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201 Cards in this Set

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What is the first line treatment for essential HTN in general population?
diuretics
First line tx for CHF?

what is contraindicated in decompensated CHF?
ACE inhibitors/ARBs

beta blockers
antihypertensive therapy for diabetic pts? why?
ACE inhibitors b/c they are protective against diabetic nephropathy
first line tx for isolated systolic HTN in general population?

how about in diabetics?
general population: thiazide or dihydropydridine (Amlodipine, Nifedipine)

diabetics: ARBs/ ACE inhibitors
first line tx for HTN in pregnancy?
Hydralazine with methyldopa
Hydralazine

MOA?
toxicity?
cGMP increases --> smooth muscle relaxation
vasodilates arteries > veins

compensatory tachycardia (contraindicated in angina/CAD), headache, lupus-like syndrome
List 2 classes of Ca channel blockers.

How are their actions different?
dihydropyridine (Amlodipine, Nifedipine); more action on smooth muscle (arteriole > veins)

non-dihydropyridine (verapamil, diltiazem): more action on heart, better for arrhthmias
which calcium channel blocker is most specific to heart tissues?

toxicity?
verapamil (non-dihydropyridine)

AV block
Nitroglycerin, isosorbide dinitrate

MOA?
toxicity?
dilate VEINS >> arteries -> decrease preload by releasing NO to smooth muscle

reflex tachycardia, hypotension, headache
What is Monday disease?

what substance is it associated with?
nitrate exposed in industrial environemnt

development of tolerance for vasodilatng action during the work week and loss of tolerance over the weekend, resulting in tachycardia, dizziness, and headache on reexposure
list 3 drug used in malignant hypertension and their MOA
Nitroprusside: increase cGMP via direct release of NO

Fenoldopam: D1 agonist; relaxes renal vascular smooth muscle

Diazoxide: K+ channel opener
Nitroprusside

indication
toxicity
malignant htn

can cause cyanide toxicity
diazoxide

indication
toxicity
malignant HTN

can cause hyperglycemia (reduces insulin release)
list 2 beta antagonists contraindicated for angina. why?
pindolol and acebutolol

partial beta agonists
HMG-CoA reductase inhibitors

side effects (4)
hepaptotoxicity (increase LFTs)
rhabdomyolysis
myopathy
teratogenic
Niacin

MOA
toxicities
MOA:
inhibits lipolysis in adipose tissue
reduces hepatic VLDL secretion into circulation

toxicities:
red, flushed face, which is decreased by aspirin or long-term use
Hyperglycemia (acanthosis nigricans)
Hyperuricemia (exacerbate gout)
hepatitis
2 lipid lowering agents that can form cholesterol gallstones.
bile acid resins (cholestyramine, colestipol, colesevelam)

fibrates (gemfibrozil, clofibrate, bezafibrate, fenofibrate)
fibrates

MOA
toxicities
upregulate LPL -> increase TG clearance

myositis, hepatotoxicity, cholesterol gallstones
Digoxin

MOA
clinical use
direct inhibition of Na/K pump -> inhibition of Ca/Na exchange -> increased intracellular Ca -> positive ionotropy

also stimulates VAGUS nerve

used in CHF and atrial fib
How do you treat Atrial Flutter?
Class IA, IC, or III antiarrhythmics
Digoxin

toxicities
cholinergic: nausea, vomiting, diarrhea, blurry yellow vision (think Van Gogh)

arrhthymia, hyperkalemia
Digoxin

antidote
slowly normalize K+, lidocaine, cardiac pacer, anti-dig Fab framgments, Mg+
General MOA of class I Antiarrhytmics?
Na channel blockers

slow or block conduction
decrease slope of phase 0 depolarization
increase threshold for firing in abnormal pacemaker cells
are state dependent (selectively depress tissue that is frequently depolarzied, e.g. fast tachycardia)
list 3 Class IA antiarrhtymics

MOA?
"the Queen Proclaims Diso's pyramid"
Quinidine, Procainamide, Disopyramide

increase AP duration, increased effective refractory period, increase QT interval
Quinidine

what class antiarrhythmics?
toxicities?
class IA

Cinchonism: headache, tinnitus, thrombocytopenia
torsades de pointes due to increased QT interval
procainamide

what class antiarrhytmics?
toxicity?
class IA

reversible SLE-like syndrome and torsade de pointe
Indication for class IA antiarrhythmics.
Quinidine, procainamide, Disopyramide

indicated for atrial and ventricular arrhythmias, esp reentrant and ectopic supraventricular and ventricular tachycardia
Class IB antiarrhythmics

List 3.
indication?
"I'd Buy Lidy's Mexican Tacos"
Lidocaine, Mexiletine, Tocainide

useful in acute ventricular arrhythmias (esp post-MI) and in digitalis-induced arrhythmias
Class IC antiarrhythmics

List 3.
Indications?
"Chipotle's Food has Excellent Produce"
Flecainide, Encainide, Propafenone

Useful for V-tachs that progress to VF and in intractable SVT. Usually used only as last resort in refractory tachyarrhthmias. For pts w/o structural abnormalities
Class IC antiarrhythmics

contraindications?
toxicities?
contraindicated in post-MI

proarrhythmic
significantly prolongs refractory period in AV node
List class II antiarrhythmics. (5)
beta blockers
Propranolol
timolol
Esmolol
metoprolol
atenolol
What is a short acting class II antiarrhythmic?
esmolol
Class II antiarrhythmics

MOA
beta blockers
decrease cAMP, Ca current
suppress abnormal pacemakers by decreasing slope of phase 4.
Clinical use for class II antiarrythmics?
V-tach, SVT, slowing ventricular rate during a-fib and a flutter
What metabolic toxicity do class II antiarrhythmics have?

tx?
may mask the signs of hypoglycemia (beta 1: adrenergic signs; beta 2: metabolic changes)

Metoprolol can cause dyslipidemia

tx overdose with glucagon
List 5 Class III antiarrhythmics

MOA?
K+ channel blockers:
Sotalol, ibutilide, bretylium, dofetilide, amiodarone

increase AP duration, ERP, QT interval (like Ia). used when other antiarrhythmics fail
Sotalol, ibutilide

class?
toxicities?
class III antiarrhythmic

both: torsades de pointes
Sotalol: excessive beta block
amiodarone

class?
toxicities?
Class III antiarrhythmic

pumonary fibrosis, hepatotoxicity, hypothyroidism/hyperthyroidism

Remember to check PFTs, LFTs, TFTs when using amiodarone
What Ca channel blocker is used in isolated systolic HTN?
amlodipine
list 2 class IV antiarrhythmics.

target tissue?
MOA?
Verapamil, diltiazem

primarily affect AV nodal cells.
Decrease conduction velocity, increase ERP, PR interval
Drug of choice in diagnosing/abolishing supraventricular tachycardia?

how do you block this drug?
Adenosine

very short acting
effects blocked by theophylline
What ion is used to stop torsades pointes and digoxin toxicity?
Mg++
What drugs are K+-channel openers (for cardio)
Minoxidil (for severe HTN) and diazoxide (for malignant HTN)
What is a side effect of diazoxide that is clinically significant
hyperglycemia (reduces insulin release by opening the K+ channels)
What are nitroglycerin, isosorbide dinitrate used for
angina, pulmonary edema
What is the main effects of these drugs:

statins
Niacin
Fibrates
Statins: decrease LDL
Niacin: increase HDL
Fibrates: decrease triglycerides
What lipid-lowering agent causes decrease absorption of fat-soluble vitamins
bile acid resins (cholestyramine)
What drug increases digoxin toxicity
quinidine
displaces digoxin from tissue-binding sites
What drug has a reversible SLE-like syndrome
"HIPP"
Hydralazine has a lupus-like syndrome
INH
Procainamide (Class IA antiarrhythmic)
Phenytoin
What class of antiarrhythmics are useful in digitalis-induced arrhythmias
Class IB
What is a toxicity of all Class 1 antiarrthythmic drugs
hyperkalemia
drugs used to prevent nodal arrhythmias
Ca channel blockers
What is the drug of choice in stopping/diagnosing SVT
Adenosine

(effects blocked by theophylline)
How does K+ act as an antiarrhythmic
depresses ectopic pacemakers in hypokalemia (like in digoxin toxicity)
List 5 classes of drugs used in glaucoma
1. alpha agonists (epi and brimonidine)
2. beta blockers
3. Acetazolamide
4. Cholinomimetics
5. Prostaglandin: Latanoprost
Brimonidine

MOA?
Indication?
alpha2 agonist
decrease aqueous humor synthesis
what drug is indicated in Emergency glaucoma?

MOA?
Pilocarpine (direct cholinomimetic)

contract ciliary muscle and open trabecular meshwork
Methadone

MOA?
Indication? why?
agonist at opioid mu receptor and opens K+ channels and close Cl- channels -> decrease synaptic tranmission

indicated for maintenance programs for addicts b/c it has a long half-life, which suppresses the withdrawal sxs and reduces risks of addiction
Morphine

toxicity?
what sxs do not develop tolerance?
addiction, respiratory depression, additive CNS depression wither other drugs, miosis, constipation

Miosis and constipation do not develop tolerance
Tramadol

class/MOA?
toxicity?
very weak opioid agonist; SNRI

decreases seizure threshold
Phenytoin

MOA?
indication?
toxicity?
increases Na channel inactivation

indicated for seizures; first line for tonic-clonic and status epilepticus prophylaxis

Gingival hyperplasia, megaloblastic anemia, fetal hydantoin syndorme, SLE-like syndrome, induction of cytochrome P450
1st line tx for status elipticus prophylaxis
phenytoin
1st line tx for acute sxs of status epilepticus
Diazepam and lorazepam
1st line tx for absence seizure
MOA?
Ethosuximide

blocks thalamic T type Ca channels
1st line tx for tonic-clonic generalized seizure (3)
Phenytoin
Valproic acid
Carbamazepine
First line tx for trigeminal neuralgia.
carbamazepine
first line tx for seizures in pregnant women and children
phenobarbital
first line tx to prevent seizures of eclampsia
MgSO4
Carbamazepine

class/MOA?
toxicity?
anti-seizure medication; increases inactivation of Na channels

agranulocytosis, aplastic anemia, teratogenesis, induction of P450, SIADH, Stevens-Johnson syndrome
List anti-seizure medications associated with Stevens-Johnson syndrome.

What is Stevens-Johnson syndrome?
Carbamazepine, Ethosuximide, lamotrigine

SJ syndrome: allergic rxn to the drugs; prodrome of malaise and fever followed by rapid onset of erythematous/purpuric macules (oral, ocular, genital). Skin lesions progress to epidermal necrosis and sloughing
Valproic acid

toxicity?
rare but fetal hepatotoxicity, spina bifida in fetus (by inhibiting intestinal absorption of folate)

contraindicated in pregnancy
Barbiturates

MOA?
toxicity?
contraindication?
facilitate GABAa axn by increasing the DURATION of Cl- channel opening, thus decreasing the neuron firing

additive CNS depression with EtOH, respiratory or CV depression, P450 induction

contraindicated in porphyria
Benzodiazepines

MOA?
Advantage over barbiturates?
facilitate GABAa axn by increasing frequency of Cl channel opening. Decreased REM sleep

less risk of respiratory depression and coma than with barbiturates
what drug is used for detoxification, esp EtOH withdrawal?
long acting benzo: diazepam and chlordiazepoxide
list 3 short-acting benzodiazepines.

side effect?
TOM Thumb
Tirazolam
Oxazepam
Midazolam

highly addictive
how do you tx overdose of benzodiazepine?
flumazenil: competitive antagonist at GABA receptor
N2O as inhaled anesthetic

induction rate?
potency?
toxicity?
low blood solubility -> fast induction
low lipid solublity -> low potency

expansion of trapped gas
Halothane as inhaled anesthetic

induction rate?
potency?
toxicity?
high blood solubility -> slow induction
high lipid solubility -> high potency

hepatotoxicity
how is potency measures?

how does AV concentration gradient related to onset of action?
potency = 1/ MAC
MAC: minimum alveolar conc at which 50% of population of anesthesized

high AV conc gradient = high solubility = more gas required to saturate tissue = SLOWER onset of action
Thiopental

class?
indication? why?
barbiturate

used for induction of anesthesia b/c it has high potency, high lipid solubility, rapid entry into brain
what is the most common anesthetic used for endoscopy?
Midazolam (benzodiazepine)
What anesthetic acts as dissociative anesthetics and causes disorientation, hallucination and bad dreams?
Ketamine (arycyclohexylamines)

A PCP analog; blocks NMDA receptors, CV stimulant
Propofol

MOA?
indication?
potentiate GABAa

for rapid anesthesia induction and short procedures
List 2 classes of local anesthetics.
Esters: procaine, cocaine, tetracaine

Amides (2 I's in the name): Lidocaine, mepivacaine, bupivavaine
tx for anorexia/bulimia
SSRIs
In what situation do you need to apply more local anesthetics to achieve the same result?
in infected (acidic) wound b/c alkaline anesthetics are charged and cannot penetrate membrane effectively
What drug intoxication is associated with pinpoint pupils? (1)

What drug intoxication is associated with dilated pupils? (4)
pinpoint pupils (constricted): opioids

dilated pupils: amphetamines, cocaine, LSD, Opioid withdrawal
What drug is co-administered to increase the effect of local anesthetics?

exception?
epinephrine to enhance local vasoconstriction

except for cocaine
List sxs of opioid intoxication.

tx?
CNS depression, nausea, and vomiting, constipation, pupil constriction, seizures (life-threatening)

tx: naloxone, naltrexone
Which sensation is blocked first with local anesthetics? last?
Pain (first) > temperature > touch > pressure (last)

small-diameter, and myelinated fibers are affected first. Size predominates over myelination
List sxs of alcohol withdrawal.

tx?
tremor, tachycardia, HTN, malaise, nausea, seizures, delirum tremens, tremulousness, agitation, hallucinations (including tactile)

tx: chlordiazepoxide, diazepam
succinycholine

class/MOA?
indications?
toxicity?
depolarizng neuromuscular (nicotinic) blocker

indicated for muscle paralysis in surgery or mechanical ventilation

complications: hypercalcemia and hyperkalemia
irreversible during depolarizing phase
List sxs of PCP intoxication.
BELLIGERENCE, impulsiveness, fever, psychomotor agitation, vertical and horizontal nystagmus, tachycadia, ataxia, homicidality, psychosis, delirium
Tubocurarine, pancuronium

class/MOA?
indication?
reversal of action?
nondepolarzing neuromuscular blocker (nicotinic receptor)

indicated for muscle paralysis in surgery or mechanical ventilation

reversal by cholinesterase inhibitors (neostigmine, edrophonium)
List sxs of LSD intoxication
marked anxiety or depression, delusions, visual hallucinations, FLASHBACKS, pupillary dilation
Malignant hyperthermia

cause?
tx?
caused by inhalation of anesthetics (except N2O) and succinycholine

treat with dantrolene
What are 2 most immediate sxs of smoking marijuana?
conjunctival injection (red eye), tachycardia
List drugs used in Parkinson's. (5)
BALSA
1. Bromocriptine: agonize DA receptors
2. Amatadine: increase DA
3. Levodopa (with carbidopa): act as DA
4. Selegiline: MAO B inhibitor; prevent breakdown of DA
5. Antimuscarinic (Benztropine): curb excess cholinergic activity
Suboxone

indication?
MOA?
advantage over the alternative?
for tx of heroin addiction

naloxone + buprenorphine (partial agonist); long acting with fewer withdrawal sxs than methadone.

Naloxone is not active when taken orally, so withdrwal sxs can occur only if injected (lower abuse potential)
List 2 phenomenon observed with long-term Parkinson's therapy.
On-off phenomenon

wearing off phenomenon
Delirum tremens (DT)

what is it?
sxs?
tx?
life-threatening alcohol withdrawal syndrome that peaks 2-5 days after last drink.

sxs in order of appearance: autonomic system hyperactivity (tachycardia, tremors, anxiety, seizures), psychotic sxs (hallucinations, delusions), confusion

tx: benzodiazepines
Benztropine

MOA
indication
muscarinic antagonist

Used in Parkinson's: improves tremor and rigidity but has little effect on bradykinesia
Antipsychotics

List high potent neuroleptics.

List low potent neuroleptics
typical antipsychotics; haloperidol + -azines

high potent (neurologic side effects): haloperidol, trifluoperazine, fluphenazine

low potent (non-neurologic side effects): thioridazine, chlorpromazine
What is co-administered with L-dopa? why?
carbidopa to prevent peripheral conversion of L-dopa to DA, which can cause arrhythmia and decreased the bioavailability in the brain
toxicities of antipsychotics (6)
1. lipid soluble -> stored in fat -> slow metabolism
2. EPS side effects
3. hyperprolactinemia -> galactorrhea
4. block muscarinic (dry mouth, constipation)
5. block alpha (hypotension)
6. block histamine (sedation)
Selegiline

MOA?
indication?
MAO-B inhibitor (MAO-B selective degrades DA over NE and 5HT)

adjunctive to L-dopa in tx of Parkinson's
special toxicity of Chlorpromazine and thioridazine

their class?
common side effects?
both are short-acting typical antipsychotics
greater anti-cholinergic (dry mouth, constipation), anti-histamine (sedation), and anti-alpha (hypotension) but NO NEUROLOGICAL SIDE EFFECTS (e.g. EPS sxs)

Chlorpromazine: Corneal deposits
Thioridazine: reTinal deposits
Tx strategy for Huntington's
Huntington's is characterized by increased DA and decreased GABA + Ach

Reserpine + tetrabenazine: amine depleting (decrease DA)

Haloperidol: DA receptor antagonist
Evolution of EPS side effects with antipsychotics.
4 hr acute dystonia (muscle spasm, stiffness, oculogyric crisis)
4 day akinesia (parksonian sxs)
4 wk akathisia (restlessness)
4 mo tardive dyskinesia (steretypic oral-facial mvmt); irreversible
Sumatriptan

MOA?
indication?
toxicity?
5-HT1b/1d agonist
causes vasoconstriction, inhibition of CN V activation and vasoactive peptide release

used in acute migraine and cluster headache

toxicity: coronary vasospasm and mild tingling
Neuroleptic malignant syndrome (NMS)

cause?
sxs?
tx?
caused by antipsychotics

sxs: think FEVER
Fever
Encephalopathy
Vitals unstable (autonomic instability)
Elevated enzymes
Rigidity for muscles (myoglobinuria)

tx: dantrolene, DA agonists (e.g. bromocriptine)
memantine

MOA?
indication?
NMDA receptor antagonist; helps prevent excitotoxicity

used in Alzheimer's drugs
List atypical antipsychotics.
it's atypical for Old CLOsets to QUIETly RISPER from A to Z

Olanzapine
Clozapine
Quetiapine
Risperidone
Aripiprazole
Ziprasidone
Olazapine

class/MOA?
indication?
adverse effect?
atypical antipsychotics
blocks 5HT2, alpha, H1, and DA receptors

used for schizophrenia (+ and - sxs), OCD

weight gain
Clozapine

class?
toxicity?
atypical antipsychotic

weight gain
agranulocytosis (requires weekly WBC monitoring)
Lithium

indication?
mood stabilizer for bipolar disorder, also SIADH
Lithium toxicity
LMNOP
Lithium side effects:
Movement (tremor)
Nephrogenic DI
hypOthyroidism
Pregnancy problems: Ebstein anomaly
List drugs that increase serum Lithium level and increase proximal tubular Na absorption.
NSAIDs, thiazide, ACE inhibitors
Buspirone

MOA?
indication?
advantage over alternatives?
5HT1a agonist

used in generalized anxiety disorder.

Minimal hypnotic effects, addiction, or tolerance. Does not interact with alcohol (vs barbiturates, Benzodiazepine)
imiprimine, amitriptyline, desipramine, nortriptyline, clomipramine, doxepin, amoxapine

class?
indication?
TCA

major depression, bedwetting (imipramine), OCD (clomipramine), fibromyalgia
List 3 major toxicities of TCA.
how do you treat one of the toxicities?
tri-C's
Convulsion, Coma, Cardiotoxicity

NaHCO3 for CV toxicity
what TCA is preferred in the elderly? why?
Nortriptyline (secondary TCA)

less anticholinergic effect -> decrease in confusion and hallucinations (anticholinergic side effects)
Fluxetine, paroxetine, sertraline, citalopram

class?
indications?
SSRIs

depression, OCD, bulimia, social phobia
List main toxicities of SSRIs.
GI distress, sexual dysfxn (anorgasmia), serotonin syndrome
What is serotonin syndrome? what drugs are associated?
associated with any drug that increase 5HT: SSRIs, SNRIs, MAO inhibitors

sxs: hyperthermia, muscle rigidity, CV collapse, flushing diarrhea, seizures.
tx for serotonin syndrome?
cyproheptadine (5HT2 receptor antagonists)
Venlafaxine, duloxetine

class?
indications?
SNRIs

depression
Venlafaxine: also used for generalized anxiety disorder
duloxetine: also used for DM peripheral neuropathy
Phenelzine, tranylcypromine, isocarboxazid

class?
indications?
nonselective MAO inhibitors: increase amine NTs (NE, 5HT, DA)

atypical depression, anxiety, hypochodriasis
Selegiline

class?
indication?
selective MAO-B inhibitor

used in Parkinson's disease in conjunction to L-dopa
Phenelzine, tranylcypromine, isocarboxazid

toxicity?
hypertensive crisis with tyramine ingestion (in foods such as wine and cheese) and beta agonists.
CNS stimulation
can cause serotonin syndrome with SSRIs or meperidine
hypertensive crisis

causative drug?
MAO inhibitors with tyramine or Beta agonists
What 2 drugs are contraindicated with MAO inhibitor administration. why?
SSRI and meperidine

can cause serotonin syndrome
what drug is indicated in pts with depression that do not want sexual dysfunction?
Bupropion (Wellbutrin)
Mirtazapine

MOA?
indication?
alpha2 antagonist (relealse NE and 5HT), 5HT2 and 5HT3 antagonists.

for depression with insomnia
Trazodone

MOA?
indication?
toxicity?
inhibits 5HT reuptake
used for insomnia, as high doses are needed for antidepressant effects.

TrazoBONE; causes priapism
List tx options for following psychiatric conditions.

Alcohol withdrawal
long acting benzodiazepine: Diazepam, Chlordiazepoxide
List tx options for following psychiatric conditions.

anorexia/bulimia
SSRIs
List tx options for following psychiatric conditions.

Anxiety
Benzodiazepines
Buspirone
SSRIs
List tx options for following psychiatric conditions.

ADHD
Methylphenidate (ritaline)
Amphetamines (dexedrine)
List tx options for following psychiatric conditions.

Atypical depression
MAO inhibitors
SSRIs
List tx options for following psychiatric conditions.

Bipolar disorder
"mood stabilizers": Lithium, Valproic acid, Carbamazepine

Atypical antipsychotics
List tx options for following psychiatric conditions.

Depression
SSRIs
SNRIs
TCAs
List tx options for following psychiatric conditions.

Depression with insomnia
Mirtazapine
List tx options for following psychiatric conditions.

Obsessive-compulsive disorder
SSRIs
Clomipramine
List tx options for following psychiatric conditions.

Panic disorder
SSRIs
TCAs
Benzodiazepines
List tx options for following psychiatric conditions.

PTSD
SSRIs
List tx options for following psychiatric conditions.

Schizophrenia
Antipsychotics
List tx options for following psychiatric conditions.

Tourette's syndrome
Antipsychotics (haloperidol)
List tx options for following psychiatric conditions.

Social phobias
SSRIs
List beta lactams.

MOA?
Penicillin
Methicillin
Ampicillin
Ticarcilln, pipercillin
Cephalosporins
Aztreonam
Imipenem

blocks peptidoglycan cross-linking
List 30S inhibitors
AT

Aminoglcosides: Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin ("GNATS")

Tetracycline (all the"-cyclines")
List 50S inhibitors.

What is the common feature?
Macrolides: Erythromycin, azithromycin, clarithrymycin

Chloramphenicol
Clindamycin

all are bacteriostatic
What antibiotic blocks DNA topoisomerases?

blocks mRNA synthesis?
Flouroquinolones: blocks topoisomerase II

Rifampin: blocks mRNA synthesis
Methicillin, nafcilin

spectrum?
toxicity?
a beta lactamase resistant

Staph aureus except MRSA

toxicity: interstitial nephritis
Ampicillin

adjunctive therapy?
indication?
combine with clavulanic acid (penicillinase inhibitor) to enhance spectrum

Gram positives + gram negative rods (HELPS)
Haemophilus influezae
E coli
Listeria
Proteus
Salmonella
Enterococci
list 3 antipseudomonals

adjunctive therapy?
Take Care of Pseudomonas

Ticarcillin
Carbenicillin
Piperacillin

adjunct with clavulanic acid (penicillinase inhibitor)
1st generation cephalosporin

2 prototypes?
specturm?
Cefazolin, cephalexin

gram+ and "PEcK"
Proteus
E coli
Klebsiella
2nd generation cephalosporin

3 prototypes?
spectrum?
cefoxitin, cefaclor, cefuroxime

gram + and "HEN PEcKS"
Haemophilus
Enterobacter aerogenes
Neisseria spp.
Proteus
E coli
Klebsiella
Serratia marcescens
3rd generation cephalosporin

3 prototypes?
spectrum?
ceftriaxone, cefotaxime, ceftazidime

serious gram-negative infections resistant to other beta-lactams; meningitis (most penetrate BBB)
Aztreonam

spectrum?
indication?
gram negative rods: Klebsiella, Pseudomonas, Serratia
NO activity against gram positives or anaerobes

for penicillin-allergic pts and those with renal insufficiency who cannot tolerate aminoglycosides
Imipenem

MOA?
adjunctive therapy?
B-lactamse resistant carbapenem

always administered with cilastatin (inhibitor of renal dihydropeptidase I) to decrease inactivation in renal tubules
Imipenem

indication?
side effects?
better alternative?
drug of choice for Enterobacter
causes seizures, GI stress, skin rash

Meropenum has a reduced risk of seizures and is stable for dihydropeptidase I
Vancomycin

MOA?
toxicity?
resistance?
blocks D-ala D-ala cell wall mucopeptide formation

NOT
Nephrotoxicity
Ototoxicity
Thrombophlebitis
diffusing flushing (red man syndrome; due to non-specific mast cell degranulation; NOT IgE-mediated)

resistance develops when mucopeptide changes to D-ala D-lac
Aminoglycosides

requirement?
indication?
toxicity?
require O2 uptake (ineffective against anaerobes)

severe gram negative rod infections

NOT
Nephrotoxicity
Ototoxicity
Teratogen (CN VIII toxicity)
Tetracycline

special direction for administration?
toxicity?
must NOT take with milk, antacids, or Fe-containing preps b/c divalent cations inhibit its absorption in the gut

discoloration of teeth and inhibition of bone growth in children
photosensitivity
contraindicated in pregnancy
Doxycycline

class?
indicaiton?
a tetracycline (30s inhibitor)

fecally eliminated so indicated for pts with renal failure
Erythromycin

MOA?
toxicity?
blocking translocation by binding to 23S rRNA of the 50S ribosomal subunit.

prolonged QT interval
Chloramphenicol

indication?
toxicities?
menigitis (H. influenzae, Neisseria m. strep pneumoniae)

Anemia, aplastic anemia
Gray baby syndrome (in premature infants b/c lack live UDP-glucoronyl transferase)
Clindamycin

indication?
toxicity?
treat anaerobic infections

pseudomembranous colitis (C. difficile overgorwth)
Sulfamethoxazole

MOA?
toxicity?
PABA antimetabolites inhibit dihydropterate synthase --> decreased THF

hemolysis in G6PD deficient
kernicterus in infants
displace other drugs from albumin
Trimethoprim

MOA?
toxicity?
inhibit bacterial dihydrofolate reductase

megaloblastic anemia, leukopenia, granulocytopenia
Ciprofloxacin

class and MOA?
toxicity?
a flouroquinolone
inhibit DNA gyrase (topoisomerase II)

damage cartilage (contraindicated in pregnant women and children)
tendonitis and tendon rupture in adults
Metronidazole

MOA?
indication?
toxicity?
toxic metabolites in bacterial cell that damage DNA

GET CAP on the Metro
Giardia
Entamoeba
Trichomonas
Gardnerella vaginalis
Anaerobes (bacteroides, Clostridium)
H. Pylori

disulfiram-like rxn with alcohol; headache, metallic taste
polymyxins

MOA?
clinical use?
disrupts cell membrnae

for resistant gram-negative infections
List 5 anti-TB drugs and their toxicity.
INH-SPiRE
INH (Isoniazid)
Streptomycin
Pyrazinamide
Rifampin
Ethambutol: red-green color blindness

all others cause hepatotoxicity
prophylactic tx for M. tuberculosis

prophylactic tx for M avium-intracellulare?
MTb: Isoniazid

M. Avium-intracellulare: Azithromycin
INH (Isoniazid)

MOA?
toxicity?
metabolism?
decreased synthesis of mycolic acid

neurotoxicity (prevent with vit B6) and hepatotoxicty

Bimodal distribution of metabolism due to different INH half-lives in fast vs slow acetylators
Rifampin

MOA?
Toxicity?
4 R's
RNA polymerase inhibitor
Revs up microsomal p450
Red/orange body fluids
Rapid resistance if used alone
prophylactic tx for menigococcal infection?
Rifampin
Prophylactic tx for Pneumocystis jiroveci pneumonia?
TMP-SMX
Treament for MRSA?

Treament for VRE?
MRSA: vancomycin

VRE: linezolid and streptogramins
Amphotericin B

MOA?
toxicity?
binds ergosterol --> pore formation

Nephrotoxicity (reduced with hydration)
arrhythmias due to hypokalemia and hypomagnesia
Nystatin

MOA?
clinical use?
binds to ergosterol

for oral candidiasis (thrush)
topical for diaper rash or vaginal candidiasis
Azoles

MOA?
toxicity?
inhibit fungal ergosterol synthesis
hormone synthesis inhibition (gynecomastia), liver dysfxn
what drug is used to tx cryptococcal meningitis in AIDS pts?
Fluconazole

can cross BBB
Caspofungin

MOA?
clinical use?
inhibit beta-glucan --> inhibit cell wall synthesis of fungus

invasive aspergillosis
Terbinafine

MOA?
clinical use?
inhibit fungal enzyme squalene epoxidase

used to tx dermatophytoses (especially onychomycosis)
Amantadine

MOA?
clincal use?
blocks viral penetration/uncoating (M2 protein)
also causes the release of DA from intact nerve terminals

prophylactic tx for influenza A
Parkinson's disease
Amantadine vs Rimantidine

compare
both block viral uncoating (M2 protein)

Rimantidine does not cross BBB, so fewer CNS side effects

Amantadine causes cerebellar problems (ataxia, dizziness, slurred speech)
what 2 drugs inhibit influenza neuraminidase?
Zanamivir, oseltamivir
Acyclovir

clinical use?
MOA?
Requirement?
for HSV, VZV, EBV

monophosphorylated by HSV/VZV thymidine kinase. Guanosine analog --> inhibit viral DNA polymerase
Ganciclovir

clinical use?
MOA?
Requirement?
for CMV, esp. immunocompromised pts

Guianosine analog --> inhibit viral DNA polymerase
activated by CMV kinase or HSV/VZV thymidine kinase
Which one is more toxic: Acyclovir or Ganciclovir?
Ganciclovir (leukopenia, neutropenia, thrombocytopenia,and renal toxicity)
Foscarnet

MOA?
Clinical use?
viral DNA polymerase inhibitor; does not require activation by viral kinase

CMV retinitis in immunocompromised pts when ganciclovir fails
in acyclovir-resistant HSV
Protease inhibitor

common postfix?
toxicity?
all end in -navir; e.g. Squinavir, indinavir

hyperglycemia, lipodystrophy (sunken cheeks and buffalo humps)
thrombocytopenia (indinavir)
Enfuvirtide

MOA?
fusion inhibitor by binding to viral gp41 subunit
Zidovudine

MOA?
toxicity?
nucleosides reverse transcriptase inhibitors

lactic acidosis
megalobalstic anemia
HAART

indication?
highly active antiretroviral therapy

initiated when pts have low CD4 counts (< 500) or high viral load.
also used as prophylactic tx in general population and during pregnancy
Nevirapine, Efavirenz, Delavirdine

class?
non-nucleoside reverse transcriptase inhibitor used in HIV therapy
List antibiotics to avoid in pregnancy (9).
SAFE Moms Take Really Good Care

Sulfonamides: kernicterus
Aminoglycosides: ototoxicity
Fluoroquinolone: cartilage damage
Erythromycin: acute cholestatic hepatitis in mom (and clarithromycin is embryotoxic)
Metronidazole: mutagenesis
Tetracycline: discolored teeth, inhibition of bone growth
Ribavirin: teratogenic
Griseofulvin: teratogenic
Chloramphenicol: gray baby syndrome
Rifampin

clinical use?
1. Mtb (must use with other agents such as INH, Pyrazinamide Ethambutol)
2. delays resistance to dapsone when used for leprosy
3. prophylaxis for meningococcal infection
4. chemoprophylaxis for contacts with children with Haemophilus influenzae type B