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FTM2 > Adrenergic Agonist/Antagonists > Flashcards

Adrenergic Agonist/Antagonists Flashcards

1
Q

Direct Acting Agonists (3)

A
  1. Epinephrine
  2. Norepinephrine
  3. Dopamine

Endogenous Catecheolamines

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2
Q

Epinephrine Effects

(7)

A
  1. Acts on both alpha and beta receptors
  2. Increases HR/Contractile force (b-1 effect)-increase O2 consuption by the heart
  3. Increases renin release (b-1)
  4. Constricts arterioles in skin and viscera (a-1)
  5. Dilates BV of skeletal muscle (b-2)
  6. Relaxes bronchiol smooth muscle (b-2)
  7. Increases glycogenolysis/lipolysis (b1,b2)
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3
Q

What happens when giving a pt a low dose of epi?

A
  1. PVR decreases d/t b-2 receptors are more sensitive to epi than a-1 receptors
  2. Diastolic pressure falls
  3. Systolic pressure increases d/t increases cardiac contractility (b-1)
  4. HR increases (b-1)

No increase in mean BP so the baroreceptor reflex does not kick in

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4
Q

What happens when giving a high dose of epi?

Uses as well

A
  1. Increase in ventricular contraction (b-1)
  2. Increase in HR (b-1)-opposed by the baroreceptor reflex
  3. Vasoconstriction (a-1)

Uses: anaphylactic shock, cardiac arrest, asthmatic attacks

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5
Q

Norepinephrine Effects

A

Alpha 1,2 and Beta 1
1. Peripheral vasoconstriction (a-1)
2. Increase cardiac contractility (b-1)
3. Increase in BP stimulates baroreceptors leading to reflex bradycardia

Tx: shock-increase BP

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6
Q

Isproterenol

A

Non-selective beta adrenergic agonist
1. Activates b-1/2
2. Increases HR, contractility, and CO (b-1)
3. Dilates arterioles of skeletal muscle (b-2)
4. Diastolic pressure decrease-systolic remains unchanged (could go up)
5. Bronchodilation (b-2)
6. Used in emergencies to stimulate HR in pt’s with HB and bradycardia

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7
Q

Dobutamine

A

Beta-1 Selective Adrenergic Agonist
1. Potent inotrope-mild chronotropic effects
2. Less increase in HR and decrease in PVR than isoproterenol
3. Mild vasodilation
4. Increase in cardiac O2 consumption-stress echocardiogram

Management of Acute HF, cardiogenic shock

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8
Q

Albuterol

A

Beta-2 Adrenergic Agonist
1. Causes bronchodilation
2. Used with ICS in asthma
3. DOC for acute asthma attacks

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9
Q

Salmeterol/Formoterol

A

Beta-2 Adrenergic Agonist
Prolonged duration compared to albuterol

Used in asthma

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10
Q

Mirabegron

A

Beta-3 adrenergic agonist-detrusor muscle relaxation and increases bladder capacity

Tx: Overactive bladder, urinary incontinence

Moderate CYP2D6 inhibitor

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11
Q

Adverse effects of Mirabegron

A
  1. Increase BP
  2. Increased UTI
  3. Headache
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12
Q

Phenylephrine

A

Alpha-1 adrenergic agonist
1. Vasoconstriction

Uses:
1. Nasal decongestant. Given PO/topical
2. Mydriasis
3. Tx of hypotension from vasodilation in anesthesia

NO CYCLOPLEGIA

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13
Q

Clonidine

A

Alpha-2 Adrenergic Agonist
CENTRALLY ACTING ANTIHYPERTENSIVE
1. Activates central presnypatic alpha-2 adrenoceptors which reduces sympathetic outflow thus reducing BP

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14
Q

Adverse effects of Clonidine

A
  1. Lethargy
  2. Sedation
  3. Xerostomia
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15
Q

Methyldopa

A

Activates central alpha 2 adrenoceptors
* Drug of choice for Tx of hypertension in pregnancy

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16
Q

Methylphenidate

A

Unknown mechanism

Increases Norepi and dopamine reuptake inhibitor

Tx: ADHD in kids

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17
Q

Atomoxetine

A

Selective inhibitor of NET

Tx: ADHD in kids

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18
Q

Modafinil

A

Psychostimulant

Inhibits norepinephrine and dopamine transporters

Tx: Narcolepsy

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19
Q

Adverse effects of Methyldopa

(3)

A
  1. Sedation
  2. Impaired mental concentration
  3. Xerostomia
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20
Q

Brimonidine

A

Highly selective alpha 2 agonist

Tx: lower intraocular pressure in glaucoma (reduces aqueous humor production and increase outflow)

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21
Q

Amphetamine

Indirect Acting Adrenergic Agonist- RELEASING AGENT

A

Causes norepinephrine release by reversing monoamine transporters

Uses: ADHD, Narcolepsy

CNS stimulatory action
Can increase BP, stimulatory effects on heart

22
Q
A
23
Q

Cocaine

Indirect Acting Adrenergic Agonist-UPTAKE INHIBITOR

A

Monoamines accumulate in synaptic space-potentiation and prolongation of their central and peripheral actions

Blocks voltage-activated sodium channels

Sympathetic effects like tachycardia, HTN, peripheral vasoconstriction, pupil dilation

*Most potent at blocking DAT (dopamine transporter)-higher concentrations block SERT and NET

SERT=5-HT transporter
NET=Norepi transporter

24
Q

Tyramine

Indirect Acting Adrenergic Agonist- RELEASING AGENT

A

Found in fermented foods-normally oxidized by MAO.

  • Causes release of catecholamines by reversal of NET (Norepi transporter)

If taken w/ MAO-Massive Vasopressive effects

25
Q

Ephedrine

Mixed Acting Adrenergic Agonist

A

Used as a pressor agent during spinal anaesthesia

Tx: Adjunct therapy in myasthenia gravis

Not a catecholamine but penetrates CNS

26
Q

Pseudoephedrine

Sudafed

A

Mixed Acting Adrenergic Agonists
-Nasal decongestant

27
Q

Phenoxybenzamine

A

Non-selective alpha Adrenergic Blocker
1. Irreversible antagonist
2. Not good for HTN

Uses: Prior to surgery for pheochromocytoma or for management of inoperable tumors

28
Q

Phentolamine

A

Non-Selective Alpha Adrenergic Blocker
1. Reversibly blocks alpha 1/2 receptors

Uses:
1. Dx of/management of pheochromocytoma (phentolamine blocking test= Decrease in BP = pheochromocytoma)
2. Prevention of dermal necrosis aftra extravasation of norepinephrine
3. HTN crisis d/t stimulate OD

29
Q

Epinephrine Reversal

A

Alpha adrenergic blockers reverse epinephrine effect but vasodilation of Beta-2 receptors not blocked.

Systemic BP decreases in response to epi given in the presence of phenoxybenzamine

30
Q

Prazosin, Terazosin, Doxazosin

A

Selective blocker of Alpha-1 adrenergic receptors
Uses:
1. HTN (not drugs of choice)
2. BPH-drug of choice for symptom relief-relaxes smooth muscle
3. First dose can have exaggerated hypotensive response so small first dose (1/4, 1/3) for first three meds

Prazosin=prototype

31
Q

Tamsulosin

A

Treatment for Benign Prostatic Hyperplasia
Selective Alpha-1A receptor (predominates in GU smooth muscle).

  • Minimal effect on BP
  • Less likely to cause orthostatic hypotension
32
Q

Propranolol, Nadolol, Timolol

A

Beta Adrenergic Blockers
CVS effects: slow HR and decrease myocardial contractility
Respiratory: contraindicated for pts with asthma
Metabolic: decrease glycogenolysis, glucagon secretion

Propranolol=prototype

33
Q

Atenolol/Metoprolol/Esmolol

A

Selective Beta-1 Adrenergic Blockers

  1. impaired pulmonary fx
  2. diabetic pts

Esmolol: ultra short half life, used for rapid control of ventricular rate

34
Q

Pindolol

A

Partial beta-Agonist
Preferred in individuals w/ diminished cardiac reserve or a propensity to bradycardia

35
Q

Labetalol/Carvedilol

A

Alpha-1, Beta-selective Blockers

Labetolol: substantially more potent b-antagonist than alpha. (Competitive)

Carvedilol: Antioxidant properties. Used for HTN/CHF

36
Q

Timolol

A

Tx for glaucoma-diminish intraocular pressure

37
Q

Beta blocker uses (10)

A
  1. HTN
  2. Glaucoma (timolol)
  3. Migraine prophylaxis
  4. Hyperthyroidism-blunt sympathetic stimulation
  5. Angina-chronic management
  6. A Fib-control ventricular rate
  7. Myocardial infaction-protective effect
  8. Prevention of bleeding from esophageal varices
  9. Performance Anxiety
  10. Essential Tremor
38
Q

Beta-blocker adverse effects

Hypoglycemia

A

Nonselective beta blockers impaire recovery of hypoglycemia d/t blockade of beta-2 receptors in liver

Also mask tachycardia seen in hypoglycemia (early warning sign)

39
Q

Beta blocker adverse effect

Lipid Metabolism

A

Inhibit release of free fatty acids from adipose tissue
1. Increase TAGs
2. REduce HDL

Both negative impact

40
Q

Can you withdraw from beta blockers abruptly?

A

No-should be taper to avoid tachycardia, htn, ischemia (rebound effect d/t increased receptor count)

41
Q

Methyltyrosine (Metyrosine)

A

Competitive inhibitor of tyrosine hydroxylase (Inhibit norepi synthesis)

  1. Management of malignant pheochromocytoma
  2. Preop preparations for pheochromocytoma
42
Q

Reserpine

A

Irreversibly blocks VMAT-vesicles that store norepi/dopamine

  1. Gradual decrease in BP and HR
  2. Treated HTN in the past
43
Q

Valbenazine

A

Reversible inhibitors of VMAT

Tx of tardive dyskinesia

44
Q

Tetrabenazine

A

Reversible inhibitors of VMAT

Tx of chorea in Huntington’s Disease

45
Q

Contraction of the pupillary dilator (radial) in the iris has what function and receptor?

A

Mydriasis

Alpha 1 receptor

46
Q

Contraction of the pupillary constrictor (sphincter) muscle in the iris causes has what function and receptor?

A

Miosis

M3 receptor

47
Q

Contraction of the ciliary muscle has what function?

And receptor

A

Adapts to short range focus (M3)

48
Q

What is the function of ciliary epithelium?

A

Produce aqueous humour

Receptors: Beta2, alpha2, D1-3, FP (prostaglandins)

49
Q

Latanoprost

A

Activates FP receptors to increase uveoscleral outflow decreasing intraocular pressure

FP=prostaglandin

50
Q

Acetazolamide, dorzolamide

A

Inhibition of carbonic anyhdrase reduces formation of aqueous humor thus decreasing intraocular pressure

51
Q

Overview table of ocular hypotensive drugs

A
52
Q

Common Autonomic Adverse Effects

Muscarinic agonists, AChE inhib, Antimuscarinics, Stimulants

A

FTM2 (10 decks)

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