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Ther 201 Exam 2 > Adrenergic Agents and Blockers > Flashcards

Adrenergic Agents and Blockers Flashcards

1
Q

Adrenergic Agents are drugs that mimic actions of ________ and ________ and activate the _______ nervous system.

A

Epinephrine & Norepinephrine; sympathetic

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2
Q

Adrenoreceptor that increases the heart rate:

A

Beta-1

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3
Q

Identify the correct analogy of Dobutamine isomers:
Vasodilation: Vasconstriction

a. - isomer: + isomer
b. + isomer: - isomer

[Organ System Effects and Clinical Application of Sympathomimetics - Cardiovascular System -]

A

b.

+ isomer: VASODILATION
- isomer: VASOCONSTRICTION

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4
Q

Catecholamines are derived from these amino acids:

A

PHENYLALANINE & TYROSINE.

Phenylalanine -> hydroxylation by the enzyme phenylalanine hydroxylase -> Tyrosine -> L-DOPA -> DOPAMINE* -> NOREPINEPHRINE* (depending on cell type) -> EPINEPHRINE*

  • Catecholamines
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5
Q

Changes During The Flight or Fight Response of the Sympathetic Nervous System (identify if inc or dec)

BRONCHODILATION

A

inc

  • Basta imagine mo lang ano mga changes saýo pag crunch time na for exams!
  • Beta-2 Adrenoreceptor activation.
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6
Q

Changes During The Flight or Fight Response of the Sympathetic Nervous System (identify if inc or dec)

Saliva amount

A

dec

Nagddry ang mouth pag kulba or stress

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7
Q

Changes During The Flight or Fight Response of the Sympathetic Nervous System (identify if inc or dec)

Sphincter Muscle Tone

A

inc

Better urinary retention pag fight or flight response!
* Mag-iincrease lahat ng sphincter tone

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8
Q

Changes During The Flight or Fight Response of the Sympathetic Nervous System (identify if inc or dec)

Detrusor muscle tone

A

dec

Kasi pag nagcontract ang detrusor muscle ng bladder, mapapaihi ka. Better urinary retention ang nangyayari pag Fight or Flight response so dapat decreased detrusor muscle tone

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9
Q

Changes During The Flight or Fight Response of the Sympathetic Nervous System (identify if inc or dec)

Blood Pressure

A

inc

Higher blood pressure kasi mas malakas pumping ng heart for increased circulation. Basta fight or flight response, isipin mo lahat ng changes na pwedeng mgcontribute to better performance + usual manifestation of stress + energy release.

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10
Q

Manifestation of ULTIMATE EFFECTS during Fight or Flight response involves release of Norepinephrine from: ________ and Epinephrine is from _________

A

a Nerve terminals

b Adrenal Medulla

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11
Q

Preganglionic axons synapse on neurons close to the:

A

SPINAL CORD

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12
Q

A drug that inhibits the enzyme tyrosine hydroxylase and, therefore, catecholamine synthesis, which, as a consequence, depletes the levels of the catecholamines dopamine, adrenaline and noradrenaline in the body.

[Happens at postganglionic nerve ending

A

METYROSINE

Order of inhibition at postganglionic nerve ending (palabas ng nerve ending):

METYROSINE (Inhibits tyrosine -> dopamine)
RESERPINE (Inhibits dopamine -> norepinephrine)
GUANITHIDINE (inhibit the Ca2+-dependent release of norepinephrine -> impedes propagation of impulses to nerve terminals)

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13
Q

Adrenergic receptor that predominates in the presynaptic membrane.

A

Alpha-2

Location: Presynaptic adrenergic nerve terminals, platelets, lipocytes, SMOOTH MUSCLE, lower brainstem region (medulla oblongata).

Mechanism of Action: Gi, causes inhibition of adenyl cyclase, decreased cAMP (causes reverse effect of adrenergic activation) -> Therefore, Alpha-2 receptors behave like BLOCKERS!!

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14
Q

DIRECT or INDIRECT

Adrenergic agonists that bind directly to receptors

[Classification of Adrenergic Receptors]

A

DIRECT

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15
Q

DIRECT or INDIRECT

affects synthesis, storage, and release

[Classification of Adrenergic Receptors]

A

INDIRECT

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16
Q

The mechanism of action of this adrenergic receptor involves G-protein type Gq.

(GPCR)

Gq-> activates Phospholipase C -> formation of IP3 and DAG -> increased intracellular calcium -> metabotropic

A

Alpha-1

Location: Postsynaptic effector cells, heart, SMOOTH MUSCLES (e.g. BLOOD VESSELS esp arteries), GLANDS

  • Basta pag Alpha receptors = Smooth Muscles.
  • Para Alpha Male, ikaw pinaka-SMOOTH
  • Remember na PRESYNAPTIC = Alpha-2, POSTSYNAPTIC = Alpha-1 (pero hindi lang siya ang postsynaptic adrenergic receptor)
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17
Q

The most clinically significant adrenergic receptor in constriction and dilatation of blood vessels.

A

Alpha-1

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18
Q

The mechanism of action of this adrenergic involves receptor Gs protein.

Gs -> stimulation of adenyl cyclase (effector) -> increased cAMP

A

All Beta Adrenergic Receptors

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19
Q

Location of this adrenergic receptor is in Postsynaptic effector cells, especially HEART, LIPOCYTES, brain, presynaptic adrenergic and cholinergic nerve terminals, JUXTAGLOMERULAR CELLS of kidney.

A

Beta-1 Adrenergic Receptor:

  • Pag Beta-1 -> HEART

at JUXTAGLOMERULAR CELLS sa Kidney

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20
Q

Location of this adrenergic receptor is mainly in Postsynaptic effector cells especially LIPOCYTES.

A

Beta-3

*Para ma-remember, murag bilbilon ang 3, so Beta-3 = LIPOCYTES

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21
Q

Location of this adrenergic recepter is in Postsynaptic effector cells, especially SMOOTH MUSCLE (e.g. GI, blood vessels, lungs) and CARDIAC MUSCLE

A

Beta-2

*Para ma-remember, 2= 2 LUNGS. Beta-receptor na pinakarelated sa smooth muscle.

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22
Q

This adrenergic receptor has an opposing effect to the Alpha-1 Adrenergic Receptor

A

Beta-2

Alpha-1 = More VASOCONSTRICTION
Beta-2 = More VASODILATION (also related to Bronchodilation)
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23
Q

Most important Dopamine Receptors

A

D1 and D2

Found in: CNS, Brain, splanchnic and renal vasculature

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24
Q

Dopamine Receptors that increase cAMP (Gs)

A

D1 & D5 (D1-like)

“1 is like an i, I for increase!”

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25
Q

Most important adrenergic receptor found in SMOOTH MUSCLES (stimulation will increase cAMP)

A

D1

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26
Q

Dopamine Receptor found in nerve endings

A

D2

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27
Q

Subtypes of these adrenergic receptors have the most importance for understanding efficacy and safety of novel antipsychotic drugs

A

Dopamine Receptors.

Dopamine Receptors are also most prominent in vertebrate CNS! Kaya siya ang pinaka-makacontribute sa brain-related drugs

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28
Q

Adrenoreceptor classification is based on

A

structure-activity relationships

Altering ligand -> change in activity

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29
Q

This constant serves as the “fingerprint” to identify receptors.

A

Kd.

  • equilibrium dissociation constant
  • the ratio of concentrations when equilibrium is reached in a reversible reaction (when the rate of the forward reaction equals the rate of the reverse reaction)
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30
Q

Decrease in Kd (equilibrium dissociation constant) would lead to Increase or Decrease in affinity of the ligand?

A

Increase.

Lesser dissociation, more binding.
↓Kd = ↑ affinity

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31
Q

TRUE or FALSE. Drugs with different affinities can

have the same potencies in eliciting a clinical effect.

A

FALSE. Drugs have different affinities because they have different potencies in eliciting a clinical effect

Notes on affinity regarding structure of catecholamines

32
Q

Structure-activity relationships are the basis for adrenoreceptor classification. What are the important structural characteristics of the following catecholamines?

Epinephrine
Norepinephrine
Isoproterenol

A

Epinephrine – with methyl group

Norepinephrine - NO methyl group - “No”epinephrine

Isoproterenol – isopropyl group

33
Q

TRUE or FALSE. Only little amounts is needed for ISOPROTERENOL to achieve maximal effect as compared to NOREPINEPHRINE and EPINEPHRINE

[EFFECTS OF ADRENERGIC RECEPTOR ACTIVATION > EFFECT ON FORCE OF CONTRACTION]

A

TRUE. ISO – more potent, same efficacy, much lower Kd
than E

ISO also has greatest affinity; E & NE – almost the same affinity

Remember: The lower the Kd, the higher the affinity, the more potent it is.

34
Q

Adrenergic agonists inhibit the degradation of:

A

cAMP.

β and α are metabotropic receptors, meaning they increase cAMP

35
Q

The most potent CATECHOLAMINE in BRONCHODILATION

[EFFECTS OF ADRENERGIC RECEPTOR ACTIVATION > EFFECT ON BRONCHODILATION]

A

ISOPROTERENOL

*Ang adrenergic receptor naman na nagccause ng bronchodilation ay Beta-2

ISO>E>=NE ang trend sa Effects on Contraction Adrenergic Receptor Activation.

ISO>E»NE naman sa Effects on Bronchodilation

E >= NE&raquo_space; ISO naman sa Effect on Vasoconstriction

36
Q

The response of any cell or organ to a sympathomimetic depends on the ______ and ______ of adrenergic receptors.

[CLASSIFICATION OF ACTIONS OF ADRENERGIC RECEPTORS]

A

DENSITY & PROPORTION

37
Q

CLASSIFICATION OF ACTIONS OF ADRENERGIC RECEPTORS:

A
  1. Peripheral excitatory action
  2. Peripheral inhibitory action
  3. Cardiac excitatory action
  4. Metabolic action
  5. Endocrine actions
  6. Actions in the CNS
  7. Prejunctional actions
38
Q

Identify the Adrenergic Receptor!

Dilates renal blood vessels (the receptor with most bearing)

A

D1

39
Q

Identify the Adrenergic Receptor!

Modulates transmitter release

A

D2. It is found on nerve endings

40
Q

Identify the Adrenergic Receptor!

Inhibition of transmitter release

A

Alpha-2. Remember na presynaptic siya.

41
Q

Identify the Adrenergic Receptor!

Erects hair

A

Alpha-1. Pag smooth muscle contraction. Hair erection is due to contraction of Pilomotor smooth muscle.

42
Q

Identify the Adrenergic Receptor!

Increase Renin release

A

Beta-1.

  • Basta pag Beta-1, associated agad sa HEART CONTRACTION at JUXTAGLOMERULAR CELLS ng KIDNEYS (Hence, association with renin release.)
43
Q

Identify the Adrenergic Receptor!

Activates lipolysis

A

Beta-3

  • Remember mo lang yung bilbil ng 3
44
Q

Identify the Adrenergic Receptor!

helps prevent premature labor

A

Beta-2

  • pnemonic: It takes -2- to make B-aby.
45
Q

Identify the Adrenergic Receptor!

Inhibition of lipolysis

A

Alpha-2

46
Q

Identify the Adrenergic Receptor!

can improve urine output

A

D1. Remember yung effect niya na mag dilate ng renal blood vessels.

47
Q

Identify the Adrenergic Receptor!

Promotes potassium uptake in skeletal muscles

A

Beta-2

  • Pag beta-2, mostly dilation effects, so less contraction, meaning less Na and more K
48
Q

Identify the Adrenergic Receptor!

stimulate phospholipase C

A

Alpha-1

The mechanism of action of this adrenergic receptor involves G-protein type Gq -> phospholipase C

49
Q

What are the selective, direct-acting, adrenergic agonists?

A

α1 - Phenylephrine

α2 - Clonidine

β1 - Dobutamine

β2 - Terbutaline

50
Q

What are the non-selective, direct-acting, adrenergic agonists?

A

α1 α2 Oxymetazoline

β1 β2 Isoproterenol

α1 α2 β1 β2 Epinephrine

α1 α2 β1 Norepinephrine

51
Q

Adrenergic agonists which are Indirect-acting RELEASING AGENTS -

A

Amphetamine
Tyramine

  • actions are dependent on the release of endogenous catecholamines; increases the release of NE from the vesicles (indirect)
52
Q

Adrenergic agonists which are Indirect-acting UPTAKE INHIBITORS

A

Cocaine
Tricyclic Antidepressants

-> decreases re-uptake of NE (remains in the synapse, prolonging the action)

53
Q

Indirect-acting Adrenergic Agonists that block the degradation of NE

A

MAO/COMT Inhibitors

54
Q

What are the mixed-acting adrenergic agonists?

A

Ephedrine α1 α2 β1 β2 and releasing agent
Dopamine D1 D2 α β and releasing agent

can bind to all different kinds of receptors; both bind to the receptor and prevent reuptake of catecholamines

55
Q

increased production of NE (but cannot be measured so request for urine vanilodilic acid)

A

PHEOCHROMOCYTOMA

56
Q

TRUE or FALSE. Receptor Specificity/ Selectivity is absolute.

A

FALSE. Receptor Specificity/ Selectivity is RELATIVE, NOT ABSOLUTE!

  • It is dependent on the amount of drug available! For example, beta-1 agonist can bind with beta-2 receptor if it is given at a higher concentration than the beta-2 agonists. Beta-2 is simply more favored.
57
Q

Dopamine Effects at different blood concentrations

A

0.3ug/mL -> D1 -> Diuresis
0.7ug/ml -> Beta-1 -> increased heart contractility
1 ug/ml -> Alpha receptors -> increased heart rate, arrythmia

58
Q

Beta-1 receptor agonist effect on cardiovascular system

A

Positive chronotropic effect (increased pacemaker activity, increased heart rate)

Positive inotropic effect (intrinsic contractility is increased)

59
Q

Adrenergic blocker that inhibits VMAT (Vesicular Monoamine Transporter)

A

RESERPINE

60
Q

Adrenergic blocker that Can inhibit the Ca2+-dependent release of norepinephrine

A

GUANITHIDINE

61
Q

Symphatomimetic drug that causes myrdriasis but treats glaucoma

A

PHENYLEPHRINE

62
Q

Drug used in the treatment of diarrhea in diabetics with autonomic neuropathy

A

CLONIDINE (Alpha-2 agonist)

63
Q

an adrenergic agonist that is also a nasal decongestant

A

PHENYLEPHRINE

64
Q

Beta-receptor agonist that helps relax uterine smooth muscle, used during preterm labor -

A

Ritodrine, Terbutaline

65
Q

A mixed-acting drug that could cross BBB, has prolonged action like amphetamine, could be given orally

A

EPHEDRINE

Basta Blood-brain barrier -> EPHEDRINE

66
Q

Agonist that could cause congestive heart failure

A

DOBUTAMINE

67
Q

Toxicity related to this drug could lead to restlessness, tremor, anxiety, paranoid state.

A

AMPHETAMINE

68
Q

Toxicity related to this drug could lead to convulsions, hemorrhage, arrhythmias, MI

A

COCAINE

69
Q

prodrug converted to alpha-methylnorepinephrine. Also an alpha-2 agonist

A

METHYLDOPA

70
Q

Selective Alpha 1 Adrenergic Antagonists

A

PTD
Prazosin, Terazosin, Doxazosin

SIN is antagonistic to the alpha.

71
Q

Use of this alpha antagonist leads to relaxation of both arterial and venous vascular smooth muscle as well as smooth muscle in prostate

A

PRAZOSIN

PR-prostate - relaxation

72
Q

Nonselective α1 antagonists

A

PHENTOLAMINE & PHENOXYBENZAMINE - PP

73
Q

Beta-Blocker used for migraine

A

PROPRANOLOL

74
Q

Beta-1 selective Adrenergic Antagonists used in patients with asthma/COPD, diabetes, peripheral vascular disease

A

METOPROLOL, ATENOLOL

75
Q

Contraindications to Beta-Blockers

A

Remember na beta- receptor function ay mainly for vasodilation

  • Asthma, other bronchospastic condition
  • Severe bradycardia
  • AV block, bradycardia-tachycardia syndrome
  • Adverse Effects:

o Related to consequences of β blockade;

o Sedation, fatigue, depression (highly lipophilic

drugs), impaired exercise tolerance, insomnia,

exacerbation of peripheral vascular disease,

erectile dysfunction

76
Q

Beta-blocker with longest half-life: up to 24 hours, excreted unchanged

A

NADOLOL

77
Q

Differences in metoprolol plasma clearance is dependent on the genotype of which CYP

A

CYP2D6

Ther 201 Exam 2 (3 decks)

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