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2 Ach agonists used for Glaucoma
- Carbachol
- Pilecarpine
- MOA: ciliary muscle contraction--- increase outflow thru the canal of schlemm
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2 Beta antagonists used for Glaucoma
- Betaxolol
- Timolol
- MOA: block NE at ciliary epithelium--decrease aqueus humor formation
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Ach esterase inhibitor?
- ecothiophate
- MOA: increase outflow
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Sympathomimetic drug for Glaucoma?
- Apraclonidine Apha 2 agonist--
- MOA: deacrease NE realease at the presynaptic junction
- Epinephrine
- MOA: increase OUTflow
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Carbonic anhydrase inhibitor for Glaucoma?
Acetozolamide, Dorzolamide--decreases HCO3 formation leading to deacreased Acqueus humor formation
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PGF2 apha analog for Glaucoma?
Latanoprost
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Inhibitor of choline at the nerve ending?
Hemicholinium
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ACh antagonists used for Asthma?
- Metaproterenol
- Albuterol
- Salmeterol
- Terbutafine
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MOA of Botulinum toxin?
inhibits Ach release from the presynaptic membrane
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What receptors signal thru the q arm of the G protein?
H1,alpha1, V1,M1,M3
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What is the signalling cascade for the q arm of the G protein?
- + phospholipace c--- + IP3--- +Ca
- --- + DAG---- + Protein Kinase C
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What receptor signal thru the inhibitory arm of the G protein?
M2, Apha2, D2
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What is the signalling cascade of the Inhibitory arm of the G protein?
--- -AC----- -cAMP ----- -Protein Kinase A
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What receptors signal thru the stimulatory arm of the G protein?
Beta1, Beta2, H2,V2, D1
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What is the signalling cascade of the stimulatory arm of the G protein?
--- +AC---- + cAMP ---- +Protein Kinase A
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Antidote for Heparin toxicity?
Protamine Sulfate
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Antidote for warfarin Toxicity?
- Vitamin K
- Fresh Frozen Plasma
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Warfarin inhibits synthesis of what clotting factors?
2,7,9,10, protein C, Protein S
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Heparin inhibits the synthesis of what clotting factors?
7, 9, 10, 11, 12
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Antidote for cholinesterase inhibitor poisoning?
atropine + pralidoxime (regenerates AchE)
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Irriversible acetylcholine esterase inhibitor?
malathion, parathion--Insecticides
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cholinestarase inhibitor used for Urinary Retention?
Neostigmine
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Cholinestarase inhibitor used for glaucoma?
ecothiophate
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Ach agonist used for asthma diagnosis?
methacholine
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MG diagnosis (short acting cholinesterase inhibitor)
edrophonium
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Ach agonist used for MG (long lasting)
Pyridostigmine
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Insecticides contain what 2 acetycholine esterase inhibitors?
malathion, parathion
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2 acetylcholine esterase inhibitors used for Glaucoma?
- physostigmine
- ecothiophate
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What are the effects of acetylcholine inhibitor poisoning?
- Diarrhea
- Urination
- Miosis
- Bronchoconstriction
- Bradycardia
- Excitation of the CNS
- Lacrimation
- Salivation
- Sweating
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Nicotinic receptor agonist?
Nicotine
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Muscarininc receptor direct agonists?
- Methacholine
- Pilocarpine
- Bethanecol
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Bethanecol is used for activation of what?
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Nn receptor antagonist?
- mecamylamine
- Hexamethonium
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Nm receptor antagonist?
- tubocurarine
- atracurium
- succinylcholine
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Benztropine used for what?
Parkinsons--PARK my BENZ
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Scopolamine used for what?
Motion sickness
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Ach antagonist used for asthma?
Ipratropium
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Nicotinic receptor stimulation at the adrenal Medulla causes what?
release of epi and Norepi
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Nicotinic stimulation at the autonomic ganglia causes what?
Stimulation
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Nicotinic stimulation at the NMJ causes what?
sk. muscle contration
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Ach at the Nn and Nm signalls how?
Na/K activation
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What 2 effects does Ach have on the eye?
- sphincter muscle contraction
- ciliary muscle contraction
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What effect does ach have on the SA and AV node?
- SA node--decreases stimulation
- AV node--decreases conduction velocity
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What effect does Ach have on the purkinje fibers and ventricles?
no effect
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Where is M1, M2, M3 found in?
- M1---GI glands and CNS
- M2- CVS
- M3--Lungs, GI, GU, Glands, BV
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What effect does M3 receptor binding of Ach have on the bladder?
Detrusor muscle and sphincter stimulation
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What are the 7 different locations for Ach receptors in the body
- 1. eye
- 2. sweat, lacrimation, gland secreations
- 3. BV
- 4. Heart
- 5. Lungs
- 6. GI
- 7. GU
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Tx for ileus and urinary retention?
Bethanechol
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Diagnosis of bronchial Hyperactivity?
methacholine
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Ach agonist treatment for glaucoma?
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Ach agonist Tx for Xerostomia?
Pilocarpine
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What acetycholine esterase is used for atropine overdose?
Physostigmine
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What ach agonist and acetylcholine esterase inhibitor is used for ileus and urinary retention?
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Tertiary amine?
Physostigmine
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Quaternary amine?
- Neostigmine
- pyridostigmine
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Reversal of nondepolarizing NM blockers i.e tuburocurarine, atriacurium, succinylcholine
- Neostigmine
- Pyridostigmine
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acetylcholinesterase Inhibitors used for Alzeimers?
- Rivastigmine
- Galantamine
- Tacrine
- Donezepil
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Acetycholine esterase inhibitor used for Glaucoma?
ecothiophate
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irriversible acetylcholine esterase inhibitors?
ecothiophate, malathion, parathion
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What drugs are contraindicated in Glaucoma?
anticholinergic
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Atropine O'D is treated with what acetylcholine estersase inhibitor?
Physostigmine
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What is given during anesthesia to block bradycardia?
anticholinergic i.e atropine
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Tropicamide, Atropine, Homatropine produce what effect?
mydriasisn cycloplegia
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Glycopyrrolate is used for what?
peptic ulcer treatment, antispasmodic
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Trihexphenidyl, benztropine are used for what?
Parkinsons
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In dually innvervated organs, which arm of the ANS predominates and is thus blocked?
parasympathetic
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Where is sympathetic activity predominant and thus blocked?
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What effect would a nicotinic antagonist such as hexamethonium have on
Heart
Pupil
GI
Gu
Salivary Glands
- Heart--tachycardia
- Pupil-mydriasis
- Constipation
- Urinary retention
- xerosthomia
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What effect would hexamethonium have on
Arterioles
Veins
Sweat Glands?
- Arterioles--dilation
- Veins--dilation, decreased venous return
- Sweat Glands--anhydrosis
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What are 2 ganglionic blockers?
- hexamethonium
- mecamylamine
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Tx for malignant hyperthermia?
MOA?
- Dantrolene
- Ca channel blocker
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What does amphetamine do to the slopw of epinephrine?
potentiates it, so it shifts it to the left
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What ach agonist is used for the sweat test in CF?
Pilocarpine
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Ach esterase inhibitors have muscarinic effects of muscarinic agonists, except in what location?
BV- bc they are not innervated so Ach esterase is absent , so the drug cannot block it and increase Ach levels
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What is a cholinergic crisis?
Nicotinic receptors are desenthysized
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How is a cholinergic crisis differentiated from MG?
- if endrophonium improves the symptoms then its MG
- if endrophonium doesn imporove symptoms--then it is cholinergic crisis
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What is the significance of a tertiary and quarternary Ach esterase inhibitors?
- tertiary are unionized so cross BBB-CNS effects
- Quarternary--are ionized---cant Cross BBB
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Antidote for Atropine O'D?
physostigmine
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Antidote for depolarizing NMJ drugs i.e tubocurarine, atracurine,
- Neostigmine
- Pyridostigmine
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Taking too much of Ach esterase inhibitors can result in what kind of crisis?
cholinergic crisis
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Sarin is an example of what type of inhibitor?
non competitive/irriversible cholinesterase inhibitor poisoning
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Phosphorylation usually occurs at what aa?
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What are the 3 C's of anti-muscariniv O'D?
- Cardiotoxicity
- Convulsions
- Coma
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What are 2 drugs used for motion sickness?
- antihistamines
- scopolamine
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What are the drugs that have anti muscarinic effects?
- Amantadine
- Merepidine
- antiPsychotics
- antiHistamines
- Quinidine
- TCA
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2 Drugs used for dyskinsia in Parkinsons diseas
- Trihexphenidyl
- Benztropine
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What drug prevents conversion of tyrosine to Dopa?
methytyrosine
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Alpha 2 receptors have what effect on the NE?
inhibits the release of NE
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Which receptors are more sensitive to stimulation, alpha or beta?
beta
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Indirect sympathomimetic that releases the mobile pool?
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Indirect sympathomimetic that blocks NE reuptake?
Cocaine, TCA
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What 2 receptors block the release of NE from the presynaptic membrane?
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What receptor stimulates the release of NE from the presynaptic membrane?
ATII
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Which MAO metabolizes NE, 5HT and Tyramine?
MAO A
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Which MAO metabolizes Dopamine?
MAO B
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MAO A inhibitors?
- phenelzine
- Tranylcypromine
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MAO B inhibitor?
Selegiline
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Selegiline is used for what condition?
Parkinsons
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What enzyme metabolizes NE and dopamine at the post junctional membrane?
COMT
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A COMT inhibitor used in Parkinsons?
entacapone
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What drug blocks the reuptake of NE from granular pool?
Reserpine
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What drug inhibits the release of NE from the Granule Pool?
Guanethedine
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Presynaptic alpha 2 agonist?
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Alpha 1 receptors are found where?
- Veins--constriction--Increased VT/Diastolic pressure
- Arteries--constriction--increased TPR/Systolic pressure
- Radial muscle of Eye
- GI and bladder Sphincter
- Decrease Insulin Release
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Alpha 2 receptors have what function?
inhibit NE release/anti sympathetic
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Beta1 receptors are found where?
- Brain
- Heart-SA, AV node, atria, ventricle, purkinje fibers
- Increase Renin release
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B2 receptor found where?
- bronchioles
- BV
- Uterus
- Increase Liplysis, glucoenogenesis, Glycogenlysis, insulin
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Whats an example of a TOCOlytic Receptor?
B2
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Which adrenergic receptor will cause reflex bradycardia?
Beta 2
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D1 receptors are found where?
- renal artery--vasodilation--maintain GFR
- in high conc. acts on B1--incrases contractility and alpha1 increases TPR all raising BP in hypotension
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At low does of adrenergic agonist, what receptors are activated?
At high doses?
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Alpha 1 agonist used as a decongestant?
Metazoline
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2 alpha 2 agonists
- clonidine
- alpha methyl dopa
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Beta 2 agonists?
- Metaproterenol
- Albuterol
- Salmetrol
- Terbutafine
- ritodrine--tocolytic
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Beta 2 agonist used as a tocolytic?
ritodrine
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Dobutamine is more selective for what receptor?
Beta 1
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Isoproterenol is specific for what adrenergic receptor?
beta 1 and beta 2
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What beta 2 agonist is used for asthma prophylaxis?
salmeterol
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What is used for treatment of acute asthma?
Albuterol
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Doputamine is used for what?
CHF
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Norepinephrine is selective for what receptors?
alpha1, alpha2, beta1
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What reflex is seen with norepinephrine?
reflex bradycardia
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Epinephrine is selective for what receptors?
alpha1, alpha2, beta1, beta2
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Epinephrine in low doses is more selective for what receptors?
in large doses?
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What reflex is seen with low doses of epinephrine?
no reflex bc beta1 increases HR but beta2 decreases TPR so the actions offset eachother
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What is the reflex with large doses of epi?
beta 1 is stimulates so u get increased HR but alpha 1 increases TPR so you get reflex bradycardia
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What alpha 1 agonist is used for nasal decongestant?
phenylephrine
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what is used for paroxysmal atrial tachycardia?
methoxyamine
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How does epi reversal work?
giving an alpha blocker you go from hypertension to hypotension
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What drug produces a hypertensive crisis with MAO inhibitors?
Tyramine
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Amphetamines and ephedrine have what effects?
Release of NE from the mobile pool
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How does ephedrine produce a decongestant effect?
ephedrine--- + NE-----vasoconstriction via alpha
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How does cocaine produce its effects?
blocks reuptake of NE, 5HT, Dopamine
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How is cocaine a local anesthetic?
blocks Na+ channels, prevents depolarization
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Dopamine at low doses has what effects?
acts on D1 on the kidney, maintainsRBF and GFR
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Dopamine at medium levels has what effects?
acts on D1 and Beta1 increases CO
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Dopamine at high levels has what effect?
- stimulates beta1 and alpha1
- Vasoconstriction and increases CO
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Alpha agonist that is a nasal decongestant?
Metazoline
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Reversible Alpha1 and Alpha2 antagonist?
phenylamine
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Irriversible alpha1 and alpha2 antagonist?
phenoxybenzamine
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Which alpha 1 and 2 antagonist is used in Pheochromocytoma?
Phenoxybenzamine
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Alpha 1 antagonist?
Prazoncin, Doxazocin, Terazocin
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Alpha1 antagonist used for BPH?
Tamsulosin
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Alpha 2 blockers?
Yohimbie
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Yohimbie is used for what?
postural hypotension, impotence
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Mirtazapine is used for what?
depression
-
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Doxazopin
Prazosin
Terazosin
are use for what?
-
Beta blockers used for Glaucoma?
-
nonselective beta blocker?
propranolol
-
2 Alpha and beta antagonists?
-
Beta1 cardioselective antagonists?
- acebutolol
- metaprolol
- atenolol
-
Beta blocker for CNS depression?
propranolol
-
Side effect of propranolol?
increased LDL and TGs
-
Beta blockers with intrinsic sympathetic activity?
-
What Beta blockers do not cross the BBB?
-
How would a beta1 blocker bloc the effects of hypoglycemia?
- in hypoglycemia you get tachycardia
- with a b blocker the tachycardia stimulus is stopped
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Why do you get tachycardia, angina, arrythmias after an abrupt withdrawal of beta blockers?
bc beta receptors are upregulated so they get over stimulated and produce increased sympathetic tone
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What stimulants are contra indicated in MAO inhibitor use?
- tyramine-wine, cheese
- ephedrine
- amphetamines
- All release NE stored in the Mobile pool
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Why do people get perforated nasal septum?
cocaine ---- + NE release + vasoconstriction --+ ischemia ---+ tissue death=perforated septum
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