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60 Cards in this Set

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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
Clearance of drug =
Cl of drug

= (drug elimination rate)/(plasma drug conc)

=Vd x Ke (elimination constant)
drug half-life
=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
how fast does drug infused at constant rate reach steady state?
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%
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)
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)
drugs w/zero-order elimination?
(at high/toxic doses) ethanol, phenytoin, aspirin
most drugs are elimination by zero or first order elimination?
first order (constant FRACTION (vs. amount) eliminated per unit time)

zero order=(at high/toxic doses) ethanol, phenytoin, aspirin
what receptor and G protein:

increases VSM contraction
a1 & V1

q (for both)

"HAV 1 M&M3, q"
what receptor and G protein:

decr sympathetic outflow?
a2

i (MAD2's "i"nhibit cAMP)
what receptor and G protein:

decr insulin release
a2

i (think "i" for "i"nhibit):

"MAD 2's [M2, A2, D2] inhibit cAMP"
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
what receptor and G protein:

incr cardiac contractility
B1

s (think "s" for "s"timulate)
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
what receptor and G protein:

incr lipolysis
B1

s (think "s" for "s"timulate)
what receptor and G protein:

aq humor formation
B1

s (think "s" for "s"timulate)
what receptor and G protein:

vasodilate
B2

s
what receptor and G protein:

bronchodilate
B2

s
what receptor and G protein:

incr glucagon release
B2

s
what receptor and G protein:

CNS
M1 (muscarinic): q

D2: i
what receptor and G protein:

decr HR
M2 (muscarinic)

i (MAD2's "i"nhibit)
what receptor and G protein:

incr exocrine gland secretions
M3

q
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
what receptor and G protein:

modulates transmitter release, esp in brain
D2

i
what receptor and G protein:

incr nasal and bronchial mucus production
H1

q
what receptor and G protein:

contract bronchioles
H1

q
what receptor and G protein:

pruritis
H1

q
what receptor and G protein:

pain
H1

q
what receptor and G protein:

incr gastric acid secretion
H2

s
what receptor and G protein:

incr VSM contraction
a1: q

V1: q
what receptor and G protein:

incr H2O permeability and reabs in kidney CT
V2

s
which G-proteins linked to which autonomic receptor
"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
Tx postoperative and neurogenic ileus
1. bethanochol (-Direct muscarinic agonist, resistant to AchE)

"B"ethanochol stimulates "B"ladder (Tx urinary retention) & "B"owel SmM


2. Neostigmine
carbachol
-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!
challenge test to Dx asthma
-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
pilocarpine
-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
cholinomimetics that are resistant to AchE
direct cholinomimetics:

-Bethanochol
-Carbochol
-Methacholine
-Pilocarpine

(see FA for my narrative)
Anticholinesterases
=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)
Neostigmine
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
Tx MG
(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)
Dx MG
Edrophonium (extremely short acting)

=indirect ACh agonist AKA anticholinesterase
Tx glaucoma
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)
Tx parathion poisoning
parathion=OP poison (anti-cholinerase==>incr PSNS)

Tx with atropine (musc antag) + pralidoxime (regenerates active cholinesterase)
Rx that produce mydriasis and cycloplegia
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
Tx Park
benztropine (poor Ben Brenners has Parkinson's).

[benzTROPINE~aTROPINE, so it's a Ach-R blocker==>incr SNS)
Tx motion sickness
scopolamine (you get seasick on a SHIP (~SCOP))

=Ach-R blocker
Tx Asthma, COPD
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)
-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)
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)
what drug prevents reflex bradycardia d/t NE
hexamethonium (ganglion blocker; Nicotinic Ach-R blocker)
isoproterenol
stim B1=B2

Tx: AV block (rare)
dobutamine
stim B1 > B2

(doBUTAmine: BUTA ~ BETA (B1 > B2)

Uses:
-shock
-cardiac stress testing
amphetamine Tx what
-ADHD (I want)
-obesity (I want)
-narcolepsy
ephedrine
(~pseudophedrine=Sudafed)

=indirect general SNS agonist: releases stored catecholamines
(~amphetamines)

Tx:
-nasal decongestant (Sudafed)
-urinary incontinence
-hypotension
phenylephrine
stim a1 > a2

Tx:
-pupil dilator (ophthalmologist)
-vasoconstriction (b/c alpha)
-nasal decongestant (a1: decr bronchial gland secretions)
Tx asthma
alBUTerol & terBUTaline (B2 > B1)

ipratropium (Ach-R blocker)
Tx HTN, esp w/renal dz
-clonidine
-alpha-methyldopa

*centrally acting alpha-agonists
==>DECR adrenergic outflow
==>thus decr BP without decr RBF (b/c adrenergic outflow incr BP & decr RBF)
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)
Tx pheochromocytoma
*Nonselective alpha blockers

1. phenoxybenzamine (PBZ)=irrevers

2. phentolamine=revers

S/E:
-orthostatic hypotension
-reflex tachycardia
S/E:

orthostatic hypotension
reflex tachycardia
*Nonselective alpha blockers

1. phenoxybenzamine (PBZ)=irrevers

2. phentolamine=revers