Theraputic Drugs For Depression

Front 1

___ – mechanism of action: these drugs inhibit the membrane protein pumps that transport released serotonin (5HT) into the neuronal ending for recycling.

Back 1

Serotonin Reuptake Inhibitors (SSRIs)

Front 2

SSRIs are administered ___

Back 2

orally

Front 3

SSRIs should not be used in combination with ___ or within two weeks of terminating treatment with ___.

Back 3

MAO inhibitors
MAO inhibitors

Front 4

SSRIs can cause a manic episode or exacerbate existing mania. They should therefore be used with caution or not at all, in ___ or ___ patients.

Back 4

bipolar
manic

Front 5

___ - are for therapy of migrane headaches

Back 5

Serotonin Receptor Agonist (SRAs)

Front 6

Mechanism of action – SRAs act as direct agonists at the serotonin (5HT_1) receptor. They ___ the effects of serotonin, causing an cerebral ___.

Back 6

mimic
vasodilation

Front 7

___ inhibit reuptake of neurotransmitter into the neuronal ending. The primary neurotransmitters affected are norepinephrine and serotonin

Back 7

tricyclic antidepressants

Front 8

tricyclic antidepressants have very low patient compliance, due to the ___ of clinical effects and the prompt onset of adverse effects

Back 8

delayed onset

Front 9

Tricyclics are very nonspecific drugs and therefore have effects at ___ – in particular they have an affinity for muscarinic and histamine receptors

Back 9

various receptors

Front 10

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.

Back 10

plasma protein bound
plasma proteins

Front 11

___ are contraindicated with any drug or substance that causes and increase in the levels of cathecholamines (e.g. norepinephrine) or serotonin levels.

Back 11

tricyclic antidepressants

Front 12

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.

Back 12

MAO inhibitor

Front 13

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.

Back 13

glaucoma

Front 14

Tricyclics are contraindicated in ___ patients, or those on exogenous thyroid medication, because of the increased sensitivity to catecholamines in these patients.

Back 14

hyperthyroid

Front 15

___ - Mechanism of action: potent antagonists at central Alpha_2 receptors, resulting in increased central levels of norepinephrine, which leads to mood elevation.

Back 15

Tetracyclic Antidepressants

Front 16

___ - 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

Back 16

Heterocyclic Antidepressants

Front 17

with ___, Mood elevation only occurs in clinically depressed persons, these are not abusable drugs.

Back 17

Heterocyclic Antidepressants

Front 18

___ is an enzyme that is attached to mitochondrial membranes with the neuronal ending. It breaks down catecholamines, such as norepinephrine and dopamine.

Back 18

Monoamine Oxidase (MAO)

Front 19

There are two types of MAO: MAO_A which breaks down ___ and epinephrine, and MAO_B which breaks down ___.

Back 19

norepinephrine
dopamine

Front 20

___ 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.

Back 20

Monoamine oxidase inhibitors
MAO

Front 21

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.

Back 21

hyptertensive

Front 22

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.

Back 22

MAO
MAO

Front 23

Sedative ___ – used in the therapy of anxiety and insomnia

Back 23

Hypnotics

Front 24

Sedative hypnotics are a group of drugs that decrease the frequency of neuronal conduction. They include two major drug classes – the ___ and the ___

Back 24

barbiturates
benzodiazepines

Front 25

___ and ___ have varied clinical uses – reduce anxiety (anxiolytics), decrease frequency of sezures (anticonvulsants), or induce sleep (hypnotic agents)

Back 25

Barbiturates
benzodiazepines

Front 26

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.

Back 26

GABA
neurons

Front 27

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 ___.

Back 27

neuron
neurotransmitter

Front 28

Inhibitory neurotransmitters bind to receptors and prevent ___.

Back 28

neurotransmission

Front 29

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.

Back 29

GABA
membrane channel
decreases

Front 30

Benzodiazepines: Few serious adverse effects, most common are sedation (drowsiness), difficulty in ___ (ataxia), visual disturbances

Back 30

movement

Front 31

Barbituates adverse effects: respiratory depression, changes in ___ function, sleep changes.

Back 31

bowel

Front 32

barbituates/benzodiazepines Interactions: ___, Opiates, other CNS drugs.

Back 32

Alcohol

Front 33

Addiction: benzodiazepines are considered to be a ___ addictive. Classified as C-III and C-IV controlled substance

Back 33

psychologically

Front 34

Barbiturates are considered to be both ___ and ___ addictive. Classified as C-II and C-III controlled substance

Back 34

physically
psychologically

Front 35

___ – drugs used for anxiety.

Back 35

Anxiolytics

Front 36

Two classes of drugs are used in the therapy of insomnia. These are ___ and certain ___

Back 36

benzodiazepines
antihistamines

Front 37

Every function of the body is regulated by some portion of the ___ system.

Back 37

nervous

Front 38

Information moves along specific neuronal pathways – formed of a number of ___ in sequence.

Back 38

neurons

Front 39

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.

Back 39

neuron

Front 40

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.

Back 40

petit mal
grand

Front 41

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.

Back 41

anticonvulsants
neuronal membranes

Front 42

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.

Back 42

contraindicated
threshold

Front 43

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.

Back 43

dopamine
neurostimulants

Front 44

Drugs that may be used are ___ antidepressants (increased levels of transmitters increase mood), ___( increase circulating levels of norepinephrine and dopamine in the CNS)

Back 44

Tricyclic
Amphetamines

Front 45

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.

Back 45

dopamine
brain stem

Front 46

Parkinson’s disease results from an imbalance of ___ and ___ in an area of the brain called the substantia nigra

Back 46

dopamine
acetylcholine

Front 47

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 ___.

Back 47

neurons
dopamine

Front 48

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.

Back 48

inhibitory
excitatory

Front 49

The drug of choice in the therapy of parkinson’s disease is ___. A dopaminergic ___, such as bromocriptine, may also be used.

Back 49

L-dopa
agonist

Front 50

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.

Back 50

enzymes

Front 51

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.

Back 51

nerve
cardiovascular

Front 52

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.

Back 52

brain
inhibits
enzyme

Front 53

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.

Back 53

neuronal ending
synaptic cleft

Front 54

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

Back 54

receptors
muscarinic
stomach

Front 55

Alzheimer’s disease is a progressive disorder involving changes in neuronal pathways and formation of neurofibrillary tangles in ___ tissue.

Back 55

brain

Front 56

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.

Back 56

acetylcholine

Front 57

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.

Back 57

destroys

Front 58

Schizophrenia is thought to be due to increased levels of ___ in an area of the brain called the striatum.

Back 58

dopamine

Front 59

Schizophrenia is treated with agents that block ___ receptors (___ antagonists).

Back 59

dopamine
dopamine

Front 60

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.

Back 60

lactation

Front 61

The oldest and most widely used class of antipsychotic drugs is the ___ antipsychotic.

Back 61

phenothiazine