PHARMACOLOGY AND NUTRITION – HNH23306
Lecture 1 + syllabus
Pharmacology = study of the effects of drugs on living systems, aiming to improve their
functioning.
Pills dont exist -> it’s a tablet
OTC: over the counter, get it without
prescribtion
Pharmacotherapy = refers to the treatment of disease with drugs in an applied science.
Pharmacokinetics = what the body does to a drug (ADME)
Drug = any substance or combination which may be administered to human being with a
view to making a medical diagnosis or t orestoring, correcting or modifying physiological
functions in human beings.
Medicines need approval
- National autorities (CBG in NL)
- European (EMA)
In the Netherlands each medicine should have a unique registration code:
Nationally approved: RVG code
Homeopathic medicines: RVH code
European registration: EU code
Naproxen-sodium
- Nonsteroidal anti-inflammatory drug (NSAID)
- Analgesic and antipyretic properties
- Basic salt, conjugated
- De NSAID binds to cyclo-oxygenase: prostaglandins (immune-sustem). They are all
formed from arachidonic acid (omgea-6, diet)
- Cox-1: constictutive, good guys always present
Cox-2 more produced with fever, bad guys (feeling bad,
not the inflammation)
There are structural differences between the substrate-binding
channels of COX-1 and COX-2 that allow the design of selective
inhibitors -> some substrates are nonselective (can bind to both). Some substrates are only
COX-2 selective inhibitors.
There need to be a balance between selectivity. Too much COX-2: higher risk of
cardiovascular diseases. Too much blocking COX-1: gastrointestinal risk.
,Tablet: used because you can’t see a very small amount (10 ug) and you can easily
modulate it (stability, uptake time): formulation. Drug substances are rarely adminstered
alone but often as a part of a formulation or dosage form.
Formulation = refers to a combination of one or
more active compounds (drugs) and one or more
excipients (hulpstoffen)
Coated tablets: protects core in the stomach,
released in the upper GI tract after the stomach.
Phases in pharmacology:
- Pharmaceutical phase: formulation,
disintegration, dissolution
- Pharmokinetic phase: ADME
- Pharmodynamic phase: interaction with molecular targets
Oral drug absorption:
Mostly in duodenum
Should be in dissolved state
Cross several semi permeable cell membranes before circulation (biological barriers
that selectively inhibits passage of drug molecules)
Often by passive diffusion, sometimes active
Lipid soluble compounds (partly) with lipids
Metabolism in intestinal wall can be considerable
Difference MTC – MEC is therapeutic window
Mechanisms transport (active/passive), rate-limiting and
excretion, biotransformation -> diettri summary
Phyto therapeutics: in NL mostly regulated as “food
supplements”
Phytotherapy is based on plants, homeopathy can use plants but not only (they will dilute
the plant extract)
Food supplements = foodstuffs the purpose of which is to supplement the normal diet and
which are concentrated sources of nutrients or other substances with a nutritional or
physiological effect.
, Food supplements, functional foods, but also normal food products may carry nutrition
and/or health claims. Such as milk: good source of calcium, calcium helps build strong
bones. It can also contain indirect claims, but these are not allowed (stophoest; is a brand
name)
Nutrition claims/ content claim = what it in the food? (without directly referring to a health
benefit)
Health claims = what does the food do?
- Function claims based on generally accepted scientific data (article 13.1)
- Function claims based on newly developed scientific data (article 13.5)
- Reduction of disease risk claims + claims growth and development of children (article
14)
Lecture 2 + syllabus
Pharmacodynamics
- The molecular action of a drug / bioactive can often be explained by- and predicted
from a receptor concept.
- Receptors are mostly normal regulatory structures
- Natural ligands: neurotransmitters, hormones or other signalling molecules
- Drugs just bind by coincidence or by design to these receptors
Receptors = macromolecules including enzymes, transporters, structures on cell
membranes, transcription factors, nucleotides etc.
Different classes of receptors
- Multi-subunit ion channels (ligand-gated ion channels)
o cell surface transmembrane (location)
o examples of ligands: Acetylcholine, GABA, glutamate, glycine
o the flow is regulated
o milliseconds; controls the fastest synaptic events
o modulated by binding of agonists or antagonists
- G-protein coupled receptors
o Cell surface transmembrane (location)
o Examples of ligands: acetylcholine, a and B-adrenergic eicosanoids
o Seconds
o Called G-proteins because of their interaction with GTP and GDP
- Protein kinases
o Cell surface transmembrane (location)
o Example of ligands: growth factors, Insulin, peptide hormones
o Hours
- Transcription factors
o Cytoplasm (location)
o Examples of ligands: steroid hormones, thyroid hormone, vitamin D
o Hours
Types of target for drug action:
- Receptors -> agonist / antagonist
- Ion channels -> blockers / modulators
- Enzymes -> inhibitor / false substrate
- Transporters
Real receptors = regulated by themselves; channels, receptors. Enzymes and transporters
aren’t real receptors.
Lecture 1 + syllabus
Pharmacology = study of the effects of drugs on living systems, aiming to improve their
functioning.
Pills dont exist -> it’s a tablet
OTC: over the counter, get it without
prescribtion
Pharmacotherapy = refers to the treatment of disease with drugs in an applied science.
Pharmacokinetics = what the body does to a drug (ADME)
Drug = any substance or combination which may be administered to human being with a
view to making a medical diagnosis or t orestoring, correcting or modifying physiological
functions in human beings.
Medicines need approval
- National autorities (CBG in NL)
- European (EMA)
In the Netherlands each medicine should have a unique registration code:
Nationally approved: RVG code
Homeopathic medicines: RVH code
European registration: EU code
Naproxen-sodium
- Nonsteroidal anti-inflammatory drug (NSAID)
- Analgesic and antipyretic properties
- Basic salt, conjugated
- De NSAID binds to cyclo-oxygenase: prostaglandins (immune-sustem). They are all
formed from arachidonic acid (omgea-6, diet)
- Cox-1: constictutive, good guys always present
Cox-2 more produced with fever, bad guys (feeling bad,
not the inflammation)
There are structural differences between the substrate-binding
channels of COX-1 and COX-2 that allow the design of selective
inhibitors -> some substrates are nonselective (can bind to both). Some substrates are only
COX-2 selective inhibitors.
There need to be a balance between selectivity. Too much COX-2: higher risk of
cardiovascular diseases. Too much blocking COX-1: gastrointestinal risk.
,Tablet: used because you can’t see a very small amount (10 ug) and you can easily
modulate it (stability, uptake time): formulation. Drug substances are rarely adminstered
alone but often as a part of a formulation or dosage form.
Formulation = refers to a combination of one or
more active compounds (drugs) and one or more
excipients (hulpstoffen)
Coated tablets: protects core in the stomach,
released in the upper GI tract after the stomach.
Phases in pharmacology:
- Pharmaceutical phase: formulation,
disintegration, dissolution
- Pharmokinetic phase: ADME
- Pharmodynamic phase: interaction with molecular targets
Oral drug absorption:
Mostly in duodenum
Should be in dissolved state
Cross several semi permeable cell membranes before circulation (biological barriers
that selectively inhibits passage of drug molecules)
Often by passive diffusion, sometimes active
Lipid soluble compounds (partly) with lipids
Metabolism in intestinal wall can be considerable
Difference MTC – MEC is therapeutic window
Mechanisms transport (active/passive), rate-limiting and
excretion, biotransformation -> diettri summary
Phyto therapeutics: in NL mostly regulated as “food
supplements”
Phytotherapy is based on plants, homeopathy can use plants but not only (they will dilute
the plant extract)
Food supplements = foodstuffs the purpose of which is to supplement the normal diet and
which are concentrated sources of nutrients or other substances with a nutritional or
physiological effect.
, Food supplements, functional foods, but also normal food products may carry nutrition
and/or health claims. Such as milk: good source of calcium, calcium helps build strong
bones. It can also contain indirect claims, but these are not allowed (stophoest; is a brand
name)
Nutrition claims/ content claim = what it in the food? (without directly referring to a health
benefit)
Health claims = what does the food do?
- Function claims based on generally accepted scientific data (article 13.1)
- Function claims based on newly developed scientific data (article 13.5)
- Reduction of disease risk claims + claims growth and development of children (article
14)
Lecture 2 + syllabus
Pharmacodynamics
- The molecular action of a drug / bioactive can often be explained by- and predicted
from a receptor concept.
- Receptors are mostly normal regulatory structures
- Natural ligands: neurotransmitters, hormones or other signalling molecules
- Drugs just bind by coincidence or by design to these receptors
Receptors = macromolecules including enzymes, transporters, structures on cell
membranes, transcription factors, nucleotides etc.
Different classes of receptors
- Multi-subunit ion channels (ligand-gated ion channels)
o cell surface transmembrane (location)
o examples of ligands: Acetylcholine, GABA, glutamate, glycine
o the flow is regulated
o milliseconds; controls the fastest synaptic events
o modulated by binding of agonists or antagonists
- G-protein coupled receptors
o Cell surface transmembrane (location)
o Examples of ligands: acetylcholine, a and B-adrenergic eicosanoids
o Seconds
o Called G-proteins because of their interaction with GTP and GDP
- Protein kinases
o Cell surface transmembrane (location)
o Example of ligands: growth factors, Insulin, peptide hormones
o Hours
- Transcription factors
o Cytoplasm (location)
o Examples of ligands: steroid hormones, thyroid hormone, vitamin D
o Hours
Types of target for drug action:
- Receptors -> agonist / antagonist
- Ion channels -> blockers / modulators
- Enzymes -> inhibitor / false substrate
- Transporters
Real receptors = regulated by themselves; channels, receptors. Enzymes and transporters
aren’t real receptors.
