Sympatomimetics Flashcards
Levodopa
presynaptic
MECHANISM
NE precursor
Passes BBB
INDICATION
Parkinson’s
SIDE EFFECTS
4-aminopyridine
presynaptic
MECHANISM
K+ channel blocker
Increases membrane potential in NE neurons, longer NT release
INDICATION
Research
SIDE EFFECTS
Latrotoxin
presynaptic
MECHANISM
Causes Ca2+ influx presynaptically, and NT release in Cholinergic and Adrenergic neurons.
INDICATION
Research
Spider venom
SIDE EFFECTS
Mianserin
presynaptic
MECHANISM
Inh a2 receptor in presynaptic neurons = stimulation
INDICATION
Depression
SIDE EFFECTS
Tyramine
presynaptic
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.
Ephedrine
Pseudoephedrine
presynaptic
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.
Amphetamine
Metamphetamine (speed)
presynaptic
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
Methylphenidate (ritalin)
presynaptic
Like metamphetamine
Dextroamphetamine (metamina)
presynaptic
Like metamphetamine
MDMA (ecstasy)
presynaptic
MECHANISM
SERT inhibitor in serotonin neurons
INDICATION
KINETICS
SIDE EFFECTS
Cocaine
presynaptic
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
Imipramine
TCA
presynaptic
MECHANISM
NET, SERT inhibitor
INDICATION
Depression
Incontinence
Pharmacologic ejaculation in stallions
KINETICS
SIDE EFFECTS Dizziness Drowsiness Orthostatic hypotension Dry mouth Urinary retention
Amytryptiline
TCA
presynaptic
MECHANISM
NET, SERT, DAT inhibitor
INDICATION
Depression
KINETICS
SIDE EFFECTS Dizziness Drowsiness Orthostatic hypotension Dry mouth
Desipramine
TCA
presynaptic
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
Tranylcypromine
presynaptic
MECHANISM
MAO inhibitor - nonselective
INDICATION
Depression
KINETICS
SIDE EFFECTS Dizziness Drowsiness Orthostatic hypotension Dry mouth
Selegiline
presynaptic
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
Clorgiline
presynaptic
MECHANISM
MAO-A inhibitor
INDICATION
Depression (not used)
KINETICS
SIDE EFFECTS
Moclobemide
presynaptic
MECHANISM
MAO-A inhibitor
INDICATION
Depression
Anxiety
KINETICS
SIDE EFFECTS Nausea Dry mouth Constipation Diarrhoea Insomnia Dizziness Anxiety Restlessness
Epinephrine
postsynaptic
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
Norepinephrine (levophed)
postsynaptic
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
Dopamine (Intropin)
Postsynaptic
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
Isoproterenol (Isuprel)
Postsynaptic
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)
Dobutamine (Dobutrex)
Postsynaptic
MECHANISM
b1 agonist
INDICATION
Acute heart failure (up C.O.)
KINETICS
SIDE EFFECTS
Tachycardia
Phenylephrine
Postsynaptic
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
Midodrine
Postsynaptic
MECHANISM
A1 agonist
INDICATION
Orthostatic hypotension
KINETICS
SIDE EFFECTS
Hypertension in supine position
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
Prenalterol
Postsynaptic
MECHANISM
B1 agonist
INDICATION
Cardiogenic shock
Chronic heart failure
KINETICS
SIDE EFFECTS
Tachycardia
Arrhythmia
Ibopamine
Postsynaptic
MECHANISM
B1 agonist
D1 agonist
INDICATION
Cardiogenic shock
Chronic heart failure
KINETICS
Prodrug to N-methyl-dopamine
SIDE EFFECTS
Tachycardia
Arrhythmia
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
Metaproterenol
Postsynaptic
MECHANISM
B2 agonist
Bronchodilator
INDICATION
Acute asthma attack
COPD (bronchitis and emphysema)
KINETICS
2-6h
Inhalation
SIDE EFFECTS
Tachycardia
Tremor
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
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
Fenoterol
Postsynaptic
MECHANISM
B2 agonist
Bronchodilator
INDICATION
Acute asthma attack
COPD (bronchitis and emphysema)
KINETICS
Short acting
Inhalation
SIDE EFFECTS
Pirbuterol
Postsynaptic
MECHANISM
B2 agonist
Bronchodilator
INDICATION
Acute asthma attack
COPD (bronchitis and emphysema)
KINETICS
Short acting
Inhalation
SIDE EFFECTS
Salmeterol
Postsynaptic
MECHANISM
B2 agonist
Bronchodilator
INDICATION
Acute asthma attack
COPD (bronchitis and emphysema)
KINETICS
Long acting
Inhalation
SIDE EFFECTS
Formoterol
Postsynaptic
MECHANISM
B2 agonist
Bronchodilator
INDICATION
Acute asthma attack
COPD (bronchitis and emphysema)
KINETICS
Long acting
Inhalation
SIDE EFFECTS
Ritodrine
Postsynaptic
MECHANISM
B2 agonist
INDICATION
Stop premature birth
(tocolytic, relaxes uterine contractions)
Contraindication: Diabetes
KINETICS
SIDE EFFECTS
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
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
Template
MECHANISM
INDICATION
KINETICS
SIDE EFFECTS
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
Guanfacine / guanabenz
MECHANISM
a2 agonist
INDICATION
ADHD (not 1st line treatment)
Anxiety
KINETICS
SIDE EFFECTS
Moxonodine / rilmenidine
MECHANISM
a2 agonist
i1 agonist (imidazole)
INDICATION
Hypertension (CNS acting)
Mild/moderate
KINETICS
SIDE EFFECTS
Apraclonidine / brimondine
MECHANISM
a2 agonist
a1 weak agonist
Decreased aqueous humor secretion
INDICATION
Glaucoma
KINETICS
SIDE EFFECTS
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
Xylamethazoline / oxymetazoline
MECHANISM
a agonist non-selective
INDICATION
Sinusitis
Allergic rhinitis
KINETICS
Nasal decogestant
Spray <7d
SIDE EFFECTS
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
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
Tolazoline
MECHANISM
a blocker non-selective
INDICATION
Peripheral vasospasm
KINETICS
SIDE EFFECTS
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
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)
Alfuzosine / Tamzulosine
MECHANISM
a1 blocker
INDICATION
Benign prostatic hyperplasia ONLY
KINETICS
SIDE EFFECTS
Urapidil
MECHANISM a1 blocker b blocker a2 agonist serotonin agonist
INDICATION
Hypertension
KINETICS
SIDE EFFECTS
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
Yohimbine
MECHANISM
a2 blocker
INDICATION
Erectile dysfunction - obsolete
Research
KINETICS
SIDE EFFECTS
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
Alprenolol
MECHANISM
b blocker non-selective
ISA
Na+ channel blocker - Weak local anaesthetic
INDICATION
Angina pectoris
KINETICS
SIDE EFFECTS
Carteolol
MECHANISM
b blocker non-selective
ISA
INDICATION
Glaucoma
KINETICS
Half life 6h
SIDE EFFECTS
Carvedilol
MECHANISM
b blocker non-selective
a1 blocker
INDICATION
Angina pectoris etc. (b racemix)
Hypertension (a1 racemix)
KINETICS
Half life 6h
SIDE EFFECTS
Labetolol
MECHANISM
b blocker non-selective
a1 blocker
INDICATION
Angina pectoris etc. (b racemix)
Hypertension (a1 racemix)
KINETICS
Half life 7-10h
SIDE EFFECTS
Nadolol
MECHANISM
b blocker non-selective
INDICATION
Hypertension
Angina pectoris etc.
KINETICS
More potent than propranolol
Half life 14-24h
SIDE EFFECTS
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
Penbutolol
MECHANISM
b blocker non-selective
ISA
INDICATION
Hypertension
Angina pectoris etc.
KINETICS
Lipophilic - crosses CNS
Half life 5h
SIDE EFFECTS
Bronchoconstriction
Pindolol
MECHANISM
b blocker non-selective
ISA
INDICATION
Hypertension
Angina pectoris etc.
KINETICS
Half life 3-4h
SIDE EFFECTS
Bronchoconstriction
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
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
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
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
Betaxolol
MECHANISM
b1 blocker
INDICATION
Glaucoma
KINETICS
Half life 14-20h
SIDE EFFECTS
Bisoprolol
MECHANISM
b1 blocker
INDICATION
Chronic heart failure
KINETICS
Half life 10-12h
SIDE EFFECTS
Celiprolol
MECHANISM
b1 blocker
ISA on b2 - Mild vasodilation and no bronchoconstriction
INDICATION
Hypertension
KINETICS
Half life 4-5h
SIDE EFFECTS
No bronchoconstriction
Esmolol
MECHANISM
b1 blocker
INDICATION
Control HR and BP during surgery or diagnostics
KINETICS
Half life 10min
SIDE EFFECTS
Metoprolol
MECHANISM
b1 blocker
Na+ channel blocker - Weak local anaesthetic
INDICATION
Chronic heart failure
KINETICS
Half life 3-4h
SIDE EFFECTS
Nebivolol
MECHANISM
b1 blocker
NO mediated vasodilation
INDICATION
Hypertension
KINETICS
Half life 10-30h
SIDE EFFECTS
