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Pharmacology > Spasmolytics > Flashcards

Spasmolytics Flashcards

1
Q

What is muscle spasticity?

A

acute injury to muscle or muscle inflammation

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2
Q

How do CNS diseases cause muscle spasticity?

A
  1. cause abnormally high reflex activity in neuronal pathways
  2. cause painful spasm(rigidity)
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3
Q

How does Malignant hyperthermia cause muscle spasticity?

A

Mutation in RYR1 gene
=Altered Ca release channel
=mutated shannel opens more easily and stays open longer
=increase in intracellular Ca
= sustained muscle contraction (rigidity), stimulated glycogenolysis and aerobic metabolism (excessive heat production)

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4
Q

How are spasmolytics administered?

A

orally

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5
Q

Why are spasmolytics preferable to NMBs

A

They are more selective to NMBs
= they block only increased muscle tone

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6
Q

Which are the centrally-acting spasmolytics?

A

Diazepam
Baclofen
Methacarbamol
Orphenadrine

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7
Q

Which are the directly-acting spasmolytics?

A

Dantrolene

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8
Q

What is Baclofen?

A

Its a GABA derivative

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9
Q

MOA of Baclofen

A

Post-synaptic cleft:
-enhances GABA effects: hyperpolarisation
muscle relaxation
Pre-synaptic cleft:
-decreases glutamate release

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10
Q

Indications of Baclofen

A

Painful muscle spasms of spinal origin
(e.g. MS, Transverse myelitis, traumatic paraplegia and paraparesis)
Pain relief in trigeminal neuroglia

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11
Q

Metabolism and Excretion of Baclofen

A

M: Liver 15%
E: renal (mainly unchanged)

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12
Q

SE of Baclofen

A

Drowsiness
Dizziness
Ataxia (lack of voluntary coordination of muscle movements)

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13
Q

What is Diazepam?

A

is a BDZ

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14
Q

MOA of Diazepam

A
  1. enhances GABA effects: hyperpolarisation=muscle relaxation
  2. Suppresses postsynaptic and monosynaptic reflexes
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15
Q

Indications of Diazepam

A

Muscle spasticity of any origin including Tetanus and reflief of local origin

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16
Q

Administration of Diazepam

A

IV,
Absorption in IM is unreliable=avoid

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17
Q

Metabolism and Excretion of Diazepam

A

M: liver
E: Renal

18
Q

SE of Diazepam

A

Sedation

19
Q

Caution in Diazepam

A

Can kill elderly patients

20
Q

What is Cyclobenzaprine

A

Is a centrally acting skeletal muscle relaxant with anti depressant activity
Is structurally similar to TCAs

21
Q

MOA of Cyclobenzaprine

A

Acts primarily within CNS at brain stem level
Reduces tonic somatic motor activity

22
Q

Indications of Cyclobenzaprine

A

Muscle spasm associated with acute, painful muscloskeletal conditions

23
Q

Is Cyclobenzaprine effective in muscle spasm of CNS origin

A

YES

24
Q

AE of Cyclobenzaprine

A

May increase HR

25
Q

What is Methacarbamol

A

A carbamate derivative of guaifenesin
Its a CNS depressant with sedative and musculoskeletal relaxant properties

26
Q

MOA of Methacarbamol

A

It has no direct action on the muscle, motor end plate or nerve fiber

27
Q

MOA of Methacarbamol as a CNS depressant

A

it blocks spinal polysynaptic reflexes, decreasing nerve transmission in spinal and supraspinal polysynaptic pathways

28
Q

Indications of Methacarbamol

A

Adjuvant in painful musculoskeletal conditions

29
Q

Metabolism and Excretion of Methacarbamol

A

M: Liver
E: Renal

30
Q

CI of Methacarbamol

A

Depression or taking CNS depressants

31
Q

SE of Methacarbamol

A

sedation
Dizziness
Lightheadedness
Drowsiness
Confusion

32
Q

What is Orphenadrine

A

is an antimuscarinic agent structurally related to diphenhydramine

33
Q

MOA of Orphanedrine

A

blocks muscarinic ACh receptors.
has central anticholinergic activity
block glutamate receptor

34
Q

How is Orphenadrine used?

A

used as a citrate salt (orphenadrine salt) to relieve pain due to muscle spasm.
Can be combined with paracetamol

35
Q

Indications of Orphenadrine

A

pain associated with muscle spasm,
tremor/stiffness in parkinsonian

36
Q

Metabolism and Excretion of Orphenadrine

A

M: liver
E: Renal

37
Q

CI of Orphenadrine

A

Myasthenia gravis

38
Q

SE of Orphenadrine

A

Sedation
Dry mouth
Dizziness

39
Q

MOA of Dantrolene

A

-acts directly on muscle
-blocks RYR1 receptor channel
-inhibits release of Ca from SR:
1. suppresses excitation-contraction coupling: relieving muscle spasticity
2. reduces Ca: relieving from malignant hyperthermia

40
Q

Indications of Dantrolene

A

Malignant hyperthermia
Muscle spasticity (neuronal origin)

41
Q

PK of Dantrolene
Absorption
Metabolism
Excretion

A

oral: slow and incomplete absorption
(IV is preferred)
M: liver
E: renal

42
Q

SE of Dantrolene

A

Drowsiness
Dizziness
Fatigue

Pharmacology (50 decks)

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