Autonomic Drugs

PharmacologyUpdated 2 min read
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AUTONOMIC NERVOUS SYSTEM

Autonomic pathways

The autonomic nervous system regulates smooth muscle, cardiac muscle and glands.

PathwayPreganglionic neurotransmitterPostganglionic neurotransmitter
SympatheticAChUsually noradrenaline
ParasympatheticAChACh
Sympathetic to sweat glandsAChACh
Adrenal medullaACh at nicotinic receptorsReleases mainly epinephrine and some norepinephrine into blood

All autonomic preganglionic neurons release acetylcholine onto nicotinic neuronal (Nn) receptors.

Receptor summary

ReceptorMain location/effectMemory Aid
α₁Vascular smooth-muscle contraction; mydriasis via radial iris muscle
α₂Presynaptic inhibition of noradrenaline release; reduced sympathetic outflow
β₁Increased heart rate, contractility and renin releaseB1 = 1 Heart
β₂Bronchodilation and relaxation of selected smooth musclesB2 = 2 Lungs
β₃Bladder detrusor relaxation; lipolysis
M₂Slows heart rate and AV nodal conduction
M₃Glandular secretion, smooth-muscle contraction and endothelial nitric oxide release
NnAutonomic ganglia and adrenal medulla
NmNeuromuscular junction of skeletal muscle

High-yield receptor effects

  • α₁ activation → vasoconstriction.
  • α₂ activation → reduced presynaptic neurotransmitter release.
  • β₁ activation → increased heart rate and contractility.
  • β₂ activation → bronchodilation.
  • M₂ activation → reduced heart rate.
  • M₃ activation → increased glandular secretion and smooth-muscle contraction.

Cholinergic drugs

DrugMechanism/useImportant adverse effects
BethanecholMuscarinic agonist; urinary retention in selected patientsBradycardia, hypotension, diarrhea
PilocarpineMuscarinic agonist; xerostomia and glaucomaSweating, salivation, bronchospasm
NeostigmineAcetylcholinesterase inhibitor; myasthenia gravis and reversal of selected neuromuscular blockadeBradycardia, secretions, diarrhea
AtropineMuscarinic antagonistDry mouth, tachycardia, blurred vision, urinary retention
IpratropiumInhaled muscarinic antagonistDry mouth, possible ocular effects if aerosol enters eyes

Organophosphate poisoning

Organophosphates inhibit acetylcholinesterase, causing excess acetylcholine at muscarinic, nicotinic and central nervous system sites.

FeatureFindings
MuscarinicSalivation, lacrimation, urination, diarrhea, bronchorrhea, bronchospasm, bradycardia
NicotinicFasciculations, weakness, paralysis
CNSConfusion, seizures, reduced consciousness

Treatment includes appropriate decontamination and supportive care, atropine for muscarinic manifestations and pralidoxime when indicated, particularly when given early. Severe poisoning is an emergency.

Adrenergic drugs

DrugMain actionCommon clinical use
Epinephrineα₁, α₂, β₁, β₂ agonistAnaphylaxis; cardiac arrest
NorepinephrinePredominantly α₁/α₂, with β₁ activityVasopressor support
Phenylephrineα₁ agonistVasoconstriction; selected hypotensive states
Salbutamolβ₂ agonistBronchospasm
ClonidineCentral α₂ agonistSelected hypertension indications
PropranololNonselective β blockerSelected cardiovascular and other indications
MetoprololRelatively β₁-selective blockerSelected cardiovascular conditions
Prazosinα₁ blockerSelected hypertension and urinary symptoms

Exam tip: Epinephrine is the first-line medication for anaphylaxis.