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Pharmacology
In the world of drug action, pharmacodynamics and dosage-effect relationships reveal complex interactions between drugs and receptors. When the LD and ED curves are not parallel or parallel, the safety and effectiveness of the drug show different patterns. Drug classification is based on its affinity and intrinsic activity, from complete agonists to antagonists, each drug has its own unique effects and effects. SAR and chemical structure determine the specificity of the drug, while physiological regulation of the receptor further affects the effect of the drug. Whether it is a gene-transduced receptor or a G-protein coupled receptor, the pharmacological effects of drugs increase with the increase of dose or concentration, forming a dosage-efficiency relationship. Understanding these mechanisms will help us better understand the therapeutic effects and adverse reactions of drugs and provide a scientific basis for precise medication use.
Edited at 2025-03-10 15:23:36- Rumi 10 spiritual high-dimensional awakenings
Rumi: 10 dimensions of spiritual awakening. When you stop looking for yourself, you will find the entire universe because what you are looking for is also looking for you. Anything you do persevere every day can open a door to the depths of your spirit. In silence, I slipped into the secret realm, and I enjoyed everything to observe the magic around me, and didn't make any noise. Why do you like to crawl when you are born with wings? The soul has its own ears and can hear things that the mind cannot understand. Seek inward for the answer to everything, everything in the universe is in you. Lovers do not end up meeting somewhere, and there is no parting in this world. A wound is where light enters your heart.
- Pathophysiology - Heart failure
Chronic heart failure is not just a problem of the speed of heart rate! It is caused by the decrease in myocardial contraction and diastolic function, which leads to insufficient cardiac output, which in turn causes congestion in the pulmonary circulation and congestion in the systemic circulation. From causes, inducement to compensation mechanisms, the pathophysiological processes of heart failure are complex and diverse. By controlling edema, reducing the heart's front and afterload, improving cardiac comfort function, and preventing and treating basic causes, we can effectively respond to this challenge. Only by understanding the mechanisms and clinical manifestations of heart failure and mastering prevention and treatment strategies can we better protect heart health.
- Pathophysiology - ischemia - reperfusion injury
Ischemia-reperfusion injury is a phenomenon that cellular function and metabolic disorders and structural damage will worsen after organs or tissues restore blood supply. Its main mechanisms include increased free radical generation, calcium overload, and the role of microvascular and leukocytes. The heart and brain are common damaged organs, manifested as changes in myocardial metabolism and ultrastructural changes, decreased cardiac function, etc. Prevention and control measures include removing free radicals, reducing calcium overload, improving metabolism and controlling reperfusion conditions, such as low sodium, low temperature, low pressure, etc. Understanding these mechanisms can help develop effective treatment options and alleviate ischemic injury.
Pharmacology
- Rumi 10 spiritual high-dimensional awakenings
Rumi: 10 dimensions of spiritual awakening. When you stop looking for yourself, you will find the entire universe because what you are looking for is also looking for you. Anything you do persevere every day can open a door to the depths of your spirit. In silence, I slipped into the secret realm, and I enjoyed everything to observe the magic around me, and didn't make any noise. Why do you like to crawl when you are born with wings? The soul has its own ears and can hear things that the mind cannot understand. Seek inward for the answer to everything, everything in the universe is in you. Lovers do not end up meeting somewhere, and there is no parting in this world. A wound is where light enters your heart.
- Pathophysiology - Heart failure
Chronic heart failure is not just a problem of the speed of heart rate! It is caused by the decrease in myocardial contraction and diastolic function, which leads to insufficient cardiac output, which in turn causes congestion in the pulmonary circulation and congestion in the systemic circulation. From causes, inducement to compensation mechanisms, the pathophysiological processes of heart failure are complex and diverse. By controlling edema, reducing the heart's front and afterload, improving cardiac comfort function, and preventing and treating basic causes, we can effectively respond to this challenge. Only by understanding the mechanisms and clinical manifestations of heart failure and mastering prevention and treatment strategies can we better protect heart health.
- Pathophysiology - ischemia - reperfusion injury
Ischemia-reperfusion injury is a phenomenon that cellular function and metabolic disorders and structural damage will worsen after organs or tissues restore blood supply. Its main mechanisms include increased free radical generation, calcium overload, and the role of microvascular and leukocytes. The heart and brain are common damaged organs, manifested as changes in myocardial metabolism and ultrastructural changes, decreased cardiac function, etc. Prevention and control measures include removing free radicals, reducing calcium overload, improving metabolism and controlling reperfusion conditions, such as low sodium, low temperature, low pressure, etc. Understanding these mechanisms can help develop effective treatment options and alleviate ischemic injury.
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Chapter 3. Pharmacology
Effects and effects of drugs
concept
Action
Refers to the initial effect between the drug and the body's tissues
Effect
Changes in the body's function or morphology caused by drug action
Drug efficacy analysis
Basic manifestations of drug effects
excited
Enhancement of original functions of the body
e.g. Adrenaline raises blood pressure, and caffeine increases nerve excitation
inhibition
The weakening of the original function of the body
e.g. Insulin lowers blood sugar, hypnotics reduce nerve excitation
Direct and indirect
Selective
Concept: Drugs only affect certain organs or systems, and only affect a few or a certain function.
Reason: Depending on the structure of the drug, the binding site and special receiving points of the target organ make it have a strong affinity and high reactivity.
Quantity-Effective Relationship
The pharmacological effect of a drug increases with the increase of dose or concentration. The regular changes between the two are called the dosage and effect relationship.
Two types of reactions
Quantitative reaction
concept
Effect intensity of response on individuals
Effects can be expressed in grading quantities
e.g.Blood pressure, urine volume, heart rate, etc.
Effectiveness curve
The drug dose/concentration is used as the horizontal coordinate, and the effect is the vertical coordinate
Illustrations
Threshold dose TD/minimum effective dose
Minimum dose that causes pharmacological effects
Performance - Maximum Effect Emax
After achieving efficacy, the dose will not increase.
If the dose is increased, it will cause toxicity (qualitative change)
Slope
The linear part between Emax and TD, most individuals have an effect within this dose range
Individual Differences
Same dose
Same effect
Validity
Refers to the relative concentration or dose that can cause an equivalent reaction
The smaller the value, the greater the titer strength
Quality reaction
concept
The degree of occurrence of a certain effect in the group
Expressed as the frequency of positive or negative reactions or %
e.g. Convulsions, death, etc.
Effectiveness curve
Taking the dose as the horizontal coordinate, the frequency of a reaction that appears in a small sample population is the vertical coordinate
Conform to normal distribution
Basic concepts
Medicinal efficacy - half effective amount ED₅₀
Dosages that can cause half of the individuals in the population to have a certain effect
e.g. Half lethality LD₅₀
Dosages that cause death in half of the individuals in the population
The smaller the value, the stronger the toxicity
Safety scope
The distance between LD₅₀ and ED₅₀
The greater the value, the safer the medicine
Treatment index TI
LD₅₀/ED₅₀
When the LD and ED curves are parallel
Reliable and Safety Index
LD1/ED99
Safety Index
LD5/ED95
When the LD and ED curves are not parallel
Structural-effect relationship SAR
Chemical structure determines the effect of drugs, and chemical structure is the material basis for drug specificity
Medicinal Chemical Structure
Classification
Like medicine
Similar chemical structure and similar efficacy
Antagonist
Similar chemical structures but opposite efficacy
Optical isomers
Left-rotor
Most have pharmacological effects
Right-handed body
No pharmacological effects generally
The nature of the action of the same class of drugs depends on its basic skeleton structure
Drug effects
mechanism
Change physical and chemical properties around cells
Supplement various substances lacking in the body
Effects on neurotransmitters, mediators or hormones
Act on a certain target
Drug-receptor interaction
Ion channels affect
Interaction with enzymes
Affecting the carrier molecule
Gene therapy
Drug selectively affects gene expression
The interaction between receptors and drugs
Occupy Theory
Concept: Receptors can only be activated and have an effect if they bind to drugs, and the intensity of the effect is proportional to the number of occupied receptors, and the maximum effect occurs when all receptors are occupied.
Affinity
The ability of drugs to bind to receptors
Intrinsic activity α
Drug action depends on affinity and intrinsic activity
Drug classification
Completely thrilling drugs
Drugs that have both affinity and intrinsic activity (can bind to receptors, and can also activate receptors to produce effects)
α=1
Antagonist/blocking drugs
Medicines with strong affinity but no internal activity
α=0
type
Competitive antagonist
Fight for the same receptor with agonist
Effects can be cancelled by increasing the dose of agonist
Increase the dosage of blocking drugs so that the dosage curve is parallel to the right
The maximum effect remains unchanged (performance remains unchanged)
Noncompetitive antagonist
It also shows that the measurement and effect curve is shifted right, but not parallel
The dosage effect curve is to inhibit the maximum effect, the dosage effect curve moves downward, and increasing the agonist cannot cancel the antagonist effect
antagonistic index pA2
Indicates the strength of competitive antagonists
A2
When increasing the concentration of agonist 2 times, the effect must be the same as the original concentration of agonist. At this time, the concentration of the antagonist required
The greater the value → the greater the concentration of the antagonist required → the weaker the antagonism effect
pA2=-logA2
The greater the value, the stronger the antagonism ability
Partial agonist/antagonist
Have strong affinity but not strong intrinsic activity
0＜α＜1
A blocking drug is present when encountering complete agonist; an agitator is present when encountering blockist
Kd
Sub-theme
Concept: The dissociation constant of the drug-receptor complex is the concentration of the drug when it causes half the maximum effect
Record the drug concentration when 50% of the receptor is occupied
The greater the Kd, the more drug concentrations are needed to cause the maximum effect, indicating the smaller the affinity.
Affinity index pD2
pD2=-log Kd
The maximum effect when the affinity is equal depends on the intrinsic activity α; the titer value when the intrinsic activity α is equal depends on the affinity.
Rate theory
Dipeptide model theory
Cellular response after drug-receptor interaction
Ion channel coupled receptor
G protein coupled receptor
Influence the Second Messenger
Kinase-coupled receptor
Gene transduction receptors
Located in the cell
The relationship between receptor physiological regulation and drug action
The number or reactivity of receptors on the cell membrane may be affected by the effect or concentration of biologically active substances or drugs (agonists or antagonists) around them.
Regulation of receptors
include
Desensitization
Increase sensitization
If sensitization/desensitization manifests in the change in receptor density is called up/downregulation
The above substances have too high concentrations, are too strong to act or have long-term agonism receptors, and the number of receptors can be reduced, which is called attenuation/downward regulation.
Conversely, long-term use of inhibitors can increase the number of receptors, called upproliferative/upward regulation
Results of drug action
Treatment effects
Treatment for causes
Antibiotics are used for bacterial infection
Symptom-based treatment
Such as aspirin for fever
Supplemental therapy/replacement therapy
What to make up for if you lack
Adverse reactions
side effect
Concept: The drug has an effect that is not related to the purpose of the treatment during the treatment dose, which may cause discomfort or pain to the patient. It is generally mild and is mostly a functional change that can be recovered.
Cause: The drug is low in selectivity and has a large range of effects. One of them is a therapeutic effect, the other is called a side effect
The therapeutic effects and side effects can be converted to each other due to different therapeutic purposes.
e.g.Atropine can inhibit gland secretion → relieve smooth muscle spasms, dry mouth and tongue
Toxic reaction
Caused by excessive dosage or excessive medication time
Legacy effects
Concept: After the drug is stopped, although the concentration of drug in plasma has dropped below the threshold concentration, there are still biological effects.
e.g. "Hangover" after taking barbital
e.g. After long-term use of adrenocorticosteroids, the initial stage of the adrenocortical function is low (not recovered yet)
Secondary reaction
A secondary reaction after drug treatment
e.g.Dual infection caused by long-term use of broad-spectrum antibiotics,
allergy
It is an immune pathological reaction that occurs after the body receives drugs, also known as an allergic reaction
e.g. Penicillin and streptomycin allergies
Special reaction
A few patients with specialized patients are particularly sensitive to certain drugs, and their reaction properties may be different from those of normal people.
Targeting a few