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IMS > PHARMACOLOGY 2 > Flashcards

PHARMACOLOGY 2 Flashcards

1
Q

what are xenobiotics?

A

foreign compounds with no nutritional value

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2
Q

what is the overall repoonse of patients due to?

A

Pharmacodynamic effects

Pharmacokinetic effects

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3
Q

what does absorption, distribution and metabolism depend on?

A

Route of administration of drug

Physico-chemical properties of drug

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4
Q

how can things diffuse through the cell membrane?

A

through the lipid bilayer, aqueous channels or special transport proteins eg. carrier/channel proteins

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5
Q

what are chemical properties of drugs?

A

Drug Structure
Molecular Weight
Lipophilicity
Ionisation

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6
Q

what are physiological variables affecting drugs absorption?

A 
pH of site
Surface area of memb
Mesenteric blood flow
Gastric emptying
Presence of food 
Efflux transporters
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7
Q

what is bioavailability?

A

% of the administered dose reaching the systemic circulation as unchanged drug (not as metabolites)

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8
Q

what is bioavailability governed by?

A

Absorption

First pass metabolism

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9
Q

where do most drugs need to be absorbed into?

A

the bloodstream, usually from the GI tract

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10
Q

where do enteral/oral go to?

A

to/through epithelium of G.I. tract (any location, from oral to rectal mucosa, could be many formulations

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11
Q

what does drugs given parenterally mean?

A

aside from intestine

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12
Q

where do drugs given parenterally cross and avoid?

A

may cross epithelium (e.g. skin, lung)

may avoid epithelium (e.g. subcutaneous, intramuscular, intrathecal, intraperitoneal injection)

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13
Q

what other ways are drugs administered?

A

directly into bloodstream

some drugs act locally at site of application, topical administration eg skin, eyes, vagina, nasal mucosa, airways

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14
Q

what do drugs given directly into the bloodstream allow?

A

absorption avoided by intravascular administration, e.g. intravenous, intra-arterial.
used for infusion, large volumes

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15
Q

what does ADME stand for?

A

absorption
distribution
metabolism
excretion

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16
Q

what is pharmacokinetics?

A

study of these processes to understand size and duration of response

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17
Q

what does distribution depend on?

A

on molecular size, ability to cross memb and extent of binding to plasma proteins.

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18
Q

what does plasma protein binding involve?

A

Loose electrostatic bonding, especially to albumin (for acidic drugs) and acid glycoprotein (for basic drugs)

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19
Q

what is equilibrium established between?

A

between bound & free form

20
Q

what does equilibrium allow?

A

reduces free drug conc available in plasma to reach site of action

21
Q

how does elimination occur?

A

Renal excretion

Liver metabolism Chemical transformation

22
Q

what are the 2 compounds not metabolised, and cleared almost exclusively by glomerular filtration?

A

Small water-soluble molecules

Some complex carbohydrates

23
Q

what drugs are extensively metabolised?

A

Lipophilic drugs

24
Q

what would happen to lipophilic drugs if metabolism didn’t occur?

A

lipophilic drugs would be recycled endlessly through glomerular or enterohepatic re-absorption

25
Q

what reactions are phase I metabolism?

A

Functionalisation reactions

26
Q

what reactions are phase II metabolism?

A

Conjugation reactions

27
Q

what reactions are phase III metabolism?

A

Formation of xenobiotic- macromolecule adducts

28
Q

what is phase I metabolism?

A

Addition or unmasking of a functional polar group

29
Q

give examples of phase I metabolism

A 
Oxidation	
Reduction 
Hydrolysis
Hydration
Isomerisation
Miscellaneous
30
Q

what occurs to go from phase I to II metabolism?

A

Addition of a polar group
Catalysed by transferases
Cofactor donor

31
Q

what are properties of drug-metabolising enzymes?

A 
Low substrate specificity 
May have low reaction specificity 
Lower catalytic rates but may be present in high conc
Substrates are usually lipophilic
Enzymes are inducible
32
Q

where does drug metabolism mainly occurs?

A

in 2 sub-cellular compartments in liver
Smooth Endoplasmic reticulum
cytosol

33
Q

what is the Smooth Endoplasmic reticulum?

A

Continuous network of filamentous, memb bound channels

34
Q

what happens when the drug reaches the Smooth Endoplasmic reticulum?

A

Cell disruption breaks the endoplasmic reticulum into small fragments which have metabolising enzymes
associated - Microsomes

35
Q

give examples of Microsomal enzymes

A

Cytochrome P450
Flavin monooxygenase (FMO)
Glucuronosyl transferase
Epoxide hydrolase

36
Q

give examples of Cytosolic enzymes

A 
Aldehyde oxidase
Aldehyde dehydrogenase
Alcohol dehydrogenase
Glutathione transferase
Sulphotransferase
37
Q

give examples of Mitochondrial enzymes

A

Aldehyde dehydrogenase

Monoamine oxidase

38
Q

what are oxidation reactions catalysed by?

A

Cytochrome P450

39
Q

give examples of factors that affect metabolism

A 
Competition between substrates
Inhibition of enzymes by drugs
Induction of enzyme systems
Age, nutritional status, liver disease
Genetic polymorphism
40
Q

how does induction of enzyme systems affect drug metabolism?

A

Inhibits function of repressor gene therefore operator gene active more mRNA more enzyme protein. rate of metabolism of barbiturates & other drugs increases and drugs become less effective

41
Q

how does genetic polymorphism affect drug metabolism?

A

individuals or population groups may have less/more of particular enzymes & show slower/faster rates of metabolism

42
Q

what is the role of the liver in drug metabolism?

A

Major site of drug metabolism & drug metabolising enzymes

43
Q

what is first pass metabolism?

A

delivery of drug direct to liver after oral administration

44
Q

what compromises metabolism/excretion of drugs?

A

Liver disease, liver function failure, reduction of synthesis of plasma proteins

45
Q

give examples of inter-individual factors

A

species
sex
genetic factors

46
Q

give examples of intra-individual factors

A 
age 
pregnancy 
stress 
disease 
nutrition 
enzyme induction 
enzyme inhibition
47
Q

what does drug effect in individual patient depend on?

A 
Dose, potency, efficacy
Mechanism of action
Route of administration, extent of absorption
Patient compliance
Age, body weight, sex
Rate of inactivation/excretion (liver, kidney function)
Genetic factors
Other drugs
Placebo effect
Disease
Tolerance to drug

IMS (52 decks)

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