Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
131 Cards in this Set
- Front
- Back
|
Vmax
|
proportional to enzyme conc
|
|
|
Comp Inh
|
no change Vmax
increase Km decrease potency no change efficacy |
|
|
Non-comp Inh
|
no change Km
decrease Vmax decrease efficacy no change potency |
|
|
Vd =
(units volume) |
total amt drug in body / [drug]plasma
|
|
|
Cl =
(units: volume/time) |
Rate of drug elim (mass/time) / Plasma drug conc (mass/volume of plasma)
= Vd * ke |
|
|
t 1/2 =
|
(0.7 * Vd) / Cl
|
|
|
LD =
(units = mass) |
(Vd*Cp) / F
note: no change w/ hepatorenal disease bc not dep on Cl |
|
|
MD =
(units = mass/time) |
(Cl * Cp) / F
|
|
|
Zero order elim drugs
|
phenytoin
ETOH ASA |
|
|
Drugs that are weak acids
|
Barbiturates
MTX ASA increase excretion by ionizing (alk urine, + HCO3-) |
|
|
Weak bases
|
Amphetamines
increase ionization and therefore elim by + NH4Cl --> acidify urine |
|
|
Quinidine
P450 |
induce
|
|
|
Barbiturates
P450 |
induce
|
|
|
St Johns Wort
P450 |
induce
|
|
|
Phenytoin
P450 |
Induce
|
|
|
Rifampin
P450 |
induce
|
|
|
Griseofulvin
P450 |
induce
|
|
|
Carbamazepine
P450 |
induce
|
|
|
Chronic ETOH
P450 |
induce
|
|
|
GCs
P450 |
induce
|
|
|
HIV protease I
P450 |
inhibit
|
|
|
INH
P450 |
inhibit
|
|
|
Sulfonamides
P450 |
inhibit
|
|
|
Cimetidine
P450 |
inhibit
|
|
|
Ketoconazole
P450 |
inhibit
|
|
|
Grapefruit juice
P450 |
inhibit
|
|
|
Omeprazole
P450 |
inhibit
|
|
|
Chloramphenicol
P450 |
inhibit
|
|
|
Marcolides
P450 |
inhibit
|
|
|
Ritonavir
P450 |
inhibit
|
|
|
HIV protease I
P450 |
inhibit
|
|
|
INH
P450 |
inhibit
|
|
|
Sulfonamides
P450 |
inhibit
|
|
|
Cimetidine
P450 |
inhibit
|
|
|
Ketoconazole
P450 |
inhibit
|
|
|
Grapefruit juice
P450 |
inhibit
|
|
|
Omeprazole
P450 |
inhibit
|
|
|
Chloramphenicol
P450 |
inhibit
|
|
|
Marcolides
P450 |
inhibit
|
|
|
Ritonavir
P450 |
inhibit
|
|
|
potency
|
how much drug for desired effect
EC50 (relates to Aff: ie- no change w/ NCI) |
|
|
Efficacy
|
Max effect a drug can produce
(relates to [S] to knock off: ie- no change w/ CI) |
|
|
Therapeutic Index (TI) =
|
LD50/ED50
high = good |
|
|
a1 receptor
|
Gq (PIP3)
vascular sm. m contraction mydriasis intestional and bladder sphincter contraction |
|
|
a2 receptor
|
Gi (decrease cAMP)
decreases sym and insulin release |
|
|
b1 receptor
|
Gs (increased cAMP)
increase - HR, contractility and renin release |
|
|
b2 receptor
|
Gs (increases cAMP)
vasodilation, bronchodilation, decreases uterine tone |
|
|
M1 receptor
|
Gq (PIP3)
CNS, gastric parietal cells |
|
|
M2 receptor
|
Gi (decrease cAMP)
decrease- HR, atrial contractility |
|
|
M3 receptor
|
Gq (PIP3)
Stim glandular secretions (sweat, gastric acid) incr gut peristalsis miosis ciliary muscle contraction (accomodation) |
|
|
D1 receptor
|
Gs (increased cAMP)
renal vascular muscle relax |
|
|
D2 receptor
|
Gi (decrease cAMP)
decrease sympathetic release NTs |
|
|
H1 receptor
|
Gq (PIP3)
incr sinus and bronchial mucus production, bronchiole constriction, itching/pain |
|
|
H2 receptor
|
Gs (incr cAMP)
increased gastric acid secretion |
|
|
V1 receptor
|
Gq (PIP3)
vascular sm m contraction |
|
|
V2 receptor
|
Gs (decr cAMP)
incr H2O reabsorbtion in CT in kidneys |
|
|
Hemicholinum
|
MOA: block choline uptake into cholinergic nerve term --> decr production ACh
|
|
|
Vesamicol
|
MOA: I ACh production from acetyl-CoA.
I Choline Acetyl Transferase |
|
|
Botulinum
|
I ACh release from pre-synaptic nerve terminal
|
|
|
Metyrosine
|
Block Tyrosine Hydroxylase
decreased amt NE precursers |
|
|
Reserpine
|
block NE uptake into vesicles
(decreased effectiveness) |
|
|
Guanethidine
|
block NE release into synapse
|
|
|
Cocaine
|
directly block NE reuptake
(potentiates) |
|
|
TCAs
|
directly block NE reuptake
(potentiates) |
|
|
Amphetamines
|
directly block NE reuptake + increases NE release from pre- synaptic nerve terminal
(potentiates!!!!) |
|
|
Bethanechol
|
M agonist
R to esterase = long acting Rx: ileus and urinary retention Bowel and Bladder |
|
|
Carbachol
|
M and nicotinic agonist
eye application: contraction of ciliary muscle (relief of OPEN-angle glaucoma) and pupil constriction |
|
|
Pilocarpine
|
M agonist
Stim: tears, sweat, saliva. Constricts pupil and ciliary muscle. Rx: acute glaucoma |
|
|
Methacholine
|
M agonist
causes bronchoconstriction when inhaled (asthma challenge test) |
|
|
Neostigmine
|
Anti-AChE
Quaternary amine (no CNS) Rx: ileus, urinary retention and myasthenia gravis Post-op reversal of nm jn blockade |
|
|
Pyridostigmine
|
anti-AChE
Quaternary amine Rx: MG |
|
|
Edrophonium
|
anti-AChE
dx: MG short acting |
|
|
Physostigmine
|
anti- AChE
tertiary amine (CNS) Rx: glaucoma, antidote for atropine tox |
|
|
Echothiophate
|
anti-AChE
Rx: glaucoma |
|
|
Cholinesterase Inhibitor Poison
(TONS ACh) |
SE:
D Urination Miosis Bronchoconstristion Bradycardia Excitation (sk and cardiac m) Lacrimation Salivation Sweating |
|
|
Atropine
|
M antagonist
Rx: antispasmodic, antisecretory, anti-AChE OD, anti-D, ophthalmology (long acting) SE: opp DUMBBELSS |
|
|
Tropicamide
|
ophthalmology (topical)
|
|
|
Ipratropium
|
M antagonist
Rx: asthma, COPD (inhaled) no CNS entry, no change in mucus viscosity |
|
|
Scopolamine
|
M antagonist
Rx: motion sickness causes sedation and short term memory blocks |
|
|
Benzotropine
|
M antagonist
lipid sol (CNS) Rx: parkinsonism and in acute extrapyramidal sx induced by antipsychotics |
|
|
Hexamethonium
|
nicotinic antagonist
used to prevent vagal reflexes d/t sym stim ie: used to prevent reflex bradycardia caused by NE induced incr BP SE: ortho hTN, blurred vision and constipation |
|
|
Epi
|
a and b agonist (low dose selective for b1 r)
Rx: anaphylaxis, open-angle glaucoma, asthma, hTN, prolonged effects locals SE: increased SP, decreased DP: therefore increased PP and reflex increased HR |
|
|
NE
|
mainly a r agonist
Rx: hTN (vasoconstriction) SE: -splanchnic vasoconstriction and decr renal perfusion -incr SP and DP (no change PP) -reflex decrease in HR |
|
|
Isoproterenol
|
b1 and b2 agonist
Rx: AV conduction block, decr DP (reflex increased HR) |
|
|
Dopamine
|
D1=D2 >b >a agonist
inotropic and chronotropic Rx; cardiogenic shock |
|
|
Ritodrine
|
b2 agonist
Rx: reduces premature uterine contractions |
|
|
Dobutamine
|
b1 > b2 agonist
inotropic Rx: heart failure, used in stress test |
|
|
Metaproterenol
Albuterol salmeterol Terbutaline |
selective b2 agonists
Acute: metaproterenol and albuterol Long-acting: Salmeterol |
|
|
Ephedrine
|
indirect sympathomimetic
induces catecholamine release Rx: nasal congestion, urinary incontinence and hTN |
|
|
Tyramine
|
indirect sympathomimetic ~ amphetamines
cleared by MAO. note: MAOI can cause HTN esp in tyramine rich foods (wine and aged cheese) |
|
|
Clonidine
|
central a2 adrenergic agonist
decr sym outflow Rx: HTN |
|
|
a-methyldopa
|
sympathoplegic
decr sym outflow: Rx: HTN |
|
|
Phenoxybenzamine
|
non-selective a1 and a2 blocker
Rx: pheochromacytoma and Raynaud's IRREV |
|
|
Phentolamine
|
non-selective a1 and a2 blocker
Rx: pheochromacytoma and Raynaud's REV |
|
|
Prazosin
|
a1 selective blocker
Rx: HTN, BPH SE: ortho hTN (take at bedtime) |
|
|
Terazosin
|
a1 selective blocker
Rx: HTN, BPH SE: ortho hTN (take at bedtime) |
|
|
Doxazosin
|
a1 selective blocker (longest acting)
Rx: HTN, BPH SE: ortho hTN (take at bedtime) |
|
|
Mirtazapine
|
a2 selective blocker
Rx: depression SE: sedation, incr chol and incr appetite |
|
|
Propranolol
|
non-specific b1 and b2 blocker
migrane prophylaxis |
|
|
Timolol
|
non-specific b1 and b2 blocker
glaucoma |
|
|
Nadolol
|
non-specific b1 and b2 blocker
|
|
|
Pindolol
|
non-specific b1 and b2 blocker
|
|
|
Metoprolol
|
b1 selective blocker
|
|
|
Atenolol
|
b1 selective blocker
|
|
|
Betaxolol
|
b1 selective blocker
|
|
|
Esmolol
|
b1 selective blocker
shortest acting |
|
|
carvediol
|
mixed a and b blocker
|
|
|
Labetalol
|
mixed a and b blocker
|
|
|
Pindolol
|
partial b agonist
|
|
|
Acebutolol
|
partial b agonist
|
|
|
Acetaminophen antidote
|
N-acetylcysteine
|
|
|
Salicylate antidote
|
none specific.
alk urine to increase excretion or dialysis |
|
|
anticholinergic antidote
ie: atropine, scopolamine OD |
physostigmine (CNS)
|
|
|
Anti-AChE OD (antidote)
ie: organophosphates |
atropine
pralidoximine (2-PAM) |
|
|
b blocker antidote
|
glucagon to increase inotropy and chronotropy of heart. improves AV conduction as well
|
|
|
Digitalis antidote
|
Anti-dig Fab frag
Normalize lytes (esp K+) Mg2+: esp w/ hK+emia Lidocaine |
|
|
Iron antidote
|
Deferoxamine
|
|
|
Lead antidote
|
Ca-EDTA chelator
dimercaprol succimer penicillamine |
|
|
Arsenic
mercury gold antidote |
dimercaprol
succimer |
|
|
Copper
Arsenic Gold |
Penicillamine
|
|
|
CN- antidote
|
Nitrite
hydroxocobalamin thiosulfate |
|
|
Methemoglobin antidote
|
Methylene blue
Vit C |
|
|
CO antidote
|
100% O2
|
|
|
Methanol (blindness)
ethylene glycol (antifreeze: nephrotox) antidote |
Ethanol
fomepizol |
|
|
Opioids antidote
|
Naloxone
Naltrexone |
|
|
Bezodiazepines antidote
|
Flumazenil
|
|
|
TCAs antidote
|
NaHCO3 IV: to combat acidosis
Rx adjunct: seizures, hyperthermia ans arrythmias |
|
|
Heparin antidote
|
Protamine
|
|
|
Warfarin antidote
|
Vit K (restore II, VII, IX, X, Prot C and S)
FFP |
|
|
tPA
Streptokinase antidote |
Aminocaproic acid
|
|
|
Theophylline antidote
|
b-blocker
|
