Adrenergic Drugs Part 1 - Dr. Konorev Flashcards
3 direct acting adrenomimetic drugs
- Alpha agonists
- Mixed alpha and beta agonists
- Beta agonists
4 Indirect adrenomimetics
- Inhibits re-uptake of DA and NE
- Inhibits MAO
- Reverse NE and DA uptake mechanisms and increase their release
- Releasing agent AND a direct adrenergic R agonist
Alpha agonists
- Phenylephrine
2. Clonidine
Mixed a and b agonists
- NE
2. Epi
B agonists
- Dobutamine
- Isoproterenol
- Albuterol
Inhibit is reuptake of NE and DA
Cocain
Inhibits MAO
Selegiline
phenelzine
Reverse NE and DA uptake mechanism and increase release of them
- Amphetamines
- Mythylphenidate
- Tyramine
Releasign agent AND direct adrenergic R agonist
Ephedrine
Cholenergic drugs control what
ACh release at adrenal medulla (N), or skeletal muscles voluntary (N), preganglionic synapse (N), parasympathetic involuntary muscles (M), sympathetic only if sweat glands (M)
Adrenergic drugs act where
Post synaptic ganglion at sympathetic involuntary muscles (cardiac, SM, glands, nerves ) = NE
AND
Postsynaptic ganglion at renal vascular SM = D
a1 type R does what biochem pathway
Increase IP3 and DAG
= Gq
a2 type R does what biochem pathway
Decrease cAMP to inhibit PKA
= Gi (so is D2)
B type R does what biochem pathway
Increase cAMP to activate PKA
=Gs (so is D1)
Direct vs indirect acting adrenergic drugs
- Direct = direct action on R
2. Indirect = increase or decrease concentration of NE or D at the receptor area
Phenylephrine R
A1 >a2
Clonidine R
A2 >a1
NE R
A1 and A2, and B1
Epi R
a1 and a2 and B1 ad B2
Dobutamine R
B1 > B2
Isoproterenol R
B1 and B2
Albuterol R
B2»_space; B1
A1 actions
4
- Vascular SM = contraction **
- Pupils = dilation by contraction of dilator muscle
- Prostate = contraction
- Heart = increase Contraction Force
A2 acts where
5
- Neurons = TR release
- Platelet = aggregation
- Adrenergic and cholinergic nerve terminals = inhibit TR release
- Some vascular SM = contraction
- Fat = inhibit Lypolysis
B1 action
1
Heart and juxtaglomerular cells = increase Force and Rate of contraction , increase RENIN release (higher BP)
B2 actions
3
- Resp**, uterine, vascular SM = relaxation
- Skeletal muscle = K+ reuptake (repolarization)
- Liver = glycogenolysis + gluconeogenesis
B3 actions
2
- Relax bladder detrusor muscle
2. Active Lypolysis in fat cells
D1
D2 actions
1 each
D1 : smooth muscles : dilate renal BVs
D2 : never endings : TR release
B1 does what mostly
Increase heart contraction and force , HR, AV conductance
B2 and A1 does what mostly when activated together
- Increase BP, NO change in mean arterial P, decrease congestion in bronchial mucosa (A1)
- Decrease in diastolic BP at times
Muscle tremors, K+ uptake, liver metabolism, RELAX bronchial muscles **(B2)
More severe elevation of BP NE or Epi
Norepinephrine because it does not activate B2 receptors also
More increase in HR NE or Epi
Epi because
In NE the more severe increase in BP = BARORECEPTORS stimulated so ——> bradycardia
(Epi is higher HR)
Phenylephrine HR and BP
A1 : High BP and
low HR as body compensates from BARORECEPTORS
Mydriasis (pupil dilation)
Clonidine BP and HR
Low BP and low HR,
Vasoconstriction (peripheral a2 R, only not very prominent)
A2
Isoproterenol
B1 = CO increase high HR B2 = bronchodilation, vasodilation low BP
Dobutamine effects
B1 : heart rate increase
Albuterol effects
B2 : bronchodilation
Indirect acting adrenomimetics have what properties
Lipophilic and cross BBB and effect CNS , unlike catacholamines, = EXCEPT tyramine **
Tryamine is used for
Evaluate peripheral adrenergic function
TX hypotensive EM, hemorrhagic shock, overdose of antihypertensives, CNS depressants
NE and Phenylephrine
TX chronic hypotension
Ephedrine
TX Cardiogenic shock
Dobutamine
TX Heart failure
Short term dobutamine in acute HF
TX HTN
A2- agonists for long-term tx
EM TX for AV block and cardiac arrest
Epinephrine and isoproterenol
TX depression
Phenelzine and Selegiline
TX Narcolepsy
Amphetamines and methylphenidate
TX ADHD, learning problems, hyperkinetic behavior
Methylphenidate
TX Obesity
Ephedrine (B3) and Amphetamines = to increase energy expenditure and lower appetite
TX bronchial asthma
Albuterol
TX decongestion of mucous membranes
Phenylephrine and ephedrine
TX anaphylaxis
Epinephrine (tax cardiac depression , severe hypotension, bronchospasms)
TX ophthalmic application : examining retina and inducing mydriasis
Phenylephrine
TX glaucoma
A2- selective agonists
GU : TX stress urinary incontinence
Ephedrine (B3)