Depressants Flashcards by tcarlso 3

What are the four lobes of the cerebrum?

Frontal
Temporal
Parietal
Occipital

How well did you know this?

Not at all

Perfectly

What is the diencephalon? What are the structures that are included in this?

Area of the brain that encloses the 3rd ventricle

Thalamus
Hypothalamus

How well did you know this?

Not at all

Perfectly

What is the function of the thalamus?

Integration of sensory relays

How well did you know this?

Not at all

Perfectly

What is the function of the hypothalamus?

Regulates temperature, appetite, emotional and hormonal regulation

How well did you know this?

Not at all

Perfectly

What is the mesencephalon?

Midbrain, the serves as a bridge between the cerebrum/diencephalon, and the brainstem

How well did you know this?

Not at all

Perfectly

What are the structures that are contained within the brainstem?

Pons

Medulla oblongata

How well did you know this?

Not at all

Perfectly

What is the function of the pons and the medulla?

Controls respiration and cardiovascular function

How well did you know this?

Not at all

Perfectly

What is the function of the reticular formation within the brainstem?

Control of consciousness, arousal, and alertness

How well did you know this?

Not at all

Perfectly

Where are the basal ganglia located?

deep within the cerebral hemispheres

How well did you know this?

Not at all

Perfectly

What is the function of the basal ganglia?

Control of motor activities, and repressing unwanted movements

How well did you know this?

Not at all

Perfectly

What are the four components of the basal ganglia?

Cortex
Striatum
Pallidum
Thalamus
**AND BACK TO CORTEX!!**

How well did you know this?

Not at all

Perfectly

What are the two components of the striatum?

caudate nucleus and putamen

How well did you know this?

Not at all

Perfectly

What are the four major areas of the brain that are part of the limbic system?

Amygdala
Hippocampus
Cingulate gyrus
Prefrontal cortex

How well did you know this?

Not at all

Perfectly

What is the function of the amygdala?

Regulation of fear

How well did you know this?

Not at all

Perfectly

What is the function of the Hippocampus?

Memory formation, conversion of short term memory into long term

How well did you know this?

Not at all

Perfectly

What is gray matter?

Synaptic connections between various neurons

How well did you know this?

Not at all

Perfectly

What is white matter?

Myelinated axons of neurons, grouped in ascending or descending tracts

How well did you know this?

Not at all

Perfectly

What forms the Blood brain barrier?

Tight junctions between endothelial cells on the CNS capillaries

How well did you know this?

Not at all

Perfectly

What is the function of astrocytes?

Homeostatic support roles for neuron (maintain nutrition etc)

How well did you know this?

Not at all

Perfectly

What is the function of oligodendrocytes?

Glial cells that wrap around the axons of projection neurons in the CNS forming the myelin sheath

How well did you know this?

Not at all

Perfectly

What are the cells that myelinate CNS neurons? PNS?

CNS = oligodendrocytes
PNS = Schwann cells

How well did you know this?

Not at all

Perfectly

What are microglia?

Glial cells derived from the bone marrow specialized in immune defense of the brain

How well did you know this?

Not at all

Perfectly

What are the two components that create the blood brain barrier?

Tight junction around capillary endothelial cells

Astrocyte foot processes

How well did you know this?

Not at all

Perfectly

What is the protein in neuronal terminals that interacts with Ca, and allows for the release of neurotransmitters?

Calmodulin

How well did you know this?

Not at all

Perfectly

What are ionotropic receptors?

receptors on synapses that activate an ion channel

What are metabotropic receptors?

receptors coupled to a second messenger enzyme system (e.g. adenylate cyclase)

What is the only enzymes that breaks down 5HT?

monoamine oxidase

What are electrical synapses?

junctions between cells that allow for ion fluxes, and immediate transmission of signal

What is EPSP?

Excitatory postsynaptic potential

What are IPSPs?

Inhibitory postsynaptic potentials

What are the roles of acetylcholine in the brain?

Memory and learning Attention Sleep

What is the function of dopamine?

brain circuits that control movement (think parkinson's)

What is the function of glutamate in the CNS?

major excitatory neurotransmitter and CNS

What is the function of GABA in the brain?

Major inhibitory neurotransmitter in the CNS

What is the function of substance P in the CNS?

Excitatory transmitter involved in spinal processing

What is the function of endorphins, enkephalins, and dynorphins?

Inhibit pain sensation

What is CNS depression?

Decreased neuronal excitability

What are CNS depressants?

agents that are mainly used to treat anxiety states and sleep disorders

What are hypnotics?

Agents that produce drowsiness and encourage the onset and maintenance of a state of sleep

What stages of sleep are amplified with hypnotics, and which are depressed?

``` Amplified = stage 2 Decreased = REM and 4NREM ```

True or false: any sedative anxiolytic given in a high enough dose will induce sleep

True

What are the four stages of effects of increasing doses of hypnotics?

Sedation Hypnosis Anesthesia Coma

What is the cause of death with depressant overdoses?

Respiratory depression

What are the two types of sedative hypnotics that have a linear slope of CNS effects, and will cause coma/death at high enough doses?

barbituates | Alcohols

What is the major type of drugs that reach a plateau in CNS depression, and are thus less likely to cause deatj?

Benzodiazepines

Why are depressants used for Szs?

Depress the CNS activity

What is the MOA of CNS depressants in causing muscle relaxation?

inhibition of polysynaptic reflexes and skeletal neuromuscular junction

What type of drugs have a -pam suffix? What are the two exceptions to this?

Benzodiazepines Alprazolam Clorazepate

What is flunitrazepam?

Roofies

What functional group on benzodiazepines is responsible for their sedative hypnotic effects?

Electronegative substituent in the 7 position

What route of administration is the best for benzodiazepines?

Oral

How are benzodiazepines metabolized? (what oran/enzymes)

In the liver by p450 CYP3A4 + glucuronidation

What are the two benzodiazepines that are metabolized into inactive water soluble glucuronides? How fast is this?

Lorazepam and oxazepam Fast metabolism

What are the benzodiazepines that are metabolized into weakly active, and have short lived active metabolites?

Alprazolam | Triazolam

true or false: most benzos have long lived active metabolites

True

What is the primary indication of, and relative half life of: midazolam?

Preanesthetic | Short acting

What is the primary indication of, and relative half life of: triazolam

Insomnia | Preanesthetic

What is the primary indication of, and relative half life of: alprazolam

Anxiety, antidepressant | Intermediate acting

What is the primary indication of, and relative half life of: clonazepam

seizures | Intermediate acting

What is the primary indication of, and relative half life of: estazolam

insomnia | Intermediate acting

What is the primary indication of, and relative half life of: lorazepam

anxiety, insomnia, szs, preanesthetic | Intermediate acting

What is the primary indication of, and relative half life of: oxazepam

Anxiety | Intermediate acting

What is the primary indication of, and relative half life of: temazepam

Insomnia | Intermediate acting

What is the primary indication of, and relative half life of: chlordiazepoxide

Anxiety, withdrawal states | Long lasting

What is the primary indication of, and relative half life of: clorazepate

Anxiety and szs

What is the primary indication of, and relative half life of: diazepam

Anxiety and withdrawal states | Long lasting

What is the primary indication of, and relative half life of: Flurazepam

Insomnia | Long lasting

What is the primary indication of, and relative half life of: prazepam

Anxiety | Long lasting

What is the primary indication of, and relative half life of: quazepam

Insomnia | Long lasting

What are the two drugs used to treat alcohol withdrawal?

diazepam and oxazepam

What is the influence of age on metabolism of benzodiazepines?

Slower hepatic processing

What happens to Vd in old age? Why?

Goes up due to decreased lean body mass

What happens to the rate of elimination of benzodiazepines in the elderly?

Decreased

What is the MOA of benzodiazepines?

Potentiate the effects of GABA(A) receptors, which are Cl- channels, by increasing the frequency of opening of the channels

What happens when GABA receptors are depolarized?

Cl- influx, increases membrane hyperpolarization and overall neuronal inhibition

What are the three effects produced by alpha 1 GABA subunit receptors?

Sedation Anticonvulsant Anterograde amnesia

What are the three effects produced by alpha 2-4 GABA subunit receptors?

Anxiolysis

What are the major side effects and toxicity of benzodiazepines?

Respiratory depression | Anterograde amnesia

What is the general principle behind withdrawal symptoms?

Opposite effect of taking them will occur

What are the relative contraindications to benzodiazepines? (non-obvious ones anyway)

Prego | Sleep disorders

What are the drugs that have an additive effect on benzodiazepines? (besides obvious) (4)

Phenothiazine Opioids antihistamines tricyclic antidepressants

What is the antidote to benzodiazepines?

Flumazenil

What is the MOA of flumazenil?

Competitive inhibit that binds to the BZ receptor

What is the relative half life for flumazenil?

Short duration

What are the three newer types of benzodiazepines?

Eszopiclone Zolpidem Zaleplon

What is eszopiclone?

Newer benzo (lunesta)

What is zolpidem?

Newer benzo (ambien)

What is zaleplon?

newer benzo (sonata)

What is the general clinical use of the newer benzos?

treat insomnia

What is the antidote for newer benzos?

Flumazenil

What are the four major barbiturates?

Pentobarbital Phenobarbital Secobarbital Thiopental

What type of drug is pentobarbital?

Barbiturate

What type of drug is phenobarbital?

Barbiturate

What type of drug is secobarbital?

Barbiturate

What type of drug is thiopental?

Barbiturate

What are the four major clinical uses of barbiturates?

Anesthesia Sedative Anticonvulsant Medically induced coma

How are barbiturates metabolized How fast is this? What are the metabolites?

In the liver by microsomal enzymes Slow No active metabolites

What is the one barbiturate that is metabolized/excreted by the kidney?

Phenobarbital

What is the MOA of barbiturates?

Increase the duration of the GABA gated chloride channel opening, via NONCOMPETITIVE ation

Which increases the rate of opening, and which increases the duration of opening: benzos vs barbiturates?

Benzos = increase rate Barbiturates = duration

What is the MOA of ramelteon?

Melatonic receptor agonist

What are the clinical uses of ramelteon?

Sedative agent for insomnia

What are the two melatonin receptors, and what is the function of each?

``` MT1 = sleep onset MT2 = circadian pattern ```

How are melatonin receptor agonists metabolized?

Extensive first pass effect via p450 enzymes

True or false: there is a high abuse liability for melatonin receptor agonists like ramelteon

False

What is the MOA of buspirone? Indication?

Partial 5HT-1A receptor agonist Anxiolytic

Is there a high or low abuse liability with buspirone?

Low

What is the function of 5HT-1A receptors, and how does buspirone's MOA relate to this?

Inhibits presynaptic release of 5HT, thus causes anxiolytic properties of buspirone

What is the role of propranolol in anxiolysis?

Inhibits the somatic manifestations of anxiety

What is the role of hydroxyzine and diphenhydramine in anxiolysis?

Mild sedative

What is the role of meprobamate in anxiolysis?

Sedative

Depressants Flashcards

(111 cards)