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99 Cards in this Set
- Front
- Back
What is phase 1 block?
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overstimulation of Nicotinic (cholinergic)stimulation.
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What can block the nicotinic receptors at the skeletal muscle?
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1. Tubocurarine
2. Trimethaphan |
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1. What is the mechanism of Vasodialation of endothelial cells by muscarinic cholinergic agonist?
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1. Release of NO (activation EDRF)
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Alpha are always exciting except for?
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GI tract
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Location of alpha 1 and alpha 2?
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1. Mostly postjunctional
2. Mainly prejunctional (except postjunctional at plt, smooth muscle, and adipocytes) |
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what are the primary effects of Beta 1 adnergic receptors?
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1. Heart rate
2. Lipolysis 3. Renin secretion |
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Isoproterenol has a greater effect on what receptor over Epi and NE?
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Beta 1 (Iso also stimulates Beta 2)
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Function of Beta 2 adrenergic receptors?
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1.Vasodilation
2. Bronchial smooth muscle relaxation 3. GI relaxation |
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Bethanechol, Carbachol and Pilocarpine are all what?
Which is the odd one out of the three? and why |
1.Muscarinic agonists
2. Carbachol- also stimulates both Muscarinic and Nicotinic |
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Effects of Parasympathetic in the Eyes?
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1. Miosis
2. Reduces intraocular pressure |
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Drugs that will cause Miosis and reduce intraocular pressure?
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Bethanechol, carbachol
most importantly Pilocarpine |
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What is the effects of alpha-adrenergic agonist on the cilliary muscle?
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None (it will contract just the iris radial m.causing mydrasis)
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What are the therapeutic effects of most Parasympathetic drugs?
Eyes GI Urinary tract |
1. Eyes - Glacoma (increase incidence of caratact)
2. GI - improves peristalsis (esp after surgery, gastric atony and postoperative abdominal distention) 3. Urinary tract - Improves urination 4. |
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What parasympathetic M. agonist can be used to diagonose Brochial hypersensitivity and asthmatic condition (constrict the bronchials)
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Methacholine
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What primary drug is used for the treatment of Open-angle glaucoma?
Any others used? |
1. Pilocarpine
2. Carbachol is used if pilocarpine is ineffective 3. B-adrenergic receptor antagonist (timolol and betaxolol) Or CA inhibitor - Acetazolamide |
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Ach agonists are contraindicated in what conditions?
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1. Asthma
2. Heart disease 3. Peptic ulcer (increase secretions) 4. Parkinsonian disease (increase Ach) |
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What is Edrophonium?
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Short acting AchE inhibitor. Used in the Tensilon test for Mys. Gravis diagnosis
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Difference between Neostigmine and Physotigmine?
What are they? |
1.Neostigmine - poorly absorbed (GI, negligible in CNS)
Physotigmine - Well absorbed (GI,Enters CNS) 2. Reversible Long acting AchE |
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Name 2 irreversible Long acting AchE inhibitor?
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1. Echothiophate and Isoflurophate
Echo is poor absorbed Isoflurophate is highly lipid solube and well absorbed even in skin |
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Name the antidote for insecticide or nerve gas poisoning (Ach E reactivator)?
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Pralidoxime (but ineffective in CNS)
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What parasympathetic drugs cause mydrasis (pupil dilation) and cycloplegia(loss of accomodation and paralysis of ciliary muscle)?
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Muscarinic -receptor antagonist e.g Atropine,Scopolamine et.c
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Is Atropine short or long acting - Muscarinic Receptor anatgonist?
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Long acting
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For each organ system list the therapeutic importance of Muscarinic Antagonist
Eye Heart Stomach GI Urinary CNS (2 things) |
1. Eye - Opthalmoscopic exam
2. Heart- Acute MI with bradycardia 3. Stomach - Treat peptic ulcer (reduce acid) but there are better drugs now 4. GI - mild diarrhea 5. Treat Urinary Urgency 6. Parkinsonian and Motion Sickness |
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what is difference between Tubocurarine, succinylcholine and Trimethaphan?
What do they all have in common? |
1. Succinylcholine is an Nictotinic depolorizing agonist
Tubocurarine and Trimethaphan are both Nicotininc antagonist 2. All are Neuromuscular blockers (Trimethaphan - blocks just the ganglionic nicotinic Receptors) |
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What is another drug you can use for Ach E inhibitor poisoning (aside from AchE regenrator Pralidoxime)?
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Atropine (Muscarinic blocker)
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Reversibly what classes of drugs can be used to treat Muscarinic antagonist (Atropine, scopolamine) overdose?
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Physostigmine(tertiary, e.g atropine) and Neostigmine (quaternery)
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what ANS system does Ganglionic block drugs (ganglionic nicotinic antagonist)?
Can they be used for what? may cause what? Name a drug with this properties? |
1. Non depolarizing blockade of both P-ANS and S-ANS
2. Decrease blood pressure (by reducing sympathetic tone in vasculature) 3. Trimethaphan |
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Trimethaphan - is what kind of drug?
Simulates the release of ------ and causing -----, -----, ----. |
1. Peripheral ganglionic nicotinic blocker.
2. Histamine, and causes Flushing, dizzines and headaches |
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Name types of muscle relaxants and give a few drug examples?
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1. Neuromuscular junction blocker - Ach R antagonist
A. Depolarizing:Succinylcholine B. Non-depolarizing: Tubocurarine 2. Spasmolytic drugs - mimic GABA in the CNS (Benzodiazapine) or some drugs interfere with release of Ca2+ in skeletal muscle (Dantrolene) |
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Tubocurarine, Atracurium, mivacurium, Pancuronium,Vecuronium and Rapacuronium are all -------- ?
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Non-depolarizing Neuromuscular blocking drugs (muscle paralysis)
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Name a drug - that will be great for muscle paralysis (but note they have to be on a mechanical ventilator or else respiratory failure)?
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Depolarizing or Non-depolaring neuromuscular blockers.
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What is the problem with Neuromuscular blocking drugs?(hint not at NMJ)
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1. Histamine release: may cause vasodialation and bronchospasms
2. Prolonged apnea (paralysis) |
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Name two drugs that may potentiate the effects of NMJ (nicotinic) blockers? (because they inhibiting Ach release)
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1. Aminoglycoside
2. Lincomycin |
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Is Succinylcholine broken down by AchE?
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1. Yes but much slower.
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Describe the reversal of succinylcholine blockade
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1. Phase 1: due slow metabolization of succinylcholine
Muscle is depolarized(inital contraction), then flaccid paralysis 2. Phase 2: In repolarization, Ach still has no effect on the AchR. |
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Adverse effects of succinylcholine?
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1. Hyperkalemia
2. Malignant hyperthermia (likely to occur than succinylcholine than Halothane) |
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Tx of Malignant hyperthermia?
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Dantrolene
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1. Name a spasmolytic drugs?
2. Best used for? 3. Name their Mechanism and primary target site? |
1. Dantrolene and Baclofen
2. Spasms (seen in cerebral palsy, MS, stroke) Muscle paralysis: Malignant hyperthermia 3. Ca2+ release in SR(dantrolene)and GABA-receptor (Baclofen) Benzodiazepine also fall in this group (their main func is sedation and antianxiety) |
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Properties of beta 1 receptors?
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increase the rate and force of heart contractions (by increasing the conduction in the AV node and lowers refractory peroid).
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Name a spasmolytic drugs? Best used for? Name their primary target site?
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1. Dantrolene and Baclofen
2. Spasms (seen in cerebral palsy, MS, stroke) Muscle paralysis: Malignant hyperthermia 3. Ca2+ release in SR(dantrolene)and GABA-receptor (Baclofen) Benzodiazepine also fall in this group (their main func is sedation and antianxiety) |
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Name drugs used to reduce intraocular pressure by the reduction of aqueous humor production?
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Epinephrine and B-receptor antagonist
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Why at low doses of epinephrine do we not get reflexive tachycardia?
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1. Increase in Heart rate (Beta1) and vasodilation (Beta1 -reduction in TPR)
= No change in mean blood pressure (HR increased, increased systolic, low diastolic) |
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Is NE used therapeutically?
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Nope - not really
(has less beta2 activity - so increase TPR and increase diastolic) |
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Name the main Beta1 agonist?
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Isoproterenol and Albuterol (same effect on Beta2)
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Name the main 3 Beta non-selective agonist drugs?
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1. Isoproterenol
2. Albuterol 3. Dobutamine |
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Why is albuterol great for asthma?
Name other drugs like it? |
1.Because it works mostly on the Beta2 receptors (lungs and blood)
Beta 2agonist 2. Terbutaline (emergency drug for status asthmaticus), Albuterol |
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Distinguish the potency of each drug on Beta 1 vs Beta 2
Dobutamine Isoproterenol Albuterol (Terbutamine) |
Dobutamine: B1>B2
Isoproterenol: B2=B1 Albuterol (Terbutamine): B2>B1 |
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Name a common alpha-adrenegic agonist and function?
Potency is greater for which alpha receptor? |
1.Phenylephrine
2. Increase TPR by vasoconstriction 2. a1>a2 |
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What is Clonidine? The clinical effect of this drug?
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1.alpha2 prejunctional agonist (reduces the release of NE)
2. Lower BP |
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What drug will you like to use in short-hypotensive emergencies?
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1. Norepinephrine
2.Epedrine |
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What drug will you like to use in Cardiogenic or septic shock? Why?
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1. Dobutamine
2. Dopamine - Increases CO,HR (B1), low vasoconstrictive - Dopamine especially for the renal perfusion (D1). |
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What Catecholamine might you use for the treatment of anaphylactic shock?Why
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1.Epinephrine
2. Reverse the hypotension and angioedema and maintain BP |
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What Drug might you use for Congestive heart failure?
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Dobutamine (apparently it stimulates B1 but the contractility property as opposed to the Heart Rate as seen with Isoproterenol)
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For Temp. emergency treatment of cardiac arrest and heart block (Stokes-Adams syndrome)? Why
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Isoproterenol and Epinephrine because they increase ventricular automaticity and rate and increase AV conduction via B1
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What drug is used for the diagnosis of Horner's syndrome?
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Hydroxyamphetamine (miosis, anhydrosis)
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What drug can be used to relax the Uterus and suppress premature labor?
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Terbutaline (beta2 agonist) and Ritodrine
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Name some alpha antagonist? Main therapies?
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1. Phentolamine (a1=a2)
2. Prazosin (a1) 3. Phenoxybenzamine (irreversible a1 antagonist) A. Hypertension B. Pheochromocytoma |
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Difference between Phentolamine, Phenoxybenzamine (a) and Prazosin, Terazosin,doxasin (b).
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a.The former are non-selective alpha antagonist
b. a1 selective antagonist |
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What drugs will you use to treat essential hypertension, urinary rentention in BPH and Raynaud's phenomenoma?
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Prazosin, Terazosin and Doxazosine
(all a1 selective antagonist) Relax the bladder, vasodilated the blood vessels peripherally |
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What is a key side effect of prazosin, terazosin and doxazosin?
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Postural hypotension
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What are the cardiovascular effects of Beta-antagonist?
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1. Lower blood pressure
A. reduce HR B. Shorten AV node time and supress automaticity C. May Increase TPR D. Reduce Renin release |
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What are the respiratory and ocular side effects of Beta antagonist?
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1. Increase airway resistance
2. Reduce intra ocular pressure (Timolol used for glaucoma) |
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What are the Endocrine and metabolic side effects of Beta antagonist?
Why should we becareful with the use of propanolol in diabetics? |
1. Decrease lipolysis
2. Decrease Gluconeogenesis (may increase the hypoglycemic effects of insulin) 3.Propanolol should be used carefully with diabetics. May mask tachycardia due to hypoglycemia |
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What drug long-term treatment of hypertension?
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1. Propranolol (not useful for hypertensive crisis)
With other drugs -diuretics and low salt diet |
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What drug is used to treat Supraventricular and ventricular arrhythmias?
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Propanolol
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1.Hexamethonium is what type of drug?
2.Why would Hexamethonium not cause Reflex tachycardia? |
1. Nicotinic antagonist
2. Will cause vasodilation but also inhibit the baroreceptor functions. |
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What drug prevents the reuptake of choline in cholinergic cells?
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Hemicholinium
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What drug prevents the conversion and packaging of Dopamine to Norepinephrine - in noradrenergic nerves?
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Reserpine
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What drug inhibits the release of NE? What drug cause the release of NE?
What drugs (2) blocks the reuptake of NE? |
1. Guanethidine
2. Amphetamine 3. Cocaine and TCA (tricyclic antidepressants) |
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What the Si/Sx of AchE inhibitor poisioning? DUMBBELSS
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Diarrhea and Urination
Miosis and Bronchospasm Bradycardia and Excitated skeletal m. Lacrimation and Sweating and Salivation |
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Which Diuretics cause
Acidosis? Alkalosis? |
1. Acidosis: Loop diuretics and Thiazides
2. Alkalosis: Carbonic anhydrase and K+ sparing diuretics |
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What drugs are similar in mechanism to Thiazides but are more potent?
How may they be better than thiazide? |
1.Quinazlinones and Indolines
2. May be effective in the presence of some renal impairment |
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Summary of the therapeutic benefits of thiazide?
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1. Prefered Tx: HTN in with nl renal func
2. Ca2+ stones: idiopathic hypercalciuria 3.Diabetes insipidus 4. Combo (edema,cirrhosis or nephrotic) |
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What type of diet is recommended for a patient on thiazide?
To avoid what Six/Sx of hypo-K,Hypo-Na,Hypo-Cl? |
1. Diet high K+
2. CNS disturbances, cardiac arrhythmias and increased sensitivity to digitalis |
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Does thiazide help with Gout Sx?
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No, may increase Urate serum levels
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What is the effect of thiazide in patients with diabetes?
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May cause hyperglycemia
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Give me an example of a "high ceiling diuretic"
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Loop diuretic
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1.What transporter is blocked by loop diuretics and location of action?
2. What key electrolytes are lost? 3.Clincially used for? |
1.Na+,K+,2Cl- of the Thick ascending limp of loop of henle.
2. Na,K,Cl and Ca2+ and Mg+ 3. Edema,HTN,Hyper-Ca2+ |
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Loop diuretics causes dose -related ototoxicity - So with this property what will be a bad combination with loop diuretic?
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Loop diuretic(furosemide, erthacryin) and Aminoglycosides
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Name the 2 types of K+-sparing drugs and examples of them?
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1. Aldosterone inhibitor-spirolactone
2. non-Aldosterone inhibitor - Amiloride and Triamterene |
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What are the adverse effects of all the K+ sparing agents?
Spirolactone-specific side effects? |
1. Hyper-K
2. Hyper-K, Endocrine effects (gynecomastia, antiandrogen efxs) |
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Location of receptor of adolsterone and spirolactone?
Location of the receptor for Amiloride and Triamterene? |
Both in the cortical collecting tubule.
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What electrolytes are involved when Spirolactone is used?
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K and H secretion is prevented
Na reabsorption is prevented Serum pic: Hyper-K, Metabolic acidosis, and Hypo-Na |
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Mechanism of Amiloride and Triamterene?
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Prevents just Na+ reabsorption and prevents K+ excretion
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Name the drug used for glaucoma, Urinary alkalinization, metabolic alkalosis and altitude sickness?
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Carbonic Anhydrase (sulfonamide derivatives)
CA prevents the exchange of H+, with Na+ and HCO3- |
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Name an important Carbonic Anhydrase?
Side effects? |
1. Acetazolamide
2. M. Acidosis, NH3 toxicity, Hyper-Cl, sulfa allergy |
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Name a few Osmotic agents
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Mannitol, glycerin and isosorbide
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Mannitol contraindicated in what?
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Anuria and CHF (may cause pulmonary edema)
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Name an ADH analog
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Vassopressin and Desmopressin
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Clinical use of ADH?
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Central Diabetes insipidus and Nocturnal enuresis
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Name drugs that increase the release of ADH? and enhance the action of ADH?
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1.Clofibrate (increase ADH release centrally)
2.Chlorpropamide, Acetominophen, indomethacin(by reducing the production of PGE and enhance the action of ADH) |
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Name the alpha agonist used for glaucoma?
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Epinephrine (outflow, mydriasis) and Brimonidine (decrease synthesis)
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what family of drugs will cause decreased aqueous humor production?
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1. Bromonidine (alpha agonist)
2. Beta-blockers - Timolol, betaxolol, Carteolol |
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What will cause increase outflow of aqueous humor in glaucoma tx?
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1. Epinephrine (as an alpha agonist)
2. Cholinomimetics: Pilocarpine, Carbachol, Physostigmine,echothiophate 3. Prostagladin - Latanoprost (darkens the color of iris) |
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what is used for glaucoma by increasing outflow - it darkens the iris(browning)?
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Prostagladin - Latanoprost
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Amantadine is used for influenza but it is also used for another condition?
Mechanism? |
1. Parkinson
2. Increases the release of dopamine |
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Name an MAO type B inhibitor for the Tx of Parkinson?
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Selegiline
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Why use Benztropine in Parkinson?
What are the therapeutic effects? |
1.To inhibit Ach effect.
2. Improves tremor and rigidity ( no effect on bradykinesia- slow movement) |
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Aside from Malignant hyperthermia - what is Dantrolene is for clinically to treat? (also dopamine agonist)
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Neuroleptic malignant syndrome - rigidity, autonomic instability, hyperpyrexia
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