Drug ProfileREX

Question 1

ANS: Vesamicol

Answer 1

Inhibit Ach carrier, Ach can no longer be stored in vesicle

Question 2

ANS:Presynaptic toxins

Answer 2

e.g. botulinum

prevents release of NT

Question 3

ANS:Hemicholinium

Answer 3

Inhibit choline carrier, choline cannot be reuptake to presynapse hulting Ach production

Question 4

ANS:Anticholinesterase

Answer 4

e.g. neostigmine

inhibit AchE reaction, Ach cannot be broken down into choline and acetate, overresponse of Ach in synaptic cleft

Question 5

ANS:Non-depolarising blocking agent

Answer 5

e.g. tubocurarine

prevents Ach from binding to receptor

Question 6

ANS: Depolarising blocking agent

Answer 6

e.g. suxamethonium

activates Ach receptor on post synapse without Ach

Question 7

ANS: Atropine

Answer 7

muscarinic receptor blocker

Question 8

ANS: Ach

Answer 8

Direct acting parasympathomimetics

M- and N-agonist
extremly short life time
degraded by AChE
no therapeutic use

Question 9

ANS: Carbachol

Answer 9

Direct acting parasympathomimetics

M » N
slow substrat for AChE
use:
s.c. (not i.v.), local
oral:  Bioavailability 10%

Question 10

ANS: Betanechol

Answer 10

Direct acting parasympathomimetics

pure M-agonist

Question 11

ANS: Pilocarpine

Answer 11

Direct acting parasympathomimetics

no ester
AChE ineffective
tertiary nitrogen
penetrates into CNS
cardial effects (bradycardia)
after systemic administration
given locally

Question 12

ANS: Direct acting parasympathomimetics examples

Answer 12

Ach, carbachol, pilocarpine, betanechol, arecoline

Question 13

ANS: What decrease the Ach activity level in plasma?

Answer 13

organophosphates

Question 14

ANS: What increase the Ach activity level in plasma?

Answer 14

pralidoxime

Question 15

ANS: carbaminacid-ester

Answer 15

physostigmine, neostigmine, pyridostigmine

Question 16

ANS: Clonidine

Answer 16

presynaptic α2 agonist

with antihypertensive action

Question 17

ANS: Direct-acting adrenomimetics

Answer 17

α-adrenomimetics (activators of phospholipase C)
- antihypotensive drugs: Etilefrinе (Effortil), NE
- local nasal decongestants: Naphazoline,
Oxymetazoline, Xylometazoline (0.1% nasal drops)
- eye drops in glaucoma: Phenylephrine

Cardioselective α1-adrenomimetics: Dobutamine

DA-ergic adrenomimetics: Dopamine

Selective β2-adrenomimetics: Fenoterol, Hexoprenaline,
Salbutamol, Salmeterol, Terbutaline

Non-selective β-adrenomimetics: Iso- and Orciprenaline

α- and β-adrenomimetics: Adrenaline(antiallergic):
amp. 0,1% 1 ml s.c.; Anapen (0,3 mg/03 ml i.m.)

Question 18

ANS: Indirect-acting adrenomimetics

Answer 18

Antihypotensive drugs

Ephedrine, Mephentermine, Midodrine

Question 19

ANS: Which drug have effect after 3 to 5 min

and duration 4–6 h

Answer 19

Salbutamol

Fenoterol

Question 20

ANS: Which drug have Effect after 15–20 min

and duration 12 h

Answer 20

Salmeterol

Question 21

ANS: β2-adrenomimetics used for

Answer 21

tocolytic effect:
Fenoterol (Partusisten: tab. 5 mg)
Hexoprenaline
Salbutamol (Salbupart)
Terbutaline