Exam 2 Flashcards
Cardiac action potential phase 0
sodium channels open (Na+ in)
Phase I action potential
sodium channels close, potassium channels begin to open (K+) out
Phase II action potential
calcium and potassium channels open (Ca++ in and K+ out)
Phase III action potential
calcium channels close
Phase IV action potential
cells return to resting membrane potential (-70 mv)
all anti-arrhythmic drugs are potentially
pro-arrhythmic as well
anti-arrhythmic drug class Ia, Ib, Ic
sodium channel blockade
anti-arrhythmic drug class II
beta adrenergic receptor blockade
anti-arrhythmic drug class III
potassium channel blockade
anti-arrhythmic drug class IV
calcium channel blockade
what do anti-arrhythmic drug class Ia do
slow phase 0 depolarization, prolong action potential and slow conduction
what do anti-arrhythmic drug class Ib do
shorten phase 3 repolarization and decrease the duration of the action potential by blocking or inactivating sodium channels
what do anti-arrhythmic drug class Ic do
markedly slow phase 0 depolarization
what do anti-arrhythmic drug class II do
diminish phase 4 depolarization, thus depressing automaticity
what do anti-arrhythmic drug class III do
agents prolong phase 3 repolarization without altering phase 0
what do anti-arrhythmic drug class IV do
agents slow phase 4 depolarization and slow conduction particularly at the AV node
class of Quinidine/Quinidex
anti-arrhythmic–Class Ia
Quinidine/Quinidex indication
A-flutter, A-fib, AV, and ventricular arrhythmias
MOA of Quinidine/Quinidex
sodium channel blocker. diminished inward flow of sodium at phase 0 results in decreased automaticity and a lengthened refractory period
Char. of Quinidine/Quinidex
PO, IV. less commonly used because of significant adverse effect profile
side effects of Quinidine/Quinidex
potentially pro-arrhythmic, nausea, vomiting, diarrhea. Cinchonism
symptoms of cinchonism include
blurred vision, tinnitus, nausea, vomiting, headache, disoreintation and possible psychotic states
Quinidine/Quinidex may induce abnormal rhythm of ventricular tachycardia known as
Torsade de Pointes
Class of Mexiletine/Mexitil
anti-arrhythmic Class Ib
indication of Mexiletine/Mexitil
ventricular arrhythmias, particularly recurrent v-tach after MI
MOA of Mexiletine/Mexitil
blocks open sodium channels and shortens phase 3 repolarization
Char. of Mexiletine/Mexitil
PO, IV
side effects of Mexiletine/Mexitil
drowsiness, confusion, potentially pro-arrhythmic
Class of Flecainide/ Tambocor
anti-arrhythmic Class Ic
indication of Flecainide/ Tambocor
treatment of many types of supraventricular tachycardias, including Wolff-Parkinson-White syndrome, paroxysmal atrial fibrillation, paroxysmal supraventricular tachycardia and ventircular tachycardia
MOA of Flecainide/ Tambocor
sodium channel blocker
Char. of Flecainide/ Tambocor
PO, IV, narrow therapeutic index
side effects of Flecainide/ Tambocor
potentially pro-arrhythmic. not indicated for patients with a history of MI or ventricular arrhythmia related to acute ischemic event
primary Class II/Beta Blocker
Atenolol/Tenormin
class of Atenolol/Tenormin
anti-arrhythmic Class II
indication of Atenolol/Tenormin
tachyarrhythmias such as A-flutter, A-fib, atrioventricular and ventricular arrhythmias, paroxysmal supraventricular tachycardias, HTN, angina
MOA of Atenolol/Tenormin
beta 1 blockade reduces sympathetic effects on myocardium. reduced phase 4 depolarization and decreased automaticity in the SA node, AV node, and the Purkinje fibers
Char. of Atenolol/Tenormin
PO, IV
side effects of Atenolol/Tenormin
Bradycardia, hypotension, dizziness. Bronchoconstriction is possible but occurs less frequently in selective beta blockers. Depression, fatigue, impotency.
Primary Class III/K+ channel blocker
Amiodarone/ Cordarone
class of Amiodarone/ Cordarone
anti-arrhythmic Class III
indication for Amiodarone/ Cordarone
ventricular arrhythmias
MOA of Amiodarone/ Cordarone
potassium channel blockade. prolongs phase 3
char. of Amiodarone/ Cordarone
PO, IV.
Amiodarone/ Cordarone contains high levels of
iodine
side effects of Amiodarone/ Cordarone
Dizziness and light headedness. Pulmonary fibrosis possible. Blue-gray coloring of skin can occur as a result of iodine deposition.
primary Class IV/Ca++ channel blocker
Verapamil/ Calan, Isoptin
class of Verapamil/ Calan, Isoptin
anti-arrhythmic Class IV
indication of Verapamil/ Calan, Isoptin
A-flutter, A-fib and paroxysmal supraventricular tachycardias, HTN, angina
MOA of Verapamil/ Calan, Isoptin
calcium channel blockade causes a slowing of phase 4 depolarization, resulting in slowed AV conduction. suppression of both SA and AV node activity often results in decreased heart rate.
Char. of Verapamil/ Calan, Isoptin
PO
side effects of Verapamil/ Calan, Isoptin
dizziness, flushing, headaches, hypotension
Adenosine/ Adenocard acts directly on the heart’s
sinus pacemaker cells and vagal nerve terminals to decrease chronotropic and ionotropic activity
Adenosine/ Adenocard is recommended as the initial drug of choice for
PSVT
class of Adenosine/ Adenocard
anti-arrhythmic-endeogenous nucleoside
indication of Adenosine/ Adenocard
abolishes acute paroxysmal supraventricular tachycardias
MOA of Adenosine/ Adenocard
prolongs the refractory period and decreases automaticity in the AV node
Char. of Adenosine/ Adenocard
IV only. Duration of action is 15 seconds.
side effects of Adenosine/ Adenocard
low toxicity but often causes transient hypotension and chest pain
class of Atropine
anti-arrhythmic
indication of Atropine
cardiac use is in treatment of bradycardia
MOA of Atropine
anticholinergic agent - atropine is a competitive inhibitor of the muscarinic acetylcholine receptors thus it can be thought of as a parasympatholytic.
Char. of Atropine
IV, PO. Can be also given via an endotracheal tube
side effects of Atropine
Blurred vision, dilated pupils, dry mouth and increased heart rate are usually among the first toxic effects of atropine. Use of atropine as a cardiac drug is generally confined to emergency treatment of life threatening bradycardia with hypotension.
by blocking the action of acetylcholine, atropine serves as an antidote for
poisoning by organophosphate containing insecticides and nerve gases
topical atropine is used as a
cycloplegic to temporarily paralyze accommodation and as a mydriatic to dilate the pupils
oral atropine can be used to treat
diarrhea as it decreases secretions and slows peristalsis
given preoperatively, atropine decreases
bronchial and salivary secretions
The classic symptoms in acute organophosphate poisoning are
muscarinic in nature…SLUDGE: salivation, lacrimation, urination, diarrhea, gastric distress, emesis
Toxicity due to atropine results in
decreased secretions; flushed, dry, warm skin, visual changes and delirium with hallucinations…Dry as a bone, red as a beet, hot as a hare, blind as a bat, mad as a hatter.
specific antidote for atropine toxicity or tropane alkaloid toxicity is
physostigmine, a reversible acetylcholinesterase inhibitor.
The two most common medications containing cardiac glycosides are
digoxin and digitoxin
Which has a longer half life and is now seldom used because of increased risks of toxicity: Digoxin or digitoxin?
Digitoxin…both has a very low TI though
Digoxin inhibits the Na+/K+ ATPase enzyme system and serves to
increase the inward flow current of sodium and calcium thereby increasing cardiac muscle contractility while also slowing conduction between atria and ventricles.
class of Digoxin/ Lanoxin
anti-arrhythmic - cardiac glycoside
indications of Digoxin/ Lanoxin
CHF. Slows ventricular response to atrial fibrillation and atrial flutter.
MOA of Digoxin/ Lanoxin
Inhibitors the Na+/K+ ATPase pump which serves to increase inward current of sodium followed by a greater influx of calcium. Cardiac contraction is enhanced by the increased concentration of intracellular calcium. Also increases renal perfusion.
Char. of Digoxin/ Lanoxin
PO, 36 hour half life, may cause characteristic flattening or even inversion of the T wave on EKG.
Side effects of Digoxin/ Lanoxin
Digitalis intoxication – observed more frequently in patients with hypokalemia as may occur in patients on thiazides, lasix or other potassium wasting diuretics.
Cardiac signs of Digitalis intoxication
arrhythmias, including bradycardia, partial or complete heart block
GI signs of Digitalis intoxication
nausea, vomiting, anorexia and diarrhea
CNS signs of Digitalis intoxication
drowsiness and fatigue
visual disturbances of Digitalis intoxication
blurred vision, double vision, flickering dots or flashes of light, halos may appear around objects
Treatment of digitalis intoxication is
Digoxin-Fab fragments/ Digibind …they attach to Digoxin molecules and rapidly remove them from receptor sites
most common organic molecule in the brain
cholesterol
leading cause of death in the US
coronary artery disease
Omega-3 fish oil available as a prescription drug
Lovaza
Five categories of cholesterol lowering agents
Niacin, Fibrates, HMG-CoA reductase inhibitors, bile acid binding resins, cholesterol absorption blockers
Side effects of Niacin/nicotinic acid
Pharmacologic use of niacin in doses of 3 grams or more has resulted in acute side effects of flushing, nausea, gastritis and headache. Longer term potential side effects of niacin toxicity include liver damage, retinal damage, gout and rhabdomyolysis (the rapid breakdown of skeletal muscle).
class of Niacin/ Niaspan
Anti-hyperlipidemic/B vitamin
indication of Niacin/ Niaspan
elevated total cholesterol, elevated VLDL, LDL, TG and low HDL levels
MOA of Niacin/ Niaspan
exact mechanism of action is not clear. Niacin appears to decrease VLDL synthesis in the liver while also increasing the clearance of VLDL in the plasma.
Char. of Niacin/ Niaspan
PO. Intense flushing and pruritis is common.
side effects of Niacin/ Niaspan
Less flushing and itching when ASA or NSAIDs taken 30 minutes to an hour before the niacin dose.
Follow LFTs to monitor for any possible hepatic damage. Also monitor glucose levels.
Niacin/Niaspan is Contraindicated in patients with
poorly controlled DM, active liver disease or active peptic ulcer disease.
safest form of niacin that is currently available
non-prescription Inositol hexaniacinate
category of meds that decrease triglyceride production in the liver
fibric acid derivatives
most commonly used fibric acid derivative
Gemfibrozil/Lopid
potential side effects of fibric acid derivatives
liver damage, gall stone formation, nausea, diarrhea, GI upset, rhabdomyolysis, and myalgias
class of Gemfibrozil/Lopid
anti-hyperlipidemic, fibric acid derivative
indication of Gemfibrozil/Lopid
elevated triglyceride levels, low HDL level, types IV and V hyperlipidemia
noted side effects for Gemfibrozil/Lopid
contraindicated in patients with pre-existing gallbladder disease and liver disease
HMG-CoA reductase inhibitors
statins
most common complaints from statins
muscle soreness and muscle weakness…less common are memory, cognitive dysfunction, and insomnia, abdominal pain, nausea, diarrhea, headache, erectile dysfunction
life-threatening side effect of statins
rhabdomyolysis, the severe and rapid muscle breakdown which can lead to acute renal failure
what causes muscle soreness, muscle weakness, and frank rhabdomyolysis when using statins
decreased CoQ10
contraindications to statins
heavy alcohol use, liver disease, unexplained elevation of liver enzymes, pregnancy, lactation
statin drugs that was recalled after multiple deaths from rhabdomyolysis
Cerivastatin/Baycol
primary statin drug
Atorvastin/Lipitor
class of Atorvastin/ Lipitor
anti-hyperlipidemic, HMG-CoA reductase inhibitor
indication of Atorvastin/ Lipitor
elevated total cholesterol, elevated LDL, low HDL levels. Indicated for symptomatic and non-symptomatic coronary artery disease
side effects of Atorvastin/ Lipitor
muscle soreness and weakness. check CPK levels to assess for possible rhabdomyolysis when complaints of severe muscle pain are noted. may cause elevated liver enzymes. follow LFTs–prior to beginning therapy and at 6 weeks and 12 weeks. Plasma drug concentrations are significantly affected by concurrent liver disease.
Can Atorvastin/ Lipitor be used by pregnant women?
no, category X. Also contraindicated in breast feeding mothers as all statin drugs are.
type of drug that binds cholesterol and forms insoluble complexes which are excreted in the feces
bile acid sequestrants
bile acid sequestrants are often used in conjunction with
niacin
primary bile acid sequestrant
cholestyramine/questran
class of Cholestyramine/ Questran
anti-hyperlipidemic, bile acid sequestrant
indication of Cholestyramine/ Questran
elevated cholesterol, elevated LDL, can be used in patients with liver failure who have pruritis, as well as patients with increasing ammonia levels, patients with c. diff.
MOA of Cholestyramine/ Questran
forms an insoluble complex with bile salts resulting in greater amounts of cholesterol being oxidized into bile acids and increased excretion of bile acids in stool
side effects of Cholestyramine/ Questran
bloating, constipation, may interfere with absorption of fat soluble vitamins and folic acid. May delay the absorption of concomitant medications. The use of bile acid sequestrants has not been adequately studied in pregnant women and thus falls into category C. That being said, I personally recommend avoiding the use of this agent in both pregnancy and during lactation.
The newest agents for the treatment of hypercholesterolemia act by
reducing the amount of cholesterol that is absorbed by the body.
class of Ezetimibe/ Zetia
anti-hyperlipidemic - cholesterol absorption inhibitor
ind. of Ezetimibe/ Zetia
elevated cholesterol, elevated LDL, elevated triglyceride and low HDL
MOA of Ezetimibe/ Zetia
inhibits intestinal absorption of cholesterol at the brush border
side effects of Ezetimibe/ Zetia
diarrhea, myalgias, arthralgias, abdominal pain. all statin concerns to be observed when Ezetimibe/ Zetia is used with a statin drug. Cautious use in pregnancy - Cat C.
what is Vytorin
Category X drugs which combines the statin Simvastatin with Ezetimibe into a single fixed dose pill
prescription fish oil
Lovaza
meaning of cidal
ability to kill a microorganism
meaning of static
ability of an agent to inhibit the proliferation of an organism
examples of synthetic antimicrobial drugs
sulfonamides and Quinolones
what is MIC
minimum inhibitory concentration
what is MBC
minimum bactericidal concentration
what is macrodilution testing
known amounts of bacteria are inoculated into a nutrient broth containing a dilutional series of antibiotic concentrations.
conjugation
passage of genes from cell to cell allows for development of drug resistance to occur
mutation
DNA of the microbe line is spontaneously modified
transduction
bacteriophage carries modified DNA into the microbe to confer resistance
what can inactivate some antimicrobials
pus (i.e. the aminoglycosides), hemoglobin in hematomas (i.e. the tetracyclines and penicillins), and the acidic environments of abscesses (i.e. the macrolides)
all antimicrobial agents have a spectrum of potential adverse side-effects including but not limited to
hypersensitivity reactions, toxicity, development of additional infection or supra-infection
class of Sulfamethoxazole/ Gantanol
sulfonamide antibiotic…he said he wont ask about this one in all likelihood
MOA of Sulfamethoxazole/ Gantanol
competitive antagonists of paraaminobenzoic acid (PABA) which is used by bacteria in the synthesis of folic acid
Char. of Sulfamethoxazole/ Gantanol
sensitive organisms are those that must synthesize their own folic acid. Broad spectrum antibiotic. Bacteriostatic. Distributed throughout all tissues of the body including the CSF.
potential MOA of antimicrobials
inhibition of cell wall synthesis, increasing permeability of cell membrane, anti-metabolite action of a drug, inhibition of microbial DNA or RNA synthesis, inhibition of action of microbial ribosomal subunits
ind. of Sulfamethoxazole/ Gantanol
UTIs, otitis media, bronchitis. has largely been replaced by Trimethoprim Sulfa which has a broader spectrum of activity.
Side effects of Sulfamethoxazole/ Gantanol
GI - upset stomach, N/V. H/A, skin rashes, and marked photosensitization
class of Sulfamethoxazole with Trimethoprim/ Bactrim
sulfonamide antibiotic in combination with an additional folic acid inhibitor
MOA of Sulfamethoxazole with Trimethoprim/ Bactrim
interference with folic acid formation at a successive step to sulfonamides
Char. of Sulfamethoxazole with Trimethoprim/ Bactrim
synergistically inhibits two steps in folic acid synthesis
naturally derived antibiotic drug classes
penicillins, cephalosporins, macrolides, tetracyclines, aminoglycosides
sensitivity is determined by several factors, including the ability of the antimicrobial agents to
reach the microorganism, bind to or enter the microorganism, interfere with a vital microbial function, remain chemically intact while acting upon the microorganism
two types of drugs that each affect folic acid production
trimethoprim and sulfonamides
what part of folic acid production do sulfonamides affect
dihydropteroate synthetase
what part of folic acid production does trimethoprim affect
dihydrofolate reductase
indications of Sulfamethoxazole with Trimethoprim/Bactrim
Urinary tract infections, Pneumocystis prophylaxis. Also for MRSA infections either empirically or proven by culture to be sensitive to TMP/ Sulfa.
side effects of Sulfamethoxazole with Trimethoprim/Bactrim
Hypersensitivity is approximately 3x more common than with Sulfamethoxazole alone. Most hypersensitivity reactions involve skin reactions such as rash and photosensitivity. Megaloblastosis, leukopenia, and thrombocytopenia - characteristics of folate deficiency – are all potential adverse effects.
major side effect of Sulfamethoxazole with Trimethoprim/Bactrim
Stevens Johnson syndrome (topical epidermal necrolysis
penicillin typically treats infections caused by
susceptible Gram-positive organisms
what type of antibiotic are penicillins
beta-lactam
class of penicillin G
beta-lactam antibiotic
MOA of penicillin G
Beta lactam component binds to PBPs on bacteria and thereafter inhibits cross linking of components of bacterial cell wall.
indication of Penicillin G
Pen G is not used as frequently now as in the past but can still be effective against many Gram positive cocci such Streptococcus and some gram negatives such as Neisseria.
Char. of Penicillin G (what is often added)
Procaine is often added to IM injections to diminish pain of injection. Procain and Benzathine also prolong the half-life of penicillin.
Side effects of Penicillin G
penicillins have most common severe drug allergy but may not be true allergy response
Amoxicillin/ Amoxil class
Penicillin derivative antibiotic containing a thiazoladine ring, a β lactam ring and side chains.
MOA of Amoxicillin/ Amoxil
Binds to penicillin binding protein and inhibits protein synthesis in the bacterial cell wall.
indications of Amoxicillin/Amoxil
Useful for urinary tract, ENT infections such as Strep throat and otitis media, lower respiratory, skin infections.
side effects of Amoxicillin/Amoxil
penicillins have most common severe drug allergy but may not be true allergy response
what causes resistance to Amoxicillin/Amoxil
Generally due to microorganisms ability to produce B-lactamase and/or modifications of the PBP sites
Distribution of Amoxicillin/Amoxil
distributed widely in all tissues except in the CSF
class of Amoxicillin and clavulanate/Augmentin
penicillin derivative antibiotic containing Amoxil with clavulanic acid added to prevent B lactamase inhibition.
MOA of Amoxicillin and
clavulanate/Augmentin
similar to Amoxil, binding to penicillin binding protein and inhibiting protein synthesis in the bacterial cell wall.
side effects of Amoxicillin and
clavulanate/Augmentin
The most severe cause of antibiotic induced diarrhea is pseudomembranous colitis
interesting thing about dose of Amoxicillin and
clavulanate/Augmentin
two 250 mg Augmentin capsules will give you twice the clavulanate dose of one 500 mg Augmentin capsule.
general action of cephalosporins
disrupt the synthesis of the peptidoglycan layer of bacterial cell walls, resulting in cytolysis and cell death
class of Cephalexin/Keflex
Cephalosporin antibiotic, first generation.
First generation of Cephalosporins start with
Ceph-
advantage of first generation cephalosporin
great gram + coverage but poor gram -
later generation Cephalosporins start with
Cef
advantage of third generation cephalosporin
great gram- coverage but poor gram+ coverage
MOA of Cephalexin/Keflex
Similar to penicillin with inhibition of protein synthesis of the bacterial cell wall via beta lactam activity.
Char. of Cephalexin/Keflex
Drug resistance generally occurs as a result of β-lactamase production or modifications of PBP.
Indications of Cephalexin/Keflex
ENT infections, bronchitis, skin infections. Varies with the generation of cephalosporin. Prophylaxis in surgery. Alternative to penicillins in allergic patients.
Side effects of Cephalexin/Keflex
Similar to penicillin. GI effects such as diarrhea. Yeast overgrowth. Approximately 5%* of penicillin allergic patients will also be allergic to the cephalosporin class of drugs.
Macrolides tend to accumulate within
leukocytes and are therefore actually transported into the site of infection
indication for Erythromycin
Erythromycin is often used to treat respiratory tract infections because it covers typical organisms such as streptococcus and has better coverage of atypical organisms (such as Mycoplasma and Legionella).
It is also used to treat Chlamydia, syphilis, and gonorrhea.
class of Erythromycin
macrolide antibiotic
MOA of Erythromycin
inhibit protein synthesis by binding to 50 S bacterial ribosome
Char. of Erythromycin
Broad spectrum antibiotic that is generally bacteriostatic in low concentrations and bactericidal in high concentrations. May be used in penicillin allergic patients.
Side effects of Erythromycin
GI distress with upset stomach and N/V are very common occurrences with Erythromycin, especially if the drug taken without food. Most tablets are enteric coated in an effort to diminish upset stomach.
class of Azithromycin/ Zithromax
Macrolide antibiotic related to erythromycin, consisting of a many membered lactone ring
MOA of Azithromycin/ Zithromax
inhibit protein synthesis by binding to 50 S bacterial ribosome
Char. of Azithromycin/ Zithromax
Broad spectrum antibiotic that is generally bacteriostatic in low concentrations and bactericidal in high concentrations. Long half life (68 hours).
Indication for Azithromycin/ Zithromax
Ear, nose and throat infections, sinusitis, bronchitis and pneumonia. Atypical infections such as Mycoplasma and Chlamydia infections. Long half-life and easy dosing schedule has made Zithromax one of most commonly used antibiotics.
Side effects of Azithromycin/ Zithromax
Similar to erythromycin but with far less GI distress. Zithromax should still be taken with food to diminish adverse effects of upset stomach, nausea and vomiting. As with all antibiotics, bacterial and yeast overgrowth is possible.
Tetracyclines should not be given concurrently with
calcium supplements or with dairy products as they are chelated by the drug and will markedly diminish drug absorption and bioavailability
Tetracyclines should never be used in
infants and children younger than age 8 or 15 or in pregnant women because they can permanently stain teeth
class of Tetracycline/ Sumycin
Tetracycline antibiotic
MOA of Tetracycline/ Sumycin
inhibits bacterial protein synthesis by interfering with 30 S ribosome. Bacteriostatic rather than bactericidal.
Indications for Tetracycline/ Sumycin
Effective in treating oral and respiratory infections caused by aerobic and anaerobic gram + and gram – organisms, killed by penicillins. Commonly used to treat acne and acne rosacea. Chlamydia. Lyme disease. Rocky Mountain Spotted Fever.
Char. of Tetracycline/ Sumycin
chelates calcium ions. Accumulates in bone and teeth. Avoid taking this class of drugs with dairy products or calcium supplements.
side effects of Tetracycline/ Sumycin
Irreversible staining of teeth. This drug and other tetracycline class drugs must be avoided in infants, children and early adolescents. GI distress. Photosensitivity.
Gentamicin/ Garamycin class
aminoglycoside antibiotic
MOA of Gentamicin/ Garamycin
Binds to 30 S and 50 S ribosomal subunits interfering with protein synthesis. Bactericidal.
Indications of Gentamicin/ Garamycin
Primarily used to treat aerobic gram negative organisms. Useful in treating potentially life threatening infections such as meningitis, endocarditis or sepsis due to gram negative organisms. May also be used to treat Tuberculosis.
Char. of Gentamicin/ Garamycin
No activity as an oral agent. Generally given IV when treating systemic infection. Often used with other antibiotics because of narrow spectrum of activity. Severe adverse effect profile. Used topically in the treatment of skin infections or infections of the eye.
Side effects of Gentamicin/ Garamycin
Potentially nephrotoxic and ototoxic. These effects may be irreversible.
mechanism of Quinolones
inhibit bacterial DNA gyrase, thereby inhibiting DNA replication and transcription
main side effect of Quinolones
tendon damage or spontaneous tendon rupture…especially when concurrently using systemic corticosteroid such as prednisone
class of Ciprofloxacin/Ciproxin
Quinolone antibiotic (synthetic)
MOA of Ciprofloxacin/Ciproxin
Inhibits DNA gyrase, an enzyme responsible for properly uncoiling DNA during transcription.
Quinolones are no longer indicated for
STI’s
Indications for Ciprofloxacin/Ciproxin
Excellent coverage of many gram negative organisms and very good coverage for many gram positive organisms. Urinary tract, ENT, upper and lower respiratory tract infections. Anthrax - made “famous” (or infamous) by post 9/11 anthrax threats.
1st generation Quinolones have good coverage with
Gram - bacteria
2nd generation Quinolones have good coverage with
Gram + bacteria
Who should Ciprofloxacin/Ciproxin be avoided in
The Quinolones chelate calcium and can be deposited in cartilage, thus the use of oral or parenteral forms should be avoided in all children and infants and all pregnant and lactating females.
Side effects of Ciprofloxacin/Ciproxin
Not for use in children or pregnant females as it is taken up by bone and cartilage. Associated with increased risk for tendon injury (esp. Achilles tendon injury) in adults taking the drug. N/V, headache, insomnia, particularly in coffee drinkers. Ciproxin reduces the metabolic breakdown of caffeine, thus prolonging the effects.
class of Metronidazole/ Flagyl
Imidazole class of antibiotics
MOA of Metronidazole/ Flagyl
activated intermediates of the drug bind to DNA and inhibit further nucleic acid synthesis
Indications for Metronidazole/Flagyl
Vaginitis due to Trichomonas vaginalis (protozoal) infection in both symptomatic patients as well as their asymptomatic sexual contacts and due to bacterial Gardnerella vaginal infection in symptomatic patients.
As part of a multi-drug regimen directed at eradication of Helicobacter pylori in peptic ulcer disease.
Metronidazole is a ___-drug
pro-drug by virtue of the fact that the therapeutic action of the drug occurs after the drug has been taken up by sensitive organisms such as anaerobic gram negative bacteria or Protozoa.
Side effects of Metronidazole/Flagyl
Common adverse drug reactions associated with oral Metronidazole therapy include: upset stomach, nausea, vomiting, and diarrhea. The sensation of a metallic taste in the mouth is another common complaint. Headaches. Thrush.
If you drink alcohol while taking Metronidazole/Flagy, it can result in l
Disulfiram-like (aka Antabuse-like) reaction with nausea, vomiting, flushing, and tachycardia.
How does Metronidazole interrupt the breakdown of alcohol
blocks the enzyme acetaldehyde dehydrogenase….blood alcohol will be far higher than usual so alcohol needs to be avoided till 24 hours after completion of treatment
class of Nitrofurantoin/ Macrobid
Nitrofuran antibacterial agents
indication of Nitrofurantoin/ Macrobid
lower urinary tract infections
What drug can cover both a parasite (protozoa) and bacteria
Metronidazole/Flagy
MOA of Nitrofurantoin/ Macrobid
disrupts both DNA and RNA of bacteria which are sensitive to the drug.
Char. of Nitrofurantoin/ Macrobid
concentrated in the urine. Indicated for lower UTI’s but no for pyelonephritis. Considered safe for use in pregnancy prior to 38 wks of gestation. Resistance to other antibiotics has led to increased interest in Nitrofurantoin.
side effects of Nitrofurantoin/ Macrobid
The most common side effects with Nitrofurantoin are nausea, vomiting, and diarrhea; less common reactions include fever and chills. Rare adverse effects include pulmonary fibrosis and drug-induced autoimmune hepatitis.
Nitrofurantoin/ Macrobid is not recommended to us for
pyelonephritis
class of Clindamycin/Cleocin
lincosamide antibiotic
MOA of Clindamycin/Cleocin
binds to 50 S ribosomal subunits of bacteria which acts to inhibit protein synthesis
common side effects of Clindamycin/Cleocin
GI upset, nausea, vomiting or diarrhea. Skin rashes, oral thrush and yeast vaginitis may occur. Pseudomembranous colitis from C. difficile overgrowth can occur.
class of Vancomycin/ Vancocin
glycopeptide antibiotic
indication of Vancomycin/ Vancocin
Infections by Gram-positive bacteria which are unresponsive to other less toxic antibiotics. These are often severe or even life threatening infections.
MOA of Vancomycin/ Vancocin
Inhibits synthesis of bacterial cell wall phospholipids as well as inhibition of peptidoglycan polymerization at a site separate from the penicillin binding proteins sites utilized by beta lactam antibiotics.
Vancomycin is used in the prophylaxis and treatment of
severe infections caused by Gram-positive bacteria…traditionally used as a last resort
Are Clindamycin and Erythromycin related drugs?
No.
what is the only indication for oral adminstration of Vancomycin
treatment of pseudomembranous colitis that is unresponsive to Metronidazole treatment or in cases in which there is a relapse of pseudomembranous colitis.
side effects of Vancomycin/Vancocin
Vancomycin must be administered in a dilute solution over at least 60 minutes. This is to reduce the high incidence of pain at the infusion site and thrombophlebitis that is more likely to occur when the drug is more concentrated or when the delivery of the drug is too rapid.
Go-to-drug for endocarditis and mrsa
Vancomycin/Vancocin
associated complication with Vancomycin
associated with a complication reffered to as Red Man Syndrome or Red Neck Syndrome…characterized by intense facial flushing, diffuse erythema, and possible bullae formation and desquamation
drug typically used to treat Mycobacterium infections, including tuberculosis and Hansen’s disease
Rifampicin/Rifampin
Rifampicin is used as prophylactic therapy against
Neisseria meningitidis…also has role in treatment of MRSA
MOA of Rifampicin/Rifampin
Rifampicin inhibits DNA-dependent RNA polymerase in bacterial cells thus preventing transcription to RNA and subsequent translation to proteins.
Common side effects of Rifampicin
fever, GI disturbances and rash
One of the most serious side effects of Rifampicin
hepatotoxicity and patients receiving Rifampicin should undergo baseline and frequent liver function tests to detect any signs of early liver damage.
Rifaximin/Xifaxan has poor
bioavailability, meaning that very little of the drug will be absorbed into the blood stream when taken orally.
Indication for Rifaximin/Xifaxan
treatment of traveler’s diarrhea, irritable bowel syndrome, small intestine overgrowth syndrome and hepatic encephalopathy.
What does Rifampicin/Rifampin do to urine and tears?
turns them orange
acceptable first line empiric choices for treating cellulitis
Clindamycin, a Cephalosporin or a Fluoroquinolone
recommended monotherapy for presumed or confirmed cutaneous CA-MRSA infection
TMP-Sulfa DS
drug of choice for SIBO
Rifaximin/Xifaxan
Mupirocin/Bactroban is originally isolated from
Pseudomonas fluorescens
MOA of Mupirocin/Bactroban
selective binding to bacterial isoleucyl-tRNA synthetase, which halts the incorporation of isoleucine into bacterial proteins.
How is Mupirocin/Bactroban used
TOPICALLY and is primarily effective against Gram +
Indication for Mupirocin/Bactroban
topical treatment for bacterial skin infections, such as impetigo, boils, and folliculitis. Mupirocin is also indicated for open wounds at risk for infection or after incision and drainage procedures of skin abscesses. Great success v. CA-MRSA too.
Which drug has supplanted all other drugs for treating impetigo?
Mupirocin/Bactroban
MOA of Bacitracin
interferes with the transfer of cell wall precursors from the bacterial cell membrane to the cell wall.
What does Bacitracin target
Gram + bacteria
Bacitracin is effective in treating
superficial infections of the skin and the eye.
Class of Neomycin
aminoglycoside antibiotics
How does aminoglycosides work
binding to the bacterial 30S ribosomal subunit, leaving the bacterium unable to synthesize proteins vital to its growth.
Neomycin and other members of the aminoglycoside class are extremely effective in killing
Gram - bacteria
Polymyxin B class
Poylmyxin group antibiotic
MOA of Polymycin B
bind to the bacterial cell membrane and alters its structure, making it more permeable. Increased cell wall permeability results in marked water uptake by the bacterial cell and subsequent cell death.
Polymycin is effective in treating
Gram - infections
what drug has a risk profile that is too great to be used for an infection like Strep throat
aminoglycosides
topical antibiotic that combines Bacitracin and Polymycin
Polysporin
Neosporin contains
contains Bacitracin along with Neomycin and Polymyxin B, (hence, the term, ‘triple antibiotic’ ointment)
topical antibiotics for superficial wounds
Polysporin and Neosporin
Most common side effects of Polysporin/Neosporin
most commonly experienced side effect from the use of either topical Polysporin or Neosporin is skin irritation that may appear as redness, swelling, or a burning sensation. Hives may develop both at the site of application and elsewhere on the body. The most severe form of allergic response, anaphylaxis, can occur with symptoms such as difficulty swallowing and breathing.