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Pharmacology Flashcards

1
Q

What is the definition of pharmacokinetics?

A

The fate of a chemical substance administered to a living organism
- what the body does to the drug

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2
Q

What is the definition of pharmacodynamics?

A

The biochemical, physiological and molecular effects of a drug on the body
- what the drug does to the body

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3
Q

What are the four pharmacokinetic processes?

A

Absorption
Distribution
Metabolism
Excretion

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4
Q

What is absorption (of a drug)?

A

The transfer of a drug from the site of administration to the systemic circulation

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5
Q

What are the three mechanisms used to permeate cell membranes and which molecules can cross them?

A
  1. Passive diffusion through hydrophobic membrane (most common) - lipid soluble molecules
  2. Passive diffusion through aqueous pores - small water soluble molecules
  3. Carrier-mediated transport - proteins transporting sugars, amino acids, neurotransmitters, trace metals
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6
Q

What are the factors affecting drug absorption?

A

Lipid solubility
Drug ionisation
Unionised/lipid soluble is able to move across the membrane

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7
Q

What are the factors affecting oral drug absorption in the stomach?

A

Gastric enzymes - could digest drug
Low pH - could degrade molecule
Food - full stomach will slow absorption
Gastric motility - could be altered by disease state or drugs
Previous surgery

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8
Q

What are the factors affecting oral drug absorption in the intestine?

A

Drug structure - unionised/lipid soluble molecule passively diffuse
Medicine formulation - coating of tablet/capsule, modified release controls absorption rate
P-glycoprotein removes substrates and moves them back to GI tract lumen

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9
Q

Where are weak acids best absorbed?

A

The stomach

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10
Q

Where are weak bases best absorbed?

A

The small instestine

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11
Q

Define first pass metabolism

A

Metabolism of drugs preventing them from reaching the systemic circulation

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12
Q

What could do first pass metabolism and how can it be avoided?

A

Enzymes in the intestinal wall
Enzymes in the liver

Can be avoided through the splanchnic circulation routes (rectal)

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13
Q

Define bioavailability (F)

A

The proportion of the administered drug that reaches the systemic circulation

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14
Q

What is bioavailability dependent on?

A

The extent of drug absorption
The extent of first pass metabolism

Not dependent on the rate of absorption

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15
Q

What are the four compartments of the body for drug distribution?

A

Fat
Plasma
Interstitial fluid
Intracellular fluid

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16
Q

What drug properties that affect their ability to move between compartments?

A

Molecule size - smaller increases dist.
Lipid solubility - lipophyllic increases dist.
Protein binding - unbound increases dist.

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17
Q

What is Volume distribution (Vd)?

A

The theoretical volume a drug will be distributed in the body
The volume of plasma required to contain the total administered dose
high Vd = well distributed

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18
Q

Define drug elimination

A

The process by which a drug becomes no longer available to exert its effect on the body

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19
Q

Define drug metabolism

A

Modification of a chemical structure to form a new chemical entity (metabolite)

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20
Q

What happens in phase 1 of drug metabolism?

A

Cytochrome p450 enzymes in the liver oxidise/reduce/hydrolyse to introduce a new reactive group to a structure

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21
Q

What happens in phase 2 of drug metabolism?

A

Conjugation of a functional group to produce a hydrophilic, non-reactive molecule

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22
Q

What is a pro drug?

A

A drug that is metabolised to its active form

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23
Q

What are the three processes of renal excretion?

A
  1. Glomerular filtration - unbound molecules pass through
  2. Active tubular secretion - OAT/OCTclear protein-bound drugs from peritubular capillaries
  3. Passive reabsorption of lipophilic molecules to the peritubular capillaries
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24
Q

What are first order kinetics?

A

Where the rate of elimination is proportional to the plasma drug concentration (a constant proportion of drug is eliminated)

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25
What are zero order kinetics?
Where the rate of elimination is not proportional to the plasma drug concentration (a constant amount of the drug is eliminated)
26
What is Cmax?
The maximum plasma concentration
27
What is tmax?
The time taken to reach maximum plasma concentration
28
What is clearance (CL)
The efficiency of irreversible elimination of a drug from the systemic circulation
29
What is the bioavailability of an IV/IA administered drug?
100%
30
What is half life (t 1/2)?
The time taken for the plasma drug concentration to fall 50%
31
What is half life dependent on?
Clearance of a drug Volume distribution
32
When is a drug considered cleared?
5 x half life
33
Define steady state
The rate of drug input equals the rate of elimination
34
What is Css?
The drug plasma concentration at steady state
35
What is time to Css considered to be?
5 x half life
36
What are the boundaries of the Css?
Maximum safe concentration (MSC) and minimum effective concentration (MEC)
37
What happens if the plasma concentration is above the maximum safe concentration?
Risk of toxicity and harm increases
38
What happens if the plasma concentration is below the minimum effective concentration?
Subtherapeutic - treatment won't be effective
39
What is a loading dose?
A larger initial dose to speed up the time to steady state
40
When and why is therapeutic drug monitoring (TDM) used?
In drugs with a narrow therapeutic window to avoid toxicity and ensure efficacy
41
Define pharmacogenomics
The use of genetic and genomic information to tailor pharmaceutical treatment to an individual
42
What are the four types of drug targets?
Receptors Enzymes Transporters Ion channels
43
What is a receptor?
A component of a cell that interacts with a specific ligand and initiates a change of biochemical events leading to ligand observed effects
44
What is a ligand?
A molecule that binds to another molecule. Could be endogenous or exogenous
45
What are the four types of receptors targeted?
1. Ligand-gated ion channels 2. G protein Coupled Receptors 3. Kinase-linked receptors 4. Nuclear/cystolic receptors
46
What is an agonist?
A compound that binds to a receptor to activate it
47
What is an antagonist?
A compound that reduces/reverses the effect of an agonist
48
What is the two state model?
Drugs can activate receptors by inducing or supporting a conformational change in the receptor
49
Define potency
How well a drug works
50
What is EC50?
The concentration that gives half the maximal response. A measure of potency
51
What is a full agonist?
An agonist that gives 100% of a response
52
What is a partial agonist?
An agonist that illicit a response but not a full response
53
Define Efficacy
How well a ligand activates a receptor The maximum response achievable (Emax)
54
Define intrinsic activity (IA)
The ability of a drug-receptor complex produce a maximum functional response
55
What is competitive antagonism?
When an antagonist binds to the same site as the agonist
56
What is non-competitive antagonism?
When an antagonist binds to an allosteric (non-agonist) site on a receptor to prevent activation of the receptor
57
Define affinity
How well a ligand binds to a receptor Agonists and antagonists have affinity
58
Do agonists and antagonists show efficacy?
Agonists do Antagonists don't because they don't activate receptors
59
What is receptor reserve?
Spare receptors after full agonists have produced a maximum response
60
What are irreversible antagonists?
Antagonists that permanently bind to a receptor
61
What are the four factors affecting drug action?
Affinity Efficacy Receptor number Signal amplification
62
What is allosteric modulation?
When an allosteric ligand binds to a second site on the receptor and affects the agonist's affect Could change EC50 (affinity modulation), Emax (efficacy modulation)
63
What is an inverse agonist?
A drug that binds to the same receptor as an agonist but induces the opposite pharmacological response to that of the agonist
64
Define tolerance
A reduction in the agonist's effect over time
65
What is desensitisation?
Sudden failure to get a response/effect
66
Which nervous system do cholinergic receptors affect?
Parasympathetic
67
What is the neurotransmitter for cholinergic receptors?
Acetylcholine (ACh)
68
What are the two subtypes of cholinergic receptors?
Nicotinic and muscarinic
69
Describe nicotinic cholinergic receptors
Between pre- and postsynaptic neurones Nerve and muscle types Ligand gated Stimulated by ACh Stimulate action potential in postsynaptic neuron or stimulate muscle contraction
70
Give an example of a drug affecting nicotinic cholinergic receptors
Botulinum - inhibits ACh release at neuromuscular junction causing paralysis Curare - antagonist, muscle relaxant
71
Describe muscarinic cholinergic receptors
G protein Coupled Receptors Post-synaptic 5 types: M1, 2, 3, 4, 5
72
Describe M1 muscarinic receptors
Cholinergic Stimulator Found in brain and stomach When activated: HCl is released, pepsinogen is released, greater cognition and memory
73
Describe M2 muscarinic receptors
Cholinergic Inhibitor Found in heart When activated: Hr decreases, force of contractility reduces
74
Describe M3 muscarinic receptors
Cholinergic Stimulator Found in glands and smooth muscle When activated: tears, saliva, bronchial secretions, digestive enzymes (pancreas), insulin release, GI mucus secretion, pupil constriction, bronchial constriction, peristalsis, detrusor muscle contraction (urination), uterine contractions
75
Give an example of an M3 antagonist
Ipratropium - stops bronchoconstriction in asthma and COPD
76
What are the side effects of agonising/activating cholinergic receptors
Diarrhoea Urinary excretion Miosis - pupil constriction Bronchoconstriction Bradycardia Emesis - vomiting Lacrimation Sweating Salivation
77
Which nervous system do adrenergic receptors affect?
Sympathetic
78
What is the neurotransmitter for adrenergic receptors?
Acetylcholine and noradrenaline
79
What are the subtypes of postganglionic adrenergic receptors?
alpha 1, alpha 2, beta 1 and beta 2 receptors
80
Describe alpha 1 receptors
Adrenergic Stimulatory Found in smooth muscle, organs and glands except cardiac muscle and juxtaglomerular cells When activated: vasoconstriction, pupil dilation
81
Describe beta 1 receptors
Adrenergic Stimulatory Found in cardiac muscle and juxtaglomerular cells When activated: increases force of contraction of heart, HR, electrical conduction, renin release (and therefore blood pressure)
82
Describe alpha 2 receptors
Adrenergic Inhibitory Found in preganglionic membranes When activated: inhibits noradrenaline release so self-inhibits
83
Describe beta 2 receptors
Adrenergic Inhibitory Found in smooth muscle, organs and glands except preganglionic membranes When activated: bronchodilation, vasodilation, reduced GI motility
84
Give an example of an adrenergic receptor drug
Adrenaline in anaphylaxis - agonist of a1, B2 and B2 Salbutamol in asthma - agonist of B2 receptors Propranolol - B1 and B2 antagonist
85
How do opioids work in analgesia?
Opioids activate G Protein Coupled Receptors on nerve cells This inhibits the release of pain transmitter at spinal cord and midbrain, blocking the descending transmission This modulates pain at the higher centres, changing the emotional perception of pain and causing euphoria
86
How is tolerance caused in opioids?
Prolonged use causes down regulation of receptors
87
What is dependence in opioids?
Psychological effect - craving euphoria
88
What is morphine metabolised to in the liver?
Morphine 6 glucuronide
89
Why does codeine need to be metabolised?
It is a prodrug
90
What are the side effects of taking opioids?
Respiratory depression Sedation Nausea and vomiting Constipation Itching Immune suppression Endocrine effects
91
What is an opioid antagonist?
Naloxone - in respiratory depression, give IV, diluted with saline
92
What is a drug interaction?
When a substance (drug, food or toxin) alters the expected performance of a drug
93
What are pharmacodynamic drug interactions?
When drugs act on the same receptor/physiological system
94
What are the two types of pharmacodynamic drug interactions?
Synergistic - two drugs having the same effect Antagonistic - two drugs cancelling each other out
95
What are the types of pharmacokinetic drug interactions?
1. Affecting the rate or extent of drug absorption by changing the GI pH, complex formulation, induction or inhibition of p-glycoproteins 2. competition for protein binding affecting drug distribution 3. inducing or inhibiting metabolic enzymes 4. competition for OATs/OCTs in renal tubule affecting excretion
96
What is an adverse drug reaction?
a response to a medicinal product (or a combination of medicinal products) that is noxious or unintended
97
What are the two classifications of ADRs?
ABCDEFG or DoTS
98
What are the ABCDEFG classes of ADRs?
Augmented Bizarre Chronic Delayed End of use/withdrawal Failure of treatment Genetic
99
What is the DoTS classification of ADRs?
Dose-relatedness - hypersusceptibility, side effects, toxic effects Timing - time independent, time dependent Susceptibility - groups of people that may be more susceptible
100
Describe the standard drug development process
1. Target identification 2. Target assay construction and screening 3. Target validation and medicinal chemistry safety 4. Phase I - safety 5. Phase II - efficacy and safety 6. Phase III - efficacy and safety 7. FDA/MHRA review and approval

Phase 2a (9 decks)

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