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Pharmacology > 3.2 - Sympathetic Drugs > Flashcards

3.2 - Sympathetic Drugs Flashcards

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1
Q

Biosynthesis of Catecholamines

A
  • Location
  • Steps
  • Fate of NE in the cleft
  • Drugs that interfere in the biosynthesis, storage, release and fate of Catecholamines
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2
Q

Catecholamines

A
  • NE
  • EPI
  • Dopamine
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3
Q

Locations

A
  • Sympathetic, post-ganglionic neurons — NE
  • Adrenal Medulla — EPI
  • CNS — Dopamine
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4
Q

Steps

A

Tyrosine ➡️1️⃣ L-DOPA ➡️2️⃣ Dopamine ➡️ vesicular transport via VMAT ➡️ formation of NE (DA ➡️3️⃣ NE) ➡️ formation of EPI (NE ➡️4️⃣ EPI)

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5
Q

REMEMBER ‼️

A
  • Tyrosine — Precursor

* L-DOPA — L-dihydroxyphenylalanine)

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6
Q

Prevent premature metabolism by pre-synaptic enzymes

A

VMAT

– Vesicular Monoamine Transporter

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7
Q

1️⃣

A

Tyrosine Hydroxylase

— rate-limiting step

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8
Q

2️⃣

A

L-DOPA decarboxylase

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9
Q

3️⃣

A

Dopamine-B-hydroxylase

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10
Q

4️⃣

A

Phenylethanolamine-N-methyltransferase

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11
Q

Fate of NE in the cleft

A
  • Binding to post-synaptic ®
  • Metabolism by MAO & COMT
  • Reuptake Process
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12
Q

– Major mechanism of excess NE in the cleft (loss)
– Transporter:
— NET (NE Transporter/ Uptake-1 Transporter

A

Reuptake Process

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13
Q

Drugs that Interfere in the Biosynthesis, Storage, Release and Fate of Catecholamines

A
  • Formation of L-Dopa
  • Vesicular Transport via VMAT
  • Release of NE
  • Reuptake Process
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14
Q

Formation of L-DOPA: INHIBITOR

A

Metyrosine

— Inhibits tyrosine hudroxylase

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15
Q

Vesicular transport via VMAT: INHIBITOR

A

Reserpine

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16
Q

Release of NE (exocytosis): STIMULATORS

— TEAAA

A
  • Tyramine
  • Ephedrine
  • Amphetamine
  • Angiotensin II
  • a-latrotoxin
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17
Q

Release of NE (expcytosis): INHIBITORS

A
  • Guanethidine
  • Guanabenz
  • Bretylium
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18
Q

Reuptake Process: INHIBITORS

A 
• TCAs 
 - Inhibits reuotake of NE > 5-HT
• Cocaine
 - Vasoconstriction
• NERI (Reboxitine)
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19
Q

Receptors

A
  • Alpha
  • Beta
  • Dopamine
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20
Q

Alpha

A
  • Alpha 1

* Alpha 2

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21
Q

Alpha 1 Receptors

A

– Gq linked — CONTRACTION

— Locations & Effects

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22
Q

Alpha 1: Locations & Effects

A
  • Vascular SM
  • Bladder Trigone & Sphincter
  • Prostatic SM
  • Radial Muscle of the 👀
  • Pilomotor SM
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23
Q

Vascular SM

A

Vasoconstriction

— ⬆️ BP

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24
Q

Bladder Trigone & Sphincter

A

Contraction

— Urinary Retention

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25
Prostatic SM
Contraction | — URinary Retention
26
Radial Muscle of the 👀
Contraction | — MYDRIASIS
27
Pilomotor SM
Piloerection | — Goosebumps
28
Alpha 2 Receptors
* Pre-synaptic a2 | * Post-synaptic a2
29
Pre-synaptic a2
– Gi-linked— ⬇️ CAMP — Location — Effect — Consequencs
30
Location
``` Vasomotor Center (Brain) — momentary regulation of BP ```
31
Effect
Autoregulation | — stimulation will INHIBIT further release of NE
32
Consequences
* Central | * Peripheral
33
Central
Sedation & Depression
34
Peripheral
Vasodilation
35
Post-synaptic a2
– Gq-linked — CONTRACTION — Location — Effects
36
Location
Peripheral Blood Vessels
37
Effect
VasoCONSTRICTION
38
Beta | – Gs-linked — ⬆️cAMP
* Beta 1 * Beta 2 * Beta 3
39
Beta 1 Receptors
• Locations & Effects
40
Heart
* (+) Inotropy — force * (+) Chronotropy — rate * (+) Dromotropy — conduction velocity
41
Kidneys (Juxtaglomerular Apparatus)
Release of the enzyme renin = HTN
42
Beta 2 Receptors
• Locations & Effects
43
Locations
* Bronchial SM * Uterine SM * Vascular SM * Skeletal Muscle Cell Membrane * Neuromuscular End Plates
44
Bronchial SM
Bronchodilation
45
Uterine SM
Uterine Relaxation (Tocolysis)
46
Vascular SM | - Blood vessels that supply skeletal muscles
VasoDILATION
47
Skeletal Muscle Cell Membrane
⬆️ inward conductance of K ions = HYPOkalemia
48
Neuromuscular End Plates
Contraction (Tremors)
49
Beta 3 Receptors
• Location - Adipose Tissues • Effect - LIPOLYSIS
50
Dopamine | – Gs-linked
* D1 Receptors | * D2 Receptors
51
D1 Receptors
* Location | * Effect
52
Renal & Splanchic Blood Vessels
Renal Vasodilation = ⬆️ GFR = ⬆️ diuresis
53
D2 Receptors
* Peripheral GIT | * CNS
54
Peripheral GIT
Loss of Peristalsis (Ileus) — Relaxation ** Antagonist: Metoclopramide
55
CNS
* Modulates motor activity | * Perception & behavior
56
Sympathomimetics | — aka Adrenergic Agonists
* Direct-acting * Indirect-acting * Centrally-acting
57
Direct-acting Sympathomimetics | – directly binds & stimulates adrenergic receptors
* Non-selective | * Selective
58
Non-selective
Directly bind & activate MORE THAN 1 general type of adrenergic receptors (a, B, DA)
59
Examples: | - Natural catecholamines
* NE * EPI * DA
60
Pharmacodynamics
⬆️ affinity at B receptors than A receptors • Low Dose: B effect • Hugh Dose: A effect
61
Pharmacodynamics
Specific: • NE: B1 ➡️ A1 • EPI: B2 = B1 ➡️ A1 (anaphylaxis) • DA: D1 ➡️ B1 ➡️ A1
62
Pharmacokinetics
* ✖️oral preparations available | * Undergo extensive first pass effect
63
Route of Administration
* IV * SQ * Inhalational
64
Metabolism (MAO, COMT)
* NE & EPI | * Dopamine
65
NE & EPI
* 3-methoxy-4-hydroxymandelic acid | * Vanillyl mandelic acid (VMA)
66
Dopamine
Homovanillic acid
67
Clinical Uses
* Epinephrine/ Adrenaline * Norepinephrine/ Noradrenaline/ Levarterenol * Dopamine
68
– 1st line: Cardiac stimulant – 1st line: Mgt of Anaphylaxis – Local Vasoconstrictor – Mgt of Glaucoma
Epinephrine/ Adrenaline
69
Pivalic acid ester of EPI
Dipivefrin
70
– 1st line: Inotropic agent for SEPTIC shock | – IV infusion
Norepinephrine/ Noradrenaline/Levarterenol
71
Dopamine
* Effects | * Uses
72
1-3 ug/kg/min
D1 activation — Renal vasodilation | = ⬆️GFR = ⬆️ diuresis
73
2-5 ug/ kg/ min
B1 activation — ➕ I, C, D
74
> 5 ug/ kg/ min
A1 activation — Vasoconstriction
75
– Mgt of Septic shock – Mgt of Cardiogenic shock – Mgt of Acute ❤️ Failure complicated by oliguria & anuria
Dopamine
76
Oliguria
< 500 ml/ day
77
Anuria
< 50 ml/ day
78
Side Effects: Non-selective
* A1 overstimulation | * B1 overstimulation
79
A1 overstimulation
Digital necrosis
80
B1 overstimulation
Tachyarrhythmias
81
Selective
Directly bind and stimulate 1 general type of adrenergic receptors
82
Selective
* Non-selective B agonists * Selective B1 agonists * Selective B2 agonists * Selective A1 agonists * Sleective A2 agonists * Selective D1 agonist
83
Non-selective B agonists
* Isoproterenol * Isoprenaline – Uses – Hx. Use
84
Uses
* Alt. during shock states | * Mgt of ❤️ Failure (acute)
85
Hx. Use
• Mgt of Brochial Asthma | — May cause TACHYPHYLAXIS (rapid dev't of tolerance to B2 = Tachyarrhythmias)
86
Selective B1 Agonist
Dobutamine
87
– 1st line: Mgt of CARDIOGENIC shock | – Pharmacologic Stress Test
Dobutamine
88
Selective B2 agonists
* SABA * LABA * Tocolytics
89
SABA | – Short Acting B2 Agonists
* Salbutamol/ Albuterol * Terbutaline — SQ * Pirbuterol * Metaproterenol
90
LABA | – Long Acting B2 Agonists
* Salmoterol — Slow onset * Formoterol — Fast onset * Bambuterol — PO * Indacaterol — COPD
91
Tocolytics
* Ritodrine * Isoxsuprine * Terbutaline
92
– Mgt of preterm labor – Mgt of bronchial asthma and COPD – Adjuncts in the mgt of hyperkalemia
Tocolytics
93
Mgt of symptomatic bradycardia
Terbutaline
94
Selective A1 Agonists
* Phenylephrine * Methoxamine * Propyhexedrine * Tetrahydrozoline * Oxymetazoline * Nafazoline
95
Uses:
* Nasal decongestants * Mgt of HYPOtension * Local Vasoconstrictors
96
S/E:
* Intranadal | * Systemis
97
Intranasal
Rhinitis Medicamentosa — rebound congestion ** given for NMT 3 days only
98
Systemic
• Exacerbation of HTN • Precipitation if Urinary Retention in BPH pts • Rapid development of Tolerance ** use for NMT 5 days
99
Selective A2 agonists
* Clonidine * Methyldopa * Guanficine * Guanabenz
100
Effects:
* Pre-synaptic | * Post-synaptic
101
Pre-synaptic: | – AUTOREGULATION
* Central: Sedation& Depression | * Peripheral: Vasodilation
102
Post-synaptic
VasoCONSTRICTION
103
Effects: Clonidine
* Initial: Vasoconstriction | * Final: Vasodilation
104
Uses: Clonidine
``` • Alt. Mgt of HTN • Alt. Mgt of ADHD • Mgt of Clonidine withdrawal-induced HTN (rebound HTN) ** Alt: Labetalol Captopril ```
105
Methydopa | — Prodrug
Methyldopa (a-methyldopa) ➡️1️⃣ a-methyldopamine ➡️2️⃣ a-methylnorepinephrine
106
1️⃣
L-dopa decarboxylase
107
2️⃣
Dopamine-B-hydroxylase
108
– False neurotransmitter – ✖️ B1 & A1 agonist – ✔️ A2 agonist
a- methylnorepinephrine
109
Use: Methyldopa
• Mgt of HTN in pregnancy | — FDA Approved
110
S/E: Methyldopa
* Sedation — most common * Hepatotoxicity (> 2g/ day) — dose dependent * ➕ Coomb's Test — Hemolytic Anemia
111
Selective D1 Agonist
Fenoldopam
112
Use: Fenoldopam
Mgt of HTN Crisis (Alt)
113
Indirect-acting Sympathomimetics
* Releasers | * Reuptake Inhibitors
114
Releasers | — ⬆️ release of NE
* Tyramine * Ephedrine * Amphetamine
115
– Ma Huang – Dual Mechanisms: - ⬆️ release of NE; Direct Action = ⬆️ Sympathetic Effect
Ephedrine
116
Uses: Ephedrine
* Nasal Decongestant * Mgt of HYPOtension * Mgt of Bronchial Asthma (Chinese Med)
117
S/E: Ephedrine
* Exacerbation of HTN * Urinary retention (BPH pts) * Tachyarrhythmias
118
Reuptake Inhibitors
``` • TCAs - Inhibit reuptake of NE and 5-HT • Cocaine - Vasoconstriction • NERI (Reboxitine) ```
119
Centrally-acting Sympathomimetics
* Phenylpropanolamine (PPA) * Phentermine * Phenmetrazine * Amphetamine * Methylphenidate
120
Uses: Centrally-acting Sympathomimetics
* Mgt of ADHD * Anorexiants * Mgt of Narcolepsy
122
1st line: Mgt of ADHD
Methylphenidate
123
Anorexiants
* PPA * Phentermine * Phenmetrazine
124
Mgt of Narcolepsy
* Amphetamine | * Phentermine
125
S/E: Centrally-acting Sympathomimetics
* ⬆️ risk if addiction * ⬆️ risk of hemorrhagic shock * ⬆️ risk of pulmonary HTN
126
⬆️ risk of hemorrhagic shock
PPA
127
⬆️ risk of pulmonary HTN
Phentermine
128
Sympatholytics | — aka Adrenergic Antagonists
* Alpha Blockers | * Beta Blockers
129
Alpha Blockers
* Non-selective * A1-selective * A2-selective
130
Non-selective
• Phenoxybenzamine — irreversible • Phentolamine — reversible
131
A1-selective | — -zosin
* Prazosin * Doxazosin * Terazosin * Alfuzosin * Tamsulosin
132
A2-selective
* Yohimbine | * Rauwolscine
133
Clinical uses: Alpha Blockers
* Mgt of Pheocytochroma * Mgt of Reynaud's Syndrome * Mgt of HTN & Urinary Retention in BPH pts * Mgt of Erectile Dysfunction * Ngt of Carxinoid Syndrome
134
Pheocytochroma
– Tumor in adrenal medulla – S/Sx: - HTN, Tachycardia, Palpitations
135
Tx for Pheocytochroma
* alpha blockers | * beta blockers
136
Raynaud's Syndrome
Digital vasospasm due to extreme cold/ stress
137
Tx for Reynaud's Syndrome
* alpha blockers — Phentolamine | * CCBs — DHP
138
Mgt of HTB & Urinary Retention in BPH pts
``` Alpha 1 blocker —‼️First Dose Phenomenon ‼️"First fall" - Remedies: - Take at bedtime - Start at lower dose ```
139
Mgt of Erectile Dysfunction
Phentolamine
140
Carcinoid Syndrome
Malignancy in the enterochromaffin cells (SI) | — > 90% of 5-HT
141
S/Sx: Carcinoid Syndrome
– Flushing – Severe HA – Watey diarrhea
142
Tx for Carcinoid Syndrome
Phenoxybenzamine | – Anti-Serotonorgic
143
Beta blockers
* Non-selective * B1-selective/ cardioselective * B blockers with ISA * B blockers with Membrane Stabilizing Effect * B blockers with a1 blocking effect
144
Nonselective — N S T P — C/I: Asthmatic pts
* Nadolol * Sotalol * Timolol * Propranolol
145
B1 selective/ Cardioselective | — C B E A M
* Celiprolol * Betaxolol * Bisoprolol * Esmolol * Acebutolol * Atenolol * Metoprolol
146
B blockers with Intrinsic Sympathomimetic Activity (ISA) — C L A P — Lesser risk of rebound HTN
* Celiprolol * Carteolol * Labetalol * Acebutolol * Pindolol * Penbutolol
147
B blockers with Membrane Stabilizing Effect — ✔️ local anesthetic effect — ✖️prepared as ophthalmic drops (corneal damage) — P A L M
* Propranolol * Pindolol * Acebutolol * Labetalol * Metoprolol
148
B blockers witg a1 bocking effect — ✔️vasodilatory effect — L C
* Labetalol | * Carvedilol
149
– B1 blocker | – ✔️vasodilatory effect = ⬆️ levels of nitric oxide — endogenous vasodilator
Nebivolol
150
Clinical Uses: Beta Blockers
* 1st line: Mgt of HTN in pts with history of post MI * Mgt: CSAP * Mgt: Stable HF * Mgt: Arrhythmia * Mgt: Glaucoma * Mgt: Sympathetic sx of hyperthyroidism * Prophylaxis: Migraine HA * Mgt: Stage fright
151
Mgt of Stable HF
* Bisoprolol * Metoprolol * Carvedilol
152
Mgt of Arrhythmia
• Class II - Penbutolol - Esmolol - Acebutolol
153
Mgt of Glaucoma
* Betaxolol | * Timolol
154
Mgt of Sympathetic sx of hyperthyroidism
Propranolol | — inhibits peripheral conversion of T4 to T3
155
Prophylaxis of Migraine HA
Propranolol
156
Mgt of Stage fright
Propranolol
157
S/E: Beta Blockers
* Bradycardia | * Mask hypoglycemic sx
158
C/I: Beta Blockers
* Pts > 65 y/o * Pts with HR < 60 bpm * Pts with unstable HF * Pts with pre-existing ❤️ block * Concomittant administration with Non-DHP CCB (cardioselective) * Pts with reduced exercise tolerance
159
Alt. Mgt of ADHD
Amphetamine

Pharmacology (21 decks)

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