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pharmachology > Sympatomimetics > Flashcards

Sympatomimetics Flashcards

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
Q

Midodrine

Postsynaptic

A

MECHANISM
A1 agonist

INDICATION
Orthostatic hypotension

KINETICS

SIDE EFFECTS
Hypertension in supine position

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26
Q

Methoxamine

Postsynaptic

A

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
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27
Q

Prenalterol

Postsynaptic

A

MECHANISM
B1 agonist

INDICATION
Cardiogenic shock
Chronic heart failure

KINETICS

SIDE EFFECTS
Tachycardia
Arrhythmia

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28
Q

Ibopamine

Postsynaptic

A

MECHANISM
B1 agonist
D1 agonist

INDICATION
Cardiogenic shock
Chronic heart failure

KINETICS
Prodrug to N-methyl-dopamine

SIDE EFFECTS
Tachycardia
Arrhythmia

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29
Q

Dobutamine

Postsynaptic

A

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

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30
Q

Metaproterenol

Postsynaptic

A

MECHANISM
B2 agonist
Bronchodilator

INDICATION
Acute asthma attack
COPD (bronchitis and emphysema)

KINETICS
2-6h
Inhalation

SIDE EFFECTS
Tachycardia
Tremor

31
Q

Salbutamol (ventoline)

Postsynaptic

A

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
Q

Terbutaline (Bricanyl)

Postsynaptic

A

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
Q

Fenoterol

Postsynaptic

A

MECHANISM
B2 agonist
Bronchodilator

INDICATION
Acute asthma attack
COPD (bronchitis and emphysema)

KINETICS
Short acting
Inhalation

SIDE EFFECTS

34
Q

Pirbuterol

Postsynaptic

A

MECHANISM
B2 agonist
Bronchodilator

INDICATION
Acute asthma attack
COPD (bronchitis and emphysema)

KINETICS
Short acting
Inhalation

SIDE EFFECTS

35
Q

Salmeterol

Postsynaptic

A

MECHANISM
B2 agonist
Bronchodilator

INDICATION
Acute asthma attack
COPD (bronchitis and emphysema)

KINETICS
Long acting
Inhalation

SIDE EFFECTS

36
Q

Formoterol

Postsynaptic

A

MECHANISM
B2 agonist
Bronchodilator

INDICATION
Acute asthma attack
COPD (bronchitis and emphysema)

KINETICS
Long acting
Inhalation

SIDE EFFECTS

37
Q

Ritodrine

Postsynaptic

A

MECHANISM
B2 agonist

INDICATION
Stop premature birth
(tocolytic, relaxes uterine contractions)
Contraindication: Diabetes

KINETICS

SIDE EFFECTS

38
Q

Fenoldopam

Postsynaptic

A

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
Q

Clonidine

Postsynaptic

A

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
Q

Template

A

MECHANISM

INDICATION

KINETICS

SIDE EFFECTS

41
Q

Methyldopa

A

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
Q

Guanfacine / guanabenz

A

MECHANISM
a2 agonist

INDICATION
ADHD (not 1st line treatment)
Anxiety

KINETICS

SIDE EFFECTS

43
Q

Moxonodine / rilmenidine

A

MECHANISM
a2 agonist
i1 agonist (imidazole)

INDICATION
Hypertension (CNS acting)
Mild/moderate

KINETICS

SIDE EFFECTS

44
Q

Apraclonidine / brimondine

A

MECHANISM
a2 agonist
a1 weak agonist
Decreased aqueous humor secretion

INDICATION
Glaucoma

KINETICS

SIDE EFFECTS

45
Q

Dexmedetomidine

A

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
Q

Xylamethazoline / oxymetazoline

A

MECHANISM
a agonist non-selective

INDICATION
Sinusitis
Allergic rhinitis

KINETICS
Nasal decogestant
Spray <7d

SIDE EFFECTS

47
Q

Ephedrine

Pseudoephedrine

A

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
Q

Phenoxybenzamine

Phentolamine

A

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
Q

Tolazoline

A

MECHANISM
a blocker non-selective

INDICATION
Peripheral vasospasm

KINETICS

SIDE EFFECTS

50
Q

Prazosin

A

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
Q

Terazosin / Doxazosin

A

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
Q

Alfuzosine / Tamzulosine

A

MECHANISM
a1 blocker

INDICATION
Benign prostatic hyperplasia ONLY

KINETICS

SIDE EFFECTS

53
Q

Urapidil

A 
MECHANISM
a1 blocker
b blocker
a2 agonist
serotonin agonist

INDICATION
Hypertension

KINETICS

SIDE EFFECTS

54
Q

Labetalol / carvedilol

A 
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
Q

Yohimbine

A

MECHANISM
a2 blocker

INDICATION
Erectile dysfunction - obsolete
Research

KINETICS

SIDE EFFECTS

56
Q

Propranolol

A

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
Q

Alprenolol

A

MECHANISM
b blocker non-selective
ISA
Na+ channel blocker - Weak local anaesthetic

INDICATION
Angina pectoris

KINETICS

SIDE EFFECTS

58
Q

Carteolol

A

MECHANISM
b blocker non-selective
ISA

INDICATION
Glaucoma

KINETICS
Half life 6h

SIDE EFFECTS

59
Q

Carvedilol

A

MECHANISM
b blocker non-selective
a1 blocker

INDICATION
Angina pectoris etc. (b racemix)
Hypertension (a1 racemix)

KINETICS
Half life 6h

SIDE EFFECTS

60
Q

Labetolol

A

MECHANISM
b blocker non-selective
a1 blocker

INDICATION
Angina pectoris etc. (b racemix)
Hypertension (a1 racemix)

KINETICS
Half life 7-10h

SIDE EFFECTS

61
Q

Nadolol

A

MECHANISM
b blocker non-selective

INDICATION
Hypertension
Angina pectoris etc.

KINETICS
More potent than propranolol
Half life 14-24h

SIDE EFFECTS

62
Q

Oxprenolol

A

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
Q

Penbutolol

A

MECHANISM
b blocker non-selective
ISA

INDICATION
Hypertension
Angina pectoris etc.

KINETICS
Lipophilic - crosses CNS
Half life 5h

SIDE EFFECTS
Bronchoconstriction

64
Q

Pindolol

A

MECHANISM
b blocker non-selective
ISA

INDICATION
Hypertension
Angina pectoris etc.

KINETICS
Half life 3-4h

SIDE EFFECTS
Bronchoconstriction

65
Q

Sotalol

A 
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
Q

Timolol

A

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
Q

Acebutolol

A

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
Q

Atenolol

A

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
Q

Betaxolol

A

MECHANISM
b1 blocker

INDICATION
Glaucoma

KINETICS
Half life 14-20h

SIDE EFFECTS

70
Q

Bisoprolol

A

MECHANISM
b1 blocker

INDICATION
Chronic heart failure

KINETICS
Half life 10-12h

SIDE EFFECTS

71
Q

Celiprolol

A

MECHANISM
b1 blocker
ISA on b2 - Mild vasodilation and no bronchoconstriction

INDICATION
Hypertension

KINETICS
Half life 4-5h

SIDE EFFECTS
No bronchoconstriction

72
Q

Esmolol

A

MECHANISM
b1 blocker

INDICATION
Control HR and BP during surgery or diagnostics

KINETICS
Half life 10min

SIDE EFFECTS

73
Q

Metoprolol

A

MECHANISM
b1 blocker
Na+ channel blocker - Weak local anaesthetic

INDICATION
Chronic heart failure

KINETICS
Half life 3-4h

SIDE EFFECTS

74
Q

Nebivolol

A

MECHANISM
b1 blocker
NO mediated vasodilation

INDICATION
Hypertension

KINETICS
Half life 10-30h

SIDE EFFECTS

pharmachology (7 decks)

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