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Therapeutics > Lecture 5 > Flashcards

Lecture 5 Flashcards

1
Q

WHat effect will an antagonist have on a receptor activation

A

No effect

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2
Q

a-adrenergic receptor antagonists (non-selective) drug names

A

Phenoxybenzamine and phentolamine

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3
Q

A1 selective drugs

A

prazosin, terazosin, doxazosin (ENDS WITH SIN)

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4
Q

A1 selective drugs ROA

A

Oral

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5
Q

A1 selective clinical use

A

HTN, BPH,

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6
Q

A non-selective clinical uses

A

Pheocromocytoma, hypertensive crisis

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7
Q

Side effects of A1 antagonists

A

Hypotension, inhibition of ejaculation, tachycardia

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8
Q

how does phenoxybenzamine form a covalent bond

A

Covalent bond forms at CL. It becomes irreversible

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9
Q

Why is phenoxybenzamine irreversible?

A

Haloalkene forms covalent bond

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10
Q

reversible non-selective a-adrenergic receptors antagonist name

A

phentolamine

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11
Q

Why are non-selective a-adrenergic blockers not used

A

A-2 blocking promotes release of NE

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12
Q

Why does phenoxybenzamine lead to long drug effects

A

It is a non-competitive irreversible drug. New receptors must be synthesized to restore receptor function.

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13
Q

Why non-selective a- adrenergic receptors not used for HTN?

A

A2 blockage will lead to increase of NE at heart and increased heart rate

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14
Q

a1 selective general structural feature.

A

Quinazoline ring

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15
Q

selective a1 antagonist clinical use

A

Hypertension, Reynauds disease, BPH

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16
Q

A1a antagonist name and use

A

Tamsulosin. Used for BPH. (A1a found in prostate urethra)

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17
Q

Why is tamsulosin less likely to lead to fall in BP?

A

Tamsulosin is very selective to A1a

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18
Q

B adrenergic antagonist structural feature

A

O/\OH/\NHR(3 carbons between NHR and O, with an aromatic on O)

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19
Q

All B blockers end with

A

Olol

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20
Q

Which side of the B blocker determines lipophilicity

A

Aromatic ring

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21
Q

Lipophilic B blockers tend to be on which organs

A

Liver

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22
Q

Lipophilic drugs tend to have
A. Strong 1st pass metabolism
B. weak 1st pass metabolism

A

A

23
Q

Non-selective B blocker name

A

Propanolol

24
Q

B antagonist pharmacologic effect

A

Decreased cardiac output
Decreased renin release
Increased bronchial airway resistance
Increased VLDL and decreased HDL

25
Q

How does timolol treat glaucoma

A

Decreased intra occular pressure by reducing secretion of aqueous humor

26
Q

B blocker effect on pupil size

A

No effect

27
Q

Why are partial agonists preferred over agonists for HTN treatment

A

Less likely to cause bradycardia and lipid abnormalities

28
Q

Name of 2 partial agonist drugs

A

pindolol
carteolol

29
Q

How many rings do B1 selective drugs have? Does it have Meta or Para?

A

1 ring attached to O, it has para.

30
Q

B1 selective blockers traits

A

Less bronchoconstriction and more bronchoconstriction

31
Q

Why does atenolol have a longer half life than metoprolol

A

Nitrogen at the end makes it lipophobic, liver metabolism reduced

32
Q

Does the liver metabolize more lipophilic or lipophobic drugs?

A

Lipophilic.

33
Q

Lipophilic B1 drugs are ______lasting than lipophobic drugs

A

Longer

34
Q

B1 blocker structure

A

Single ring, Para R group

35
Q

Know B agonist structure

A
36
Q

Know B blocker structure

A
37
Q

Known A blocker structure

A
38
Q

Effect of chronic B-receptor blockade

A

Upregulation (overexpression) of B blockers, leading to high sensitivity

39
Q

Two mixed adrenergic enantiomer receptor antagonist names

A

Labetolol and carvedilol

40
Q

Which receptor does labetalol block

A

A1, B1, B2

41
Q

Which enantiomer of labetolol has B blocking activity

A

1R, 1R

42
Q

Which enantiomer of labetolol has A blocking activity

A

1S, 1R

43
Q

Physiological advantage of mixed adrenergic antagonist enantiomer

A

B blocking activity prevents tachycardia associated with A1 antagonist

44
Q

Carvedilol acts on which receptors

A

A1, B1 and B2

45
Q

Which enantiomers antagonize alpha receptors in carvedilol

A

Both enantiomers antagonize alpha receptors

46
Q

Which enantiomer possesses b blocking activity

A

S enantiomer

47
Q

How does metyrosine indirectly inhibit sympatholytic drugs

A

Inhibits tyrosine hydroxylase (RLS)

48
Q

How does resperine indirectly inhibit sympatholytic drugs

A

Inhibits VMAT

49
Q

How does bretylium indirectly inhibit sympatholytic drugs

A

Inhibits release of Norepinephrine

50
Q

how does metyrosine inhibiting tyrosine hydroxylase affect the body

A

Depletes catecholamines everywhere

51
Q

Clinical use of metyrosine

A

Management of pheochromocytoma

52
Q

Bretylium tosylate inhibition mechanism

A

Inhibits release of NE and stops long term NE release

53
Q

resperine inhibition mechanism

A

Inhibition of VMAT

Therapeutics (46 decks)

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