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FDN2_SM_Drugs & Targets Flashcards

1
Q

What are _____-azapam drugs?

A

Long-lasting Benzodiazepines

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2
Q

Benzodiazepines have the suffix…

A

_____- azapam (long lasting)

_____- azolam (normal)

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3
Q

What are _____-azolam drugs?

A

Benzodiazepines (not long lasting)

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4
Q

Which CYP metabolizes ____-azapam drugs?

A

CYP2C19 (and maybe CYP3A4?)

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5
Q

What are ____-prazole drugs?

A

Proton pump inhibitors (Prazoles inhibit proton pumps)

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6
Q

What do benzodiazepines do?

A

They enhance the effect of GABA at the GABAA Receptor

The effects can be sedative, sleep-promoting, anti-anxiety, anticonvulsant, muscle relaxant

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7
Q

Which CYP metabolizes ____-prazole drugs?

A

CYP2C19 and CYP3A4

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8
Q

Which CYP metabolizes ____-azolam drugs?

A

CYP3A4

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9
Q

What are ____-olol drugs?

A

Beta-Blockers

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10
Q

What is the difference between Metoprolol and Propanolol?

A

Metroprolol is a selective Beta1 blocker

Propanolol blocks both Beta1 and Beta2 receptors

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11
Q

What does a beta1 blocker do?

A

Selective Beta1 blockers reduce cardiac contractility and output.

They are prescribed to treat high blood pressure (Example: Metroprolol)

(When activated, the Beta1 receptor increase heart contractions)

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12
Q

What does a non-selective beta blocker do?

A

Beta 1 effects: Inhibits cardiac contraction -> reduces cardiac contractility and

Beta 2 effects: inhibits smooth muscle relaxation

Prescribed for anti-arrhythmia, high blood pressure, and to improve survival after a heart attack

Example: Propanolol

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13
Q

What are ___-tidine drugs?

A

Histimine H2 Receptor Blockers (competitive antagonist); they prevent the secretion of gastric acid

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14
Q

Which CYP metabolizes ____-olol drugs?

A

CYP2D6

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15
Q

Whare are two examples of methylxanthines?

A

Caffeine, theophylline

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16
Q

How does cimitidine affect the metabolism of other drugs?

A

Cimitidine inhibits a lot of CYPS

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17
Q

How might caffeine and theophylline interact with other drugs?

A

Caffeine and theophylline are competitive inhibitors of adenosine.

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18
Q

Which CYP metabolizes caffeine and theophylline?

A

CYP1A2

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19
Q

Which CYP metabolizes NSAIDS?

A

CYP2C9

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20
Q

Which CYP metabolizes warfarin?

A

CYP2C9

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21
Q

Which CYP metabolizes clopidogrel?

A

CYP2C19 activates clopidogrel

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22
Q

What do Thiopurine drugs treat?

A

Some autoimmune-y disorders

Leukemia, IBD, organ transplantation rejection, rheumatic disease

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23
Q

Which CYP metabolizes codeine

A

CYP2D6 activates codeine

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24
Q

How does Ethanol affect acetaminophen toxicity?

A

At low levels, ethanol is metabolized by aldohol dehydrogenases.

At higher levels, ethanol:

- activates CYP2E1, which promotes the formation of toxic NAPQI

  • Inhibits GST, which saves hepatocytes from NAPQI by conjugating glutathione
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25
What is digoxin prescribed for?
Atrial Fibrilation Note: It has a narrow therapeutic window; Amenable to therapeutic drug monitoring
26
What do theophylline and caffeine do?
They are bronchodilators
27
What are caffeine and theophylline prescribed for?
They are prescribed as bronchodilators
28
Name 2 non-selective agonists of adrenergic receptors
Norepinephrine, epinephrine
29
Which adrenergic receptor is largely unaffected by norepinephrine?
Beta2
30
How are Beta 2 receptors activated by sympathetic action?
Sympathetic innervation to the adrenal medula causes the release of Epinephrine (80%) and Norepinephrine (20%). - Beta 2 receptors are activated - Gloal increase in all adrenergic receptor activation (coordinated effect of the fight or flight resposne)
31
What type of drug is phenylephrine? What does it do? What is it used for?
Selective alpha 1 agonist Increases vasoconstriction of smooth muscles Used to increase blood pressure during surgery, and decrease nasal congestion
32
What are 2 clinical uses of selective alpha 1 agonists?
Increase blood pressure during surgery/anesthesisa Nasal sprays decrease congestion
33
Which two drugs might you give durins spinal anesthesia to maintain the patient's heart rate and blood pressure?
**Phenylphrine**: Increase blood pressure **Atropine**: Inhibit drop in heart rate (acts via parasympathetic pathway) | (acts via sympathetic pathway)
34
What type of drug is an "-erol"? What do these drugs do? What are they used for?
Selective Beta2 agonist **-erol**s increase smooth muscle relaxation in airways They are used to treat airway disorders like **asthma** and **COPD**
35
What type of drug is metoprolol? What does it do? What is it used for?
Selective Beta 1 blocker (a competitive antagonist) Metoprolol decreases heart contractility It is used to treat high blood pressure and arrythmia with a sympathtic origin
36
What type of drug is propanolol? What does it do? What is it used for?
Non-selective Beta blocker (competitive antagonist of Beta 1 and Beta 2 adrenergic receptors) Propanolol nhibits heart contractility and smooth muscle relaxation =\> more forceful heart contractions, more constricted airway Propanolol treats hypertension
37
Describe a patient who you would need metoprolol instead of propanolol
A patient with hyperension and any respiratory disorder (asthma, COPD)
38
What type of drug is atropine? What does it do? What is it used for?
Muscarinic antagonist (competitive inhibitor) Increases heart rate Used during spinal anesthesia
39
What kind of drugs are "-tropium" drugs? What do they do? What are they used for?
Muscarinic antagonists (competitive inhibitors) -tropine drugs open airways They treat asthma and COPD
40
Which two drug classes can be used to treat asthma? Which branch of the autonomic nervous system does each drug act on?
- erol drugs (albuterol): sympathetic action; Beta 2 agonist, promotes airway relaxation - tropium drugs (ipratropium, tiptropium): parasympathetic action; muscarinic antagonist, inhibits airway constriction
41
At his office visit, your patient's blood pressure measures 150/100. You see on the medication list that the patient is already taking tiotropium. Which blood pressure medication would you prescribe, and why?
You would prescribe metoprolol Tiotropium indicates that the patient most likely has a respiratory disorder like asthma or COPD; therefore, you would **not** want to prescribe a blood pressure medication with a Beta 2 side-effect. **The patient needs a selective Beta 1 blocker to treat his blood pressure.**
42
Before a patient's visit, you see on their chart that they were prescribed phenylephrine at their last vist. What did this prescription most likely treat?
Nasal congestion Phenylphrine is an alpha-1 agonist that increases vasoconstriction. Phenylphrine can be used in surgery to increase blood pressure (which usually happens in the hospital and not at home), or as a nasal spray to treat congestion
43
What is Tetrodotoxin? What does it do?
Tetrodotoxin (TTX) is the pufferfish poison It blocks voltage-gated Na+ channels, preventing action potential initiation in **nerves and skeletal muscle** (Cardiac and smooth muscle are not sensitive to TTX)
44
What agent cleaves SNARE SNAP-25?
Botulinum Toxin Type A (Botox A)
45
What do botulinum toxins do? What are they used for?
Botunlinum toxins irreversibly cleave a specific part of one of 3 SNARE proteins This prevents priming of the ACh release machinery, and therefore, the release of ACh, in somatic neuromuscular signaling Botox A is used to treat spasticity (epilepsy, blepharospasm) by cleaving SNARE SNAP-25
46
Which agent acts at the neuromuscular junction of the somatic nervous system to treat epilepsy? How?
Botox A Cleaves SNARE SNAP-25 to prevent priming of the fusion machinery and the subsequent release of ACh This prevenst muscle contraction
47
What type of drug is a "-curonium" drug? What do they do? What are they used for?
-curonium drugs are non-depolarizing nicotinic receptor blockers (competitive inhibitors) They are competitive inhibitors of ACh at nicotinic receptors; they prevent muscle contraction They are used to relax skeletal muscle in surgical procedures
48
What drug would you give to a patient to relax skeletal muscles during surgery?
a -curoinium drug (rocuronium, vecuronium)
49
What type of drug is succinylcholine? What does it do? What is it used for?
Succinylcholine is a fast-acting **noncompetitive** depolarizing blocker It rapidly activates and then inactivates skeletal muscle It is used to relax skeletal muscle in intubation | (2 ACh molecules end to end)
50
Emergency!! You need to inubate your patient? What agent do you give them to make intubation easier?
Succinylcholine; it rapidly relaxes skeletal muscle
51
What type of drug is neostigmine? What does it do? What is it used for?
Neostigmine is a **reversible inhibitor** of acetylcholinesterase By inhibiting the enzyme that degrades ACh, neostigmine acts to **increase ACh concentration** in the synaptic cleft It is used to improve cholinergic signaling when nicotinic and muscarinic receptors are imparied (ex: Myasthenia Gravis)
52
Which drug would you prescribe to treat myasthenia gravis? Why?
Neostigmine - A competitive inhibitor of Acetylcholinesterase (The drug competes with ACh) Myasthenia Gravis is a disease that destroys nicotinic ACh receptors. Neostigmine -\> ACh stays in the synaptic cleft longer -\> improves signaling even with few receptors
53
Which drug woud you prescribe to inhibit AChE? Why would you want to do this?
Neostigmine inhibits AChE AChE (acetylcholinesterase) degrades ACh so it can be re-updaken by the nerve ending and recycled. Inhibiting AChE results in increased ACh in the synaptic cleft. You would prescribe neostigmine to patients with reduced or impaired nicotinic or muscarinic receptors.
54
55
What do vecuronium and succinylcholine have in common? What is different about them?
Both drugs are nicotinic receptor blockers Vercuronium is a non-depolarizing blocker, used to relax skeletal muscle during surgery Succinylcholine is a rapid depolarizing blocker, used to relax skeletal muscles for intubation
56
Which drugs would you use as non-depolarizing nicotinic receptor blockers during surgery?
-curonium drugs (Rocuronium, vecuronium)
57
What substances would reduce the effect of adenosine as a method to treat tachycardia?
Caffeine and theophylline
58
What is quinidine?
Class I anti-arrhythmic drug ## Footnote **Note: it has a high affinity for p-glycoprotein, which means that it may have significant interactions with other drugs (the other drugs may be displaced)**
59
How does quinidine affect p-glycoprotein?
Quinidine has a high affinity for p-glycprotein. This can displace other drugs from P-glycoprotein, resulting increased levels of these drugs in the body due to: 1. Increased absorption of these drugs from the intestine 2. Decreased tubular secretion of these drugs in the renal tubule
60
Describe the interaction of quinidine and digoxin
Quinidine and digoxin use the same transporters to get into the renal tubule from the bloodstream. Quinidine impairs the renal clearance of digoxin by displacing it from the transporter during tubular secretion

FDN2 (14 decks)

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