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Introduction to Pharmacology 2


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What is a drug?
Any Chemical that can affect living processes
What is Pharmacology?
Study of drugs and their interactions with living systems
What are the most important characteristics of an ideal drug?
Effective, Safe, and Selective
What is the therapeutic objective?
Provide maximum benefit with minimal harm
When a drug is effective it ___.
elicits the responses for which it is given
When a drug is safe it ___.
cannot produce harmful effects
When a drug is selective it ___.
elicits only the response for which it is given
Pharmacokinetics is __.
the study of how a drug moves through out the body
What is absorption?
Movement of a drug from it site of administration into the blood
What is distribution?
Drug movement from the blood to the interstitial space of tissues and into target cells
What is metabolism (Biotransformation)?
Mediated alteration of drug structure by enzymes
What is excretion?
Movement of drugs out of the body
What are 3 ways a drug can cross the cell membrane?
1) Passage through passive channel or pore
2) Passage actively through a transport system
3)Penetration of the membrane
What does P-glycoprotein do?
Transports a wide variety of drugs out of cells
A drug must be ____ to directly penetrate membranes.
What compounds are unable to cross the membranes?
Lipophobic (Hydrophilic) and Ions
What factors affect absorption?
Rate of Dissolution, Surface Area, Blood Flow, & Lipid Solubility
Parenteral is given by ___ and Enteral is given by ____.
injection (IV, IM, SubQ); GI (PO)
When you increase the amount of a drug ____ (less, more) is released from the plasma proteins.
What is the name of the hepatic drug-metabolizing enzymes?
P450 System; 12 Cytochromes (CYP)
What is the proper name for drug metabolism?
What is a prodrug?
Administered inactive and becomes active after conversion in the body
What is the first pass effect?
Rapid hepatic inactivation of oral drugs (carried to liver directly by the portal vein)
If someone has liver or renal failure, what would be compromised?
What is enterohepatic recirculation?
Drugs in the bile may undergo reabsorption into the blood
What is the MEC?
Minimum effective concentration, first theraputic effects felt at this dose
What is therapeutic range?
Above the MEC but below toxic concentration
What is the drug half-life?
Time required for the amount of drug in the body to reduce by half
What is the time period in which a drug will reach plateau?
Approximately four half-lives
What is the time period for most of the drug to be eliminated from the body?
Approximately four half-lives
What is Pharmacodynamics?
What drugs do to the body and how they do it
What is the maximal efficacy?
Largest effect a drug can produce (effect). Y-axis
What is the relative potency?
Amount of drug that must be given to elicit an effect. (amount) X-axis
What are the four receptor groups?
Cell membrane enzymes, Ion Channels, G-Protein Systems, & Transcription Factors
What is affinity?
Reflected in potency; Strength of the bond between the receptor and the ligand
What is intrinsic activity?
Reflected in maximal efficacy; Ability to activate a receptor upon binding
Agonist are ___ and have both ____ and ____.
Molecules that activate receptors; affinity; high intrinsic activity
Antagonist are ____ and have ___ but no ____.
Molecules that prevent activation of receptors by agonists; affinity; intrinsic activity
When continually exposed to a agonist a cell will ___ regulate.
Continuous exposure to a antagonist will cause the cell to ____ regulate or become ____.
up; hypersensitive
What is the ED50?
Dose at the middle of the distribution curve (average effective dose)
What is the therapeutic index and what does it indicate?
Ratio of the LD50 to ED50; High therapeutic index means a drug is safe
What are direct chemical or physical interactions?
Drugs combined before administered interact
What are inducing agents?
stimulate the synthesis of CYP and increase drug metabolism
What is an ADR?
Adverse Drug Reaction; unintended and undesired effect that occurs at normal doses
Who experiences the most ADRs?
Elderly and the very young
What is a side effect?
Nearly unavoidable secondary effect produced at normal doses
What is toxicity?
An ADR caused by excessive dosing
What is the Idiosyncratic effect?
Uncommon drug effect caused by genetic predisposition
What is an iatrogenic disease?
Disease caused by drugs
Dose are adapted for the size of the patient based on the ___ .
Body Surface Area
What is tolerance?
Decreased responsiveness to a drug as a result of repeated drug administration
Exposure during the the fetal will cause ___ while exposure during the embryonic period causes ____.
function abnormalities; gross anatomy abnormalities
Explain the FDA Pregnancy Categories.
Five Categories A, B, C, D, and X
The category A is the least dangerous and X is proven risk of fetal harm
Drug sensitivity in the very young is a result of ___ while sensitivities in the elderly are a result of ____.
Organ system immaturity; Organ system degeneration
Name some differences in the very young that change pharmacokinetics in the young
Low gastric acidity
Low Amount of Plasma Proteins
Low Hepatic Metabolism
Development of BBB not complete
By the age of ___ the child has similar pharmacokinetics as an adult.
1 year
Dosage is based on ____ for patients of different sizes.
Surface Area
Name some differences in the very old that change the pharmacokinetics of the elderly.
Increased body fat
Decreased Water and Plasma Proteins
Low Drug metabolism
Nonadherence common
Drugs that affect the axonal conduction are ___ (common, rare) and are ____.
Rare, local anesthetics
Name the steps in synaptic transmission.
Transmitter Synthesis
Transmitter Storage
Transmitter Release
Receptor Binding
Termination of Transmission
Explain the divisions of the Nervous System.
Central- Brain and Spinal Cord
Peripheral- Somatic and Automatic
Automatic- Sympathetic and Parasympathetic
The Parasympathetic System:
___ heart rate
___ gastric secretion
___ of the bowel and bladder
___ the pupil
___ bronchial smooth muscle
Name the functions of the sympathetic system.
Regulating Cardiovascular System
Temperature Regulation
Fight or Flight Reaction
The sympathetic system:
___ heart rate and BP
___ of the skin
___ of the bronchi
___ the pupils
___ stored energy
What is the baroreceptor reflex?
A Feedback loop that regulates BP
What is an automatic tone?
The main or predominant state that an organ is receiving input
Where is acetylcholine found?
In all preganglionic neurons
The postganglionic neurons of the parasympathetic system
All motor neurons of the skeletal system
Postganglionic neurons of the sympathetic system that go to sweat glands
Where is norepinephrine found?
All postganglionic neurons of the sympathetic system (except sweat glands)
Where is epinephrine found?
Transmitter that is released fro m the adrenal medulla; Acts similar to a hormone
What neurotransmitters do adrenergic receptors mediate?
Epinephrine and Norepinephrine
What neurotransmitters do cholinergic receptors mediate?
What are the subgroups of the Cholinergic Receptors?
Nicotine N, Nicotine M, and Muscarinic
What are the subgroups of the Adrenergic Receptors?
Alpha 1, Alpha 2, Beta 1, Beta 2, and Beta 3
Where are Nicotine N receptors located?
All preganglionic synapses in the automatic nervous system
Where are Nicotine M receptors located?
Neuromuscular Junctions
Where are Muscarinic receptors located?
All parasympathetic target organs:
Eye, Lung, Heart, Bladder, GI tract, sweat glands, sex organs, and blood vessels
What are the responses to muscarinic stimulation?
___ of the pupil
___ heart rate
___ of bronchi
___ of bowel and bladder
___ of the penis
___ of blood vessels
Where are Alpha 1 receptors located?
Blood vessels
Sex organs
Where are the Alpha 2 receptors located?
Presynaptic nerve terminals
Where are Beta 1 receptors located?
Where are Beta 2 receptors located?
Where are Dopamine receptors located?
Where are Beta 3 receptors located?
Adipose tissue

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