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.
- Lipophilic
- 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.
- more
- What is the name of the hepatic drug-metabolizing enzymes?
- P450 System; 12 Cytochromes (CYP)
- What is the proper name for drug metabolism?
- Biotransformation
- 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?
- Biotransformation
- 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.
- down
- 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 -
Slowing
Increasing
Emptying
Constricting
Contraction - 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 -
Increase
Constriction
Dilation
Dilation
Mobilization - 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?
- Acetylcholine
- 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 -
Constriction
Decreased
Constriction
Emptying
Erection
Dilation - Where are Alpha 1 receptors located?
-
Eye
Blood vessels
Sex organs
Bladder - Where are the Alpha 2 receptors located?
- Presynaptic nerve terminals
- Where are Beta 1 receptors located?
-
Heart
Kidneys - Where are Beta 2 receptors located?
-
Lung
Uterus
Liver - Where are Dopamine receptors located?
- Kidney
- Where are Beta 3 receptors located?
- Adipose tissue