Adrenergic drugs

Question 1

Drugs and MOA of alpha 2 receptor agonists.

Answer 1

Clonidine and Methyldopa- activation of a2 rors decreasing release of NE. For HTN

Question 2

These drugs constrict smooth muscles such as pupillary dilator, prostate GI tract, bladder, pilomotor and uterus) Inc ♥️ contract. and drug examples with indications.
glycogenolysis, gluconeogenesis

Answer 2

Alpha-1 agonists:
E- septic/anaphylactic shock
Midodrine- orthostatic hypotension
Phenylephrine- nasal decongestant

Question 3

They increase ♥️ force and rate, renin secretion from kidneys and ghrelin secretion from stomach. Drugs and indications.

Answer 3

Beta 1 agonists:

Dobutamine and Iso, Prenalterol- CHF, cardiogenic shock

Question 4

For asthma:
SABA: Terbutaline, salbutamol, prenalterol
LABA: salmeterol, formoterol

Answer 4

Beta 2 agonists: Bronchodilation, increases K uptake in muscles, glycogenolysis, gluconeogenesis, lipolysis

Question 5

Sympathomimetics SAR

Answer 5

• C3 and C4 aryl OHs elevate potency but dec. oral bioav and duration of action
• Larger the alkyl subs. on amino grp, greater Beta selectivity
• alpha-C subs. prolongs DOA by interfering w dg Ox’n by MAO
• Beta OH facilitates ror activation

Question 6

As you increase DOPA dose what happens with A and B effects

With Epinephrine dose?

Answer 6

DOPA: vasoconstriction (b-effect)
VD (a-effect)
E: VD (b)
VC (a)

Question 7

Action for B3 agonists and main location, drug example and indication.

Answer 7

Adipose tissue and bladder: relaxes detrusor muscle, lipolysis and thermogenesis
Mirabegron for overactive bladder

Question 8

Alpha antagonists for HTN and BPH drug examples.

Answer 8

Alpha 1 ant: Prazosin (shortest) Tera Doxa (longest and Tamsulosin
Used for Pheochromocytoma
A1 and 2: Phentolamine
Irrev ant: Phenoxybenzamine

Question 9

A2 agonist with SE rebound HTN

Answer 9

Clonidine

Question 10

A1 antagonist with SE syncope

Answer 10

Terazosin

Question 11

Mostly replaced by phosphodiesterase inhibitors for erectile dysfunction.

Answer 11

Alpha 1 antagonists

Question 12

Non selective Beta blockers.

B and A blockers.

Answer 12

• Nado, Timo, Propranolol

- Carve and Labetalol

Question 13

B blockers with Intrinsic Sympathomimetic Activity

Answer 13

Acebutalol, Pindolol

Question 14

About SNS (differentiating from PSNS)

Answer 14

Originates from thoracic and lumbar regions
short preganglionic, long post nerve fibers
ganglia near spinal cord
NT: E NE DOPA ACh

Question 15

Adrenergic receptors and classifications.

Answer 15

a1- postsynaptic in the SNS
a2- pre in the SNS and post in the brain
b1- in the heart
b2- sympathetically innervated structures

Question 16

SAR. What ring system does a-blockers contain attached to a piperazine ring?

Answer 16

4-amino-6-7-dimethylxoquinazoline ring system

Question 17

SAR. Reduction of this ring of Prazosin to the ring of Terazosin alters metabolism rate.

Answer 17

Reduction of furan ring of Prazosin to the tetrahydrofuran ring of Terazosin increases DOA by altering metabolism rate.

Question 18

BB drugs that are renally cleared?

Cleared by the liver?

Answer 18

• Hydrophilic: Ateno, Nadolol

- Lipophilic: Propra, Pindo, Metoprolol (hepatic elimination)

Question 19

The only BB that can be used for anxiety, CNS SEs insomia, depression and vivid dreams. Why?

Answer 19

Propranolol can penetrate into the CNS

Question 20

These BB drugs block b2 rors in ciliary muscles (produces aqueous humor)

Answer 20

Timo, Betaxo, Metoprolol