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68 Cards in this Set

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What is the MOA of fibrates?
The MOA of this drug is to stimulate LPL.
Peroxisome Proliferator Activated Receptor (PPARalpha) agonists
Common side effects of fibrates?
These side effects are associated with what drugs?

GI Symptoms
Pruritis
Rash
Rare- Acute renal failure and Rhabdomyolysis
Clofibrate can only be used in patients who...
Have no gallbladder.
This med predisposes to gallstones.
Fibrates should not be combined with ________.
Statins should not be combined with __________.
Name angiotensin receptor antagonists.
Who are these guys?

Losartan
Valsartan
Candersartan
Patients with COPD and asthma should not take_______
Non-selective B1/B2 Blockers are contraindicated in what patients?
Alpha-2 receptor stimulant
What does Clonidine do?
Name an Alpha-2 receptor inhibitor.
What does Yohimbine do?
Name the Class I Na Channel Blockers.
Who are these guys?

IA Quinidine, Procainimide, Disopyramide
IB Lidocaine, Tocainide,Mexilitine
IC Flecainide, Encainide
B-Blockers for CHF
These are the _____ used in _____.

Carvdilol
Metoprolol
Aldosterone Antagonists
Spironolactone
Eplerenone
What meds should not be prescribed with B-Blockers?
Verapamil
Beperidil
Diltiazem
(Ca channel blockers that cause heart failure or AV Block)
What meds would you use for unstable angina?
Aspirin (stable also)
Heparin
Abciximab
Tirofiban
Statins
What are the major side effects of Ca Channel Blockers?
reflex tachycardia
headache
edema (ankle/general)
Nitrates are contraindicated in patients taking what?
Phosphodiesterase (PDE) Inhibitors like sildenifil or tadalafil for erectile dysfunction.
Which vasodilator can actually WORSEN angina?
Dipyridamole because it does not dilate collateral arteries to increase amount of blood flow.
What is the MOA of organic nitrates?
Bypass the endothelial cell production of NO and go straight to relaxation of sm. muscle (vasodilate).

NO stim GP => stim GTP => cGMP => relaxation
Name the B-Adrenoceptor antagonists used in angina.
NS Propanolol, Pindolol
B1S Metoprolol, Atenolol
Name the muscarinic agonists.
Ach
Carbechol
Methacholine
Bethdanechol
Pilocarpine
Oxotremorine
*
Anticholinesterases are often used to treat _________. Name them.
Myasthenia Gravis

Edrophorium
Neostigmine
Physostigmine
Pyridostigmine
Dyflos
Ecothiopate
Parathion
Glaucoma is treated with which med?
Pilocarpine
What are the major side effects of muscarinic antagonists?
Dry Mouth
Constipation
Blurred Vision
What is the difference between real and pseudo Acetylcholine Esterase?
real: degrades Ach released from nerve terminals
pseudo: removes circulating Ach
Adrenal Medulla secretes what?
What secretes Chatecholamines?
Glucuronidation, Transacetylation, Transulfonation, are examples of _______ rxn.
An example of Phase II drug biotransformation reaction is __________.
Examples of Enzymes in a Phase I reaction
Cytochrome p450
Aldehyde dehydrogenase
Alcohol dehydrogenase
Drug Excretion is usually enhanced by a drug being what?
Highly ionized
Therapeutic Index of a drug is what ratio?
TD50/TE50
Clinical use as an inhalant for asthma/bronchitis.
Ipratropium
Atropine
Atropine Methonitrate
Scopolomine
Used for gastrointestinal hypermotility.

Add motion sickness for one.
Which meds are used for ophthalmic production of mydriasis.
Tropicamide
Cyclopentolate
Pirenzipine is used for what? It is selective for what receptors?
Used for peptic ulcers (inhibits gastric secretions) and is selective for M1 receptors.
What drugs inhibit Ach release (act presynaptically)?
Aminoglycosides
(streptomycin/neomycin, also inhibit Ca release)
Botulinum Toxin
Bungarotoxin
Net transfer of drug during passive diffusion is directly proportional to what in drug absorption?
Concentration gradient and lipid:water partition coefficient play a major role in what?
Pinocytosis is...
Microscopic particle engulfed by cell membrane is called...
Active transport is used to transport what?
Highly specific for naturally occurring substances such as amino acids, sugars, and vitamins.
Uncharged drugs are...
not easily absorbed by the GI tract.
The lower the pH relative to pKa, the ____ the drug is unionized, and therefore ____ lipid soluble.
More unionized drugs are more lipid soluble. What is the pH like compared to pKa?
Define Distribution.
Process by which a drug reversibly leaves the blood stream and enters the interstitium (extracellular fluid).
Volume of Distribution =
VD = amt of drug in body / plasma concentration
What is the major mechanism for drug elimination?
Drug Metabolism / Biotransformation
Enzyme Inducers like barbiturates and rifampin
ibuprofen
phenytoin
steroids
ethanol
have what effect?
What can increase the metabolism of acetominophen?
What are the effects of the following enzyme inhibitors?
Allopurinol
Cimetidine
Erythromycin
Decreased metabolism of the following is caused by what action?

Oral anticoagulants/probenicid
Benzodiazepines
Astemizole/Terfenadine
Net Renal Excretion =
Drug Filtered at Glomerulus
+
Drug Secreted by AT in kidney
-
Amount of drug passively resorbed in tubule
Excretion is...

Excretion is NOT...
The mode of elimination for drugs that are not metabolized. It is not the same as elimination. (Stupid Fuck of a professor.)
Zero Order Elimination
Occurs at a constant rate regardless of concentration.
Clearance
Volume of Plasma from which a drug is completely removed by the process of excretion or metabolism per unit time.
First Order Elimination
Rate of Elimination is proportionate to concentration.
Glucuronidation is the mode of metabolism for what drugs?
Acetominophen, Diazepam, Morphine, sulfthiazole, digoxin, and digitoxin are metabolized how?
Metabolism of Digitoxin and Cortisol is enhanced or induced enzymatically by what substances?
Phenobarbitol
Phenylbutazone
Phenytoin
Rifampin

All of these enhance what?
p450 inhibitors are ____.

p450 inducers are _____.
Tea and herb sounding things ______ p450.

Veggies, meat, and oregano ______ p450.
Bioavailability is ....
Proportion of UNCHANGED drug that reaches systemic circulation.

Affected by first pass metab, drug formulation, route of administration.
Efficacy measures...
Define it.
Intrinsic Activity is measured by _____. It is the ability of a drug, once bound to receptor, to generate a biological effect.
Agonists have both _______,
while Antagonists have only one.
Affinity and Intrinsic Activity
Fractional occupancy is measured by the equation
(AR)/R = L / (L + KD)

KD = K(-1)/K(+1)
= (A)(R)/ (AR)
= 50% of rcptrs occupied
Full/Partial Agonist based on
relative efficacey decides what?
Measure of potency, the concentration that produces 50% of a maximal response.
EC50
In competitive antagonism, the efficacy of the agonist ______ and the efficacy of the antagonist _______.
agonist efficacy stays the same and antagonist efficacy increases in what type of antagonism?
In non-competetive antagonism, the efficacy of the agonist _____ and the efficacy of the antagonist _____.
The efficacy of the agonist decreases and the efficacy of the antagonist increases in what type of antagonism?
A maximal agonist effect is achieved at a lower dose than that required for saturation (without 100% rcptr occupancy) when?
When spare receptors are present, what is possible?
G-protein target enzymes are who?
Adenylate Cyclase
Guanylate Cyclase
Phospholipase C
Name the 2nd messengers. The G-Protein target NZ's act on them.
cGMP, CAMP, IP3, DAG, AA are all ______ acted on by ______.
Refractoriness refers to...
The loss of therapeutic effectiveness is...
What is the difference between desensitization and tachyphylaxis and tolerance?
Tolerance takes longer than what two other processes?
Nicotinic Receptor Antagonists
Hexamethonium (acts on AG)
Trimetaphan (BP) (acts on AG)
Tubocurarine (acts on NMJ)
Pancuronium (acts on NMJ)
Atracurium (acts on NMJ)
Vecurium (MR) (acts on NMJ)
Nicotinic Receptor Agonists
Epibatidine
Succinylcholine (MR)
Decamethonium
*
Muscarinic Antagonists
Atropine
Scopolamine
Atropine Methonitrate
Ipratropium
Tropicamide
Cyclopentolate
Pirenzepine
Which drugs cause hypotension from histamine release?
What's a side effect of these guys?

Tubocurarine
Atracurium
Mivacurium

BUT NOT PANCURONIUM