Cholinergic Drugs Flashcards
Individual direct-acting agents:
Approved for intraocular use during surgery and causes miosis (reduction in pupil size)
Acetylcholine
Individual direct-acting agents:
- Selective mAChR agonist that primarily affects the urinary and GU tracts
- Can be used to treat patients with urinary retention and heartburn
- Little cardiovascular stimulation
- May produce urinary tract infection if sphincter fails to relax
Bethanechol
Individual direct-acting agents:
•Nonspecific cholinergic agonist that is used for the treatment of glaucoma or to produce miosis during surgery or ophthalmic examination
Carbachol
Individual direct-acting agents:
•Oral tablet used to treat dry mouth (xerostomia) in patients with Sjögren syndrome
Cevimeline
Individual direct-acting agents:
- Approved for xerostomia treatment in patients with Sjögren syndrome or head and neck cancer treatment related xerostomia (PO), miosis during ophthalmic procedures (topical), and for glaucoma (topical)
- Pure mAChR agonist
Pilocarpine
- FDA approved for smoking cessation ***
- Partial agonist that binds with high affinity and selectivity to α4β2 nAChRs (NN)
- MOA: stimulation and subsequent moderate, sustained release of mesolimbic dopamine are thought to reduce craving and withdrawal symptoms associated with smoking cessation
Varenicline (Chantix)
What are some adverse effects to Varenicline (Chantix)?
- Nausea is most common adverse effect;
- serious adverse effects include neuropsychiatric symptoms, including changes in behavior, agitation, depressed mood, suicidal ideation, and attempted and completed suicide
Anticholinergic agents:
Drugs used for motion sickness
Scopolamine
Anticholinergic agents:
Drugs for gastrointestinal disorders
- Atropine
- Dicyclomine
- Glycopyrrolate
- Hyoscyamine
Anticholinergic agents:
Drugs used in ophthalmology
- Atropine
- Cyclopentolate
- Homatropine
- Scopolamine
- Tropicamide
Anticholinergic agents:
Drugs used for respiratory disorders
- Ipratropium
* Tiotropium
Anticholinergic agents:
Drugs used for urinary disorders
- Darifenacin
- Oxybutynin
- Solifenacin
- Tolterodine
- Trospium
Anticholinergic agents:
Drugs used for cholinergic poisoning
Atropine (+ pralidoxime)
Anticholinergic agents:
Drugs used for movement disorders
- Benztropine
- Biperiden
- Orphenadrine
- Procyclidine
- Trihexyphenidyl
Anticholinergics for CNS disorders:
What drugs are used for Parkinson disease?
- mAChR antagonists can reduce tremors
- Not as effective as standard dopaminergic therapy (often used in combination)
- Tertiary amines benztropine, trihexyphenidyl, and procyclidine
Anticholinergics for CNS disorders:
What drugs are used for motion sickness?
Scopolamine – PO, injection, transdermal
Anticholinergics for CNS disorders:
What drugs are used for anesthesia?
- Atropine is given to block responses to vagal reflexes induced by surgical manipulation of visceral organs
- Atropine or glycopyrrolate is paired with the cholinesterase inhibitor neostigmine to block its parasympathetic effects
List of Direct-acting cholinomimetics
- Acetylcholine
- Bethanechol
- Carbachol
- Cevimeline
- Methacholine
- Pilocarpine
- Varenicline (Chantix)
List of Cholinesterase inhibitors
- Ambenonium
- Donepezil
- Echothiophate
- Edrophonium
- Galantamine
- Neostigmine
- Physostigmine
- Pyridostigmine
- Rivastigmine
- Tacrine
List of Cholinesterase regenerator
Pralidoxime
List of Ganglion blockers
Mecamylamine
ACh Receptors: M1
- Location
- Structural features
- Mechanism
- Location: Nerves
- Structural features: GPCR, Gq/11
- Mechanism: IP3, DAG cascade
ACh Receptors: M2
- Location
- Structural features
- Mechanism
- Location: Heart, nerves, smooth muscle
- Structural features: GPCR, Gi/o
- Mechanism: Inhibition of cAMP production, activation of K+ channels
ACh Receptors: M3
- Location
- Structural features
- Mechanism
- Location: Glands, smooth muscle, endothelium
- Structural features: GPCR, Gq/11
- Mechanism: IP3, DAG cascade
ACh Receptors: M4
- Location
- Structural features
- Mechanism
- Location: CNS
- Structural features: GPCR, Gi/o
- Mechanism: Inhibition of cAMP production
ACh Receptors: M5
- Location
- Structural features
- Mechanism
- Location: CNS
- Structural features: GPCR, Gq/11
- Mechanism: IP3, DAG cascade
ACh Receptors: Nm
- Location
- Structural features
- Mechanism
- Location: Skeletal muscle neuromuscular junction
- Structural features: Pentamer, α2β8 and y/ε
- Mechanism: Na+, K+ depolarizing ion channel
ACh Receptors: Nn
- Location
- Structural features
- Mechanism
- Location: Postganglionic cell body, dendrites, CNS
- Structural features: α and β only. Examples: (α4)2(β4)3; (α7)5
- Mechanism: Na+, K+ depolarizing ion channel
- Approved for intraocular use during surgery and causes miosis (reduction in pupil size)
- Rarely given systemically
Acetylcholine
- Administered by inhalation for the diagnosis of bronchial airway hyperreactivity in patients
who do not have clinically apparent asthma - Rarely used due to need for emergency resuscitation equipment, oxygen, and medications
to treat severe bronchospasm (e.g., B2 adrenergic receptor agonists)
Methacholine
- Can be used to treat patients with urinary retention and heartburn
- Selective mAChR agonist
- Little cardiovascular stimulation
- May produce urinary tract infection if sphincter fails to relax
Bethanechol
Nonspecific cholinergic agonist that is used for the treatment of glaucoma or to produce mitosis during surgery or ophthalmic examination
Carbachol
- Oral tablet used to treat dry mouth (xerostomia) in patients with Sjögren’s syndrome
- Metabolized via P450 pathways and eliminated in urine
Cevimeline
- Approved for xerostomia treatment in patients with Sjögren’s syndrome or head and neck cancer treatment related xerostomia (PO), miosis during ophthalmic procedures (topical), and for glaucoma (topical)
- Pure mAChR agonist
Pilocarpine
- FDA approved for smoking cessation
- Partial agonist that binds with high affinity and selectivity to α4β2 nicotinic acetylcholine
receptors located in the brain to stimulate receptor-mediated activity, but at a substantially lower level than nicotine - Stimulation and subsequent moderate, sustained release of mesolimbic dopamine are
thought to reduce craving and withdrawal symptoms associated with smoking cessation (reward pathway) - Greater than 90% eliminated in urine as unchanged drug
- Nausea is most common adverse effect; serious adverse effects include neuropsychiatric
symptoms, including changes in behavior, agitation, depressed mood, suicidal ideation, and attempted and completed suicide - Treatment comes with the following warning: If patients, their families, or caregivers notice agitation, depressed mood, or changes in behavior that are not typical for the patient or if the patient has suicidal thoughts or actions, the patient should stop taking it and contact their healthcare professional.
Varenicline
