Week 1:
Chapter 4-10
Differentiate pharmacodynamics (PD) from pharmacokinetics (PK).
● Pharmacodynamics
The study of the biochemical and physiologic effects of drugs on the body and the
molecular mechanisms by which those effects are produced. To participate rationally in
achieving the therapeutic objective, an understanding of pharmacodynamics is essential
● Pharmacokinetics
The study of drug movement throughout the body.
Four main principles: absorption, distribution, metabolism, excretion
Understand drug-receptor interactions on a molecular level.
Drugs produce their effects by interacting with other chemicals. Receptors are the
special chemical sites in the body that most drugs interact with to produce effects. We
can define a receptor as any functional macromolecule in a cell to which a drug binds to
produce its effects.
Explain the various types of agonists and antagonists.
● Agonists
Are molecules that activate receptors. Because neurotransmitters, hormones, and other
endogenous regulators activate the receptors to which they bind, all these compounds
are considered agonists. When drugs act as agonists, they simply bind to receptors and
mimic the actions of the body's own regulatory molecules. For example, dobutamine is a
drug that mimics the actions of NE at receptors on the heart, thereby causing heart rate
and force of contraction to increase.
● Antagonists
Antagonists produce their effects by preventing receptor activation by endogenous
regulatory molecules and drugs. Antagonists have virtually no effects of their own on
receptor function. In terms of a receptor but with no intrinsic activity. Affinity allows the
antagonist to bind the receipts, but lack of intrinsic activity prevents the bound
antagonist from causing receptor activation. Although antagonists do not cause receptor
activation they most certainly do prevent the activation of receptors by endogenous
regulatory molecules. The response to an antagonist is determined by how much agonist
is present.
List the four basic concepts of pharmacokinetics.
1. Absorption: into blood
2. Distribution: movement from blood to interstitial space of tissues
3. Metabolism:(biotransformation)
4. excretion
Understand the physicochemical properties for drug transfer.
● Placental drug trnsfer: the membranes of the placent separate the maternal
circulation from the fetal circulation. However, the membranes of the placenta do
not constitude an absolute barrier to the passage of drugs. Most drugs cross the
placenta via simple siffusion. Drugs can form reversible bonds with various
proteins in the body. Of all the proteins with which drugs can bind, pasma
albumin is the most important. Like other proteins, albumin is a large molecule.
Because of
,NURS 5663 Pharmacology Exam 1.
its size, albumin is too large to leve the bloodstream.
Understand the factors that modify drug absorption in relation to the method of drug
administration and the effect on bioavailability.
Understand the factors that modify drug distribution and its relationship to elimination.
“Movement of drugs from the systemic circulation to the site of drug action”
1. Blood flow to tissues
2. Ability of a drug to exit the vascular system
3. Ability of a drug to enter the cells
Explain the factors that affect metabolism, and differentiate between Phase I and Phase
II metabolism.
Drug metabolism, also known as biotransformation, is defined as the enzymatic
alteration of drug structure. Most drug metabolism takes place in the liver.
● Hepatic drug metabolising enzymes
Most drug metabolism that takes place in the liver is performed by the hepatic
microsomal enzyme system (P450 system) which is a group of 12 closely related enzyme
families.
● There are six possible consequences of therapeutic significance
1. Accelerated renal excretion of drugs
By converting lipid-soluble drugs into more hydrophilic forms, metabolic conversion can
accelerate renal excretion
2. Drug inactivation
Convert active to inactive
3. Increased therapeutic action
Metabolism can increase effectiveness of some drugs
4. Activation of prodrugs
A prodrug is a compound that are pharmacologically inactive as administered and then
undergoes conversion to ist active form through metabolism
5. Increased toxicity
6. Decreased toxicity
Understand the basic parameters of clearance pharmacokinetics.
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Explain how pharmacokinetics impacts therapeutic dosing.
Pharmacokinetic processes determine how much drug will be at its sites of action at any
given time. In most cases the time course of drug action bears a direct relationship to
the concentration of a drug in the blood. Monitoring plasma drug levels is important to
measure drug responses. Single dose time course shows how plasma drug levels
change over time after a single dose of an oral medication. Important To stay in
therapeutic range. Drug half life means the time required for the amount of drug in the
body to decrease by 50%.
Discuss the mechanisms of drug
toxicity. Idk too much
Week 2:
Chapter 11-17
Identify the two major divisions of the peripheral nervous system.
, NURS 5663 Pharmacology Exam 1.
● Somatic nervous system:
● Autonomic nervous system: regulation of heart, regulation of secretory
glands, regulation of smooth muscles
Differentiate between the sympathetic and parasympathetic branches of the autonomic
nervous system.
● Sympathetic
1. Regulation the cardiovascular system
2. regulating body temperature
3. implementing the acute stress response
● Parasympathetic
1. Slowing heart rate
2. Increased gastric secretion
3. Emptying of bladder
4. Emptying of bowel
5. Focusing the eye for near vision
6. Constricting the pupil
7. Contracting bronchial smooth muscle
Differentiate between the four main subtypes of adrenergic receptors: alpha1, alpha2,
beta1, and beta2.
● Alpha1
Located in eyes, blood essels, male sex organs, prostatic capsule, bladder
● Alpha2
Nerve terminals are referred to as presynaptic or prejunctional. Inhibition of transmitter
release.
● Beta1
Located in the heart, kidneys. Activation of these receptors increases heart rate, force of
contraction, and velocity of impulse conduction through the AV node.activation of B1 in
kidney causes release of renin into blood which promotes synthesis of angiotensin, a
vasoconstrictor.
● beta 2
Mediate several important processes. Activation of b2 receptors in the lung leads to
bronchial dilation. Activation of b2 receipts in the uterus causes relaxation of uterine
smooth muscle. In the heart, lungs, and skeletal muscles, it causes vasodilation. In the
liver and skeletal muscles it promotes glycogenolysis thereby increasing blood levels of
glucose.
Differentiate between the three main subtypes of cholinergic receptors: nicotinicN,
nicotinicM, and muscarinic.
● Muscarinic
In the sweat glands, blood vessels, all organs are regulated by the parasympathetic
nervous system. Decreases heart rate, increases gland secretion and smooth muscle
contraction. Agonist: bethanechol
● nicotinicN
All ganglia of the autonomic nervous system. Promotes ganglionic transmission.
Agonist: nicotine