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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?

A

CYP1A2

21
Q

How is Tizanidine administered?

A

Orally

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
Q

What is the mechanism of action of Chlorzoxazone and Carisoprodol?

A

Inhibition of polysynaptic reflexes

26
Q

What is the clinical use of Mephenesin?

A

Muscle spasm accompanying trauma and inflammation

27
Q

What is the clinical use of Guaiphenesin?

A
  • Muscle spasm accompanying trauma and inflammation

- Abdominal and anorectal surgery

28
Q

What are the clinical uses of Chlorzoxazone and Carisoprodol?

A

Muscle spasm accompanying trauma and inflammation

29
Q

What are the adverse effects of Carisoprodol?

A
  • It has the potential to be abused

- Meprobamate is hepatotoxic

30
Q

What type of drug is Dantrolene?

A

Direct acting Ryanodine receptor antagonist

31
Q

What is the mechanism of action of Dantrolene?

A

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
Q

Why does Dantrolene only affect skeletal muscles?

A

Because cardiac and SMCs use RyR2 whereas skeletal muscles have RyR1

33
Q

What is the clinical use of Dantrolene?

A

Malignant hyperthermia (IV)
Spinal injury
Spasm after stroke (oral)

34
Q

How is Dantrolene administered in malignant hyperthermia?

A

IV

35
Q

How is Dantrolene administered when used to treat spasms after strokes?

A

Orally

36
Q

What are the adverse effects of Dantrolene?

A

Hepatotoxic
Sedation
Generalised muscle weakness

37
Q

What type of compound is Botulinum toxin?

A

Exotoxin

38
Q

Which pathogen produces Botulum toxin?

A

Clostridium Botulinum

39
Q

What is the mechanism of action of botulinum toxin?

A

BT inhibits the release of Ach from vesicles by binding synaptobrevin

40
Q

What are the clinical uses of botulinum toxin?

A 
Blepharospasm 
Dystopia
Strabismus
Cosmetics(wrinkles)
Generalised spastic disorders (e.g.,cerebral palsy)
41
Q

What is blepharospasm?

A

Uncontrolled movement of the eyelid

42
Q

What is dystonia?

A

Uncontrollable muscle contraction

Pharma (23 decks)

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