AUTACOIDS

H1 RECEPTOR
ALLERGIC AND ANAPHYLACTIC RESPONSES

ORGAN

ACTION
BronchoCONSTRICTION
(CONTRACTION of bronchial
smooth muscles difficulty in
breathing)
Catecholamine RELEASE
(Sympathetic response)
Constriction
Increase permeability
(edema)
Contraction (diarrhea)
Dilation
Positive inotropic and
chronotropic

Lung

Adrenal medulla
Veins
Capillaries
GI muscles
Arteries
Heart

ORGAN

H2 RECEPTOR
SECRETION OF ACID AND PEPSIN

ACTION
INCREASE rate and
contraction

Heart

Stomach

INCREASE HCl
Secretion of pepsin
Increase permeability
Dilation

Capillaries
Arteries

Antihistamines
PHYSIOLOGIC ANTAGONIST

B2-ADRENERGIC RECEPTOR
AGONISTS

MAST CELL STABILIZERS

H1 receptor blockers
2nd generation

1st generation
Dimenhydrinate*
Diphenhydramine*
Doxylamine
Pyrilamine
Tripelennamine

Cyproheptadine
Nausea and vomiting associated
with motion sickness and vertigo*

Hydroxyzine mild anxiolytic

Cyclizine
Meclizine* (Dizitab)
Brompheniramine
Chlorpheniramine (Neozep,
Bioflu)

Promethazine - antiemetic

ADVERSE EFFECTS

Fexofenadine
(Telfast)
Loratadine (Allerta)
Astemizole
Terfenadine

Acrivastine
Cetirizine

H2 receptor blockers
-

Peptic ulcer, GERD, erosive esophagitis,

Zollinger-Ellison syndrome
OD hs up to 8 weeks

ADVERSE EFFECTS

SEROTONIN RECEPTORS
RECEPTOR SUBTYPE
5Ht1

5HT1D
5HT2

5HT3

5HT4

Serotonin agonists
Buspirone anxiolytic
Dexfenfluramine
- appetite suppressant
Cisapride increase gastric motility, GERD
Tegaserod IBS (short-term treatment)
(-TRIPTAN)
Migraine
CI: HTN
Sumatriptan
Rizatriptan
Naratriptan
Zolmetriptan

Ergot alkaloids
migraine
Ergotamine Postpartum hemorrhage,
migraine

ACTION
Vasoconstriction
Behavioral actions (anxiety, appetite, depression,
aggression, impulsivity)
DECREASE presynaptic NT release
Platelet aggregation
Vasoconstriction
Behavioral actions (anxiety, appetite, depression,
aggression, impulsivity)
Nausea/emesis
Behavioral actions (anxiety, appetite, depression,
aggression, impulsivity)
INCREASED Ach release in the enteric region
INCREASED GI motility

Serotonin antagonists
(-SERIN) inhibits platelet aggregation
Ketanserin
Ritanserin
(-SETRON) nausea and vomiting secondary
to antineoplastic therapy
Ondansetron
Granisetron
Dolasetron
Alosetron diarrhea-predominant IBS

Ergonovine Postpartum hemorrhage,

migraine
Methysergide migraine PROPHYLAXIS
Bromocriptine hyperprolactinemia,
Parkinsons
Cyproheptadine (H1 antagonist)

prostaglandins
PGE

INHIBIT platelet
aggregation
RELAX bronchial and GI
smooth muscle
CONTRACT uterine
smooth muscle
INHIBIT gastric acid
secretion
VasoDILATION

PGF
Smooth muscle
CONTRACTION
VasoDILATION
Luteolytic

PGi ANALOGUeS

PGF ANALOGUeS

PGE ANALOGUeS

PGI
INHIBITS platelet aggregation
Stimulates gastric release of bicarbonate and
mucus
INHIBITS gastric and intestinal secretions
BronchoDILATION
VasoDILATION

Carboprost induce 2nd

trimester abortion
Dinoprost tromethamine
induce abortion in
pregnancy longer
than 15 weeks
Latanoprost intraocular
pressure in glaucoma
Travoprost
Bimatoprost
Unoprostone

Alprostadil
maintenance of PDA,
impotence due to
erectile dysfunction
Misoprostol (Cytotec)
NSAID-induced
ulcer
Dinoprostone

Epoprostenol
Platelet aggregation
Emergent pulmonary
HTN
Prostacyclin

PROSTAGLANDIN INHIBITORS

Inhibit phospholipase

Inhibit COX

THROMBOXANES

VasoCONSTRICTION
Platelet aggregation
Hypertension

LEUKOTRIENES

LEUKOTRIENE ANTAGONISTS

LIPOOXYGENASE (lox) INHIBITOR

BronchoCONSTRICTION
Smooth muscle chemotaxis
INCREASE vascular permeability
INCREASED mucus production
NEGATIVE inotropic