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MindMap Gallery Pharmacology 9th Edition Chapter 3 Drug Effect Kinetics Mind Map

Pharmacology 9th Edition Chapter 3 Drug Effect Kinetics Mind Map

About Pharmacology 9th Edition Chapter 3: Drug Effect Kinetics Mind Map, including the basic functions of drugs, the relationship between drug dosage and effects, drugs and receptors, etc.

Edited at 2023-11-22 19:39:45

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Pharmacology 9th Edition Chapter 3 Drug Effect Kinetics Mind Map

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Outline

pharmacodynamics

Overview: Study the effects and mechanisms of drugs on the body

Section 1: Basic functions of drugs

1. Drug effects and pharmacological effects

The meanings of the two are close, and customs do not strictly distinguish them, but when they are shared, the order should be reflected.

First drug effect: the initial effect of the drug on the body. is the cause

Post-drug effect: the result of drug action, the manifestation of the body's reaction

Basic functions of drugs: excitement, inhibition

Main types of drug effects

Scope: local effect, systemic effect

Sequence: primary (direct) effect, secondary (indirect) effect

Selectivity

High selectivity - strong effect - narrow range - few side effects

Low selectivity - weak effect - wide range - many side effects

2. Treatment effect

1. Treatment of the cause: eliminate the primary causative factors and achieve complete cure.

2. Symptomatic treatment: improve symptoms

3. Adverse reactions

Meaning: Any reaction that has nothing to do with the purpose of medication and causes discomfort or pain to the patient is collectively called adverse drug reaction.

1. Side reactions

Meaning: Due to low selectivity, pharmacological effects involve multiple organs. When a certain effect is used for therapeutic purposes, other effects become side effects (also called side effects)

Conditions of occurrence: What occurs at therapeutic doses is an inherent effect of the drug itself, which may be mild and predictable.

2. Toxic reactions

Meaning: A harmful reaction (generally predictable) that occurs when the dose is too high or when the drug accumulates too much in the body

3. After Effects

Meaning: The remaining pharmacological effect when the blood drug concentration has dropped below the minimum effective concentration after stopping the drug

4. Drug withdrawal reaction

Meaning: Exacerbation of a pre-existing condition after sudden discontinuation of medication. (also called rebound reaction)

5. Allergy

A reaction (also known as allergic reaction) that occurs after non-peptide drugs serve as haptens and bind to body proteins as antigens, after a sensitization process of about 10 days of exposure.

Tips: The nature of the reaction has nothing to do with the original effect of the drug; the severity of the reaction has nothing to do with the dose.

6. Idiosyncratic reactions

7.Drug dependence

Meaning: After using a drug for a long time or repeatedly, you will feel pleasant and want to continue taking the drug.

Divided into: psychological dependence and physical dependence

expand

Most adverse reactions are inherent effects of the drug and are generally predictable

A few serious adverse reactions are difficult to recover from and are called drug-induced diseases.

Section 2: Relationship between drug dosage and effect

The pharmacological effect is proportional to the effect within a certain range, which is the dose-effect relationship (referred to as the dose-effect relationship). Use the effect intensity as the ordinate and the drug dose or drug concentration as the abscissa to get a dose-effect curve.

Extension: Change the drug concentration to log value as the abscissa, and the effect intensity as the ordinate, then it will be a typical symmetrical S-shaped curve.

specific point

Minimum effective dose: the minimum dose that can cause a pharmacological effect (threshold dose)

Maximum effective dose: The dose at which the greatest therapeutic effect occurs

Maximum effect (also called potency): the limit of pharmacological action

Minimum poisonous dose: the minimum dose at which poisoning occurs

Maximum dosage: The limit of therapeutic dosage specified in the pharmacopoeia

Potency intensity: the relative concentration or dose that can cause an equivalent response (usually 50% effect size)

therapeutic index

Meaning: the ratio of LD50/ED50 of the drug

LD50: The dose of drug that kills half of the experimental animals

Half effective dose (ED50): The dose of drug at which half of the experimental animals show a positive reaction

Clinical significance: The larger the value, the safer it is

Section 3: Drugs and Receptors

Overview: The mechanism of action of a drug is the study of how the drug binds to the cells of the body to exert its effect. Known drug action mechanisms involve receptors, enzymes, ion channels, nucleic acids, vectors, immune systems, genes, etc. Here we focus on the receptor mechanism.

1. Receptor

Meaning: biological macromolecules in cell membranes or cells that can bind to corresponding ligands, conduct signals, and cause biological effects.

Binding site (acceptor site): a site or active group on a receptor that can specifically bind to a ligand

characteristic

①Sensitivity

②Specificity

③Saturation

④Reversibility

⑤Diversity: The same receptor can be widely distributed in different cells and produce different effects

⑥Affinity

How drugs bind to specific receptors: ionic bonds, hydrogen bonds, van der Waals forces, covalent bonds

2. Interaction between receptors and drugs

(1) Classical receptor theory-occupation theory

Meaning: The binding of drugs to receptors requires not only affinity, but also intrinsic activity to stimulate the receptors and produce effects.

Intrinsic activity: the ability of a drug to produce an effect after binding to a receptor

(2) Receptor drug response kinetics

KD=[D][R]\[DR]

D: drug, R: receptor, DR: drug-receptor complex, RT: total number of receptors = R DR

When R=DR, that is, [DR]\[RT]=50%, KD=[D]

The meaning of KD: the dose of drug required to cause half of the maximum effect (that is, 50% of the receptors are occupied). Unit is mole

KD is inversely proportional to affinity

3. Classification of drugs that act on receptors

(1) Agonist drugs

Meaning: A drug that has both affinity and intrinsic activity, can bind to receptors and stimulate the receptors to produce effects

Category: Intrinsic activity size

Complete agonist: Stronger affinity and stronger intrinsic activity (a=100%)

Partial agonist: Strong affinity, weak intrinsic activity (0<a<100%)

Tip: Used together with a complete agonist, it can also antagonize some of the effects of the complete agonist.

(2) Antagonists

Meaning: Drugs that can bind to receptors and have strong affinity but no intrinsic activity (a=0)

Mechanism of action: It does not produce any effect itself, but antagonizes the effect of agonists or endogenous ligands by occupying receptors.

Classification: Is binding to the receptor reversible?

Competitive Antagonists: Reversible. By increasing the dose of the agonist to compete with the antagonist for the binding site, the dose-effect curve can be shifted to the right in parallel, but the maximum efficacy remains unchanged. Affinity decreases but intrinsic activity remains unchanged

The antagonism parameter (pA2) can be used to express the intensity of the competitive antagonist drug. pA2 is proportional to the antagonistic strength Meaning: When an agonist and an antagonist are used together, if the effect of twice the concentration of the agonist is exactly equal to the effect of the agonist without the addition of the antagonist, then the negative logarithm of the molar concentration of the added antagonist is pA2.

Noncompetitive Antagonists: Irreversible. The dose-effectiveness curve shifts parallel to the right, and the maximum efficacy decreases Decreased affinity and intrinsic activity

mechanism

Antagonists form strong bonds with receptors, such as covalent bonds, and the dissociation rate = 0, which is equivalent to inactivating part of the receptor.

Antagonists block a certain intermediate reaction link after receptor binding, and the binding of the receptor is not affected.

Extension: Reserve Receptor

Meaning: Emax is usually produced when all receptors are occupied. Highly active drugs activate part of the receptors to produce Emax. The remaining unactivated receptors are called reserve receptors.

Application: Antagonists must completely occupy the reserve receptor before they can exert their antagonistic effect.

Significance: Increase sensitivity to agonists

4. Receptor Type

(1) G protein-coupled receptor

(2) Ligand-gated ion channel receptors

N-type acetylcholine receptor

(3) Receptors with tyrosine kinase activity

(4) Intracellular receptors

5. Regulation of receptors

Receptor desensitization: After long-term use of an agonist, the sensitivity and responsiveness of tissues or cells to the agonist decreases.

Receptor sensitization: a phenomenon in which the level of receptor agonists decreases or the long-term use of antagonists causes the sensitivity and reactivity of tissues or cells to agonists to increase.