Adrenergic Receptor Agonist And Antagonist Flashcards by Iseoluwa Ojo

ADRENOCEPTORS

 NA & Adr. play important roles in ___ control, _____ contractile rate & force, _____ reactivity and variety of metabolic & CNS functions.

myocardial

airway

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ADRENOCEPTORS CONT’D
 Agonists & antagonists have proved useful in treatment of variety of diseases including ______, _____ , CHF, _____, ______ , _____ & ______.

hypertension

angina pectoris; asthma

depression; BPH

Glaucoma

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ADRENOCEPTORS CONT’D

Also useful in therapeutic situations e.g. ____ ,_____ labour, _______ & as adjuncts to general _______.

shock

premature; opioid withdrawal

anaesthesia

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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

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Location of beta1 receptors

Heart

Juxtaglomerular cells

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Location of beta 3 receptors

Fat cells

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Beta 2 isn’t in 3 places

List them

Eye
Skin
Genital tract

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Alpha 1 isn’t in some places
Mention them

Lungs, bronchioles, pancreas, kidney

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Location of alpha 1 receptors

Most vascular smooth muscle
Pupillary dilator muscle
Pilomotor smooth muscle

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Location of beta 2 receptors

Respiratory, uterine and vascular smooth muscle
Liver
Pancreatic B cells

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Location of alpha 2 receptors

Platelets
Some vascular smooth muscle
Adrenergic and cholinergic nerve terminals

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Action of alpha 1 receptor in the pilomotor smooth muscle

Contracts to erect hair

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Action of alpha 2 receptor in the Adrenergic and cholinergic nerve terminals

Inhibit neurotransmitter release

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Action of alpha 2 receptor in platelets

Stimulates aggregation

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Action of beta 1 receptor in the juxtaglomerular cells

Stimulates renin release

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Action of beta 2 receptor in the respiratory, uterine, and vascular smooth muscle

Relaxes

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Action of beta 2 receptor in the liver

Stimulates glycogenolysis

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Action of beta 2 receptor in the pancreatic B cells

Stimulates insulin release

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Action of beta 2 receptor in the somatic motor nerve terminals

Causes tremor

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Action of beta 3 receptor in the fat cells

Lipolysis

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AGONISTS

 Non-selective agonists: ____. (α1, α2, β1 , β2 , β3); ____ (α1, α2, β1&raquo_space; β2 ); ______ (β1 + β2).

Adr
NA

Isoprenalol

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Isoprenalol uses _____ adrenergic receptors

Beta1 and beta2

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α1 agonists:

List 6

Methoxamine,
Mephentermine
Phenylephrine
Midodrine
Oxymetazoline
Tetrahydrozoline
Xylometazoline
Metaraminol

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Alpha 1 agonists

________ and ______also act indirectly to release NA.

Mephentermine & Metaraminol

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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

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