Name the Spasmolytics /Antispasmodics
- Chronic CNS actions (4)
- Chronic Muscle Action (2)
- Acute Use (1)
- Baclofen, Diazepam, Tizandine, Cyclobenzaprine
- Dantrolene, Botulism
- Cyclobenzaprine
Spasmolytics treat 2 conditions
• Spasticity from _____ motor neuron lesions (spasmolytics)
Spasms from _______ musculoskeletal condtitions
- Upper
* Peripheral
What is the site of Spasmolytic action?
GABA receptors
• Which medication is centrally acting, inhibits spinal motor neurons by decreasing excitatory trasnmitters?
• Baclofen - GABA receptor for pain
• What is the use of Baclofen?
Severe spasticity from Cerebral palsy, multiple sclerosis, or Stroke
• Which medication is a central acting, is a GABA enhancer, and causes Central sedation and inhibits primary motor afferent in spinal cords
• Diazepam
- What is Diazepam used for?
- Where is Diazepam metabolized
- What are adverse effects of Diazepam
- Spasm from MS, CVA, ALS
- Liver = Hepatic metabolism
- Sedation, Antegrade amnesia, Addictive
- What drug inhibits motor reflex outputs, is an Alpha 2 Agonist in the spinal cord
- Is used to treat MS, CVAs, and ALS
• Tizanidine
- Where is Tizanidine metabolized.
* What are Tizanidine’s 3 ADEs?
- Renal and Hepatic elimination.
* (SHoW) Sedation, HoTN, Weakness
- What is Cyclobenzaprine used for?
- Where is Cyclobenzaprine metabolized
- What are adverse effects of Cyclobenzaprine
- Only Acute spasms from muscle injury or inflammation
- Hepatic metabolism
- Strong Antimuscarinic = Dumb as a bitch + ocular effects
• What are the antispasmodic drugs?
CCOMM
(CCOMM) • Carisoprodol (Soma) • Chlorzoxazone • Orphenadrine • Metazalone • Methocarbamol
What do the Antispasmodics?
• Acute muscle spams relief
- What is Carisoprodol drug classification? (Car ->Mepro -> extensive withdrawal sxs)
- How can you limit these sxs?
- Schedule IV: metabolized to meprobamate (another Class IV) which is a central muscle relaxant.
- Taper over 14 days
• What drug blocks RyR1 Ca channels in the sacroplasmic reticulum in skeletal muscle, and Weakens muscle contraction due to few myosin-actin
• Dantrolene
• What is Dantrolene used for?
- Malignant Hyperthermia (IV)
* Spasm due to Cerebral Palsy, SCI, MS
• What is botulism used for?
• Cleaves fusion proteins in nerve ending = Flaccid paralysis
• F/T: Botulism is used for cerebral palsy spasm, MS, Overactive bladder, Migraine?
True
