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77 Cards in this Set

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this receptor is located -->
-radial muscle in the eyes
- arterioles in the skin
- veins
- bladder trigone and sphincter
- male sex organs
- liver
-kidney
Alpha one receptors
alpha 1 stimulation of radial muscle causes?
- radial muscle contraction = mydriasis
alpha 1 stimulation of arterioles in skin and viscera?
- contraction --> incrse tpr , diastolic pressure, afterload
alpha 1 stim of veins causes what?
venous contraction, incrsd vns return, increase preload
alpha 1 + of bladder / trigone ?
contraction --> urinary retention
alpha 1 stimulation of vas deferens?
ejaculation
alpha 1 stim of liver ?
INCREASE in GLCYOGENOLYSIS --> causes increased blood glucose levels
alpha 1 stim of kidney?
DECREASE renin release
Alpha 2 receptors are located on the presynpatic terminals and do what ?
inhibit the release of NE and its synthesis
alpha 2 stimulation on platelets causes them to do what ?
platelets aggregate together
stimulation of this receptor can a DECREASE IN INSULIN secretion
alpha 2 stimulation causes a DECREASE in INSULIN release
B1 receptors are located where?
- SA,AV node, Atrial and ventricular muscle, purkinje-his bundle , and the kidney
B1 stimulation of SA/Av node causes
increase in HR (sa), Conduction velocity (av)
B1 stimulation of atria and ventricular muscle
increased force of contraction, conduction velocity and O2 DEMAND
B1 stimulaton of his-purkinje?
increased automaticity and conduction velocity
B1 stimulation of kidney causes?
increased Renin release
B2 receptors are located where in the body? what r their fx?
- all blood vessels
- uterus (relaxation)
- bronchioles (dilation)
- skeletal muscle (incrsd glycognolysis --> contractility ~ tremor)
-Liver (incrsd glycogenolysis --> incrsd blood glucose)
- Pancreas (incrsd insulin secretion)
Dopamine (D1) receptors are located where ? (peripheral)
- renal, mesenteric and coronary vasculature
- VASODILATION --> incrse RBF, GFR, NA+ secretion
alpha 1 receptors , g protein?
Gq coupled --> increse PLC = Incrsd IP3, DAG , CA2+
ALPHA 2 receptors ?
Gi coupled --> inhibitory action
- dcrse cAMP
B1,2, D1
G-STIMULATORY coupled
= increase Adenylyl cyclase --> increase cAMP
name 2 drugs that are ALPHA - 1 AGONISTS
Phenylephrine
Methoxamine
moa of alpha 1 agonists?
increase TPR, BP
uses of phenylephrine?
nasal decongestant and opthalmic uses (mydriasis without affecting ability to accomodate)
uses of METHOXAMINE?
paroxysmal atrial tachy --> through the effects of increased vagal reflex
name 2 main Alpha 2 agonists?
- clonidine
- methyldopa
moa of Alpha 2 agonists?
stimulate the prejunctional receptors in CNS to DECREASE CNS SYMPATHETIC OUTFLOW
what is the primary use of alpha 2 agonists?
mild/moderate hypertension
Beta 1 agonist fx?
Increase HR, SV, CO and INCREASED PULSE PRESSURE
beta 2 agonist fx?
decrease TPR , BP
this drug has B1=B2, used for bronchospasm, heart block, and brady arrythmias
Isoproterenol
side fx of Isoproterenol?
flushing
angina
arrythmias
this drug stimulates B1 MORE than B2 and is often used in the treatment of heart failure
Dobutamine
These 2 drugs are BETA non-selective agonists?
Isoproterenol
Dobutamine
this drug is B2 selective agonist, and is use in premature labor
RITODRINE
B2 selective agonist used in the Rx of asthma
Salmeterol
albuterol
terbutaline
These 2 drugs are MIXED-ACTING AGONISTS OF ALPHA AND BETA RECEPTORS
Norepinephrine, Epinephrine
Norepinephrine mainly hits which receptors?
alpha 1,2 and beta 1
alpha 1 , B1 affects of norepi?
alpha 1 = increase tpr, bp
b1 = increase HR, SV, CO, Pulse pressure
does epinephrine hit all 4 receptors?
yes, epinephrine hits alpha1,2 and B1,2
low dose epi fx?
B1= incrse HR, SV, CO, pulse pressure
B2= dcrse TPR, BP
Medium dose epi fx?
B1, B2 and ALPHA 1 (Increase TPR,BP)
high dose epi fx? similar to NE
b1,b2,alpha1 and INCREASED POTENTIAL FOR REFLEX BRADY
B2 specific fx?
-smooth muscle relaxation of bronchioles, uterus and blood vessels
metabolic b2 fx?
- incrse glycogenolysis in muscle and liver
- increase gluconeogenesis
- incrse mobilization and use of fat
how do u reverse an overdose of epinephrine?
- use alpha1 blocker to reverse hypertension to hypotension
how did epi cause the hypertension in the overdose?
epi caused the PREDOMINANT alpha 1 tone on the vasculature
uses of NE and E?
- cardiac arrest
- help local anesthetic
- hypotension
- anaphylaxis and asthma (EPI ONLY)
this drug causes the RELEASE of NE from the mobile pool in the presynaptic neuron?
Tyramine
- red wine, cheese
what can tyramine and MAOa inhibitors cause?
hypertensive crisis!
moa of amphetamines?
causes central release of DA,NE,5HT
use of amphetamines?
methylphenidate --> narcolepsy and adhd
ephedrine?
cold medications
these 2 drugs are REUPTAKE INHIBITORS
COCAINE
TCA'S
name 2 NON-SELECTIVE ALPHA RECEPTOR BLOCKER
- phentolamine (competitive inhibitor; iv only)
- phenoxybenzamine (irreversible blocker)
fx of blockage of alpha 1 receptor?
dcrse tpr, bp
- used in htn
- pheochromocytoma
- bph (alpha 1 selective blocker)
where is MAOa located?
mainly in LIVER
- but metabolizes NE,5HT AND TYRAMINE anywhere in the body
Mao B located?
brain - metabolizes DOPAMINE
-zosins? what type of drug?
SELECTIVE ALPHA1 BLOCKER
fx of -zosins?
relaxes bladder sphincters and helps complete the voiding
Yohimbine, Mirtazapine
selective alpha 2 blocker
what is the only way to prevent prostate growth?
block DHT w/ 5 ALPHA REDUCTASE inhibitors (finasteride)
- also used for male pattern baldness
BEAM beta blockers moa?
B- betaxolol/
E- esmolol
A- atenolol/ acebutolol
M- metoprolol
Pindolol, Propranolol, Timolol moa?
Beta non-selective blockers
B1 blockade causes?
- dcrse hr,sv,co, renin release, aqueous humor release
B2 blockade causes?
can cause bronchospasm in asthmatics and vasospasm
make sure you AVOID bb's in which types of patients?
- asthmatics
- people with reynaud's and prinzemetals angina
bb w/ most sedative fx?
propranolol
2 bb's w/ ISA activity
acebutelol, pindolol
- also have no change in blood lipids
propranol also does what to thyroid hormones?
inhibits 5' deiodinase (t4 conversion to t3)
this bb is used for essential tremors?
propranolol ; also used for performance anxiety, migraine and thyrotoxicosis
ALL bb's should be avoided in which patients?
DIABETICS
- can mask hypoglycemia
this bb has no cns entry
atenolol
bb used in glaucoma?
timolol
this bb has a combined alpha-1 and BB activity?
labetolol and carvedilol
- used in chf
ISA (instrinsic sympathomimetics) activities means what ?
- bb's act as partial agonists
- less bradycardia
- slight vaso/bronchodilation
- minimal change in the blood lipids
main uses of bb's?
angina, htn, and post-mi
- antiarrythmics --> class 2 drugs (propranolol, acebutolol, esmolol)