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Relaxants
I Wayan Sumardika
Pharmacology Department
Faculty of Medicine, Udayana
University
Muscle Relaxants
Facilitate intubation of the
trachea
Facilitate mechanical ventilation
conditions
Reduce abnormally elevated tone
minutes
Dose 0.04-0.07 mg/kg
Pyridostigmine
Edrophonium
Antagonism of
Neuromuscular
Blockade
Mechanis of action
Inhibiting activity of acetylcholineesterase
More Ach available at NMJ, compete for
sites on nicotinic cholinergic receptors
Action at muscarinic cholinergic receptor
Bradycardia
Hypersecretion
Increased intestinal tone
Antagonism of
Neuromuscular
Blockade
Muscarinic side effects are
minimized by anticholinergic
agents
Atropine
Dose 0.01-0.02 mg/kg
Scopolamine
glycopyrrolate
SPASMOLYTIC DRUGS
Diseases of the CNS (cerebral palsy,
multiple sclerosis)
Abnormal high reflex activity in the neural
pathways that control skeletal muscle
Painful spasm
Therapy: reduction of excessive sceletal
muscle tone without reduction of strength.
Drugs for Chronic Spasm
Act in the CNS or in the sceletal
muscle cell rather than at the NMJ
Diazepam
Baclofen
Tizanidine
Dantrolene
Mechanism of Action
Diazepam---facilitates GABA-mediated
presynaptic inhibition
Baclofen---acts as a GABA agonist causing
membrane hyperpolarization via increased K+
conductance
----decrease the release of excitatory
neurotransmiter
Tizanidine---significant Alpha 2 agonist activity,
reinforce both presynaptic and postsynaptic
inhibition in the cord
Dantrolene---reduce the release of
activator calcium from the
sarcoplasmic reticulum
Effective in the treatment of
malignant hypertermia (massive
calcium release from the
sarcoplasmic reticulum of skeletal
muscle)
Drugs for Acute Muscle
Spasm
Treatment of acute spasm resulting
from muscle injury
Sedative or act in the brain stem or
spinal cord
Cyclobenzaprine
Antimuscarinic actions
Cause confusion and visual hallucination