-
NE release and receptor binding?
- release: sympathetic nerve terminals
- receptors: alpha and Beta 1
-
Epi release and receptor binding?
- release: adrenal medulla
- receptors: alpha, Beta 1 & 2
-
2 Direct acting effects of denervation or reserpine?
- 1) No affect
- 2) increase response to drug
-
indirect effect of amphetamine & tyramine?
increase release of NE
-
indirect effect of cocaine & TCA's
inhibit NET so NE is not recycled into cleft
-
Indirect effect of MAOIs
inhibit degradation of NE
-
Indirect effect of reserpine (or denervation)
No packaging into vesicle = no response
-
Mixed effect of ephedrine
- some direct receptor activity
- some indirect action
-
Mixed effect of denervation
blunt but not eliminate effect
-
Adrenergic receptors on synaptic button, platelets, Smooth mm, and heart?
- button: Alpha 2
- platelets: alpha 2 & Beta 2
- Smooth mm: alpha 1 & Beta 2
- Heart: Beta 1
-
Alpha 1 function
excitatory
-
Alpha 2 function
inhibitory
-
Main alpha 1 agonist?
Phenylephrine
-
Main Alpha 2 agonist?
Clonidine
-
Epi, noradernaline & isoproterenol effectivity on alpha receptors?
Epi > noradrenaline >> isoproterenol
-
Isoproterenol, epi & NE strengths on B1, B2 & B3 receptors?
- B1: Iso > Epi=NE
- B2: Iso > Epi >> NE
- B3: Iso=NE > Epi
-
Dobutamine receptor and effect
- receptor: B1
- effect: increase heart rate & contractility, increase renin
-
Albuterol receptor and effect
- receptor: B2
- effect:
- same as B1 on heart + relaxed bronchial, uterus, bladder, GI, muscle blood vessels
- Increase K uptake into muscles
- Glycogenolysis/gluconeogenesis
- B3 = fat lipolysis
-
DA receptor effect on blood vessels
- Dilate renal vessels, increse flow
- Dilate coronary vessels
-
Two molecules that metabolize NE & Epi
MAO and COMT
-
Alpha1 receptor effect on Cardiovascular system
- Vasoconstrict
- some increase in contraction
- increased BP (stimulate baroreceptor, slow Heart)
- Atherosclerosis = baroreceptor response decreased
-
Alpha receptor effect on eye
- contract radial pupillary = mydriasis
- no accomodation effect
- increase aqueous humor outflow (1 & 2)
- treat glaucoma
-
Alpha receptor effect on respiration
- A1 constrict nasal & upper airway vessels
- decongestants
-
Alpha receptor effect on GI
- A1 = relax GI
- A2 = inhibit Ach release = less motility
-
Alpha receptors on genitourinary
- A1 increase continence, constrict sphincters
- ejaculation
-
Alpha receptor effects on metabolism
- A1 increase glycogenolysis / gluconeogenesis
- A2 inhibit lipolysis, inhibit insulin secretion, decrease renin
-
Beta receptor effects on Cardio
Increase everything (dilation, blood flow, contraction, O2 consumption, etc..)
-
B receptor effects in eye
B2 increase aqeous humor secretion, increase intraocular pressure
-
B receptor effect on respiration
B2 relax bronchial Sm mm
-
B receptor effect on Genitourinary
B2 relax uterus (pregnant) and relax bladder wall
-
B receptor effect on metabolism
- B1 increase renin = increased BP
- B2 stimulate glycogenolysis, increase K uptake, increse insulin secretion
- B3 = stimulate lipolysis
-
What happens to Pulse Pressure when B1 and alpha are activated w/ NE?
unchanged
-
Alpha receptor effect on BP?
Increased if alpha 1
-
What receptors does NE activate
Alpha and B1
-
What receptors does Epi activate
Alpha, Beta 1 & 2
-
Cardiac effects of NE
- A = B1 >> B2
- Inc peripheral resistance (A)
- Inc. BP
- PP unchanged
- HR inc then baroreceptors activate to slow
-
Cardiac effects of Epi @ low dose
- A, B1 & B2 (more effect than alphas @ low dose)
- A = vasoconstriction
- B1 = inc HR & contraction (systolic)
- B2 = dilate Sk BV (dec. diastolic)
- BP unchanged or slight inc
- Inc PP & inc HR
-
Effects of high dose/low dose Epi on HR, BP
- high dose epi: HR inc, BP inc.
- low dose epi: HR inc, BP dec. (due to more B2 stim.)
-
What does Ephedrine release and what are its effects?
- release: NE to stimulate A & B
- effects: similar to EP
- longer duration
- bronchodilator
- CNS stimulant
-
function and cautions of Phenylephrine/Pseudoephedrine?
- function
- decongestant
- may increase BP
- Pseudoephedrine = more effective
- Caution
- Rebound Effect
-
Methoxamine function
IV for HTN
-
Midrodrine function
postural HTN
-
Xylometazoline / Oxymetazoline function
- Function
- alpha agonist
- Caution
- rebound effet = receptor down-regulation
- narrow angle glaucoma or HTN
-
Clonidine function
- A2 agonist
- brain = inhibit NE release
- decrease SNS output from CNS
- decrease PR & BP
- decrease craving for addicts
- Cautionsever HTN of withdrawn abruptly
-
Isoproterenol function
- B >> A
- inc contration
- vasodilation Sk mm vessels
- dec BP
- inc CO
-
Dobutamine function
- B1 agonist
- inc contraction
- little effect on PR or HR
- inc CO in heart failure/shock
- short duration
- Stress test
-
Ritrodine receptor, function and side effect
- B2
- - relax uterus for premature labor
- - side effect = headache
-
Albuterol function & side effect
- functionasthma treatment
- tremor, tachycardia, palpitations
- side effect
- headache
-
Along w/ albuterol, what other 4 drugs are commonly used for Asthma
- Terbutaline
- Pirbuterol
- Bitolterol
- Salmeterol
-
Dopamine receptor, function
- D1
- vasodilate renal beds
- treat cardiac schock
- inc BF & CO w/o vasoconstriction
- high doses = B1 stim, NE release and inc BP
-
Fenoldopam function
- more selective D1 agonist
- dec BP
-
Amphetamine function
NE release in brain
- side effectsHTN
- psychosis
- alert, aware, euphoria
- headache
- hemorrhage, convulsions, coma
-
Methylphenidate (ritalin) function
decrease ADHD
-
Cocaine function and side effects
- functioninhibit NE & DA reuptake
- side effects
- HTN
- psychosis
- tachycardia
-
Tyramine function and side effects
- functioninc NE releae from nerve terminals
- side effectstachyphylaxis
- Sever HTN if MAO blocked = from sever NE release
|
|