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health and wellbeing > exam 3 > Flashcards

exam 3 Flashcards

1
Q

pharmacokinetics

A

a study of the interactions that determine the speed of onset, intensity and duration of drug action

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2
Q

What are the different mechanisms in which drugs can cross membranes?

A
  • passive diffusion through call membranes
  • carrier-mediated transport
  • endocytosis and exocytosis
  • diffusion through aqueous pores and intracellular pores
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3
Q

Which factors influence passive diffusion through call membranes?

A

lipid solubility
area of absorption
magnitude of concentration gradient

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4
Q

drug distribution

A

the process by which a drug is transferred from the bloodstream (plasma) to tissues (interstitial fluid and cells)

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5
Q

At a resting state the inside of a cell is _______ with respect to the outside

A

negative

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6
Q

What is the donnan equilibrium

A

A skewed distribution of osmolytes

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7
Q

Ohms law

A

voltage = current x resistance
V=IR

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8
Q

The major determinant of membrane potential is…

A

the extracellular K+ conc

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9
Q

Na+/K+ATPase pump

A

3Na out, 2K in (maintains the ionic balance/conc gradient where Na+ concs are high extracellularly and K+ are high intracellularly)

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10
Q

What does the Na+/K+ATPase pump pump against?

A

the electrical gradient of K+ (membrane is relatively permeable to K+ so these ions pass out the cell, this small portion passing out establish the resting membrane potential)

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11
Q

Cells are negatively charged on the inside because….

A

they are leaking positive charge (K+) to the extracellular space

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12
Q

What is an indicator of sever hyperkalemia?

A

wide QRS complex

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13
Q

What is the typical range of potassium levels?

A

3.5 to 5.3 mmol/l

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14
Q

What is the approx serum potassium level for those with hyperkalemia?

A

8.4 mmol/l

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15
Q

Formula of the nernst equation?

A

E ion = 61/z log (C out/C in)

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16
Q

Nernst potential for Na+

A

61/1 log (140/10) = 69.9mV

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17
Q

Nernst potential for K+

A

61/1 log (4/120) = -90.1mV

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18
Q

Nernst potential for hyperkaleima?

A

(8.4/120) = -70.4mV

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19
Q

Summarize an action potential

A

-70mV at resting membrane potential
Voltage-gated Na+ ion channels open = depolarization
Once threshold has been reached an action potential can occur
Overshoot
Na+ channels start to become inactive and close
K+ channels begin to open and repolarize the cell membrane to its resting value
Absolute refractory period (cell cannot be excited as channel is inactive)
Hyperpolarization occurs
Relative refractory period (Na+ channels go to closed state second A.P can be produced)

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20
Q

How can current carried by potassium affect current carried by sodium?

A

Current carried by potassium affects current carried by sodium, because the sodium ion channels WILL remain inactive, unless they experience the ‘electrical pull’ when the membrane potential changes from positive to negative, that is, repolarization. It is the flux of POTASSIUM ions that are responsible for repolarization.

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21
Q

AP in cardiac muscles

A

SA node in right atrium > atria > AV node in right atrium/ventricle > bundle of His > purkinje fibers > ventricles

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22
Q

Refractory periods in cardiac cells

A

Absolute refractory period: depolarization, plateau, half of repolarization
Relative refractory period: end of repolarization into pacemaker potential
The inactivation of Na+ channels + long depolarized plateau = no summation of contractions

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23
Q

Difference between skeletal and cardiac muscle regarding relaxation

A

Skeletal muscle does not undergo mandatory relaxation and can undergo summation or smooth tetanus

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24
Q

Name a blocker of the Na+/K+ ATPase

A

Ouabain

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25
Q

What does the Goldman-Hodgkin-Katz equation predict?

A

membrane potential (incl. A.P)
the summed effect of relative permeability of different species of ions

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26
Q

Excitatory Post-Synaptic Potential

A

makes a new post-synaptic action potential MORE likely

(activation + depolarization)

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27
Q

Signalling across a synapse

A

rise in intracellular Ca+ = exocytosis of NT vesicles = NT into synaptic cleft

NT binds to receptors on post synaptic terminal = inhibition or activation of neuron

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28
Q

Inhibitory Post-Synaptic Potential

A

makes a new post-synaptic action potential LESS likely

(inhibition + hyperpolarization)

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29
Q

synapses near the ___________ have a greater effect (than synapses near the ________)

A

Initial Segment
dendrites

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30
Q

Temporal summation

A

summed potential created by more than one EPSP and/or IPSP arriving at a single synapse on a postsynaptic cell membrane in quick succession

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31
Q

Spatial summation

A

summed potential created by more than one EPSP and/or IPSP arriving together at different synapses on a postsynaptic cell membrane

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32
Q

What makes the neuromuscular junction different to other synapses?

A

In NMJ’s in most instances any solitary action potential coming from the motor neuron, will give rise to to an action potential.
In most other synapses, any solitary action potential on the pre-synapse will only have a miniscule effect on the post-synapse.
The NMJ is different due to the high density of many ion channels on the post-synapse, of the nicotinic (N) acetylcholine-binding kind (when open, it allows for the flux of both sodium and potassium(!) but because the electrochemical gradient of sodium ions is stronger than that of potassium ions, many more sodium ions enters the cell than potassium ions leave the cell = depolarization = action potential).

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33
Q

What characteristics enable rapid conduction along neurons?

A

A sheet of myelin - insulates the nerve
Areas where myelin in absent = nodes of ranvier = depolarization ‘jumps’ from node to node = rapid conduction of electrical activity ‘saltatory conduction’

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34
Q

Gap junctions (function + location)

A

Pores that enable ions from one cell to diffuse into other cells
Between heart muscle cells, some neurons, smooth muscle cells, endothelium and smooth muscle cells

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35
Q

In which cell types is ability to generate action potentials fundamental to their function?

A

Neurons, cardiac muscle, skeletal muscle

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36
Q

In the relative refractoy period ______ _____ ______ sodium ion channels can ________

A

only a few
open

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37
Q

concentration of ions relevant to the membrane potential is
typically measured in

A

mM

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37
Q

In a 1M solution, the amount of molecules per liter is 6.023
times 10 raised to the power of ____ Avogrado’s constant)

A

23

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37
Q

The electric field Volts/meter) across the cell membrane at
rest is approximately

A

10MV/m

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38
Q

What is approximately the concentration of sodium ions in the
extracellular fluid (in mM, millimolar)

A

140

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39
Q

What is approximately the concentration of sodium ions in the
intracellular fluid (in mM)

A

10

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40
Q

What is approximately the concentration of potassium ions in
the extracellular fluid (in mM)

A

4

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41
Q

What is approximately the concentration of potassium ions in
the intracellular fluid (in mM)

A

120

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42
Q

Are organic ions, like {molecular backbone}COO, at greater
concentration in the intracellular fluid than or the extracellular
fluid

A

intracellular fluid

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43
Q

What is a graded potential?

A

small, variable changes in membrane potential, often sub-threshold and localized, triggered by stimuli
graded potential must reach a certain threshold level of depolarization before an A.P can occur

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44
Q

What is the section at the end of the spine called?

A

Cauda equina

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45
Q

Roles of the vagus nerve?

A

control of heart rate + sensing of stretch of stomach wall

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46
Q

What is the limbic system composed of? and what is it involved in?

A

the hippocampus, amygdala, septal nucleus, cingulated gyrus and fornix

involved in motivation, emotion, long-term memory and olfaction

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47
Q

Which NT can be found in the limbic system?

A

Glutamate
Dopamine (may relate to addiction)

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48
Q

Role of the thalamus?

A

Integrates motor input and output Integrates sensory input and output
Is probably involved in consciousness

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49
Q

Role of the hypothalamus?

A

Homeostasis!!!
Body temperatureWater balanceEnergy balance
Emotions
Behaviors

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50
Q

Functions of the thalamus:

A

emotional behavior subjective states, memory function, hearing, vision, relay of somatosensory info, performance of voluntary movements

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51
Q

Spinothalamic:

A

sensory pathway conveying information of pain, temperature, light touch and pressure…
Most spinothalamic axons terminate in the ventral posterolateral (VPL) nucleus of the thalamus

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52
Q

Nuclei of the hypothalamus and their function?

A

Supra-optic area (supra-optic nuclei + supra-chiasmatic nuclei) - water balance + hormone ADH
Lateral nucleus - satiety (orexigenic pathway of leptin goes to this nucleus)
Arcuate nucleus - hunger + satiety (start of leptin pathway, both pathways go to this nucleus)
Paraventricular nucleus - water balance (ADH) + satiety (anorexigenic pathway of leptin goes to this nucleus)

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53
Q

Transduction

A

The conversion of the sensory stimulus into the electrochemical energy of the nerve impulse = a number of action potentials per second

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54
Q

Regardless of the sense, all information is ______, into a number of action potentials with a certain _________ within __________

A

coded
frequency
a time span

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54
Q

The brain has dedicated regions for interpreting information on ________ and __________

A

position
modality

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55
Q

How alike are the motor cortex and the somatosensory cortex structurally?

A

very much

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56
Q

What is the treatment for subarachnoid bleeding (stroke)?

A

platinum coils inserted into subarachnoid spaces

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57
Q

Most of the 12 pairs (left + right) of cranial neves - neves III to
XII - exists from which pat of the central nervous system?

A

the brainstem

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58
Q

You have _____ pairs of spinal neves

A

31

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59
Q

The central nervous system is bathed in the _________ fluid

A

cerebrospinal

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60
Q

Most somatosensory input passes through the ___________
before being relayed to the somatosensory area of the post-
central gyrus.

A

thalamus

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61
Q

In relation to respiration and acid-base status, it is important to
realize that the cerebrospinal fluid has ______ proteins

A

has a low conc of

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62
Q

The central nervous system receives sensory input from two
divisions, the somatosensory and _______ sensations

A

special

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63
Q

Sensory input from which special senses is relayed in nuclei of
the Thalamus?

A

Visual
Auditory
Vestibular
Taste

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64
Q

At the level of the synapse, _____-_____ ____________ is thought
to underlie memory and the ability to lean

A

long-term potentiation

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65
Q

The neurotransmitter __________ binds to alfa and beta-
adrenoceptors

A

noradrenaline

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66
Q

The neurotransmitter __________ binds to D1-D5 receptors

A

dopamine

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67
Q

The neurotransmitter __________ binds to muscarinic receptors

A

acetylcholine

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68
Q

The neurotransmitter __________ binds to nicotinic receptors

A

acetylcholine

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69
Q

The neurotransmitter __________ binds to H1-H3 receptors

A

histamine

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70
Q

Neuropeptide ____ is pat of the orexigenic pathway that
augments appetite

A

Y

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71
Q

The hormone Leptin is released from adipose tissues and
________ the release of Neuropeptide Y and thus the orexigenic
pathway

A

inhibits

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72
Q

Within the motor system, the _____________ tracts are involved in
executing voluntary, discrete, and skilled movements

A

corticospinal

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73
Q

Within the motor system, the _____________ tracts are involved in
maintaining balance

A

vestibulospinal

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74
Q

Motor neurones are located in the ventral horns of the spinal
cord and innevate

A

The musculature of the rib cage (respiration)The skeletal musculature

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75
Q

The movement of skeletal musculature is under the control of
__________ motor neurons

A

alpha

76
Q

The axons of alpha motor neurons have a ______ diameter compared to axons of other neurons

A

large

77
Q

During inflammation, _____ cells have released histamine that causes a vaso______ and thus _______ blood flow, and exudation of ______, in the inflamed region.

A

mast
dilation
enhanced
plasma

78
Q

Characteristics of inflammation

A

heat, pain, redness, swelling, impaired function

79
Q

Effect of lung tissue inflammation

A

Vasodilation (widening of blood vessels)
Increased permeability/leakiness in vessels
Exudation (exit of blood plasma)
Stasis (no/little flow in vessels)
Leucocyte invasion

80
Q

What % of your blood is white blood cells and platelets?
So what else maintains out immune system?

A

~1% (50g)
there are resident immune system cells in organs and tissues

81
Q

Outcomes of infection?

A

death, fever, scarring, Abscesses-chronic inflammation

82
Q

Fever production

A

raised levels of proinflammatory cytokines (TNF, IL-1, and IL-6) affect hypothalamus behavior (hypothalamic control of body temp). It increases the ‘set point’ value = fever

83
Q

Empyema

A

pus in the pericardial cavity
The result of exudation and the accumulation of cell bodies, foreign and self, and their debris.

84
Q

Coccidioides immitis infection.

A

Fungus causing ‘valley fever’

85
Q

Key characteristics of bacteria:
+ e.g

A

No nucleus
Very proliferative
Damages host cells by releasing toxins
Example: Staphylococcus aureus

86
Q

Key characteristics of fungi:
+ e.g

A

Cell walls made of chitin
Damages host cells by releasing enzymes
Example: Penicillium

87
Q

invertebrate parasites e.g

A

Example: Plasmodium falciparium
Malaria caused by the single cell animals of the genus Plasmodium

88
Q

Key characteristics of viruses:
+ e.g

A

Key characteristics:
Require host cells
Damages host cells by lysis
Example: H1N1 influenza (swine flu)
Hx, which hemagglutinin
Nx, which neuraminidase

89
Q

SARS-CoV2 is a single stranded ____ (ssRNA) coronavirus
Its membrane is studded with _______________________
Its membrane is derived from _____ cell membrane

A

RNA
Spike glycoproteins
host

90
Q

How does corona virus infection work?

A
  • Triggers the infected cells to produce and secrete interferons
  • Interferons bind to receptors on neighbouring cells and trigger an antiviral state (degradation of viral mRNA and inhibit protein synthesis)
  • Interferons also enhance expression of HLA class I, thereby making cells better targets for CD8 cytotoxic T cells, and activate
    natural killer cells
91
Q

The corona virus particle binds (via Spike) to the enzyme __________________

A

ACE2, Angiotensin Converting Enzyme 2

92
Q

Of the different cells of the lungs, it appears it is the ________________ that are particularly susceptible to take in SARS-CoV2

A

Type II pneumocytes

(these cells produce surfactants, molecules with soap-like properties that thus reduces the surface tension of water in the lungs, making the lungs a lot easier to inflate)

93
Q

Part of the adaptive immune response to covid virus involves the activation of ___________ cells

A

T helper

94
Q

The major functions of the immune system are the recognition of pathogens by interacting with ______________________, and defence of the body by the elimination them

A

microbes and their components

95
Q

Characteristics of innate immunity:

A

non-specific immunity
response is antigen-independent
there is immediate maximal response
not antigen-specific
exposure results in no immunologic memory

96
Q

Characteristics of adaptive immunity:

A

specific immunity
response in antigen-dependent
there is a lag time between exposure and maximal response
antigen-specific
exposure results in immunologic memory

96
Q

Name one type of PAMP involved in molecular recognition in innate immunity

A

RNA

96
Q

Describe the process of cell receptor recognition in innate immunity:

A

Natural killer cells is a group of lymphocytes (white blood cells)
Kill cells that lack the right (molecular) appearance (MHC I or its synonym HLA I)
Kills by activation of programmed cell death (apoptosis)

97
Q

Name one complement protein used in complement opsonisation? + what is it used for? + explain its results

A

C-reactive protein, which is used in the clinic to test for intensity of infection
Normal reading 1-5 mg/L
pneumonia ~95 mg/L

98
Q

Overview of early induced response in innate immune response:

A

activation of mast cells
neutrophils engulf microbes

98
Q

Overview of immediate local response in innate immune response:

A

macrophages engulf microbes using pathogen recognition receptors (PRRs)
mast cells release inflammatory mediators such as histamine

99
Q

1 B cell has only 1 kind of ________ _____________________

A

surface immunoglobulin

100
Q

In adaptive immunity: If an antigen is bound, the B cell starts to ___________ (make clones) and ___________ its production and secretion of its immunoglobulin

A

proliferate
enhances

101
Q

In adaptive immunity: Some clones are maintained as _________________

A

memory cells

102
Q

Full activation of B-cells requires the activation of ______ AND _______ molecules

A

signal 1
signal 2

103
Q

Do T cells secrete antibodies?

A

no

104
Q

How are T cells activated?

A

by the presentation of processed antigens on self-proteins

105
Q

T helper cells activate….

A

B cells

106
Q

__________________ kill infected cells by activation of programmed cell death (apoptosis)

A

T cytotoxic cells

107
Q

What are the best treatments against pathogens?

A

proton inhibitors + antibiotics

108
Q

What does Koch postulate regarding infection?

A

The organism must be present in every case of the disease.
The organism must be isolated from diseased host and grown in pure culture.
The pure culture must be shown to induce the disease in an experimentally infected host.
The organism must be recoverable from the experimentally infected host.

109
Q

Overview of adaptive immunity:

A

antigens are carried to lymph nodes to initiate this response

some antigens are carried free in the lymph + some captured by antigen-presenting cells (APCs)

In the lymphoid tissues, the antigens activate T and B lymphocytes
These lymphocytes + antibodies (produced by the B lymphocytes) can
then recirculate back to the site of infection.

antigens localise to follicular dendritic cells (FDCs)
Antigen transported by APCs is presented to T helper cells
which come into close contact with the APCs that become interdigitating
dendritic cells (IDC). These T cells then assist in the generation
of B lymphoblasts, which then migrate in to the follicle (together with
some T cells), where they undergo further maturation and selection
through interaction with FDCs in germinal centres. Specific T and B
lymphocytes then leave the lymph nodes via the medulla and efferent
lymphatics to enter the blood via the thoracic duct.

110
Q

What may increase your likelihood of developing cervical carcinoma?

A

Viral product interferes with tumor suppressor gene activity and cancer therefore becomes more likely

111
Q

In the cell cycle what is the restriction point and when does it occur?

A

It occurs in the G1 phase
The point where a cell will not pass if DNA damage is detected

112
Q

Which tumor suppressor gene is responsible for controlling passage through G1, G2 and M phases of the cell cycle? what percentage of cancers is this protein mutated?

A

p53
~70%

113
Q

What percentage of protection did the covid vaccine provide?

A

90%

114
Q

Outline how an RNA vaccine would work for covid:

A

Part of the virus genetic code (RNA) which tells cells what to build is taken + coated in a lipid (so it can enter the body’s cells)
Injected into patient
Vaccine enters cells + tells them to produce the coronavirus spike protein = prompts production of antibodies + activation of T cells
If patient encounters coronavirus, antibodies + T cells are triggered to fight the virus

115
Q

The Gram staining procedure preferentially stains bacteia
___________ an outer membrane, but with _______________

A

without
lipoteichoic acid

116
Q

The malaria parasite is a _________ ?

A

protozoa

117
Q

Pions are

A

proteins

118
Q

which organisms have a nucleus?

A

protozoa and fungi

119
Q

Vascular permeability is an important process for?

A

the invasion of neutrophils in the tissues

120
Q

Mast cells are an important pat of the ____________ immune
response

A

innate

121
Q

The primary function of mast cells is to…

A

release signalling molecules

122
Q

interleukins 1 and 6 that reach the hypothalamus of the brain,
contribute to the induction of _________ ?

A

fever

123
Q

The conquistadores who invaded the Americas also brought,
unintentionally, disease like smallpox and common cold. Rough
estimates suggest that as many as ________ of the indigenous
American population died due to diseases introduced by
Europeans.

A

50

124
Q

cancer related deaths are due to metastasis in approximately
_____ of cases

A

90%

125
Q

Cancer is uncontrolled cellular proliferation. Proliferation is
usually controlled by what?

A

Tumor supressor genes

126
Q

Which phase of the cell cycle is controlled by
p53 proteins?

A

G1

127
Q

Cell cycle phase in correct order

A

S, G2, mitosis, G1

127
Q

What is the cause of cholera?

A

intestinal infection of Vibrio cholerae

128
Q

What is the mechanism of disease of cholera:

A

Hijacks the production of cyclicAMP

Leads to exaggerated release of Cl-
from intestinal cells to lumen

Water follows Cl-, massive diarrhea

Up to 2L of water lost every hour

129
Q

Which factors are the most important in epidemiology?

A

People
Time
Place

129
Q

Which detective work founded epidemiology?

A

Cholera in London
John Snow (analyst)(collaborating with a Priest): plotted into a map where you find a lot of water pumps and where those who died live. Water pump handle was removed and they saw fewer deaths

129
Q

Morbidity

A

General term relating to incidence and/or prevalence of a disease

129
Q

Mortality

A

Death rate in a population
By defining populations and cause of disease, hypotheses can be tested!
(value is relative to the start population (for %))

130
Q

Incidence

A

New cases of disease

131
Q

Prevalence

A

The number of people who has the disease

132
Q

Objective of the framingham study:
+ type of study

A

to identify the common factors or characteristics that contribute to cardiovascular disease by following its development over a long period of time in a large group of participants who had not yet developed overt symptoms of CVD or suffered a heart attack or stroke

Longitudinal study in a Cohort

133
Q

Background of the framingham study:

A

the death rates for cardiovascular disease had been increasing steadily since the beginning of the [20th] century and had become an American epidemic

134
Q

Approach of the Framingham study:

A

The researchers recruited 5,209 men and women between the ages of 30 and 62 from the town of Framingham … Since 1948, the subjects have continued to return to the study every two years for a detailed medical history, physical examination, and laboratory tests

135
Q

In epistemology what are some issues with data collection? e.g with hypertension

A

New guidelines lower the threshold for high blood pressure, adding 30 million Americans to those who have the condition

High pressure, which for decades has been a top reading of at least 140 or a bottom one of 90, drops to 130 over 80 in advice announced Monday by a dozen medical groups.”

136
Q

Where do daily estimated excess deaths arise from?

A

compare the incidence of daily deaths presently with the incidence of dying of the same periods of previous years

137
Q

The Economist lists as their best estimate on the 10th of November 2021 that ______ million people have died from Covid19 since the pandemic began.

A

17.1

138
Q

Problems with data collection:

A

Absence of information
Inconsistent information
Case ascertainment
Diagnostic criteria
Variable formats for data

139
Q

E.g of Iraq to present issues with data collection:

A

No reliable numbers on excess deaths (deaths in excess of what could be expected) due to
# Poor state infrastructure
# Most deaths are not reported to morgues and hospitals
# Political control

140
Q

“We estimate that through July 2006, there have been __________ “excess deaths”—fatalities above the pre-invasion death rate—in Iraq as a consequence of the war.”

A

654,965

141
Q

What is one method to combat a lack of reliable data?

A

National cluster survey

1 sampling cluster per ~500,000 people

1 cluster starts from a randomly selected household, and then surveys the nearest 39 other households

141
Q

What is a case of imperfect data?

A

noncompaction cardiomyopathy to the left ventricle of the heart

142
Q

What is left ventricular noncompaction?

A

Excessive trabeculae, sometimes poor pump function

143
Q

In a report from Switzerland, what % of patients undergoing echocardiography … were identified as LVNC cases ? + what has led to a greater detection?

A

0.014%
increased awareness of the disorder, as well as improvements in echocardiographic image acquisition and processing

144
Q

Procedure for data collection on LVNC:

A

Manually screened hearts from 2 pathology archives.# From in-house pathology (N=483).# From other centers (N=629).

Assessed Trabeculae-Compact ratio by eye.(Hearts with abnormal trabeculation were also put aside, but not systemically).

22 were put aside (6 normal, 16 abnormal). Wall thicknesses were measured by ruler.Of these, 6 normal and 6 abnormal hearts were MRI scanned.

144
Q

LV trabeculae can be excessive in which factors? + what is the incidence of LVNC?

A

number, size, extent, and locations

low incidence: In total, 5 out of 1112 hearts were LVNC positive
# in-house (1/483)
# other centers (4/629

145
Q

How to avoid case ascertainment in data collection?

A

increased awareness and better diagnostics

146
Q

When calculating incidence or prevalence it is important to know which factors?

A

population size + time period

147
Q

What are the modifiable risk factors of a fatal cardiovascular event:
+ non modifiable

A

Smoking and exposure to smoke Drinking alcohol
Cholesterol
Blood pressure

Age
Gender

148
Q

Population dynamic factors to consider in relation to transmittable disease:

A

population densities are on the rise (the world population is going to increase by billions in the next decades)

urbanization (= higher population densities. Living in a city generally leads to easier access to better health care – although not necessarily so in the developing world)

Rapid increment in tourism -more international connections, easier spread of disease

149
Q

Where is raised blood pressure the highest? Obesity? Cardiovascular disease?

A

Africa
USA, Saudi Arabia, Oman, Libya
Former soviet union

150
Q

Pharmacokinetics

A

what does the human body do with the drug

a study of the interactions that determine the speed of onset, intensity and duration of drug action

151
Q

Pharmacodynamics

A

what does the drug do with the human body

151
Q

In terms of drugs
Absorption:
Distribution:
Metabolism:
Elimination:

A
  • into the body and into cells
  • around the different compartments of the body
  • when the drug is broken down and inactivated, or sometimes transformed into an activeform
  • excretion from the body
152
Q

Routes of drug administration w/ e.g

A
  • Oral e.g ACE inhibitors, Statins
  • Inhalation (Lungs)Asthma medication,Anesthetics
  • Topical (Skin)NicotineAnti-histamines
  • (Intravenous) PropofolAspirin
153
Q

Which mechanisms allows drugs to be absorbed and cross membranes?

A

Passive diffusion through cell membranes True of most drugs, depends ona) Lipid solubilityb) Area of absorptionc) Magnitude of concentration gradient

Carrier-mediated transport

Endocytosis and exocytosis

Diffusion through aqueous pores and intracellular pores.

154
Q

Which form of acid and base of the drug gets absorbed?

A

The neutral form
HA and B

155
Q

Why can the ionized form of a drug not pass a membrane?

A

The neutral form can cross a fatty membrane and gets absorbed, the ionized form may get trapped

156
Q

What can be do to manipulate the levels of drug in the body?

A

know the drugs tendency to behave as acid or base

157
Q

The rate and degree of drug distribution depends on:

A

Blood flow (distribution is fast in well perfused tissues)

Capillary permeability (great in liver, very low in brain)

Protein binding (affinity of the drug for various constituents of cells)

Accumulation in and redistribution to other sites.

158
Q

What buffers the effect of many drugs?

A

Plasma proteins (e.g. albumin)
Drugs bound to proteins have no pharmacological effect

158
Q

What terminates the general anaesthetic effect?

A

redistribution of drug e.g into adipose tissue for thiopental

159
Q

Characteristics of propofol:

A

Works quick
Highly protein bound
Clinical effect very short due to distribution in fatty tissues

160
Q

What is the therapeutic window?

A

the range of drug dosage / concentration in which there is a positive effect AND there are no indications of poisoning.

161
Q

What is the major site of drug metabolism?

A

The liver

162
Q

Mechanism of drug metabolism in the liver:

A

Phase I: oxidation (or reduction or hydrolysis) via Cyt P450
Phase II: transferase reaction + conjugation (via glucuronate or acetylation) to promote elimination

163
Q

Role of drugs in cholesterol synthesis:

A

statins inhibit the pathway of cholesterol synthesis

164
Q

What are the outcomes of drug metabolism?

A

The production of metabolites with less biological activity

The production of active metabolites that may be more potent and persist longer

The conversion of an inactive pro-drug to the active forme.g. the ACE inhibitor Ramipril, anti-viral molnupiravir

The production of toxic metabolites e.g. conversion of methanol to formaldehyde and formic acid

The production of inactive metabolites that are water soluble for excretion

165
Q

Side effects of morphine?

A

hypoventilation, congestion, addiction

166
Q

Biological half life of morphine?

A

~2-3 hours

167
Q

Name one synthetic opioid + its side effects and half life

A

Remifentanil
Side effects: hypoventilation
Biological half life: ~ 4 min

168
Q

What is different about remifentanil compared to other synthetic opioids?

A

remifentanil has anesterlinkage which undergoes rapid hydrolysis by non-specific tissue and plasmaesterases. This means that accumulation does not occur with remifentanil and itscontext-sensitive half-liferemains at 4 minutes

169
Q

Name an ACE inhibitor used to treat hypertension

A

Ramipril

169
Q

Which enzyme complex is responsible for ~50% of drug oxidation + e.g

A

CYP3A4
e.g. Dexamethasone

170
Q

Characteristics of Ramipril:

A

prodrug + is converted in the liver by de-esterification into its active form ramiprilat
inhibits renin-angiotensin-aldosterone system

171
Q

Barriers, like membranes, generally have to be crossed for a
drug to exert its action. By this route of administration, the
fewest barriers have to be overcome:

A

intravenous

172
Q

The distribution of a drug throughout the body first and
foremost relies on

A

systemic circulation

173
Q

The concept of ion trapping shows that a weak acid (which most drugs are) will accumulate in compartments with relatively ______ pH

A

high

174
Q

The concept of ion trapping shows that a weak base will accumulate in compartments with relatively ______ pH

A

low

175
Q

Which tissue will be slow to take up a drug but may nonetheless over time become a large depository of
the drug?

A

adipose

176
Q

which tissue has particularly leaky
capillaries? + tight capillaries?

A

liver
brain

177
Q

The blood-brain-barrier results from the presence of _______.

A

tight junctions

177
Q

ACE inhibitors, such as Ramipril, are often given to patients
with heart failure. This is because ACE inhibitors reduces the
production of __________

A

angiotensin II

health and wellbeing (3 decks)

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