Part 3 - SMOOTH MUSCLE - AUTACOIDS

Proverbs 16:3

b. Localized hormones

AUTACOIDS are also known as ________.

a. Systemic hormones
b. Localized hormones
c. Endocrine stimulants
d. Skeletal muscle blockers

b. Near the site of action

The site of release of AUTACOIDS is ________.

a. Far from the site of action
b. Near the site of action
c. Inside endocrine glands only
d. Limited to the brain

b. Virtually all cells

AUTACOIDS are produced by ________.

a. Specific endocrine glands only
b. Virtually all cells
c. Skeletal muscles only
d. The adrenal medulla only

c. Systemic and produced by specific cells

AUTACOIDS - local & all cells

Endocrine- systemic & specific cells

AUTACOIDS differ from endocrine hormones because endocrine hormones are ________.

a. Localized and produced by all cells
b. Produced by virtually all cells
c. Systemic and produced by specific cells
d. Limited to the gastrointestinal tract

All

“BESH”

AUTACOID:

a. Histamine
b. Eicosanoids
c. Bradykinin
d. Serotonin

b. Mast cells

[HISTAMINE]

One major location of Histamine is ________.

a. Skeletal muscle only
b. Mast cells
c. Kidneys only
d. Thyroid gland

a. Basophils

[HISTAMINE]

Histamine is stored in ________.

a. Basophils
b. Hepatocytes
c. Osteocytes
d. Erythrocytes

a. Stomach

[HISTAMINE]

a. Stomach
b. Pancreas only
c. Adrenal cortex only
d. Bone marrow only

b. Central Nervous System (CNS)

[HISTAMINE]

Histamine is present in the ________.

a. Peripheral bones
b. Central Nervous System (CNS)
c. Skeletal joints only
d. Liver only

c. L-histidine

[HISTAMINE]

Histamine is synthesized from ________.

a. Tyrosine
b. Tryptophan
c. L-histidine
d. Glycine

c. L-histidine decarboxylase

[HISTAMINE]

The enzyme responsible for Histamine biosynthesis is ________.

a. Acetylcholinesterase
b. Monoamine oxidase
c. L-histidine decarboxylase
d. Tyrosine hydroxylase

b. L-histidine

[HISTAMINE]

Histamine is formed through the decarboxylation of ________.

a. Dopamine
b. L-histidine
c. Epinephrine
d. Acetylcholine

a. Ca²⁺-dependent and Ca²⁺-independent degranulation

[HISTAMINE]

The mechanism of Histamine release includes ________.

a. Ca²⁺-dependent and Ca²⁺-independent degranulation
b. Adrenergic and cholinergic stimulation
c. Alpha and beta receptor activation
d. Endocrine and exocrine secretion

a. Ca²⁺-dependent degranulation

[HISTAMINE]

Induced by immunoglobulin E (IgE) fixation to mast cells

a. Ca²⁺-dependent degranulation

b. Ca²⁺-independent degranulation

a. Ca²⁺-dependent degranulation

[HISTAMINE]

Anaphylaxis

a. Ca²⁺-dependent degranulation

b. Ca²⁺-independent degranulation

b. Ca²⁺-independent degranulation

[HISTAMINE]

Induced by drugs

a. Ca²⁺-dependent degranulation

b. Ca²⁺-independent degranulation

b. Ca²⁺-independent degranulation

[HISTAMINE]

Anaphylactoid reaction

a. Ca²⁺-dependent degranulation

b. Ca²⁺-independent degranulation

All

“TAG Mo”

[HISTAMINE]

Drugs that can induce Ca²⁺-independent Histamine degranulation.

(Multiple Answers)

a. Morphine
b. Tubocurarine
c. Guanethedine
d. Amine Antibiotics

b. Binding histaminic receptors

[HISTAMINE]

The mechanism of action of Histamine is ________.

a. Blocking acetylcholine receptors
b. Binding histaminic receptors
c. Stimulating dopamine release
d. Inhibiting ion channels

a. Histaminic-1 (H1)

[HISTAMINE]

Vasodilation

a. Histaminic-1 (H1)

b. Histaminic-2 (H2)

c. Histaminic-3 (H3)

d. Histaminic-4 (H4)

a. Histaminic-1 (H1)

[HISTAMINE]

Bronchoconstriction

a. Histaminic-1 (H1)

b. Histaminic-2 (H2)

c. Histaminic-3 (H3)

d. Histaminic-4 (H4)

a. Histaminic-1 (H1)

[HISTAMINE]

Pain and itchiness

a. Histaminic-1 (H1)

b. Histaminic-2 (H2)

c. Histaminic-3 (H3)

d. Histaminic-4 (H4)

a. Histaminic-1 (H1)

[HISTAMINE]

Contraction of endothelial cells

a. Histaminic-1 (H1)

b. Histaminic-2 (H2)

c. Histaminic-3 (H3)

d. Histaminic-4 (H4)

a. Histaminic-1 (H1)

[HISTAMINE]

a. Histaminic-1 (H1)

b. Histaminic-2 (H2)

c. Histaminic-3 (H3)

d. Histaminic-4 (H4)

b. Histaminic-2 (H2)

[HISTAMINE]

Increase gastric acid production

a. Histaminic-1 (H1)

b. Histaminic-2 (H2)

c. Histaminic-3 (H3)

d. Histaminic-4 (H4)

b. Histaminic-2 (H2)

[HISTAMINE]

Enhances degranulation of histamine

a. Histaminic-1 (H1)

b. Histaminic-2 (H2)

c. Histaminic-3 (H3)

d. Histaminic-4 (H4)

c. Histaminic-3 (H3)

[HISTAMINE]

Decrease histamine release

a. Histaminic-1 (H1)

b. Histaminic-2 (H2)

c. Histaminic-3 (H3)

d. Histaminic-4 (H4)

d. Histaminic-4 (H4)

[HISTAMINE]

Chemotaxis

a. Histaminic-1 (H1)

b. Histaminic-2 (H2)

c. Histaminic-3 (H3)

d. Histaminic-4 (H4)

b. Histamine

[HISTAMINE]

___agonist no longer used clinically.

a. Betahistine
b. Histamine
c. Epinephrine
d. Impromidine

a. Pulmonary challenge test

[HISTAMINE]

An obsolete use of Histamine agonist is the ________.

a. Pulmonary challenge test
b. Management of Parkinsonism
c. Treatment of hyperacidity
d. Bronchodilation in COPD

b. Gastric secretory function

[HISTAMINE]

Histamine agonist was formerly used to test ________.

a. Skeletal muscle contraction
b. Gastric secretory function
c. Renal filtration rate
d. Dopamine release

H1 agonist ; H3 antagonist

[HISTAMINE]

Betahistine

(Multiple Answers)

a. H1 agonist

b. H2 agonist

c. H3 agonist

d. H4 agonist

a. Betahistine

[HISTAMINE]

Management of Meniere’s Disease associated with vertigo

a. Betahistine
b. Morphine
c. Tubocurarine
d. Neostigmine

a. Betahistine

[HISTAMINE]

Endolymph, presence of fluid in the inner ear, is managed by

a. Betahistine
b. Morphine
c. Tubocurarine
d. Neostigmine

a. Impromidine

[HISTAMINE]

________ is classified as investigational.

a. Impromidine
b. Betahistine
c. Epinephrine
d. Histamine

b. Epinephrine

[HISTAMINE]

_______ is a functional antagonist of Histamine.

a. Betahistine
b. Epinephrine
c. Antihistamine
d. Histamine

b. Pharmacologic

Functional Antagonists- Epinephrine

Pharmacologic Antagonists- Antihistamines

[HISTAMINE]

_______ antagonism of Histamine is produced by antihistamines.

a. Functional
b. Pharmacologic

a. Alpha (α)

Functional: Epinephrine

• α- vasoconstriction

• β- bronchodilation

[HISTAMINE]

___ receptor activation by Epinephrine produces vasoconstriction.

a. Alpha (α)
b. Beta (β)
c. Histaminic
d. Muscarinic

c. Beta (β)

Functional: Epinephrine

• α- vasoconstriction

• β- bronchodilation

[HISTAMINE]

_______ receptor activation by Epinephrine produces bronchodilation.

a. Alpha (α)
b. Histaminic
c. Beta (β)
d. Nicotinic

a. H1 antihistamines

anti-allergy

do not give for bronchial asthma

[HISTAMINE]

Use: allergic reaction, asthma

a. H1 antihistamines

b. H2 antihistamines

b. Lipophilic and can cross the Blood-Brain Barrier (BBB)

Correct:

c. Powerful central anticholinergics
d. Sedating agents

[HISTAMINE]

First-generation (classical) antihistamines are ________.

a. Hydrophilic and cannot cross the BBB
b. Lipophilic and can cross the Blood-Brain Barrier (BBB)
c. Limited to peripheral tissues only
d. Non-sedating agents only

c. Ethanolamines

[HISTAMINE]

______ antihistamines are considered the most sedating and most efficacious.

a. Piperazines
b. Alkylamines
c. Ethanolamines
d. Phenothiazines

a. Diphenhydramine

[HISTAMINE]

_____ is an ethanolamine antihistamine used in the management of Acute Dystonic Crisis.

a. Diphenhydramine
b. Hydroxyzine
c. Promethazine
d. Cetirizine

a. Doxylamine

[HISTAMINE]

______ is an ethanolamine used as a sleeping aid.

a. Doxylamine
b. Carbinoxamine
c. Chlorpheniramine
d. Meclizine

a. Pyrilamine

[HISTAMINE]

_______ is an Ethylenediamine that may cause moderate sedation and GI upset.

a. Pyrilamine
b. Cyclizine
c. Hydroxyzine
d. Brompheniramine

b. Motion sickness

[HISTAMINE]

Meclizine and Cyclizine are used for ________.

a. Hyperacidity
b. Motion sickness
c. Acute dystonic crisis
d. Serotonin syndrome only

a. Hydroxyzine

[HISTAMINE]

A prodrug whose active form is Cetirizine.

a. Hydroxyzine
b. Cyclizine
c. Promethazine
d. Tripelennamine

a. OTC cold medications

[HISTAMINE]

Brompheniramine and Chlorpheniramine are components of ________.

a. OTC cold medications
b. Antidepressants
c. Muscle relaxants
d. Antipsychotics

a. Promethazine

[HISTAMINE]

Used as a preanesthetic agent.

a. Promethazine
b. Hydroxyzine
c. Cyproheptadine
d. Doxylamine

a. Cyproheptadine

[HISTAMINE]

Also possesses antiserotonergic and anticholinergic activities used in management of serotonin syndrome

a. Cyproheptadine
b. Tripelennamine
c. Cyclizine
d. Doxylamine

b. Less lipophilic and less sedating

[HISTAMINE]

Second-generation antihistamines are ________.

a. More lipophilic and highly sedating
b. Less lipophilic and less sedating
c. Unable to act on histamine receptors
d. Powerful central anticholinergics

a. Less sedating

Piperidines- True, non-sedating

[HISTAMINE]

2nd generation Piperazines

a. Less sedating

b. True, non-sedating

b. True, non-sedating

Piperazines- Less sedating

[HISTAMINE]

2nd generation Piperidines

a. Less sedating

b. True, non-sedating

Piperazines ____a. Meclizine

Ethanolamines__b. Dimenhydrinate

Alkylamines ____c. Brompheniramine

Ethylenediamine_d. Pyrilamine

Ethanolamines __e. Diphenhydramine

Ethylenediamine _f. Tripelennamine

Ethanolamines __g. Carbinoxamine

Piperazines_____h. Hydroxyzine

Piperidine_______j. Cyproheptadine

Ethanolamines___k. Doxylamine

Piperazines______l. Cyclizine

Alkylamines_____m. Chlorpheniramine

Phenothiazine ___n. Promethazine

[HISTAMINE]

1st generation (classical)

Choices: Ethanolamines, Ethylenediamine, Piperazines, Alkylamines, Phenothiazine, or Piperidine

___a. Meclizine

___b. Dimenhydrinate

___c. Brompheniramine

___d. Pyrilamine

___e. Diphenhydramine

___f. Tripelennamine

___g. Carbinoxamine

___h. Hydroxyzine

___j. Cyproheptadine

___k. Doxylamine

___l. Cyclizine

___m. Chlorpheniramine

___n. Promethazine

II. Cetirizine

IV. Levocetirizine

[HISTAMINE]

2nd generation Antihistamine: Piperazines

I. Loratadine

II. Cetirizine

III. Desloratadine

IV. Levocetirizine

V. Fexofenadine

I. Loratadine

III. Desloratadine

V. Fexofenadine

[HISTAMINE]

2nd generation Antihistamine: Piperidines

I. Loratadine

II. Cetirizine

III. Desloratadine

IV. Levocetirizine

V. Fexofenadine

c. Cimetidine

Cimetidine (least potent)

Famotidine (most potent)

[HISTAMINE]

_______ is the least potent H₂ receptor antagonist.

a. Famotidine
b. Ranitidine
c. Cimetidine
d. Nizatidine

a. Famotidine

Cimetidine (least potent)

Famotidine (most potent)

[HISTAMINE]

_______ is the most potent H₂ receptor antagonist.

a. Famotidine
b. Cimetidine
c. Ranitidine
d. Nizatidine

b. Gastric and duodenal ulcers

-Nizatidine???

[HISTAMINE]

H₂ blockers promote healing of ________.

a. Motion sickness
b. Gastric and duodenal ulcers
c. Acute dystonic crisis
d. Parkinsonism

c. Zollinger-Ellison Syndrome

[HISTAMINE]

H₂ blockers are used for treatment of hypersecretory states such as ________.

a. Motion sickness
b. Parkinson disease
c. Zollinger-Ellison Syndrome
d. Diabetes mellitus

c. Cimetidine

[HISTAMINE]

______ is considered the prototype H₂ blocker.

a. Famotidine
b. Ranitidine
c. Cimetidine
d. Nizatidine

b. Enzyme inhibitor

[HISTAMINE]

Cimetidine acts as an ________, leading to drug interactions and toxicity.

a. Histamine agonist
b. Enzyme inhibitor
c. Enzyme inducer
d. CNS stimulant

b. Gynecomastia, loss of libido, and infertility

[HISTAMINE]

Cimetidine may cause antiandrogenic effects such as ________.

a. Myalgia and rhabdomyolysis
b. Gynecomastia, loss of libido, and infertility
c. Hyperactivity and insomnia
d. Bronchospasm and cough

c. Serotonin

______ is an autacoid found in enterochromaffin cells, platelets, stomach, and CNS.

a. Histamine
b. Bradykinin
c. Serotonin
d. Eicosanoids

c. L-tryptophan

[Serotonin]

Serotonin is synthesized from ________.

a. L-tyrosine
b. Glycine
c. L-tryptophan
d. Histidine

a. Hydroxylation

Serotonin = hydroxylation → decarboxylation

Histamine = decarboxylation agad

[Serotonin]

Biosynthesis of Serotonin involves ________ followed by decarboxylation.

a. Hydroxylation
b. Oxidation
c. Acetylation
d. Phosphorylation

a. 5-hydroxytryptamine

[Serotonin]

Serotonin (5-HT) is also known as ________.

a. 5-hydroxytryptamine
b. 5-hydroxytyrosine

c. 5-hydroxytryptophan
d. Dopamine hydroxylase

b. Interacts with serotonergic receptors

[Serotonin]

Serotonin MOA

a. Interacts with histaminic receptors
b. Interacts with serotonergic receptors
c. Interacts with nicotinic receptors
d. Interacts with adrenergic receptors

a. 5-HT_1A

[SEROTONERGIC RECEPTORS]

Decrease cAMP

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

a. 5-HT_1A

[SEROTONERGIC RECEPTORS]

mainly located in the presynaptic receptor in the CNS

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

a. 5-HT_1A

[SEROTONERGIC RECEPTORS]

Function is for Autoregulation by inhibiting further release of serotonin

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

_b. 5-HT_1B/1D

-Not involved: blood vessels in the heart ❤ and in the skeletal muscles 💪🏼

[SEROTONERGIC RECEPTORS]

are found in vascular smooth muscles

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

_b. 5-HT_1B/1D

[SEROTONERGIC RECEPTORS]

produce vasoconstriction

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

c. 5-HT₂

[SEROTONERGIC RECEPTORS]

Enhances phospholipase C activity

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

c. 5-HT₂

[SEROTONERGIC RECEPTORS]

Smooth muscles (bronchi 🫁, blood vessels🩸, intestines⚕) → contraction

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

c. 5-HT₂

[SEROTONERGIC RECEPTORS]

Platelets -> aggregation

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

c. 5-HT₂

[SEROTONERGIC RECEPTORS]

CNS -> hallucination

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

d. 5-HT₃

[SEROTONERGIC RECEPTORS]

Inotropic receptors

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

d. 5-HT₃

[SEROTONERGIC RECEPTORS]

Chemoreceptor trigger zone -> nausea anc vomiting

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

e. 5-HT₄

[SEROTONERGIC RECEPTORS]

Enhances cAMP

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

e. 5-HT₄

[SEROTONERGIC RECEPTORS]

GIT -> peristalsis

a. 5-HT_1A

_b. 5-HT_1B/1D

c. 5-HT₂

d. 5-HT₃

e. 5-HT₄

a. Buspirone

[Serotonin Agonists]

______ is a partial 5-HT₁A agonist with anxiolytic effects.

a. Buspirone
b. Cyproheptadine
c. Ondansetron
d. Sumatriptan

a. Buspirone

[Serotonin Agonists]

______ acts as a partial agonist at 5-HT₁_A receptors.

a. Buspirone
b. Prucalopride
c. Granisetron
d. Naratriptan

c. 2 weeks

[Serotonin Agonists]

The therapeutic effects of Buspirone usually appear after ________.

a. 24 hours
b. 3 days
c. 2 weeks
d. 1 month

b. 5-HT₁B/1D agonists

[Serotonin Agonists]

-triptans (e.g., Sumatriptan, Naratriptan, Zolmitriptan) are ________.

a. 5-HT₂ antagonists
b. 5-HT₁B/1D agonists
c. 5-HT₄ antagonists
d. 5-HT₃ blocker

d. -triptans (Sumatriptan, Naratriptan, Zolmitriptan)

[Serotonin Agonists]

Inhibits vasodilation of cerebral blood vessels

a. Buspirone
b. Prucalopride
c. Granisetron
d. -triptans

d. -triptans (Sumatriptan, Naratriptan, Zolmitriptan)

[Serotonin Agonists]

Inhibits inflammation of meninges

a. Buspirone
b. Prucalopride
c. Granisetron
d. -triptans

d. -triptans (Sumatriptan, Naratriptan, Zolmitriptan)

[Serotonin Agonists]

Use: Anti-migraine Agents

a. Buspirone
b. Prucalopride
c. Granisetron
d. -triptans

d. -triptans (Sumatriptan, Naratriptan, Zolmitriptan)

-5-HT_1B/1D = Vasoconstriction = inc BP

[Serotonin Agonists]

A/E: Increase in blood pressure

a. Buspirone
b. Prucalopride
c. Granisetron
d. -triptans

a. Partial 5-HT4 agonists

-Cisapride, Tegaserod

[Serotonin Agonists]

Management of irritable bowel syndrome with predominant constipation

a. Partial 5-HT4 agonists

b. Full 5-HT4 agonists

a. Partial 5-HT4 agonists

[Serotonin Agonists]

Cisapride

a. Partial 5-HT4 agonists

b. Full 5-HT4 agonists

a. Partial 5-HT4 agonists

[Serotonin Agonists]

Tegaserod

a. Partial 5-HT4 agonists

b. Full 5-HT4 agonists

b. Full 5-HT4 agonists

[Serotonin Agonists]

Prucalopride

a. Partial 5-HT4 agonists

b. Full 5-HT4 agonists

a. Blocks 5-HT1 and 5-HT2 receptors

[Serotonin Antagonists]

Cyproheptadine

a. Blocks 5-HT1 and 5-HT2 receptors

b. Block 5-HT3 receptors

c. Prevention/ Treatment of chemotherapy

b. Antihistaminic

[Serotonin Antagonists]

Cyproheptadine

a. Block 5-HT3 receptors

b. Antihistaminic

c. Prevention/ Treatment of chemotherapy

a. Anticholinergic

[Serotonin Antagonists]

Cyproheptadine

a. Anticholinergic

b. Block 5-HT3 receptors

c. Prevention/ Treatment of chemotherapy

b. Block 5-HT3 receptors

[Serotonin Antagonists]

-setrons: Ondansetron Granisetron Palonosetron

a. Anticholinergic

b. Block 5-HT3 receptors

c. Blocks 5-HT1 and 5-HT2 receptors

c. Prevention/ Treatment of chemotherapy- induced nausea and vomiting

[Serotonin Antagonists]

-setrons: Ondansetron Granisetron Palonosetron

a. Anticholinergic

b. Antihistaminic

c. Prevention/ Treatment of chemotherapy- induced nausea and vomiting

b. Claviceps purpurea (Ergoline)

[ERGOTS ALKALOID]

Ergot alkaloids are derived from ________.

a. Bacteria
b. Claviceps purpurea
c. Platelets
d. Enterochromaffin cells

b. Dopamine (DA), norepinephrine (NE), and serotonin (5-HT)

[ERGOTS ALKALOID]

Ergot alkaloids have strong structural similarity to ________.

a. Acetylcholine, histamine, and GABA
b. Dopamine (DA), norepinephrine (NE), and serotonin (5-HT)
c. Insulin, glucagon, and cortisol
d. Nicotine, muscarine, and epinephrine