CHAPTER 7: DRUGS THAT AFFECT THE PARASYMPATHETIC NERVOUS

SYSTEM

Cholinergic Nerve Activity

 Cholinergic nerves/receptors release/receive acetylcholine
 ACH synthesized from choline (from B vitamins) and acetyl coenzyme A and stored in
vesicles
 Enzymes acetylcholinesterase and pseudocholinesterase inactivate ACH quickly so the
effects only last a few seconds
 Some toxins that produce food poisoning can inhibit ACH release

3 Types of Cholinergic Receptors

 Muscarinic: at postganglionic nerve endings, on smooth and cardiac muscle
 Nicotinic-Neural (Nn): cholinergic receptors at ganglionic sites, present in
parasympathetic and sympathetic NS
 Nicotinic-Muscle (Nm): on skeletal muscle, receive ACH signals from somatic neurons,
not part of autonomic nervous system
Cholinergic Drugs
 Also known asparasympathomimetic
 Direct acting: bind to muscarinic receptors and produce similar effects to ACH
o ACH is fast acting so direct acting drugs are made to inactivate slower

 Pharmacological Effects: produce GI secretions and urination, and pupil constriction

  Clinical Indications: rarely used systematically, but can be used to stimulate urinary tract,
and to constrict pupil to promote drainage of fluid in eye, preventing damage from
glaucoma
 Indirect acting: inibit acetylcholinesterase enzyme, which increases concentration and
effect of ACH at both muscarinic and nicotinic receptors
o Reversible Inhibitors: used to treat myasthenia gravis (fluctuating skeletal muscle
weakness and paralysis) and Alzheimer’s
 increase ACH concentration which strengthens muscular contractions
o Irreversible Inhibitors: form irreversible bonds with acetylcholinesterase
 Mainly used to treat glaucoma
 Can cause toxicity easily with a large dose

 Adverse and Toxic Effects: nausea, vomiting, diarrhea, blurred vision, sweating,
bronchoconstriction, all due to excessive parasympathetic stimulation
o Antidote is anticholinergic drugs
Clinical Indications for Anticholinesterase Drugs
 Glaucoma: reduce metabolism of ACH, increase levels to produce miosis, reducing fluid
in eye and reducing pressure
 Myasthenia Gravis:
o Autoimmune disease, antibodies attack Nm receptors, reducing muscle strength
o Use longer lasting reversible anticholinesterase drugs
 Can increase bladder contractions when a patient has urinary retention
 Alzheimer’s: results from a loss of synapses and decreased ACH levels
o Some treatment with reversible anticholinesterase drugs which increase ACH
levels
 Used to reverse the effects of induced skeletal muscle paralysis during surgery
 Botulinum Toxin: used to inhibit ACH release, causes paralysis (decrease wrinkling)
Anticholinergic Drugs
 Also known as parasympatholytic, bind to muscarinic receptors and block ACH
Pharmacological Effects and Clinical Indications
 Cardiovascular System: block nerve activity, increase heart rate, alternative to beta drugs
 Respiratory System: produce bronchodilation, used in prep of anesthetics
 GI Tract: decrease all GI secretions
 Urinary: promote urinary retention
 CNS: small doses can be used in sleep aids
Adverse and Toxic Effects
 Produced by excessive parasympathetic blockage
 Dry mouth, visual disturbance, flushing and dryness of skin, fever, etc.
 Paralysis, coma and death can occur
 Poisonous quantities in many noneatable plant substances