FDN2_SM_Drugs & Targets Flashcards
What are _____-azapam drugs?
Long-lasting Benzodiazepines
Benzodiazepines have the suffix…
_____- azapam (long lasting)
_____- azolam (normal)
What are _____-azolam drugs?
Benzodiazepines (not long lasting)
Which CYP metabolizes ____-azapam drugs?
CYP2C19 (and maybe CYP3A4?)
What are ____-prazole drugs?
Proton pump inhibitors (Prazoles inhibit proton pumps)
What do benzodiazepines do?
They enhance the effect of GABA at the GABAA Receptor
The effects can be sedative, sleep-promoting, anti-anxiety, anticonvulsant, muscle relaxant
Which CYP metabolizes ____-prazole drugs?
CYP2C19 and CYP3A4
Which CYP metabolizes ____-azolam drugs?
CYP3A4
What are ____-olol drugs?
Beta-Blockers
What is the difference between Metoprolol and Propanolol?
Metroprolol is a selective Beta1 blocker
Propanolol blocks both Beta1 and Beta2 receptors
What does a beta1 blocker do?
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)
What does a non-selective beta blocker do?
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
What are ___-tidine drugs?
Histimine H2 Receptor Blockers (competitive antagonist); they prevent the secretion of gastric acid
Which CYP metabolizes ____-olol drugs?
CYP2D6
Whare are two examples of methylxanthines?
Caffeine, theophylline
How does cimitidine affect the metabolism of other drugs?
Cimitidine inhibits a lot of CYPS
How might caffeine and theophylline interact with other drugs?
Caffeine and theophylline are competitive inhibitors of adenosine.
Which CYP metabolizes caffeine and theophylline?
CYP1A2
Which CYP metabolizes NSAIDS?
CYP2C9
Which CYP metabolizes warfarin?
CYP2C9
Which CYP metabolizes clopidogrel?
CYP2C19 activates clopidogrel
What do Thiopurine drugs treat?
Some autoimmune-y disorders
Leukemia, IBD, organ transplantation rejection, rheumatic disease
Which CYP metabolizes codeine
CYP2D6 activates codeine
How does Ethanol affect acetaminophen toxicity?
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
What is digoxin prescribed for?
Atrial Fibrilation
Note: It has a narrow therapeutic window; Amenable to therapeutic drug monitoring
What do theophylline and caffeine do?
They are bronchodilators
What are caffeine and theophylline prescribed for?
They are prescribed as bronchodilators
Name 2 non-selective agonists of adrenergic receptors
Norepinephrine, epinephrine
Which adrenergic receptor is largely unaffected by norepinephrine?
Beta2
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)
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
What are 2 clinical uses of selective alpha 1 agonists?
Increase blood pressure during surgery/anesthesisa
Nasal sprays decrease congestion
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)
What type of drug is an “-erol”?
What do these drugs do?
What are they used for?
Selective Beta2 agonist
-erols increase smooth muscle relaxation in airways
They are used to treat airway disorders like asthma and COPD
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
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
Describe a patient who you would need metoprolol instead of propanolol
A patient with hyperension and any respiratory disorder (asthma, COPD)
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
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
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
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.
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
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)
What agent cleaves SNARE SNAP-25?
Botulinum Toxin Type A (Botox A)
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
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
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
What drug would you give to a patient to relax skeletal muscles during surgery?
a -curoinium drug (rocuronium, vecuronium)
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)
Emergency!! You need to inubate your patient? What agent do you give them to make intubation easier?
Succinylcholine; it rapidly relaxes skeletal muscle
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)
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
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.
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
Which drugs would you use as non-depolarizing nicotinic receptor blockers during surgery?
-curonium drugs (Rocuronium, vecuronium)
What substances would reduce the effect of adenosine as a method to treat tachycardia?
Caffeine and theophylline
What is quinidine?
Class I anti-arrhythmic drug
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)
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:
- Increased absorption of these drugs from the intestine
- Decreased tubular secretion of these drugs in the renal tubule
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
