Neuromuscular Blocking Agents Flashcards
NMBA prevent what?
Acetylcholine from activating nicotinic M receptors on skeletal muscle.
NMBA AKA?
Nicotinic Cholinergic transmission
NMBA block what receptors? and what two types of categories are there?
Acetylcholine from activating nicotinic M receptors on skeletal muscle.
Depolarizing and
Non-depolarizing
What is excitation contraction coupling?
The process in which action potential in a motor neuron leads to contraction of a muscle.
When a muscle is relaxed, there is an uneven distribution
of electrical charge across the inner and outer surfaces of
the cell membrane (polarized membrane)
Positive charges cover the outer surface of the
membrane, negative charges cover the inner surface
What is the Polarization or the resting motor end-plate and muscle membrane?
What phases are included.
The uneven distribution of charge, this means
that the muscle is polarized
Positive charges move from outside to inside causing depolarization of the motor end-plate in response to binding acetylcholine to nicotinic M receptors (more positive inside then out)
Depolarization of the end plate triggers action potential (depolarization) to move down the entire muscle membrane.
Immediately after depolarization occurs, the membrane
returns back to its original resting state by pumping out
positively charged ions from inside the cell
Repolarization follows the unbinding of acetylcholine to Nicotinic M receptors.
Steps of muscle contractions
6 Steps
- An action potential arrives at the terminal of a motor neuron, causing the release of Ach into the junction
- Ach then binds reversibly to nicotinic m receptors on
the motor end plate - The binding of Ach causes the end plate to depolarize
- This initiates a muscle action potential (depolarization
wave that spreads over the entire muscle membrane)
5. This causes a release of calcium ions from the sarcoplasmic reticulum (SR)
- Calcium permits the interaction of actin & myosin, and
when this happens a muscle contraction occurs
Ach then quickly dissociates from the receptors on the
motor end plate and repolarization occurs
Calcium is taken back into the SR, and this causes
relaxation because the actin and myosin cannot work in
the absence of calcium ions
Nondepolarizing (competitive) NMBAs
Non depolarizing (competitive) neuromuscular blockers:
Competitive neuromuscular blocking agents are drugs
that compete with Ach for binding to nicotinic m
receptors. These drugs do not depolarize the motor end plate. When these drugs bind to the nicotinic m receptors, they do not cause receptor activation – they block the effects of Ach. This blocking effect causes muscle relaxation throughout the body. Muscle relaxation persists until the amount of drug in the junction is insufficient to prevent receptor occupation by Ach
Binding of non depolarizing neuromuscular blocking
agents to nicotinic m receptors prevents Ach from
binding. This means that with no Ach binding there is no
contraction of the muscles
NMBAs Pharmacological effects
Muscle relaxation is the primary effect and this is known
as flaccid paralysis
Muscles of the eyes and face are the first to relax, then
the limbs, abdomen, and glottis. The last muscles
affected are the respiratory muscles (intercostals and
diaphragm)
Hypotension - side effect
Hypotension – some neuromuscular blockers can cause
hypotension due to the blockade of nicotinic m receptors,
and also from histamine release (some vasodilation may
occur)
What is the effect on consciousness?
These drugs do not cross the blood brain barrier,
therefore they have no effect of consciousness.
It is very important to sedate before giving any paralytic
to our patients
Depolarizing muscular agents
Succinylcholine is an ultrashort acting drug and is the
only depolarizing NMB
Succinylcholine binds to nicotinic m receptors on the
motor end plate and causes it to depolarize
This depolarization causes transient muscle contractions
(fasciculations) to occur
Depolarizing muscular agents - adverse effects
1
Succinylcholine Dose Card
1
Rocuronium Dose Card
1
Vecuronium Dose Card
1