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Intro 2 Pharmacolog
| Question | Answer |
|---|---|
| Propranolol | nonselective beta-1 & beta-2 blocker |
| Metoprolol | selective” beta-1 blocker |
| Atenolol | selective β-1 blocker; limited CNS penetration |
| Carvedilol | β-1, β-2, a-1 blocker + antioxidant |
| Labetalol | β-1, β-2, a-1 blocker |
| Nebivolol | β-1 selective blocker + NO generator |
| Name the alpha antagonists | Phentolamine Phenoxybenzamine Prazosin |
| Name the Beta antagonists | Propranolol Metoprolol atenolol |
| Name the mixed alpha beta antagonists | Labetalol |
| Name the 3rd generation β-AR antagonists | Carvedilol Nebivolol |
| What do phenoxybenzamine cause? | irreversible blockade of α-adrenoceptors |
| What is carvedilol | an anti-oxidant |
| What does nebivolol produce? | nitric oxide |
| What are the uses for Uses alpha-AR Antagonists | Acute hypertensive crisis (e.g., phentolamine Essential hypertension (e.g., prazosin) Raynaud’s syndrome Combined with B-AR blocker for pre- & operative management of pheochromocytoma |
| What does meta-analysis suggest compared with other anti-hypersensitives? | Beta blockers may increase risk adverse CV outcomes especially in elderly |
| Activation of Sympathetic and Renin-Angiotension Aldosterone systems are compensatory for what type of myocardial inadequacy? | Acute |
| What is the Frank-Starling mechanism? | Venous constriction to Increase venous return and increase cardiac filling |
| What does the pre-synaptic alpha 2 do? | decrease neurotransmitter release |
| what does the post synaptic alpha 2 do | decrease sympathetic outflow |
| What is norepinephrine's greatest affinity? Least affinity? | a-1~a2>B-1>>B-2 |
| What is epinephrines greatest affinity? Least affinity? | B1~B2>a-1~a-2 |
| What is Isoproterenol's greatest affinity? Least affinity? | B-1~B-2>>>a |
| What is Dopamine's greatest affinity? Least affinity? | D-receptor>>B-AR>>a-AR |
| What is a characteristic of Dopamine? | Vasodilation via D-1 receptor in Renal, Mesenteric, Intracerebral, Coronary Beds |
| What is a characteristic of Norepinephrine? | Vagal mediated reflex DECREASE in HR |
| Describe a characteristic of Ephedrine. | Release of cytosolic catecholamine pool via facilitated transport by uptake I |
| Name 3 special characteristics of Amphetamine | alpha mediated vasoconstriction increase BP and vagal mediated reflex bradycardia Contracture of urinary sphincter |
| The Parasympathetic system and the sympathetic system does what? | Serve most of the same organs but cause opposing or antagonistic effects |
| Name 2 natural alkaloids | Muscare & Pilocarpine |
| Does muscarine, benztropine, civemline, edrophonium, or hexamethonium act as a poison in mushrooms? | Muscarine |
| What is pilocaripine? | Pure muscarinic agent in low doses; ganglionic stimulation in overdose (cardiovascular stimulation) |
| How was pilocarpine first used? | First agent used in dentistry |
| Name some effects of Muscarine | Emesis, diarrhea, urination, cramps, salivation, sweating, bradycardia, hypotension, bronchospasm, miosis |
| Name 2 charateristics of acetylcholine | -Brief acting -Rlatively muscarinic selective |
| Name a characteristic of methacholine | Sensitive to acetylcholinesterase |
| Name two characteristics of bethanechol | -Pure muscarinic (low in M2 activity) -Resistant to hydrolysis by cholinesterases |
| Name 2 characteristics of carbachol | -Strong nicotinic agonist, causes acetylcholine release from nerve terminals -Resistant to hydrolysis by cholinesterases |
| What is an H1 histamine RECEPTOR blocking agent? | Dephenhydramine |
| Describe Amitriptyline | Affinity of M receptor is 1/10 of atropine |
| What is Darifenacin | M3 Muscarinic Receptor Antagonist |
| Describe the characteristics of Darifenancin | -Blocks the M3 receptor -Blocks the actions of acetylcholine at smooth muscles and glands -Detrusor smooth muscle urinary bladder |
| Name a M2 Muscarinic Receptor Antagonist | Tripitamine |
| Describe 2 characteristics of Tripitamine | -Blocks the M2 receptor -Blocks the action of acetylcholine at cardiac muscle fibers |
| Name an M1 Muscarinic Receptor Antagonist | Pirenzepine |
| Name three therapeutic uses of pirenzepine | -has selectivity for the M1 over M2 and M3 -exhibits affinity for the M4 receptor -Useful for peptic ulcer |
| Ipratropium (N+) | blocks all subtypes of M receptors |
| Tiotropium (N+) | M1 and M3 selectivity |
| Name a tertiary Muscarinic antagonist? | Tolterodine |
| Name a use of tolterodine | Urinary bladder |
| What is shorter acting than atropine and can cross the blood brain barrier? | Tertiary Muscarinic Antagonists |
| Discuss a characteristic of Tropicamide | has a much shorter duration of action than atropine |
| Name a muscarinic antagonist for Parkinson's disease | Benztropine |
| Discuss the actions of the Eye | mydriasis and cycloplegia (paralyze accomodation) |
| Mucus glands of the pharynx and nasal cavity does what? | inhibit secretions |
| What does the bronchial smooth muscle do? | inhibits bronchoconstriction |
| What does the gastric glands do? | Reduce secretions |
| What does the pancreas do? | Reduce secretions |
| What happens to the mucus glands of the respiratory track? | It becomes dry |
| What happens with eccrine sweat glands? | Inhibits sweating |
| Is atropine competitive or non competitive? | Competitive |
| How can the inhibition of Atropine be overcome? | With Ach |
| What does the therapeutic doses of scopolamine normally produce? | CNS depression, manifested as drowsiness, amnesia, fatigue, dreamless sleep, reduction in REM, euphoria |
| In the presence of pain,scopolamine's therapeutic dose can produce... | excitement, restlessness, hallucinations, or delirium |
| What is scopolamine's main therapeutic use? | Prophylaxis of motion sickness |
| What happens when give 0.5 mg of atropine? | -Slowing of Heart Rate -Dryness of mouth -Inhibition of sweating |
| What happens when give 1.0 mg of atropine? | -Definite dryness of mouth -Thirst -Increased Heart Rate -Increase dilation of pupil |
| What happens when given 2.0 mg of atropine? | -Rapid Heart Rate;palpitations -Marked dryness of mouth -dilated pupils -Some blurring of vision |
| What happens when give 5.0 mg of atropine? | -All the rest plus -difficultly in speaking; swallowing -restlessness -Fatigue -Headache -Hot skin -Difficulty in urination -Decrease intestinal peristalsis |
| What happens when given 10 mg of atropine? | -All the rest, plus -rapid weak pulse -iris very wide (even visible) -Vision very blurred -Skin flushed: hot dry; scarlet -Ataxia -Restlessness and excitement -Hallucination +/-coma |
| Name 3 reversible inhibitors | -Edrophonium -Neostigmine -Physostigmine |
| Name 2 characteristics of Edrophonium | -truly reversible -short acting |
| Name 2 characteristics of Neostigmine | -Typical 'reversible" type -Binds irreversibly but is slowly hydrolyzed |
| Name 2 characteristics of physostigmine | -Lipid soluble -Used for central effects |
| Name 2 "irreversible" organophosphate inhibitors for nerve gases | -Sarin -Tabus |
| Name 2 "irreversible" organophosphate inhibitors for insecticides | -malathion -parathion |
| Name 2 "irreversible" organophosphate inhibitors for therapeutic agents | -echothiophate -isoflurophate |
| What are 2 alzheimer's disease agents? | -donepezil -rivastigmine |
| In the mechanisms of clinesterate inhbition was reactivating agent may be used? | Pralidoxime |
| Pralidoxime has a ___ that interacts with ____ site | nucleophilic site that interacts with phosphorylated site |
| Pralidoxime must be given ___ AChE has ___ in order to be effective as a reactivator of the enzyme | must be given BEFORe achE has AGED in order to be effective.. |
| Name two Carbamyl inhbitors of Ache | -Physostigmine -Neostigmine (N+) |
| Donepezil and Rivastigmine are used for what? | Alzheimer's disease |
| Name a therapeutic used of Edrophonium | Diagnosis of myasthenia gravis |
| What is both less specific and less sensitive than antibody titers? | Edrophonium, or Tensilon Test |
| miosis, blurred vission, and headache are toxic effects of Inhibitors of ACETYLCHOLINESTERASE for what receptor? | Ocular Muscarinic |
| Toxic effects of inhibitors of acetylcholinesterase that include lacrimal, salivary, bronchial are for what receptor? | Muscarinic Secretions |
| Toxic effects of inhibitors of acetylcholinesterase that include contraction, bronchial, visceral, are for what receptor? | Muscarinic smooth muscle |
| Toxic effects of inhibitors of acetylcholinesterase that include bradycardia, hypotension | Muscarinic cardiovascular |
| Toxic effects of inhibitors of acetylcholinesterase that include fasciculation, and weakness | Nicotinic skeletal muscle |
| Toxic effects of inhibitors of acetylcholinesterase that include tachycardia, blood pressure instability | Nicotinic Cardiovascular |
| Toxic effects of inhibitors of acetylcholinesterase that include mixed excitatory and depresseant effects | CNS |
| Toxic effects of inhibitors of acetylcholinesterase that include respiratory and circulatory collapse | CNS |
| Name a treatment of toxicity. What does it do? | Pralidoxime as a reversal agent It binds to clinesterase at sites outside the CNS Displaces organophosphate before irreversible binding |
| Name four organophosphate inhibitors of Acetylcholinesterase | -Echothiophate (N+) -Sarin -Malathion -Parathion |
| What is echothiophate used for? What does it do? | For wide angle glaucoma reduces pressure in the eye by increasing the amount of fluid that drains from the eye |
| Malathion and parathion are hydrolyzed by birds but not by? | Insects |
| What is malathion used for? | Pediculosis (lice) |
| Agents such as tabun, soman, and ____ may be used as ___ in chemical warfare | Sarin, nerve agents |
| Accumulation of Ach at cloinergic receptors produces effects reflecting? | Stimulation of cardiac muscle, smooth muscles, and galnds |
| What happens to the body in chemical warfare? | Bradycardia and hypotension occurs |
| Irreversible inhibition of acetylcholinesterase by chemical agents produces____. Where does it happen? | Accumulation of ACh. It happens at the end plate of skeletal muscle fibers |
| What happens when the accumulation of ACh at the end plate of skeletal muscle fibers leads to depolarizing blockade of Nm nicotinic receptor? | There is a skeletal and diaphragm paralysis. |
| What does an individual eventually dies from in chemical warfare? | Respiratory paralysis |
| How does cholinergic agonists work? | By mimicking the action of acetycholine |
| Name the seven characteristics that cholinergic agonists produce when combining with receptors on the cell membranes | -salivation -bradycardia -dilation of blood vessels -constriction of the pulmonary bronchioles -increased activity of the GI tract -increased tone and contraction of the muscles in the bladder constriction of the pupils |
| What does Cholinomimetic agents do? | reproduce the effects of acetylcholine, by direct or indirect action. |
| Directly acting cholinomimetic drugs do? | the other cholinomimetic agents act preferentially on a given type of receptor, either muscarinic or nicotinic receptors. |
| Name some irreversible organophosphate inhibitors | -Sarin -Tabun -Malathion -Parathion -Echothiphate |
| What can be used for Glaucoma? | Physostigmine |
| What cab be used for the atony of the bladder, parlytic ilieus? | neostigmine |
| What can be used for intoxication by antimuscarinic agents? | physostigmine |
| What can be used for intoxication by ticyclic antidepressants or phenothiazines? | Physostigmine |
| What can be used for myasthenia gravis? | neostigmine |
| What two drugs can be used for reversal of neuromuscular block? | edrophonium, neostigmine |
| WHat can be used for atropine poisoning and central anticholinergic syndrome? | physostigmine |
| What can be used for alzheimer's disease? | Donepezil, Rivastigmine |
| What can be used for lice? | Malathion |
| Name the organophosphate inhibitor that therapeutic use is to localize application to the eye for wide angle glaucoma | Echothiophate |
| Atropine is used in what type of cases? | Increased vagal outflow |
| What will be used for improper use of choline esters? | Atropine |
| What will be used for the simus or nodal bradycardia in cases of excessive vagal tone associated with myocardial infarct? | Atropine |
| What will be used for hyperactive carotid sinus? | Atropine |
| What will be used for second degree heart block? | Atropine |
| What will be used for prophylaxis of motion sickness | Scopolamine |
| What will be used for poisoning by inhibitors of acetylcholinesterase? | atropine |
| What will be used for mushroom poisoning due to muscarine? | atropine |
| What will be used in conjunction with inhibitors of acetylcholinesterase when they are used to promote recovery from neuromuscular blockade after surgery? | atropine |
| What will prevent vagal reflexes induced by surgical manipulation of visceral organs? | Atropine |
| What will be injudicious use of choline esters? | atropine |
| What will be used to reduce urinary urgency? | Tolterdonine |
| What does Darifenacin block? | -Blocks the M3 receptor -Blocks the actions of acetylcholine at smooth muscles and glands |
| What is Edrophonium used for | Myasthenia gravis |
| Edrophonium is it reversible or irreversible? | Reversible |
| ____ and ____ are hydrolized by birds and mammals but not by insects | -Malathion -Parathion |
| What can inhibit malathion? | Organophosphates |
| What kind of drug is d-Tubocurarine? | -a neuromuscular-blocking drug or skeletal muscle relaxant |
| What category does d-Tubocurarine | Competitive antagonist |
| What does Hexamethonium do? | -Blocks the response of acetylcholine at the autonomic ganglia -Does not depolarize or stimulate the ganglion |
| What does d-Tubocurarine produce? | Paralysis of skeletal muscles |
| Prolonged weakness, bronchoconstriction, increase in bronchial secretion, and hypotension is an adverse effect of what drug? | d-Tubocurarine |
| Name an adverse effect of d-Tubocurarine | Histamine release |
Created by:
cweir22
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