Skeletal Muscle Relaxants and Antimigraine Agents Flashcards

Question

Dosage Forms - Eletriptan

Answer 1

Tablet: 20 mg, 40 mg

Answer 2

Tablet: 5 mg, 10 mg | Orally-Disintegrating Tablet: 5 mg, 10 mg

Answer 3

``` 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 ```

Answer 4

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.

Answer 5

Block interneuronal activity in the descending reticular formation and spinal cord causing muscle relaxation

Answer 6

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.

Answer 7

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.

Answer 8

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.

Answer 9

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

Answer 10

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 D1 or D2; muscarinic; or opioid receptors. Serotonin receptor agonists are believed to be effective in migraine, either through vasoconstriction (via activation of 5-HT1 receptors located on intracranial blood vessels) or through activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system, resulting in the inhibition of proinflammatory neuropeptide release.

Answer 11

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-HT1 receptors located on intracranial blood vessels) or through activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system resulting in the inhibition of proinflammatory neuropeptide release.

Answer 12

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 D1 or D2; muscarinic; or opioid receptors. Serotonin receptor agonists are believed to be effective in migraine either through vasoconstriction (via activation of 5-HT1 receptors located on intracranial blood vessels) or through activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system resulting in the inhibition of proinflammatory neuropeptide release.

Answer 13

1. Spasticity: 5 mg TID (can increase by 5 mg/dose every 3 days) (adult MDD = 80 mg)

Answer 14

1. Disorder musculoskeletal system: 250-350 mg TID and QHS

Answer 15

1. 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)

Answer 16

1. Musculoskeletal pain or spasm: 800 mg TID-QID

Answer 17

1. 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)

Answer 18

1. Muscle spasticity: 2 mg up to TID (may titrate to 8 mg q6-8h; MDD = 36 mg)

Answer 19

1. Migraine: 20-40 mg at onset of migraine, may repeat in 2 hours PRN (Max single dose: 40 mg; MDD = 80 mg)

Answer 20

1. Migraine (adults): 5-10 mg at onset of migraine, may repeat after 2 h PRN (MDD = 30 mg) 2. Migraine (children >6 years old and adolescents <40 kg): 5 mg at onset of migraine, multiple doses in a 24 hour period NOT recommended

Answer 21

1. Migraine a) Oral: 25-100 mg at onset of migraine, may repeat after 2h PRN (MDD = 200 mg) b) Nasal: 5-20 mg in 1 nostril, may repeat after 2h (MDD = 40 mg) c) Subcutaneous: inject 6 mg (MDD = 12 mg) d) Transdermal: apply 1 patch, may apply a 2nd patch after 2h (MDD = 2 patches) 2. Cluster headaches: 6 mg SQ once (MDD = 12 mg)

Answer 22

1. Intractable hiccoughs: 5-10 mg BID (increase to 15-45 mg/day in 3 divided doses OR 10-20 mg BID-TID) 2. Alcohol use disorder: 5 mg TID (may increase to 10 mg TID after 3-5 days; MDD = 60 mg) 3. Muscle spasm and/or musculoskeletal pain: 5 mg TID PRN

Answer 23

1. Temporomandibular Joint Disorder (TMJ): a) IR: 10 mg QD x 3 weeks 2. Fibromyalgia: 5-10 mg QHS (may titrate to 10-40 mg in 1 to 3 divided doses)

Answer 24

1. Acute low back pain: 2-4 mg q6-12h (MDD = 24 mg) alone or in combination with NSAIDs

Answer 25

Absorption: F = 100% Distribution: Vd = 59.1 L; 30% protein bound Metabolism: Limited Elimination: Renal 60-80%; T1/2 = 3-7 hours Hepatic Dose Adjustment: None Renal Dose Adjustment: Monitor

Answer 26

``` Absorption: unknown Distribution: unknown Metabolism: hepatic; major CYP2C19 substrate Elimination: renal; T1/2 = 8 hours Hepatic Dose Adjustment: low and slow Renal Dose Adjustment: none ```

Answer 27

``` Absorption: F = 33-55% Distribution: 93% protein bound Metabolism: extensive hepatic; CYP1A2 substrate Elimination: renal 50%; T1/2 = 18 hours Hepatic Dose Adjustment: a) Mild: 5 mg QD (IR; avoid ER) b) Severe: avoid Renal Dose Adjustment: none ```

Answer 28

``` Absorption: ?? food enhances Distribution: Vd = 800 L Metabolism: hepatic; multiple CYP substrate Elimination: renal; T1/2 = 8-9 hours Hepatic Dose Adjustment: low and slow Renal Dose Adjustment: low and slow ```

Answer 29

Absorption: ?? Distribution: protein-binding 45-50% Metabolism: hepatic via dealkylation and hydroxylation Elimination: renal (as metabolites); T1/2 = 1-2 hours Hepatic Dose Adjustment: low and slow Renal Dose Adjustment: none

Answer 30

Absorption: F = 40%, food increases tablet absorption and decreases capsule absorption; hepatic 1st pass Distribution: Vd = 2.4 L/kg; 30% protein bound Metabolism: extensive hepatic; CYP1A2 substrate Elimination: renal 60%; T1/2 = 2 hours Hepatic Dose Adjustment: not recommended Renal Dose Adjustment: CrCl <25 mL/min = reduce dose

Answer 31

Absorption: F = 50%; high fat food increases 20-30% Distribution: Vd = 138 L Metabolism: hepatic; CYP3A4 Elimination: nonrenal 90%; T1/2 = 4 hours Hepatic Dose Adjustment: severe = AVOID Renal Dose Adjustment: none

Answer 32

``` Absorption: F = 45% Distribution: Vd = 110-140 L Metabolism: hepatic via MAO Elimination: renal 82%, feces; T1/2 = 2-3 hours Hepatic Dose Adjustment: none Renal Dose Adjustment: none ```

Answer 33

Absorption: F = 15%, high fat food increases Distribution: Vd = 2.4 L/kg; 14-21% protein bound Metabolism: hepatic via MAO Elimination: renal 60%; T1/2 = 2.5 hours Hepatic Dose Adjustment: max single dose = 50 mg Renal Dose Adjustment: none

Answer 34

1. CYP1A2 inducers/inhibitors = monitor 2. CNS depressants (opioids, benzodiazepines, alcohol) = AVOID 3. Anticholinergic agents = AVOID

Answer 35

1. CYP2C19 inducers/inhibitors = monitor | 2. CNS depressants (opioids, benzodiazepines, alcohol) = AVOID

Answer 36

1. CNS depressants = AVOID

Answer 37

1. CNS depressants = AVOID

Answer 38

1. CYP1A2 inducers/inhibitors = do not co-administer with inhibitors 2. CNS depressants = AVOID 3. Phenytoin/Fosphenytoin = monitor

Answer 39

1. CYP3A4/5 = monitor 2. SSRIs = AVOID 3. Other 5-HT agonists = contraindicated if administered within 24 hours

Answer 40

1. SSRIs = AVOID 2. Other 5-HT agonists = contraindicated if administered within 24 hours 3. Ergot alkaloids = contraindicated 4. MAOI = contraindicated

Answer 41

1. SSRIs = AVOID 2. Other 5-HT agonists = contraindicated if administered within 24 hours 3. Ergot alkaloids = contraindicated 4. MAOI = contraindicated

Answer 42

Pregnancy: risk Lactation: probably compatible

Answer 43

Pregnancy: no data Lactation: probably compatible

Answer 44

Pregnancy: low risk? Lactation: probably compatible

Answer 45

Pregnancy: no data Lactation: potential toxicity

Answer 46

Pregnancy: low risk Lactation: probably compatible

Answer 47

Pregnancy: risk Lactation: potential toxicity

Answer 48

Pregnancy: moderate risk Lactation: compatible

Answer 49

Pregnancy: moderate risk Lactation: probably compatible

Answer 50

Pregnancy: moderate risk Lactation: probably compatible

Answer 51

Avoid abrupt discontinuation of oral or intrathecal product

Answer 52

1. Carisoprodol 2. Cyclobenzaprine 3. Metaxalone 4. Methocarbamol

Answer 53

1. Hypersensitivity to meprobamate | 2. Acute intermittent porphyria

Answer 54

1. Concomitant MAOI use 2. Heart failure 3. Acute coronary phase of AMI 4. Heart block 5. Hyperthyroidism

Answer 55

1. Significantly impaired renal or hepatic function

Answer 56

1. Concurrent use with CYP1A2 inhibitors

Answer 57

Cerebrovascular syndromes, hemiplegic or basial migraine, ischemic bowel disease, ischemic heart disease, peripheral vascular disease, severe hepatic impairment, uncontrolled HTN

Answer 58

Cerebrovascular syndromes, hemiplegic or basial migraine, ischemic bowel disease, ischemic heart disease, peripheral vascular disease, severe hepatic impairment, uncontrolled HTN, MAOIs, ergot alkaloids

Answer 59

Common: Nausea, asthenia, dizziness, somnolence, confusion Less common: Constipation, fatigue, hypotension, shivering, urinary symptoms, peripheral edema, difficulty in micturition Rare but serious: Slowed or difficult breathing when used in combination with opioids, pneumonia, GI hemorrhage, seizure

Answer 60

Common: drowsiness, dizziness Less common: headache Rare but serious:Slowed or difficult breathing when used in combination with opioids, seizure, drug dependence, withdrawal symptoms upon discontinuation after chronic use

Answer 61

Common: Xerostomia, headache, dizziness, drowsiness Less common: onstipation, indigestion, nausea, pharyngeal dryness, asthenia, confusion, blurred vision Rare but serious: Cardiac dysrhythmia, cholestasis, hepatitis, jaundice, anaphylaxis, immune hypersensitivity reaction, slowed or difficult breathing when used in combination with opioids

Answer 62

Common: dizziness Less common: N/V, headache, somnolence Rare but serious: Hemolytic anemia, leukopenia, jaundice, immune hypersensitivity reaction, maculopapular rash, slowed or difficult breathing when used in combination with opioids

Answer 63

Common: somnolence Less common: Flushing, pruritus, rash, urticaria, nausea, vomiting, dizziness, headache, nystagmus, vertigo, blurred vision, conjunctivitis Rare but serious: Bradyarrhythmia, hypotension, syncope, leukopenia, anaphylactoid reaction, slowed or difficult breathing when used in combination with opioids

Answer 64

Common: Hypotension, xerostomia, asthenia, dizziness, somnolence, muscle weakness Less common: Constipation, vomiting, dyskinesia, amblyopia, feeling nervous, syncope, depression Rare but serious: AMI, thrombocytopenia, hepatitis, PE, hypersensitivity, death, slowed or difficult breathing when used in combination with opioids

Answer 65

Common: weakness Less common: Nausea, asthenia, dizziness, somnolence Rare but serious: Angina, cardiac dysrhythmia, coronary arteriosclerosis, heart block, HTN, acute myocardial infarction, aphasia, cerebral ischemia, stroke, dystonia, hemiplegia, neuropathy, transient ischemic attack, oculogyric crisis

Answer 66

Common: none Less common: Nausea, asthenia, dizziness, somnolence Rare but serious: Angina, cardiac dysrhythmia, coronary arteriosclerosis, heart block, HTN, acute myocardial infarction, aphasia, cerebral ischemia, stroke, dystonia, hemiplegia, neuropathy, transient ischemic attack, oculogyric crisis

Answer 67

Efficacy: Reduction in muscle spasm, passive limb movement and pain relief Toxicity: Severe dizziness, confusion, sedation, or rebound spasticity occurs.

Answer 68

Efficacy: Reduction in pain and muscle spasms Toxicity: Idiosyncratic symptoms such as extreme weakness, transient quadriplegia, dizziness, confusion occur within minutes or hours after first dose

Answer 69

Efficacy: Reduction in pain and muscle spasms Toxicity: Sx of Hepatic failure

Answer 70

Efficacy: Reduction in pain and muscle spasms Toxicity: Monitor LFTs and CBC

Answer 71

Efficacy: Reduction in pain and muscle spasms Toxicity: Idiosyncratic symptoms such as extreme weakness, transient quadriplegia, dizziness, and confusion occur within minutes or hours after 1st dose; Vital signs

Answer 72

Efficacy: Reduction in pain and muscle spasms & in passive limb movement Toxicity: Monitor BP, LFTs, SCr, and CBC

Answer 73

Efficacy: Resolution of signs of migraine headache Toxicity: Ischemic bowel disease (eg, sudden severe abdominal pain, bloody diarrhea) or peripheral vascular disease (eg, Raynaud syndrome), serotonin syndrome (eg, agitation, hallucinations, tachycardia, hyperreflexia, incoordination, diarrhea, nausea), ischemic cardiac syndrome, or hypertensive crisis

Answer 74

Counseling: Caution when operating motor vehicles or dangerous machinery due to sedation. CNS effects may be additive when used with alcohol or other CNS depressants. Pearls: Implantable pumps that administer baclofen intrathecally are also available for patients with spasticity. Constipation occurs in 100% of patients undergoing intrathecal administration, and abrupt discontinuation of intrathecal therapy (intentional or inadvertent) can result in seizures, coma, and death. Avoid concomitant use with opioids.

Answer 75

Counseling: Avoid consuming alcohol. Avoid activities requiring mental alertness or coordination until drug effects are known, as drug may cause dizziness or sedative effects. Patients withdrawing from prolonged therapy should be monitored carefully for withdrawal symptoms, including seizures. Pearls: Carisoprodol should be used for only short periods (up to 2 or 3 wk). It was approved in 1959, so limited pharmacologic and kinetic data available. May require tapering at discontinuation after chronic use. Avoid concomitant use with opioids.

Answer 76

Counseling: Avoid activities requiring mental alertness or coordination until drug effects are known, as drug may cause dizziness or sedative effects. Take extended-release capsule same time each day. Pearls: Cyclobenzaprine should be used for only short periods (up to 2-3 wk). Avoid concomitant use with opioids. Use with caution in patients with glaucoma, increased IOP, urinary retention, etc, as cyclobenzaprine has anticholinergic-like effects. Avoid use in elderly; may be more sensitive to effects.

Answer 77

Counseling: Avoid activities requiring mental alertness or coordination until drug effects are known, as drug may cause dizziness or sedative effects. Pearls: Metaxalone should be used for only short periods (up to 2 or 3 wk). Not for use in children <12 y of age. Use with caution in elderly who may be more susceptible to adverse effects. Should avoid concomitant use with opioids.

Answer 78

Counseling: Avoid activities requiring mental alertness or coordination until drug effects are known, as drug may cause dizziness or sedative effects. Pearls: Methocarbamol should be used for only short periods (up to 2 or 3 wk). Drug may color urine brown, black, or green. Injectable form available, used for spasticity associated with tetanus. Should avoid concomitant use with opioids.

Answer 79

Counseling: Be cautious of risk of dizziness and somnolence when initiating therapy; do not drive until effects of drug are known. Rise slowly from a lying/sitting position, as this drug may cause hypotension. May cause xerostomia (dry mouth) and asthenia (weakness). Pearls: While this drug may be taken with or without food, patients should take the drug in the same way (fasting or fed) every time to avoid inconsistent absorption patterns and resulting changes in efficacy and adverse effects. Effect of food on extent of absorption differs for tablets and capsules. Abrupt discontinuation can cause rebound HTN and tachycardia. Taper dose by 2-4 mg/d if used at high dose (20-28 mg daily) or for an extended period of time. Should avoid concurrent use with opioids. Capsules and tablets are not interchangeable.

Answer 80

Counseling: Avoid activities requiring mental alertness or coordination until drug effects are realized, as this drug may cause dizziness or somnolence Pearls: These agents are not for prophylaxis—these are used for the treatment of acute migraine headache. Several serotonin agonists (“triptans”) exist for migraine, administered via a variety of routes (oral, inhaled, injected). Each differs in onset and duration of action. If an agent is ineffective at max dose, recommend changing agents or route. Instruct patient to take a 2nd dose ≥2 h after the 1st if needed, but no >80 mg/d. Overuse of acute migraine medications can lead to medication overuse headache that may present similarly to migraine; may require detoxification including management of withdrawal symptoms.

Answer 81

Counseling: Avoid alcohol, CNS depressants. Caution with driving and other tasks requiring alertness. Allow disintegrating tablet to dissolve on tongue and then swallow, do not chew. Pearls: Serotonin agonists are not for prophylaxis; only for the treatment of acute migraine headache. Several serotonin agonists (“triptans”) are available for migraine, administered via a variety of routes (oral, inhaled, and injected). Each differs in onset and duration of action. If one agent is ineffective at max dose, recommend changing agents or route.

Answer 82

Counseling: Avoid activities requiring mental alertness or coordination until drug effects are realized, as this drug may cause dizziness or somnolence. Pearls: Sumatriptan is also available in formulations for injectable administration, and as an oral dosage form in combination with naproxen. These agents are not for prophylaxis; only for the treatment of acute migraine headache. Several serotonin agonists (“triptans”) exist for migraine, administered via a variety of routes (oral, inhaled, and injected). Each differs in onset and duration of action. If 1 agent is ineffective at max dose, recommend changing agents or route.