Pharmacology - Antibiotics Part 2 (Exam 2) Flashcards
Name the major classes of antibiotics (5)
- Beta Lactams
- tetracylcines
- aminoglycosides
- macrolides
- fluoroquinolones
Mechanism of action of B-lactams
inhibit cell wall synthesis by covalently binding to active site of PBPs
Most important B-lactams
penicillins
cephalosporins
T/F: B-lactams have a linear arrangement
False! They have a B-lactam ring (an amide)
What does PBP remove when forming peptidoglycan cell wall?
terminal D alanine
What are the natural penicillins?
Penicillin G
Penicillin V
What are the anti-staphylococcal penicillins?
Nafcillin
Dicloxacillin
What are the extended spectrum penicillins (antipseudomonal)?
Piperacillin
Ticarcillin
What are the extended spectrum penicillins (aminopenicillins)?
Ampicillin
Amoxicillin
Spectrum of natural penicillins
Gram + and gram - cocci
gram + bacilli
spirochetes
Spectrum of anti-staphylococcal penicillins
penicillinase-producing stapylococci
Spectrum of extended spectrum penicillins (antipseudomonal)
pseudomonas aeruginosa
Spectrum of extended spectrum penicillins (aminopenicillins)
same as penicillin G and more Gram -
Penicillin ___ and _________ are orally adminstered
V; amoxicillin
Adverse effects of penicillins
-allergy
-amoxicillin rash
-GI upset
-hyperexcitability, seizures, hallucinations
-rare side effects (acute pancreatitis)
Which immunoglobulin is involved in allergic rxn with penicillin?
IgE
T/F penicillin allergies are more common than penicillin rash
False! Rashes are more common
Oral penicillin is antagonized by?
bacteriostatic antibiotics (tetracycline and erythromycin)
What do NSAIDS and probenecid do to penicillin?
increase half-life by decreasing renal excretion
When penicillin interacts with this drug, there can be anaphylactic bronchospasm
B-adrenergic blocking drugs
Penicillin interacts with allopurinol which leads to?
non-urticarial rash
Cephalosporins are classified by
generations
As cephalosporin generation increases, you lose ________ action and gain _________ action
gram +; gram -
First generation cephalosporins are very sensitive to?
B-lactamase hydrolysis
T/F first generation cephalosporins have best gram-positive activity
True
Cephalosporin general use chart
Cephalosporins indications in dentistry are good against __________ but limited activity against ____________
orofacial pathogens; oral anaerobes
Adverse effects of cephalosporins
-allergy
-cross allergy w/ penicillins
-anaphylactic runs are rare
-rare stuff like increase in liver enzyme, nephrotoxicity, thrombocytopenia
Cephalosporins have drug interactions with these drugs so you want to reduce oral absorption of these
- antacids
- H2 histamine receptor antagonists
- proton pump inhibitors
- iron supplements
- food
Combination of cephalosporins with ______________ or ______ _________ leads to Nephrotoxicity
aminoglycosides or loop diuretics
If you combine cephalosporins with ethanol, what is the result?
disulfiram-like reaction and possible hypoprothrombinemia
Contraindications of cephalosporins
Allergy to these drugs
* A history of severe penicillin reactions or a positive skin test reaction to the penicillin minor determinant mixture
Which B-lactams cause serious infections
carbapenems
monobactems
Carbacephems
Carbapenems use is for?
highly resistant gram - and some anaerobes
Symptoms of toxicity of carbapenems
GI distress, skin rash, CNS toxicity (seizures) at high plasma levels
Erythromycin, azithromycin, and clarithromycin are examples of
macrolides
Mechanism of action of macrolides
Inhibit protein synthesis by binding to 50S ribosomal subunit & preventing translocation
Use of eryhtromycin in dentistry?
acute orofacial infections
gram + aerobic/facultative cocci
Use of clarithromycin in dentistry?
gram + anaerobes
Use of azithromycin in dentistry?
gram - anaerobes
Name some adverse effects of macrolides
- Epigastric pain (most common serious AE)
- Ototoxicity (deafness)
- Ventricular arrhythmias (torsades de pointes)
- Long QT syndrome
- Acute pancreatitis
- Cholestatic hepatitis (erythromycin estolate
- Hypersensitivity syndrome
Name some drug interactions of macrolides
-inhibit liver enzyme (cytochrome P450) -> can affect GI microbial flora
-avoid medications that prolong QT
Contraindications of macrolides
-allergy
-history of allergic cholestatic hepatitis
Mechanism of action of ketolides
Inhibits bacterial protein synthesis (50S + formation of 50S and 30S).
Name the activitiy of ketolides
wide spectrum of respiratory pathogens
Adverse effects of ketolides
diarrhea, nausea
inhibit CytP450
Long QT syndrome
Mechanism of action of tetracycline
Reversible binding to 30s, preventing charged tRNA from binding to acceptor site
T/F tetracyclines are bacteriostatic
True
Use of tetracyclines in dentistry
-managing localized aggressive periodontitis
-sub-gingivally
Adverse effects of tetracyclines
-photosensitiviy,
-liver dysfunction
-teeth staining
-pigment changes in hair skin and nails
Tetracyclines orał absorption can be impaired by
chelation
Tetracycline metabolism is mostly?
hepatic (CYP3A4)
______ dose adjustment is required for tetracycline
Renal
Contraindications of tetracycline
known drug allergies, avoid for pregnany and nursing women, should not be given to children younger than 8 yrs old
Drug interactions of tetracycline
warfarin
iron
barbituates
Mechanism of action of aminoglycosides
Bactericidal.
Irreversible inhibition of initiation complex through binding of the 30S subunit to inhibit protein synthesis
concentration-dependent
Clinical use of aminoglycosides
-good against gram - aerobic
-no indication for orofacial infection
Adverse effects of aminoglycosides
ototoxicity and nephrotoxicity
Drugs interactions of aminoglycosides
-increased toxicity by loop diuretics
-increase neuromuscular blocking effect of curare-type drugs
The root floxacin tells you the drug is a….
fluroquinolone
Mechanism of action of fluroquinolones
Blocks DNA synthesis by interfering with bacterial DNA gyrase & topoisomerase
Clinical use for fluroquinolones
-pnuemonia
-UTI
-intraabodominal infections
Adverse effects of fluroquiolones
- Nausea/vomiting
- Dyspepsia
- Abdominal pain
- PMC and diarrhea
- Headache
- Phototoxicity
- QTc interval prolongation
- Chondrotoxicity
Drugs interactions of fluoroquinolones
-don’t combines with:
other drugs that increase CNS toxicity like TCAs, phenothiazines, and erythromycin
-warfarin
-antacids
Contraindications of fluoroquinolones
allergy
-under 18 yrs
This class of drugs has high oral bioavailability and the metabolism is hepatic
fluoroquinolones
One of the first groups of antibiotics
Sulfonamides
Mechanism of action of sulfonamides
Inhibit the synthesis of folic acid (folate)
Clinical use for sulfonamides
-UTI
-acute bronchitis
-pneumonia
-traveler’s diarrhea
Adverse effects of sulfonamides
- Nausea/vomiting
- Blood dyscrasias
- Crystalluria
- Photosensitivity
- Stevens-Johnson syndrome (skin eruptions)
Mechanism of action of chloramphenicol
Inhibits protein synthesis by reversibly binding to the 50S subunit
bacteriostatic
-aerobic and anaerobic Gram + and Gram -
T/F Chloramphenicol are commonly prescribed in the US
False! They’re rarely used bc there are better alternatives
Mechanism of action of vancomycin
Binds D-Ala-D-Ala to inhibit a rxn in peptidoglycan synthesis to inhibit cell wall synthesis
bactericidal
Clinical use of vancomycin
gram + infections
Name some topical antibiotics (neosporin)
- Bacitracin
- Neomycin
- Polymyxin B
- Mupirocin