Module 4 Chapter 22/27 Flashcards
True or False:
Drugs that treat spasticity don’t relieve acute muscle spasm and drugs that treat acute muscle spasm don’t treat muscle spasticity
True they are not interchangeable
THE ONLY EXCEPTION IS DIAZEMPAM (VALIUM)
What is spasticity?
movement of group disorders of the CNS; characteristics are heightened muscle tone, spasm, and loss of dexterity
what are the 4 drugs that relieve spasticity?
All act on the CNS except which drug?
Baclofen, Diazepam, Dantrolene, and Tizanidine
Dantrolene is the only one that does not act within the CNS; it acts on skeletal muscle
What is Baclofen’s mechanism of action?
acts within the spinal cord to suppress hyperactivity reflexes
thought to mimic actions of GABA on spinal movement
Does baclofen cause muscle weakness?
It does not decrease muscle strength which is why its preferred over dantrolene
what are the CNS and anticholinergic adverse effects of baclofen?
CNS effects: drowsiness, dizziness, weakness, fatigue
- this decreases with continued use
- can cause coma and respiratory depression if overdose occurs
anticholinergic effects: can cause urinary retention, hypotension can also occur
How should you discontinue baclofen? and WHY?
it should be d/c slowly over 1-2 weeks
abrupt withdrawal can cause visual hallucinations, paranoid ideations, and seizures
what are contraindications for patients taking baclofen?
Should not be given with alcohol, opioids, 1st gen antihistamines, or benzos because it can cause severe respiratory depression.
Don’t give to schizophrenia pts b/c they could have an exacerbation psychosis and confusion
What is important to know about Diazepam (valium)?
it is used to treat both muscle spasticity and muscle spasm
what is the generic name for Zanaflex?
Tizanidine
what is the mechanism of action for Tizanidine?
promotes inhibition of spasticity by acting as an agonist at presynaptic alpha 2 receptors
in discontinuing Tizanidine you should taper the dose because of?
rebound hypertension
taking food with Tizanidine does what?
increases bioavailability
What is an adverse effect of TIzanidine?
can cause hallucinations and psychosis, more sedating than most
What is dantrolene’s mechanism of action?
Acts directly on skeletal muscles and relieves spasms by suppressing calcium (causes muscle to contract less)
What is significant about dantrolene in regards to muscle spasticity?
It can cause a significant reduction in strength
When should dantrolene be discontinued?
If beneficial effects don’t develop within 45 days the med should be d/c
What are the common adverse effects of dantrolene?
It can cause liver damage or hepatotoxicity which is common in women over 35. Rare in children
Muscle weakness, drowsiness, diarrhea, dysphasia and erectile dysfunction can occur
what are muscle spasms?
its an involuntary contraction of a muscle or a muscle group.
they can be painful and reduce ability to function
what are the two drug classes used to treat muscle spasms?
analgesics (NSAIDs) and centrally acting muscle relaxants
what is the drug of choice for acute muscle spasms?
Cyclobenzaprine
What 3 adverse effects does cyclobenzaprine have?
CNS depressant (drowsiness, dizziness, and fatigue are common though diminish over time
Anticholinergic effects: dry mouth, blurred vision, photophobia, urinary retention, and constipation.
Cardiac rhythm disturbances: can cause sinus tachycardia and conduction delays (similar to TCAs)
what drug class is a major contraindication for cyclobenzaprine?
MAOIs, SSRIs, SNRIs, and TCAs as they can cause serotonin syndrome
how long should MOAIs be discontinued when about to use MAOIs.
MAOI should be discontinued for at least 2 weeks before therapy begins as serotonin syndrome may result.
what is the interaction between cyclobenzaprine and alcohol?
This can lead be an additive effect to CNS depression when used with other CNS depressants and alcohol.
which 2 drugs of the anti-spasmodic class have significant anticholinergic effects?
Cyclobenzaprine and orphenadrine
which antispasmodic turns the urine a orange to purple-red color but is harmless and can cause fatal hepatic necrosis
Chlorzoxazone
which anti-spasmodic turns the urine brown black to dark green?
methocarbamol
which 2 drugs can cause liver damage among the antispasmodics and the anti-spastic drugs?
Tizanidine and Metaxalone
what drugs can’t be used for muscle spasm and spasticity in children?
think COT
Chlorzoxazone
Orphenadrine
Tizanidine
what drug is safe to use for pregnancy when considering use for muscle spasticity and muscle relaxant?
cyclobenzaprine
what 2 drugs of the anti-spasmodic and the anti-spasticity are not safe in pregnancy?
Baclofen and diazepam
which drugs are used for breast feeding among the anti-spastic and anti-spasmodic drugs?
ALL OF THEM
These drugs treat what? muscle spasticity or muscle spasms?
Cyclobenzaprine
Tizanidine
Metaxalone
Chlorzoxazone
Muscle spasm
These drugs treat what? Muscle spasticity or Muscle spasm?
Baclofen
Valium
Dantrolene
Muscle spasticity
Symptoms of depression must be going on for how long?
At least two weeks
symptoms of depression must be present for how long?
at least 2 weeks
what is depression caused by?
by a functional deficiency of monoamine neurotransmitters (norepinephrine, serotonin, or both)
True or false: drugs are the major therapy for depression but benefits are limited mainly to patients with severe depression.
TRUE
pts who have mild to moderate depression, antidepressants have little or no beneficial effect for them
what are the 5 major classes of antidepressants?
SSRIs, SNRIs, TCA, MAOIs, AND ATYPICAL ANTIDEPRESSANTS
What are three basic considerations of antidepressants?
Symptoms resolve slowly for all
Initial response develops in 1 to 3 weeks and a maximum response is not seen until 12 weeks
Selection is based on tolerability and safety
For anti-depressant, failure should not be considered until the drug has been taken for how long?
At least one month
What are the first choice for anti-depressant drugs? List them in order
SSRIs, SNRIs, Bupropion, and mirtazapine
For patient experiencing fatigue, they should use drugs that cause CNS stimulation which would be which drugs? List 2
Fluoxetine and bupropion
Patient experiencing insomnia, they should use drugs that caused sedation. What anti-depressant would be good for this patient?
Mirtazapine
Patients that are experiencing sexual dysfunction Should use drugs that enhance libido. What antidepressant would be best?
Bupropion
Patients that experience chronic pain and have depression, they should be given drugs that relieve pain. Which drugs should they be given? It’s one drug specifically and a class of antidepressants
Duloxetine and tricyclic antidepressant
For patients given a anti-depressant, how long should be given to assess efficacy of the drug?
At least 4 to 8 weeks to assess efficacy
If the medication is not effective for antidepressants what are 4 options in managing anti-depressant treatment?
Increase the dosage, switch to another drug in the same class, switch to a drug in a different class, add a second drug such as in a typical anti-depressant
Once a patient is in remission after symptoms have resolved for depression,
Treatment should continue for how long after to prevent a relapse?
Treatment should continue for at least 4 to 9 months to prevent relapse
How often should a patient see their provider when starting an antidepressant and there after?
Patient should meet with a prescriber at least weekly during the first four weeks of treatment, then biweekly for the next four weeks, then once a month, and then periodically
What are the four Nero transmitters a part of Monoamines means?
Dopamine, epinephrine, norepinephrine, serotonin
What SSRI is the only one that causes sedation?
List 4
Fluvoxamine (Luvox)
What are the adverse effects of fluoxetine/Prozac?
Sexual dysfunction, weight gain, serotonin syndrome, hyponatremia
To help with sexual dysfunction while taking fluoxetine, an SSRI, what meds can be added?
Yohimbine, buspirone, Atypical antidepressants, or sildenafil
What are the signs of serotonin syndrome? List a few
Altard metal status, Agitation, confusion, disorientation, anxiety, hallucinations, poor concentration, Maye clonus, sweating, tremor, fever
When taking an SSRI when can serotonin syndrome start?
It begins 2 to 72 hours after treatment onset
Where are the principal differences within the class of selective serotonin reuptake inhibitor’s?
The principal differences among SSRIs relate to the duration of action
How long is fluoxetine half life?
Two days
Fluoxetine has a prolonged half life which means to produce a steady state and to wash out the medication after stopping how many weeks should it take?
Takes about four weeks to produce a steady state and four weeks to wash out after stopping the medication
SSRIs can have what pregnancy and neonatal effects?
SSRIs are teratogenic And can cause septal heart defects
Neonatal abstinence syndrome can occur along with persistent pulmonary hypertension of the newborn.
Pulmonary hypertension of the newborn should be monitored if exposed to SSRIs
MAOIs and SSRIs can cause what?
They can cause an increase risk for serotonin syndrome which can be life-threatening and it’s absolutely contraindicated
How long should MAOIs Be discontinued before switching to an SSRI?
two weeks
SSRIs Must be discontinued for how long before switching to an MAOI?
They must be discontinued for five weeks before switching to an MAOIs
Inhibitors of the CYP2D6 isoenzyme, increase risk for serotonin syndrome what drugs are included in this?
Tramadol and Linezolid antibiotics
What interaction does SSRIs have with lithium and tricyclic antidepressants?
SSRIs can increase lithium levels and increase levels of tricyclic antidepressant
What is the drug interaction between SSRIs and anti-platelet drugs such as aspirin NSAIDS, and anticoagulants like warfarin?
There is an increased risk for G.I. bleeding
What drug is safe for breast-feeding?
Antidepressants are generally safe and breast-feeding women. Sertraline/Zoloft is especially safe
Serotonin norepinephrine reuptake inhibitors have what Mechanism of action?
Blocks the neuronal reuptake of serotonin and norepinephrine
What are some major side effects of SNRIs?
Nausea very common
Headache, nervousness, sweating, insomnia, dose-dependent weight loss, anorexia, diastolic hypertension, sexual dysfunction, mydriasis, hyponatremia, and serotonin syndrome
How long should a patient wait before switching from a SNRI to a MAOI?
1 week
How long should a patient wait before switching from a MAOI to an SNRI?
Two weeks
How long should SNRIs be discontinued for?
Should slowly discontinue over 2 to 4 weeks
What is the mechanism of action for tricyclic antidepressants?
It blocks the neuronal reuptake of norepinephrine and serotonin.
Some TCAs block reuptake of norepinephrine and serotonin while others only block the reuptake of norepinephrine
What are the uses for tricyclic antidepressants?
Depression, fibromyalgia syndrome, neuropathic pain, chronic insomnia, ADHD, panic disorder, OCD
Tricyclic antidepressants can block what three receptors?
They can block histamine receptors, acetylcholine receptors, and norepinephrine receptors
What are the adverse effects of tricyclic antidepressants?
Sedation, seizures, diaphoresis, anticholinergic effects and orthostatic hypotension
Diaphoresis is a paradoxical side effect
Anticholinergic effects Include dry mouth, blurred vision, photophobia, constipation, urinary hesitancy, tachycardia
What drug interaction do tricyclic antidepressants have with MAOIs?
Increased risk for severe hypertension due to the excessive adrenergic stimulation
What therapeutic range does tricyclic antidepressants have?
A narrow therapeutic range because the lethal dose is only eight times the average therapeutic dose
MAO is found where?
It is an enzyme that’s found in the liver, intestinal walls, and terminals of monoamine containing neurons
MAO-A Inactivates what 2
neurotransmitters?
It inactivates norepinephrine and serotonin
MAO-B Inactivates what Neurotransmitter?
Dopamine
MAOIs Used for depression are non-selective and inhibit which of the MAOs?
They inhibit both MAO-A and MAO-B
What is important to know about Selegiline?
At low doses it is used for Parkinson’s disease and high doses of these for depression
Risk for hypertensive crisis is a lot lower than oral dosing
What are the two major adverse effects of monoamine oxidase inhibitors?
CNS stimulation and Hypertensive crisis with dietary tyramine
CNS stimulation Can produce anxiety, insomnia, agitation, hypo mania and mania
Foods that contain tyramine include what? What effect they have on monoamine oxidase inhibitors
Vegetables, fruits, meats, fish, sausages, milk, all cheeses, yeast extract, beer wine other foods
Increased her mean from these foods can cause hypertensive crisis due to promoting the release of norepinephrine from sympathetic neurons
Indirect acting sympathomimetics like a veteran, and feta means, cold remedies, asthma medication can have what effect on MAOIs?
They can produce hypertensive crisis
Antihypertensive drugs and monoamine oxidase inhibitor’s have what drug interaction?
It may result in excess of Lowering of blood pressure
Bupropion (Wellbutrin, forfivo xl, Alpenzin) belong to what class of antidepressants?
A typical antidepressants
What is important to know about bupropion?
Similar instruction to amphetamines
Unknown mechanism of action
Before it does not cause weight gain or sexual dysfunction like SSRIs, but increases sexual desire and pleasure pleasure
Low bioavailability
What are the uses for bupropion?
Major depressive disorder, seasonal affective disorder, used as an aid to quit smoking and used to relieve neuropathic pain
What are the adverse effects of bupropion?
Greatest concern for seizures which can be avoided by avoiding high doses.
Anticholinergic symptoms such as dry mouth, constipation,Blurred vision, tachycardia.
Agitation headache and weight loss can occur as well
How long should MAOIs Be discontinued before starting before bupropion?
Two weeks
SSRIs like sertraline, fluoxetine, and Parotexine Can have what affect on bupropion levels?
It can elevate the levels which increases seizure risk
What is important to know about Mirtazapine (Remeron)?
Is an atypical anti-depressant
It is a powerful blocker of 2 serotonin receptors and histamine
Benefits appear to result from increased release of serotonin and norepinephrine
Half life is 20 to 40 hours
Generally well tolerated and somnolent is the most prominent adverse effect
Weight gain, increased appetite and elevated cholesterol are common
For treatment of Peripartum depression What call some medication’s would be first line and what would be second line?
SSRIs such as fluoxetine, sertraline, venlafaxine would be first line.
some tricyclic antidepressants would be Second line drugs for this
Why should fluoxetine not be given while breast-feeding?
It appears unsafe to the breast-fed infant and can include consequences of colic and impaired weight gain
what is Prozac’s generic name?
Fluoxetine
SSRI
what is the mechanism action for selective serotonin reuptake inhibitors?
blocks neuronal reuptake of serotonin which causes increase activation of postsynaptic receptors
Does fluoxetine produce CNS depression or excitation?
it produces CNS excitation
