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Sympatomimetics Flashcards

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1
Q

Levodopa

presynaptic

A

MECHANISM
NE precursor
Passes BBB

INDICATION
Parkinson’s

SIDE EFFECTS

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2
Q

4-aminopyridine

presynaptic

A

MECHANISM
K+ channel blocker
Increases membrane potential in NE neurons, longer NT release

INDICATION
Research

SIDE EFFECTS

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3
Q

Latrotoxin

presynaptic

A

MECHANISM
Causes Ca2+ influx presynaptically, and NT release in Cholinergic and Adrenergic neurons.

INDICATION
Research
Spider venom

SIDE EFFECTS

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4
Q

Mianserin

presynaptic

A

MECHANISM
Inh a2 receptor in presynaptic neurons = stimulation

INDICATION
Depression

SIDE EFFECTS

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5
Q

Tyramine

presynaptic

A

MECHANISM
Indirect sympatomimetic effect

INDICATION
No clinical use

KINETICS
Degraded by MAO-A in GI

SIDE EFFECTS
Hypertensive crisis
Cheese/wine contains tyramine. Don’t eat cheese in case of taking MAO-A inh antidepressants, as tyramine will cause excessive sympathetic effect, hypertensive crisis.

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6
Q

Ephedrine
Pseudoephedrine

presynaptic

A

MECHANISM
direct a + b agonist
indirect NE release from presynaptic neurons

INDICATION
nasal decongestant
allergic rhinitis

KINETICS
long duration due to poor MAO/COMT degradation

SIDE EFFECTS
tachycardia
anxiety etc.

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7
Q

Amphetamine
Metamphetamine (speed)

presynaptic

A

MECHANISM
NET, DET, SERT reuptake inhibitor
Prefers dopamine neurons
VMAT inhibitor –> i.c. NT concentration increase and reversal of reuptake transporters, spilling NT into synaptic cleft.

5-HT agonist

Inhibits MAO A/B

INDICATION
adhd
narcolepsy
obesity

KINETICS

SIDE EFFECTS
CNS effects: hyperactivity, high social communication, decreased thirst/hunger, high short term memory, euphoria

Necrotizing arterolitis with abuse
Neurotoxic
Depression
Excessive thirst with continued use
Oversleeping 18h after effect wears off
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8
Q

Methylphenidate (ritalin)

presynaptic

A

Like metamphetamine

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9
Q

Dextroamphetamine (metamina)

presynaptic

A

Like metamphetamine

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10
Q

MDMA (ecstasy)

presynaptic

A

MECHANISM
SERT inhibitor in serotonin neurons

INDICATION

KINETICS

SIDE EFFECTS

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11
Q

Cocaine

presynaptic

A

MECHANISM
NET, DAT inhibitor
Na+ channel blocker

INDICATION
Local anaesthetic in topical ENT procedures
Hemostasis (intense vasoconstriction effect)

KINETICS
2h duration IV
30min duration by inhalation (crack cocaine)

SIDE EFFECTS
Tachycardia
Arrhythmia
Seizure
Respiratory depression
Aggressivity
Dependence
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12
Q

Imipramine
TCA

presynaptic

A

MECHANISM
NET, SERT inhibitor

INDICATION
Depression
Incontinence
Pharmacologic ejaculation in stallions

KINETICS

SIDE EFFECTS
Dizziness
Drowsiness
Orthostatic hypotension
Dry mouth
Urinary retention
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13
Q

Amytryptiline
TCA

presynaptic

A

MECHANISM
NET, SERT, DAT inhibitor

INDICATION
Depression

KINETICS

SIDE EFFECTS
Dizziness
Drowsiness
Orthostatic hypotension
Dry mouth
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14
Q

Desipramine
TCA

presynaptic

A 
MECHANISM
SNRI (selective NE reuptake inhibitor)
weak SSRI (selective serotonin reuptake inhibitor)

INDICATION
Depression - 2nd generation drug (better)

KINETICS

SIDE EFFECTS
Less side effects than the others

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15
Q

Tranylcypromine

presynaptic

A

MECHANISM
MAO inhibitor - nonselective

INDICATION
Depression

KINETICS

SIDE EFFECTS
Dizziness
Drowsiness
Orthostatic hypotension
Dry mouth
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16
Q

Selegiline

presynaptic

A

MECHANISM
MAO-B inhibitor, which increases dopamine levels

INDICATION
Early Parkinsons (delays L-DOPA need for 18 months)
Depression

KINETICS

SIDE EFFECTS
nausea
hallucinations
confusion
depression
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17
Q

Clorgiline

presynaptic

A

MECHANISM
MAO-A inhibitor

INDICATION
Depression (not used)

KINETICS

SIDE EFFECTS

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18
Q

Moclobemide

presynaptic

A

MECHANISM
MAO-A inhibitor

INDICATION
Depression
Anxiety

KINETICS

SIDE EFFECTS
Nausea
Dry mouth
Constipation
Diarrhoea
Insomnia
Dizziness
Anxiety
Restlessness
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19
Q

Epinephrine

postsynaptic

A 
MECHANISM
a1, a2, b1/2/3 agonist
b2 vasodilation in skeletal muscle
b2 glucagon/insulin secretion, glucose uptake in skeletal muscle
a1 vasoconstriction
b1 inotropic / chronotropic
b2 bronchodilation

INDICATION
Anaphylaxis
Complete heart block
Hemostasis
Cardiac arrest (1mg IV)
Asthma attack (if B2 agonist not enough)
Croup (subglottic laryngitis) inhaled
Local vasoconstriction (combination w/local anaesthetics)

KINETICS
Short duration
No CNS entry
IV, topical

SIDE EFFECTS
Hypertension
Arrhythmia
Stroke
MI
Pulm. edema
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20
Q

Norepinephrine (levophed)

postsynaptic

A

MECHANISM
a1, a2, b1/2/3 agonist
a1 vasoconstriction
Weak b2 effect (overall vasoconstriction)

INDICATION
Shock

KINETICS
IV only

SIDE EFFECTS
Vasospasm
Tissue necrosis
Hypertension
Arrhytmias
MI
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21
Q

Dopamine (Intropin)

Postsynaptic

A

MECHANISM
D1 agonist
a1/2 agonist
b1/3 agonist

In low doses constricts vessels except in brain and kidney, thus preserving flow to these vital organs. In high doses constricts all vessels.

INDICATION
Cardiogenic Shock (protects renal blood flow)
Bradycardia
Severe hypotension
Renal shutdown 
Heart failure

KINETICS
Only IV during shock

SIDE EFFECTS
Cardiovascular disturbance
Tachycardia 
Arrhythmias
GFR up
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22
Q

Isoproterenol (Isuprel)

Postsynaptic

A 
MECHANISM
b1/2/3 agonist
b1 inotropic/chronotropic
b2 Intense vasodilation
b2 bronchodilation

INDICATION
AV block
Bradycardia / cardiac arrest (until pacemaker can be installed)
Acute asthma

KINETICS
Nebulizer
IV

SIDE EFFECTS
Low BP (overall vasodilation effect)
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23
Q

Dobutamine (Dobutrex)

Postsynaptic

A

MECHANISM
b1 agonist

INDICATION
Acute heart failure (up C.O.)

KINETICS

SIDE EFFECTS
Tachycardia

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24
Q

Phenylephrine

Postsynaptic

A

MECHANISM
a1 agonist
Vasoconstriction

INDICATION
mydriasis (pupil dilator)
nasal decongestant
Internal urethral sphincter contraction
prostate contraction
erector pili contraction
KINETICS
15-60 minutes effect
Oral
Topical
Parenteral
SIDE EFFECTS
Compensatory reflex bradycardia
High BP
Stroke
MI
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25
Midodrine Postsynaptic
MECHANISM A1 agonist INDICATION Orthostatic hypotension KINETICS SIDE EFFECTS Hypertension in supine position
26
Methoxamine Postsynaptic
MECHANISM A1 agonist ``` INDICATION mydriasis (pupil dilator) nasal decongestant bladder contraction prostate contraction erector pili contration ``` KINETICS More prolonged vasoconstriction than phenylephrine ``` SIDE EFFECTS Compensatory reflex bradycardia High BP Stroke MI ```
27
Prenalterol Postsynaptic
MECHANISM B1 agonist INDICATION Cardiogenic shock Chronic heart failure KINETICS SIDE EFFECTS Tachycardia Arrhythmia
28
Ibopamine Postsynaptic
MECHANISM B1 agonist D1 agonist INDICATION Cardiogenic shock Chronic heart failure KINETICS Prodrug to N-methyl-dopamine SIDE EFFECTS Tachycardia Arrhythmia
29
Dobutamine Postsynaptic
MECHANISM B1 agonist INDICATION Cardiogenic shock Cardiac decompensation Acute congestive heart failure KINETICS SIDE EFFECTS Less tachycardia No significant O2 demand of myocardium, a great advantage over other sympatomimetic drugs
30
Metaproterenol Postsynaptic
MECHANISM B2 agonist Bronchodilator INDICATION Acute asthma attack COPD (bronchitis and emphysema) KINETICS 2-6h Inhalation SIDE EFFECTS Tachycardia Tremor
31
Salbutamol (ventoline) Postsynaptic
MECHANISM B2 agonist Bronchodilator INDICATION Acute asthma attack COPD (bronchitis and emphysema) Contra: Diabetes (hyperglycemia) KINETICS 2-6h Inhalation SIDE EFFECTS Hypokalemia Tachycardia Tremor
32
Terbutaline (Bricanyl) Postsynaptic
MECHANISM B2 agonist Bronchodilator INDICATION Acute asthma attack COPD (bronchitis and emphysema) Contra: Diabetes, arrhythmia KINETICS 2-6h Inhalation ``` SIDE EFFECTS Hyperglycemia Hypokalemia Tachycardia Tremor ```
33
Fenoterol Postsynaptic
MECHANISM B2 agonist Bronchodilator INDICATION Acute asthma attack COPD (bronchitis and emphysema) KINETICS Short acting Inhalation SIDE EFFECTS
34
Pirbuterol Postsynaptic
MECHANISM B2 agonist Bronchodilator INDICATION Acute asthma attack COPD (bronchitis and emphysema) KINETICS Short acting Inhalation SIDE EFFECTS
35
Salmeterol Postsynaptic
MECHANISM B2 agonist Bronchodilator INDICATION Acute asthma attack COPD (bronchitis and emphysema) KINETICS Long acting Inhalation SIDE EFFECTS
36
Formoterol Postsynaptic
MECHANISM B2 agonist Bronchodilator INDICATION Acute asthma attack COPD (bronchitis and emphysema) KINETICS Long acting Inhalation SIDE EFFECTS
37
Ritodrine Postsynaptic
MECHANISM B2 agonist INDICATION Stop premature birth (tocolytic, relaxes uterine contractions) Contraindication: Diabetes KINETICS SIDE EFFECTS
38
Fenoldopam Postsynaptic
MECHANISM D agonist INDICATION Hypertensive crisis Post operative hypertension Contra: glaucoma KINETICS Rapid acting vasodilator 4min onset IV 10min duration ``` SIDE EFFECTS Headache Flushing Hypotension Reflex tachycardia High intraoccular pressure ```
39
Clonidine Postsynaptic
MECHANISM a2 agonist i1 agonist (imidazole) ``` INDICATION Hypertension (CNS acting) Mild/moderate ADHD Anxiety Tic disorders Withdrawal Migrane ``` KINETICS IV or topical - vasoconstriction Oral - vasodilation, because it has specificity in CNS and decreases sympathetic outflow from the medulla SIDE EFFECTS
40
Template
MECHANISM INDICATION KINETICS SIDE EFFECTS
41
Methyldopa
MECHANISM a2 agonist False substrate in NE synthesis (less NE/dopamine produced) INDICATION Hypertension (CNS acting) Mild/moderate Can be used in pregnancy KINETICS SIDE EFFECTS depression, anxiety, apathy and parkinsonism
42
Guanfacine / guanabenz
MECHANISM a2 agonist INDICATION ADHD (not 1st line treatment) Anxiety KINETICS SIDE EFFECTS
43
Moxonodine / rilmenidine
MECHANISM a2 agonist i1 agonist (imidazole) INDICATION Hypertension (CNS acting) Mild/moderate KINETICS SIDE EFFECTS
44
Apraclonidine / brimondine
MECHANISM a2 agonist a1 weak agonist Decreased aqueous humor secretion INDICATION Glaucoma KINETICS SIDE EFFECTS
45
Dexmedetomidine
MECHANISM a2 agonist INDICATION ICU sedation Cocaine/amphetamine overdose 2nd line after benzodiazepines such as diazepam (Valium) Sedation and non opioid pain relief w/o respiratory depression KINETICS SIDE EFFECTS
46
Xylamethazoline / oxymetazoline
MECHANISM a agonist non-selective INDICATION Sinusitis Allergic rhinitis KINETICS Nasal decogestant Spray <7d SIDE EFFECTS
47
Ephedrine | Pseudoephedrine
MECHANISM Direct: a+b receptor agonist Indirect: NE release from presynaptic terminal ``` INDICATION Better sympathomimetic stimulants exist Nasal decongestant Allergic rhinitis Vasoconstrictor ``` KINETICS Poor MAO/COMT degradation gives longer duration of action SIDE EFFECTS
48
Phenoxybenzamine | Phentolamine
MECHANISM a blocker non-selective serotonin receptor blocker Vasodilation INDICATION Pheochromocytoma (NE) Carcinoid (serotonin GI/flushing symtoms) Raynauds phenomenon KINETICS Oral 1-2 days half life (phenoxybenzamine) IV 2-4h half life (phentolamine) SIDE EFFECTS
49
Tolazoline
MECHANISM a blocker non-selective INDICATION Peripheral vasospasm KINETICS SIDE EFFECTS
50
Prazosin
MECHANISM a1 blocker vasodilation INDICATION Hypertension - 2nd line treatment Benign prostatic hyperplasia - a1 receptors are in the bladder neck and prostate capsule/stroma KINETICS 8h Oral SIDE EFFECTS
51
Terazosin / Doxazosin
MECHANISM a1 blocker vasodilation INDICATION Hypertension - 2nd line treatment Benign prostatic hyperplasia - a1 receptors are in the bladder neck and prostate capsule/stroma KINETICS 12-24h SIDE EFFECTS Priapism (constant erection)
52
Alfuzosine / Tamzulosine
MECHANISM a1 blocker INDICATION Benign prostatic hyperplasia ONLY KINETICS SIDE EFFECTS
53
Urapidil
``` MECHANISM a1 blocker b blocker a2 agonist serotonin agonist ``` INDICATION Hypertension KINETICS SIDE EFFECTS
54
Labetalol / carvedilol
``` MECHANISM a1 blocker b blocker non-selective Angina pectoris etc. (b racemix) Hypertension (a1 racemix) ``` ``` INDICATION Hypertension Pheochromocytoma hypertension Preclampsia High BP in pregnancy with proteinuria, which develops to eclampsia with seizure if left untreated Congestive heart failure - CARVEDILOL ``` KINETICS IV in hypertensive crisis Oral long term SIDE EFFECTS
55
Yohimbine
MECHANISM a2 blocker INDICATION Erectile dysfunction - obsolete Research KINETICS SIDE EFFECTS
56
Propranolol
MECHANISM b blocker non-selective Na+ channel blocker - Weak local anaesthetic ``` INDICATION Hypertensive crisis - by decreasing CO and renin release, and decreased sympathetic outflow from CNS Angina pectoris Supra-ventricular arrhythmias MI - 2ndary prophylaxis Migrane prophylaxis Esophageal varices Hyperthyroidism ``` KINETICS Half life 4-6h Oral / parenteral High lipid solubility - Can cross BBB and cause CNS side effects such as depression and nightmares ``` SIDE EFFECTS Bronchoconstriction Hypoglycemia Use with caution in DM and hyperthyroidism Worse lipid balance Cardiac decompensation Bradycardia Cold extremities Reflex peripheral vasoconstriction Arrhythmias - If medication is stopped abruptly Depression Sleeping problems ```
57
Alprenolol
MECHANISM b blocker non-selective ISA Na+ channel blocker - Weak local anaesthetic INDICATION Angina pectoris KINETICS SIDE EFFECTS
58
Carteolol
MECHANISM b blocker non-selective ISA INDICATION Glaucoma KINETICS Half life 6h SIDE EFFECTS
59
Carvedilol
MECHANISM b blocker non-selective a1 blocker INDICATION Angina pectoris etc. (b racemix) Hypertension (a1 racemix) KINETICS Half life 6h SIDE EFFECTS
60
Labetolol
MECHANISM b blocker non-selective a1 blocker INDICATION Angina pectoris etc. (b racemix) Hypertension (a1 racemix) KINETICS Half life 7-10h SIDE EFFECTS
61
Nadolol
MECHANISM b blocker non-selective INDICATION Hypertension Angina pectoris etc. KINETICS More potent than propranolol Half life 14-24h SIDE EFFECTS
62
Oxprenolol
MECHANISM b blocker non-selective ISA Na+ channel blocker - Weak local anaesthetic INDICATION Hypertension Angina pectoris etc. KINETICS Lipophilic - crosses CNS Half life 1-2h SIDE EFFECTS Bronchoconstriction
63
Penbutolol
MECHANISM b blocker non-selective ISA INDICATION Hypertension Angina pectoris etc. KINETICS Lipophilic - crosses CNS Half life 5h SIDE EFFECTS Bronchoconstriction
64
Pindolol
MECHANISM b blocker non-selective ISA INDICATION Hypertension Angina pectoris etc. KINETICS Half life 3-4h SIDE EFFECTS Bronchoconstriction
65
Sotalol
``` MECHANISM b blocker non-selective K+ channel blocker - Used as class 3 antiarrhythmic drug ``` INDICATION Serious tachyarrhythmias Life-threatening ventricular tachycardias Symptomatic atrial fibrillation KINETICS Half life 12h SIDE EFFECTS QT prolongation
66
Timolol
MECHANISM b blocker non-selective INDICATION Open angle glaucoma - Reduces aqueous humor production - Does not widen pupil or affect accommodation Hypertension KINETICS More potent than propranolol Half life 4-6h SIDE EFFECTS
67
Acebutolol
MECHANISM b1 blocker ISA Na+ channel blocker - Weak local anaesthetic INDICATION Angina Hypertension w/pulmonary disease KINETICS Half life 3-4h Lipid soluble - Crosses CNS SIDE EFFECTS No hyperlipidemia
68
Atenolol
MECHANISM b1 blocker ``` INDICATION hypertension angina long QT syndrome acute MI supraventricular tachycardia ventricular tachycardia alcohol withdrawal ``` KINETICS Half life 6-9h Water soluble SIDE EFFECTS Safer to use in patients treated with benzodiazepine for insomnia
69
Betaxolol
MECHANISM b1 blocker INDICATION Glaucoma KINETICS Half life 14-20h SIDE EFFECTS
70
Bisoprolol
MECHANISM b1 blocker INDICATION Chronic heart failure KINETICS Half life 10-12h SIDE EFFECTS
71
Celiprolol
MECHANISM b1 blocker ISA on b2 - Mild vasodilation and no bronchoconstriction INDICATION Hypertension KINETICS Half life 4-5h SIDE EFFECTS No bronchoconstriction
72
Esmolol
MECHANISM b1 blocker INDICATION Control HR and BP during surgery or diagnostics KINETICS Half life 10min SIDE EFFECTS
73
Metoprolol
MECHANISM b1 blocker Na+ channel blocker - Weak local anaesthetic INDICATION Chronic heart failure KINETICS Half life 3-4h SIDE EFFECTS
74
Nebivolol
MECHANISM b1 blocker NO mediated vasodilation INDICATION Hypertension KINETICS Half life 10-30h SIDE EFFECTS

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