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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)