Skeletal Muscle Relaxants and Antimigraine Agents Flashcards
Baclofen
Lioresal, Ozobax
Carisoprodol
Soma, Vanadom
C-IV
Cyclobenzaprine
Flexeril
Metaxalone
Skelexin
Methocarbamol
Robaxin
Tizanidine
Zanaflex
Eletriptan
Relpax
Rizatriptan
Maxalt
Sumatriptan
Imitrex
Therapeutic Class - Baclofen
Centrally acting skeletal muscle relaxant
Therapeutic Class - Carisoprodol
Centrally acting skeletal muscle relaxant
Therapeutic Class - Cyclobenzaprine
Centrally acting skeletal muscle relaxant
Therapeutic Class - Metaxalone
Centrally acting skeletal muscle relaxant
Therapeutic Class - Methocarbamol
Centrally acting skeletal muscle relaxant
Therapeutic Class - Tizanidine
Centrally acting skeletal muscle relaxant
Alpha-2 agonist
Therapeutic Class - Eletriptan
Antimigraine serotonin receptor agonist
Therapeutic Class - Rizatriptan
Antimigraine serotonin receptor agonist
Therapeutic Class - Sumatriptan
Antimigraine serotonin receptor agonist
Dosage Forms - Baclofen
Tablet: 5 mg, 10 mg, 20 mg
Dosage Forms - Carisoprodol
Tablet: 250 mg, 350 mg
Dosage Forms - Cyclobenzaprine
Tablet: 5 mg, 7.5 mg, 10 mg
ER Capsule: 15 mg, 30 mg
Dosage Forms - Metaxalone
Tablet: 400 mg, 800 mg
Dosage Forms - Methocarbamol
Tablet: 500 mg, 750 mg
Dosage Forms - Tizanidine
Tablet: 2 mg, 4 mg
Capsule: 2 mg, 4 mg, 6 mg
Dosage Forms - Eletriptan
Tablet: 20 mg, 40 mg
Dosage Forms - Rizatriptan
Tablet: 5 mg, 10 mg
Orally-Disintegrating Tablet: 5 mg, 10 mg
Dosage Forms - Sumatriptan
Tablet: 25 mg, 50 mg, 100 mg Nasal Solution: 5 mg/actuation Nasal Exhaler Powder: 11 mg/nosepiece Solution for Subcutaneous Injection: 3 mg/0.5 mL, 4 mg/0.5 mL, 6 mg/0.5 mL Transdermal (patch): 6.5 mg/4 h
MOA - Baclofen
Inhibits both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect
Analogue of γ-aminobutyric acid (GABA), but there is no conclusive evidence that actions on GABA systems are involved in the production of its clinical effects.
MOA - Carisoprodol
Block interneuronal activity in the descending reticular formation and spinal cord causing muscle relaxation
MOA - Cyclobenzaprine
Relieves skeletal muscle spasm of local origin without interfering with muscle function.
Ineffective in muscle spasm due to CNS disease
Evidence suggests that the net effect of cyclobenzaprine is a reduction in tonic motor activity, influencing both gamma (𝛾) and alpha (α) motor systems.
MOA - Metaxalone
Not well established likely due to CNS depression. No direct action on the contractile mechanism of striated muscle, the motor end plate, or the nerve fiber.
MOA - Methocarbamol
Not well established likely due to CNS depression. No direct action on the contractile mechanism of striated muscle, the motor end plate, or the nerve fiber.
MOA - Tizanidine
Imidazole derivative, structurally unrelated to other muscle relaxants - centrally acting muscle relaxant. Agonist of alpha-2 adrenergic receptors leads to decreased spasticity by increasing presynaptic inhibition. NO antihypertensive properties
MOA - Eletriptan
Binds with high affinity to serotonin (5-HT) subtypes 1B, 1D, and 1F receptors.
No significant affinity or pharmacological activity at adrenergic α1, α2, or β; dopaminergic D1or D2; muscarinic; or opioid receptors.
Serotonin receptor agonists are believed to be effective in migraine, either through vasoconstriction (via activation of 5-HT1receptors located on intracranial blood vessels) or through activation of 5-HT1receptors on sensory nerve endings in the trigeminal system, resulting in the inhibition of proinflammatory neuropeptide release.
MOA - Rizatriptan
Binds with high affinity to serotonin (5HT) receptor subtypes 1B and 1D.
Serotonin receptor agonists are believed to be effective in migraine either through vasoconstriction (via activation of 5-HT1receptors located on intracranial blood vessels) or through activation of 5-HT1receptors on sensory nerve endings in the trigeminal system resulting in the inhibition of proinflammatory neuropeptide release.
MOA - Sumatriptan
Binds with high affinity to serotonin (5-HT) subtypes 1B, 1D, and 1F receptors
No significant affinity or pharmacologic activity at adrenergic α1, α2, or β; dopaminergic D1or D2; muscarinic; or opioid receptors.
Serotonin receptor agonists are believed to be effective in migraine either through vasoconstriction (via activation of 5-HT1receptors located on intracranial blood vessels) or through activation of 5-HT1receptors on sensory nerve endings in the trigeminal system resulting in the inhibition of proinflammatory neuropeptide release.
FDA-Approved Indications - Baclofen
- Spasticity: 5 mg TID (can increase by 5 mg/dose every 3 days) (adult MDD = 80 mg)
FDA-Approved Indications - Carisoprodol
- Disorder musculoskeletal system: 250-350 mg TID and QHS
FDA-Approved Indications - Cyclobenzaprine
- Skeletal muscle spasm:
a) IR: 5 mg TID (can titrate up to 10 mg TID) and treat 2-3 weeks
b) ER: 15 mg QD (can titrate up to 30 mg QD)
FDA-Approved Indications - Metaxalone
- Musculoskeletal pain or spasm: 800 mg TID-QID
FDA-Approved Indications - Methocarbamol
- Musculoskeletal pain or spasm: 1500 mg QID for 48-72 hours (can titrate to 750 mg q4h or 1500 mg TID or 1000 mg QID)
FDA-Approved Indications - Tizanidine
- Muscle spasticity: 2 mg up to TID (may titrate to 8 mg q6-8h; MDD = 36 mg)