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34 Cards in this Set
- Front
- Back
Drugs to Avoid in Pregnancy
SAFE Moms Take Really Good Care |
Sulfonamides (kernicterus), Aminoglycosides (ototoxic), Fluoroquinilones (cartilage damage), Erythromycin (acute cholestatic hepatitis), Metronidazole (mutagenic), Tetracycline (discolored teeth), Ribavarin, Griseofulvin, Chloramphenicol (gray baby)
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Volume of Distribution
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Vd= amount of drug in body / plasma drug concentration
If bound to plasma proteins, this is altered in liver disease |
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Clearance
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CL= rate of elimination / plasma concentration
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Half Life
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t1/2= [0.7 * Vd] / CL
If infused at a constant rate, it reached 94% of steady state in 4 t1/2 |
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Dosage Calculation
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Loading Dose = Desired Conc * [Vd/bioavailability]
Maintainance Dose= Desired Conc * [Clearance/Bioavailability] In pts with Renal/Liver disease, the loading dose is constant, it's the maintainance dose that decreases |
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Zero Order Elimination
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Cp (plasma conc) falls at a steady rate no matter what the starting point (linear decrease)
Ex- EtOH, Phenytoin, Aspirin |
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First Order Elimination
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Rate of elimination is proportional to concentration (faster at high concentration, slower at low) -- exponential curve
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Excretion occurs in 2 phases
Phase 1 occurs in ____ and yields _____. An example is the ______ system Phase 2 uses ______ and yields _______ |
Liver
Oxidized and Reduced compounds that are slightly polar and still active Cyt p450 System Acetylation, Glucuronidation Very polar substances that are inactive |
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Competitive Antagonist
Will shift the curve to the _____ |
To achieve the same % maximum effect req's a higher dose --> curve shifts to the right
Still able to achieve 100% max effect |
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Irreversible Antagonist
Will shift the curve ______ |
Decreases the % maximum effect --> shifts the curve downward.
Even at high concentrations of the drug, it cannot overcome the antagonist and it's effect is decreased |
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EC(50) vs Kd
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Kd= dose req'd to occupy 50% of all receptors
EC(50)= dose req'd to get 50% of maximum effect --> this is most imp't clinically EC(50) < Kd means that there are "spare receptors" or less than 50% receptors need to be occupied for activity |
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Potency
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Dose req'd to get an effect...it is independent of full or partial agonist
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Full agonist v Partial Agonist
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Partial Agonist is never able to reach the same maximum effect as a Full Agonist (it has lower efficacy). However, the partial agonist can be more potent.
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Therapeutic Index
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TD50/ED50
Dose to get 50% people sick/ Dose to get 50% people better Narrow Index= lower dose causes more toxic effects compared to therapeutic Large Index(desirable)= need a higher dose to cause toxicity compared to effective dose |
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Guanylate Cyclase q receptor
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HAV 1 M&M
H1, alpha 1, V1, M1, and M3 |
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Guanylate Cyclase i receptor
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MAD 2's
M2, alpha 2, D2 |
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Guanylate Cyclase s receptor
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B1, B2, D1, H2, V2
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Cholinomimetics (Direct Agonists)
1)Bethanechol 2)Pilocarpine |
1) Used for post-op ileus and bladder retention (Bowel and Bladder)
2)Used for Glaucoma by opening the angle via cilary muscle contraction and by dilating the pupilary sphincter. Works on narrow angle and open angle |
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Cholinomimetics (Indirect via AChE inhibition)
1)Neostigmine 2)Pyridostigmine 3)Edrophonium 4)Physostigmine 5)Echothiophate |
1) Myasthenia gravis, post-op reversal of neuromuscular blockade
2)Myasthenia gravis 3)Short acting, used to diagnose Myasthenia gravis 4) Glaucoma -->able to cross BBB and Atropine overdose 5)Glaucoma |
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Signs of Cholinesterase Poisoning
DUMBBELSS Caused by Parathion and Organophosphates |
Diarhhea, Urination ,Miosis, Bronchospasm, Bradycardia, Excitation of muscles, Lacrimation, Sweat, Salivate
Trt- Atropine (blocks muscarinic receptors) and pralidoxime (regenerates AChE) |
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Cholinoreceptor Blockers
1)Atropine,Homatropine 2)Benztropine 3)Ipatropium |
1) Used in eye to cause Mydriasis (dilation) and cycloplegia(can't focus)
2)Used in CNS for Parkinson's (blocks indirect pathway) 3) Used in Lungs for Asthma/COPD |
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Atropine
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MOA= muscarinic anatogonist
Blocks Salivation, Lacrimation, Urination, and Defecation Toxic= Hot, Dry, Red Flushed Skin, Vision problems, Disorientation |
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Hexamethonium
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MOA= Blocks nicotinic receptors
Use= used to block vasovagal response to prevent reflex bradycardia with NE increase BP |
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Epinephrine
1)receptor specificity 2)Low Dose 3)High Dose 4)Uses |
1) Beta>Alpha but more Alpha receptors in body
2) Binds only Beta receptors causing inc HR,Contractility via B1, but also Vasodilation via B2 --> no change in Blood Pressure 3) Mostly alpha receptor effects--> vasoconstriction causing increased BP....prevented by giving Alpha Blocker previously leading to decreased BP (Epi reversal) 4) Anaphylaxis, open angle glaucoma, asthma (B2 stim), hypotension |
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NorEpi
1)receptors 2)Effects 3)Pretreat with Alpha blocker 4)Uses |
1) Alpha1 > Beta 1
2) causes increased vasoconstriction along with increased contractility leading to massive increase in BP --> reflex bradycardia 3)Will prevent pressor effect but no reversal to depressor like Epi 4) Hypotension |
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Isoproterenol
1)receptors 2)effects |
1) only B1 and B2
2) decreases BP via B2 leading to reflex Tachy |
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Dopamine
1)Receptors 2)Effects 3)Use |
1) D1=D2>Beta>Alpha
2)Low Dose= Renal vasodilation to help in cardiac shock Med Dose= increase HR High Dose= Increase Vasoconstriction to Inc BP 3) Cardiac Shock, Heart Failure |
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Ephedrine
1)MOA 2)Use |
1)increase release of stored catecholamines
2)nasal decongestion, urinary incontinence, hypotension |
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Phenylephrine
1)MOA 2)Uses |
1)Acts on Alpha receptors
2)Dilates pupil, vasoconstrictor, nasal decongestion |
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Albuterol
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B2 agonist used in Asthma
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Clonidine and Methyldopa
1)MOA 2)Use |
1)Binds alpha 2 receptors in CNS to prevent catecholamine outflow
2) Hypertension in pts with renal disease because it won't decrease renal blood flow |
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Nonselective Alpha Blockers
1) Irreversible is ____ 2) Reversible is ______ 3) Used to trt 4) Toxicity |
1)Phenoxybenzamine
2)Phentolamine 3)Pheochromocytoma 4)Hypotension with reflex tachy |
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Alpha 1 blockers
Prazosin, Terazosin |
1) used in hypertension, urinary retention from BPH
2)can cause 1st dose hypotension and dizziness |
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Beta Blockers
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All that start with A-->M are selective for B1 receptor (safe in asthmatics)
Used to lower BP, lower HR, slow CHF progression, lower Aqueous humor production (Glaucoma) Toxicity- Impotence, Bradycardia, sedation, can cause hyperglycemia in Diabetics |