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Boards Review
Boards Review
221
Pharmacology
Graduate
06/06/2013

Additional Pharmacology Flashcards

 


 

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Term
granulocytes
Definition
neutrophils: PMNs, polys, segs, bands; left shift = increase in bands

eosinophils: parasites, allergic reactions

eosinophils: parasites, allergic reactions

basophils
Term
agranulocytes
Definition
monocytes: cancer and TB

lymphocytes: viral or fungal infections

agraulocytosis = lack of agranulocytes
Term
macrocytic anemia
Definition
lack of folate or B12
Term
microcytic anemia
Definition
blood loss or iron
Term
Cockcroft-Gault equation
Definition
140-age*wt/72*SrCr

*0.85 for a woman
Term
Child Pugh Score
Definition
liver dysfunction

bilirubin, albumin, PT/INR, ascites, hepatic encephalopathy, liver enzymes are NOT included
Term
epilepsy
Definition
partial - simple and complex

generalized - results in loss of consciousness
tonic clonic
absence - DOC are ethosuximide and valproic acid
myoclonic

infantile

status epilepticus - treated with BZDs (diazepam, lorazepam) and follow with phenytoin (or fosphenytoin)
Term
phenobarbital
Definition
dosing: 1-5 mg/kg/day

metabolism: inducer (most anticonvulsants are inducers - carbamazepine, oxcarbamazepine, phenytoin, phenobarbital), inhibitors (valproic acid - the one that is different)

excretion: biliary or renal; gabapentin and levetiracetam are renally cleared

t1/2 = 3-5 days

therapeutic concentration = 15-40

SE:
CNS - seizures
GI 2
BMS - R (macrocytic anemia due to folate inhibition)
derm - rash (a lot of the newer anticonvulsants, and lamotrigine)
Term
primidone (Mysoline)
Definition
metabolized to phenobarbital

SE: osteomalacia (decrease Ca absorption)
Term
phenytoin (Dilantin)
Definition
effective for all seizure types except absence

dosage: 4-6 mg/kg/day

LOADING DOSE: 15-20 mg/kg; often with fosphenytoin

with phenytoin you can give it at 50 mg/min (hypotension)

with fosphenytoin you can give it at 150 mg/min

once daily dosing is for Kapseals only!

adjust doses in small increments - Mikalis-Menton (saturable kinetics)

absorption - tube feeds, protein, plastic can decrease absorption; hold tube feeds around it or switch to IV

therapeutic level = 10-20...but have to know ALBUMIN
low albumin creases phenytoin levels
free phenytoin level (therapeutic level = 1-2)

SE:
CNS 1 2 - nystagmust with toxicity
CV - hypotension with loading doses
GI 2
BMS - R (macrocytic anemia due to folate malabsorption)
derm - rash including SJS
other - lupus like reaction; gingival hyperplasia
Term
carbamazepine (Tegretol)
Definition
used in trigeminal neuralgia

dosing = 300-600 mg BID

therapeutic level = 4-12

SE:
CNS 1 2
GI 1 2 - drug induced hepatitis
BMS R W - leukopenia
endo - SIADH (too much antidiuretic hormone, hyponatremia); oxcarbamazepine is worse)

unique metabolism: inducer and it's an autoinducer
Term
ethosuximide
Definition
DOC for absence seizures

SE:
CNS 1 2 - psychosis
GI 2
BMS W (leukopenia)
derm - rash
other - parkinsonian like syndrome (tremors)
Term
valproic acid (Depakene) or divalproex (Depakote)
Definition
therapeutic level of 50-100

dosing: 500-1500 mg/day

used for migraine prophylaxis and bipolar disorder

VPA is an enzyme inhibitor

SE:
CNS 1 2
GI 1 2 - hepatitis
BMS T - thrombocytopenia
endocrine - menstrual cycle changes
derm - RASH including SJS
others - alopecia and weight gain
Term
felbamate (Felbatol)
Definition
used in grand mal seizures

SE: aplastic anemia (1:3000 patients) and acute hepatic failure (1:10,000)
Term
gabapentin (Neuronitin)
Definition
used off-label for neuropathic pain

dose: 1200 mg/day for seizures, much higher for pain up to 3600-4500 mg/day

PK: renally excreted!!

SE:
CNS 1 2
other - peripheral edema and weight gain
Term
pregabalin (Lyrica)
Definition
used for diabetic neuropathic pain, post herpetic neuralgia, fibromyalgia

similar SEs to gabapentin

angioedema
Term
lamotrigine (Lamitcal)
Definition
SE:
CNS 1 2 (diplopia)
RASH!!!!!!!!!!!!!!!!!!!!!!!!!!!!!!!!!
Term
topiramate (Toopamax)
Definition
SE:
CNS - slowed speech, difficulty concentrating
renal - kidney stones (carbonic anhydrase inhibitor)
weight loss
used for migraine prophylaxis
Term
levetiracetam (Keppra)
Definition
SE: sedation

renally excreted like gabapentin

has an IV formulation (also phenytoin, fosphenytoin, valproic acid)
Term
zonisamide (Zonegran)
Definition
SE: oligohydrosis, kidney stones, metabolic acidosis
Term
MAOIs
Definition
isocarbaoxazid (Marplan), phenelzine (Nardil), tranylcypromine (Parnate)

hypertensive crisis precipitated by certain foods (tyramine containing foods - wine, aged cheese, pickled herring, chicken livers)

how to treat HTN crisis: phentolamine (alpha antagonist)

serotonin syndrome: agitation, restlessness, confusion, HTN, tachycardic, sweating, diarrhea, shivering, goosebumps, myoclonus, fever

drug interactions: meperidine (Demerol), tramadol, linezolid (weak MAOI)

takes 2 weeks for the drug to wash out
Term
TCAs
Definition
class wide SE:
CNS 2 (in toxic doses CNS 1 - seizures)
GI 2
CV - arrhythmias
anticholinergic - urinary retention, blurred vision, constipation, dry mouth

tertiary amines: imipramine (Tofranil), amitriptyline (Elavil) - lots of sedation and anticholinergic SEs, doxepin (Sinequan)

secondary amines: amoxapine (Asendin), desipramine (Norpramin) - less anticholinergic SEs compared to amitriptyline, nortriptyline (Pamelor)
Term
tetracyclic antidepressant
Definition
mirtazapine (Remeron)

MOA: central presynaptic alpha 2 antagonist; 5HT2 and 3 antagonist; H1 antagonist

dosing: higher doses give less sedation

SE:
CNS 2 - lots of sedation
GI - weight gain
Term
SSRIs
Definition
paroxetine (Paxil) - most sedating, highest incidence of discontinuation syndrome (shortest t1/2), strong 2D6 inhibitor - watch tramadol

fluoxetine (Prozac) - most stimulating (insomnia), least incidence of discontinuation syndrome due to prolonged t1/2 ~7-9 days of metabolite norfluoxetine, stronge 2D6 inhibitor

citalopram (Celexa)

escitalopram (Lexapro) - maybe less SE

sertraline (Zoloft)

fluvoxamine (Luvox) - used in OCD

SE:
GI 2 - N/V/D can be really bad when starting therapy, counsel patients

takes weeks for full effect
Term
trazodone (Desyrel)
Definition
great hypnotic often combined with SSRI

SE:
CV - EKG changes (QT prolongation)
other - priapism
Term
bupropion (Wellbutrin)
Definition
promotes dopamine

3S: smoking cessation, seizures (doses >/= 450 mg/day can cause), lack of sexual dysfunction

highly activating
Term
venlafaxine (Effexor)
Definition
SNRI

SE:
CNS 2
CV - hypertension (diastolic BP increases doses > 225 mg/day)
GI 2
Term
duloxetine (Cymbalta)
Definition
used for diabetic neuropathy, fibromyalgia
Term
anticoagulant monitoring
Definition
PT/INR for warfarin

aPTT for heparin

ACT (activated coagulation time) used for heparin in cath lab or surgery
Term
warfarin (Coumadin)
Definition
vitamin K antagonist

MOA: factors 2, 7, 9, 10, and protein C and S

INR goals
Afib 203
mitral valve replacement 2.5-3.5
DVT/PE 2-3

dosing: usually start at 5 mg/day but highly individualized

start lower doses: elderly, liver disease, on concurrent amiodarone (reducing 25-50%)

pregnancy category X

SE:
bleeding
purple toes syndrome

questions to ask patients: bleeding/bruising; diet - stable in vitamin K containing foods; any new medications

drug interactions:
drugs that decrease INR - phenobarbital, carbamazepine, phenytoin, rifampin, cholestyramine (space it out), nafcillin
drugs that increase INR - amiodarone*****, antibiotics especially Bactrim, fluconazole, clarithromycing, erythromycing (not azithromycin), metronidazole, FQs

patients with high INRs:
vitamin K and fresh frozen plasma
low doses of vitamin K (1-2.5 mg) for most cases
IV vitamin K = risk of anaphylaxis when given push
Term
dabigatran (Pradaxa)
Definition
direct thrombin inhibitor = no antidote

approved only for non-valvular afib

renally excreted (80%); adjust for renal dysfunction

SE: bleeding, dyspepsia

hemodialysis will remove it
Term
heparin and LMWH
Definition
MOA: binds to antithrombin III to facilitate anticoagulation

heparin: bolus plus an IV infusion

LMWH: SQ injections

SE:
bleeding
heparin - osteoporosis

how to reverse heparin - protamine

how to reverse LMWH - ?????

LMWH is renally excreted must adjust in renal dysfunction

use actual body weight for dosing

enoxaparin (Lovenox) dosing: 1 mg/kg BID or 1.5 mg/kg daily

heparin induced thrombocytopenia (HIT): clot kills; usually within 5-14 days of heparin initiation unless previous exposure
treatment: stop the drug; argatroban (hepatically metabolized); lepirudin (renally cleared), bivalirudin (cleared by enzymes - short t1/2)

fondaparinux (Arixtra)
dosing - 2.5 mg SQ daily or weight based for treatment
renally cleared with longer t1/2 than enoxaparin
no good reversal agent
Term
aspirin
Definition
doses: 81-325 mg daily

used in afib with clopidogrel (not as effective)

SE: GI 1 2 - GI bleeding
Term
dipyridamole with ASA (Aggrenox)
Definition
used in TIA/strokes refractory to ASA

SE: high incidence of treatment discontinuation due to HA
Term
ticlopidine (Ticlid)
Definition
ADP receptor antagonist

SE: rash (TTP)
BMS W (leukopenia)
Term
clopidogrel (Plavix)
Definition
ADP receptor antagonist

activated to 3A4 to active metabolite

used in combination with ASA for afib or post stents due to ACS

loading doses of 300-600 mg x1 then 75 mg daily

how long to wait prior to CABG? 5 days

SE: bleeding TTP
Term
prasugrel (Effient)
Definition
ADP receptor antagonist

does not have to be activated

dosing: 60 mg LD; 10 mg daily used for ACS

more effective than Plavix; higher bleeding than Plavix

contraindicated in previous TIA or stroke, >75 years, active bleeding, low weight <60 kg

low long to wait prior to CABG? 7 days

TTP rare
Term
IIb/IIIa inhibitors
Definition
abciximab (Reopro) - MAB acute thrombocytopenia immune mediated response

eptifibitide (Integrelin)

tirofiban (Aggrestat)
Term
lithium
Definition
narrow therapeutic index drug

used for bipolar disorder

PK: renally excreted which can cause toxicity when fluid status or renal perfusion is affected

therapeutic levels:
1-1.5 (acute mania)
0.8-1 (maintenance)
toxic above 2

hemodialysis removes

SE:
CNS 2 - tremor
GI 2
BMS W (leukocytosis)
endocrine - diabetes insipidus; thyroid (usually hypo)
nephrotoxicity

drug interactions: anything that affects sodium (take away sodium, increase Li)
NSAIDs and ACEIs can increase levels as well as volume depletion
Term
narcotics
Definition
opiates - morphine, codeine, hydrocodone, oxycodone

synthetic narcotics - fentanyl, meperidine

SE:
CNS 1 2 - delirium, hallucinations
respiratory depression
CV - hypotension primarily due to morphine derivatives (histamine release)
GI 2 - constipation that does not get tolerant; bowel regimens needed for chronic narcotic therapy
derm - rash/flush due to histamine release
Term
morphine
Definition
dosing: PO, IM, IV, SR product (DO NOT CRUSH)

PK: hepatically metabolized to an active metabolite that is renally cleared (accumulation in CrCL < 30 mL/min)

Avinza (long acting morphine) - immediate and ER beads that can be sprinkled on food - cannot crush or chew

Kadian (long acting morphine) - alcohol increases release of drug; max dose of 1600 mg/day due to jumaric acid causing renal toxicity
Term
codeine
Definition
metabolized to morphine by 2D6 (some people cannot metabolize it)
Term
meperidine (Demerol)
Definition
huge euphoric effect

poor absorption of oral therapy

neurotoxicity due to accumulation of normpeteridine (active metabolite) in renally impaired patients and high doses

used for rigors

no MAOIs within 14 days of meperidine
Term
fentanyl (Duragesic)
Definition
less histamine release, very short acting

patch therapy:
opioid naive patients not candidates
change every 72 hours
NOT FOR ACUTE PAIN
do not add heat to patch
disposal: fold it and flush it
Term
hydromorphone (Dialudid)
Definition
more potent than morphine
Term
methadone
Definition
extremely long t1/2 can accumulate
Term
oxycodone
Definition
given often with acetaminophen (Percocet)
Term
tramadol (Ultram)
Definition
weak mu agonist, inhibits NE and 5HT reuptake)

watch drug interactions

reaally excreted, adjust in renal dysfunction
Term
naltrexone
Definition
used in opiate withdrawal clincs
Term
buprenorphine and naloxone (Suboxone)
Definition
used for narcotic dependence
Term
methylnaltrexone (Relistor)
Definition
indication: opioid induced constipation refractory to laxative therapy

SQ injection 0.5 mg/kg SQ every other day x2 weeks

mu antagonist in the gut
Term
alvimopan (Entereg)
Definition
mu antagonist in the gut

used preoperatively (30 minutes - 5 hours prior) for partial bowel resections to speed up bowel recovery

contraindicated: chronic opioid therapy

only dispense int he hospital up to 15 doses
Term
acetaminophen
Definition
dose limit 3-4 g/day

peds dose: 10-15 mg/kg/dose

IV, PO, PR

SE: hepatotoxicity due to metabolite (normally is conjugated with glutathione and excreted)

N-acethylcystein: dose is 140 mg/kg first dose then 70 mg/kg q4 hours for 17 doses
Term
NSAIDs
Definition
class wide SEs:
CNS 2
respiratory - allergic reactions
CV - some concern over MIs (naproxen is the safest)
GI 1 2 - ulcers (celecoxib less ulcers due to COX 2
BMS - thrombocytopenia (reversible inhibition of platelets)
renal - AKI

drug interactions:
decrease effectiveness of diuretics and ACEIs
increase methotrexate levels
Term
indomethacin (Indocin)
Definition
vert potent prostaglandin inhibitor

use: gout attacks, RA flares

short term use b/c the risk of GI ulcers if very high
Term
diclofenac (Voltaren)
Definition
Flector patch, Voltaren 1% gel, or Pennsaid 1.5% topical solution

SE: hepatotoxicity
Term
ketorolac (Toradol)
Definition
IV and PO

5 day BBW on duration of therapy due to toxicity (liver and renal)
Term
etodolac (Lodine)
Definition
better GI tolerability but less effective
Term
piroxicam (Feldene)
Definition
dose is once daily

more toxicity than traditional NSAIDs (GI)
Term
celecoxib (Celebrex)
Definition
COX 2 inhibitor with less risk of ulceration

ASA therapy with celecoxib negates the benefit

can cause rash due to sulfa moiety
Term
gout
Definition
high uric acid plus crystals

patients at risk are obesity, HTN, hyperlipidemia, high purine diet

medications that can precipitate a gout attack: diuretics (loops or thiazides), niacin, pyrazinamide, low dose ASA, cyclosporine

goals of therapy:
control the current attack
prevent further attacks
reduce modifiable risk factors
Term
acute gout attack
Definition
NSAIDs (indomethacin)

colchicine
MOA - inhibits phagocytosis of urate crystals by neutrophils
used for both the acute and prophylaxis
dose: 1.2 mg x1; may repeat with 0.6 mg x1 2 hours later
SE: GI 2 (bad diarrhea), BMS neutropenia and anemia, IV formulation can cause extravastation

corticosteroids
used in refractory cases or when other drugs are contraindicated
SE: CNS 1 2 (psychoses), CV (fluid retention, GI 1 2 (ulcers, appetite simulation), endocrine (hyperglycemia, osteoporosis), adrenal suppression (14 days), immunosuppression
Term
prevention of gout attacks
Definition
reduce purine rich foods and alcohol - red meat, shellfish, beer, peas, beans

stay hydrated

weight loss

allopurinol (Zyloprim)
MOA: xanthine oxidase inhibitor
use with acute agents to prevent further attacks
SE: GI 2, derm (rash), other (vasculitis or interstitial nephritis
drug interactions: 6-MP (metabolized by xanthine oxidase, reduce 6-MP by 75% when given with allopurinol)

feboxustat (Uloric)
dose: 40-80 mg daily
GI 1 - liver enzyme elevation, arthralgias, rash

rasburicase (Elitek)
use for prevention of tumor lysis syndrome
0.2 mg/kg IV over 30 minutes up to 5 days
SE: methemoglobinemia
check for G6PD deficiency
Term
asthma
Definition
clinical presentation: SOB, dyspnea, wheezing, chest tightness, cough***

goals of treatment:
prevent chronic troublesome symptoms
keep near pulmonary function
require infrequent use of B2 agonist
normal activity levels
prevent exacerbations
limit ED or clinic visits
Term
beta-2 agonists (short acting)
Definition
albuterol (Proventil)

levalbuterol (Xopenex) - less tachycardia

SE:
CNS 1 2 - anxiety, insomnia, agitation
CV - tachycardia or arrhythmias
GI 2 - metallic taste, hoarseness, throat irritation
Term
beta-2 agonists (long acting)
Definition
formoterol (Foradil)

salmeterol (Serevent)

not for acute exacerbations

not for asthma monotherapy (long acting)
Term
inhaled corticosteroids
Definition
STANDARD OF CARE FOR ASTHMA

chronic persistent asthma get inhaled corticosteroids

fluticasone with salmeterol (Advair)

mometasone with formoterol (Dulera)

budesonide with formoterol (Symbicort)

SE:
local SEs - dry mouth, hoarseness, oral candidiasis
Term
leukotriiene antagonists
Definition
zafirlukast (Accolate)

montelukast (Singulair)

less effective than corticosteroids for asthma

useful for exercise induced or allergic rhinitis

singulair oral chewable tablet as well as granules

SE: well tolerated
Churg-Sstrauss syndrome - eosinophilic vasculitis
Term
lipoxygenase inhibitor
Definition
zileuton (Zyflo)

dose 600 mg QID

SE: liver enzyme elevation (requires monitoring frequently
Term
mast cell stabilizers
Definition
chromolyn (Intal)

takes 4-6 weeks for full effect
Term
theophylline
Definition
aminophylline is the IV version

aminophyllin is 80% of theophylline

therapeutic levels = 10-20

toxicities:
CNS 1 2 - seizures
CV - tachycardia and arrhythmias
GI 2
Term
anticholinergics
Definition
little role in asthma, first line in COPD

ipratropium (Atrovent)

tiotropium (Spiriva)

used for acute asthma exacerbations

ipratropium/albuterol (Combivent) - avoid in peanut allergy (nebs okay)
Term
anti-IgE antibody
Definition
Xolair

SQ injection given in office

patient has to be monitored for 2 hours after 1st injection; 30 minutes after subsequent injections
Term
COPD
Definition
first line are bronchodilators (anticholinergics and beta agonists)

anticholinergics are first line

what are the role of steroids? prevent exacerbations, severe disease (FEV1 <60%), asthma component
Term
roflumilast (Daliresp)
Definition
PDE-4 inhibitor

oral agen: 500 mcg PO daily

NOT for acute exacerbations, to prevent COPD exacerbations

hard to tolerate

CNS 1 2 suidical ideation and depression

GI - weight loss
Term
drugs that increase incidence of PUD and GERD
Definition
NSAIDs****, corticosteroids, alcohol, smoking

goals of PUD and GERD therapy:
promote ulcer healing
relieve ulcer pain
prevent complications
prevent recurrences
Term
H. pylori treatment
Definition
2 antibiotics and a PPI

amoxicillin + macrolide (clarithromycin, NOT azithromycin) + BID PPI

sequential therapy: 5 days of amoxicillin followed by 5 days of clarithromycing and PPI the whole time
Term
H2 receptor antagonists
Definition
inferior to PPIs for reflux healing and symptoms

cimetidine (Tagamet)

ranitidine (Zantac)

famotidine (Pepcid)

nizantadine (Axid)

SE:
CNS 2 - dizziness, disorientation in elderly patients or in renally insufficient
BMS T (thrombocytopenia)
cimetidine - gynecomastia; LOTS of drug interaction; STRONG INHIBITOR of enzymes
Term
antacids
Definition
very short acting

usually have a combination of 2 cations: Al, Mg, Ca (associated with a lot of rebound)

Al and Ca can be constipating

Mg = diarrhea

drug interactions due to binding in the GI tract
Term
PPIs
Definition
esomeprazole (Nexium) - IV and PO formulations

lansoprazole (Prevacid) - PO and solutab formulation

omeprazole (Prilosec)

pantoprazole (Protonix) - PO and IV; IV drips used for acute GI bleeds

rabeprazole (Acephex)

SE:
GI 1 2 - C. diff
CNS 2
hypoagnesemia
Term
drugs that lower LES tone
Definition
estrogen, CCBs, peppermint, smoking
Term
misoprostol (Cytote)
Definition
used in place of PPIs for ulcer healing

SE:
GI 2 (severe diarrhea)
spontaneous abortion

Arthrotec (diclofenac with misoprostol)
Term
gestational diabetes
Definition
NO ORAL AGENTS

insulin only
Term
goal blood sugar
Definition
70-120 fasting
Term
diagnosis of DM
Definition
fasting blood sugar >/= 126 mg/dL on 2 occasions

2-h glucose >/= 200 on OGTT or classic signs of DM + random glucose >/= 200

A1c >6.5%
Term
only insulin you can give IV
Definition
regular insulin
Term
sulfonylureas
Definition
pump insulin from pancreas

SE: hypoglycemia, rash, weight gain

renally cleared...accumulate and cause more hypoglycemia in AKI or CKD

glipizide is preferred over glyburide
Term
metformin
Definition
first line T2DM drug

generally, you need 1500 mg/d for effectiveness; titrate upward slowly

max dose of 2550 mg/day

SE:
GI 1 2 - lactic acidosis, diarrhea
no hypoglycemia as monotherapy
weight neutral or weight loss
Term
alpha glucosidase inhibitors
Definition
MOA: digestion of carbohydrates (postprandial hyperglycemia)

SE:
GI 2 - flatulence
no hypoglycemia as monotherapy

acarbose (Precose)

miglitol (Glyset)
Term
thiazolidinediones (TZDs)
Definition
MOA: decrease insulin resistance at PPAR gamma receptor

SE:
CV - edema (watch in HR)
GI 2
endo - osteoporosis
Term
meglitinides
Definition
repaglinide (Prandin)

nateglinide (Starlix)

MOA: short acting insulin secreting drugs

hypoglycemia is skip meal
Term
GLP-1 agonists
Definition
liraglutide (Victoza) 1.2-1.8 mg/day

exenatide (Byetta or Bydureon)

Byetta 5-10 mcg BID
Bydureon 2 mg q7d

MOA: hypoglycemia rare due to control on glucagon

SE: GI 1 2 pancreatitis, weight loss common
Term
DPP-IV inhibitors
Definition
oral agents

saxagliptin (Onglyza)

sitagliptin (Januvia)

GI 2 - N/V

bladder cancer
Term
hypertension stages
Definition
prehypertension: SBP 120-139 or DBP 80-89

Stage I: 140-159 or 90-99

Stage II: >/= 160 or >/= 100
Term
thiazide diuretics
Definition
work in the distal tubule

chlorthalidone (Hygroton)

chlorthiazide (Diuril) - IV syndergy with loops

HCTZ

indapamide (Lozol)

metolazone (Zaroxolyn) - used in synergy with loops in HF patients

SE:
hypokalemia, hyperuricemia, hypercalcemia (different from loops!!!), hyperglycemia, hyponatremia, hypomagnesemia

monitoring: BP, fluid losses, renal function (BUN/SrCr)
Term
loop diuretics
Definition
remove more fluid

cause hypocalcemia

potential in high doses for ototoxicity

bumetanide (Bumex)

furosemmide (Lasix)

torsemide (Demadex)

ethacrynic acid (Edecrin) - no sulfa group

when to use loops over thiazide in HTN? CrCl < 30 mL/min
Term
K sparing diuretics/aldosterone antagonists
Definition
work in the late distal tubule and collecting ducts

spironolactone (Aldactone)

elperenone (Inspra)

triamterene (Dyrenium) - usually in combination with HCTZ

SE:
electrolytes - hyperkalemia
monitoring kidney function (BUN/SrCr)
spironolactone - gynecomastia
Term
beta blocker with intrinsic sympathomimetic activity
Definition
pindolol (Visken)
Term
B1 selective beta blockers
Definition
atenolol (Tenormin) - renally excreted

bisoprolol (Zebeta) - good in HF but not FDA approved

metoprolol (Lopressor - tartrate BID; Toprolo XL - succinate daily); good data in HF for succinate

esmolol (Brevibloc) - IV agent for HTN emergency (drip)

nebivolol (Bystolic) - promotes nitric oxide

betaxolol (kerlone)
Term
nonselective beta blockers
Definition
nadolol (Corgard)

propranolol (Inderal) - off label for tremors, cirrhosis with esophageal varices, and migraine prophylaxis
Term
nonselective beta blockers with alpha blockade (alpha 1)
Definition
labetalol (Normodyne)

carvedilol (Coreg or Coreg CR)
Coreg CR dumps with alcohol

not 1st line for HTN; must have compelling indication (afib)

SE:
CNS 1 2 - depression
CV 1 2 - complete heart block, bradycardia
respiratory - bronchospasms (especially nonselective agents or high doses of selective agents)
endocrine - mask hypoglycemia
Term
peripheral alpha blockers
Definition
bad data

only use is concomitant BPH

doxazosin (Cardura)

prazosin (Minipres)

terazosin (Hytrin)

SE: orthostatic hypotension and first dose syncope
Term
centrally acting alpha agonists
Definition
oral dosing 2-3 times daily bad for compliance

clonidine patch given q7 days

guanfacine (Tenex)

methyldopa (Aldomet) - DOC in pregnancy (and hydralazine)

SE:
CNS 2 - sedation
GI 2 - dry mouth
CV - withdrawal hypertension
derm - contact dermatitis from the patch
Term
ACEIs
Definition
first line for DM patients especially with microalbuminuria; post MI with depressed EF or anterior wall MI; high coronary disease risk (ramipril); CKD

SE:
cough
angioedema (do not rechallenge)
GI 2 - loss of taste with captopril
derm - rash (captopril)
renal - AKI; CI'd in bilateral renal artery stenosis
electrolyte - hyperkalemia (due to aldosterone blockade)

CI: pregnancy, angioedema, bilateral renal artery stenosis
Term
ARBs
Definition
only in refractory ACEI patients b/c no cough

telmisartan (Micardis)

HTN: irbesartan and telmisartan

DM: ADA recommends for T2DM patients with microalbuminuria or proteinuria

HF: candesartan or valsartan
Term
nondihydropyridine CCBs
Definition
verapamil (Calan)

diltiazem (Cardizem)

work centrally, directly on the heart to slow down heart rate

not great for BP control
Term
dihydropyridine CCBs
Definition
amlodipine (Norvasc)

felodipine (Plendil)

isradipine (Dynacirc)

nifedipine (Adalat or Procardia)

nisoldipine (Sular)

nicardipine (Cardene) - IV drip for HTN emergencies (target organ damage of stroke)

SE:
CNS 2 - HA
GI 2
misc - peripheral edema (DHP)
verapamil - constipation
Term
direct vasodilators
Definition
hydralazine (Apresoline) - in patients usually dosed 3-4 times daily

minoxidil (Loniten) - HTN resistant patients

SE:
CV - tachycardia and NA and fluid retention (usually on beta blocker and diuretic already)
hydralazine can cause drug induced systemic lupus
minoxidil - hirsutism
Term
compelling indications for HTN drugs
Definition
DM with proteinuria: ACEI

HF: ACEI, beta blocker, ARB, aldosterone antagonist

post MI: beta blockers, ACEI (anterior wall MIs)

angina: beta blockers, CCBs

cyclosporoine induced HTN: CCB (DHP)

essential tremor: beta blockers

migraine prophylaxis: beta blockers

renal insufficiency: ACEI and ARB
Term
diagnosis of HIV
Definition
screening test: ELISA - detecting HIV antibodies

confirmatory test: Western blot
Term
who are good candidates for antiretroviral therapy?
Definition
CD4 count <500 cells/mm3

symptomatic disease (opportunistic infection or AIDS defining illness)

HBV coinfection

pregnancy
Term
first line HIV regimens
Definition
2 nucleoside reverse transcriptase inhibitors

emtricitabine and tenofovir

PLUS one of the following:

NNRTI (efavirenza, Sustiva) - Atripla combination product

protease inhibitors: atazanavir or darunavir plus ritonavir (to boost effects of the drug)

integrase inhibitor: raltegravir
Term
nucleoside RTIs
Definition
class wide SEs:
lactic acidosis, hepatic steatosis (fatty liver), lipodystrophy (more common with PIs)
Term
tenofovir (TDF, Viread)
Definition
dose: 300 mg daily

SE: nephrotoxicity (acute or chronic), reduce bone mineral density

caution: stopping therapy may cause HBV flares
Term
emtricitabine (FTC, Emtriva)
Definition
dose: 200 mg daily (capsule), 240 mg daily (solution)

SE: hyperpigmentation of palms, soles

caution: stopping therapy may cause HBV flares
Term
zidovudine (AZT, Retrovir)
Definition
300 mg BID or 200 mg TID

renally cleared (have to adjust in CKD or AKI

SE: BMS - macrocytic anemia or neutropenia

hyperpigmentation

lactic acidosis
Term
abacavir (ABC, Ziagen)
Definition
dose: 300 mg BID of 600 mg daily

SE: life threatening rash with fever, respiratory distress, GI effects, SOB

test for HLA-B 5701 - if positive do not use (have a higher risk of the hypersensitivity reaction)

not used in patients with baseline viral load > 100,000
Term
lamivudine (3TC, Epivir)
Definition
SE: pancreatitis (especially in children)

caution: stopping may increase HBV flair
Term
didanosine (Videx)
Definition
>60 kg - 400 mg daily; < 60 kg - 250 mg daily

SE: pancreatitis (high risk); peripheral neuropathy; optic neuritis
Term
stavudine (Zerit)
Definition
dosing > 60 kg - 40 mg BID; < 60 kg - 30 mg BID

SE: fatal lactic acidosis!; lipodystrophy, peripheral neuropathy; hyperlipidemia; DM; rapid neuromuslcular weakness
Term
NNRTIs
Definition
key treatment principle: resistance to one = resistance to class

class wide SE: RASH
Term
efavirenz (Sustiva)
Definition
dosing 600 mg HS

SE:
rash
CNS 1 2 - dizziness, HA, insomnia, vivid dreams and nightmares, inability to concentrate

contraindicated in first trimester of pregnacy
Term
nevirapin (Viramune)
Definition
SE: life threatening rash...including SJS and hepatotoxicity

CI: women with CD4 > 250 or men > 400; they have increased risk of hepatotoxicity
Term
etravirine (Intelence)
Definition
rash including SJS; peripheral neuropathy
Term
riplivirine (Edurant)
Definition
combination product with tenofovir and emtricitabine called Complera

Complera not to be used in patients with baseline viral load > 100K

SE: depression, insomnia, fat redistribution
Term
protease inhibitors
Definition
class wide SE: hyperlipidemia, hyperglycemia

all are combined with ritonavir
Term
atazanavir (Reyataz)
Definition
SE: increased indirect hyperbilirubinemia; rash; prolonged QT interrval; fat redistribution; nephrolithiasis

caution: do not give with PPIs due to decreased absorption (>20 mg of omeprazole)
Term
arunavir (Prezista)
Definition
SE: rash including SJS, new onset DM, increased liver enzymes

caution: has a sulfonamide moiety
Term
lopinavir with ritonavir (Kaletra)
Definition
refrigerated

SE:
GI 2
hyperlipidemia - TG predominant
increased liver enzymes
Term
fosamprinavir (Lexiva)
Definition
SE: rash, oral paresthesias, hyperlipidemia, hypertriglyceridemmia, fat redistribution

caution: sulfa allergic patients
Term
tipranavir (Aptivus)
Definition
SE: rash, hepatitis, transaminitis
Term
nelfinavir (Viracept)
Definition
not boosted with ritonavir

SE:
GI 2 - flatulence
transaminitis
phenylketonuria
Term
saquinavir (Invirase)
Definition
SE: PR and QT prolongation; hepatotoxitiy, transaminitis
Term
indinavir (Crixivan)
Definition
SE: crystaluria causing AKI

patient counseling: drink lots of water
Term
raltegravir (Insentress)
Definition
integrase inhibitor

SE:
GI2
myalgias
CPK elevations
Term
maraviroc (Selzentry)
Definition
CCR5 antagonist

SE: hepatotoxicity; coughing spells, drug fever, rash

have to do tropism testing prior to ensure effectiveness
Term
stribild (quad)
Definition
elvitegravir/emtricitabine/tenofovir/cobicistat

cobicistat inhibits metabolism of elvitegravir
Term
enfuviritide (Fuzeon)
Definition
fusion inhibitor

SE: injection site reactions, increased risk of bacterial pneumonia; hypersensitivity reaction

injection site reactions expected to occur in every patient; site rotation necessary
Term
opportunistic infection prophylaxis
Definition
CD4 < 200 - primary prophylaxis vs pneumocystis
bactrim or if allergic dapsone or pentamidine (inhaled)

CD4 < 100 - toxoplasmosis
bactrim or if allergic then atovaquone or dapsone plus pyramethamine plus leucovorin

MAC
initiate primary prophylaxis when < 50
preferred: azithromycing 1200 mg once weekly
alternative: clarithromycin 500 mg BID or rifabutin
Term
cell cycle dependent - chemotherapy
Definition
resting phase (G0): alkylating agents, nitrosoureas, antitumor antibiotics, cisplatin/carboplatin, procarbazine, dacarbazine

S phase (DNA synthesis or replication): 5-FU, gemcitabine, methotrexate, hydroxyurea, 6-MP

mitotic phase (M phase): vinca alkaloids, paclitaxel, docetaxel
Term
alkylating agents
Definition
nitrogen mustards - low emetogenic potential

nitrosoureas
Term
busulfan (Myleran)
Definition
nitrogen mustard

use: CML

oral

SE: hepatic veno-occlusive disease, pulmonary fibrosis
Term
chlorambucil (Leukeran)
Definition
nitrogen mustard

oral

SE: pulmonary toxicity (not as much as busulfan); thrombocytopenia
Term
cyclophosphammide (Cytoxan)
Definition
nitrogen mustard

use: breast, ovarian, prostate, lung

non-oncology uses: RA, glomerulonephritis

SE: metabolite is acrolein which causes hemorrhagic cystitis

prevent this with lots of hydration and optional infusion of mesna (binds acrolein in the bladder)

also can cause SIADH (metabolite)
Term
ifosfammide (Ifex)
Definition
nitrogen mustard

structural analog of cyclophosphamide

use: lung, testicular, lymphomas, and sarcomas

always give with mesna to prevent hemorrhagic cystitis
Term
mechlorethamine (Mustargen)
Definition
nitrogen mustard

one of the original nitrogen mustards

use: multiple including polycythemia vera, CLL, CML, and Hodgkins disease

part of the MOPP regimen
Term
melphalan (alkeran)
Definition
nitrogen mustard

use: lymphoma, breast, ovarian

SE: BMS (thrombocytopenia)

do NOT crush tablets
Term
thiotepa (Thioplex)
Definition
nitrogen mustard

use: bladder

SE: BMS
Term
nitrosoureas
Definition
carmustine (BiCNU)

lomustine (CeeNU)

strepozocin (Zanosar)

all used for brain malignancies

SE:
leukopenia about 3-5 weeks after therapy (more delayed than the other)

lots of N/V

prolonged carmustine associated with pulmonary toxicity
Term
altretamine (Hexalen)
Definition
platinum analogue

use: ovarian (orally)

SE: GI 2
Term
carboplatin (Paraplatin)
Definition
platinum analog

cisplatin analog with less nephrotoxicity (but still there) but more BMS

calculate dose using AUC values and targets
Term
cisplatin (Platinol)
Definition
platinum analog

use: testicular, ovarian, lung, head and neck

SE:
high emetogenic potential
nephrology: high incidence of AKI
ototoxicity
peripheral neuropathy
hypomagnesemia
Term
dacarbazine (DTIC-Dome)
Definition
platinum analog

use: melanomas, Hodgkin's idsease, sarcomas

SE: severe N/V
Term
procarbazine (Matulane)
Definition
platinum analog

use: Hodgkin's disease and other lymphomas

drug interactions with MAOIs and TCAs and tyramine containing foods

disulfiram reaction

SE: CNS 1 2 - depression
Term
antibiotics and anthracyclines
Definition
cardiotoxicity!!!!

patients get pre-treatment with either ECHO or MUGA
Term
daunorubicin (Cerubidine)
Definition
anthracycline

SE: cardiotoxicity, alopecia, stomatitis

dose limit of 550 mg/2
Term
doxorubicine (Adriamycin)
Definition
anthracycline

same dose limit of 550 mg/m2

urine discoloration (red)
Term
idarubicine (Idamycin)
Definition
anthracycline

lifetime dose is 137.5 mg/m2
Term
mitoxantrone (Novantrone)
Definition
anthracycline

lifetime dose is 160 mg/m2

urine discoloration (blue-green)

used in MS patients
Term
Doxil - doxorubicine liposomal formulation
Definition
used to decrease the cardiotoxicity
Term
dexrazosane (Zinecard)
Definition
iron chelator used to prevent oxygen free radicals and cardiotoxicity

dose: 500 mg/m2 of Zinecard for every 50 mg/m2 of doxorubicine
Term
bleomycin (Benoxan)
Definition
antibiotic

use: Hodgkin's lymphoma (ABVD), testicular cancer

SE: pulmonary toxicity especcially with doses > 200 units/m2
mucositis, BMS
Term
dactinomycin (Cosmegen)
Definition
antibiotic

SE:
GI 2 - mucositis
BMS
Term
mitomycin (Mutamycin)
Definition
antibiotic

SE:
stomatitis
GI 2
Term
methotrexate (MTX, Amethopterin)
Definition
antimetabolite

folic acid antabonist

uses: variety of cancers and RA, psoriasis, ectopic pregnancy abortion

SE: BMS and GI 2

leucovorin rescue: 10-100 mg/m2 q6h until MTX levels start falling; done with high doses of methotrexate

other non chemo uses oral dosing (once weekly); IM doses can also be once weekly
Term
cytarabein (Cytosar, ARA-C)
Definition
antimetabolite

use: induction of AML

SE: myelosuppression common with HIDAC (high dose cytarabine), can cause conjunctivitis (give them corticosteroid eye drops)
Term
fludarabine (Fludara)
Definition
antimetabolite - purine antagonist

use: CLL

SE: myelosuppression, neurotoxicity, pulmonary toxicity

BMS severe sometimes you will prophylaxis with Bactrim for PCP
Term
mercaptopurine (6-MP)
Definition
antimetabolite

use: ALL and chronic leukemia

dose reduce when given with allopurinol (75%)

SE: cholestatic liver dysfunction
Term
cladribine (Leustatin)
Definition
antimetabolite

use: hairy cell leukemia

SE: neutropenia and drug fever
Term
pentostatin (Nipent)
Definition
antimetabolite

SE: nephrotoxic (hydrate well), drug fever

use: hairy cell leukemia
Term
gemcitabine (Gemzar)
Definition
pyrimidine antagonist

use: pancreatic cancer

SE: neutropenia (rare), increased liver enzymes
Term
fluorouracil (Adrucil, 5-FU)
Definition
pyrimidine antagonist

use: breast, colon, head/neck

may add leucovorin for increased colon cancer response

SE: BMS and mucositis, nausea very low
Term
capecitabine (Xeloda)
Definition
pyrimidine antagonist

use: colorectal cancer and metastatic breast cancer

oral 5-FU

SE: GI 2 a lot of patients stop due to GI SEs

treat in 2 week oral cycles
Term
floxuridine (FUDR)
Definition
pyrimidine antagonist

drying or darkening of nails and hair (sunlight can worsen this)
Term
vinca alkaloids
Definition
vincristine (Oncovorin)

vinorelbine (Navelbine)

vinblastine (Velban)

SE: vincristing and vinblastine are vesicants

neurotoxic medications

dose maximum for vincristine is 2 mg

vincristine not to be given intrathecally!!!
Term
epipodophyllotoxin
Definition
etoposide (Vepesid): PO and IV
refrigerate
SE: well tolerated; alopecia and mucositis

tenoposide (Vumon)
SE: hypotension and hypersensitivity due to castor oil
Term
paclitaxel (Taxol)
Definition
taxane

use: lung, ovarian, and breast

SE: neutropenia (greater with 24 hour infusion)
CV - bradycardia, hypersensitivity reaction (premed with H2 antagonists, steroids, H1 antagonists)
CNS - neurotoxicity with parasthesia
Term
docetaxel (Taxotere)
Definition
taxanes

SE: neutropenia, fluid retention with high cumulative doses > 500 mg/m2
Term
camptothecins
Definition
topotecan (Hycamtin)

irinotecan (Camptosar)

SE: severe diarrhea (give some loperamide in case it happens)
Term
trastuzumab (Herceptin)
Definition
biologic

HER2 positive good candidate for Herceptin

use: breast cancer

SE: cardiotoxicity (baseline ECHO or MUGA)
Term
ribuximab (Rituxan)
Definition
biologic

monoclonal antibody that binds to CD20 antigen expressed in many b-cell NHL lymphomas

use: b-cell lymphomas as well as follicular lymphoas (CD-20 positive)

SE: infusion related reactions that have resulted in death, especially the initial infusion!!! hypoxia, pulmonary infiltrates, ARDS, MI, vfib

start low and go slow
Term
asparaginase (Elspar)
Definition
requires a test dose for administration

used in ALL

SE: hyperglycemia, CNS disturbances, pancreatitis
Term
hydroxyurea (Hydrea)
Definition
used in oncology (leukemia); used in sickle cell disease as well as essential thrombocytosis)
Term
tamoxifen (Nolvadex)
Definition
antiestrogenic compound (PO)

use: breast cancer

SE: flushing, weight gain

premenopausal patients
Term
aromatase inhibitors
Definition
anastrazole (Arimidex)

letrozole (Femera)

used in postmenopausal patients

SE: HTN, flushing, mood disturbances

amifostine

used to prevent cisplatin induced nephro and neurotoxicity

SE: transietn hypotension during the infusion
Term
chemotherapy induced nausea and vomiting
Definition
5-HT3 (trons): very effective agents with low toxicity
palonesetron (Aloxi) has a 40 hour t1/2 - give 1 dose

aprepitant (Emend): used with refractory N/V or in cisplatin containing regimens

corticosteroids: useful for prevention of delayed N/V

anticipatory N/V: BZDs like lorazepam
Term
colony stimulating factors
Definition
G-CSF (Neupogen or Neulasta)
refrigerate
Neulasta is pegfilgrastim (6 mg SQ injection one time 24 hours after cycle
SE: bone pain can be severe

GM-CSF (sargramostim or Leukine(
refrigerate
Term
eltotinib (Tarceva)
Definition
epidermal growth factor

oral EGRF

GI 2
Term
bevacizumab (Avastin)
Definition
epidermal growth factor

SE: hypertension, HA, GI 2
Term
cetuximab (Erbitux)
Definition
epidermal growth factor

SE: infusion reactions, fever, sepsis, PE, kidney failure (monitor urinalysis or protein in urine)
Term
epoetin alpha (Epogen/Procrit)
Definition
used for chemotherapy induced enemia or in CKD induced anemia

SE: hypersensitivity to the albumin (CI)

increased risk of CV events (MI and stroke)

may increase risk of certain cancers (breast, cervical, head and neck)

targeting Hgb of 10-12

darbepoetin (Aranesp) - longer t1/2 than epsoetin alpha
Term
risk factors for CHD
Definition
family history of early heart disease: MI or sudden death in parent or 1st degree relative (males < 55 or females < 65)

age: males > 45 or females > 55

current smoker

HTN

low HDL (<40)

high HDL (>60 is a negative risk factor)
Term
bile acid sequestrants
Definition
nonabsorbable resins

bind bile acids in GI tract disrupting enterohepatic reuptake

decrease LDL by 5-30%; may increase TG

cholestyramine (Questran)

coclestipol (Colestid)

colesevelam (Welchol)

GI 2

drug interactions due to binding - thiazides, digoxin, amiiodarone, warfarin, MTX, levothyroxine, NSAIDs

separate 1 hour before or 4-6 hours after

drink plenty of water to limit constipation
Term
niacin
Definition
best HDL increasing drug but outcome data not good so far

SE:
derm - flushing (prostaglandin mediated vasodilation); pruritis and dry skin; take 325 mg ASA 30-60 minutes prior to dose to limit flushing. ETOH and hot beverages can increase flushing
GI - liver toxicity with SR products
endo - hyperglycemia or hyperuricemia
myopathy when given with statins or gemfibrozil
Term
HMG CoA reductase inhibitors
Definition
statins

very well studied for decreasing morbidity and mortality for both primary and secondary prevention

SE:
CNS 2
GI 2
endo - new onset DM (benefit must higher than the risks)
musculoskeletal - myalgias, myositis, muscle weakness...rhabdomyolysis); simvastatin has the highest risk of musculoskeltal SE (if occurs try pravastatin or rosuvastatin)

CI with protease inhibitors, gemfibrozil, clarithromycin, erythromycin, ketoconazole

10 mg max of simvastatin with dilt/verap

20 mg max with amio/amlodipine, ranolazine

pravastatin - safe med for drug interactions

fluvastatin - problem with warfarin (2D9)

monitoring: SEs, lipid panels usually q4-6 weeks
Term
fibrinic acid deriatives
Definition
gemfibrozil (Lopid)

fenofibrate (Tricor)

SE:
CNS 2
GI 1 2 - gallstones
fenofibrate can cause photosensitivity

used to lower TG
Term
ezetimibe (Zetia)
Definition
decreases intestinal absorption of cholesterol

clinically decreases LDL about 18%

SE: GI 1 2 increased liver enzymes

drug interactions: Al and Mg can bind and lower levels
Term
fish oils
Definition
omega 3 fatty acids (Lovaza)

primarily used to decrease TGs

Lovaza 1 g capsule (need 4 g/day for efficacy)

SE: GI 2 taste perversions, burping, dyspepsia

monitor: liver enzymes while on therapy

can increase LDL
Term
nitrates
Definition
dilate primarily veins and some arterial dilation as well

relax smooth muscle

nitrate tolerance - when you continuously give the drug you get tolerant to the effect and need more for effect
try to give a 12 hour nitrate free interval to prevent tolerance from happening

purely for symptom control

dosage forms:
SL tablet - once bottle is opened, can keep it for 6 months; can take it 3 times, then need to go to the ER; very quick onset
translingual spray: quick onset
sustained release capsule
ointment 2% paste
transdermal patch - apply usually on for 12 hours, off for 12 hours
IV drip - comes in glass bottle (not stable in plastic bottles); used for rapid titration

SE:
CNS - lots of HAs, facial flushing
CV - hypotension, reflex tachycardia due to rapid vasodialtion
GI 2 - tingling under tongue with SL dosage form
derm - contact dermatitis with ointment and transdermal patch

drug interactions: avoid with PDE 5 inhibitors (get profound hypotension)
Term
ranolazine (Ranexa)
Definition
SE:
CV - QT prolongation
GI 2
CNS 2

used for angina, reduces oxygen demand

weak-moderate 2D6 inhibitor
Term
what to do if diuretic resistance occurs
Definition
increase the dose to a point; then may switch from furosemide to bumetaide or torsemide for improved absorption

if high IV doses aren't working convert to a continuous drip (Lasix drips or Bumex drips)

add thiazides for potentiation (metolazone or IV chlorthiazide (Diruil)
Term
ARBs in HF
Definition
candesartan - has data to preserve EF

valsartan - decreased morbidity in HR
Term
digoxin
Definition
does not affect mortality, only morbidity (hospitalizations)

DIG trial - averag elevels < 1

increasing the strength of contraction through Na/K/ATPase

monitoring: renal function!!!!

what electrolytes potentiate digoxin toxicity? hypomagnesemia and hypokalemia and hypercalcemia

therapeutic levels: 0.8-2

SE:
CV - bradycardia, multiple arrhythmias
toxicity manifested by severe N/V, green halos

toxicity treatment - make sure electrolytes repleted (K and Mg); Digibind antibody if needed)
Term
beta-lactams
Definition
inhibit cell wall formation by binding to the penicillin binding protein

penicillin G (IV)/VK (PO): still excellent coverage against Strep species

antistaphylococcal PCNs: methicillin, nafcillin, oxacillin, dicloxacillin
DOC for MSSA

aminopenicillins: ampicillin (IV) and amoxicillin (PO)
better gram (-) coverage than PCN

antipseudomonal penicillins: piperacillin

beta lactam/beta lactamase inhibitors: amoxicillin/clavulanate (Augmentin), ampicillin/sulbactam (Unasyn), ticarcillin/clavulanate (Timentin), piperacillin/tazobactam (Zosyn)

beta lactamase inhibitors add anaerobic coverage and better gram negative coverage

SE:
hypersensitivity reactions including anaphylaxis: do not challenge anaphylaxis with cephalosporins; 5-10% cross reactivity with cephs and carbapensems (mild reactions only)
BMS - hemolytic anemia
hypernatremia due to ticarcillin
nephron - acute interstitial nephritis (nafcillin)
Term
cephalosporins
Definition
NO ENTEROCOCCUS activity (ampicillin is DOC)

E. faecalis
E. faecium (more drug resistant strain; VRE)
Term
1st generation cephalosporins
Definition
primarily gram (+) coverage (Staph and Strep species)

cefazolin (Ancef) IV version used in surgical prophylaxis

cephalexin (Keflex) PO version

active against MSSA
Term
2nd generation cephalosporins
Definition
add more gram negative coverage

cephamycins: cefoxitin (Mefoxin) - good anaerobic coverage (surgical phrophylaxis with colorectal cases)

cefuxoime (Zinacef) IV; ceftin PO

cefaclor (Ceclor) - lots of rash

cefdinir (Omnicef) - good for kids b/c it tastes good
Term
3rd generation cephalosporins
Definition
more gram (-) coverage, lose some gram positive coverage

cefotaxime (Claforan) - studied well in SBP, used in infant sepsis

ceftriaxone (Rocephin)
dosed once daily except in meningitis where it is dosed q12 hours for BBB penetration
biliary sluddging
do not give with Ca containing foods (precipitation)

cefpodoxime (Vantin)
oral agent for step down for Rocephin

cefixime (Suprax)
not good coverage against Strep species
good for gonorrhea (STIs)

ceftazidime (Ceftaz)
has pseudomonal coverage
lacks good Strep coverage
Term
4th generation cephalosporin
Definition
cefepime (Maxipime)

good gram (+) and gram (-) coverage including Pseudomonas

SE: neurotoxicity (seizures with cefipime)
Term
carbapenems
Definition
imipenem with cilastin (Primaxin)
cilastatin is a renal dihydropeptidase inhibitor (brush border cells will break down imipenem without this)

meropenem (Merrem)

doripenem (Doribax(

ertapenem (Invanz)
differnet from others b/c no Pseudomonas coverage
dosed once daily

broad coverage!!!!!!!!

holes in coverage are MRSA and Stenotrophomonas

SE: seizures (most with imipenem), use meropenem with meningitis patients
Term
monobactams
Definition
aztreonam (Azactam)

aerobic gram negative coverage only including Pseudomonas

niche drug in patients with anaphylactic reactions to penicillin
Term
glycopeptides
Definition
vancomycin

gram (+) activity only except VRE

oral vancomycin used for severe C. diff colitis

targeting troughs of 15-20 for invasive MRSA infections

dosing usually 15-20 mg/kg IV q8-12 hours

SE:
red man syndrome - flushing, pruritis over neck and trunk; how to fix? slow the injusion plus antihistamines if needed
nephrotoxicity
ototoxicity (rare)
BMS (leukopenia and thrombocytopenia)

daptomycin (Cubicin)
NOT for pneumonia (gets in the lung but surfactant inactivates it)
mainly for MRSA skin ans MRSA bacteremia and endocarditis
monitor CPK weekly due to risk of myalgias, CPK elevation (potential additive toxicity with statins)
IV only...no PO version
bactericidal activity

quinupristin/dalfopristin (Synercid)
gram (+) activity only including VRE (only E. faecium NOT faecalis)
SE:
GI 1 2 - hyperbilirubinemia and increased liver enzymes
skin - phlebitis and pain at infusion site (give via a central line)
flu like symptoms

linezolid (Zyvox)
gram (+) activity only
some activity vs. mycobacterium including TB
used for skin infections, pneumonia, not bacteremia
oral dosage form (100% bioavailable)
SE:
GI 2
BMS R W T - thrombocytopenia is the more important one (risk increases after 2 weeks of therapy!)
other: peripheral neuropathy; lactic acidosis; optic neuritis
drug interactions: it is a weak MAOI; SSRIs, tyramine containing foods, venlafaxine, etc.
Term
ceftaroline (Teflaro
Definition
only anti-MRSA cephalosproin

has littel gram (-) activity; no enterococcus activity

bacteriidal: used for skin/soft tissue infections and CAP (MRSA was excluded)
Term
aminoglycosides
Definition
gram (-) agents including Pseudomonas but used with other agents for gram (+) synergy (endocarditis with enterococcus b/c vancomycin or ampicillin by themselves not cidal, with aminoglycosides becomes cidal)

concentration dependent killers
single daily dosing vs. traditional dosing
SDD may offer greater killing and less nephrotoxicity

SE:
nephrotoxicity!!!!!!!!!
ototoxicity both hearing and balance
neuromuscular blockade with NM blockers
Term
macrolides
Definition
erythromycin (not really used except for GI motility)
clarithromycin (Biaxin): H. pylori; tastes like metal; peds suspension keep at room temp

azithromycin (Zithromax): 5 day dosing due to very long tissue t1/2 of about 60 hours

used for respiratory infections and for STI (Chlamydia - 1 gram)

watch for drug interactions with erythromycin and clarithromycin (stron 3A4 inhibitors)
Term
tetracyclines
Definition
tetracycline (not the best)

doxycycline - better tolerated

minocycline - better toleraged

used primarily in MRSA uncomplicated skin/skin structure infections

not great activity vs. Strep species

avoid in pregnancy and in kids < 8 years old (discolors teeth)

drug interactions: cations can bind tetracycline products
Term
clindamycin (Cleocin)
Definition
gram (+) coverage including gram (+) anaerobes

used for gram (+) anaerobes above the diaphragm (metronidazole for anaerobes below the diaphragm)

IV dose is more than PO dose

used in toxic shock with Strep to shut toxin production down (protein synthesis inhibitor)
Term
trim/sulfa
Definition
used clinically for UTIs (E. coli), Pneumocystis infection or prophy, MRSA skin abscess, Stenotrophomonas

dose based on trimethoprim component

doses are hight for Pneumocycstis (15-20 mg/kg/day)

SE:
GI 1 2
BMS W T R
electrolytes: hyperkalemia
Derm - rash including SJS or TEN

counsel patients on photosensitivity

bad drug with warfarin

be careful with G6PD deficiency

falsely increases SrCr (competes for active tubular secretion)

kernicterus (avoid in newborns or 3rd trimester)
Term
metronidazole (Flagyl)
Definition
great activity against anaerobes and (C. difficile (mild-moderage disease) and Trichomonas vaginalis (2 g x 1)

used in Chron's disease as an anti-inflammatory

SE:
GI 2 - metallic taste; disulfiram reaction with ETOH
neuro - peripheral neuropathy
Term
nitrofurantoin (Macrodantin - QID; Macrobid - BID)
Definition
only for uncomplicated UTIS, not for pyelonephritis; cystitis only

SE:
GI 2
CI in CrCl < 60 mL/min
increased hemolytic anemia in G6PD deficiency

peripheral neuropathy and pulmonary toxicity
Term
fosfomycin (Monurol)
Definition
dose: 3 g single dose sachet dissolved in water

similar to nitrofurantoin only for cystitis

SE: GI 2
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