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;
107 Cards in this Set
- Front
- Back
Hexamethonium:
Effects Drug Class |
Nicotinic antagonist (blocks transmission of PSymp and Symp--this is at the level of the autonomic--first--ganglion)
Dominant tone of tissue will prevail. So drug can look either symp or psymp antagonist. |
|
Hexamethonium effects:
BP HR Q Urine Output GI Motility Pupil of Eye |
Dominant tone at arteries/veins = symp, so will appear anti-symp. BP will decrease
At other tissues, dom tone is psymp. So will appear anti-parasymp. HR: Up Q: Down Urine Output: Down GI Motility: Down Pupil of Eye: Mydriasis (dilation) |
|
Muscarinic vs Nicotinic Receptors:
Biochemical receptor tyoe |
Musc: G-protein coupled receptors
Nicotinic: Sodium/K+ channels |
|
Production of ACh.
List enzymes and drugs that block each step. What causes vesicle release? |
Choline enters via Na+-Co-transporter (uses Na+ gradient)-RATE LIMITING STEP; blocked by HEMICHOLINIUM
Acetyl CoA added to Choline; via Choline Acetyltransferase; blocked by VESAMICOL Vesicles released by Ca2+ Inhibited by BOTULINUM |
|
Botulinum toxin:
MOA Symptom |
Prevents release of ACh vesicles
Symptom: Flaccid paralysis |
|
Black Widow Spider Toxin:
MOA |
Stimulates release of Ach into synapse
|
|
Production of NE.
List enzymes and drugs that block each step. What causes vesicle release? What inhibits reuptake? |
Tyrosine transported into cell with Na+ co-transporter
Tyrosine-->DOPA via TYROSINE HYDROXYLASE; inhibited by METYROSINE L-DOPA-->DA-->NE Packaged into vesicles. This step blocked by RESERPINE. -->Epi Ca2+ causes release; release inhibited by GUANETHIDINE, BRETYLIUM NE can undergo re-uptake--inhibited by Cocaine, Amphetamines, TCA (tricyclic anti-depressants) |
|
Pre-cursor of Tyrosine.
|
Phenylalanine
|
|
Pre-cursor of Thyroxine.
|
Tyrosine
|
|
What drus stimulate the release of NE?
|
Amphetamine
Ephedrine Tyramine |
|
Pre-Synaptic Auto-Receptors:
Effect Example for NE |
Regulate release of NT
alpha-2 receptor inhibits release of NE when NE binds to it. |
|
Enzymes that metabolize NE
|
COMT (Catechol-O-methyltransferase)--methylates NE
MAO (monoamine oxidase)--oxidate NE |
|
MAO-inhibitors:
Effect |
Inhibit MAO (enzyme that metabolizes NE) so that NE sticks around longer.
Used in anti-depressants |
|
What substance is contraindicated with MAO-inhibitors?
|
Tyramine--can result in hypertensive crisis. Stimulates release of NE.
Would have too much NE if took both! |
|
Byproducts of breakdown of NE.
|
VMA
Metanephrines Normetanephrines |
|
alpha-1 receptor effects
|
vascular SM contraction (raise BP)
mydriasis |
|
alpha-2 receptor effects
|
vasodilation (decrease
|
|
beta-1 receptor effects
|
act at heart, increase heart rate
|
|
beta-2 receptor effects
|
vasodilation, bronchodilation***
also compensatory HR increase due to drop in BP |
|
GQ Receptor effects
Example receptor |
GQ receptor: QC
activates phospholipase C Cleaves lipids into PIP2 PIP2 broken down to IP3 (inositol triphosphate) and DAG (diacylglycerol) IP3-->increases intracell Ca2+ DAG-->activates Protein Kinase C |
|
GS Receptor effects
|
GS stimulates adenylyl cyclase
Cleaves ATP-->cAMP-->activates Protein Kinase A |
|
Gi Receptor effects
|
INhibits adenylyl cyclase
Decrease cAMP-->dec Protein Kinase A |
|
Tyrosine kinase receptor effects
|
GF's bind tyrosine kinase receptors
Use PLC to make IP3 and DAG OR bind adaptor prots-->activate Ras-->activates Protein Kinase I-->activates Protein Kinase II-->activates Protein Kinase III |
|
Specific G protein receptors for:
alpha-1 alpha-2 beta-1 beta-2 D1 D2 H1 |
alpha-1 GQ
alpha-2 Gi beta-1/2 GS D1: GS D2: Gi H1: GQ (QIS SIQ)--kiss sick |
|
D1 receptor effects
|
relaxes renal vessels
|
|
D2 receptor effects
|
Modulates NT release, esp in brain
|
|
M1 receptor effects
|
CNS, enteric NS
|
|
M2 receptor effects
|
dec heart rate, contractility of atria
|
|
M3 receptor effects
|
inc exocrine gland secretions (sweat, stomach acid)
inc gut persitalsis inc bladder contraction bronchoconstriction inc miosis ciliary muscle contraction (accommodation) |
|
G-protein class for muscarinic receptors.
|
M1 Q
M2 I M3 Q |
|
Epinephrine:
receptors it acts at uses |
alpha 1, beta 1, alpha 2, beta 2
anaphylactic shock, asthma |
|
NE:
receptors it acts at uses |
alpha 1, alpha 2>>beta 1
not very strong heart effects septic shock (bc there's vasodilation of BVs)--will tighten BVs without inc'd heart rate (like Epi would) |
|
Isoprotenelol
receptors it acts at |
beta 1, beta 2
|
|
Dopamine:
receptors it acts at uses |
beta 1, beta 2 >>alpha 1, alpha2
shock (renal perfusion) heart failure D1>beta>alpha |
|
Dobutamine:
receptors it acts at uses |
beta-1
ionotropic and chronotropic used in cardiogenic shock, cardiac stress testing |
|
Phenylephrine:
receptors it acts at uses |
alpha 1, alpha2
pupillary dilaiton, vasoconstriciotn, nasal decongestion |
|
Metaproterenol:
receptors it acts at uses |
beta 2 > beta 1
asthma |
|
Albuterol:
receptors it acts at uses |
beta 2 > beta 1
asthma |
|
Salmeterol:
receptors it acts at uses |
beta 2>beta1
Long-Term asthma tx |
|
Terbutaline:
receptors it acts at uses |
beta 2>beta 1
Reduces premature uterine contractions |
|
Amphetamine:
MOA Use |
Releases stored catechols
Uses: narco, obesity, ADD |
|
Ephedrine:
MOA Use |
releases stored catechols
nasal decongest, urinary incont, hypotn |
|
Cocaine:
MOA Use |
Symp uptake inhibitor
Vasoconstriction, local anesthesia |
|
Effect of NE on:
BP HR |
NE: alpha1 > beta1
Results in Inc BP (due to vasoconstriction) and a REFLEX BRADYCARDIA |
|
Effect of isoproterenol on:
BP HR |
beta 1 = beta 2 activity
BP: drops HR: increases (beta1), reflexive tach |
|
Clonidine:
Receptors act on Uses |
Centrally acting alpha-2 agonist
Use in HTN, esp with renal dz (no blood flow to kidney) |
|
alpha-methyldopa:
Receptors act on Uses |
Centrally acting alpha-2 agonist
Use in HTN, esp with renal dz (no blood flow to kidney) SAFE IN PREGNANCY |
|
beta-blocker:
Effects AEs |
dec'd cardiac output
dec'd renin secretion AE's: ED Asthma exacerbation Bradycardia, AV block Sedation, fatigue Use in caution w/DM (blocks syx of hypoglycemia--tachycardia, diaphoresis) |
|
beta-blockers that decrease AV conduction velocity.
When would this be necessary? |
Use in SVT:
propranolol Esmolol |
|
This beta-blocker is used in glaucoma. Why?
|
Timolol
dec'd secretion of aqueous humor |
|
Which beta-blockers aren't selective?
|
N-->Z non-zelective
|
|
Which beta-blockers are selective? Which receptor do they select for?
|
beta-1>beta-2
A-->M Advantageous in pts with pulm dz. |
|
Which beta-blockers are also partial beta-agonists?
|
PAPA
Partial Agonist: Pindolol, Acebutolol |
|
What are the effects of cocaine on arterial pressure?
Is this an indication for beta-blockers? |
Cocaine increases arterial pressure
But BP will increase even more if you treat with beta-blocker! |
|
Glaucoma:
Aqueous humor pathway Pathophys |
Aq humor formed in ciliary body
-->posterior chamber -->anterior chamber via lens/iris angle -->reabsorbed via canal of schlemm Glaucoma: impaired flow of aq humor-->inc'd intraocular pressure-->optic disc atrophy with cupping |
|
Open angle glaucoma:
Pathophys Syx Visual Changes |
Obstructed outflow--problem with canal of schlemm; can't get rid of aqueous humor
This is common and insidious (comes on slowly); silent glaucoma Almost always bilateral Risk factors: Myopia Age >40 DM Visual changes: reduced/absent vision, contraction of visual field (peripheral-->central) |
|
Acute angle glaucoma:
Pathophys Syx Visual Changes |
Obstruction of flow between iris and lens (between posterior and anterior chamber), pressure builds up behind iris.
Very painful! abrupt onset of syx. abrupt decrease in vision.frontal headache. EMERGENCY! Colored halos, rainbows around light |
|
Epi exacerbates which glaucoma?
|
close angle
epi causes mydriasis, makes situation worse (pressure buildup behind iris) |
|
Fixed, mid-dilated pupil not reactive to light =
|
acute angle-closure glaucoma
also is firm to palpation |
|
Cup:Disc ratio > _____ = glaucoma
|
Greater than 1:2
|
|
60 year-old male has hard time driving at night because of worsening vision, appearance of halos around oncoming headlights.
Dx? |
Cataracts
Not an abrupt change, not painful. |
|
beta-blockers in glaucoma treatment:
Examples |
beta-blockers: timolol, betaxolol
Lower intraocular pressure |
|
Alpha agonists in glaucoma treatment:
MOA Examples |
alpha-agonists: epi, brominidine--vasoconstriction-->dec aq humor synthesis due to vasoconstriction (OPEN ANGLE ONLY)
|
|
Diuretics in glaucoma treatment:
MOA Examples |
Diuretics: mannitol, azetazolamide; dec'd humor secretion due to dec'd HCO3-
|
|
PGs in glaucoma treatment:
MOA Examples AEs |
LatanoPROST; inc outflow of aqueous humor
AE: darkens color of iris |
|
Cholinomimetics in glaucoma treatment:
MOA Examples |
Inc outflow of aq humor; contract ciliary muscle, open trabecular meshwork
Pilocarpine (direct cholinomimetic) Physostigmine--indirect cholinomimetic |
|
Phenoxybenzamine:
Drug Class Use |
IRREVERSIBLE (NONCOMP)
nonselective alpha blocker: alpha1, alpha2 both blocked use in pheochromocytoma--must give phenoxybenzamine first! or you'll get rid of beta-2 effect and will inc BP. |
|
Phentolamine:
Drug Class |
REVERSIBLE (COMP)
nonselective alpha blocker: alpha1, alpha2 both blocked |
|
Prazosin:
Drug Class Use AE |
alpha-1 blocker (selective)
Use in HTN, urinary retention in BPH AE: first dose orthostatic hypotension--start with a low dose at night |
|
Terazosin:
Drug Class Use |
alpha-1 blocker (selective)
Use in HTN, urinary retention in BPH AE: first dose orthostatic hypotension--start with a low dose at night |
|
Mirtazapine:
Drug Class Use |
alpha-2 selective
Use in depression May cause sedation, inc'd appetite AE: first dose orthostatic hypotension--start with a low dose at night |
|
Tamsulosin:
Drug Class Use |
alpha-1 antag; selective for alpha-1 A receptors-->relaxes prostatic urethra
DOESN'T LOWER BP Use in urinary retention due to BPH |
|
Epi:
Low vs High Doses Effect of large dose after alpha-blocker administration |
Low doses: vasodilation, lower BPs (Beta 2 vasodilation predominates)
High doses: alpha-1 constriction predominates Need high doses of Epi for constrictive effects (raise BP) Large dose after alpha-blockade results in decreased BP because there are no alpha-receptors to act on (acts on beta receptors) |
|
Phenylephrine:
Low vs High Doses Effect of large dose after alpha-blocker administration |
No beta effect, all alpha effect.
If alpha blockade and then administer phenylephrine-->no effect. |
|
Sildenafil:
Suffix Drug Category |
-denafil
PDE5 Inhibitor (inc'd cGMP)-->Vasodilate; ED |
|
Halothane:
Suffix Drug Class |
-ane
Inhalational anesthetics |
|
Diazepam:
Suffix Drug Class |
-azepam
Benzodiazepine |
|
Chlorpromazine:
Suffix Drug Class |
-azine
Phenothiazine (neuroleptic, antiemetic) |
|
Ketoconazole:
Suffix Drug Class |
-azole
Anti-fungal |
|
Metronidazole:
Drug Class |
Anti-biotic, NOT antifungal
|
|
Phenobarbital:
Suffix Drug Class |
-barbital
Barbiturate |
|
Lidocaine:
Suffix Drug Class |
-caine
Local anesthetic |
|
Tetracycline:
Suffix Drug Class |
-cycline
Abx: protein synthesis inhibitor |
|
Paroxetine:
Suffix Drug Class |
-etine
SSRI |
|
Imipramine:
Suffix Drug Class |
-ipramine
TCA |
|
Saquinavir:
Suffix Drug Class |
-avir
Preotase inhibitor (for HIV) |
|
Haloperidol:
Suffix Drug Class |
-operidol
Butrophenone (neuroleptic) |
|
Digoxin:
Suffix Drug Class |
-oxin
Cardiac glycoside (inotropic) |
|
Captopril:
Suffix Drug Class |
-pril
ACE inhibitor |
|
Albuterol:
Suffix Drug Class |
-terol
beta-2 agonists |
|
Cimetidine:
Suffix Drug Class |
-tidine
H2 antagonist |
|
Sumatriptan:
Suffix Drug Class |
-triptan
5-HT agonists (migraine) |
|
Amitryptyline:
Suffix Drug Class |
-triptyline
TCA |
|
Somatotropin:
Suffix Drug Class |
-tropin
Pituitary hormone |
|
Alprazolam:
Suffix Drug Class |
-zolam
Benzodiazepine |
|
Alendronate:
Suffix Drug Class |
-dronate
Bisphosphonate |
|
Losartan:
Suffix Drug Class |
AgII receptor antagonist
|
|
Bethanechol:
Suffix Drug Class |
-chol
Musc agonist |
|
Neostigmine:
Suffix Drug Class |
-stigmine
Anti-AChE |
|
Lomustine:
Suffix Drug Class |
-mustine
Put Nitro on a Mustang Nitrosureas (brain ca; cross BBB) |
|
Atracurium:
Suffix Drug Class |
-curium
Paralytic; non-depolarizing NM blockage Reversed with neostigmine (AntiAChE) |
|
Vecuronium:
Suffix Drug Class |
-curonium
Paralytic drug; non-depolarizing NM blockage Reversed with neostigmine (Anti-AChE) |
|
Atorvastatin:
Suffix Drug Class |
-statins
HMG CoA reductase inhibitors |
|
Rosiglitazone:
Suffix Drug Class |
-glitazones
Inc target cell response to insulin |
|
Albendazole:
Suffix Drug Class |
-bendazole
Antiparasite/antihelmintic |
|
Nifedipine:
Suffix Drug Class |
-dipine
Dihydropyridine Calcium Channel Blocker |
|
Travoprost:
Suffix Drug Class |
-prost
Prostaglandin analog (tx glaucoma) |