31/01/2025 11:47:55
Pharmacology
what is a drug
any chemical that changes the processes of living
Drug Nomenclature
Chemical name: N-Acetyl-p-aminophenol (development stage)
Generic Name: Acetominophen (easier to pronounce and remember) *only 1 generic
name. They all have the same suffix.
Trade name: Tylenol (can be numerous trade names)
Drug Resources
1. physicians desk reference (PDR)
2. Nursing drug guides (mosby's' et al.)
3. Online resources (epocrates.com)
What is a receptor? 5 components
1. some component on or inside a cell that substances can bind
2. Most drugs and endogenous substances bind receptors
3. Most protein based
4. Lock and key (structurally match up to receptor)
5. Receptor Subtypes (ex: ACH-nicotinic receptor: recognizes both autonomic
ganglion and skeletal muscle, but can make one that only recognizes on area)
Types of Receptors
1. Receptors located on the cell surface
2. Intracellular Receptors
-Cytosolic receptors
-Nuclear receptors
Why have receptors on the cell surface?
Majority of hormones are not have able to cross the membrane through diffusion, so
they have to bind to a receptor on the surface to get into the cell.
They are not lipid soluble.
most hormones and neurostransmitters are lipid INSOLUBLE, so they need
receptors to bring them into the cell.
Receptors on the cell surface
Communication of hormones and receptors.
1. Receptors are linked to ion channels. They control the opening of it. (Ex:
acetylcholine is able to get Na+ into the cell by initiating opening of ion channels
when it binds)
2. receptors linked to enzymes (ex: insulin or GH, bind to receptor on surface and
causes the enzymatic portion to produce changes within the cell. *Picture ^)
,31/01/2025 11:47:55
3. Receptors linked to second messengers
(Both use G proteins: Adenylate Cyclase System, IP3 system)
Second Messenger System
Adenylate Cyclase steps
1. hormone binds to the specific receptor (1st messenger) *The receptor must be
COUPLED to the G protein to work.
2. Causes GTP to bind to protien
3. Causes G protein to move away from receptor through the membrane until it
encounters an enzyme
4. the enzyme is adylte. cyclase
5. ad cly. takesATP and convert it to cyclic ATP
6 .CYClic ATP is our second messenger.
7. Cyclic ATP activates an enzyme and triggers responses of the target cell.
Second messenger system
Phospholipase C Mechanism (IP3 system) Steps
1. hormone binds to receptor
2. receptor coupled to g protein
3. G protein moves away from receptor into the membrane
4. moves through membrane and encounters enzyme phospholipase C
5. Phospholipase C causes the production of 2 products (BAG and IP3)
6. It allows the signals to become amplified.
Ex: Every step of the way the response gets bigger. 2 --> 4 --> 8 -->16
Intracellular Receptors (2)
LIPID SOLUBLE substances
1. Cytosolic (cytoplasm) ex: thyroid hormone
2. Nuclear (goes into nucleus)
Non receptor mechanisms
- Nitrates- reduced to NO, bind guanylate cyclase
Ex: vasodilators
-Some chemotherapeutic agents become incorporated into cellular components and
block metabolic reactions
agonist
antagonist
ag: drug that binds a receptor and produces a biochemical response
Ant: binds the receptor but doesn't produce a biochemical response. "it's a blank" No
second messenger is produced.
, 31/01/2025 11:47:55
*So why have it? tumor causing too much epinephrine binding, so antagonist drug
competes with epinephrine for that receptor and blocks its ability to bind and cause
the heart to contract too much.
Affinity: high vs low.
Specificity= selectivity (dose-dependent)
* You want highly selective/specific drugs. So you don't produce side-affects
A: attraction between a drug and a receptor
High affinity: drug will bind, even when the drug is in extremely low concentration
Low affinity: won't bind drug until there is a high concentration of it.
S: How specific the drug is for a particular type of receptor.
Drugs that are highly selective, ONLY bind to that one receptor.
As the dose is increased, it may become less and less selective.
*this causes side-affects to go up.
Efficacy
Intrinsic Activity ~ efficacy
E: Does the drug to what it was intended. Effectiveness of the drug.
*more important than potency
IA: More effective response even by stimulating it just a little bit.
Potency
Tolerance
Additive/synergistic drug interactions
P: how concentrated a drug is.
T: need for a higher dose of a drug to produce the standard effect
Ex: oxycotin for pain, after 2 week, the oxycotin won't produce the same pain
modulating affects as before.
Add/syn: more than one drug can produce one type of response.
Ex: NE and E increases HR.
Giving both at the same time, and 20 bpm happened, the drugs were additive. 10
bpm from NE, and 10 bpm from E.
BUT if a 30 bpm happens, its a synergistic interaction.
The SUM is greater than it's parts.
Drug Receptor interactions
Occupancy Theory: if 1mg dose was given, a certain percent of receptors would be
blinded. But if you give a 10mg dose, you'd bind more receptors and so on. Bigger
responses based on # of receptors bound.
*BUT you don't have to bind all the receptors to get 100% of the response you
Pharmacology
what is a drug
any chemical that changes the processes of living
Drug Nomenclature
Chemical name: N-Acetyl-p-aminophenol (development stage)
Generic Name: Acetominophen (easier to pronounce and remember) *only 1 generic
name. They all have the same suffix.
Trade name: Tylenol (can be numerous trade names)
Drug Resources
1. physicians desk reference (PDR)
2. Nursing drug guides (mosby's' et al.)
3. Online resources (epocrates.com)
What is a receptor? 5 components
1. some component on or inside a cell that substances can bind
2. Most drugs and endogenous substances bind receptors
3. Most protein based
4. Lock and key (structurally match up to receptor)
5. Receptor Subtypes (ex: ACH-nicotinic receptor: recognizes both autonomic
ganglion and skeletal muscle, but can make one that only recognizes on area)
Types of Receptors
1. Receptors located on the cell surface
2. Intracellular Receptors
-Cytosolic receptors
-Nuclear receptors
Why have receptors on the cell surface?
Majority of hormones are not have able to cross the membrane through diffusion, so
they have to bind to a receptor on the surface to get into the cell.
They are not lipid soluble.
most hormones and neurostransmitters are lipid INSOLUBLE, so they need
receptors to bring them into the cell.
Receptors on the cell surface
Communication of hormones and receptors.
1. Receptors are linked to ion channels. They control the opening of it. (Ex:
acetylcholine is able to get Na+ into the cell by initiating opening of ion channels
when it binds)
2. receptors linked to enzymes (ex: insulin or GH, bind to receptor on surface and
causes the enzymatic portion to produce changes within the cell. *Picture ^)
,31/01/2025 11:47:55
3. Receptors linked to second messengers
(Both use G proteins: Adenylate Cyclase System, IP3 system)
Second Messenger System
Adenylate Cyclase steps
1. hormone binds to the specific receptor (1st messenger) *The receptor must be
COUPLED to the G protein to work.
2. Causes GTP to bind to protien
3. Causes G protein to move away from receptor through the membrane until it
encounters an enzyme
4. the enzyme is adylte. cyclase
5. ad cly. takesATP and convert it to cyclic ATP
6 .CYClic ATP is our second messenger.
7. Cyclic ATP activates an enzyme and triggers responses of the target cell.
Second messenger system
Phospholipase C Mechanism (IP3 system) Steps
1. hormone binds to receptor
2. receptor coupled to g protein
3. G protein moves away from receptor into the membrane
4. moves through membrane and encounters enzyme phospholipase C
5. Phospholipase C causes the production of 2 products (BAG and IP3)
6. It allows the signals to become amplified.
Ex: Every step of the way the response gets bigger. 2 --> 4 --> 8 -->16
Intracellular Receptors (2)
LIPID SOLUBLE substances
1. Cytosolic (cytoplasm) ex: thyroid hormone
2. Nuclear (goes into nucleus)
Non receptor mechanisms
- Nitrates- reduced to NO, bind guanylate cyclase
Ex: vasodilators
-Some chemotherapeutic agents become incorporated into cellular components and
block metabolic reactions
agonist
antagonist
ag: drug that binds a receptor and produces a biochemical response
Ant: binds the receptor but doesn't produce a biochemical response. "it's a blank" No
second messenger is produced.
, 31/01/2025 11:47:55
*So why have it? tumor causing too much epinephrine binding, so antagonist drug
competes with epinephrine for that receptor and blocks its ability to bind and cause
the heart to contract too much.
Affinity: high vs low.
Specificity= selectivity (dose-dependent)
* You want highly selective/specific drugs. So you don't produce side-affects
A: attraction between a drug and a receptor
High affinity: drug will bind, even when the drug is in extremely low concentration
Low affinity: won't bind drug until there is a high concentration of it.
S: How specific the drug is for a particular type of receptor.
Drugs that are highly selective, ONLY bind to that one receptor.
As the dose is increased, it may become less and less selective.
*this causes side-affects to go up.
Efficacy
Intrinsic Activity ~ efficacy
E: Does the drug to what it was intended. Effectiveness of the drug.
*more important than potency
IA: More effective response even by stimulating it just a little bit.
Potency
Tolerance
Additive/synergistic drug interactions
P: how concentrated a drug is.
T: need for a higher dose of a drug to produce the standard effect
Ex: oxycotin for pain, after 2 week, the oxycotin won't produce the same pain
modulating affects as before.
Add/syn: more than one drug can produce one type of response.
Ex: NE and E increases HR.
Giving both at the same time, and 20 bpm happened, the drugs were additive. 10
bpm from NE, and 10 bpm from E.
BUT if a 30 bpm happens, its a synergistic interaction.
The SUM is greater than it's parts.
Drug Receptor interactions
Occupancy Theory: if 1mg dose was given, a certain percent of receptors would be
blinded. But if you give a 10mg dose, you'd bind more receptors and so on. Bigger
responses based on # of receptors bound.
*BUT you don't have to bind all the receptors to get 100% of the response you
