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pharmachology > Skeletal Muscle Relaxants > Flashcards

Skeletal Muscle Relaxants Flashcards

1
Q

Diazepam

Central spasmolytic

A

MECHANISM
GABA a agonist
Increases interneuron inhibition

INDICATION
Acute / chronic spasm - caused by cerebral palsy or stroke

KINETICS
Oral / Parenteral
12-24h
Hepatic excretion

SIDE EFFECTS
Sedation
Weakness

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2
Q

Baclofen

Central spasmolytic

A

MECHANISM
GABA b agonist

INDICATION
Acute SEVERE muscle spasm - caused by cerebral palsy or stroke

KINETICS
Oral / intrathecal

SIDE EFFECTS
Sedation
Weakness
Respiratory depression

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3
Q

Tizanidine

Central spasmolytic

A

MECHANISM
a2 agonist in spinal cord
Pre and postsynaptic inhibition
Related to clonidine

INDICATION
Acute / chronic spasm - caused by cerebral palsy or stroke

KINETICS
Oral

SIDE EFFECTS
Sedation
Weakness
Hypotension
Less cardiovascular side effects compared to clonidine
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4
Q

Tolperisone

Central spasmolytic

A

MECHANISM
VDNa inhibitor
VDCa inhibitor
In reticular formation in brain stem

INDICATION
Acute / chronic spasm
Multiple sclerosis
Encephalomyelitis
Myelopathy

KINETICS

SIDE EFFECTS

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5
Q

Cyclobenzaprine
1/4

Central spasmolytic

A

MECHANISM
Unknown
Antimuscarinic

INDICATION
Acute muscle spasm - caused by local trauma

KINETICS
Oral

SIDE EFFECTS
Sedation
Hallucinations
Respiratory depression

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6
Q

Mephenesine
2/4

Central spasmolytic

A

MECHANISM
Unknown
Antimuscarinic

INDICATION
Acute muscle spasm - caused by local trauma

KINETICS
Oral

SIDE EFFECTS
Sedation
Hallucinations
Respiratory depression

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7
Q

Guaiphenesine
3/4

Central spasmolytic

A

MECHANISM
Unknown
Antimuscarinic

INDICATION
Acute muscle spasm - caused by local trauma

KINETICS
Oral

SIDE EFFECTS
Sedation
Hallucinations
Respiratory depression

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8
Q

Chlorzoxazone
4/4

Central spasmolytic

A

MECHANISM
Unknown
Antimuscarinic

INDICATION
Acute muscle spasm - caused by local trauma

KINETICS
Oral

SIDE EFFECTS
Sedation
Hallucinations
Respiratory depression

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9
Q

Omega-conotoxin
(Ziconotide)

Peripheral spasmolytic - presynaptic

A

MECHANISM
Ca channel inhibitor
NT vesicle release inhibitor

INDICATION
Surgical narcosis (main indication)
Chronic pain (CSF injection)
Severe COPD (on artificial respiration)
Intubation
Electroshock therapy (in catatonic schizophrenia)
Seizure / epilepsy
Amphetamin overdose

KINETICS
CSF injection for chronic pain, FDA approved

SIDE EFFECTS

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10
Q

Botulinum toxin

Peripheral spasmolytic - presynaptic

A

MECHANISM
NT vesicles release (Snare) inhibitor

INDICATION
Plastic surgery, muscle relaxant

KINETICS

SIDE EFFECTS

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11
Q

Aminoglycosides
Tetracyclines

Peripheral spasmolytic - presynaptic

A

MECHANISM

INDICATION

KINETICS

SIDE EFFECTS
Muscle weakness

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12
Q

d-tubocurarine (not used)

Peripheral spasmolytic - postsynaptic

A

MECHANISM
nAchR muscular type (NMJ)
Isoquinoline competitive antagonist

INDICATION
Surgical narcosis (main indication)
Severe COPD (on artificial respiration)
Intubation
Electroshock therapy (in catatonic schizophrenia)
Seizure / epilepsy
Amphetamin overdose

KINETICS
IV only
Full paralysis in 2-6min
No CNS effect

SIDE EFFECTS
Muscle weakness
After the drug is gone, unknown reason

Acetylcholinesterase inhibitors used to antagonise effect
Neostigmine
Distigmine

Atropin must be coadministered to antagonize parasympathetic effects on heart

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13
Q

Doxacurium

Peripheral spasmolytic - postsynaptic

A

MECHANISM
nAchR muscular type (NMJ)
Isoquinoline competitive antagonist

INDICATION
Surgical narcosis (main indication)
Severe COPD (on artificial respiration)
Intubation
Electroshock therapy (in catatonic schizophrenia)
Seizure / epilepsy
Amphetamin overdose
KINETICS
Long acting (60-180min)

SIDE EFFECTS
Muscle weakness
After the drug is gone, unknown reason

Acetylcholinesterase inhibitors used to antagonise effect
Neostigmine
Distigmine

Atropin must be coadministered to antagonize parasympathetic effects on heart

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14
Q

Atracurium

Peripheral spasmolytic - postsynaptic

A

MECHANISM
nAchR muscular type (NMJ)
Isoquinoline competitive antagonist

INDICATION
Surgical narcosis (main indication)
Severe COPD (on artificial respiration)
Intubation
Electroshock therapy (in catatonic schizophrenia)
Seizure / epilepsy
Amphetamin overdose
KINETICS
Medium acting (30-60min)

SIDE EFFECTS
Histamine release - Itching, hypotension
Muscle spasm - metabolite Laudanosin is causing it

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15
Q

Cisatracurium

Peripheral spasmolytic - postsynaptic

A

MECHANISM
nAchR muscular type (NMJ)
Isoquinoline competitive antagonist

INDICATION
Surgical narcosis (main indication)
Severe COPD (on artificial respiration)
Intubation
Electroshock therapy (in catatonic schizophrenia)
Seizure / epilepsy
Amphetamin overdose
KINETICS
Medium acting (30-60min)

SIDE EFFECTS
Muscle weakness - antagonise with neostigmine

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16
Q

Mivacurium (not used)

Peripheral spasmolytic - postsynaptic

A

MECHANISM
nAchR muscular type (NMJ)
Steroid competitive antagonist

INDICATION
Surgical narcosis (main indication)
Severe COPD (on artificial respiration)
Intubation
Electroshock therapy (in catatonic schizophrenia)
Seizure / epilepsy
Amphetamin overdose

KINETICS
Short acting (10-15min)
Sugammadex - neutralizes steroids in the plasma

SIDE EFFECTS
Muscle weakness - antagonise with neostigmine

17
Q

Pancuronium

Peripheral spasmolytic - postsynaptic

A

MECHANISM
nAchR muscular type (NMJ)
Steroid competitive antagonist

INDICATION
Surgical narcosis (main indication)
Severe COPD (on artificial respiration)
Intubation
Electroshock therapy (in catatonic schizophrenia)
Seizure / epilepsy
Amphetamin overdose

KINETICS
Long acting (60-180min)
Kidney excretion
Sugammadex - neutralizes steroids in the plasma

SIDE EFFECTS
Muscle weakness - antagonise with neostigmine

18
Q

Pipecuronium

Peripheral spasmolytic - postsynaptic

A

MECHANISM
nAchR muscular type (NMJ)
Steroid competitive antagonist

INDICATION
Surgical narcosis (main indication)
Severe COPD (on artificial respiration)
Intubation
Electroshock therapy (in catatonic schizophrenia)
Seizure / epilepsy
Amphetamin overdose

KINETICS
Long acting (60-180min)
Kidney excretion
Sugammadex - neutralizes steroids in the plasma

SIDE EFFECTS
Muscle weakness - antagonise with neostigmine

19
Q

Vecuronium

Peripheral spasmolytic - postsynaptic

A

MECHANISM
nAchR muscular type (NMJ)
Steroid competitive antagonist

INDICATION
Surgical narcosis (main indication)
Severe COPD (on artificial respiration)
Intubation
Electroshock therapy (in catatonic schizophrenia)
Seizure / epilepsy
Amphetamin overdose

KINETICS
Medium acting (30-60min)
Liver excretion
Sugammadex - neutralizes steroids in the plasma

SIDE EFFECTS
Muscle weakness - antagonise with neostigmine

20
Q

Rocuronium

Peripheral spasmolytic - postsynaptic

A

MECHANISM
nAchR muscular type (NMJ)
Steroid competitive antagonist

INDICATION
Surgical narcosis (main indication)
Severe COPD (on artificial respiration)
Intubation
Electroshock therapy (in catatonic schizophrenia)
Seizure / epilepsy
Amphetamin overdose

KINETICS
Medium acting (30-60min)
Liver excretion
Sugammadex - neutralizes steroids in the plasma

SIDE EFFECTS
Muscle weakness - antagonise with neostigmine

21
Q

Succinylcholine

Peripheral spasmolytic - postsynaptic

A

MECHANISM
nAchR muscular type (NMJ)

Depolarization blockade
Succinylcholine is not degraded by Acholinesterase and causes continuous stimulation of nAchR, Na+ influx, and inactivation of the channel, causing a blockade for 5-10min.
Phase 1 - muscle fibrillation, inactivation
Phase 2 - muscle desensitization after drug removal

INDICATION
Short surgical interventions
Intubation
Laprascopy

KINETICS
Medium acting (30-60min)
Liver excretion
Sugammadex - neutralizes steroids in the plasma

SIDE EFFECTS
Muscle pain - due to fibrillation

Malignant hyperthermia
in case of mutated Ryanodine receptor. Succinylcholine activates it permanently –> muscle shivering, hyperthermia, lactic acidosis, myoglobinemia. Treatment is:
1) Dantrolene (ryanodin receptor antagonist - Hepatotoxic effect in 1-2%
2) Bicarbonate to counteract acidosis
3) Physical cooling

Hyperkalemia - due to nAchR outward K+ current

Bradycardia - SA node M2 receptor stimulation -Antagonise this effect using atropine.

Increased intraoccular pressure - don’t use in glaucoma

pharmachology (7 decks)

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