |
|
Definition
Transpeptidation of cell wall synthesis
-formation of the PEP to PEP bond by cleavage of a D-alanine |
|
|
Term
| What do Beta Lactams bind to? |
|
Definition
Penicillin Binding Protein, in the active site-
this is the enzyme that makes cell walls |
|
|
Term
|
Definition
Helps degrade bacterial cell walls at the same time that new cell wall is being made-
Activity is enhanced by Beta Lactams |
|
|
Term
| What do Beta Lactams mimic? |
|
Definition
| The D-alanines on peptidoglycan, thus bunging up the formation of bacterial cell wall because PBP binds covalently to the drug |
|
|
Term
| Name the REGULAR penicillins: |
|
Definition
| Penicillin G, Benzathine Penicillin G |
|
|
Term
| Name the Extended Spectrum penicillins: |
|
Definition
| Amoxicillin, Ampicillin, Piperacillin, Ticarcillin |
|
|
Term
| Name the Antistaphylococcal Penicillins: |
|
Definition
| Oxacillin, Nafcillin, Methicillin |
|
|
Term
| What's the big deal about the antistaphylococcal penicillins? |
|
Definition
| They are resistant to Beta Lactamase |
|
|
Term
| What Beta Lactam's absorption is NOT impaired by food? |
|
Definition
|
|
Term
| What two antistaphylococcal penicillins are stable to penicillinase? |
|
Definition
|
|
Term
| What two extended spectrum penicillins are stable to penicillinase? |
|
Definition
Amoxicillin+Clavulonic Acid
Ampicillin+Sulbactam |
|
|
Term
| What two antipseudomonal drugs are stable to penicillinase? |
|
Definition
Ticarcillin+clavulonic acid
Piperacillin+tazobactam |
|
|
Term
| In what chemical state are Beta Lactams? |
|
Definition
| Weak acids- DOSAGE MODIFICATION FOR RENAL IMPAIRMENT |
|
|
Term
| When do penicillin drugs penetrate the CNS? |
|
Definition
| Only if meninges are inflamed |
|
|
Term
| How are Beta Lactamase resistant penicillins excreted? |
|
Definition
|
|
Term
| What drugs is given to keep blood levels appropriate when giving penicillin drugs in the hospital? |
|
Definition
|
|
Term
| Which penicillin is always given IV? |
|
Definition
|
|
Term
| How do we cure syphillis? |
|
Definition
| A single treatment with penicillin is curative for primary and secondary syphilis- no resistance reported |
|
|
Term
| How do we prevent gonococcal opthalmia in newborns? |
|
Definition
| Silver nitrate drops in the eyes |
|
|
Term
| How do we treat penicillinase-producing strains of gonorrhea, and what is the backup? |
|
Definition
| Ceftriaxone, with spectinomycin as the backup |
|
|
Term
| What 5 groups of bugs are treated with Penicillin G? |
|
Definition
Gm+ Cocci-S. Pneumo,S. Pyogenes,S. Virid
Gm+bacilli- anthrax, diptheria
Gm-cocci- neisseria gon and mening
Anaerobes- c. perfringens
Spirochetes- Syphilis, Yaws |
|
|
Term
| What happens to penetration of penicillin into the CNS as meningitis is treated? |
|
Definition
| Penetration goes down because meninges get less inflamed |
|
|
Term
| What do we use to treat Beta Hemolytic Strep Pharyngitis (strep throat) and Syphilis? |
|
Definition
|
|
Term
| What two penicillins are given IM to yield low but prolonged drug levels? |
|
Definition
Benzathine Penicillin G
Procaine Penicillin G |
|
|
Term
| What do we give for MSSA? |
|
Definition
|
|
Term
| What do we give for MRSA? |
|
Definition
|
|
Term
| What drugs do we use for mild to moderate localized staph infections? |
|
Definition
| OCD- Oxacillin, Cloxacillin, Dicloxacillin |
|
|
Term
| How do we treat serious systemic staph infections? |
|
Definition
|
|
Term
| What do we give for penicillin resistant pneumococci? |
|
Definition
| Amoxicillin and Ampicillin |
|
|
Term
| What do we use to treat Listeria? |
|
Definition
|
|
Term
| What is similar between amoxicillin and ampicillin and what is different? |
|
Definition
Similar spectrum of action to Penicillin G (both)
Drugs of choice for resistant pneumo.
AMOXICILLIN HAS BETTER ORAL ABSORPTION
AMPICILLIN TO TREAT LISTERIA |
|
|
Term
| Ticarcillin and piperacillin are used to treat? |
|
Definition
PSEUDOMONAS, UTIs
-gram (-) rods- Enterobacter, E. Coli, Proteus, H. Influenza, Pseudomonas |
|
|
Term
| What are the 3 Beta Lactamase inhibitors and what do they do? |
|
Definition
Clavulanic Acid
Sulbactam
Tazobactam
-they inhibit many Beta Lactamases
-given in conjunction with other drugs
(have little or no intrinsic antibiotic properties) |
|
|
Term
| Amoxicillin is given in combination with what Beta Lactamase inhibitor? |
|
Definition
| Clavulonic Acid- together they make Augmentin |
|
|
Term
| Ampicillin is given in combination with what Beta Lactamase inhibitor? |
|
Definition
| Sulbactam- together they make Unasyn |
|
|
Term
| Piperacillin is given in combination with what Beta Lactamase inhibitor? |
|
Definition
| Tazobactam- together they make Zosyn |
|
|
Term
| Ticarcillin is given in combination with what Beta Lactamase inhibitor? |
|
Definition
| Clavulanic Acid- together they make Timentin |
|
|
Term
| If a 23 year old soccer player comes to you with a serious addiction to Diazepam, what do you do? |
|
Definition
|
|
Term
What are the two most important adverse effects of penicillins?
What are some less common ones? |
|
Definition
HYPERSENSITIVITY- ANAPHYLAXIS
SKIN RASH- Bazillions of red welts
less common: diarrhea, nephritis (especially underlying renal disease), neurotoxicity, cation toxicity, hematologic toxicity |
|
|
Term
| How are cephalosporins different from penicillins? |
|
Definition
Broader spectrum of action
More stable to many Beta Lactamases |
|
|
Term
| What generation cephalosporin is Cefadroxil? |
|
Definition
|
|
Term
| What generation cephalosporin is Cefazolin? |
|
Definition
|
|
Term
| What generation cephalosporin is Cephalexin? |
|
Definition
|
|
Term
| What generation cephalosporin is Cephradine? |
|
Definition
|
|
Term
| What generation cephalosporin is Cefaclor? |
|
Definition
|
|
Term
| What generation cephalosporin is Cefuroxime? |
|
Definition
|
|
Term
| What generation cephalosporin is Cefoxitin? |
|
Definition
| Second, but is a cephamycin |
|
|
Term
| What generation cephalosporin is Cefotetan? |
|
Definition
| Second, but is a cephamycin |
|
|
Term
| What generation cephalosporin is Cefotaxime? |
|
Definition
|
|
Term
| What generation cephalosporin is Ceftazidime? |
|
Definition
|
|
Term
| What generation cephalosporin is Ceftriaxone? |
|
Definition
|
|
Term
| What generation cephalosporin is Cefipime? |
|
Definition
|
|
Term
| What are the cephamycins, and what's the big deal with them? |
|
Definition
| Cefoxitin, Cefotetan- similar activity to second generation cephalosporins, but enhanced activity against anaerobes |
|
|
Term
| What is the spectrum of action of the first generation cephalosporins? |
|
Definition
Similar to penicillin- GRAM + COCCI EXCEPT MRSA
GRAM - Against PROTEUS, E COLI, KLEBSIELLA (P e.C K)
(rarely the drug of choice for anything) NO CNS PENETRATION |
|
|
Term
| What first generation cephalosporins do we give to treat UTI's, staph or strep infections, CELLULITIS, or SOFT TISSUE ABSCESSES? |
|
Definition
| Cefadroxil, cephalexin, cephradine |
|
|
Term
| What first generation cephalosporin penetrates most tissues well and is the drug of choice for SURGICAL PROPHYLAXIS? |
|
Definition
|
|
Term
If we know the infection is not MRSA, we don't need to penetrate the CNS, and we want to give prophylactic treatment, what drug do we use?
(Hint: first gen cephalosporin) |
|
Definition
|
|
Term
| What is the spectrum of action of second generation cephalosporins? |
|
Definition
Same as first generation, plus extended coverage of gram negatives
NO CNS PENETRATION |
|
|
Term
| What do we use Cefuroxime to treat? |
|
Definition
Sinusitis, otits, lower RTI
COMMUNITY ACQUIRED PNEUMONIA
(H. Influenzae, Moraxella, Klebsiella, Penicillin-Resistant Pneumo.) |
|
|
Term
| What do we give to treat MIXED ANAEROBIC INFECTIONS? |
|
Definition
Cefoxitin and Cefotetan
-peritonitis or diverticulitis |
|
|
Term
| What is the spectrum of action of third generation cephalosporins? |
|
Definition
Same as first and second generation, BUT:
More expanded Gram - coverage
Some can cross BBB (Cefotaxime, Ceftriaxone)
Activity against BETA-LACTAMASE-PRODUCING HAEMOPHILUS AND NEISSERIA |
|
|
Term
| What class of drugs is effective against Beta-lactamase producing strains of haemophilus and neisseria? |
|
Definition
Third Generation Cephalosporins
THINK CEFTRIAXONE! IT'S THE BIGGIE |
|
|
Term
What do we give to treat meningitis?
(3rd Gen) |
|
Definition
Ceftriaxone and Cefotaxime are both approved
-Pneuomo, meningococci, H. Influenzae, susceptible enteric gram- |
|
|
Term
| What do we give for meningitis caused by highly resistant strains of pneumococci? |
|
Definition
| Ceftriaxone or Cefotaxime in combination with VANCOMYCIN |
|
|
Term
| Ceftriaxone and Cefotaxime are most active against what? |
|
Definition
| PENICILLIN-RESISTANT STRAINS OF PNEUMOCOCCI |
|
|
Term
| What is the drug of choice for empirical therapy of serious infections? |
|
Definition
| Ceftriaxone or Cefotaxime |
|
|
Term
| What do we give for empirical therapy of sepsis with unknown cause? |
|
Definition
| Third Generation Cephalosporin: CEFTRIAXONE or Cefotaxime |
|
|
Term
| In neutropenic, febrile, immunocompromised patients, 3rd generation cephalosporins are given in combination with what? |
|
Definition
|
|
Term
| This FOURTH GENERATION cephalosporin is effective against (who cares, just know the name) P. aeruginosa, enterobacteriaceae, S. aureus, and S. pneumoniae: |
|
Definition
CEFEPIME- FOURTH GENERATION
CEFEPIME- FOURTH GENERATION
CE-FOURTH-PIME
Get it?
Ok |
|
|
Term
| How are most cephalosporins excreted? What is the exception? |
|
Definition
Most in the urine
Ceftriaxone is excreted in the bile |
|
|
Term
Organisms that are not covered by cephalosporins are sooooo LAME:
(what does LAME stand for?) |
|
Definition
Listeria
ATYPICALS- chlamydia, mycoplasma
MRSA
Enterococci |
|
|
Term
| If a patient has an anaphylactic response to a penicillin drug, can we give them cephalosporins? |
|
Definition
Sure, if we want a law suit!
NO: Cephalosporins may induce hypersensitivity reactions identical to penicillins- if the patient is allergic to penicillin, cephalosporins are OFF THE TABLE |
|
|
Term
What is the side effect risk with cefotetan?
What causes this? |
|
Definition
Hypoprothrombinemia
Disulfiram-like reactions (mimics the effects of antibuse- NO ALCOHOL)
Caused by THIOL group |
|
|
Term
| What class of drug is Aztreonam, and what is its mechanism of action? |
|
Definition
Aztreonam is a monobactam
It has the same MOA as penicillin
It is resistant to most Beta Lactamases |
|
|
Term
| What drug can be given to penicillin-allergic patients without reaction and has a similar spectrum of activity to 3rd generation cephalosporins? |
|
Definition
|
|
Term
| What drug can we use to treat pneumonia, meningitis, and sepsis caused by Gram-negative pathogens that does NOT cause a reaction in penicillin-allergic patients? |
|
Definition
|
|
Term
| What drug, which has a very huge spectrum of action, is only reserved for highly resistant bugs? |
|
Definition
| IMIPENEM (du du duhhhhhhh.....) |
|
|
Term
| What must imipenem always be given in combination with and why? |
|
Definition
| Cilastatin- to prevent inactivation by DEHYDROPEPTIDASE in renal tubules |
|
|
Term
| What are the adverse effects of imipenem? |
|
Definition
Nause, vomiting, diarrhea
Rashes, reactions at infusion site
CAN CAUSE SEIZURES IN RENAL PATIENTS SO MUST MONITOR RENAL FUNCTION
Patients allergic to penicillins MAY be allergic to imipenem |
|
|
Term
| What is the mechanism of action of Vancomycin? |
|
Definition
| Binds to D-Ala-D-Ala terminus preventing peptidoglycan elongation and cross-linking |
|
|
Term
| How is resistance to Vanco established? |
|
Definition
Those sneaky bugs convert their terminal D-Ala (the target of Vanco) to D-LACTATE
(brought to you by VRSA) |
|
|
Term
| What is the spectrum of action of Vanco? |
|
Definition
Gram +
Anaerobes
(S. aureus, S. epi, Strep A, B, C, Strep Pneumo, Entero. Faecalis, Actinomyces, Listeria, Clostridium) |
|
|
Term
| What are the clinical uses of Vanco? |
|
Definition
Sepsis or endocarditis of MRSA
Used in combo with ceftriaxone or cefotoxime for treatment of MENINGITIS caused by highly resistant PNEUMOCOCCUS |
|
|
Term
| How do we give Vanco for Enterocolitis? |
|
Definition
|
|
Term
| What is important about the administration and clearance of vancomycin? |
|
Definition
USE A SLOW IV!!!!
-it is DIRECTLY proportional to Creatinine Clearance
-DOSAGE REDUCED IN RENAL PATIENTS |
|
|
Term
| Does Vanco cross the Blood Brain Barrier? |
|
Definition
| Only if the meninges are inflamed |
|
|
Term
| What are the adverse effects of Vanco? |
|
Definition
RED MAN SYNDROME- if infusion rate too high
Ototoxicity and Nephrotoxicity when given with other drugs that have these side effects (like AMINOGLYCOSIDES) |
|
|
Term
| What is the mechanism of action of Bacitracin? |
|
Definition
| Inhibits cell wall synthesis by interfering with the LIPID CARRIER that transfers peptidoglycan subunits to the growing cell wall |
|
|
Term
|
Definition
Against gram +
ONLY USE TOPICALLY- HIGHLY NEPHROTOXIC
Use for surface lesions, in wounds, or mucous membranes |
|
|
Term
| What modification occurs at the terminal end of the peptidoglycan pentapeptide to make RESISTANCE TO VANCO? |
|
Definition
| D-alanine becomes D-LACTATE |
|
|
Term
| What drug is inactivated by dehydropeptidase and must be given with cilastatin? |
|
Definition
|
|
Term
| A 25 year old pharmacy student comes down with gonorrhea. What do we give him? |
|
Definition
|
|
Term
| If a kiddo has honey crusted lesions with pus that are gram+ cocci in both grape like clusters and chains, and the little dude has swollen lymph nodes too, what two diseases does he have and how do we treat? |
|
Definition
Impetigo and strep- S. Pyogenes, and S. Aureus
PENICILLIN G and Cephalexin |
|
|
