Unit 1 Flashcards
Type of process:
Formulation of drug into suitable dosage form, administration of drug, disintegration and dissolution of drug.
How is drug getting into the patient? What form is it- liquid, tablet, PO, IV, etc?
Pharmaceutical Process
Type of process:
Absorption, distribution, metabolism, excretion.
What the body does to the drug and how does it get to the site of action?
Pharmacokinetic process
Type of process:
Drug-receptor interaction.
What the drug does to the body and is it able to produce the desired effects?
Efficacy and therapeutic index.
Pharmacodynamic process
Type of process:
Therapeutic effects and possible adverse reactions.
Are the drug effects appropriate?
Therapeutic process
4 factors of core drug knowledge
Therapeutic applications, interactions, side effects, and mechanisms of action
Factors of core patient knowledge
Age, sex, body mass, health status, genetics
STEPS stands for:
Safety, Tolerability, Efficacy, Price, and Simplicity of Use
How the drug produces its effects of its mechanism of action
Pharmacologic classification
The drugs chemical composition and molecular structure
Chemical Name
Nonproprietary name- name given by the US Adopted Name Council
Generic Name
Proprietary name- registered trademark, use of the name restricted by the drug’s patent owner
Trade Name
Helps us understand how the body handles the medication, understand the action and side effects of the drug, and understand the obstacles the drug faces to reach target cells (site of action)
Pharmacokinetics
Movement of drugs into and out of the body
Pharmacokinetics
Time it takes for the drug to be absorbed into the systemic circulation- determines how soon effects will begin
Rate of absorption
Amount of the drug absorbed- determines how intense effects of the drug will be
Extent of absorption
The amount of the drug dose that reaches the systemic circulation- looks at the extent of absorption
Bioavailability
What route provides 100% bioavailability?
IV
Important when evaluating the characteristic of a generic and trade drug
• Pharmaceutical equivalent drugs need to have the same amount of active drug but may contain different amounts of other buffers, making absorption different
Bioequivalence
Process through which larger molecules are transported through cell membrane
o Cell cytoplasm surrounds (engulfs) the molecule and draws it into the cells
o Fat soluble vitamins are taken in this way
Pinocytosis
Most drugs-move from area of higher concentration to lower concentration to get into the cell
Passive Diffusion
Drug molecule diffuses with the help of a carrier (mainly protein receptors found on cell membranes)
Facilitated Diffusion
Drug molecules have to move against a gradient using energy (ATP)
o Electrolytes and levodopa
Active Transport
A drug’s ________ effects the rate and extent of absorption of a drug
Route of administration
Food in stomach increases gastric blood flow, which does what to drug absorption?
Increases
Most drug absorption occurs in the ______.
Small intestine
Route with the fastest absorption.
Parenteral
Parts of body with faster distribution (more blood flow)
Heart, liver, kidneys, and brain
Parts of body with slower distribution (less blood flow)
Muscle, skin, and fat
More protein bound, less available to the tissues
Water-soluble drugs
Have poor protein binding and are easily taken into tissues and distributed throughout the body
Fat-soluble drugs
Do drugs need to be bound or unbound to protein to produce a response?
Unbound (or “free”)
Which phase of metabolism?Oxidation- where cytochrome P-450 molecules come into play
o Reduction- removal of oxygen or addition of hydrogen to drug molecule
o Hydrolysis- splitting of drug molecule by addition of water
I
Which phase of metabolism?Conjugation or glucuronidation- attachment of another chemical group to the drug, making it more water soluble for easier excretion
II
Reside in ribosomes, Group of 57 families- 15 are involved in metabolism of drugs, 6 are involved in 95% of drug metabolism
P450 enzyme system
When a drug is metabolized by a CYP, it is said to be a _______ of that
Substrate
A drug that causes acceleration in the enzyme metabolization of another drug
Inducer
A drug that causes inhibition inhibition in the enzyme metabolization of another drug
Inhibitor
Delayed drug metabolism results in:
- Accumulation of drugs
- Prolonged action of the drugs
- Increased risk for adverse effects
Metabolism of a drug by the liver before its systemic availability
o Can decrease the bioavailability of a drug
First-pass effect/phenomenon
PO meds
A decrease in renal function effects elimination in what ways?
- Can prolong action or accumulation of the drug
2. Can increase adverse effects and toxicity
Amount of drug needed to elicit a minimal therapeutic effect
Minimum Effective Concentration (MEC)
Time it takes for the drug to elicit a therapeutic effect
Onset
The time it takes for the drug to reach maximum therapeutic response
When drug reaches its highest blood concentration
Peak
Length of time concentration is sufficient to elicit a therapeutic effect
Duration
A physiologic state in which the amount of drug removed via elimination is equal to the amount of drug absorbed with each dose
Steady-state
The time required for one half of a given amount of a drug in the body to be eliminated from the body
Half-life
Higher amount of drug given so a plateau is reached faster
Quickly produces a therapeutic response
Loading dose
Keeps plasma-drug concentration in therapeutic range
Maintenance Dose
If a patient has liver or kidney failure, what needs to be adjusted on the medication you are prescribing?
Either lower the dose or give the drug at a longer frequency
Cellular processes involved in the drug and cell interaction
Drug action
Physiologic reaction of the body to the drug
Result of an interaction between the drug and target cell/receptor
Drug effect
The magnitude of a maximal response that can be produced
Efficacy
Produces a therapeutic effect at a lower dose compared to a drug with the higher dose
Potency
The degree to which a drug molecule binds to a receptor and elicits a response
Affinity
Drugs that bind to a receptor and produce a response- mimics the response of naturally occurring processes in the body
Agonists
Drugs that attach to a receptor (but not completely) and blocks the receptor and associated response to it
Antagonists
Average lethal dose
LD50 (lethal dose)
Average or standard dose- predicts therapeutic dose for ½ of the population, dose required to produce a response in 50% of clients
ED50 (effective dose)
Measures a drug’s safety using a margin of safety
Therapeutic Index
Therapeutic index formulat
LD50/ED50
Narrow margin of safety and requires close monitoring of drug levels to ensure client is not in toxic range
Low therapeutic index
Wide margin of safety- does not require monitoring
High therapeutic index
When two drugs with similar action are given together they have an increased effect than either of them alone
Additive effects
The effects of two combined drugs are better than what can be achieved by either alone
Synergism
Effects of two drugs are less than the sum of the effects for each drug given separately- can sometimes cancel each other out
Antagonism
The physical interaction of 2 drugs interferes with the effects of at least one of the drugs
• Can result in chemical deterioration of one or both drugs
Incompatibility
When is the period of greatest danger for teratogenic drugs and why?
Embryonic period (14 days to 8 weeks), because organ development is occurring
Pregnancy class- adverse effects seen in animals, no info in humans available
C
Pregnancy class- possible risk in humans have been reported, need to consider risk vs benefit before prescribing
D- ace inhibitors and tetracyclines
Pregnancy class-contraindicated in pregnant women
X- thalidomide, cocaine, vitamin A
A state in which the body has adapted to drug exposure in such a way that an abstinence syndrome will result if drug use is discontinued
Dependence
Pregnancy Category:
Adequate and well controlled studies have failed to demonstrate a risk to the fetus in the 1st trimester (no evidence in later trimesters)
A
Pregnancy Category:
Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well controlled studies in pregnant women
B
Pregnancy Category: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risk
C
Pregnancy Category: There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks
D
Pregnancy Category: Studies in animals or humans have demonstrated fetal abnormalities and/or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience, and the risks involved in use of the drug in pregnant women clearly outweigh the potential benefit
X
Decreased responsiveness to a drug as a result of repeated drug administration
Tolerance
The plasma level at which toxic effects begin
Toxic concentration
Drugs must be ______ to penetrate cell membranes
Lipid-soluble
