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Pharmacology > 3.2 - Sympathetic Drugs > Flashcards

3.2 - Sympathetic Drugs Flashcards

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
Q

Prostatic SM

A

Contraction

— URinary Retention

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26
Q

Radial Muscle of the 👀

A

Contraction

— MYDRIASIS

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27
Q

Pilomotor SM

A

Piloerection

— Goosebumps

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28
Q

Alpha 2 Receptors

A
  • Pre-synaptic a2

* Post-synaptic a2

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29
Q

Pre-synaptic a2

A

– Gi-linked— ⬇️ CAMP

— Location
— Effect
— Consequencs

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30
Q

Location

A 
Vasomotor Center (Brain)
— momentary regulation of BP
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31
Q

Effect

A

Autoregulation

— stimulation will INHIBIT further release of NE

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32
Q

Consequences

A
  • Central

* Peripheral

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33
Q

Central

A

Sedation & Depression

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34
Q

Peripheral

A

Vasodilation

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35
Q

Post-synaptic a2

A

– Gq-linked — CONTRACTION

— Location
— Effects

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36
Q

Location

A

Peripheral Blood Vessels

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37
Q

Effect

A

VasoCONSTRICTION

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38
Q

Beta

– Gs-linked — ⬆️cAMP

A
  • Beta 1
  • Beta 2
  • Beta 3
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39
Q

Beta 1 Receptors

A

• Locations & Effects

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40
Q

Heart

A
  • (+) Inotropy — force
  • (+) Chronotropy — rate
  • (+) Dromotropy — conduction velocity
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41
Q

Kidneys (Juxtaglomerular Apparatus)

A

Release of the enzyme renin = HTN

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42
Q

Beta 2 Receptors

A

• Locations & Effects

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43
Q

Locations

A
  • Bronchial SM
  • Uterine SM
  • Vascular SM
  • Skeletal Muscle Cell Membrane
  • Neuromuscular End Plates
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44
Q

Bronchial SM

A

Bronchodilation

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45
Q

Uterine SM

A

Uterine Relaxation (Tocolysis)

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46
Q

Vascular SM

- Blood vessels that supply skeletal muscles

A

VasoDILATION

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47
Q

Skeletal Muscle Cell Membrane

A

⬆️ inward conductance of K ions = HYPOkalemia

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48
Q

Neuromuscular End Plates

A

Contraction (Tremors)

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49
Q

Beta 3 Receptors

A

• Location
- Adipose Tissues
• Effect
- LIPOLYSIS

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50
Q

Dopamine

– Gs-linked

A
  • D1 Receptors

* D2 Receptors

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51
Q

D1 Receptors

A
  • Location

* Effect

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52
Q

Renal & Splanchic Blood Vessels

A

Renal Vasodilation = ⬆️ GFR = ⬆️ diuresis

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53
Q

D2 Receptors

A
  • Peripheral GIT

* CNS

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54
Q

Peripheral GIT

A

Loss of Peristalsis (Ileus)
— Relaxation
** Antagonist: Metoclopramide

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55
Q

CNS

A
  • Modulates motor activity

* Perception & behavior

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56
Q

Sympathomimetics

— aka Adrenergic Agonists

A
  • Direct-acting
  • Indirect-acting
  • Centrally-acting
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57
Q

Direct-acting Sympathomimetics

– directly binds & stimulates adrenergic receptors

A
  • Non-selective

* Selective

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58
Q

Non-selective

A

Directly bind & activate MORE THAN 1 general type of adrenergic receptors (a, B, DA)

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59
Q

Examples:

- Natural catecholamines

A
  • NE
  • EPI
  • DA
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60
Q

Pharmacodynamics

A

⬆️ affinity at B receptors than A receptors
• Low Dose: B effect
• Hugh Dose: A effect

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61
Q

Pharmacodynamics

A

Specific:
• NE: B1 ➡️ A1
• EPI: B2 = B1 ➡️ A1 (anaphylaxis)
• DA: D1 ➡️ B1 ➡️ A1

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62
Q

Pharmacokinetics

A
  • ✖️oral preparations available

* Undergo extensive first pass effect

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63
Q

Route of Administration

A
  • IV
  • SQ
  • Inhalational
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64
Q

Metabolism (MAO, COMT)

A
  • NE & EPI

* Dopamine

65
Q

NE & EPI

A
  • 3-methoxy-4-hydroxymandelic acid

* Vanillyl mandelic acid (VMA)

66
Q

Dopamine

A

Homovanillic acid

67
Q

Clinical Uses

A
  • Epinephrine/ Adrenaline
  • Norepinephrine/ Noradrenaline/ Levarterenol
  • Dopamine
68
Q

– 1st line: Cardiac stimulant
– 1st line: Mgt of Anaphylaxis
– Local Vasoconstrictor
– Mgt of Glaucoma

A

Epinephrine/ Adrenaline

69
Q

Pivalic acid ester of EPI

A

Dipivefrin

70
Q

– 1st line: Inotropic agent for SEPTIC shock

– IV infusion

A

Norepinephrine/ Noradrenaline/Levarterenol

71
Q

Dopamine

A
  • Effects

* Uses

72
Q

1-3 ug/kg/min

A

D1 activation — Renal vasodilation

= ⬆️GFR = ⬆️ diuresis

73
Q

2-5 ug/ kg/ min

A

B1 activation — ➕ I, C, D

74
Q

> 5 ug/ kg/ min

A

A1 activation — Vasoconstriction

75
Q

– Mgt of Septic shock
– Mgt of Cardiogenic shock
– Mgt of Acute ❤️ Failure complicated by oliguria & anuria

76
Q

Oliguria

A

< 500 ml/ day

77
Q

Anuria

A

< 50 ml/ day

78
Q

Side Effects: Non-selective

A
  • A1 overstimulation

* B1 overstimulation

79
Q

A1 overstimulation

A

Digital necrosis

80
Q

B1 overstimulation

A

Tachyarrhythmias

81
Q

Selective

A

Directly bind and stimulate 1 general type of adrenergic receptors

82
Q

Selective

A
  • Non-selective B agonists
  • Selective B1 agonists
  • Selective B2 agonists
  • Selective A1 agonists
  • Sleective A2 agonists
  • Selective D1 agonist
83
Q

Non-selective B agonists

A
  • Isoproterenol
  • Isoprenaline

– Uses
– Hx. Use

84
Q

Uses

A
  • Alt. during shock states

* Mgt of ❤️ Failure (acute)

85
Q

Hx. Use

A

• Mgt of Brochial Asthma

— May cause TACHYPHYLAXIS (rapid dev’t of tolerance to B2 = Tachyarrhythmias)

86
Q

Selective B1 Agonist

A

Dobutamine

87
Q

– 1st line: Mgt of CARDIOGENIC shock

– Pharmacologic Stress Test

A

Dobutamine

88
Q

Selective B2 agonists

A
  • SABA
  • LABA
  • Tocolytics
89
Q

SABA

– Short Acting B2 Agonists

A
  • Salbutamol/ Albuterol
  • Terbutaline — SQ
  • Pirbuterol
  • Metaproterenol
90
Q

LABA

– Long Acting B2 Agonists

A
  • Salmoterol — Slow onset
  • Formoterol — Fast onset
  • Bambuterol — PO
  • Indacaterol — COPD
91
Q

Tocolytics

A
  • Ritodrine
  • Isoxsuprine
  • Terbutaline
92
Q

– Mgt of preterm labor
– Mgt of bronchial asthma and COPD
– Adjuncts in the mgt of hyperkalemia

A

Tocolytics

93
Q

Mgt of symptomatic bradycardia

A

Terbutaline

94
Q

Selective A1 Agonists

A
  • Phenylephrine
  • Methoxamine
  • Propyhexedrine
  • Tetrahydrozoline
  • Oxymetazoline
  • Nafazoline
95
Q

Uses:

A
  • Nasal decongestants
  • Mgt of HYPOtension
  • Local Vasoconstrictors
96
Q

S/E:

A
  • Intranadal

* Systemis

97
Q

Intranasal

A

Rhinitis Medicamentosa
— rebound congestion
** given for NMT 3 days only

98
Q

Systemic

A

• Exacerbation of HTN
• Precipitation if Urinary Retention in BPH pts
• Rapid development of Tolerance
** use for NMT 5 days

99
Q

Selective A2 agonists

A
  • Clonidine
  • Methyldopa
  • Guanficine
  • Guanabenz
100
Q

Effects:

A
  • Pre-synaptic

* Post-synaptic

101
Q

Pre-synaptic:

– AUTOREGULATION

A
  • Central: Sedation& Depression

* Peripheral: Vasodilation

102
Q

Post-synaptic

A

VasoCONSTRICTION

103
Q

Effects: Clonidine

A
  • Initial: Vasoconstriction

* Final: Vasodilation

104
Q

Uses: Clonidine

A 
• Alt. Mgt of HTN
• Alt. Mgt of ADHD
• Mgt of Clonidine withdrawal-induced HTN (rebound HTN)
  ** Alt: Labetalol
             Captopril
105
Q

Methydopa

— Prodrug

A

Methyldopa (a-methyldopa) ➡️1️⃣ a-methyldopamine ➡️2️⃣ a-methylnorepinephrine

106
Q

1️⃣

A

L-dopa decarboxylase

107
Q

2️⃣

A

Dopamine-B-hydroxylase

108
Q

– False neurotransmitter
– ✖️ B1 & A1 agonist
– ✔️ A2 agonist

A

a- methylnorepinephrine

109
Q

Use: Methyldopa

A

• Mgt of HTN in pregnancy

— FDA Approved

110
Q

S/E: Methyldopa

A
  • Sedation — most common
  • Hepatotoxicity (> 2g/ day) — dose dependent
  • ➕ Coomb’s Test — Hemolytic Anemia
111
Q

Selective D1 Agonist

A

Fenoldopam

112
Q

Use: Fenoldopam

A

Mgt of HTN Crisis (Alt)

113
Q

Indirect-acting Sympathomimetics

A
  • Releasers

* Reuptake Inhibitors

114
Q

Releasers

— ⬆️ release of NE

A
  • Tyramine
  • Ephedrine
  • Amphetamine
115
Q

– Ma Huang
– Dual Mechanisms:
- ⬆️ release of NE; Direct Action = ⬆️ Sympathetic Effect

116
Q

Uses: Ephedrine

A
  • Nasal Decongestant
  • Mgt of HYPOtension
  • Mgt of Bronchial Asthma (Chinese Med)
117
Q

S/E: Ephedrine

A
  • Exacerbation of HTN
  • Urinary retention (BPH pts)
  • Tachyarrhythmias
118
Q

Reuptake Inhibitors

A 
• TCAs
 - Inhibit reuptake of NE and 5-HT
• Cocaine
 - Vasoconstriction
• NERI (Reboxitine)
119
Q

Centrally-acting Sympathomimetics

A
  • Phenylpropanolamine (PPA)
  • Phentermine
  • Phenmetrazine
  • Amphetamine
  • Methylphenidate
120
Q

Uses: Centrally-acting Sympathomimetics

A
  • Mgt of ADHD
  • Anorexiants
  • Mgt of Narcolepsy
122
Q

1st line: Mgt of ADHD

A

Methylphenidate

123
Q

Anorexiants

A
  • PPA
  • Phentermine
  • Phenmetrazine
124
Q

Mgt of Narcolepsy

A
  • Amphetamine

* Phentermine

125
Q

S/E: Centrally-acting Sympathomimetics

A
  • ⬆️ risk if addiction
  • ⬆️ risk of hemorrhagic shock
  • ⬆️ risk of pulmonary HTN
126
Q

⬆️ risk of hemorrhagic shock

127
Q

⬆️ risk of pulmonary HTN

A

Phentermine

128
Q

Sympatholytics

— aka Adrenergic Antagonists

A
  • Alpha Blockers

* Beta Blockers

129
Q

Alpha Blockers

A
  • Non-selective
  • A1-selective
  • A2-selective
130
Q

Non-selective

A

• Phenoxybenzamine
— irreversible
• Phentolamine
— reversible

131
Q

A1-selective

— -zosin

A
  • Prazosin
  • Doxazosin
  • Terazosin
  • Alfuzosin
  • Tamsulosin
132
Q

A2-selective

A
  • Yohimbine

* Rauwolscine

133
Q

Clinical uses: Alpha Blockers

A
  • 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
Q

Pheocytochroma

A

– Tumor in adrenal medulla
– S/Sx:
- HTN, Tachycardia, Palpitations

135
Q

Tx for Pheocytochroma

A
  • alpha blockers

* beta blockers

136
Q

Raynaud’s Syndrome

A

Digital vasospasm due to extreme cold/ stress

137
Q

Tx for Reynaud’s Syndrome

A
  • alpha blockers — Phentolamine

* CCBs — DHP

138
Q

Mgt of HTB & Urinary Retention in BPH pts

A 
Alpha 1 blocker
 —‼️First Dose Phenomenon
      ‼️"First fall"
     - Remedies: 
        - Take at bedtime
        - Start at lower dose
139
Q

Mgt of Erectile Dysfunction

A

Phentolamine

140
Q

Carcinoid Syndrome

A

Malignancy in the enterochromaffin cells (SI)

— > 90% of 5-HT

141
Q

S/Sx: Carcinoid Syndrome

A

– Flushing
– Severe HA
– Watey diarrhea

142
Q

Tx for Carcinoid Syndrome

A

Phenoxybenzamine

– Anti-Serotonorgic

143
Q

Beta blockers

A
  • Non-selective
  • B1-selective/ cardioselective
  • B blockers with ISA
  • B blockers with Membrane Stabilizing Effect
  • B blockers with a1 blocking effect
144
Q

Nonselective
— N S T P
— C/I: Asthmatic pts

A
  • Nadolol
  • Sotalol
  • Timolol
  • Propranolol
145
Q

B1 selective/ Cardioselective

— C B E A M

A
  • Celiprolol
  • Betaxolol
  • Bisoprolol
  • Esmolol
  • Acebutolol
  • Atenolol
  • Metoprolol
146
Q

B blockers with Intrinsic Sympathomimetic Activity (ISA)
— C L A P
— Lesser risk of rebound HTN

A
  • Celiprolol
  • Carteolol
  • Labetalol
  • Acebutolol
  • Pindolol
  • Penbutolol
147
Q

B blockers with Membrane Stabilizing Effect
— ✔️ local anesthetic effect
— ✖️prepared as ophthalmic drops (corneal damage)
— P A L M

A
  • Propranolol
  • Pindolol
  • Acebutolol
  • Labetalol
  • Metoprolol
148
Q

B blockers witg a1 bocking effect
— ✔️vasodilatory effect
— L C

A
  • Labetalol

* Carvedilol

149
Q

– B1 blocker

– ✔️vasodilatory effect = ⬆️ levels of nitric oxide — endogenous vasodilator

150
Q

Clinical Uses: Beta Blockers

A
  • 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
Q

Mgt of Stable HF

A
  • Bisoprolol
  • Metoprolol
  • Carvedilol
152
Q

Mgt of Arrhythmia

A

• Class II

  • Penbutolol
  • Esmolol
  • Acebutolol
153
Q

Mgt of Glaucoma

A
  • Betaxolol

* Timolol

154
Q

Mgt of Sympathetic sx of hyperthyroidism

A

Propranolol

— inhibits peripheral conversion of T4 to T3

155
Q

Prophylaxis of Migraine HA

A

Propranolol

156
Q

Mgt of Stage fright

A

Propranolol

157
Q

S/E: Beta Blockers

A
  • Bradycardia

* Mask hypoglycemic sx

158
Q

C/I: Beta Blockers

A
  • 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
Q

Alt. Mgt of ADHD

A

Amphetamine

Pharmacology (21 decks)

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