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Anatomy (AIM) > Pharmacology E2 > Flashcards

Pharmacology E2 Flashcards

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1
Q

Two divisions of the ANS

A

Parasympathetic (medulla and sacral output)

Sympathetic (thoracic and lumbar output)
* outweighs parasympathetic bc of adrenal gland

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2
Q

Adrenal gland

A

secretes epinephrine into systemic circulation

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3
Q

POTS (Postural Orthostatic Tachycardia Syndrome)

A

Form of dysautonomia. HR>120 bpm within the first 10 minutes of standing; PositiveTilt Table test

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4
Q

Dysautonomia

A

disorder of ANS function that involves dysfuction of either the sympathetic or parasympathetic components

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5
Q

Parasympathetic ganglia

A

located in close to end organs
1st neuron –> long
2nd neuron –> short

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6
Q

Sympathetic ganglia

A

located closer to CNS and farther from end organs
1st neuron –> short
2nd neuron –> long

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7
Q

Blood-brain-barrier

A

lipophilic, small, uncharged molecules readily pass through

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8
Q

NT at preganglionic synapse (nicotinic)

A

ACh

*different receptors than those at NMJ

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9
Q

Responses to parasympathetic innervations

A
  • Pupil constriction
  • Bronchi: constriction, inc secretion
  • GI tract: inc peristalsis, inc sphincter tone, inc blood flow
  • Saliva: copious, liquid
  • Heart: dec HR, dec BP
  • bladder: dec sphincter tone, stim detrusor muscle (urine void)
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10
Q

Main transmitter that innervates end organs

A

NE

*exception: sweat glands, skeletal muscle, blood vessels - ACh

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11
Q

Responses to sympathetic innervations

A
  • Pupil dilation
  • CNS: drive, alertness
  • Liver: glycogenolysis, glucose release
  • GI tract: dec peristalsis, inc sphincter tone, dec blood flow
  • Saliva: little, viscous
  • Heart: inc HR, inc force, inc BP
  • fat tissue: lipolysis, FA liberation
  • Bladder: inc sphincter tone, relax detrusor muscle (inc urine accommodation)
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12
Q

ACh

A

50% in SV, 50% free in cytoplasm

  • SV release is via Ca/E-requiring exocytosis
    ^botulinum inhibits, leading to flaccid paralysis
  • AChase terminates ACh action
  • primary receptors for ACh  nicotinic (@ganglia and NMJ) or muscarinic (@ end organs)
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13
Q

Bethanechol

A

Direct Cholinomimetic
Agonist (mAchR)
Causes GI/Bladder contraction, used to treat post-operative “lazy gut syndrome”

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14
Q

Succinylcholine

A

Direct Cholinomimetic
Agonist (nAchR)
Depolarizing NMJ blocker –> spastic paralysis by continued activation of muscle nAchRs.
(Used pre-operatively).

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15
Q

Carbachol

A

Direct Cholinomimetic
Agonist (mAchR)
stim miosis (pupil constriction)
tx: glaucoma

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16
Q

Pilocarpine

A

Direct Cholinomimetic
Agonist (mAchR)
Stim sweat glands
Dx: cystic fibrosis

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17
Q

Atropine

A

Antagonist (mAchR)
Tx: Achase blocker overdose
(tx: acute spastic paralysis)

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18
Q

Tubocurarine

A

Antagonist (Ach-nicotinic (NMJ))
Non-depolarizing blocker Pre-op muscle relaxation

a-Bungarotoxin (snake venom)
(Flaccid paralysis)

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19
Q

Trimethaphan

A

Antagonist (Ach-nicotinic-ganglia)

Tx: malignant hypertension

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20
Q

Pyridostigmine

A

ACHase inhibitor
Reversible
Does NOT cross BBB
Tx; myasthenia gravis

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21
Q

Physostigmine

A

ACHase inhibitor
Reversible
Crosses BBB
Tx; myasthenia gravis

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22
Q

Edrophonium

A

ACHase inhibitor
Short-acting
Does NOT cross BBB
Dx: myasthenia gravis

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23
Q

Parathion

Organophosphate

A 
ACHase inhibitor
Irreversible
Crosses BBB
Used to kill rodents
--> rural pediatric poisoning 
--> looks like flour
--> spastic paralysis 
--> nerve gas (warfare)
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24
Q

Antidote for human poisoning due to organophosphates

A

Pralidoxime (2-PAM)=regenerates AChase

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25
Myasthenic crisis
Flaccid paralysis (blocked or lack of receptors) due to insufficient tx of myasthenia gravis IMPROVES w/ short-acting AChase inhibitor (edrophonium)
26
Cholinergic crisis
Spastic paralysis (excessively stimulated receptors) due to too much ACh (bradycardia and hyper salivation) WORSENS w/ AChase inhibitor Tx: atropine (anti-cholinergic med)
27
Catecholamines
Norepinephrine and epinephrine (noradrenaline and adrenaline)
28
Catecholamine Synthesis and secretion
- Active TYR uptake pump - Tyr --> dopa--> dopamine --> NE --> EPI ^tyr hydroxylase=RLS - Active transport of cytoplasmic NE and DO into SV - NE transport out of vesicles, methylation to EPI in cytoplasm and uptake back into vesicles (adrenal medulla*) - Release of NE via vesicular exocytosis (Ca, E dep; inhib via Mg) - NE binding to pre- and post- synaptic receptors - active reuptake of NE into neurons from synaptic cleft - catabolism of NE and DO by monoamine oxidases
29
α-methyl-para-tyrosine
Feedback inhibition from Epinephrine Norepinephrine Dopamine
30
α-methyl DOPA
Affects adrenergic system Inhibits synthesis of NE Target: DOPA decarboxylase Sympatholytic Tx of Hypertension (crossed the BBB)
31
Carbidopa
Affects adrenergic system Inhibits synthesis Target: DOPA decarboxylase Sympathomimetic Tx of Parkinsonism (does NOT cross the BBB, prevents DOPA from being decarboxylated in the periphery)
32
Monoamine-oxidase (MAO)
DA, NE, EPI, serotonin degradation | - MAO inhib: depression tx
33
"False transmitters" (can displace NE from synaptic vesicles)
Alpha-methyl NE Tyramine (cheese, metabolized to octopamine) Avoid when on MAO inhibitor (Displaced NE can diffuse out of presynaptic terminus --> constrict blood vessels --> inc bp --> HYPERTENSIVE CRISIS
34
Drugs that inhibit catecholamine reuptake
Some antidepressants - tricyclics (amitriptyline) inhibit NE, 5HT uptake - SSRIs (fluoxetine) inhibit only 5HT uptake Do NOT give with clonidine
35
Why should reuptake inhibitor antidepressants not be taken with presynaptic α2 agonists?
presynaptic α2 agonists (clonidine) inhibit catecholamine synthesis and release --> worsening depression
36
Amitriptyline
Catecholaminomimetic (sympathomimetic) - TCA - Blocks reuptake of NE and 5-HT Tx: Depression
37
Bupropion
Catecholaminomimetic - DNRI - Blocks reuptake of DO and NE Tx: Depression
38
Citalopram
Catecholaminomimetic - SSRI - Blocks reuptake of 5HT Tx: Depression
39
Venlafaxine
Catecholaminomimetic - SNRI - Blocks reuptake of 5HT and NE Tx: Depression
40
Phenelzine
Catecholaminomimetic (sympathomimetic) - MAO inhibitor Tx: depression
41
Amphetamine | Methylphenidate
Catecholaminomimetic - stimulant - NE reuptake inhibitor and weak agonist Tx: ADHD, obesity
42
Clonidine
Affects adrenergic system Presynaptic α2 agonist Inhibits catecholamine release Sympatholytic *don't give with reuptake inhibitor antidepressants (TCA, SSRIs)
43
Receptors for NE and EPI
α -Adrenergic receptors: NE higher affinity β-Adrenergic receptors: EPI higher affinity
44
β1 - Adrenergic receptors
Heart | Stim: - inc HR, inc contractility, inc metabolism, inc O2 consumption, inc BP
45
β1 BLOCKERS
- dec HR - dec contractility - dec workload - have anxiolytic action Tx for HTN and post-MI Exp. Propanolol (non-selective) Metoprolol/Atenolol (selective)
46
Which beta blockers are contraindicated in asthma and why?
Non-selective beta blockers (propranolol) bad for pts w/ pulm disorders bc blocking B2 --> bronchoconstriction Use selective like metoprolol/atenolol instead
47
β2 – Adrenergic receptors
Lungs | Stim: Bronchodilation, smc relaxation, inc dilation of blood vessels (brain)
48
β2 AGONISTS
Used for asthma tx
49
α1 – Adrenergic receptors
Blood vessels, constriction
50
α2 - Adrenergic receptors
Brain, on surface of pre-syn membranes | When stim --> suppress NE release --> AUTOINHIBITION
51
Yohimbine
α2 -Antagonist | tx: erectile dysfunction
52
Cardiovascular effects of PNS (ACh)
dec HR dec contractility dec O2 consumption dec blood pressure
53
Norepinephrine | Receptor type, clinical use?
Sympathomimetic Receptor type: α1>β1 Hypotension
54
Epinephrine | Receptor type, clinical use?
Sympathomimetic β>α Tx: Anaphylaxis **EpiPen
55
Isoproterenol | Receptor type, clinical use?
Sympathomimetic β1=β2 Tx: Cardiac arrest
56
Albuterol, terbutaline | Receptor type, clinical use?
Sympathomimetics β2 Tx: Asthma
57
Dobutamine | Receptor type, clinical use?
Sympathomimetic β1>β2 Tx: Congestive heart failure
58
Dopamine | Receptor type, clinical use?
Sympathomimetic D1=D2>β2>β1>α Tx: Congestive heart failure
59
Tx of HTN | CNS, heart, blood vessels
a-methyldopa ↓NE, E Clonidine ↓NE Atenelol ↓b1 Labetalol ↓ α1>b1 Propanalol ↓b1 = b2↓ Prazosin ↓α1 Phenoxybenzamine ↓α1 = α2↓
60
Cholinomimetics (direct-acting)
Bethanechol Carbachol Pilocarpine Succinylcholine
61
Acetylcholine Receptor Antagonists
Atropine Tubocurarine Trimethaphan
62
AChases
``` Pyridostigmine Physostigmine Edrophonium Parathion Organophosphate ```
63
Catecholaminomimetics | Indirect CNS Stimulants
``` Amitriptyline Bupropion Citalopram Venlafaxine Phenelzine Amphetamine Methylphenidate ```
64
Drugs Affecting the Adrenergic System
``` α-methyl DOPA Carbi DOPA Clonidine Amitriptyline, amphetamine Phenelzine ```
65
Adrenergic Receptor Agonists | Sympathomimetics
``` Norepinephrine Epinephrine Isoproterenol Albuterol Terbutaline Dobutamine Dopamine ```
66
Adrenergic Receptor Antagonists | Sympatholytics
``` Atenolol Metoprolol Propanolol Labetalol Phentolamine Phenoxybenzamine Prazosin ```

Anatomy (AIM) (13 decks)

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