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Terms in this set (145)
What are the medical uses of CNS drugs?
- Relief of pain
- Suppression of seizures
- Production of anesthesia
- Treatment of psychiatric disorders
What are the nonmedical uses of CNS drugs?
Stimulant, depressant, euphoriant, and other "mind-altering" abilities.
How many neurotransmitters are there in the CNS?
How many neurons in the cerebral hemisphere alone?
What impedes the entry of drugs into the brain + only lipid soluble molecules and drugs with specific transport systems can cross?
Blood Brain Barrier
What cannot cross the BBB?
Protein bound drugs and highly ionized drugs.
At birth infants are more sensitive to CNS drugs because...
The BBB is not fully developed
How does the CNS adapt to prolonged drug exposure?
Increased therapeutic effect (takes a while for drugs to reach full effect so CNS has to compensate for this)
Decreased side effects (decreased ntensity of side effects while therapeutic effects remain the same)
Physical Dependence where stopping drugs abruptly will cause withdrawals until the CNS reverts back to prior state.
- A slowly progressive neurodegenerative disorder that results in variable complications of tremor, rigidity, and bradykinesia.
- 2nd most common neurodegenerative disease
- Multifactorial disease
What are the etiologies of Parkinson's Disease?
- Dopamine depletion from degeneration of dopamine nigrostriatal system
- Postencephalitic syndrome
- Side effect of antipsychotic drugs
- Toxic effect of chemical agents
- Brain tumors
- Repeated head trauma
What is the genetic basis behind PD?
Multiple genes. One is autosomal recessive, esp in early onset.
How would wisnewski describe Parkinson's in one sentence?
"Too little dopamine and too much acetylcholine"
Levodopa/Carbidopa (Sinemet) method of action?
- Carbidopa enhances effects of levodopa.
- Levodopa reduces symptoms of PD by increasing dopamine synthesis in striatum.
How does carbidopa enhance the effect of levodopa?
- inhibits decarbox. of levodopa in intestine and peripheral tissues.
Advantages of Sinemet?
- Reduces dosage of levodopa
- Reduced production of dopamine in periphery
- Reduces CV & N/V response
- Indirect inhibition of decarboxylase
- Eliminates concerns about decreasing the effects of levodopa since you don't have to take as much.
Need to knows for administering Sinemet?
- Can cause
abnormal movements and psychiatric disturbances
- Available IR and CR
- Dose starts low and gradually increases
Avoid high protein diets
which reduces drug absorption.
Spread proteins throughout the day.
- Monitor ALT/AST, BUN, Creatinine, and CBC.
- Contraindicated with
(blocks dopamine receptors) and
momamine causes hypertensive crisis
. Stop these drugs two weeks prior.
Adverse effects of Sinemet?
- CV: Postural hypotension and dysrhytmias due to activation of beta 1 receptors.
- Psychosis: Use 2nd-gen anti-psychotic clozapine to manage
- Anxiety and agitation, memory and cognitive impairment,
darkened sweat and urine (harmless -> educate since the pt will most likely ask)
Entacapone (Comtan) method of action?
- Inhibits COMT.
COMT competes with levodopa
for transport in the intestines and peripheral tissues.
- Prolongs time levodopa is available to the brain.
Entacapone (Comtan) adverse effects?
Adverse effects of levodopa PLUS...
Yellowish orange discoloration of urine.
Entacapone is available in a fixed dose combo with...
Selegiline (Eldepryl, Zelapar) aka MAO-B inhibitor
Method of action?
- Selective and irreversible inhibiton of Monoamine Oxidase B, which breaks down dopamine.
- Therefore, it suppresses the destruction of dopamine derived from levodopa and prolongs the effects of levodopa.
Selegiline (Eldepryl, Zelapar) need to knows for administering?
dramatically within 12 to 24 months
- At recommended dosages, it does NOT pose a risk for depression/hypertensive crisis.
- Administer last dose by 12 noon since it causes
- Contraindicated with
(stupor, rigidity, agitation, hyperthermia), SSRIs that lead to fatal
- Separate meds by atleast
Name a dopamine receptor agonist that...
- is used alone in early PD
- with levodopa in advanced PD
When are maximal benefits expected for Pramipexole?
Adverse effects of Pramipexole monotherapy?
Nausea, dizziness, daytime somnolence, insomnia, constipation, weakness, and hallucinations
Adverse effects of Pramipexole w/ Levodopa?
Orthostatic hypotension, dyskinesias, increase in hallucinations
Rare side effects of Pramipexole?
Pathologic gambling and other complusive self-reward behaviors
List the PD drugs you just studied :D
- Carbidopa/Levodopa (Sinemet)
- Entacapone (Comtan)
- Selegiline (Eldepryl, Zelapar)
- Progressive memory loss
- Devastating illness
- Impaired thinking
- Neuropsychiatric symptoms
- Inability to perform routine tasks of daily living.
- Sixth leading cause of death in the US
- Most common neurodegenerative disease.
Early degeneration of neurons occurs where?
Hippocampus -> short term memory failure
Later degeneration of neurons occurs where?
- Loss of higher function
- Decline in cerebral volume
- Dysphasia and aphasia
- Eventually destroys enough to kill
- However, others will die of flu and pneumonia.
Overall look of AD?
- Accumulation of amyloid beta leads to dementia.
- Microsopes show senile plaques and fibrile tangles
- Decreased acetylcholine (memory loss)
- Gene association, esp. with early onset.
There is no cure for AD and drugs are given in early stages for mild cognitive impairment.
What are the goals for cognitive impairment drugs?
- Reverse cognitive decline, however current drugs cannot do this.
- Slow loss of memory, cognition
- Prolong independent function.
Donepezil (Aricept, Aricept ODT) method of action?
Increases availability of acetylcholine at the synpases.
- Metabolized by hepatic cytochrome P450 enzymes.
- Indicated for mild, moderate, and severe AD
Donepezil (Aricept, Aricept ODT) adverse effects?
- N/V, dyspepsia, and diarrhea
- Dizziness, headache, bronchoconstriction
-> fainting, falls, pacemaker needed.
What do you do if there are no cognitive benefits of using Donepezil?
Stop the drug. Typically only 1 in 12 get a benefit.
Doneprezil (Aricept, Aricept ODT)
- How is it administered?
- Give in the evening and slowly (4-6weeks)
- Titrate up. 5mg -> 10mg -> 23mg.
Memantine (Namenda, Namenda XR) drug class?
N-methyl-D-aspartate receptor antagonist
Memantine (Namenda, Namenda XR) method of action?
- Modulates the effects of
to improve memory.
Which drug is..
- Indicated for moderate to severe AD
- Better tolerated than cholinesterase inhibitors?
Memantine (Namenda, Namenda XR)
Memantine (Namenda, Namenda XR) adverse effects?
Name the AD drugs!
Doneprezil (Aricept, Aricept ODT)
Memantine (Namenda, Namenda XR)
- A disorder where there are excessive excitability of neurons in the central nervous system
- Produces symptoms of unconsciousness to violent convulsions
- Causes learning, memory, and mood problems
What are some epilepsy therapeutic precautions?
- Monitor plasma drug levels
- Promote patient compliance
- Antiepileptic drug withdrawals
- Suicide risk with antiepileptic drugs
Phenytoin (Dilantin) method of action?
- Selective inhibition of sodium channels
Phenytoin (Dilantin) indications and route?
- Given for partial and tonic-clonic seizures.
- Varied oral absorption
Phenytoin (Dilantin) adverse effects?
Main adverse effect: Gingival Hyperplasia
Second line drug of choice for cardiac issues
- Cognitive Impairment
- Skin rash
- Effects in pregnancy
Phenytoin (Dilantin) drug interactions? When is Phenytoin best taken?
- Decreases OCP, warfarin, and glucocorticoid effects.
- Increases levels of diazepam, isoniazaid, cimetidine, alcohol, and valproic acid.
- Administer with food. Best taken with meals.
Two words to describe how Phenytoin (Dilantin) is dosed?
Carbamazepine (Tegretol) method of action and indications?
- Suppresses high-frequency neuronal discharge in and
around the seizure foci.
- Used for epilepsy, biopolar disorder, and trigemnal/glossopharyngeal neuralgias.
Carbamazepine (Tegretol) adverse effects. (NHD)
- Neuro: Nystagmus and ataxia
- Hemato: Leukopenia, anemia, and thrombocytopenia.
- Birth defects
- Hypo osmolarity
- Dermo: Rash and photo-sensitivity reactions.
Valproic Acid (Depakene, Depakote, Depacon) method of action?
- Suppresses high-frequency neuronal firing through the
blockade of sodium channels
- Suppresses calcium influx through T-type calcium channels
- Auguments the inhibitory influence of GABA.
Phenobarbital method of action?
- Reduces seizures without causing sedation from long term exposure/CNS adaptation (thanks Sou)
- Anticonvulsant barbiturate
- Potentiates the effects of GABA
- Induction of sleep
Gabapentin (Neurontin, Gralise) therapeutic use?
- Adjunctive therapy of partial seizures
Gabapentin (Neurontin, Graise) Off-label use?
- Neuropathic pain
- Prophylaxis of migraines
- Treatment of fibromyalgia
- Relief of postmenopausal hot flashes.
Fewer drug interaction compared to other drugs
How is Convulsive Status Epilepticus diagnosed?
- Continuous series of tonic-clonic seizures that lasts 20-30 minutes
What should be included in a nursing plan of care for a patient with Convulsive Status Eplilepticus?
- Maintain ventilation
- Correct Hypoglycemia
- Terminate seizures
- Initiate or continue long term suppression drugs such as Phenytoin (dilantin) or fosphenytoin (Cerebyx)
Name the anitseizure medications you just learned!
- Phenytoin (Dilantin)
- Carbamazepine (Tegretol)
- Valproic Acid (Depakene, Depakote, Depacon)
- Gabapentin (Neurontin, Graise)
Sedative-Hypnotic Drug definition and uses?
- Depresses CNS function
- Primarily used for anxiety and insomnia
- Antianxiety agents or anxiolytics (acute or chronic anxiety drug)
Difference between antianxiety effects and hypnotic effects is often a matter of ____________.
Therapeutic uses of Benzodiazepines?
Ben, the alcoholic seizure patient, was so anxious before his surgery that he couldn't sleep
- Seizure Disorders
- Muscle Spasms
- Alcohol Withdrawals
- Perioperative applications
Adverse effects of Benzodiazepines?
After surgery, Ben was so depressed that he couldnt remember how to drive or breath. Ben can't get pregnant cause he's a male.
- CNS depression
(inability to remember new information after amnesia)
- Respiratory depression
- Do not use in pregnancy and lactation.
Drug interactions with Benzodiazepines?
- CNS depressants
How does tolerance and physical dependence develop with prolonged Benzodiazepine use?
- Tolerance develops to some effect but sometimes not at all.
- Incidence of dependence is fairly low.
What is a Benzodiazepine-like drug example?
Zolpidem (Ambien) method of action
Zolpidem (Ambien) indications for usage?
- Most widely used hypnotic
- Short term for insomnia treatment
- Long term uses shows no tolerance or increase in adverse effects
Zolpidem (Ambien) side effects?
- Daytime drowsiness
Name the drug classification for anxiety and an example!
- Zolpidem (Ambien)
What classification of drugs describes...
- Suppresses pain by blocking sodium channels and by blocking impulse conduction along axons
- Only in neurons near the site of administration
- Suppresses pain without generalized depression of nervous system?
How does epinephrine (and other vasoconstrictors) affect anesthesia?
- Decreases local blood flow with delays systemic absorption of anesthetic.
- Prolongs the effect of anesthesia and reduces the risk of toxicity.
Adverse effects of Local Anesthetics taken w/ Vasoconstrictors?
Systemic toxicity reactions like..
Which anesthetic is...
- The most widely used local anesthetic
- Applied topically or injected
- Also used for cardiac dysrhythmias
Different preparation methods for lidocaine?
What anesthetic is...
- Producing unconsciousness and lack of responsiveness to all painful stimuli?
What are the properties of an ideal inhalation anesthetic? (She might not test us on this, dont stress if you dont memorize it)
- Muscle relaxation
- Induction brief and pleasant
- Emergence brief and pleasant
- Depth of anesthesia raised or lowered with ease
- Minimal adverse effects
- Large margin of safety
Err, summary of ideal inhalation anesthetics?
- No pain
- Knock em out
- Induction and emergence are quick and easy
- Increase or decrease dose easily
- Be safe
Three pharmocokinetic phases of inhalation anesthesia?
Uptake, distribution, and elimination.
Describe inhalation anesthesia uptake.
- From the lungs
- More concentration the faster the uptake.
Inhalation anesthesia distribution.
- Where does it travel to?
- What determines effectiveness of distribution?
- To the CNS and other tissues
- Determined largely by regional blood flow.
Describe inhalation anesthesia elimination.
- Exported in the expired breath
- Almost entirely eliminated in lungs
- Some hepatic metabolism
Drug interactions of general anesthesia?
- Analgesics, CNS depressants, and CNS stimulants can influence the amount required.
Opioids reduce the amount
- CNS depressants
add on to the depressant
effect of anesthesia
What is the most widely used IV anesthetic?
Actions and uses of Propofol?
- Unconsciousness within 60 seconds and lasts 3-5 minutes
- Sedative/Hypnotic for the
induction and maintenance of analgesia
- Used in procedures with
Adverse effects of Propofol?
- Respiratory depression
- Risk of bacterial infection
- Risk for abuse
Why is propofol a high risk for abuse?
- Not a controlled substance
- Supplies not closely monitored
- Widely available
- No "high"
- Instant but brief sleep period
- Pts report feeling refreshed and talkative, elated and euphoric.
- Relieve pain without causing the loss of consciousness?
Analgesics and Opioids with Opioids being the most effective pain relievers available.
Method of action for Pure Opioid Agonists?
- produces analgesia, euphoria, sedation, respiratory depression, physical dependence, and other effects.
Examples of Pure Opioid Agonists?
Morphine (strong or moderate-strong)
Method of action for Pure Opioid Antagonists?
- Antagonists at mu and kappa receptors
- Reverses respiratory and CNS depression from overdosage of Pure Opioid Agonists.
Example of PO Antagonist?
What is used to treat opioid-induced constipation?
- Naloxone (Narcan)
- Methylnaltrexone (for constipation)
What are the pharmacologic actions of Morphine Sulfate?
(Post-op, MI, cancer)
- Tinctures of morphine used to
- Mental Clouding
- Anxiety Reduction
- Sense of wellbeing
What must the RR be to administer Morphine Sulfate to a pt?
Respiratory depression can last how long and requires what?
- May last up to 5-6 hours
- Ventilator support
How does morphine sulfate cause constipation?
- Drug attaches to mu receptors in the gut causing it difficult to manage.
How might patients with BPH respond to morphine sulfate?
- Urinary retention and hesitancy.
- May need catherization.
How can morphine sulfate increase lung secretions?
- It also acts as a cough suppressant.
- Codeine is also found in cough medicine.
Which opioid should you give to a patient with pancreatitis?
- Meperidine (Demerol)
- Morphine Sulfate causes spasm of the Odi duct, leading to intensification of pain.
What should you do to prevent emesis of a patient with Morphine Sulfate?
Give patient a pretreatment with an anti-emetic.
Other effects of Morphine Sulfate?
- Elevation of intracranial pressure
(excessive constriction of pupil, <2mm)
Symptoms and management of neurotoxicity from morphine sulfate?
- Delirium, agitation
- reducing dosage
- opioid rotation for longterm use.
Different routes of morphine sulfate?
- Intrathecal (occurring within or administered into the spinal theca. "intrathecal injection")
What two characteristics of morphine sulfate affect how much reaches the site of action?
- Not lipid soluble
- Does not cross BBB easily
Therefore, only a small fraction of each dose reaches site of analgesic action.
What are the implications of Morphine Sulfate tolerance?
- Increased dosage needed to obtain the same response
- Develops tolerance vs analgesia, euphoria, sedation, and respiratory depression.
to other opioid agonists.
to miosis or constipation occurs.
Which drugs do Morphine Sulfate interact with?
- CNS depressants
- Anticholinergic Drugs
- Hypotensive Drugs
- MAO inhibitors
- Agonist/Antagonist Opioids
What is the classic triad of Morphine Sulfate toxicity clinical manifestations?
Treatment and guidelines of Morphine Sulfate toxicity?
Guidelines to prevent toxicity:
- Monitor vitals before giving
- Give on a fixed schedule
Define drug tolerance
- State in which a larger dose is needed to produce the same response that a smaller dose required.
Tolerance occurs to ____________________ but not to ______________________.
Respiratory depression but not to constipation.
Cross tolerance occurs between all opioid agonsits but not to ______________________ such as barbiturates.
General CNS depressants
How does Fentanyl compare to Morphine?
Fentanyl has 100 times the potency of morphine.
Seen in patients with end-stage cancer.
Brand names of Fentanyl?
Three routes of Fentanyl?
Parenteral (Surgical Anesthesia)
Different formulations of transdermal Fentanyl?
Patch: Heat acceleration
Iontoporetic system: Needle-free
Different formulations for transmucosal Fentanyl?
- Lozenge on a stick (Actiq)
- Buccal film (Onsolis)
- Buccal tablets (Fentora)
- Sublingual tablets (Abstral)
- Sublingual spray (Subsys)
Other strong opioid agonists?
How moderate-to-strong opioid agonists different to morphine/fentanyl?
- Produce less analgesia and respiratory depression
- Lower potential for abuse
- Most widely prescribed drug in the US
- Combined with aspirin, acetaminophen, or ibuprofen
Define physical dependence of a drug.
- Abstinence syndrome occurs if drug is abruptly stopped.
- Body now requires the continued presence of opioids in order to function normally.
S/S of abstinence syndrome in highly dependent individuals?
Onset after 10 hours last dose
- Violent sneezing
- Muscle spasms
- Abdominal cramps
- Withdrawal takes 7-10 days
- Rarely dangerous but unpleasant
Which withdrawal can actually be life threatening?
General CNS depressant withdrawals
What is given to infants to wean off infants exposed in the uterus from dependence?
What are the three dosing guidelines for opioids?
- Assessment of pain
- Dosage determination
- Dosing schedule
When should pain be assessed for opioid admin?
Before and 1 hour after
(30min after IV route)
How must opioid dosage be adjusted?
To accommodate individual variation.
What is the rule for chronic opioid admin?
Administer on a fixed schedule to prevent toxicity.
What are the rules for acute opioid admin?
- Usually given Q3-4h prn
- Nurse should try to wean off about 3-4 days or even less after surgery
What are the Schedule II Narcotic rules?
- Very high abuse liability
- Must be counted every shift
- Discrepancies are reported and immediately investigated.
- Nurses cannot leave unit until count is correct.
- Schedule III and IV drugs are also counted but less abuse liability.
Method of action for Naloxone (Narcan)?
Therapeutic uses of Narcan?
- Reversal of opioid overdose
- Post-op opioid effects
- Neonatal respiratory depression.
How is Narcan admin'd?
- Titrated cautiously with physical dependence
- Titrated post op for adequate ventilation and maintain pain relief.
- Given to neonate to reverse resp. depression.
Which groups should you be extremely cautious of administering opioids to?
- Decreased respiratory reserve
- Patients with head injury (might confound dx)
- Infants and older adults. (Highly prone to RD)
- Liver impairment (Opioids inactivated by liver enzymes)
- Drug Interactions (table 28-4, p266)
Method of Action for Tramadol (Ultram)?
- Combination of opioid and and non-opioid mechanisms
- Interacts with CNS depressants
- XR and IR
- Throbbing head pain of moderate to severe intensity
- Sensitivity to light and sound
- Highly debilitating
Patho Review of a Migraine
- NV disorder where intracranial blood vessels dilate and become inflammed.
- Vasodilation leads to pain
- Neurons of the trigeminal vascular system
- Calcitonin gene-related peptide
- Decreased serotonin causing dilation
- Serotonin 1b/1d Receptor Agonist
- Method of action for Sumatriptan (Imitrex)
- Binds to receptors on intracranial blood vessels and causes
Aborts ongoing migraine
attack to relieve headache + other symptoms.
How is Sumatriptan admin'd?
Oral or intranasal admin
Adverse effects of Sumatriptan?
Chest symptoms: Heavy arms/Chest pressure experienced by 50% of users.
Coronary Vasospasm: Rare angina from vasospasms
Teratogenesis: Congential malformation (fetus)
- Vertigo, malaise, fatigue, tingling.
- Bad taste when taken in intranasal form.
Drug interactions of SRAs?
- Ergot alkaloids
- Other triptans
(-triptan causes vasoconstriction)
How are SRAs prepared?
Oral or nasal spray
- Second-line drug for stopping an ongoing migraine attack in patients who have not responded to triptan.
- Risk for dependence
Ergot Alkaloids like Ergotamine
MOA of Ergot Alkaloids like Ergotamine?
- Agonist activity at subtypes of serotonin HT18 and 5-HT1D receptors.
- Suppresses release of CGRP to block inflammation associated with the trigeminal vascular system
What are the different forms of preventive therapy for migraines?
- Beta Blockers (-olol)
- Antiepileptic Drugs (Divalproex, topiramate, gabapentin, and tiagabine)
- Tricyclic antidepressents (Amitriptyline)
- Estrogen, triptans, and naproxen sodium for menstrually associated migraine.
- Estrogen gel and patches (Climara, Estraderm)
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