PT6 JAM - exam 1 (steroids, muscle relaxants pharmacology study guide)

glutamate

main target excitatory neurotransmitter to inhibit to terminate skeletal muscle spasms

hyperpolarization

_______ is good for reducing activity as it makes inside of neuron more negative, which inhibits neuron + makes less likely to fire action potential

depolarization

______ is bad for reducing activity as it makes inside of neuron less negative, which excites neuron + makes more likely to fire action potential

chloride

major ion that suppresses neurotransmitter release when ion enters neuron

calcium

major ion that triggers neurotransmitter release when ion enters neuron

benzodiazepines

MOA: drug class that works in brain + spinal cord to increase GABAa receptor response to GABA binding

baclofen

MOA: possibly activates GABAb receptors; enhances K+ efflux leading to hyperpolarization

tizanidine

MOA: dual effects:

1. activates alpha-2 receptors on presynaptic neurons

2. enhances K+ efflux leading to hyperpolarization + inhibits voltage-gated Ca channels

cyclobenzaprine

MOA: increased NE release in dorsal horn of spinal cord; acts like TCAs

(mechanism not fully understood)

methocarbamol

MOA: unknown; likely general CNS depression with no direct action on skeletal muscle

dantrolene

MOA: blocks ryanodine receptor in skeletal muscle, directly reducing muscle contractile strength via reducing CA release

(only drug that works directly in skeletal muscle)

chronic

developing Cushing's-like symptoms is associated with ________ steroid use

sudden discontinuation

developing Addison's Disease-like symptoms is associated with _______ steroids

diabetes, osteoporosis, insomnia/depression, increased platelets

list the remaining symptoms of Cushing's Syndrome:

1. muscle wasting

2. fat redistribution (moon facies, trunk, back)

3. plethoric face (red + swollen)

4. skin thinning + head alopecia (+ hair growth in women)

5. ?

6. ?

7. ?

8. ?

lethargy, joint/muscle pain, postural hypotension

list the remaining symptoms of Addison's Disease:

1. anorexia

2. nausea/vomiting

3. weight loss

4. ?

5. ?

6. ?

transcription

steroids take several hours for significant effect due to slow penetration into nucleus + time for ______ to occur

nucleus

MOA: corticosteroids (inhibition of proinflammatory gene transcription + activation of anti-inflammatory gene transcription) work within the _____ of cells

C21

mineralocorticoid activity structural groups:

OH group required off _____

C16

mineralocorticoid activity structural groups:

MC removed by ______ groups

C9 fluorination

mineralocorticoid activity structural groups:

MC enhanced by ____