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41 Cards in this Set
- Front
- Back
Direct Acting Drugs? |
Acetylcholine, Bethanechol, Carbachol,
Cevimeline, Pilocarpine, Muscarine, Methacholine, Nicotine, Varenicline, Succinylcholine |
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Indirect Acting Drugs? |
Ambenonium, Demecarium, Donepezil,
Edrophonium, Neostigmine, Parathion, Malathion, Sarin, Physostigmine, Pyridostigmine, Rivastigmine, Galantamine, Tacrine |
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What Are the 6 Fates of Acetylcholine? |
1. Synthesis (Transport of Choline Inhibited by Hemicholinium) 2. Uptake into Storage Vesicles (Prevents Degradation) 3. Release (Caused by Spider Venom, Inhibited by BoTox) 4. Binding to Postsynaptic Receptor (Activate) 5. Degradation by AchE in Synaptic Cleft |
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General MOA for Cholinergic Agonists? |
Direct:
Indirect: Inhibit AchE |
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What Are Some Choline Esters? |
Acetylcholine, Bethanechol, Carbachol, Methacholine |
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What Are Some Natural Alkaloids? |
Muscarine, Pilocarpine, Cevimeline
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In the Sympathetic Innervation of the Adrenal Medulla, The____Neurons release the NT___, which binds to the____receptors on the Adrenal Medulla, release the NTs____and____into the blood and they bind to____receptors in the effector organs. |
Preganglionic Ach Nicotinic NP and EP Adrenergic |
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In the Sympathetic Pathway, The____Neurons release the NT___, which binds to the____receptors, activate___Neurons that releases the NT____, which binds to the____receptors in the effector organs. |
Preganglionic Ach Nictotinic Postganglionic NP Adrenergic |
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In the Parasympathetic Pathway, The____Neurons release the NT___, which binds to the____receptors, activate___Neurons that releases the NT____, which binds to the____receptors in the effector organs. |
Preganglionic
Ach Nicotinic Postganglionic Ach Muscarinic |
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In the Somatic Pathway, there are___ganglia. Instead___is directly released into the blood and binds to the___receptors in the___of Skeletal Muscle. |
No Ach Nicotinic NMJ |
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What Are the Most Common Effects of Cholinergic Agonists? |
Diarrhea Miosis Urinary Urgency Diaphoresis Nausea |
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Besides Nicotine, What is the Other Drug Specific for Only the Nicotinic Receptor? Which Receptor Do the Other Drugs Bind? |
Succinylcholine Muscarinic |
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What Are the General Uses and Contradictions of Muscarinic Agonists? |
Contraindications: asthma, ulcer, GI/urinary obstruction,Parkinson's, some CV diseases (AV block, bradycardia), surgery, seizures |
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Describe Acetylcholine, be sure to include MOA and Physiological Effects. |
NT that binds to Nicotinic and Muscarinic Rec. Pharmacological Effects: Cardiac: Muscle: -Excitatory neurotransmitter CNS: -Arousal,reward, neuromodulatory actions -Damage to cholinergic neurons in CNS is associated with Alzheimer's disease Gastro-intestinal: Stimulates intestinal secretions and motility |
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What Are the Theraputic Uses and Adverse Effects of Acetylcholine? |
It's rapidly degraded by cholinesterases and so has no real therapuetic uses other than Intraocular use during cataract surgey for rapid Miosis. It has no significant Clinical Adverse Effects. |
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Describe Muscarine, be sure to include MOA and Physiological Effects. |
Has no medical uses due to high toxicity. Pharmacological Effects: Salivation, Miosis, Urination/defecation, Sweating, Bronchial constriction/ secretion, Bradycardia, Nausea/ vomiting, Headache, Hypotension, Shock |
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What Are the Systemic and Localized Adverse Effects of Muscarinic Cholinoceptor Stimulation? |
Systemic: Sweating, Salivation, Flushing, Decreased blood pressure, Nausea, Abdominal pain, Diarrhea, Bronchospasm Localized: Visual difficulty on far vision or in dim light, Reddening, stinging and burning of the conjunctiva, Postoperative iritis, Cataract (8-10% of patients, with long-term use), Retinal detachment (with long-term use) |
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Describe Metacholine and it's MOA, PK and Clinical Use. |
MOA:
-Magnitude of response is unpredictable PK:
Clinical use:
-Bronchial reactivity testing |
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What Are the Adverse Effects and Contradictions of Methacholine? |
Adverse effects:
Contraindications:
-Recent heart attack -Stroke -Aortic aneurysm -Uncontrolled hypertension |
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Describe Bethanechol including its MOA, PK, PE and TE. |
MOA:
PK:
-Expulsion of Urine Pharmacological effects:
TE:
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Describe Carbachol including it's MOA, PK and Systemic Effects. |
MOA:
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Describe Carbachol and it's PE, TE and AE. |
Pharmacological effects:
TE:
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Describe Pilocarpine and it's MOA and PK. |
MOA:
-Less potent than acetylcholine PK:
-Stimulates profuse sweating and salivation
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What's the Theraputic Use of Pilocarpine? |
Therapeutic Uses:
-Rapid miosis and contraction of cilliary muscle -Drug of choice for immediate drop in intraocular pressure
-“sweat test”-Chloride & sodium levels |
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Describe Cervimeline and It's Key Theraputic Use. |
Selective Muscarinic (M1 & M3) agonist
-Sometimes in combination with pilocarpine |
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Describe Nicotine and it's Adverse Effects. |
Has no therapeutic indications except for smoking cessation
-dose dependent,can be fatal
-tolerance develops to many effects -Cardio vascular abnormalities (1/3 of CV fatalities related to nicotine)
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Describe Succinylcholine including MOA, PK and Clinical Use. |
MOA:
PK:
Clinical uses:
-Brief excitement> widespread fasciculations> flaccid paralysis
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What Are the AE of Succinylcholine? |
Adverse effects:
-Overcome with Dantrolene
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Describe Varenicline (Chantix) and It's MOA, PK, Clinical Uses and AE. |
MOA:
PK:
Clinicaluses:
Adverse effects:
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What is the Principle Difference Between Direct and Indirect Acting Cholinergic Drugs? |
The direct acting will always cause and effect where the indirect will only have an effect if there is a background parasympathetic tone of target. |
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Describe Cholinergic Crisis, It's Common Symptoms and the Best Treatment. |
Acetylcholinesterase inhibitors increase circulating Ach, which can lead to cholinergic crisis. Symptoms:
Atropine is the drug of choice for combating cholinergic crisis. |
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Describe Physostigmine and it's MOA, PK, PE and AE. |
MOA:
PK:
-Intermediate-acting Pharmacological effect:
-Convulsions,bradycardia, decrease cardiac output -Accumulation of ACh in NMJ leads to skeletal muscle paralysis |
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Describe Neostigmine and it's MOA, PK, TE and AE. |
MOA:
PK:
Therapeutic effects:
Adverse effects:
|
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What is Myasthenia Gravis and Which Drugs Would You Use to Treat it? |
It's an autoimmune disease caused by antibodies attacking the nicotinic receptors in the NMJ, leading to muscle weakness. Neostigmine is more potent, however Pyridostigmine has a longer duration of action. (3-4 hours). |
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What is Demarcium and What Is It Used For? |
It's similar to Neostigmine in it's structure, MOA and AE. Used in the treatment of chronic glaucoma Used in diagnosis and treatment of accommodative esotropia |
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Describe Edrophonium and it's TE and AE. |
Similar to Neostigmine but:
TE:
AE:
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Which Drugs Are Commonly Used to Treat AD, Dementia or PD? |
AchE Inhibitors such as Tacrine, Donepezil, Rivastigmine and Galantamine. |
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Describe Rivastigmine and It's AE? |
AE: Diarrhea, Nausea, Vomiting, Cramps, Anorexia, Vivid Dreams. |
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What is Aging and What Drug Can Be Used Against It? |
Aging is when strong covalent bonds between inhibitor and enzyme or loss of a functional group reders the complex irreversible. Pralidoxime given before aging can reverse Organophosphate (Insecticides) Poisoning. |
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Describe Malthion. |
Most commonly used organophosphate insecticide in the US. Rapidly degraded by exposure to sunlight, but trace levels found in water run off Linked to increased ADHD prevalence Used in the treatment of head lice |
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Describe Parathion? |
Similar to malathion, but only used as insecticide Pharmacological effects: -Parasympathetic effects -Muscle paralysis Coma/death |