Neurology and Psychiatry Flashcards
This is a long-acting cholinesterase inhibitor and muscarinic modulator, was the first drug shown to have any benefit in Alzheimer’s disease.
Tacrine (tetrahydroaminoacridine, THA)
Drug for Alzheimer’s Disease that binds to NMDA receptor channels in a use-dependent manner and produces a noncompetitive blockade.
Memantine
This is an inhibitor of beta-site amyloid precursor protein cleaving enzyme (BACE1), reduces the production of amyloid β.
Verubecestat
2 newer drugs for the treatment of amyotrophic lateral sclerosis (ALS) that appear to have spasm reducing effects, possibly through inhibition of glutamatergic transmission in the CNS.
Idrocilamide and riluzole
3 MAO inhibitors that increase dopamine stores and are used as adjunct for levodopa in PD therapy
Rasagiline
Selegiline
Safinamide
This is a non-ergot derivative for mild Parkinsonism that may ameliorate affective symptoms. A possible neuroprotective effect has been suggested by its ability to scavenge hydrogen peroxide and enhance neurotrophic activity in mesencephalic dopaminergic cell cultures.
Pramipexole
What receptors do pramipexole bind?
D3 family of receptors
Another nonergoline derivative that is a relatively pure D2 receptor agonist that is effective as monotherapy in patients with mild disease and as a means of smoothing the response to levodopa in patients with more advanced disease and response fluctuations.
Ropinirole
This dopamine agonist is delivered daily through a skin patch, is approved for treatment of early Parkinson’s disease. It supposedly provides more continuous dopaminergic stimulation than oral medication in early parkinsonism
Rotigotine
Lithium ion, used in treatment of bipolar (manic-depressive) disorder, affects the cellular metabolism of:
phosphoinositides
This prototypical sodium channel-blocking antiseizure drug is also effective for the treatment of trigeminal and glossopharyngeal neuralgia, and mania in bipolar disorder
Carbamazepine
This sodium channel-blocking antiseizure drug effective for the treatment of focal and generalized tonic-clonic seizures can also improve depression in patients with epilepsy and reduce the risk of relapse in bipolar disorder
Lamotrigine
Aripiprazole, quetiapine, and olanzapine were the first-line drugs known as _________ for nearly all phases of bipolar disorder across guidelines
Atypical antipsychotics
Some of the intramuscular antipsychotics, like haloperidol, have been approved for the control of _________ associated with bipolar disorder and schizophrenia.
agitation
Catatonic forms of schizophrenia are best managed by intravenous:
benzodiazepine
The most commonly used off-label symptomatic medications for MS fatigue are:
amantadine and modafinil
____________, the most commonly used PD medication with anticholinergic effects, is thought to reduce classic motor symptoms through its antimuscarinic effect, enhancement of dopaminergic transmission, and non-selective NMDA receptor antagonism.
Amantadine
Which antiseizure drug has gingival hyperplasia and hirsutism occur to some degree in most patients?
Phenytoin
What are the most common dose-related adverse effects requiring dosage adjustment for phenytoin?
Diplopia and ataxia
What dose-dependent ADE of carbamazepine occurs first?
diplopia
This sodium channel-blocking antiseizure drug either enhances a poorly understood type of sodium channel inactivation called slow inactivation or binds selectively to the fast inactivated state of sodium channels—as is the case for other sodium channel-blocking antiseizure drugs, except that the binding is much slower.
Lacosamide
What congenital disorder is contraindicated for the use of lacosamide
PKU
The oral solution contains aspartame, which is a source of phenylalanine and could be harmful in people with phenylketonuria.
2 antiseizure drugs that contain sulphur and can cause kidney or renal stones
Zonisamide and Topiramate
Long-term __________ therapy for seizures is often associated with significant weight loss, primarily due to a reduction in body fat mass.
topiramate
Acute myopia and angle-closure glaucoma is an ADE of which anti-seizure drug?
topiramate
Less common but more serious SE of this antiseizure drug are behavioral and mood changes, such as irritability, aggression, agitation, anger, anxiety, apathy, depression, and emotional lability
Levetiracetam
The metabolism of levetiracetam occurs in the:
blood
There is no metabolism in the liver, and drug interactions are minimal.
MS drug that downregulates the immune response to myelin antigens by induction and activation of suppressor T cells that migrate to the central nervous system.
Glatiramer acetate
MS drug for activation of the NRF-2 pathway resulting in reduction of the oxidative stress that contributes to demyelination; it also appears to help protect the nerve cells from inflammation.
Dimethyl fumarate
This is FDA-approved for the treatment of relapsing-remitting multiple sclerosis. It is hypothesized to decrease the number of activated lymphocytes in the central nervous system.
Teriflunomide
2 idiosyncratic ADEs of Valproate
hepatic toxicity and thrombocytopenia
Valproate can cause lethargy associated with increased blood _____ concentrations
ammonia
Fatal hyperammonemic encephalopathy has occurred in patients with genetic defects in urea metabolism; the drug is contraindicated in these patients.
Because of the risk of agranulocytosis, patients receiving clozapine must have weekly blood counts for the first __________ of treatment and every __________ thereafter.
6 months of treatment
3 weeks thereafter
This is the most important unwanted effect of antipsychotic drugs.
Tardive dyskinesia
This drug has relatively very little affinity for NET but potently binds SERT. This selectivity for the serotonin transporter contributes its known benefits in the treatment of OCD.
clomipramine (TCA)
The ___________provide much more
rapid relief of both generalized anxiety and panic than do any of the antidepressants.
benzodiazepines
This is a selective MT1 and MT2
agonist that is approved for the medical treatment of insomnia. This drug has no addiction liability (it is not a controlled substance), and it appears to be distinctly more efficacious than melatonin (but less efficacious than benzodiazepines) as a hypnotic.
Ramelteon
This is a selective inhibitor of the GAT-1 GABA transporter, is a second-line treatment for focal seizures. It is contraindicated in generalized onset epilepsies.
Tiagabine
This is considered a “rationally designed” antiseizure drug because it was developed with the understanding that potentiation of GABA action in the brain is a possible antiseizure mechanism.
Tiagabine
Gabapentinoids bind avidly to ____, a protein that serves as an auxiliary subunit of voltage-gated calcium channels but may also have other functions.
α2δ
These drugs are used in the treatment of focal seizures and various nonepilepsy indications, such as neuropathic pain, restless legs syndrome, and anxiety disorders.
Gabapentinoids (gabapentin and pregabalin)
The chemical structure of tiagabine consists of the active moiety—__________—and a lipophilic anchor that allows the molecule to cross the blood-brain barrier.
nipecotic acid
This differs from other SSRIs in
some important respects as it’s metabolized to an active product which may have greater plasma concentrations. The elimination half-life of this active product is about three times longer than the drug itself and contributes to the longest half-life of all the SSRIs.
Fluoxetine
Fluoxetine has to be discontinued _____________ before an MAOI can be administered to mitigate the risk of serotonin syndrome.
4 weeks or longer
Selective serotonin reuptake inhibitors (SSRIs): [P] Fluoxetine and paroxetine inhibit _________ and increase concentrations of timolol, propranolol, metoprolol, carvedilol, and nebivolol
CYP2D6
Thus, clozapine should never be discontinued abruptly unless clinically needed because of adverse effects such as _______ or ________, which are true medical emergencies.
myocarditis or agranulocytosis
This is the only second-generation antipsychotic drug approved to reduce the risk of suicide in patients with history of schizophrenia
Clozapine
__________ dried leaf extract is usually standardized to contain 24% flavone glycosides and 6% terpene lactones. The daily dose most commonly studied and associated with a benefit in clinical trials of dementia is 240 mg daily of the dried extract in two divided doses.
Ginkgo biloba
Peptide deposits in the cerebral cortex in Alzheimer’s disease, which eventually forms extracellular plaques and cerebral vascular lesions
amyloid beta (Aa)
Proteins that form intra- and interneuronal fibrillary tangles in Alzheimer’s disease
tau protein
Pharmacologic doses of ____________ enhance the extracerebral metabolism of levodopa and may therefore prevent its therapeutic effect unless a peripheral decarboxylase inhibitor is also taken.
pyridoxine (vitamin B6)
Levodopa + MAO-A inhibitors can cause:
hypertensive crisis
This is a calcium channel blocker used in Europe, has been reported in clinical trials to effectively reduce the severity of the acute attack and to prevent recurrences of migraine
Flunarizine
___________, a 5-HT1a agonist and 5-HT2A antagonist, is approved for treatment of hypoactive sexual desire disorder in women.
Flibanserin
A drug that inhibit
microtubule disassembly that may be helpful in Alzheimer’s disease
epothilone-D
If the patient improves with edrophonium, a/an (increase or decrease) in cholinesterase inhibitor dosage may be indicated
increase
Drug for long-term therapy of myasthenia gravis
pyridostigmine
If the patient has myasthenia
gravis, an improvement in muscle strength that lasts about ________ minutes with 2-8 mg IV injection of edrophonium
can usually be observed
5 minutes
The short-acting cholinesterase inhibitor edrophonium was used to treat arrhythmias, particularly:
paroxysmal supraventricular tachycardia (supraventricular tachyarrhythmias)
This is an oxazoline derivative of prednisolone with anti-inflammatory and immunosuppressive activity for the treatment of DMD
Deflazacort
Selective COMT inhibitors such as ________ and ________ also prolong the action of levodopa by diminishing its peripheral metabolism
tolcapone
entacapone
The commercial preparation named _______ consists of a combination of levodopa with both carbidopa and entacapone. It is available in three strengths: 50, 100, 150
Stalevo
Subcutaneous injection of _________ , a potent nonergoline dopamine agonist that interacts with post-synaptic D2 receptors in the caudate nucleus and putamen, is effective for the temporary relief (“rescue”) of off-periods of akinesia in patients on optimized dopaminergic therapy.
apomorphine hydrochloride (Apokyn)
Apomorphine + Serotonin antagonists can cause
severe hypotension
Overdosage of amantadine for PD can produce what adverse effect?
acute toxic psychosis
COMT inhibitor for PD that may cause an increase in liver enzyme levels and has been associated rarely with death from acute hepatic failure
Tolcapone
A humanized IgG4 that inhibits the α4-mediated adhesion of leukocytes to their cognate receptor. It is indicated for patients with multiple sclerosis and Crohn’s disease who have not tolerated or had inadequate responses to conventional treatments.
Natalizumab
