Diazepam Mechanism of Action

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LucrativeGorgon
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What is the main mechanism of action of diazepam on the CNS?

Increasing the inhibitory effects of GABA

How does diazepam exert its muscle relaxant properties?

By potentiating the inhibitory effect of GABA on alpha motor neuron activity

What is the effect of diazepam on GABA-induced inhibition?

It increases the inhibition

What is the consequence of diazepam's action on alpha motor neuron activity?

Decreased muscle contraction

What is the role of GABA in the mechanism of action of diazepam?

It is an inhibitory neurotransmitter

What is the primary advantage of administering baclofen intrathecally compared to oral administration?

Reduced systemic side effects

What is the purpose of the programmable pump in intrathecal baclofen administration?

To deliver the drug at a slow, continuous rate

What is the location of the open end of the catheter in intrathecal baclofen administration?

Subarachnoid space

Why is intrathecal administration of baclofen effective with smaller drug doses?

Because the drug is delivered directly to the spinal cord

What is the typical location of the programmable pump in intrathecal baclofen administration?

Abdominal wall

What is the primary goal of adjusting the rate of infusion over time in intrathecal baclofen administration?

To achieve the best clinical reduction in spasticity

Study Notes

Diazepam Mechanism of Action

  • Diazepam works by increasing the central inhibitory effects of gamma-aminobutyric acid (GABA) on the CNS.
  • It binds to receptors located at GABAergic synapses and increases the GABA-induced inhibition at that synapse.

Muscle Relaxant Mechanism

  • Diazepam acts as a muscle relaxant by potentiating the inhibitory effect of GABA on alpha motor neuron activity in the spinal cord.
  • Some of its muscle relaxant properties may derive from the drug's ability to produce a more generalized state of sedation.

Additional Effects

  • Diazepam also exerts some supraspinal sedative effects.

Baclofen Administration

  • Oral administration is the most common method of administering baclofen to patients.
  • Intrathecal administration is an alternative method for patients with severe, intractable spasticity.

Intrathecal Administration

  • Involves delivering the drug directly into the subarachnoid space surrounding a specific level of the spinal cord.
  • Benefits include:
    • Increased drug effectiveness with smaller doses.
    • Fewer systemic side effects since the drug remains close to the spinal cord rather than circulating in the bloodstream.

Intrathecal Baclofen Infusion System

  • Consists of a small catheter implanted surgically with the open end in the subarachnoid space.
  • The other end is attached to a programmable pump implanted subcutaneously in the abdominal wall.
  • The pump delivers the drug at a slow, continuous rate, which is adjusted over time to achieve the best clinical reduction in spasticity.

Learn how diazepam affects the central nervous system and its usage as an anti-anxiety drug. Understand its mechanism of action and its role as a muscle relaxant.

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