FDN2 Drugs Week 1 and some CYP stuff

Question 1

What does Diazepam do?

Answer 1

It is a benzodiazepine and thus acts as an Allosteric activator of GABAA receptors

This benzo binding increases the frequency of opening of GABA_A-gated Cl^- channels and enhances synaptic inhibition. The TI for diazepam is very good (~100)

Used to treat anxiety, to produce sleep and reduce muscle spasms.

Question 2

What is Warfarin used for?

Answer 2

The effect of this block is to inhibit the synthesis of clotting factors.

Used clinically to prevent blood clots after surgery and to treat atrial fibrillation.

Question 3

Drugs with -setron suffix do what?

Answer 3

Competitive inhibitors of Serotonin 5HT-3. Treat Nausea and vomiting.

Question 4

What does Memantine do?

Answer 4

Open channel blocker of NMDA receptors.

Question 5

This drug is a positive allosteric modulator and it can be prescribed for sleep for years without a waning of the effect

Answer 5

Zolpidem

Question 6

azepam or ..azolam suffix is seen in what drugs?

Answer 6

Benzodiazepines

Question 7

What receptor does Penicillin produce major side effects on?

Answer 7

Blocks the open channel GABAA receptor channel and inducing seizures.

Question 8

What does strychnine do?

Answer 8

It is a glycine receptor competitive inhibitor.

Question 9

What does tetanus toxin do?

Answer 9

It is a presynaptic inhibitor of glycine receptors.

Question 10

What receptor is effected by the disease hyperekplexia?

Answer 10

Glycine receptors. Mutated alpha subunits.

Question 11

Fluticasone and drugs with a -son or -one suffix bind where?

Answer 11

Cytoplasmic glucocorticoid receptor.

Question 12

What does minoxidil do?

Answer 12

Activation of KATP channels by minoxidil causes membrane hyperpolarization, closure of voltage-gated calcium channels, and vasodilation

Question 13

What does tetrodotoxin (TTX) do?

Answer 13

Blocks voltage-gated Na+ channels in nerve and muscle (TTX acts like a plug at the extracellular surface of the voltage-gated sodium channel)

Question 14

What do local anesthetics do?

Answer 14

Blocks the voltage-gated Na+ channel associated with the action potential. (The main difference between local anesthetics and TTX is that local anesthetics preferentially bind to the inactivated state of the Na+ channel)

Question 15

Where are Furanocoumarins found and what do they do?

Answer 15

found in grapefruit inhibit CYP3A4 and p-glycoprotein

Question 16

What is the target of SSRIs?

Answer 16

SLC6A4

Question 17

Penicillin is what type of inhibitor?

Answer 17

Uncompetitive

Question 18

What type of inhibitor is memantine?

Answer 18

Uncompetitive

Question 19

What is IL-5’s primary signaling mechanism?

Answer 19

JAK/STAT pathway

Question 20

What are two examples of adenosine receptor agonists?

Answer 20

Caffeine and theophylline (Methylxanthines)

Question 21

What do NSAIDs do?

Answer 21

Block COXs

Question 22

Celecoxib and Ibuprofen are what type of drugs?

Answer 22

NSAIDs

Question 23

The majority of Phase 1 reactions are handled by___

Answer 23

CYP3A4

Question 24

Most common polymorphisms of CYPs are seen in this CYP.

Answer 24

CYP2D6

Question 25

What are CYP2C19 substrates?

Answer 25

- …**azepam** benzos (di**azepam**, flur**azepam**, etc.) - **Proton pump inhibitors** (the ..**prazole**s, such as ome**prazole-****also CYP 3A4**) - **Clopidogrel (Plavix)** a prodrug activated by this CYP (and others) but it is 2C19 where polymorphisms are important

Question 26

Ethanol at high concentrations induces what CYP?

Answer 26

CYP2E1

Question 27

This CYP converts codeine to morphine.

Answer 27

CYP2D6

Question 28

Metoprolol and opioids are substrates for this CYP.

Answer 28

CYP2D6

Question 29

Acetominophen is made into what toxic compound and by what CYP?

Answer 29

NAPQI by CYP2E1.

Question 30

Insulin receptors stimulate what pathways?

Answer 30

RAS/MAPK: Growth PI-3K/AKT/mTOR: Metabolic

Question 31

EGF Receptors stimulate what pathway?

Answer 31

RAS/MAPK

Question 32

What does Phenylephrine do?

Answer 32

Acts to increase blood pressure and to decrease nasal congestion. Agonist at alpha-1 adrenoreceptors