exam 2 Flashcards
1) B2 adrenergic agonists (sympathomimetics)
2) Antimuscarinics/Anticholinergics
Relax airway smooth muscle (bronchodilators)
asthma RELIEVERS
o 1) Glucocorticoids
o 2) Leukotriene Modifiers
o 3) Cromones
o 4) Biologic Therapies
Decrease underlying inflammation
controllers
Methylxanthines (Theophylline)
Both Relievers and Controllers
MOA
B2 receptor couples to a “Gs” protein activation of adenylyl cyclase increased cAMP increased PKA increased bronchodilation
B2 Adrenergic Agonists (Sympathomimetics)
Major effector tissues: smooth muscle including bronchiolar, liver, skeletal muscle
Major functions: relaxes/dilates smooth muscle + gluconeogenesis + glycogenolysis
B2 Adrenergic Agonists (Sympathomimetics)
- Terbutaline: SC and oral
- Albuterol: oral and nebulizer
Short Acting Beta2 Agonists (SABAs)
- Formoterol* (this has rapid onset for inhaler, can be used as rescue inhaler)
- Salmeterol
- Indacaterol (only used for COPD)
all of these MUST be combined with glucocorticoid
Long Acting Beta2 Agonists (LABAs)
MOA:
Normally: Ach stimulates M3 couple with Gq increases IP3 intracellular calcium calmodulin binding myosin and actin contract bronchoconstriction + increased pulmonary secretions
^^ _________________/__________________ block this!
Anticholinergics/antimuscarinics
Ipratropium (Atrovent)
Also used for rhinorrhea
Short Acting Muscarinic Antagonists (SAMAs)
- Tiotropium (Spiriva): once daily
- Glycopyrrolate: once daily
Long-Acting Muscarinic Antagonists (LAMAs)
B2 agonists > Antimuscarinics: _________
B2 agonists = Antimuscarinics: ______
B2 agonists > Antimuscarinics: ASTHMA
B2 agonists = Antimuscarinics: COPD
MOA
Inflammatory stimuli increase in inflammatory proteins
________________ binds to intracellular receptors goes to cell nucleus decreases expression of genes encoding for inflammatory proteins
Glucocorticoids
Inhalers
Beclomethasone (QVAR)
Budesonide (Pulmicort)
Fluticasone (Flovent)
Oral/IV
Hydrocortisone: short acting (½ life: <12 hours)
Prednisone: intermediate acting (½ life: 12-36 hours)
Methylprednisone: intermediate acting (½ life: >48 hours)
Dexamethasone: long acting (½ life: >48 hours)
all have “SON” in them
glucocorticoids
________________ _____________: existing in the cell membrane
Types
1) CysLT1 Antagonists
* Not as effective as glucocorticoids
2) 5-Lipoxygenase Inhibitor
Leukotriene Modifiers
Mild persistent asthma
Exercise induced bronchospasm/asthma
Allergic rhinitis
May reduce the need for glucocorticoids in select patients
CysLT1 Antagonists
Montelukast (Singulair)
What drug class decreases both COX (prostaglandins) + lipoxygenase (leukotrienes) pathways*
Glucocorticoids
NSAIDS will block COX, which will shunt over to the lipoxygenase/leukotriene pathway (this will cause “aspirin exacerbated respiratory disease”; more bronchoconstriction
MOA
Elevated IgE antibodies and sensitivity to perennial allergens (pollen)
Anti-IgE Therapy: anti-IgE antibody binds to circulating IgE and INHIBITS its interaction with receptors on mast cells and other effector cells
biologic therapies
(OmalizuMAB)
MOA
Increase in cAMP = increase in bronchodilation
Increases cAMP by:
1) Inhibiting phosphodiesterase
AND
2) Blocks adenosine receptor, thereby, INCREASING adenylyl cyclase
AND
Enhances histone deacetylation, decreasing inflammation
Methylxanthines (Theophylline)
Both a Reliever and a Controller
Narrow therapeutic index!
Large variation in ½ life (due to it being metabolized in the liver)
o Very similar to caffeine
o CNS excitation (can cause seizures)
o Weak diuretic
o CV stimulation (chronotropy, inotropy, arrhythmias)
o N/V
theophylline
Inducers = ______________ blood levels of theophylline
DECREASED
Inhibitors = ______________ blood levels of theophylline (toxicity risk)
INCREASED
major triggers of asthma attack (4)
beta adrenergic receptor antagonists
aspirin/NSAIDS
histamine (morphine, demerol, Sch, atracurium)
preservatives
______________ is a reliever + controller of asthma but is 2nd line therapy due to risk of AEs
Theophylline
_______________________ is used in select patients to decrease need or dose of glucocorticoid inhaler
Montelukast (Singular)
COPD best treatment option
Long-Acting Muscarinic Antagonists (LAMAs)
MOA
o Mild mucolytic activity via inhalation or intratracheal instillation
o Thins secretions, reduces risk of exacerbations
N-acetylcysteine
Nasocort
Flonase
Intranasal glucocorticoids
used for allergic rhinitis
Chlorpheniramine
Hydroxyzine (Vistaril)
1st gen “sedating” antihistamines
Impaired cognition (caution with elderly) *
Antimuscarinic effects (opposite of DUMBBELSS)
1st gen “sedating” antihistamines
MOA
Primarily stimulates alpha adrenergic (A1) receptors, causing vasoconstriction
Some also release NE
decongestants (sympathomimetics)
- Direct + indirect (NE release): mixed acting
- Can create meth, that is why you show your license
Pseudoephedrine
- Direct acting only
- Not as effective
Phenylephrine
____________ route is preferred for decongestants (does not go systemic) however, overuse can cause rebound vasodilation
topical (limit to < 5 days!)
- Ipratropium (Atrovent)
short acting muscarinic agent (SAMA)
- Tiotropium (Spiriva): once daily
- Glycopyrrolate: once daily
long acting muscarinic agent (LAMA)
best treatment for COPD!
the only methylxanthine
theophylline
select drug triggers of asthma attack
morphine
meperidine
atracurium
Sch
you notice the presence of oral candidiasis in a patient with asthma. Which of the following is most likely the cause?
fluticaSONe (flovent)
more common with AEROSOL use!
(flovent, pulmicort, QVAR)
man with history of BPH, asthma, and allergic rhinitis has developed urinary retention following surgery. Which drug contributed to the urinary retention?
Diphenhydramine (Benadryl)
antimuscarinic! (trop)
this is because it is oral! it is NOT TIOTROPIUM because that is an inhaler
Ach and monoamines come from
biogenic amines
serotonin and catecholamines (NE, Epi, Dopamine) come from
monoamines
3 ways of termination of NT activity
reuptake
enzymatic degradation
diffusion
Drugs can block everything except diffusion
BLOCKING muscarinics/cholinergic (aka antimuscarinics) receptors causes:
opposite of DUMBBELSS
* Hypomania
* Constipation
* Urinary retention (especially BPH)
* Blurred vision, glaucoma
* Bronchodilation
* Tachycardia
* Dry mouth/eyes
* Overheating/hypohidrosis
Altered cognition
BLOCKING dopaminergic receptors causes*
there is LESS dopamine
Extrapyramidal symptoms (parkinsonian-like)
Prolactin release (lactation, impotence)
BLOCKING histaminergic receptors causes*
sedation
impaired cognition
BLOCKING alpha1 adrenergic receptors causes*
orthostatic hypotension
reflex tachycardia
major antidepressant drug targets (4)
NET
SERT
MAO
DAT
antidepressant drug classes (6)*
Most Commonly Used/Frontline Therapy:
1) SSRIs: increases serotonin
2) SNRIs: increases serotonin + NE
3) Atypical antidepressants: increases NE and dopamine
4) Serotonin modulator
Least Commonly Used/Secondary Therapy:
1) TCAs: tricyclic antidepressants: increases serotonin + NE + additional actions
2) MAOIs: monoamine oxidase inhibitors
MOA
Blockage/inhibition of serotonin-5HT reuptake transporter (SERT) only
NO blockage of H1, Ach, or NE!
SSRIs
o Sertraline (Zoloft)
o Fluvoxamine (Luvox)
o Fluoxetine (taken once a week)
o Paroxetine
o Citalopram
o Escitalopram
SSRIs
o Serotonin Syndrome
o Hyponatremia
o Withdrawal Syndrome
o Bleeding
SSRIs
Inhibition of CYP2D6 (codeine, hydrocodone effectiveness would be decreased)
Fluvoxamine
Fluoxetine
Bupropion
MOA
Increases serotonin + NE activity; blocks SERT + NET activity
NET blockade: treats multiple pain syndromes
NO blockage of H1, Ach, or muscarinic receptors!
SNRIs
o Effexor
o Cymbalta
Often used for fibromyalgia and pain associated with neuropathy*
SNRIs
o Increase in BP* (this is unique to _______)
with Effexor only !
o Serotonin Syndrome
o Hyponatremia
o Bleeding
SNRIs
MOA
o Increase NE + dopamine (DA) activity; blocks NET and DAT
o Noncompetitive antagonist/blocker of nicotinic receptors
atypical antidepressants
Buproprion
bupropion
atypical antidepressant
Use:
Individuals who do not want any sexual dysfunction*
o Depression
o Smoking cessation
bupropion; atypical antidepressant
MOA
o Low doses: hypnotic/sedation/sleep aid
o High doses: increases serotonin activity; blocks serotonin (5HT2)
Blocks H1, and adrenergic receptors
serotonin modulator (trazadone)
Hypnotic/sedation/sleep aid
serotonin modulator (trazadone)
MOA:
MAOIs will block MAO enzyme, leading to _______________ of monoamines:
MAOI-A
MAOI-B
MAOIs
ACTIVATION of monoamines
MAOI-A: an increase in: ____________________
MAOI-B: an increase in: _____________
MAOI-A: tyramine + NE +serotonin
MAOI-B: dopamine only
Only Refractory/Severe/Atypical Depression due to adverse effects*
Exception: Selegiline: patch/SQ is less likely to cause adverse effects
MAOIs (nonselective, irreversible)
what drugs can cause
Life-threatening HYPERtensive crisis due to interactions with foods + drugs
Orthostatic hypotension (normal doses)
MAOIs
MOA
Blocks NE + serotonin (5HT) reuptake into presynaptic nerve terminal, increased NT activity at postsynaptic neuron and increased subsequent neurological events
and blocks H1, A1, muscarinic receptors
TCAs
o AmiTRIptyline
o NorTRIptyline
TCAs
Life threatening arrythmias is main reason not to use them! (QT prolongation)
Cardiotoxicity, caution with other cardiac depressive drugs
TCAs
Hyperreflexia, clonus (of the muscles), agitation, AMS, diaphoresis, autonomic instability, fever, death
serotonin syndrome
4 opioids that can cause serotonin syndrome
tramadol
meperidine (demerol)
methadone
fentanyl
drug classes that can cause serotonin syndrome (4)
Direct 5HT Stimulators: triptans (sumatriptan)
SSRIs, SNRIs, TCAs
Opioids: Tramadol, Meperidine, Methadone, Fentanyl
Zofran
what is the direct serotonin stimulator
sumatriptan
only SSRI that can be used for OCD
fluvoxamine
lithium
bipolar disorder
chlorpromazine
promethazine
haldol
droperidol
phenergan* (actually an antiemetic)
conventional (1st gen) antipsychotics
risperidone
ziprasidone (geodon)
seroquel
zyprexa
abilify (partial dopamine agonist)
atypical (2nd gen) antipsychotics
dantrolen
bromocriptine (parlodel)
benzos
TREATMENT for neuroleptic malignant syndrome
benztropine (cogentin)
benadryl
TREATMENT for antipsychotic acute dystonia
o Narrow therapeutic index
o Renal excretion
contraindications to ___________ use:
o Hyponatremia (dehydration, diarrhea, diuretics): can cause lithium levels to increase
o Renal impairment
o Pregnancy and lactation (teratogenic)
lithium
Monitor thyroid levels, __________ level, fluid, and electrolytes (hyponatremia)!
may prolong NMBs
lithium
positive symptoms, high dopamine =
1st generation OR 2nd generation
Negative symptoms + cognitive symptoms = low dopamine =
2nd generation
o Schizophrenia
o Delusional disorders
o Bipolar disorder
o Psychoses (depressive, drug-induced reaction)
o Drug-resistant depression
Other Uses
ANTIEMETICS
Tourette’s syndrome
Huntington’s chorea
Antipsychotics
HIGHER risk of:
sedation
hypotension
antimuscarinic effects
Chlorpromazine
LOW potency antipsychotics
phenergen
medium potency antipsychotic/antiemetic
LOWER risk of sedation
HIGHER risk of extrapyramidal symptoms
haldol
droperidol
With LOW levels of synaptic DA: increases activity
With HIGH levels of synaptic DA: decreases activity
Abilify
DA system stabilizer/2nd gen
Least amount of side effects of all antipsychotics
abilify (DA system stabilizer)
severe muscle spasm including torticollis, oculogyric crisis, trismus
Acute dystonic reaction
treatment for acute dystonic reaction
antimuscarinic
Benadryl, Benztropine
Lower risk of extrapyramidal symptoms
2nd Generation/Atypicals
Block A1 adrenergic, muscarinic, H1 receptors (leads to adverse effects discussed earlier)
Decreased seizure threshold (increased risk of seizures)
Prolonged QT interval/arrythmias
Neuroleptic malignant syndrome
antipsychotics
“lead-pipe” muscle rigidity, dysautonomia, AMS, fever
cause: blocking dopamine receptors
neuroleptic malignant syndrome
what drugs BLOCK dopamine, leading to a DECREASE in dopamine
1st generation antipsychotics (most common)
2nd generation antipsychotics
DA2 antagonist/blockers: antiemetics (Droperidol)
prokinetics (REGLAN)
what drugs INCREASE dopamine
drugs used for parkinsons
Benzodiazepines
Dantrolene
Bromocriptine (dry up lactation)
treatment for neuroleptic malignant syndrome
causes of prolonged QT interval (6)
TCAs (high doses)
Antipsychotics/antiemetics
High risk: Haldol (especially IV), Droperidol, Geodon
Methadone
Zofran
Perioperative Drugs
* Sevoflurane, Desflurane, Isoflurane
* Amiodarone
A patient that receives promethazine (Phenergan) for post-operative nausea suddenly develops a sustained, involuntary muscle contraction involving the neck. Which of the following would most likely be used to treat this reaction?
Benadryl
man with a history of bipolar disorder is scheduled for surgery. He is currently treated with lithium. If lithium is continued perioperatively, which of the following drugs is most likely to increase his lithium serum concentration?
Ibuprofen
man with a history of BPH develops urinary retention following surgery. Which of the following home medications most likely contributed to his condition?
Amitriptyline
which class of antidepressants is least likely to triggers symptoms of serotonin syndrome
atypical antidepressants (NE + dopamine)
can cause hyponatremia
SSRIs and SNRIs
MOA
o Partial serotonin 5HT-1A agonist (increases serotonin)
used for anxiety (no sedative effects)
Buspirone
o Muscle relaxant
o Anticonvulsant
benzos
Midazolam/Versed: _______-acting
Lorazepam/Ativan: ____________-acting
No metabolite
Diazepam/Valium: long-acting
versed=short
ativan=intermediate (DRUG OF CHOICE, less lipophilic)
Insomnia (appear to induce more normal sleep patterns; however, less restful)
anxiolytic
sedative-hypnotic
z compounds
o Zolpidem (Ambien)
o Zaleplon (Sonata)
z compounds
Hepatotoxicity
Pancreatitis
Exfoliative dermatitis (Steven’s Johnson Syndrome, Toxic Epidermal Necrolysis)
Blood dyscrasias (agranulocytosis, aplastic anemia, etc.)
idiosyncratic reactions
epileptic drugs
Phenobarbital, phenytoin, carbamazepine, valproic
Phenytoin (Dilantin)
Carbamazepine (Tegretol)
sodium channel targets (anti-epileptics)
All forms of epilepsy (except absence seizures)
Narrow therapeutic index + variable metabolism: monitor levels
Induces multiple CYPs
Many drug interactions (>100)
Metabolized by CYP2C9/19
NON-linear kinetics
phenytoin
Asian ancestry with polymorphism increased risk
monitor blood count
carbamazepine
o Benzodiazepines
o Barbiturates (Phenobarbital)
chloride channel (anti-epileptics)
calcium channel target
Block calcium influx channels
+ ___________ ___ _________
Decrease NT release
Gabapentinoids:
Gabapentin and Pregabalin/Lyrica
calcium channel targets (anti-epileptics)
Uses
* Neuropathic pain
* Fibromyalgia
gabapentinoids
fibromyalgia=lyrica
Valproate Sodium/Valproic Acid (Divalproex)
Topamax
Lamictal
mixed channel targets
the only inhibitor of multiple CYPs
for anti-epileptics
toxicity risk for other drugs!
hepatotoxicity (monitor LFTs!)
Valproate Sodium/Valproic Acid (Divalproex)
Uses
Seizures
Bipolar disorder
Migraine prophylaxis
Valproate Sodium/Valproic Acid (Divalproex)
Uses
Seizures
Migraine prophylaxis
Weight loss programs
topamax
Antiepileptic therapy + antiparkinson’s therapy is usually _____________ perioperatively
continued
What is the most teratogenic (avoid pregnant patients) AED?
Valproate Acid
What AED drugs are potent inducers?
Phenytoin, phenobarbital, carbamazepine
Adverse Effects
o N/V
o Dyskinesias (tics, grimacing)
o CV: postural hypotension, arrhythmias
o Psychosis (may treat with atypical antipsychotic)
Indications/Uses
o Advanced PD and >70 years of age
levodopa (increases synthesis of dopamine)
o Mild to moderate PD
o Restless leg syndrome
dopamine agonists
o ROPinirole
o PramiPEXole
(BOXING)
MOA
o Inhibits peripheral COMT
Indications/Uses
o _____________ + Levodopa + Carbidopa = improved motor fluctuations
o Never used alone
Entacapone
o Selegiline
o Rasagiline
MAOI-B
Mao’s styling with GEL
o Benztropine (Cogentin)
o Trihexyphenidyl (Artane)
MILD parkinson’s, 1st line therapy
Antimuscarinics/Anticholinergics (Centrally-Acting)
2 drug classes for alzheimers
Centrally acting acetylcholinesterase inhibitors (AchE-I)
NMDA type glutamate (excitatory) antagonists
most effective treatment for alzheimers
NMDA type glutamate antagonists
(memantine)
o GALantamine
o DONepezil
o RIVastigmine
Acetylcholinesterase Inhibitors (AchE-I)
treatment for alzheimers:
AchE-I works to ___________ ACh
INCREASE ACh (this is what we want!)
can have dumbelss effect
increases DA release
Antiparkinson’s drug
amantadine
high therapuetic index = _________ toxic for the patient
less toxic
what are the top 2 safest antibiotic classes
penicillins + cephalosporins
More clinically relevant!
Determined in vitro (the lab)
Drug + microbe specific
minimum inhibitory concentration (MIC)
The MIC is higher and cannot be achieved at therapeutic or non-toxic doses
resistant
Test tubes have different concentrations of the antibiotic, MIC has been determined
serial dilution susceptibility testing
antibiotics are added to a plate after an organism is streaked onto the agar
disk diffusion (kirby-bauer method)
Trends in antibacterial resistance for an institution*
Aids in selecting EMPIRIC treatment, monitor resistance trends over time
antibiogram
Primarily acts on the cell wall, cell membrane and/or DNA synthesis:
bacteri_______
CIDAL
Primarily acts through inhibition of protein synthesis; works with host/patient’s defenses:
bacteri_______
STATIC
true or false:
bacteriCIDAL is overall the best option for all patients (especially those immunocompromised)
true
name the 5 antibiotics that are bacterioSTATIC
Bactrim
Tetracyclines
Macrolides
Clindamycin
Linezolid
“Banking The Money, Can’t Love”
how long the concentration is maintained above MIC
TIME dependent
increases with increasing concentration (AUC:MIC)
CONCENTRATION dependent
TIME dependent
examples (4)
- Beta-lactams
- Vancomycin
- Linezolid
- Clindamycin
“Beta’s Can’t Love Vanc”
CONCENTRATION dependent
examples (4)
Aminoglycosides
Fluroquinolones
Daptomycin
Metronidazole
“AF, Dab Men”
3 post antibiotic effects*
Aminoglycosides
Fluoroquinolones
Fidaxomicin
“AFF”
How are NAM + NAG “linked” together?
Glycosyltransferase (GT) enzyme
How are the murein chains cross-linked to one another, removing the terminal d-alanine?
Transpeptidases TP)/Penicillin Binding Proteins (PBP)
antibiotic MOA:
bind covalently to transpeptidase/PBP and prevent cross-linking (NO effect on the murein chain)*
Beta-lactams
antibiotic MOA:
binds to d-alanine, prevents cross-linking + polymerization (the making of the NAM and NAG chain)
(NO effect on the enzyme)*
vancomycin
4 major subclasses of beta-lactams
penicillins
carbapenems
cephalosporins
monobactams
Hydro________ agents can penetrate the GN via membrane pores
philic
(phobic can still do it, just lower ability, they canNOT penetrate pores)
beta-lactamases:
inactivate penicillins + cephalosporins + monobactams
extended-spectrum b-lactamases (ESBL)
beta-lactamases:
inactivate all B-lactams + inactivate B-lactamase inhibitors
Carbapenemases
beta-lactamase inhibitors end in
____________bactam
what are the 3 major differences between subclasses
1) pH (gastric acidity) + oral bioavailability
2) Porins/penetration of GN
3) Stabilize liability by beta lactamases
4 types of penicillins
natural: pen G + V
anti-staph: NOD
aminopenicillins: amoxicillin, ampicillin
anti-psuedomonal: zosyn
true or false
NO PENICILLINS cover MRSA or ATYPICAL bacteria
true
what drug is IM ONLY
procaine or benzathine (from pen G)
which penicillins are the most RESISTANT to b-lactamases
anti-staph penicillins
which class of penicillins are best for bile elimination
anti-staph penicillins
Nafcillin
Oxacillin
Dicloxacillin
which penicillin is good for psuedomonas
zosyn
increased CNS penetration in penicillins if:
1) If meninges inflamed
2) High doses
3) Reduced renal elimination
4) More frequent doses
most important thing to determine cross reactivity
if the side chain (R-group) is not similar
which cephalosporin is NOT renally eliminated
ceftriaxone
which 10 drugs cover pseudomonas
- Zosyn (penicillin)
- Cefepime, Ceftazidime (cephalosporins)
- Doripenem, Imipenem, Meropenem
- Aztreonam (monobactam)
Polymyxins B + E (not a b-lactam)
Ciprofloxacin and Levofloxacin (fluroquinolones, NOT b-lactams)
What is the only B-LACTAM that covers MRSA?
Ceftaroline “think of Caroline from work”
What is the best cephalosporin for anaerobes?
Cefotetan
which cephalosporins barely cover GN
cefazolin (ancef)
cephalexin
which cephalosporin is contraindicated in neonates due to biliary sludging (interacts with calcium containing products)
ceftriaxone
which b-lactam has the broadest coverage (GP, GN, beta-lactamases, ANaerobes)
carbapenems
what is the only monobactam, and what is it good for
aztreonam
aerobic GN (pseudomonas), cystic fibrosis
do any b-lactams cover atypical bacteria
no
Blocks 1st step in bacterial cell wall synthesis by inhibiting the enzyme “UDP-N-acetylglucosamine enolpyruvyl transferase” (MurA), inhibiting the formation of N-acetylmuramic acid (NAM)
o Mainly for uncomplicated UTIs
fosfomycin
drug of choice for MRSA and C diff (and some VRE)
vancomycin
MOA
1) Same as Vancomycin +
2) Destabilizes/disrupts the inner cell membrane
lipoglycopeptides (vancomycin derivatives)
telaVANCIN, oritaVANCIN, dalbaVANCIN
which lipoglycopeptide does NOT effect coagulation tests
dalbavancin
lipoglycopeptides target what
GP bacteria (MRSA), GP ANaerobes
MOA
1) Causes rapid depolarization of bacterial cell membrane
and
2) Affects synthesis of DNA, RNA & protein synthesis
daptomycin
which drug causes
Myopathy/rhabdomyolysis*
Monitor creatine kinase levels
Additive/increased risk when used with statins
good for MRSA + VRE + some GP anaerobes
daptomycin
MOA
Bind to lipopolysaccharides in the membrane of GN bacteria
and
Detergent-like effect on the membrane
Causes cell lysis
polymyxin B + E
(think, “detergent MYXes”)
very old antibiotic
good for MDROs, GN bacteria, cystic fibrosis (pseudomonas)
polymyxin B + E
Which 3 drugs can affect coagulation tests?
- Telavancin, Oritavancin (lipoglycopeptide)
- Daptomycin (lipopeptide)
5 drug classes for antibiotics that target PROTEIN synthesis
1) macrolides
2) aminoglycosides
3) clindamycin
4) linezolid
5) tetracyclines
MOA
o Binds to the 50s ribosomal subunit near the peptidyl transferase center
o Blocks the polypeptide exit tunnel and prevents peptide chain elongation
2 classes!
macrolides (ACE) + clindamycin
azithromycin
clarithromycin
erythromycin
what are 2 antibiotics that are cyp3a4 inhibitors
clarithromycin
erythromycin
what 3 classes cover atypical bacteria
macrolides
tetracyclines
fluroquinolones
which macrolide is the best option, great for mycobacterium (MAC) in HIV
azithromycin
which macrolide stimulates gut motility the most, is cheap, needs frequent dosing
erythromycin
alters the macrolide ITSELF
esterases
alters the methylate binding site on the RIBOSOME
methylases
Highest risk of c-diff super infections! Boxed warning*
clindamycin
double disk diffusion test compares what 2 antibiotics
clindamycin and erythromycin
MOA
o Binds to 50s subunit blocking formation of the initiation complex (ribosomal complex) with the 30s
linezolid
what are the 4 side effects of linezolid
o Bone marrow suppression
o HYPOglycemia
o Mitochondrial dysfunction (peripheral + optic neuropathy, lactic acidosis)
o Reversible MAO inhibitor (MAOI)
which antibiotic can lead to serotonin syndrome*
linezolid
MOA
Irreversibly bind to 30s subunit to block the initiation complex
and
Causes misreading of mRNA
and
Premature termination of protein synthesis
and
“Garbage” protein chain; causes cell lysis
aminoglycosides
6 examples of aminoglycosides
amikacin
gentamicin
tobramycin
streptomycin
plazomicin
neomycin
ototoxicity, nephrotoxicity*, prolongs NMB, teratogenic
use infrequent, high doses
aminoglycosides
MOA
o Reversibly bind to the 30s ribosomal subunit, prevents “tRNA” binding
Tetracyclines
doxycycline (more common)
minocycline
tetracyclines
true or false
tetracyclines are bile elimination
true
Oral: epigastric pain, N/V, & anorexia
MUST sit upright with a full glass of water, wait at least 10-15 minutes
o Photosensitivity reactions
o Suppresses bone growth related to calcium; permanently discolors teeth (NO CHILDREN)
doxycycline (tetracycline)
what are the 2 drug classes that target NUCLEIC ACID synthesis
1) fluroquinolones
2) metronidazole (flagyl)
enzyme that:
RELAXES bacteria DNA
and
GN
dna gyrase
enzyme that:
UNLINKS/DECATENATION
and
GP
topoisomerase IV
what is the only fluroquinolone that is NOT renally eliminated
moxifloxacin
o Tendon inflammation or rupture!
o Neurotoxicity
o Photosensitivity
Chelation
o Hyper/hypoglycemia
o Aortic aneurysm + dissection
o Hepatotoxicity, crystalluria
o Exacerbation of muscle weakness in Myasthenia gravis
o Joints: pain, stiffness
o QT prolongation
fluroquinolones
MOA
o Nitro group reduced by bacterial ferredoxin reductase
o Activated radical binds to DNA, causes strand breaks
metronidazole (flagyl)
ANaerobic GN + ANaerobic GP
GI parasites
Intra-abdominal/colorectal surgeries
metronidazole (flagyl)
what 3 things are affected by alcohol
disulfiram
cefotetan
metronidazole
MOA
o Inhibits bacterial RNA polymerase + prevents protein synthesis
used for Cdiff
post antibiotic effect
fidaxomicin
MOA
o Metabolized by bacteria to reactive metabolites that disrupt ribosomes
o Prevents protein synthesis, DNA, and citric acid cycle
o Uncomplicated UTIs
Nitrofurantoin
MOA
Inhibits bacterial FOLATE synthesis
and
Affects DNA, RNA, and protein synthesis
bactrim
o Staph
o Community only acquired MRSA
o Strep
o Opportunistic HIV infections: Pneumocystis and Toxoplasmosis*
bactrim
Last 2 months of pregnancy (teratogenic), breastfeeding and newborns
Kernicterus risk: bilirubin crossing the BBB, causing brain damage*
bactrim
best drug for appendectomy
cefazolin (ancef) + metronidazole
or
cefotetan
or
cefoxitin
best drug for hernia repair
cefazolin (ancef)
best drug for
total joint replacement
or
breast cancer procedures
cefazolin (ancef)
If patient is allergic or has MRSA:
Vancomycin
Clindamycin
which drugs do NOT require renal dose adjustments*
Nafcillin
Oxacillin
Dicloxacillin
Ceftriaxone
Doxycline + Minocyline (tetracyclines)
Moxifloxacin
which 2 drug classes are good for AEROBIC GN
aminoglycosides
and
monobactam (aztreonam)
What is the best way to improve a penicillin’s GN coverage?
Add a beta lactamase inhibitor (the best option)
2nd best: add an aminoglycoside
What 2 aminoglycosides are good to use for colorectal surgeries
- Neomycin and erythromycin
What is propanidid used for?
- Increases CNS penetration for penicillins
What 3 antibiotics can cause photosensitivity*
Tetracyclines,
fluroquinolones,
bactrim
What 2 drugs can chelate?
Tetracyclines
fluroquinolones
What is the ideal drug for syphilis?
- Benzathine salt (pen G)
IM ONLY
What is most common cause of UTIs?
E coli (GN)
What is most common cause of SSI (infection) post appendectomy?
Bacteroides (especially b fragilis)
e coli (GN)
What is the most common bacteria post c-section?
staph aureus (GN)
What drugs cause bone marrow suppression?
linezolid and bactrim
tetrocyclines= NOT THIS, only suppress bone growth
what are the 2 drugs for c diff
vancomycin
fidaxomicin
What 2 drug classes have QT prolongation?
macrolides
fluroquinolones
With time-dependent abx, your goal is to keep the abx concentration above the MIC for as long as possible
true
Administration of an additional dose of abx during a surgical procedure is determined by 3 things
length of surgery
half life of abx
blood loss
What is Avibactam
beta lactamase inhibitor
__________bactam
Which antibiotics can prolong the effects of neuromuscular blockade during surgery?
clindamycin
aminoglycosides
What drug is good with MRSA?
- Vancomycin
which drug can be used for GN and GP (NOT MDR)
cefazolin (ancef)
if MDR, use ertapenem
true or false:
all of the ____________mycins cover ONLY GP bacteria
true