Autacoids

Question 1

Histamine

Answer 1

Target: H1 in endothelium, smooth muscle and nerve endings; H2 in gastric mucosa, cardiac muscle and immune cells

Question 2

Epinephrine

Answer 2

Physiologic antagonist of Histamine

Question 3

Cromolyn

Answer 3

Histamine release inhibitor
Action: reduce mast cell degranulation when it is immunologically induced
*β2 agonists are also capable of reducing Histamine release

Question 4

First Generation H1 Receptor Antagonists

Answer 4

Chlorpheniramine, Cyclizine, Diphenhydramine, Dimenhydrinate, Hydroxyzine, Meclizine, Promethazine
*sedative properties d/t CNS effects are use to tx insomnia

Question 5

Second Generation H1 Receptor Antagonists

Answer 5

Fexofenadine, Loratadine, Cetirizine

*fewer CNS effects bc they are less lipophilic and are substrates of P-glycoprotein

Question 6

Serotonin

Answer 6

Target: 5-HT3 receptor is only monoamine neurotransmitter receptor known to function as ligand-gated ion channel (the other 6 are G-protein coupled)

Question 7

Sumatriptan

Answer 7

5-HT 1D/1B receptor agonist
Use: first line therapy for acute severe migraine attacks
SE: coronary vasospasm (contraindicated w/ CAD or angina)

Question 8

Metoclopramide

Answer 8

5-HT4 receptor agonist
Action: prokinetic agent
SE: somnolence, nervousness, dysgenic rxn

Question 9

Cisapride

Answer 9

5-HT4 receptor agonist
Action: prokinetic agent, prolonged QT interval
SE: cardiac adverse effects so it is NO LONGER available in US

Question 10

Cyproheptadine

Answer 10

5-HT2 receptor antagonist

Use: allergic rhinitis, vasomotor rhinitis, tx/management of Serotonin Syndrome

Question 11

Ondansteron

Answer 11

5-HT3 receptor antagonist

Use: anti-emetic, tx N/V in chemotherapy pt

Question 12

Dinoprostone

Answer 12

PGE2 analog

Use: ripen cervix at/near term, abortifacient

Question 13

Misoprostol

Answer 13

PGE1 analog
Use: present ulcers in pt taking high dose NSAIDs
Off label uses: ripen cervix at/near term, management of postpartum hemorrhage

Question 14

Alprostadil

Answer 14

PGE1

Use: maintain latency of ductus arteriosus, impotence

Question 15

Prostacyclin

Answer 15

Prostacyclin aka PGI2 - synthesized by vascular endothelium (by COX) as anticoagulant via vasodilation and inhibition of platelet aggregation

Question 16

Latanoprost

Answer 16

PGF2α derivative

Use: open-angle glaucoma

Question 17

Zileuton

Answer 17

5-LOX inhibitor

Question 18

Zafirlukast

Answer 18

Antagonist of LTD4 receptor

Question 19

Montelukast

Answer 19

Antagonist of LTD4 receptor

Question 20

H2 Receptor Antagonists

Answer 20

Cimetidine, Ranitidine, Famotidine, Nizatidine

Question 20

H2 Receptor Antagonist Uses

Answer 20

Tx peptic ulcers, acute stress ulcers, and prevent/tx heart-burn
(Action: inhibition of gastric acid secretion)

Question 20

Ergot Alkaloids

Answer 20

Ergotamine, Dihydroergotamine, Bromocriptine, Cabergoline, Ergonovine, Methylergonovine
*produced by fungus that infects grain

Question 21

Ergotamine or Dihydroergotamine Use?

Answer 21

Migraine

Question 22

Bromocriptine and Cabergoline Use?

Answer 22

Hyperprolactinemia from prolactinoma

Question 23

Ergonovine or Methylergonovine Use?

Answer 23

Postpartum hemorrhage tx if Oxytocin is ineffective

Question 24

Ergonovine Use

Answer 24

Dx of variant angina bc it provokes coronary artery vasospasm

Question 25

Ergot Alkaloid SEs

Answer 25

Vasospasm, CI in pregnancy and pts w/ CAD, HTN, impaired renal or hepatic function

Question 26

Epoprostenol

Answer 26

PGI2

Use: pulmonary HTN, prevent platelet aggregation in dialysis machines

Question 27

Cimetidine

Answer 27

SE: inhibits CYP450, gynecomastia, reduced sperm count in men, galactorrhea in women