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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

Pharmacodynamics

Mechanism of action in addition to the actions of different drug concentrations and doses

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

Bioavailability

What fraction of a drug reaches its action site, or body fluid where it has access to action site.

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)

Passive diffusion

Mechanism of drug entry into cell - no energy, determined by concentration gradient, how lipophilic the drug is and cell surface area

Facilitated diffusion

Protein carrier in cell membrane facilitates drugs movement to interior. No energy

Active transport

Uses a protein carrier and requires energy input (usually ATP)

Types of administration, with descriptions

Enteral - through GI tract


Parenteral - outside GI tract (IV)


Inhalation - gas, small particles

Distribution

Process through which drug leaves the blood stream and enters the interstitial or tissue cells

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.)

Class 1 drugs

Dose is less than albumins ability to bind

Class 2 drugs

Given is doses that are much greater than albumins ability to bind = lots of drugs free in the blood stream

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

Metabolism

Bio transformation of a drug into another chemical.

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.

Elimination

Removal of drug from the body. KIDNEYS! bile, intestines, lungs, breasts also.


Total body clearance, adds up all modes of elimination.

Kinetics

Rates or speeds of reactions: absorption, distribution, metabolism, elimination, steady state calculations, fixed dose and fixed time regimens.

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.

Drug receptors

Protein complexes on a cell surface, or within cell, that causes changes to cell or its function.

Ligand

Anything that binds to a receptor

Antagonist vs agonists

Antagonists - inhibit or slow down receptors


Agonists - increase function of receptors

Antagonist vs agonists

Antagonists - inhibit or slow down receptors


Agonists - increase function of receptors

Functional antagonism

Antagonistic effects, result from agonizing a different receptor

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.

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.

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

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.

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.

Drugs / methods that treat anemia

1. EPO - erythropoietins (hormone that controls red blood cell production from the bone marrow)


2. Iron.


3. Blood transfusion

Uses of aspirin

HT attack, platelet agregation, transient cerebral ischemia

Ephedrine

asthma, not for severe cases.

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.

Benziodiazophine, two uses

anxiolytic / hypnotic category. muscle tension, convulsions, anxiety, sleep disorders, epilepsy.

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

Inotropes

contraction of the HT, positive increase the strength, negative reduce contractility.




Increase contractility by increasing cytoplasm calcium concentration.

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

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

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.

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.

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

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.

anti-rhythmic drugs

Modify action potential, reducing the potential for arrhythmia

Monoimine oxidase inhibitors

treat depression, Parkinson's, by inhibiting MAO, which breaks down dopamine in the synaptic cleft.

side effects of ephedrine

Revs up everything, dizziness, nausea, nervousness, tremor, trouble sleeping, etc.

Drug that treats mania

lithium

Organic nitrates, nitroglycerine treats

angina, pain, vasodialates

What drug category treats pain??

Opiod, analgesics, antagonists, NSAIDs

Side effects of anti-platelet drugs

prolonged bleeding: hemorrhagic stroke and gastrointestinal bleeding.


Red flag: ticlopidine

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.

What do diuretics do?

induce urination

What type of drug reduces lipids

HMG CoA reductase inhibitors - statins

drug that relaxes smooth muscle in blood vessels

vasodilator: anti-muscarinics, atropine, beta blockers, calcium blockers