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Pharm 124--chap 4
Drug Administration
90
Nursing
Undergraduate 2
08/28/2011

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Cards

Term
An __ drug is administered directly into the bloodstream.
Definition
Intravenous
Term
A ___ tablet is formulated to release a drug slowly over an extended period.
Definition
Sustained-release
Term
Pharmacokinetics
Definition
is the movement of the drug particles inside the body and the process that occur during this movement.
Term
Pharmacokinetics is made up of four phases:
Definition

Absorption

Distribution

Metabolism

Excretion

Term
Absorption
Definition
the movement of the drug from the site of administration into the bloodstream.
Term
Distribution
Definition
is movement of the drug through the bloodstream, into the tissues, and eventually into the cells.
Term
Metabolism
Definition
is the conversion of the drug into another substance or substances.
Term
Excretion
Definition
is the removal of the drug, or what the drug became after metabolism, from the body.
Term
Drug molecules can cross cells membranes in one in one of three ways:
Definition

-pass between the spaces or channels between the molecules

 

-pass through the membrane with the help of a transport system (energy or no energy)

 

-can penetrate the membrane  directly. Drug must be lipophilic (soluble in lipids). This is used by most drugs to cross cell membrane.

Term
Polar molecules are___
Definition
Charged molecules that are hydrophilic (soluble in water), not lipophilic.
Term

Polar drug molecules are not able to penetrate cell membranes.

 

true or false

Definition
True
Term

Nonpolar molecules are lipophilic (soluble in lipids/fat); therefore, nonpolar molecules are able to penetrate cell membranes.

 

true or false

Definition
true
Term
bloodstream and are not technically absorbed.
Definition
Drugs that are administered intravenously are placed directly into the_____
Term
capillaries
Definition
Drugs that are administered subcutaneously  or intramuscularly are absorbed into the____
Term
The distribution of a drug throughout the body depends on three factors:
Definition

-blood flow to the tissues

-the drug's ability to leave the blood

-the drug's ability to enter cells

Term

Protein bining of drugs affects their distribution but is not an important concept to understand.

 

true or false

Definition
false
Term

Drug that is free (unbounded to protein) is active.

 

true or false

Definition
true
Term

Only drug molecules that are unattached to protein are capable of moving to their site of action (distribution) and achieving the desired therapeutic effect.

 

true or false

Definition
true
Term
Only free drug (unattached) is ____
Definition
active
Term
Drug dosages are calculated by the drug manufacturer base on the ____ characteristics of the drug.
Definition
protein-binding
Term
When the patient has a lower-than-expected protein level (liver failure or severe burns), the distribution is altered. How much should be given.
Definition
you would need less drugs because the person has a low protein level, meaning less proteins to bind with drug--therefore, more free drug in system and active.
Term
Pharmacotherapeutics
Definition
desired effects of the drug.
Term
Pharmocokinetics
Definition
___ is influenced by health status, life span, gender, and culture.
Term
Pharmacodynamics
Definition
is the biologic, chemical, and physiologic actions of a particular drug within the body and the study of how those actions occur. How the drug affects the body.
Term
Absorption
Definition
is dependent on route of administration, solubility and concentration of the drug, circulation, surface conditions, contact time and pH at the site, and cell membrane transport mechanisms.
Term
Distribution
Definition
dependent on drug flow to the tissues, the drug's ability to leave the vascular system and enter cells, the drug's lipid affinity (lipophilic) or water affinity (hydrophilic), and the drug's ability to bind with protein (usually albumin) in the blood.
Term

Drugs cannot create new responses in the body; they can only turn on, turn off, promote, or block a response that the body is inherently capable of producing.

 

true or false

Definition
true
Term

Most drugs produce their effects from drug-receptor interactions.

 

true or false

Definition
true
Term

Drugs are designed to fit certain receptors. If the drug activates the response when it is on the receptor, it is said to be agonist or stimulant of the receptor.

 

true or false

Definition
true
Term
Antagonist or blocker of the receptor
Definition
If the drug blocks another chemical from activating the receptor, the drug is called an___
Term

Drugh have same affinities for binding with serum proteins.

 

true or false

Definition
false
Term
Free/active
Definition
Drug particles that are not bound to protein. Exert an effect by attaching to a receptor or working in another way.
Term
increases the drug's effect
Definition
An increase in the number of free drug particles (from low protein levels)____, even though the dose of the drug is unchanged.
Term
desired effect
Definition
The potency of a drug refers to hom many particles of a drug are needed to produce a ___.
Term
Efficacy
Definition
___is the innate ability of the drug to produce a desired effect.
Term
 Blood-brain barrier
Definition
The capillary beds in the brain that affects distribution of a drug to the brain is called ____, the cells are packed tightly together--preventing drug molecules, and other foreign substances from passing through and entering the brain.
Term

Only lipophilic drug molecules or that have a transport system can penetrate the barrier and get to the other side to the brain.

 

true or false

Definition
true
Term
The placental membrane is not a barrier like the blood-brain barrier. In order to pass through the placenta, a drug must be lipophilic, not ionized, and not protein bound.
Definition
true
Term
Liver
Definition
Metabolism of drugs occurs primarily in the ___.
Term

Other than the liver, GI, lungs, kidney and skin, research has shown that the intestinal mucosa is a major metabolic organ (after the liver) for some drugs.

 

 

true or false

Definition
true
Term
Biotransformation
Definition
another name for metabolism is ___.
Term
Prodrugs
Definition
Drugs that are inactive until metabolized into an active form are called ___.
Term

Some drug are highly metabolized, meaning that every time drug molecules are circulated to the liver (25% of cardiac output sent to liver), a large percentage of the drug molecules is metabolized.

 

true or false

Definition
true
Term
First-pass effect
Definition
This loss of effectiveness is called____.
Term

Drugs that are highly metabolized gain much of their effectiveness during this first pass through the liver, before they reach general circulation.

 

true or false

Definition
False
Term

Drugs that are metabolized are generally changed into an inactive form, having no effect on the body as they travel throughout the body waiting to be excreted. Occasionally, a drug is metabolized into an active metabolite.

 

true or false

Definition
true
Term
P-450 system
Definition
Liver metabolism is predominantly achieved by specific live microsomal enzymes called ___.
Term
naturally occurring substances
Definition
P-450 group (group of cytochromes) metabolize ____, such as fatty acids.
Term
CYP3A4
Definition
___ is the most common enzyme and is responsible for the metabolism of most drugs.
Term

Some drugs either induce or inhibit the p-450 system, altering metabolism of other drugs--usually, just one P-450 family is affected.

 

true or false

Definition
true
Term
increase
Definition
Drugs that induce a hepatic enzyme ___ the amount of that enzyme present in the liver--accomplished most frequently by stimulating enzyme systhesis, som more metabolism can occur through this pathway.
Term
slow
Definition
Drugs that inhibit a particular hepatic enzyme slow the metabolism that occurs through this pathway, causing an increase in the amount of circulating, active drug.
Term

Metabolism returns tonormal after the inducing or inhibiting drug is no longer administered, although it may take several days after an inducer is discontinued.

 

true or false

Definition
true
Term
poor metabolizers
Definition
8% American whites, 2-7% African-americans, 1% Asian are what type of metabolizers?
Term

CYP3A4 varies by the sex of the pateint. More of this isoenzyme is present in the liver of women than in men.

 

true or false

Definition
true
Term
Glomerular filtration
Definition
Three processes are involved in renal excretion of drugs: The first is ___. drugs come to the kidney through the capillaries surrounding Bowman's capsule. Then most drug particles pass easily through the spaces of the capillary walls into the urine in the proximal tubule. Only very large particles like proteins cannot pass.  The second, is passive tubluar reabsorption. The third process that affects excretion is active tubular secretion.
Term
Because ions cannot be passively reabsorbed from the tubule, drug excretion can be increased if the pH of the urine encourages the drug to become an ion.
Definition
true or false
Term

Acids will ionize in basic environments and bases will ionize in acidic enironments.

 

true or false

Definition
true
Term
Half-life
Definition
The amount of time that is required to remove half (50%) of the blood concentration of a drug.
Term

The combined processes of metabolism and excretion are responsible for elimination of a drug from the body.

 

true or false

Definition
true
Term
steady state
Definition
A point at which the amount of drug being administered and the amount being eliminated balance off. it becomes balanced of a stable level of the drug in the blood called___.
Term

A 100% steady state can be achieved if a particular drug is give more than one time.

 

true or false

Definition
false
Term

97% of steady state can be acheived.

 

true or false

Definition
true
Term

Most of steady state (94%) is achieved in four half-lives.

 

true or false

Definition
true
Term

Achievement of steady state is not based on drug dose--it is based on the amount of time required for four to five half-lives to occur, and hlaf-life is related to the rate of elimination of the drug.

 

true or false

Definition
true
Term
Clearance/clearance rate
Definition
____ are pharmacokinetic factors work together to affect the rate at which drug molecules disappear from the circulatory system. The Renal excretion and hepatic metabolism are the major modes.
Term

Drug cannot create new responses in the body; they can only turn on, off, promote, or block a rsponse that the body is inherently capable of producing.

 

true or false

Definition
true
Term
receptors
Definition
Drugs attach to the body's __ for intrinsic element such as hormones, neurotransmitter, or othe internal methods of regulating cell function.
Term
Single Occupancy Theory
Definition

The intensity of the body's response to the drug is directly related to the number of receptors

 occupied by the drug. The more occupied, the stronger the response that is produced. Second, the maximum respnse occurs when all of the receptors have drug molecules attached. This is known as ___.

Term
Ceiling effect
Definition
No matter how much more drug you give, you cannot get any additional therapeutic response.
Term
Modified Occupancy Theory
Definition
__ is based on different assumptions about how drugs work at recptors. It states that different drugh have different strengths of attraction or affinity, for receptor sites. Drus with high affinity are strongly attracted to a recptor; drugs with low affinity are not very stongly attracted to a receptor.
Term

Low doses of a drug with high affinity for a receptor will bind with that receptor and produce an effect.

 

true or false

Definition
true
Term
sensitivity
Definition
Receptors are not static; they are continuously stimulated to act or continually inhibited from action. Receptor response can be modified either by changing the number of receptor on the cell or by changing the __ of the current receptors.
Term

Most drug effects are related to drug-receptor responses, some drugs exert their effect by reacting physically or chemically with other molecules in the body.

 

true or false

Definition
true
Term
Nonreceptor response--drugs exert their effect by reacting physically or chemically with other molecules in the body.
Definition
antacids create their effect by mixing with stomach contents to raise the pH, making it less acid. This is an example of what?
Term

Two drugs may have different potencies but the same efficacy.

 

true or false

Definition
true
Term
maintenance dose
Definition
Once a dose is chosen and administered consistently over time and arrive at steady state after 4 or 5 half-lives.
Term
Loading dose
Definition
When a larger dose than usual is given initially is called ___, it computed so that after some of the drug is eliminated, the drug concentration in the body is still in the therapeutic range.
Term

If less potent but equally effective drug is less expensive or is better tolerated by the patient, it will be the preferred drug.

 

true or false

Definition
true
Term
ED(effective dose) 50
Definition
The dose that is required to produce the therapeutic response in 50% of the population.
Term
Therapeutic Index
Definition
A measurement of the safety of the drug. drugs having a narrow therapeutic index do not have much difference between the effective dose and the toxic or lethal dose.
Term

Pateint receiving a drug with a narrow therapeutic index do not need to be monitored closely for adverse effects.

 

true or false

Definition
false
Term

A wider therapeutic index means that the amount required to be effective is very small, compared with the amount required to be lethal. The closer the TI is to 1.00, the more difficult it is to use the drug to treat patients--lethal. 0.025-safe.

 

true or false

Definition
true
Term

Minimum concentration of a drug is required to achieve the desired pharmacotherapeutic effect (the MEC).

 

true or false

Definition
true
Term
adverse effects
Definition
As drug levels within the body increase, the patient is more likely to experience ____ from drug therapy.
Term
Blood levels
Definition
___ reflect the changes that have occurred from drug metabolism and excretion. Note last time drug  was administered.
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