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Intro to pharm
Physiology of PNS/cholinergics/adrenergics/fluid-electrolyte imbalance
| Question | Answer |
|---|---|
| What are the two divisions of the nervous system? | Central NS & Peripheral NS (includes somatic + autonomic: parasympathetic & autonomic: sympathetic) |
| What are three functions of the autonomic nervous system? | regulates heart, secretory glands, & smooth muscles |
| What are the functions of the parasympathetic nervous system? | (GI/bladder/eye) housekeeping (always "on"), slowing of heart rate, increased gastric secretion, emptying of bladder/bowel, focusing of the eye, constriction of pupil, contraction of bronchi |
| What are the functions of the sympathetic nervous system? | (heart/lungs) fight or flight, increased heart rate & blood pressure, dilation of pupils, dilation of bronchi, shunt blood from skin-->muscle, mobilization of stored energy |
| The parasympathetic nervous system dominates except what? | except the vascular system |
| What are the main components of the basic parasympathetic nervous system pathway? | spinal cord, preganglionic neuron, ganglion, postganglionic neuron, various organs |
| What are the main components of the basic sympathetic nervous system pathway? | spinal cord, preganglionic neuron-->ganglion-->postgangionic neuron-->various organs OR spinal cord-->"preganglionic neuron"-->adrenal medulla-->various organs |
| What are the main components of the basic somatic motor system pathway? | spinal cord, motor neuron, skeletal muscle |
| Where do drugs work? | at the ganglionic junction or effector organ |
| What are the neurotransmitters used in the parasympathetic nervous system? | ACh (acetylcholine) at both junctions (ganglionic & at junction with organ) |
| What are the neurotransmitters used in the sympathetic nervous system? | ACh (acetylcholine) at the ganglionic junction & at the adrenal medulla & at the junctions with sweat glands; NE (norepinephrine) at the junctions with various organs & the postgranglionic neuron; Epinephrine Epi) after adrenal medulla-->organ |
| What neurotransmitter is used in the somatic motor system? | ACh(acetylcholine) between the motor neuron & skeletal muscle |
| What are three cholinergic (ACh) receptor subtypes? | NicotinicN, NicotinicM, Muscarinic |
| What are the adrenergic (Epi & NE) receptor subtypes? | Alpha1, Alpha2, Beta1, Beta2, dopamine |
| What are the receptor subtypes located in the parasympathetic nervous system? | At the ganglionic junction, ACh binds to a nicotinicN receptor; At the organ junction, ACh binds to a muscarinic receptor |
| What are the receptor subtypes located in the sympathetic nervous system? | At the ganglionic junction, ACh binds to a nicotinicN receptor; at the organ junction, NE binds to alpha or beta receptors; at the sweat gland junction, ACh binds to a muscarinic receptor; at the adrenal medulla-organ junction, Epi binds to alpha or beta |
| What receptor subtype is located in the somatic motor system? | At the neuromuscular junction (motor neuron-skeletal muscle), ACh binds to a muscarinic receptor |
| Where are nicotinicN (cholinergic) receptor subtypes located? | all autonomic nervous system ganglia & the adrenal medulla |
| What is the NicotinicN (cholinergic) receptor subtype response to receptor activation? | stimulation of parasympathetic postganglionic nerves & release of epinephrine from the adrenal medulla |
| Where are nicotinicM (cholinergic) receptor subtypes located? | at the neuromuscular junction |
| What is the NicotinicM (cholinergic) receptor subtype response to receptor activation? | contraction of skeletal muscle |
| Where are muscarinic (cholinergic) receptor subtypes located? | all parasympathetic target organs: eye, heart, lung, bladder, GI tract, sweat glands, sex organs, blood vessels |
| What is the muscarinic (cholinergic) receptor response to receptor activation in the eye? | contraction of the ciliary muscle focuses the lens for near vision; contraction of the iris sphincter muscle causes miosis (decreased pupil diameter) |
| What is the muscarinic (cholinergic) receptor response to receptor activation in the heart? | decreased heart rate |
| What is the muscarinic (cholinergic) receptor response to receptor activation in the lung? | CONSTRICTION of bronchi, promotion of secretions |
| What is the muscarinic (cholinergic) receptor response to receptor activation in the bladder? | promotes voiding |
| What is the muscarinic (cholinergic) receptor response to receptor activation in the GI tract? | salivation, increased gastric secretions, increased intestinal tone & motility, defacation |
| What is the muscarinic (cholinergic) receptor response to receptor activation in the sweat glands? | generalized sweating |
| What is the muscarinic (cholinergic) receptor response to receptor activation in the sex organs? | erection |
| What is the muscarinic (cholinergic) receptor response to receptor activation in the blood vessels? | vasodilation |
| Where are Alpha1 (adrenergic) receptor subtypes located? | eye, arterioles (skin, viscera, mucous membranes), veins, sex organs (male), bladder neck & prostatic capsule |
| What is the Alpha1 (adrenergic) receptor response to receptor activation? | eye:contraction of radial muscle of iris causes mydriasis (increased pupil size); arterioles (skin, viscera, mucous membranes): constriction; veins: constriction; male sex organs: ejaculation; bladder neck & prostatic capsule: contraction |
| Where are Alpha2 (adrenergic) receptor subtypes located? | presynaptic nerve terminals (NOT ORGANS) (in CNS are postsynaptic) |
| What is the Alpha2 (adrenergic) receptor response to receptor activation? | inhibition of neurotransmitter release |
| Where are Beta1 (adrenergic) recptor subtypes located? | HEART, kidneys |
| What is the Beta1 (adrenergic) receptor response to receptor activation? | heart: increased rate, increased force of contraction, increased AV conduction velocity; kidney: renin release |
| Where are Beta2 (adrenergic) receptor subtypes located? | LUNGS, arterioles (heart, lung, skeletal muscle), bronchi, uterus, liver, skeletal muscle |
| What is the Beta2 (adrenergic) receptor response to receptor activation? | arterioles (heart/lung/skeletal muscle): dilation; bronchi: dilation; uterus: relaxation; liver: glycogenolysis; skeletal muscle: enhanced contraction/glycogenolysis |
| Where are the dopamine (adrenergic) receptor subtypes located? | kidney |
| What is the dopamine (adrenergic) receptor response to receptor activation? | dilation of kidney vasculature |
| What is the specificity of epinephrine (which receptors won't it bind to)? | no dopamine |
| What is the specificity of norepinephrine (which receptors won't it bind to)? | no beta2 or dopamine |
| What is the specificity of dopamine (which receptors won't it bind to)? | no alpha2 or beta2 |
| What are the basic steps in the life cycle of ACh? | choline + acetylcoenzyme A (acetyl CoA); STORED; destroyed by acetylcholinesterase (enzymatic degradation terminates transmission); uptake of choline |
| What are the basic steps in the life cycle of NE? | precursors: amino acids; vesicles; reuptake (terminates transmission NOT enzymatic degradation); converted to Epi |
| What is the representative drug for muscarinic agonists? | Bethanechol |
| What is the representative drug for muscarinic antagonists? | atropine |
| What is the representative drug for ganglionic stimulating agents? | nicotine |
| What is the representative drug for ganglionic blocking agents? | Trimethaphan |
| What is the representative drug for neuromuscular blocking agents? | d-Tubocurarine, succinylcholine |
| What is the representative drug for cholinesterase inhibitors? | Neostigmine, physostigmine |
| What are the characteristics of muscarinic receptor subtypes? | Location: sweat glands/blood vessels/all organs regulated by parasympathetic nervous system; effects of receptor activation: many/decreased heart rate/increased gland secretion/smooth muscle contraction; receptor agonists: Bethanechol/Cholinesterase inhib |
| What are the characteristics of NicotinicN receptor subtypes? | Location: all ganglia of the autonomic nervous system; effects of receptor activation: promotes ganglionic transmission; receptor agonists: Nicotine/cholinesterase inhibitors-physosttigmine/neostigmine); receptor antagonists: Trimethaphan |
| What are the characteristics of NicotinicM receptor subtypes? | location: neuromuscular junction; effects of receptor activation: skeletal muscle contraction; receptor agonists: nicotine/cholinesterase inhibitors: physostigmine/neostigmine; receptor antagonists: d-Tubocurarine, succinylcholine |
| What are some examples of muscarinic agonists (parasympathetic: mimic PSNS-decreased heart rate, increased sweating, voiding, salivation, pupil constriction)? | Bethanechol: relieves urinary retention + side effects include hypotension, excessive salivation/gastric acid secretion, bronchoconstriction; Pilocarpine (glaucoma med); Acetylcholine (Michol- used with opthalmic surgery) |
| What are some characteristics of muscarinic antagonists? | used for muscarinic poisoning (mushrooms/muscarinic agonists/cholinesterase inhibitors); example is Atropine; also used for preanesthetic + disorders of the eye + bradycardia + decrease intestinal motility + stabilize blood pressure |
| What are some symptoms of muscarinic poisoning (mushrooms/muscarinic agonists/cholinesterase inhibitors)? | excessive sweating, tearing, hypotension |
| What are some possible side effects of muscarinic antagonists? | dry mouth, blurred vision, elevation of eye pressure, constipation, tachycardia |
| What are some potential drug interactions for muscarinic antagonists? | antihistamines, antipsychotics, antidepressants |
| What are some examples of muscarinic antagonists used for urge incontinence? | Oxybutynin (Nitropan) & Tolterodine (Detrol) |
| What is a muscarinic antagonist used for motion sickness? | Scopolamine |
| What is a muscarinic antagonist used for asthma? | Ipatropium Bromide |
| What are some characteristics of antimuscarinic poisoning? | treated with natural products/muscarinic antagonists/antimuscarinic properties; signs of poisoning: Hot as Hare + dry as bone + red as beet + blind as bat + mad as hatter (delerium is step further); use charcoal & physostigmine (inhibitor of acetylcholine |
| What are two reversible cholinesterase inhibitors? | Neostigmine (Prostigmin) + Physostigmine (Antilirium) |
| What are some characteristics of Neostigmine (Prostigmin)? | reversible cholinesterase inhibitor; binds to cholinesterase preventing it from catalyzing breakdown of ACh; used with myasthenia gravis; side effects: salivation, GI secretion, sweating; interactions: muscarinic antagonists, neuromuscular blockers; does |
| What are some characteristics of Physostigmine (Antilirium)? | crosses membranes, drug of choice to treat Atropine poisoning |
| What are some characteristics of Myasthenia Gravis? | fluctuating muscle weakness & rapid fatigue; drooping eyelids, difficulty swallowing, weakness of muscle, difficulty breathing; autoimmune-antibodies against nicotinicM receptors (can result in 70-90% decrease) |
| What are some characteristics of irreversible cholinesterase inhibitors? | highly toxic (insecticides & nerve agents); glaucoma (only use for these: Echothiopate-phospholine iodide) |
| What are some characteristics of poisoning due to irreversible cholinesterase inhibitors? | symptoms: profuse sweating/urination/bronchoconstriction/paralysis; treat with ventilation/atropine/Pralidoxime (Protopam) |
| What receptor subtype is blocked by neuromuscular blocking agents? | block nicotinicM receptors (result in muscle relaxation) |
| What receptor subtype is blocked by ganglionic blocking agents? | block nicotinicN (mostly replaced by newer drugs though) |
| During neuromuscular excitation-contraction depolarization, does positve charge go in or out? | positive goes in during depolarization |
| During neuromuscular excitation-contraction repolarization, does positive charge pump in or out? | during repolarization, positive pumps out |
| What are some characteristics of the non-depolarizing neuromuscular blocking agent Tubocurarine (curare)? | mechanism of action: competes with ACh to bind to nicotinicM receptors; used for muscle relaxation during surgery, mechanical ventilation, endotrachial intubation, & electroconvulsive therapy; side effects: respiratory paralysis, hypotension; drug interac |
| What is the main thing to watch for when a patient has taken neuromuscular blocking agents? | respiratory distress |
| What are some characteristics of the depolarizing neuromuscular blocking agent Succinylcholine (Anectine, Quelicin)? | binds to nicotinicM receptors (& remains bound: constant depolarization); used for endotrachial intubation, electroconvulsive therapy, endoscopy; side effects: apnea, malignant hyperthermia, postoperative muscle pain, hyperkalemia; drug interactions: chol |
| What are some therapeutic uses for neuromuscular blocking agents? | muscle relaxation during surgery, mechanical ventilation, electroconvulsive therapy, endotracheal intubation |
| What are some characteristics of ganglionic blocking agents? | lack selectivity; example is Trimethaphan (Arfonad) which competes with ACh for binding to nicotinicN receptors; controlled hypertension in surgery, hypertensive crisis; side effects include antimuscarinic effects (dry mouth/blurred vision/elevation of ey |
| What are some characteristics of adrenergic agonists (sympathomimetics)? | direct receptor binding, promotion of NE release (indirect), inhibition of NE uptake (indirect): termination, inhibition of NE inactivation (indirect): MAO, catecholamines & noncatecholamines |
| What are some characteristics of adrenergic agonists-catecholamines? | Epinephrine, NE, Isoproterenol, Dopamine & Dobutamine; cannot give orally (MAO-liver, COMT-intestine); cannot cross BBB, brief duration of action; chemistry: catechol group + amine |
| What are some characteristics of adrenergic agonists-non-catecholamines? | Ephedrine, Phenylephrine, & Terbutaline; given orally; penetrates BBB, longer duration of action |
| Which catecholamines activate alpha1 receptors? | Dopamine, epinephrine, norepinephrine |
| Which noncatecholamines activate alpha1 receptors? | phenylephrine, ephedrine |
| Which catecholamines activate alpha2 receptors? | epinephrine, norepinephrine |
| Which noncatecholamines activate alpha2 receptors? | ephedrine |
| Which catecholamines activate beta1 receptors? | epinephrine, norepinephrine, isoproterenol, dobutamine, dopamine |
| Which noncatecholamines activate beta1 receptors? | ephedrine |
| Which catecholamines activate beta2 receptors? | epinephrine, isoproterenol |
| Which noncatecholamines activate beta2 receptors? | ephedrine, terbutaline |
| Which catecholamines activate dopamine receptors? | dopamine |
| Which nonchatecholamines activate dopamine receptors? | none |
| What are the uses for alpha1 activation? | vasoconstriction-hemostasis (Epi), nasal decongestion (phenylephrine & ephedrine), delay of anesthetic absorption (Epi), elevation of blood pressure (not primary drugs used), pupil dilation |
| What are some side effects of alpha1 activation? | mostly relate to vasoconstriction, hypertension, necrosis, bradycardia |
| What are some uses for alpha2 activation? | peripheral-inhibits NE release; CNS-reduce stimulation of adrenergic receptors |
| What are some uses for beta1 activation? | cardiac arrest (helps to get contraction going), heart failure (increases force of contraction), shock (increase heart rate & blood flow), AV heart block (increase impulse conduction) |
| What are some side effects of beta1 activation? | altered heart rate or rhythm, angina pectoris (insufficient oxygen compared to demand) |
| What are some uses for beta2 activation? | asthma (bronchodilation), delay of preterm labor (relaxation of uterus) |
| What are some side effects of beta2 activation? | hyperglycemia, tremor (most common) |
| What are some uses for dopamine activation? | shock (dilation of kidney vasculature) |
| What are some characteristics of anaphylactic shock? | hypotension, bronchoconstriction, edema, Epi (all receptors) |
| What are some characteristics of the catecholamine Epinephrine (Adrenalin, EpiPen)? | binds to all receptors except dopamine (alpha 1&2, beta 1&2), used for anaphylactic shock, delay absorption of anesthetics, hemostasis, overcome AV heart block, pupil dilation, asthma |
| What are some side effects of the catecholamine epinephrine (adrenalin, epipen)? | hypertensive crisis, dysrhythmias, angina, necrosis, hyperglycemia |
| What are some drug interactions for the catecholamine epinephrine (adrenaline, epipen)? | MAO inhibitors, tricyclic antidepressants |
| What are some characteristics/side effects/drug interactions for the catecholamine norepinephrine (Levophed)? | bind to alpha1, alpha2, beta1; used for hypotension & cardiac arrest; side effects: hypertensive crisis, dysrhythmias, angina, necrosis |
| What are some characteristics of the catecholamine Isoproterenol (Isuprel)? | bind to beta1 & beta2; used for AV heart block, asthma, bronchospasm |
| What are some side effects of the catecholamine Isoproterenol (Isuprel)? | dysrhythmias, angina, hyperglycemia |
| What are some drug interactions for the catecholamine Isoproterenol (Isuprel)? | MAO inhibitors, tricyclic antidepressants |
| What are some characteristics of the catecholamine dopamine (Intropin)? | bind to dopamine/alpha1/beta1 receptors, used for shock, heart failure, acute renal failure |
| What are some side effects of the catecholamine dopamine (Intropin)? | tachycardia, dysrhythmias, angina, necrosis |
| What are some drug interactions for the catecholamine dopamine (Intropin)? | MAO inhibitors, tricyclic antidepressants |
| What are some characteristics of the catecholamine Dobutamine (Dobutrex)? | binds to beta1 receptors, used for heart failure, side effect is tachycardia, drug interactions with MAO inhibitors/tricyclic antidepressants/anesthetics |
| What are some characteristics of the noncatecholamine Terbutaline (Brethine)? | binds to beta2 receptors, used for asthma & delay of preterm labor, side effect is tremor |
| What are the characteristics of the noncatecholamine Ephedrine? | binds to alpha1, alpha2, beta1, beta2 receptors; mixed drug (direct activation of alpha/beta & indirect by releasing NE); used for nasal decongestion & narcolepsy |
| What are the side effects for the noncatecholamine Ephedrine? | hypertensive crisis, dysrhythmias, angina, necrosis, hyperglycemia, insomnia |
| Which adrenergic antagonists (blocking agents) block both alpha1 and alpha2 receptors? | Phentolamine, Phentoxybenzamine |
| Which adrenergic antagonists block only alpha1 receptors? | Doxazosin, Prazosin, Terazosin, Tamsulosin |
| Which adrenergic antagonists block both beta1 & beta2 receptors? | Carteolol, Carvedilol, Labetalol, Nadolol, Penbutolol, Pindolol, Propranolol, Sotalol, Timolol |
| Which adrenergic antagonists block only beta1 receptors? | Acebutolol, Atenolol, Betaxolol, Bisoprolol, Esmolol, Metoprolol |
| What are some uses for alpha-adrenergic antagonists? | hypertension, reversal of alpha1 agonist toxicity, benign prostatic hyperplasia, pheochromocytoma, Raynaud's Disease |
| What are some side effects of alpha-adrenergic antagonists? | orthostatic hypotension, reflex tachycardia, nasal congestion |
| What are some characteristics of the alpha-adrenergic antagonist Prazosin (Minipress)? | alpha1 blockers, used for hypertension & benign proststic hyperplasia; side effects: orthostatic hypotension, reflex tachycardia, nasal congestion |
| What are some characteristics of the alpha-adrenergic antagonist Phentolamine (Regitine)? | alpha1 & alpha2 blockers, used for pheochromocytoma; side effects: orthostatic hypotension, reflex tachycardia, nasal congestion (same as Prazosin) |
| What are some general characteristics of beta-adrenergic antagonists? | used for angina pectoris, hypertension, dysrhythmias, MI, heart failure; side effects (depend on receptor blocked): beta1-bradycardia/precipitation of heart failure/AV heart block; beta2-bronchoconstriction/inhibits glycogenolysis |
| What receptors does the beta-adrenergic antagonist Proprandolol (Inderal) block & what are its uses? | blocks beta1 & beta2; used for hypertension, MI, angina |
| What are the side effects of the beta-adrenergic antagonist Propranolol (Inderal)? | bradycardia, heart failure, inhibition of glycogenolysis, bronchoconstriction, CNS effects |
| What are the contraindications & drug interactions for the beta-adrenergic antagonist Propranolol (Inderal)? | contraindications: diabetics, severe allergic reaction, heart failure, asthma, depression; drug interactions: calcium channel blockers, insulin |
| What receptor does the beta-adrenergic antagonist Metoprolol (Lopressor) block & what are its uses? | blocks beta1; uses: hypertension, patients with asthma or diabetes & angina or MI |
| What are the side effects of the beta-adrenergic antagonist Metoprolol(Lopressor)? | bradycardia, AV heart block |
| What are the contraindications for the beta-adrenergic antagonist Metoprolol (Lopressor)? | heart failure, sinus bradycardia |
| What are the characteristics of the indirect acting antiadrenergic agent Reserpine (adrenergic neuron-blocking agent)? | suppresses NE synthesis & displaces NE from vesicles, hypertension, side effects: depression/bradycardia/orthostatic hypotension; Guanethidine (Ismelin): no CNS effects b/c does not cross BBB |
| What are some characteristics of the centrally acting alpha2 agonist (indirect agent) Clonidine (Catapres)? | activates alpha2 receptors to decrease transmitter release; used for hypertension & severe pain; side effects: drowsiness, dry mouth, rebound hypertension; other drugs: Guanabenz (Wytensin) & Guanfacine (Tenex) |
| What are some characteristics of the centrally acting alpha2 agonist (indirect agent) Methyldopa (Aldomert)? | similar to clonidine except must be converted to methylNE; used for hypertension; side effects: hemolytic anemia & liver toxicity |
| What are some applications for diuretics? | increase output of urine; hypertension; mobilization of fluid; prevent renal failure |
| What is the functional unit of the kidney? | Nephron (including glomerulus, proximal convoluted tubule, loop of Henle, distal convoluted tubule, collecting duct) |
| What are some kidney functions? | cleansing of extracellular fluid (ECF), maintenance of acid-base balance, excretion of metabolic wastes & foreign substances |
| What are three basic renal processes? | filtration, reabsorption, active secretion |
| What are some characteristics of renal filtration? | occurs at glomerulus, small molecules such as sodium/chloride (smaller amounts of bicarbonate, potassium ions), 125mL of filtrate per minute (180L per day), non-selective |
| What are some characteristics of renal reabsorption? | very selective, 99% undergoes reabsorption, active transport, water follows passively, diuretics interfere |
| What are some characteristics of renal secretion? | "pumps" for active secretion, located in proximal convoluted tubules, organic acids/organic bases |
| What are some characteristics of the reabsorption site: proximal convoluted tubule? | 65% of Na+ & Cl-; all of bicarb & K+; water passively follows, isotonic, dilute urine |
| What are some characteristics of the reabsorption site: loop of Henle? | descending loop: permeable to water, concentrated urine; ascending loop: 20% of Na+ & Cl-; NOT permeable to water, returns to original isotonic urine |
| What occurs in the distal convoluted tubule (early segment)? | 10% of Na+ & Cl-; water passively follows |
| What occurs at the late distal convoluted tubule & collecting duct (distal nephron)? | exchange of Na+ & Cl-; urine concentration by ADH (antidiuretic hormone), deficiency =diabetes |
| What are some characteristics of diuretics? | blockade of Na+ & Cl- reabsorption; prevents reabsorption of water/retention; small blockade = large effect |
| What are some general adverse effects of diuretics? | acid-base imbalance, disturbance of electrolytes, severe dehydration |
| What are the most effective diuretics? | High-ceiling Loop diuretics (work in the loop of henle), such as Furosemide (Lasix) |
| What are some characteristics of Furosemide (Lasix)? | blocks Na+ & Cl- reabsorption (some K+); high-ceiling loop diuretic, possible adverse effects: dehydration (headache/pain in chest, calves, pelvis), hypotension, hypokalemia-Digoxin toxicity, ototoxicity |
| What are some characteristics of Thiazide diuretics? | block Na+ & Cl- reabsorption (K+), elevate uric acid & glucose, example is Hydrochlorothiazide (HydroDIURIL), which works at the early segment of distal tubule & depends on kidney function |
| What are some potential adverse effects of Hydrochlorothiazide (HydroDIURIL), a thiazide diuretic? | dehydration (headache/pain in chest, calves, or pelvis), hypotension, hypokalemia-Digoxin toxicity, not for use during pregnancy |
| What are some characteristics of Potassium-sparing diuretics? | modest increase in urine production, decrease in K+ excretion, aldosterone & non-aldosterone, examples: Spironolactone (Aldactone), Triamterene (Dyrenium), Amiloride (Midamor) |
| What are some characteristics of Spironolactone (Aldactone)? | potassium-sparing diuretic, aldosterone antagonist, retains potassium & excretes sodium, adverse effects: hyperkalemia |
| What are some characteristics of Triamterene (Dyrenium)? | potassium-sparing diuretic, non-aldosterone antagonist, direct inhibitor of potassium/sodium exchange, quicker than spironolactone, adverse effects: hyperkalemia |
| What are some characteristics of osmotic diuretics? | creates osmotic force as undergoes minimal reabsorption, example: Mannitol (Osmitrol) |
| What are some characteristics of Mannitol (Osmitrol)? | Intracranial pressure & intraocular pressure are uses, adverse effect is edema(don't use this drug to treat edema) |
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mpost51
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