How Do Cholinergic Agonists Work?

Cholinergic agonists are drugs that mimic the action of the neurotransmitter acetylcholine. The parasympathetic nervous system controls various organ and gland functions at rest, including digestion, defecation, lacrimation, salivation, and urination, and primarily uses acetylcholine as its main neurotransmitter.

Cholinergic agonists are of two types:

• Direct-acting cholinergic agonists: directly bind to cholinergic receptors.
• Indirect-acting cholinergic agonists: increase the availability of acetylcholine at the cholinergic receptors.

Cholinergic agonists act by enhancing the acetylcholine release following a signal sent from the brain.

Cholinergic agonists are mainly used to treat:

• Myasthenia Gravis
• Muscle weakness and fatigue associated with Lambert-Eaton Myasthenic Syndrome

Cholinergic agonists may cause the following side effects:

• Bone marrow suppression
• Sore throat
• Blurred vision
• Increased sweating and salivation
• Increased urinary frequency
• Rash
• Fever
• Dry mouth
• Gastric irritation
• Flushing
• Abnormal liver function tests
• Palpitation
• Irregular heart rate
• Dryness and scaling of the skin
• Nausea
• Diarrhea
• Abdominal cramping
• Low blood pressure

The information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of cholinergic agonists include:

• Guanidine
• Varenicline intranasal (pending FDA approval)
• Ambenonium (discontinued)
• Mytelase (discontinued)