Term
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Definition
causes muscle relaxation;
Uses: malignant hyperthermia, long-term control of muscle spasms
SEs: muscle weakness, hepatotoxicity |
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Term
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Definition
used to tx blephorospasm (involuntary eyelid closing), strabismus (eye spasms), and wrinkle treatment
SEs: upregulation of post-synaptic nicotinic ACh receptors at previous injection site; eyelid droop (ptosis) |
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Term
| Paralysis characteristics of NMJ blockers |
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Definition
| small rapid moving muscles first --> then limb trunk muscles --> then intercostal muscles --> lastly, diaphragm |
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Term
| Side Effects of Non-depolarizing NMJ Blockers |
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Definition
| prolonged apnea, histamine release (bronchospasm, hypotension) |
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Term
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Definition
| drug that binds steroidal NMJ blockers in a dose-dependent manner to encapsulate & inactivate steroidal NJM blockers like rocuronium within minutes; encapsulated drug complex is then eliminated via kidney filtration |
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Term
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Definition
non-depolarizing NMJ blocker with shortest duration of action;
Onset: 2-4 min
Metabolized in PLASMA by butyrylcholinesterase |
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Term
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Definition
newer non-depolarizing NMJ blocker with INTERMEDIATE duration of action;
Onset: 1-2 min;
Duration: 30-60 min |
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Term
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Definition
non-depolarizing NMJ blocker with intermediate duration of action;
Onset: 2-4 min;
Duration: 60-90 min |
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Term
| atracurium [Tracrium], cisatracurium [Nimbex] (3x more potent than atracurium) |
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Definition
non-depolarizing NMJ blockers with intermediate duration of action;
Onset: 2-4 min
Duration: 30-90 min
NOT metabolized by enzymes;
degraded by temp. & pH-dependent Hofmann rxn |
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Term
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Definition
steroidal non-depolarizing NMJ blocker; 2nd drug used in lethal injection protocol behind sodium pentathol;
Onset: 4-6 min
Duration: 120-180 min |
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Term
| succinylcholine [Anectine] |
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Definition
depolarizing NMJ blocker;
Duration: 5-8 min;
Time to onset: 1-1.5 min;
Uses: very short procedures (i.e. intubation);
Initial fasciculations --> chest & abdomen mostly; NO ANTIDOTE;
MoA: excessive opening of ACh receptors --> decreased electrochemical driving forces --> less positive ion entry --> less muscle response to motor neuron activity;
SEs: malignant hyperthermia, muscle soreness, histamine release, sinus bradycardia, prolonged muscle depolarization (hyperkalemia, cardiac arrest);
Phase I: fast onset, only a single dose required, neostigmine augments blocking action;
Phase II: occurs after prolonged infusion or high dose (10x normal dose), slow onset, neostigmine antagonizes drug block |
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Term
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Definition
1) lipophilic domain allows entry into neuronal axon;
2) intermediate chain determines degree of metabolism - amides = long-acting, esters = short-acting;
3) hydrophilic N terminal or domain determines inhibitory action at Na channel |
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Term
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Definition
co-administer with LAs to double duration of action & reduce amount of LAs by 1/3rd;
SEs: gangrene at small, peripheral sites |
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Term
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Definition
| subcutaneous injection of LA to numb sites distal to injection site |
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Term
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Definition
| inject peripheral nerves or plexus; requires less LA for this type of anesthesia |
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Term
| intravenous regional anesthesia |
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Definition
| injection of LA into vein of limb with tight tourniquet to occlude blood flow; whole limb is affected; surgery must be finished within 2 hrs due to tourniquet pain & time allowed to be in a tourniquet |
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Term
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Definition
| injection into space within vertebral canal but superficial to dural sac |
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Term
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Definition
| injection into CSF in subarachnoid space |
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Term
| Advantages of Spinal Block |
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Definition
| less time; less discomfort; less LA is needed; more intense sensory & motor block; correct placement of needle can be confirmed with CSF; Limited to injection sites below termination of spinal lumbar cord (2nd lumbar vertebra) |
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Term
| Advantages of Epidural Block |
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Definition
NOT limited to injection sites below termination of spinal cord;
less risk for post-dural puncture HA;
placement of catheter for long-term pain reduction;
fine tune anesthesia by varying dose of LA into catheter |
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Term
| Ester LAs - procaine, tetracaine, benzocaine, cocaine |
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Definition
| LAs metabolized in plasma --> metabolized too fast to be redistributed at low doses |
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Term
| Amide LAs - lidocaine, bupivicaine, prilocaine, dibucaine |
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Definition
| LAs that are taken up by fat, brain, kidney, liver, then muscle & gut; highly protein bound; metabolized in liver |
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Term
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Definition
Low conc.: sleepiness, dizziness, restlessness;
High Conc.: nystagmus, shivering, CNS depression, respiratory failure --> death, restlessness & tremor --> tonic-clonic convulsions (tx with barbiturates or benzodiazepines IV) |
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Term
| Cardiovascular Side Effects of LAs |
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Definition
minimimal changes in electrical excitability, conduction rate, force of contraction;
Higher, toxic levels: depression of cardiac excitability --> cardiovascular collapse, death;
vasodilators |
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Term
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Definition
amides; most widely used LA;
Uses: infiltration, nerve block, spinal, epidural, topical, & IV;
Usually administered with Epi --> increased length of anesthesia; |
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Term
| bupivicaine [Marcaine, Sensorcaine] |
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Definition
amide LA;
long duration of action;
Uses: infiltration, nerve block, spinal, epidural
NOT RECOMMENDED for IV use;
CARDIOTOXIC |
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Term
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Definition
similar to lidocaine; amide LA;
most often used for infiltration anesthesia in DENTISTRY |
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Term
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Definition
| amide LA; topical application to skin &/or mucosal membranes; NOT used in USA |
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Term
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Definition
ester LA;
Uses: infiltration, nerve block, spinal, epidural, topical, & IV;
Slower onset of action;
Onset of action: 2-5 min;
Duration: 1 hr |
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Term
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Definition
ester LA;
MOST common LA for spinal anesthesia;
NOT recommended for any administration form;
Slow onset, toxicity, metabolism is SLOW;
10x more toxic than procaine |
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Term
| benzocaine [Americaine, Hurricaine, Chloraseptic] |
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Definition
ester LA;
used TOPICALLY for skin;
toxicity due to methemoglobin production (rare);
poorly water soluble; NOT well absorbed;
LOW TOXICITY |
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Term
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Definition
ester LA; topical use only;
well absorbed via mucuous membranes;
vasoconstrictor (only LA for this);
Toxicity: nervousness, tonic-clonic seizures, cardiac failure;
DO NOT give with Epi --> increases cardiac toxicity |
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