Part 6.2 - Autacoids - Serotonin, Eicosanoids

e. None

Serotonin locations except:

a. Enterochromaffin cells

b. Thrombocytes or Platelets

c. Stomach

d. CNS: Brain

e. None

c. Both

Enterochromaffin cells.

a. Found in the small intestine

b. Majority of serotonin, NMT 90% is being synthesize by Enterochromaffin cells

c. Both

d. None

b. Tryptophan

Precursor of biosynthesis of serotonin.

a. Tyrosine

b. Tryptophan

c. Dopamine

d. Threonine

e. Histidine

d. a and b

tryptophan (hydroxylase) → 5-hydroxytrytophan (decarboxylase) → 5-hydroxytryptamine

Tryptophan under go this/these reaction/s to be converted to 5-hydroxytryptamine.

a. Hydroxylation

b. Decarboxylation

c. Methylation

d. a and b

e. b and c

f. All

a. 5-hydroxytryptamine (5HT)

Serotonin is commonly referred to as its chemical name which is.

a. 5-hydroxytryptamine (5HT)

b. 5-hydroxytyrosine (5HT)

c. 5-hydroxytrypthopan (5HT)

d. 5-hydroxythreonine (5HT)

a. I, II, III, IV, V

Types of Serotonergic Receptor

I. 5-HT1A

II. 5-HT1B/1D

III. 5-HT2

IV. 5-HT3

V. 5-HT4

a. I, II, III, IV, V

b. I, II, III, IV

c. II, III, IV, V

d. I, II, III

e. III, IV, V

f. All

5-HT1A receptor.

a. Pre-synaptically located

b. Inhibitory effect thus it decrease cAMP levels

c. Effect is autoregulation wherein it inhibits further release of serotonin once activated

d. a and b

e. b and c

f. All

f. All

5-HT1B/1D receptor.

a. Located in the vascular smooth muscles

b. Not seen in all blood vessels like in the heart and skeletal muscles

c. Causes vasoconstriction

d. a and b

e. b and c

f. All

a. I, II, III, IV, V

5HT2 receptor.

I. Enhances Phospholipase C activity

II. Causes contraction of smooth muscles (Bronchi, Blood vessels, Intestines)

III. Located in the thrombocytes/platelets

IV. Responsible for blood clot formation (aggregation) thus is a pro-aggregant

V. Can cause hallucination as it is CNS acting

a. I, II, III, IV, V

b. I, II, III, IV

c. II, III, IV, V

d. I, II, III

e. III, IV, V

f. All

5HT3 receptor.

a. Ionotropic receptors

b. Centrally located specifically in the Chemoreceptor Trigger Zone (CTZ)

c. Causes nausea and vomiting when activated

d. a and b

e. b and c

f. All

f. All

5HT4 receptor.

a. Increase cAMP

b. Located at the GIT

c. Causes peristalsis

d. a and b

e. b and c

f. All

a. 5-HT1A

Serotonin receptor type that causes autoregulation.

a. 5-HT1A

b. 5-HT1B/1D

c. 5-HT2

d. 5-HT3

e. 5-HT4

b. 5-HT1B/1D

Serotonin receptor type that is not found in the blood vessel in the heart and skeletal muscles.

a. 5-HT1A

b. 5-HT1B/1D

c. 5-HT2

d. 5-HT3

e. 5-HT4

c. 5-HT2

Serotonin receptor type that is pro-aggregant.

a. 5-HT1A

b. 5-HT1B/1D

c. 5-HT2

d. 5-HT3

e. 5-HT4

d. 5-HT3

Serotonin receptor type that is an ionotropic receptor.

a. 5-HT1A

b. 5-HT1B/1D

c. 5-HT2

d. 5-HT3

e. 5-HT4

d. 5-HT3

Serotonin receptor type that is found in the Chemoreceptor Trigger Zone (CTZ).

a. 5-HT1A

b. 5-HT1B/1D

c. 5-HT2

d. 5-HT3

e. 5-HT4

f. I, II, III, IV, V, VI, VII

5HT Agonists

I. Buspirone

II. Sumatriptan

III. Naratriptan

IV. Zolmitriptan

V. Cisapride

VI. Tegaserod

VII. Prucalopride

a. I

b. II, III, IV

c. V, VI, VII

d. V, VI

e. VII

f. I, II, III, IV, V, VI, VII

a. I - Buspirone

Partial 5-HT1A agonist

I. Buspirone

II. Sumatriptan

III. Naratriptan

IV. Zolmitriptan

V. Cisapride

VI. Tegaserod

VII. Prucalopride

a. I

b. II, III, IV

c. V, VI, VII

d. V, VI

e. VII

f. I, II, III, IV, V, VI, VII

c. II, III, IV - "triptans"

5-HT1B/1D Agonists

I. Buspirone

II. Sumatriptan

III. Naratriptan

IV. Zolmitriptan

V. Cisapride

VI. Tegaserod

VII. Prucalopride

a. I

b. I, II

c. II, III, IV

d. V, VI, VII

e. V, VI

f. VII

d. V, VI, VII

Cisapride

Tegaserod

Prucalopride

5-HT4 agonist.

I. Buspirone

II. Sumatriptan

III. Naratriptan

IV. Zolmitriptan

V. Cisapride

VI. Tegaserod

VII. Prucalopride

a. I

b. I, II

c. II, III, IV

d. V, VI, VII

e. V, VI

f. VII

e. V, VI - Cisapride , Tegaserod

5-HT4 partial agonist.

I. Buspirone

II. Sumatriptan

III. Naratriptan

IV. Zolmitriptan

V. Cisapride

VI. Tegaserod

VII. Prucalopride

a. I

b. I, II

c. II, III, IV

d. V, VI, VII

e. V, VI

f. VII

f. VII - Prucalopride

5-HT4 full agonist.

I. Buspirone

II. Sumatriptan

III. Naratriptan

IV. Zolmitriptan

V. Cisapride

VI. Tegaserod

VII. Prucalopride

a. I

b. I, II

c. II, III, IV

d. V, VI, VII

e. V, VI

f. VII

a. I

Anxiolytic with therapeutic effects of 2 weeks.

I. Buspirone

II. Sumatriptan

III. Naratriptan

IV. Zolmitriptan

V. Cisapride

VI. Tegaserod

VII. Prucalopride

a. I

b. I, II

c. II, III, IV

d. V, VI, VII

e. V, VI

f. VII

a. I, II, III, IV, V

Triptans: Sumatriptan, Naratriptan, Zolmitriptan

I. Inhibit vasodilation of cerebral blood vessels

II. Inhibits inflammation of meninges

III. Anti-migraine Agents

IV. A/E: Increase in Blood Pressure

V. C/I: Patients with Hypertension

a. I, II, III, IV, V

b. I, II, III, IV

c. II, III, IV, V

d. I, II, III

e. III, IV, V

b. Sumatriptan

Serotonin agonist that is anti-migraine agent.

a. Buspirone

b. Sumatriptan

c. Cisapride

d. Cyproheptadine

d. V, VI, VII

Cisapride

Tegaserod

Prucalopride

Management of Irritable Bowel Syndrome with Predominant Constipation.

I. Buspirone

II. Sumatriptan

III. Naratriptan

IV. Zolmitriptan

V. Cisapride

VI. Tegaserod

VII. Prucalopride

a. I

b. I, II

c. II, III, IV

d. V, VI, VII

e. V, VI

f. VII

c. Cisapride

Serotonin agonist used for management of Irritable Bowel Syndrome with predominant constipation.

a. Buspirone

b. Sumatriptan

c. Cisapride

d. Cyproheptadine

e. Naratriptan - this is 5HT 1B/1D agonist.

Serotonin antagonists except:

a. Cyproheptadine

b. Ondansetron

c. Granisetron

d. Palonosetron

e. Naratriptan

f. None

a. I - Cyproheptadine

Blocks 5-HT1 and 5-HT2 receptors.

I. Cyproheptadine

II. OndansetroN

III. Granisetron

IV. Palonosetron

a. I

b. II

c. I, II

d. I, II, III

e. II, III, IV

f. I, II, III, IV

f. All

Cyproheptadine.

a. Blocks Antihistaminic receptors

b. Blocks Anticholinergic (Muscarinic) receptors

c. Management of serotonin syndrome (Hyperthermic disorder)

d. a and b

e. b and c

f. All

e. II, III, IV - "setrons"

Blocks 5-HT3 receptors.

I. Cyproheptadine

II. OndansetroN

III. Granisetron

IV. Palonosetron

a. I

b. II

c. I, II

d. I, II, III

e. II, III, IV

f. I, II, III, IV

c. Both

"Setrons" uses.

a. Anti-emetic

b. Prevention/treatment of chemotherapy-induced N&V

c. Both

d. None

a. I, II, III, IV, V

Ergots

I. Isolated from Claviceps purpurea

II. Core nucleus: Ergoline

III. Structural similarities with Serotonin, thus, they can modify the effect of serotonin

IV. Strong structural similarities to Dopamine, Norepinephrine

V. Have agonist and antagonist property in Alpha, Dopamine, and Serotonin receptors

a. I, II, III, IV, V

b. I, II, III, IV

c. II, III, IV, V

d. I, II, III

e. III, IV, V

c. Ergoline

Core nucleus of ergot.

a. Proline

b. Ergotine

c. Ergoline

d. Erstopline

a. Methylergonovine

Ergot drug:

α-Adrenoceptor agonist.

a. Methylergonovine

b. Ergotamine

c. Methysergide

b. Ergotamine

Ergot drug:

α-Adrenoceptor agonist

5HT receptor agonist

a. Methylergonovine

b. Ergotamine

c. Methysergide

c. Methysergide

Ergot drug:

5-HT receptor antagonist

a. Methylergonovine

b. Ergotamine

c. Methysergide

a. Methylergonovine

(also, ergometrine)

Ergot drug:

Used for postpartum hemorrhage.

a. Methylergonovine

b. Ergotamine

c. Methysergide

b. Ergotamine

Ergot drug:

Used for acute migraine attacks.

a. Methylergonovine

b. Ergotamine

c. Methysergide

c. Methysergide

Ergot drug:

Used for migraine prophylaxis.

a. Methylergonovine

b. Ergotamine

c. Methysergide

a. Methylergonovine

Ergot drug:

Causes hypertension and nausea.

a. Methylergonovine

b. Ergotamine

c. Methysergide

b. Ergotamine

Ergot drug:

Causes nausea and diarrhea.

a. Methylergonovine

b. Ergotamine

c. Methysergide

c. Methysergide

Ergot drug:

Causes fibroblastic changes.

a. Methylergonovine

b. Ergotamine

c. Methysergide

c. Both

Eicosanoids.

a. Compounds that are derived from metabolism of 20-carbon, unsaturated fatty acids generally referred to as eicosanoic acid.

b. Arachidonic acid is most utilized which is a of poly unsaturated fatty acid due having 4 double bonds.

c. Both

d. None

d. Arachidonic acid

Most utilized 20-C unsaturated fatty acids (Eicosanoic acid)

a. Oleic acid

b. Myristic acid

c. Stearic acid

d. Arachidonic acid

e. Arachidinic acid

a. I, II, III

Biosynthesis of eicosanoids

I. Phospholipid is the source of arachidonic acid

II. Hydrolyzable lipids with ester functional group is hydrolyze by the enzyme Phospholipase A2 to form Arachidonic acid

III. Arachidonic acid then serves as a substrate for certain enzyme to act in production of eicosanoids.

a. I, II, III

b. I, II

c. I, III

d. III

a. Leukotrienes

Arachidonic acid through enzyme Lipooxygenase will form

a. Leukotrienes

b. Prostanoids

b. Prostanoids

Arachidonic acid through enzyme Cyclooxygenase will form

a. Leukotrienes

b. Prostanoids

f. All

Prostanoids.

a. Prostaglandins

b. Prostacyclins

c. Thromboxanes

d. a and b

e. a and c

f. All

e. None

Eicosanoids in the vascular smooth muscles except:

a. PGE 2

b. PGF 2α

c. PGI 2 (Prostacylin)

d. TXA 2 (Thromboxane)

e. None

f. a and b

Eicosanoids in the vascular smooth muscles that causes vasodilation.

a. PGE 2

b. PGI 2 (Prostacyclin)

c. PGF 2α

d. TXA 2 (Thromboxane)

e. a and b

f. a, b, and c

f. c and d

PGF

TXA2 (Thromboxane)

Eicosanoids in the vascular smooth muscles that causes vasoconstriction.

a. PGE 2

b. PGI 2 (Prostacyclin)

c. PGF 2α

d. TXA 2 (Thromboxane)

e. a and b

f. c and d

g. a, b, and c

f. All

Eicosanoids causing inflammation.

a. PGI2 (Prostacylin)

b. PGE2

c. Leukotrienes (LTB4)

d. a and b

e. b and c

f. All

a. PGI2 (Prostacylin)

Eicosanoids causing inflammation that increase blood flow.

a. PGI2 (Prostacylin)

b. PGE2

c. Leukotrienes (LTB4)

d. a and b

e. b and c

f. All

b. PGE2

Eicosanoids causing inflammation that increase blood flow as well as bradykinin.

a. PGI2 (Prostacylin)

b. PGE2

c. Leukotrienes (LTB4)

d. a and b

e. b and c

f. All

b. PGE2

Dominant eicosanoids causing inflammation.

a. PGI2 (Prostacylin)

b. PGE2

c. Leukotrienes (LTB4)

d. a and b

e. b and c

f. All

c. Leukotrienes (LTB4)

Chemotactic factor which induced movement of inflammatory cells to the effected sites.

a. PGI2 (Prostacylin)

b. PGE2

c. Leukotrienes (LTB4)

d. a and b

e. b and c

f. All

f. All

Eicosanoids in the bronchi.

a. PGE series

b. LTC4

c. LTD4

d. a and b

e. b and c

f. All

a. PGE series

(PGE, PGI2)

Eicosanoids in the bronchi that causes bronchodilation.

a. PGE series

b. LTC4

c. LTD4

d. a and b

e. b and c

f. All

e. b and c

Eicosanoids in the bronchi that causes bronchoconstriction.

a. PGE series

b. LTC4

c. LTD4

d. a and b

e. b and c

f. All

e. b and c

Eicosanoids in the bronchi which are leukotrienes and referred to as the Slow-reacting Substances of Anaphylaxis (SRSAs).

a. PGE series

b. LTC4

c. LTD4

d. a and b

e. b and c

f. All

c. Both

Eicosanoids in the uterus.

a. PGE2

b. PGF

c. Both

d. None

f. All

Effect of PGE2 and PGF in the uterus.

a. Contraction

b. Oxytocic

c. Dysmenorrhea

d. a and b

e. b and c

f. All

a. PGE

Eicosanoids in the stomach.

a. PGE

b. PGF

c. Both

d. None

f. All

(pepsinogen is converted to pepsin with the use of HCl)

Effect of PGE in the stomach.

a. Cytoprotection

b. Inhibit acid secretion

c. Inhibit pepsinogen secretion

d. a and b

e. b and c

f. All

PGE, PGI2

PGF, TXA2

Eicosanoids acting on the platelets.

a. PGE, PGI2

Eicosanoids acting on the platelets that is anti-aggregant promoting bleeding.

a. PGE, PGI2

b. PGF, TX2

c. Both

d. None

b. PGF, TXA2

Eicosanoids acting on the platelets that is antagonist of prostacyclin causing clotting.

a. PGE, PGI2

b. PGF, TXA2

c. Both

d. None

c. PGF2a

Eicosanoid in the eyes that enhances outflow of aqueous humor reducing Intra ocular pressure (IOP).

a. PGI2

b. PGE2

c. PGF2a

d. LTC4

f. None

"MADLE”

Prostaglandin analogs except:

a. Misoprostol

b. Alprostadil

c. Dinoprostone

d. Latanosprost

e. Epoprostenol

f. None

a. Misoprostol

Prostaglandin analog:

1) PGE1 analog: Cytoprotectant

2) Provide clinical benefit to patients having stomach problems

3) Used for NSAID induced ulcers, but already banned from the market due to abortifacient use

a. Misoprostol

b. Epoprostenol

c. Dinoprostone

d. Alprostadil

e. Latanosprost

b. Epoprostenol

Prostaglandin analog:

PGI2 analog

a. Misoprostol

b. Epoprostenol

c. Dinoprostone

d. Alprostadil

e. Latanosprost

b. Epoprostenol

Prostaglandin analog:

1) Causes vasodilation

2) Use in the management of primary pulmonary hypertension

a. Misoprostol

b. Epoprostenol

c. Dinoprostone

d. Alprostadil

e. Latanosprost

c. Dinoprostone

Prostaglandin analog:

PGE2 analog

a. Misoprostol

b. Epoprostenol

c. Dinoprostone

d. Alprostadil

e. Latanosprost

c. Dinoprostone

• used for cervical ripening

Prostaglandin analog:

US FDA approved abortifacient

a. Misoprostol

b. Epoprostenol

c. Dinoprostone

d. Alprostadil

e. Latanosprost

d. Alprostadil

Prostaglandin analog:

PGE1 analog causing marked vasodilation that is administered locally for the treatment of Erectile Dysfunction

a. Misoprostol

b. Epoprostenol

c. Dinoprostone

d. Alprostadil

e. Latanosprost

e. Latanosprost

Prostaglandin analog:

PGF2α analog

a. Misoprostol

b. Epoprostenol

c. Dinoprostone

d. Alprostadil

e. Latanosprost

e. Latanosprost

Prostaglandin analog:

Enhance drainage of aqueous fluid in the eyes lowering IOP thus used for treatment of glaucoma

a. Misoprostol

b. Epoprostenol

c. Dinoprostone

d. Alprostadil

e. Latanosprost