Parasympathetic Drugs (Cholinomimetic) Flashcards
Direct Acting Cholinomimetics
A. Choline Esters (ABC,M)
* Acetylcholine (N,M)
* Bethanecol (M)
* Carbachol (N,M)
* Methacholine (N,M)
B. Cholinergic Alkaloids
* Pilocarpine (M) Pilocarpus jaborandi
* Muscarine (M)
* Nicotine (N) Nicotiana tabacum
* Lobeline (N) Lobelia inflata
* Arecoline (N,M) Areca catechu; betel nut,
nga nga!
* Varenicline (N) - smoking cessation
* Cevimeline (M3) - smoking cessation
Indirect-Acting Cholinomimetics
A. Short-Acting (Edrophonium)
* duration of action: 15-30 mins (average of 20 mins)
* chemical structure: Amino alcohol
* Edrophonium (Tensilon)
* Reversible inhibitor
B. Intermediate Acting (-tigmines)
* duration of action: 2-8 hours
* chemical structure: Carbamates / Carbamyl Esters
* Stigmine:
* Physostigmine
* Neostigmine
* Pyridostigmine
* Demecarium
* Amberonium
* reversible inhibitor
C. Long-acting
* chemical structure: Organophosphates
* Echothiopate (Medically useful)
* Isofluorophate
* Malathion
* Parathion
* Nerve gases (Sarin, Tabun, Soman)
* duration of exposure: <24-48 hours = potentially reversible
inhibition
* > or = 24-48 hours = irreversible
D. Drugs for Alzheimer’s Disease
* Rivastigmine
* Galantamine
* Donepezil
* Tacrine
No clinical use, primary transmitter at cholinergic nerve endings
Acetylcholine
Stimulate bladder or GI muscle without affecting heart rate or blood pressure; Enhance bladder tone; for post-op urinary retention
Bethanechol (Urecholine)
Used in ophthalmic surgery (Cataract Surgery & Iridectomy)
Carbachol (Miostat, Carbastat)
Diagnosis of Asthma
Methacholine
Alkaloid found in Mushroom; Poison
Muscarine
Chewing gums, transdermal patch used as Smoking deterrent
Nicotine
Second line drug for glaucoma; Treatment of Sjogren Syndrome
Pilocarpine - Tertiary amine
Synthetic muscarinic receptor agonist; treatment of sjogren syndrome
Cevimeline (Evoxac) - Selective activate of M3
Smoking deterrent
Varenicline - Partial agonist at N alpha 4, B2
Black Box warning of Varenicline
High risk of neuropsychiatric effects
- Mood Changes
- Erratic behavior
- Suicide ideation
Diagnosis of myasthenia gravis
Edrophonium
Treatment of myasthenia gravis
Carbamates (-stigmines)
Antidote of Atropine Poisoning; Anti-glaucoma
Physostigmine - natural, tertiary amine
Antidote for Tubocurarine Poisoning; Tx Myasthenia gravis & Post op ileus
Neostigmine, Pyridostigmine - Synthetic, polar
Treatment of Chronic glaucoma that does not responds to more conservative therapy
Echothiopate, Isoflurophate
Pesticide, treat head lice
Malathion
Nerve gases, chemical warfare agents
Soman, Sarin
Management of all stages of Alzheimers
Donepezil
Management of Mild to Moderate Alzheimers
Galantamine, Rivastigmine
Parasympathetic Toxicity
Diarrhea
Urination
Miosis
Bradycardia
Bronchoconstriction
Emesis
Lacrimation
Salivation
Sweating
Parasympathetic Toxicity
Diarrhea
Urination
Miosis
Bradycardia
Bronchoconstriction
Emesis
Lacrimation
Salivation
Sweating
