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pharm > L4 Adrenergic Agonist and Antagonist > Flashcards

L4 Adrenergic Agonist and Antagonist Flashcards

1
Q

what are the Direct acting- selective drugs

A

a1- phenylephrine
a2-clonidine
b1-dobutamine
b2-terbutamine

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2
Q

what are the direct acting- non selective drugs

A

a1a2-oxymetazoline
b1b2-isoproterenol
a1a2b1b2-epinephrine
a1a2b1-norepinephrine

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3
Q

what is the mixed acting drug

A

a1a2b1b2-ephedrine

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4
Q

what are the indirect acting- releasing agents drugs

A

-amphetamine
-tyramine

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5
Q

what are the indirect acting-uptake inhibitor

A

cocaine

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6
Q

what are the indirect acting- MOA inhibitor

A

Seleliline

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7
Q

what are the indirect acting- COMT Inhibitor

A

entacapone

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8
Q

what drug when uses causes response that are NOT REDUCED WITH PRIOR TREATMENT for the direct acting selective and non selective drugs

A

RESERPINE OR GUANETHEDINE WHICH DEPLETE NE

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9
Q

What drugs cause the response to be potentiated for direct acting selective and non selective drugs

A

COCAINE, RESERPINE AND GUANETHEDINE

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10
Q

what drug when uses causes response that are REDUCED WITH PRIOR TREATMENT for the mixed- acting drug

A

RESERPINE AND GUANETHEDINE

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11
Q

what drug causes response to be abolished by prior treatment for indirect acting-releasing agent amphetamine and tyramine

A

RESERPINE AND GUANETHEDINE

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12
Q

what is the main agonist for the a1 b1 b2 receptor

A

NE

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13
Q

where is the alpha 1 receptor primarily found

A

blood vessels

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14
Q

Agonist and Antagonist of alpha 1

A
  • Agonist: NE
  • Antagonist: Phentolamine
    (and phenoxybenzamine, which is used to treat hypertension, MOA is vasodilation

Any drug that looks like NE and causes VC and increase in BP

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15
Q

what is the effect of a tumor of the adrenal gland

A

causes excessive production of NE and EPi, the treatment would be to administer phentolamine because it inhibits NE from binding to the synapse so blood pressure is reduced.

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16
Q

where is alpha 2 receptors found

A

presynaptic nerve terminals of postganglionic nerve
Control the release of neurotransmitters

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17
Q

Agonist and Antagonist for Alpha 2

A

Agonist: NE
* Antagonist: none
Quanidine (stimulate a2 receptor, used to treat hypertension)

  • Feedback mechanism and therefore decrease release of NE or dec BP
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18
Q

predominant alpha-adrenergic agonist responses are

A
  • Vasoconstriction and CNS stimulation
  • Primarily located on smooth muscle. vasculature or blood vessels and prostate
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19
Q

what is the function of NE transporter(NET)

A

carries NE into the cytoplasm of nerve cell

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20
Q

what is the function of VMAT

A

which carry NE into the vesicle

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21
Q

what is the effect of cocaine

A

blocks the NET protein, inhibits the NE reuptake

NE stays in the synapse cleft longer causing prolonged sympathetic activity

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22
Q

what is the effect of reserpine

A

-used to treat hypertension
-inhibits VMAT
prevents the refilling of vesicles of NE’, MAO in cytosil will breakdown the NE

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23
Q

where is Beta 1 primarily located

A

heart

Stimulate B1 will case increase in heart rate

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24
Q

where are beta 2 receptors primarily located

A

smooth muscle of the bronchioles, arterioles, and visceral organs, skeletal muscle, activates glycogenolysis

Stimulate B2 relax smooth muscle and cause bronchodilation or vasodilation

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25
Q

The beta-adrenergic agonist response results in

A
  • Bronchial, GI, and uterine smooth muscle relaxation
  • Glycogenolysis (B-receptor activation leading to activation of glycogen phosporylase which is rate limiting step in glycogenolysis)
  • Cardiac stimulation
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26
Q

what is the effect of dopamine(adrenergic receptor)

A

Stimulated by dopamine (inc HR)
* Causes dilation of the following blood vessels, resulting in INCREASED blood flow
* Renal
* Mesenteric * Coronary
* Cerebral

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27
Q

what are the 3 adrenergic receptors

A

Alpha
Beta
Dopamine

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28
Q

Effects of beta 1 at different locations

A

cardiac muscles- Increased contractility
AV Node- Increased heart rate
SA Node- Increased heart rate

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29
Q

Effects of beta 2 at different locations

A

Blood vessels- dilation
Muscle- Decreased motility
Bronchial- dilation, relaxation
uterus- relaxation

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30
Q

Effects of Alpha 1 at different locations

A

Blood vessels- constriction
bladder Sphincters- constriction
uterus- constriction

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31
Q

what examples cathecholamines molecules

A

-dopamine
-Norepinephrine (Norepinephrine)
-Epinephrine
-Isoproterenol (Isuprel)
-Dobutamine

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32
Q

where does cathechloamines binds

A

adrenergic receptors

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33
Q

what is the half life of catheclolamines

A

20 secs

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34
Q

what is the parent compound of catecholamines

A

Phenylethylamine(benzene ring without the OH on c3 and C4) is considered the parent compound which sympathomimetic drugs are derived

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35
Q

describe the chemical structure of catecholamines

A

-benzene ring with OH on c3 and c4
-ethylamine side chain

36
Q

How does increasing the size of the amino group affect the catecholamine structure

A

increase the alpha and beta receptor activity when groups are added at the (Beta carbon)

37
Q

how is the half life increased for catecholamines

A

altering the structure by adding groups to the (alpha carbon)

38
Q

Epinephrine

A

50%- Alpha
50%-Beta

39
Q

Norepinephrine

A

95%- Alpha
5%- Beta/Dopamine

40
Q

Isoproterenol

A

5%- Alpha
95%- Beta phenylephrine, Dobutamine

41
Q

Examples of noncatecholamines

A

-Ephedrine
-Phenylephrine
-Albuterol
-Methoxamine
-Amphetamine

42
Q

can catecholamine be administered orally

A

-no
it can be administered orally when the OH group on the benzene ring is removed.

43
Q

what is the rate limiting step in catecholamine synthesisq

A

Tyrosine——Tyrosine Hydroxylase—–> DOPA

44
Q

What is the major metabolite of NE/ EPI

A

-Vanillymandelic Acid (VMA), via MAO and COMT enzyme
-is the major metabolite found in the urine

45
Q

Describe the tyramine like effect

A

Drug interaction of MAOI with tyramine foods (beer, fava beans, cheese, yeast red wine…) will result in hypertensive crisis

-Tyramine inhibits MAO is NE is not degraded in the synapse, so the increased amount of NE binding to alpha 1 receptor causes BP to increase drastically
-also tyramine produces tyrosine which is the substrate for catecholamine production so this increase NE production

Patient on MAOI must avoid tyramine containing foods
* Broad beans, fava beans
* Cheese, natural or aged, cheddar gruyere, stilton * Chicken liver
* Chocolate
* Sausage
* Smoked herring
* Snails
* Wine
* yeast

46
Q
  • Increased force of contraction
A

(positive inotropic effect)

47
Q

Increased heart rate

A

(positive chronotropic effect)

48
Q

Increased conduction through the AV node

A

(positive dromotropic effect)

49
Q

One Therapeutic Use of Adrenergic Agents:

A

Anorexiants: adjuncts to diet in the short-term management of obesity

Examples: benzphetamine phentermine
dextroamphetamine Dexedrine

50
Q

One Therapeutic Use of Adrenergic Agents:

A

Bronchodilators: treatment of asthma and bronchitis

Examples:
albuterol
isoetharine
metaproterenol
ephedrine
isoproterenol
salmeterol
epinephrine
levalbuterol
terbutaline

51
Q

Bronchodilators- * Isoproterenol

A

Non selective B1, B2 agonist
* Most potent
* Indication: Bronchodilator
* Inhaler rapid onset
* Side effect: cardiac arrhythmia, due to B1 being stimulated

52
Q

Bronchodilator-Isoethraine

A
  • Inhaler
  • B1, B2
  • Indication: Bronchodilator
53
Q

Bronchodilator-Terbutaline

A
  • Prototype oral
  • B2 selective
  • PO, sc, inhaler, iv
  • PO long duration
  • Will cause caridac arrhythmia only art higher doses
  • SE: skeletal m tremor, restlessness
    -used to decrease uterine contraction to slow down the laboring process.
54
Q

Ritoridine

A
  • B2 agonist
  • Relaxes uterine smooth muscle
  • Indication: premature labor
  • May also use Terbutaline
55
Q

One Adrenergic Agents: Therapeutic Uses

A

Reduction of intraocular pressure and mydriasis (pupil dilation): treatment of open-angle glaucoma

Examples: epinephrine and dipivefrin

56
Q

One Adrenergic Agents: Therapeutic Uses

A

Nasal decongestant:
* Intranasal (topical) application causes constriction of dilated arterioles and reduction of nasal blood flow, thus decreasing congestion.

Examples: epinephrine, ephedrine, pseudoephedrine,naphazoline phenylephrine
tetrahydrozoline

57
Q

Nasal decongestants

A

-Phenylepherine
-Pseudophedrine
* Oral or nasal drops
* A1 agonist VC of mucosa in
nostrils
* “rebound nasal stuffiness” * Ischemia of nostrils
* Topical SE like cocaine
* CNS stimulation

58
Q

Nasal Decongestants Inhalers

A
  • Oxymetazoline LA (Afrin) * Xylometazoline LA
  • Tetrahydrazoline
  • Propylhexadrine
  • Phenylproponolamine
59
Q

Vasoconstrictors- Norepineherine (levaterenol, noradrenaline)

A
  • NE-like
  • Indicated for vascular shock
  • Vasopressor
60
Q

Vasoconstrictors- Epinepherine

A

-stimulates the a1 b1 b2 receptor
* VC and cardiac stimulant
* Increase in BP secondary to cardiac
* Indicated for anaphylaxsis ie insect bite, drug allergy
* Not as potent as levaterenol
* Will elevate BP by causing VC,
Inc HR
* SE: cardiac arrhythmias

61
Q

Vasoconstrictors-Ephedrine

A
  • Mau Huang
  • Oral form of epi
  • Resist breakdown by GI mucosa
  • A1, B1, B2
  • Indication: asthma attack (dilate airway)
  • Derivative of pseudoephedrine (difficult to get in pharmacy)
  • CNS stimulation
62
Q

Vasoconstriction- * Metaraminol iv

A
  • Vasopressor
  • Indirect acting amine
63
Q

Vasoconstriction-* Mephenteramine iv

A
  • Vasopressor
  • Direct and indirect
  • LA (long lasting)
64
Q

Phenmetrazine is a

A

anorexant

65
Q

Methylphenidate is a

A

Attention deficient disorder

66
Q

Pemoline is a

A

Attention deficient disorder

67
Q

Cocaine

A
  • Local anestetic
  • MOA: inhibit reuptake at noradrenergic synapses, inhibit dopamine
    ru pleasure center
  • Enters CNS and causes amphetamine like effect * Routes: smoked, snorted, injection
68
Q

Salmeterol

A

is indicated for PREVENTION of bronchospasms, not management of acute symptoms.

69
Q

Non selective alpha blocker

A

Phenoxybenzamine
Phentolamine

70
Q

Selective alpha 1 blocker

A

Prazosin
Doxazosin
Tamsulosin
Terazosin

-All except Tamsulosin is used to treat hypertension

71
Q

selective alpha 2 blocker

A

Mirtazapine
Yohimbine

72
Q

What are 2 drugs that are alpha and beta blocker

A

carvedilol
labetalol

73
Q

Alpha 1 Antagonist

A
  • Phentolamine (not a prodrug)
    -competitive inhibitor- reversible binding
  • Imidazole, a1
  • SE: a2, mild Ser, H1
  • Reduce periperhal vascular resistance
  • Cardiac stimulation due to baroreflex
  • iv
  • Tx: Pheochromocytoma
  • Phenoxybenzamine (a prodrug)
    -Covalently bond to a receptor-irreversible binding
  • a1 blockade LA
  • SE: same
  • Little fall in BP in normal patients only when BP is high
  • po
  • Tx; Pheochromocytoma
74
Q

Alpha 1 Antagonists

A
  • Prazosin, terazosin, doxazosin (HTN) * Tolazoline (PVD?)
  • Tamulosin, Alfuzosin a1a (BPH)
75
Q

Side Effects of Alpha blockers

A

Cardiovascular:Palpitations, orthostatic hypotension, tachycardia, edema, dysrhythmias, chest pain

CNS: Dizziness, headache, drowsiness, anxiety, depression, vertigo, weakness, numbness, fatigue

Gastrointestinal: Nausea, vomiting, diarrhea, constipation, abdominal pain

Other: Incontinence, nose bleeding, tinnitus, dry mouth, pharyngitis, rhinitis, nasal stuffiness, inhibit

76
Q

What molecules does beta blockers compete with

A
  • Compete with norepinephrine and epinephrine
77
Q

What receptors does Nonspecfic beta blockers block

A

block both beta1 and beta2 receptors

78
Q

Beta Blockers Cardiovascular effects

A
  • Reduction in cardiac output
  • Reduction of renin release from Juxtaglomerular cells of kidney
  • Central action to reduce sympathetic activity
79
Q

Beta Blockers
Metabolic and Endocrine Effects

A

-glycogenolysis is partially inhibited after B-2 receptor blockade(b2 blocker inhibits glycolysis)

80
Q

What is the outcome of giving a diabetic patient a non seclective beta blocker

A

the beta 2 being blocked would cause the inhibition of glycogenolysis, which reduces the glycogen level, plus the administration of insulin further reduce the glucose level and leads to hypogylcemia.

81
Q

What is the outcome of giving a asthmatic patient a non seclective beta blocker

A

the blockage of beta 2 receptor will cause bronchoconstriction, resulting in difficulty to breathe

82
Q

Beta Blockers Specific agents

A
  • Propranolol prototype B-blocker
  • Metoprolol and atenolol B1-selective
  • Nadolol long duration of action
  • Timolol: nonselective, use: glaucoma
  • Levobunolol (nonselective), Betaxolol (b1-selective) use: glaucoma
  • Pindolol, acebutolol, carteolol, bopindolol, oxprenolol, celiprolol, penbutolol, partial B agonist activitiy, less bradycardia, ISA uncertain, less lipid abnprmalities ie VLDL
83
Q

Esmolol (Beta Blocker)

A

ultra-short acting B1-selective blocker, short T1/2, iv infusion, use: supraventricular arrhythmias, arrhythmias associated with thyrotoxicosis, perioperative HTN, myocardial ischemia acutely ill

84
Q

Acetbutolol (Beta Blocker)

A

PVC= Premature Ventricular Contraction

-membrane stablizing drug= activity at the myocardium, so the drug has arrthymic properties

85
Q

Sotalol

A

ventricular arrhythmias and atrial fibrillation

86
Q

Beta blockers that also cause vasodilation

A
  • Labetalol , racemic mixture of two chiral isomers non selective beta blocker with alpha 1 blocking activity (less than Phentolamine)
  • Nebivolol B1 selective antagonist that causes vasodilation through and endothelium dependent mechanism
  • Carvedilolol (drug interactions due to inhibition CYP2D6 activity ie Quinidine and Fluoxetine) Medroxalol. Bucindolol, nonselective b blocker with capacity to block a1
87
Q

what is rebound hypertension

A

the use of a Beta blocker causes an increase in NE overtime, when a patient stop taking the beta blockers abruptly, the increase amount of NE binds to the receptor which causes drastic increase in blood pressure

pharm (5 decks)

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