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Pharmacology > Intro > Flashcards

Intro Flashcards

1
Q

Pharmacology

A

science of drugs including their origin, composition, pharmacokinetics, therapeutic use, and toxicology

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2
Q

Pharmacokinetics

A

what the body does to a drug as it goes through absorption, distribution, metabolism, and elimination

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3
Q

Pharmacodynamics

A

what the drug does to the body

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4
Q

Pharmacokinetic properties determine

A

the onset
the intensity
the duration of drug action

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5
Q

How can pharmacokinetic properties optimize drug regimens?

A

route of administration
dose
frequency
duration of treatment

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6
Q

Absorption

A

process of a drug entering the systemic circulation

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7
Q

distribution

A

process of a drug leaving the systemic circulation and entering the interstitium (ECF) and the tissues

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8
Q

metabolism

A

process of a drug converting from its original chemical structure into other forms to facilitate elimination from the body

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9
Q

elimination

A

process of removal of a drug from the body

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10
Q

bioavailability

A

extent of administered drug that reaches systemic circulation
high >70%
low < 10%

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11
Q

What affects bioavailability?

A

first pass metabolism in intestine/liver
solubility of drugs
chemical instability
nature of drug formation

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12
Q

Hydrophilic drugs are poorly absorbed due to their inability to cross?

A

lipid-rich cell membranes

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13
Q

enteral

A

admin by mouth
includes enteric coated, extended release, sublingual, and buccal

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14
Q

Parenteral

A

admin directly into systemic circulation
includes IV, IM, SC

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15
Q

Enteral Absorption is

A

variable

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16
Q

Advantages of Oral admin

A

safe and common
convenient
economical

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17
Q

disadvantages of oral admin

A

limited absorption of some drugs due to physical characteristics
1st pass metabolism
drug absorption affected in presence of food/other drugs
low patient compliance

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18
Q

What is 1st pass metabolism?

A

Destruction of drugs by digestive enzymes or low gastric pH before reaching systemic absorption

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19
Q

Enteric coated preparations

A

chemically envelope drugs
prevent a drug from causing gastric irritation
prevent a drug from dissolving in stomach acid, helps it to reach the site of action in the ileum and colon

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20
Q

Extended Release preparations

A

decrease the rate of dissolution to provide slow uniform absorption > 8 hr or longer

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21
Q

Advantages of Extended released preparations

A

decr frequency of dosing, incr patient compliance
maintain therapeutic effect overnight
decr incidence of adverse effects
decr non therapeutic blood levels of the drug that often occur after admin of IR dosage forms

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22
Q

Sublingual admin

A

under the tongue

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23
Q

buccal admin

A

between cheek and gum

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24
Q

Absorption pattern of sublingual and buccal admin

A

rapid
direct systemic absorption

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25
Q

Advantages of Sublingual/ buccal admin

A

easy admin
rapid absorption
bypass 1st pass metabolism

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26
Q

Disadvantages of sublingual and buccal admin

A

limited application to certain types of drugs
only drugs with small doses
must be nonirritating

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27
Q

Parenteral Admin advantages

A

rapid onset of action
bypass 1st pass metabolism
useful for drugs that are poorly absorbed/ unstable in GI tract
highest bioavailability
deliver to unconscious patients

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28
Q

Disadvantages of Parenteral admin

A

irreversible admin not good if ADR occurs
pain, necrosis
infections at site of injection

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29
Q

IV admin

A

into venous blood stream directly
absorption not required

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30
Q

IV admin advantages

A

immediate effect
ideal for drugs with large volumes
suitable for irritating substances and complex mixes
dose titration
ideal for protein and peptide drugs

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31
Q

IV admin disadvantages

A

unsuitable for oily substances
irreversible admin not good in case ADR occurs
precipitation of blood constituents, hemolysis
requires slow injection

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32
Q

IM admin

A

into the muscle

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33
Q

IM admin absorption

A

depends on drug diluent
in aq solns prompt
in depot preparations slow and sustained

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34
Q

IM admin advantages

A

moderated drug volume
suitable for oily vehicles and some irritating substances

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35
Q

IM admin disadvantages

A

painful
potential IM hemorrhage

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36
Q

SC admin

A

beneath the skin

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37
Q

SC admin absorption

A

depends on drug diluents
in aq solns prompt
in depot preparations slow and sustained

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38
Q

SC admin advantages

A

suitable for slow-release drugs
suitable for some poorly soluble suspensions

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39
Q

SC admin disadvantages

A

pain/necrosis if irritating drugs
unsuitable for large volumes of drugs

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40
Q

Inhalation absorption

A

systemic

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41
Q

Inhalation admin advantages

A

rapid absorption
access to blood due to large lung surface area
ideal for gases/volatile substances
dose titration
localized effect to target lungs
fewer systemic side effects

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42
Q

Inhalation admin disadvantages

A

most addictive route
difficulty in regulating dose
difficulty using inhalers

43
Q

Topical admin

A

local admin for local effects

44
Q

mucous membranes

A

conjunctiva
nasopharyngeal
oropharynx
vagina
colon
urethra
urinate bladder

45
Q

In mucous membranes absorption is generally ?

A

excellent

46
Q

What are some examples of topical eye admin?

A

Drug loaded contact lenses
ocular inserts

47
Q

Transdermal admin

A

admin to skin

48
Q

Transdermal admin absorption

A

slow and sustained
dependent on surface area and lipid solubility of drugs

49
Q

Transdermal admin advantages

A

convenient
painless
bypass 1st pass effect

50
Q

Transdermal admin disadvantages

A

irritation
only highly lipophilic drugs
delayed drug delivery to site of action
only drugs with small daily doses

51
Q

rectal admin

A

drug absorbed via rectal mucosa

52
Q

rectal admin absorption

A

erratic and variable

53
Q

Rectal admin advantages

A

partially bypass 1st pass metabolism
ideal for drugs that cause gastric irritation, nausea and vomiting
ideal for patients that are comatose

54
Q

Rectal admin disadvantages

A

irritation to rectal mucosa
lack of patient acceptability

55
Q

intra-arterial admin

A

delivers drug to a particular tissue, or as a diagnostic agent

accidental admin here cause serious complications

56
Q

Intrathecal admin

A

injection directly into the cerebrospinal fluid
bypass blood-brain barrier
used for treatment of brain tumors and for spinal anesthesia

57
Q

What affects drug absorption?

A

pH
blood flow to the absorption site
total surface area available for absorption
contact time at the absorption surface
expression of a transmembrane transporter protein

58
Q

Can charged drugs (A^- or BH^+) diffuse through biological membranes?

A

no

59
Q

For drugs to cross biological membranes what do they need?

A

to be lipid soluble/ have a specific transporter

60
Q

What affects drug distribution?

A

blood flow
capillary permeability
binding of drugs to plasma proteins and tissue proteins
lipophilicity of the drug
volume of distribution

61
Q

Which organs receive most of the administered drug?

A

liver
kidney
brain
other well-perfused organs (lungs)

62
Q

Which organs have slow drug distribution?

A

muscle
visceral organs
skin
fat tissues

63
Q

Does plasma protein binding increase or decrease the amount of drug that can enter tissues from the blood?

A

decrease

64
Q

Albumin

A

binds to acidic drugs

65
Q

alpha1-acid glycoprotein

A

binds basic drugs

66
Q

Fat tissue reservoirs

A

where lipid soluble drugs accumulate
prolongs half-life of drug and duration of action

67
Q

Bone tissue reservoir

A

mostly seen with divalent metal-ion chelating agents and heavy metals accumulate into bone crystal lattice

slow release of toxic agents

68
Q

What do the tight junction in brain capillary endothelial cells prevent?

A

The diffusion of hydrophilic drugs from the blood into the CNS

69
Q

What do the membrane transporters in brain capillary endothelial cells of the blood brain barrier do?

A

remove drugs from the CNS
decr effectiveness of protease inhibitors for treating HIV in the CNS

70
Q

What do pericapillary glial cells in the blood brain barrier do?

A

Form and maintain the blood-brain barrier
establish a diffusion barrier

71
Q

Placental barrier

A

placenta has a [high] of metabolic enzymes and export transporters to decrease the [drugs] that enter fetal circulation

to some degree the fetus is exposed to all drugs taken by the mother

72
Q

Can uncharged drugs diffuse through biological membranes?

A

yes, so HA will diffuse through acidic environments, and bases will diffuse through basic environments

73
Q

Distribution of the drug between ionized and non-ionized forms is dependent on?

A

pH and pKa of the drug

74
Q

When pH = pKa what is the behavior of acids and bases?

A

[HA] = [A^-]
[BH^+] = [B]

75
Q

When pH<pKa what is the behavior of acids and bases?

A

[HA] > [A^-]
[BH^+] > [B]
protonation is favored

76
Q

When pH>pKa what is the behavior of acids and bases?

A

[HA] < [A^-]
[BH^+] < [B]
deprotonation is favored

77
Q

What is the henderson - hasselbalch equation

A

ratio of nonionized to ionized drug at given pH
log (protonated form/unprotonated form) = pKa - pH

78
Q

What percentage of drugs are eliminated unchanged in the urine?

A

25-30%

79
Q

What are the primary organs of metabolism?

A

liver
GI tract
kidneys
lungs

80
Q

Biotransformation

A

process by which lipophilic, xenobiotic, or endobiotic chemicals are converted in body by enzymatic reactions to products that are more hydrophilic.

81
Q

Metabolism Phase 1 reaction

A

oxidation, reduction, hydrolysis
drug may be activated, unchanged, or often inactivated
done by cytochrome P450
converts lipophilic drugs in to polar molecules
result: loss of pharmacologic activity, can sometimes prolong/enhance it

82
Q

Metabolism phase 2 reaction

A

conjugation
conjugated drug is usually inactive
drugs are bound covalently to polar water soluble molecules which are then removed in urine or feces

83
Q

Prodrugs

A

drugs that are inactive in the original structure but activated by phase 1 metabolism

84
Q

What reactions are included in phase 2 metabolism?

A

glutathione conjugation
sulfation
acetylation
glucuronidation

85
Q

Which is eliminated more rapidly, water soluble polar molecules or lipid soluble drugs?

A

water soluble polar molecules

86
Q

What is the general process of drug clearance by the kidney?

A
  1. Glomerular filtration
  2. Active Tubular secretion
  3. passive tubular secretion
87
Q

What is glomerular filtration

A

Free drug passes through the capillary into the bowman space

88
Q

What is the glomerular filtration rate?

A

125 mL/min

89
Q

If renal disease is present what decreases?

A

GFR

90
Q

Does lipid solubility of drug and the pH of the medium affect the glomerular filtration process?

A

no

91
Q

Does GFR and drug-protein binding affect glomerular filtration process?

A

yes

92
Q

Proximal Tubular secretion

A

for drugs not transferred into glomerular filtrate
drugs leave glomeruli through efferent arteries
secretion of organic cationic drugs and organic bases primarily happens by energy-requiring active transport systems

93
Q

Distal tubular reabsorption

A

as a drug moves towards this its concentration incr
uncharged drugs diffuse out the nephric lumen and go back into systemic circulation n
can manipulate urine pH to minimize this

94
Q

To minimize distal tubular reabsorption what should be done for an acidic drug? A basic drug?

A

for acidic drugs alkaline the urine
for basic drugs acidify the urine

95
Q

When drug concentration in the filtrate is greater than in the tubular lumen…

A

hydrophobic drugs diffuse out

96
Q

Are polar/ionized conjugate able to diffuse out of the kidney lumen?

A

no

97
Q

Biliary Excretion

A

transporters in liver cells transport amphipathic lipid soluble drugs into the bile which is then eliminated in feces

98
Q

Enterohepatic Recycling

A

some drugs that are secreted into the bile can be reabsorbed by the intestinal tract and renter the circulation

99
Q

passive diffusion

A

concentration gradient across a membrane
[high] the gut lumen -> [low] the blood
no energy/carrier
not saturable
majority of drugs absorbed this way
water soluble drugs: aqueous channels/pores
lipid-soluble drugs: dissolve in lipid bilateral membranes and cross the biological membranes

100
Q

facilitated diffusion

A

concentration gradient across a membrane
does not require energy
[high] -> [low]
requires carriers
- conformational changes
- can be saturated
- could be inhibited by compounds competing for the carrier

101
Q

Active transport

A

against a concentration gradient across a membrane
[low] -> [high]
requires energy
requires carriers
- can be saturated
- selective
- may be inhibited by co-transported substances competing for the carrier

102
Q

endocytosis

A

large drug molecules engulfed by the cell membrane and transported into the cell through a vesicle

103
Q

P-glycoprotein

A

transmembrane transporter protein
transports drugs from tissues to blood by pumping drugs out of cell
if highly expressed it reduces drug absorption
associated with multidrug resistance

Pharmacology (16 decks)

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