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168 Cards in this Set

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What is Km?
then conc. of the substrate at which enzyme is at 1/2Vmax

reflects the affinity of an enzyme for it's substrate
Which has higher affinity, a low or high Km?
lower Km = higher affinity
What does a non-competitive inhibitor do to the enzyme's kinetics?
It decreases the enzyme's Vmax but doesn't affect it's affinity for substrate (Km unchanged)
What does a competitive inhibitor do to the enzyme's kinetics?
It decreases the enzyme's affinity for substrate (bigger Km) but the Vmax stays the same
What do competitive antagonists do to the pharmacodynamics?
Decrease potency
right shit on curve - more agonist needed to achieve same effect
What do non-competitive antagonists do to the pharmacodynamics?
Decrease efficacy
down shift on curve. lower maximum effect of agonist
What is volume of distribution (Vd)?
amt of drug deliver (mg)/conc. in blood (mg/L)
units are in L
What is a low Vd?
~4L-8L ==> indicates most of the drug stayed in the blood
what is the formula for half-life?
(0.7xVd)/CL
What is the formula for loading dose?
(Cp x Vd)/F
Cp = target plasma conc.
F = bioavailability of drug (=1 when given IV)
What is the formula for maintenance dose?
(Cp x CL) /F
Cp = target plasma conc.
F=bioavailability of drug
What is the formula for clearance of a drug?
CL = rate of elimination of drug/plasma drug conc.
also =VdxKe

where Ke=elimination constant
What is zero-order elimination?
Rate of elimination is constant regardless of plasma concentration
constant amount of drug eliminated per time
What are examples of drugs with zero-order elimination?
alcohol
aspirin
What is a first order elimination?
rate of elimination is proportion to the drug concentration
constant fraction eliminated per unit time
How do you speed up elimination of a drug (as in during overdose)?
You give them something to cause the drug to go into it's ionized form.

Ionized molecules can be filtered but not readily reabsorbed so they will be more likely to pee it out
If the drug is a weak acid ==> treat with bicarbonate (raise pH, make pee more basic)

If the drug is a weak base ==> treat with ammonium chloride to lower the pH (make pee more acidic)
What are examples of drugs that are weak acids that might be overdosed?
methotrexate
phenobarbital
aspirin
treat with bicarb to make them pee it out
What is a Phase 1 reaction?
P-450 in liver causes reduction, oxidation, hydrolysis ==> slightly polar, water soluble metabolites that are often still active
this is what you loose with age
What is a Phase 2 reaction?
acetylation, glucuronidation and sulfation yielding very polar, inactive metabolites that can be renally excreted
What is the difference between efficacy and potency?
efficacy is the max effect a drug can have

potency is how much drug you need to give to achieve a given effect
What does a partial agonist do to the pharmacodynamics of a reaction?
It decreases the efficacy and can either raise or lower the potency
what is therapeutic index?
median lethal dose/median effective dose
safer drugs have higher TI values
What does it mean if a drug has a low therapeutic index?
It has a very narrow therapeutic window. You have to careful because the toxic dose may not be much higher than the effective dose.
Nicotinic receptors work how/where?
Na+/K+ ligand-gated Ach receptor in autonomic ganglin (Nn) and skeletal muscle (Nm)
How do Muscarinic receptors work (generally)?
they are G-protein couple receptors found in the parasympathetic branch the autonomic nervous system.
What do alpha-1 receptors do?
inc. vascular SM contraction

inc. pupillary dilator muscle contraction (mydriasis)

Inc. intestinal bladder and sphincter muscle contraction
Gq-->phospholipace C ==> PIP2 ==> IP3/Dag ==> inc. Ca2+ and PKC
What do alpha-2 receptors do?
dec. sympathetic outflow

dec. insulin release
Gi ==> inhibits adenylyl cyclase ==> dec. cAmp ==> dec. PKA
What do beta-1 receptors do?
inc. HR

inc. contractility

inc. renin release

inc. lipolysis
Gs ==> activated adenylyl cyclase ==> inc. cAMP ==> inc. PKA
What do beta-2 receptors do?
Vasodilation

Bronchodilation

inc. HR

inc. contractility

inc. lipolysis

inc. insulin release

dec. uterine tone
Gs (same as Beta-1)
What do M1 receptors do?
?? found in CNS and enteric nervous system
Gq
What do M2 receptors do?
dec. HR

dec. contractility of atria
Gi
What do M3 receptors do?
inc. exocrine glad secretion

inc. gut peristalsis

inc. bladder contractions

bronchoconstriction

inc. pupillary sphincter muscle contraction (miosis)

ciliary muscle contraction (accommodation)
Gq (like M1)
What do D1 receptors do?
relaxes renal vascular smooth muscle
Gs
What do D2 receptors do?
modulated transmitter release, especially in the brain
Gi
What do H1 receptors do?
inc. nasal and bronchial mucus production

contraction of bronchioles

pruritus

pain
Gq
What do H2 receptors do?
Inc. gastric acid secretion
Gs
What do V1 receptors do?
inc. vascular smooth muscle contraction
Gq
What do V2 receptors do?
inc. H20 permeability and reabsorption in the collecting tubules of the kidney
Gs
Which receptors are Gq coupled?
H1, alpha-1, V1, M1, M3
HAVe 1 M&M
Which receptors are Gs coupled?
B1, B2, D1, H2, V2
Which receptors are Gi coupled?
M2, alpha-2, D2
MAD 2's
Bethanechol MOA
cholinomimetic, Ach direct agonist at muscarinic receptors - activates bladder and bowel
Bethanechol clinical use
post-operative neurogenic ileus and urinary retention
Carbachol MOA
cholinomimetic, Ach direct agonist at muscarinic receptors - causes pupillary sphincter muscle contraction
Carbachol clinical use
glaucoma

relief of intraocular pressure
Pilocarpine MOA
cholinomimetic, Ach direct agonist at muscarinic receptors - contracts ciliary muscle of the eye (so opens the angle), contracts the pupillary sphincter (accomodation)
Pilocarpine clinical use
potent stimulator of sweat, tears, saliva
Methacholine MOA
cholinomimetic, Ach direct agonist at muscarinic receptors (M3 receptors in airway SM causes bronchoconstriction)
Methacholine clinical use
challenge test of asthma diagnosis
Neostigmine MOA
anti-cholinesterase (indirect agonist of Ach - cholimimetic)
can not penetrate BBB
Neostigmine clinical use
postoperative and neurogenic ileus and urinary retention

myasthenia gravis

reversal of neuromuscular junction blockade (post-surgery)
Pyridostigmine MOA
anti-cholinesterase (indirect Ach agonist - cholimimetic) so inc. endogenous Ach by keeping it around in the synaptic junction
no CNS penetration
Pyridostigmine clinical use
myasthenia gravis (long acting)
Physostigmine MOA
anti-cholinesterase (indirect Ach agonist - cholimimetic) so inc. endogenous Ach by keeping it around in the synaptic junction
Physostigmine clinical use
glaucoma

atropine overdose (outc
crosses BBB
Echothiophate MOA
anti-cholinesterase (indirect Ach agonist - cholimimetic) so inc. endogenous Ach by keeping it around in the synaptic junction
Echothiophate clinical use
glaucoma
Cholinesterase inhibitor poising symptoms
Diahrrea/urination
miosis
bronchospasm
bradycardia
excitation of skeletal muscle and CNS
lacrimation/sweating/salivation
caused by organophosphates used in fertilizers and insecticides
Organophosphate poisoning antidote
Atropine + pralidoxime
The atropine blocks the Ach while the pralidoxime helps regenerate the AchE
What is organophosphate poisoning?
The chemical irreversibly inhibits AchE so there is too much Ach in the synapse causing too much parasympathetic activation
What are the direct agonist cholimimetics?
Bethanechol
Carbachol
Pilocarpine
Methacholine
Atropine clinical use
Muscarinic antagonist: produces mydriasis (pupillary dilation) and cycloplegia (inability to accommodate) for ophtho exam
Homatropine
Muscarinic antagonist eye drop: produces mydriasis (pupillary dilation) and cycloplegia (inability to accommodate) for ophtho exam
Tropicamide
Muscarinic antagonist eye drop: produces mydriasis (pupillary dilation) and cycloplegia (inability to accommodate) for ophtho exam
Benztropine
Muscarinic antagonist - blocks Ach in CNS

used for Parkinson's
Scopolamine
blocks Ach in CNS

used for motion sickness
Ipratropium
Muscarinic antagonist - blocks Ach in the respiratory system preventing bronchoconstriction

Used for asthma and COPD
Oxybutynin
Muscarinic antagonist - blocks Ach in genitourinary system so prevents bladder contraction

used for cystitis and OBS
Glycopyrrolate
same as oxybutynin:

Muscarinic antagonist - blocks Ach in genitourinary system so prevents bladder contraction

used for cystitis and OBS
Methscoplamine
Muscarinic antagonist - block Ach affect on stomach so dec. H+ secretion

used for peptic ulcers
Pirenzepine
Muscarinic antagonist - block Ach affect on stomach so dec. H+ secretion

used for peptic ulcers
Propantheline
Muscarinic antagonist - block Ach affect on stomach so dec. H+ secretion

used for peptic ulcers
What are the symptoms of atropine poisoning?
block parasympathetic response:
inc. temp (due to dec. sweating)
rapid pulse
dry mouth
dry, flushed skin
cycloplegia
constipation
disorientation
Hot as a hare
Dry as a bone
Red as a beet
Blind as a bat
Mad as a hatter
Hexamethonium
nicotinic antagonist - Ach blocker at the ganglion

not used clinically
Epinephrine MOA
stimulates alpha1, alpha2, beta1, beta2

at low doses it is beta2 selective
Epinephrine clinical use
anaphylaxis
open angle glaucoma
asthma
severe hypotension (shock)
Norepinepherine MOA
alpha1/2 > B1
Norepinepherine clinical use
Hypotension (but not really because it dec. renal perfusion too)
Isoproterenol MOA
beta-adrenergic direct agonist

B1=B2
Isoproterenol clinical use
AV block (rarely used)
Dopamine MOA
D1/D2 > beta1/2 > alpha 1/2

inotropic and chronotropic
Dopamine clinical use
inotropic and chronotropic and relaxes renal vascular smooth muscle so good for:

shock (also inc. renal perfusion)

heart failure
Dobutamine MOA
beta-1 > beta-2

inotropic but not chronotropic
Dobutamine clinical use
heart failure

cardiac stress testing
Phenylephrine MOA
alpha-1 > alpha-2
Phenylephrine clinical use
pupillary dilation

vasoconstriction

nasal decongestion
Metaproterenol MOA
Selective Beta-2 agonist (B2>B1)

stimulates bronchodilation
Metaproterenol clinical use
acute asthma
Terbutaline MOA/clinical use
selective beta-2 agonist

decreases uterine vascular tone

used to slow contractions in premature labor
Ritodrine MOA/clinical use
beta-2 agonist

reduces premature uterine contractions
Pseudephedrine side effect
urinary retention (cuz it's a general agonist releasing stored catecholamines, which includes stimulating urinary sphincter contraction)

bad for men with BPH, e.g
What does exogenous NE do to blood pressure?
Widens the pulse pressure

Beta-1 effects raise systolic

Alpha-1 effects lower the diastolic
What does exogenous NE do to heart rate?
reflex bradycardia
What does isoproterenol do to blood pressure?
lowers it (slightly) cuz beta>alpha

the Beta-2 causes vasodilation
What does isoproterenol do to heart rate?
reflex tachycardia
Clonidine MOA
centrally acting alpha-2 agonist ==> dec. central adrenergic outflow
alpha-methyldopa MOA
centrally acting alpha-2 agonist ==> dec. central adrenergic outflow
Clonidine clinical use
to treat hypertension (esp. in renal disease cuz doesn't dec. renal perfusion)
alpha-methyldopa clinical use
to treat hypertension (esp. in renal disease cuz doesn't dec. renal perfusion)
Phenoxybenzamine - MOA/use/toxicity
non-selective, irreversible alpha-blocker

used pre-operatively for pheochromocytoma
orthostatic hypotension

reflex tachycardia
Phentolamine MOA/use/toxicity
non-selective, reversible alpha-blocker

used in pheochromocytoma (esp. pre-op)
toxicity includes orthostatic hypotension and reflex tachycardia
Prazosin/terazosin/doxazosin

MOA/use/toxicity
alpha-1 selective antagonists

used for HTN

treats urinary retention in men with BPH
toxicity: 1st dose orthostatic hypotension

dizziness

headache
Mirtazipine MOA/use/toxicity
alpha-2 selective antagonist

used for depression
toxicity:
inc. sedation
inc. serum cholesterol
inc. appetite
What happens to BP if you give a large dose of epi and then phentolamine
the blood pressure will raise due to the alpha effect from the epi but then lower to below baseline after the phentolamine because there is an alpha but no beta blockade
What happens to BP if you give a large dose of phenylephrine and then phentolamine
The blood pressure will rise from the alpha-response induced by phenylephrine and then lower back to baseline due to alpha-blockade of phentolamine
How do beta-blockers treat HTN?
dec. cardiac output

dec. renin secretion (Beta-1 on JGA cells)
How do beta-blockers treat angina?
dec. HR and contractility resulting in dec. O2 consumption
How do beta-blockers treat SVT?
dec. AV conduction velocity

(class II anti-arrhythmic)
What do beta-blockers treat?
HTN
CHF
angina
MI
SVT
glaucoma
How do beta-blockers treat glaucoma?
dec. secretion of aqueous humor
What are the side effects of beta-blockers?
impotence
exacerbation of asthma
bradycardia
AV block
CHF worsening
sedation/sleep alterations
use with caution in diabetics
Which are the non-selective Beta-blockers?
propranolol
timolol
nadolol
pindolol
Which are the Beta-1 selective beta-blockers?
Atenolol
Metoprolol
Esmolol (short-acting)
Betaxolol
Which are the nonselective alpha- and beta-antagonists?
Carvedilol
labetalol
Which are the partial beta-agonists?
Pindolol
Acebutlol
antidote for acetaminophen overdose
N-acetylcysteine
antidote for salicylates overdose
Bicarb
alkalinize the urine
antidote for amphetamines overdose
NH4Cl
acidify the urine
antidote for Organophosphate overdose
atropine + pralidoxime
antidote for Antimuscarine/anticholinesterase overdose
physostigmine (direct Ach agonist)
B-blocker overdose antidote
glucagon
Digitalis overdose antidote
normalize K+
lidocaine
anti-dig Fab
Mg2+
Iron overdose antidote
Deferoxamine
Lead poisoning antidote
CaEDTA, dimercaprol, succimer, penicillamine
Mercury/arsenic/gold poisoning antidote
dimercaprol, succimer
Copper, arsenic poisoning antidote
penicillamine
cyanide poisoning antidote
nitrite, hydroxocobalamin, thiosulfate
Methemoglobin poisoning antidote
Methylene blue, vitamin C
TCA's overdose antidote
Bicarb
Heparin overdose antidote
Protamine
Warafin overdose antidote
Vitamin K, fresh frozen plasma
tPA, streptokinase overdose antidote
aminocaproic acid
Theophylline overdose antidote
Beta-blocker
Drugs that cause atropine-like side effects
TCAs
Drugs that cause cutaneous flushing
Vancomycin
Adenosine
Niacin
Calcium-channel blockers
Drugs that cause torsades de pointes
Class III antiarrhythmics (sotalol)

Class IA antiarrhythmics (quinidine)
Drugs that cause agranulocytosis
clozapine
carbamazepine
colchicine
propylthiouracil
methimazole
dapsone
Drugs that cause aplastic anemia
chloramphenicol
benzene
NSAIDs
PTU
methimazole
Drugs that cause hemolysis in G6PD deficient patients
Isoniazid
Sulfonamides
Primaquine
Aspiring
Ibuprofen
Nirtofurantoin
Drugs that cause megaloblastic anemia
Phenytoin
Methotrexate
Sulfa drugs
Drugs that cause pulmonary fibrosis
Bleomycin
Amiodarone
Busulfan
Drugs that cause hepatotoxicity
Halothane
Calproic acid
Acetaminophen
INH
Drugs that cause gynecomastia
Spironolactone
Digitalis
Cimetidine
Alcohol
Ketoconazole
Drugs that cause hypothyroid
Lithium
Amiodarone
Drugs that cause gout
furosemide
thiazides
Drugs that cause osteoporosis
Corticosteroids
Heparin
Drugs that cause photosensitivity
Sulfonamides
Amiodarone
Tetracyclines
Drugs that cause severe rash (Stevens-Johnson syndrome)
Ethosuximide
Lamotrigine
Carbamazepine
Phenobarbital
Phenytoin
Sulf drugs
Penicillin
Allopurinol
Drugs that cause SLE-like syndrome
Hydralazine
INH
Procainamide
Phenytoin
Drugs that cause interstitial nephritis
Methicillin
NSAIDs
Furosemide
Drugs that cause pulmonary fibrosis
Bleomycin
Amiodarone
Busulfan
Drugs that cause hepatotoxicity
Halothane
Calproic acid
Acetaminophen
INH
Drugs that cause gynecomastia
Spironolactone
Digitalis
Cimetidine
Alcohol
Ketoconazole
Drugs that cause hypothyroid
Lithium
Amiodarone
Drugs that cause gout
furosemide
thiazides
Drugs that cause osteoporosis
Corticosteroids
Heparin
Drugs that cause photosensitivity
Sulfonamides
Amiodarone
Tetracyclines
Drugs that cause severe rash (Stevens-Johnson syndrome)
Ethosuximide
Lamotrigine
Carbamazepine
Phenobarbital
Phenytoin
Sulf drugs
Penicillin
Allopurinol
Drugs that cause SLE-like syndrome
Hydralazine
INH
Procainamide
Phenytoin
Drugs that cause interstitial nephritis
Methicillin
NSAIDs
Furosemide
Drugs that cause diabetes insipidus
Demeclocycline
Lithium
Drugs that cause Parkinsonian effects
Haloperidol
Chlorpromazine
Reserpine
Metoclopramide
Drugs that cause seizures
Buproprion
Imipenem/cilastatin
Isoniazid
Drugs that cause disulfram-like reactions
Metronidazole
Cephalosporins (some)
Procarbazine
1st generation sulfonylureas
Drugs that cause nephro- and ototoxicity
Aminoglycosides
Vancomycin
Loop diuretics
Cisplatin
P-450 inducers
Quinidine
Barbituates
St. John's wort
Phenytoin
Rifampin
Griseofulvin
Carbamazepine
Chronic alcohol use
Queen Barb Steals Phen-phen and Refuses Greasy Carbs Chronically

makes drugs wear-off quicker
P-450 inhibitors
HIV protease inhibitors
Ketoconazole
Erythromycin
Grapefruit juice
Acute alcohol use
sulfonamides
isoniazid
cimetidine
"inhibit yourself from drinking beer from a KEG because it makes you Acutely SICk"

makes drugs more potent and/or stay around longer
What are the symptoms of sulfa-drug allergies?
fever
pruritic rash
urticuria
Steven-Johnson syndrome
hemolytic anemia
thrombocytopenia
agranulocytosis