Neuromuscular Relaxants 2

Front 1

Action of non-depolarizing curare type muscle relaxants

Back 1

compete w/ and prevent Ach action at Sk MM endplate, may actually plug ion channel. Is a surmountable block, can be reversed by giving AchE inhibitors (neostigmine); they don't cross BBB!

Front 2

General effects of non-depolarizing curare type muscle relaxants

Back 2

Eyes & Face MM first (check for poker face & ptosis on induction), next large muscles, and finally respiratory mm. (Respiratory mm have LARGEST receptor reserve!) Respiratory paralysis may occur at full doses, give mechanical ventilation to support patient

Front 3

Reversal of non-depolarizing curare type muscle relaxants

Back 3

use neostigmine or pyridostigmine to increase endogenous NT at receptors

Front 4

Action of depolarizing neuromuscular relaxants

Back 4

acts like N-agonist, depolarizes NM endplate but it is a continuous depolarization (Too long)
continuous depolarization results in muscle relaxation & paralysis
continuous administration results in a phase I (continous depol)… ...to phase II shift (gradual repol w/resistance to depolarization)

Front 5

How to reverse a depolarizing neuromuscular relaxants

Back 5

phase 1 is helped by cholinesterase inhibitors & phase II is reversible

Front 6

Action of spasmolytics

Back 6

spasmolytics do not resemble Ach at all, they work in the CNS or INSIDE of the sk mm cell

have several MOA, some involving GABA, some in skeletal muscle cell to block SR release of Calcium (use of Ryanodine R)

Front 7

Reversal of spasmolytics

Back 7

dantrolene (to block Ca from SR) can reverse malignant hyperthermia caused by too much SR Ca output!

Front 8

Why use Tubocurarine

Back 8

you wouldn't!
not used clinically
only for lethal injection

Front 9

What type of NM is Tubocurarine

Back 9

NONDEPOLARIZING NM relaxant

Front 10

PK of Tubocurarine

Back 10

equal kidney & renal excretion, LONGEST t 1/2 of class (greater than 60 minutes)

Front 11

Drug interactions of Tubocurarine

Back 11

enhanced Ab effect; pts. Can develop malignant hyperthermia

Front 12

Overall length of half life

Back 12

Tubo>Pan>Vec>Roc>Miva

Front 13

Why use Pancuronium

Back 13

adjuvant in surgery, abdominal wall relaxation, orthopedic procedures

Front 14

Method of action of Pancuronium

Back 14

NONDEPOLARIZING NM relaxant

Front 15

PK of Pancuronium

Back 15

renal excretion, duration 30-60 minutes (intermediate)

Front 16

Drug interactions of Tubocurarine

Back 16

enhanced Ab effect; pts. Can develop malignant hyperthermia

Front 17

Pancuronium contraindicated for

Back 17

renal failure (see PK)

Front 18

Overall length of half life

Back 18

Tubo>Pan>Vec>Roc>Miva

Front 19

Drug interactions of Pancuronium

Back 19

enhanced effect of antibiotics, particularly aminoglycosides

Front 20

Why use Pancuronium

Back 20

adjuvant in surgery, abdominal wall relaxation, orthopedic procedures

Front 21

Why use Vecuronium

Back 21

adjuvant in surgery, abdominal wall relaxation, orthopedic procedures
OK for patients with ORGAN problems (renal, hepatic)

Front 22

Method of action of Pancuronium

Back 22

NONDEPOLARIZING NM relaxant

Front 23

MOA of Vecuronium

Back 23

Non-depolarizing NM relaxant

Front 24

PK of Pancuronium

Back 24

renal excretion, duration 30-60 minutes (intermediate)

Front 25

PK of Vecuronium

Back 25

metabolic elimination, t 1/2 about 30-45 min

Front 26

Pancuronium contraindicated for

Back 26

renal failure (see PK)

Front 27

Drug interactions of Pancuronium

Back 27

enhanced effect of antibiotics, particularly aminoglycosides

Front 28

Why use Vecuronium

Back 28

adjuvant in surgery, abdominal wall relaxation, orthopedic procedures
OK for patients with ORGAN problems (renal, hepatic)

Front 29

MOA of Vecuronium

Back 29

Non-depolarizing NM relaxant

Front 30

PK of Vecuronium

Back 30

metabolic elimination, t 1/2 about 30-45 min

Front 31

Drug interactions with Vecuronium

Back 31

enhanced Ab effect

Front 32

Why use Rocuronium

Back 32

intubation, relaxation during surgery or ventilation

Front 33

MOA of Rocuronium

Back 33

Non-depolarizing NM relaxatn

Front 34

PK of Rocuronium

Back 34

hepatic elimination; t 1/2 (25 minutes)

Front 35

Contraindications for Rocuronium

Back 35

NOT for hepatic failure patients
okay for renal failure

Front 36

Drug interactions of Rocuronium

Back 36

enhanced Ab effect

Front 37

Why use Mivacuronium

Back 37

good for intubation or surgery in pts w/renal failure

Front 38

MOA of Mivacuronium

Back 38

NONDEPOLARIZING NM relaxant

Front 39

PK of Mivacuronium

Back 39

FAST metabolic elimination, SHORTEST t 1/2 here (=15-20 minutes!)

Front 40

Drug interactions of Mivacuronium

Back 40

enhanced Ab effect

Front 41

Affect of Succinylcholine

Back 41

causes flaccid paralysis, generally only use for Phase I and not Phase II

Front 42

MOA of Succinylcholine

Back 42

DEPOLARIZING NM relaxant

Front 43

PK of Succinylcholine

Back 43

metabolized by plasma cholinesterases (liver, plasma); so very short t 1/2 if single dose; succinylcholine is just 2Ach's hooked together

Front 44

Adverse effects of Succinylcholine

Back 44

not an analgesic, muscle pain (from induction fasciculations), hyperkalemia (K+ release from Motor End-Plate), autonomic problems due to N-ganglion stimulation, cardiac arrythmia

Front 45

Drug interactions of Succinylcholine

Back 45

interaction w/inhaled anesthetics can cause malignant hyperthermia! Early sign is jaw mm contraction (trismus)

Front 46

Contraindications of Succinylcholine

Back 46

not for BURN patients (K+ situation) or major soft tissue injury or myopathies

patients that have genetic mutations of plasma cholinesterase metabolize succinylcholine real slow so be careful

Front 47

Why useBaclofen

Back 47

spinal cord spasticity; multiple sclerosis

Front 48

Drug action of Baclofen

Back 48

Direct AGONIST of GABAB receptors on 1a nerve terminals (muscle spindle)

Front 49

MOA of Baclofen

Back 49

SPASMOLYTIC (CNS GABA AGONIST)

Front 50

Adverse effects of Baclofen

Back 50

drowsiness, mental disturbances (altered mental state)

Front 51

How do I know what GABA receptor Baclofen works on

Back 51

Baclofen starts w/B, is Gaba B' muscle spindles=sensory afferents

Front 52

Why use Diazapam (Valium)

Back 52

flexor & extensor spasm, spinal spasticity, multiple sclerosis

Front 53

MOA of Diazapam (Valium)

Back 53

SPASMOLYTIC, technically a benzodiazapine, GABA pre-synaptic AGONIST

Front 54

Drug action of Diazapam (Valium)

Back 54

GABAA agonist, increase Cl-influx to decrease excitability of neurons

Front 55

Adverse events of Diazapam (Valium)

Back 55

drowsiness, sedation

Front 56

Contraindication for Diazapam (Valium)

Back 56

narrow angle glaucoma or untreated open-angle glaucoma

Front 57

What type of receptor does Diazapam (Valium) work on

Back 57

DiAzApAm gives you THREE clues that it is Gaba A

Front 58

Why use Tizanidine

Back 58

Multiple Sclerosis, spinal spasticity

Front 59

Drug effects of Tizanidine

Back 59

alpha-2 agonist activity, see pre/post synaptic inhibition in the spinal cord

Front 60

MOA of Tizanidine

Back 60

SPASMOLYTIC (alpha 2 agonist) is in CLOZAPINE family

Front 61

Adverse effects of Tizanidine

Back 61

drowsiness and hypotension

Front 62

Why use Dantrolene

Back 62

spasticity from stroke, spinal cord injury, MS or Cerebral Palsy. Malignant Hyperthermia.

Front 63

Drug Affect of Dantrolene

Back 63

acts in sk mm cell to block RyR (Ca Channel on SR)

Front 64

MOA of Dantrolene

Back 64

SPASMOLYTIC (MM CELL)

Front 65

Adverse effects of Dantrolene

Back 65

muscle weakness, sedation, hepatitis

Front 66

Drug interactions of Dantrolene

Back 66

can treat malignant hyperthermia from succinylcholine

can treat malignant hyperthermia from inhaled anesthetics (block Ca relese)