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baby pharm > Exam 1 > Flashcards

Exam 1 Flashcards

1
Q

T/F
Covalent bonds are always stronger than ionic bonds.

A

False

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2
Q

Which type of bonds are often irreversible by biological systems?

A

Covalent

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3
Q

Van der Waals forces are usually associated with

A

Lipid bonding

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4
Q

Disulfide bridges are examples of ______ bonding and are found in ____.

A

Covalent; DNA

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5
Q

Electrostatic forces are an example of ____ bonding.

A

Ionic

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6
Q

T/F
Hydrogen bonding is weaker than ionic bonds.

A

True

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7
Q

T/F
Hydrophobic interactions are generally strong.

A

False; they’re weak

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8
Q

What bond/interactions exist between lipophilic drugs and lipid component of membrane/receptor?

A

Hydrophobic

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9
Q

Most drugs are _____.

A

Weak bases

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10
Q

Diffusion thru cell membrane requires _____.

A

Lipid solubility

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11
Q

T/F
Drugs that are proteins are best given by mouth.

A

False; stomach acid denatures proteins

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12
Q

Pharmacodynamic examines the effect the ____ has on the ____.

A

How the drug affects the body

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13
Q

Pharmacodynamics relates ____ and ____.

A

Drug concentration & its effect.

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14
Q

Pharmacokinetics relate ____ and ____.

A

Dose & tissue concentration.

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15
Q

T/F
All drugs can be mathematically modeled to predict absorption and metabolism.

A

False

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16
Q

Acidic Rx in acidic conditions will….

A

Cross the GI mucosa and enters bloodstream.

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17
Q

Basic drugs are best absorbed ____.

A

In lower GI tract; below beginning of SM intestine

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18
Q

T/F
Drugs with high affinity always give high effect.

A

False; high affinity does not guarantee high effect. It can bind without producing effects.

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19
Q

Affinity

A

Level of attraction between compound and receptor.

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20
Q

High affinity + low intrinsic activity

A

Competitive antagonist

must have affinity b/c it binds
little/no intrinsic activity b/c it does not stimulate receptor very well

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21
Q

What aspect contributes to higher side effects?

A

Low specificity

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22
Q

Low affinity drugs have a (higher/lower) KD than high affinity drugs.

A

Higher

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23
Q

High affinity drugs occupy _____ receptors at ____ concentrations.

A

High affinity occupies many receptors at low concentrations.

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24
Q

More potent drugs have (higher/lower) EC50.

A

Lower EC50
EC50 = concentration that gives half of max effect

Higher potency = lower [ ] needed

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25
Q

Which is more potent?
Which has higher efficacy?

A

A is more potent (more to the left)
B has higher efficacy (reaches higher point on y axis)

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26
Q

(T/F)
The action of an agonist at a receptor can also be a side effect.

A

True

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27
Q

Which part of the neuron generates the action potential?

A

Axon hillock

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28
Q

(T/F)
Drug receptors can be found in the cytoplasm and nuclear envelope.

A

True

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29
Q

Digitalis works by

A

Inhibiting Na/K/ATPase pump of myocytes

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30
Q

What are some types of nonspecific acting drugs?

A

Carbon Monoxide (binds to Hgb)
Alkalinizing drugs
Acidifying drugs
Mannitol (pulls water into urine)

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31
Q

Anesthetics mechanism of action

A

Most effects are receptor mediated.
Alters membrane fluidity, making it less gelatinous and losing membrane pump function.

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32
Q

Aminoglycoside antibiotics act on…
What are some examples of aminoglycoside meds?

A

The ribosome
Impairs bacterial protein production.
gentamicin, amikacin, tobramycin, neomycin, and streptomycin

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33
Q

Neuroleptics act in ____ and are used as ____

A

The CNS
Tranquilizers

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34
Q

(T/F)
All drugs exert their effects via receptor-mediated response.

A

False
Mannitol, methyl cellulose and dextrans are non-receptor mediated drugs.

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35
Q

_____ is/are responsible for transduction of biologic signals.

A

Receptors

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36
Q

(T/F)
Enzymes can be drug receptors.

A

True

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37
Q

What drug acts on nucleic acids?

A

Actinomycin D

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38
Q

Altering the ligand structure will affect its

A

Affinity and/or intrinsic activity (due to required fit for binding site)

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39
Q

Examples of drugs that do not act on receptors

A

Some anesthetics, hypnotics, and sedatives
Alcohols
Osmotically-active drugs
Acidifying/alkalinizing agents
Antiseptics
Mannitol
Methyl cellulose
Dextrans

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40
Q

Nonspecific receptors require ____ drug concentrations to produce effect. Specific receptors require ____ .

A

Nonspecific receptors need high concentrations of drug for effect (milimoles or moles).
Specific needs only low concentration (nano to mili moles).

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41
Q

When active, _____ converts ATP to cAMP.

A

Adenylate cyclase

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42
Q

_____________ function as pores, allowing passage of Na into smooth muscle.

A

Electrotonic gap junctions

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43
Q

(T/F)
When part of a motor unit, a muscle fiber can be stimulated individually.

A

False; they are stimulated as a unit.

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44
Q

Propagation vs. diffusion of a charge down the axon

A

Diffusion is less effective, as the charge would be reduced once it reaches the terminal.

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45
Q

Na coming into the neuron _____ voltage.

A

Increases

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46
Q

When K exits the neuron, it restores the more ____ charge.

A

Negative

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47
Q

Local anesthetics work by

A

Blocking Na channels in the neuron, preventing transmission of the impulse down the axon.

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48
Q

Noncompetitive antagonism on a response curve will show as

A

Flattening curve as more inhibitor is added

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49
Q

Positive allosterism is seen on a response curve as

A

Left shift, similar to increasing potency

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50
Q

What happens in positive allosterism?

A

The ligand increases receptor affinity for agonist.

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51
Q

What happens in negative allosterism?

A

Inhibitor decreases affinity for agonist to bind to receptor.
Response curve looks similar to non-competitive antagonism; curve flattens as more inhibitor is added.

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52
Q

Fat receives less of what supply?

A

Water and blood

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53
Q

(T/F)
The constituents of ICF and ECF are identical, but vary in quantity.

A

True

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54
Q

Proteins are more abundant in the (ICF/ECF).

A

ICF

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55
Q

Which are mostly in ECF? Which are mostly in ICF?
K
Cl
Na

A

ECF: Na, Cl
ICF: K

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56
Q

ECF is regulated by the ____

A

Kidneys

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57
Q

(T/F)
All cells have a nucleus.

A

False
RBCs do not have a nucleus.

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58
Q

What are the most abundant constituents of lipid membranes?

A

Proteins and phospholipids

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59
Q

How does water enter the cell?

A

Passive diffusion & aquaporins (proteins that fxn as water channels)

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60
Q

T/F
Glucose can readily enter the cell.

A

False
The membrane is nearly impermeable to ions and glucose.

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61
Q

T/F
Steroids can readily pass thru the cell membrane.

A

True
Fat-soluble substances, such as steroids readily cross the membrane.

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62
Q

Gases such as O, CO2, & N pass thru the membrane easily via _____

A

Diffusion

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63
Q

Glucose and amino acids enter the cell thru _______.

A

Facilitated diffusion

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64
Q

How can a cell uptake material without it actually passing thru the membrane?

A

Endocytosis

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65
Q

_____ ions are required to eject neurotransmitters via ____.

A

Calcium
Exocytosis

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66
Q

T/F
The goal of the Na/K/ATPase pump is to reduce the number of ions in the ICF.

A

True
Must balance the large amount of protein and other intracellular stuff

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67
Q

Malignant hyperthermia is linked to a defect in the gene encoding proteins for the ______ receptor, the primary receptor for releasing Ca from the sarcoplasmic reticulum.

A

Ryanodine

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68
Q

The Na/K/ATPase pump, pumps Na and K _____ their gradient.

A

Against
Requires ATP = active transport = against gradient

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69
Q

What is the primary transmembrane transporter for drugs across the BBB?

A

P-glycoprotein

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70
Q

When going against the concentration gradient, a _____ is often needed, which requires ____.

A

Proteins are often needed, which require ATP

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71
Q

Genetic defects in aquaporins may cause which diseases?

A

Congenital cataracts
Nephrogenic diabetes insipidus

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72
Q

T/F
The nucleus of an egg cell has 46 chromosomes.

A

False
All nucleus have 46 chromosomes, except eggs which have 23

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73
Q

Histones

A

Proteins that cover DNA and regulate transcription

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74
Q

What passes thru nuclear pores?

A

Large mlcls, such as proteins, DNA & RNA

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75
Q

What does the nucleolus do?

A

Synthesize ribosomes

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76
Q

________ coordinates movement of chromosomes during cell division.

A

Centrioles

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77
Q

What happens to noncoding genes?

A

They are transcribed to RNA but not translated into proteins.

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78
Q

Mitochondria contain…..

A

Enzymes and substrates of the Krebs cycle and ETC.

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79
Q

Oxidative phosphorylation occurs ______.

A

In the mitochondria

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80
Q

Where are the protons generated through the ETC?

A

Between the 2 lipid membranes of the mitochondria

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81
Q

In the ETC, what drives the conversion from ADP to ATP?

A

The movement of protons back into the mitochondrial matrix through the inner membrane.

moves: intermembrane space –> thru inner membrane –> mitochondrial matrix

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82
Q

What enzyme converts ADP to ATP?

A

ATP synthase

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83
Q

T/F
Mitochondria are always inherited from the mother.

A

True
Sperm have no mitochondria

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84
Q

Ribosomes are mainly composed of ____.

A

RNA

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85
Q

T/F
The rough endoplasmic reticulum lacks ribosomes.

A

False
The smooth ER lacks ribosomes

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86
Q

The sarcoplasmic reticulum is a reservoir for ___.

A

Calcium

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87
Q

Proteins made in the rough ER are sent to _______ where they are stored in __________.

A

Golgi apparatus
Secretory vesicles

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88
Q

_____ vesicles continuously secrete their content. ____ vesicles release their content when a trigger signal is received.

A

Exocytotic vesicles continuously secrete.
Secretory vesicles secrete when signaled.

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89
Q

What makes lysosomes?

A

Golgi apparatus

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90
Q

Regulated secretion in anesthesia includes

A

Neurotransmitter release

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91
Q

Studies what the body does to a drug.

A

Pharmacokinetics

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92
Q

Studies what the drug does to the body.

A

Pharmacodynamics

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93
Q

T/F
Different patients can have similar plasma concentrations of a drug but vary in response.

A

True

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94
Q

Chiral

A

A center with 3-dimensional asymmetry

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95
Q

T/F
Enantiomers can be superimposed on each other if rotated correctly.

A

False
Enantiomers are non-superimposable mirror images

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96
Q

A D enantiomer rotates light in which direction? Is it negative or positive?

A

D config:
Clockwise
+
Dextrorotatory

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97
Q

An L enantiomer rotates light in which direction? Is it negative or positive?

A

L config:
Counterclockwise
-
Levorotatory

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98
Q

Racemic mixture

A

Contains equal parts of two enantiomers. They cancel each other out. No rotation of light.

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99
Q

T/F
Enantiomers usually have identical pharmacological activity.

A

False
They can have different absorption, distribution, potency, clearance and toxicity.

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100
Q

T/F
Enantiomers can antagonize each other’s effects.

A

True

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101
Q

T/F
Systemic therapy can be achieved through topical administration.

A

True
transdermal patches and some creams/ointments can achieve this

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102
Q

T/F
Aerosols penetrate completely to the alveoli.

A

False
Aerosols are used for localized airway and bronchial tissue.
Gaseous and volatile agents penetrate completely to the alveoli.

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103
Q

What is one challenge with rectal administration?

A

There is an unpredictable volume of water, making absorption unpredictable.

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104
Q

T/F
First pass metabolism can be avoided with rectal administration.

A

True
Drugs absorbed in the lower intestines do not go directly to liver before the heart.

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105
Q

Which route of administration has no absorptive phase?

A

IV

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106
Q

Why give a drug through an artery?

A

give high concentration to a target tissue
chemo & diagnostics
fewer local irritations

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107
Q

Epidural injections are made inside ____ but external to ______.

A

inside the bony spine but external to the dura matter

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108
Q

Max volume for IM injection

A

5 ml

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109
Q

Which absorbs faster into systemic circulation? SubQ or IM?

A

IM

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110
Q

Depot injection

A

Offers slow absorption of the agent over a prolonged period.
Long term therapy with fewer doses.
Usually prepared in oil.

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111
Q

Most drugs cross tissue membranes by _____.

A

simple lipid diffusion

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112
Q

What happens with drugs that are too lipid soluble?

A

Cannot move out of the membrane once it enters

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113
Q

Lipid solubility to water solubility
“oil-to-water partition coefficient”

A

Predicts how well a drug will cross biological membranes.
Measures the [ ] of each.
Octanol is used b/c its similar to biological membranes.
Larger value = more lipid soluble

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114
Q

T/F
Amino acids are neutral at biological pH.

A

False
they are charged

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115
Q

Transport molecules are proteins and can be found ____.

A

in cell membranes

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116
Q

Gases and volatile agents must possess ____ to cross from the alveoli into the blood?

A

some blood & lipid solubility

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117
Q

The blood-to-gas partition coefficient uses the _____ of the agent in each component.

A

partial pressure

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118
Q

What is the driving force to bring gases and volatile agents in the blood?

A

The higher initial partial pressure of a gas/volatile agent at the alveoli is the driving force for the movement of the molecules into the blood until equilibrium is reached.

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119
Q

Tissue-to-blood partition coefficient

A

Relative solubility of a drug in a tissue compared with the blood.
Determines what tissues Rx enters and to what extent.

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120
Q

T/F
Tissue-to-blood partition coefficient can be used to determine effect.

A

False
Some drugs may enter tissue to a small extent but have great effect.

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121
Q

An acidic compound is uncharged in the (protonated/unprotonated) form.

A

Acidic:
uncharged when protonated

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122
Q

A basic compound is uncharged in the (protonated/unprotonated) form.

A

Basic:
uncharged when unprotonated

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123
Q

T/F
Procaine has a slower onset than Lidocaine

A

True
Lidocaine pKa 7.9
Procaine pKa 8.9

With procaine, it takes longer for the ionized molecules to become unionized.

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124
Q

A weak base drug in acidic conditions will be (ionized/not ionized).

A

Ionized

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124
Q

T/F
Onset of a drug is affected by pKa.

A

True

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125
Q

T/F
The thickness of a membrane does not affect rate of diffusion.

A

False
Thicker membrane = slower diffusion

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125
Q

T/F
Diffusion rate can increase if there is a large difference in drug concentrations from one side of the membrane to the other.

A

True

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125
Q

T/F
Drugs that are weak bases absorb well in the stomach.

A

False

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126
Q

Solid dosage forms, such as tablets and capsules must undergo ____ before being absorbed.

A

dissolution
the process by which solid dosage form breaks into individual molecules/small absorbable particles

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127
Q

Acid labile

A

Easily denatured by acid.
Enteric coating used to protect from stomach so it can be dissolved in small intestine.

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128
Q

Acidic drugs in acidic conditions will be (ionized/not ionized).

A

Not ionized

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129
Q

Which type of drug will absorb well in the stomach? Weak acid or weak base?

A

Weak acid drugs absorb well in the stomach.

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130
Q

Passive diffusion requires a drug to be ___.

A

Passive diffusion requires a drug to be in a lipid soluble form.

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131
Q

Most drugs are best absorbed in ______.

A

Most drugs are best absorbed in the small intestine.

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132
Q

What feature of the small intestine increases absorption? What feature might make absorption more difficult?

A

Microvilli increase the surface area for absorption.
The glycocalyx layer keeps very lipid-soluble drugs from entering epithelium (Large octanol-to-buffer values)

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133
Q

Epithelial endocytosis

A

In GI tract, highly lipid-soluble drugs can bind to fats and be absorbed this way as opposed to passive diffusion.

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134
Q

Distribution

A

after absorption, the drug is transported through the body and crosses into tissues

135
Q

The 2 most common proteins to which drug molecules bind are _____. How strong are these bonds?

A

albumin
a1-acid glycoproteins
weakly bonded

136
Q

T/F
Only free, unbound drug can cross into tissue and act. Drug bound to protein is unavailable to act.

A

True

137
Q

T/F
Plasma protein binding can act as a reservoir of drug.

A

True
Protein binding is an equilibrium. Plasma protein binding can slowly supply additional free drug into plasma as drug plasma levels drop d/t distribution or elimination.

138
Q

T/F
As more drug leaves the plasma into tissues or is excreted, protein-bound drug is released into plasma to restore an equilibrium.

A

True

139
Q

What methods are able to bring drug into tissues?

A

passive diffusion
transport protein
endocytotic mechanisms

140
Q

The driving forces for diffusional distribution into a tissue are…… (3)

A

relative solubility in a given tissue
concentration gradient
rate of blood flow to tissue

141
Q

Redistribution

A

drug moves from one tissue to another in response to equilibrium shifts

142
Q

As plasma concentration of a drug decreases (distribution or elimination), the drug will….

A

move back into plasma from tissue to establish equilibrium

143
Q

Highly lipophilic anesthetics exit ____ and redistribute to _____ where they are more soluble, which causes short duration of action.

A

Exit the brain and redistribute to body fat

144
Q

The primary organ of metabolism

A

liver
others:
kidneys, lungs, skin, GI epithelium, plasma

145
Q

Drugs metabolized to less polar forms may lead to…..

A

build up and toxicity

146
Q

In order to excrete drugs, they must be metabolized into a more ____ form.

A

polar

147
Q

Phase I metabolism involves mostly _____ reactions.

A

oxidation-reduction

148
Q

The four types of reactions in Phase I metabolism

A

hydroxylation
oxidation
reduction
hydrolysis

149
Q

Drugs may be removed from the body by …..

A
  1. kidneys
  2. enter the biliary fluid and excrete thru bile
150
Q

T/F
Phase I metabolism is not enzymatic, so its capacity cannot be oversaturated.

A

False
Phase I metabolism IS enzymatic, so the enzymes can be overwhelmed (too high of a dose or multiple drugs that work the same enzyme). Risk buildup and toxicity.

151
Q

Induction (metabolism)

A

A drug may increase the number of active enzymes. Shortens the half-life of a drug metabolized by the affected enzyme. Smoking can do this.

152
Q

The goal of metabolism and elimination is to make the drug…..

A

more water-soluble or at least less lipid soluble

153
Q

Prodrug

A

A group is added to the drug itself to aid in absorption. This group is metabolized, leaving the active form of the drug.

154
Q

Which phase of metabolism is known as synthetic?

A

Phase II

155
Q

Which phase of metabolism is characterized by CYPs? What do these do?

A

Phase I
The cytochrome P450 enzymes (“mixed function oxidase system”).
Have a heme group that helps carry out redox reactions.
Mostly hepatic microsomal enzymes (observed via lab technology) & some mitochondrial P450.

156
Q

Mixed function oxidase system

A

The CYPs!
Phase 1 metabolism
Have a heme group that helps carry out redox reactions.
Mostly hepatic microsomal enzymes (observed via lab technology) & some mitochondrial P450.

157
Q

Which CYP enzymes metabolize most drugs?

A
  1. CYP3A4/5
  2. CYP2D6
  3. CYP2C8/9
158
Q

Synthetic reactions

A

Phase II metabolism
attach large polar groups to the molecule being metabolized

159
Q

In hepatocytes, the enzymes for Phase II metabolism are located…

A

in the cytoplasm and on smooth ER

160
Q

What is the most common reaction in Phase II? What happens?

A

Glucuronic acid conjugation/ “Glucuronidation”
A sugar group (uridine diphosphoglucuronic acid, UDPGA) is attached

161
Q

Are sugar groups lipid or water soluble?

A

water soluble

162
Q

Glutathione conjugation
When does it occur?
What happens?

A

Phase II metabolism
The tripeptide glutathione is attached (makes more water-soluble), eventually producing a mercapturic acid derivative, which can be excreted.

163
Q

What are the synthetic reactions of Phase II metabolism?(7)

A

Glucuronic acid conjugation/ “Glucuronidation”
Glutathione conjugation
Sulfate conjugation
Glycine conjugation
Glutamate conjugation
Acylation/acetylation
Nonmicrosomal hydrolysis

164
Q

First pass effect

A

(oral absorption)
Drugs absorbed thru GI enter hepatic portal system to liver, which may highly metabolize the drug before reaching systemic circulation.
ex: lidocaine

165
Q

Bioavailability

A

amount of drug that reaches systemic circulation after absorption

166
Q

T/F
All drugs are subject to first pass effect.

A

False
IV and rectal administration do not experience first pass effect.
Oral route is mostly affected.

167
Q

Local anesthetics are (strong/weak) (bases/acids).

A

Weak bases

168
Q

Some examples of ester drug molecules. How are what enzyme helps to metabolize/inactivate them?

A

plasma esterase or pseudocholinesterase

Succinylcholine
Etomidate
Procaine

169
Q

In the ____, angiotensin I is converted into angiotensin II by _______.

A

Angiotensin I is converted to angiotensin II in the lungs by angiotensin-converting enzyme.

170
Q

T/F
Metabolism is a form of drug elimination.

A

True
Metabolizing a drug into a different form (active or not) is a type of drug elimination.

171
Q

T/F
A drug can still be considered in its original form after metabolism, depending on the changes made.

A

False
Metabolites are not the same as the original drug. The original drug molecule is no longer present in the body.

172
Q

What is the primary excretory organ?

A

kidneys

173
Q

What conditions must a drug meet to be easily/readily filtered at the glomerulus?

A

unbound
MW up to 5000 amu
positively charged

174
Q

Where does the reabsorption occur in the kidney?

A

proximal and distal regions

175
Q

T/F
Weak acids and weak bases are easily excreted via urine.

A

True
They are somewhat ionized.
Urinary acidifiers can help enhance the excretion of weak base drugs. Urinary alkalinizers enhance the elimination of weak acid drugs.

176
Q

To enhance excretion of weakly acidic drugs via urine, _______ may be given.

A

Urine alkalinizers

Urinary acidifiers can help enhance the excretion of weak base drugs. Urinary alkalinizers enhance the elimination of weak acid drugs.

177
Q

T/F
Liver cells can secrete drug molecules and metabolites into bile. This requires active transport carriers.

A

True

178
Q

T/F
Clearance, measured in volume/time, uses volume of the drug.

A

False
Volume reflects plasma containing the drug, not just the drug itself.

179
Q

What is the goal of pharmacokinetics?

A

Quantitatively depict ADME and clearance.
Predict the fate of the drug, dosing, and best route.

180
Q

What makes a drug difficult to predict mathematically?

A

irreversibly acting drugs
drugs that tend to develop tolerance
drugs that act synergistically

181
Q

Drug synergism versus additive effects

A

Additive effects will give you a sum of the two different meds.

Synergism will have a higher effect than the sum of the two.

182
Q

T/F
Drugs that follow total body water are difficult to predict mathematically.

A

False
This attribute makes for easier prediction

183
Q

T/F
Intensity of effect is r/t to the concentration of bound drug in plasma.

A

False
Free drug

184
Q

Pros of synergism

A

Less anesthetic required
lower doses of each drug
lower risk of toxicity

Ex: Versed in pre-op working synergistically with anesthetics d/t its CNA depressive effects

185
Q

Fick’s Law

A

larger molecules are more difficult/slower to diffuse/absorb

memory tip: “big Fick energy”

186
Q

T/F
Drugs only need to be lipid soluble to be absorbed.

A

False
High lipid solubility may prevent a drug from crossing the glycocalyx

187
Q

Why should you not apply topical creams to abraded skin?

A

It will absorb faster than formulated to do so, creating a higher concentration in plasma. Risk of increased side effects.

188
Q

PO medications take how long for effect?

A

~40 mins

189
Q

T/F
Topical medications do not require lipid solubility.

A

False
they do!

190
Q

What drugs absorb best in the stomach? Acids or bases?

A

Acids
Acidic drug in acid = keeps its proton/H = uncharged = cross lipid bilayer

191
Q

Which will absorb faster: IM or subQ injection? Why?

A

IM
higher blood flow

192
Q

T/F
Irritating agents can be given IM or subQ, as long as they are given slowly.

A

False
IV: Irritating drugs are okay if given slowly
IM/subQ: no irritating agents

193
Q

T/F
The blood brain barrier can be bypassed through fluid channels.

A

False
The BBB does not have fluid channel entry. But we can bypass the BBB using intrathecal drug administration.

194
Q

T/F
Chemo drugs can be given arterially.

A

True
Doesn’t sound like a great idea but it is lol.

Allows targeted treatment of cancerous tissue; remaining drug is diluted in veins.

195
Q

What does the blue dot tell us?
What does the purple highlighted region tell us?

A

Blue dot = peak of drug concentration
At this point, drug absorption rate = elimination rate

Purple line = elimination is occurring faster than absorption

196
Q

When does elimination begin?

A

immediately after administration

197
Q

Which order of kinetics removes drug at a constant rate, maxing out the enzymes?

A

Zero order

Your enzymes: I’m doing the best I can, ma’am. I can go zero percent faster.

198
Q

Which order of kinetics removes drugs at a rate dependent on the plasma concentration?

A

First Order

199
Q

The duration of action is the time spent…

A

above minimum effective dose

200
Q

Therapeutic window is the area between….

A

BELOW the minimum effective concentration for adverse response
ABOVE the minimum effective concentration for desired dose

201
Q

Distribution

A

movement of drug out of plasma to site of action (tissue)

202
Q

T/F
Aqueous channels allow passive diffusion of small, water-soluble drugs.

A

True

203
Q

Facilitated diffusion vs. Active transport

A

Facilitated diffusion: moves HI to LO; don’t need ATP

Active transport: moves LO to HI; needs ATP

204
Q

T/F
A longer carbon chain increased water solubility.

A

False
Longer carbon chain = nonpolar = increased lipid solubility & character

205
Q

What is Octanol/buffer partition coeffecient?

A

measures lipid solubility; higher values = higher lipid solubility
BUT, very high values can inhibit absorption

206
Q

T/F
Very high lipid solubility can inhibit absorption.

A

True
Cannot cross glycocalyx, a sugar layer outside membrane.

207
Q

In what conditions are basic drugs charged?

A

Basic drugs are charged in acidic conditions.

208
Q

Basic drugs are unprotonated in which conditions?

A

basic conditions

209
Q

When are acidic drugs protonated? Are they ionized or unionized in this scenario?

A

in acidic conditions; nonionized/uncharged

210
Q

T/F
The BBB is an example of a gap junction.

A

False
Its an example of a tight junction

211
Q

T/F
Amino acids can quickly cross into CSF even though they are charged at body pH.

A

True
carrier proteins make this possible

212
Q

T/F
Very lipid-soluble drugs accumulate in CSF quickly.

A

True
they easily go from plasma into the brain

213
Q

Which feature of the lungs allows drugs to quickly move into the alveolar space?

A

transient fenestrae (fenestrations) make the lungs more permeable

214
Q

What parts of the body feature fenestrations? What significance is this to ADME?

A
  • lungs and capillaries (this includes the gomerulus)
  • increases absorption
215
Q

T/F
Eyedrops are considered topical medication.

A

True

216
Q

Most of the body’s water is located (inside/outside) the cells.

A

inside

217
Q

Most extracellular fluid is located….

A

in between cells
most ECF is interstitial

218
Q

Blood is mostly composed of…

A

plasma

219
Q

Drugs that follow _____ tend to distribute well.

A

Total body water

220
Q

T/F
Metabolites are the inactive form of drugs.

A

False
Metabolites can be active or inactive.

221
Q

T/F
Drugs can travel to tissue depots, where they exert their effects.

A

False
Drugs can bind to tissue depots, but they do not act there.

222
Q

T/F
Any change to a drug is considered a metabolite.

A

True

223
Q

T/F
Protein-drug binding is a strong bond.

A

False
it is weak; drug can dissociate from protein, especially in response to bound drug to free drug equillibrium

224
Q

Volume of Distribution
What does it tell us?
Common values and their interpretation?

A

Volume of Distribution: where the drug goes

5 L = stays in plasma
10-12 L = concentrated in ECF
1500 L = moves rapidly out of plasma into the tissues

225
Q

T/F
Volume of distribution should reflect the actual total body fluid volume.

A

False
Values can far exceed normal body fluid volume
Ex: 1500 L, which means the drug travels out of the vascular compartment

226
Q

What is K1 and K2?

A

K1 = rate of association
K2 = rate of dissociation

one = ON
two = OFF

K2 —>✌🏼 the drug is peacing out

227
Q

We would expect IV doses to rapidly decrease in concentration because…

A

IV drugs rapidly mix

228
Q

Which of the following holds drugs the longest?
Vessel rich group
Vessel poor group
Muscles
None of these are correct

A

vessel poor group holds drugs the longest

229
Q

Once we stop administering the drug, concentrations will first drop in the:
Vessel rich group
Vessel poor group
Muscles
None of these are correct

A

Vessel rich group

230
Q

Which phase of metabolism focuses on adding groups?

A

Phase II (synthetic/anabolic)

231
Q

T/F
Most tissues metabolize and eliminate drugs to some degree.

A

True

232
Q

Primary reactions of Phase I include all of the following except:
Hydration
Hydrolysis
Oxidation
Reduction

A

Hydration

“Hydro O.R.”
Hydrolysis
Oxidation
Reduction

233
Q

Grapefruit juice inhibits which enzyme?

A

CYP3A4/5

234
Q

Which enzyme metabolizes opioids?

A

CYP3A4/5

also:
local anesth.
benzos
1/2 of the drugs we handle

235
Q

The ____ group allows CYP enzymes to…

A

heme
transfer e-‘s; perform redox reactions

236
Q

T/F
Hydrolysis usually occurs in the liver.

A

False
usually in plasma/tissues

237
Q

T/F
Cholinesterase is an example of a CYP enzyme.

A

False
it is considered a non-cytochrome enzyme

238
Q

CYPs are used in Phase ___ metabolism.
Phase ___ uses many transferase enzymes.

A

CYPs are phase I
transferases are phase II

239
Q

How does mucomyst reverse Tylenol toxicity?

A

It repletes the enzyme that metabolizes Tylenol, glutathione

240
Q

What are some limitations of Phase II metabolism?

A

precursors are required for the synthesis/anabolic reactions
If precursors are exhausted, Phase II metab stops

241
Q

What happens in these reactions?
Is this Phase I or II?

A

Phase I

242
Q

Is this an oxidation or reduction reaction?

A

Reduction (phase II)
Nitro group —> amine group

243
Q

What happens in glucuronidation?

A

A sugar group is added to a molecule, making it more water-soluble

GLUCurONidation —> glucose on

244
Q

What groups can be added to a drug to aid in elimination? What phase does this occur in?

A

Phase II

Can add:
Acetyl (from acetylCoA)
Sulfate (SO4)
Glutathione (amino acid)
Glucose/sugar group

245
Q

In nonmicrosomal hydrolysis, Cholinesterase breaks a _____ bond to form a ____ group.

A

breaks ester bond
hydroxy group formed (OH)

246
Q

What ultimately decides proper dosing?

A

Relationship between drug [ ] and effect.
(Pharmacodynamics)

247
Q

What kinda of drug is propanolol?

A

B-adrenergic antagonist
Proved that receptors exist

248
Q

Do osmotic laxatives act on a receptor?

A

No

249
Q

Receptor Structures (4)

A

Can be single protein or multiple protein subunits
Types:
Ligand Gated Ion Channels/Ionophores
Metabophores
G-protein Couples Receptors
Intracellular Receptors (steroid receptors)

250
Q

KA

A

Association constant
Equals Kon/Koff
Higher value = higher affinity

251
Q

KD

A

Equilibrium dissociation constant

[ ] @ which 50% of the receptors are occupied

Equal to 1/KA (or: K off/ K on)

252
Q

Brownian Motion

A

Drug molecules move in this way

random movement displayed by small particles that are suspended in fluids

253
Q

Who dis

A

Relative affinity constant
shows rate of binding and release

D= drug [ ]
R= free receptor [ ]
DR= [ ] drug-occupied receptors

254
Q

T/F
High-affinity drugs act on the receptor for long periods of time.

A

False
Even high-affinity drugs may interact with a receptor briefly. Long duration of action is not guaranteed.

255
Q

Intrinsic activity

A

describes the effect the ligand has when it interacts with the receptor

256
Q

T/F
A low affinity drug may still illicit effects if the intrinsic activity is very high.

A

False
a drug with a high level of intrinsic activity but low affinity may not elicit much of a response.

257
Q

(In a dose-response curve) Once a critical number of receptors are occupied, increasing the dose will increase the response. The increase in response is described as ______.

A

logarithmic

258
Q

(In a dose-response curve) What is happening when increasing the dose does not increase the response?

A

maximal response has been reached; the tissue cannot produce a greater response

259
Q

pH and receptor shape

A

pH changes can change receptor shape; the receptor protein may be become charged or uncharged

260
Q

Endogenous benzos

A

endozepines

P.S. they need to get to workin’ cuz ya girl is ANXIOUS

261
Q

What does it take to be a good agonist?

A

good affinity
good intrinsic activity

262
Q

Partial agonists have good affinity & their intrinsic activity is (higher/lower) than the endogenous compound.

A

Lower

partial agonist:
good affinity
lower instrinsic activity than the endogenous

263
Q

What receptor does buprenorphine act on?

A

Mu receptor

264
Q

Buprenorphine vs Morphine
Which has higher agonist effect?
Which is the partial agonist?

A

Morphine

(Buprenorphine is a partial agonist)

265
Q

Fentanyl is about _____ times more potent than morphine at the _____ receptor, making it a superagonist.

A

100x
Mu opioid receptor

266
Q

Physiologic agonist
definition & example

A

produce same bodily effects but use a different receptor system & mechanism

Ketamine and propofol are physiologic agonists.
Ketamine acts on NMDA receptors. Propofol acts on GABA(A) receptor complex.
Both produce loss of consciousness.

**NMDA: N-methyl-D-aspartate

267
Q

Coagonists
definition & example

A

Certain agonists need help of another agonist to produce effects. These are called coagonists.

Glycine & Glutamate
some NMDA receptors must bind with both

**NMDA: N-methyl-D-aspartate

268
Q

Isoproterenol vs. Albuterol
Which is selective?
Which is non-selective?

A

Isoproterenol: nonselective Beta-adrenergic 1 & 2 agonist
Albuterol: selective Beta 2 agonist

269
Q

Law of Mass Action

A

greater [ ] of drug around receptor = greater chance receptor will be occupied

Memory tip: If there’s a MASSive crowd of drug, there will be ACTION

270
Q

How can we use competitive antagonists and agonists to control effects? Think of Vecuronium, acetylcholine and neostigmine.

A

Add competitive antagonist to decrease normal effects (vecuronium)

Add agonist to compete away the competitive antagonist.

Scenario:
Vecuronium (competitive antag) blocks acetylcholine (endogenous agonist) @ neuromuscular nicotinic receptor.
Compete away Vec using more agonist.
Neostigmine increases agonist (acetylcholine) by decreasing its metabolism.

271
Q

Which drug can reverse Vecuronium?

A

Neostigmine
It decreases the metabolism of acetylcholine.
More ACh
ACh competes with Vecuronium (comp. antag)
Reversal of Vecuronium

272
Q

Noncompetitive antagonism can occur by 2 mechanisms. What are they?

A
  1. Binds irreversibly
  2. Allosteric inhibition: binds to allosteric site & changes receptor conformation (agonist may no longer be able to bind). This can reverse when [ ] of antagonist decreases.
273
Q

Irreversible inhibitor of alpha adrenergic receptors

A

phenoxybenzamine

274
Q

T/F
Irreversible antagonism
Antagonistic effects will stop if the concentration of the antagonist decreases.

A

False
Even if antagonist [ ] around receptor decreases, effects of antagonism will continue.

275
Q

T/F
Allosteric inhibition may stop if concentration of the allosteric antagonist decreases.

A

True
Unlike irreversible antagonism, it’s not necessarily irreversible.

As the concentration of the allosteric antagonist decreases, the
receptor complex may return to its previous conformation
and function normally

276
Q

Example of allosteric inhibition

A

In certain neuronal pathways in the spinal cord,

-Glycine binds with its receptors to inhibit the pathway
-Allosteric binding of strychnine decreases the affinity of glycine for its site (glycine receptor complex)
-Increased stimulation of the pathway (convulsions)

In this case, strychnine is an allosteric inhibitor.

277
Q

Allosteric potentiation
definition & example
is it agonism or antagonism?

A

Ligand binds to the allosteric site and increases the affinity of normal agonist for the receptor.

Benzo’s and some anesthetics increase GABA’s affinity for its receptor.

It’s a form of Agonism

278
Q

Inverse agonist vs. antagonist

A

Inverse agonists:
-appear as if antagonist was given.
-can reverse with competitive antagonist

Cannot reverse antagonist in this way.

279
Q

Partial agonist

A

gives less effect than normal agonist
appears as if we gave antagonist

280
Q

Agonist/antagonist
definition & example

A

ligand acts as an agonist at certain receptors, but as an antagonist in others

Nalbuphine:
antagonist @ M-opioid receptor
agonist @ K-opioid receptor

281
Q

Up-regulation
definition and resulting effects

A

Can increase number of receptors in reponse to lack of normal stimulation.

Ex: Destroy nerve leading to receptor zone on a muscle cell = no ACh.
Cell senses missing ACh & increases number of ACh receptors.

Result:
Cell becomes hypersensitive to agonist
Can be overstimulated
Cell injury/death

282
Q

Down regulation
definition
how does this apply to medication management?

A

Can decrease number of receptors due to excessive stimulation.

Prolonged use of a medication should not be stopped suddenly as this will cause inadequate receptor stimulation. Taper off.

283
Q

How is down regulation related to tolerance?

A

Some drugs may cause tolerance by down-regulation.
Less receptors = more drug needed for effect

284
Q

T/F
Morphine tolerance is mainly due to down-regulation.

A

False
This is not the only way morphine tolerance develops.

285
Q

T/F
The inward rectifier potassium channel is always open.

A

True

286
Q

Ionophores

A

Aka Ligand-gated ion channels

5 protein subunit
in active state, span entire cell membrane
ligand binding will open or close (induces opposite state)
may require >1 molecule @ >1 site
respond to NT’s and ions

287
Q

Most ligand-gated ion channels are activated by ______ which include…

A

Neurotransmitters
ACh
glycine
GABA
glutamic acid
serotonin

288
Q

Metabophores

A

transmembrane receptors
external binding site
internal enzyme component
ligand modifies intracellular enzyme component

take part in conversion of GTP to cGMP

289
Q

Neuromuscular nicotinic ACh receptors are located on ______ muscle.

A

skeletal

290
Q

Describe the ACh activity at the neuromuscular junction that initiates muscle contractions.

A
  1. ACh released from somatic cholinergic nerve terminals
  2. binds to two receptor sites on the nicotinic receptor (postsynaptic membrane)
  3. stimulates an allosteric change in the pentameric receptor complex
  4. complex opens ion channel
  5. Na ions enter the cell
  6. This initiates local depolarization, which can initiate muscle contraction

(skeletal muscle @ NMJ)

291
Q

cGMP is a (primary/secondary) messenger. Its purpose is to….

A

secondary
trigger additional biochemical processes

292
Q

G-protein coupled receptors

A

large transmembrane protein
7 transmembrane loops
extracellular binding site
detects specific ligands in ECF & initiate intracellular response

293
Q

G-protein coupled receptors vs. metabophore

A

metabophore: directly link enzymatic fxn to ligand interaction

G protein: initiates series of changes that may eventually lead to control of a specific enzyme

(Metabophores are more direct in their enzymatic control)

294
Q

Which receptor family is the most common type of receptor found on cell membranes?

A

G-protein coupled receptor family

295
Q

The G-protein complex is located (inside/outside) of the cell membrane.

A

Inside

296
Q

Activation of the G-protein complex & following events

A
  1. Ligand binds to the extracellular site
  2. conformational change triggers substitution of GTP on the G-protein in place of GDP
  3. activates the G-protein complex
  4. G-protein separates from the transmembrane protein
  5. G-protein migrates & interacts with effector macromolecules (activating/inhibiting them)
  6. Hydrolysis of G-protein: converts GTP to GDP & deactivates the effector molecule.
  7. G-protein complex recombines with the transmembrane protein

Repeats

297
Q

Internal effectors activated/inhibited by G-protein subunits include….

A

phospholipase C
adenylyl cyclase
phosphodiesterase

298
Q

The Beta-adrengeric receptors are are what type of receptor?

A

G-protein coupled

note the transmembrane loops (7)

299
Q

Beta-adrenergic receptors must be stimulated by an (antag/agonist) to activate adenylyl cyclase, which catalyzes the conversion of ___ to ___.

A

Beta-adrenergic receptor + agonist = ATP into cAMP

300
Q

Where are steroid receptors?

A

intracellular

301
Q

How do steroids enter the cell?

A

passive diffusion

302
Q

What happens once steroids enter the cell?

A
  1. binds to a specific inactive protein complex.
  2. inactivating protein dissociates from the complex.
  3. Complex now active!
  4. activated complex goes to nucleus
  5. forms a dimer with another activate receptor complex.
  6. binds to specific regions of DNA.
  7. increase/decrease transcription of specific genes into RNA for translation into proteins.
303
Q

receptor-mediated ion channel Interactions vs. steroid
receptor-induced effects

A

ion channel interactions: nearly instantaneous in response

steroid receptor–induced effects: slower &
last longer due to the lag time for protein synthesis

304
Q

T/F
Without energy, transport proteins cannot work.

A

False
transporters may or may not need energy

305
Q

SSRI’s, such as fluoxetine, act on the transport protein ____, which is responsible for serotonin reuptake.

A

SERT

(SERT sounds similar to SERoTonin)

306
Q

Ammonium chloride (increases/decreases) the pH of urine.

A

decreases

307
Q

Ammonium chloride can increase elimination of (acidic/basic) compounds.

A

basic

it makes urine more acidic, and helps excrete the basic

308
Q

General anesthetics appear to elicit their effects by…

A

still unclear but….

increasing inhibitory signals or decreasing excitatory signals in the brain &/or spinal cord

physical properties + multiple receptor zone effects

309
Q

Agents that work on the ______ complex increase inhibitory pathways.

A

GABA(A) ionophoric
complex.

310
Q

The GABA(A) ionophoric
complex opens and allows _____ ions to enter the cell.

A

Cl

311
Q

How do cells become hyperpolarized?

A

increasing negative charge (ex: chloride ion influx) lowers the local intracellular voltage
makes cell more resistant to depolarization.

312
Q

Agents that allosterically potentiate GABA binding to its receptor site

A

Many of the general anesthetic agents including:
barbiturates
propofol
etomidate
isoflurane
desflurane
sevoflurane

313
Q

Influx of Cl- into the cell causes increased (excitatory/inhibitory) activity.

A

inhibitory

314
Q

Non-neuronal receptors

A

located throughout body cells (ex – ADP receptors on platelets, insulin receptors, LDL receptors)

315
Q

Atropine
what does it do?
agonist or antagonist?

A

Atropine blocks muscarinic ACh receptors
antagonist

316
Q

Whats going on here?

A

potentiation
or
positive allosterism

317
Q
A

noncompetitive antagonsim
or
negative allosterism

318
Q

Total body water accounts for __% of body mass.

A

60%

319
Q

Intracellular fluids accounts for ___% of body mass.

A

40%

320
Q

Extracellular fluid accounts for ___% of body mass.

A

20%

321
Q

Interstitial fluid accounts for __% of body mass.

A

15%

322
Q

The body contains about ___L of plasma.

A

3

323
Q

T/F
Sublingual drugs are subject to first pass effect.

A

False
Oral route is though

sublingual or buccal route of administration permits a rapid onset of drug effect because this blood bypasses the liver

324
Q

What kind of drug is vecuronium?

A

competitive antagonist @ neuromuscular nicotinic receptors (blocks ACh)

325
Q

Acetylcholine released from _____ nerve terminals at the synapse binds to two receptor sites on the ____ receptor.

A

somatic cholinergic
nicotinic

326
Q

Neuromuscular nicotinic acetylcholine receptor1 is located on _____ muscle at the neuromuscular junction.

A

skeletal

327
Q

Which anesthetic agents appear to act by decreasing excitatory signaling through NMDA glutamate receptors and nicotinic acetylcholine receptors in the brain or spinal cord?

A

nitrous oxide, xenon, ketamine

328
Q

2 receptors that ACh binds to

A

muscarinic (G-protein coupled)
nicotinic (ionotropic)

329
Q

Drugs administered into the proximal rectum are absorbed into the ___ veins and transported via the portal venous system to the liver.

A

superior hemorrhoidal

330
Q

Butorphanol is a (full/partial) agonist.

A

partial

331
Q

Partial agonist + full agonist = what effect?
Example

A

partial reversal of agonist

Butorphanol (partial) + Fentanyl (full) = Partial reversal of Fentanyl
High dose opioid users may withdraw!

332
Q

Protein binding
Acidic drugs bind to ___. Basic drugs bind to ___.

A

acidic –> albumin

basic –> alpha 1 glycoprotein

333
Q

T/F
The G-protein coupled receptor is a muscarinic receptor.

A

True

G-protein = muscarinic
ionotropic= nicotinic

334
Q

Ka

A

dissociation constant of an acid

335
Q

uptake of particulate matter (bacteria, damaged cells) by cells

A

phagocytosis

336
Q

uptake of materials in solution in the extracellular fluid

A

pinocytosis

337
Q

How can enterohepatic recycling affect half-life?

A

can greatly extend half life

“attached glucuronide group is removed, releasing the original drug molecule. If this molecule is reabsorbed into the body, the duration of effect of the drug may be increased “

338
Q
A

baby pharm (4 decks)

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