Cholinomimetrics/ Cholinoreceptor Blockers Flashcards
Cholinomimetic drugs (direct acting):
Nicotinic: Nicotine
Muscarinic:
- Bethanechol
- methacholine
- pilocarpine
Choline Esters:
- Acetylcholine
- Bethanechol
- Carbachol
Plant Alkaloids:
- Muscarine
- Nicotine
- Pilocarpine
Other drugs:
- Cevimeline
- Varenicline
Mnemonic: ABC; MNoP; CV
Bethanechol
- Cholinomimetic drugs (direct acting) – Muscarinic Agonists
- Ileus and urinary retention
Methacholine
- Cholinomimetic drugs (direct acting) – Muscarinic Agonists
- Diagnostic of Bronchial hyperactivity; challenge test for asthma
Pilocarpine
- Cholinomimetic drugs (direct acting) – Muscarinic Agonists
- Glaucoma and xerostomia
Cholinoreceptors Blockers
Nicotinic (Nn):
- Hexamethonium
- Mecamylamine
Nicotinic (Nm):
- succinylcholine
- atracurium
- tubocurarine
Muscarinic:
- benzatropine
- atropine
- glycopyrrolate
- scopolamine
Mnemonics: He and Me SAT by the BAGS
Muscarinic receptor Antagonist/ Parasympatholytics:
Belladonna Alkaloids
- Hyoscyamine
- Atropine
- Scopolamine
Mnemonics: HAS
Semisynthetic and synthetic muscarinic receptor antagonists:
- Tropicamide
- Tolterodine and Tropium
- Tiotropium and Ipratropium
- Pirenzepine
- Dicyclomine
- Oxybutynin
- Glycopyrrolate
- Solifenacin
Mnemonics: TTTTIP DOGS
Muscarinic receptors antagonists Toxicity:
- Tachycardia
- Constipation
- Urinary retention
- Mydriasis with cycloplegia
- Decreased salivation, sweating and lacrimation
- Hyperthermia
- Bronchodilation: Rx Asthma
Muscarinic receptors antagonists Toxicity causing Meds:
- Antihistamines
- Cold meds
- Antidepressants
- Antipsychotics
Treatment of Toxicity: Physostigmine
Nicotinic Receptor Antagonists
Ganglion Blocking Agents:
- Trimethaphan
- Hexamethonium and Mecamylamine (Ganglion Blockers)
Nondepolarizing Neuromuscular blocking agents:
- Cisatracurium
- Pancuronium
- Rocuronium
- Atracurium
- Tubocurarine
- Vecuronium
Mnemonic: CPR AT VinnyS’
Depolarizing Neuromuscular blocking agents:
- Succinycholine
Pancuronium
Atracurium
Tubocurarine
Mivacurium
- Non-depolarizing (Competitive) Neuromuscular (Nm) Blockers
- Muscle relaxation in anesthesia; Endotracheal intubation
- Block acetylcholine –> paralysis of eyes and face, then progress to the limbs and respiratory muscles. No effect on cardiac or smooth muscles or consciousness
- Malignant hyperthermia; muscle rigidity, hypertension, acidosis, and hyperkalemia
Mivacurium: metabolized by plasma pseudocholine esterase and has a short duration of action
Antidote: Neostigmine
Succinylcholine
- Depolarizing (Noncompetitive) Neuromuscular (Nm) Blockers
2.
- Phase I: fasciculation which gets worse if neostigmine is given. Phase II: Desensitization (membrane is desensitized –> becomes unresponsive to Acetylcholine for some time
- Malignant hyperthermia; muscle rigidity, hypertension, acidosis, and hyperkalemia
Note: Succinylcholine is metabolized by plasma pseudocholine esterase and has a short duration of action
Benzodiazepines (Diazepam)
- Spasmolytic (Skeletal muscle relaxants)
2.
- Increases GABA actions at GABAa receptors –> reduce the tone of spinal motor neurons
- Malignant hyperthermia
Baclofen
- Spasmolytic (Skeletal muscle relaxants)
2.
- Direct agonist at GABAb receptors in the spinal cord
- Malignant hyperthermia
Note: As good as diazepam with less sedation
Dantrolene
- Spasmolytic (Skeletal muscle relaxants)
2
- Blocks Ca++ release from the sarcoplasmic reticulum –> decrease contractility on skeletal muscle
- Malignant hyperthermia
