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PHARMACOLOGY (2nd year) > DR.LEAL - DRUGS WITH IMPORTANT ACTIONS ON SMOOTH MUCLES PART1 > Flashcards

DR.LEAL - DRUGS WITH IMPORTANT ACTIONS ON SMOOTH MUCLES PART1 Flashcards

1
Q

released when there are allergies, asthma, and rhinitis, thereby antihistamines are
taken.

A

HISTAMINE

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2
Q

Examples of antihistamines:

A

Cetirizine,
Loratadine
Hydroxyzine

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3
Q

happy neurotransmitter that affects mood
and sleep

A

SEROTONIN

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4
Q

Important mediator of immediate allergic (such as urticaria) and inflammatory reactions (Type I hypersensitivity reactions)

A

HISTAMINE

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5
Q

Role in gastric acid secretion
○ Attachment of histamine to H2 receptors
will promote gastric acid secretion; hence,
H2 blockers are given
○ Example of H2 blockers (antacids):
Famotidine, Cimetidine, Ranitidine

A

HISTAMINE

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6
Q

anesthetic drug classified under opioids; pain reliever

A

MORPHINE

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7
Q

neuromuscular blocking agent

A

TUBOCURARINE (CURARE)

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8
Q

requiring energy and calcium
○ A drug that can release histamine in its bulk form

A

Compound 48/80

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9
Q

Four Histamine receptors:

A

○ H1: Smooth muscle, endothelium, brain
○ H2: Gastric mucosa, cardiac muscle, mast
cells, brain
○ H3: Presynaptic autoreceptors and
heteroreceptors: brain, myenteric plexus,
other neurons
○ H4: Eosinophils, neutrophils, CD4 T cells

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10
Q

Smooth muscle, endothelium, brain

A

H1

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11
Q

Gastric mucosa, cardiac muscle, mast
cells, brain

A

H2

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12
Q

Presynaptic autoreceptors and
heteroreceptors: brain, myenteric plexus,
other neurons

A

H3

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13
Q

Eosinophils, neutrophils, CD4 T cells

A

H4

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14
Q

action of histamine on arterioles and
precapillary sphincters
○ Result: ↓ Blood pressure (Anaphylactic shock)
○ Anaphylactic shock: Allergy + Hypotension

A

VASODILATION

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15
Q

Intradermal injection of histamine:
characteristic

A

RED SPOT
EDEMA
FLARE

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16
Q

vasoconstrictor; have smooth
muscle actions opposite to those of histamine (act on different receptors)

A

EPINEPHRINE

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17
Q

causes vasodilation, consequently lowering blood pressure.

A

HISTAMINE

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18
Q

a vasoconstrictor, is given to counteract the effects of histamine.

A

EPINEPHRINE

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19
Q

○ Drugs that inhibit the release of histamine
○ Reduce the degranulation of mast cells that results from immunologic triggering by antigen-IgE interaction

A

RELEASE INHIBITORS

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20
Q

treatment of asthma

A

CROMOLYN
NEDOCROMIL

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21
Q

Selective H2-receptor antagonists:
therapy for peptic disease (Ex. antacids -
drugs used for hyperacidity)

A

Histamine Receptor Antagonists

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22
Q

Thioperamide and Clobenpropit

A

H3 RECEPTOR ANTAGONIST

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23
Q

ANTIHISTAMINE THAT Can cross the blood-brain barrier → effect
in the central nervous system → Strong
sedative effects

A

1ST GEN

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24
Q

antihistamine that is Less sedating (reduced distribution into the CNS) treatment of allergic rhinitis and chronic urticaria.
○ Example: Cetirizine

A

2ndGEN

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25
Q

H1 antagonists
○ First generation antihistamine

A

SEDATION

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26
Q

Scopolamine, Dimenhydrinate
○ Prevents motion sickness
○ Example: Bonamine® generic name:
meclizine hydrochloride

A

Antinausea and antiemetic actions

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27
Q
  • Significant acute suppressant effects on the extrapyramidal symptoms associated with certain antipsychotic drugs
  • Can also be used to sedate the patient
A

Diphenhydramine

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28
Q

Significant atropine-like effects on peripheral muscarinic
receptors
- During an allergic reaction, the patient can experience drooling. Atropine-like action of antihistamine can cause dry mouth, increased heart rate, etc.

A

Antimuscarinic actions

○Ethanolamine and Ethylenediamine

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29
Q
  • Alpha-receptor-blocking (orthostatic hypotension)
  • Used during painful labor of pregnant women. It has localized anesthetic activity and sedative. This can be used to lessen the pain of labor.
A

Promethazine

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30
Q

Inhibit mast cell release of histamine and some other mediators of inflammation

A

CETIRIZINE

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31
Q

found in the gastric mucosa. Once histamine is released and attached to the H2 receptors, they promote gastric acid secretion.

A

H2 RECEPTORS

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32
Q

Medicine used to counteract histamine-2 receptors are:

A

○ Cimetidine (Prototype)
○ Ranitidine
○ Famotidine
○ Nizatidine

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33
Q

● Blocks H2 receptors
● Relatively selective or specific to H2 receptor only,
have no significant blocking actions at H1 or autonomic receptors

A

Histamine H2 Antagonist

34
Q

is the drug usually given to treat hyperacidity. H2 blockers can be an alternative drug for hyperacidity

A

OMEPRAZOLE

35
Q

Has significant antiandrogen effects in patients receiving high doses.
- Can cause gynecomastia on male patients.

A

CIMETIDINE

36
Q

○ Has a weaker inhibitory effect on hepatic drug metabolism
○ No androgenic effects
○ Safer

A

RANITIDINE

37
Q

● Important neurotransmitter in the CNS and and Enteric NS (GI Tract nervous system)
● A local hormone in the gut
● A component of the platelet clotting process
● Play a role in migraine headache

A

SEROTONIN (5-HYDROXYTRYPTAMINE; 5-HT) & RELATED AGONISTS

38
Q

neoplasm (cancer) of
enterochromaffin cells in the gastrointestinal tract that produce large amounts of serotonin.
○ High levels of serotonin play a role in migraine headache.

A

CARCINOID SYNDROME

39
Q

rate-limiting step ON SYNTHESIS OF SEROTONIN

A

Hydroxylation by tryptophan hydroxylase-1:

40
Q

neoplasm in the GIT

A

CARCINOID SYNDROME

41
Q

CARCINOID SYNDROME TRIAD

A

DIARRHEA
FLUSHING
CARDIAC INVOLVEMENT

42
Q

To treat diarrhea of patients with carcinoid
syndrome would be

A

telotristat ethyl.

43
Q

○ Orally active hydroxylase inhibitor
○ Approved for the treatment of diarrhea due
to carcinoid tumor

A

Telotristat ethyl

44
Q

sleeping pill that has selectivity for Melatonin 1 receptor and Melatonin 2 receptors.

45
Q

Spinal anesthesia blocks T4 down to extremities. Upon blocking the T4 level, the cardioaccelerators are also blocked, hence lowering heart rate then blood pressure.

A

Bezold-Jarisch Reflex

46
Q

powerful vasoconstrictor except in skeletal muscle and the heart (dilates blood vessels) resulting to a decrease in blood pressure

47
Q

Powerful stimulant of gastrointestinal smooth
muscle, increasing tone and facilitating peristalsis causing diarrhea

48
Q

● Excess serotonergic activity in the central nervous
system
● Skeletal muscle contractions / muscle rigidity
caused by serotonergic activity in the CNS.

A

SEROTONIN SYNDROME

49
Q

Malignant hyperthermia DOC

A

DANTROLENE

50
Q

○ Most important in the brain and mediate
synaptic inhibition via increased potassium
conductance
○ Always remember that serotonin 1 receptors are located in the brain or the CNS

A

5HT1 receptors

51
Q

○ Important in both brain and peripheral
tissues

A

5HT2 receptors

52
Q

Found in the CNS, especially in the chemoreceptive area and vomiting center,

A

5HT3 receptors

53
Q

setron” from serotonin; an antiemetic drug used in cancer patients.
- They block serotonin in the serotonin 3 receptor

A

Ondansetron

54
Q

○ A 5 HT1A agonist
○ Drug that helps the attachment of serotonin to the 5HT1A receptor
○ Effective nonbenzodiazepine anxiolytic

55
Q

○ selective 5 HT agonist
○ appetite suppressant but was withdrawn
because of cardiac valvulopathy

A

Dexfenfluramine

56
Q

○ a 5 HT2C agonist
○ weight loss medication

A

Lorcaserin

57
Q

○ α adrenoceptors and serotonin receptor
blocking effects
○ Used in pheochromocytoma

A

Phenoxybenzamine

58
Q

treatment of the smooth muscle
manifestations of carcinoid tumor and in
cold induced urticaria

A

Cyproheptadine

59
Q

○ ○
prototypical 5 HT3 antagonist
prevention of nausea and vomiting associated with surgery and cancer chemotherapy

A

Ondansetron

60
Q

aura of variable duration, followed by severe
throbbing unilateral headache that lasts for a few hours to 1-2 days

A

MigraineHeadache

61
Q

in migraine headache
trigeminal nerve distribution to intracranial (and possibly extracranial) arteries releases

A

calcitonin gene related peptide (CGRP; powerful vasodilator)

62
Q

MIGRAINE TREATMENTS

A

○ 5 HT1D/1B agonists (sumatriptan)
○ Ergot alkaloids
○ NSAIDs (Ex. Mefenamic acid, celecoxib)
○ β adrenoceptor blockers
○ Calcium channel blockers
○ TCA
○ SSRIs
○ Antiseizure agents

63
Q

● produced by Claviceps purpurea, a fungus that infects grasses and grains especially rye under damp growing or storage conditions
● synthesizes histamine, acetylcholine, tyramine

A

ERGOT ALKALOIDS

64
Q

○ dementia with florid hallucinations;
prolonged vasospasm,
which may result in gangrene; and
stimulation of uterine smooth muscle,
which in pregnancy may result in abortion

A

Ergotism (St. Anthony’s Fire/Holy Fire)

65
Q

ORGAN SYSTEMS EFFECTS
○ Synthetic ergot compound
○ Hallucinogen

A

Lysergic Acid Diethylamide (LSD; “acid”)

66
Q

ORGAN SYSTEM EFFECTS OF ERGOTS
○ Suppress prolactin secretion from pituitary cells by activating regulatory dopamine receptors
○ Bromocriptine 2.5 mg BID or TID
○ Peripartum cardiomyopathy

A

Bromocriptine, Cabergoline, and Pergolide

67
Q

○ Constrict vessels (prolonged vasospasm)
○ Prevent vascular headache
○ blocked by α blocking agents
ERGOT EFFECTS

A

ERGOTAMINE

68
Q

ERGOT EFFECTS
○ For uterine contraction
○ Postpartum Hemorrhage (2nd choice)
○ Oxytocin (1st choice)

A

ERGONOVINE

69
Q

3RD CHOICE FOR POSTPARTUM HEMORRHAGE

A

CARBOPROST

70
Q

produce prompt vasoconstriction during coronary angiography

A

ERGOT ALKALOIDS

71
Q

ERGOT ALKALOID FOR
used in the treatment of
Alzheimer’s dementia

A

ERGONOVINE

72
Q
  1. Serotonin antagonists include the following, except
    a. Phenoxybenzamine
    b. Cyproheptadine
    c. Ergonovine
    d. Ondansetron
A

C. ERGONOVINE

73
Q

Which of the following is not a serotonin agonist
a. Buspirone
b. Dexfenfluramine
c. Ergotamine
d. Lorcaserin

A

C. ERGOTAMINE

74
Q

Which receptor is the most important in the brain and mediates synaptic inhibition via increased potassium conductance
a. 5HT2
b. 5HT4
c. 5HT1
d. 5HT11

75
Q

The following are effects of Bromocriptine, Cabergoline, and Pergolide, except:
a. Suppress prolactin secretion from pituitary cells by activating regulatory dopamine receptors
b. Bromocriptine 2.5 mg BID or TID
c. Peripartum cardiomyopathy
d. AOTA
e. NOTA

A

E. NOTA
ALLARE FOR Bromocriptine, Cabergoline, and Pergolide

76
Q

Whichcorresponding location in the body?
histamine receptor is correctly paired with its
a. H1: cardiac muscle
b. H2: smooth muscle
c. H3: brain
d. H4: gastric mucosa

A

C. H3:BRAIN

77
Q

Drug that prevents nausea and vomiting associated with surgery and cancer chemotherapy
a. Buspirone
b. Ondansetron
c. Bromocriptine
d. Ergonovine

A

B. ODANSETRON

78
Q

Used to treat diarrhea in patients with carcinoid syndrome
Loratadine
Odansetron
Dexfenfluramine
Telotristat ethyl

A

Telotristat ethyl

79
Q

A potent vasodilator released in migraine headaches
Histamine
Calcitonin gene related peptide (CGRP)
Methysergide
p-chlorophenylalanine (PCP)

A

Calcitonin gene related peptide (CGRP)

80
Q

Considered the 2nd choice for the management of postpartum hemorrhage
a. Ergonovine
b. Cabergoline
c. Pergolide
d. LSD

A

A. ERGONOVINE

81
Q

Serotonin antagonist used in pheochromocytoma
a. Cyproheptadine
b. Odansetron
c. Phenoxybenzamine
d. Dexfenfluramine

A

c. Phenoxybenzamine

PHARMACOLOGY (2nd year) (16 decks)

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