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Pharmacology Flashcards

1
Q

Vd: Definition and physiological significance

A

Volume of distribution

Measurement of how much of a drug is distributed into organs/tissues rather than remaining in systemic circulation

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2
Q

Who is the first line of defense against a pt getting on the wrong medication?

A

prescribers

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3
Q

What is pharmacokinetics?

A

how the body impacts the drug–> absorbed, distributed, eliminated

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4
Q

What is a standard drug dose?

A

based on trials in “healthy” individuals with “average” physiologic processes

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5
Q

In what form is a drug able to go to and have an effect on target receptors?

A

free form/ not bound

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6
Q

If needed how do drugs, which are usually large and polar, get through the cell membrane?

A

protein pores/channels, facilitated/active carriers, some can move through based on diffusion

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7
Q

uncharged molecules are readily…

A

lipid-soluble

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8
Q

charged molecules are readily…

A

water-soluble

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9
Q

pKa

A

charged

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10
Q

pKa>pH (drug form)

A

uncharged

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11
Q

Alkaline urine favors the excretion of…

A

weak acids

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12
Q

Acidic urine favors the excretion of…

A

weak bases

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13
Q

Drugs designed to act on the CNS must be…

A

hydrophobic

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14
Q

intrathecal administration

A

drug is directly injected into the CSF/ bypasses the BBB

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15
Q

What are four ways drugs can be taken up?

A

enteral, parenteral, transdermal, and mucous membranes

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16
Q

First-pass metabolism occurs where and affects what drugs?

A

in the liver, oral drugs only

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17
Q

What is first-pass metabolism?

A

drugs are carried from GI to the liver via the hepatic portal vein and since the liver is a major site of metabolism, the liver may modify drugs rendering them inactive or reduce how much is actually sent to the target tissue (sometimes the opposite will occur and the drug will activate)

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18
Q

Bioavailability

A

(drug reach systemic circulation/drug administered)
the fraction of uncharged drug reaching the system circulation
between 0-100

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19
Q

Bioequivalence

A

compares the bioavailability of a generic drug to the brand name–> should have the same amount of active ingredient and the same predictable response

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20
Q

What is a loading dose?

A

initial doses of a drug that is administered to compensate for distribution into the body tissues; gets the pt to steady state quicker

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21
Q

What is loading dose dependent on?

A

volume of distribution

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22
Q

If Vd is high then plasma drug concentration is…

A

low; the drug will be extensively distributed to the tissues(muscle, adipose, and other non-vascular compartments)–> has a LONG duration of action

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23
Q

What is the steady state?

A

therapeutic dosing of a drug maintained during peaks(high [drug]) and lows(low [drug])– usually takes between 3-5 half-lives to achieve

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24
Q

What is a maintenance dose?

A

subsequent doses used to replace the amount of drug lost through metabolism/excretion/ goal is to maintain a steady state concentration

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25
What is a maintenance dose dependent on?
clearance = (metabolism+excretion)/[drug]plasma
26
Tight junctions restrict drug distribution into the sanctuary compartments. What are these?
the blood-brain barrier in the CNS and the blood-testes barrier in the testes
27
Where in the body are you likely to find water-soluble drugs?
blood
28
Where in the body are you likely to find fat-soluble drugs?
cell membranes, adipose, and other fat-rich areas
29
Vd (equation)
= amount of drug in body/ plasma drug [ ] | remember it can exceed body volume
30
Example of a drug with a low Vd
heparin (mostly found in the vascular compartment)
31
Vd of 42L example
alcohol
32
Examples of high Vd (over 42L)
chloroquine, azithromycin, digoxin
33
Rate of accumulation into tissue compartments depends on?
blood flow, the chemistry of the drug, and plasma protein binding of the drug
34
What are the three binding proteins?
albumin (acidic binding), alpha 1 acid glycoprotein (basic drug binding), and lipoprotein (lipophilic drug binding)
35
Only _____ drugs can act at target sites and elicit biological responses
free, unbound
36
A disease state of drug can displace a highly bound protein drug and _____ the free drug state. Two examples are
hypoalbuminemia and ceftriaxone(exacerbate the hyperbilirubinemia)
37
Monitor a _____ clearance drug with a low therapeutic window when coadministered with a drug known to cause_______. Three examples are...
low; displacement interactions | Warfarin, phenytoin, and tolbutamide
38
How do you calculate drug doses for neonates/infants?
mg/kg (remember adults are given a standard dose
39
Peds- as you increase TBW and EC what happens to VD for hydrophilic drugs?
increases
40
Elderly- as TBW decreases, what happens to Vd for hydrophilic drugs?
also decreases; this results in higher serum levels
41
Elderly during acute illness - decrease in plasma protein (albumin) - increase alpha 1 acid glycoprotein
- increase % of unbound drug | - decrease % of unbound drug (basic)
42
Drug metabolism/biotransformation utilizes endogenous enzyme systems such as:
cytochrome P540 systems(oxidative biotransformation), alcohol dehydrogenase, monoamine oxidase (MAO)
43
Phase I reactions
oxidation/reduction Goal: add/uncover polar moiety mediated by cytochrome 450
44
Phase II reactions
conjugation/hydrolysis | Goal: increases polarity by adding more soluble moiety
45
What is the aim of Phase I and Phase II rxns?
reduce lipid solubility/increase hydrophobicity
46
What are three important conjugation rxns?
glucuronidation, acetylation, sulfation
47
Cytochrome P450 System
heme protein mono-oxygenases smooth ER CYP
48
CYP 3A4
inhib- grapfruit | induce- St. John's Wort
49
CYP 2E1
induce- ethanol
50
CYP 1A2
induce- Tobacco smoke
51
First-Order Elimination
divide by half each time
52
Zero-Order Elimination
a constant amount of excretion
53
What is the clinical significance of zero-order elimination?
a small increase in dose = large increase in blood levels
54
Maximal efficacy, Emax
largest effect that a drug can produce
55
ED50
dose of a drug required to produce a defined therapeutic effect in 50% of the population
56
LD50
dose that is lethal 50% of animals treated or adverse effects
57
Therapeutic Index (TI)
the ratio Ld50/ED50; relative safeness of a drug
58
efficacy
effectiveness
59
potency
smaller ED50
60
Botulinum toxin
clostridium botulinum--> inhibits skeletal muscle contraction(no ACh released at the neuromuscular jxn)
61
Pharmacological agonist
mimic actions of endogenous NT
62
Pharmacological antagonist
block actions of NT
63
competitive antagonist
reduce potency, no effect on the efficacy
64
noncompetitive antagonist
reduce efficacy
65
inverse agonist
action opposite to agonist
66
partial agonist
acts at the same site as the full agonist but lower maximal efficacy
67
Sensitivity
up-regulation
68
tolerance
down-regulation
69
additive
equal to the sum of their individual effects
70
synergistic
together the effect is greater than the sum of their individual effects
71
tachyphylaxis
decreased drug response by many potential mechanisms
72
pharmacodynamics
study of drugs on people
73
Why is pharmacotherapy described as a double-edged sword?
It can have both therapeutic benefits and unintended effects of the drug
74
ADE/ADR
Adverse Drug Effects/Adverse Drug Responses
75
What organs are most likely to be involved in an ADE? Why?
liver and kidneys-- they metabolize and filter
76
What are dose-dependent types/mechanisms of toxicity?
pharmacological toxicity, pathological toxicity, genotoxicity
77
What is a dose-independent mechanism of toxicity?
allergic rxn
78
What are idiosyncratic mechanisms of toxicity?
extreme sensitivity, extreme insensitivity
79
In dose-dependent ADRs, the severity of the toxic event depends on ______________.
length of exposure----> affected by the ability to eliminate/metabolize drugs
80
What are 4 drugs with narrow therapeutic windows?
anticoagulants(warfarin), antiarrhythmics, anticonvulsants, digoxin
81
What are some considerations you should take when prescribing a drug with a narrow therapeutic window?
monitoring blood levels of the drug, assess the necessity of the drug, and monitor the health of organ systems
82
Hepatotoxicity
elevated serum levels of bilirubin and intracellular hepatic enzymes: ALT and AST and ALP(shouldn't even be in serum)
83
Nephrotoxicity
reduced creatinine in urine--> signals muscle breakdown; also will have some edema
84
Hypersensitivity
rash, IgE levels
85
Pharmacological Toxicity (dose-dependent): On-target
inappropriate interaction with the intended receptor | Eg. overdose, right receptor but wrong tissue, effects of chronic inhibition/activation
86
Pharmacological Toxicity (dose-dependent): Off-target
interactions with unintended receptors
87
What is one example of a drug with an off-target effect? What happens in this case?
Propranolol is a non-selective beta-blocker; it works on beta-1 and beta-2 receptors alike. Inhibition of B1 receptors led to reduced HR and decreased BP, the intended effect. Inhibition B2 receptors led to reduced bronchodilation and worsened asthma, an unintended effect.
88
Pathological Toxicity (dose-dependent)
body's ability to metabolize or inactivate damaging toxicants is overwhelmed --> can lead to irreversible cell injury and uncontrolled cell death aka necrosis(cellular damage/organ damage)
89
Pathological Toxicity (dose-dependent) BSEP example?
Off-target bile salt export protein(BSEP) inhibition: The BSEP transports digestive bile salts from hepatocytes into the biliary duct. Inhibition of the BSEP causes bile salts to accumulate in the hepatocytes leading to a necrotic effect(on a large enough scale; intrahepatic choleostasis).
90
Pathological Toxicity (dose-dependent) Biotransformation of Acetaminophen example?
Drugs can undergo biotransformation into toxicants. Acetaminophen can be metabolized into NAPQ, which in the absence of GSH can lead to hepatotoxicity/liver failure.
91
Genotoxic Toxicity (dose-dependent)
results from damage to DNA; usually a long-term development | EG. chemotherapeutic agents, environmental toxins, ionizing radiation
92
Apparent Dose
the dose equivalent that would have resulted in the blood concentration levels observed under "normal" circumstances
93
What are some absorption factors that affect apparent dose?
slower motility= other drug slows motility(anticholinergic agent), drug itself slows motility (aspirin overdose) altered gastric pH= high pH means there are less protons available; lower pH means there are more protons available---effect on absorption depends on drugs pKa
94
What is a distribution factor affecting apparent dose?
Hypoproteinemia-> reduced plasma protein binding can increase the fraction of free drug Due to malnutrition, liver disease, nephrotic syndrome, sepsis(elevated TNF-alpha in the bloodstream)
95
What are some elimination factors affect the apparent dose?
reduced elimination renal clearance depends on adequate blood flow, drugs can block the blood filtration process, alteration of urine pH can be used to enhance elimination
96
What are some metabolic factors affect apparent dose?
impaired hepatic fxn--> impaired blood flow, blockade of transporters, reduced expression/inhibition of metabolizing enzymes
97
What effect do inhibition and induction have on apparent dose?
``` Inhibition = increases levels of the drug in the blood Eg. grapefruit juice on CYP3A4 Induction= decreases levels of drug in the blood Eg. rifampin CYP3A4 ```
98
What are two examples of drug pairings that have pharmacodynamic interactions that can stimulate elevated drug levels?
propofol and barbiturate | warfarin and aspirin
99
Type I: Hypersensitivity (dose-independent/ allergy)
IgE antibodies bind to an allergen(drug) or hapten and inflammatory mediators are released(histamine, serotonin, leukotrienes) vasodilation, edema, inflammation, asthma, anaphylaxis Eg. penicillin-occurs immediately
100
Red Man Syndrome: Type I: Hypersensitivity (dose-independent/ allergy)
IV administration, anaphylactoid mechanism--> mast cells degranulate independent of stimulation by IgE flushing, erythema, pruritus, mostly in upper body Eg. vancomycin, ciprofloxacin, amphotericin B, rifampin
101
Type II: Cytolytic Reactions (dose-independent/ allergy)
antibody-dependent cytotoxic hypersensitivity autoimmune response--> drug binds to RBC--> IgE/IgM recognize drug-cell complex--> cells are lysed(complement and cytotoxic Tcells) Eg. penicillin-induced hemolytic anemia
102
Type III: Arthus Reactions (dose-independent/ allergy)
serum sickness soluble antigens(drugs) are complexed with IgG and IgM then are deposited into the vasculature endothelium; tissue may undergo necrosis Eg. antivenins (antivenom)
103
Type IV: Delayed Hypersensitivity Reactions
results from sensitized T cells encountering a familiar antigen, first exposure doesn't cause a response, repeated exposure can cause a cytokine storm Eg. contact dermatitis, poison ivy, latex allergy, ciprofloxacin, Stevens-Johnson Syndrome, toxic epidermal necrolysis

Foundations (6 decks)

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