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Pharm Exam 1 > Wakade - Adrenergic Pharmacology IV > Flashcards

Wakade - Adrenergic Pharmacology IV Flashcards

1
Q

Antiasthmatic Agents:

A

EPI, ISO, Ephedrine

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2
Q

EPI:

Effects:
Used for:

A

EPI: potent beta2 agonist used for severe cases of asthma (status asthmaticus)

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3
Q

ISO:

Effects
Why is it no longer used?

A

ISO: potent beta2 agonist that is no longer used (risk of cardiac stimulation because of beta1 R)

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4
Q

Ephedrine:

May also be used prophylactically to:

Nose and eyes:

A

Ephedrine: used to treat asthma and chronic bronchitis

May also be used prophylactically to prevent asthma attacks

Nasal decongestant and pupil dilator

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5
Q

More Selective Beta2 Agonist: although not 100% selective (4)

A

 Orciprenaline
 Salbutamol
 Terbutalin
 Salmeterol (TOSS)

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6
Q

Anaphylactic Shock:

Treat

A

Anaphylactic Shock: parenteral EPI, NE or phenylephrine

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7
Q

Circulatory Shock:

Treat

A

Circulatory Shock: IV NE, metaraminol (may not be useful and may even worsen condition)

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8
Q

Use with local ansthetics:

EPI/PE (phenylephrine)

A

EPI/PE: employed with local anesthetics to cause vascoconstriction and to keep drug at injection site longer

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9
Q

Use with local ansthetics:

EPI/PE/Methoxamine/NE

A

Employed to maintain BP during spinal anesthesia

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10
Q

Urticaria (Hives)

Nasal decongestant:

Mydriatic agent:

CNS stimulant:

A

Urticaria: EPI

Nasal Decongestant: Phenylephrine (PE), naphazoline

Mydriatic Agent: PE, ephedrine (topical to the eyes)

CNS Stimulant: amphetamine, methamphetamine

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11
Q

Dobutamine (Unique Adrenergic Agonist):

L Isomer:

D Isomer:

Use:

A

Racemic Mix:

L Isomer: acts on both types of receptors
 Alpha agonist
 Weak beta1 agonist

D Isomer:
 Alpha1 antagonist
 Potent beta1 agonist
- Overall Result: selective beta1 agonist

Acute management of heart failure (improve cardiac output)
o Stimulate heart for stress test

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12
Q

ADRENERGIC RECEPTOR BLOCKING AGENTS:

• General:

A

Inhibit Agonist Actions: NE, EPI and others at the level of the RECEPTOR (inhibit effector organ responses)

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13
Q

Alpha Adrenergic Antagonists

2 major classes

A

Alpha 1——–postsynaptic- smooth muscles of blood vessels, secretory glands, GI muscle,
etc,

Alpha 2 ——-presynaptic- sympathetic neurons, CNS, blood platelets, Beta cells of
pancreas, etc.

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14
Q

Selectivity:

A

Alpha1| Prazosin > Phenoxybenzamine > Phentolamine > Yohimbine |Alpha2

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15
Q

Result of Alpha Adrenergic Blockade:

Both Alpha 1 and 2

Just alpha 2

A

Both Alpha1 and 2 (General):

  • Decrease in BP due to decrease in vascular resistance
  • Decreased blood pressure causes reflex tachycardia and increased CO

Alpha2 Antagonists:

  • Exaggerate these reflexive effects because of enhanced release of NE that acts on beta1 receptors of the heart
  • Blockade in the CNS (pontomedullary region) can “disinhibit” SS drive to the periphery, resulting in increase SS outflow and NE release in heart and blood vessels
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16
Q

Alpha Adrenergic Antagonists Drugs Divided into 3 Chemical Groups:

A
  1. Haloalkylamines: phenoxybenzamine
  2. Imidazolins: phentolamine
  3. Qunazolins: prazosin (gaining popularity)
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17
Q

Haloalkylamines (Phenyoxybenzamine):

Mechanism

A

Mechanism: non-competitive reversible inhibitor of alphaR
- Forms a covalent bond with alphaR (occupies for 12-24 hours)

Other Actions:

  • Blocks neuronal/extraneuronal uptake of NE
  • Blocks 5-T, ACh and histamine receptors as well

Use:

  • Management of pheochromocytoma and severe HTN
  • Treatment of peripheral vascular disease (Raynaud’s Syndrome)
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18
Q

Imidazolins (Phentolamine):

Mechanism:

Use:

A

Imidazolins (Phentolamine):

Mechanism: competitive reversible antagonist of alphaR

Use:

  • Control HTN in patients with pheochromocytoma
  • Treatment of hypertensive crisis following abrupt withdrawal of clonidine or the ingestion of tyramine when using MAOIs
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19
Q

Quanazolins (Prazosin):

Mechanism:

Use:

Duration:

What is Doxazosin?

A

Mechanism: selective alpha1 antagonist (1000 times greater affinity for alpha1 than alpha2)

Use: favored over previous two

  • Primary HTN (decreases BP)
  • Congestive cardiac failure (reduces preload and afterload)

Short duration of action: 6 hours (downfall)

Doxazosin: newer alpha1 blocker with longer duration of action (20 hours)

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20
Q

Tamulosin

Mechanism:

Use:

A

(Flomax):

Mechanism: targets specifically alpha1A receptors that are abundant in the smooth muscle of the human prostate gland

Use: treatment of patients with urinary issues due to BPH

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21
Q

Beta Adrenergic Antagonists:

Basics:

A

Most important agents from clinical standpoint

22
Q

Conditions Treated with Beta Blockers: many, including the following

A 
o	High blood pressure
o	Angina
o	Irregular heart rhythms 
o	Prevention of a second heart attack
o	MI
o	Migraines
o	Tremors
o	Alcohol withdrawal
o	Anxiety (PTSD)
o	Glaucoma
23
Q

Propanolol:

Mechanism:
Partial agonist activity?

Effects:
Alone?
What activates it?
What results in decreased HR and CO?
Blockage of exercise/stress induced effects result in:
How is peripheral resistance affected?
Renin:
A

Protypic classic beta blocker

Mechanism: selective competitive beta-receptor antagonist
 No partial agonist activity
 Membrane stabilization activity (local anesthetic-like activity)

Effects: has very little effect of its own on the heart or CV system; however, exerts profound effects when SS control is elevated (ie. exercise or stress)

  • Blockage of B1 receptors of heart results in decreased HR and CO
  • Also reduces sinus rate and slows conduction
  • Blockage of exercise/stress induced effects result in decreased O2 demands (use in angina and coronary artery disease)
  • Peripheral resistance increased (beta2 block) –> possible increase in BP initially
  • This could produce compensatory decrease in SS discharge to the heart
  • Blocks release of renin from juxtaglomerular apparatus (beta1 block)
  • Anti-HTN effect
24
Q

Other general beta blocker effects:

Hyperthyroidism
Glaucoma/Occular HTN
Anxiety
migraine

A

Hyperthyroidism: reduce peripheral manifestations(increased HR/CO, tremors)

Glaucoma/Occular HTN: reduce intraocular pressure (reduction in aqueous humor)
- Timolol Issue: also non-specific (blocks beta1 and beta2), and some entered system complicating asthma (block beta2 receptors leading to ↓ bronchodilation)

Anxiety: normally due to increased activity of SNS

Prophylaxis of migraine headaches: blockage of CNS beta receptors, reducing vasodilation

25
Q

Important Considerations Before Recommending Beta Blockers

A

Should not be given to patients with diabetes (mask signs of hypoglycemia)

Should not be given to asthmatic patients

Can worsen congestive heart failure, Raynaud’s syndrome and diabetes

Should not use concomitantly with Ca++ channel blockers (AV block)

Should be withdrawn gradually after prolonged use (avoid withdrawal, which can precipitate MI)

26
Q

Other Non-Selective Beta Blockers (block both beta1 and beta2): (6)

A 
o	Carteolol (slight partial agonist activity)
o	Levobunolol
o	Nadolol (long half life compared to others)
o	Pindolol (partial agonist activity + slightly membrane stabilizing)
o	Timolol (slight partial agonist activity)
o	Penbutolol (slight partial agonist activity)
27
Q

Selective Beta Blockers:

Examples of Beta1 Selective Blockers: heart specific (5)

A

Important Note: the higher the concentration of these drugs, the less selective they become

Acebutolol (some partial agonist activity)

Atenolol

Betaxolol (slight membrane stabilizing activity)

Esmolol (very short half life compared to others)

Metoprolol (slight membrane stabilizing activity)

28
Q

Bystolic:

Effects:

A

Recently approved: more specific for beta-1 blocker

Effects:
Reduces cardiac force of contraction
Reduces HR
Causes vasodilation and reduction in TPR

29
Q

Alpha and Beta Receptor Blocking Agents:

General:

A

Block both alpha and beta adrenergic receptors (relatively new)

30
Q

Labetelol (Normodyne, Trandate):

Mechanism:

  • Ratio of activity:
  • Membrane stabilizing?
  • Action on presynaptic alpha2R
  • NET

Effects:
Effect on HR/CO:

Use:

A

Mechanism: nonselective competitive blocker (alpha and beta)

Ratio of beta:alpha activity is ~3:1 (orally) or ~7:1 (IV)
- Also has some intrinsic activity (partial agonist)
- Also has good membrane stabilizing action (less excitable membrane; local anesthetic-like action)
- Very little action on presynaptic alpha2 receptors
 Can block NET

Effects:
Most prominent effect in humans is lowering peripheral vascular resistance WITHOUT a major change in HR or CO

Use:

  • Primary hyptertension
  • Hypertension with angina
  • Preoperative management of patients with phechromocytoma
31
Q

Alpha-methyl tyrosine
Site of Action:
For use in:

A

Alpha-methyl tyrosine

blockade of tyrosine hydroxylase

rarely used

32
Q

Reserpine
Site of Action:
For use in:

A

Reserpine
inhibition of storage of NE
hypertension

33
Q

Guanethidine
Site of Action:
For use in:

A

Guanethidine
inhibition of release & storage of NE
hypertension

34
Q

Clonidine
Site of Action:
For use in:

A

Clonidine

inhibition of release of NE (alpha2)

hypertension
Diarrhea
In diabetic neropathy
Narcotic, alcohol withdrawal
Quit smoking
Reduce menopausal hot flashes
35
Q

Apraclonidine
Site of Action:
For use in:

A

Apraclonidine

inhibition of NE release (alpha2)

Decrease in intraoccular pressur
glaucoma

36
Q

Brimonidine
Site of Action:
For use in:

A

Brimonidine

inhibition of NE release (alpha2)

glaucoma

37
Q

Alpha-methyl –DOPA
Site of Action:
For use in:

A

Alpha-methyl –DOPA

inhition of release of NE (alpha2)

hypertension

38
Q

Imipramine, desipramine
Site of Action:
For use in:

A

Imipramine, desipramine

inhibition of NE transporter

depression

39
Q

Cocaine

Site of Action:
For use in:

A

Cocaine

inhibition of NE transport

no use, abused for CNS stimulation

40
Q

Amphetamines
Site of Action:
For use in:

A

Amphetamines

inhibition of NE transport

narcolepsy, weight loss (?)

41
Q

Epinephrine
Site of Action:
For use in:

A

Epinephrine

bronchodilation ( beta2 receptors): bronchospasm

Vasoconstriction (alpha1 receptors): anaphylactic shock, Urtcaria local & spinal anestesia

42
Q

Isoproterenol
Site of Action:
For use in:

A

Isoproterenol
bronchodilation ( beta2 receptors)
bronchospasm

43
Q

Orciprenaline
Site of Action:
For use in:

A

Orciprenaline

bronchodilation ( beta2 receptors)

bronchospasm

44
Q

Salbutamol

Site of Action:
For use in:

A

Salbutamol

bronchodilation ( beta2 receptors)

bronchospasm

45
Q

Terbutalin

Site of Action:
For use in:

A

Terbutalin

bronchodilation ( beta2 receptors) bronchospasm

relaxation of pregnant uterus (beta 2) delay premature labor

46
Q

Ritodrine

Site of Action:
For use in:

A

Ritodrine

relaxation of pregnant uterus (beta 2)

delay premature labor

47
Q

Ephedrine

Site of Action:
For use in:

A

Ephedrine

bronchodilation (beta2 receptors) bronchospasm

Release of NE ( alpha1 receptors) eye examination (mydriatic)

48
Q

Phenylephrine

Site of Action:
For use in:

A

Phenylephrine

vasoconstriction (alpha1 receptors) local & spinal anesthesia

Constriction of mucous membranes (alpha) nasal decongestion

49
Q

Methoxamine

Site of Action:
For use in:

A

Methoxamine

vasoconstriction (alpha1 receptors)

local & spinal anesthesia

50
Q

Metaraminol

Site of Action:
For use in:

A

Metaraminol

vasoconstriction (alpha1 receptors)

local & spinal anesthesia

51
Q

Dopamine

Site of Action:
For use in:

A

Dopamine

increase heart rate, contraction & cardiac output
( release of NE, beta1 receptors of the heart,
dilation of renal blood vessels, D1 receptor )

cardiogenic shock

52
Q

Dobutamine

Site of Action:
For use in:

A

Dobutamine

direct activation of beta1 receptors,
dilation of renal blood vessels (D1)

cardiogenic shock

Pharm Exam 1 (23 decks)

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