CNS Pharma

Question 1

Importance of drugs on CNS

Answer 1

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

Question 2

Agonist action at receptor

Answer 2

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

Question 3

Antagonist action at receptor

Answer 3

Direct (comp inhibition)
Indirect antagonist decease availability of neurotransmitter

Question 4

Conduction pathways in CNS

Answer 4

Excitatory or inhibitory, redundant or not

Question 5

5 major processes identifying a neurotransmitter

Answer 5

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

Question 6

Ionotropic receptors

Answer 6

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

Question 7

Metabotropic receptors

Answer 7

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

Question 8

Only Ionotropic receptor

Answer 8

Glutamate

Question 9

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

Answer 9

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

Question 10

T/F

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

Answer 10

True

Question 11

Synthesis and degradation of glutamate and
GABA are interrelated.

Answer 11

True

Question 12

Dopamine, norepinephrine and serotonin have similar synthetic pathways.

Answer 12

True

Question 13

4. Identified CNS neurotransmitters are routinely
   modulated for therapeutic purposes.

Answer 13

True

Question 14

Glutamate

Answer 14

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

Question 15

GABA

Answer 15

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

Question 16

Ketamine

Answer 16

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

Question 17

Drugs for Ionotropic receptors

Answer 17

Glutamate, glycine, aminoglycosides, antibiotics, hallucinogens

Question 18

Receptors for gaba

Answer 18

GABAa - cl - channels
GABAb

Question 19

Drugs that target GABA

Answer 19

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

Question 20

What GABA drugs are controlled drugs?

Answer 20

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

Question 21

Why are obese patients risky for dosing?

Answer 21

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

Question 22

Opioids

Answer 22

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

Question 23

Opioid drugs

Answer 23

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

Question 24

Action of opioids

Answer 24

Act on presynaptic sensory neurons to reduce pain causing neurotransmitter release

Question 25

What drug targets Kappa receptors?

Answer 25

Tramadol

Question 26

Biggest risk to opioids

Answer 26

Respiratory depression Analgesic action

Question 27

Weak bases of opioids

Answer 27

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

Question 28

PK of opioids

Answer 28

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

Question 29

Metabotropic receptors of opioids

Answer 29

Mu, Kappa Antidotes - competitive antagonist

Question 30

Use of opioids

Answer 30

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

Question 31

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

Answer 31

False

Question 32

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

Answer 32

False

Question 33

3. T/F Excitatory and inhibitory pathways can stimulate the same postsynaptic neuron.

Answer 33

True

Question 34

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

Answer 34

False Act on Ca channels blocked

Question 35

Monoamines

Answer 35

Dopamine, norepinephrine, serotonin

Question 36

Features of monoamines

Answer 36

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

Question 37

Role of monoamines in disease and treatments

Answer 37

Analgesics Disorders of behavior Chemical restrains/tranquil Emesis/antiemetics

Question 38

Functions drugs can alter

Answer 38

Release, receptors, enzymes of degredation, reuptake

Question 39

Monoamine agonists

Answer 39

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

Question 40

Monoamine antagonist

Answer 40

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

Question 41

Vet use of Monoamine antagonist

Answer 41

Tranq and antiemetics

Question 42

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

Answer 42

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