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Anatomy (AIM) > Pharmacology E2 > Flashcards

Pharmacology E2 Flashcards

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
Q

Myasthenic crisis

A

Flaccid paralysis (blocked or lack of receptors) due to insufficient tx of myasthenia gravis

IMPROVES w/ short-acting AChase inhibitor (edrophonium)

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26
Q

Cholinergic crisis

A

Spastic paralysis (excessively stimulated receptors) due to too much ACh (bradycardia and hyper salivation)

WORSENS w/ AChase inhibitor

Tx: atropine (anti-cholinergic med)

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27
Q

Catecholamines

A

Norepinephrine and epinephrine (noradrenaline and adrenaline)

28
Q

Catecholamine Synthesis and secretion

A
  • 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
Q

α-methyl-para-tyrosine

A

Feedback inhibition from
Epinephrine
Norepinephrine
Dopamine

30
Q

α-methyl DOPA

A

Affects adrenergic system
Inhibits synthesis of NE
Target: DOPA decarboxylase
Sympatholytic

Tx of Hypertension (crossed the BBB)

31
Q

Carbidopa

A

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
Q

Monoamine-oxidase (MAO)

A

DA, NE, EPI, serotonin degradation

- MAO inhib: depression tx

33
Q

“False transmitters” (can displace NE from synaptic vesicles)

A

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
Q

Drugs that inhibit catecholamine reuptake

A

Some antidepressants

  • tricyclics (amitriptyline) inhibit NE, 5HT uptake
  • SSRIs (fluoxetine) inhibit only 5HT uptake

Do NOT give with clonidine

35
Q

Why should reuptake inhibitor antidepressants not be taken with presynaptic α2 agonists?

A

presynaptic α2 agonists (clonidine) inhibit catecholamine synthesis and release –> worsening depression

36
Q

Amitriptyline

A

Catecholaminomimetic (sympathomimetic)
- TCA
- Blocks reuptake of NE and 5-HT
Tx: Depression

37
Q

Bupropion

A

Catecholaminomimetic
- DNRI
- Blocks reuptake of DO and NE
Tx: Depression

38
Q

Citalopram

A

Catecholaminomimetic
- SSRI
- Blocks reuptake of 5HT
Tx: Depression

39
Q

Venlafaxine

A

Catecholaminomimetic
- SNRI
- Blocks reuptake of 5HT and NE
Tx: Depression

40
Q

Phenelzine

A

Catecholaminomimetic (sympathomimetic)
- MAO inhibitor
Tx: depression

41
Q

Amphetamine

Methylphenidate

A

Catecholaminomimetic
- stimulant
- NE reuptake inhibitor and weak agonist
Tx: ADHD, obesity

42
Q

Clonidine

A

Affects adrenergic system
Presynaptic α2 agonist
Inhibits catecholamine release
Sympatholytic

*don’t give with reuptake inhibitor antidepressants (TCA, SSRIs)

43
Q

Receptors for NE and EPI

A

α -Adrenergic receptors: NE higher affinity

β-Adrenergic receptors: EPI higher affinity

44
Q

β1 - Adrenergic receptors

A

Heart

Stim: - inc HR, inc contractility, inc metabolism, inc O2 consumption, inc BP

45
Q

β1 BLOCKERS

A
  • dec HR
  • dec contractility
  • dec workload
  • have anxiolytic action
    Tx for HTN and post-MI
    Exp. Propanolol (non-selective)
    Metoprolol/Atenolol (selective)
46
Q

Which beta blockers are contraindicated in asthma and why?

A

Non-selective beta blockers (propranolol) bad for pts w/ pulm disorders bc blocking B2 –> bronchoconstriction

Use selective like metoprolol/atenolol instead

47
Q

β2 – Adrenergic receptors

A

Lungs

Stim: Bronchodilation, smc relaxation, inc dilation of blood vessels (brain)

48
Q

β2 AGONISTS

A

Used for asthma tx

49
Q

α1 – Adrenergic receptors

A

Blood vessels, constriction

50
Q

α2 - Adrenergic receptors

A

Brain, on surface of pre-syn membranes

When stim –> suppress NE release –> AUTOINHIBITION

51
Q

Yohimbine

A

α2 -Antagonist

tx: erectile dysfunction

52
Q

Cardiovascular effects of PNS (ACh)

A

dec HR
dec contractility
dec O2 consumption
dec blood pressure

53
Q

Norepinephrine

Receptor type, clinical use?

A

Sympathomimetic
Receptor type: α1>β1
Hypotension

54
Q

Epinephrine

Receptor type, clinical use?

A

Sympathomimetic
β>α
Tx: Anaphylaxis
**EpiPen

55
Q

Isoproterenol

Receptor type, clinical use?

A

Sympathomimetic
β1=β2
Tx: Cardiac arrest

56
Q

Albuterol, terbutaline

Receptor type, clinical use?

A

Sympathomimetics
β2
Tx: Asthma

57
Q

Dobutamine

Receptor type, clinical use?

A

Sympathomimetic
β1>β2
Tx: Congestive heart failure

58
Q

Dopamine

Receptor type, clinical use?

A

Sympathomimetic
D1=D2>β2>β1>α
Tx: Congestive heart failure

59
Q

Tx of HTN

CNS, heart, blood vessels

A

a-methyldopa ↓NE, E
Clonidine ↓NE

Atenelol ↓b1
Labetalol ↓ α1>b1
Propanalol ↓b1 = b2↓

Prazosin ↓α1
Phenoxybenzamine ↓α1 = α2↓

60
Q

Cholinomimetics (direct-acting)

A

Bethanechol
Carbachol
Pilocarpine
Succinylcholine

61
Q

Acetylcholine Receptor Antagonists

A

Atropine
Tubocurarine
Trimethaphan

62
Q

AChases

A 
Pyridostigmine
Physostigmine
Edrophonium
Parathion
Organophosphate
63
Q

Catecholaminomimetics

Indirect CNS Stimulants

A 
Amitriptyline
Bupropion
Citalopram
Venlafaxine
Phenelzine
Amphetamine
Methylphenidate
64
Q

Drugs Affecting the Adrenergic System

A 
α-methyl DOPA
Carbi DOPA
Clonidine
Amitriptyline, amphetamine
Phenelzine
65
Q

Adrenergic Receptor Agonists

Sympathomimetics

A 
Norepinephrine
Epinephrine
Isoproterenol
Albuterol
Terbutaline
Dobutamine
Dopamine
66
Q

Adrenergic Receptor Antagonists

Sympatholytics

A 
Atenolol
Metoprolol
Propanolol
Labetalol
Phentolamine
Phenoxybenzamine
Prazosin

Anatomy (AIM) (13 decks)

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