Autocoids

Question 1

Epinephrine

Answer 1

DOC for Anaphylaxis and other
conditions that involve massive
histamine release

Question 2

First Generation H1 Antagonists

Answer 2

Chlorpheniramine
Cyclizine
Dimenhydrinate
Diphenhydramine
Hydroxyzine
Meclizine
Promethazine

Cross the BBB-Sedative effects

Inverse Agonist,Also block cholinergic, α-adrenergic, serotonin
and local anesthetic receptor sites (unrelated to
their blocking of H1 receptors

DOC in controlling sxs of allergic
rhinitis and urticaria, also treats motion sickness

AE: sedation, dry mouth, hallucinations

Question 3

Second generation H1 Antagonist

Answer 3

Less sedating less able to cross BBB

Fexofenadine
Loratadine
Cetirizine
Astemizole
Terfenadine

Inverse Agonist!↓ constitutive activity

DOC in controlling sxs of allergic
rhinitis and urticaria

AE:Cardiac toxicity (besides Fexofenadine) ,

Question 4

H2 Antagonist

Answer 4

Cimetidine
Ranitidine
Famotidine
Nizatidine

Competitively and reversible H2 inhibitors!
↓cAMP! ↓ gastric acid secretion

Used for GERD,Peptic ulcers

AE: extreme safe, Cimetidine via IV can lead to confusion and hallucination, inhibits CYP450 (lower metabolism of other drugs)

Question 5

Serotonin (5-HT)

Answer 5

No clinical applications as a drug

Question 6

Sumatriptan

Answer 6

5-HT 1D/1B
Agonist

Reduce both sensory activation in the periphery
and nociceptive transmission in the brainstem
trigeminal nucleus!diminish central sensitization
-cause vasoconstriction

DOC for acute severe migraines

Question 7

Metoclopramide

Answer 7

5-HT4 Agonist

Prokinetic Agent! promote and organize gut
motility
-facilitates ACh release from enteric neurons
Central anti-dopaminergic actions! antinauseant,
antiemetic
Peripheral anti-dopaminergic actions!enhance
prokinetic activity by counteracting the inhibitory
effect of D2 receptors

Used for Gastroparesis
Emesis GERD

AE:Somnolence, Nervousness, & Dystonic rxns Extrapyramidal effects & tardive dyskinesia, Galactorrhea

Question 8

Cisapride

Answer 8

5-HT4 Agonist

Prokinetic Agent! promote and organize gut
motility
-facilitates ACh release from enteric neurons
Central anti-dopaminergic actions! antinauseant,
antiemetic
Peripheral anti-dopaminergic actions!enhance
prokinetic activity by counteracting the inhibitory
effect of D2 receptors

Used for Gastroparesis
Emesis GERD

AE:Somnolence, Nervousness, & Dystonic rxns Extrapyramidal effects & tardive dyskinesia, Galactorrhea, NO LONGER USED INCREASES QT

Question 9

Cyproheptadine

Answer 9

5-HT2 Antagonist

Potent H1 blocking actions

Used for: Allergic rhinitis
vasoactive rhinitis .
Serotonin Syndrome ( ↑5-

Question 10

Ondansetron

Answer 10

5-HT3 Antagonist

Powerful anti-emetic

used for controls severe nausea and vomiting in
patients undergoing chemotherapy

Question 11

Dihydroergotamine

Answer 11

Ergot Alkaloids

Used for migraines (Triptans preferred)

Question 12

Ergotamine

Answer 12

Ergot Alkaloids

Used for migraines (Triptans preferred)

Question 13

Bromocriptine

Answer 13

Ergot Alkaloids

Used for Hyperprolactinemia d/t pituitary tumor

Question 14

Cabergoline

Answer 14

Ergot Alkaloids

Used for Hyperprolactinemia d/t pituitary tumor

Question 15

Ergot Alkaloids

Answer 15

Agonist, partial agonist, and antagonist actions at
α-adrenoceptors and 5-HT receptors
Agonist or partial agonist action at CNS dopamine
receptor

AE: Nausea and vomiting (most common)

Contraindicated in pregnant women, pts with
peripheral vascular disease. CAD, HTN, and impaired
hepatic/renal fxn
Should not be used concurrently with drugs that cause
vasoconstriction

Question 16

Ergonovine

Answer 16

Ergot Alkaloids

Uses Postpartum Hemorrhage when oxytocin is ineffective Ergonovine: provoke coronary artery
spasm! diagnose variant angina

AE: vasospasms

Question 17

Methylergonovine

Answer 17

Ergot Alkaloids

Uses Postpartum Hemorrhage when oxytocin is ineffective

AE: vasospasms

Question 18

Misoprostol

Answer 18

PGE 1 analog (Eicosanoid)

Used in Ripen cervix at or near term
Postpartum hemorrhage
Abortion when used in combination with a progesterone
antagonist (mifepristone/methotrexate)
Prevention of peptic ulcers in patients taking high does of NSAIDS

Question 19

Eicosanoids

Answer 19

Act in autocrine and paracrine fashion
Bind to G-protein coupled receptors (Gs, Gi or Gq)
Contractile effects on smooth mm. are mediated by release of
Ca2+
Relaxing effects are mediated by elevation in cAMP

Question 20

Dinoprostone

Answer 20

PGE2 (Eicosanoid)

used for Ripen cervix at or near term, Abortion

Question 21

Alprostadil

Answer 21

PGE1(Eicosanoid)

Used for maintain patency of the ductus arteriosus in infants with transposition of the great vessels

Impotence

Question 22

Epoprostenol

Answer 22

PGI2 Prostacyclin(Eicosanoid)

Used in Severe pulmonary HTN (↓ peripheral, pulm, and coronary
resistance)
Prevents platelet aggregation in dialysis machines

Question 23

Latanoprost

Answer 23

PGF2α(Eicosanoids)

Used for glaucoma

Question 24

Zileuton

Answer 24

Eicosanoid
Antagonists

Leukotriene inhibitors

Inhibits 5-lipoxygenase

Used for Moderate-severe asthma in pts. who are poorly controlled by
conventional therapy or experience adverse effects with corticoids

Question 25

Montelukast

Answer 25

Eicosanoid
Antagonists

Leukotriene inhibitors

Inhibits binding of LTD4

Used for Moderate-severe asthma in pts. who are poorly controlled by
conventional therapy or experience adverse effects with corticoids

Question 26

Zafirlukast

Answer 26

Eicosanoid
Antagonists

Leukotriene inhibitors

Inhibits binding of LTD4

Used for Moderate-severe asthma in pts. who are poorly controlled by
conventional therapy or experience adverse effects with corticoids

Question 27

Glucocorticoids

Answer 27

Stimulate lipocortin! Inhibit cytosolic phospholipase A2!
block arachidonic acid
Inhibit COX-2 synthesis

Used for anti-inflammatory actions

Question 28

NSAIDs

Answer 28

Inhibit COX 1 and COX 2

Used for anti-inflammatory actions