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Therapeutics > Exam 4 lecture 4 > Flashcards

Exam 4 lecture 4 Flashcards

1
Q

What is GABA receptor coupled to? location? Inhibitory functions?

A

Gi/o coupled receptor
Location- brain, limbic system
Inhibitory- presynaptic- decreased Ca conductance
Postsynaptic- Increase K conductance
Postsynaptic- increase K conductance

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2
Q

Name GABA agonists and antagonists

A

Agonists- Baclofen (skeletal muscle relaxant that treats alcoholism(
-Gamma hydroxybutyric acid (GHB) (CNS depressant)

Antagonist- Phaclofen, saclofen and 2hydroxysaclofen

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3
Q

Difference between GABA a and GABA b

A

GABA a is an ion channel that takes a short time to act

GABAb is a GPCR hat takes a long time to act

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4
Q

What is Xyrem? what does it do?

A

C I illicit use and C III medical use that with concomitant stimulant use can decrease excessive daytime sleepiness and increase daytime wakefulness. It can also decrease cataplexy

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5
Q

GHB side effects and prodrugs

A

CNS depression (dose dependent)
-dizziness, drowsiness, coma

Prodrugs
GBL and 1,4 Butanediol

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6
Q

What are concerns about GHB

A

No antagonist to counter effects

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7
Q

What are the melatonin agonist drugs

A

Ramelteon and Tasimelteon

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8
Q

Ramelteon MOA, metabolism, abuse?

A

MOA- high affinity for MT1 and MT2 melatonin receptors. Melatonin is the master clock serving as circadian rhythms.

Metabolism- CYP1A2 substrate

No abuse, withdrawal or dependency

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9
Q

Tasimelteon MOA? Use?

A

MOA- high affinity for MT1 and MT2 melatonin receptors.

Treatment of non 24 hr sleep wake disorder

ORPHAN PRODUCT registration

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10
Q

Name orexin receptor antagonists? MOA? USE?

A

Suvorexant

MOA- high affinity antagonist for OX1 and OX2 orexin receptors located in HYPOTHALAMUS

It reduces rewarding stimuli (DA release) via receptors that modulate mesolimbic projections between the VTA AND THE NUCLEUS ACCUMBENS

Treats insomnia

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11
Q

What did the FDA require a label change of

A

Required a label change for all sleep disorder drug products
(including the newer nonbenzodiazepine drugs Eszopiclone, Ramelteon, Zaleplon, Zolpidem)

FDA required labeling needs to include information about sleep related behaviors (sleep driving, eating and cooking and phonecalls)

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12
Q

What are some more sedative hypnotics in history? Drugs/uses

A

Trazodone
-antidepressant
-hypnotic unlabeled/investigational use

Antihistamines (OTC drugs)
-diphenhydramine
-doxylamine-pyrilamine

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13
Q

Herbal and natural hypnotics

A

Melatonin
valerian (hepatotoxicity has been noted)

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14
Q

Sedative hypnotics overdose treatment

A

Flumenazil for BZDs and Z hypnotics

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15
Q

What are the types of anxiety

A

GAD
Panic disorder
Social anxiety disorder
OCD
PTSD
Anxiety associated with autism/depression

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16
Q

What are drugs and diseases that could cause drug induced anxiety

A

Cocaine, psychostimulants (Caffeine), social media withdrawal.

also antidepressant and anxiolytic drug withdrawal

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17
Q

What are some neurotransmitters in anxiety

A

NE
GABAergic system
serotonin
CRF

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18
Q

How does NE take part in anxiety

A

Over active locus coeruleus release NE
Dysregulated in GAD and other types of anxiety

Projects to amygdala (fear center)

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19
Q

GABAergic system role in anxiety

A

GABA system normally counteracts/balances stimulatory effects of excess NE

GABA/Glutamate is converted to GABA by glutamic acid decarboxylase, leading to generalized anxiety disorder in CNS

Agents that increase GABA are anxiolytic

20
Q

Role of serotonin in anxiety

A

SSRIs are effective and partial agonists of %HT1A receptors are effective

21
Q

Drug treatment choices of anxiety

A

BZDs (quick and effective)- there is an abuse potential
Antidepressants- SSRIs, SNRIs,- take weeks to act. Ketamine nasal spray is a game changer

BB

buspirone

22
Q

How is Buspirone an anxiolytic

A

Partial agonist on brain 5HT1A receptor
Low abuse potential
Not good for panic disorders (BZD is much faster)

23
Q

How is BB an anxiolytic

A

Propanolol- uses may need test dose initially
-social anxiety
-PTSD nightmare

decreased peripheral sx of anxiety

24
Q

Name some miscellaneous anxiolytics

A

Hydroxyzine- H1 agonists

Clonidine- Alpha 2 agonist

25
Q

What are some investigational anxiolytics

A

Glutamatergic agents
-NMDA receptor modulators
-mGluR5 antagonist
mGlu R2/3

26
Q

What is ADHD? Pathophysiology? what type of drug do we use? WHen do symptoms start? What does interfere with?

A

ADHD shows changes in metabolic activity (Brain activity is lower)

genetic (2/3) vs non-genetic (1/3)

Use something to increase activity opposite to seizure

ADHD interferes with functioning and development

symptoms start at age 5-9 y/o

27
Q

implicated systems in ADHD

A

Dopamine transporter, cholinergic, CNS

28
Q

symptoms of ADHD

A

Inattention and hyperactivity

29
Q

What part of the brain might not be fully functional in ADHD

A

prefrontal cortex (mPFC)

30
Q

Explain methylxanthines and how the treat ADHD

A

Methylxanthines indirect acting sympathomimetics- stimulant compounds mimic the effect of endogenous agonists of the sympathetic nervous system.

31
Q

Name a methylxanthine

A

Caffeine

32
Q

methylxanthine effect on adenosine recetor

A

antagonizes it. Increases cAMP, leading to increased intracellular Ca

33
Q

What are methylxanthines linked to with regard to A1 GPCR? What effect does this have on neurotransmitters? How does this affect the CNS and peripheral?

A

A1- Gi/o linked inhibitory modulation of many neurotransmitters

CNS activation- sedation, anxiolysis, anticonvulsant activity

Peripheral activation- Decreased heart rate

34
Q

What effect do methylxanthines have on A2a receptors? A2b? A3?

A

A2a- Gs linked, causes vasodilation.
A2b- GS linked, mostly on glial cells
A3- Gq linked. hippocampus and thalamus activated

35
Q

When are Gq linked hippocampus and thalamus activated

A

Only activated in states of excessive catabolism. Seizures, hypoglycemia, stroke, not antagonized by methylxanthines.

36
Q

WHat are two things we need to do to treat ADHD

A

Increase alertness
Reduce fatigue

37
Q

What are some monoamine transporters

A

Dopamine, norepinephrine, serotonin

38
Q

What are some indirect acting sympathomimetics

A

Cocaine (3-phenyltropanes)
Amphetamines

39
Q

Explain how cocain and amphetamine work

A

Cocaine directly blocks NET (blocks transporter)

Amphetamine- mimics and leads to reverse transportation.

40
Q

What does cocaine inhibit? WHat us ut used as

A

Inhibits monoamine transporters (NE, 5-HT, DA)

used as anesthetic and blocks transporter

41
Q

Amphetamines MOA

A

Non selective activation of monoamines.

Highly reqarding, abuse potential

42
Q

Name some examples of amphetamines

A

Dextroamphetamine
Lisdexamphetamine
Amphetamine vs methamphetamine

Methylphenidate
Dexmethylphenidate

Aderall

Mydayis (mixture of amphetamine salts)

43
Q

Uses of amphetamines

A

Narcolepsy, anorexiant/weightloss

44
Q

non stimulants for ADHD

A

Atomoxetine- NET inhibitor
TCAs
Bupropion
Clonidine
Modafinil (approved for narcolepsy not ADHD)

45
Q

Alternative therapies approaches for ADHD

A

EEG biofeedback
essential fatty acid supplementation
Yoga/massage
Green outdoor spaces
elimination of artificial food addiives, colors and or preservatives

46
Q

Narcolepsy symptoms

A

Excessive daytime sleepiness
Wakening of muscle
Poor quality of sleep
sleep paralysis
Hypnogogic hallucination

47
Q

Treatment of narcolepsy

A

Stimulants for sleepiness

-Solriamfetol- NET and DAT

treats obstructive sleep apnea and narcolepsy excessive sleepiness (TONES)

-modafinil

-antidepressants
-xyrem
-pitosilant- H3 receptor antagonist

Therapeutics (38 decks)

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