Adrenergic Drugs Flashcards

1
Q

Epinephrine

A

Direct Acting Endogenous Catecholamine

Receptors: a &B2 (low dose B, high Dose a)

Effect: Increase lipolysis, hyperglycemia,High dose-potent vasopressor, bronchodilation Low dose-tachycardia , Does not Enter CNS

Uses: DOC patient in anaphylactic shock

AE: Not given orally, CNS disturbances, intracranial hemorrhage, cardiac arrhythmias, pulm. edema

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2
Q

Norepinephrine

A

Direct Acting Endogenous Catecholamine

Receptors: A&B1> B2

Effects: Bradycardia, vasoconstriction, induces hyperglycemia

Uses: Limited therapeutic value, can treat shock, control BP

AE: may cause kidney shutdown

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3
Q

Dopamine

A

Direct Acting Endogenous Catecholamine

Receptors: D& a& B

Effects: Low dose-vasodilate, Intermediate-increasing release of NE, High Dose-a1 mediated vasoconstriction( increase BP)

Uses: DOC for cardiogenic and hypovolemic shock, TXT for severe CHF

AE: ineffective orally, Overdose causes sympathomimetic symptoms, causes nausea.

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4
Q

Isoproterenol

A

Direct Acting B-agonist

Receptor: B1 & 2

Effects: CVS-increase: CO, lipolysis,HR, hyperglycemia Decrease: MAP, TPR, DBP GI relax

Uses: Stimulate heart in emergency pts. bradycardia or heart lock + cardiogenic shock

AI: Similar adverse effects

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5
Q

Dobutamine

A

Direct acting B-agonist

Receptor: B1

Effect: increase CO with little change in heart rate

Uses:Acute management of congestive heart failure

AE: can build up tolerance

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6
Q

Albuterol

A

Direct Acting B-Agonist

Uses: Relief symptoms in asthma (no effect on heart)

AE: tremor, restlessness, apprehension and anxiety

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7
Q

Salmeterol

A

Direct Acting B-agonist

Uses: long acting Bronchodilator (note used for prompt relief of bronchospasm)

AE: tremor, restlessness, apprehension and anxiety

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8
Q

Formoterol

A

Direct Acting B-agonist

Uses: long acting Bronchodilator (note used for prompt relief of bronchospasm)

AE: tremor, restlessness, apprehension and anxiety

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9
Q

Phenylephrine

A

Direct Acting a-agonist

Receptor:a1

MOA: peripheral vasoconstriction

Effect: vasoconstrictor, increases: SBP and DBP(No effect on hear but causes reflex bradycardia)

Uses: Nasal decongestant, TXT of supraventricular tachycardia

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10
Q

Clodine

A

Direct Acting a-agonist

Receptor:a2

MOA: Partial agonist

Uses: Antihypertensive

AE: Sedation, Mental lassitude, impaired concentration, Xerostomia, Lethargy

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11
Q

Methyldopa

A

Direct Acting a-agonist

Receptor:a2

MOA: central acting anti-HTN

Uses: DOC in pregnant patient with HT N

AE: Sedation, Mental lassitude, impaired concentration, Xerostomia, Lethargy

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12
Q

Brimonidine

A

Direct Acting a-agonist

Receptor:a2

MOA: decreases aqueous humor production along with increased outflow

Uses: Glucom

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13
Q

Amphetamine

A

Indirect Acting Agonist

Receptor:little effect on post sympatic a and B

MOA: displaces catechol form storage vesicle,weak MAO, blocks catecholamine reuptake

Uses: Depression, narcolepsy, appetite suppression

AE: fatigue and depression following stimulation

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14
Q

Methylphenidate

A

Indirect Acting Adrenergic Agonist

Receptor: structural analog of amphetamine

Uses: ADHD in children, Narcolepsy

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15
Q

Tyramine

A

Indirect Acting Agonist

Uses:not clinically useful but is found in fermented foods(cheese & wine)

AE: serious vasopressor episodes in patients on MAO-I release of NE

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16
Q

Cocaine

A

Presynaptic Indirect Agonist

Receptor: DAT,SERT, NET

MOA: Blocks dopamine(major), serotonin NE transporters

Uses: local anesthetic of the resp. tract

AE: Intense euphoria

17
Q

Atomoxetine

A

Presynaptic Indirect Agonist

Receptor:NET

MOA:selective NET inhibitor

Uses:ADHD

18
Q

Modafinil

A

Presynaptic Indirect Agonist

Receptor: DAT,NET

MOA:inhibit NE and Dopamine transporter (increases: NE, Dopamine, Serotonin, glutamate Decreases: GABA)

Uses: Narcolepsy

19
Q

Ephedrine

A

Mixed Acting Agonist

Receptor: a & B

Uses:Asthma, synergistic effect with anti- AChe in treatment of MG, increases athletic performance

AE: Banned in 2004 due to life-threatening cardiovascular reactions

20
Q

Pseudoephedrine

A

Mixed Acting Agonist

Receptor: a & B

MOA: Ephedrine enantiomer

Uses: Nasal decongestant with H1 histamine antagonist

21
Q

Phenoxybenzamine

A

a-antagonist

Receptor: non selective a

MOA:Alkylation irreversibly blocks receptor, slight a1 selective also block:H1, M and 5-Ht receptors, inhibits NET

Effects: prevents vasoconstriction of peripheral vessels, increases CO

Uses: DOC pheochromocytoma

AE: Postural hypotension, Nasal stuffiness, Inhibits ejucatation. Contraindicated in pts with low coronary perfusion

22
Q

Phentolamine

A

a-antagonist

Receptor: non selective a

MOA:reversible a block, Serotonin blocker, Muscarinic, H1 and H2 agonist

Uses: hypertensive episodes of pheochromocytoma, prevents dermal necrosis, antihypertensive in stimulant overdose,

AE: Postural hypotension, Arrhythmia & angina, contraindicated in pts with low coronary perfusion

23
Q

Prazosin

A

a-antagonist

Receptor: selective a1, useful in treatment of HTN

MOA:↓TPR through relaxation of
arterial and venous smooth
muscle

Effects:↓ BP without reflex
tachycardia […α2]↓ LDL/TAG, ↑HDL Improves urinary
blood flow

Uses: TXT of HTN, BPH

AE:First dose effect may cause exaggerated
hypotensive response and syncope [adjust 1st
dose ¼ of normal]

24
Q

Terazosin

A

a-antagonist

Receptor: selective a1, useful in treatment of HTN

MOA:Structural analog of prazosin →longer t1/2 → Less frequent dosing

Effects:↓ BP without reflex
tachycardia […α2]↓ LDL/TAG, ↑HDL Improves urinary
blood flow

Uses: TXT of HTN, BPH

AE:First dose effect may cause exaggerated
hypotensive response and syncope [adjust 1st
dose ¼ of normal]

25
Q

Doxazosin

A

a-antagonist

Receptor: selective a1, useful in treatment of HTN

MOA:Structural analog of prazosin →longer t1/2 → Less frequent dosing

Effects:↓ BP without reflex
tachycardia α2]↓ LDL/TAG, ↑HDL Improves urinary
blood flow

Uses: TXT of HTN, BPH

AE:First dose effect may cause exaggerated
hypotensive response and syncope [adjust 1st
dose ¼ of normal]

26
Q

Tamsulosin

A

a-antagonist

Receptor: selective a1, useful in treatment of HTN

MOA:Selective for α1A receptor found in genitourinary smooth muscle

Effects:Relaxes genitourinary
smooth muscle

Uses:Used in TXT of BPH with little effect on BP

AE:First dose effect may cause exaggerated
hypotensive response and syncope [adjust 1st
dose ¼ of normal]

27
Q

Propranolol

A

B-antagonist

Receptor:β1 & β2

MOA:CVS: ↓ HR, ↓contractility &↑TPR [β2] Metabolic: ↓
glycogenolysis and glucagon
secretion→ severe hypoglycemia in pts on insulin

Uses:DOC for performance anxiety/stage fright, HTN [through ↓CO, not the DOC] Migraine [blocks vasodilation] Hyperthyroidism Chronic angina [↓O2 requirement] A-fib, MI (protective)

AE:Bronchoconstriction→ Contraindicated in patients with COPD or asthma

CNS: sedation, dizziness, lethargy, fatigue, depression

28
Q

Nadolol

A

B-antagonist

Receptor:β1 & β2

MOA:Longer duration of
action

Uses:Long term treatment of angina and HTN

29
Q

Timolol

A

B-antagonist

Receptor:β1 & β2

Uses:HTN prophylaxis for migraines Glaucoma [open angle]

30
Q

Atenolol

A

B-antagonist

Receptor: β1 Cardioselective

Uses:Management of HTN in pts with impaired pulmonary
function or IDDM
Long term mgmt. of pts w/ angina pectoris/acute MI

AE:Less likely to induce bronchospasm contraindicated in asthmatics

31
Q

Metoprolol

A

B-antagonist

Receptor: β1 Cardioselective

Uses:Management of HTN in pts with impaired pulmonary
function or IDDM
Long term mgmt. of pts w/ angina pectoris/acute MI

AE:Less likely to induce bronchospasm contraindicated in asthmatics

32
Q

Esmolol

A

B-antagonist

Receptor: β1 Cardioselective

Uses:Useful in controlling arrhythmia [supraventricular or
thyrotoxicosis] Perioperative HTN, MI in acutely ill pts

AE:Associated with hepatic injury

33
Q

Labetalol

A

Combined a1 & B antagonist

Receptor:α1 & β

MOA:Decrease in BP:
α1→ relaxation of arterial smooth muscle
β1→ blocks sympathetic reflex
β2→ sympathomimetic action contributes to vasodilation

AE:Orthostatic hypotension and dizziness [α1]

34
Q

Carvedilol

A

Combined a1 & B antagonist

Receptor:α1 & β

Uses: pts with CHF and HTN Antioxidant properties

35
Q

a-methyltyrosine

A

Presynaptic Antagonist

MOA:Blocks NE [& Epi] synthesis through competitive inhibition of tyrosine hydroxylase

Uses adjuvant therapy with Phenoxybenzamine in treatment of malignant
pheochromocytoma [when surgery is not possible]

36
Q

Reserpine

A

Presynaptic Antagonist

MOA:Irreversible damage to VMAT→ ↓NE and dopamine
availability→ sympatholytic response

Uses:Unable to concentrate and store NE and dopamine in the vesicle→ continuous breakdown by MAO ↓BP and ↓HR

37
Q

Tetrabenazine

A

Presynaptic Antagonist

MOA:Reversible inhibitor of VMAT- catecholamines
presynaptically

Uses:Chorea associated with Huntington’s Disease