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Botany > adrenoceptor blockers > Flashcards

adrenoceptor blockers Flashcards

1
Q

 All active by
 Oral route
 Parenteral route

A

alpha blocking drugs

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2
Q

IRREVERSIBLE LONG-ACTING

	Prototype
	Only slightly alpha1 selective
	Short elimination half life
	Long duration of action (48 hours)
	Binds covalently to the alpha receptors
A

PHENOXYBENZAMINE

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3
Q

DoA of PHENOXYBENZAMINE

A

48 hours)

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4
Q

REVERSIBLE SHORT-ACTING

•	Prototype
•	Nonselective (alpha1=alpha2)
	Duration of action
	Oral (2-4 hours)
	IV (20-40 minutes)
A

PHENTOLAMINE

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5
Q

ALPHA1 SELECTIVE

 Prototype
 Selective reversible alpha1 blocker
 Duration of action 8-24 hours
 Doxasozin, terazosin and tamsulosin

A

PRAZOSIN

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6
Q
  • Prototype
  • Selective alpha2 competitive blockers
  • Used primarily in research application
A

YOHIMBINE, RAUWOLSCINE

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7
Q

NONSELECTIVE BLOCKERS

 Most important effects are on the ??

A

CVS system

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8
Q

 Predictable result of the use of an agonist in a patient who has received
an alpha-blocker
 Reversal in the BP effect of large doses of epinephrine
 From pressor response (alpha receptors) to a depressor response (beta receptors)
 Not observed with phenylephrine or NE because they lack sufficient beta2 effects

A

EPINEPHRINE REVERSAL

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9
Q

 Block alpha1 receptors much more effectively

 Cause much less tachycardia than the nonselective blockers when reducing BP

A

SELECTIVE ALPHA1 BLOCKERS

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10
Q

• Tumor that secretes cathecolamines

A

pheochromocytoma

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11
Q

type of BLOCKERS

• Severe hypertension caused by overdose with drugs of abuse such as amphetamine, cocaine, or phenylpropanolamine

A

NONSELECTIVE ALPHA

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12
Q

type of BLOCKERS
 Prazosin, doxazosin, and terazosin are used in hypertension
 Used together with tamsulosin for urinary hesitancy and prevention of urinary retention with benign prostatic hyperplasia

A

SELECTIVE ALPHA

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13
Q

Prazosin, doxazosin, and terazosin Used together with ? for urinary hesitancy and prevention of urinary retention with benign prostatic hyperplasia

A

tamsulosin

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14
Q

• TOXICITY of alpha blockers

•

A

Main manifestation is orthostatic hypotension

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15
Q

 Competitive pharmacologic antagonists
 Propranolol is the prototype
 Developed for chronic oral use
• Bioavailability and duration of action vary widely

A

BETA BLOCKING DRUGS

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16
Q

Beta1 receptor selectivity

A

Acebutolol
Atenolol
Esmolol
Metoprolol

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17
Q

Advantage when treating patients with asthma

A

Beta1 receptor selectivity

PARTIAL AGONIST ACTIVITY

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18
Q

Nonselective beta-blockers

A

 Nadolol
 Propranolol
 Timolol
 Pindolol

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19
Q

 Combined alpha and beta-blockers
 Optically active

A

Labetalol

 Carvedilol

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20
Q

PARTIAL AGONIST ACTIVITY
 ”Intrinsic sympathomimetic activity”

 May be an advantage in treating patients with asthma
 At maximum dose, can cause some bronchodilatation

A

Pindolol
 Acebutolol
 Labetalol

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21
Q

 ”Membrane stabilizing ability”
 Disadvantage when a beta-blocker is used topically in the eye because it decreases protective reflexes and increases the risk of corneal ulceration

A

LOCAL ANESTHETIC ACTIVITY

22
Q

LOCAL ANESTHETIC ACTIVITY

A 
	Acebutolol
	Labetalol
	Metoprolol
	Propranolol 	
	Pindolol
23
Q
  • Short-acting ester

* Used only parenterally

A

ESMOLOL

24
Q
  1. Longest acting beta-blocker
A

NADOLOL

25
Q

 Less lipid soluble

 Enter the CNS to a lesser extent

A

ACEBUTOLOL, ATENOLOL and NADOLOL

26
Q

 EFFECTS of beta blockers in CVS

A

 Decrease BP
 Antagonize renin secretion
 (-) inotropic effect
 (-) chronotropic effect

27
Q

 EFFECTS of beta blockers in RESPIRATORY

A

Bronchoconstriction

Increase airway resistance

28
Q

EFFECTS of beta blockers in EYE

A
  • Decrease intraocular pressure

* Decrease production of aqueous humor

29
Q

EFFECTS of beta blockers inMETABOLIC AND ENDOCRINE

A
  • Reduce insulin secretion

* Caution for insulin dependent DM

30
Q

 CLINICAL USES of beta blockers

A 
	Open-angle glaucoma
	Hypertension 
	Angina 
•	Arrhythmias
•	Chronic heart failure
•	Pheochromocytoma
31
Q

TOXICITY in CVS

A
  1. CVS
  2. Bradycardia
  3. AV blockade
  4. Heart failure
32
Q

TOXICITY in RESPIRATORY

A
  1. Worsen the asthma
33
Q

TOXICITY in CNS

A
  1. Sedation
  2. Fatigue
  3. Sleep alteration
  4. Depression
  5. Psychosis
34
Q

TOXICITY in CNS

A
  1. Sedation
  2. Fatigue
  3. Sleep alteration
  4. Depression
  5. Psychosis
35
Q

Conversion of the pressor response to epinephrine (typical of large doses) to a blood
pressure–lowering effect; caused by α blockers, which unmask the β2 effects of epinephrine

A

Epinephrine reversal

36
Q

Partial agonist action by adrenoceptor blockers; typical of several β blockers (eg, pindolol,
acebutolol)

A

Intrinsic sympathomimetic

activity (ISA)

37
Q

Local anesthetic action; typical of several β blockers (eg, propranolol)

A

Membrane-stabilizing

activity (MSA)

38
Q

Hypotension that is most marked in the upright position; caused by venous pooling (typical of α blockade) or inadequate blood volume (caused by blood loss or excessive diuresis)

A

Orthostatic hypotension

39
Q

A tumor consisting of cells that release varying amounts of norepinephrine and epinephrine
into the circulation

A

Pheochromocytoma

40
Q

Drugs used in glaucoma.

Beta blockers

A

Timolol, others

41
Q

Drugs used in glaucoma

Prostaglandins

A

Latanoprost, others

42
Q

Drugs used in glaucoma.

Cholinomimetics

A

Pilocarpine, physostigmine

43
Q

Drugs used in glaucoma.
Alpha agonists
Nonselective:

A

epinephrine

44
Q

Drugs used in glaucoma.

Alpha2-selective agonists

A

Apraclonidine, brimonidine

45
Q

Drugs used in glaucoma.

Carbonic anhydrase inhibitors

A

Acetazolamide, dorzolamide

46
Q

Drugs used in glaucoma.

Osmotic agents

A

Mannitol

47
Q

Clinical Applications

Pheochromocytoma, antidote to overdoseof α agonists

A

Phentolamine

48
Q

Clinical Applications
Pheochromocytoma,
carcinoid, mastocytosis, Raynaud’s
phenomenon

A

phenoxybenzamine

49
Q

Clinical Applications
Hypertension, benign
prostatic hyperplasia

A

PRAZOSIN

50
Q

Clinical Applications
Obsolete use for
erectile dysfunction •
research use

A

YOHIMBINE

51
Q 
Clinical Applications
Angina, arrhythmias
(treatment and prophylaxis), hypertension, thyrotoxicosis,
tremor, stage fright,
migraine
A

PROPRANOLOL

Botany (324 decks)

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