Cholinergics And Adrenergics

Front 1

synaptic location of parasympathetic preganglionic neuron

Back 1

ganglia near organ innervated

Front 2

synaptic location of sympathetic preganglionic neuron

Back 2

ganglia located near spinal cord

Front 3

neurotransmitter for parasympathetic preganglionic and postganglionic neuron

Back 3

ACh for both

Front 4

neurotransmitter for sympathetic preganglionic and postganglionic neuron

Back 4

ACh for preganglionic and NE for postganglionic

Front 5

M1 receptor

Back 5

neural

Front 6

M2 receptor

Back 6

cardiac

Front 7

M3 receptor

Back 7

glandular

Front 8

Two types of nicotinic receptor?

Back 8

ganglionic and NMJ

Front 9

For cholinergic agonist, describe change in airway resistance, GI function, pupil function

Back 9

increase airway resistance
increase GI motility
pupils will contract (miosis)

Front 10

How is ACh synthesized?

Back 10

acetyl CoA + choline, w/ choline acetyltransferase as enzyme

Front 11

benthenacol

Back 11

- directly acting muscarinic agonist
- stimulate atonic bladder
- not degraded by AChE

Front 12

carbachol

Back 12

- directly acting muscarinic agonist
- can be used to treat glaucoma... but is rarely used
- resistant to AChE

Front 13

pilocarpine

Back 13

- directly acting muscarinic agonist
- drug of choice to treat glaucoma (esp emergency)
- resistant to AChE

Front 14

physostigmine

Back 14

- reversible cholinesterase inhibitor
- used to treat atony of GI and bladder

Front 15

neostigmine

Back 15

- reversible cholinesterase inhibitor
- treat symptomatic myasthania gravis

Front 16

pyridostigmine

Back 16

- reversible cholinesterase inhibitor
- treat chronic myasthania gravis
- duration of action is longer than neostigmine

Front 17

edrophonium

Back 17

- reversible cholinesterase inhibitor
- diagnosis of myasthania gravis
- short duration of action

Front 18

isofluorate

Back 18

- irreversible cholinesterase inhibitor
- can be used for open-angle glaucoma (echotiophate is used instead)

Front 19

pralidoxine

Back 19

- aka 2-PAM
- used to reactivate AChE that has been inhibited by isofluorate
- cannot penetrate CNS

Front 20

atropine

Back 20

- given iv
- to treat bradycardia after MI

Front 21

tropacamide
cyclopentolate

Back 21

- to dilate pupil
- tropacamide short acting
- cyclopentolate long acting
- muscarinic antagonist

Front 22

scopolamine

Back 22

- prevent motion sickness

Front 23

benztropine

Back 23

- parkinson's
- muscarinic antagonist

Front 24

ipratropium

Back 24

- inhibit bronchoconstriction
- treat asthma
- muscarinic antagonist

Front 25

dicyclomine

Back 25

- irritable bowel syndrome
- colonic diverticular disease
-muscarinic antagonist

Front 26

pirenzepine

Back 26

- peptic ulcer disease
- muscarinic antagonist

Front 27

nicotine

Back 27

- low conc - ganglionic stimulation
- high conc - ganglionic blockade
- both sympathetic and parasympathetic are stimulated

Front 28

hexamethonium
trimethaphan
trbucurarine

Back 28

- block all autonomic ganglia and enteric ganglia
- hypotension, loss of cardiovascular reflexes, inhibition of secretions, GI paralysis, impaired micturition
- clinically obsolete except trimethaphan

Front 29

substances that block choline uptake

Back 29

hemicholinium
triethylcholine

Front 30

substances that block ACh release

Back 30

aminoglycoside antibiotics
botulinum toxin

Front 31

drugs used to cause paralysis during anaesthesia

Back 31

turbocurarine
gallamine
pancuronium
atracurium
succinylcholine

Front 32

curare

Back 32

- non-depolarizing competitive blocker
- in low conc, combines with nAChR and prevents binding of ACh
- in high conc, blocks ion channels

Front 33

succinylcholine

Back 33

- depolarizing blocker
- binds to nAChR, acts like ACh and depolarizes muscle
- not destroyed by AChE
- causes flaccid paralysis
- adverse effects: hyperthermia, apnea

Front 34

B1 receptors are found on.... (3)

Back 34

heart
kidney
fat cells

Front 35

B2 receptors are found on.. (3)

Back 35

BRONCHIAL tree
ciliary muscle
detrusor muscle

Front 36

a1 receptors are found on...

Back 36

ARTERIES
uterus
ureter/trigone/spincter
SMOOTH MUSCLE
secretion/glands
..everything basically

Front 37

a2 receptors are found on

Back 37

GI
bronchial tree
insulin from pancreas

Front 38

What is the rate limiting step in the synthesis of norepinephrine?

Back 38

tyrosine -> DOPA
w/ tyrosine hydroxylase

Front 39

COMT metabolizes norepinephrine and epinephrine into what products?

Back 39

norepinephrine -> normetanephrine

epinephrine -> metanephrine

Front 40

Which receptors does epinephrine act on?

Back 40

ALL adrenergic receptors (a1, a2, b1, b2)

Front 41

In terms of skeletal muscle dilatation, how do epinephrine, norepinephrine, and isoproterenol differ?

Back 41

Epi and Iso dilate skeletal muscle vessals, NE does not

Front 42

Which receptors does isoproterenol act on, and what is its major effect?

Back 42

- b1 and b2
- major cardiac effect (increases HR, decreases peripheral resistance)
- used for emergency heart situations

Front 43

Why is dopamine the choice drug for shock?

Back 43

- has an effect on heart function (b1)
- also causes renal and messenteric vasodilation b/c of D1 and D2... this increases kidney blood flow, glomerular filtration rate and Na+ diuresis which the other drugs do not do

Front 44

What are the differences between cathecholamines and noncatecholamines?

Back 44

- C are rapidly metabolized by COMT/MAO, NC are not
- C have poor CNS penetration b/c they are polar... NC are more lipid soluble therefore can penetrate CNS
- NC have longer duration of action

Front 45

What are the major uses for epinephrine?

Back 45

- acute asthma attack (bronchodilation, b2)
- anaphylactic shock
- glaucoma (applied topically to reduce intra-ocular pressure.. decreased production of aqueous humor)
- anaesthetic

Front 46

What receptor does dobutamine act on and what is its therapeutic use?

Back 46

b1, used to increase CO in congestive heart failure

Front 47

What receptor does phenylephrine act on and what is its use?

Back 47

- a1 agonist
- used as nasal decongestant (vasoconstrictor)

Front 48

methoxamine receptor and use

Back 48

- a1 agonist
- used to raise blood pressure during surgery (also raises TPR)

Front 49

How does clonidine lower blood pressure in essential hypertension?

Back 49

- a2 receptor
- dimishes sympathetic outflow from medulla, which decreases CO, TPR and HR

Front 50

albuterol
pirbuterol
terbutaline
salmeterol

Back 50

- b2 bronchodilators
- duration of action varies

Front 51

amphetamine

Back 51

- indirect acting agonist
- peripheral action via release of stored catecholamines..
- can increase BP and stimulate heart

Front 52

tyramine

Back 52

- enters nerve terminal and displaces stored NE.. can increase BP
- not a useful clinical drug
- found in ripe cheese and wine

Front 53

phentolamine

Back 53

- direct acting antagonist (a)
- causes postural hyptension
- reflex cardiac stim. and tachycardia; blocks a2 receptors on cardiac sympathetic nerves

Front 54

phenoxybenzamine

Back 54

- noncompetitive, irreversible alpha antagonist
- not useful in maintaining lower BP in hypertension
- used in pheochromocytoma removal

Front 55

prazosin
terazosin
tamsulosin

Back 55

- alpha 1 blockers (competitive)
- treat hypertension
- "first-dose" exaggerated hypotensive effect

Front 56

propranolol

Back 56

- nonspecific beta blocker (competitive)
- decreases HR, BP, CO
- bronchostriction
- increased Na+ retention and plasma volume can lead to compesatory increase in BP
- used to treat glaucome, hypertension, migraine, hyperthyroidism, angina, MI patient to prevent second heart attack

Front 57

What receptor(s) does propanolol affect?

Back 57

b1 and b2. .nonspecific beta blocker

Front 58

Why might propanolol lead to a compensatory increase in blood pressure?

Back 58

b/c decreased blood pressure and renal perfusion leads to Na+ retention and plasma volume

Front 59

What are the therapeutic uses for propanolol?

Back 59

- glaucoma (decrease secretion of aqueous humor)
- migraine
- hyperthyroidism
- angina
- MI patient

Front 60

timolol and nadolol

Back 60

nonspecific b1 and b2 blockers
more potent than propanolol
timolol useful for glaucoma

Front 61

atenolol
acebutolol
pindolol

Back 61

b1 specific blocker
lower blood pressure in hypertension (esp diabetic)
acebutolol and pindolol are partial agonists

Front 62

carvedilol
labetalol

Back 62

alpha and beta blockers
reduce blood pressure

carvedilol benefits heart failure patients
labetalol for black hypertensives

Front 63

reserpine

Back 63

- affects transport of catecholamines from cytoplasm to storage vehicles
- therefore MAO metabolizes cytoplasmic NE
- gradual decline in blood pressure

Front 64

guanethidine

Back 64

- blocks release of stored NE
- gradual decline of BP and HR
- rarely used

Front 65

cocaine

Back 65

blocks Na-K-APTase which is needed for NE uptake

NE accumulate in synaptic cleft, duration of NE action increased

Front 66

amitriptyline

Back 66

tricyclic antidepressant
prevent uptake of NE and serotonin

Front 67

phenelzine

Back 67

MAO inhibitor
similar to normal substrate of MAO; binds covalently to MAO and inactivates it

Front 68

ephedrine

Back 68

mixed action adrenergic agonist
- induce release of NE from presynaptic terminals and activate post synaptic adrenergic receptors
- not metabolized by MAO or COMT
- raises BP, bronchodilator
- penetrates CNS