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53 Cards in this Set
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Pharmacokinetics |
Actin of drugs in the body - absorption, distribution, metabolism, elimination, rate at which drugs work |
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Pharmacodynamics |
Mechanism of action in addition to the actions of different drug concentrations and doses |
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Absorption |
The rate and extent that the drug leaves the site of administration, how long it takes oral drugs to enter bloodstream and much makes it |
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Bioavailability |
What fraction of a drug reaches its action site, or body fluid where it has access to action site. |
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T1/2 |
Half life - time for drug concentration to drop by half (drug concentration relates to dosage given, frequency of dose and rate at which drug breaks down in the body) |
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Passive diffusion |
Mechanism of drug entry into cell - no energy, determined by concentration gradient, how lipophilic the drug is and cell surface area |
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Facilitated diffusion |
Protein carrier in cell membrane facilitates drugs movement to interior. No energy |
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Active transport |
Uses a protein carrier and requires energy input (usually ATP) |
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Types of administration, with descriptions |
Enteral - through GI tract Parenteral - outside GI tract (IV) Inhalation - gas, small particles |
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Distribution |
Process through which drug leaves the blood stream and enters the interstitial or tissue cells |
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Distribution effected by: |
Blood flow, capillary permeability, drug structure, degree of protein binding. (Albumin, serum protein, binding will slow down distribution by keeping the drug in the blood.) |
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Class 1 drugs |
Dose is less than albumins ability to bind |
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Class 2 drugs |
Given is doses that are much greater than albumins ability to bind = lots of drugs free in the blood stream |
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Volume of distribution Vd |
Total amount of drug in the body / drug concentration in plasma. Small number = drug is primarily in plasma. Large number = relatively little drug stays in plasma |
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Metabolism |
Bio transformation of a drug into another chemical. |
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Two phases of metabolism |
Usually in the liver Phase 1 - convert lipophilic drugs into polar molecules Phase 2 - conjugation of the drug makes it more polar, which usually makes it inactive and ready to be eliminated. |
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Elimination |
Removal of drug from the body. KIDNEYS! bile, intestines, lungs, breasts also. Total body clearance, adds up all modes of elimination. |
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Kinetics |
Rates or speeds of reactions: absorption, distribution, metabolism, elimination, steady state calculations, fixed dose and fixed time regimens. |
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Steady state Vs fixed dose |
Steady state - continuous IV infusion, steady state reached by 4 half lives. Fixed dose - oral dosage regimen, steady fixed time dosages will add up in concentration until the body fluctuates around a steady state. |
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Drug receptors |
Protein complexes on a cell surface, or within cell, that causes changes to cell or its function. |
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Ligand |
Anything that binds to a receptor |
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Antagonist vs agonists |
Antagonists - inhibit or slow down receptors Agonists - increase function of receptors |
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Antagonist vs agonists |
Antagonists - inhibit or slow down receptors Agonists - increase function of receptors |
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Functional antagonism |
Antagonistic effects, result from agonizing a different receptor |
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Acidity and pH effects on drug absorption |
acid environments can convert drugs into an absorbable state. pH also effects charge, which can determine a molecules ability to pass into the cell. |
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Drugs effects on GI motility |
GI motility (intestinal peristalsis) is effected by certain drugs, which can effect the absorption of other concurrently prescribed medication. Motility is increased with cholinergic agents and decreased with anti-cholinergics, narcotics, anti-depressants. |
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Therapeutic margin |
can be effected by individual response (factors such as age, gender, diet, other drugs, digestion). Warfarin, phenytoin, digoxin.digitoxin and lithium have small therapeutic margins |
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Antimuscarinic Agents are used to... |
Relax the GI tract and bladder, treat Parkinson's, antispasmatic. Muscarinic receptors accept Ach, which then creates a parasympathetic reaction. Anti-muscarinic agents would block this response. |
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Beta andrenogenic drugs and the Heart |
B1 (on the HT) receptors can cause tachycardia. B2 receptors have a red flag association for significant arrythmias and cardiac infraction. B2 recpetors vasodilate. |
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Drugs / methods that treat anemia |
1. EPO - erythropoietins (hormone that controls red blood cell production from the bone marrow) 2. Iron. 3. Blood transfusion |
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Uses of aspirin |
HT attack, platelet agregation, transient cerebral ischemia |
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Ephedrine |
asthma, not for severe cases. |
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Barbiturates, uses and side effects |
Predominantly hypnotic (sleep aid). Tolerance, dependance and sever withdrawal are the down sides. Drowsiness and confusion are common side effects. Overdose can be fatal, causing decrease in respiration and cardiovascular system. |
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Benziodiazophine, two uses |
anxiolytic / hypnotic category. muscle tension, convulsions, anxiety, sleep disorders, epilepsy. |
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Calcium channel blockers useful for what condition |
Hypertension, asthma, diabetes, angina, peripheral vascular disease. Block voltage gated calcium channels that trigger contraction in cardiac and vascular smooth muscle |
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Inotropes |
contraction of the HT, positive increase the strength, negative reduce contractility. Increase contractility by increasing cytoplasm calcium concentration. |
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Ace inhibitors in type 1 vs. type 2 diabetes |
Shown to be effective in protecting the Kidneys of type 1 diabetics, results are mixed for type 2 diabetics |
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Reversible anti-choleneserase uses |
Effects the acetylcholinesterases (which breaks down Ach) so more Ach can bind to receptor. Creates parasympathetic reaction. Treats myasthenia gravis, alzheimers |
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loop diuretics |
Loop diuretics promote calcium excretion and reduce pulmonary edema from heart failure (ER). Can be ototoxic, effects hearing and balance. Minimized by oral administration. |
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therapeutic index, definition |
Also caused therapeutic margin or therapeutic window, it is a measurement of how safe a drug is. The ratio between the toxic dose and therapeutic dose. Larger = safer. |
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efficacy |
A measurement of how efficient the drug produces its effects. Dependent on the number of drug-receptor complexes formed and how efficient these complexes create cellular responses |
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Potency |
The concentration of a drug that produces 50% of maximal effect of drug. The more potent a drug is, the less drug per dose. |
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anti-rhythmic drugs |
Modify action potential, reducing the potential for arrhythmia |
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Monoimine oxidase inhibitors |
treat depression, Parkinson's, by inhibiting MAO, which breaks down dopamine in the synaptic cleft. |
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side effects of ephedrine |
Revs up everything, dizziness, nausea, nervousness, tremor, trouble sleeping, etc. |
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Drug that treats mania |
lithium |
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Organic nitrates, nitroglycerine treats |
angina, pain, vasodialates |
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What drug category treats pain?? |
Opiod, analgesics, antagonists, NSAIDs |
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Side effects of anti-platelet drugs |
prolonged bleeding: hemorrhagic stroke and gastrointestinal bleeding. Red flag: ticlopidine |
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Seritonin reuptake inhibitors |
Treat depression, GAD, panic disorder, anxiety, OCD and pain. Work by preventing the re-uptake of serotonin into the presynaptic cleft, resulting in more serotonin the the synapse. |
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What do diuretics do? |
induce urination |
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What type of drug reduces lipids |
HMG CoA reductase inhibitors - statins |
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drug that relaxes smooth muscle in blood vessels |
vasodilator: anti-muscarinics, atropine, beta blockers, calcium blockers |