Pharm Memorization

What are the CYP3A4 inducers?

“primary Care physicians “R” saints”

pheytoin, carbamazepine, phenobarbitol, rifampin, St. John’s Wort

What are the CYP3A4 Inhibitors?

“Can everyone keep calm in good raves?”

cimetidine, erythromycin, ketoconazole, clarithromycin, itraconazole, grapefruit, ritonavir

What are the CYP1A2 inducers?

cigarette smoke

What are the beta-lactamase inhibitors?

“The cat sleeps tightly and has a very real dream”

irreversible: clavulanic acid, sulbactam, tazobactam

reversible: avibactam, vaborbactam, relebactam, durlobactam

What happens when OAT is inhibited?

the other drug will not get secreted renally and this will lead to increased drug levels that can lead to toxicity

What is the mechanism of the aminoglycosides?

they bind to the 30S subunit and cause mRNA misreading

what is the mechanism of the tetracyclines?

they bind to the 30S subunit and prevent tRNA binding

What is the mechanism of the macrolides?

they bind to the 50S subunit and stop translocation (tunnel plug)

what is the mechanism of the beta-lactams?

they target the peptidoglycan cell wall; they interrupt cell wall cross-linking by binding to PBPs (penicillin binding proteins) which triggers autolysins (osmotic rupture)

what are the beta-lactams?

penicillins, cephalosporines, carbapenems, and monobactams

What is the mechanism of the oxazolinones?

they bind to the 23S ribosomal RNA of the 50S subunit and inhibit the formation of the 70S initiation complex

the bind to the 23S rRNA in the 50S subunit in the A site pocket near the interface with the 30S subunit

What is the mechanism of chloramphenicol?

binds to the 50S subunit and inhibits the interaction between the amino acid and the peptidyl transferase

What is the mechanism of the sulfonamides?

they compete with PABA for dihydropteroate synthase which prevents the conversion of PABA to dihydrofolic acid (inhibits folic acid synthesis and is taken along with trimethoprim)

What is the mechanism of the lipopeptides?

they have a lipid tail that makes a hole in the membrane for ions to leak out of which leads to the arrest of DNA, RNA, and protein synthesis (leads to rapid cell death)

What are the natural penicillins?

Penicillin G and V

what are the penicillinase-resistant penicillins?

nafcillin, oxacillin, dicloxacillin, cloxacillin

What are the aminopenicillins?

ampicillin and amoxicillin

What are the 1st generation cephalosporins?

cefazolin and cephalexin

what are the 2nd generation cephalosporins?

cefuroxime and cefoxitin

what are the 3rd generation cephalosporins?

ceftriaxone, cefotaxime, cefdinir, ceftazidime

What are the 4th generation cephalosporins?

cefepime

What are the advanced generation cephalosporins?

ceftaroline and cefiderocol

What are the carbapenems?

imipenem and meropenem

what are the monobactams?

aztreonam

What are the glycopeptides?

vancomycin

what are the lipopeptides?

daptomycin

What are the aminoglycosides?

gentamycin, tobramycin, amikacin, streptomycin, and neomycin

What are the oxazolidinones?

linezolid

What are the tetracyclines?

doxycycline, minocycline, demeclocycline, and tigecycline

What are the macrolides?

erythromycin, clarithromycin, and azithromycin

What are the sulfonamides?

trimethoprim-sulfamethoxazole, sulfamethoxazole, silver sulfadiazine, sulfadiazine, mafenide acetate, and sulfadoxine

What do we use to treat gonorrhea?

cetriaxone

What do we use to treat treponema pallidum (syphilis)?

Penicillin G with benzathine

What do we use to treat Neiserria Meningitidis?

penicillin G and V

ceftriaxone and cefotaxime

What beta-lactam can we use for MRSA?

ceftaroline

What beta-lactam can we use to treat MDR GNB?

cefiderocol

What do we use to treat bacterioides fragilis?

cefoxitin, ceftazoline-avibactam, all carbapenems

what is preferred for neonates? ceftriaxone or cefotaxime

cefotaxime (does not cause kernicterus)

ceftriaxone: this can displace unconjugated bilirubin and lead to kernicterus

P aeruginosa lung infection in cystic fibrosis patients use:

aztreonam inhalation

What drug is associated with red man syndrome when administered too fast?

vancomycin

What drugs can we not give with statins?

daptomycin

What drug can you not give with SSRIs because of serotonin sickness?

linezolid

What are the toxicities are risks associated with aminoglycosides?

nephrotoxicity, ototoxicity, and neuromuscular blockade/ respiratory paralysis

What tetracycline is 100% bioavailable?

minocycline

What penicillin is 100% bioavailable?

amoxicillin

Which tetracyclines can be taken with food and which ones have to be taken on an empty stomach?

food: doxycycline and minocycline

empty stomach: tetracycline and demeclocycline

What drug class is associated with growing bones and staining teeth? What is the one exception in this class and why?

tetracyclines

doxycycline: it has a low affinity for calcium

What do we use to treat whooping cough?

Azithromycin and clarithromycin

What drug has an interaction known to cause gray syndrome/ gray baby syndrome?

chloramphenicol

What do we use to treat Pneumocystis jirovecii?

trimethoprim-sulfamethoxazole

What is contraindicated for treating Rickettsia?

sulfonamides have been known to stimulate the growth of Rickettsia

What is the drug of choice for nocardia?

Trimethorpim-sulfamethoxazole

What is the mechanism of fluoroquinolones?

they inhibit bacterial DNA gyrase and topoisomerase IV

What are the fluoroquinolones?

ciprofloxacin, levofloxacin, moxifloxacin, and delafloxacin

What is the interaction between diphenhydramine and tricyclic antidepressants?

both of them act on muscarinic receptors, this can lead to additive anticholinergic toxicities (like dry mouth, blurry vision, and drowsiness)

What is the interaction between nitroglycerin and sildenafil?

increased vasodilation when used together; there is a risk of profound hypotension due to synergistic effects

What is the interaction between codeine and acetaminophen?

they have an enhanced analgesic effect when combined; this allows for lower doses of each drug for effective pain relief

What is the interaction between methadone and itraconazole?

both drugs prolong QT interval, increasing the risk of ventricular arrhythmia (torsades de pointes)

What is the interaction between sulfonamide and trimethoprim?

enhanced antibacterial action: bacteriostatic becomes bactericidal

What is the interaction between amoxicillin and clavulanic acid?

increased antibacterial activity; clavulanic acid protects amoxicillin from degradation

What are the drugs that are effective against psuedomonas?

piperacillin-tazobactam; cefapime, ceftaroline, cefiderocol, all carbapenems, aztreonam, ciprofloxacin, levofloxacin, delafloxacin, ceftazidime

What are the drugs for MSSA and MSSE?

penicillinase resistant penicillins (nafcilin, oxacilin, dicloxacillin, and cloxacillin), sulfonamide (MSSA), and levofloxacin, moxifloxacin, and delafloxacin (MSSA)

What are the drugs for MRSA?

vancomycin, daptomycin, sulfonamide, delafloxacin

What drugs are used for Listeria Monocytogenes (gram-positive)?

ampicillin, linezolid, and trimethoprime-sulfamethoxazole

What are the drugs used for

What drug do we use for a C diff infection?

vancomycin

What do we use to treat lyme disease?

doxycycline

What drug do we use for most zoonoses?

doxycycline

What drug do we use for community acquired pneumonia?

cetaroline

What are the acquired resistance mechanisms against beta lactams?

1. enzymatic degradation of the drugs (beta-lactamases break ring, staph and gram neg are notorious for this)

2. modification of penicillin binding protein/transpeptidase (drug target)

   1. staph, MRSA, strep pneumo, and enterococcus

3. reduced drug concentration at the site of action (efflux by gram neg bacteria

What are the intrinsic resistance mechanisms against beta lactams?

obligate intracellular bacteria have intrinsic resistance, so do the atypicals (chlamydia, legionella, rickettsia)

What has intrinsic resistance to penicillin G?

gram negative bacilli (pen G cannot penetrate the porins)

What are the mechanisms of resistance for vancomycin?

changing of the site of action: enterococci change D-ala-D-ala to D-ala-D-lactate which decreases binding of the drug

S aureus: VanA gene confers a high level of resistance; can also develop thick cell wall that traps vancomycin in the cell wall

What has intrinsic resistance to vancomycin?

all gram neg drugs and mycobacteria (causes TB)

What drugs are active against the “gut bugs” (aerobic gram-neg organisms)?

aminoglycosides

What is the intrinsic resistance to aminoglycosides?

anaerobic bacteria, facultative anaerobes in anaerobic environment

What are the mechanisms of acquired resistance to aminoglycosides?

1. inactivation (production of transferase enzymes that inactivate the drug)

2. impaired entry: change porins

3. target alteration: change the 30S ribosome binding site

What drug is cautioned with patients who have myasthenia gravis or are pregnant/breast-feeding?

aminoglycosides

What are the mechanisms of acquired resistance against tetracyclines?

1. Efflux pumps (TetK and TetAE)

   1. gram-neg

2. ribosomal protection proteins (RPPs)

What are the mechanisms of intrinsic resistance against tetracyclines?

proteus and P aeruginosa have intrinsic resistance by chromosomally encoded MDR efflux pumps

When tetracycline is out of date what happens?

it can become toxic and cause renal acidosis

What are the mechanisms of resistance for macrolides?

ribosomal modification (methylase modifies the macrolide binding site; ERM gene makes methylase)

What is the mechanism of resistance against oxazinones (linezolid)?

mutation at binding site

intrinsic resistance: aerobic gram negative and all anaerobic bacteria

What drug should you not use when a patient has a high intake of dietary tyramine (cheese, wine, pickles)?

linezolid

What is the acquired resistance against sulfonamides?

decreased intracellular concentration of drug (decreasing cellular permeability or efflux)

increase PABA production

modified targets that have low affinity for the drug (altered dihydropteroate synthase or altered dihydrofolate reductase)

What drug is associated with tendon rupture, neuropathy, tendonopathy?

fluoroquinolones

What are the mechanisms of resistance against fluoroquinolones?

1. chromosomally-mediated mechanisms (most common)

   1. target modification or reduced accumulation of drug (porin changes or efflux)

2. plasmid-mediated mechanisms

   1. topo protection

   2. drug modification (acetylation by acetyltransferase that inactivates the drug)

What drug is used for acne?

doxycycline (photosensitivity)

What drug is this?

prevents transpeptidation (causing dissociation of unfinished peptide)

wide spectrum of activity (especially respiratory pathogens)

high prevalence to S pneumo

extensive sequestration in tissues

causes QT interval prolongation

once daily dosing

azithromycin

What drug is this?

inhibits bacterial cell wall synthesis

wide spectrum of activity

parenteral use only

once daily dosing

not recommended for new born babies

cetriaxone

What beta lactamase inhibitor do you pair with amoxacillin?

clavulanic acid

What beta lactamase inhibitor do you pair with ampicillin?

sulbactam

What beta lactamase inhibitor do you pair with imapenem?

relebactam (silastatin)

What beta lactamase inhibitor do you pair with meropenem?

vaborbactam

What beta lactamase inhibitor do you pair with piperacillin?

tazobactam

Fun facts about amoxacillin

activity against S pneumo

only oral penicillin

100% bioavailability

What do we use to treat cellulitis?

first gen cephalosporins (cefalexin and cefazolin)

What do we use to treat prostatitis (due to E coli)?

fluoroquinolone

What do we use to treat carbapenem resistant E coli, MDR UTIs, and renal tubular necrosis?

amikacin

If one drug achieves the same effect as another but with lower dose it will be _____, meaning it has ______

potent, has higher affinity for the receptor (making it more potent)