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Pharma > Centrally acting skeletal muscle relaxants (Spasmolytics). Datrolene. Botulinum toxin > Flashcards

Centrally acting skeletal muscle relaxants (Spasmolytics). Datrolene. Botulinum toxin Flashcards

1
Q

Name the spasmolytics

A

Baclofen
Diazepam
Tizanidine
Tolperisone

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2
Q

Name the direct acting muscle relaxants

A

Dantrolene and Botulinum toxin

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3
Q

Name the drugs used in acute muscle spasm with unknown mechanism

A

Mephensin
Guaiphenesin
Chlorzoxasone
Carisoprodol

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4
Q

What receptor does Baclofen work on?

What sort of drug is Baclofen?

A

GABA B

GABA B agonist

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5
Q

What are the clinical uses of Baclofen?

A
  • Decrease spasm in patients with MS
  • Decrease pain in patients with spasticity by inhibiting substance P in the spinal cord
  • Decrease craving in recovering alcoholics
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6
Q

How can Baclofen be administered?

A
  • Oral and intrathecal uses
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7
Q

When would you administer Baclofen intrathecally?

A
  • When patients are not responding to medication by other routes
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8
Q

What are the characteristics of Baclofen when it is administered orally?

A

Rapid and complete absorption in the oral route

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9
Q

What are the adverse effects of Baclofen?

A
  • Sedation
  • Tolerance with chronic use
  • Enhancement of sedative and respiratory effect of opiates and alcohol
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10
Q

What sort of drug is Diazepam?

A

GABA A agonist

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11
Q

What receptor does Diazepam work on?

A

GABA A receptor

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12
Q

What are the clinical uses of Diazepam?

A
  • Muscle spasm of almost any origin
  • Cervical and lumbar syndromes
  • Spasticity induced by neurological disorders
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13
Q

What enzyme is Diazepam metabolised by?

A

CYP1A2

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14
Q

How is Diazepam administered?

A

Oral and parental routes

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15
Q

What is the dosage of Diazepam in non epileptics?

A

5-10mg

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16
Q

What is the dose of Diazepam for status epilepticus?

A

IV 30mg

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17
Q

What sort of drug is Tizanidine?

A

Alpha 2 agonist

18
Q

What is the mechanism of action of Tizanidine?

A

It is an alpha 2 agonist - it reinforces the presynaptic inhibition of the spinal cord.

19
Q

What are the clinical uses of Tizanidine?

A
  • Muscle spasm of almost any origin
  • Cervical and lumbar syndromes
  • Spasticity induced by neurological disorders
20
Q

What enzyme is Tizanidine metabolised by?

21
Q

How is Tizanidine administered?

22
Q

What are the adverse effects of Tizanidine?

A
  • Asthenia
  • Drowsiness
  • Dry mouth
  • Hypotension
23
Q

What is the mechanism of action of Mephenesin?

A

Inhibition of polysynaptic reflexes

24
Q

What is the mechanism of action of Guaiphenesin?

A

Inhibition of polysynaptic reflexes

25
What is the mechanism of action of Chlorzoxazone and Carisoprodol?
Inhibition of polysynaptic reflexes
26
What is the clinical use of Mephenesin?
Muscle spasm accompanying trauma and inflammation
27
What is the clinical use of Guaiphenesin?
- Muscle spasm accompanying trauma and inflammation | - Abdominal and anorectal surgery
28
What are the clinical uses of Chlorzoxazone and Carisoprodol?
Muscle spasm accompanying trauma and inflammation
29
What are the adverse effects of Carisoprodol?
- It has the potential to be abused | - Meprobamate is hepatotoxic
30
What type of drug is Dantrolene?
Direct acting Ryanodine receptor antagonist
31
What is the mechanism of action of Dantrolene?
Dantrolene acts on the skeletal muscular cells to reduce the release of calcium from the SR by interacting with the RyR1 receptor - reducing the actin-myosin interaction. Cardiac and SMC use RyR2 receptors so they are minimally affected
32
Why does Dantrolene only affect skeletal muscles?
Because cardiac and SMCs use RyR2 whereas skeletal muscles have RyR1
33
What is the clinical use of Dantrolene?
Malignant hyperthermia (IV) Spinal injury Spasm after stroke (oral)
34
How is Dantrolene administered in malignant hyperthermia?
IV
35
How is Dantrolene administered when used to treat spasms after strokes?
Orally
36
What are the adverse effects of Dantrolene?
Hepatotoxic Sedation Generalised muscle weakness
37
What type of compound is Botulinum toxin?
Exotoxin
38
Which pathogen produces Botulum toxin?
Clostridium Botulinum
39
What is the mechanism of action of botulinum toxin?
BT inhibits the release of Ach from vesicles by binding synaptobrevin
40
What are the clinical uses of botulinum toxin?
``` Blepharospasm Dystopia Strabismus Cosmetics(wrinkles) Generalised spastic disorders (e.g.,cerebral palsy) ```
41
What is blepharospasm?
Uncontrolled movement of the eyelid
42
What is dystonia?
Uncontrollable muscle contraction

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