CNS part 1 Flashcards
Opioids work by binding to the ____ and _______ receptors that we have around our body.
mu and kappa
Pure Opioid Agonists (______, codeine, meperidine), bind with…
Pure Opioid Agonists (morphine, codeine, meperidine), bind with mu and kappa receptors (agonist for both).
Agonist-Antagonist Opioids (pentazocine, nalbuphine, butorphanol, buprenorphine), don’t bind so much with ___ (________ & partial ________) which is good because binding with mu could cause respiratory depression and it may not cause the euphoria that could happen. They still bind with ______ (except for buprenorphine)
Agonist-Antagonist Opioids (pentazocine, nalbuphine, butorphanol, buprenorphine), don’t bind so much with mu (antagonist & partial antagonist) which is good because binding with mu could cause respiratory depression and it may not cause the euphoria that could happen. They still bind with kappa (except for buprenorphine)
Pure Opioid Antagonists (naloxone, naltrexone), does not bind with ____ or ______; like an ________ to the other drugs
Pure Opioid Antagonists (naloxone, naltrexone), does not bind with mu or kappa; like an antidote to the other drugs
Opioid/Morphine adverse effects that do not go away with time
Sedation, Miosis, Constipation
Other opioid/morphine adverse effects
- Euphoria/dysphoria
- Pruritus: itching but does subside with time
- Sedation: side effect that will not go away
- Miosis (constricted pupils): side effect that will not go away
- Neurotoxicity (delirium, agitation, hyperalgesia)
- Renal impairment
- Birth defects
- Constipation: side effect that will not go away; most patients require meds to prevent (stool softeners, laxative)- they will not build up a tolerance to the constipation.
- Orthostatic hypotension: will go away with time
- Cough suppression
- Emesis (N/V)- will go away with time/meds
- Urinary retention- will go away with time
What are the immediate concerns for the patient who is opioid naïve?
Respiratory depression- which is the most serious adverse effect of opioids, “especially for those who are opioid naïve, they have never been on opioids”
Tolerance to respiratory depression can develop over time (usually 72 hrs), so risk ________ over that period.
When you start adding other drugs that are CNS depressants (eg, _______, barbiturates, benzodiazepines)- _____ risk for respiratory depression
Tolerance to respiratory depression can develop over time (usually 72 hrs), so risk decreases over that period.
When you start adding other drugs that are CNS depressants (eg, alcohol, barbiturates, benzodiazepines)- higher risk for respiratory depression
ii. What is one of the potential side effects that continue as long as the patient is taking an opioid? Why does this occur (underlying physiology)
Constipation- occurs due to a decreased/suppressed peristalsis, increased tone of anal sphincter, and reduced secretion of fluids into intestinal lumen
Know the advantages to around the clock (ATC) dosing compared to PRN dosing with opioids.
The research shows that patients on ATC get better _____ _____ and require less ____ _______. ATC dosing has more of a ____ state. So, ATC is better, esp. with chronic pain. Typically used w sustained/extended release drugs.
PRN: Usually end up requiring _____ pain medicine and not _______ with pain management
Basically, the more we can keep them in a steady state, the better pain is managed, the less pain medicine they require, and the more ______ they are with pain management (for ATC)
The research shows that patients on ATC get better pain relief and require less pain medicine. ATC dosing has more of a steady state. So, ATC is better, esp. with chronic pain. Typically used w sustained/extended release drugs.
PRN: Usually end up requiring more pain medicine and not satisfied with pain management
Basically, the more we can keep them in a steady state, the better pain is managed, the less pain medicine they require, and the more satisfied they are with pain management (for ATC)
What drugs are considered opioid antagonists?
Naloxone and Naltrexone
Opioid antagonists (Naloxone and Naltrexone) are used for:
-treatment of opioid overdose
-relief of opioid-induced constipation
-reversal of postoperative opioid effects
-management of opioid addiction
Drug of choice for complete or partial reversal of opioid-induced respiratory depression?
Naloxone Hydrochloride (Narcan)
Naloxone Hydrochloride (Narcan):
- Drug of choice for complete or partial reversal of opioid-induced _______ ________
- Failure of the drug to significantly reverse effects of a presumed opioid overdose indicate the condition may ____be related to opioid overdose
- Remember that it also reverses ____ ______
- Has a half life of ___ hrs- only lasts for a _____ time (__ hrs); still need to go to ER
- ___ mg cumulative dose should see response
- Drug of choice for complete or partial reversal of opioid-induced respiratory depression
- Failure of the drug to significantly reverse effects of a presumed opioid overdose indicate the condition may not be related to opioid overdose
- Remember that it also reverses pain control
- Has a half life of 2 hrs- only lasts for a short time (2 hrs); still need to go to ER
- 10 mg cumulative dose should see response
Naltrexone (ReVia): drug of choice with…
pure opioid agonist overdose; blocks euphoria that they get
Naltrexone (ReVia)
- _______ ________ with physical dependence
- Reverses ____ _____ (analgesia), resp. depression, coma, euphoria, and sedation
- Half life of __ hrs; __ mg cumulative dose should see response
- Titrated cautiously with physical dependence
- Reverses pain control (analgesia), resp. depression, coma, euphoria, and sedation
- Half life of 2 hrs; 10 mg cumulative dose should see response
a. Know signs and symptoms of opioid withdrawal: CNS related symptoms would be:
- Diuresis
- Miosis
- Seizures
- N/V
- Respiratory depression
a. Know signs and symptoms of opioid withdrawal: Non-CNS related (due to release of histamine) symptoms would be:
- Hypotension
- Spasms of the colon- diarrhea
- Urinary retention
- Dilation of blood vessels- sweating, pruritus
Altogether- s/s of opioid withdrawal
- Diuresis
- Miosis
- Seizures
- N/V
- Respiratory depression
- Hypotension
- Spasms of the colon- diarrhea
- Urinary retention
- Dilation of blood vessels- sweating, pruritus
b. Review video on how to administration naloxone:
- Put on gloves
- Remove vial’s cap
- Pull plunger on syringe to bring air into it
- Remove cap on needle
- Insert needle into vial and inject air into it
- Pull plunger up to fill syringe w entire content of vial
- Slightly press down on plunger to remove air bubbles
- Hold syringe at ___ degrees and inject into ______ (___)
- Remove needle at same angle and firmly press down on plunger to pull the needle back into the syringe
- Put on gloves
- Remove vial’s cap
- Pull plunger on syringe to bring air into it
- Remove cap on needle
- Insert needle into vial and inject air into it
- Pull plunger up to fill syringe w entire content of vial
- Slightly press down on plunger to remove air bubbles
- Hold syringe at 90 degrees and inject into muscle (IM)
- Remove needle at same angle and firmly press down on plunger to pull the needle back into the syringe
What is the purpose of using Naltrexone to prevent relapse opioid use?
They use this drug because it blocks the euphoria effect
Know signs and symptoms of alcohol withdrawal
- Elevated blood pressure, pulse rate, and temperature
- Insomnia
- Tremors
- Agitation
What class of medication is used to manage alcohol withdrawal?
Benzodiazepines
The drugs for migraines end with
-triptan or -tripta
Migraine: Know how the class of drugs work (-triptan or -tripta) (mechanism of action)
The migraine causes a drop in serotonin, which causes the blood vessels in the brain to vasodilate. The rush of blood through those dilated cerebral arteries is what causes the pain/headache.
So, the drug’s MOA:
Triptans work as a ______ agonist; they ____ with receptors on _____ ______ leading to _______ and inhibition of ________
Triptans work as a serotonin agonist; they bind with receptors on blood vessels leading to constriction and inhibition of inflammation
Migraines-
What are the contraindications to taking the medications?
- History of heart-related problems like Prinzmetal angina
- Dyslipidemia
- Hypertension
- History of stroke
- Peripheral arterial disease
- Seizure disorder
- History of hepatitis, cirrhosis, liver failure
Review the common presenting symptoms of Parkinson’s disease.
Resting tremor, bradykinesia (slow movement), rigidity (stiffness of limbs/trunk), postural instability, and hypotension
Review the underlying pathophysiology of Parkinson’s disease.
Dopamine in the substantia nigra is not sufficiently produced to bind to receptor
Review the relationship between dopamine and acetylcholine neurotransmitters:
Dopamine ______/_______acetylcholine, and acetylcholine works with ____________ NS. Decrease in dopamine means acetylcholine works __________ because there is an ________ between the dopamine and acetylcholine.
Goal is to balance out these neurotransmitters
Dopamine counters/balances acetylcholine, and acetylcholine works with parasympathetic NS. Decrease in dopamine means acetylcholine works unopposed because there is an imbalance between the dopamine and acetylcholine.
Know how the drug levodopa works to manage Parkinson’s disease:
Levodopa is the drug of choice for
the symptomatic treatment of bradykinesia
MOA of Levodopa:
Relieves _____ symptoms by ________to _______ in surviving nerve ______ in the brain- increases _______ __________ and enhances the __________ of dopamine.
Relieves motor symptoms by conversion to dopamine in surviving nerve terminals in the brain- increases dopamine concentration and enhances the neurotransmission of dopamine.
Limitations of Levodopa:
- It can take ______to get to a full_____ _____
- Highly effective, but benefits _______ ____ _____
- ____ _____ are needed to get to the CNS (except it increases adverse effects; BUT if levodopa is given with carbidopa, it prevents enzyme in the gut from breaking down levodopa so there isn’t any need to increase dose )
- Can’t eat _____ _____ meals/ avoid _______/ spread it out (dietary issue)
- It can take months to get to a full therapeutic effect
- Highly effective, but benefits diminish over time
- High doses are needed to get to the CNS (except it increases adverse effects; BUT if levodopa is given with carbidopa, it prevents enzyme in the gut from breaking down levodopa so there isn’t any need to increase dose )
- Can’t eat high protein meals/ avoid proteins/ spread it out (dietary issue)
Levodopa must be taken on a
empty stomach because food delays absorption
Food interaction of Levodopa:
high protein meals -> slows absorption -> reduces therapeutic effect
Vitamin B6 (fish, beef liver)
Levodopa has something called an ___ ___ syndrome- what does this mean?
- “On-off” syndrome: it works for 2-5 yrs, but you get a loss of response over time. Gradual “wearing off” at end of dose; and abrupt loss of effect (“on-off” phenomenon) can happen at any time in dosing
Drug holidays with Levodopa:
- With long-term use of levodopa, adverse effects tend to increase and therapeutic effects tend to diminish. For some patients, taking time off from treatment, say, 10 days, may produce a beneficial effect with lower doses. This is a dangerous time.
- Drug holidays must take place in the ______, because drug withdrawal _________ the patient. The patient is at risk for all of the physical and psychological effects of this stress.
- Drug holidays must take place in the hospital, because drug withdrawal immobilizes the patient. The patient is at risk for all of the physical and psychological effects of this stress.
Class – dopamine agonists.
Primary drug used in practice is
levodopa/carbidopa
Drug Therapy for Parkinson’s Disease:
- Achieved by correcting the _____ of neurotransmitters by
Dopamine and Ach:
imbalance
Dopamine agonists: two types-
Derivatives of ergot and Nonergot derivatives
Derivatives of ergot –____ selective for ______ (Bromocriptine – rarely used, SE) Not reliant on ______conversion. Less likely to cause _______
Derivatives of ergot – less selective for Dopamine (Bromocriptine – rarely used, SE) Not reliant on enzyme conversion. Less likely to cause dyskinesias.
Non-ergot derivatives (_______ selective for Dopamine receptors & less S/E. (newer) ___ line motor drug
Ex drugs: _______ (Mirapex) ; ________ (Requip) also used for restless leg syndrome.
Non-ergot derivatives (highly selective for Dopamine receptors & less S/E. (newer) 1st line motor drug
Ex drugs: Pramipexole (Mirapex) ; Ropinirole (Requip) also used for restless leg syndrome.
Non-ergot derivatives S/E
nausea, dizziness, daytime somnolence- (“sleep attacks”) AKA narcolepsy, insomnia, constipation, weakness, and hallucinations
If non-ergot derivatives are combined w levodopa, you’ll see more (what S/E)
orthostatic hypotension, dyskinesias, and increase in hallucinations
Most common drugs for PD
Dopaminergic agents- they promote the activation of dopamine receptors
ex: levodopa
Another drug for PD
Anticholinergic agents
* Block receptors for ACh (prevent activation of
cholinergic receptors)
Non-ergot derivatives are a first line
motor drug
