Pharm: Anesthetics Flashcards
inhalation anesthetics
make patient unconscious
IV anesthetics
make patient unconscious
highly lipid soluble: need pH adjustment or surfactant (can lead to toxicity)
INSTANTANEOUS compared to inhaled
rate limiting step of elimination: release from adipose
LONG T1/2, SHORT duration of action due to redistribution
nitrous oxide
gas inhalation anesthetic potentiate 2 pore K channel inhibit NMDA, nicotinic ACh, serotonin, kainate RAPID onset maintains protective reflexes (resp. and CV) can us less volatile agent PAIN RELIEF teratogen in animals inhibits vit. B12 synthetase 2ND GAS EFFECT, DIFFUSIONAL HYPOXIA, INCREASE PRESSURE AE: N/V (important in anesthesia)
volatile liquids
-urane inhalation anesthetic potentiate GABA(A) explosive: add FLUORINE (can cause renal damage) NO pain relief LOSS of REFLEXES AE: MALIGNANT HYPERTHERMIA
halothane
volatile liquid SLOW onset and recovery most POTENT hepatic metabolism AE: ARRHYTHMIA, HEPATIC
enflurane
volatile liquid
MUSCLE RELAXATION
AE: SMELL, SEIZURE
isoflurane
volatile liquid
potentiate 2 pore K channel, glycine, serotonin, kainate
inhibit inward rectifying K channel, AMPA
MUSCLE RELAXATION
AE: SMELL
desflurane
volatile liquid inhibit: NMDA, voltage gated K channel, kainate most RAPID onset and recovery least potent AE: SMELL
sevoflurane
volatile liquid
potentiate: glycine
inhibit: NMDA, serotonin, AMPA
RAPID onset and recovery
thiopental
IV anesthetic: induction agent
barbiturate
CYP induction
AE: PORPHYRIA
propofol
IV anesthetic: induction agent
potentiate GABA(A) and glycine
minor NMDA inhibition: blocks glutamate from binding receptor
high concentration: acts like GABA
ANTIEMETIC
AE: INFUSION SYNDROME, CV/ organ failure when used for long time
etomidate
IV anesthetic: induction agent potentiate GABA(A) and 2 pore K channel NO CV effects AE: inhibit STEROIDS do NOT use in ICU
ketamine
IV anesthetic, IM
inhibit NMDA: PHYSICALLY occludes channel
inhibit muscarinic ACh
increase: cerebral blood flow, ICP, CV (HR, MAP, CO)
NO effects on respiratory rate
other: ANALGESIC, intact PHARYNGEAL/ LARYNGEAL REFLEX, BRONCHODILATOR
AE: emergence HALLUCINATION, EYES OPEN when unconscious (dissociative)
diazepam
IV anesthetic
benzodiazepine
perioperative drug: sedation
LONG duration
lorazepam
IV anesthetic
benzodiazepine
perioperative drug: sedation
midazolam
IV anesthetic
benzodiazepine
SHORT duration
morphine
IV anesthetic opioid LONG LASTING SLOW onset peri-operative analgesia
meperidine
IV anesthetic
opioid
fentanyl
IV anesthetic peri-operative analgesia and RSI neruolept-analgesia agent opioid FAST ONSET SHORT acting decrease sympathetic response during intubation
remifentanil
IV anesthetic
opioid
ULTRA SHORT ACTING
no accumulation: RAPID LOSS OF ANALGESIA
benzodiazepine
potentiate GABA(A): allosteric change (shift dose response and increase POTENCY)
CEILING EFFECT: safe
ANTICONVULSANT, AMNESIA, ANXIOLYTIC
minimal CV and respiratory depression
longer onset compared to other IV anesthetics
NO ANALGESIA
barbiturates
potentiate GABA(A): PROLONG binding (increase EFFICACY)
high concentrations: open GABA channel in absence of GABA: COMA, DEATH
inhibit muscarinic ACh, AMPA, kainate
CYP inducer
opioid: reasons for/against use
For
- no effect on heart
- decrease airway reflex: intubation
- pain relief
- no malignant hyperthermia
- maintain regional blood flow
Against
- incomplete amnesia
- histamine reaction
- increase blood req.
- respiratory depression
- CV instability
opioid
OP1-3 receptors in spinal cord and CNS
AE: bradycardia, hypotension,, HTN, RESPIRATORY DEPRESSION, loss of response to PaCO2, WOODEN CHEST, increase CBF and ICP; CONSTIPATION, MIOSIS, N/V
amide type local anesthetic
prefix contains i
injection or infiltration
metabolized in liver
ester type local anesthetic
NO i in prefix
injection or infiltration
metabolized in any tissue by esterases: SHORTER DURATION
genomic changes in enzyme effect accumulation
topical only anesthetics
poor aqueous solubility and/or undesirable toxicity
EMLA (eutectic mixture of local anesthetics) cream
lidocaine and prilocaine
apple to skin with occlusive dressing before painful procedure
LET (lidocaine-epinephrine-tetracaine)
use in pediatric ED
liquid application to lacerations req. stitches
analgesia and vasoconstriction
vasoconstrictors: use with local anesthetics
- improve intensity of local anesthetic
2. increase duration of blockade
local anesthetics
-caine
bind INNER surface of voltage gated Na channel and inhibit AP in active or inactive state (does not bind in resting state)
act on nerve AXON
unconsciousness ONLY with incorrect administration
lipophilicity: benzene ring
AE: allergy (give other type of local anesthetic); allergy to preservative (sulphites)
lidocaine
amide type local anesthetic
peri-operative RSI
RAPID ONSET
decrease ICP and bronchospasm in intubation
mepivacaine
amide type local anesthetic
LEAST POTENT
SLOW ONSET
prilocaine
amide type local anesthetic
RAPID ONSET
AE: METHEMOGLOBINEMIA
bupivacaine
amide type local anesthetic POTENT LONG ACTING SLOW ONSET AE: CARDIOTOXIC if systemized
ropivacaine
amide type local anesthetic POTENT LONG ACTING SLOW ONSET reduced cardiotoxicity (reason produced)
articaine
amide type local anesthetic ester link cleavage: inactivation lipophilicity: thiophene ring RAPID ONSET BONE PENETRATION: dental block AE: PARESTHESIA
procaine
ester type local anesthetic
LEAST POTENT
SHORT ACTING, SLOW ONSET
chloroprocaine
ester type local anesthetic
SHORT ACTING, FAST ONSET
tetracaine
ester type local anesthetic
POTENT
LONG ACTING
SLOW ONSET
cocaine
ester type local anesthetic
benzocaine
topical only local anesthetic: mucous membranes and skin
AE: METHEMOGLOBINEMIA
dyclonine
topical only local anesthetic: mucous membranes and skin
dibucaine
topical only local anesthetic: SKIN ONLY
pramoxine
topical only local anesthetic: SKIN ONLY
epinephrine
vasoconstrictor
peri-operative anaphylaxis
DI: B blocker, TCA, halothane, HTN, heart block, cerebral vascular insufficiency
CI: close angle glaucoma, HF, CAD, HTN, arrhythmia, cerebrovascular disorder, DM, hyperthyroid
phenylephrine
vasoconstrictor
peri-operative CV support for hypotension
oxymetazoline
vasoconstrictor