Histamine and Serotonin Drugs Class/Mechanism Flashcards Preview

Pharm Unit 2 MJC > Histamine and Serotonin Drugs Class/Mechanism > Flashcards

Flashcards in Histamine and Serotonin Drugs Class/Mechanism Deck (26)
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1
Q

How are H1 receptor antagonists metabolized and how fast?

A

rapidly metabolized via liver microsomes

2
Q

What are H1 receptor antagonists used for and what are their general side effects?

A

Use: allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids.

SE: sedation; anti-muscarinic action, poisoning (especially children) with convulsions, allergy, local anesthesia

3
Q

Diphenhydramine (Benadryl)
class
mech
SE

A

Ether/ethanolamine derivative
H1 receptor antagonist
SE: anti-muscarinic, sedation

4
Q

Tripelennamine
Class
Mech
Use

A

ethylenediamine derivative
H1 receptor antagonist
Use: OTC sleep aid

5
Q

Cyclizine
Class
Mech
Use

A

Piperazine derivative
H1 receptor antagonist
Use: Motion sickness

6
Q
Promethazine
class
mech
use
SE
A

phenothiazine derivative
H1 receptor antagonist
Use: Antiemetic
SE: Anti-muscarinic, sedation

7
Q
Chlorpheniramine
Class
mech
use
SE
A

Alkylamine
H1 receptor antagonist
Use: Component of cold meds
SE: less sedation

8
Q
Laratadine (claritin)
class
mech
use
SE
A

Piperidine derivative
2nd gen H1 receptor antagonist
Use: Allergic rhinitis
SE: no sedation, rare CV effects

9
Q
Fexofenadine (allegra)
Class
mech
use
SE
A

Piperidine derivative
2nd gen H1 receptor antagonist
Use: Allergic rhinitis
SE: no sedation, rare CV effects

10
Q

Azelastine
mech
use
SE

A

2nd gen H1 receptor antagonist
Use: allergic rhinitis (internasal spray), allergic conjunctivitis (opthalmic solution)
SE: No sedation

11
Q

Cetirizine
mech
use
SE

A

2nd gen H1 receptor antagonist
Use: allergic rhinitis
SE: No sedation

12
Q

Cimetidine
Mech
use
SE

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Use: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
SE: Antiandrogen (causing impotence and gynecomastia), inhibition of P450 enzymes

13
Q

Ranitidine (Zantac)
Mech
Use
SE

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Use: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
SE: Liver toxicity

14
Q

Famotidine
Mech
Use

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Use: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

15
Q

Nizatidine
Mech
Use

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Use: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

16
Q

Why do second gen H1 antagonists cause less sedation?

A

poorly cross BBB

17
Q

What is a possible SE of all H2 antagonists?

A

CNS dysfunction possible

18
Q

Cyproheptadine
mech
Use
SE

A

Antihistaminic and antiserotinergic
Use: Skin allergies (urticaria, anti-5HT1)
Diarrhea of carcinoid syndrome (anti 5HT2)

SE: Sedation, antimuscarinic

19
Q

Ketanserin
Mech
Use

A

Selective 5HT2A, 2C receptor antagonist as well as alpha 1 and H1 receptor antagonist

Use: Antihypertensive (Relaxes vascular and tracheal smooth muscle), antiplatelet aggregation

20
Q

Odansetron
Mech
Use

A

5HT3 receptor antagonist

Use: Nausea and vomiting in chemotherapy

21
Q

Ergot Alkaloids
Mech
SE

A

Agonist and antagonist actions at 5HT and alpha adrenergic receptors (also some dopamine)

SE: powerful hallucinations, smooth muscle contraction (vascular and uterine)

22
Q
Ergotamine
Class
Mech
Use
SE
A

Ergot alkaloid
nonspecific partial agonist at all 5HT1,2 receptors; partial agonist at alpha adrenergic receptors
Use: Prodrome of migraines
SE: N/V, cumulative and prolonged vasoconstriction

23
Q
Methysergide
Class
Mech
use
SE
A

Ergot alkaloid
partial agonist at all 5HT1 receptors, antagonist at 5HT2
Use: Prophylaxis of migraines
SE: GI disturbances, inflammatory fibrosis (chronic use), hallucinations

24
Q

Ergonovine
Class
Mech
Use

A

ergot alkaloid
alpha agonists
pospartum hemorrhage (Oxytocic)

25
Q

Bromocriptine
Class
Mech
Use

A

Ergot alkaloid
Dopamine agonist
Use: parkinsonism, hyperprolactinemia

26
Q

Triptans
Class
Mech
Use

A

Non-ergot serotonin analog
5HT1,b,D receptor agonist
Use: Effective (70%) migraine treatment.