Adrenergic Antagonist Eliud

Question 1

Phenoxybenzamine

Answer 1

Nonselective alpha antagonist (inhibits alpha 1 irreversibly)
-To treat Pheochromocytoma

Nitrógeno en el centro rodeado por dos anillos y un cloro que lo hace un electrofilo para enlazarse al receptor.

Question 2

Tolazoline and Phentolamine

Answer 2

Nonselective Alpha Antagonist
-To treat pheochromocytoma and hypertensive crisis by illicit drugs

Tolazoline - Nitrógeno en un un anillo de 5 y acompañado por un ciclo hexano. No puede tener grupos voluminosos en posición orto y/o para

Phentolamine - Nitrógeno en el centro acompañado de tres anillos

Question 3

Which are selective alpha 1 antagonist and put them in order of longest action duration. (Son medicamentos para hypertension and BPH)

Answer 3

1. Doxazosin (18-36 hr) por el grupo benzodioxane que es más estable y menos frágil
2. Terazosin (>18 hr) por el grupo tetrahydofuran (anillo de 5, no doble enlace)
3. Prazosin (4-6 hr) por el grupo furan (anillo de 5, doble enlace) más frágil

Question 4

Which are the three selective Alpha 1 A Antagonist? (for treating BPH)

Answer 4

Alfuzosin tiene una elongacion y un grupo furano
Tamsulosin tiene un grupo voluminoso terminando con CH3
Silodosin tiene un grupo voluminoso terminando en CF3

Question 5

Which of the following is the drug that we use today that have an oxymethylene bridge and is a nonselective beta blocker?
-Dichloroisoproterenol
-Pronethanol
-Propranolol

Answer 5

Propranolol

Question 6

What are the two essential thing a beta adrenergic antagonist must have to bind with the Asn of a Beta receptor?

Answer 6

-S configuration at the carbon and also have an OH group.

Question 7

What does R1 and R2 properties gives to a beta adrenergic antagonist?

Answer 7

Un grupo voluminoso en R1 le da mayor selectividad a receptores Betas que alphas

R2 determina Hidrofilicidad y selectividad. El anillo monosubstituido en para o disubstituido en orto y para le da beta selectividad.

Question 8

Determina la función de Nevivolol dependiendo de su configuración del centro esteriogenico.

Answer 8

The stereoisomer (+) SRRR is a selective Beta1 blocker

The stereoisomer (+) RSSS is a vasodialator (Increase Nitric Oxide)

Question 9

Which Beta Blocker has a structure exception to common beta antagonists?

Answer 9

Sotalol

Question 10

Labetalol (Mixed alpha and Beta Antagonists)

Answer 10

The R(OH), R(CH3) isomer is a nonselective beta blocker with minimal alpha 1 antagonism.

The R(OH), S(CH3) isomer is alpha 1 blocker.

Question 11

Carvedilol (Mixed alpha and Beta Antagonists)

Answer 11

The R enantiomer is a selective alpha 1 antagonist

The S enantiomer is both an alpha 1 antagonist and nonselective beta blocker

Question 12

Which drug inhibits Norepinephrine/Epinephrine Synthesis

Answer 12

Metyrosine

-Inhibits Tyrosine Hydroxylase