SKELETAL MUSCLE RELAXANTS

Drugs Pharmacodynamics/Pharmacokinetics Clinical Use Adverse Effects Drug

Interactions
NEUROMUSCULAR BLOCKING AGENTS
Nondepolarizing  Prevent access of Ach to its receptor and thereby prevent depolarization 1. Surgical Relaxation (especially d-tubucurarine:
Relaxant Drugs  Prototype drug – d-tubucurarine intraabdominal and intrathoracic hypotension
 Act predominantly at the nicotinic receptor site by competing with Ach surgery)
 Also block prejunctional sodium channels  interfere with the mobilization of 2. Endotracheal Intubation
Ach at the nerve ending and cause fade of evoked nerve twitch contractions 3. Control of ventilation
 During anesthesia, initially causes motor weakness followed by skeletal muscle 4. Treatment of convulsions
become flaccid and inexcitable to electrical stimulation (diaphragm – last
muscle to be depolarized and 1sr to regain function)
Nondepolarizing Relaxant Drugs – Steroid
Vecuronium  Intermediate-acting steroid muscle relaxant Minimal CV
Rocuronium  Dependent on biliary excretion or hepatic metabolism for their elimination effects
 More commonly used clinically
 Least potent (rocuronium) have the fastest onset and the shortest duration of
action
Pancuronium  Long-acting steroid muscle relaxant Moderate
increase in HR
and smaller
increase in CO
Tachycardia
Nondepolarizing Relaxant Drugs – Isoquinoline
Atracurium  Intermediate-acting isoquinoline non depolarizing relaxant Seizure Increase in
 Main breakdown product – luadanosine Hypotension the volatile
d/t histamine anesthetic
release requirement
Bronchospasm
Citracurium  Atracurium stereoisomer Minimal CV
 Less dependent on hepatic inactivation effect
 Less likely to produce histamine
 Hass all the advantages of atracurium with fewer adverse effects
Gantacurium  Asymmetric mixed-onium chlorofumarates
 Currently in phase 3 clinical trials
 Rapid onset of effect and predictable duration of action that can be reversed
with neostigmine

SOURCE: BASIC AND CLINICAL PHARMACOLOGY BY KATZUNG 13TH EDITION | the LEV guide
Depolarizing  Blockade can be produced by an excess of a depolarizing agonist (Ach) * Same with nondepolarizing
Relaxant Drugs
Succinylcholine  Extremely short duration of action (5-10min) Flaccid Malignant
 Dibucaine number – measure the ability of a patient to metabolize paralysis hyperthermia
succinylcholine Transient (with volatile
 MOA – phase 1 block: depolarizing; phase 2 block: desentizising fasciculation anesthetics)
over the chest Cardiac
and abdomen arrhythmia
(30sec) (esp with
Negative halothane)
inotropic and
chronotropic
Hyperkalemia
Increase IOP
increased
intragastric
pressure
Myalgia
REVERSAL OF NONDEPOLARIZING NEUROMUSCULAR BLOCKADE
Neostigmine  Antagonize nondepolarizing neuromuscular blockage by increasing the
Pyridostigmine availability of Ach
 Inhibit acetylcholinesterase
Edrophonium  Antagonizes neuromuscular blockade purely by inhibiting acetylcholinesterase Hypoventilation
activity
 More rapid onset of action; but less effective
Sugammadex  Novel reversal agent Induce
 Modified gamma-cyclodextrin that binds tightly to rocunium coagulopathy
Hypersensitivity
SPASMOLYTIC DRUGS
Diazepam  Facilitate the action of GABA in the CNS Patients with spinal cord transection Sedation
 Acts at GABAa synapses Muscle spasm of any origin
 Action in reducing spasticity is mediated in the spinal cord
Baclofen  Orally active GABA-mimeti agent and is an agonist at GABAa receptors Intrathecal – control severe spasticity and Less sedation C/I:
 Does not reduce overall muscle strength muscle pain unresponsive to other meds Seizure in pregnancy
Intractable low back pain epileptics (sternal
Stiff person syndrome Respiratory ossification
Trigeminal neuralgia depression and
Intractable hicuups coma omphalocele
Tic disorder in fetus)
GERD
Alcohol, nicotine, and cocaine craving
Tizanidine  Congener of clonidine Drowsiness
 Significant alpha2 adrenoceptor agonist effects Hypotension
 Reinforces presynaptic and postsynaptic inhibition in the cord Dizziness
 Inhibits nociceptive transmission in spinal dorsal horn Asthenia
Hepatotoxicity
Gapentin  Antiepileptic drug Multiple sclerosis

SOURCE: BASIC AND CLINICAL PHARMACOLOGY BY KATZUNG 13TH EDITION | the LEV guide
Pregabalin  Analog of gabapentin Useful in relieving painful disorders that
involve a muscle spam component
Progabide  GABAa and GABAb agonist
Glycine  Inhibitory amino acid NT
 Given orally
 Readily pass BBB
Idrocilamide  Inhibit glutamatergic transmission in the CNS ALS
Riluzole
Dantrolene  Hydrantoin derivative related to phenytoin Treatment of malignant hyperthermia Reduces
 Interferes with the release of activator calcium through sarcoplasmic reticulum skeletal muscle
calcium channel binding to the RyR1 and blocking the opening of the channel strength
Muscle
weakness
Sedation
Hepatitis
Botulinum Toxin  Neurotoxin produces chemodenervation and local paralysis when injected into Short-term treatment (1-3months) of Respiratory
a muscle wrinkles tract infections
Generalized spastic disorders – cerebral Falls
palsy Fever
Dystonia Pain
Incontinence d/t overactive bladder
Chronic migraine
Carisoprodol  Centrally active drugs Acute local Muscle Spasm Sedation
Chlorphenesin  Prototype – cyclobenzaprine Transient visual
Chlorzoxasone  Cyclobenzaprine is structurally r/t TCA and produce antimuscarinic side effects hallucinations
Cyclobenzaprine  Ineffective in treating muscle spasm d/t cerebral palsy or SCI
Metaxalone
Methocarbamol
Orphenadrine

SOURCE: BASIC AND CLINICAL PHARMACOLOGY BY KATZUNG 13TH EDITION | the LEV guide