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CPR II Pharm > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

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1
Q

Direct-acting Adrenomimetic Classes

A
  • Alpha agonists
  • Mixed alpha and beta agonists
  • Beta agonists
  • Dopamine agonists
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2
Q

Alpha agonists

A
  • Phenylephine

- Clonidine

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3
Q

Mixed alpha and beta agonists

A
  • NE

- Epi

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4
Q

Beta agonists

A
  • Dobutamine
  • Isopreterenol
  • Albuterol
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5
Q

Dopamine agonists

A
  • Dopamine
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6
Q

Indirect adrenominetics classes

A
  • inhibitors of MAO
  • inhibitors of reuptake of DA and NE
  • Reverse NE and DA uptake mechanisms and increase their release
  • Releasing agent and direct adrenergic receptor agonist
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7
Q

Inhibitor of re-uptake of DA and NE

A
  • Cocaine
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8
Q

Inhibitors of MAO

A
  • Phenelzine

- Selegiline

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9
Q

Reverse NE and DA uptake mechanisms

A
  • Amphetamines
  • Methylphrnidate
  • Tyramine (byproduct of tyrosine metabolism, not a drug)
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10
Q

Releasing agent and a direct adrenergic receptor agonist

A
  • Ephedrine
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11
Q

Direct acting antiandrenergic drug classes

A
  • alpha adrenergic antagonists
  • mixed blockers
  • beta adrenergic antagonists
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12
Q

Non-selective receptor antagonists

A
  • Phentolamine (reversible, competitive)

- Phenoxybenzamine (non-competitive, irreversible)

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13
Q

Alpha 1 selective antagonists

A
  • Prazosin
  • Tamsulosin
  • Doxazosin
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14
Q

Mixed antagonists (blockers)

A
  • Labetalol
  • Carvedilol
  • both are alpha and beta 1 antogonists
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15
Q

Beta 1 and Beta 2 blockers (nonselective)

A
  • Propranolol
  • Pindolol
  • Nadolol
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16
Q

B1 selective blockers

A
  • Metoprolol
  • Betaxolol
  • Acebutolol
  • Atenolol
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17
Q

Indirect acting antiandrenergic drug groups

A
  • NE release inhibitor

- inhibitor of tyrosine hydroxylase

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18
Q

NE release inhibitor

A
  • Guanethudine (indirect)
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19
Q

Inhibitor of tyrosine hydroxylase

A

Metyrosine (indirect)

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20
Q

Alpha 1 G protein and effects

A

Gq - Increase IP3 and DAG

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21
Q

Alpha 2 G protein and effects

A

Gi - decrease cAMP

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22
Q

Beta type G protein and effects

A

Gs - increase cAMP

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23
Q

Dopamine type G proteins

A
  • D1 and D5 - Gs - increase cAMP

- D2 - D4 - Gi - decrease cAMP

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24
Q

Epinephrine

A
  • a1 = a2; B1 = B2
  • Effects on cardiac function (B1)
  • – increase HR
  • – Increase force of contraction
  • – increase conduction velocity at AV node
  • Effects on vascular tone (B2 and a1)
  • – increases systolic BP
  • – may decrease diastolic BP and TPVR
  • Effects on respiratory system
  • – relaxed bronchial muscle (b2)
  • – decreased bronchial secretion and congestion within bronchial mucosa (a1)
  • Skeletal muscle
  • – muscle tremor (B2)
  • – increase K uptake by skeletal muscle (B2)
  • elevates blood glucose levels
  • – enhances liver gluconeogenesis and glycogenolysis (B2)
  • increases free fatty levels in blood (B)
  • increases renin release (B1)
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25
Norepinephrine
- a1 = a2; B1 >> B2 - cardiac stimulant but reduces HR - pontent vasoconstrictor - Lacks B2 agonist effects - Increases PVR and BP - Role of baroreflex
26
Phenylephrine
- alpha agonist; a1 - effective mydriatic and decongestant - severe vasoconstriction, BP elevation and severe bradycardia - role of baroreflex in the response to phenylephrine
27
Clonidine
- selective a2 agonist - central effect on a2 receptors in lower brainstem area - -- decreasing sympathetoc outflow - -- reduction in BP - -- bradycardia - local application produces vasoconstriction
28
Isoproterenol
- B agonist; B1 = B2 - nonselective - positive inotropic and chronotropic action, increases CO (B1) - vasodilator, decreases arterial pressure (B2) - causes bronchodilation (B2)
29
Dobutamine
- Beta agonist; B1 > B2, a1 - selective B1 agonist - (-) isomer is agonist; (+) isomer is antagonist (of a1) - potent inotropic action - less prominent chronotropic action compared to isoproterenol
30
Albuterol
- selective B2 agonist | - cause bronchodilation and relaxation of the uterus
31
Dopamine
- D1 = D2 - D1 stimulation causes vasodilation - activation of presynaptic D2 suppresses NE release - activate B1 in heart at higher doses - at even higher doses, stimulates vascular a1 AR to cause vasoconstriction
32
Indirect adrenergic agonist properties
- usually more lipophilic compounds | - easily penetrate BBB
33
Amphetamine , methamphetamine
- marked stimulant effect on mood and alertness - decrease appetite - drugs of abuse
34
Methylphenidate
- used in children with ADHD | - has abuse potential
35
Cocaine
- inhibits transmitter reuptake at adrenergic synapses - peripheral and intense central action - local anesthetic properties - heavily abused drug
36
Ephedrine
- releases stored catecholamines w/ some direct action - long duration of action - nonselecive - mild stimulant - clinical use - -- nasal decongestant - -- increases BP - -- stress incontinence in women
37
Phenelzine, Selegiline
- inhibitors of MAO - increase NE stores in CNS - antidepressant action
38
Tyramine
- product of tyrosine metabolism found in cheese, cured meats, smoked and pickled fish - releases stored NE from presynaptic terminals (if given parenterally) - is metabolized by MAO in live - may lead to increase in BP in patients taking MAO inhibitors
39
Which adrenergic agonist used to increase BP
- hypotensive emergencies - -- NE - -- Phenylephrine - Chronic hypertension - -- ephedrine - cardiogenic shock - -- dopamine - -- dobutamine
40
Heart Failure
- short term use of dobutamine in acute HF | - dopamine in congestive severe HF w/ reduced renal perfusion
41
Hypertension drug
Alpha 2 agonists for long term treatment
42
Emergency therapy for complete AV block and cardiac arrest
- Epi | - Isoproterenol
43
Narcolepsy Drugs
- amphetamines | - methyphenidate
44
ADHD drug
- methylphenidate
45
Obesity drug
- ephedrine | - amphetamines
46
Decongestion of mucous membranes
- phenyephrine | - ephedrine
47
Examination of retina (mydriasis)
- phenylephrine
48
Glaucoma
- alpha-2 selective agonists
49
GU applications
- ephedrine for urinary incontinence
50
CV adverse effects of adrenergic agonists
- elevation of BP - Increased cardiac work may precipitate myocardial ischemia and heart failure - sinus tachycardia and serious ventricular arrhythmias, may induce sudden cardiac death
51
Central nervous system toxicity
- insomnia - lack of appetite - anxiety, restlessness - psychoses - convulsions and hemorrhagic stroke (cocaine)
52
Effects of Alpha antagonists on CV system
- decreased PVR and BP - postural hypotension - reflex tachycardia
53
Effects of Alpha antagonists on GU system
- relaxation of sm muscle in prostate | - decreased resistance to the flow of urine
54
Effects of Alpha antagonists on the eye
- relaxation of pupillary dilator muscle - miosis
55
Pheochromocytoma treatment
- antag - phentolamine - phenoxybenzamine
56
Chronic (essential) hypertension treatment
- antag - Prozosin, Doxasin (a1 selective) - -- work well in moderate hypertension - -- generally well tolerated
57
Erectile dysfunction treatment
- combination of phentolamine and papaverine
58
BPH treatment
- Tamsulosin - -- greater affinity for a1A - Prozosin and doxazosim are also effective but will cause more pronounced drop in BP
59
Adverse Effects of alpha antagonists
- seen less with a1 selective - postural hypotension - tachycardia - retention of fluid and salt - impaired ejaculation - nasal stiffness
60
B blocker antagonists
- Atenolol - Nadolol - Propranolol - Betaxolol
61
B blocker partial agonists
- acebutolol - Lebetalol - Pindolol
62
B blocker inverse agonists
- Carvedilol | - Metoprolol
63
Full agonists
- fully activate receptors - produce maximal pharmacological effect when all receptors occupied - maximal intrinsic activity
64
Partial agonists
- partially activate upon binding - produce sub-maximal effect - intrinsic efficacy varies depending on drug
65
Inverse agonists
- decrease receptor signaling - decrease response at receptors with significant level of constitutive receptor activity - intrinsic activity present and related to inhibition of receptor function
66
Antagonists
- do not activate the receptor upon binding - no effect is agonist is not present - no intrinsic activity
67
Effects of B-blocker on CV
``` Heart - negative inotropic and chronotropic effect - slow AV node conduction Blood vessels - initially - rise in PVR - chronic - decrease in PVR RAS - inhibit renin release ```
68
Effects of B-blocker on respiratory system
- increase airway resistance
69
Effects of B-blocker on Eye
- reduce production of aqueous humor - reduce intracular pressure
70
Metabolic Effects of B-blocker
- inhibit lipolysis - increase VLDL and decrease HDL - inhibit glycogenolysis and glugoneogenesis in the liver
71
Clinical uses of Beta blockers
- hypertension (both b and mixed blockers) - angina pectoris - MI - cardiac arrhythmias - heart failure - glaucoma - hyperthyroidism (propranolol)
72
CNS B-blocker adverse effects
- sedation - sleep disturbances - depression - switch to more hydrophilic drug
73
Respiratory B-blocker adverse effects
- increased airway resistance - trigger bronchospasm and asthma attack in susceptible people - switch to B1 selective
74
CV B-blocker adverse effects
- depression of HR, cardiac contractibility and excitability | - exacerbation of peripheral vascular disease
75
Lipid profile B-blocker adverse effects
- chronic use - increase VLDL, decrease HDL - seen with both selective and non-selective - switch to partial agonist
76
Hypoglycemic episodes B-blocker adverse effects
- switch to B1 selective | - more on slide 49
77
Abrupt discontinuation of B blocker therapy
- increased numbers and responsiveness of receptors to endogenous agonists - enhanced cardiac stimulation and arrhythmias

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