Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
66 Cards in this Set
- Front
- Back
|
Actions of mAch agonists
|
vasodilation (NO), constriction of bronchi and increased mucous, miosis, contracts ciliary muscle, thin and watery salivation, tearing, diphoresis, increased GI motility and relaxation of sphincters, contraction of bladder detrusor and relaxion of sphincter (makes you pee), bradycardia and decrease ionotropy
|
|
|
Symptoms of muscarine poisoning
|
Salivation and lacrimation, nausea and vomiting, headache, visual disturbances, bronchospasm, hypotension and bradycardia, shock....reverse with atropine
|
|
|
Bethanachol
|
Direct mAchR agonist choline ester
-Used postpartum or post-op to reduce bladder distension -Used to treat urinary retention -Used to treat neurogenic ileus -Used to promote salivation resistant to AchE and no nicotinic activity |
|
|
Carbachol
|
Direct mAchR agonist choline ester
-2nd or 3rd line for wide-angle glaucoma -resistant to AchE -significant nicotinic activity |
|
|
Methacholine
|
Direct mAchR agonist choline ester; test for asthmatic hyperreactivity; use very carefully because has strong cardiovascular effects
|
|
|
Pilocarpine
|
Direct mAchR agonist muscarinic
-used as a miotic agent (lasts 1 day) -used for wide angle glaucoma -used for narrow-angle glaucoma with physostigmine -used for xerostomia |
|
|
Contraindications for mAchR agonists
|
-Asthmatics (cause bronchoconstriction)
-urinary obstruction (stimulates urination) -Peptic ulcer disease (stimulates gastric secretions and motility) |
|
|
Atropine
|
mAchR antagonist tertiary amine
-produces ong-lasting mydriasis -Used to reverse muscarinic poisoning -Used to reverse anti-AchE poisoning (organophosphate) -used with diphenoxylate (mild opioid agonist) as antidiarrheal (Lomotil) |
|
|
Tropicamide
|
mAchR antagonist tertiary amine
-rapid & short-acting mydriatic agent |
|
|
Scopolamine
|
mAchR antagonist tertiary amine
-used to treat motion sickness |
|
|
Oxybutinin
|
-mostly M3 mAchR antagonist tertiary amine
-used to treat overactive bladder with incontinence and/or increased frequency and urgency -CI for narrow-angle glaucoma |
|
|
Propantheline
|
mAchR antagonist quaternary amine
-used to treat GI disturbances, lasting 6 hours with few side effects -lesser alternative for peptic ulcer disease -used to stop excessive sweating |
|
|
Ipratroprium and Tiotroprium
|
mAchR antagonists quaternary aminea
-Used as bronchodilators for COPD -Tiotroprium is longer acting |
|
|
Side effects of anti-muscarinics
|
-Xerostomia
-blurred vision from mydriasis and cyclopegia -Anhidrosis leading to cutaneous vasodilation (hot, flushed skin) -constipation -difficulty urinating -tachycardia -tertiary amines have CNS effects of confusion, sedation, and delirium |
|
|
Classes of drugs that have anti-muscarinic effects
|
Anti-histamines (diphenhydramine)
-Tricyclic anti-depressants; -Phenothiazine antipsychotics (chlorpromazine) -Neuromuscular blockers (gallamine) |
|
|
Acebutolol
|
-Selective B1 antag
-Low plasma binding -short acting, take 4x/day -Some membrane stabilizing activity, can be used as anti-arrhytmic -used for angina, HPTN, hyperthyroidism |
|
|
Atenolol
|
-Selective B1 antag
-Low plasma binding -taken 1x day -#1 drug for HPTN; also used for angina and Hyperthyroidism |
|
|
Esmolol
|
-Selectve B1 antag
-Used IV as acute anti-arrhytmic |
|
|
Metoprolol
|
-Selective B1 antag
-Some CNS effects -Take 4x/day -Used for HPTN, Angina, Hyperthyroidism |
|
|
Naldolol
|
-Non-selective B antag
-Long lasting, take 1x/day -Used for HPTN, angina, and hyperthyroidism |
|
|
Pindolol
|
-Non-selective B antag
-Safer than most B blockers for CHF patients because has some intrinsic sympathetic activity -4x/day -Has some Membrane Stabilizing Activity -Used for HPTN, Angina, and Hyperthyroidism |
|
|
Propanolol
|
-Non-selective B antag
-Has greatest CNS effects because lipid soluble (sedation and depression) -Greater than 90% is bound to plasma proteins -metabolized by P450 -Given both oral and IV -Has very high membrane stabilizing activity (causes mouth to get numb) -Used as anti-arrhythmicm HPTN, Angina, and hyperthyroidism |
|
|
Timolol
|
Non-selective B antag
-Taken 4x/day -#1 for glaucoma, also used for HPTN, Angina, and Hyperthyroidism |
|
|
Sotalol
|
Non-selective B antag
-Used as anti-arrhytmic, HPTN, Angina, and hyperthyroidism |
|
|
Labetalol and Carvedilol
|
-Non selective Beta blockers and selective a1 blockers
-#1 ER HPTN and Per. Vas. Dis. |
|
|
Edrophonium
|
Quaternary amine, competitive inhibitor of AchE
-Given IV to test for myasthenia gravis; has short duration of action and will transiently improve strength |
|
|
Physostigmine
|
-Tertiary amine Carbamate, reversible cholinesterase inhibitor; used for wide angle glaucoma
-adverse effect=causes cataracts |
|
|
Neostigmine
|
-Quaternary amine Carbamate, reversible cholinesterase inhibitor
-Short duration of action (30 min. to 2 hours) -Standard treatment for myasthenia gravis -Used for post-surgical reversal of neuro-muscular blockade -Drug of choice for paralytic loss of tone in GI tract and bladder |
|
|
Pyridostigmine
|
-Quaternary amine Carbamate, reversible cholinesterase inhibitor
-Drug of choice for myasthenia gravis because has longer duration of action (3-6 hours) than neostigmine -Used as pretreatment to reduce mortality on exposure to nerve gas |
|
|
Ambenonium
|
-Carbamate, reversible cholinesterase inhibitor
-Lasts 4-8 hours, alternative for myasthenia gravis |
|
|
Demacarium
|
-reversible cholinesterase inhibitor
-alternative for myasthenia gravis |
|
|
Toxicity of local exposure of carbamates
|
1. Miosis if toxic dose exposed to eye
2. Tigthness in chest, increased bronchial secretion, wheezing 3. Localized sweating 4. Localized muscle fasciulation |
|
|
Toxicity of ingestion of carbamates
|
1. Muscarinic-related responses: Vomiting and diarrhea, profuse salivation, tearing, blurred vision, wheezing from bronchoconstriction and congestion; involuntary defecation and urination
2. Direct effects of increased Ach: Bradycardia, increased sweating 3. Hypotension from ganglionic blockade 4. CNS effects: generalized convulsions, coma; less severe for quaternary amines 5. Muscle effects: Generalized weakness, paralysis, and cessation of respiration (more severe for quaternary amines) |
|
|
Echothiphate
|
Only clinically useful organophosphate cholinesterase inhibitor used in glaucoma
|
|
|
Malthion
|
Organophosphate insecticide
|
|
|
Parathion
|
Organophosphate insecticide responsible for most cases of poisoning and death, pro drug metabilized by mixed-function oxygenases to paraoxon
|
|
|
Sarin gas
|
organophosphate poision
|
|
|
Donepezil
|
Orally active, CNS cholinesterase inhibitor used for Alzheimers
-No hepatotoxicty (unlike tacrine) -Once-a-day dosing |
|
|
Rivastigmine
|
Carbamate anti-cholinesterase used for Alzheimer's disease, twice a day dosing
|
|
|
Galantamine
|
Both a mild cholinesterase inhiviotr and potent allosteric enhancer of CNS nicotonic receptors; used to improve cognitive function and delay progression of Alzheimers; once-a-day dosing
|
|
|
Treatment of carbamate poisioning
|
Atropine; ventilation if have respiratory distress; diazepam to reduce convulsions
|
|
|
Treatment of organophosphate poisoning
|
-Pralidoxime (PAM), needs to be given before AchE ages
-Carbamates -Diazapam to stop convulsions -Supportive measures to stop respiratory distress |
|
|
Symptoms of acute nicotine toxicity
|
Mild: vomiting, transient increase in salivation, cold sweat, disturbed vision, dizziness, muscular weakness
Severe: tachycardia and arrhythmia, respiratory distress, convulsion, death |
|
|
Mecamylamine
|
Non-depolarizing, nAchR ganglionic blocker; Improves GI absorption and Tourette's Syndrome
|
|
|
Curare
|
Non-depolarizing, nAchR ganglionic blocker; once used as a neuromuscular blocker
|
|
|
Effect of ganglionic blockade
|
1. Vasodilation and hypotension (blocks SNS)
2. Venodilation and reduced venous return/cardiac output (blocks SNS) 3. Mydriasis (blocks PSNS) 4. Cyclopegia (blocks PSNS effect on ciliary muscle) 5. Decreased tone and motility of GI tract, constipation (blocks PSNS) 6. Urinary retention (blocks PSNS) 7. Xerostomia (PSNS) 8. Anhidrosis 9. Heart rate may vary |
|
|
Adverse side effects of succinylcholine
|
-Apnea
-Hyperkalemia and cardiac arrest in burn victims and people with massive muscle nerve damage (because of upregulated nAchR allowing more K+ to leak out); don't give to children -Malignant hyperthermia -Increased gastric pressure -Increased intraocular pressure -A genetic polymorphism in plasma cholinesterase can prolong its action |
|
|
Tubocurarine
|
-Long acting NMJ blocker (1-2 Hours)
-excreted by the kidney unchanged -Also blocks autonomic ganglia -Causes histamine release-contraindicated for asthmatics -excreted by the kidney unchanged -No longer available |
|
|
Metocurine
|
-Long acting NMJ blocker (1-2 Hours)
-excreted by the kidney unchanged -Also blocks autonomic ganglia -Causes Histoamine release, contra-indicated for asthmatics |
|
|
Pancuronium
|
-Long acting NMJ blocker (1-2 Hours)
-deacetylated by the kidney -Moderate block on cardiac mAchRs, causing tachycardia; also increases blood pressure -do not use in patients with heart problems or kidney transplants |
|
|
Pipecuronium
|
-Long acting NMJ blocker (1-2 Hours)
-deacetylated by the kidney |
|
|
Doxacurium
|
-Long acting NMJ blocker (1-2 Hours)
-excreted by the kidney unchanged |
|
|
Vecuronium
|
-Intermediate acting NMJ blocker (20-60 min)
-Deacetylated by kidney and liver -Widely used for surgery, no side effects |
|
|
Atracurium
|
-Intermediate acting NMJ blocker (20-60 min)
-Eliminated by spontaneous hydrolysis -Slight release of Histamine; may cause bronchoconstriction and hypotension |
|
|
Cisatracurium
|
-Intermediate acting NMJ blocker (20-60 min)
-Eliminated by spontaneous hydrolysis -Slight release of Histamine; may cause bronchoconstriction and hypotension |
|
|
Rocuronium
|
-Intermediate acting NMJ blocker (20-60 min)
-Rapid onset; used as alternative to succinylcholine -Eliminated by the liver -Slight activation of cardiac mAchRs, causing bradycardia |
|
|
Mivacurium
|
-Short acting NMJ blocker (5-15 min)
-Eliminated by plasma cholinesterase (action prolonged by plasma AchE variants) -Used for brief procedures and as an alternative to succinylcholine |
|
|
Succinylcholine
|
-Short acting, NMJ depolarizer (5-15 min)
-Stimulates autonomic ganglia -Causes Histamine release, causing bronchocontriction -stimulates cardiac mAchRs, causing bradycardia -Eliminated by plasma cholinesterase -used for brief procedures, like intubation |
|
|
Phentolamine
-MOA -Uses -Adverse effects |
-non-selective alpha blocker
-Used for pheochromocytoma -Has sympathomimmetic activity on the heart, causing tachycardia -Has cholinomimmetic effect on the gut, increasing GI motility -Has H2 agonistic properties, increasing acid and pepsin production |
|
|
Phenoxybenzamine
-MOA -Uses -Adverse effects |
-Non-selective alpha blocker
-Used for Pheochromocytoma; also Raynaud's Disease -Causes severe hypotension and tachycardia; sedation |
|
|
Reserpine
-MOA |
-Depletes nerve of NE and DA by blocking the pump that reuptakes NE and DA into synaptic vesicles
-Works both centrally and peripherally |
|
|
Reserpine
-Administration -Uses |
-Given orally, 1x day
-HPTN |
|
|
Reserpine
-Adverse effects |
-#1=suicide and depression
-Impotence, hypotension, edema -Bad diarrhea -Bradycardia |
|
|
Tolterodine (Detrol LA),
|
mostly M3 mAchR antagonist tertiary amine
-used to treat overactive bladder with incontinence and/or increased frequency and urgency -CI for narrow-angle glaucoma |
|
|
Darifinicen
|
mostly M3 mAchR antagonist tertiary amine
-used to treat overactive bladder with incontinence and/or increased frequency and urgency -CI for narrow-angle glaucoma |
|
|
Drugs @ Cholinergic Neuroeffector Junction:
1) hemicholinium 2) botulinum toxin 3) ACE inhibitors |
1) blocks the uptake of choline
2) prevents ACh release 3) prevent ACh degradation |
