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Skeletal Muscle Relaxants

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1 Skeletal Muscle Relaxants
CHAPTER 9 Skeletal Muscle Relaxants

2 Clinical Indication A. Prevent or interrupt muscle spasm associated with Spastic diseases Spinal cord damage Overexertion of muscles B. Adjunct medication for anesthesia intubation, surgical and orthopedic procedures

3 Types of Muscle Relaxants
Muscle Relaxants differ by the location and mechanism that muscle contraction is inhibited Centrally- within the spinal cord Peripherally- within the muscle

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5 Paralysis Spastic – upper motor neuron lesion
Can use central or peripheral relaxer Stroke Brain trauma Multiple sclerosis Spinal cord transection Flaccid – lower motor neuron lesion  atrophy

6 Peripherally Acting Muscle Relaxants
Mechanism of Action Peripherally acting muscle relaxants interact with nicotinic-muscle (Nm) receptors to block acetylcholine (ACH) attachment on the receptors nondepolarizing blockers curare, gallamine, pancuronium OR • stimulate the receptor followed by inability of the receptor to respond to ACH depolarizing blockers succinylcholine

7 Neuromuscular blockers - uses
Any situation where impaired relaxation interferes with function Before surgery Allows intubation Relax abdominal muscles Orthopedic procedures fibromyalgia

8 NMJ blockers Tubocurarin (Curare) – arrow poison
Nondepolorizing-lasts min – releases histamine – not in asthma Pancuronium (Pavulon) – nondepolorizing does not release histamine Nondepolorizing blockers – competitive – reversed by prostigmine Succinylcholine (Anectine) depolarizing – rare pseudocholinesterase deficiency

9 Peripherally Acting Muscle Relaxants
Mechanism of Action (continued) OR The muscle relaxant may interact with the biochemical pathway within contractile proteins that make up the muscle fibers direct acting skeletal muscle relaxant dantrolene Used in MS, cerebral palsy and cord injury

10 Other Effects Cardiovascular blockade of ACH vagolytic increase heart rate (tachycardia) histamine release or decreased sympathetic tone vasodilation Respiratory histamine release bronchospasm increase in bronchial secretions

11 Cautions, Toxicity, and Drug Interactions
All peripheral muscle relaxants Paralysis of respiratory muscles Succinylcholine Enhanced relaxation in Myasthenia Gravis, spinal cord lesions, ACHesterase inhibitors Malignant hyperthermia Dantrolene Hepatotoxicity elevated serum liver enzymes Peripheral and Central muscle relaxants Potential muscle relaxation- CNS depressants- alcohol, sedatives, tranquilizers

12 Central Skeletal Muscle Relaxants
Mechanism of Action Centrally acting muscle relaxants inhibit reflexes within the spinal cord chlordiazepoxide, diazepam inhibit gamma-aminobutyric acid (GABA) receptors baclofen inhibit alpha-2-adrenergic receptors in the CNS tizanidine

13 Central muscle relaxents
Used – chronic spasticity, overexertion, muscle trauma – sprains and strains, nervous tension Cyclobenzaprine (Flexeril) Diazepam (Valium) Methocarbamol (Robaxin) Often used with aspirin or anti-inflammatory drug

14 Other Effects CNS blurred vision, dizziness, lethargy, decreased mental alertness Vascular-decreased sympathetic tone vasodilation, orthostatic hypotension Dependence with prolonged use

15 Drug Interactions Neuromuscular blocking drugs
Potentiate muscle relaxation- antibiotics, antiarrhythmic drugs, general anesthetics Potentiate potassium loss- diuretics, digitalis


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