DIT Pharm Flashcards
Parasympathetic nerves (thanks severson):
III, VII, IX and X and S2,3,4
70% are vagal
Receptors on muscle?
Nitotinic (Na/K channel)
Also on autonomic ganglion
What is bethanechol?
CHOL cholinomimetic for post op ileum and urinary retention
Bethany, call (bethanechol) me maybe if youw ant to activate Bowel and Bladder
Carbechol
CARBon copy of acetylCHOLine for glaucoma relief
What is donepezil? Galantamine, rivastigmine
Anticholinesterase for alzheimers
I’m DONE forgetting
Guzman (Galantamine) and RIVAS never forget them
What is myasthenia gravis associated with?
hyperplastic thyroid, atrophic thyroid, tumor (In fact, most of time, thyroid is just removed)
What is benztropine?
Antimuscarinic
Parkinsons and helps reduce antipsychotic side effects
Urge type urinary incontinence meds? Mnemonic
On The Darn Toilet (muscarinic antagonist)
Oxybutynin
Tolterodine
Darifenacin and solifenacin
Trospium
What drugs initiate p450? mnemonic
Corona, Guiness and PBRs induce chronic alcoholism.
Carbamazapine griseofulvan phenytoinbarbituates rifamycin st johns wart chronic alcoholism
More anti epileptic and anesthetic stuff
pg 59, 60
Why does sympathetic nervous system activate a lot of things?
B/c short preganglionic activates long post ganglionics releasing NE on multiple organs
Alpha2 receptor
Only on Beta cells and certain smooth muscles
PRESYNAPTIC nerve, when stimulated inhibits norepinephrine release (negative feedback mechanism)
Beta1 receptor?
Tachycardia, lipolysis, myocardial contractility, more RENIN release
Beta2 receptor?
Vasodilation, BRONCHODILATION, lipolysis, more insulin release, LESS UTERINE TONE, more heart rate (compensatory from vasodilation)
What symp receptors are on skel muscle vasc?
on heart?
on lung?
Think phys, it makes sense.
Skel muscle vasc: alpha2 and beta2 (more beta 2)
Heart: Beta1 big time
Lung: Beta2 (epi!!)
What does epi hit?
alpha 1, 2 and beta 1, 2.
anaphylaxis
What does NE hit?
alpha1, 2, Beta1 (No beta 2, not vasodilation, so good for septic shock, but not for anaphylaxis)
Careful, decreases renal perfusion if used in shock
Isoproterenol hits what?
betas!
What does dopamine hit?
low doses: D1 and D2
Medium doses Beta1 and Beta 2
High doses alpha1 and alpha2
What does dobutamine do?
doBETAmine. Beta1
What does phenylephrine do?
Alpha1, so hypotension and vasoconstriction
What does terbutaline do?
BETA2 (Terbutaline!) Reduces premature conraction (relax uterus)
also subQ for asthma
What does salmeterol do?
Its a name like albuterol.
Beta 2. It is long acting asthma vs albuterol which is short acting
What is clonidine?
Alpha2! decreases blood pressure b/c less NE release.
CAREFUL with stopping it
What do alpha 1 blockers do? What do they end in?
End in azosin (or osin).
Used for BPH, PTSD, HTN
Loosens bladder and less peripheral pressure.
What is tamsulosin? When do you use it?
Alpha1 blocker that is selective on the prostate to help relax smooth muscle near prostate to HELP PISS in BPH
Doesn’t hit alpha1b receptor in BP (so safer if normotensive than the azosins)
What is phenoxybenzamine?
non selective and nonreversible alpha blocker used for PHEOCHROMOCYTOMA (we learned about that and was on Q bank) and prevents hypertensive crisis.
Phentolamine (reversible) is for MAO inhibitors who have tyramine foods
What is carvedilol? What is labetalol?
alpha and beta1 blocker.
Some vasodilation happens!
(modified suffix)
What do beta blockers do for glaucoma?
Less vitreous humor production!
Timolol, Nadolol (trachte taught us (first time Jeff noticed LOL)
What happens with hypoglycemia (what are the symptoms and why are you mentioning it in the autonomic nervous system pharm lecture)?
tachycardic, shaky, sweaty.
PROBLEM is beta blockers block the sign, and it makes it dangerous hypoglycemia
What is the drug used in hypertensive urgency?
Clonidine (alpha2 agonist) does not reduce renal blood flow.
Alpha(2)methyldopa also works
What is the antihypertensive for pregnancy?
alpha-methyldopa (ALPHA2 methyldopa) is for preggers! safe in pregnancy. Can cause SLE like symptoms (positive Direct Coombs with hemolytic anemia)
Who are you worried about with beta blockers?
Cocaine users (unappeased alpha work) Diabetics (masks hypoglycemia symptoms) COPD/Asthma (bronchoconstriction)
What inhibits choline/Na symptort into presynaptic cholinergic neurons?
Hemicholinium (think only hemiCHOLIN so not enough choline)
what signals for acetylcholine release?
Caclium, duh.
Release blocked by Botulism
Release increased with black widow toxin
What drugs block NE release?
Guanethidine (remember NE is guan from synapse (never there in first place))
Bretylium (calcium channel blocker for heart)
What drug blocks tyrosine hydroxylase?
Metyrosine (think MEtyrosine, like I want more tyrosine!!) not wanting more dopa
What prevents NE being put into vesicles for export?
Reserpine call it reservine in the cell, not exocytosing in vesicles
(reserveNE)
What prevents Ach into vesicles?
VESamiCOL
Vesamicol
Vesicle acetylcholine stopper. Easy to remember
What does D1 receptor do?
What about D2?
D1 is vasodilation in kidney! (good for hypertensive event!)
D2 modulaes transmitter release in the brain (basal ganglia)
What are Gq receptors?
What are downstream effects?
Cute C’s HAV 1 M&M
Ca++ and Protein Kinase C
What are the Gi?
MAD 2’s (mad b/c inhibitory)
X intercept on lineweaver burke?
What happens with competitive inhibitor?
What happens with noncompetitive inhibitor?
X axis is 1/-Km
It is closer to zero with competitive inhibitor
It is unchanged with noncompetitive inhibitor
Y intercept on lineweaver burke plot?
What happens with competitive inhibitor?
What happens with noncompetitive inhibitor?
It is 1/Vmax
It is unchanged with competitive inhibitor (Vmax doesn’t change)
It moves higher with noncompetitive (b/c it is 1/vmax, and vmax is less)
What is Vd=?
Drug volume/Concentration
What does Clearance=?
Rate elimination/plasma concentration
also
0.7 Vd/half life
What is Loading Dose=?
(steady state concentration) Css X Vd
What is maintenance dose?
CSS X clearance
How many half lives does it take for drug to be at steady state with constant infusion?
4-5 for boards
Efficacy vs potency?
Efficacy is most a drug can produce
Potency is amount of drug needed for an effect
How does competitive agonist change potency? Efficacy?
no effect of efficacy.
lower potency
What does a partial agonist do to efficacy and potency?
Partial agonist ALWAYS Decrease efficacy.
Variable affect on potency
Do you want high therapeutic index or low therapeutic index?
what is the calculation?
You want a high TI
LD50/ED50
Phase 1 does what? Phase 2 metal does what?
What do old people have?
Geriatrics have GAS. Note phases aren’t in order
Glucuronidation, Acetylation, Sulfation GAS (very polar! BECOMES inactive)
Phase 1 is lost first in old people (hydroxylation, oxidation, reduction, slightly soluble)
P450 inhibitors?
CRACK AMIGOS
Cimetidine Ritonavir (protease inhibitor) Amiodarone Ciprofloxacin Ketoconazole Acute alcohol use Macrolides Isoniazid Grapefruit juice Omeprazole Sulfonamides
What do you use to treat methanol and ethylene glycol?
Fomepizole!!!!
Blocks alcohol dehydrogenase which would make formaldehyde (blindness) or oxalic acid (KIDNEY DAMAGE b/c oxalate makes stones) which causes acidosis (respectively)
They are in MUDPILES for acidosis if not treated
What blocks acetaldehyde dehydrogenase?
Disulfiram (makes boozers feels sick)
Disulfiram like reactions?
Metronidazole (BIGGIE)
Certain cephalosporines
Procarbazine
First gen sulfonylureas (nobody uses those anymore)
Drugs of zero order elimination (three of them)
PEA is round like 0
Phenytoin
Ethanol
Aspirin
What type of drug is trapped in alkaline urine?
Acidic drugs will lose a proton and not be reabsorbed and will be trapped
(bicarb can do it, so NaHCO3)
What acidifies urine? When would you use it?
Ammonium chloride NH4Cl
Amphetamine overdose b/c they are basic
