MUSCLE RELAXANTS

Oleh : Agnes Christiani (0710113) Ferry Yulianto (0710101) Lani Oktaviani (0710080) Pembimbing : dr.Christin.,

SMF Anestesiologi Fakultas Kedokteran Universitas Kristen Maranatha Rumah Sakit Immanuel Bandung 2011

Indikasi
Fasilitasi intubasi trachea Fasilitasi ventilasi mekanik Optimalisasi kondisi bedah

Relaksasi Otot Skelet didapatkan dengan cara :

Dosis

tinggi anestetik inhalasi Anesthesia regional Neuromuscular blocking agents Proper patient positioning on the operating table

Muscle Relaxants
Muscle relaxants tidak boleh diberikan tanpa dosis obat analgesik & hipnotik adekuat Inappropriately given : pasien paralisis tanpa teranestesi

Muscle relaxant bekerja di:

Neuromuscular
Nerve

junction

terminal Motor endplate of a muscle Synaptic cleft

Nerve

stimulation Release of Acetylcholine (Ach) Postsynaptic events

Neuromuscular Junction (NMJ)

Impuls sarafmotor nerve terminalinflux Caexocytosis synaptic vesicles containing ACHdiffuses across synaptic clefthydrolysed by AchE/bind nicotinic receptors on the motor end plate The binding of two ACH moleculesconformational change opens sodium-potassium channel of the nicotinic receptor. Na+ & Ca2+ ions to enter the cell & K+ ions leave the cell depolarization of the end platemuscle contraction

Neuromuscular Junction (NMJ)

Following depolarization, the acetylcholine molecules are then removed from the end plate region and enzymatically hydrolysed by acetylcholinesterase

Neuromuscular Junction (NMJ)

Binding of Ach to receptors on muscle end-plate

Muscle Relaxants dibagi menjadi:

Depolarizing muscle relaxant

Succinylcholine

Nondepolarizing muscle relaxants

Short

acting Intermediate acting Long acting

Depolarizing Muscle Relaxant

Succinylcholine Mekanisme kerja:

Secara

fisik mirip dengan Ach Berperan sebagai acetylcholine receptor agonist Tidak dimetabolisme secara lokal di NMJ Dimetabolisme oleh pseudocholinesterase dalam plasma Masa depolarisasinya lebih panjang dari Ach Depolarisasi terus menerus menyebabkan relaksasi otot

Depolarizing Muscle Relaxant

Succinylcholine Penggunaan secara klinis:

Paling

sering digunakan untuk fasilitasi intubasi

Dosis succinylcholine untuk intubasi:

1-1.5

mg/kg Onset 30-60 detik, durasi 5-10 menit

Depolarizing Muscle Relaxant

Efek Succinylcholine
Cardiovascular
Fasciculation Muscle

pain Increase intraocular pressure Increase intragastric pressure Increase intracranial pressure Hyperkalemia Malignant hyperthermia

Nondepolarizing Muscle Relaxants

Mekanisme kerja:
Kompetisi

dengan Ach pada binding sites Tidak terjadi depolarisasi pada motor endplate Berperan sebagai competitive antagonist Konsentrasi berlebih menyebabkan channel blockade
Berperan

di presynaptic sites, mencegah berpindahnya Ach ke release sites

Nondepolarizing Muscle Relaxants

Long acting

Pancuronium

Intermediate acting
Atracurium Vecuronium Rocuronium Cisatracurium

Short acting

Mivacurium

Nondepolarizing Muscle Relaxants

Pancuronium
Aminosteroid

compound Onset 3-5 menit, durasi 60-90 menit Dosis intubasi 0.08-0.12 mg/kg Eliminasi terutama di ginjal (85%), hepar (15%) Efek samping: hypertension, tachycrdia, dysrhythmia

Nondepolarizing Muscle Relaxants

Vecuronium
Analogue

of pancuronium Efek vagolytic lebih sedikit dan durasi lebih singkat daripada pancuronium Onset 3-5 menit, durasi 20-35 menit Intubating dose 0.08-0.12 mg/kg Eliminasi di 40% ginjal, 60% hepar

Nondepolarizing Muscle Relaxants

Atracurium
Dimetabolisme
Ester

oleh

hydrolysis Hofmann elimination

Onset

3-5 menit, durasi 25-35 menit Dosis intubasi 0.5 mg/kg Efek samping:
histamine

release causing hypotension, tachycardia, bronchospasm Laudanosine toxicity ( kejang )

Nondepolarizing Muscle Relaxants

Cisatracurium
Isomer

of atracurium Dimetabolisme oleh Hofmann elimination Onset 3-5 minutes, duration 20-35 minutes Intubating dose 0.1-0.2 mg/kg Minimal cardiovascular side effects Produksi laudanosine lebih sedikit

Nondepolarizing Muscle Relaxants

Rocuronium
Analogue

of vecuronium onset cepat 1-2 minutes, duration 20-35 minutes Onset of action mirip dengan succinylcholine Intubating dose 0.6 mg/kg Eliminasi terutama di hepar, sebagian di ginjal

Respon obat tergantung pada:

Temperature Acid-base balance Electrolyte abnormality Age Penyakit penyerta Drug interactions

Alteration of responses

Penyakit penyerta:
Neurologic

diseases Muscular diseases

Myasthenia

gravis Myasthenic syndrome (Eaton-Lambert synrome)

Liver

diseases Kidney diseases

Alteration of responses

Drug interactions
Inhalation

agents Intravenous anesthetics Local anesthetics Neuromuscular locking drugs Antibiotics Anticonvulsants Magnesium

Hierarchy of Neuromuscular Blockade

Fraction of receptor occupied by nondepolarizing muscle relaxant Response to nerve stimulator Whole body signs

99-100 95

No response Posttetanic facilitation present

Flaccid, extreme relaxation Diaphragm moves, hiccough possible

90
75 50 30

One of four twitch of TOF present

Four twitch of TOF present, TOF ratio 0.7

Abdominal relaxation adequate for most prcedure

Tidal volume and vital capacity normal

100-Hz tetanus sustained Passes inspiratory pressure test 200-Hz tetanus sustained Head lift and hand-grip sustained

Antagonism of Neuromuscular Blockade

Effectiveness of anticholinesterases depends on the degree of recovery present when they are administered Anticholinesterases
Neostigmine Onset 3-5 minutes, elimination halflife 77 minutes Dose 0.04-0.07 mg/kg Pyridostigmine Edrophonium

Antagonism of Neuromuscular Blockade

Mekanisme kerja:
Inhibisi

aktivitas acetylcholineesterase Ach semakin banyak di NMJ, berkompetisi menduduki nicotinic cholinergic receptors Bekerja di muscarinic cholinergic receptor
Bradycardia Hypersecretion Increased

intestinal tone

Antagonism of Neuromuscular Blockade

Efek Muskarinik diminimalisasi oleh anticholinergic agents

Atropine
Dose

0.01-0.02 mg/kg

Scopolamine
glycopyrrolate

Reversal of Neuromuscular Blockade

Tujuan : terjadinya spontaneous respiration dan kemampuan untuk mencegah aspirasi