Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

581 - Pharmacology I > Exam 5 - Cholinergic Antagonists & Adrenergic Receptors > Flashcards

Exam 5 - Cholinergic Antagonists & Adrenergic Receptors Flashcards

(60 cards)

Start Studying
1
Q

Cholinergic agonists site of action

A
  • Pre-ganglion of adrenal medulla/sympathetic/parasymp
  • Post-ganglion of parasympathetic
  • skeletal muscle
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Cholinergic antagonist site of action

A 
- Same as cholinergic agonists...but in sub-groups
Sub-groups:
- Selective muscarinic blockers
- Ganglionic blockers
- Neuromuscular blockers
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Cholinergic antagonist

A
  • bind to cholinoceptors and prevent effects of Ach/cholinergic agonists
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Selective muscarinic blockers

A
  • Most clinically useful
  • Block at post-ganglion of parasympathetic
  • anticholinergic/muscarinic agents
  • parasympolytics
  • sympathetic stimulation not interrupted
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Ganglionic blockers

A
  • block nicotinic receptors of sympathetic and parasymp preganglia
  • are not selective…block all ANS
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Neuromuscular blockers

A
  • block impulses to skeletal muscles
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Antimuscarinics

A
  • one of selective muscarinic blockers
  • most can selectively block (except Atropine)
  • block sympathetic cholinergic neurons (sweat/salivary glands)
  • No action at NMJ
  • No action at autonomic ganglia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Atropine

A
  • Belladonna alkaloid
  • Competitive
    Actions:
  • eye dilation (like at eye doctor)
  • GI relax
  • dry mouth/ no sweat/ no tears
  • high dose: increase HR (block SA node)
  • low dose: decrease HR (block autoreceptors)

Uses:

  • Relax GI for IBS
  • treat bradycardia
  • block respiratory secretions for pre-op
  • antidote for organophosphate poisoning or agonist overdose
  • AV block
  • Pulseless electrical activity
  • ENTERS CNS

Dose: 1.0 mg/ml

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Scopolamine

A

Like atropine but…

  • longer duration
  • better on CNS

Uses:

  • motion sickness
  • nausea / vomiting
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Ipratropium (Atrovent)

A
  • Derivative of atropine
  • Bronchodilator for COPD
  • Inhaled
  • Positive charge…can’t enter systemic circulation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Emphysema

A
  • destruction and enlargement of air spaces
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Bronchitis

A
  • increased mucosa and inflammation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

COPD

A
  • Emphysema w/ chronic bronchitis
  • Irreversible block of airflow
  • smoking greatest risk factor
  • therapy aimed at symptoms and prevention of progression
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Benztropine (Cogentin)

A
  • centrally acting

- treat Parkinson’s tremors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Parkinson’s Disease

A
  • Decrease in dopaminergic activity
  • leads to imbalance with cholinergic activity
  • too much Ach activity in Parkinson’s
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Glycopyrrolate (Robinul)

A
  • for peptic ulcers
  • pre-op to reduce secretions in mouth/throat/airway
    • prevent aspiration
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Adverse effects of antimuscarinics

A
  • blurred vision
  • confusion
  • mydriasis (eye dilation)
  • tachycardia
  • constipation
  • urinary retention
  • bad for glaucoma (stops drainage of vitreous)
  • blocks parasympathetic outflow
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Atropine poisoning

A
  • Hot as a hare
  • Dry as a bone
  • Blind as a bat
  • Red as a beet
  • Mad as a hatter
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Ganglionic blockers

A
  • block entire ANS at nicotinic receptors (symp/para preganglion)
  • RARELY used therapeutically…not selective enough
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Nicotine

A
  • poison w/ no therapeutic benefit…bad for health
  • no effect at NMJ
  • depolarizes autonomic ganglia
    • low dose: stimulate
    • high dose: block
  • Increases release of neurotransmitters
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Neuromuscular blockers

A
  • block Ach at NMJ
  • similar to Ach and can be:
    • antagonist: nondepolarizing/competitive
    • agonist: depolarizing
  • useful for surgery…muscle relaxation
    • intubation
    • lower anesthesia dose needed
    • less post-op respiratory depression
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Nondepolarizing neuromuscular blockers

A
  • started as Curare….poison darts to paralyze prey
  • block post-synaptic receptors (nicotinic)
  • increase safety for anesthesia…but NO substitute
    Mechanism:
    -low dose: competitively block Ach at receptor / no depol
    overcome w/ ACE inhibitors (neostigmine, edrophonuium)
    -high dose: block ion channels of motor end plate
    Cannot be overcome w/ ACE inhibitors
  • Not effective orally….IV or IM
  • Cannot enter cells or BBB
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Muscle recovery of Nondepolarizing blockers

A
  • Face/eye (first to paralyze)
  • Fingers/limbs/neck/trunk
  • Intercostals
  • Diaphragm
  • Recover in reverse order
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Nondepolarizing blockers drug interactions

A
  • Cholinesterase inhibitor: antagonize effect if not in ion channel
  • Halogenated hydrocarbon anesthetics: enhance
  • Aminoglycoside antibiotic: enhance effect
  • Ca channel blockers: enhance effect
  • Last two block Ca from entering neuron
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Nondepolarizing blocker drugs
``` - Vecuronium 45 min - Cisatracurium (Nimbex) 90 min - Pancuronium (Pavulon) 90 min - Rocuronium (Zemuron) 45 min ``` - decrease O2 consumption on CPB...Venous sats will tell
26
Nondepolarizing blocker reversal drug
Sugammadex (Bridion) - reverses Roc / Vecuronium / Pancuronium - does not inhibit ACE - no cholinergic side effects - surrounds blocker and prevents its interaction
27
Depolarizing neuromuscular blocker
- Depolarize muscle fiber like Ach - resistant to ACE and remains attached to receptor - constant stimulation and persistent depolarization - prevents repolarization - removed by psuedocholinesterase in plasma (not at NMJ) - patient will convulse first....then paralyzed
28
Succinylcholine (Anectine)
- Sux - rapid onset (good for intubation) - last only minutes - IV - Respiratory muscles last to be paralyzed - May cause muscle soreness (initial convulsions) - can deliver nondepolarizer first to help with this Side effects: - Hyperthermia (can induce malignant hyperthermia) - Apnea (in Persian Jews / Indian Hindu) - Hyperkalemia (increased K) - burn patients susceptible
29
Malignant hyperthermia
- extra metabolism in muscles....life threatening - inherited disorder - triggered by sux and volatile anesthesia - increase CO2 / heat production - activates SNS - DIC: disseminated intravascular coagulation - multiple organ dysfunction - death
30
Depolarizing vs Nondepolarizing blockers
- Depolarizing cause persistent contraction...NonD stop depolarization altogether - Depolarizing paralyze large muscles -> short -> resp NonD paralyze short muscles -> large -> resp - Depolarizing irreversible...NonD reversible - Depolarizing stimulate first, then flaccid...NonD just flaccid
31
Antimuscarinics
- Atropine - Glycopyrrolate (Robinul) - Benztropine (Cogentin) - Scopolamine - Ipratropiuim (Atrovent)
32
Ganglionic Blcokers
- Nicotine
33
Nondepolarizing NM Blcokers
- Vecuronium - Cisatracurium (Nimbex) - Pancuronium (Pavulon) - Rocuronium (Zemuron)
34
Nondepolarizing NM Blocker Reversal
- Sugammadex (Bridion)
35
Depolarizing NM Blocker
- Succinylcholine (Anectine)
36
NE
- primary transmitter released by adrenergic neurons | - CNS and sympathetic
37
Epi
- released from adrenal medulla as hormone
38
Sympathomimetics
- drugs that activate adrenergic receptors | - can be direct or indirect acting
39
Sympatholytics
- drugs that block activation of adrenergic receptors
40
Steps of adrenergic neurotransmission
``` - similar to cholinergic, except NE is neurotransmitter Steps: - synthesis - storage - release - receptor binding - removal - metabolism ```
41
Step 1 of NE transmission
- Tyrosine is co-transported into neuron - Tyrosine converted to DOPA (via tyrosine hydroxylase) - RATE LIMITING - DOPA converted to dopamine inside neuron
42
Step 2 of NE transmission
- Dopamine moved into vessicle - Dopamine into NE (via dopamine B-hydroxylase) - step inhibited by Reserpine
43
Step 3 of NE transmission
- Action potential causes influx of Ca - Vessicle fuses w/ membrane - Exocytosis release NE and cofactors into synapse - Release blocked by Guanethidine
44
Step 4 of NE transmission
- NE binds to receptors on effective organ and auto-receptors - NE is metabotropic....2nd messenger system
45
Step 5 of NE transmission
NE removed from synapse via: - diffuses out - taken back into neuron - metabolized by COMT into inactive metabolites into urine
46
Step 6 of NE transmission
- COMT metabolizes in cleft - MAO metabolizes once taken back into neuron - Both convert to inactive metabolites into urine
47
Adrenergic receptor location
- post-synaptic ganglia of sympathetic and adrenal medulla
48
Alpha adrenoreceptors affinity
Epi NE Isoproterenol - High down to low...EPI/NE much higher than Iso - divided into a1 and a2
49
Beta adrenoreceptor affinity
Isoproterenol Epi NE High down to low...Iso much higher than Epi/NE Divided into B1/B2/B3
50
Alpha 1 adrenoreceptor
- high affinity for phenylephrine - mostly affects vasculature - postsynaptic membrane of effector organ - Smooth muscle constriction (adrenergic effects) - activates G-protein 2nd messenger systems - DAG: turns on other proteins - IP3: release of Ca into cytosol - further divided into A/B/C/D
51
Alpha 1 effects
- increase vascular tone -> increase BP - increase PVR - mydriasis - increase bladder tone - increase tension in prostate - Think fight or flight
52
Alpha 2 adrenoreceptors
- high affinity for clonidine - affects CNS feedback loops for HTN and sedation - sympathetic PREsynaptic nerve ending (also PRE para) - control release of NE (inhibitory autoreceptors) - effect mediated by inhibition of adenylyl Cyclades / drop in cAMP - divided into A/B/C
53
Alpha 2 effects
- blocks NE release / sympathetic tone - blocks Ach release - blocks insulin release - used as sedative in CV surgery
54
B1 adrenoreceptor
- Equal affinity for NE/Epi (both much less than iso) | - major role on heart
55
B1 effects
- tachycardia - increase contractility - increase in renin from kidneys (increase BP...hold water) - increase in lipolysis (for energy)
56
B2 adrenoreceptors
- higher affinity for EPI over NE | - mostly in lungs
57
B2 effects
- relaxation of pulmonary smooth muscle (airway open) - vasodilation of skeletal muscles (more flow) - decrease PVR - increase glucagon release (for energy) - uterine muscle relaxation
58
B3 adrenoreceptors
- involved in lipolysis - effects muscles of bladder - not big player
59
Dopaminergic Receptors
5 subtypes: - D1/D2: peripheral mesenteric and renal beds - D2: presynaptic adrenergic neurons - Dopamine can bind to all other adrenergic receptors (a/B) - interfere with release of NE Dopamine sites of action: - brain - renal/visceral arterioles (dilation/natriuresis...Na in urine) - CV system (activate B receptors...HR/contractility up) - Vascular PVR (up or down depending on dose)
60
Receptor desensitization
``` - prolonged exposure to catecholamines reduces responsiveness (NE/Epi/Dopa) Via: - sequestration of receptors - down-regulation - deactivation of G protein ```

581 - Pharmacology I (6 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions