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(Local anesthetics, Inhalation anesthetic, Induction time, endogenous…
Local anesthetics
features
Frequency-dependent
正比
Voltage-dependent
正比
Internal site block
需有較高的脂溶性
pH too low -> effect decreases
Aminoamide
Lidocaine
frequency-dependent block
Mepivacaine
intermediate acting amide
Spinal or epidural anesthetic
產科不可以使用此藥
Bupivacaine、Ropivacaine
Spinal anesthesia
適用於剖腹產的半身麻醉
具有心臟跟 CNS 的毒性
(S)-isomer
Etidocaine
motor block w/心毒性
Mechanism
cytoplasmic site of IV domain S6 segment @ Na+ channel α subunit
Maintain inactivated state
Local anesthetic-like effect
Quinidine
Vasoconstrictor potentiation
(phenylephrine,selective α adrenergic agonist)
AE
Ester form -> PABA
procaine
Inhalation anesthetic
Volatile anesthetics
Ether
Chloroform
halogenated anesthetics
hepatic toxicity
Best potency -> halothane
Best induction -> Desflurane
almost no hepatic toxicity
Cough + sputum
Malignant hyperthermia
Genetic susceptibility
ryanodine receptors -> autosomal dominant mutation
Ca2+ cant be retook
解藥:IV Dantrolene
Halothane/ Enflurane
Risk
w/ Succinylcholine(muscle relaxant
intravenous anesthetics
血流越快,induction 越快
Type
barbiturates
Methohexital(Brietal)
Common in clinical use
stage of excitement = hiccup
Thiamylal (Surital)
Thiopental (Pentothal)
redistribution
FAT
Slow recovery
超短效安眠藥
Contraindication
Porphyria
Shock
Respirator not available
AE
Laryngeal spasm
GABAA receptor -> Cl- channel open time
No pain easing effect
may lower threshold
benzodiazepines
Lorazepam (Ativan)
Midazolam (Dormicum)
Common use
Diazepam (Valium)
IM
Benzodiazepine binding site @ GABAA receptor
No pain easing eff.
sedation
AE
Amnesia
Flunitrazepam = 迷姦藥 FM2
解藥 -> flumazenil
Dissociative anesthetic
Ketamine(Ketaral)
AE
Nightmare
muscle tone increases
Other usage
Fast-acting anti-depressant
Block thalamus to cortex
IV and good pain easing eff.
Ultrashort non-barbiturate hypnotics
ICU & EM
Propofol(Diprivan)
GABA uptake inhibitor
prevent V+
Respiratory and cardiovascular depression
Etomidate (Hypnomidate)
GABA uptake inhibitor
Sedation but no pain easing eff.
Neuroleptic Analgesia
Opioids
Droperidol + fentanyl
Opioid receptor agonist
Nausea, vomiting
Droperidol = D2 receptor blocker
Antiemetic
Gaseous anesthetic
Nitrous oxide(N2O)
low induction time
No AE on heart (so called)
Cons
Low Potency
diffusion hypoxia
N2O pockets
Induction time
FACTOR
step 1
Pulmonary ventilation
呼吸越快、換氣體積越大,則誘導時間越短
Anesthetic concentration
濃度越高、混有誘導期快的麻醉藥物,則誘導時間越短
Step 2
Blood-gas partition coefficient
在血中的溶解度越大,induction time 越長
Pulmonary blood flow
肺部血流越快,induction time 越長
Gradient of Parterial/Pvenous
正比
Cardiac output
正比
Step 3
Redistribution
Tissue-blood partition coefficient
Tissue blood flow
time of reaching steady state
endogenous opioid peptides
Family
Endorphin
α-Endorphin(16 a.a.)
β-Endorphin(31 a.a.):最強效
γ-Endorphin(17 a.a.)
Dynorphins
Dynorphin B(13 a.a.)
Dynorphin A(17 a.a.):強效
Enkephalin
Leucine-enkephalin(5 a.a.)
Methionine-enkephalin(5 a.a.):強效
Opioid receptors
μ receptor(OP3、MOP)
Endorphin > enkephalin > dynorphin
κ receptor(OP1、KOP)
Dynorphin > endorphin & enkephalin
δ receptor(OP2、DOP)
Enkephalin > endorphin & dynorphin
Gi receptor
Recovery
Diffusion hypoxia
低溶解度的麻醉藥太快進入alveola, alveolar 氧分壓太低