Pharmacology
Lec. 1 in Pharmacology II
4th year students
1st semester
(2024-2025)
By: Ibraheem Akram Omar, Ph.D
• What is Pharmacology?
• Pharmakon + logos
• What is a drug?
• The three characteristics of drug effects
What is the objective of studying
pharmacology?
Drug classes Drug effects
Drug
Mechanism of action Side effects
What are the two main areas of
pharmacology?
• Pharmacokinetics
• Pharmacodynamics
Pharmacokinetics
• Onset
• Intensity
• Absorption
• Duration
• Distribution
• Metabolism
• Elimination
• Route
• Dose
• Frequency
• Duration
Pharmacodynamics
• Drug-receptor interaction
• Agonist
• Full agonist
Intrinsic efficacy
• Partial agonist
• Inverse agonist.. Constitutive activity
• Antagonist
• Competitive
• Non-competitive
Types of antagonism
• Pharmacologic antagonism- beta-blockers
• Chemical antagonism- antacids
• Functional (physiological) antagonism- adrenaline
Introduction to CNS pharmacology
The nervous system's main
function is to send messages
from various parts of the
body to the brain, and from
the brain back out to the
body to tell the body what to
do. These messages regulate:
Thoughts, memory, learning,
feelings and Movements
(balance and coordination).
What is a neuron?
• Neurons (nerve cells) are the fundemental units of the
brain and the nervous system.
• Neurons are the cells responsible for:
• Recieving sensory input
• Sending motor commands
• Transforming and relaying the electrical signals in between.
• Neurons are electrically excitable cells composed, in general, of one or more
dendrites, a single soma, a single axon and one or more axon terminals.
• Dendrites are designed to capture the neurotransmitters released by the
presynaptic neuron and have a high concentration of ligand-gated ion channels.
• The axon hillock is characterized by having a very high concentration of voltage-
activated sodium channels.
• Neurons are electrically excitable cells.
The neuron has a cell body (soma), axon and dendrites.
• Nonneuronal support cells:
• Astrocytes- regulation of neurotransmission.
• Microglia- involved in neurodegenerative diseases.
• Oligodendrocytes- form myelin sheath- damaged in multiple sclerosis.
Synapse
• The site of transmission of
electric nerve impulses between
two nerve cells (neurons) or
between a neuron and a gland or
muscle cell (effector)
• When an action potential arrives
at the end of the pre-synaptic
axon (top), it causes the release
of neurotransmitter molecules
that open ion channels in the
post-synaptic neuron (bottom).
Neurotransmitters
• Most drugs that affect the central nervous system (CNS) act by
altering some step in the neurotransmission process.
• What are neurotransmitters?
• Endogenous chemical substances that allow neurons to communicate
with each other throughout the body.
Criteria of a neurotransmitter
1. Neurotransmitters must be synthesized and released by neurons.
2. The substance should be released from the nerve terminal in a
chemically or pharmacologically identifiable form.
3. A neurotransmitter should bind to a post-synaptic receptor and
produce a specific effect.
4. The effetcs of a neurotransmitter should be blocked by competitive
antagonists for that transmitter.
5. There should be active mechanisms to terminate the action of that
transmitter.
Neuronal action potential
• Nearly all cell membranes in animals maintain a
voltage difference between the exterior and
interior of the cell, called the membrane
potential.
• A typical voltage across an animal cell membrane
is −70 mV. This means that the interior of the cell
is more negative relative to the exterior.
Excitatory vs. inhibitory postsynaptic potential
• An excitatory postsynaptic potentials (EPSP)
is a temporary depolarization of postsynaptic
membrane caused by the flow of positively
charged ions into the postsynaptic cell as a
result of opening of ligand-gated ion
channels.
• Depolarization results from the opening of
sodium channels and the influx of Na+ ions.
• An inhibitory postsynaptic
potentials (IPSP) is a temporary
hyperpolarization of postsynaptic
membrane caused by the flow of
negatively charged ions into the
postsynaptic cell.
• Hyperpolarization results from
either:
• The opening of potassium
channels and the efflux of K+
ions.
• The opening of chloride channels
and the influx of Cl- ions.
Neurotransmitters exert their actions by binding to two types of
receptors: ionotropic and metabotropic receptors
Sites of drug actions
Quiz
• Neurotransmitters:
1. are synthesized in the neurons.
2. are responsible for signal transmission in the nervous
system.
3. depolarize neurons by the opening of potassium channels
and efflux of potassium.
4. are inhibitory when hyperpolarization occurs
Neurotransmitter Glutamate GABA Acetylcholine Serotonin Dopamine Norepinephrine
Excitatory ✓
Inhibitory
NMDA
Ionotropic receptors AMPA
KA
Metabotropic receptors Glu1-Glu8
Role Memory
