Exam #4

Question 1

3-methoxy-4hydroxy-mandelic acid

Answer 1

The result of metabolism of NE and Epi

Measure if trying to know the amount of catacholamine in the body

Question 2

Isoproterenol

Answer 2

Non-selective beta agonist

Example for structure

Beta-selective means isopropyl group is large and thus not a good substrate for MAO

Question 3

Metaproterenol

Answer 3

B-2 agonist

Treats asthma, causes bronchodilation (inhaled)

Rapid onset and longish 1/2 life (6hrs)

Not good substrate for MAO or COMT

Question 4

Albuterol

Answer 4

B-2 agonist

Treats acute asthma, causes bronchodilation (inhaled)

Rapid onset

1:1 racemic mix of R and S

Question 5

Salmeterol

Answer 5

Long acting B-2 agonist

Large lipophilic group (more selective to B-2)

Long onset and 1/2 life

Used with fluticasone (corticosteroid) to treat inflammation

Question 6

Formoterol

Answer 6

Long acting B-2 agonist

Amide type function

Long duration and onset

Used with corticosteroid

Question 7

Mirabegron

Answer 7

B-3 selective agonist (has some selectivity for B-1 and B-2 but not much)

Results in the relaxation of the bladder for incontinence

Question 8

Naphazoline

Answer 8

A-1 agonist

Nasal and ophthalmic decongestant

Must get into the CNS to work

Question 9

Guanfacine

Answer 9

A-2a agonist

Affects the CNS receptors (allowed by ketone group)

Anti-hypertensive and causes bradycardia

Question 10

Brimonidine

Answer 10

A-2b agonist

First line treatment for glaucoma

Causes outflow and decrease in formation of aqueous humor

Question 11

Ephedrine

Answer 11

Sympathomimetic agonist with mixed MOA

D-(-)-Ephedrine is the most potent

No -OH on aromatic ring (detriment to potency but prevents COMT metabolism)

CH3 on alpha-C disallows MAO metabolims (also causes indirect effect)

Interact directly with receptors and indirectly by releasing endogenous NE from neurons

Question 12

Pseudophedrine

Answer 12

Sympathomimetic Indirect acting agonist

Nasal decongestant

diasteriomer of ephedrine (wrong sterochem to interact with receptor)

Releases NE from nerve end

Not as potent as ephedrine

Question 13

Metyrosine

Answer 13

Adrenergic blocking agent

Blocks synthesis of NE and Epi to cause to lower BP

Treats Phenochromocytoma (overproduction of NE and Epi)

competitive inhibitor of tyrosine hydroxylase

Take with lots of water to reduce crystallization and reduce kidney damage

Question 14

Prazosin

Answer 14

A-1 antagonist

anti-hypertensive (A-1b - vasodilation) and benign prostate hypertrophy (A-1a - relaxes bladder neck and prostate) to help urinate

Can cause orthostatic hypotension at first

Question 15

Tamsulosin

Answer 15

A-1a antagonist

Relaxes bladder neck, prostate, ureter, and urethra to help urinate

Less orthostatic hypotension side effects

Question 16

Propranolol

Answer 16

Non-selective B-antagonist

Treats hypertension, angina, cardiac arrhythmias, migraines, stage fright

Contraindicated in those with asthma and COPD

Question 17

Metoprolol

Answer 17

B-1 antagonist

Treats hypertension

Less bad for those with COPD and asthma

Question 18

Carvedilol

Answer 18

Dual A and B antagonist

hypertension, urinary problems, heart problems

Antioxidant properties due to carbazole ring (good for those with minor myocardial infarction - mitigates ROSs)

higher selectivity and potency for Beta receptors (B-1)

better than other beta blockers

Question 19

Nebivolol

Answer 19

B-1 antagonist with vasodilatory properties

No release ((-)-isomer) causes vasodialatory effect

(+)-isomer for B-1 antagonist

Question 20

Edrophonium

Answer 20

Reversible competitive inhibitor of acetylcholinesterase

diagnostic agent to diagnose myasthenia gravis (antibodies inhibit Ach receptors)

rapid onset and short duration

Question 21

Donepezil

Answer 21

Reversible inhibitor of acetylcholinesterase

Treats Alzheimer’s

Affects the CNS by enhancing cholinergic neurotransmission in the CNS

Question 22

Huperzine

Answer 22

Reversible competitive inhibitor of acetylcholinesterase

natural product

Question 23

Rivastigmine

Answer 23

Pseudo reversible carbamate inhibitor

Treats Alzheimer’s by enhancing cholinergic transmission in CNS

Gets into CNS and inhibits Ach esterase by carbomylation

Question 24

Varenicline

Answer 24

Cholinomimetic muscarinic partial agonist

Smoking cessation

A-4-B-2 receptor partial agonist in CNS

Will act as an antagonist in the presence of a full agonist. When the full agonist is not present, the partial agonist acts as a partial agonist.

Contraindicated in those with neurophysciatric problems. Can cause anger (banned for pilots and traffic controllers)

Question 25

Ipratropium

Answer 25

Muscarinic antagonist

Given by inhalation to treat COPD and asthma

non-selective to all muscarinic receptors, so given by inhalation to target M3 and cause bronchodilation

slow onset and longer lasting

Question 26

tiotropium

Answer 26

Muscarinic antagonist

Given by inhalation to treat COPD and asthma

kinetic selectivity towards M3, so is kinda selective and also long lasting

slow onset and longer lasting

Question 27

Umeclidinium

Answer 27

Muscarinic antagonist

Potentially used for Asthma and COPD

Has quinuclidine base that helps binding

kinetic selectivity towards M3, so selective and also long lasting

slow onset and longer lasting

Question 28

Oxybutynin

Answer 28

Muscarinic antagonist

primarily target bladder to help control overactive bladder

Not selective for M3

can be used with B-3 agonists

Question 29

darifenacin

Answer 29

Muscarinic antagonist

primarily target bladder to help overactive bladder

Selective for M3, help mitigate cardiovascular effect from Oxybutynin

Question 30

Succinylcholine

Answer 30

Depolarizing neuromuscular blocking drug

block NMJ and cause desensitization and transmission blockade

Used for intubation and muscle relaxant with quick recovery