Muscle Relaxants and Anesthetic Drugs (Iszard) Flashcards
Neuromuscular blockers are divided into what 2 categories?
Non-depolarizing: Isoquinolines and Aminosteroids
Depolarizing: Succinylcholine
What is the MOA of the non-depolarizing neuromuscular blockers?
competitive antagonist of nAChR; they are highly polar so parenterally administered; some antibiotics enhance their blockage activity
What are the 4 isoquinoline non-depolarizing neuromuscular blockers?
“curiums”
Atracurium (least histamine release)
Cisatracurium (fewer side effects and can be given to patients with hepatic and renal impairment)
Doxacurium (contraindicated in renal failure)
Mivacurium
“curiums” neuromuscular blockers
isoquinolines
Atracurium (least histamine release)
Cisatracurium (fewer side effects and can be given to patients with hepatic and renal impairment)
Doxacurium (contraindicated in renal failure)
Mivacurium
Cisatracurium
isoquinoline non-depolarizing neuromuscular blocker; fewer side effects and can be given to patients with hepatic and renal impairment
Which neuromuscular has agent fewer side effects and can be given to patients with hepatic and renal impairment?
Cisatracurium
What are the 4 aminosteroids non-depolarizing neuromuscular blockers?
“curoniums”
Pancuronium (long acting; contraindicated in renal impairment)
Pipecuronium (long acting; contraindicated in renal and hepatic impairment)
Rocuronium (most rapid onset 60-120 secs; contraindicated in hepatic impairment)
Vercuronium (contraindicated in renal and hepatic impairment)
Which aminosteroids non-depolarizing neuromuscular blocker has the quickest onset?
Rocuronium; most rapid onset 60-120 secs; contraindicated in hepatic impairment; only aminosteroid that is not eliminated by the kidneys
Rocuronium
aminosteroids non-depolarizing neuromuscular blocker; most rapid onset 60-120 secs; contraindicated in hepatic impairment; only aminosteroid that is not eliminated by the kidneys
What is the prototypte non-depolarizing neuromuscular blocker and why is it less favorable?
d-tubocurarine; very long duration of action; shorting-acting blockers are more favorable
What is the one depolarizing neuromuscular blocker?
Succylcholine; contraindicated in malignant hyperthermia (do not use with Dantrolene); Black Box Warning of cardiac arrest
Succycholine is contraindicated in what malignancy?
malignant hyperthermia
Which aminosteroid non-depolarizing neuromuscular blocker is a good alternative to succinylcholine?
Rocuronium; most rapid onset 60-120 secs; contraindicated in hepatic impairment; only aminosteroid that is not eliminated by the kidneys
What are the 3 subgroups of acetylcholinesterase Inhibitors?
- alcohols - reversible
- carbonic acid esters - reversible (neostigmine and pyridostigmine)
- organophosphates - IRREVERSIBLE (ecothiophate)
organophosphates
an irreversible acetylcholinesterase Inhibitor; ecothiophate “nerve gas”
can try to treat with regeneration of AChE (Pralidoxime)
Which drug is used for the regeneration of AChE
Pralidoxime
Pralidoxime
regeneration of AChE; used in cholinergic crisis along with atropine
Which drugs are indicated for myasthenia gravis?
reversible acetylcholinesterase inhibitors that do not cross the BBB; increases available ACh; neostigmine and pyridostigmine
Drug used to reverse neuromuscular blockage in drug induced paralysis?
reversible acetylcholinesterase inhibitor neostigmine (carbonic acid ester)
What are the 9 centrally acting spasmolytics?
- baclofen - GABAb agonist
- Carisoprodol - schedule IV controlled substance; metabolized by CYP2C19
- Chlorzoxazone - acts on spinal cord
- Cyclobenzaprine - causes significant sedation; metabolized by CYP450s
- Diazepam - schedule IV controlled substance
- Metaxalone - interrupts spasm-pain-spasm cycle
- Methocarbamol - causes general CNS depression
- Orphenadrine
- Tizanidine
Which centrally acting spasmolytic interrupts spasm-pain-spasm cycle?
Metaxalone
What are the two scheduled IV controlled centrally acting spasmolytics?
Carisoprodol and Diazepam
What are the two centrally acting spasmolytics metabolized by CYP proteins?
Carisoprodol and Cyclobenzaprine
What are the 2 non-centrally acting spasmolytics?
- Dantrolene (do not use with Succylcholine); causes inhibition of RyR receptors on skeletal muscles
- Botulism toxin - cleaves SNARE proteins preventing release of ACh
What are the 5 ester local anesthetics?
“caines”
Cocaine
Procaine
Benzocaine
Chloroprocaine
Tetracaine
What is the difference between amide and ester local anesthetics?
amides are chemically stable in vivo and esters are rapidly hydrolyzed by proteins in vivo
What is the general route of administration of general anesthetics?
inhalation or IV injection
What are the 4 IV injected general anesthetics?
- propofol (adults; general anesthesia)
- Thiopental
- Etomidate (general anesthesia)
- ketamine (pediatrics)
What are the 6 inhaled general anesthetics?
“fluranes”
1. Desflurane
2. Enflurane
3. Halothane “ane”
4. Isoflurane
5. N2O
6. Sevoflurane
Which general anesthetic is commonly used for short out-patient surgeries or procedures?
propofol (adults; general anesthesia)
What is the most commonly used amide local anesthetic?
Lidocaine
