Intro to PMC
Basic Principals of Pharmacology
1. Define Pharmacology principles and definitions
a. Pharmacology: study of substances (chemical, herbal product, drug)
that interact with living systems via chemical processes by binding to
regulatory molecules (receptors)
i. Science of substances that are used to prevent, diagnose, and
treat disease
b. Pharmacodynamics: effect of drugs on your body (what do drugs do
to your body)
c. Pharmacokinetics: effect of body on the drugs (what does your body
do to the drugs)
d. Drug dose response curve: a graph created using concentration of
the drug as X axis and the physiological effect as Y axis
e. Emax: Maximum effect that can be elicited by a particular drug
f. EC50: The concentration of the drug that gives 50% of the maximal
effect
2. Discuss basic concepts of drugs and receptors
a. Drug: a substance that brings about a change in biological function
through its chemical actions
i. Drug Groups:
1. Drugs can be arranged in several groups
2. Drugs within a group are similar in pharmacodynamic
actions and pharmacokinetic properties
3. For a particular group few prototypic drugs will be
identified and discussed in detail
ii. Can either be synthesized by body (insulin), or a foreign
chemical (xenobiotic)
iii. All drugs are poisons if you take a large quantity
iv. Possess a specific charge, size, shape and atomic composition
v. Needs to be transported to the site of action from the site of
administration
vi. Clearance: Needs to be eliminated from the body at a
reasonable rate
, vii. Physical Nature: solid, liquid, gas
viii. Organic (carbs, lipids, proteins) or inorganic (Li, iron, heavy
metals)
ix. Drug size: in most cases, in order to achieve selective binding
to a receptor drug size need to be at least 100 MW units. Too
big drugs have a difficulty transporting the site of action
b. Drug receptor: Specific molecule (protein) that the drug interacts
with
i. Protein in the cell membrane or nuclear membrane or in the
cytoplasm
ii. Receptor has a specific shape that drug can fit into
iii. Located either on the cell membrane or inside the cell
iv. 5 trans-membrane signaling mechanisms
1. Intracellular receptors (e.g. steroid hormone receptor)
2. Receptor could be an enzyme located in the membrane
3. Receptor could be an ion channel protein located in the
membrane
4. Receptor could be a protein bound to tyrosine kinase
5. Receptor could be G protein coupled receptor
c. Drug Shape
i. Drug: Receptor = Key: Lock
ii. Drugs should have a specific shape that fits into receptors
specific site
iii. Chirality: most drugs are stereo isomers (mirror images)
iv. Properties of the isoforms may vary (one isomer may be more
potent than the other)
3. Describe drug receptor interactions
a. Drug Reactivity: bonds between the drug and the receptor/substarte
b. 3 kinds
i. Covalent – strong bond
ii. Electrostatic – weak bonds
iii. Hydrophobic – weak bonds
c. Drug-receptor interaction triggers cascade of events (e.g. activiation
of enzymes, blocking the enzyme’s action etc.)
, d. Example:
4. Discuss pharmacodynamic & pharmacokinetic processes
a. Pharmacodynamic
i. Processes: action of drugs on your body
ii. Principals:
1. Types of drug-receptor interactions
a. Agonist drugs: binds the receptor and brings the
effect
b. Antagonist drugs: binds the receptor and prevent
binding of other molecules
c. Partial agonist/antagonist
d. Drugs that mimic agonist drugs by inhibiting the
desensitization
2. Receptors and inert binding sites
a. In order to function as a receptor a molecule in
your body should selectively choose and bind to
the drug (ligand)
b. Upon this binding the molecule must change its
function resulting in a change in a biological
system
c. Inert binding sites: some molecules bind drugs
and this binding doesn’t result in a change in
biological function
b. Pharmacokinetics
i. Processes: action of the body on the drug
1. Regulate the absorption, distribution, and elimination of
the drugs
Basic Principals of Pharmacology
1. Define Pharmacology principles and definitions
a. Pharmacology: study of substances (chemical, herbal product, drug)
that interact with living systems via chemical processes by binding to
regulatory molecules (receptors)
i. Science of substances that are used to prevent, diagnose, and
treat disease
b. Pharmacodynamics: effect of drugs on your body (what do drugs do
to your body)
c. Pharmacokinetics: effect of body on the drugs (what does your body
do to the drugs)
d. Drug dose response curve: a graph created using concentration of
the drug as X axis and the physiological effect as Y axis
e. Emax: Maximum effect that can be elicited by a particular drug
f. EC50: The concentration of the drug that gives 50% of the maximal
effect
2. Discuss basic concepts of drugs and receptors
a. Drug: a substance that brings about a change in biological function
through its chemical actions
i. Drug Groups:
1. Drugs can be arranged in several groups
2. Drugs within a group are similar in pharmacodynamic
actions and pharmacokinetic properties
3. For a particular group few prototypic drugs will be
identified and discussed in detail
ii. Can either be synthesized by body (insulin), or a foreign
chemical (xenobiotic)
iii. All drugs are poisons if you take a large quantity
iv. Possess a specific charge, size, shape and atomic composition
v. Needs to be transported to the site of action from the site of
administration
vi. Clearance: Needs to be eliminated from the body at a
reasonable rate
, vii. Physical Nature: solid, liquid, gas
viii. Organic (carbs, lipids, proteins) or inorganic (Li, iron, heavy
metals)
ix. Drug size: in most cases, in order to achieve selective binding
to a receptor drug size need to be at least 100 MW units. Too
big drugs have a difficulty transporting the site of action
b. Drug receptor: Specific molecule (protein) that the drug interacts
with
i. Protein in the cell membrane or nuclear membrane or in the
cytoplasm
ii. Receptor has a specific shape that drug can fit into
iii. Located either on the cell membrane or inside the cell
iv. 5 trans-membrane signaling mechanisms
1. Intracellular receptors (e.g. steroid hormone receptor)
2. Receptor could be an enzyme located in the membrane
3. Receptor could be an ion channel protein located in the
membrane
4. Receptor could be a protein bound to tyrosine kinase
5. Receptor could be G protein coupled receptor
c. Drug Shape
i. Drug: Receptor = Key: Lock
ii. Drugs should have a specific shape that fits into receptors
specific site
iii. Chirality: most drugs are stereo isomers (mirror images)
iv. Properties of the isoforms may vary (one isomer may be more
potent than the other)
3. Describe drug receptor interactions
a. Drug Reactivity: bonds between the drug and the receptor/substarte
b. 3 kinds
i. Covalent – strong bond
ii. Electrostatic – weak bonds
iii. Hydrophobic – weak bonds
c. Drug-receptor interaction triggers cascade of events (e.g. activiation
of enzymes, blocking the enzyme’s action etc.)
, d. Example:
4. Discuss pharmacodynamic & pharmacokinetic processes
a. Pharmacodynamic
i. Processes: action of drugs on your body
ii. Principals:
1. Types of drug-receptor interactions
a. Agonist drugs: binds the receptor and brings the
effect
b. Antagonist drugs: binds the receptor and prevent
binding of other molecules
c. Partial agonist/antagonist
d. Drugs that mimic agonist drugs by inhibiting the
desensitization
2. Receptors and inert binding sites
a. In order to function as a receptor a molecule in
your body should selectively choose and bind to
the drug (ligand)
b. Upon this binding the molecule must change its
function resulting in a change in a biological
system
c. Inert binding sites: some molecules bind drugs
and this binding doesn’t result in a change in
biological function
b. Pharmacokinetics
i. Processes: action of the body on the drug
1. Regulate the absorption, distribution, and elimination of
the drugs
