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Antiadrenergic Drugs (Exam 1) Flashcards

1
Q

Antiadrenergics

A
  • Compound that inhibits the effects of exogenous catecholamines or adrenergic agonists
  • Also includes Adrenergic blocking agents/drugs that deplete catecholamines (epi/NE/dopamine)
  • Adrenergic alpha and beta blockers
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2
Q

Sympatholytic

A

Compound that inhibits the response due to sympathetic nerve stimulation on alpha or beta receptors

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3
Q

Adrenergic antagonists

A

Agents that inhibit or reverse the effects of NE and epinephrine (alpha and beta antagonists)

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4
Q

-osin

A

Alpha antagonist

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5
Q

-lol

A

Beta antagonist

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6
Q

Mixed Antagonists

A

labetalol (Trandate)

carvedilol (Coreg)

Receptor Affinity: ß1=ß2 ; a1>a2

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7
Q

doxazosin (Cardura)

prazosin (Minipress)

terazosin (Hytrin)

A

alpha1 selective antagonists

-direct relaxation of arterioles and veins

*Peripheral vascular disease and pheochromocytoma (Adrenal gland tumor)

High incidence of orthostatic/postural hypotension

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8
Q

afluzosin (Uroxatral)

*doxazosin (Cardura)

*prazosin (Minipress)

silodosin (Rapalfo)

tamsulosin (Flomax)

*terazosin (Hytrin)

A
  • Benign Prostatic Hyperplasia
  • Blockade of alpha1a receptor in prostate = smooth muscle relaxation in bladder neck and prostate (increasing urine flow)

*Note doxazosin, prazosin, and terazosin are also used to manage hypertension

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9
Q

What should you think when you see B2? How about B1?

A

B2 think lungs

B1 think heart

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10
Q

What are some of the major therapeutic adrenergic antagonists used for hypertension? What’s an important not to add on beta blockers in general?

A

Note: beta blockers in general are old medications and FDA-approved indications do not necessarily reflect current practice

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11
Q

What is the drug of choice for a hypertensive emergency (historically used for a cocaine overdose)? Why?

A

IV labetalol (Trandate)

  • ß1 = ß2 and alpha blockade (antagonist)
  • No unopposed alpha unlike other beta-blockers
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12
Q

How do certain beta blockers indicated for hypertension control act? (3)

A
  • Decrease:
    1) Heart rate
    2) Renin release (BP decrease)
    3) Myocardial contractility and cardiac output (block epinephrine)
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13
Q

What are certain beta blockers with an established mortality benefit for systolic heart failure? (reduced ejection fraction)

A
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14
Q

Which beta blockers have intrinsic sympathomimetic activity? What are these contraindicated for?

A

acebutolol (Sectral)

penbutalol (Levatol)

pindolol (Visken)

-Mycocardial infarction or angina

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15
Q

Which beta blockers have been shown to improve mortality, prevent cardiac remodeling/arrythmias, and reduce angina in patients with ischemic heart disease or recent MI?

A
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16
Q

Which beta blocker is a class 3 K+ channel blocker and also considered an anti-arrythmic?

A

sotalol (Betapace)

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17
Q

How can beta blockers be used for rate control in the treatment of supraventricular arrythmias such as atrial fibrillation?

A

Because they block conduction through AV node via ß1 blockade

*metoprolol (Lopressor/Toprol) is the most common for a-fib

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18
Q

What are specific examples of beta blockers used for glaucoma and what is their mechanism of action?

A

They decrease aqueous humor production by the ciliary body to decrease introcular pressure

*eye drop form

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19
Q

What are some miscellaneous uses of propranolol (Inderal) due to certain special properties?

A

Special properties: very lipophilic & penetrates the BBB; membrane stabilizing effects, which inhibits action potentials across membranes acting like a local anesthetic

-Migraine prophylaxis

-Essential (benign) tremor

Thyrotoxicosis

Antipsychotic-induced akathisia (movement disorder)

Off-labels: stage fright

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20
Q

What are some of the side effects of beta blockers?

A
  • Bradycardia and heart block
  • Bronchospasm
  • Disturbance in glucose metabolism
  • CNS
  • Sexual
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21
Q

Which is worse for bronchospasm: selective or non-selective beta blockers?

A

Non-selective are worse (best to use a ß2-specific antagonist)

-At high doses, ALL beta blockers become non-selective

22
Q

How can you tell if someone on beta-blockers is hypogycemic (or becoming hypoglycemic)?

A

They will have excessive sweating and and mood changes still; however, other signs and symptoms are inhibited

23
Q

What are some of the CNS side effects of beta blockers?

A

Fatigue, drowsiness, depression, sleep disturbance, and nightmares

*Dependent on lipid solubility

24
Q

What are the low lipid soluble beta blockers?

A

acebutolol, atenolol, betaxolol, bisoprolol, esmolol, nadolol, and timolol

25
Q

What are the medium lipid-soluble beta blockers?

A

Labetalol, metoprolol, and pindolol

26
Q

What are the high lipid soluble beta-blockers?

A

Carvedilol, nebivolol, and propranolol

27
Q

Phentolamine (OraVerse)

A

Nonselective alpha blocker

  • Vasodilation around area of injection
  • Used for reversal of soft tissue anesthesia

*Side effect is marked orthostatic hypotension

28
Q

phenoxybenzamine (Dibenzyline)

A

Non-selective Alpha blocker

  • Long acting and irreversible
  • Blocks both pre- and post-synaptic receptors causing vasodilation

(Pheochromocytoma sweating and hypertension)

*Side effect is marked orthostatic hypotension

29
Q

Ergot Alkaloids effects

A
  • Produced by a fungus that infects rye/other grains
  • Gangrene of extremities, hallucinations, delirium, uterine stimulation/miscarriage

Affects alpha adrenergic receptors (coonstriction) seratonergic and dopaminergic receptors (hallucinations)

30
Q

ergonovine (Ergotrate)

A

Control of postpartum/postlabortal hemhorrage

Alpha and seratonin agonist

31
Q

methylergonovine (Methergine)

A

Used to induce uterine contraction and to control bleeding

Seratonin agonist

32
Q

bromocriptine (Cycloset, Parlodel)

A

treatment of Parkinson’s disease (dopamie agonist)

33
Q

ergotamine/dihydroergotamine

A

Migraine treatment (alpha vasoconstriction and stimulation of serotonin receptors)

*Often combined with caffeine in formulations to facilitate absorption

34
Q

What is the toxicity of ergot alkaloids for:

  • Acute use
  • Chronic use
  • Overdose
A

Acute use: GI disturbances (diarrhea/nausea/vomit)

Chronic use: gangrene of nose, finger, and ears due to severe vasoconstriction and prolonged vasospasm

OD: muscle contraction, hallucination, delirium, and convulsion

35
Q

What is a contraindication to Ergot Alkaloid use?

A

Obstructive vascular disease and collagen diseases

(can cause connective tissue proliferation)

36
Q

How many serotonin receptors have been cloned? What are the most common?

A

14

Most common:

  • 5-HT1
    • ​Brain
  • 5-HT2
    • ​Brain and peripheral tissue​
  • 5-HT3
    • ​Chemoreceptive and vomiting centers in CNS/periph. sensory and enteric nerves
37
Q

What are the effects of seratonin on the CV system?

A

Contraction of smooth muscles

Constricts most vascular beds

38
Q

What are the effects of seratonin on blood platelets? Small intestine? CNS?

A
  • Enhances platelet aggregation
  • Increased intestinal motility
  • Mood changes/cognition/sexual behavior/learning/memory/sleep/appetite/perception of pain/depression/anxiety
39
Q

5-HT1B/1D Receptor agonists

A

Triptans

-Used to treat migraines by preventing vasodilation

Stimulation of these receptors ( presynaptic trigeminal nerve endings) inhibits the release of vasodilating peptide (Calcitonin gene related peptide/CGRP)

Contraindications: coronary/cerebral vasospasm; coronary artery disease or stroke

40
Q

sumatriptan (Imitrex)

A

Selective Seratonin 5-HT1B/D agonist

migraine treatment

41
Q

When are selective serotonin receptor agonists especially toxic?

A

When they are used in comnination with anti-depressants that increase serotonin levels! This can lead to Serotonin Syndrome

42
Q

Seratonin Syndrome Management

  • Mild
  • Moderate
  • Life Threatening
A

Mild: Observe 6 hours and Benzodiazepines (sedative)

Moderate: Admit to hospital/heart monitoring/Cyproheptadine

Life Threatening: ICU; Esmolol (IV ß1 agonist)

43
Q

Symptoms of Serotonin Syndrome

  • Mild
  • Moderate
  • Life Threatening
A

Mild: pupils dilated (mydriasis), shivering, sweating, and mild tachycardia

Moderate: Altered mental status, autonomic hyperactivity, and neuromuscular abnormalities

Life threatening: delirium, hypertension, hyperthermia, muscle rigidity, and tachycardia

44
Q

CGRP Antagonists

A

Migraine specific and monoclonal antibodies (-mab suffix)

  1. Fremanezumab: attaches to CGRP receptor
  2. Galcanezumab: attaches to CGRP receptor
  3. Erenumab: blocks CGRP receptor
45
Q

How many half lives before a medication’s effect is gone?

46
Q

If drug A has a therapeutic index of 3 and drug B has a therapeutic index of 50, which would be the greatest safety concern?

A

Drug A (drug b is safer)

47
Q

Which agency regulates safety and efficacy of drugs?

48
Q

Which route of administration works the fastest?

49
Q

Will a drug bound to plasma-protein have activity?

50
Q

What are the parts of kinetics of drugs (pharmacokinetics)?

A

ADME

Absorption, Distribution, Metabolism, Elimination

Pharmacology (7 decks)

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