Drugs Mentioned in Lecture Flashcards
d-Tubocurarine
NOT ON STUDY GUIDE BUT ON LECTURES
Class: Nicotinic Antagonist - Nondepolarizing Neuromuscular Blocker
Indications: Previously used for paralysis during surgery.
Contradictions: Should never be used a Toxin
MoA: Competes with ACh at nicotinic cholinergic receptors, notably at the neuromuscular junction. Prevents depolarization of skeletal muscle.
Adverse Effects: Tachycardia, causes hypotension and bronchospasms due to histamine release.
Carbachol
Class: Direct Cholinergic Agonist - Choline Ester
Indications: Induce miosis, topical application.
Contrindications: NONE
MoA: Activates ocular M3 cholinergic receptors, not metabolized by corneal AChE so can be used topically.
Adverse Effects: Overdose can lead to cholinergic toxicity
Methacholine
Class: Direct Cholinergic Agonist - Choline Ester
Indications: Diagnostic test for asthma.
Contrindications: None
MoA: Activates bronchial M2 & M3 receptors, causing bronchoconstriction in asthmatics.
Adverse Effects: Overdose can lead to cholinergic toxicity
Bethanocol
MUSCURINIC SPECIFIC
Class: Direct Cholinergic Agonist - Choline Ester
Indications: Used to treat urinary retention.
Contraindication: NONE
MoA: Activates M3 cholinergic receptors of detrusor muscle, causing contraction.
Adverse Effects: Overdose can lead to cholinergic toxicity
Muscarine
Class: Direct Cholinergic Agonist - Plant Alkaloid
indication: No known medical uses.
Contraindications: No known medical uses.
MoA:Specific agonist of muscarinic cholinergic receptors.
Adverse Effects: Cholinergic toxicity.
Pilocarpine
Class: Direct Cholinergic Agonist - Plant Alkaloid
Indications: Treating glaucoma or xerostomia, topical or oral.
Contraindications: Only works for open angle glaucoma.
MoA: Cholinergic agonist, higher affinity for muscarinic receptors. Activates M3 receptors of ciliary muscles, causing them to contract and pull open drainage network. Activates M3 receptors of salivary glands.
Adverse Effects: Overdose can lead to cholinergic toxicity
Cevimeline(Evoxac)
Class: Direct Cholinergic Agonist - Synthetic Drug
Indications: Treating xerostomia associated with radiation of head & neck or Sjogren syndrome.
Contraindications: None
MoA: Cholinergic agonist that binds to M3 cholinergic receptors of salivary glands. Adverse effects due to M3 activation in sweat glands and eyes.
Adverse Effect: Sweating, visual disturbances due to miosis.
Edrophonium(Tennsilon)
Class: Indirect Cholinergic Agonist - Reversible AChE Inhibitor
Indication: Diagnostic test for myasthenia gravis.
Contraindications: Does not treat MG, only works at low doses.
MoA: Competitive AChE inhibitor increases active ACh in the neuromuscular junction. In Myasthenia Gravis low # of muscular receptors, low doses will improve muscle function.
Physostigamine(Mestinon)
Class: Indirect Cholinergic Agonist - Reversible AChE Inhibitor
Indications: Treatment of anticholinergic toxicity.
Contraindications: NONE GIVEN
MoA: Competitive AChE inhibitor which increases active Ach in synapses, reversing the effects of anticholinergics. Well-absorbed by gut and crosses BBB.
Adverse Effects: None Given
Neostigmine(Prostigmin)
Class: Indirect Cholinergic Agonist - Reversible AChE Inhibitor
Indications: Long term treatment of myasthenia gravis.
Contraindications: None Given
MoA: Competitive AChE inhibitor, very slowly hydrolyzed by AChE, increasing ACh in synapse. Does not cross BBB.
Adverse Reaction: None Given
Pyridostigmine
Not on study guide but in lecture
Class: Indirect Cholinergic Agonist - Reversible AChE Inhibitor
Indication: Long term treatment of myasthenia gravis.
Contraindication: None Given
MoA: Competitive AChE inhibitor, very slowly hydrolyzed by AChE, increasing ACh in synapse. Does not cross BBB.
Adverse Effects: Lower incidence of side effects than neostigmine.
Organophosphates
Not on study Guide but in lecture
Class: Indirect Cholinergic Agonist - Quasi-reversible AChE Inhibitor
Indications: Treatment of head lice, bioterrorism.
MoA: Binds up AChE, reversible for a while by pralidoxime, but eventually becomes irreversible (aging). Significantly increases ACh in synapse, especially nicotinic sites, causes muscle paralysis by over-depolarization. Lipophilic so it can cross skin and mucous membranes.
Adverse Effects: Very toxic, causes muscle paralysis and respiratory paralysis. To treat toxicity, give cardiopulmonary support, give atropine (ACh antagonist), and give pralidoxime (2-PAM), which can compete for AChE binding.
Sildenafil
Class: Indirect Cholinergic Agonist - Phosphodiesterase Inhibitor
Indications: Erection
Contraindications: None given
MoA: Inhibits type-5 phosphodiesterase, which degrades cGMP, increasing cGMP. cGMP promotes vasodilation in response to ACh. Specific for arterioles leading to erectile tissue.
Adverse Effects: None given
Donepezil(Glantamine and rivastigmine)
*NOT ON STUDY GUIDE BUT ON LECTURES
Class: Indirect Cholinergic Agonist - Reversible AChE Inhibitor
Indications: Alzheimer’s disease.
Contraindications: NONE
MoA: Competitive AChE inhibitor, crosses the BBB so it increases activity of cholinergic receptors in the brain. Selective for the hippocampus and frontal cortex, supposedly improves memory.
Adverse Effects: None given
Atropine
Class: Muscarinic Antagonist - Belladonna Alkaloid
Indication: Mydriasis and blocking accomodation for eye exams. Treatment of bradycardia (IV). Reduces GI spasms and diarrhea. Support for OPP poisoning.
Contraindications: Few uses at clinical doses, synthetic drugs are usually better at various indications.
MoA: Competes with ACh at muscarinic cholinergic receptors, well-absorbed by gut and crosses BBB, so systemic effects. Inhibits actions of PNS, notably in the eyes, heart, and gut.
Adverse Effects: Elevated temperature, decreased sweating, confusion, delirium, flushed face, tachycardia, decreased secretions, dry eyes, thirsty.
Pralidoxime(2-PAM)
Class: AChE Reactivator
Indications: Treatment of organophosphate poisoning.
Contraindications: NONE GIVEN
MoA: Displaces organophosphates from AChE, freeing up AChE and decreasing ACh in the synapse, reversing the muscle paralysis.
Adverse Effects: NONE given
Tadalafil (Cialis)
Not in Study guide but given in lecture
Class: Indirect Cholinergic Agonist - Phosphodiesterase Inhibitor
Indications: Erection
Contrindications: None Given
MoA: Inhibits type-5 phosphodiesterase, which degrades cGMP, increasing cGMP. cGMP promotes vasodilation in response to ACh. Specific for arterioles leading to erectile tissue.
Adverse Effects: None Given
Vardenafil(Levitra)
Class: Indirect Cholinergic Agonist - Phosphodiesterase Inhibitor
Indications: Erection
Contrindications: None Given
MoA: Inhibits type-5 phosphodiesterase, which degrades cGMP, increasing cGMP. cGMP promotes vasodilation in response to ACh. Specific for arterioles leading to erectile tissue.
Adverse Effects: None Given
Scopolamine
Class: Muscarinic Antagonist - Belladonna Alkaloid
Indications: Treats motion sickness.
Contraindications: None Given
MoA: Competes with ACh at M1 cholinergic receptors in the brain, specifically from transmission from the vestibular apparatus (ears) to the vomiting center (brainstem). Administered transdermally, can cross skin and BBB.
Adverse Effects: Drowsiness or memory loss.
TRANSDERMAL PATCH FOR MOTION SICKNESS
Hyoscyamine
Not on Study Guide but mentioned in lecture
Class: Muscarinic Antagonist - Belladonna Alkaloid
Indications: Reduces spasms caused by disorders of the gut and bladder.
Contraindications: None Given
MoA: Competes with ACh at muscarinic cholinergic receptors, well-absorbed by gut and crosses BBB, so systemic effects. Inhibits actions of PNS, notably in gut and urinary tract.
Adverse Effects: Elevated temperature, decreased sweating, confusion, delirium, flushed face, tachycardia, decreased secretions, dry eyes, thirsty.
Ipratropium(Atrovent)
Class: Muscarinic Antagonist - Synthetic
Indications: Treatment of asthma and COPD.
Contraindications: None Given
MoA: Competes with ACh at M3 cholinergic receptors in the lungs, reducing PNS bronchoconstriction. Inhaled and poorly absorbed by the lungs, so effects are local.
Adverse Effects: Minimal side effects.
Tolterodine and Oxybutynin
Class: Muscarinic Antagonist - Synthetic
Indications: Treatment of overactive bladder.
Contraindications: None Given
MoA: Competes with ACh at M3 cholinergic receptors in the bladder, preventing detrusor contractions and spasms.
Adverse Effects: None Given
Tolterodine and Oxybutynin
Class: Muscarinic Antagonist - Synthetic
Indications: Treatment of overactive bladder.
Contraindications: None Given
MoA: Competes with ACh at M3 cholinergic receptors in the bladder, preventing detrusor contractions and spasms.
Adverse Effects: None Given