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What is the primary focus of clinical pharmacology?
What is the primary focus of clinical pharmacology?
What is a drug, according to the definition?
What is a drug, according to the definition?
What is the main focus of pharmacodynamics?
What is the main focus of pharmacodynamics?
Which of the following is NOT a mechanism of drug action?
Which of the following is NOT a mechanism of drug action?
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What is a receptor in the context of pharmacodynamics?
What is a receptor in the context of pharmacodynamics?
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What is the primary focus of medical pharmacology?
What is the primary focus of medical pharmacology?
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Which of the following is an example of a direct chemical or physical mechanism of drug action?
Which of the following is an example of a direct chemical or physical mechanism of drug action?
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What is the interaction between the drug and the patient in clinical pharmacology?
What is the interaction between the drug and the patient in clinical pharmacology?
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What is the role of a ligand that blocks the receptor?
What is the role of a ligand that blocks the receptor?
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What determines the number of receptors occupied by a drug?
What determines the number of receptors occupied by a drug?
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What is characteristic of the response of ion channel-linked receptors?
What is characteristic of the response of ion channel-linked receptors?
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What is the function of an agonist?
What is the function of an agonist?
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What is the composition of an ion channel-linked receptor?
What is the composition of an ion channel-linked receptor?
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What happens when an agonist binds to the extracellular part of an ion channel-linked receptor?
What happens when an agonist binds to the extracellular part of an ion channel-linked receptor?
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What is the role of affinity in the receptor-ligand interaction?
What is the role of affinity in the receptor-ligand interaction?
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What is the term for the molecule that combines with a receptor?
What is the term for the molecule that combines with a receptor?
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Which type of receptors are located in the motor end plate and respond to nicotinic Ach?
Which type of receptors are located in the motor end plate and respond to nicotinic Ach?
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What is the response of GABA receptors in the brain to stimulation?
What is the response of GABA receptors in the brain to stimulation?
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What is the general structure of G-protein-linked receptors?
What is the general structure of G-protein-linked receptors?
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What is the effect of G-protein activation on GTP?
What is the effect of G-protein activation on GTP?
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What is the consequence of stimulatory G-protein activation?
What is the consequence of stimulatory G-protein activation?
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Which of the following receptors are examples of Gs-coupled receptors?
Which of the following receptors are examples of Gs-coupled receptors?
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What is the effect of ion channel receptors compared to G-protein-linked receptors?
What is the effect of ion channel receptors compared to G-protein-linked receptors?
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What is the consequence of binding of an agonist to the extracellular part of a G-protein-linked receptor?
What is the consequence of binding of an agonist to the extracellular part of a G-protein-linked receptor?
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What is the effect of inhibitory G-protein (Gi) on adenyl cyclase enzyme?
What is the effect of inhibitory G-protein (Gi) on adenyl cyclase enzyme?
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What is the effect of Gq-coupled receptors on inositol triphosphate (IP3)?
What is the effect of Gq-coupled receptors on inositol triphosphate (IP3)?
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What is the function of the TK-binding domain in tyrosine kinase (TK)-linked receptors?
What is the function of the TK-binding domain in tyrosine kinase (TK)-linked receptors?
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Which of the following receptors is NOT an example of a Gi-coupled receptor?
Which of the following receptors is NOT an example of a Gi-coupled receptor?
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What is the effect of IP3 on free intracellular Ca2+?
What is the effect of IP3 on free intracellular Ca2+?
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Which domain of the tyrosine kinase (TK)-linked receptor binds to hormones?
Which domain of the tyrosine kinase (TK)-linked receptor binds to hormones?
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What is the effect of Gi-coupled receptors on protein kinases?
What is the effect of Gi-coupled receptors on protein kinases?
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What is the function of the transmembrane segment in tyrosine kinase (TK)-linked receptors?
What is the function of the transmembrane segment in tyrosine kinase (TK)-linked receptors?
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What happens when an agonist binds to the hormone-binding domain of a receptor?
What happens when an agonist binds to the hormone-binding domain of a receptor?
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Where are intracellular receptors located?
Where are intracellular receptors located?
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What is a characteristic of intracellular receptors?
What is a characteristic of intracellular receptors?
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What type of bond is strong and irreversible?
What type of bond is strong and irreversible?
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What is the role of signaling proteins in the signaling pathway?
What is the role of signaling proteins in the signaling pathway?
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What must happen for an agonist to bind to an intracellular receptor?
What must happen for an agonist to bind to an intracellular receptor?
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What is an example of a receptor that is an intracellular receptor?
What is an example of a receptor that is an intracellular receptor?
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What is the characteristic of an ionic bond?
What is the characteristic of an ionic bond?
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Study Notes
Medical Pharmacology
- Medical pharmacology is a basic science that deals with small molecules used to prevent, diagnose, or treat diseases.
- Clinical pharmacology is the science concerned with the rational, safe, and effective use of drugs in humans.
Pharmacodynamics
- Pharmacodynamics is the study of what a drug does to the body.
- A drug can produce its effects through:
- Interaction with body control systems (regulatory proteins)
- Direct chemical or physical mechanisms
- Interaction with certain metabolic pathways
Receptors
- Receptors are protein macromolecules that combine with a drug to produce an effect.
- Ligand: any molecule that can combine with receptors.
- Agonist: a ligand that activates the receptor.
- Antagonist: a ligand that blocks the receptor.
- Affinity: the empathy of the receptor to the ligand, determining the number of receptors occupied by the drug.
Types of Receptors
-
Ion channel-linked receptors (direct ligand-gated ion channels):
- The receptor is an ion channel consisting of 5 transmembrane subunits.
- Binding of the agonist to the extracellular part of the receptor causes opening of the channel for a specific ion.
- Examples: nicotinic Ach receptors in the motor end-plate, GABA receptors in the brain.
-
G-protein-linked receptors:
- The receptor consists of 7 membrane subunits.
- Binding of the agonist to the extracellular part of the receptor causes activation of intracellular G-protein.
- Examples: stimulatory G-protein (Gs) leads to increase in adenyl cyclase enzyme → ↑ cAMP, inhibitory G-protein (Gi) leads to decrease in adenyl cyclase enzyme → ↓ cAMP.
-
Gq-coupled receptors:
- They increase inositol triphosphate (IP3) and diacylglycerol (DAG).
- IP3 increases free intracellular Ca.
- Examples: α1-adrenergic receptors, M1 and M3 muscarinic receptors.
-
Tyrosine kinase (TK)-linked receptors:
- The receptor consists of 2 large domains: an extracellular hormone-binding domain and an intracellular TK-binding domain.
- Binding of the agonist to the hormone-binding domain causes activation of the intracellular domain to activate TK enzyme.
- Examples: insulin receptors.
-
Intracellular receptors:
- They are located inside the cell, either in the cytoplasm or directly on the DNA.
- They regulate transcription of genes in the nucleus or the mitochondria.
- Examples: receptors for corticosteroids, sex hormones, thyroxin, etc.
Types of Drug-Receptor Bonds
-
Ionic bond:
- Electric attraction between two opposing charges.
- Strong but reversible.
-
Hydrogen bond:
- Attraction between two hydrogen bonds.
- Weak and reversible.
-
Covalent bond:
- Very strong and irreversible.
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Description
Learn about medical pharmacology, clinical pharmacology, and pharmacodynamics, including the effects of drugs on the body and their mechanisms.