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68 Cards in this Set
- Front
- Back
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What is the MOA of fibrates?
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The MOA of this drug is to stimulate LPL.
Peroxisome Proliferator Activated Receptor (PPARalpha) agonists |
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Common side effects of fibrates?
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These side effects are associated with what drugs?
GI Symptoms Pruritis Rash Rare- Acute renal failure and Rhabdomyolysis |
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Clofibrate can only be used in patients who...
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Have no gallbladder.
This med predisposes to gallstones. |
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Fibrates should not be combined with ________.
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Statins should not be combined with __________.
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Name angiotensin receptor antagonists.
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Who are these guys?
Losartan Valsartan Candersartan |
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Patients with COPD and asthma should not take_______
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Non-selective B1/B2 Blockers are contraindicated in what patients?
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Alpha-2 receptor stimulant
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What does Clonidine do?
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Name an Alpha-2 receptor inhibitor.
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What does Yohimbine do?
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Name the Class I Na Channel Blockers.
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Who are these guys?
IA Quinidine, Procainimide, Disopyramide IB Lidocaine, Tocainide,Mexilitine IC Flecainide, Encainide |
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B-Blockers for CHF
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These are the _____ used in _____.
Carvdilol Metoprolol |
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Aldosterone Antagonists
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Spironolactone
Eplerenone |
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What meds should not be prescribed with B-Blockers?
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Verapamil
Beperidil Diltiazem (Ca channel blockers that cause heart failure or AV Block) |
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What meds would you use for unstable angina?
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Aspirin (stable also)
Heparin Abciximab Tirofiban Statins |
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What are the major side effects of Ca Channel Blockers?
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reflex tachycardia
headache edema (ankle/general) |
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Nitrates are contraindicated in patients taking what?
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Phosphodiesterase (PDE) Inhibitors like sildenifil or tadalafil for erectile dysfunction.
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Which vasodilator can actually WORSEN angina?
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Dipyridamole because it does not dilate collateral arteries to increase amount of blood flow.
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What is the MOA of organic nitrates?
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Bypass the endothelial cell production of NO and go straight to relaxation of sm. muscle (vasodilate).
NO stim GP => stim GTP => cGMP => relaxation |
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Name the B-Adrenoceptor antagonists used in angina.
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NS Propanolol, Pindolol
B1S Metoprolol, Atenolol |
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Name the muscarinic agonists.
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Ach
Carbechol Methacholine Bethdanechol Pilocarpine Oxotremorine * |
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Anticholinesterases are often used to treat _________. Name them.
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Myasthenia Gravis
Edrophorium Neostigmine Physostigmine Pyridostigmine Dyflos Ecothiopate Parathion |
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Glaucoma is treated with which med?
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Pilocarpine
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What are the major side effects of muscarinic antagonists?
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Dry Mouth
Constipation Blurred Vision |
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What is the difference between real and pseudo Acetylcholine Esterase?
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real: degrades Ach released from nerve terminals
pseudo: removes circulating Ach |
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Adrenal Medulla secretes what?
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What secretes Chatecholamines?
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Glucuronidation, Transacetylation, Transulfonation, are examples of _______ rxn.
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An example of Phase II drug biotransformation reaction is __________.
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Examples of Enzymes in a Phase I reaction
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Cytochrome p450
Aldehyde dehydrogenase Alcohol dehydrogenase |
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Drug Excretion is usually enhanced by a drug being what?
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Highly ionized
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Therapeutic Index of a drug is what ratio?
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TD50/TE50
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Clinical use as an inhalant for asthma/bronchitis.
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Ipratropium
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Atropine
Atropine Methonitrate Scopolomine |
Used for gastrointestinal hypermotility.
Add motion sickness for one. |
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Which meds are used for ophthalmic production of mydriasis.
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Tropicamide
Cyclopentolate |
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Pirenzipine is used for what? It is selective for what receptors?
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Used for peptic ulcers (inhibits gastric secretions) and is selective for M1 receptors.
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What drugs inhibit Ach release (act presynaptically)?
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Aminoglycosides
(streptomycin/neomycin, also inhibit Ca release) Botulinum Toxin Bungarotoxin |
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Net transfer of drug during passive diffusion is directly proportional to what in drug absorption?
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Concentration gradient and lipid:water partition coefficient play a major role in what?
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Pinocytosis is...
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Microscopic particle engulfed by cell membrane is called...
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Active transport is used to transport what?
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Highly specific for naturally occurring substances such as amino acids, sugars, and vitamins.
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Uncharged drugs are...
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not easily absorbed by the GI tract.
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The lower the pH relative to pKa, the ____ the drug is unionized, and therefore ____ lipid soluble.
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More unionized drugs are more lipid soluble. What is the pH like compared to pKa?
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Define Distribution.
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Process by which a drug reversibly leaves the blood stream and enters the interstitium (extracellular fluid).
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Volume of Distribution =
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VD = amt of drug in body / plasma concentration
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What is the major mechanism for drug elimination?
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Drug Metabolism / Biotransformation
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Enzyme Inducers like barbiturates and rifampin
ibuprofen phenytoin steroids ethanol have what effect? |
What can increase the metabolism of acetominophen?
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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 |
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Net Renal Excretion =
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Drug Filtered at Glomerulus
+ Drug Secreted by AT in kidney - Amount of drug passively resorbed in tubule |
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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.)
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Zero Order Elimination
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Occurs at a constant rate regardless of concentration.
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Clearance
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Volume of Plasma from which a drug is completely removed by the process of excretion or metabolism per unit time.
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First Order Elimination
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Rate of Elimination is proportionate to concentration.
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Glucuronidation is the mode of metabolism for what drugs?
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Acetominophen, Diazepam, Morphine, sulfthiazole, digoxin, and digitoxin are metabolized how?
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Metabolism of Digitoxin and Cortisol is enhanced or induced enzymatically by what substances?
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Phenobarbitol
Phenylbutazone Phenytoin Rifampin All of these enhance what? |
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p450 inhibitors are ____.
p450 inducers are _____. |
Tea and herb sounding things ______ p450.
Veggies, meat, and oregano ______ p450. |
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Bioavailability is ....
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Proportion of UNCHANGED drug that reaches systemic circulation.
Affected by first pass metab, drug formulation, route of administration. |
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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.
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Agonists have both _______,
while Antagonists have only one. |
Affinity and Intrinsic Activity
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Fractional occupancy is measured by the equation
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(AR)/R = L / (L + KD)
KD = K(-1)/K(+1) = (A)(R)/ (AR) = 50% of rcptrs occupied |
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Full/Partial Agonist based on
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relative efficacey decides what?
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Measure of potency, the concentration that produces 50% of a maximal response.
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EC50
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In competitive antagonism, the efficacy of the agonist ______ and the efficacy of the antagonist _______.
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agonist efficacy stays the same and antagonist efficacy increases in what type of antagonism?
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In non-competetive antagonism, the efficacy of the agonist _____ and the efficacy of the antagonist _____.
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The efficacy of the agonist decreases and the efficacy of the antagonist increases in what type of antagonism?
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A maximal agonist effect is achieved at a lower dose than that required for saturation (without 100% rcptr occupancy) when?
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When spare receptors are present, what is possible?
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G-protein target enzymes are who?
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Adenylate Cyclase
Guanylate Cyclase Phospholipase C |
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Name the 2nd messengers. The G-Protein target NZ's act on them.
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cGMP, CAMP, IP3, DAG, AA are all ______ acted on by ______.
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Refractoriness refers to...
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The loss of therapeutic effectiveness is...
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What is the difference between desensitization and tachyphylaxis and tolerance?
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Tolerance takes longer than what two other processes?
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Nicotinic Receptor Antagonists
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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) |
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Nicotinic Receptor Agonists
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Epibatidine
Succinylcholine (MR) Decamethonium * |
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Muscarinic Antagonists
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Atropine
Scopolamine Atropine Methonitrate Ipratropium Tropicamide Cyclopentolate Pirenzepine |
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Which drugs cause hypotension from histamine release?
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What's a side effect of these guys?
Tubocurarine Atracurium Mivacurium BUT NOT PANCURONIUM |
