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pharma sem 2 block 1 Flashcards

1
Q

what is pharmacokenetics?

A

its what the body does to the drug and includes absorption, distribution and metabolism and excretion

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2
Q

what is pharmacodymanics?

A

its what the drug does to the body

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3
Q

what is the shape of the concentraion-time curve shaped by?

A

the rate of absorption, how quickly its distributed and how quickly its eliminated

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4
Q

what is first pass metabolism?

A

its how much of the drug is directly excreted before going into the circulation

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5
Q

what are the characteristics of a drug formulation if its to be administered orally?

A

solid aggregates (usually cristalline)
water soluble salts

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6
Q

What does pharmacokinetics study?

A

Drug absorption, distribution, metabolism, excretion, and how the body affects the drug.

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7
Q

What is clinical pharmacokinetics?

A

The application of pharmacokinetic methods to ensure patients are treated safely and effectively.

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8
Q

What is drug absorption?

A

The transportation of the unmetabolized drug from the administration site to the body circulation system.

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9
Q

List the mechanisms of drug absorption.

A
  • Passive diffusion
  • Carrier-mediated membrane transport
  • Active diffusion
  • Facilitated diffusion
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10
Q

What factors can affect drug absorption?

A
  • Drug-specific factors
  • Patient-specific factors
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11
Q

What is bioavailability?

A

The rate and extent of a drug’s absorption.

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12
Q

What is the primary route of drug administration discussed in the article?

A

Oral route.

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13
Q

What is passive diffusion?

A

The most common mechanism of absorption for drugs, explained through the Fick law of diffusion.

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14
Q

What is Fick’s law of diffusion?

A

The principle that a drug moves according to the concentration gradient from higher concentration to lower concentration.

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15
Q

What is the role of P-glycoprotein in drug absorption?

A

It is an energy-dependent efflux transporter that restricts overall drug absorption.

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16
Q

How does active diffusion differ from passive diffusion?

A

Active diffusion requires energy and moves drugs against a concentration gradient, while passive diffusion does not.

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17
Q

What are physicochemical variables that affect drug absorption?

A
  • Drug solubility
  • pH and pKa
  • Particle size
  • Surface area
  • Dissolution rate
  • Polymorphism
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18
Q

What is the significance of drug solubility in absorption?

A

Ionized drugs are hydrophilic and cannot cross cell membranes, while non-ionized drugs are lipophilic and can penetrate easily.

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19
Q

What is polymorphism in pharmacokinetics?

A

The existence of more than one crystalline form of a solid substance.

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20
Q

What physiological factors affect drug absorption?

A
  • Age
  • Gastric emptying time
  • Intestinal transit time
  • Blood flow
  • Presystemic metabolism
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21
Q

How does age affect drug absorption?

A

Physiological changes with increased age may lead to decreased drug absorption.

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22
Q

What is first-pass metabolism?

A

The metabolism of orally administered drugs within the gut wall or liver before reaching circulation.

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23
Q

What is absolute bioavailability?

A

The bioavailability of an orally administered drug compared to its bioavailability following IV administration.

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24
Q

What is relative bioavailability?

A

The comparison of the bioavailability of an orally administered drug with that of an oral standard of the same drug.

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25
What is the order of bioavailability among different routes of administration from highest to lowest?
* Parenteral * Rectal * Oral * Topical
26
Why are IV drugs administered?
For rapid onset of response, in unconscious patients, or when the GI tract is non-functional.
27
What are bioequivalence studies?
Studies conducted to differentiate between two drug products with the same active ingredients.
28
True or False: Bioavailability directly affects the therapeutic range of a drug.
True.
29
what is the route most drugs take to systemic circulation?
through the portal blood vessel
30
what is the rate limiting step for the absorption of tablets?
the rate at which it dissolved
31
is the unionised form of the drug good or bad for absorption?
good as its got good lipophilicity for absorption
32
what determines the extent of ionisation of a drug?
the pH of the GIT fluid and the pKa of the drug
33
what is the bioavailability of the drug?
its the amount of drug which is still around after the drug has passed through the liver
34
what is the difference between the oral and IV administration called?
the bioavailability of the drug
35
what factors do you have to consider for oral administration?
food incompatibilities first pass effects irritability of the drugs incompatible physico-chemical properties i.e. non-ionic highly lipophilic drugs wont be able to pass through membranes in the gut to be absorbed the chemical stability the onset of action i.e. opioids are usually IV as theyve got a faster onset location of action- asthma and acute pain systemic or local effects- i.e. steroids for rashes
36
what are enteric coated tabs used for?
to avoid being broken down in the acidic stomach environment
37
what is the positive of buccal/sublingual administration?
it avoids the first pass effects and has a fast onset
38
why administer omeprazole at the same time as ibuprofen?
as its a proton pump inhibitor so it stops the harmful gastric effects of the ibuprofen
39
what helps with the formation of a dynamic equlibrium for the drug?
the binding of drug molecules to plasma proteins, only unbound molecules are able to leave the circulation and cause a theraputic effect
40
how does plasma albumin contribute to drug interactions?
the drugs compete for the same binding sites on the plasma albumin and can result in changing the free concs of the drugs in circulation
41
what effects on the drug distribution does plasma protein binding have?
it makes the action of the drugs longer and less intesnse as theres less free drug available
42
how is the volume of distribution measured?
Vd = dose/ plasma conc
43
what are the four patterns of distribution?
in the vascular system (i.e. warfarin) where drugs stay in the bloodstream due to them being strongly bound to the plasma protein in the extracellular fluid where they dont usually do into the cells (streptomycin) uniformly distributed (paracetamol) low molecular weight and easily moves through tissues concentrated in specific tissues (chloroquine an anti-malarial is concentrated in the liver) however most drugs are a combo of these and have non-uniform distribution throughout the whole body and can pass through membranes when the carry a positive charge
44
why are there high levels of bound drug on plasma albumin?
as plasma albumin has a naturally positive charge due to the high percentage of amines and positive proteins making it good for binding high levels of negatively charged ionised drugs
45
why does it take longer for acidic drugs to distribute round the body?
as theres lower levels of free drug due to the majority of acidic drugs binding to plasma proteins such as albumin
46
what is the absorption of drugs from the blood stream into the tissues determined by?
the high levels of phosphilipid content in the cellular membranes meaning that basic drugs can easily pass through due to the mutual attraction to the pps
47
what are some examples of acidic drugs?
gentamycin, ibuprofen and naproxen
48
what are some examples of basic drugs?
paracetamol, ketamine and morphine, theyve all got Vd>0.7
49
what characteristics affect Vd?
the drugs relative water and lipid solubility the plasma/tissue binding properties if it required loading doses to establish theraputic drug concentrations
50
what drugs need loading doses?
amiodarone or digoxin
51
what ways can drugs get through the BBB?
through tight junctions- water soluble drugs through the membrane of the endothelium- lipid-soluble drugs transport proteins by specific receptor mediated endocytosis- i.e. transferrin (rivagastine binds to transferin through its Fab fragment to allow the mAb ganterneumab to clear amyloid-beta aggragates in AD) cationisation of native plasma proteins increases their uptake by absorptive-mediated endocytosis
52
why is the uptake of drugs through the BBB much smaller than other lipid membranes?
because the tight junctions only allow in very small molecules and normal blood proteins arent able to cross
53
what clinical considerations do you have to have when thinking about drug distribution?
how widely distributed it is, the wider its distributed, the harder it is to remove from the body as its far away from the liver if certian disease states affect its metabolism and excretion how the drug will get to the target tissue how available it is in the circulation, very available and its effects will wear off quickly and will be vv strong
54
what are compartment models in pharmacokenetics?
its the model used to investigate the distribution of drugs accross the fast and slow distributing tissues fast= muscle slow=fat just think of athletes and obese people
55
what is the three compartment model?
its the distribution of drugs between the central compartment of blood, brain and liver with the slow redistributing tissues of adipose tissue and the fast redistributing tissues of muscle and vicera
56
what diseases impact pharmacokenetics?
diabetes, liver and renal diseases, heart failure and sepsis, dysregulation of hepatic enzymes
57
what are the things to think about when it comes to pharmacokenetics?
Absorption Distribution Metabolism Excretion
58
how does diabetes alter PK?
Absorption, due to changes in subcutaneous adipose blood flow, muscle blood flow and gastric emptying; (ii) distribution, due to non-enzymatic glycation of albumin; (iii) biotransformation, due to regulation of enzymes/transporters involved in drug biotransformation; and (iv) excretion, due to nephropathy
59
how does age alter PK?
it leads to changes in drug deposition and sensitivity due to physiological chnages in childhood and as a result of ageing which impact the dynamics of compounds
60
what is ageing associated with?
a reduction in first-pass metabolism
61
what is the irrational use of medicines?
the over or underuse or misuse of drugs and expensive drug administration i.e. drugs given via IV when they can be given orally
62
what are the most common measures of inequality?
Life Expectancy Infant Mortality Obesity and Overweightness (BMI) Mortality Rate Regular smokers/tobacco consumption Self-perceived health
63
what are some factors in improving lifespan?
hygine and clean water treatment of infectious diseases treatment of CVD effective cancer treatments
64
what are some reasons for inequalities in health?
bad environments poor conditions during development income differences educational differences
65
what are the inequalites relative to birth?
theres more adversde intra-uterine conditions in more deprived areas due to more chronic illness, poor maternal nutrition (linked with T2D) low birth weight- heart problems and vascular problems
66
what are the effects of neglect?
alteration of the HPA axis - alters the natural biological stress response, risk factor for anxiety, depression, CVD and chronic health impairments learning difficulties leading to reduced attainment
67
what are the effects of alcohol on health?
liver disease cancer risks CV effects- hypertension, stroke, arrhythmia and MI neurological degeneration leading to dementia fetal alcohol syndrome
68
what are the effects of the health inequality life cycle on adults?
smoking obestity alcohol dependance drug abuse
69
what are the effects of obestity on health?
less heathy eating, nutrition and excersize increase levels of adipose tissue leading to increased rates of cancer, death + T2D+ CVD+ muscoskeletal diseases impacts on PK due to increases in slow redistributing adipose tissue, difficulty with IV access + incr absorption due to increased gastric emptying, increased elimination of drugs
70
what treatments are there for AD?
lecanumab- mAb which binds AB with high affinity sage-718 - modulates NMDA receptors beta-secretase inhbitors gamma-secretase inhibitors gamma secretase AChE inhibitors NMDA antagonists
71
what drugs are given on the NHS for AD?
AChE inhibitors like donepzil, galantmine and rivastigine NMDA antagonists like memantamine for severe AD
72
what are the reccomendations for SZ treatments?
give a 1st gen typical anti-psycotic such as chloropromazine, haloperdiol, levopromazine or sulpride OR give a 2nd gen atypical antipsycotic if 1st gen didnt work like amisupride, clozapine, olnazepine or rispodarone or for noncompliant patients, consider giving a depot-injection such as haloperdiol or rispodarone
73
what is the only anti-psychotic which is suitable for anyone with psychosis?
clozapine but should not be considered before giving two other anti-psycotics with one of them being a non-clozapine 2nd gen
74
what else should be given in addition to an antipsycotic drug?
psycological therapies incluiding CBT for the patient and family therapy also a healthy eating plan and an excersize plan should be reccommended in addition to the anti-psycotic
75

pharmacology sem 2 (5 decks)

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