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Pharmacology > Basic Concepts > Flashcards

Basic Concepts Flashcards

1
Q

Drug nomenclature

A

chemical name

generic name

brand name

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2
Q

Chemical name refers to:

A

the compound’s structure

  • not typically used
    ex: 2-acetoxybenzoic acid
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3
Q

Generic name

A

non-proprietary- not owned or trademarked

may be less well recognized

appropriate to use in medical literature

similarities across drug classes

ex: acetylsalicylic acid

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4
Q

Brand name

A

proprietary name- privately owned

in case presentations must include generic name, brand name optional

ex: aspirin is a registered trademark owned by Bayer

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5
Q

over the counter medication

A

no prescription required

can be purchased directly to the consumer

deemed to be safe without direct medical supervision

some of these drugs move to OTC status after rx

OTC drugs can still be involved in significant drug interactions

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6
Q

prescription medication

A

requires prescription from licensed health care provider (HCP)

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7
Q

what is the purpose of controlled substance scheduling?

A

drugs are scheduled I-V primarily for the purpose of prosecution

regulates the amount

who is prescribing and how much of certain substances? (Dr.s have DEA #s)

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8
Q

schedule I controlled substances

A

highest potential for abuse

no accepted medical use in the US or lacks accepted safety for use in the treatment in the US

ex: heroine (legal in some other countries), marijuana

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9
Q

schedule II controlled substances

A

2nd highest potential for abuse

has a currently accepted medical use in the US

abuse of substance may lead to severe psychological or physical dependence

ex: opiates in pure form (oxy cotin, morphine; excludes codine. also, adderall and ritalin: drugs prescribed for 1 reason but used for others)

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10
Q

schedule III controlled substances

A

abuse potential less than scheduled I or II substances

currently accepted medical use in the US

abuse may lead to moderate or low physical dependence or high psychological dependence

ex: vicodin, percocet, certain codine products

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11
Q

schedule IV controlled substances

A

abuse potential less than schedule III substances

currently accepted medical use in the US

abuse may lead to limited physical or psychological dependence relative to schedule III

ex: benzodiazepines

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12
Q

schedule V controlled substances

A

low potential for abuse relative to schedule IV

currently accepted medical use in the US

some schedule V products may be sold in limited amounts w/out a prescription at the discretion of a pharmacist

ex: low dose condone (often in syrup form)- based on the dose

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13
Q

where should you look for drug information

A 
E facts and comparisons
clinical pharmacology
Lexi-comp
MICROMEDEX
product package insert
national guidelines
primary literature
Ehealth
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14
Q

new drug approval process (7 steps)

A

once a compound is “discovered” it must be rigorously evaluated in both animal and human trials

1- compound discovery & “bench” testing/evaluation

2- animal phase of testing

3- human phase I (primarily looking at dosing)

4- human phase II (efficacy becomes more critical)

5- human phase III (typically larger population, placebo enrolled, mix of 1 &2)

6- FDA approval w/ patent

7- human phase IV - post marketing phase (no defined end point- determining if there is anything missed)

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15
Q

off label usage=

A

drugs prescribed for reasons other than what they were approved for

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16
Q

why are mice/rats used for drug testing?

A

have a fast reproduction rate

small, cheaper

much similarity between mice and humans

condensed life span- able to look at a life in a relatively short amount of time

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17
Q

pharmaceutical=

A

drug dose administration

disintegration of drug formulation

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18
Q

pharmacokinetics=

A 
what the body does to the drug
absorption
distribution
metabolism
excretion
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19
Q

pharmacodynamics=

A

drug/receptor interaction
what the drug does the body

study of biochemical and physiological effects of drugs and their mechanism of action

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20
Q

pharmacotherapeutics=

A

drug effect or response

therapeutic use of the drug (why wold you use it?)

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21
Q

what are the different types of preparations of drugs?

A 
aqueous
alcohol
solid or semi-solid
powder
tablets
lozenge
capsule
delayed-release (time release)
enteric coated products
suppositories
ointments
transdermal
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22
Q

what are the routes of administration?

A

1: oral or PO (per os/ per oral)
2: enteral: directly passes through GI
3: Parenteral: bipasses the GI: injections of all sorts, transdermal patches, sprays, inhalers, topical cream

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23
Q

what is ADME?

A

absorption: stomach & SI
distribution: bloodstream
metabolism: liver
excretion: kidney & LI

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24
Q

drug absorption refers to:

A

the entrance of a drug into the bloodstream

occurs in the stomach and/or small intestine

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25
Q

what drug factors effect the speed of drug absorption?

A

1- dosage form

2- drug water solubility

3- drug lipid solubility

4- drug particle size

5- drug configuration

**properties of the drug

***properties of the environment the drug is entering

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26
Q

what are physiologic factors affecting drug absorption?

A

1- biologic membranes act as barriers- protective

2- body is separated into various “compartments”

3- drug may need to cross several membrane barriers to reach target tissue

4- cell membrane- phospholipid bilayer (impermeable to water)

*small Uncharged ions are able to cross lipid bilayer but large uncharged or small charged ions are denied

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27
Q

what is bioavailability?

A

the percentage of the administered dose that is absorbed into systemic circulation

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28
Q

what are some factors that influence bioavailability?

A

1- physical properties of the drug

2-lipid solubility

3- affinity

4- drug protein complex

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29
Q

after a drug gains access to the bloodstream it is distributed to ?

A

the organ/tissues of the body

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30
Q

what factors effect the amount of drug penetrating specific tissue?

A

1- physical properties of the drug

2-lipid solubility

3- affinity

4- drug protein complex

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31
Q

what are 4 special anatomical barriers?

A

1- blood brain barrier (BBB)

2- plasma protein binding

3- blood flow

4- fetal-placental barrier

32
Q

what is the blood brain barrier?

A

an additional lipid barrier that protects the brain by restricting the passage of electrolytes and similar water soluble substances into the brain

drugs must have a certain degree of lipid solubility to penetrate the BBB

general body capillaries allow drug molecules to pass freely into the surrounding tissue– brain capillaries have a dense-walled structure and are surrounded by glial cells (lipid). This prevents many drug molecules from entering the surrounding tissue.

tight junctions prevent flow of ionized substances and large particles. (small, unionized, lipophilic are most likely to permeate BBB)

33
Q

what has high brain bioavailability?

A

small, ionized, lipophilic ions- most likely to permeate BBB

34
Q

what is plasma protein binding?

A

plasma proteins assist in the transport of hormones and vitamins through the body. Many drugs are also able to attach to plasma proteins, specifically albumin

only the unbound portion of the drug is able to exert its pharmacologic activity. the remainder of the bound drug will continue to circulate in the bloodstream

35
Q

what parts of the body receive the largest blood supply?

A

the liver, kidneys and brain

therefore they are exposed to the largest amount of the drug

36
Q

Vd=

A

volume of distribution (volume in which the drug appears to distribute)

Vd is not a physical volume; it is simply the size of the compatment necessary to account for total amount of drug in the body if it were present throughout in the same concentration found in plasma

Vd= (amount of drug administered) / (plasma concentration of drug)

37
Q

what is drug metabolism?

A

1- conversion of a drug to a form easily excreted

2- usually converted to an inactive form

3- some drugs are activated (pro-drugs)

*metabolism occurs in the liver

38
Q

what is biotransformation?

A

chemical alteration of drugs and foreign compounds in the body

39
Q

what is the most critical organ involved in drug metabolism?

A

the liver

40
Q

are other organs capable of drug metabolism?

A

yes!

kidney, lung, GI, skin, etc

41
Q

what are the phases of metabolism?

A

can be metabolized by either one or both

phase I- biochemical reactions

phase II- conjugation reactions

42
Q

what are biochemical reactions?

A

phase I of metabolism

```
forms of metabolism in the liver:
hydrolysis
oxidation
reductions
DMMS/hepatic microsomal enzyme system
~~~

43
Q

what it the main function of the DMMS?

A

to take lipid-soluble drugs and prepare them for excretion via the renal system

44
Q

what is drug metabolism?

A

1- conversion of a drug to a form easily excreted

2- usually converted to an inactive form

3- some drugs are activated (pro-drugs)

*metabolism occurs in the liver

45
Q

what is biotransformation?

A

chemical alteration of drugs and foreign compounds in the body

46
Q

what is the most critical organ involved in drug metabolism?

A

the liver

47
Q

are other organs capable of drug metabolism?

A

yes!

kidney, lung, GI, skin, etc

48
Q

what are the phases of metabolism?

A

can be metabolized by either one or both

phase I- biochemical reactions

phase II- conjugation reactions

49
Q

what are biochemical reactions?

A

forms of metabolism in the liver

hydrolysis
oxidation
reductions
DMMS/hepatic microsomal enzyme system

50
Q

what is drug excretion?

A

clearance (CL)

the ability of the body to remove drug from the blood or plasma

expressed as volume per unit time (mL/min)

the amount of drug removed depends on plasma concentration as well as clearance

51
Q

what are conjugation reactions?

A

phase II of metabolism

adds charge to the drug in order to make it inactive (ionized)

52
Q

what is first-pass effect?

A

drugs taken orally are absorbed through the GI tract into portal circulation. This transports the drug to the liver BEFORE they are distributed through the body. Many drugs administered orally are INACTIVATED by the liver..

if a drug is metabolized significantly before reaching general circulation this can reduce the amount of active drug that reaches general circulation

53
Q

what are some alternative routes of administration that by-pass first-pass effect?

A

up the dosage

alter the route of administration- parenteral

54
Q

what is enzyme induction?

A

when used repetitively, some drugs may increase enzyme activity. This may lead to FASTER METABOLISM of the drug and SHORTER DURATION of drug action

metabolic tolerance/ drug disposition

55
Q

what is enzyme inhibition?

A

some drugs may cause enzyme inhibition- will SLOW METABOLISM of all other drugs metabolized by the enzyme system and will INCREASE DURATION and INTENSITY of the drug

56
Q

what are the common pathways of drug excretion?

A

kidney/renal

liver/hepatic

lungs/pulmonary

57
Q

what is drug excretion?

A

clearance (CL)

the ability of the body to remove drug from the blood or plasma

expressed as volume per unit time (mL/min)

the amount of drug removed depends on plasma concentration as well as clearance

58
Q

what is entero-hepatic recirculation?

A

drug is secreted into bile- may go to feces OR

some drugs are reabsorbed, and the process may be repeated

59
Q

what are drug levels in the bloodstream?

A

the plasma level of a drug is always changing

once a drug is administered the plasma level increases as absorption and distribution occur

later, the plasma level will fall as drug metabolism and excretion occur

periodic measurements of a drug can help establish the correct therapeutic range for the given drug

60
Q

dosing concepts

A

minimum effective concentration- where the drug becomes active

therapeutic range- b/t min effective concentration and toxic concentration

toxic concentration

loading dose- trying to get into therapeutic range quickly

maintenance dose-

potency- strength

efficacy- effect, how it works

61
Q

what is plasma half-life (t1/2)?

A

the half life of a drug= the time required for the plasma concentration of a given drug to fall to half of its original level

62
Q

what does plasma half life depend on?

A

CL= clearance

Vd= volume of distribution

63
Q

why is establishing a half life important?

A

to determine dose frequency (maintain consistency or effective dose)

64
Q

median effective dose (ED50)=

A

the dose required to produce a specific therapeutic response in 50% of a group of patients

65
Q

median lethal dose (LD50)=

A

the dose that causes lethality in 50% of a group of animals

66
Q

therapeutic index (T1) =

A

(median lethal dose) / median effective dose

67
Q

receptors=

A

specific molecules in the body that control the action of cells and tissues

many drugs act though interaction with specific molecules in the body

68
Q

drug receptor interactions & drugs as agonists

A

lock and key mechanism: agonist binds perfectly to the receptor and the agonist-receptor interaction facilitates the receptors normal function

69
Q

drug receptor interactions & drugs as antagonists

A

the antagonist binds to the receptor and blocks binding of an agonist- therefore the antagonist-receptor complex prevents the receptors normal function

ex: anti-psychotic drugs - D2 (dopamine)
psychotic patient- getting too much dopamine, antagonist drug blocks D2-dopamine receptor so no more can reach

70
Q

competitive antagonists

A

compete for the binding site

reversible:

irreversible:

71
Q

non-competitive antagonists

A

bind elsewhere in the receptor (channel blockers)

72
Q

what are some of the factors that influence drug response? (physiological & psychological)

A 
age
weight
gender
percent body fat
genetics
emotional state
placebo effect
presence of disease
patient compliance
73
Q

what are teratogens?

A

certain drugs taken by the mother that can be harmful to the developing fetus

the placenta is NOT a drug barrier

74
Q

what is passive exposure?

A

drugs can be passed from the breast milk to the infant, termed passive exposure, possibly causing harm

75
Q

why are there PK and PD differences between pediatric and adult patients?

A

infants and young children have:

thinner skin
less skeletal muscle
higher percentage of body water
lower body fat
higher percentage of unbound drug due to reduced plasma protein levels
76
Q

physiology of aging…

A

due to the physiologic changes of age, the elderly process drugs differently than young/middle aged adults:

CO decreases at an average of 1%/year after age 30

BF decreases due to CO reduction

reduced gastric acid secretion, motility and intestinal absorption

lean body mass and total body water decrease with age while percent body fat increases

the rate of drug metabolism decreases with age

many enzyme systems have decreased production w/age: the enzyme system that appears to be most affected is the mixed function oxidase system

renal BF decreases with age

bioavailability of oral drugs may increase w/ age

**these factors lead to an expected reduced rate of drug metabolism and an increase in duration of drug action

77
Q

special populations?

A

patients taking numerous meds

acute or chronic illness

patients in drug/alcohol recovery

known of suspected alterations in drug metabolism (genetic or other)

Pharmacology (8 decks)

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