MCQ Flashcards

1
Q

D: 100% bioavailability is by definition achieved by:

A

intravenous

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2
Q

A:The neurotransmitters in the autonomous nervous system are

A

Acetylcholine + noradrenaline

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3
Q

P: A true competitive antagonist …

A

binds to the same site as an agonist but does not cause a conformational change that can activate the receptor

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4
Q

C: Which central acting drugs as central stimulative?

A

Analeptics

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5
Q

C: Which is a pre-condition for central action of a drug?
Lipophobic properties
Passage through the BBB and interaction with central structures like receptors
Increasing Adrenaline levels significantly
lowering memb potential
Boosting GABAergic function

A

Passage through the BBB and interaction with central structures like receptors

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6
Q

A: In the autonomous nervous system nicotine is

1) Dose-dependently an agonist and a blocker at the nicotinergic ganglia
2) Just an agonist without effects
3) An agonist at muscarinergic R
4) An agonist at ganglia, but a blocker at NMJ

A

Dose-dependently an agonist and a blocker at the nicotinergic ganglia
(Nicotine binds to Ach receptors)

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7
Q

B:What energy sources do plasma membrane transporters of neurotransmitters mainly use?

A

Na+ gradient across the membrane

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8
Q

B:What are the differences between plasma membrane transporters and vesicular transporters for neurotransmitters?

A

Plasma membrane transporters use the Na+ gradient to clear the synaptic cleft of the released neurotransmitter. Vesicular transporters use (among others) a pH gradient to pump neurotransmitter molecules into synaptic vesicles.

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9
Q
C:Which class does not belong to the antidepressants?
SSRI
Monoamine Oxidase Inhibitors
Psychostimulants
Butyrophenones
Non-selective NA-5HT reuptake inhibitors
A

Butyrophenones

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10
Q

P:An ideal agonist will

A

shift the ratio in favor of the active state

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11
Q

P: Randomisation

A

removes sources of bias, even those that are not known

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12
Q

B: Neurotransmitter activity can be terminated by:

A

Enzymatic inactivation, diffusion and uptake

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13
Q

B: Which of the following statement(s) is/are correct?

Glutamate is synthesized in the soma and packed into vesicles which are transported to the synapse. The source of Glutamate is Tyrosine, which is decarboxylated and than aromatized by specific enzymes in the trans-Golgi network.

Neurons don’t synthesize Glutamate at all, but depend entirely on supply by Glial cells

Glutamate concentration in the cerebrospinal fluid is high and it can be taken up directly

There are 2 main sources for Glutamate, -ketoglutarate taken from the Krebs-cycle and Glutamine, which is partially delivered by glia cells.

Glutamate is an essential amino acid, it has to be included in the diet and is taken up directly into the blood stream which delivers it through the blood brain barrier to the brain.

A

There are 2 main sources for Glutamate, -ketoglutarate taken from the Krebs-cycle and Glutamine, which is partially delivered by glia cells.

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14
Q

P: Which of these statements about the Schild Method is false?
The Schild method requires binding to be at equilibrium.

The Schild method cannot estimate the number of binding sites in a receptor.

The Schild method provides a microscopically correct estimate of the binding affinity of a competitive antagonist.

The Schild method is appropriate for ligand gated ion channels, but not for metabotropic receptors.

The affinity of the agonist used does not affect the antagonist KB determined by Schild’s method.

A

The Schild method requires binding to be at equilibrium.

The Schild method cannot estimate the number of binding sites in a receptor.

The Schild method provides a microscopically correct estimate of the binding affinity of a competitive antagonist.

-> The Schild method is appropriate for ligand gated ion channels, but not for metabotropic receptors.

The affinity of the agonist used does not affect the antagonist KB determined by Schild’s method.

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15
Q

C: Benzodiazepines do not

A
Induce Cognitive Improvement
But does
Influence GABAergic function	
Have antiepileptic effects
Have a wide therapeutic range
Reduce anxiety
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16
Q

P: Which of these statements about agonists is correct?

A

Full agonists evoke stronger responses than partial agonists

17
Q

P: Which of these statements about ligands is correct?

A

Antagonists do not change the response of a receptor.

18
Q

P: Computational drug design

A

allows the identification of promising novel therapeutic agents that can be refined with other methods.

Not true:

  • only works if you want to design lipophilic molecules.
  • cannot be used to design a drug that passes BBB
19
Q

A: Muscle relaxants do not

  • act as agonist @NMJ
  • depolarize memb
  • relax skeletal muscle
  • induce anaesthesia
  • have adverse drug effects
A

Induce anaesthesia

20
Q

C: Dopaminergic drugs in Parkinsons disease do not
Promote dopamine synthesis
Decrease Ach levels by competitive mechanisms
Prevent DA degradation
Promote DA release
Act as receptor agonists at D2-R alone

A

Decrease Ach levels by competitive mechanisms

21
Q

B: Which of the following statement(s) is/are correct? About GABA synthesis

A

GABA is synthesized directly from Glutamate via Glutamatedecarboxylases. Two Isoforms of this enzyme exist, GAD65 and GAD67

22
Q

A: An indirectly acting parasympathomimetic drug acts

1) blocking Ach release
2) selective at muscarinergic R
3) Increasing acetycholine levels in the synaptic cleft
4) Lowering adrenaline levels significantly
5) Boosting GABAergic function

A

Increasing acetycholine levels in the synaptic cleft

23
Q

P: A partial agonist will

A

fix the ratio of inactive to active receptor at a given, agonist specific value, regardless of its concentration

24
Q

A: Beta-2-sympathomimetic drugs do not

1) Have an anabolic effect
2) Used as tocolytics
3) Dilate arterioles
4) Decrease heart rate
5) Cause bronchodilation

A

4)Decrease heart rate

25
Q

P: Glutamate receptors are amongst the best understood receptors in terms of mechanisms of activation because

1) numerous co-crystals of the ligand binding domain with a range of agonists and antagonists have been published
2) the crystal structure of the full length receptor revealed a single Glutamate binding site
3) glutamate acts at only one class od receptors, making it easy to work out all the details
4) each subtype is only expressed in a few cells in the brain
5) they are surprisingly simple molecules, consisting of only a single transmembrane helix

A

numerous co-crystals of the ligand binding domain with a range of agonists and antagonists have been published