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Pharmacology-Pharmacodynamics Mind Map
This is a mind map about pharmacology-pharmacodynamics, including the basic functions of drugs, receptor theory, overview of pharmacodynamics, etc. Final review, welcome to refer to it!
Edited at 2023-12-16 15:41:15- One Hundred Years of Solitude Character Relationship Chart
One Hundred Years of Solitude is the masterpiece of Gabriel Garcia Marquez. Reading this book begins with making sense of the characters' relationships, which are centered on the Buendía family and tells the story of the family's prosperity and decline, internal relationships and political struggles, self-mixing and rebirth over the course of a hundred years.
- One Hundred Years of Solitude Character Relationship Chart
One Hundred Years of Solitude is the masterpiece of Gabriel Garcia Marquez. Reading this book begins with making sense of the characters' relationships, which are centered on the Buendía family and tells the story of the family's prosperity and decline, internal relationships and political struggles, self-mixing and rebirth over the course of a hundred years.
- Project Management Process Template
Project management is the process of applying specialized knowledge, skills, tools, and methods to project activities so that the project can achieve or exceed the set needs and expectations within the constraints of limited resources. This diagram provides a comprehensive overview of the 8 components of the project management process and can be used as a generic template for direct application.
Pharmacology-Pharmacodynamics Mind Map
- One Hundred Years of Solitude Character Relationship Chart
One Hundred Years of Solitude is the masterpiece of Gabriel Garcia Marquez. Reading this book begins with making sense of the characters' relationships, which are centered on the Buendía family and tells the story of the family's prosperity and decline, internal relationships and political struggles, self-mixing and rebirth over the course of a hundred years.
- One Hundred Years of Solitude Character Relationship Chart
One Hundred Years of Solitude is the masterpiece of Gabriel Garcia Marquez. Reading this book begins with making sense of the characters' relationships, which are centered on the Buendía family and tells the story of the family's prosperity and decline, internal relationships and political struggles, self-mixing and rebirth over the course of a hundred years.
- Project Management Process Template
Project management is the process of applying specialized knowledge, skills, tools, and methods to project activities so that the project can achieve or exceed the set needs and expectations within the constraints of limited resources. This diagram provides a comprehensive overview of the 8 components of the project management process and can be used as a generic template for direct application.
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- Outline
pharmacodynamics
Basic effects of drugs
The dual nature of drug action
Therapeutic effect
concept
Any effect that can achieve a preventive effect becomes a therapeutic effect
Classification
Treatment for the cause (standard)
Symptomatic treatment (this book)
Adverse reactions
concept
Does not meet the purpose of medication and has adverse effects on patients
Classification
Side effects (side effects)
A reaction inherent to the drug itself that occurs at therapeutic doses and is unrelated to the therapeutic purpose
Features
Therapeutic effects and side effects are relative
Depends on the selectivity of the drug. Drugs with low selectivity have many side effects.
toxic reactions
concept
Collective damaging reactions caused by excessive drug dosage or prolonged use
Features
acute toxicity
Immediately after taking the medicine, circulation and respiratory nerves (related to life)
Chronic
Occurs after long-term medication, damaging metabolically active systems (liver, kidney, bone marrow)
special
carcinogenic, teratogenic, mutagenic
carryover effect
concept
After stopping the drug, the blood drug concentration drops below the threshold concentration, and the remaining effect
Example
Hangover caused by sedative-hypnotics
allergy
concept
(Allergy) An immune reaction occurs in a small number of patients with abnormal immune response after being stimulated by certain drugs.
Features
Allergy
Fewer symptoms after first use of medication
Allergy lasts forever
cross-reactivity
Differences from toxic reactions
It has nothing to do with dosage or treatment duration, has nothing to do with pharmacological effects, and is unpredictable.
idiosyncratic reaction
concept
Reactions due to congenital genetic abnormalities, favismosis
secondary effects
concept
Adverse consequences caused by the therapeutic effects of drugs
example
Superinfections caused by broad-spectrum antibiotics
Withdrawal reaction (rebound)
concept
The original disease reappears or even worsens after long-term medication is suddenly stopped.
example
Glucocorticoids
Propranolol (beta blocker) (receptor upregulation)
clonidine
dependency
Psychological (spiritual)
Drug-seeking behavior (drugs)
physiological
withdrawal syndrome
receptor theory
concept
receptor (lock)
Membrane, nuclear and cytoplasmic macromolecular compounds
Binding to specific ligands produces effects
Ligand (Key)
A general term for substances that can bind to receptors
Receptive point (keyhole)
Reactive groups capable of binding to ligands
Receptor properties
saturation
Maximum drug effect (potency)
specificity
Specific receptor specific ligand specific effect
Reversibility
Ligand dissociable
High affinity (sensitive)
Use less, but more effective
structural specificity → specificity
Stereoselectivity (chirality)
Regional distribution (certain receptors only in specific tissues) drug selectivity
subcellular or molecular properties
Different subtypes of the same receptor
Ligand binding strength is positively correlated with pharmacological activity
endogenous ligand
type
Receptors are located in different locations
cell membrane receptor
choline
Adrenaline
dopamine
cytoplasm
Adrenocorticotropic hormone
sex hormones
nucleus
thyroid hormone
Receptor protein structures and signal transduction mechanisms are different
ion channel-containing receptors
GABA
G protein coupling
M
adrenergic receptors
dopamine receptor
tyrosine kinase receptor
insulin
growth hormone
receptors that regulate gene expression
steroid hormones
thyroid hormone
receptor modulation
concept
Changes in receptor number and affinity are called receptor modulation
Classification
Down regulation (receptor desensitization)
Long-term use of agonists reduces the number of receptors
Tolerance
Isoproterenol is less effective in treating asthma
Up regulation (receptor sensitization)
Long-term use of antagonists increases the number of receptors
rebound
Propranolol, sudden discontinuation, manifested by increased sensitivity
Receptor signal transduction
first messenger
Can't enter cells
Binds to specific receptors on the surface of the target cell membrane and activates the receptors
second messenger
cAMP was first discovered
Cyclic adenosine monophosphate, cyclic guanosine monophosphate, diacylglycerol, inositol triphosphate, calcium nitric oxide, prostaglandins
third messenger
Inside and outside the nucleus
growth factors
conversion factor
Pharmacodynamic overview
drugs that act on receptors
Kinetics of drug-receptor interactions
Drugs bind to receptors
Affinity
Drug-receptor binding ability; prerequisite
Demonstrated efficacy
intrinsic activity
The ability of a drug to agonize receptors to produce maximum effect, potency
α
1
intrinsically active
0
none
Occupy the latrine and don't poop, blocker
Between 01
There are parts
Drug Classification
agonist
full agonist
Has affinity and intrinsic activity α=1
partial agonist
Affinity, but not strong intrinsic activity 0<α<1
Binding to the same receptor site, competition exists
Antagonist
competitive antagonist
Affinity, no intrinsic activity α=0
Binds to the same receptor site, competition exists (same as above)
noncompetitive antagonist
It does not compete with the agonist for the corresponding site, but it affects the agonist and the receptor after binding to the receptor.
Act on other sites on the receptor
Comparison of the action characteristics of competitive antagonists and non-competitive antagonists
main
Agonist Competitive Antagonist
Affects affinity but does not affect intrinsic activity
Agonist Noncompetitive Antagonist
Affects both affinity and intrinsic activity
Section comparison
Mechanism
competitive antagonist
Compete with the agonist for the same binding site and block the agonist from binding to the receptor.
noncompetitive antagonist
Binds to groups outside the site, affecting the binding of agonists to receptors
medicine interactions
compete
By adding an agonist to compete for the same site, the agonist can be blocked from binding to the receptor.
No
None of the above
Effects on agonists
compete
Affects agonist affinity but not intrinsic activity
No
Both are affected (both decrease)
Effect on agonist dose-response curve
compete
Decreased potency
Performance remains unchanged
Curve moves parallel to the right
Summarize
使激动剂亲和力下降，效价值加大，效价强度减小
不影响内在活性，不影响效能
药时曲线平行右移
No
Decreased potency Potency: Affinity index: The greater the potency value, the lower the potency and the lower the potency affinity.
Reduced performance Potency: intrinsic activity indicator
The curve is not parallel and moves to the right
Summarize
既影响亲和力，使效价值加大，效价强度减小
也影响内在活性，使效能减小
药时曲线右移但不平行
drug mechanism of action
non-specific drug effects
concept
Mainly related to the physical and chemical properties of the drug, it works by changing the physical and chemical conditions around the cells.
example
change osmotic pressure
Mannitol dehydration
magnesium sulfate
change pH
Antacids Treat Ulcers
complexation
Sodium dimercaptosuccinate relieves heavy metal poisoning
specific drug effects
concept
Structural-specific drugs work by binding to functional groups of biological macromolecules (such as enzymes and receptors). Most drugs fall into this category.
Structure-activity relationship and dose-effect relationship of drugs
QSAR
The relationship between drug structure and pharmacological activity
clinical development drugs
Dose-effect relationship
Concept: Within a certain range, when the dose (or concentration) of a drug increases or decreases, the effect of the drug increases or decreases accordingly. The relationship between the dose or concentration of the drug and the effect is called the dose-effect relationship. Relationship between drug dosage and pharmacological activity
Dose-response curve (concentration-response curve)
abscissa
Drug dosage: blood concentration
constant
logarithm
Y-axis
drug effects
quantitative response
test subject
individual
drug effects
Continuous change, gradation of quantity, or percentage of maximum response
Example
Increase or decrease in heart rate
rise and fall in blood pressure
amount of urine
Dose-response dose-effect curves and related parameters
picture
Performance: than the maximum value BCA on the ordinate
Potency Strength ABC
parameter
Maximum effect (potency)
definition
Continuing to increase the dose of the drug will no longer enhance its effect, which is the limit of pharmacological effect.
significance
Reflects the intrinsic activity of the drug, which is the ability of the drug to produce effects
Potency strength (potency)
definition
Refers to the relative dose or concentration that can cause an equivalent response. The smaller the value, the greater the potency.
significance
drug affinity
Half effective concentration (EC50)
definition
The drug dose or concentration at which 50% of the maximum effect is achieved
significance
When the drug concentration changes around EC50, the drug efficacy changes most sensitively.
slope
definition
In the area of approximately 16% to 84% of the effect, the dose-response curve is almost a straight line, and the tangent value of the angle between it and the abscissa is called the slope of the dose-response curve.
significance
For drugs with a large slope, small changes in dosage can cause significant changes in the effect. The size of the slope reflects the safe dosage range of clinical medication to a certain extent.
threshold dose
minimum effective dose
The minimum dose or concentration of a drug that causes an effect
Commonly used amount
Treatment amount
Greater than threshold dose, less than maximum dose
extreme amount
maximum effective dose
The maximum dosage of certain drugs specified in the National Pharmacopoeia
minimum poisoning dose
Minimum dose for toxic reactions
minimum lethal dose
Minimum dose at which death occurs
qualitative reaction
test subject
group
drug effects
The frequency or percentage of positive (or negative) reactions
Example
death and survival
Convulsions and no convulsions
Coma and wakefulness
Dose-response curves and related parameters of mass response
Half effective dose ED50
The dose that causes half of the individuals in the population to experience a certain effect
LD50
The dose that kills half of the individuals in the population
therapeutic index
TI=LD50/ED50
Safety rate
LD5/ED95
safety range
The distance between the minimum effective dose and the minimum toxic dose
Reflect drug safety, the bigger the better
Factors affecting drug efficacy
Organism (human cause)
age, gender
Pathological factors
Liver and renal insufficiency
Tolbutamide and chloramphenicol are metabolized by the liver, and the biotransformation rate of the liver is slowed down, the effect is strengthened, and the duration is prolonged.
Cortisone and prednisone are prodrugs that need to be processed by the liver, and their effects are weakened in patients with liver insufficiency; the use of drugs that are not converted by the liver is not affected (hydrocortisone)
Renal insufficiency, renal elimination and excretion of drugs are slowed down, leading to drug accumulation and poisoning (aminoglycosides, first-generation cephalosporins)
Malnutrition
Too little plasma protein, more free drugs, and easy poisoning
Hepatic drug enzyme activity decreases and drug metabolism slows down
Less fat tissue affects drug storage
Individual differences and genetic factors
species differences, racial differences
Drug effects
Dosage form
Absorption rate for oral administration: aqueous solution > powder > tablet
Sustained release agent: the drug is released slowly at a first-level rate, the absorption time is long, and the maintenance time of the drug effect is also extended.
Controlled-release preparations: blood drug concentration is stabilized at the effective concentration level and produces lasting drug effects.
dose
The higher the dose, the stronger the effect.
produce different effects
Diazepam: low-dose sedative, medium-dose hypnotic, high-dose anticonvulsant
affect selectivity
dopamine
Small and medium doses can dilate renal blood vessels and prevent renal failure; large doses can shrink renal blood vessels and cause renal failure.
Route of administration
Affects the time when the drug effect appears: the speed of onset of effect
Intravenous injection > Inhalation > Intramuscular injection > Subcutaneous injection > Oral administration > Dermal administration
Influence properties
Magnesium sulfate
oral
Causing catharsis
injection
Anticonvulsant vasodilator/pregnancy-induced hypertension
External application
Reduce inflammation and swelling
Dosing time
If administered before meals, it is well absorbed and takes effect quickly.
Stimulant drugs should be taken after meals
Hypnotic drugs should be taken before going to bed, and insulin should be injected before meals
Medication according to biological rhythm
Take once a day in the morning to reduce the side effects of adenohypophysis suppression
repeated administration
Tolerance
The body's response to drugs decreases after continuous use
tachyphylaxis
Nitroglycerin
heparin
critical emergency
slow tolerance
drug resistance
The tolerance developed by pathogens and tumor cells after long-term drug use is called drug resistance
dependency
rebound
drug interactions
Incompatibility
concept
Drugs mixed together undergo physical and chemical reactions
Example
Beta lactams and aminoglycosides cannot be used together
Penicillin is susceptible to allergies and unstable in glucose solution
Ceftriaxone is incompatible with calcium-containing injections (Ringer's, compound)
Erythromycin cannot be dissolved in saline
pharmacokinetic interactions
Antacids affect the absorption of weakly acidic drugs in the stomach Acid and alkali promote absorption, acid and alkali promote excretion
Combined with drugs with high plasma protein binding rate, the effect will be enhanced and the toxicity will be increased Aspirin has a high plasma protein binding rate and can be used in combination with the following, which can be easily dissociated, overdosed, and poisoned Glitaxel → hypoglycemia; warfarin → hypocoagulation
Free type
exert pharmacological effects
transmembrane transport
Metabolism and excretion
combined type
No activity
temporary repository
pharmacodynamic interactions
Collaboration
Add
The combined use is the sum of the single uses
Enhance
Used together is better than used alone
Sensitizing
One drug makes tissues or receptors more sensitive to another drug
antagonistic
Subtract
The combined use is less than the sum of the individual uses
offset
The combined effect is 0
physiological antagonism
Atropine rescues organophosphorus poisoning (agonist and antagonist receptors)
chemical antagonism
Protamine rescues heparin overdose (one drug acts on another)