Cholinergic: paraysympathomimetics (cholinomimetics)

Type Receptor activity Drugs Mechanism of Action Uses Side effects

Muscarinic: salivation,
flushing, bronchospasm,
Acetylcholine
Urinary retention after surgery or sweating, nausea, abdominal
Cholinergic Carbachol
postpartum pain, GI cramps, diarrhea,
agonists Bethanechol
Glaucoma BP
Pilocarpine
Nicotinic: fascicultations,
respiratory arrest
Fasciculations, respiratory
Direct acting Overstimulation results in Muscle relaxation/paralysis
Succinylcholine arrest, malignant
depolarizing blockade associated w/ intubation
hyperthermia
Low doses ganglionic
Nicotinic agonists stimulation causing Vomiting, convulsions,
euphoria & arousal hypertension, cardiac
Nicotine
CNS affects cause arrhythmias, respiratory arrest
relaxation & improve PNS ganglia stimulation
attention
Edrophonium Prolongs duration of ACh by
Reversible Myasthenia gravis
Neostigmine binding w/ & block
cholinergic Glaucoma
Pyridostigmine acetylcholinesterase (BOTH
agonists Atropine poisoning Salivation, flushing,
Physostigmine N & M effects)
bradycardia, bronchospasm,
Reversible Donepezil cerebral concentrations
sweating, nausea, abdominal
Indirect acting cholinergic Galantamine of ACh by inhibiting
pain, diarrhea, BP, muscle
agonists CNS Rivastigmine acetylcholinesterase
fasiculations (N), respiratory
Prolongs duration of ACh by
Irreversible arrest (N)
permanently inactivating
cholinergic Echothiophate Glaucoma
acetylcholinesterase (BOTH
agonists
N & M effects)
Cholinergic: parasympatholytics (anticholinergics)
Receptor activity Drugs Mechanism of Action Uses Side effects
Atropine cholinesterase
poisoning, bradycardia
Benztropine - parkinsonism
Dicyclomine - IBS Autonomic: dry mouth,
Ipratropium COPD, Block muscarinic receptors blurred vision, tachycardia,
rhinorrhea on the effector organs of Varies urinary retention,
Muscarinic receptor antagonists Oxybutynin overactive the parasympathetic Specificity for M receptors is constipation, inhibition of
bladder nervous system & on the useful sweating
Tolterodine overactive sweat glands CNS: restlessness, confusion,
bladder hallucinations
Trpicamide - mydriasis
Scopolamine motion
sickness, amnesia
Nicotinic Ganglionic Mecamylamine non Hypotension, orthostatic
receptor blockers (Nn) depolarizing, competitive hypotension, atony of bladder
antagonists blocker & GI tract, cycloplegia,
Nicotine depolarizing xerostomia, sexual
blocker, can cause dysfunction, hyperthermia
 respiratory paralysis &
hypotension & high doses

Tubocurarine
Competitive blocker
Atracurium
Neuromuscular Action can be reversed by Muscle relaxation/paralysis
Pancuronium Respiratory arrest
blockers (Nm) increasing concentration of associated w/ intubation
Rocuronium
ACh
Vecuronium

Adrenergic
Type Receptor activity Drugs Mechanism of Action Uses Side effects
High potency
Epinephrine Activate both &
Norepinephrine receptors
Catecholamines Dopamine Rapidly destroyed by
Dobutamine MAO & COMT
Isoproterenol Not effective when
given orally
Not destroyed by COMT
Non-catecholamines & MAO
Better CNS penetration
Mimic NE, EPI
Bind to adrenergic
Direct acting receptors w/o
Adrenergic agonist interacting w/ the
prejunctional neuron
Displaces NE from
storage sites
(amphetamine,
Amphetamine
tyramine)
Tyramine
Indirect acting Block the uptake of NE
Cocaine
at storage sites
TCAs
(cocaine)
Inhibit enzymatic
breakdown of NE (TCAs)
Stimulate receptors &
Ephedrine
Mixed acting displaces NE from
Pseudoephedrine
storage sites
Nasal decongestant,
mydriatic Hypertension,
Phenylephrine
Direct acting 1 agonist Systemically nervousness,
Ozymetazoline
vasopressor for headaches
hypotension to BP
Direct acting 2 agonist Clonidine Hypertension Caution for withdrawal
Apraclonidine inhibition of supersensitivity
 sympathetic vasomotor
centers, decreasing BP
Brimonodine ADHD & impulsive
behavior
Glaucoma
Tachycardia,
palpitations, severe
Primarily 1
hypotension (
Direct acting 1 agonist Dobutamine CO w/ few heart rate Congestive heart failure
antagonist effect)
or vascular effects
Can ventricular rate
in atrial fibrillation
Albuterol Nervousness, muscle
Terbutaline tremors, tachycardia
Bronchodilator, asthma,
Direct acting 2 agonists Metaproterenol Systemically =
long actings in COPD
Salmeterol, formoterol hypokalemia,
(long acting) hyperglycemia

Sympatholytics
Type Drugs Mechanism of Action Uses Side effects
Prevents uptake of
biogenic amines in
Diarrhea, cramps, GI acid secretion, postural
both central &
Adrenergic neuronal hypotension, bradycardia, sexual
Reserpine (d/c in US) peripheral neurons Hypertension
blocking dysfunction, sedation, depression
results in biogenic
Caution for supersensitivity
amine depletion
causing denervation
Phentolamine
(reversible &
Diagnosis & Orthostatic hypertension, exaggerated reflex
Nonselective competitive)
Block both 1 & 2 treatment of tachycardia, nasal stuffiness, ejaculatory
adrenergic blocking Phenozybenzamine
pheochromocytoma dysfunction
(irreversible & non-
competitive)
First dose effect exaggerated hypotension
Hypertension that can lead to syncope especially when pt
Prazosin
Benign prostatic stands after sitting or lying down (orthostatic
Doxazosin
1 selective hypertrophy relaxes hypotension)
Terazosin
adrenergic blocking bladder neck & Less reflex tachycardia
Tamsulosin (selective
prostate smooth Na & H2O retention
for 1a)
muscle Nasal stuffiness
Ejaculatory dysfunction
adrenergic blocking Propranolol* * = nonselective, Prevention of Bradycardia, heart block, heart failure,
Timolo* both 1 & 2 migraines may Raynauds, vivid dreams, depression,
 prevent
catecholamine
vasodilation in the
brain vasculature
Hyperthyroidism
Nadolol* thyroid storm bronchoconstriction in asthmatics/COPD,
Atenolol** ** = cardioselective, Glaucoma sexual dysfunction, glycogenolysis &
Metoprolol** 1 specific Arrhythmias, angina glucagon secretion
Esmolol** pectoris, myocardial Caution for withdrawal supersensitivity
infarction, heart
failure protective
effect against
sympathetic
overstimulation
Block both 1 &
adrenoceptors
Result in peripheral Hypertension* &
& adrenergic Labetalol* Combines BOTH & adrenoceptor blocker
vasodilation that congestive heart
blocking Carvedilol** adverse effects
lowers BP w/ reduced failure**
cardia rate &
contraction