Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

PCM Exam 2 Pharm > AUTACOIDS & AUTACOID ANTAGONISTS > Flashcards

AUTACOIDS & AUTACOID ANTAGONISTS Flashcards

1
Q

What are the 3 AUTACOIDS

A
  • Histamine
  • Serotonin
  • Eicosanoids
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Where are H1 and H2 present?

A

H1 receptors are present in endothelium, smoothmuscle cells and nerve endings
H1 receptors are coupled to activation of PLC

H2 receptors are present in gastric mucosa, cardiac muscle cells and some immune cells. •H2 receptors are linked to activation of adenylyl cyclase.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are the TISSUE & ORGAN SYSTEM EFFECTS OF HISTAMINE?

CARDIOVASCULAR SYSTEM

Heart

Capillary Permeability

GI Tract Smooth Muscle

Bronchiolar Smooth Muscle

NERVOUS SYSTEM

SECRETORY TISSUE

A

CARDIOVASCULAR SYSTEM • H2 receptors are located on vascular smooth muscle and the vasodilation is mediated by cAMP.• H1 receptors are on endothelial cells and their
stimulation leads to formation of NO.

HEART : • Increased contractility and increased pacemaker rate via H2

Capillary Permeability : • Histamine-induced edema results from the action of histamine on H1 receptors in blood vessels. • The effect is due to separation of the endothelial
cells which permits the transudation of fluid and molecules into the perivascular tissue.

GI Tract Smooth Muscle • Contraction (H1 effect).

Bronchiolar Smooth Muscle: • Bronchoconstriction (H1 effect).

NERVOUS SYSTEM: • Histamine is a powerful stimulant of sensory nerve endings, especially those mediating pain and itching via H1

SECRETORY TISSUE : • Histamine is a powerful stimulant of gastric acid secretion. • Due to H2 receptors in gastric parietal cells.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

How does HISTAMINE cause ANAPHYLAXIS ?

A

Systemic mast cell degranulation can cause the life-threatening condition known as anaphylaxis.
• Anaphylactic shock can be lethal within minutes if not treated rapidly with epinephrine.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are HISTAMINE ANTAGONISTS RELEASE INHIBITORS ?

A

Cromolyn & nedocromil

  • Reduce immunologic mast cell degranulation.
  • B2-agonists also appear capable of reducing histamine release.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are the two classes of H1 RECEPTOR ANTAGONISTS and what is their common effect?

A
  • First-generation have sedative effects and are more likely to block autonomic receptors.
  • Second-generation are less sedating because they are less liposoluble.
  • Also, they are substrates of the P-glycoprotein transporter.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the 1st generation H1 RECEPTOR ANTAGONISTS?

A
  • Chlorpheniramine
  • Cyclizine
  • Diphenhydramine
  • Dimenhydrinate
  • Hydroxyzine
  • Meclizine
  • Promethazine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are the 2nd generation H1 RECEPTOR ANTAGONISTS?

A

• Fexofenadine • Loratadine • Cetirizine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is the mechanism of action of H1 RECEPTOR ANTAGONISTS?

A
  • H1-blockers were considered H1 receptor antagonists.
  • They are now known to be inverse agonists.
  • First-generation H1 antagonists have additional effects due to blocking of cholinergic, a-adrenergic, and serotonin receptors, and Na+ channels.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

How does H1 RECEPTOR ANTAGONISTS cure MOTION SICKNESS & NAUSEA?

A
  • First-generation H1 receptor blockers block central H1 and M1 receptors.
  • Effective for prevention of motion sickness.
  • Second generation H1 antagonists lack central actions and are ineffective antiemetics.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

SOMNIFACIENTS class and effect?

A

H1 RECEPTOR ANTAGONISTS

• Some first-generation H1 blockers have strong sedative properties and are used in the treatment of insomnia.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

H1 RECEPTOR ANTAGONISTS: ADVERSE EFFECTS?

A
  • Dry mouth: due to anticholinergic effects.
  • Sedation: less common with second generationagents
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are the H2 RECEPTOR ANTAGONISTS?

A

• Cimetidine • Ranitidine • Famotidine • Nizatidine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are the uses for H2 RECEPTOR ANTAGONISTS ?

A

.
• Main clinical use: inhibitors of gastric acidsecretion

  • By competitively blocking H2 receptors, these agents reduce secretion of gastric acid.
  • Peptic ulcers: promote healing of duodenal and gastric ulcers.
  • Acute stress ulcers
  • GERD: effective in prevention and treatment of heart-burn
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

H2 RECEPTOR ANTAGONISTS: ADVERSE EFFECTS

A
  • H2 antagonists are extremely safe drugs.
  • Adverse effects occur in less than 3% of patients.
  • Include: headache, dizziness, diarrhea, muscular pain, constipation.
  • Confusion, hallucinations and agitation may occur when given IV, especially in patients in the ICU who are elderly or who have renal or hepatic dysfunction.
  • These adverse effects may be more common with cimetidine.
  • Cimetidine inhibits cytochrome P450 and can slow metabolism of several drugs.
  • Cimetidine binds to androgen receptors and has antiandrogenic effects: gynecomastia and reduced sperm count in men and galactorrhea in women.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

SEROTONIN: MECHANISM OF ACTION ?

A
  • Seven families of 5-HT receptor subtypes have been characterized.
  • Six are G protein-coupled receptors.
  • One is a ligand-gated ion channel.
  • The 5-HT3 receptor is the only monoamine neurotransmitter receptor known to function as a ligand-gated ion channel.
17
Q

Sumatriptan?

A

5-HT 1D/1B RECEPTOR AGONISTS

  • Sumatriptan is the prototype.
  • Triptans are first-line therapy for acute severemigraine attacks.
  • Triptans may cause coronary vasospasm.
  • They are contraindicated in patients with coronary artery disease or angina.
  • Bind to receptor and prevent release pf CGRP and less action and no vasodilation OR binds to Recetor on blood vessel causing vasoconstriction and relieving the migraine
18
Q

METOCLOPRAMIDE

A

5-HT 4 RECEPTOR AGONISTS

  • Prokinetic agent.
  • Its administration results in coordinated contractions that enhance transit.
  • The most common adverse effects are somnolence, nervousness and dystonic reactions.
  • Extrapyramidal effects and tardive dyskinesia, although rare, may occur.
19
Q

CISAPRIDE?

A

5-HT 4 RECEPTOR AGONISTS

  • Prokinetic agent.
  • Prolongs QT interval.
  • Due to serious cardiac adverse effects it is nolonger generally available in t he US.
  • The drug is available only on a limited basis.
20
Q

CYPROHEPTADINE

A

5-HT2 RECEPTOR ANTAGONISTS

CYPROHEPTADINE

• Also has potent H1 blocking actions.

USES • Allergic rhinitis

  • Vasomotor rhinitis
  • Management of serotonin syndrome.
21
Q

ONDANSETRON

A

5-HT3 RECEPTOR ANTAGONISTS

  • Anti-emetic.
  • Particularly for the severe nausea and vomitingthat occurs with cancer chemotherapy.
22
Q

THE ERGOT ALKALOIDS

A

• Ergotamine • Dihydroergotamine • Bromocriptine • Cabergoline • Ergonovine • Methylergonovine

23
Q

THE ERGOT ALKALOIDS: USES

Migraine

Hyperprolactinemia

Postpartum Hemorrhage

Diagnosis Of Variant Angina

A

Migraine: Triptans are preferred, but therapy with ergotamine or dihydroergotamine can be effective.

Hyperprolactinemia: • Bromocriptine and cabergoline are effective in
reducing the high levels of prolactin that result from pituitary tumors.

Postpartum Hemorrhage :Postpartum Hemorrhage • Oxytocin is the preferred agent for control of postpartum hemorrhage, but if it is ineffective,
ergonovine or methylergonovine IM can be tried

Diagnosis Of Variant Angina • Ergonovine IV provokes coronary artery spasm
in patients with variant angina.

24
Q

THE ERGOT ALKALOIDS: ADVERSE EFFECTS

A
  • Vasospasm.
  • Contraindicated in pregnant women because the drugs may cause fetal distress and miscarriage.
  • Contraindicated in patients with peripheral vascular disease, CAD, hypertension, and impaired hepatic or renal function.
  • Should not be used concurrently with other drugs that can cause vasoconstriction
25
Q

EICOSANOIDS: two pathways for synthesis?

A

• Lipoxygenases: which initiate the synthesis
of leukotrienes, and other compounds.
• Cyclo-oxygenases: which initiate thebiosynthesis of prostaglandins, prostacyclins and thromboxanes

26
Q

THE CYCLO-OXYGENASE PATHWAY : what are they two enzymes and what is their function?

A
  • COX-1 is found in most cells as a constitutive enzyme and the prostaglandins it produces are involved in normal homeostasis.
  • COX-2 is found mainly in inflammatory cells and is induced by inflammatory stimuli.
27
Q

THE LIPOXYGENASE PATHWAY : what is their function?

A
  • Leukotrienes are associated with asthma, anaphylactic shock and cardiovascular disease.
  • The leukotrienes LTC4 and LTD4 are potent bronchoconstrictors and are secreted in asthma and anaphylaxis.
28
Q

EICOSANOIDS: MECHANISM OF ACTION?

A
  • The contractile effects of eicosanoids on.smooth muscle are mediated by Ca2+.
  • Their relaxing effects are mediated by cAMP.
29
Q

Misoprostol

A

EICOSANOIDS(PGE1 analog)

• Prevention of peptic ulcers in patients taking high
doses of NSAIDs.

  • To ripen the cervix at or near term.
  • Management of postpartum hemorrhage.
  • Abortifacient in combination with the antiprogestin mifepristone or methotrexate.
30
Q

Dinoprostone

A

EICOSANOIDS (PGE2)

  • To ripen cervix at or near term.
  • Abortifacient.
31
Q

Alprostadil

A

EICOSANOIDS (PGE1)

  • To maintain patency of the ductus arteriosus.
  • For impotence.
32
Q

Epoprostenol

A

Epoprostenol (PGI2)

  • Used in severe pulmonary hypertension
  • To prevent platelet aggregation in dialysis machines.
33
Q

Latanoprost

A

EICOSANOIDS(PGF2 a derivative)

• Used for glaucoma.

34
Q

What are the two classes of LEUKOTRIENE PATHWAY INHIBITORS

A
  • Inhibitors of 5-lypoxygenase: zileuton
  • Antagonists of LTD4 receptors: zafirlukast, montelukast
35
Q

GLUCOCORTICOIDS function?

A
  • Glucocorticoids inhibit PLA2, thus blocking the release of arachidonic acid.
  • Glucocorticoids inhibit synthesis of COX-2.

PCM Exam 2 Pharm (14 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions