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Musculoskeletal - Pharmacology > Fibromyalgia and Spasticity > Flashcards

Fibromyalgia and Spasticity Flashcards

1
Q

Duloxentine
• Indication
• MOA
• Elmination
• Adverse Effects
• Contraindications

A

Indication
• Fibromyalgia

MOA:
• Serotonin-Norepinephrine Reuptake inhibitor w/ greater inhibition of SEROTONIN reuptake

Note: there is NO direct action upon ANY receptors themselves OR upon reuptake of Dopamine

Elmination:
• Liver metabolizes (CYP 2D6 used), Urinary Elmination of byproducts

Adverse Effects:
• CV effects: increased HR and BP
• SIADH - resulting in hyponatremia
• BBW = SUICIDAL IDEATION

Contraindications:
• Do not give in severe liver dysfunction or chronic EtOHism.
• No not give to ppl. with CLOSED ANGLE glaucoma
• Ppl. taking MAOIs

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2
Q

Milnacipran

A

Indication
• Fibromyalgia

MOA:
• Serotonin-Norepinephrine Reuptake inhibitor w/ greater inhibition of *NOREPINEPHRINE* reuptake

Note_: there is NO direct action upon ANY receptors themselves OR upon reuptake of Dopamine_

Elmination:
• Liver metabolizes (NO CYPs used), Urinary Elmination of byproducts

Adverse Effects:

  • *• CV effects**: increased HR and BP
  • *• SIADH** - resulting in hyponatremia
  • *• BBW** = SUICIDAL IDEATION

Contraindications:
• Do not give in severe liver dysfunction or chronic EtOHism.
• No not give to ppl. with CLOSED ANGLE glaucoma
• Ppl. taking MAOIs

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3
Q

Pregabalin
• Indication
• MOA
• Elmination
• Adverse Effects
• Contraindications

A

Indication:
• Fibromyalgia

MOA:
• Inhibition of the alpha-2-delta subunits of L-type Ca2+ channels leading to inhibition of the excitatory transmission by glutamate.

Elimination:
• Unchanged Renal Elmination - Reduce Dose in Renal Failure

Adverse Effects:
• Rebound on Withdrawl - Dependence Possible
• Additive Sedation with other CNS sedatives
• Suicidal thoughts/Depression
• Dizziness/Blurred Vision (especially the elderl y)

Contraindications:
• Reduce dose in renal failure and MONITOR SERUM CREATININE

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4
Q

Amitriptyline
• Indication
• Drug Class

A

Indication:
• Off-label use in fibromyalgia

Drug Class:
• Tricyclic Antidepressant

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5
Q

Cyclobenzprine
• Indication
• MOA
• Elmination
• Adverse Effects
• Contraindications

A

(aka Flexeril)

Indication:
• Fibromyalgia, Muscle Relaxer

MOA:
• Central Action (maybe at the brainstem)

Elmination:
• Enterohepatic Recirculation, EXTENSIVE hepatic metabolism (3A4, 1A2, 2D6). (old ppl. and EtOHics stay away)

Adverse Effects:
• Anticholinergic Action => Drowsiness, xerostomia, dizziness, fatigue, N/V/C, blurred vision
• Additive Effects with CNS depressants and EtOH
• Additive Effects with Anticholinergics
• PARALYTIC ILEUS (via anticholinergic effects) = MOST SIGNIFICANT EFFECT
• QT prolongation

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6
Q

Fluoxetine
• Indication
• MOA

A

Indication:
• Off-label use for fibromyalgia

MOA:
• Selective Serotonin Reuptake inhibitor

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7
Q

What are the only two differences between Duloxentine and Milnacipran?

A

Duloxentine:
• Metabolized by CYPs in the liver
• Greater Inhibition of Serotonin Reuptake than of NE reuptake

Milnacipran:
• Metabolized in the liver but NOT by CYPs
• Greater inhibition of NE uptake than Serotonin Reuptake

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8
Q

What are the 4 muscle relaxers we need to know for this block?

A
  • **Carisoprodol
  • Cyclobenzprine
  • Methocarbamol
  • Tizanidine**
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9
Q

Carisoprodol
• Indication
• MOA
• Elmination
• Adverse Effects
• Contraindications

A

Indication:
• Muscle Relaxer (fibromyalgia?)

MOA:
• CNS action in Reticular Activating System with NO DIRECT EFFECT on neuronal conduction, neuromuscular transmission, or muscle excitability. Relief is believed to be the result of Sedation.

Elimination:
• Extensive Hepatic CYP(2C19) Metabolism and Released in Urine - beware of anyone with hepatic or renal dysfunction that’s on this drug

Adverse Effects:
• Vertigo/Ataxia
• Temporary Vision loss
• Mydriasis/Orthostatic HTN
• Additive sedation when used with other sedatives

Contraindications:
• Watch out for Renal Dysfunction - MONITOR SERUM BUN/CREATININE

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10
Q

Methocarbamol
• Indication
• MOA
• Elmination
• Adverse Effects
• Contraindications

A

Indication:
• Muscle Relaxer - Muscle Spasm, Tetanus

MOA:
• Sedative action with altered pain perception, direct effects on muscle or excitation/contraction

Elmination:
• Hepatic Dealkylation and Hydroxylation with Urinary Elmination

Adverse Effects:
• Additive CNS depression
• Drowsiness, dizziness, lightheadedness, blurred vision, N/V

Contraindications:
• nothing too big just severe hepatic or renal dysfunction, but no risk big enough to warrant monitoring

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11
Q

Tizanidine
• Indication
• MOA
• Elmination
• Adverse Effects
• Contraindications

A

Indication:
• Muscle Relaxer - Multiple Sclerosis, Spasticity, Spinral Cord Trauma

MOA:
• Alpha-2 agonist on pre-synaptic receptor. Decreased activation in polysynaptic spinal cord motor neurons with reduction in muscle tone but not strength.

Elimination:
• Extensive First-Pass Metabolism
• Extensive Renal Excretion (watch out for the elderly)

Adverse Effects:
• Hepatotoxicity
• Hypotension with Reflex Tachycardiaand Reboud HTN on cessation (much less common than clonidine)
• Asthenia, Xerostomia, Dizziness, Sedation

Contradindications:
• People Need Regular LFTs
•Additive effects when given with other alpha-2 drugs (methyldopa, guanfacine, guanabenz)

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12
Q

Which of these drugs do you need to monitor Serum Creatinine and BUN for?

A
  • Carisoprodol
  • Pregabablin
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13
Q

What drugs are given for Spacticity? (4 of them)

A
  • Baclofen
  • Botulism Toxin
  • Dantrolene
  • Tizanidine
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14
Q

Balcofen
• Indication
• MOA
• Elmination
• Adverse Effects
• Contraindications

A

Indication:
• Muscle Spasticity (Multiple Sclerosis, Muscle Spasm, Spasticity, Spinal Cord Trauma)

MOA:
• GABAb agonist produces either: 1) inhibitory signals 2) hyperpolarizing signals
• Pain relief comes from inhibition of Substance P

Elimination:
• Orally active drug that undergoes extensive renal elimination - but no need for monitoring

Adverse Effects:
• BBW - AVOID ABRUPT discontinuance of therapy because of REBOUD NEURAL ACTIVITY => seizures, confusion, hallucinations, psychiatric disturbances, increased spasticity, RHABDOMYOLYSIS, death

  • Hypotenstion with other antihypertensive agents and MAOIs
  • Overall CNS Depression

Contraindications:
• Adjust dose of Anti-diabetic agents (blacofen may raise Blood Glucose)

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15
Q

Botulism Toxin
• Indication
• MOA
• Elmination
• Adverse Effects
• Contraindications

A
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16
Q

Dantrolene
• Indication
• MOA
• Dosing*
• Elmination
• Adverse Effects
• Contraindications

A

Indication:
• Muscle Spasticity (Multiple Sclerosis, Neuroleptic Malignant syndrome)
• Malignant Hyperthermia

MOA:
• Interferes with release of Ca2+ from the Sarcoplasmic Reticulum by acting on the RyR. By doing this it uncouples the excitation-contraction process.

Dosing:
• Oral or IV (solublized with surfactant + H2O, very alkaline) - Need for this delays administration

Elmination:
• Hepatic Metabolism with Renal Elimination

Adverse Effects:
• Vfib and CV collapse possible when given with CCBs to counteract malignant HTN.

• Drooling, Dysarthria, Enuresis, Myalgias, Backage
Contraindications:
• Crosses placenta to cause Floppy Child Syndrome
• Regular LFTs must be done

Musculoskeletal - Pharmacology (5 decks)

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