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Pharmacology-PA

Antibiotics

QuestionAnswer
What are some of the factors clinicians typically consider in selecting an empiric antibiotic therapy? 1- Gram Stain results- Gram + / Gram -, 2-Co-morbidity, 3-Drug allergies, 4-Severity of pneumonia, 5- Antibiotic cost, 6-Patient convenience as it relates to compliance
What are the common antibiotic treatments for sinusitis? Amoxicillin and TMP/SMX
Why is Amoxicillin used as a common antibiotic tx for sinusitis? AKA: aminopenicillin,1-Dose should be doubled in areas where resistance to S. pneumoniae is high, 2-Can penetrate through some Gram + / Gram – organisms, 3-Amino side group makes these agents hydrophilic enough to penetrate the porins in gram negative
Why is TMP/SMX used as a common antibiotic tx for sinusitis? AKA: Bactrim, 1-prevent intracranial complications, 2-help with the restoring and improvement of sinus functions, 3-eradicating the causative pathogen(s)
What are some of the non-antibiotic treatments employed in sinusitis that we discussed in class? 1- Phenylephrine or Oxymetazoline vasoconstrictor sprays or drops, 2- Phenylephrine or Neo- Synephrine, 3-Oxymetazoline
Why and how is Phenylephrine or Oxymetazoline vasoconstrictor sprays or drops used against sinusitis as a form of non-antibiotic tx? Phenylephrine or Oxymetazoline vasoconstrictor sprays or drops may facilitate drainage.The use of such agents should not exceed 72 hours owing to a tolerance effect and possible rebound congestion. Antihistamines are not effective in the treatment of a
Why and how is Phenylephrine or Neo-Synephrine used against sinusitis as a form of non-antibiotic tx? Phenylephrine or Neo-Synephrine is an α1-adrenergic receptor agonist used primarily as a decongestant, mydriatic, and vasopressor. It is available as an oral medicine or as a nasal spray. It is now the most common over-the-counter (OTC) decongestant.
What are the Adverse reactions of Phenylephrine or Neo-Synephrine? 1-hypertension, 2-prostatic hyperplasia, 3-rebound hyperemia with chronic use
Why and how is Oxymetazoline used against sinusitis as a form of non-antibiotic tx? Oxymetazoline is a selective alpha-1 agonist and partial alpha-2 agonist topical decongestant, found in products such as Afrin, Dristan, Nasivin, Vicks,Sinex, Visine L.R., and Zicam. It is available as a nasal spray.
What is a cause of Oxymetazoline? It causes down-regulation of alpha-2 receptors, and therefore becomes less effective after a few doses.
What happens when there is an overuse of Oxymetazoline? It can cause a "rebound congestion”
What kind of an application is Oxymetazoline? Topical
True/False. Since the application of Oxymetazoline is topical, it has practically no CNS stimulation as of the systemic application of decongestants such as pseudoephedrine. True
What are the antiviral medications we have discussed so far in class? 1- Amantadine/ Rimantadine, 2- Amantadine, 3- Rimantadine, 4- Ribavirin
What is the antiviral spectrum of Amantadine/ Rimantadine? limited to influenza A virus, with effectiveness related to preventing infection – start therapy within 48 hours of exposure to the virus
What is the Mechanism of Action (MOA) of Amantadine/ Rimantadine? It is unknown, possibly blockage of the viral membrane matrix protein, which functions as an ion channel
True or False. Both Amantadine/ Rimantadine are well absorbed in the GI tract. True
True or False. Is Amantadine/ Rimantadine widely distributed throughout the body. True
How is Amantadine eliminated? primarily in the urine
True/False. Amantadine is not distributed throughout the body and the CNS. False
True/False. Amantadine appears to inhibit in an early stage of viral replication. True
True/False. Amantadine is not extensively metabolized and may reach toxic levels in pts with renal compromise. True
What are the ADR of Amantadine? CNS (ataxia, dizziness, insomnia – more seriously, hallucinations and seizures)
True/False. Amantadine should be avoided in pregnant and nursing mothers. True
True/False. Rimantadine is not extensively metabolized and then excreted in urine. False
True/False. Does Rimantadine inhibits viral RNA and protein synthesis. True
True/False. Rimantadine does not cross the BBB. True
True/ False. Rimantadine relies heavily on the liver for metabolism with metabolites excreted by the kidneys. True
What are the ADR of Rimantadine? less CNS toxicity than Amantadine (ataxia, dizziness, insomnia – more seriously, hallucinations and seizures)
Should Rimantadine be avoided in pregnant and nursing mothers like Amantadine? Yes
How is Ribavirin administered? Administered by nasal or oral inhalation
Where is Ribavirin metabolized? In the liver and by RBCs
True/False. Ribavirin is excreted primarily by the kidneys, with some excreted in stool. True
What is the antiviral spectrum of Ribavirin? Antiviral Spectrum:pediatrics with severe RSV infection, some efficacy against acute hepatitis A, influenza A, and influenza B reported
What is the Mechanism of Action of Ribavirin? guanosine analog that converts ribavirin – triphosphate which purportedly inhibits viral mRNA synthesis
True/False. Ribavirin has good penetration into the CNS. False, It has poor penetration into CNS
True/ False. Ribavirin is used in treatment of RSV. True
How is Ribavirin used? It is used as an aerosol
True/False. When Ribavirin is taken metabolites and the drug is excreted in urine. True
True/False. What are the ADR of Ribavirin? Anemia and elevated bilirubin
True/False. Ribavirin is not dose-dependent. False, It is dose-dependent
True/False. Ribavirin is CONTRAINDICATED IN PREGNANCY. True
What antibacterial is one of the most imp. and useful? Penicillins
What is the therapeutic uses of Penicillins? It works in the prevention and treatment of infections caused by susceptible bacteria, such as Gram + bacteria (Streptococcus, Enterococcus, Staphylococcus species)
When was the Penicillins first introduced? 1940’s
True/False. Does Penicillins bind with transpeptidases? True
How is cross-linking of cell walls prevented? The binding of penicillin-binding proteins
True/False. Can Penicillins activate autolytic enzymes? True
What kind of bacteria does Penicillin kill? It kills a wide variety of bacteria, such as Gram + ,Gram – and Spirochetes.
What is another name for the penicillins? “beta-lactams”
What is the Mechanism of action for penicillin? 1-To enter the bacteria via cell wall, 2-inside the cell, they bind to penicillin-binding proteins, 3-once bound, normal cell wall synthesis is disrupted, 4- results in bacteria cells dying from cell lysis.
What is the mechanism of Tetracycline? Bacteriostatic, which inhibit bacterial growth
True/False. Tetracycline binds reversibly to 50 S ribosomal subunit. False, It binds reversibly to 30 S
ribosomal subunit.
How does Tetracyclines inhibit protein systhesis? By blocking attachment of aminoacyl-tRNA to
ribosome due to the reversible binding to the 30 S ribosomal unit.
True/False. Are tetracyclines natural and semi-synthetic? True
How does Tetracyclines form insoluble complexes? It binds to Ca2+ and Mg2+ and Al3+ ions
What reduces the absorption of tetracyclines? Dairy, antacids, and iron salts
What advice is given to pts that are going to be taking tetracyclines? Not to eat anything with dairy
products (Milk), Antacids and avoid foods with high amts of iron salts
True/False. Tetracyclines stop many essential functions of the bacteria. True
What are the therapeutic uses of Tetracycline? Wide Spectrum
What are the wide spectrum bacterias involved with Tetracyclines? 1-Gram -, 2-Gram + , 3-protozoa, 4-
mycoplasma, 5-rickettsia, 6-chlamydia, 7-syphilis, 8-Lyme Disease, 9-Acne, 10-Vibrio cholerae
What are the side effects of Tetracyclines? 1-Chelates Calcium, 2-GI fungal infection, 3-N/V, diarrhea, gastric upset, enterocolitis, pseudomembranous colitis, 4-Candida, 5-Vaginal moniliasis, 6-Maculopapular rash
What is Demeclocycline used for? To treat SIADH, pleural and pericardial effusions
What Bacteria causes Lyme Disease that is treated with Tetracyclines? Borrelia Burgdoferi
What is Chelates calcium? Discoloration in permanent teeth and tooth enamel in fetuses and children
What can be a side effect of Tetracycline if taken during pregnancy? It can also lead to retard fetal skeletal development if taken during pregnancy.
True/False. Tetracycline can alter the normal flora that may result in some of the side effects that are possible. False, it alters the intestinal flora.
True/False. Macrolides bind to 30 S ribosomal subunit. False, it binds to 50 S ribosomal subunit.
What is the purpose of Macrolides binding to the 50 S ribosomal subunit? To prevent the continuation of protein synthesis
True/False. Macrolides are acid-sensitive? True
Why must Macrolides be buffered or have a enteric coating? To prevent it from being destructed by the gastric acid due to the fact that Macrolides are acid-sensitive.
True/False. Macrolides and Lincosamides inhibit RNA-dependent protein synthesis by acting on a small portion of the ribosome (50 S). True
Where are the Macrolides absorbed? Duodenum
What metabolizes the Macrolides? The liver
Where is the Macrolides excreted in? In the Bile in high concentrations
True/False. Small amts of Macrolides are excreted in stools. False, it is excreted in the urine.
True/False. Macrolides crosses placental barrier and is secreted in breast milk. True
Macrolides provide broad spectrum of antimicrobial activity against what? Gram + / Gram –
Macrolides are distributed to most tissues and body fluids except one, which fluid is that one? The CSF (only when meninges are inflamed)
What is the mechanism of action for the cephalosporins? Bactericidal action
Does Cephalosporins have broad or narrow spectrum? broad spectrum
What antibiotic class is structurally and pharmacologically related to the antibiotic class of Penicillins? Cephalosporins
What Antibiotic class is a semi-synthetic derivative from a fungus? Cephalosporins
True/False. Cephalosporins are grouped according to their antimicrobial activity. True
What is the name of the bacterial enzyme that Cephalosporins binds to in order to inhibit cell-wall synthesis? PBP’s
Where is the enzyme PBP’s located? Cell membrane
True/False. Carbapenem is not part of the class beta-lactam antibiotics. False, it is part of the beta lactam antibiotics
True/False. Carbapenem have a narrow spectrum of antibacterial activity. False, it has a broad spectrum of antibacterial activity.
True/False. Are Carbapenem highly resistant to beta-lactamases? True
True/False. Carbapenem are not used for serious or life-threatening infection. False, they are used.
Are Carbapenem used for Gram + or Gram – nosocomial infections? They are used for both Gram + and Gram -.
What is the mechanism of action of Sulfonamides? Bacteriostatic action
What does bacteriostatic action do in Sulfonamides? They Decrease the number of bacterial nucleotides.
What does Sulfonamides prevent synthesis of and How? Folic Acid through diet
Why does the Sulfonamides want to prevent the synthesis of Folic Acid? To promote the synthesis of purines and nucleic acid.
True/False. Sulfonamides does not affect human cells or certain bacteria. True, Humans obtain their folic acid through their diet
What are the adverse reactions for Sulfonamides? 1-Hypersensitivity reactions, 2-hemolysis in G6PD-pts, 3-nephrotoxicity, 4-kernicterus in infants
True/False. Sulfonamides bind to albumin. True
What are the side effects of Sulfonamides in the Blood? 1-hemolytic and aplastic anemia, 2-thrombocytopenia
What are the side effects of Sulfonamides in the Integumentary System? 1- Photosensitivity, 2-exfoliative dermatitis, 3-Stevens-Johnson syndrome (erythema Multiforme), 4-epidermal necrolysis
What are the side effects of Sulfonamides in the GI Tract? 1-nausea, 2-vomiting,3-diarrhea, 4-pancreatitis
What are the other side effects of Sulfonamides not assoc. with a system? 1-convulsions, 2-crystalluria, 3-toxic nephrosis, 4-headache, 5-peripheral neuritis, 6-urticaria
True/False. Quinolones do not have excellent oral absorption. False, they have excellent oral absorption.
Do antacids reduce the absorption when Quinolones are taken? Yes
True/False. Are your chances higher to get Achilles Tendon Rupture when Quinolones are taken? True
True/False. Were Quinolones the first oral antibiotics against gram – bacterias? True
What is the mechanism of action for Quinolones? Bacteriocidal
True/False. Quinolones are effective against Gram – and some Gram + organisms. True
When Quinolones taken, how can the host cell enter? Via Porins
Do humans have DNA gyrase and Topoisomerase IV? No, which is why Quinolones are used for humans.
What is DNA gyrase? an essential enzyme of replicating DNA
True/False. DNA gyrase targets Gram + bacteria. False, it targets gram – bacterias.
What does the Topoisomerase IV do? It blocks the DNA replication and transcription.
True/False. Topoisomerase IV targets Gram + bacterias. True
What are the side effects of Quinolones in the CNS? headache, dizziness, fatigue, depression, restlessness
What are the side effects of Quinolones in the GI tract? Nausea/Vomitting, diarrhea, constipation, thrush, increased liver function
What are the side effects of Ouinolones in the Integumentary system? rash, pruritis, urticaria, flushing, photosensitivity (w/ lomefloxacin)
What are the side effects of Quinolones in the other systems? fever, chills, blurred vision, tinnitus
What is the mechanism of action of Aminoglycosides? Bactericidal
True/False. Aminoglycosides bind to 50 S ribosomal subunit. False, it binds to the 30 S ribosomal subunit.
True/False. Aminoglycosides are natural and semi-synthetic. True
True/False. Aminoglycosides are not produced by Streptomyces, which is a form of fungus. False, it is produced by streptomyces.
True/False. Aminoglycosides have poor oral absorption and have no PO forms. True
Does Aminoglycosides require O2 uptake? Yes
True/False. Aminoglycosides are very potent antibiotics with serious toxicities. True
True/False. Aminoglycosides kill mostly gram – and some gram +. True
Are Aminoglycosides used in combinations with other antibiotics for a synergistic effect? Yes
What are Aminoglycosides used to kill? Gram – bacterias (Pseudomonas, Proteus, E. coli, Klebsiella, Serratia) (PPEKS)
True/False. In Aminoglycosides, patients must be monitored for drug level to prevent toxicitity. True
What two toxicities are caused by Aminoglycosides? Nephrotoxicitiy and Ototoxicity
What are the three common systemic drugs of the class Aminoglycosides? 1-Gentamycin, 2-tobramycin, 3-amikacin
Is Aztreonam called monobactams? Yes
What is the mechanism of action of Aztreonam? Bactericidal
True/False. Aztreonam has inhibition of bacterial cell-wall synthesis. True
What does Aztreonam bind to? Binds to PBP-3 of susceptible Gram – bacterial cells, inhibiting cell wall division & lysis
True/False. Aztreonam does not contain the bicyclic adjoining ring fused to the Beta-lactam ring. True
Is Aztreonam active against Gram – rods including Pseudomonas. True
Aztreonam is not synergistic w/ aminoglycosides. False, it is synergistic w/ aminoglycoside
In Aztreonam, is there little or no activity against Gram + organisms/ anaerobes. True
Is Aztreonam used for pts w/ severe PCN allergy and renal dysfunction? Yes
What are the adverse reactions of Aztreonam? GI upset, headache, vertigo, superinfection
True/ False. Clindamycin is part of the Lincosamide antibiotic class. True
True/False. Clindamycin binds to the 50 S ribosomal subunit. True
True/False. Clindamycin inhibits bacterial protein synthesis and may also inhibit the binding of bacterial ribosomes. True
True/False. Clindamycin is not effective against Gram + and anerobic bacteria (bacteroides). False, they are effective against gram + and anarobes.
What are the adverse reactions of Clindamycin? diarrhea, pseudomembranous colitis (liver), Clostridium difficile infection (rash)
What are the four groups of Penicillins? 1-Natural, 2-Penicillinase-resistant penicillins (narrow spectrum), 3-Aminopenicillins (Wide Spectrum), 4-Extended Spectrum (antipseudomonal) penicillin.
What are the Natural penicillins? 1-penicillin G benzathine, 2-penicillin G potassium, 3-penicillin G procaine, 4-penicillin G sodium, 5-penicillin V potassium
What are the Penicillinase-resistant penicillins (narrow-spectrum)? 1-dicloxacillin, 2-nafcillin, 3-oxacillin, 4-cloxacillin, 5-methicillin
What drug is associated w/ interstitial nephritis? methicillin
What are the Aminopenicillins? 1-amoxicillin, 2-ampicillin, 3-bacampacillin
What are the Extended-Spectrum Penicillins? 1-carbenicillin, 2-ticarcillin, 3-piperacillin, 4-mezlocillin
Which of the following is not a penicillin beta-lactamase inhibitor combination drug? 1- Augmentin, 2-Bactrim, 3-Timentin, 4-Zosyn, 5-Unasyn, 6-Pedizole. 6-Pediazole is not a beta-lactamase inhibitor, it is a sulfonamide (sulfisoxazole)
What combination makes up Augmentin? Amoxicillin + Clauvulanic acid
What combination makes up Bactrim? trimethoprim + sulfamethoxazole
What combination make up Timentin? Ticarcillin + Clauvulanic acid
What combination make up Zosyn? Piperacillin + Tazobactam
What combination make up Unasyn? Ampicillin + Sulbactam
What combination make up Pediazole? Erythromycin (Macrolide) + Sulfonamide
What is Pediazole used for? To treat otitis media in children
Which generation of cephalosporin acts primarily against Gram +? First Generation Cephalosporin
T/F First Generation Cephalosporin act primarily against Gram + organisms. True
T/F First Generation Cephalosporin may be used as alternative therapy in pts allergic to penicillin (depends on sensitivity to penicillin). True
T/F First Generation Cephalosporin is used to treat staphylococcal and streptococcal infections  pneumonia, cellulites, osteomyelitis. True
T/F First Generation Cephalosporin is Effective against Proteus mirabilis, E. coli, Klebsiella pneumoniae, Shigella. True
T/F Second Generation Cephalosporin have Good Gram + coverage. True
T/F Second Generation Cephalosporin act against Gram – bacteria but better than first generation. True
T/F Second Generation Cephalosporin Cefoxitin and cefotetan are the only cephalosporins effective against anaerobes. True
T/F Second Generation Cephalosporin has No activity against enterococcus or Pseudomonas. True
T/F Second Generation Cephalosporin has Limited activity against Enterobacter, Citrobacter, Serratia. True
T/F Third Generation Cephalosporin are Less active against Gram + organisms. True
T/F Third Generation Cephalosporin are Less active against Staphylococci. True
T/F Third Generation Cephalosporin has No activity against enterococcus. True
T/F Third Generation Cephalosporin act primarily against Gram – organisms. True
T/F Third Generation Cephalosporin are the drugs of choice for infections caused by: Enterobacter, Pseudomonas, anaerobic organisms (minimal activity for anaerobes). True
T/F Fourth Generation Cephalosporin are active against many Gram + / Gram – bacteria (good efficacy)* except for MRSA and enterococcal infections. True
T/F Fourth Generation Cephalosporin has a broader spectrum of antibacterial activity than third generation, esp Gram + bacteria True
T/F Fourth Generation Cephalosporin are usually placed in “reserve” for multi-resistant, nosocomial strains causing infections. True
T/F First Generation Cephalosporin Cefazolin: (Ancef and Kefzol) are given by IV and PO and used for surgical prophylaxis, URIs, otitis media. True
T/F First Generation Cephalosporin Cephalexin: (Keflex and Keftab) are given PO and used for surgical prophylaxis, URIs, otitis media. True
T/F Second Generation Cephalosporin Cefoxitin: (Mefoxin) are given IV and IM and are used prophylactically for abdominal or colorectal surgeries; also kills anaerobes. True
T/F Second Generation Cephalosporin Cefuroxime: (Kefurox and Ceftin) are given PO and used for surgical prophylaxis; does not kill anaerobes. True
T/F Third Generation Cephalosporin Cefixime: (Suprax) is the ONLY ORAL 3rd generation agent and is the best available oral cephalosporins against Gram – organisms and are given by tablet and suspension. True
T/F Third Generation Cephalosporin Ceftriaxone: (Rocephin) is given by IV and IM, has a long half life, is a once a day dosing and it easily passes meninges and diffused into CSF to treat CNS infections. True
T/F Third Generation Cephalosporin Ceftazidime is given IV and IM, has excellent Gram – coverage and is used for difficult to treat organisms such as Pseudomonas and is eliminated by renal instead of biliary route and has excellent spectrum of coverage. True
What are the fourth generation Cephalosporins? 1-Cefepine (Ceftrixone + Ceftazidme)
What is Cefepime? 4th gen cephalosporin (Maxipime)-newest
T/F Fourth Generation Cephalosporin Cefepime: (Maxipime) is the newest and has broader spectrum than 3rd generation, esp Gram + bacteria. True
T/F Fourth Generation Cephalosporin has Good efficacy against Gram + / Gram – organisms (except MRSA and enterococcal infections). True
T/F Fourth Generation Cephalosporin is Usually placed “in reserve” for multi-resistant nosocomial strains causing infections. True
Created by: sap_213 on 2008-10-06



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