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ms 2 - unit 2 > Histamine & Serotonin > Flashcards

Histamine & Serotonin Flashcards

1
Q

What is an H1 antagonist used for?

A

Allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids

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2
Q

What are common side effects of H1 antagonists?

A

Sedation, anti-muscarinic action, poisoning (especially children) with convulsions, allergy, local anesthesia

Older agents cross CNS to cause central effects

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3
Q

Where are H1 antagonists metabolized? What are the oral absorption and distribution properties?

A

rapid metabolism by liver microsomes

Rapidly absorbed orally and widely distributed

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4
Q

What is the mechanism of action of these drugs?

Tripelennamine (Pyribenzamine)

Meclizine (Dramamine II, Antivert)

Hydroxyzine (Atarax)

Promethazine (Phenergan)

Chlorpheniramine (Chlor-Trimeton)

Diphenhydramine (Benadryl)

A

H1 receptor antagonists

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5
Q

what is a common OTC sleep aid?

A

Tripelennamine (Pyribenzamine)

Ethylenediamine derivitive

H1 receptor antagonist

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6
Q

What histamine blockers are used for motion sickness?

A

Meclizine (Dramamine II, Antivert)

Hydroxyzine (Atarax)

Piperazine derivative

H1 receptor antagonist

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7
Q

What is a major side effect of diphenhydramine?

A

Anti-muscarinic, sedating

Ether/ethanolamine derivitive

H1 receptor antagonist

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8
Q

What is promethazine used for?

A

Antiemetic

Phenothiazine derivative

H1 receptor antagonist

Anti-muscarinic, sedating

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9
Q

what is chlorpheniramine?

A

Alkylamine derivitive

H1 receptor antagonist

Component of “cold” medications

Less sedating

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10
Q

What is the mechanism of action? What are they used to treat?

Loratadine
Fexofenadine
Azelastine
Cetirizine

A

2nd generation H1 receptor antagonists

2nd gen H1 blockers treat allergic rhinitis

Loratadine (Claritin)
Fexofenadine (Allegra)
Azelastine (Astelin)
Cetirizine (Zyrtec)

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11
Q

What is major difference between 1st and second gen H1 blockers?

A

second gen blockers poorly cross BBB, so fewer central and side effects - e.g. no sedation, although rare cadiovascular effects at high doses in loratadine (claratin) and fexofenadine (allegra)

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12
Q

What is azelastine?

A

2nd generation H1 receptor antagonist

Treats allergic rhinitis (intranasal spray), allergic conjunctivitis (ophthalmic solution)

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13
Q

What antihistamines can cause cardiovascular effects at high doses?

A

Loratadine (Claritin)
Fexofenadine (Allegra)

2nd generation H1 receptor antagonist

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14
Q

What is the mechanism of action? What are the “…tidine” drugs used for?

Cimetidine
Ranitidine
Famotidine
Nizatidine

A

H2 receptor antagonists; block gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

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15
Q

What class of drugs are used to treat dyspepsia, duodenal and gastric ulcers, hypersecretory conditions? What is a common possible side effect?

A

H2 receptor antagonists; block gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

CNS dysfunction

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16
Q

Of the H2 receptor antagonists, which has the most side effects? What are they?

A

Cimetidine (Tagamet)

Antiandrogen effects (causing impotence and gynecomastia), inhibition of P450 enzymes

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17
Q

What is Rantidine? What is the most concerning side effect?

A

Zantac - H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

liver toxicity

CNS dysfunction possible

18
Q

Of the H2 antagonists, which has the least side effects?

A

Nizatidine (Axid)

19
Q

What is ketanserin? what is it used for?

A

Selective 5HT2A,2C receptor antagonist, as well as α1 and H1 receptor antagonist

Antihypertensive (relaxes vascular and tracheal smooth muscle), antiplatelet aggregation

20
Q

Mechanism of action for the “…setron” drugs? Used for?

Odansetron
Granisetron

A

5HT3 receptor antagonists

Nausea and vomiting in chemotherapy

“…SErotoninThreeReceptor antagonist used by ONcologists”

5-HT = serotonin

21
Q

What is Cyproheptadine?

A

Dual action antihistaminic and antiserotinergic

used for skin allergies (urticaria, anti-5HT1), diarrhea of carcinoid syndrome (anti-5HT2)

Side effects: Sedation, antimuscarinic

22
Q

What class of drugs? What is a common side effect?

Methysergide
Ergonovine
Bromocriptine
Ergotamine

A

Ergot alkaloid

Powerful hallucinations, smooth muscle contraction (vascular and uterine)

23
Q

Which ergot alkaloid is used to treat hyperprolactinemia? Why?

A

Bromocriptine (Sansert)

because it’s a dopamine agonist - DA inhibits prolactin release from anterior pituitary

24
Q

What does ergonovine treat?

A

Postpartum hemorrhage (Oxytocic)

25
Q

What is methysergide? What is it used for?

A

ergot alkaloid

Partial agonist at all 5HT1 receptors, antagonist at 5HT2

Prophylaxis of migraines

26
Q

What is ergotomine? What is it used for?

A

Ergot alkaloid

Nonspecific partial agonist at all 5HT1,2 receptors; partial agonist at α-adrenergic receptors

Prodrome of migraines

27
Q

What are triptans? Mechanism? Used for?

Sumatriptan
Naratriptan
Rizatriptan
Zolmitriptan

A

Non-ergot serotonin analogs

5HT1B,D receptor agonist

Effective (70%) migraine treatment

28
Q

Why should you analyze doses of other drugs and consider lowering them in a patient who is taking cimetidine?

A

Cimetidine has an effect on the cytochrome P450 system.

29
Q

H1 receptors are found mainly:

A

skin, lungs, GI, nasal mucosa and blood

30
Q

What drugs induce histamine release?

A

Morphine
Codeine
ACh
tubocurarine

31
Q

H1 receptors are found:

A

smooth muscle, endothelium brain (hence drowsiness - CNS effect of H1 antagonism)

32
Q

H2 receptors are found:

A

gastric mucosa (think H-blockers for acid reflux), cardiac muscle, mast cells, brain

33
Q

H3 receptors are found:

A

CNS

34
Q

H4 receptors are found:

A

eosinophils
neutrophils
CD4+ T cells

35
Q 
These classes of drugs are all what kind of drug?
Ethers or ethanolamine derivatives
Ethylenediamine derivative
Piperazine derivative
Phenothiazine derivative
Alkylamine derivative
Piperidine derivative
Azelastine
A

H1 receptor antagonists

Antihistamines

36
Q

H1 receptor antagonists are largely ineffective for what conditions?

A

Bronchial asthma

colds

37
Q

How is Nizatidine different from other H2 receptor antagonists?

A

It does not affect the cytochrome P450 system

38
Q

Liver toxicity is a side effect of what H2 receptor blocker?

A

Ranitidine

39
Q

Gynecomastia and impotence are side effects of what H2 receptor blocker?

A

Cimetidine

40
Q

How are loradidine and fexofenadine different from other H1 receptor blockers?

A

They cross the BBB poorly, so less sedating;

fewer side effects in general

41
Q

What is 5-hydroxytryptamine?

A

Serotonin

42
Q

Release of 5-HT can be induced by what drug?

A

Reserpine

ms 2 - unit 2 (26 decks)

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