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Pharm > Lecture 8 > Flashcards

Lecture 8 Flashcards

1
Q

What is the inhibitory neurotransmitter?

A

GABA

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2
Q

What is the excitatory neurotransmitter?

A

Glutamate

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3
Q

What mediates the decarboxylation of glutamate to GABA?

A

Glutamic acid decaroxylase (GAD)

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4
Q

What inhibits the decarboxylation of glutamate to GABA?

A

Allylglycine (convulsant)

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5
Q

What vitamine is required by GAD as a cofactor?

A

Pyridoxine (vitamin B6)

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6
Q

What packages GABA into storage vesicles?

A

VGAT

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7
Q

What inhibits GABA release into synaptic cleft?

A

Tetanus toxin

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8
Q

The neurons and glia take up GABA via _________________.

A

GABA transporters (GATs)

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9
Q

What is a competitive inhibitor of GAT-1 and is used for epilepsy?

A

Tiagabine

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10
Q

What inhibits GABA-T? used as an antivonvulsant.

A

Vigabatrin

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11
Q

What are the 2 types of GABA receptors?

A

Iontropic (GABA A and GABA C)

Metabatropic (GABA B)

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12
Q

What type GABA receptor binds GABA and opens an intrinsic chloride ion channel?

A

Inotropic GABA receptors (GABA A and C)

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13
Q

What type GABA receptor is G-protein couples and affects neuronal ion currents via second messenger?

A

Metabatropic GABA receptors (GABA b)

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14
Q

The activation of GABAa requires the binding of how many molecules of GABA?

A

2, one to each agonist site

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15
Q

All of these (Pregnenolone, DHEA, DHDOC, THDOC, oleamide) are neurosteroids that modulate GABAa by binding to _____ sites on the receptor and cause increased reception activation.

A

Allosteric

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16
Q

What are 2 drugs that bind directly to GABAa receptors?

A

Muscimol and gaboxadol

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17
Q

What are 2 drug classes that are modulators of GABA a receptors and bind to allosteric sites to enhance GABAergic neurotransmission.

A

Benzodiazepines

Barbiturates

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18
Q

What suffix do benzodiazepines typically end in?

A

Pam

exception- triazolam, zolpidem

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19
Q

Do benzodiazpeines activate a receptor in the absence of GABA?

A

nope

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20
Q

Are benzodiazepines bound to protein usually?

A

Yes- highly protein bound

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21
Q

What is the potency of benzodiazepines correlated to?

A

Hydrophobicity

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22
Q

What metablizes benzodiazepines?

A

CYP3A4

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23
Q

What is an ADR of benzos?

A

amnesia

24
Q

When can benzos cause death?

A

When combined with alcohol (CYP3A4 inhibitor and CNS depressant)

25
Q

What is an antagonist of benzos?

A

Flumazenil

26
Q

What are some uses of benzos?

A 
sleep enhances
anxiolytics
sedatives
antiepileptics
muscle relaxers
treatment for alcohol withdrawal
27
Q

What suffix do barbiturates usually end with?

A

“tal”

28
Q

What CNS sites do barbiturates affect?

A

spinal cord
brain stem
brain

29
Q

What do barbiturates do?

A

Sedation
Amnesia
Loss of consciousness by affecting GABA receptors in the brain

30
Q

What are these barbiturates used for?

Thiopental, pentobarbital, methohexital

A

Anesthetic barbiturates

Act as agonists at GABA a

31
Q

What are is a barbiturates used as anticonvulsants?

A

Phenobarbital

less direct agonism

32
Q

What does the termination of barbiturates effects depend primarily on?

A

Redistribution from CNS to highly perfused areas

33
Q

What happens with chronic use of barbiurates?

A

High uptake into adipose tissue and there is a longer elimination 1/2 life

34
Q

What metabolizes barbiturates?

A

Hepatic metabolism, P450

35
Q

What 2 drugs enhance the activaiton of GABA a by GABA and at high doses act as agonists? They also help induce anesthesia.

A

Etomidate

propofol

36
Q

Where are most GABA B receptors found?

A

Spinal cord

37
Q

What is a GABA B agonist that is used primarily for treatment of spasticity associated with motor neuron diseases. Can be administered orally in mild cases and intrathecal in severe cases.

A

Baclofen

38
Q

Can withdrawl occur with baclofen?

A

yes, can result in acute hypersensitivty, rhabdomyolysis, pruritis, delerium and fever. Especially found with intrathecal route

39
Q

What targets does Ethanol have?

A

GABA A and glutamate receptors as well as others

40
Q

What is a GABA isomer clinically used for narcolepsy?

A

Gamma hydroxybutyric acid (GHB)

41
Q

What are the 2 pathways for glutamate synthesis?

A
  1. Product formed in Kerbs cycle is transaminated to glutamate
  2. Glutamien produced in glial clles can enter Krebs cycle and converted to glutamate in nerve terminal
42
Q

How is glutamate terminated?

A

REuptake transporters take glutamate up and plutamine synthetase converts glutamate into glutamine

43
Q

What are the 3 inotropic glutamate receptors?

A

AMPA
Kainate
NMDA

44
Q

What 2 glutamate receptors are foudn throughout the CNS and activation results in NA influx and K efflux (possible Ca permeability)

A

AMPA and Kainate

45
Q

What inotropic glutamate receptor is foudn primarily in hippocampus, cerebral cortex and spinal cord. Requires binding of glutamate and glycine for activation and then allows for K efflux, Na and CA influx. Requires a depolorization to remove Mg block

A

NMDA

46
Q

What type of metabotropic glutamate receptor causes neuronal excitation through phospholipase C activation?

A

Group I

47
Q

What 2 types of metabotropic glutamate receptors work by inhibiting adenyl cyclase and decrease cAMP production?

A

Group II and Group III

48
Q

What can happen with too much glutamate release or decreased reuptake?

A

Increased intracellular Ca resulting in cellular damage and further glutamate release

49
Q

What are some conditions where you see excitotxicity?

A

Stroke
Trauma
Hyperalgesia
Epilepsy

50
Q

What are 3 NMDA agntagonists?

A

Riluzole
Memantine
Amatadine

51
Q

What NMDA antagonist works by blocking Na channels and decreasing glutamate

A

Riluzole

52
Q

What 2 NMDA antagonists are non-competitive blockers of NMDA?

A

Memantine and Amatadine

53
Q

What NMDA antagonist is used in Alzheimers?

A

Memantine

54
Q

What NMDA antagonist is used in Parkinson’s to decrease dyskinesia?

A

Amatadine

55
Q

What is an drug that stabilizes inactivate state of Na channel reducing excitability and glutamate release-seizures?

A

Lamotrigine

56
Q

What is a drug that inhibits NMDAs and is used in seizures?

A

Felbamate

Pharm (29 decks)

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