Adrenergic Receptor Agonist And Antagonist Flashcards
ADRENOCEPTORS
NA & Adr. play important roles in ___ control, _____ contractile rate & force, _____ reactivity and variety of metabolic & CNS functions.
BP
myocardial
airway
ADRENOCEPTORS CONT’D
Agonists & antagonists have proved useful in treatment of variety of diseases including ______, _____ , CHF, _____, ______ , _____ & ______.
hypertension
angina pectoris; asthma
depression; BPH
Glaucoma
ADRENOCEPTORS CONT’D
Also useful in therapeutic situations e.g. ____ ,_____ labour, _______ & as adjuncts to general _______.
shock
premature; opioid withdrawal
anaesthesia
Outliers
_____ may represent a particular conformational state of the α1A-ADR.
___ is a species orthologue of the human α2A subtype hence it is not considered to be a separate subtype.
α1L
α2D
Location of beta1 receptors
Heart
Juxtaglomerular cells
Location of beta 3 receptors
Fat cells
Beta 2 isn’t in 3 places
List them
Eye
Skin
Genital tract
Alpha 1 isn’t in some places
Mention them
Lungs, bronchioles, pancreas, kidney
Location of alpha 1 receptors
Most vascular smooth muscle
Pupillary dilator muscle
Pilomotor smooth muscle
Location of beta 2 receptors
Respiratory, uterine and vascular smooth muscle
Liver
Pancreatic B cells
Location of alpha 2 receptors
Platelets
Some vascular smooth muscle
Adrenergic and cholinergic nerve terminals
Action of alpha 1 receptor in the pilomotor smooth muscle
Contracts to erect hair
Action of alpha 2 receptor in the Adrenergic and cholinergic nerve terminals
Inhibit neurotransmitter release
Action of alpha 2 receptor in platelets
Stimulates aggregation
Action of beta 1 receptor in the juxtaglomerular cells
Stimulates renin release
Action of beta 2 receptor in the respiratory, uterine, and vascular smooth muscle
Relaxes
Action of beta 2 receptor in the liver
Stimulates glycogenolysis
Action of beta 2 receptor in the pancreatic B cells
Stimulates insulin release
Action of beta 2 receptor in the somatic motor nerve terminals
Causes tremor
Action of beta 3 receptor in the fat cells
Lipolysis
AGONISTS
Non-selective agonists: ____. (α1, α2, β1 , β2 , β3); ____ (α1, α2, β1»_space; β2 ); ______ (β1 + β2).
Adr
NA
Isoprenalol
Isoprenalol uses _____ adrenergic receptors
Beta1 and beta2
α1 agonists:
List 6
Methoxamine,
Mephentermine
Phenylephrine
Midodrine
Oxymetazoline
Tetrahydrozoline
Xylometazoline
Metaraminol
Alpha 1 agonists
________ and ______also act indirectly to release NA.
Mephentermine & Metaraminol
Alpha 1 agonists
________ is a pro-drug.
Midodrine
AGONISTS (α1 agonists)
Prominent Pharmacological Action (PPA): vaso_______
Principal Therapeutic Uses (PTUs):
Pressor agents (Rx of _____ & shock – _______ and _______ )
_____ decongestants (_____,_____,_____,______ & some preparations of phenylephrine).
Vasoconstriction
hypotension; methoxamine & phenylephrine
nasal; oxymetazoline, tetrahydrozoline, xylometazoline, naphazoline
________________________ (PPA)
Prominent Pharmacological Action
PTU= ________
Principal therapeutic uses
AGONISTS (α1 agonists)
Adverse Effects (AEs): ____tension, headache, ______ cardia, excitability, restlessness, ____ mouth, sedation & rebound ______ ff. abrupt withdrawal.
Hyper
reflex brady
dry
Sedation
hypertension
α2 agonists:
List 8
Clonidine
Apraclonidine
Brimonidine
dexmedetomidine
Guanfacine
Guanabenz
α-methyldopa
Clenbuterol.
α2 agonists
_______ and ______ are used topically for glaucoma and ocular hypertension.
_______ is converted in CNS to α-methylNA (α2 agonist).
Apraclonidine & Brimonidine
Methyldopa
Alpha 2 agonist drugs Used very often as centrally-acting sympatholytic
vasodilators for the Rx of hypertension.
F
occasionally as centrally-acting sympatholytic
vasodilators for the Rx of hypertension.
AGONISTS (α2 agonists)
PPAs: (decreased or increased?) sympathetic outflow resulting in (decreased or increased?) peripheral vascular resistance and (decreased or increased?) production of aqueous humour.
Decreased
Decreased
Decreased
Alpha 2 agonists
PTUs:
Adjunct therapy in _____; ____tension; to (decrease or increase?) sympathetic response to withdrawal from narcotics, alcohol & tobacco; ______.
shock
hyper; decrease
glaucoma
AE=________
Adverse effects
Alpha 2 agonists
AEs:_______, ____ mouth & nasal mucosa, cardia, orthostatic ____tension, _____, constipation, nausea & gastric upset, ____arrythmia, (reduced or increased?) CO, ___tension etc.
Sedation
dry; brady
hypo; impotence
brady
Reduced; hypo
β1 agonists:
Mention 3
Dobutamine, Denopamine and Xamoterol.
β1 agonists:
Use with caution in patients with _______ or ________
Administer only through ___.
Hypertension or cardiac arrhythmias
IV
β1 agonists:
PPAs:
(decrease or increase?) in cardiac contractility
some (decrease or increase?) in HR
(decrease or increase?) AV conduction.
Increase
Increase
Increase
β1 agonists:
Dobutamine has strong _____ effect with little __ effect = ________________________
inotropic; chronotropic
increase in CO without significant increase in HR.
β1 agonists:
PTUs: (Short or long?) -term treatment of impaired cardiac function after cardiac surgery, CHF and myocardial infarction.
Short
β1 agonists:
AEs: (increased or decreased?) BP and HR.
Increased
β2 agonists:
List 11
Albuterol
Bitolterol
Fenoterol
Procaterol
Formoterol
Salmeterol
Isoetharine
Ritodrine
Terbutaline
Metaproterenol
Salbutamol.
Salmeterol is a (short or long?) acting beta ___ agonist
2
Beta 2 agonist
Use with caution in patients with __________
Danger is reduced by ______ administration; as _____)
minimal side effects →_____ acting.
CV disease
inhalational; aerosols
intermediate
Agonists (β2 agonists)
PPAs:
(Contraction or Relaxation?) of bronchial smooth muscle
(Contraction or Relaxation?) of uterine SM
activation of other β2Rs after ____
Relaxation
Relaxation
systemic administration.
Agonists (β2 agonists)
PTUs:
______ and _______ disease
acute _____ (use ______ acting drugs);
______________
prophylaxis in respect of _______ (use ____ acting agents).
Asthma & chronic obstructive pulmonary
bronchospasm
short & intermediate
premature labour
premature labour; long
For premature labour use ______
Ritodrine
Agonists (β2 agonists)
AEs: Headache, anxiety, nausea, muscle ______, ________,_______etc
tremors
nervousness
palpitations
β3 agonists:
List 4 etc.
Amibegron, Mirabegron, Ro40-2148, Solabegron, Vibegron
α1 Adrenergic Receptors
Are positively coupled to ____ via ______ α protein of the heterotrimetric G protein family to increase ____
PLC
Gq/11
IP3/DAG.
α1 Adrenergic Receptors
Sequence of events e.g. for vascular smooth muscle contraction
I.________
II. Activation of ____ by ____ subunit
III. Liberation of ____
IV. Activation of ____ receptors ( ____release channel in ___ )
V. Release of _____ into intracellular space leading to increased __ concentrations
VI.Stimulation of smooth muscle (contraction or relaxation?)
Binding of agonist
PLC; Gαq
IP3 and DAG
IP3; Ca; SR
stored Ca
Ca
Contraction
α2 Adrenergic Receptors
_____vely couple to __ via ____ subunit which (stimulates or inhibits ?) ____ formation.
Negati
Adenyl Cyclase
Gαi
Inhibits; cAMP
α2 Adrenergic Receptors
Sequence of events e.g. for inhibition of NT release
I. Binding of agonist
II. Inhibition of _______
III. Reduced ____
IV. Reduced activation of ____
V. Reduced ______ of __-type ___ channels on nerve terminals
VI. Reduced _____ during membrane depolarization
VII. Reduced vesicular release of NT
adenylyl cyclase
cAMP
PKA
phosphorylation; N; Ca
Ca influx
β1 Adrenergic Receptors
___vely couple to ________ via ___ protein leading to ____eased ——- formation.
Posti
adenylyl cyclase
Gαs
increased cAMP
β1 Adrenergic Receptors
Sequence of events e.g. for positive chronotropy
I. Binding of agonist
II. Activation of _____
III. Increased ____
IV. Activation of ___
V. Promotion of ______ of ____ channels in the membrane of _____ cells
VI. Increased __ward ___ current
VII. (Slower or Faster?) nodal cell _______ to the _______
VIII.Positive chronotropy
adenylyl cyclase
cAMP; PKA
phosphorylation; Ca; SA node
in; Ca
Faster; depolarization; firing threshold
β1 Adrenergic Receptors
Sequence of events e.g. for positive ionotropy
I. Binding of agonist
II. Activation of _____
III. Increased ____
IV. Increased _____-dependent ____ of __-type calcium channels in _____ membrane
V. Enhanced ___ influx
VI. Larger trigger signal for release of Ca from the ___ into the intracellular space
VII. Entry of trigger Ca into the ___ leading to ______ such that next trigger _____________ through _______ receptors
adenylyl cyclase
cAMP; PKA
phosphorylation; L; myocyte
Ca; SR
SR; increased Ca storage
initiates larger efflux of calcium
ryanodine
β2 Adrenergic Receptors
Sequence of events e.g. for vascular smooth muscle relaxation:
I. Binding of agonist
II. _______ of adenylyl cyclase
III.______ cAMP
IV._____ of PKA
V._______ and ______ of ________ kinase
VI. Reduced ___________________
VII. Reduced ______ thus ability to _________ is inhibited.
VIII.Reduced smooth muscle contraction
Activation
Increased; Activation
Phosphorylation and inactivation; myosin light chain
affinity of MLCK for Ca-calmodulin
activity of MLCK; phosphorylate myosin light chain
α2 Adrenergic Receptors
Sequence of events e.g. for peripheral vasoconstriction
I. Binding of agonist
II.______ of adenylyl cyclase
III._______ camp
IV._______ of pKa
V. _______ of MLCK
VI. Vascular smooth muscle constriction
Inhibition
Reduced
Inhibition
Activation
Alpha 1 ANTAGONISTS
PPAs:
(increased or decreased?) peripheral vascular resistance (promote vaso_____)
(Tense or relax?) smooth muscles in neck of bladder & in prostate.
Decreased ; dilation
Relax
Alpha 1 ANTAGONISTS
PTUs: Primary ___tension; ____ retention; (increased or decreased?) urine flow in BPH.
hyper
urinary
Increased
Alpha 1 ANTAGONISTS
AEs: _______ tension when therapy is instituted; reflex _____cardia
Postural hypo
tachy
α2 antagonists
PPAs:
(Increased or decreased?) sympathetic outflow & potentiate release of NA from nerve endings
Results in _______ of α1 & β1 Rs in the heart & peripheral vasculature → ↑ BP.
Increased
activation
Alpha 2 ANTAGONISTS
PTUs: Ingredient in many _____ products; extensive use in treatment of _________
AEs: ____eased HR ,BP and can cause _____
weight loss
male sexual dysfunction.
Incr; severe tremors
β-BLOCKERS
PPAs:
(Increased or decreased?) HR
(Increased or decreased?) contractility
(Increased or decreased?) CO
(Fast or slow?) conduction in atria & AV node
(Increased or decreased?) refractory period, AV node
Broncho (constriction or dilatation?)
prolonged ____glycaemia
(Increased or decreased?) plasma free fatty acids
(Increased or decreased?) HDLc
(Increased or decreased?) LDLc & triglycerides
——kalemia.
Decreased
Decreased
Decreased
Slow
Increased
Constriction
Hypo
Decreased
Decreased
Increased
Hypo
β-BLOCKERS
PTUs:
______
____tension
cardiac _____
__________ failure
______________
________
hypertropic obstructive cardiomyopathy
_____thyroidism
____ prophylaxis
_________ symptoms
substance _______
_______ bleeding in portal hypertension.
Angina pectoris hyper
arrhythmias
Congestive heart
pheochromocytoma
glaucoma
Hyper
migraine
acute panic
withdrawal
variceal
β-BLOCKERS
AEs:
___cardia
__ve ionotropic effect
(Increased or decreased ?)CO
___________
(Increased or decreased ?) AV conduction
Broncho (constriction or dilatation?)
fatigue
____ disturbances
prolongation of ___glycemia
__________ in men
drug interactions.
Brady
Negati
Decreased
bradyarrythmias
Decreased
constriction
Sleep
hypo
sexual dysfunction
Beta blockers
Pharmacological effects depend largely on _________________
degree of sympathoadrenal tone.
Beta blockers
Bronchoconstriction is of concern in _______ and _____
asthmatics & COPD.
β-BLOCKERS CONT’D
Hypoglycemia is of concern in ______ and ______
hypoglycemics and diabetics.
β-BLOCKERS CONT’D
3rd generation non-selective agents have as their PPAs – _________ effect; ISA; _________.
membrane stabilizing
vasodilation
ISA =_________________
Intrinsic sympathomimetic activity
The non-selective alpha adrenergic blocker; *_______________ * is the major drug used to treat PHEOCHROMOCYTOMA
PHENOXYBENZAMINE
Alpha 1 agonists end with ????
Mention the exception
Ines (mine, line, rine)
Metaraminol
Alpha 2 agonists end with ????
Mention the exception
Dine
Clenbuterol
Alpha methyl dopa
Guanfacine
Guanabenz
List the beta 1 agonists
Dobutamine
Denopamine
Xamoterol
Beta 2 agonists all end with???
List the exceptions
Terol
Metaproterenol
Isoetharine
Ritodrine
Salbutamol
Terbutaline
Beta 3 agonists all end with ??
Begron
List the alpha non selective antagonists
Phenoxybenzamine
Phentolamine
Tolazoline
Alpha 1 selective antagonists end with ??
Osin
List the alpha 2 selective Antagonists
Yohimbine
Imiloxan
Idazoxan
Beta 2 selective antagonists?
Butoxamine
Beta non selective antagonists end with ?
Lol
Beta 1 selective antagonists are?
A
A
B iso
B eta
M
E
N ebivolol
