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60 Cards in this Set
- Front
- Back
Vd= ?
-drugs with low Vd distribute where? -medium Vd? -high Vd? |
Vd=(amt of drug in body)/(plasma drug conc)
-low Vd==>plasma -med Vd==>extracellular space -high Vd==>tissue |
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Clearance of drug =
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Cl of drug
= (drug elimination rate)/(plasma drug conc) =Vd x Ke (elimination constant) |
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drug half-life
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=time req to change amt of drug in body by 1/2 during elimination or during constant infusion
half-life = (0.7 x Vd)/Cl |
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how fast does drug infused at constant rate reach steady state?
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drug infused at constant rate will reach 94% of steady state in 4 half-lives.
1 half life= 50% 2 half lives=75% 3 half lives=87.5% 3.3 half lives=90% 4 half-lives=94% |
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loading dose=
-what happens in pts w/impaired renal or hepatic fxn? |
[target plasma] * Vd/F
(F=bioavailability=1 via iv) -in pts w/impaired renal or hepatic fxn, loading dose is the same (b/c Vd is the same), but maintenance dose is decr (b/c Cl is decreased) |
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maintenance dose=
-what happens in pts w/impaired renal or hepatic fxn? |
[target plasma] * Cl/F
(F=bioavailability=1 via iv) -in pts w/impaired renal or hepatic fxn, loading dose is the same (b/c Vd is the same), but maintenance dose is decr (b/c Cl is decreased) |
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drugs w/zero-order elimination?
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(at high/toxic doses) ethanol, phenytoin, aspirin
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most drugs are elimination by zero or first order elimination?
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first order (constant FRACTION (vs. amount) eliminated per unit time)
zero order=(at high/toxic doses) ethanol, phenytoin, aspirin |
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what receptor and G protein:
increases VSM contraction |
a1 & V1
q (for both) "HAV 1 M&M3, q" |
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what receptor and G protein:
decr sympathetic outflow? |
a2
i (MAD2's "i"nhibit cAMP) |
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what receptor and G protein:
decr insulin release |
a2
i (think "i" for "i"nhibit): "MAD 2's [M2, A2, D2] inhibit cAMP" |
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what receptor and G protein:
incr HR |
B1
s (think "s" for "s"timulate) Tip: if the receptor not in the other mneumonics ["HAVe 1 M&M3, 'q' "==>Gq] or [MAD2's==>Gi], then the receptor is linked to Gs |
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what receptor and G protein:
incr cardiac contractility |
B1
s (think "s" for "s"timulate) |
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what receptor and G protein:
incr renin release? |
B1
s Tip: if the receptor not in the other mneumonics ["HAVe 1 M&M3, 'q' "==>Gq] or [MAD2's==>Gi], then the receptor is linked to Gs |
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what receptor and G protein:
incr lipolysis |
B1
s (think "s" for "s"timulate) |
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what receptor and G protein:
aq humor formation |
B1
s (think "s" for "s"timulate) |
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what receptor and G protein:
vasodilate |
B2
s |
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what receptor and G protein:
bronchodilate |
B2
s |
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what receptor and G protein:
incr glucagon release |
B2
s |
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what receptor and G protein:
CNS |
M1 (muscarinic): q
D2: i |
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what receptor and G protein:
decr HR |
M2 (muscarinic)
i (MAD2's "i"nhibit) |
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what receptor and G protein:
incr exocrine gland secretions |
M3
q |
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what receptor and G protein:
relax renal VSM |
D1
s Tip: if the receptor not in the other mneumonics ["HAVe 1 M&M3, 'q' "==>Gq] or [MAD2's==>Gi], then the receptor is linked to Gs |
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what receptor and G protein:
modulates transmitter release, esp in brain |
D2
i |
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what receptor and G protein:
incr nasal and bronchial mucus production |
H1
q |
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what receptor and G protein:
contract bronchioles |
H1
q |
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what receptor and G protein:
pruritis |
H1
q |
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what receptor and G protein:
pain |
H1
q |
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what receptor and G protein:
incr gastric acid secretion |
H2
s |
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what receptor and G protein:
incr VSM contraction |
a1: q
V1: q |
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what receptor and G protein:
incr H2O permeability and reabs in kidney CT |
V2
s |
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which G-proteins linked to which autonomic receptor
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"HAV 1 M&M3, queer"==>Gq
(H1, A1, V1, M1, M3) "MAD 2's"==>Gi (MAD2's "i"nhibit cAMP) (M2, A2, D2) the other receptors are Gs a1: q a2: i B1: s B2: s M1: q M2: i M3: q D1: s D2: i H1: q H2: s V1: q V2: s menum: "qiss" (kiss) and "qiq" (kick) til you're "siq" (sick) of "sqs" (sex) "kiss & kick" refer to a1,a2,B1,B2,M1,M2,M3 "sick & sex" refer to D1,D2,H1,H2,V1,V2 |
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Tx postoperative and neurogenic ileus
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1. bethanochol (-Direct muscarinic agonist, resistant to AchE)
"B"ethanochol stimulates "B"ladder (Tx urinary retention) & "B"owel SmM 2. Neostigmine |
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carbachol
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-Direct muscarinic agonist
CHOL=PSNS effect Tx (eye stuff): -glaucoma/release IOP -cause pupillary contraction (makes sense; PSNS effect) Action: -contracts ciliary muscle (open angle) & pupillary sphincter (narrow angle) ==>incr AH outflow -resistant to AchE mneum: Tell a diabetic, "Don't eat too many CARBs, or you'll get glaucoma! |
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challenge test to Dx asthma
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-Direct muscarinic agonist
an asthmatic "MET COLE" (Methacholine) and he took her breath away (Dx asthma) action: stimulates muscarinic receptors==>contract bronchial SmM==>asthmatics can't breathe |
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pilocarpine
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-Direct muscarinic agonist
potent stimulator of tears, saliva, sweat Action: stimulates muscarinic receptors in airway when inhaled mneum: when I smell a PILE OF CARP (carp=fish), it makes me salivate, sweat, and cry |
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cholinomimetics that are resistant to AchE
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direct cholinomimetics:
-Bethanochol -Carbochol -Methacholine -Pilocarpine (see FA for my narrative) |
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Anticholinesterases
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=Indirect Muscarinic Agonists
(Anticholinesterases==>incr endogenous Ach) -NeoSTIGMINE (Tx MG/NMB reversal) -PyridoSTIGMINE (Tx MG) -Edrophonium (Dx MG) -PhysoSTIGMINE (Tx Glaucoma (cross BBB==>CNS) & atropine OD; PHYSostigmine is PHYSically fit and can cross BBB AND overpower atropine, defeating NEO) -Echothiophate (Echothiophate is a huge admirer of physostigmine and "ECHOes" what physostigmine does: Tx glaucoma) |
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Neostigmine
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NEO from The Matrix stays, "I will "STIck MINE" ("stigmine") my great manhood/penis into 3 situations to defeat the great AchE:
1. the NMJ: to rescue the poor person with MG 2. the NMJ: to reverse NMB (postoperative) 3. the GI/urinary tract (he really goes all out): to get the bowel and bladder going (Tx post-op/neurogenic ileus & urinary retention) -sadly, Neo is actually impotent, so he cannot PENETRATE (ha!) the CNS |
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Tx MG
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(both are indirect ACh agonists AKA they are anticholinesterases)
1. neostigmine (does not penetrate CNS; NEO is impotent, so he can't penetrate) 2. Pyridostigmine: DOES penetrate CNS==>incr strength (the PYRAmids are STRONG enough to penetrate the CNS and give some of their STRENGTH to ppl with MG) |
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Dx MG
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Edrophonium (extremely short acting)
=indirect ACh agonist AKA anticholinesterase |
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Tx glaucoma
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I. alpha agonists:
1. Epi--incr AH outflow 2. Brimonidine--decr AH syn ("Ramona" (~BRIMONIdine), the lazy child (DECR AH synthesis) took her grandma's EPI and is now hyper (INCR AH outflow.) II. B-blockers (decr AH secretion) 1. timOLOL 2. betaxOLOL 3. carteOLOL III. Acetozolamide (inhibit CA==>decr bicarb==>decr AH secretion) IV. PROSTAGLANDIN= LatanoPROST (incr AH outflow) -S/E= darkens color of iris (browning) [mneum: "Latins" (Latano) have brown skin] V. ACH AGONISTS (all incr AH outflow; contract ciliary muscle==>open canal of Schlemm) IVa. Carbachol & Pilocarpine (direct Ach agonists; use Pilocarpine in emergencies) IVb. Physostigmine & Echothiophate (indirect ACh agonists AKA anticholinesterase==>incr endogenous ACh) |
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Tx parathion poisoning
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parathion=OP poison (anti-cholinerase==>incr PSNS)
Tx with atropine (musc antag) + pralidoxime (regenerates active cholinesterase) |
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Rx that produce mydriasis and cycloplegia
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these are SNS effects, so what causes this are Ach-R blockers:
1. aTROPIne 2. homaTROPIne 3. TROPICamide Atropine and his HOMO gay twin brother, HOMOatropine, went to the TROPICs together to do ecstasy==>mydriasis and cycloplegia==>awesome gay sex |
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Tx Park
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benztropine (poor Ben Brenners has Parkinson's).
[benzTROPINE~aTROPINE, so it's a Ach-R blocker==>incr SNS) |
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Tx motion sickness
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scopolamine (you get seasick on a SHIP (~SCOP))
=Ach-R blocker |
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Tx Asthma, COPD
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Ipratropium
(Ipra, a young black girl slave, went with the white family to the TROPICs: the old, fat white father with COPD & the bratty white boy with asthma) |
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-reduce urgency in mild cystitis
-reduce bladder spasms |
(all are Ach-R blockers):
1. methscopolamine: scopolamine prevents stuff from coming out your mouth (prevents vomiting; Tx motion sickness), so methscopolamine prevents stuff from coming out your pee-hole 2. oxybutin (an old medical method of Tx urinary incontinence is to stick OXYgen IN your BUTt; I guess they got the holes confused) 3. glycopyrrolate Narrative for Ach-R blockers: Ship ("scop") covered with methyls (thus "methscop", which is ~scopalamine, which we know is an Ach-R blocker) puts OXYgen up INto its ship BUTt hole (OXYBUTIN) to prevent "sugar pirates" (GLYCOPYROlate; GLYCO=sugar, PYRO=pirate) from leaking out (like pee) |
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what can cause:
-acute angle-closure glaucoma in eldery -urinary retention in BPH -hyperthermia in infants |
atropine (musc antag)
Hot as a Hare Dry as a Desert Red as a Beet Blind as a Bat (gluacoma; cycloplegia) Mad as a hatter (disorientation) |
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what drug prevents reflex bradycardia d/t NE
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hexamethonium (ganglion blocker; Nicotinic Ach-R blocker)
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isoproterenol
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stim B1=B2
Tx: AV block (rare) |
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dobutamine
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stim B1 > B2
(doBUTAmine: BUTA ~ BETA (B1 > B2) Uses: -shock -cardiac stress testing |
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amphetamine Tx what
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-ADHD (I want)
-obesity (I want) -narcolepsy |
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ephedrine
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(~pseudophedrine=Sudafed)
=indirect general SNS agonist: releases stored catecholamines (~amphetamines) Tx: -nasal decongestant (Sudafed) -urinary incontinence -hypotension |
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phenylephrine
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stim a1 > a2
Tx: -pupil dilator (ophthalmologist) -vasoconstriction (b/c alpha) -nasal decongestant (a1: decr bronchial gland secretions) |
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Tx asthma
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alBUTerol & terBUTaline (B2 > B1)
ipratropium (Ach-R blocker) |
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Tx HTN, esp w/renal dz
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-clonidine
-alpha-methyldopa *centrally acting alpha-agonists ==>DECR adrenergic outflow ==>thus decr BP without decr RBF (b/c adrenergic outflow incr BP & decr RBF) |
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alpha blockers
-nonselective -selective |
alpha blockers:
I. Nonselective (Tx pheochromocytoma) 1. phenoxybenzamine (PBZ)=irrevers 2. phentolamine=revers II. A1-selective (Tx HTN & urinary retention in BPH) -prAZOSIN, terAZOSIN, doxAZOSIN III. A2-SELECTIVE: -Mirtazapine (Tx depression) |
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Tx pheochromocytoma
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*Nonselective alpha blockers
1. phenoxybenzamine (PBZ)=irrevers 2. phentolamine=revers S/E: -orthostatic hypotension -reflex tachycardia |
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S/E:
orthostatic hypotension reflex tachycardia |
*Nonselective alpha blockers
1. phenoxybenzamine (PBZ)=irrevers 2. phentolamine=revers |