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61 Cards in this Set
- Front
- Back
___ – mechanism of action: these drugs inhibit the membrane protein pumps that transport released serotonin (5HT) into the neuronal ending for recycling.
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Serotonin Reuptake Inhibitors (SSRIs)
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SSRIs are administered ___
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orally
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SSRIs should not be used in combination with ___ or within two weeks of terminating treatment with ___.
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MAO inhibitors
MAO inhibitors |
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SSRIs can cause a manic episode or exacerbate existing mania. They should therefore be used with caution or not at all, in ___ or ___ patients.
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bipolar
manic |
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___ - are for therapy of migrane headaches
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Serotonin Receptor Agonist (SRAs)
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Mechanism of action – SRAs act as direct agonists at the serotonin (5HT_1) receptor. They ___ the effects of serotonin, causing an cerebral ___.
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mimic
vasodilation |
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___ inhibit reuptake of neurotransmitter into the neuronal ending. The primary neurotransmitters affected are norepinephrine and serotonin
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tricyclic antidepressants
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tricyclic antidepressants have very low patient compliance, due to the ___ of clinical effects and the prompt onset of adverse effects
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delayed onset
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Tricyclics are very nonspecific drugs and therefore have effects at ___ – in particular they have an affinity for muscarinic and histamine receptors
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various receptors
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Interactions: Tricyclics are highly ___, so drug interactions with other drugs that bind into ___ may cause fluctuations in plasma concentration of the drug and potential toxicity.
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plasma protein bound
plasma proteins |
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___ are contraindicated with any drug or substance that causes and increase in the levels of cathecholamines (e.g. norepinephrine) or serotonin levels.
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tricyclic antidepressants
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Tricyclics should not be administered within 14 days of treatment with an ___. Doing so could result in a hypertensive crisis, due to radically increased levels of norepinephrine.
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MAO inhibitor
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Tricyclics should not be administered during the acute phase of recovery from a myocardial infarction, or to a patient with ___, because of the drug’s antimuscarinic affects.
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glaucoma
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Tricyclics are contraindicated in ___ patients, or those on exogenous thyroid medication, because of the increased sensitivity to catecholamines in these patients.
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hyperthyroid
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___ - Mechanism of action: potent antagonists at central Alpha_2 receptors, resulting in increased central levels of norepinephrine, which leads to mood elevation.
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Tetracyclic Antidepressants
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___ - Mechanism of action: Serotonergic neurons also contain Alpha_2 receptors, called heteroreceptors, which decrease serotonin release. These drugs block heteroreceptors, which results in increased release of 5HT
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Heterocyclic Antidepressants
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with ___, Mood elevation only occurs in clinically depressed persons, these are not abusable drugs.
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Heterocyclic Antidepressants
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___ is an enzyme that is attached to mitochondrial membranes with the neuronal ending. It breaks down catecholamines, such as norepinephrine and dopamine.
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Monoamine Oxidase (MAO)
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There are two types of MAO: MAO_A which breaks down ___ and epinephrine, and MAO_B which breaks down ___.
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norepinephrine
dopamine |
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___ work by inhibiting __ in a dose- dependent manner, which results in a decrease in the rate of metabolism of norepinephrine. This results in more norepinephrine available to be released from the neuron.
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Monoamine oxidase inhibitors
MAO |
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There are many problems with MAO inhibitors. The effects of any drug that raises levels of norepinephrine will be potentiated, as the increased levels of norepinephrine can not be broken down. This results in ___ crisis, which can be life-threatening.
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hyptertensive
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There are food interactions with ___ inhibitors: feel good foods such as wine, cheese, chocolate contain a substance called tyramine, which is normally broken down by ___ shortly after ingestion.
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MAO
MAO |
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Sedative ___ – used in the therapy of anxiety and insomnia
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Hypnotics
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Sedative hypnotics are a group of drugs that decrease the frequency of neuronal conduction. They include two major drug classes – the ___ and the ___
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barbiturates
benzodiazepines |
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___ and ___ have varied clinical uses – reduce anxiety (anxiolytics), decrease frequency of sezures (anticonvulsants), or induce sleep (hypnotic agents)
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Barbiturates
benzodiazepines |
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sedative-hypnotic drugs work by augmenting the actions of inhibitory neurotransmitter ___. They thus decrease the frequency and amplitude (strength) of neuronal transmission. This results in decreased rate of firing of ___, decreased mental acuity, relaxation, and eventually sleep.
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GABA
neurons |
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Excitatory neurotransmitters bind to receptors on the surface of a post-synaptic ___ and cause stimulation of that neuron, which results in synaptic transmission from the neuron and release of ___.
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neuron
neurotransmitter |
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Inhibitory neurotransmitters bind to receptors and prevent ___.
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neurotransmission
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The inhibitory neurotransmitter ___ binds to a receptor, which permits chloride ions to flow through a ___. This flow of negatively charged ions into the cell ___ excitation of the cell membrane.
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GABA
membrane channel decreases |
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Benzodiazepines: Few serious adverse effects, most common are sedation (drowsiness), difficulty in ___ (ataxia), visual disturbances
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movement
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Barbituates adverse effects: respiratory depression, changes in ___ function, sleep changes.
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bowel
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barbituates/benzodiazepines Interactions: ___, Opiates, other CNS drugs.
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Alcohol
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Addiction: benzodiazepines are considered to be a ___ addictive. Classified as C-III and C-IV controlled substance
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psychologically
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Barbiturates are considered to be both ___ and ___ addictive. Classified as C-II and C-III controlled substance
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physically
psychologically |
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___ – drugs used for anxiety.
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Anxiolytics
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Two classes of drugs are used in the therapy of insomnia. These are ___ and certain ___
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benzodiazepines
antihistamines |
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Every function of the body is regulated by some portion of the ___ system.
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nervous
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Information moves along specific neuronal pathways – formed of a number of ___ in sequence.
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neurons
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What causes a seizure: A neuronal pathway that regulates one function may lie very close to other pathways that regulate other functions. Since the neuronal membranes are excitable, “over excitation” of a neuron in one pathway may cause an electrical “spike” which, if it is powerful enough, excites a ___ in an adjacent pathway. This adjacent pathway is now activated and whatever function it regulates is stimulated (e.g. muscle contraction) even through it is not needed.
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neuron
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Small seizures are called ___ seizures, and are usually associated with abnormal small movements or memory. Seizures that involved the whole body are termed ___ mal seizures.
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petit mal
grand |
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Drugs used in the therapy of seizures are correctly termed ___. The function of these drugs is to decrease the excitability of ____, so that aberrant electrical “spikes” will not be formed.
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anticonvulsants
neuronal membranes |
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Alcohol is ___ with any antiseizure agent, as the effect of alcohol lowers the ___ for seizure activity and potentiates adverse effects of anticonvulsants (e.g. sedation) Alcohol can also interfere with the metabolism of anticonvulsants.
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contraindicated
threshold |
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Attention Deficit Hyperactivity Disorder (ADHD) is commonly seen among children.The condition is treated by increasing ___ levels and activity in certain parts of the brain. Oddly enough, the drugs used to treat this disorder are stimulants, ___ to be exact.
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dopamine
neurostimulants |
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Drugs that may be used are ___ antidepressants (increased levels of transmitters increase mood), ___( increase circulating levels of norepinephrine and dopamine in the CNS)
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Tricyclic
Amphetamines |
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The drug of choice is Methylphenidate. Brand Name Ritalin, Concerta. Mechanism of action: blocks neuronal reuptake of ___ in the central nervous system. This results in an increase in central levels of dopamine in the ___, which regulates arousal, and the cerebral cortex, which regulates cognitive ability.
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dopamine
brain stem |
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Parkinson’s disease results from an imbalance of ___ and ___ in an area of the brain called the substantia nigra
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dopamine
acetylcholine |
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Dopaminergic neurons begin to degenerate and die, due to hold age, drug use, or infectious disease. This leaves the area with too many ___ that make acetylcholine and too few that make ___.
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neurons
dopamine |
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Since dopamine acts as an ___ neurotransmitter and acetylcholine is an ___, and imbalance produces things like unnecessary or uncontrolled muscle contractions, excess salivation, and so on.
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inhibitory
excitatory |
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The drug of choice in the therapy of parkinson’s disease is ___. A dopaminergic ___, such as bromocriptine, may also be used.
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L-dopa
agonist |
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L-dopa is a brain chemical found in dopaminergic neurons, which is converted to dopamine by ___ in the dopaminergic neuron. It is also called levodopa.
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enzymes
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A major problem with the use of L-dopa is that it can be converted to dopamine in any dopaminergic ___ terminal. This includes dopaminergic neurons in the body (peripheral), as well as the brain (central). This can produced unwanted changes in ___ and renal activity.
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nerve
cardiovascular |
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In addition, the peripheral nerve terminals will remove the L-dopa from the bloodstream, before it can get to the ___ where it is needed, resulting in less drug available to be converted to dopamine in the CNS.
To avoid this problem, we give a second drug that ___ the neuronal conversion of L-dopa into dopamine. This drug is called carbidopa and inhibits the ___(dopa decarboxylase), which is necessary for the conversion. |
brain
inhibits enzyme |
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PHYSIOLOGY REVIEW – The metabolism of catecholamines
There are two major ways that catecholamines, such as norepinephrine and dopamine, are metabolized A mitochondrial enzyme, monoamine oxidase, or MAO breaks down these transmitters as they are taken back up into the ___ from the synaptic cleft, MAO_A breaks down norepinephrine, while another MAO, MAO_B metabolizes dopamine. Neurotransmitter released into the ___ is broken down and inactivated by tissue enzyme called catechol-O-methyl transferase or COMT. |
neuronal ending
synaptic cleft |
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AGENTS THAT DECREASE LEVELS OF ACTIVITY OF ACETYLCHOLINE (ANTIMUSCARINIC AGENTS)
Mechanism of action: These drugs block muscarinic ___ and decrease cholinergic activity. Therapeutic effects: blockade of ___ effects in the nigrostriatal tract, resulting in normalization of acetylcholine/dopamine activity ratio. Contraindications: glaucoma, obstruction of the lower ___ valve or duodenum, enlarged prostate |
receptors
muscarinic stomach |
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Alzheimer’s disease is a progressive disorder involving changes in neuronal pathways and formation of neurofibrillary tangles in ___ tissue.
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brain
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The primary areas affected by Alzheimer's are the cerebral, cortex, forebrain, and limbic system, which regulate coherent thought, reasoning, and memory/emotion, respectively.
Since ___ is a primary excitatory neurotransmitter in these areas, it is thought that raising available levels of acetylcholine will provide symptomatic relief. Thus drugs currently useful in the therapy of Alzheimer’s are targeted to raise levels of acetylcholine in these portions of the brain. |
acetylcholine
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drugs for Alzheimer's bind to the enzyme acetylcholinesterase. Binding occurs at the site where the enzymes normally binds acetylecholine, and ___ it. This results in in more available acetycholine.
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destroys
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Schizophrenia is thought to be due to increased levels of ___ in an area of the brain called the striatum.
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dopamine
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Schizophrenia is treated with agents that block ___ receptors (___ antagonists).
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dopamine
dopamine |
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Schizophrenia drugs have a wide variety of undesirable effects, and patient compliance is poor. These agents can cause ___ in both men and women, enlarged breasts, cardiodepressant actions, Parkinson-like symptoms.
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lactation
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The oldest and most widely used class of antipsychotic drugs is the ___ antipsychotic.
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phenothiazine
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