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Cholinergic Agonists
Module 2 Drug Classifications
| Question | Answer |
|---|---|
| What does the PNS (parasympathetic nervous system) do? | Rest and digest. Pupils constrict (miosis), induces salivation, and vasodilation which causes heart rate & BP to decrease. Bronchoconstriction occurs which increases respiratory secretions. Peristalsis (muscle contraction in the digestive tract). Bile is |
| What are cholinergic drugs? | Drugs that mimic/act like the PNS. They act on the same site as the neurotransmitter acetylcholine (ACh) |
| Use of cholinergic agonist agents across the Lifespan | Increased risk of adverse effects in children & older adults. Cholinergic dosages should be based on weight for infants. Caution adults against driving while taking these meds. There are no adequate studies on effects during pregnancy & lactationl; howe |
| What are the two types of cholinergic agents? | Direct-acting and Indirect acting cholinergic agonists. |
| What are direct-acting cholinergic agonists? | Occupy receptor sites for ACh on the membranes of the effector cells of the postganglionic cholinergic nerves, which causes increased stimulation of the cholinergic receptor. |
| What are indirect-acting cholinergic agonists? | React with the enzyme acetylcholinesterase (AChE) and prevents it from breaking down the ACh that was released from the nerve causing increased stimulation of the ACh receptor sites |
| What is acetylcholinesterase (AChE)? | An enzyme that catalyzes the breakdown of acetylcholine |
| What are direct-acting cholinergic agonists? | Bethanechol, Carbachol, Cevimeline, and Pilocarpine |
| What is Bethanechol used for? | It is the prototype for direct-acting cholinergic agonists and used for urinary retention & salivation production. |
| What is Carbachol used for? | Used for glaucoma (pressure in the eye) |
| What are Cevimeline & Pilocarpine used for? | Used for dry mouth |
| What are the indications for DA cholinergic agonists? | Urinary retention, treat dry mouth, and induce miosis |
| What are the contraindications for DA cholinergic agonists? | ◦ Any condition that would be exacerbated by parasympathetic effects—bradycardia, hypotension ◦ Known allergy, peptic ulcer disease ◦ Intestinal obstruction or recent GI surgery ◦ Asthma ◦ Bladder obstruction ◦ Epilepsy and parkinsonism Caution in P |
| What are the adverse effects for DA cholinergic agonists? | ◦ Nausea, vomiting, cramps, diarrhea, increase salivation, and involuntary defecation ◦ Bradycardia, heart block, hypotension ◦ Urinary urgency ◦ Flushing or increased sweating |
| What is a drug-drug interaction for DA cholinergic agonists? | Acetylcholinesterase (AChE) inhibitors |
| Define Myasthenia Gravis | ◦ Chronic muscular disease caused by a defect in neuromuscular transmission ◦ Autoimmune disease; patients make antibodies to ACh receptors, causing gradual destruction of them |
| What drug classification is used to treat Myasthenia Gravis & Alzheimer's disease? | Indirect-acting cholinergic agonists are used to treat these two diseases. |
| What indirect-acting cholinergic agonists treat Myasthenia Gravis? | Pyridostigmine, Neostigmine, and Edrophonium |
| What indirect-acting cholinergic agonists treat and slow progression of Alzheimer's disease? | Donepezil, Galantamine, and Rivastigmine |
| Which indirect-acting cholinergic drug is most common and has a long path life to treat Alzheimer's disease? | Donepezil |
| What is Alzheimer's disease? | A progressive disorder involving neural degeneration in the cortex. Leads to a marked loss of memory and the ability to carry on activities of daily living. There is a progressive loss of ACh-producing neurons and their target neurons. |
| What is the action for Indirect-Acting Cholinergic Agonists? | Blocks ACh at the synaptic cleft, which allows the accumulation of ACh released from the nerve endings and leads to increased and prolonged stimulation of ACh. |
| What are the indications for IA cholinergic Agonists? | Myasthenia gravis & Alzheimer's disease |
| What are the contraindications for IA cholinergic agonists? | ◦ Allergy ◦ Bradycardia ◦ Intestinal or urinary tract obstruction ◦ Pregnancy and lactation |
| What should you be cautious for when administering IA cholinergic agonists? | ◦ Any condition that could be exacerbated by cholinergic stimulation. ◦ Asthma, coronary disease, peptic ulcer, arrhythmias, epilepsy, or parkinsonism. |
| What are the adverse effects of IA cholinergic agonists? | ◦ Bradycardia ◦ Hypotension ◦ Increased GI secretions and activity ◦ Increased bladder tone ◦ Relaxation of GI and genitourinary sphincters ◦ Bronchoconstriction ◦ Pupil constriction |
| What are drug-drug interactions for IA cholinergic agonists? | NSAIDs and cholinergic drugs |
| What is the most common drug used to treat Myasthenia Gravis? | Pyridostigmine. Has a longer duration of action. |
| Which IA cholinergic drug increases survival after exposure to nerve gas? | Pyridostigmine |
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jmajalca
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