CNS Pharma Flashcards

1
Q

Importance of drugs on CNS

A

Action of neurotransmitter and or receptors contributes to therapeutic benefit /side effects
Can enhance or diminish action of endogenous neurotransmitters
- kinetic differences can include route/rate of elim

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2
Q

Agonist action at receptor

A

Direct
Indirect (increases action of exogenous neurotransmitter, often by decreasing degredation)

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3
Q

Antagonist action at receptor

A

Direct (comp inhibition)
Indirect antagonist decease availability of neurotransmitter

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4
Q

Conduction pathways in CNS

A

Excitatory or inhibitory, redundant or not

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5
Q

5 major processes identifying a neurotransmitter

A

1 - synthesis
2 - storage
3 - release
4 - receptor interaction
5 - inactivation

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6
Q

Ionotropic receptors

A

GABA, glutamate, ACh
Send electrical signals, short term effect

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7
Q

Metabotropic receptors

A

GABA, opioids, monoamines (norepinephrine, DA, Serotonin) also ACh

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8
Q

Only Ionotropic receptor

A

Glutamate

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9
Q

Why do not all patients respond the same when administered the same drugs?

A

Glutamate can make gaba
GABA can make glutamate
GABA = inhibitory
Glutamate = excitatory

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10
Q

T/F

Neurotransmitters of the peripheral nervous
system (ANS) can also be neurotransmitters of the CNS.

A

True

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11
Q

Synthesis and degradation of glutamate and
GABA are interrelated.

A

True

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12
Q

Dopamine, norepinephrine and serotonin have similar synthetic pathways.

A

True

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13
Q
  1. Identified CNS neurotransmitters are routinely
    modulated for therapeutic purposes.
A

True

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14
Q

Glutamate

A

Excitatory
Pain perception
Overstimulation detriments - seizures, brain damage
Multiple sites on this Ionotropic receptor for drugs
- glutamate, glycine, aminoglycosides antibiotics, hallucinogens
Antagonist used as dissociative anesthetic
- ketamine

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15
Q

GABA

A

Amino acid neurotransmitter
Inhibitory
2 receptors, GABAa (Cl- channel) GABAb
Structural analogs for pain modification (gabapentin, NOT GABAa receptor targeting)
GABA receptor agonist drugs are tranquilizers, anticonvulsants/muscle relaxants, anesthetics
- benzodiazepines (oral IV)
- barbiturates (oral IV)
- general anesthetics (inhalants, IV) low safety margin

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16
Q

Ketamine

A

Could be aware but not able to move, only comes in injectable form
Good for cardiac risk clients

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17
Q

Drugs for Ionotropic receptors

A

Glutamate, glycine, aminoglycosides, antibiotics, hallucinogens

18
Q

Receptors for gaba

A

GABAa - cl - channels
GABAb

19
Q

Drugs that target GABA

A

Benzodiazepines (oral IV)
Barbiturates (oral IV)
General anesthetics (inhalants, iV)

20
Q

What GABA drugs are controlled drugs?

A

Class III, class IV
Barbiturates - cause respiratory depression
Benzodiazepines - muscle relaxants

21
Q

Why are obese patients risky for dosing?

A

All drugs are lipid soluble, drugs linger in fat, just because drugs aren’t present in blood concentration could still be too high
- lower secondary dose

22
Q

Opioids

A

Enkephalins, endorphins are endogenous neuropeptides w role in tolerance to pain

23
Q

Opioid drugs

A

Agonist used for analgesia
- mu, kappa receptors - full and partial agnoists
- respiratory & cardio depressants, antitussives, emetics
- antagonist
- oral, parenteral & topical preparations

24
Q

Action of opioids

A

Act on presynaptic sensory neurons to reduce pain causing neurotransmitter release

25
Q

What drug targets Kappa receptors?

A

Tramadol

26
Q

Biggest risk to opioids

A

Respiratory depression
Analgesic action

27
Q

Weak bases of opioids

A

Lipophilic, low margin of safety
Dose response for resp t and cardio depression

28
Q

PK of opioids

A

Oral or parenteral, microsomal metabolism
Urinary excretion, variable duration based on route/formulation

29
Q

Metabotropic receptors of opioids

A

Mu, Kappa
Antidotes - competitive antagonist

30
Q

Use of opioids

A

Analgesics, emetics, antitussives, vet sedatives
Controlled substances (class III)

31
Q

T/F All receptors for GABA, glutamate and natural opioids are ionotropic

A

False

32
Q
  1. T/F Drugs that are agonists at GABA, glutamate and enkephalin receptors act at the same site on the receptors as the natural neurotransmitters.
A

False

33
Q
  1. T/F Excitatory and inhibitory pathways can stimulate the same postsynaptic neuron.
A

True

34
Q

T/F Relief of pain occurs because opioid analgesics have a direct effect on neurotransmitter release

A

False
Act on Ca channels blocked

35
Q

Monoamines

A

Dopamine, norepinephrine, serotonin

36
Q

Features of monoamines

A

Multiple roles/receptors - role in direct agonist
Nonspecific action with indirect agonist
- action on degredation enzymes
- nonspecific reuptake inhibition
More specific action w direct agonist and drugs are more specific reuptake inhibitors

37
Q

Role of monoamines in disease and treatments

A

Analgesics
Disorders of behavior
Chemical restrains/tranquil
Emesis/antiemetics

38
Q

Functions drugs can alter

A

Release, receptors, enzymes of degredation, reuptake

39
Q

Monoamine agonists

A

Norepinephrine
Alpha 1 - stimulates
Alpha 2 - analgesics, tranq, antihypertensives, emetics in cats

40
Q

Monoamine antagonist

A

Dopamine
Antiemetics
- phenothiazine - antihistaminic & anti cholinergic action
Metocolpramide - antagonists, prokinetic agent

41
Q

Vet use of Monoamine antagonist

A

Tranq and antiemetics

42
Q

C hoose from (a) glutamate, (b) GABA, (c) opioids, (d) monoamine (dopamine, norepinephrine, serotonin) as major contributor to –
1. general anesthesia
2. pain tolerance during surgery 3. pain perception 4. behavioral changes associated with pain 5. addiction 6. emesis (for early treatment of

A

General anesthesia - B
pain tolerance during surgery - B
Pain perception - A
Behavioral changes - C
Additiction = C
Emesis -
Antiemetics - D