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PHARMACOLOGY (2nd year) > DR.LEAL- DRUGS WITH IMPORTANT ACTIONS ON SMOOTH MUSCLES PART 2 > Flashcards

DR.LEAL- DRUGS WITH IMPORTANT ACTIONS ON SMOOTH MUSCLES PART 2 Flashcards

1
Q

also known as autacoids.

A

VASOACTIVE PEPTIDES

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2
Q

Angiotensin II, endothelins, and neuropeptide Y
ARE VASOCONSCTRICTOR OR DILATOR?

A

VASOCONSTRICTORS

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3
Q

Bradykinin, BNP (Brain Natriuretic Peptide), ANP
(Atrial Natriuretic Peptide), CGRP (Calcitonin Gene-Related Peptide that causes migraine, and the VIP VIP (vasoactive Intestinal Peptide)
VASOCONSTRICTORS OR VASODILATORS?

A

VASODILATORS

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4
Q

The end point of RAAS is to __________________ to maintain homeostasis.

A

increase blood pressure

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5
Q

potent vasoconstrictor via an enzyme called angiotensin-converting enzyme.

A

angiotensin II

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6
Q

produced in the lungs, but a little amount of it can also be produced by the kidneys.

A

Angiotensin-converting enzyme

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7
Q

conversion takes place in the lungs because angiotensin-converting enzyme is predominantly produced in the lungs.

A

Angiotensin I

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8
Q

antihypertensive drug especially used for pregnant patients that are eclamptic,

A

hydralazine
VD

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9
Q

hair grower with antihypertensive effect, nitroprusside

A

MINOXIDIL

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10
Q

Production of angiotensinogen is increased by:

A

○ Corticosteroids, estrogens, thyroid
hormones, and angiotensin II
○ Elevated during pregnancy
- That’s why pregnant patients can develop gestational hypertension.
○ Oral contraceptives (Pills) can increase blood pressure.

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11
Q

● Potent pressor agent (increase in blood pressure)
● Direct contraction of vascular especially arteriolar
smooth muscle

A

AngiotensinII

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12
Q

● Increases the release of epinephrine and
norepinephrine
● Direct positive inotropic (increases heart rate) action
on the heart

A

ANGIOTENSIN 2

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13
Q

Common side effect of this drug classification is cough.

A

ACE INHIBITORS

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14
Q

● Block angiotensin receptors
● Slow the progression of diabetic nephropathy

A

Angiotensin Receptor Blockers (ARBs)
LOSARTAN OR VALSARTAN

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15
Q

● Blocks the renal beta receptors involved in the sympathetic control of renin release
● E.g. Propranolol

A

Beta-adrenoceptor Blocking Drugs

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16
Q

● Dose-dependent reductions in plasma renin activity and plasma angiotensin I, angiotensin II, and aldosterone concentrations
● Contraindicated in pregnancy

A

ALISKIREN

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17
Q

which is a vasodilator: produce the four
classic symptoms of inflammation:
○ Redness
○ Local heat
○ Swelling

A

BRADYKININ

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18
Q

● Control of blood pressure through its action on the kidney: increase water reabsorption
● Regulation of arterial pressure by its vasoconstrictor action

A

Arginine Vasopressin (AVP)
Antidiuretic Hormone (ADH)

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19
Q

Beneficial in the treatment of septic and other vasodilatory shock states (V1a agonist activity)

A

AVP + Norepinephrine

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20
Q

● Release ANP from cardiac cells for homeostasis
● Synthesized primarily in cardiac atrial cells, but it is also synthesized in the ventricular myocardium, neurons in the CNS, PNS and in the lungs.

A

Atrial Natriuretic Peptide (ANP)

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21
Q

● Synthesized primarily in the heart
● Volume related
○ If there is an increase in volume, ____ is released to increase the pressure.

A

Brain Natriuretic Peptide (BNP)

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22
Q

Treatment of Congestive Heart Failure

A

Vasodilation and natriuresis

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23
Q

● Widely distributed in the CNS and PNS
● Major peptide neurotransmitters
● Marked vasodilation in most vascular beds

A

Vasoactive Intestinal Peptide

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24
Q

Most potent vasodilator

A

Calcitonin Gene-Related Peptide

——-Calcitonin, Adrenomedullin, Amylin

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25
Q

● Readily available
● Expressed constitutively in most cells
● Generates prostanoids for “housekeeping” functions,
such as gastric epithelial cytoprotection

A

PGH synthase-1 (COX-1)

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26
Q

● Readily inducible, its expression levels being dependent on the stimulus
● Major source of prostanoids
● Present when there is inflammation

A

PGH synthase-2 (COX-2)

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27
Q

Exert their therapeutic effects through inhibition of the COXs

A

NSAIDS

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28
Q

Indomethacin, Sulindac, Meclofenamate,
and Ibuprofen

A

Non-selective COX inhibitors:

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29
Q

Celecoxib = Diclofenac = Meloxicam = Etodolac < Valdecoxib &laquo_space;Rofecoxib < Lumiracoxib = Etoricoxib
(increasing COX-2 selectivity)

A

Selective COX-2 inhibitors:

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30
Q

cyclooxygenase pathway inhibitor but irreversible
acetylates and inhibits both enzymes covalently and hence irreversibly

A

ASPIRIN

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31
Q

○ Abortifacient drug
○ A PGE1 derivative cytoprotective
prostaglandin used in preventing peptic ulcer (main use) and in combination with Mifepristone (RU-486) for terminating early pregnancies

A

MISOPROSTOL (CYTOTEC)

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32
Q

○ Inserted intravaginally to open the cervix and deliver the baby
○ Used in obstetrics to induce labor

A

Dinoprostone (PGE2) and PGF2α

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33
Q

○ Topically active PGF2α derivatives used in
ophthalmology to reduce intraocular pressure in open-angle glaucoma or ocular hypertension

A

LATANOPROST

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34
Q

Synthesized mainly by the vascular endothelium and is a powerful vasodilator and inhibitor of platelet aggregation

A

PROSTACYCLIN

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35
Q

pulmonary hypertension

A

Epoprostenol, Iloprost, Treprostinil

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36
Q

Block all the known pathways of eicosanoid synthesis

A

Corticosteroids

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37
Q

○ Block both prostaglandin and thromboxane formation by reversibly inhibiting COX activity

A

NSAIDs

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38
Q

an irreversible COX inhibitor

39
Q

Mild to moderate asthma

A

LOX (Lipoxygenase) inhibitors (Zileuton, Zafirlukast, Montelukast, and Pranlukast)

40
Q

○ Synthetic preparation of PGE2
○ Administered vaginally for oxytocic use
○ Induction of labor or softening of the cervix

A

DINOPROSTONE

41
Q

○ Induce second trimester abortions and to
control postpartum hemorrhage

A

CARBOPROST TROMETHAMINE

42
Q

postpartum hemorrhage

A

1ST CHOICE - OXYTOCIN
2ND CHOICE- ERGONOVINE
3RD CHOICE - CARBOPROST

43
Q

○ A form of inflammation that happens during the menstrual period.
○ Increase PGE2 and PGF2α during menstruation
○ NSAIDs inhibit formation of PG

A

DYSMENORRHEA

44
Q

○ Erectile dysfunction

○ Prolonged erection and priapism

A

ALPROSTADIL (PGEI)

45
Q

○ Pulmonary Hypertension
○ Lowers peripheral, pulmonary, and coronary
resistance

A

EPOPROSTENOL (PGI2)

46
Q

vasodilator and an inhibitor of platelet aggregation

A

ALPROSTADIL

PATENT DUCTUS ARTERIOSUS

47
Q

inhibit synthesis of PGE2 and so close the ductus

A

Indomethacin

48
Q

Inhibit platelet aggregation

A

PGI2, PGE2 AND PGD2

49
Q

○ Promotes platelet aggregation

50
Q

○ Remarkable protective effect of the E prostaglandins against peptic ulcers
○ Enprostil, Misoprostol

A

CYTOPROTECTION

51
Q

PGF 2α derivative used for glaucoma

A

LATANOPROST
BIMATOPROST
TRAVOPROST

52
Q

Treatment of eyelash hypertrichosis

A

BIMATOPROST

53
Q

Activates soluble guanylyl cyclase to
elevate cGMP levels in vascular smooth
muscle

A

NITRIC OXIDE (NO)

54
Q

○ Vasodilation
○ Relaxes other smooth muscle
○ Inhalation of NO leads to dilation of
coronary blood vessels and increased blood flow to parts of the lung exposed to NO and decreased pulmonary vascular resistance

A

NITRIC OXIDE (NO)

55
Q

○ Most common Nitric Oxide
○ Dilates veins and coronary
arteries

A

Nitroglycerin

56
Q

A Nitric Oxide donor for vasodilation

A

Isosorbide Dinitrate

57
Q

Antianginal inhalant
- Do not give excessive amounts to sexually active men, especially older men.

Arterial vasodilators

Euphoric effects

A

Amyl Nitrite

58
Q

AMYL NITRATE + _____
can cause lethal hypotension
- Check if the patient is taking viagra because it can cause lethal hypotension.

A

SILDENAFIL

59
Q

● Dilates arterioles and venules
● For rapid pressure reduction in arterial hypertension

A

SODIUM NITROPRUSSIDE

60
Q

● Mediated by immune globulin (IgE)
● Produced in response to exposure to foreign proteins (house dust mite, cockroach, animal
danders, molds and pollens)

61
Q

○ attract and activate eosinophils
○ stimulate IgE production by B lymphocytes
○ stimulate mucus production by bronchial
epithelial cells

A

LATE ASTHMATIC RESPONSE
CYTOKINES

62
Q

inhibition of the production
of proinflammatory cytokines in the airways
○ Blocks all the four pathways of arachidonic acid
○ Blocks the different prostaglandins, thromboxanes, cyclooxygenase pathways, formation of leukotrienes

A

Corticosteroid Therapy

63
Q

mimics the sympathetic nervous system

A

SYMPATHOMIMETIC AGENTS:

64
Q

○ Mainstays in the treatment of asthma

○ Inhibit microvascular leakage and increase
mucociliary transport

A

Adrenoceptor Agonists

65
Q

○ For severe asthma, anaphylactic shock

○ Maximal bronchodilation is achieved within 15 minutes after inhalation and lasts 60-90 minutes.
○ Stimulates α, β1, β2 receptors: tachycardia, arrhythmias, and worsening of angina pectoris

A

Epinephrine

66
Q

○ Nonselective β1 and β2 bronchodilator
- β1: heart
- β2: lungs
○ Also a sympathomimetic agent and a
drug used in asthma

○ Cardiac Arrhythmias caused by tachycardia

A

Isoproterenol

67
Q

● β2 involves the lungs
● Albuterol, Terbutaline, Metaproterenol and
Pirbuterol

A

BETA 2-SELECTIVE DRUGS:

68
Q

○ Metered-dose inhalers
○ “Puffs/puffers” used by COPD and
asthmatic patients.
○ Its effect is on the lungs which opens the
bronchial airway.

A

Albuterol,
Terbutaline,
Metaproterenol
Pirbuterol

69
Q

○ Available in oral form
○ Skeletal muscle tremor, nervousness, and
occasional weakness.
○ More pronounced adverse effects and is
thus rarely prescribed.

A

Albuterol and Terbutaline

70
Q

○ Sometimes used to inhibit the uterine contractions associated with premature
labor.

A

Terbutaline

71
Q

○ 12-hour durations of action (high lipid solubility)
○ Salmeterol and Formoterol
○ No anti-inflammatory action
○ Not used as monotherapy for asthma

A

Long-acting β2-Selective Agonists (LABA)

72
Q

● Decreased arterial oxygen tension (PaO2): ○ Treatment: Supplemental oxygen
● Cardiac arrhythmias
● Tachyphylaxis

A

Toxicities of Beta 2-Selective Drugs:

73
Q

Frequent repetitive administration will cause tolerance in which there will be a need to adjust to a higher dose since there will be no effect if given in the usual dose.

A

Tachyphylaxis

74
Q

Theophylline (tea),
Theobromine (cocoa) and
Caffeine (coffee)

A

METHYLXANTHINE DRUGS:

75
Q
  1. High concentration: Inhibit phosphodiesterase enzyme, thereby increasing concentrations of intracellular cAMP.
    ● Cyclic AMP: stimulation of cardiac function, relaxation of smooth muscle, and reduction in the immune and inflammatory activity of specific cells.
  2. Inhibition of cell surface receptors for adenosine.
  3. Enhancement of histone deacetylation.
A

METHYLXANTHINE DRUGS:

76
Q

Competitively inhibit the action of acetylcholine at muscarinic receptors.

A

ANTIMUSCARINIC AGENTS:

77
Q

○ Bronchodilator
○ Potent competitive inhibitor of acetylcholine
at postganglionic muscarinic receptors.
○ Can cross the blood-brain barrier.

78
Q

Potent atropine analog.
- Atropine are anesthetic agents which cause an increase in heart rate and are also bronchodilators.

A

Ipratropium

79
Q

The bronchodilation effect of Ipratropium causes dry mouth and increased heart rate.

A

Salbutamol + Ipratropium

seen in formulations for nebules such as the Salbutamol + Ipratropium used in nebulizers for asthmatic patients.

80
Q

● Inhibition of production of inflammatory cytokines.
● Do not relax airway smooth muscle directly but reduce bronchial hyperreactivity and reduce the
frequency of asthma exacerbations.

A

CORTICOSTEROIDS

81
Q

● Inhibition of the infiltration of asthmatic airways by
lymphocytes, eosinophils, and mast cells.

A

CORTICOSTEROIDS

82
Q

Inhibition of 5-lipoxygenase, thereby preventing leukotriene synthesis.

83
Q

Inhibition of the binding of LTD4 to its receptor on target tissues thereby preventing its action.

A

Zafirlukast and Montelukast

84
Q

The following are corticosteroid inhalation treatment, EXCEPT
A. Beclomethasone
B. Budesonide
C. Montelukast
D. Ciclesonide

85
Q

TRUE OR FALSE. Albuterol is a selective β2 agonist.

86
Q

The following describes Atropine, EXCEPT
A. Bronchoconstrictor
B. Potent competitive inhibitor of acetylcholine at postganglionic muscarinic receptors.
C. Bronchodilator
D. Can cross the blood-brain barrier

87
Q

Which is an irreversible cyclooxygenase pathway
inhibitor.
A. Latanoprost
B. Dinoprostone
C. Aspirin
D. Prostacyclin

A

C. ASPIRIN

88
Q

The main use is to prevent peptic ulcer and in combination with Mifepristone (RU-486) for terminating early pregnancies
A. Epoprostenol (PGI2)
B. Alprostadil (PGE1)
C. Misoprostol (Cytotec)
D. Prostacyclin (PGI2)

A

C. Misoprostol (Cytotec)

89
Q

Came from a 20-carbon fatty acid known as the arachidonic acid in the membrane phospholipid.
A. Prostaglandin
B. Eicosanoids
C. Prostanoids
D. BothB&C

A

D. EICOSANOIDS OR PROSTANOIDS

90
Q

Nonselective β1 and β2 bronchodilator and also a sympathomimetic agent and a drug used in asthma
A. Isoproterenol
B. Epinephrine
C. Albuterol
D. Terbutaline

A

A. Isoproterenol

91
Q

Potent competitive inhibitor of acetylcholine at postganglionic muscarinic receptors.
A. Albuterol
B. Atropine
C. Epinephrine
D. Isoproterenol

A

B. Atropine

92
Q

T/F. Tachyphylaxis is the frequent repetitive administration that will cause tolerance in which there will be a need to adjust to a higher dose since there will be no effect if given in the usual dose.

93
Q

Metered-dose inhalers or puffs used by COPD and asthmatic patients, EXCEPT
A. Albuterol
B. Terbutaline
C. Metaproterenol
D. NOTA

A

D. NOTA
ALL ARE METERED PUFFS

PHARMACOLOGY (2nd year) (16 decks)

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