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week 11 (Y2) > the medicine > Flashcards

the medicine Flashcards

1
Q

what is pharmacokinetics

A

processes that affect the drugs stay in the body

Study of what the body does to the drug.
Examines processes of absorption, distribution, metabolism, and excretion.
Influences drug concentration in the body over time, aiding in dosage determination.

studys how the body processes the drug

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2
Q

what is pharmacodynamics

A

drug or target / drug interactions

Study of the effects of drugs on the body and their mechanisms of action.
Explores interactions with target receptors and molecular components.
Focuses on dose-response relationship, potency, and efficacy of drugs.

looks at drugs effects on the body

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3
Q

describe the process of physiology and mission control

A

cellular/tissue/organ housekeeping/maintenance

instruction outflow: neuronal/peptides and small molecules

activators: release of factors
increased neuronal output
increased protein synthesis

activator effects feedback to mission control indirectly via sensors

biosensors: pressure
neuronal activity
change in peptides
small molecules
ions

data flow:
neuronal/ peptides/ small molecules

site: organelles, cells, tissues, organs

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4
Q

mission control overview

A

mission
instruction outflow (neuronal)
activators
effects feedback
biosensors
data inflow
site (organelles / cells)

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5
Q

medulla oblongata overview
pathology BP control

A

mission: BP control

hypertension: command to increase BP

instruction outflow: neuronal / peptides

activators: vascular resistance / heart rate and force

activator effects feedback to mission co tell i directly via sensors

sensors: peripheral vascular resistance / central medulla pressure receptors

hypertension: se sores read pressure as too low

data inflow: largely neuronal

back to medulla oblongata

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6
Q

what is physiology

A

Physiology is the study of animal (including human) function and can be investigated at the level of cells, tissues, organ systems and the whole body. The underlying goal is to explain the fundamental mechanisms that operate in a living organism and how they interact.

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7
Q

what is pathology

A

the science of the causes and effects of diseases, especially the branch of medicine that deals with the laboratory examination of samples of body tissue for diagnostic or forensic purposes.

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8
Q

treated pathology (medulla oblongata example)

A

drug to lower BP

sensors detect drug effect

this is reported to the medulla

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9
Q

what do we demand from drugs

A

hit the target and nothing else

the drug must be selective

drug must have specificity

drug must have efficacy
(affinity and potency)

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10
Q

what does specificity mean

A

the quality of belonging or relating uniquely to a particular subject

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11
Q

what does efficacy mean

A

the ability to produce a desired or intended result

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12
Q

what does affinity mean

A

.
BIOCHEMISTRY
the degree to which a substance tends to combine with another

attraction between drug and receptor of enzyme

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13
Q

what does potency mean

A

Potency is an expression of the activity of a drug in terms of the concentration or amount of the drug required to produce a defined effect,

wether the interaction operates the receptor system

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14
Q

what is affinity plus potency

A

agonist

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15
Q

what is affinity plus no potency

A

antagonist

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16
Q

what do agonists do

A

mimic endogenous agents

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17
Q

what do antagonists do

A

drug blocks endogenous agent

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18
Q

what are anticander drugs

A

cytotoxic

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19
Q

what are streptokinase drugs

A

enzymatic

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20
Q

what are antacids

A

neutralizing agents

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21
Q

what are chelators in metal poisoning

A

binding agents

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22
Q

what are antibiotics

A

they kill invadors

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23
Q

what happens when an antagonist / agonist is activated

A

transporter molecule

function of receptor/protein channel/transporter has changed

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24
Q

how do agonists work

A

endogenous agent stimulates a substrate of a receptor / enzyme

the effect is proportional to the conc of the agent

drug conc is proportional to its pharmacological effect based on a certain affinity and maximal response

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25
what happens with a partial agonist
burning or ligand response is less than 100% / response of full agonist
26
how do antagonists work
endogenous agent stimulates substrate of receptor or enzyme effect is proportional to conc of the agent blocks the endogenous agent or drug agonist and prevents the endogenous effect antagonist has a similar affinity for the receptor / enzyme. it has no potency so prevents the function
27
what is competitive
agonist / antagonist have similar affinities bind to the receptor / enzyme active site
28
what is non competitive
antagonist binds at a different site and prevents function
29
what is uncompetativity
inhibitor binds to receptor / enzyme / agonist complex
30
what is irreversibility
drug destroys enzyme or receptor
31
what is the law of mass action
when the agonist overcomes the inhibitor effect
32
when do you need enough agonist
lower affinity can still reach max potency by adding more agonist
33
what can non competitive inhibition overcome
the law of mass action binds to allosteric site antagonist cuts back max potency
34
what type of interaction is uncompetitive inhibition
three way not a common interaction substrate binds to active site inhibitor is on top of the substrate no example of this
35
what is quasi irreversible binding
binding of metabolic intermediate complex MIC active site metabolite mediates destruction
36
when do you have to make a new enzyme
irreversible antagonists
37
how to calculate the therapeutic index
TI = toxic concentrations / normal therapeutic range changes in a narrow TI are more serious
38
what % of hospital admissions can be drug adverse effect related
15% half of these admissions are drug interaction related
39
drugs that cancel each others effects
acwtylcholinesterases amd neuromuscular blockers
40
binding to different systems but achieving the same effect drug examples
benzodiazepines and propofol
41
same site competition drugs examples
benzodiazepines and barbiturates
42
drug interactions serotonin syndrome symptoms
agitation restlessness confusion rapid and high heart rate BP dilated pupils loss of muscle co ordination twitching muscles muscle rigidity heavy sweating diarrhea headache shivering fever seizures death
43
what is the key reasons for pharmacokinetic changes
hepatic metabolic changes accumulation - drug toxicity - hours disappearance - drug failure - days
44
how can drugs be limited in their effectiveness
pharmacokinetics pharmacodynamics biological systems are dynamic, aware, and resistant
45
what is the difference between specificity and selectivity
In summary, while specific drugs target a particular receptor or pathway with high affinity, selective drugs exhibit a preference for their intended target while minimizing interactions with other similar targets. Specificity refers to the precision of drug-target interactions, while selectivity relates to the degree of preference for a particular target over others. selective - preferance for a receptor / target specific - higher affinity
46
describe non competative inhibition
Non-competitively-antagonist binds at a different site*, prevents function.
47
example of non competative inhibition
miraviroc (anti-HIV) allosteric effect
48
what is preformulation
Preformulation is a branch of pharmaceutical sciences that utilizes biopharmaceutical principles in the determination of physicochemical properties of a drug substance involves the preliminary investigation of a drug's physical and chemical properties before formulation into a dosage form.
49
goals of preformulation
to choose the correct form of drug substance evaluate its physical properties generate a thorough understanding of the material's stability under various conditions, leading to the formulation of optimal drug delivery system
50
why is preformulation so important
First learning phase in dosage form development Fundamental physical and chemical properties are ascertained Only small quantity of drug substance available (mg)
51
what two things can you caracterise from preformulation
drug characterisation analytical charactisation
52
pharmaceutical profiling of drug charactarisation, how do you do it give examples of methods used
Assay - UV, HPLC, TLC Solubility (aqueous, pKa, salts, solvents, partition co efficient, dissolution) Melting point Stability Microscopy Powder flow (bulk density, angle of repose) Compression properties Excipient compatibility
53
Analytical preformulation give examples of methods used
Identity - NMR, IR, UV, DSC, TLC Purity - Moisture content, inorganic and organic impurities, DSC Assay - UV, HPLC Quality - Appearance, odour, colour, melting point All the above used to confirm structure and purity
54
when do compounds tend to have bioavailibility issues
Compounds with solubility less than 1% (pH 1-7 at 37⁰C) potentially have bioavailability issues
55
what are the poential solutions for drugs that may have possible solubility issues
Solubility in the range of 1-10mg/ml – salt formation desirable (only possible for ionisable drugs) Alternatively, liquid filling in capsules eg: neutral molecules, steroids etc
56
what is the definition of intrinsic solubility (Co)
– the fundamental solubility in an unionised state
57
why is solubility measured at two tempratures
Solubility measured at two temperatures – 4⁰C (to support physical stability and short term storage) and 37⁰C (for biopharmaceutical evaluation)
58
what does solubility data shed light on?
Solubility data sheds light on pKa and formulation approaches
59
tell me about pKa, and what is it?
75% of all drugs are basic 20% are weak acids 5% non ionic pKa stands for the acid dissociation constant, which is a measure of the strength of an acid in a solution. Specifically, it represents the equilibrium constant for the dissociation reaction of an acid in water.
60
why is pKa useful
Used to maintain solubility by altering pH of solution Formation of appropriate salts for the poorly soluble parent drug
61
tell me abot salt formation, adv and dis
Salts of strong acids/bases are freely soluble but suffer from high hygroscopicity leading to instability in tablet/capsule formulation Weaker acids/bases used to form salts (eg: maleate, acetate, aluminium)
62
what is intrinsic pH
"Intrinsic pH" typically refers to the inherent pH of a solution or medium without the addition of any external acidic or basic substances. It is determined by the concentration of hydrogen ions (H+) in the solution, which in turn affects its acidity or basicity.
63
what are the impacts of salt formation
Lowers intrinsic pH thereby increasing solubility exponentially Dissolution rate of salt higher than parent drug However, alterations in solubility/dissolution may affect bioavailability
64
what is QbD
QbD stands for Quality by Design, a systematic approach to pharmaceutical development that emphasizes the understanding of product and process variability and the application of scientific principles to ensure product quality. In essence, QbD shifts the focus from merely testing the final product to designing quality into the product from the outset of the development process.
65
Preformulation characteristics of Temazolamide?
Temazolamide is a medication used primarily in the treatment of certain types of brain tumors, such as glioblastoma multiforme. Before formulating Temazolamide into a dosage form, various preformulation studies would be conducted to understand its physical and chemical characteristics. Here are some preformulation characteristics of Temazolamide: solubiity stability particle size pKa
66
tell me about solvents and the most commonly used one
Water is the commonly employed solvent However aqueous instability is sometimes an issue (eg: chlordiazepoxide HCl is hydrolysed) Water miscible solvents used instead To improve solubility/ stability eg; glycerol, propylene glycol In analysis for extraction and separation eg: methanol, ethanol
67
what is the partition coefficient
Kw Def: the solvent : water quotient of drug distribution Uses: - gives information on aqueous and mixed solvent solubility - drug absorption in vivo - choice of column (HPLC) or plate (TLC)
68
what is the equation for Kw
K⁰w = (∑C-Cw)/(Cw) C = concentration in aqueous phase before partitioning Cw = concentration after partitioning
69
what partition is the most commonly employed
Octanol/ water partition most commonly employed Method : Shake flask method - drug assayed in aqueous phase of the mixture
70
tell me about dissolution
Dissolution rate of drug is important where it is the rate limiting step in absorption When dissolution controlled solely by diffusion, rate proportional to the saturated concentration of the drug in solution
71
what are the two types of dissolution and the differneces between them
Dissolution rate of drug is important where it is the rate limiting step in absorption When dissolution controlled solely by diffusion, rate proportional to the saturated concentration of the drug in solution In summary, intrinsic dissolution measures the rate of dissolution of pure drug substance under controlled conditions, providing insights into its inherent dissolution properties. Total dissolution, on the other hand, assesses the complete release of the drug from a dosage form, helping to evaluate its performance and bioavailability in practical applications. Both intrinsic dissolution and total dissolution testing are important tools in drug development and quality control.
72
what are the units for intrinsic dissolution
mg cm^2 / min^-1
73
what are the units for total dissolution
mg/ml
74
what is IDR
intrinsic dissolution rate It refers to the rate at which pure drug substance dissolves under standardized conditions, typically measured in micrograms per minute or milligrams per square centimeter per minute. Independent of formulation effects and measures intrinsic properties of drug
75
IDR equation
IDR = K1 X Cs IDR = rate constant X solubility or concentration in sink conditions
76
what is total dissolution, and what cannot be controlled
exposed surface area cannot be controlled as disintegration, disaggregation and dissolution proceed
77
what is the equation for total dissolution
Dc/Dt = A/V X K1 X Cs surface area / volume X rate constant X solubility or concentration in sink conditions
78
what is the common ion effect
Common ion significantly reduces the solubility of a slightly soluble electrolyte Two types Salting out: due to removal of water molecules as solvents i.e. hydration of other ions Salting in: due to larger anions which open the structure of water eg: benzoates, salicylates
79
what is salting in
Salting in: due to larger anions which open the structure of water eg: benzoates, salicylates Salting out: due to removal of water molecules as solvents i.e. hydration of other ions
80
what is salting out
Salting out: due to removal of water molecules as solvents i.e. hydration of other ions Salting out occurs when the addition of a common ion to a solution decreases the solubility of a slightly soluble salt.
81
how can melting point be measured
Can be measured using three different techniques Capillary melting- to determine melting range Hot stage microscopy – consists of heated sample stage Differential scanning calorimetry (DSC) Uses Melting point determination and phase changes shed light on polymorphism Also used for excipient selection
82

week 11 (Y2) (3 decks)

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