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MindMap Gallery pharmacodynamics
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pharmacodynamics
This is a mind map about pharmacodynamics. Pharmacodynamics is a discipline that studies the effects of drugs on the body and their laws, and elucidates the mechanisms by which drugs prevent and treat diseases.
Edited at 2024-03-02 22:21:45
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pharmacodynamics
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- Outline
pharmacodynamics
pharmacodynamics
Basic rules of drug action
The relationship between drug action and pharmacological effects
Drug effects: contact between drug and body
Changes in the contact between drugs and the body
Basic functions of drugs
hormesis
inhibitory effect
Type of medicine
Direct action: Direct contact with organs
Direct action: reflected through reflection and regulation
Regional action: Before the drug is absorbed into the blood, it is not absorbed into the blood (anesthetic)
Absorption: After the drug is absorbed from the site of administration into the bloodstream (systemic effect)
Selectivity of drug action (your preference and my preference)
Drugs with high selectivity have fewer adverse reactions and have a narrow range of applications. Drugs with low selectivity have many adverse reactions and have a wide range of applications.
The dual nature of drug action
Prevention and treatment effect (medication brings good effects)
Preventive and therapeutic effects (treating causes and symptoms)
Adverse reactions (bring about bad)
Side effects (side effects)
Reason: The drug has low selectivity and a wide range of effects
Features: ① The effect of the drug itself (therapeutic effect and side effects); ② The general reaction is mild and predictable ③ Side effects and therapeutic effects can be converted into each other (example of atropine)
toxic reactions
Acute toxicity: Toxic reactions that occur rapidly due to excessive dosage More damage to the respiratory, circulation, and central nervous system.
Chronic toxicity: Toxic reactions that gradually occur due to long-term drug accumulation in the body More damage to liver, kidney, bone marrow and endocrine (Teratogenic, carcinogenic, mutagenic)
allergy
Features (test)
A few patients with allergies
The severity and nature of the reaction are independent of the original action and dose of the drug
Reaction results vary
Drugs with similar structures may have cross-allergic reactions For example, penicillin can cause anaphylactic shock. An allergy test should be done before taking the drug. Penicillin and cephalosporins have similar structures and can cause allergic reactions.
withdrawal reaction
Aftereffects: Effects that remain after the blood drug concentration drops below the national concentration. Phenobarbital hypnosis → dizziness and drowsiness the next morning
Secondary reactions: Refers to the adverse consequences caused by drug treatment, also known as treatment contradictions (broad-spectrum antibiotics for anti-infection)
Write down examples of idiosyncratic reactions (genetic)
Tolerance (the body’s response to the drug)
Cross-tolerance (similar structures or identical properties)
Tachyphylaxis (nitroglycerin)
Drug resistance (pathogens or tumor cells killed by drugs continue to grow)
drug dependence
Physical dependence (addiction): Withdrawal symptoms (objective) appear once the drug is stopped → white powder
Mental dependence (habitual): subjective (self-feeling) discomfort after stopping the drug, but no withdrawal symptoms. Hypnotics, smoking, drinking, central depression
drug relationship
QSAR
Dose-effect relationship
Mass-response dose-effect curve
Dose-response curve
Potency = No matter how great the effect is: no matter how great the (active) effect of the drug is (no matter how much the dose of aspirin is increased, the analgesic effect cannot match that of morphine)
Potency intensity: the dose required for a drug to achieve a certain effect (the smaller the dose required for the same effect, the stronger the potency intensity)
Half effective dose = ED50: 50% of the dose produces the greatest effect
LD50: The dose that causes the death of half of the animals
Relationship between dose and intensity of action
extreme amount
No matter how small the effective dose is
Commonly used amount
Drug mechanism of action
drugs and receptors
Receptor properties
specificity
sensitivity
Saturation: limited number, competition
Affinity: Binding of receptor to drug
Diversity: The same receptor acts on different effectors to produce different effects (M receptor)
Reversibility: can both combine and dissociate
Ligand (binds with receptor)
endogenous
Exogenous: drugs and poisons
Essential properties for drug-receptor interactions
Affinity: the ability of a drug to bind to a receptor
Intrinsic activity = effector: the effect (effect) produced after the drug binds to the receptor
Drug Classification
Agonist = agonist drug = no matter how effective it is: it has affinity and intrinsic activity
Partial agonist = partial agonist: stronger affinity, weaker intrinsic activity
According to the antagonist: affinity, no intrinsic activity (also called active ingredient)
Agonist drugs. Combined use of partial agonists: antagonize the effect of agonists and reduce the effect of agonists. Example on page 30 of the textbook.
Antagonists ① Competitive antagonism (competition with agonists for the same receptor is reversible, only 2 grams of aspirin can compete with 1 gram of morphine) ② Non-competitive antagonism (strongly binds to receptors, preventing agonists from binding to receptors)
receptor modulation
Receptor downregulation: Reduced number of receptors, low affinity = weakened effect (tolerance). If receptor agonists are used to treat asthma for a long time, tolerance will occur.
Receptor upregulation: Increased number and affinity of receptors = enhanced effect ("rebound" phenomenon)
Pharmacokinetics
drug transport across membranes
passive transport
active transport
Drug processes in the body
affecting absorption
Route of administration
Not absorbed: intravenous injection and intravenous drip drugs directly enter the blood circulation (vascular injection)
Absorption: Inhalation > Sublingual > Rectal > Intramuscular injection > Subcutaneous injection > Oral mucosal administration > Skin administration (non-vascular administration)
First level elimination:
💊Physical and chemical properties
Absorb the environment
affecting distribution
Binding of drugs to plasma proteins
Bound drugs (can bind to plasma proteins)
The large molecular weight makes it difficult to be transported across membranes to organs and stored in the blood.
The binding is reversible (it can both bind and dissociate) and it is a free drug if it is dissociated.
Saturated competitive displacement (limited quantity, two drugs AB compete for the same plasma protein at the same time, A competes to displace B, resulting in an increase in the proportion of free drugs (absorption), enhanced effects or increased toxicity)
Free drugs (not bound to plasma proteins)
pH of body fluids
Acid and alkali promote absorption, acid and alkali promote excretion (weak acidosis is rescued by weak alkali, which is easy to excrete, in contrast to this)
organ blood flow
Features ① Rapidly distributed to organs with large blood flow ② Liver, kidney, brain, and heart blood flow decreases sequentially. ③Redistribution
Tissue affinity: Iodine → thyroid Tetracycline → bone (strong affinity)
body barrier
Blood-cerebrospinal fluid barrier: 1. Larger fat-soluble, smaller molecular weight and a few water-soluble drugs 2. Meningitis 3. Infants and young children
Placental barrier: Almost all drugs can cross the placental barrier and enter the fetal circulation. Therefore, pregnant women should be careful when using the drug to prevent fetal poisoning or teratogenesis.
Blood-eye barrier: Clinically, local eye drops or periorbital administration are commonly used, such as subconjunctival injection, retrobulbar injection, etc.
metabolism ∽ inactivation
The liver is the main organ for drug metabolism, followed by the intestines, kidneys, lungs and brain tissue.
Three changes in pharmacological activity: ① Inactivation (main) ② Activation (such as cortisone-hydrocortisone (pharmacologically active)) ③ Toxic metabolites
drug metabolizing enzyme system
CYP450 (most important)
Features: low selectivity, large individual differences, enzyme activity can be induced or inhibited by drugs
Liver drug enzyme inducers: any drug that can enhance the activity of liver drug enzymes or increase the production of liver drugs (tolerance) → fast metabolism → fast excretion → short residence time in the body → weak drug effect → low effect eg phenobarbital, phenytoin Sodium, rifampicin
Liver enzyme inhibitors: Any drugs that can weaken the activity of liver enzymes or reduce the production of liver enzymes. (Enhanced drug efficacy, poisoning) Slow metabolism → Slow excretion → Long residence time in the body → Strong drug effect → Low effect eg para-aminosalicylic acid, tobacco, chloramphenicol
Non-microsomal enzymes: cholinesterase, monoamine oxidase, etc.
drug excretion
Pathway: kidneys (most important) bile (secondary), other pathways: lungs, milk, sweat, saliva, tears
Renal excretion: weakly acidic carrier, weakly alkaline carrier, (carrier transport)
Characteristics of renal excretion of drugs
Urinary drug reabsorption: low polarity, high fat solubility = non-dissociated drugs and original metabolites → reabsorbed into the blood → slowly excreted
Competitive inhibition phenomenon: Probenecid inhibits the active secretion of penicillin, which increases the blood concentration of penicillin, slows down its excretion, and prolongs the action time of penicillin in the body.
Factors affecting renal excretion of drugs
In cases of renal insufficiency, the dose of the drug should be reduced and the interval between doses should be extended.
Urine pH
Bile excretion (conjugated drugs) and enterohepatic circulation remind us to prevent poisoning
Drug rate process in the body
drug time curve
room model
One room model
Two-room model
Drug in vivo rate change curve
Blood drug concentration changes over time
drug time curve
room model
One room model
Two-room model
drug elimination kinetics
First-level kinetics: constant ratio elimination (100 grams * 80% = 80, the second time 80 grams * 80% = 64 in sequence) most use this
Zero-pole Dynamics: Mechanics: fast elimination speed, constant quantity elimination (a total of 500 grams of drug, 50 grams for the first time, 50 grams for the second time) in a few cases
Pharmacokinetic parameters
Bioavailability (F)
significance
half life
Apparent volume of distribution (vd): Drugs with small Vd values are excreted quickly, and drugs with larger Vd values are excreted more slowly.
Clearance rate (CL)
Steady-state blood concentration (CSS)
Peripheral nervous system medications
Overview of Efferent Nerve Medications
efferent neural classification
Efferent nerves classified by transmitter
Norepinephrine (NA)
Acetylcholine (ACh): Storage: Stored in vesicles, disappear: ACh AChE → Choline Acetate Cholinesterase (AChE.)
efferent nerve receptors
choline receptor
Muscarinic cholinergic receptors (M-R) and atropine act on blood vessels in the same way
nicotinic cholinergic receptor
adrenergic receptors
Dopamine receptor (DA-R)
Efferent Nervous System Drug Classification
Classification of cholinergic drugs (similar effects)
anticholinesterase drugs
Reversible anticholinesterase drugs (easy to dissociate)
neostigmine
Mechanism
internal processes
Pharmacological effects: The strongest effect on stimulating skeletal muscles (main)
Clinical application
Myasthenia gravis: excites skeletal muscles and improves myasthenia symptoms
Postoperative abdominal distension and urine retention: strengthen the gastrointestinal wall and bladder wall to promote defecation and urination
Paroxysmal supraventricular tachycardia: heart rate 150-250 beats/min. Stimulates M receptors, inhibits the heart, and slows down atrioventricular conduction.
Rescue from muscle relaxant poisoning: rescue from tubocurarine overdose poisoning
Adverse reactions
Small therapeutic dose: can cause nausea, vomiting, abdominal pain, bradycardia, muscle tremors, etc.
Overdose causes "cholinergic crisis"
Contraindications
Physostigmine (Eserin)
Irreversible anticholinesterase drugs (strongly bound)
pralidoxime chloride
choline receptor agonists
M, N cholinergic receptors
M choline receptor
Pilocarpine
①Eye: Pilocarpine stimulates M receptors and miosis (stimulates M receptors in the iris and pupillary sphincter), intraocular pressure ↓, regulates spasm (see near objects clearly) ② Glands: It can increase gland secretion, especially sweat glands and salivary glands.
clinical application
Glaucoma♥ is mainly used to treat angle-closure glaucoma, and it also has certain curative effects in the early stages of open-angle glaucoma.
Iritis ♥ is mainly used alternately with mydriasis (atropine) to prevent adhesion between the iris and the lens.
M. Rescue of choline receptor blocker drug poisoning ♥ Such as atropine poisoning, ★ regular (agonists and antagonists of the same receptor) agonist poisoning, antagonist poisoning; antagonist drug poisoning, agonist rescue
Adverse reactions
Salivation, sweating, abdominal pain, diarrhea, bronchospasm
Rescue with atropine
.Ncholine receptor
anticholinergics
M choline receptor blockers
atropine
internal processes
Widely distributed across the blood-brain barrier and placental barrier {a small amount is excreted in breast milk}
Mainly taken orally {fast absorbed}
The kidneys mainly excrete
Pharmacological effects
Inhibit gland secretion {no matter how strong the sweat glands and salivary glands are, they inhibit the secretion of gastric juice}
Effects on the eyes: dilate pupils {block M receptors}, increase intraocular pressure, regulate paralysis [opposite effect to pilocarpine]
subtopic
The middle zone of excitement is not obvious
Clinical application
Relief of visceral, biliary and renal colic with atropine and pethidine
Inhibit glandular secretion
Ophthalmic applications are mainly used in children
Bradyarrhythmias {sinus bradycardia, atrioventricular block
Anti-shock {vasodilator effect}
Rescue organophosphate poisoning
Adverse reactions
common
overdose poisoning
poisoning rescue
Contraindications
Anisodamine
Functional characteristics, atropine comparison
Clinical application
Scopolamine
Pharmacological effects
Clinical application
Synthetic substitutes for atropine
homatropine
Tropicamide
synthetic antispasmodics
ipratropium bromide
Benatezine is similar to Brubacin
N-choline receptor blockers
Skeletal muscle relaxant N2
Skeletal muscle relaxants
Noncompetitive relaxants = depolarizing relaxants
Representative medicine
Non-depolarizing muscle relaxants
Representative medicine
others
Ganglion blocking drug N1 (no longer used clinically)
Mecamylamine
Cimeprofen
adrenergic agonists
RB receptor agonists
adrenaline main
In vivo process {usually administered by intravenous drip}
Pharmacological effects
Blood vessel
B2 receptor: skeletal muscle blood vessels, coronary blood vessels relax
R1 receptor: contraction of skin, mucous membranes, and visceral blood vessels
heart
excited heart
Small dose of blood pressure {first raises blood pressure [main R1]] large dose then lowers blood pressure [main B2 receptor]
smooth muscle
B2 smooth muscle relaxation (running), R1 smooth muscle mucosal vasoconstriction (reduced secretions, reduced edema)
Enhanced metabolism: increased blood sugar, etc.
clinical application
subtopic
Anaphylaxis, anaphylactic shock is the first choice for epinephrine
acute bronchial asthma attack
Compatible with regional anesthesia (constriction of regional blood vessels) for tooth extraction,
Local hemostasis (nosebleeds, gum bleeding)
Treat glaucoma
Adverse reactions
Main: palpitations, irritability, pain, elevated blood pressure
Contraindications
dopamine
Binds to dopamine receptors
clinical application
Mainly used for renal and mesenteric vasodilation
Ephedrine
Non-catecholamine, centrally apparent (through blood-brain barrier), contraindicated by athletes
Mainly used for nasal congestion caused by colds
R receptor agonists
Norepinephrine
intravenous drip
Pharmacological effects
Systemic vasoconstriction (R1), except coronary arteries (B1)
(B1) Excites the heart, but overall, the heart rate reflexively slows down
Metahydroxylamine
phenylephrine
Methoxamine
B receptor agonists
isoproterenol
anti-adrenergic drugs
R receptor blockers
Non-selective α-blockers
Short-acting: phentolamine, tolazoline
Long-acting type: phenoxybenzamine
Selective α1 receptor blocker: pazosin
Selective α2 receptor blocker: Yohimbine
floating theme