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