Neuro 1 Flashcards
What are neurotransmitter connector sites called?
Neurotransmitters respond through the stimulation of connector sites called synapses
What is the effect of the chloride coming in and potassium coming out in regards to the neurotransmitter?
The resulting flow of ions (chloride in; potassium out) increases the membrane potential to the point that it counteracts any excitatory signals that arrive at that neuron
Where is ACh released?
Released at the terminals of all motor neurons
What is ACh responsible for?
stimulation of muscles (GI tract and movement)
rapid eye movement (REM) sleep
thought, learning, and memory
The use of drugs that enhance/ inhibit the destruction of ACh are helpful in the tx of which diseases?
Alzheimer’s disease because acetylcholine levels are low in the brains of these patients
How does the black spider venom work w/ ACh?
release of acetylcholine - leads to severe muscle contractions, spasms, paralysis, and even death
How do nerve agents work w/ ACh?
Nerve agents, such as sarin gas, are potent acetylcholinesterase inhibitors
Death by asphyxiation due to a loss of control of the respiratory muscles
Blocking/ antagonizing ACh does what to muscles?
Causes them to relax
Botulinum toxin (Botox) causes what to ACh?
prevents the release of acetylcholine - causing muscle relaxation
What is Dopamine derived from?
Manufactured inside dopamine neurons from an amino acid precursor, L-tyrosine
What does the release of dopamine do to the body?
Feelings of pleasure, and also addiction
Movement and motivation
How is Parkinson’s tx?
Treatment of Parkinson’s disease provides the patient with levodopa (L-dopa)
Midbrain dopamine and its receptors are involved in which actions?
Behavior, attention, and arousal (also Parkinson’s disease)
What inactivates endorphins?
They are rapidly inactivated by enzymes called peptidases
When are endorphins released?
Released during exercise, excitement and sex
Endorphins do what to the body?
Act as analgesics by diminishing the perception of pain (also slow HR, respiration, and metabolism)
Is GABA excitatory or inhibitory and why?
inhibitory neurotransmitter - responsible for slowing or stopping the excitatory neurotransmitters that give rise to anxiety
What does GABA do in terms of overexcitation?
helps induce relaxation and sleep by inhibiting overexcitation
What are gamma-aminobutyric acid enhancers?
Drugs that increase GABA levels in the brain
What drugs influence GABA?
benzodiazepines*, alcohol, sedatives, narcotics, and barbiturates
What is the MC neurotransmitter in the CNS?
Glutamate
Is glutamate excitatory or inhibitory?
Excitatory
Where are Noroepi and Epi released for in reflex to stress?
Adrenal glands
What do Noroepi and Epi do to the body?
Causes increase in heart rate and BP
Causes physical boost and heightened awareness
Is serotonin excitatory or inhibitory?
Inhibitory neurotransmitter
Low serotonin leads to what?
depression, problems with anger control, obsessive-compulsive disorder, suicidal ideation, increased appetite for carbohydrates, trouble sleeping, irritable bowel syndrome, and fibromyalgia
Appetite suppression drugs
benzenediamine
diethylpropion
phentermine* - available PO
Appetite suppression drugs MOA
These drugs are sympathomimetic amines - stimulate the hypothalamus mimicking satiety
Drugs for Appetite Suppression use
Obesity or overweight in the presence of at least one weight-related comorbidity
Drugs for Appetite Suppression SE
Hypertension, tachycardia, Dry mouth, Changes in libido, Depression, insomnia
Drugs for Appetite Suppression + MAOIs can cause what?
Coadministration of monoamine oxidase inhibitors (MAOIs) may cause a life-threatening hypertensive crisis.
Drugs for Appetite Suppression + EtOH causes what?
Depression
Why are Drugs for Appetite Suppression contraindicated in pts w/ substance abuse?
Substance abuse (cocaine/methamphetamine) because of the potential for excessive adrenergic stimulation.
Why are Drugs for Appetite Suppression contraindicated in pts w/ substance abuse?
Substance abuse (cocaine/methamphetamine) because of the potential for excessive adrenergic stimulation.
Drugs for Appetite Suppression contraindications
Substance abuse (cocaine/methamphetamine) because of the potential for excessive adrenergic stimulation.
Advanced arteriosclerosis
Concomitant use, or use within 14 days, of a MAO inhibitor
Hyperthyroidism
Moderate to severe hypertension
Pregnancy
How long should a pt be off of MAOI to be able to use an appetite suppressant?
At least 14 days
In which pt population can appetite suppressants be used and how should they be used?
severely obese patients only as short-term adjuncts to other weight-loss measures
What can occur w/ stopping an appetite suppressant?
Effective in the short term, but weight gain occurs almost universally upon stopping them.
Which schedules are Diethylpropion and phentermine and Benzphetamine and phendimetrazine?
Benzphetamine and phendimetrazine are schedule III
Diethylpropion and phentermine are schedule IV
What time of day should appetite suppressants NOT be taken in and why?
Avoid an evening dose because of resultant insomnia or sleeplessness.
Drugs to Aid Sleep schedule rating
Schedule IV drugs because they are benzodiazepine-like
Drugs to Aid Sleep should not be used for > 7-10 days, why?
Can be habit forming because they act on benxo receptors
Drugs to Aid Sleep examples (nonbenzos)
zolpidem
eszopiclone
zalepon
nonbenzodiazepine GABAergics MOA
selective for the GABA-1 receptor complex, where they enhance chloride conductance on the neuronal membrane
How do nonbenzodiazepine GABAergics compare to regular benzos?
Strong hypnotic properties and weak anxiolytic, muscle relaxant, and anticonvulsant properties compared to benzodiazepines
Drugs to Aid Sleep use
To provide sedation during episodes of insomnia
Drugs to Aid Sleep SE
xerostomia, Headache, balance disorder, abnormal dreams, sleepwalking, hallucinations, memory impairment, lethargy
Drugs to Aid Sleep SE
xerostomia, Headache, balance disorder, abnormal dreams, sleepwalking, hallucinations, memory impairment, lethargy
Drugs to Aid Sleep contraindications
Hypersensitivities
Pregnancy
Drugs to Aid Sleep black box warning
Rare but serious injures due to abnormal sleep behaviors
Drugs to Aid Sleep combined w/ ketoconazole, erythromycin, clarithromycin, and protease inhibitors can cause what?
Increased blood levels of sleep aids
Sleep aid time limitations
It is best if these agents are used no >2 weeks (acutely) or 3 months (chronically) without careful evaluation of the treatment
Use of sleep aids for greater than 2 wks then cessation can cause what?
withdrawal symptoms (fatigue, nausea, flushing, uncontrolled crying, nausea, vomiting, GI upset, panic attacks, nervousness)
What happens to hormones during a migraine HA?
During an attack, serotonin levels drop, resulting in expansion of the brain’s blood vessels and throbbing pain
What happens to hormones during a migraine HA?
During an attack, serotonin levels drop, resulting in expansion of the brain’s blood vessels and throbbing pain
What is the goal to migraine HA tx?
to minimize the impact these headaches have on the patient’s quality of life and the patient’s ability to work
Serotonin Receptor Agonists (Triptans) examples
sumatriptan (SC, PO, nasal spray)
zolmitriptan
rizatriptan
Serotonin Receptor Agonists (Triptans) MOA
Acts selectively on serotonin receptors in cranial arteries, causing vasoconstriction
Triptan use
Relief of migraine, either to abort an attack or to be used prophylactically
Triptan SE
Tingling, warm sensation, flushing, paresthesia, dizziness
Biggest drug interaction w/ Triptans
All triptans can interact with the SSRIs, possibly causing serotonin syndrome
Triptan contraindications
ischemic heart disease, peripheral vascular disease, cerebral vascular syndromes, or uncontrolled HTN - d/t vasoconstriction
When/ how should triptans be used?
Should be administered at any sign of an impending migraine attack or during an attack, a second dose may be given if there has been at least 2 hours between doses.
Ergotamines examples
ergotamine
dihydroergotamine
ergotamine + caffeine
Ergotamines MOA
Acts selectively on serotonin receptors in cranial arteries, causing vasoconstriction
Ergotamines use
To abort or prevent vascular-based headaches, such as migraine
Ergotamines SE
Vasospasm, ischemia, hypertension, Nausea, Hot flashes, paresthesia
Ergotamines contraindications
pregnancy, Uncontrolled HTN, peripheral vascular disease, and ischemic heart disease.
Ergotamines blood levels can increase when used with which drugs?
Do not use with strong/potent CYP3A inhibitors, such as azole antifungals, protease inhibitors and macrolides. OR grapefruit juice
Ergotamines black box warning
Increase in blood levels leading to stroke or MI when combined w/ CYP3A4 inhibitors
What can lead to ergotamine noncompliance?
Nausea will often limit the dose or lead to nonadherence
Ergotamines fail to relieve HA, what should be done?
If an initial dose has failed, repeating the dose rarely mitigates the migraine.
